dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-111c3c38c2084791aebe57e394f1900a
CN(C)CCNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.NCC(N)=O>>NC(=O)CNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC1=CC=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C(NCCN(C)C)=O)C=C1.NCC(=O)N>>C(N)(=O)CNC(=O)C=1C=C(C(=CC1)C1=CC=C(C=C1)Cl)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CN(C)CCN[C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11](-[c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]2)[c:19](-[c:20]2[cH:21][cH:22][c:23]3[cH:24][c:25](-[c:26]4[n:27][c:28]5[cH:29][c:30]([C:31](=[O:32])[OH:33])[cH:34][cH:35][c:36]5[n:37]4[CH:38]4[CH2:39][CH2:40][CH2:41][CH2:42][CH2:43]4)[cH:44][cH:45][c:46]3[n:47]2)[cH:4...
CN(C)CCNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.NCC(N)=O
NC(=O)CNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
Acylation
OtherReaction
1f65584d811005ce14184af76efdc3ec878b3e465d13ed08b308dc607a0589b2
03a81fa1546c38bfa4e40f8ce9e6dc6167e96678946fcdc6826a1cac3ec22183
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
C-N(-C)-C-C-N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[N;D1;H2:6]-[C:7](=[O;D1;H0:8])-[C:9]-[NH2;D1;+0:10]>>[N;D1;H2:6]-[C:7](=[O;D1;H0:8])-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
The title compound was synthesized as described for Compound 491, except glycine-amide was used instead of N1,N1-dimethyl-ethane-1,2-diamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine.Tertiary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
Other
null
null
null
CN(C)CCNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.NCC(N)=O>>NC(=O)CNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-99c6a1e8c6c7464bab7e2cd7672dc794
CN.CN(C)CCNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1>>CNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC1=CC=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C(NCCN(C)C)=O)C=C1.CN>>ClC1=CC=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C(NC)=O)C=C1
[CH3:1][NH2:2].CN(C)CCN[C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[c:16](-[c:17]2[cH:18][cH:19][c:20]3[cH:21][c:22](-[c:23]4[n:24][c:25]5[cH:26][c:27]([C:28](=[O:29])[OH:30])[cH:31][cH:32][c:33]5[n:34]4[CH:35]4[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]4)[cH:41][cH:42][c:43]3[...
CN.CN(C)CCNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
CNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
Acylation
OtherReaction
1f65584d811005ce14184af76efdc3ec878b3e465d13ed08b308dc607a0589b2
03a81fa1546c38bfa4e40f8ce9e6dc6167e96678946fcdc6826a1cac3ec22183
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
C-N(-C)-C-C-N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[NH2;D1;+0:7]>>[C;D1;H3:6]-[NH;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
The title compound was synthesized as described for Compound 491, except methyl amine was used instead of N1,N1-dimethyl-ethane-1,2-diamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine.Tertiary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
Other
null
null
null
CN.CN(C)CCNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1>>CNC(=O)c1ccc(-c2ccc(Cl)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-3bc369d38810466ab18eca61c30d4b9c
CCOC(=O)c1ccc(NC2CCCCC2)c(N)c1.CN(C)C(On1nnc2ccccc21)=[N+](C)C>>Nc1ccc(-c2nc3cc(C(=O)O)ccc3n2C2CCCCC2)cc1N
O.CCN(C(C)C)C(C)C.C(C)OC(C1=CC(=C(C=C1)NC1CCCCC1)N)=O.CN(C)C(=[N+](C)C)ON1C2=C(C=CC=C2)N=N1.[B-](F)(F)(F)F>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C2=CC(=C(C=C2)N)N
CC[O:13][C:11]([c:10]1[cH:9][c:8]([NH2:7])[c:16]([NH:17][CH:18]2[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]2)[cH:15][cH:14]1)=[O:12].CN(C)[C:6](O[n:1]1n[n:26][c:25]2[c:2]1[cH:3][cH:4][cH:5][cH:24]2)=[N+](C)C>>[NH2:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][c:8]3[cH:9][c:10]([C:11](=[O:12])[OH:13])[cH:14][cH:15][c:16]3[n:17]2[...
CCOC(=O)c1ccc(NC2CCCCC2)c(N)c1.CN(C)C(On1nnc2ccccc21)=[N+](C)C
Nc1ccc(-c2nc3cc(C(=O)O)ccc3n2C2CCCCC2)cc1N
null
null
CCO.CN(C)C=O
C-C Coupling
OtherReaction
d39ae955bfa4ef5891d52b381ea2e0e1ca27cefff268c209f2c6b3d4e1830bd5
9c4acf9207ee3ded4a6acb3ac7c7bac8cb4fb0acc2fea04aa290e99ed7cf07f9
c1ccc(-c2nc3ccccc3n2C2CCCCC2)cc1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[c:6](-[NH2;D1;+0:7]):[c:8](-[NH;D2;+0:9]-[C:10](-[C:11])-[C:12]):[c:13].C-N(-C)-[C;H0;D3;+0:14](-O-[n;H0;D3;+0:15]1:n:[n;H0;D2;+0:16]:[c:17]2:[c:18]:[cH;D2;+0:19]:[c:20]:[c:21]:[c:22]:2:1)=[N+](-C)-C>>[C:11]-[C:10](-[n;H0;D3;+0:9]1:[c:8](:[c:13]):[c:6](:[c:5]:[c:4]-[C...
95.5
[{"value": 95.5, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C2=CC(=C(C=C2)N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of 1 g (2.84 mmol) of the product of the previous step, 0.91 g (2.84 mmol) of TBTU and 0.73 g (5.68 mmol) of DIEA in 10 mL anhydrous DMF was allowed to stand at room temperature for 15 min. To this solution was added 0.90 g (3.41 mmol) of Compound 11, and the solution was allowed to stand at room temperature...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Ester.Primary amine.Secondary amine
Carboxylic acid.Primary amine.Primary amine
c1ccccc1.c1ccc2[nH]nnc2c1
c1ccccc1.c1ccc2nc[nH]c2c1
c1ccccc1.c1ccc2nc[nH]c2c1.C1CCCCC1
HO-
CCO.CN(C)C=O
null
0.25
CCOC(=O)c1ccc(NC2CCCCC2)c(N)c1.CN(C)C(On1nnc2ccccc21)=[N+](C)C>CCO.CN(C)C=O>Nc1ccc(-c2nc3cc(C(=O)O)ccc3n2C2CCCCC2)cc1N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-afe93530b68c4c44afbddeeb0e91daec
Nc1ccc(-c2nc3cc(C(=O)O)ccc3n2C2CCCCC2)cc1N.O=C(C(=O)c1ccccc1)c1ccccc1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C2=CC(=C(C=C2)N)N.C1(=CC=CC=C1)C(=O)C(=O)C1=CC=CC=C1>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=C(C(=NC1=CC2)C2=CC=CC=C2)C2=CC=CC=C2
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10][c:11](-[c:12]1[cH:13][cH:14][c:15]([NH2:16])[c:32]([NH2:31])[cH:33]1)[n:34]2[CH:35]1[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]1.O=[C:17]([c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)[C:24](=O)[c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1>>[O:1]=[C:2]([OH:3])[c:...
Nc1ccc(-c2nc3cc(C(=O)O)ccc3n2C2CCCCC2)cc1N.O=C(C(=O)c1ccccc1)c1ccccc1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
80ad7d4b359f2683f57c053570cf5c6857c4f32e8ec9869e4f38f79c70cafc8c
d53d864708a4cd37c2fe33ca368498c017ca81ee7d694ff92f9c935efef6bc9e
c1ccc(-c2nc3ccc(-c4nc5ccccc5n4C4CCCCC4)cc3nc2-c2ccccc2)cc1
O=[C;H0;D3;+0:1](-[C;H0;D3;+0:2](=O)-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7])-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12].[NH2;D1;+0:13]-[c:14](:[c:15]):[c:16](-[NH2;D1;+0:17]):[c:18]>>[c:15]:[c:14]1:[n;H0;D2;+0:13]:[c;H0;D3;+0:1](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]):[c;H0;D3;+0:2](-[c;H0;D3;+0:3](:[c:4]:[c:5...
null
[]
null
null
null
null
A solution of 100 mg (0.29 mmol) of Compound 406b and 74 mg (0.35 mmol) of benzil was stirred at room temperature overnight. The solvent was evaporated and the residue was purified on preparative HPLC yielding 10 mg. Conditions: See reaction.notes.procedure_details. Workup: The solvent was evaporated; the residue was p...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Primary amine.Primary amine
null
c1ccccc1
c1ccc2nccnc2c1
c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.c1ccccc1.C1CCCCC1
HO-
null
null
null
Nc1ccc(-c2nc3cc(C(=O)O)ccc3n2C2CCCCC2)cc1N.O=C(C(=O)c1ccccc1)c1ccccc1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8ebb6a21559541998650aed95637c609
O=C(C(=O)c1ccc(Br)cc1)c1ccc(Br)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Br)cc4)c(-c4ccc(Br)cc4)nc3c1)n2C1CCCCC1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=C(C(=NC1=CC2)C2=CC=CC=C2)C2=CC=CC=C2.BrC1=CC=C(C=C1)C(=O)C(=O)C1=CC=C(C=C1)Br>>BrC1=CC=C(C=C1)C1=NC2=CC=C(C=C2N=C1C1=CC=C(C=C1)Br)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
O=C(C(=O)c1cc[c:21]([Br:22])[cH:20][cH:19]1)c1ccc([Br:30])cc1.c1c[c:18](-[c:17]2[n:16][c:15]3[cH:14][cH:13][c:12](-[c:11]4[n:10][c:8]5[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]5)[n:36]4[CH:37]4[CH2:38][CH2:39][CH2:40][CH2:41][CH2:42]4)[cH:35][c:34]3[n:33][c:25]2-[c:26]2[cH:27][cH:28][cH:29][cH:31][cH:32]2)[cH:2...
O=C(C(=O)c1ccc(Br)cc1)c1ccc(Br)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Br)cc4)c(-c4ccc(Br)cc4)nc3c1)n2C1CCCCC1
null
null
null
Functional Group Interconversion
OtherReaction
98c5779329f45f09a0843f1bf721d339deed59a6f832812172b8f93f23ccaf08
59f867651ee848cc4c1fb1fe036b1f8eb00c88c7ac0bcbe7091b43bab11dfa25
c1ccc(-c2nc3ccc(-c4nc5ccccc5n4C4CCCCC4)cc3nc2-c2ccccc2)cc1
O=C(-C(=O)-c1:c:c:c(-[Br;H0;D1;+0:1]):c:c:1)-c1:[cH;D2;+0:2]:[c:3]:[c;H0;D3;+0:4](-[Br;D1;H0:5]):c:c:1.[#7;a:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10](-[c:11]2:[c:12]:[c:13]:[cH;D2;+0:14]:[c:15]:[c:16]:2):[c:17]:1-[c;H0;D3;+0:18]1:[c:19]:[cH;D2;+0:20]:c:c:c:1>>[Br;D1;H0:5]-[c;H0;D3;+0:4]1:[c:3]:[cH;D2;+0:2]:[c;H0;D3;+0:18](-[c:1...
null
[]
null
null
null
null
Prepared as described for Compound 406 using 4,4′-dibromobenzil in place of benzil. Conditions: See reaction.notes.procedure_details. Workup: Prepared
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Ketone.Ketone
Aromatic halide.Aromatic halide
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.c1ccccc1.C1CCCCC1
HO-
null
null
null
O=C(C(=O)c1ccc(Br)cc1)c1ccc(Br)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Br)cc4)c(-c4ccc(Br)cc4)nc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-c5ab237a4e2847d4b2dfa35bd3ca34f0
Cc1ccc(C(=O)C(=O)c2ccc(C)cc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>Cc1ccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2ccc(C)cc2)cc1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=C(C(=NC1=CC2)C2=CC=CC=C2)C2=CC=CC=C2.CC1=CC=C(C=C1)C(=O)C(=O)C1=CC=C(C=C1)C>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=C(C(=NC1=CC2)C2=CC=C(C=C2)C)C2=CC=C(C=C2)C
O=C(C(=O)c1[cH:4][cH:3][c:2]([CH3:1])[cH:42][cH:41]1)c1[cH:35][cH:36][c:37]([CH3:38])[cH:39][cH:40]1.c1cc[c:5](-[c:6]2[n:7][c:8]3[cH:9][cH:10][c:11](-[c:12]4[n:13][c:14]5[cH:15][c:16]([C:17](=[O:18])[OH:19])[cH:20][cH:21][c:22]5[n:23]4[CH:24]4[CH2:25][CH2:26][CH2:27][CH2:28][CH2:29]4)[cH:30][c:31]3[n:32][c:33]2-[c:34]2...
Cc1ccc(C(=O)C(=O)c2ccc(C)cc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
Cc1ccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2ccc(C)cc2)cc1
null
null
null
Miscellaneous
OtherReaction
1080d35fbc20debb247878370c355dffb0943784f68c8ccbb2f515015cf67436
04b105348625c11d88400601d6084fcf4ec5b44daa0c1f8954a37a3ab783d9c2
c1ccc(-c2nc3ccc(-c4nc5ccccc5n4C4CCCCC4)cc3nc2-c2ccccc2)cc1
O=C(-C(=O)-c1:[cH;D2;+0:1]:[c:2]:[c:3]:[c:4]:[cH;D2;+0:5]:1)-c1:[cH;D2;+0:6]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1.[#7;a:11]1:[c:12]:[c:13]:[#7;a:14]:[c:15](-[c;H0;D3;+0:16]2:c:c:c:c:c:2):[c:17]:1-[c;H0;D3;+0:18]1:c:c:c:c:c:1>>[#7;a:11]1:[c:12]:[c:13]:[#7;a:14]:[c:15](-[c;H0;D3;+0:16]2:[cH;D2;+0:1]:[c:2]:[c:3]:[c:4]:[cH;D2...
null
[]
null
null
null
null
Prepared as described for Compound 406 using 4,4′-dimethylbenzil in place of benzil. Conditions: See reaction.notes.procedure_details. Workup: Prepared
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccc2nccnc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1.c1ccccc1
HO-
null
null
null
Cc1ccc(C(=O)C(=O)c2ccc(C)cc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>Cc1ccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2ccc(C)cc2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-62f9c186bdfe4c8fa50217e496f9f459
O=C(C(=O)c1ccc(F)cc1)c1ccc(F)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(F)cc4)c(-c4ccc(F)cc4)nc3c1)n2C1CCCCC1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=C(C(=NC1=CC2)C2=CC=CC=C2)C2=CC=CC=C2.FC1=CC=C(C=C1)C(=O)C(=O)C1=CC=C(C=C1)F>>FC1=CC=C(C=C1)C1=NC2=CC=C(C=C2N=C1C1=CC=C(C=C1)F)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
O=C(C(=O)c1cc[c:21]([F:22])[cH:20][cH:19]1)c1cc[c:29]([F:30])[cH:28]c1.c1c[c:18](-[c:17]2[n:16][c:15]3[cH:14][cH:13][c:12](-[c:11]4[n:10][c:8]5[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]5)[n:36]4[CH:37]4[CH2:38][CH2:39][CH2:40][CH2:41][CH2:42]4)[cH:35][c:34]3[n:33][c:25]2-[c:26]2[cH:27]cc[cH:31][cH:32]2)[cH:24][...
O=C(C(=O)c1ccc(F)cc1)c1ccc(F)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(F)cc4)c(-c4ccc(F)cc4)nc3c1)n2C1CCCCC1
null
null
null
Miscellaneous
OtherReaction
b5ff1b757421adc68e8cc3a1c1e937d4ca45b2b3b7a71e8daf44d408f820e81f
b09cc8aea5fe7202f020f87a8357f25a62cf266759134ef33fd12748362eb2c8
c1ccc(-c2nc3ccc(-c4nc5ccccc5n4C4CCCCC4)cc3nc2-c2ccccc2)cc1
O=C(-C(=O)-c1:c:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[F;D1;H0:3]):c:c:1)-c1:[cH;D2;+0:4]:[c:5]:[c;H0;D3;+0:6](-[F;D1;H0:7]):c:c:1.[#7;a:8]1:[c:9]:[c:10]:[#7;a:11]:[c:12](-[c:13]2:[c:14]:[cH;D2;+0:15]:c:c:[cH;D2;+0:16]:2):[c:17]:1-[c;H0;D3;+0:18]1:[c:19]:[cH;D2;+0:20]:c:c:c:1>>[F;D1;H0:7]-[c;H0;D3;+0:6]1:[c:5]:[cH;D2;+0:4]:[c;H...
null
[]
null
null
null
null
Prepared as described for Compound 406 using 4,4′-difluorobenzil in place of benzil. Conditions: See reaction.notes.procedure_details. Workup: Prepared
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Ketone.Ketone
Aromatic halide.Aromatic halide
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.c1ccccc1.C1CCCCC1
HO-
null
null
null
O=C(C(=O)c1ccc(F)cc1)c1ccc(F)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(F)cc4)c(-c4ccc(F)cc4)nc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d1fc82499d874ad5a57215b2516ffb39
COc1cccc(C(=O)C(=O)c2cccc(OC)c2)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>COc1cccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2cccc(OC)c2)c1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=C(C(=NC1=CC2)C2=CC=CC=C2)C2=CC=CC=C2.COC=1C=C(C=CC1)C(=O)C(=O)C1=CC(=CC=C1)OC>>COC=1C=C(C=CC1)C1=NC2=CC=C(C=C2N=C1C1=CC(=CC=C1)OC)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
O=C(C(=O)[c:36]1[cH:37][cH:38][cH:39][c:40]([O:41][CH3:42])[cH:43]1)[c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[cH:44]1.c1ccc(-[c:8]2[n:9][c:10]3[cH:11][cH:12][c:13](-[c:14]4[n:15][c:16]5[cH:17][c:18]([C:19](=[O:20])[OH:21])[cH:22][cH:23][c:24]5[n:25]4[CH:26]4[CH2:27][CH2:28][CH2:29][CH2:30][CH2:31]4)[cH:32][c:33]3[n:3...
COc1cccc(C(=O)C(=O)c2cccc(OC)c2)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
COc1cccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2cccc(OC)c2)c1
null
null
null
C-C Coupling
OtherReaction
2585b5e7fc7fd47b3598fef6a2f3603251109daf26aba6843a50175402531759
99def8b73cb571e88df07b5a7104de2d97f258f18cfc88f7c0d26bf53483ceb8
c1ccc(-c2nc3ccc(-c4nc5ccccc5n4C4CCCCC4)cc3nc2-c2ccccc2)cc1
O=C(-C(=O)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5])-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10].[#7;a:11]1:[c:12]:[c:13]:[#7;a:14]:[c;H0;D3;+0:15](-c2:c:c:c:c:c:2):[c;H0;D3;+0:16]:1-c1:c:c:c:c:c:1>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:16]1:[#7;a:11]:[c:12]:[c:13]:[#7;a:14]:[c;H0;D3;+0:15]:1-[c;H0;D3;+0:1](:[c:2]:[c:3...
null
[]
null
null
null
null
Prepared as described for Compound 406 using 3,3′-dimethoxybenzil in place of benzil. Conditions: See reaction.notes.procedure_details. Workup: Prepared
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2nccnc2c1.c1ccccc1
c1ccccc1.c1ccc2nccnc2c1.c1ccccc1
c1ccccc1.c1ccc2nccnc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1.c1ccccc1
HO-
null
null
null
COc1cccc(C(=O)C(=O)c2cccc(OC)c2)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>COc1cccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2cccc(OC)c2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-83f7de4a108e48e1bf8dcf3c67b92b2e
COc1ccc(C(=O)C(=O)c2ccc(OC)cc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>COc1ccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2ccc(OC)cc2)cc1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=C(C(=NC1=CC2)C2=CC=CC=C2)C2=CC=CC=C2.COC1=CC=C(C=C1)C(=O)C(=O)C1=CC=C(C=C1)OC>>COC1=CC=C(C=C1)C1=NC2=CC=C(C=C2N=C1C1=CC=C(C=C1)OC)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
O=C(C(=O)[c:35]1[cH:36][cH:37][c:38]([O:39][CH3:40])[cH:41][cH:42]1)c1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:44][cH:43]1.c1ccc(-[c:34]2[c:7](-[c:6]3ccccc3)[n:8][c:9]3[cH:10][cH:11][c:12](-[c:13]4[n:14][c:15]5[cH:16][c:17]([C:18](=[O:19])[OH:20])[cH:21][cH:22][c:23]5[n:24]4[CH:25]4[CH2:26][CH2:27][CH2:28][CH2:29][CH2:30]4)[...
COc1ccc(C(=O)C(=O)c2ccc(OC)cc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1
COc1ccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2ccc(OC)cc2)cc1
null
null
null
C-C Coupling
OtherReaction
2585b5e7fc7fd47b3598fef6a2f3603251109daf26aba6843a50175402531759
99def8b73cb571e88df07b5a7104de2d97f258f18cfc88f7c0d26bf53483ceb8
c1ccc(-c2nc3ccc(-c4nc5ccccc5n4C4CCCCC4)cc3nc2-c2ccccc2)cc1
O=C(-C(=O)-c1:[cH;D2;+0:1]:[c:2]:[c:3]:[c:4]:[cH;D2;+0:5]:1)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10].[#7;a:11]1:[c:12]:[c:13]:[#7;a:14]:[c:15](-[c;H0;D3;+0:16]2:c:c:c:c:c:2):[c;H0;D3;+0:17]:1-c1:c:c:c:c:c:1>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:17]1:[#7;a:11]:[c:12]:[c:13]:[#7;a:14]:[c:15]:1-[c;H0;D3;+0:16]1:[cH;D...
null
[]
null
null
null
null
Prepared as described for Compound 406 using 4,4′-dimethoxybenzil in place of benzil. Conditions: See reaction.notes.procedure_details. Workup: Prepared
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2nccnc2c1
c1ccccc1.c1ccc2nccnc2c1.c1ccccc1
c1ccccc1.c1ccc2nccnc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1.c1ccccc1
HO-
null
null
null
COc1ccc(C(=O)C(=O)c2ccc(OC)cc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)c(-c4ccccc4)nc3c1)n2C1CCCCC1>>COc1ccc(-c2nc3ccc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)cc3nc2-c2ccc(OC)cc2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a95e450f826d44a79035dcf9ee69447b
COc1ccc(-c2ccc(C(=O)N3CCCC3)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1OC.O=[N+]([O-])c1ccc(B(O)O)cc1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(C(=O)N5CCCC5)ccc4-c4ccc([N+](=O)[O-])cc4)ccc3c1)n2C1CCCCC1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC(=C(C=C2)OC)OC)C(=O)N2CCCC2.[N+](=O)([O-])C1=CC=C(C=C1)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)[N+](=O)[O-])C(=O)N2CCCC2
COc1cc[c:31](-[c:30]2[c:18](-[c:17]3[n:16][c:15]4[cH:14][cH:13][c:12](-[c:11]5[n:10][c:8]6[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]6)[n:44]5[CH:45]5[CH2:46][CH2:47][CH2:48][CH2:49][CH2:50]5)[cH:43][c:42]4[cH:41][cH:40]3)[cH:19][c:20]([C:21](=[O:22])[N:23]3[CH2:24][CH2:25][CH2:26][CH2:27]3)[cH:28][cH:29]2)cc1OC...
COc1ccc(-c2ccc(C(=O)N3CCCC3)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1OC.O=[N+]([O-])c1ccc(B(O)O)cc1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(C(=O)N5CCCC5)ccc4-c4ccc([N+](=O)[O-])cc4)ccc3c1)n2C1CCCCC1
null
null
null
Miscellaneous
OtherReaction
e7016461b6a49ddcd965abff2980136a10dc812f0b18d6cf61eecb08e136094b
87db1303acea5973f03a377de30076eddd78bf401fd841439ee11d6ebfb23f8b
O=C(c1ccc(-c2ccccc2)c(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)c1)N1CCCC1
C-O-c1:c:c:[c;H0;D3;+0:1](-[c:2](:[c:3]):[c:4]):c:c:1-O-C.O-B(-O)-c1:[cH;D2;+0:5]:[c:6]:[c:7]:[c:8]:[cH;D2;+0:9]:1>>[c:3]:[c:2](-[c;H0;D3;+0:1]1:[cH;D2;+0:5]:[c:6]:[c:7]:[c:8]:[cH;D2;+0:9]:1):[c:4]
null
[]
null
null
null
null
The title compound (5.2 mg yield) was prepared as described for Compound 419 using 4-nitrophenylboronic acid in place of 3,4-dimethoxyphenylboronic acid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Boronic acid
null
c1ccccc1.c1ccccc1
c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1CC[NH]C1.c1ccccc1.C1CCCCC1
HO-.B
null
null
null
COc1ccc(-c2ccc(C(=O)N3CCCC3)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1OC.O=[N+]([O-])c1ccc(B(O)O)cc1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(C(=O)N5CCCC5)ccc4-c4ccc([N+](=O)[O-])cc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8a2b9777bb2f40ab8aa7be56f19d678a
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)OCC)C=2C=C1C=CC(=NC1=CC2)C(=O)O.[OH-].[Na+]>>C(=O)(O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(=O)O)C2CCCCC2)C=C1
CC[O:3][C:2](=[O:1])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10][c:11](-[c:12]1[cH:13][cH:14][c:15]3[n:16][c:17]([C:18](=[O:19])[OH:20])[cH:21][cH:22][c:23]3[cH:24]1)[n:25]2[CH:26]1[CH2:27][CH2:28][CH2:29][CH2:30][CH2:31]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10][c:11](-[c:12]1[cH:13][cH:14][c:1...
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1
null
null
CO
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1cnc2ccc(-c3nc4ccccc4n3C3CCCCC3)cc2c1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
null
null
A solution of 90 mg (0.2 mmol) of Compound 402a and 1 mL 2 N aq. NaOH in 4 mL MeOH was heated overnight at 55° C. The solvent was evaporated, the residue was dissolved in H2O and neutralized. The precipitate was filtered, washed with H2O and dried. The product was purified by HPLC to yield 34 mg. Conditions: See reacti...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.C1CCCCC1
Other
CO
null
null
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1>CO>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ef9a621588f5428ca617a34cf18decac
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1.C[C@H](N)C(N)=O>>CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1
CC1(C2CCC1(C(=O)C2)CS(=O)(=O)O)C.C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)OCC)C=2C=C1C=CC(=NC1=CC2)C(=O)O.N[C@@H](C)C(=O)N.C1CCN(C1)[P+](N2CCCC2)(N3CCCC3)Br.F[P-](F)(F)(F)(F)F.CCN(C(C)C)C(C)C>>C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC(C)C(N)=O)=O)C2CCCCC2)C=C1
O[C:20]([c:19]1[n:18][c:17]2[cH:16][cH:15][c:14](-[c:13]3[n:12][c:10]4[c:9]([cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:11]4)[n:32]3[CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[cH:31][c:30]2[cH:29][cH:28]1)=[O:21].[NH2:22][C@@H:23]([CH3:24])[C:25]([NH2:26])=[O:27]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]...
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1.C[C@H](N)C(N)=O
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1
null
CN(C)C=1C=CN=CC1
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1cnc2ccc(-c3nc4ccccc4n3C3CCCCC3)cc2c1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6].[C;D1;H3:7]-[C@H;D3;+0:8](-[NH2;D1;+0:9])-[C:10](-[N;D1;H2:11])=[O;D1;H0:12]>>[C;D1;H3:7]-[CH;D3;+0:8](-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6])-[C:10](-[N;D1;H2:11])=[O;D1;H0:12]
42.3
[{"value": 42.3, "product": "C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC(C)C(N)=O)=O)C2CCCCC2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
A solution of 100 mg (0.23 mmol) of Compound 402a, 86 mg (0.69 mmol) of L-alaninamide, 322 mg (0.69 mmol) of PyBroP, 84 mg (0.69 mmol) DMAP and 89 mg (0.69 mmol) DIEA in 5 mL anhydrous CH2Cl2 was stirred at room temperature for 24 h. To this solution was added 214 mg (0.92 mmol) of CSA. The solution was stirred for ano...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.C1CCCCC1
HO-
CN(C)C=1C=CN=CC1.C(Cl)Cl
null
24
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)O)ccc3c1)n2C1CCCCC1.C[C@H](N)C(N)=O>CN(C)C=1C=CN=CC1.C(Cl)Cl>CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-325e96fcb26e4bd99c7218c85a49fa0c
CC(C)[C@H](N)C(N)=O.CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1>>CC(C)C(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O
C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC(C)C(N)=O)=O)C2CCCCC2)C=C1.N[C@@H](C(C)C)C(=O)N.C(N)(=O)C(C)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O>>C(N)(=O)C(C(C)C)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
NC(=O)[C@@H](N)[CH:2]([CH3:1])[CH3:3].CC[O:21][C:19]([c:18]1[cH:17][c:16]2[n:15][c:14](-[c:13]3[cH:12][c:11]4[cH:10][cH:9][c:8]([C:6]([NH:5][CH:4](C)[C:36]([NH2:37])=[O:38])=[O:7])[n:35][c:34]4[cH:33][cH:32]3)[n:25]([CH:26]3[CH2:27][CH2:28][CH2:29][CH2:30][CH2:31]3)[c:24]2[cH:23][cH:22]1)=[O:20]>>[CH3:1][CH:2]([CH3:3])...
CC(C)[C@H](N)C(N)=O.CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1
CC(C)C(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O
null
null
null
C-C Coupling
OtherReaction
071c3b4b41af2985190b2d71847b92cd1df6399508b7de3ff4e79668678a14ff
18b0ca9d4623aa7b1f5ac4c47828d437c9d9d5901ab32e97d4b5aa357afc07ba
c1cnc2ccc(-c3nc4ccccc4n3C3CCCCC3)cc2c1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].C-[CH;D3;+0:5](-[#7:6]-[C:7](=[O;D1;H0:8])-[c:9]:[#7;a:10])-[C:11](-[N;D1;H2:12])=[O;D1;H0:13].N-C(=O)-[C@@H](-N)-[CH;D3;+0:14](-[C;D1;H3:15])-[C;D1;H3:16]>>[#7;a:10]:[c:9]-[C:7](=[O;D1;H0:8])-[#7:6]-[CH;D3;+0:5](-[C:11](-[N;D1;H2:12])=[O;D1;H0:13])-[CH;D3;+0:14](-[C;D1;H3:1...
null
[]
null
null
null
null
The title compound (5 mg yield) was prepared as described for Compound 497a using L-valinamide in place of L-alaninamide, and hydrolyzed as described for Compound 497. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amide.Primary amine
Carboxylic acid
null
null
c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HO-
null
null
null
CC(C)[C@H](N)C(N)=O.CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1>>CC(C)C(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5461eb862a184c4eb8708425c0f39fb1
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)Cc1c[nH]cn1>>NC(=O)C(Cc1ncc[nH]1)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC(C)C(N)=O)=O)C2CCCCC2)C=C1.N[C@@H](CC1=CNC=N1)C(=O)N.C(N)(=O)C(C)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O>>C(N)(=O)C(CC=1NC=CN1)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
[NH2:1][C:2](=[O:3])[CH:4]([CH3:5])[NH:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][c:17]2[cH:18][c:19](-[c:20]3[n:21][c:22]4[cH:23][c:24]([C:25](=[O:26])[OH:27])[cH:28][cH:29][c:30]4[n:31]3[CH:32]3[CH2:33][CH2:34][CH2:35][CH2:36][CH2:37]3)[cH:38][cH:39][c:40]2[n:41]1.NC(=O)[C@@H](N)C[c:6]1[n:7][cH:8][nH:10][cH:9]1>>[NH2:1]...
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)Cc1c[nH]cn1
NC(=O)C(Cc1ncc[nH]1)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
null
C-C Coupling
OtherReaction
ed8571bde74ccaf30384e39acb413fdaeeeeafa1a6ef5fae77a2a4b0bdef3321
81758d3c7ce7424f80d9452cdaded113984934370422cdecceaeafd777340c3b
O=C(NCCc1ncc[nH]1)c1ccc2cc(-c3nc4ccccc4n3C3CCCCC3)ccc2n1
N-C(=O)-[C@@H](-N)-C-[c;H0;D3;+0:1]1:[#7;a:2]:[cH;D2;+0:3]:[nH;D2;+0:4]:[cH;D2;+0:5]:1.[CH3;D1;+0:6]-[C:7](-[#7:8]-[C:9]=[O;D1;H0:10])-[C:11](-[N;D1;H2:12])=[O;D1;H0:13]>>[N;D1;H2:12]-[C:11](=[O;D1;H0:13])-[C:7](-[#7:8]-[C:9]=[O;D1;H0:10])-[CH2;D2;+0:6]-[c;H0;D3;+0:1]1:[#7;a:2]:[cH;D2;+0:3]:[cH;D2;+0:5]:[nH;D2;+0:4]:1
null
[]
null
null
null
null
The title compound (8 mg yield) was prepared as described for Compound 497a using L-histidinamide in place of L-alaninamide and hydrolyzed as described for Compound 497. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amide.Primary amine
null
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HO-
null
null
null
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)Cc1c[nH]cn1>>NC(=O)C(Cc1ncc[nH]1)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e94738fce59f4a0a8f2a34c090dfa959
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)CO>>NC(=O)C(CO)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC(C)C(N)=O)=O)C2CCCCC2)C=C1.N[C@@H](CO)C(=O)N.C(N)(=O)C(C)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O>>C(N)(=O)C(CO)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
C[CH:4]([C:2]([NH2:1])=[O:3])[NH:7][C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13]2[cH:14][c:15](-[c:16]3[n:17][c:18]4[cH:19][c:20]([C:21](=[O:22])[OH:23])[cH:24][cH:25][c:26]4[n:27]3[CH:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]3)[cH:34][cH:35][c:36]2[n:37]1.NC(=O)[C@@H](N)[CH2:5][OH:6]>>[NH2:1][C:2](=[O:3])[CH:4]([CH2:5][...
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)CO
NC(=O)C(CO)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
null
C-C Coupling
OtherReaction
16e3eb214afab89471a8ad9638384fe82f9cab3b7c6b51c1bd1dce3fca169e66
6a8e7848616d1b73cc1c93873f769d63755d34e8c82bb0761cae921db7d11456
c1cnc2ccc(-c3nc4ccccc4n3C3CCCCC3)cc2c1
C-[CH;D3;+0:1](-[#7:2]-[C:3](=[O;D1;H0:4])-[c:5]:[#7;a:6])-[C:7](-[N;D1;H2:8])=[O;D1;H0:9].N-C(=O)-[C@@H](-N)-[CH2;D2;+0:10]-[O;D1;H1:11]>>[#7;a:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#7:2]-[CH;D3;+0:1](-[CH2;D2;+0:10]-[O;D1;H1:11])-[C:7](-[N;D1;H2:8])=[O;D1;H0:9]
null
[]
null
null
null
null
The title compound (5 mg yield) was prepared as described for Compound 497a using L-serinamide in place of L-alaninamide and hydrolyzed as described for Compound 497. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amide.Primary alcohol.Primary amine
Primary alcohol
null
null
c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HO-
null
null
null
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)CO>>NC(=O)C(CO)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f65a74023abf49d7bf98eb90d732f5aa
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)Cc1ccccc1>>NC(=O)C(Cc1ccccc1)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC(C)C(N)=O)=O)C2CCCCC2)C=C1.N[C@@H](CC1=CC=CC=C1)C(=O)N.C(N)(=O)C(C)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O>>C(N)(=O)C(CC1=CC=CC=C1)NC(=O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(N[C:13](=[O:14])[c:15]1[cH:16][cH:17][c:18]2[cH:19][c:20](-[c:21]3[n:22][c:23]4[cH:24][c:25]([C:26](=[O:27])[OH:28])[cH:29][cH:30][c:31]4[n:32]3[CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[cH:39][cH:40][c:41]2[n:42]1)C(N)=O.[NH2:1][C:2](=[O:3])[C@H:4]([CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)[NH2:12]>>[N...
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)Cc1ccccc1
NC(=O)C(Cc1ccccc1)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
null
Acylation
OtherReaction
f4c2f638e60318948ac90dfa9c03d3444d08f75e7747dac6cdda352858bbba9d
32a49b43181b22bb62827dc53d8257f7b05464280b1d25a887c02a1434554159
O=C(NCCc1ccccc1)c1ccc2cc(-c3nc4ccccc4n3C3CCCCC3)ccc2n1
C-C(-N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6])-C(-N)=O.[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[C@@H;D3;+0:10](-[NH2;D1;+0:11])-[C:12]-[c:13]>>[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[CH;D3;+0:10](-[C:12]-[c:13])-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
null
null
The title compound (5 mg yield) was prepared as described for Compound 497a using L-phenylalaninamide in place of L-alaninamide and hydrolyzed as described for Compound 497. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amide.Secondary amide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HO-
null
null
null
CC(NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1)C(N)=O.NC(=O)[C@@H](N)Cc1ccccc1>>NC(=O)C(Cc1ccccc1)NC(=O)c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e7621ebc89f2442885f3f2fb8659b267
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1.Nc1ccc(Cl)cc1>>CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)Nc4ccc(Cl)cc4)ccc3c1)n2C1CCCCC1
C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC(C)C(N)=O)=O)C2CCCCC2)C=C1.ClC1=CC=C(N)C=C1>>C(C)OC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C(NC2=CC=C(C=C2)Cl)=O)C2CCCCC2)C=C1
CC(N[C:20]([c:19]1[n:18][c:17]2[cH:16][cH:15][c:14](-[c:13]3[n:12][c:10]4[c:9]([cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:11]4)[n:34]3[CH:35]3[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]3)[cH:33][c:32]2[cH:31][cH:30]1)=[O:21])C(N)=O.[NH2:22][c:23]1[cH:24][cH:25][c:26]([Cl:27])[cH:28][cH:29]1>>[CH3:1][CH2:2][O:3...
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1.Nc1ccc(Cl)cc1
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)Nc4ccc(Cl)cc4)ccc3c1)n2C1CCCCC1
null
null
null
Acylation
OtherReaction
f4c2f638e60318948ac90dfa9c03d3444d08f75e7747dac6cdda352858bbba9d
32a49b43181b22bb62827dc53d8257f7b05464280b1d25a887c02a1434554159
O=C(Nc1ccccc1)c1ccc2cc(-c3nc4ccccc4n3C3CCCCC3)ccc2n1
C-C(-N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6])-C(-N)=O.[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10])-[c:3](:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
null
null
The title compound was prepared as described for Compound 497a using 4-chloroaniline in place of L-alaninamide yielding 91 mg yellow solid. MS: 553.23 (M+H+). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amide.Secondary amide.Primary amine
Secondary amide
null
null
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1CCCCC1
HO-
null
null
null
CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)NC(C)C(N)=O)ccc3c1)n2C1CCCCC1.Nc1ccc(Cl)cc1>>CCOC(=O)c1ccc2c(c1)nc(-c1ccc3nc(C(=O)Nc4ccc(Cl)cc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2610541fefbf4ea1800dbbcae7606982
COC(=O)c1ccc(N)c(C=O)c1.Cc1cc(Br)ccc1[N+](=O)[O-]>>Nc1ccc(Br)cc1C=O
COC(C1=CC(=C(C=C1)N)C=O)=O.BrC=1C=CC(=C(C1)C)[N+](=O)[O-]>>NC1=C(C=O)C=C(C=C1)Br
COC(=O)c1ccc(N)c(C=[O:10])c1.O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]([Br:6])[cH:7][c:8]1[CH3:9]>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([Br:6])[cH:7][c:8]1[CH:9]=[O:10]
COC(=O)c1ccc(N)c(C=O)c1.Cc1cc(Br)ccc1[N+](=O)[O-]
Nc1ccc(Br)cc1C=O
null
null
null
Functional Group Interconversion
OtherReaction
042e2a520cc0a3baccb3b60d9fbdcea907b8d1ba199d2456815b2bfb5d0e80b1
30708cab4f6652df3674dd025998f44e75ccf959034240412389cee4d338a191
c1ccccc1
C-O-C(=O)-c1:c:c:c(-N):c(-C=[O;H0;D1;+0:1]):c:1.O=[N+;H0;D3:2](-[O-])-[c:3](:[c:4]):[c:5](-[CH3;D1;+0:6]):[c:7]>>[NH2;D1;+0:2]-[c:3](:[c:4]):[c:5](-[CH;D2;+0:6]=[O;H0;D1;+0:1]):[c:7]
null
[]
null
null
null
null
The title intermediate was synthesized as described for Compound 7 in five steps starting from 5-bromo-2-nitrotoluene instead of 3-methyl-4-nitrobenazoic acid methyl ester. MS: 199.97 & 201.97 (M+H+); H1-NMR (CDCl3): δ (ppm) 9.75 (s, 1H), 7.71 (s, 1H), 7.39 (d, 1H, J=9.3 Hz), 7.22 (s, 2H), 6.72 (d, 1H, J=9.3 Hz); Condi...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Nitro group.Primary amine
Aldehyde.Primary amine
c1ccccc1
null
c1ccccc1
HO-
null
null
null
COC(=O)c1ccc(N)c(C=O)c1.Cc1cc(Br)ccc1[N+](=O)[O-]>>Nc1ccc(Br)cc1C=O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-996865c270684c3fb0cde1f265a144da
CO.Cc1ccc(C(=O)O)cc1[N+](=O)[O-]>>COC(=O)c1ccc(C)c([N+](=O)[O-])c1
CC1=C(C=C(C(=O)O)C=C1)[N+](=O)[O-].CO>>COC(C1=CC(=C(C=C1)C)[N+](=O)[O-])=O
[CH3:1][OH:2].O[C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH3:9])[c:10]([N+:11](=[O:12])[O-:13])[cH:14]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH3:9])[c:10]([N+:11](=[O:12])[O-:13])[cH:14]1
CO.Cc1ccc(C(=O)O)cc1[N+](=O)[O-]
COC(=O)c1ccc(C)c([N+](=O)[O-])c1
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[OH;D1;+0:7]>>[C;D1;H3:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
99
[{"value": 99.0, "product": "COC(C1=CC(=C(C=C1)C)[N+](=O)[O-])=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
4-Methyl-3-nitro benzoic acid (12.5 g, 69 mmol) was dissolved in anhydrous methanol (500 mL) in a 1 L flask. HCl gas was then bubbled through the solution until saturation (3 h). The HCl source was then removed, and the reaction was stirred at room temperature overnight. The reaction was then concentrated to dryness an...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
null
null
8
CO.Cc1ccc(C(=O)O)cc1[N+](=O)[O-]>>COC(=O)c1ccc(C)c([N+](=O)[O-])c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-51e6b8b87432486790abfede31b72046
O=C(O)c1ccc2ccc(-c3ccccc3)nc2c1>>O=C(O)c1ccc2cc(-c3ccccc3)cnc2c1
C1(=CC=CC=C1)C1=NC2=CC(=CC=C2C=C1)C(=O)O.COC(C1=CC(=C(C=C1)C=O)N)=O.C1(=CC=CC=C1)CC=O>>C1(=CC=CC=C1)C=1C=NC2=CC(=CC=C2C1)C(=O)O
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][cH:9][c:16](-[c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[n:17][c:18]2[cH:19]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][c:9](-[c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[cH:16][n:17][c:18]2[cH:19]1
O=C(O)c1ccc2ccc(-c3ccccc3)nc2c1
O=C(O)c1ccc2cc(-c3ccccc3)cnc2c1
null
null
null
Miscellaneous
OtherReaction
f6f691826e88d07057a5cbcf7d3e652d23ee5c4f22ff42f1e6c791dc9f00b283
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccc(-c2cnc3ccccc3c2)cc1
[c:1]:[c:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:4]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:[cH;D2;+0:9]:1):[c:10]:[c:11]>>[c:1]:[c:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:9]1:[c:8]:[c:7]:[c:6]:[#7;a:5]:[cH;D2;+0:4]:1):[c:10]:[c:11]
87
[{"value": 87.0, "product": "C1(=CC=CC=C1)C=1C=NC2=CC(=CC=C2C1)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the same reaction procedure and workup for Compound 405f, 500 mg (2.8 mmol) of Compound 53 was reacted with 340 mg (2.8 mmol) phenylacetaldehyde to produce 603 mg (87% yield) of the title intermediate. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2ncccc2c1.c1ccccc1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2ncccc2c1.c1ccccc1
null
null
null
null
O=C(O)c1ccc2ccc(-c3ccccc3)nc2c1>>O=C(O)c1ccc2cc(-c3ccccc3)cnc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-7b5b89fcdf564fe386e02f5424db8de5
O=C(O)c1ccc2c(c1)nc(-c1ccc3ccc(-c4ccccc4)nc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3cc(-c4ccccc4)cnc3c1)n2C1CCCCC1
[OH-].[Na+].C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C2=CC=C1C=CC(=NC1=C2)C2=CC=CC=C2.C(C)(=O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C2=CC=C1C=C(C=NC1=C2)C2=CC=CC=C2
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10][c:11](-[c:12]1[cH:13][cH:14][c:15]3[cH:16][cH:17][c:24](-[c:18]4[cH:19][cH:20][cH:21][cH:22][cH:23]4)[n:25][c:26]3[cH:27]1)[n:28]2[CH:29]1[CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10][c:11](-[c:1...
O=C(O)c1ccc2c(c1)nc(-c1ccc3ccc(-c4ccccc4)nc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3cc(-c4ccccc4)cnc3c1)n2C1CCCCC1
null
null
CCO
Miscellaneous
OtherReaction
f6f691826e88d07057a5cbcf7d3e652d23ee5c4f22ff42f1e6c791dc9f00b283
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccc(-c2cnc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3c2)cc1
[c:1]:[c:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:4]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:[cH;D2;+0:9]:1):[c:10]:[c:11]>>[c:1]:[c:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:9]1:[c:8]:[c:7]:[c:6]:[#7;a:5]:[cH;D2;+0:4]:1):[c:10]:[c:11]
17
[{"value": 17.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C2=CC=C1C=C(C=NC1=C2)C2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the same reaction procedure and workup as for Compound 405, 450 mg (0.9 mmol) of the product from the previous step was cyclized with 40 mL acetic acid and saponified with 35 mL EtOH and 7 mL 1M NaOH to produce 70 mg (17% yield) of the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2ncccc2c1.c1ccccc1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1CCCCC1
null
CCO
null
null
O=C(O)c1ccc2c(c1)nc(-c1ccc3ccc(-c4ccccc4)nc3c1)n2C1CCCCC1>CCO>O=C(O)c1ccc2c(c1)nc(-c1ccc3cc(-c4ccccc4)cnc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f19e1d607e984d218444c87191fc51c7
Nc1cccc2ccc(O)cc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>O=C(Nc1cccc2ccc(O)cc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
N1(CCOCC1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1.NC=1C=CC=C2C=CC(=CC12)O>>OC1=CC=C2C=CC=C(C2=C1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1
[NH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:13][c:14]12.C1CN(N[C:2](=[O:1])[c:15]2[cH:16][cH:17][c:18]3[c:19]([cH:20]2)[n:21][c:22](-[c:23]2[cH:24][cH:25][c:26]4[n:27][c:28](-[c:29]5[cH:30][cH:31][cH:32][cH:33][cH:34]5)[cH:35][n:36][c:37]4[cH:38]2)[n:39]3[CH:40]2[CH2:41][CH2:42][CH2:43][CH2:44]...
Nc1cccc2ccc(O)cc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
O=C(Nc1cccc2ccc(O)cc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
null
null
null
Acylation
OtherReaction
4f548ec504fff937628077160178b3c9fed85cfac0828da72bbcc9b51360aa57
8f23d7ecda4d84b4383fd8be386f02db6f882d0b1474d7b6f40bedcbb175410a
O=C(Nc1cccc2ccccc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-N-N1-C-C-O-C-C-1):[c:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]):[c:7]
20
[{"value": 20.0, "product": "OC1=CC=C2C=CC=C(C2=C1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The general procedure described for Compound 574 was used with 8-amino-naphthalen-2-ol (15.9 mg), producing 5 mg of the title compound (20% yield). MS: 590.25 (M+H+) HPLC Procedure A, retention time=15.31 min. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Ether.Primary amine
Secondary amide
C1COCCN1
null
c1ccc2ccccc2c1.c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.C1CCCCC1
HO-
null
null
null
Nc1cccc2ccc(O)cc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>O=C(Nc1cccc2ccc(O)cc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6d15d8fd54c041dc9ea09e3f50429660
Nc1cccc2c(O)cccc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>O=C(Nc1cccc2c(O)cccc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
N1(CCOCC1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1.NC1=C2C=CC=C(C2=CC=C1)O>>OC1=C2C=CC=C(C2=CC=C1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1
[NH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]([OH:10])[cH:11][cH:12][cH:13][c:14]12.C1CN(N[C:2](=[O:1])[c:15]2[cH:16][cH:17][c:18]3[c:19]([cH:20]2)[n:21][c:22](-[c:23]2[cH:24][cH:25][c:26]4[n:27][c:28](-[c:29]5[cH:30][cH:31][cH:32][cH:33][cH:34]5)[cH:35][n:36][c:37]4[cH:38]2)[n:39]3[CH:40]2[CH2:41][CH2:42][CH2:43][CH2:44]...
Nc1cccc2c(O)cccc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
O=C(Nc1cccc2c(O)cccc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
null
null
null
Acylation
OtherReaction
4f548ec504fff937628077160178b3c9fed85cfac0828da72bbcc9b51360aa57
8f23d7ecda4d84b4383fd8be386f02db6f882d0b1474d7b6f40bedcbb175410a
O=C(Nc1cccc2ccccc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-N-N1-C-C-O-C-C-1):[c:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]):[c:7]
25
[{"value": 25.0, "product": "OC1=C2C=CC=C(C2=CC=C1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The general procedure described for Compound 574 was used with 5-amino-naphthalen-1-ol (15.9 mg), producing 7 mg of the title compound (25% yield). MS: 590.24 (M+H+) HPLC Procedure A, retention time=15.26 min. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Ether.Primary amine
Secondary amide
C1COCCN1
null
c1ccc2ccccc2c1.c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.C1CCCCC1
HO-
null
null
null
Nc1cccc2c(O)cccc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>O=C(Nc1cccc2c(O)cccc12)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f90156ac52c440d7a7ecf69af9d377f2
Nc1ccc2cc(C(=O)O)ccc2c1.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>O=C(O)c1ccc2cc(NC(=O)c3ccc4c(c3)nc(-c3ccc5nc(-c6ccccc6)cnc5c3)n4C3CCCCC3)ccc2c1
N1(CCOCC1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1.NC=1C=C2C=CC(=CC2=CC1)C(=O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)NC=2C=C1C=CC(=CC1=CC2)C(=O)O)C=2C=C1N=CC(=NC1=CC2)C2=CC=CC=C2
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][c:9]([NH2:10])[cH:44][cH:45][c:46]2[cH:47]1.C1CN(N[C:11](=[O:12])[c:13]2[cH:14][cH:15][c:16]3[c:17]([cH:18]2)[n:19][c:20](-[c:21]2[cH:22][cH:23][c:24]4[n:25][c:26](-[c:27]5[cH:28][cH:29][cH:30][cH:31][cH:32]5)[cH:33][n:34][c:35]4[cH:36]2)[n:37]3[CH:38]2[CH2:39][CH2:40][...
Nc1ccc2cc(C(=O)O)ccc2c1.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
O=C(O)c1ccc2cc(NC(=O)c3ccc4c(c3)nc(-c3ccc5nc(-c6ccccc6)cnc5c3)n4C3CCCCC3)ccc2c1
null
null
null
Acylation
OtherReaction
4f548ec504fff937628077160178b3c9fed85cfac0828da72bbcc9b51360aa57
8f23d7ecda4d84b4383fd8be386f02db6f882d0b1474d7b6f40bedcbb175410a
O=C(Nc1ccc2ccccc2c1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-N-N1-C-C-O-C-C-1):[c:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]):[c:7]
53
[{"value": 53.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)NC=2C=C1C=CC(=CC1=CC2)C(=O)O)C=2C=C1N=CC(=NC1=CC2)C2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The general procedure described for Compound 574 was used with 6-amino-naphthalene-2-carboxylic acid (18.7 mg), producing 15 mg of the title compound (53% yield). MS: 618.30 (M+H+) HPLC Procedure A, retention time=16.24 min. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Ether.Primary amine
Secondary amide
C1COCCN1
null
c1ccc2ccccc2c1.c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.C1CCCCC1
HO-
null
null
null
Nc1ccc2cc(C(=O)O)ccc2c1.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>O=C(O)c1ccc2cc(NC(=O)c3ccc4c(c3)nc(-c3ccc5nc(-c6ccccc6)cnc5c3)n4C3CCCCC3)ccc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-4fd734490f3241b4926853d768dbdc08
Cc1cc(=O)oc2cc(N)ccc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>Cc1cc(=O)oc2cc(NC(=O)c3ccc4c(c3)nc(-c3ccc5nc(-c6ccccc6)cnc5c3)n4C3CCCCC3)ccc12
N1(CCOCC1)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1.NC1=CC=C2C(=CC(OC2=C1)=O)C>>CC1=CC(OC2=CC(=CC=C12)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1)=O
[CH3:1][c:2]1[cH:3][c:4](=[O:5])[o:6][c:7]2[cH:8][c:9]([NH2:10])[cH:44][cH:45][c:46]12.C1CN(N[C:11](=[O:12])[c:13]2[cH:14][cH:15][c:16]3[c:17]([cH:18]2)[n:19][c:20](-[c:21]2[cH:22][cH:23][c:24]4[n:25][c:26](-[c:27]5[cH:28][cH:29][cH:30][cH:31][cH:32]5)[cH:33][n:34][c:35]4[cH:36]2)[n:37]3[CH:38]2[CH2:39][CH2:40][CH2:41]...
Cc1cc(=O)oc2cc(N)ccc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
Cc1cc(=O)oc2cc(NC(=O)c3ccc4c(c3)nc(-c3ccc5nc(-c6ccccc6)cnc5c3)n4C3CCCCC3)ccc12
null
null
null
Acylation
OtherReaction
4f548ec504fff937628077160178b3c9fed85cfac0828da72bbcc9b51360aa57
8f23d7ecda4d84b4383fd8be386f02db6f882d0b1474d7b6f40bedcbb175410a
O=C(Nc1ccc2ccc(=O)oc2c1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-N-N1-C-C-O-C-C-1):[c:7].[#8;a:8]:[c:9]:[c:10]:[c:11](-[NH2;D1;+0:12]):[c:13]>>[#7;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-[NH;D2;+0:12]-[c:11](:[c:13]):[c:10]:[c:9]:[#8;a:8]):[c:7]
27
[{"value": 27.0, "product": "CC1=CC(OC2=CC(=CC=C12)NC(=O)C1=CC2=C(N(C(=N2)C=2C=C3N=CC(=NC3=CC2)C2=CC=CC=C2)C2CCCCC2)C=C1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The general procedure described for Compound 574 was used with 7-Amino-4-methyl-chromen-2-one (17.5 mg), producing 8 mg of the title compound (27% yield). MS: 606.29 (M+H+) HPLC Procedure A, retention time=19.22 min. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Ether.Primary amine
Secondary amide
C1COCCN1
null
c1ccc2cccoc2c1.c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.C1CCCCC1
HO-
null
null
null
Cc1cc(=O)oc2cc(N)ccc12.O=C(NN1CCOCC1)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>Cc1cc(=O)oc2cc(NC(=O)c3ccc4c(c3)nc(-c3ccc5nc(-c6ccccc6)cnc5c3)n4C3CCCCC3)ccc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-69d0562ddf334b968cb7cf8b9f8bccaf
CO.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3c(c1)CCC(c1ccccc1)N3)n2C1CCCCC1
C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=CC(=NC1=CC2)C2=CC=CC=C2.CO>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1CCC(NC1=CC2)C2=CC=CC=C2
O[CH3:18].n1[c:16]2[c:15]([cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:28]3[CH:29]3[CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]3)[cH:17]2)[n:27][c:20](-[c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[cH:19]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10][c:1...
CO.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3c(c1)CCC(c1ccccc1)N3)n2C1CCCCC1
null
[Pt]=O
null
C-C Coupling
OtherReaction
8ccad5df995a0e3ae8425227ec1de04f50da0fb9dd9e80ad7109b42b2b8b7108
d80e9c8f1cb73de4407c680a89390fbbfe9dc0b798896329454cba59f37c6e63
c1ccc(C2CCc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3N2)cc1
O-[CH3;D1;+0:1].[c:2]:[c:3]:[c;H0;D3;+0:4]1:n:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[n;H0;D2;+0:12]:[c:13]:1:[c:14]>>[c:2]:[c:3]:[c;H0;D3;+0:4]1:[c:13](:[c:14])-[NH;D2;+0:12]-[CH;D3;+0:6](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11])-[CH2;D2;+0:5]-[CH2;D2;+0:1]-1
37
[{"value": 37.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1CCC(NC1=CC2)C2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of Compound 203 (100 mg, 0.23 mmol) and platinum oxide (12 mg, 0.048 mmol) in methanol (5 mL) was hydrogenated at 40 psi for 3 h. The reaction was evaporated to dryness, and purified via HPLC. The resulting compound was then converted to the HCl salt using the standard method, yielding 40 mg (37% yield) of t...
10.6084/m9.figshare.5104873.v1
null
Methanol
Secondary amine
c1ccc2nccnc2c1
c1ccc2c(c1)CCCN2
c1ccc2nc[nH]c2c1.c1ccc2c(c1)CCCN2.c1ccccc1.C1CCCCC1
Other
[Pt]=O
null
null
CO.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2C1CCCCC1>[Pt]=O>O=C(O)c1ccc2c(c1)nc(-c1ccc3c(c1)CCC(c1ccccc1)N3)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6407c5c47c5d40179ff0ffbe2a0ddb91
O=Cc1ccccc1Br>>OC(Cc1ccccc1)c1ccccc1Br
BrC1=C(C=O)C=CC=C1>>BrC1=C(C=CC=C1)C(CC1=CC=CC=C1)O
[O:1]=[CH:2][c:10]1[cH:11][cH:3][cH:13][cH:14][c:15]1[Br:16]>>[OH:1][CH:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[Br:16]
O=Cc1ccccc1Br
OC(Cc1ccccc1)c1ccccc1Br
null
null
C(C)OCC
Functional Group Interconversion
OtherReaction
e0491bf6f518a9ce005e928ff9be06918efd8060222a74d00b75b1e53a66a5b1
6318a0e9fb1d756c97d86db7e28e5f6266d7a157dcbb02a5dab947d71eb6de40
c1ccc(CCc2ccccc2)cc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:1>>[OH;D1;+0:1]-[CH;D3;+0:2](-[CH2;D2;+0:7]-[c:9](:[c:10]):[c:11])-[c:3]1:[c:4]:[c:5]:[cH;D2;+0:6]:[c:12]:[cH;D2;+0:8]:1
69.5
[{"value": 33.0, "product": "BrC1=C(C=CC=C1)C(CC1=CC=CC=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.5, "product": "BrC1=C(C=CC=C1)C(CC1=CC=CC=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-10
CELSIUS
1
HOUR
A mixture of 2-bromobenzaldehyde (1 mL, 5.4 mmol) in diethylether (2 mL) was added to a flame dried flask, and flushed with argon. The temperature was reduced to −10° C. and benzylmagnesium chloride was slowly added to the flask via syringe. The reaction was stirred at −10° C. for 1 hour and then stirred at room temper...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Other
C(C)OCC
-10
1
O=Cc1ccccc1Br>C(C)OCC>OC(Cc1ccccc1)c1ccccc1Br
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ac96ea8dd609482fadcaf9874f73ccec
O=C(Cc1ccccc1)c1ccccc1Br.O=C(O)c1ccc2ccc(-c3ccccc3)nc2c1>>O=C(O)c1ccc2nc(-c3ccccc3)c(-c3ccccc3Br)cc2c1
[OH-].[K+].BrC1=C(C=CC=C1)C(CC1=CC=CC=C1)=O.C1(=CC=CC=C1)C1=NC2=CC(=CC=C2C=C1)C(=O)O.COC(C1=CC(=C(C=C1)C=O)N)=O>>BrC1=C(C=CC=C1)C=1C(=NC2=CC=C(C=C2C1)C(=O)O)C1=CC=CC=C1
O=[C:16]([CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[Br:23].c1ccc(-c2c[cH:24][c:25]3[cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:26][c:7]3[n:8]2)cc1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[n:8][c:9](-[c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[c:16](-[c:17]3[cH:18][c...
O=C(Cc1ccccc1)c1ccccc1Br.O=C(O)c1ccc2ccc(-c3ccccc3)nc2c1
O=C(O)c1ccc2nc(-c3ccccc3)c(-c3ccccc3Br)cc2c1
null
null
C(C)O
Miscellaneous
OtherReaction
ae62b681ea84868d1d2f7aa4b1dc673955b875637d3380e3d8040d09295c977f
9db0f73aed071f5fa7238b261fc87a241efa69e871d2f239452605149d0c954e
c1ccc(-c2cc3ccccc3nc2-c2ccccc2)cc1
O=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7])-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](-[Br;D1;H0:12]):[c:13].[O;D1;H0:14]=[C:15](-[O;D1;H1:16])-[c:17]1:[c:18]:[cH;D2;+0:19]:[c;H0;D3;+0:20]2:[cH;D2;+0:21]:c:c(-c3:c:c:c:c:c:3):[n;H0;D2;+0:22]:[c;H0;D3;+0:23]:2:[cH;D2;+0:24]:1>>[Br;D1;H0:12]-[c:11...
40
[{"value": 40.0, "product": "BrC1=C(C=CC=C1)C=1C(=NC2=CC=C(C=C2C1)C(=O)O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the same reaction procedure and workup as for Compound 405f (235 mg, 1.31 mmol) of Compound 53 was reacted with the product of the previous reaction, Compound 424b (360 mg, 1.31 mmol), in ethanol (12 mL) using 10% w/v KOH in ethanol (1.1 mL) to produce the title compound (210 mg, 40% yield). Conditions: See r...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1.c1ccccc1
HO-
C(C)O
null
null
O=C(Cc1ccccc1)c1ccccc1Br.O=C(O)c1ccc2ccc(-c3ccccc3)nc2c1>C(C)O>O=C(O)c1ccc2nc(-c3ccccc3)c(-c3ccccc3Br)cc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-c0877fc4f7d040d7b6c35f3309892e7a
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4Br)c(-c4ccccc4)cc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)cc1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4-c4ccc(Cl)cc4)c(-c4ccccc4)cc3c1)n2C1CCCCC1
BrC1=C(C=CC=C1)C1=NC2=CC=C(C=C2C=C1C1=CC=CC=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O.ClC1=CC=C(C=C1)B(O)O.[F-].[Cs+].C1(CCCCC1)P(C1=C(C=CC=C1)C1=CC=CC=C1)C1CCCCC1>>ClC1=CC=C(C2=CC=CC=C2C2=NC3=CC=C(C=C3C=C2C2=CC=CC=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C=C1
Br[c:23]1[c:18](-[c:17]2[n:16][c:15]3[cH:14][cH:13][c:12](-[c:11]4[n:10][c:8]5[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]5)[n:41]4[CH:42]4[CH2:43][CH2:44][CH2:45][CH2:46][CH2:47]4)[cH:40][c:39]3[cH:38][c:31]2-[c:32]2[cH:33][cH:34][cH:35][cH:36][cH:37]2)[cH:19][cH:20][cH:21][cH:22]1.OB(O)[c:24]1[cH:25][cH:26][c:2...
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4Br)c(-c4ccccc4)cc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)cc1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4-c4ccc(Cl)cc4)c(-c4ccccc4)cc3c1)n2C1CCCCC1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
O1CCOCC1
C-C Coupling
Suzuki coupling with boronic acids
d79a78c79f0c392f0911481acf5c300cc98205269acdb93c24fb610a61c4c868
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccccc2-c2nc3ccc(-c4nc5ccccc5n4C4CCCCC4)cc3cc2-c2ccccc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].O-B(-O)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]):[c:2]:[c:3]
10
[{"value": 10.0, "product": "ClC1=CC=C(C2=CC=CC=C2C2=NC3=CC=C(C=C3C=C2C2=CC=CC=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 7.6, "product": "ClC1=CC=C(C2=CC=CC=C2C2=NC3=CC=C(C=C3C=C2C2=CC=CC=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C=C1", "details": "CALCULATEDP...
null
null
null
null
Compound 424 (50 mg, 0.083 mmol), 4-chlorophenylboronic acid (20 mg, 0.125 mmol), and CsF (143 mg, 0.94 mmol) were added to degassed dioxane (6 mL). A solution of 2-(dicyclohexylphosphino)biphenyl (5 mg, 0.0125 mmol) and palladium acetate (2 mg, 0.0083 mmol) in degassed dioxane (3 mL) was added to the reaction solution...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.c1ccccc1.c1ccccc1.C1CCCCC1
HBr.B
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].O1CCOCC1
null
null
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4Br)c(-c4ccccc4)cc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)cc1>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].O1CCOCC1>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4-c4ccc(Cl)cc4)c(-c4ccccc4)cc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8bed7191e06c456c8c8827c4bb81f6b9
CC(=O)c1sc(C)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1nc(C)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)s1
[OH-].[K+].CC=1SC(=C(N1)C)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(N=C(S2)C)C
CC(=O)[c:6]1[c:4]([CH3:5])[n:3][c:2]([CH3:1])[s:35]1.Oc1ccc(Br)cc1-[c:7]1[cH:8][cH:9][c:10]2[cH:11][c:12](-[c:13]3[n:14][c:15]4[cH:16][c:17]([C:18](=[O:19])[OH:20])[cH:21][cH:22][c:23]4[n:24]3[CH:25]3[CH2:26][CH2:27][CH2:28][CH2:29][CH2:30]3)[cH:31][cH:32][c:33]2[n:34]1>>[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6](-[c:7]2[cH...
CC(=O)c1sc(C)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1nc(C)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)s1
null
null
C(C)O
C-C Coupling
OtherReaction
1d5c6f5b005ed70236ee338e17825f9573e4b8d5662849fd033a7cd4739092e7
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4cncs4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#16;a:7]:[c:8](-[C;D1;H3:9]):[#7;a:10]:[c:11]:1-[C;D1;H3:12]>>[C;D1;H3:9]-[c:8]1:[#16;a:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:11](-[C;D1;H3:12]):[#7;a:10]:1
12
[{"value": 12.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(N=C(S2)C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(2,4-dimethyl-thiazol-5-yl)-ethanone (40 mg, 0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (14 mg, 12% yield). Conditions: See reaction.notes.procedur...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cscn1.c1ccccc1.c1ccc2ncccc2c1
c1cscn1.c1ccc2ncccc2c1
c1cscn1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1sc(C)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1nc(C)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)s1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-3596edbd2f384c0d836cf126775eadf5
CC(=O)c1cnccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cnccn4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1=C(C=NC=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=NC=CN=C2
CC(=O)[c:18]1[cH:19][n:20][cH:21][cH:22][n:23]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:28]3[CH:29]3[CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]3)[cH:27][c:26]2[cH:25][cH:24]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)...
CC(=O)c1cnccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cnccn4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
8d7f7f838313f3fa8ed1d397054cedde74cba805c43cafbd7c0fcc30f04297af
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4cnccn4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#7;a:7]:[c:8]:[c:9]:[#7;a:10]:[c:11]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[#7;a:7]:[c:8]:[c:9]:[#7;a:10]:[c:11]:1):[c:4]:[c:5]
10
[{"value": 10.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=NC=CN=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-pyrazin-2-yl-ethanone (32 mg, 0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (15 mg, 10% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cnccn1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1cnccn1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1cnccn1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cnccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cnccn4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-561575b8e7704ae387f663ecc1da3ca6
CC(=O)c1cc(C)sc1-c1ccccc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(-c2ccccc2)s1
[OH-].[K+].CC1=CC(=C(S1)C1=CC=CC=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(SC(=C2)C)C2=CC=CC=C2
CC(=O)[c:4]1[cH:3][c:2]([CH3:1])[s:40][c:33]1-[c:34]1[cH:35][cH:36][cH:37][cH:38][cH:39]1.Oc1ccc(Br)cc1-[c:5]1[cH:6][cH:7][c:8]2[cH:9][c:10](-[c:11]3[n:12][c:13]4[cH:14][c:15]([C:16](=[O:17])[OH:18])[cH:19][cH:20][c:21]4[n:22]3[CH:23]3[CH2:24][CH2:25][CH2:26][CH2:27][CH2:28]3)[cH:29][cH:30][c:31]2[n:32]1>>[CH3:1][c:2]1...
CC(=O)c1cc(C)sc1-c1ccccc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(-c2ccccc2)s1
null
null
C(C)O
C-C Coupling
OtherReaction
720f87d7df89fae5bee313ea8aae90dd7d141265b6e283e34e49e8dc216a5da5
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2sccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[c:8](-[C;D1;H3:9]):[#16;a:10]:[c:11]:1-[c:12]>>[C;D1;H3:9]-[c:8]1:[#16;a:10]:[c:11](-[c:12]):[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:7]:1
6
[{"value": 6.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(SC(=C2)C)C2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(5-methyl-2-phenyl-thiophen-3-yl)-ethanone (56 mg, 0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (8 mg, 6% yield). MS: 544.27 (M+H+) HPLC Procedure A,...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccsc1.c1ccccc1.c1ccc2ncccc2c1
c1ccsc1.c1ccc2ncccc2c1
c1ccsc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1.c1ccccc1
HBr
C(C)O
null
null
CC(=O)c1cc(C)sc1-c1ccccc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(-c2ccccc2)s1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d0314f5eca9248e8bebd8db872902711
CC(=O)c1cccnc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccnc4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1=CC(=CC=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=NC=CC2
CC(=O)[c:18]1[cH:19][cH:20][cH:21][n:22][cH:23]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:28]3[CH:29]3[CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]3)[cH:27][c:26]2[cH:25][cH:24]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1...
CC(=O)c1cccnc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccnc4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
d5534b6176d25a1cb3e85eefaaaa0dc1ef5ab28f7e223e08a461bb05612a5757
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1cncc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)c1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[c:9]:[#7;a:10]:[c:11]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[c:9]:[#7;a:10]:[c:11]:1):[c:4]:[c:5]
17
[{"value": 17.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=NC=CC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-pyridin-3-yl-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (19 mg, 17% yield). MS: 449.21 (M+H+) HPLC Procedure A, retention time=7.96 min. ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccncc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccncc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccncc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cccnc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccnc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6683c72d96d44e91a5ddb2d6855abedd
CC(=O)Nc1ccc(C(C)=O)cc1Br.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1Br
[OH-].[K+].C(C)(=O)C1=CC(=C(C=C1)NC(C)=O)Br.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>NC1=C(C=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)Br
CC(=O)[NH:1][c:2]1[cH:3][cH:4][c:5](C(C)=O)[cH:34][c:35]1[Br:36].Oc1ccc(Br)cc1-[c:6]1[cH:7][cH:8][c:9]2[cH:10][c:11](-[c:12]3[n:13][c:14]4[cH:15][c:16]([C:17](=[O:18])[OH:19])[cH:20][cH:21][c:22]4[n:23]3[CH:24]3[CH2:25][CH2:26][CH2:27][CH2:28][CH2:29]3)[cH:30][cH:31][c:32]2[n:33]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5](-[c:6]...
CC(=O)Nc1ccc(C(C)=O)cc1Br.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1Br
null
null
C(C)O
C-C Coupling
OtherReaction
b0109585fb62adf21b170d8a9b3adf76273dcbc10a034897a2b5300b11ff5c59
5ca2dbb86b1d71648651aa5e8bd2a294710e9b63655fd94318bc1399c5ea000e
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[NH;D2;+0:6]-[c:7]1:[c:8]:[c:9]:[c;H0;D3;+0:10](-C(-C)=O):[c:11]:[c:12]:1>>[NH2;D1;+0:6]-[c:7]1:[c:8]:[c:9]:[c;H0;D3;+0:10](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:11]:[c:12]:1
15
[{"value": 15.0, "product": "NC1=C(C=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)Br", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with N-(4-acetyl-2-bromo-phenyl)-acetamide (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (16 mg, 15% yield). Conditions: See reaction.notes.procedure_detail...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Secondary amide.Aromatic alcohol
Primary amine
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)Nc1ccc(C(C)=O)cc1Br.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1Br
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-96ce9955b25e4e4398cc1e634f7c3ab1
CC(=O)c1sc(N)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1nc(N)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].NC=1SC(=C(N1)C)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>NC=1SC(=C(N1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)[c:7]1[c:2]([CH3:1])[n:3][c:4]([NH2:5])[s:6]1.Oc1ccc(Br)cc1-[c:8]1[cH:9][cH:10][c:11]2[cH:12][c:13](-[c:14]3[n:15][c:16]4[cH:17][c:18]([C:19](=[O:20])[OH:21])[cH:22][cH:23][c:24]4[n:25]3[CH:26]3[CH2:27][CH2:28][CH2:29][CH2:30][CH2:31]3)[cH:32][cH:33][c:34]2[n:35]1>>[CH3:1][c:2]1[n:3][c:4]([NH2:5])[s:6][c:7]1-[c:8...
CC(=O)c1sc(N)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1nc(N)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
1d5c6f5b005ed70236ee338e17825f9573e4b8d5662849fd033a7cd4739092e7
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4cncs4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#16;a:7]:[c:8](-[N;D1;H2:9]):[#7;a:10]:[c:11]:1-[C;D1;H3:12]>>[C;D1;H3:12]-[c:11]1:[#7;a:10]:[c:8](-[N;D1;H2:9]):[#16;a:7]:[c;H0;D3;+0:6]:1-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
9
[{"value": 9.0, "product": "NC=1SC(=C(N1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(2-amino-4-methyl-thiazol-5-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (8 mg, 9% yield). MS: 484.19 (M+H+); HPLC Procedure A, retenti...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cscn1.c1ccccc1.c1ccc2ncccc2c1
c1cscn1.c1ccc2ncccc2c1
c1cscn1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1sc(N)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1nc(N)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2cb1bd4899fc45fe94e854b6f97a9f52
CC(=O)c1cc2cccc(O)c2o1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc5cccc(O)c5o4)ccc3c1)n2C1CCCCC1
[OH-].[K+].OC1=CC=CC=2C=C(OC21)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2OC1=C(C2)C=CC=C1O
CC(=O)[c:18]1[cH:19][c:20]2[cH:21][cH:22][cH:23][c:24]([OH:25])[c:26]2[o:27]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:32]3[CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[cH:31][c:30]2[cH:29][cH:28]1>>[O:1]=[C:2]([OH:3])[c:4]1[c...
CC(=O)c1cc2cccc(O)c2o1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc5cccc(O)c5o4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
6652b3d332750b9521edc9f82282db3de6903bc89164acd6b71bb882c727b5c6
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2oc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cc2c1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#8;a:7]:[c:8]:[c:9]:[c:10]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[#8;a:7]:[c:8]:[c:9]:[c:10]:1):[c:4]:[c:5]
20
[{"value": 20.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2OC1=C(C2)C=CC=C1O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(7-hydroxy-benzofuran-2-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (19 mg, 20% yield). MS: 504.22 (M+H+); HPLC Procedure A, retention...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2occc2c1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccc2occc2c1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccc2occc2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cc2cccc(O)c2o1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc5cccc(O)c5o4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-4c01ec35257e41d6b0e9098be9038ce2
CC(=O)c1ccccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccn4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1=C(C=CC=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=NC=CC=C2
CC(=O)[c:18]1[cH:19][cH:20][cH:21][cH:22][n:23]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:28]3[CH:29]3[CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]3)[cH:27][c:26]2[cH:25][cH:24]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1...
CC(=O)c1ccccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccn4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
d5534b6176d25a1cb3e85eefaaaa0dc1ef5ab28f7e223e08a461bb05612a5757
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)nc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[#7;a:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[#7;a:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
61
[{"value": 61.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=NC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-pyridin-2-yl-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (66 mg, 61% yield). MS: 449.19 (M+H+); HPLC Procedure A, retention time=9.85 min....
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccncc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccncc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccncc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccn4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a729877e4fcc43ea942f71b55ecab342
CC(=O)c1ccncc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccncc4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1=CC=C(C=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=NC=C2
CC(=O)[c:18]1[cH:19][cH:20][n:21][cH:22][cH:23]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:28]3[CH:29]3[CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]3)[cH:27][c:26]2[cH:25][cH:24]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1...
CC(=O)c1ccncc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccncc4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
d5534b6176d25a1cb3e85eefaaaa0dc1ef5ab28f7e223e08a461bb05612a5757
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccncc4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]:[c:11]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]:[c:11]:1):[c:4]:[c:5]
62
[{"value": 62.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=NC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-pyridin-4-yl-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (68 mg, 62% yield). MS: 449.19 (M+H+); HPLC Procedure A, retention time=7.98 min....
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccncc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccncc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccncc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccncc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccncc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-3a60b87d9e7242568651ab3ec98cd8ec
CC(=O)c1ccc2c(c1)CCCC2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCCC5)ccc3c1)n2C1CCCCC1
[OH-].[K+].C1=C(C=CC=2CCCCC12)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=1CCCCC1C=C2
CC(=O)[c:18]1[cH:19][cH:20][c:21]2[c:22]([cH:23]1)[CH2:24][CH2:25][CH2:26][CH2:27]2.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:32]3[CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[cH:31][c:30]2[cH:29][cH:28]1>>[O:1]=[C:2]([OH:3])[c...
CC(=O)c1ccc2c(c1)CCCC2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCCC5)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
078f91edee6b5c6d7b7edf432944d3142beda02044934488d4cffac72c411ca2
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCCC5)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
60
[{"value": 60.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=1CCCCC1C=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(5,6,7,8-tetrahydro-naphthalen-2-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in Ethanol (506 μL, 0.64 mmol) to produce the title compound (65 mg, 60% yield). Conditions: See reaction.notes.proced...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2c(c1)CCCC2.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccc2c(c1)CCCC2
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccc2c(c1)CCCC2.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc2c(c1)CCCC2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCCC5)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-cf096c975d6f49ce992b5d9c9a8dca70
CC(=O)c1ccc(-n2ccnc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(-n5ccnc5)cc4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1(C=NC=C1)C1=CC=C(C=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)N2C=NC=C2
CC(=O)[c:18]1[cH:19][cH:20][c:21](-[n:22]2[cH:23][cH:24][n:25][cH:26]2)[cH:27][cH:28]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:33]3[CH:34]3[CH2:35][CH2:36][CH2:37][CH2:38][CH2:39]3)[cH:32][c:31]2[cH:30][cH:29]1>>[O:1]=[C:2]([OH:3]...
CC(=O)c1ccc(-n2ccnc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(-n5ccnc5)cc4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(-n5ccnc5)cc4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
59
[{"value": 59.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)N2C=NC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(4-imidazol-1-yl-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (75 mg, 59% yield). MS: 514.23 (M+H+); HPLC Procedure A, retention ti...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.c1c[nH]cn1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(-n2ccnc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(-n5ccnc5)cc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a67946a7234243fc9a807d1bcb5858dc
CC(=O)c1ccc2c(c1)OCO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)OCO5)ccc3c1)n2C1CCCCC1
[OH-].[K+].O1COC2=C1C=CC(=C2)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>O1COC2=C1C=CC(=C2)C2=NC1=CC=C(C=C1C=C2)C2=NC1=C(N2C2CCCCC2)C=CC(=C1)C(=O)O
CC(=O)[c:18]1[cH:19][cH:20][c:21]2[c:22]([cH:23]1)[O:24][CH2:25][O:26]2.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:31]3[CH:32]3[CH2:33][CH2:34][CH2:35][CH2:36][CH2:37]3)[cH:30][c:29]2[cH:28][cH:27]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c...
CC(=O)c1ccc2c(c1)OCO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)OCO5)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
9be81f0fe3669a9a52d6d38cfbe45d9e257f62642d0dc37167152cef6460bdb7
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)OCO5)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]-[#8:11]>>[#8:11]-[c:10]:[c:9]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:7]:[c:8]
24
[{"value": 24.0, "product": "O1COC2=C1C=CC(=C2)C2=NC1=CC=C(C=C1C=C2)C2=NC1=C(N2C2CCCCC2)C=CC(=C1)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-benzo[1,3]dioxol-5-yl-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (30 mg, 24% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2c(c1)OCO2.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccc2c(c1)OCO2
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccc2c(c1)OCO2.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc2c(c1)OCO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)OCO5)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-74d401b8ec4242da885bcb02ec2dc6e1
CC(=O)c1ccc(Oc2ccccc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Oc5ccccc5)cc4)ccc3c1)n2C1CCCCC1
[OH-].[K+].O(C1=CC=CC=C1)C1=CC=C(C=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)OC2=CC=CC=C2
CC(=O)[c:18]1[cH:19][cH:20][c:21]([O:22][c:23]2[cH:24][cH:25][cH:26][cH:27][cH:28]2)[cH:29][cH:30]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:35]3[CH:36]3[CH2:37][CH2:38][CH2:39][CH2:40][CH2:41]3)[cH:34][c:33]2[cH:32][cH:31]1>>[O:1]...
CC(=O)c1ccc(Oc2ccccc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Oc5ccccc5)cc4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(Oc2ccc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cc2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
31
[{"value": 31.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)OC2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(4-phenoxy-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in Ethanol (506 μL, 0.64 mmol) to produce the title compound (42 mg, 31% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(Oc2ccccc2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Oc5ccccc5)cc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2ba75bfd167246c3be98eb0925ef2372
CC(=O)c1ccc(N2CCNCC2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCNCC5)cc4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1(CCNCC1)C1=CC=C(C=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)N2CCNCC2
CC(=O)[c:18]1[cH:19][cH:20][c:21]([N:22]2[CH2:23][CH2:24][NH:25][CH2:26][CH2:27]2)[cH:28][cH:29]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:34]3[CH:35]3[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]3)[cH:33][c:32]2[cH:31][cH:30]1>>[O:1]=[...
CC(=O)c1ccc(N2CCNCC2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCNCC5)cc4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCNCC5)cc4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
91
[{"value": 91.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)N2CCNCC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(4-piperazin-1-yl-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (120 mg, 91% yield). MS: 532.21 (M+H+); HPLC Procedure A, retention ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1C[NH]CCN1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(N2CCNCC2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCNCC5)cc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-85a15cee2a5e499393429284ebf976d1
CC(=O)Nc1ccc(C(C)=O)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>CC(=O)Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
[OH-].[K+].C(C)(=O)C1=CC=C(C=C1)NC(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C(C)(=O)NC1=CC=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)[c:8]1[cH:7][cH:6][c:5]([NH:4][C:2]([CH3:1])=[O:3])[cH:38][cH:37]1.Oc1ccc(Br)cc1-[c:9]1[cH:10][cH:11][c:12]2[cH:13][c:14](-[c:15]3[n:16][c:17]4[cH:18][c:19]([C:20](=[O:21])[OH:22])[cH:23][cH:24][c:25]4[n:26]3[CH:27]3[CH2:28][CH2:29][CH2:30][CH2:31][CH2:32]3)[cH:33][cH:34][c:35]2[n:36]1>>[CH3:1][C:2](=[O:3])[NH:4]...
CC(=O)Nc1ccc(C(C)=O)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
CC(=O)Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:5]:[c:4]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[#7;a:2]:[c:3]
15
[{"value": 15.0, "product": "C(C)(=O)NC1=CC=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with N-(4-acetyl-phenyl)-acetamide (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (19 mg, 15% yield). MS: 505.26 (M+H+); HPLC Procedure A, retention time=9.9...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)Nc1ccc(C(C)=O)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>CC(=O)Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-172f2be876094ff0ae6346fa773a22d3
CC(=O)c1ccc(N)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
[OH-].[K+].NC1=CC=C(C=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>NC1=CC=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)c1c[cH:3][c:2]([NH2:1])[cH:35][cH:34]1.Oc1ccc(Br)[cH:4][c:5]1-[c:6]1[cH:7][cH:8][c:9]2[cH:10][c:11](-[c:12]3[n:13][c:14]4[cH:15][c:16]([C:17](=[O:18])[OH:19])[cH:20][cH:21][c:22]4[n:23]3[CH:24]3[CH2:25][CH2:26][CH2:27][CH2:28][CH2:29]3)[cH:30][cH:31][c:32]2[n:33]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:...
CC(=O)c1ccc(N)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
null
null
C(C)O
Miscellaneous
OtherReaction
d719b5773425a1262e3c8365a5fe3595c74e53585547b38c08bc2408e1828872
5d663a6f3250645b78580d7f1b46d37e7983f21b5145184e88099bc5e394410f
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):c(-O):c:c:1.C-C(=O)-c1:[cH;D2;+0:7]:[c:8]:[c:9](-[N;D1;H2:10]):[cH;D2;+0:11]:c:1>>[N;D1;H2:10]-[c:9]1:[c:8]:[cH;D2;+0:7]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):[cH;D2;+0:1]:[cH;D2;+0:11]:1
10
[{"value": 10.0, "product": "NC1=CC=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(4-amino-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (14 mg, 10% yield). MS: 463.23 (M+H+); HPLC Procedure A, retention time=8.62 ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(N)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Nc1ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d8474d7d175943d79dbc7974c9e6d8b8
CC(=O)c1ccc(O)c(C(N)=O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>NC(=O)c1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)ccc1O
[OH-].[K+].C(C)(=O)C=1C=CC(=C(C(=O)N)C1)O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C(N)(=O)C=1C=C(C=CC1O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)c1[cH:5][c:4]([C:2]([NH2:1])=[O:3])[c:37]([OH:38])[cH:36][cH:35]1.Oc1ccc(Br)c[c:6]1-[c:7]1[cH:8][cH:9][c:10]2[cH:11][c:12](-[c:13]3[n:14][c:15]4[cH:16][c:17]([C:18](=[O:19])[OH:20])[cH:21][cH:22][c:23]4[n:24]3[CH:25]3[CH2:26][CH2:27][CH2:28][CH2:29][CH2:30]3)[cH:31][cH:32][c:33]2[n:34]1>>[NH2:1][C:2](=[O:3])[c:4]...
CC(=O)c1ccc(O)c(C(N)=O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
NC(=O)c1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)ccc1O
null
null
C(C)O
Miscellaneous
OtherReaction
d719b5773425a1262e3c8365a5fe3595c74e53585547b38c08bc2408e1828872
5d663a6f3250645b78580d7f1b46d37e7983f21b5145184e88099bc5e394410f
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):[c;H0;D3;+0:1](-[c:2](:[c:3]):[#7;a:4]:[c:5]):c:1.C-C(=O)-c1:[cH;D2;+0:6]:[c:7]:[c:8]:[c:9](-[C:10](-[N;D1;H2:11])=[O;D1;H0:12]):[cH;D2;+0:13]:1>>[N;D1;H2:11]-[C:10](=[O;D1;H0:12])-[c:9]1:[c:8]:[c:7]:[cH;D2;+0:6]:[c;H0;D3;+0:1](-[c:2](:[c:3]):[#7;a:4]:[c:5]):[cH;D2;+0:13]:1
10
[{"value": 10.0, "product": "C(N)(=O)C=1C=C(C=CC1O)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 5-acetyl-2-hydroxy-benzamide (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in Ethanol (506 μL, 0.64 mmol) to produce the title compound (13 mg, 10% yield). MS: 507.24 (M+H+); HPLC Procedure A, retention time=10.3...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(O)c(C(N)=O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>NC(=O)c1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)ccc1O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d01a71d18ef842d18ec04cd6910db6df
CC(=O)CCCO.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(CCCO)ccc3c1)n2C1CCCCC1
[OH-].[K+].OCCCC(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)CCCO
CC(=O)[CH2:18][CH2:19][CH2:20][OH:21].Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:26]3[CH:27]3[CH2:28][CH2:29][CH2:30][CH2:31][CH2:32]3)[cH:25][c:24]2[cH:23][cH:22]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10][c:1...
CC(=O)CCCO.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(CCCO)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
34d51f83d7f890fb6f9dfb3778fa6ac322c2fffc538848b96a4366ff4d298284
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1cnc2ccc(-c3nc4ccccc4n3C3CCCCC3)cc2c1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[CH2;D2;+0:6]-[C:7]-[C:8]>>[C:8]-[C:7]-[CH2;D2;+0:6]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
90
[{"value": 90.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)CCCO", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 5-hydroxy-pentan-2-one (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (96 mg, 90% yield). MS: 430.23 (M+H+); HPLC Procedure A, retention time=6.84 min, ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)CCCO.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(CCCO)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-c59f3b6cd3754c419fc2134e1bdefb94
CC(=O)c1ccc(N2CCOCC2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCOCC5)cc4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1(CCOCC1)C1=CC=C(C=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)N2CCOCC2
CC(=O)[c:18]1[cH:19][cH:20][c:21]([N:22]2[CH2:23][CH2:24][O:25][CH2:26][CH2:27]2)[cH:28][cH:29]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:34]3[CH:35]3[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]3)[cH:33][c:32]2[cH:31][cH:30]1>>[O:1]=[C...
CC(=O)c1ccc(N2CCOCC2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCOCC5)cc4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCOCC5)cc4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
30
[{"value": 30.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC=C(C=C2)N2CCOCC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(4-morpholin-4-yl-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (37 mg, 30% yield). MS: 533.28 (M+H+); HPLC Procedure A, retention t...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1COCC[NH]1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(N2CCOCC2)cc1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(N5CCOCC5)cc4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f5c7f22729a94281b64769d245a1673a
CC(=O)c1ccccc1[N+](=O)[O-].O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2[nH]c(C3(c4ccccc4[N+](=O)[O-])C=Cc4ncccc4C3)nc2c1
[OH-].[K+].[N+](=O)([O-])C1=C(C=CC=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>[N+](=O)([O-])C1=C(C=CC=C1)C1(CC=2C=CC=NC2C=C1)C1=NC2=C(N1)C=CC(=C2)C(=O)O
C[C:10](=O)[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[N+:17](=[O:18])[O-:19].Oc1ccc(Br)cc1-[c:24]1[n:23][c:22]2[cH:21][cH:20]c(-[c:9]3[n:8](C4CCCCC4)[c:7]4[cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:31][c:30]4[n:29]3)[cH:28][c:27]2[cH:26][cH:25]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[nH:8][c:9]([C:10]3([c:11]4[cH:...
CC(=O)c1ccccc1[N+](=O)[O-].O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2[nH]c(C3(c4ccccc4[N+](=O)[O-])C=Cc4ncccc4C3)nc2c1
null
null
C(C)O
C-C Coupling
OtherReaction
c629e1407087f3538759c24058fac17e10e3a113a6a18de8478b6567833ad370
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
C1=CC(c2ccccc2)(c2nc3ccccc3[nH]2)Cc2cccnc21
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1]2:[#7;a:2]:[c:3]3:[cH;D2;+0:4]:[cH;D2;+0:5]:c(-[c;H0;D3;+0:6]4:[#7;a:7]:[c:8](:[c:9]):[c:10](:[c:11]):[n;H0;D3;+0:12]:4-C4-C-C-C-C-C-4):[cH;D2;+0:13]:[c:14]:3:[c:15]:[c:16]:2):c:1.C-[C;H0;D3;+0:17](=O)-[c:18](:[c:19]):[c:20]>>[c:19]:[c:18](-[C;H0;D4;+0:17]1(-[c;H0;D3;+0:6]2:[#7;a:7]:[c:...
10
[{"value": 10.0, "product": "[N+](=O)([O-])C1=C(C=CC=C1)C1(CC=2C=CC=NC2C=C1)C1=NC2=C(N1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(2-nitro-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (11 mg, 10% yield). MS: 493.21 (M+H+); HPLC Procedure A, retention time=12.72...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccc2ncccc2c1.C1CCCCC1.c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1.C1=Cc2ncccc2CC1
c1ccc2[nH]cnc2c1.c1ccccc1.C1=Cc2ncccc2CC1
HBr
C(C)O
null
null
CC(=O)c1ccccc1[N+](=O)[O-].O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2[nH]c(C3(c4ccccc4[N+](=O)[O-])C=Cc4ncccc4C3)nc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-51db0a9a57474c7c8a17668faefa5361
CC(=O)c1ccc(OCc2ccccc2)c(C)c1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1c(OCc2ccccc2)ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1O
[OH-].[K+].C(C1=CC=CC=C1)OC1=C(C(=C(C=C1)C(C)=O)O)C.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C(C1=CC=CC=C1)OC1=C(C(=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O)C
CC(=O)[c:14]1[cH:13][cH:12][c:3]([O:4][CH2:5][c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[c:2]([CH3:1])[c:43]1[OH:44].Oc1ccc(Br)cc1-[c:15]1[cH:16][cH:17][c:18]2[cH:19][c:20](-[c:21]3[n:22][c:23]4[cH:24][c:25]([C:26](=[O:27])[OH:28])[cH:29][cH:30][c:31]4[n:32]3[CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[cH:39][cH:40]...
CC(=O)c1ccc(OCc2ccccc2)c(C)c1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1c(OCc2ccccc2)ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1O
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(COc2ccc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cc2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9](-[O;D1;H1:10]):[c:11]>>[O;D1;H1:10]-[c:9](:[c:11]):[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:7]:[c:8]
10
[{"value": 10.0, "product": "C(C1=CC=CC=C1)OC1=C(C(=C(C=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(4-benzyloxy-2-hydroxy-3-methyl-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (73 mg, 10% yield). MS: 584.29 (M+H+); HPLC Procedure ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(OCc2ccccc2)c(C)c1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1c(OCc2ccccc2)ccc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-dd4bee7afe7d442a83a108fc3240271f
CC(=O)CCn1cccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(CCn4cccn4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1(N=CC=C1)CCC(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)CCN2N=CC=C2
CC(=O)[CH2:18][CH2:19][n:20]1[cH:21][cH:22][cH:23][n:24]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:29]3[CH:30]3[CH2:31][CH2:32][CH2:33][CH2:34][CH2:35]3)[cH:28][c:27]2[cH:26][cH:25]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8...
CC(=O)CCn1cccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(CCn4cccn4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
34d51f83d7f890fb6f9dfb3778fa6ac322c2fffc538848b96a4366ff4d298284
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(CCn4cccn4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[CH2;D2;+0:6]-[C:7]-[#7;a:8]>>[#7;a:8]-[C:7]-[CH2;D2;+0:6]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
50
[{"value": 50.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)CCN2N=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 4-pyrazol-1-yl-butan-2-one (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in Ethanol (506 μL, 0.64 mmol) to produce the title compound (14 mg, 50% yield). MS: 466.27 (M+H+); HPLC Procedure A, retention time=8.41 m...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1cn[nH]c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)CCn1cccn1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(CCn4cccn4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-9a816d7855224c32910f87aadd2f86cc
CCCN(CCC)CC(C)=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>CCCN(CCC)Cc1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].C(CC)N(CC(C)=O)CCC.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)CN(CCC)CCC
CC(=O)[CH2:8][N:4]([CH2:3][CH2:2][CH3:1])[CH2:5][CH2:6][CH3:7].Oc1ccc(Br)cc1-[c:9]1[cH:10][cH:11][c:12]2[cH:13][c:14](-[c:15]3[n:16][c:17]4[cH:18][c:19]([C:20](=[O:21])[OH:22])[cH:23][cH:24][c:25]4[n:26]3[CH:27]3[CH2:28][CH2:29][CH2:30][CH2:31][CH2:32]3)[cH:33][cH:34][c:35]2[n:36]1>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][C...
CCCN(CCC)CC(C)=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
CCCN(CCC)Cc1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
34d51f83d7f890fb6f9dfb3778fa6ac322c2fffc538848b96a4366ff4d298284
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1cnc2ccc(-c3nc4ccccc4n3C3CCCCC3)cc2c1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[CH2;D2;+0:6]-[#7:7](-[C:8])-[C:9]>>[C:8]-[#7:7](-[C:9])-[CH2;D2;+0:6]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
58
[{"value": 58.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)CN(CCC)CCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-dipropylamino-propan-2-one (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (70 mg, 58% yield). MS: 485.34 (M+H+); HPLC Procedure A, retention time=9.20...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CCCN(CCC)CC(C)=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>CCCN(CCC)Cc1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e80f58ddc4ce449f857fd2bc8077933f
CC(=O)C1CC(CC(=O)O)C1(C)C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>CC1(C)C(CC(=O)O)CC1c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].C(C)(=O)C1C(C(C1)CC(=O)O)(C)C.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C(=O)(O)CC1C(C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)(C)C
CC(=O)[CH:10]1[C:2]([CH3:1])([CH3:3])[CH:4]([CH2:5][C:6](=[O:7])[OH:8])[CH2:9]1.Oc1ccc(Br)cc1-[c:11]1[cH:12][cH:13][c:14]2[cH:15][c:16](-[c:17]3[n:18][c:19]4[cH:20][c:21]([C:22](=[O:23])[OH:24])[cH:25][cH:26][c:27]4[n:28]3[CH:29]3[CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]3)[cH:35][cH:36][c:37]2[n:38]1>>[CH3:1][C:2]1([CH3...
CC(=O)C1CC(CC(=O)O)C1(C)C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
CC1(C)C(CC(=O)O)CC1c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
b9a481f72a28ac7b25e12538b523667d411e0d7cc54c6ec4a4e21063acb325e9
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(C4CCC4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[CH;D3;+0:6]1-[C:7]-[C:8]-[C:9]-1(-[C;D1;H3:10])-[C;D1;H3:11]>>[C;D1;H3:10]-[C:9]1(-[C;D1;H3:11])-[C:8]-[C:7]-[CH;D3;+0:6]-1-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
16
[{"value": 16.0, "product": "C(=O)(O)CC1C(C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e 100 mg, 0.256 mmol) was reacted with (3-acetyl-2,2-dimethyl-cyclobutyl)-acetic acid (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (21 mg, 16% yield). MS: 512.31 (M+H+); HPLC Procedure A, re...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
C1CCC1.c1ccccc1.c1ccc2ncccc2c1
C1CCC1.c1ccc2ncccc2c1
C1CCC1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)C1CC(CC(=O)O)C1(C)C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>CC1(C)C(CC(=O)O)CC1c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-daddd1a164d64e08853823a139fc8a8c
COc1cc(Br)c2oc(C(C)=O)cc2c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>COc1cc(Br)c2oc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)cc2c1
[OH-].[K+].BrC1=CC(=CC=2C=C(OC21)C(C)=O)OC.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>BrC1=CC(=CC=2C=C(OC21)C2=NC1=CC=C(C=C1C=C2)C2=NC1=C(N2C2CCCCC2)C=CC(=C1)C(=O)O)OC
CC(=O)[c:9]1[o:8][c:7]2[c:5]([Br:6])[cH:4][c:3]([O:2][CH3:1])[cH:40][c:39]2[cH:38]1.Oc1ccc(Br)cc1-[c:10]1[cH:11][cH:12][c:13]2[cH:14][c:15](-[c:16]3[n:17][c:18]4[cH:19][c:20]([C:21](=[O:22])[OH:23])[cH:24][cH:25][c:26]4[n:27]3[CH:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]3)[cH:34][cH:35][c:36]2[n:37]1>>[CH3:1][O:2][c...
COc1cc(Br)c2oc(C(C)=O)cc2c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
COc1cc(Br)c2oc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)cc2c1
null
null
C(C)O
C-C Coupling
OtherReaction
6652b3d332750b9521edc9f82282db3de6903bc89164acd6b71bb882c727b5c6
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2oc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cc2c1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#8;a:7]:[c:8]:[c:9]:[c:10]:1>>[c:5]:[c:4]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[#8;a:7]:[c:8]:[c:9]:[c:10]:1):[#7;a:2]:[c:3]
17
[{"value": 17.0, "product": "BrC1=CC(=CC=2C=C(OC21)C2=NC1=CC=C(C=C1C=C2)C2=NC1=C(N2C2CCCCC2)C=CC(=C1)C(=O)O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(7-bromo-5-methoxy-benzofuran-2-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound, 17% yield). Conditions: See reaction.notes.procedure_deta...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2occc2c1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2occc2c1.c1ccc2ncccc2c1
c1ccc2occc2c1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
COc1cc(Br)c2oc(C(C)=O)cc2c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>COc1cc(Br)c2oc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)cc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-61f6d499bfb541ab9f870eff861e92d7
CC(=O)c1cn(-c2cccnc2Cl)c(=O)[nH]c1=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cn(-c5cccnc5Cl)c(=O)[nH]c4=O)ccc3c1)n2C1CCCCC1
[OH-].[K+].C(C)(=O)C=1C(NC(N(C1)C=1C(=NC=CC1)Cl)=O)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>ClC1=NC=CC=C1N1C(NC(C(=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)=O)=O
CC(=O)[c:18]1[cH:19][n:20](-[c:21]2[cH:22][cH:23][cH:24][n:25][c:26]2[Cl:27])[c:28](=[O:29])[nH:30][c:31]1=[O:32].Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:37]3[CH:38]3[CH2:39][CH2:40][CH2:41][CH2:42][CH2:43]3)[cH:36][c:35]2[cH:34][...
CC(=O)c1cn(-c2cccnc2Cl)c(=O)[nH]c1=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cn(-c5cccnc5Cl)c(=O)[nH]c4=O)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
d74850c02e111b96eecc8999c56e0c6b62ebedb77fd1307314c936eb4f7f10de
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
O=c1[nH]c(=O)n(-c2cccnc2)cc1-c1ccc2cc(-c3nc4ccccc4n3C3CCCCC3)ccc2n1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[#7;a:8](-[c:9]:[c:10]:[#7;a:11]):[c:12]:[#7;a:13]:[c:14]:1=[O;D1;H0:15]>>[#7;a:11]:[c:10]:[c:9]-[#7;a:8]1:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:14](=[O;D1;H0:15]):[#7;a:13]:[c:12]:1
31
[{"value": 31.0, "product": "ClC1=NC=CC=C1N1C(NC(C(=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 5-acetyl-1-(2-chloro-pyridin-3-yl)-1H-pyrimidine-2,4-dione (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound 45 mg, 31% yield). MS: 593.17 (M+H+); HPLC Pro...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cncnc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1cncnc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1cncnc1.c1ccncc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cn(-c2cccnc2Cl)c(=O)[nH]c1=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cn(-c5cccnc5Cl)c(=O)[nH]c4=O)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5ab4352dcc90475294b7e409811e18dd
CC(=O)c1c(C)oc2ccc(OCc3ccccc3)cc12.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1oc2ccc(OCc3ccccc3)cc2c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].C(C1=CC=CC=C1)OC=1C=CC2=C(C(=C(O2)C)C(C)=O)C1.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C(C1=CC=CC=C1)OC=1C=CC2=C(C(=C(O2)C)C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C1
CC(=O)c1[c:2]([CH3:1])[o:3][c:4]2[cH:5][cH:6][c:7]([O:8][CH2:9][c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[cH:16][c:17]12.Oc1ccc(Br)c[c:18]1-[c:19]1[cH:20][cH:21][c:22]2[cH:23][c:24](-[c:25]3[n:26][c:27]4[cH:28][c:29]([C:30](=[O:31])[OH:32])[cH:33][cH:34][c:35]4[n:36]3[CH:37]3[CH2:38][CH2:39][CH2:40][CH2:41][CH2:42]3)...
CC(=O)c1c(C)oc2ccc(OCc3ccccc3)cc12.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1oc2ccc(OCc3ccccc3)cc2c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
Miscellaneous
OtherReaction
f9053fce08ec002275338459f38665d646e016556869f4887fb8b643aa6892eb
5d663a6f3250645b78580d7f1b46d37e7983f21b5145184e88099bc5e394410f
c1ccc(COc2ccc3occ(-c4ccc5cc(-c6nc7ccccc7n6C6CCCCC6)ccc5n4)c3c2)cc1
Br-c1:c:c:c(-O):[c;H0;D3;+0:1](-[c:2](:[c:3]):[#7;a:4]:[c:5]):c:1.C-C(=O)-c1:[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9](:[c:10]):[#8;a:11]:[c;H0;D3;+0:12]:1-[C;D1;H3:13]>>[C;D1;H3:13]-[c;H0;D3;+0:12]1:[#8;a:11]:[c:9](:[c:10]):[c;H0;D3;+0:6](:[c:7]:[c:8]):[c;H0;D3;+0:1]:1-[c:2](:[c:3]):[#7;a:4]:[c:5]
49
[{"value": 49.0, "product": "C(C1=CC=CC=C1)OC=1C=CC2=C(C(=C(O2)C)C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(5-benzyloxy-2-methyl-benzofuran-3-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (75 mg, 49% yield). MS: 608.25 (M+H+); HPLC Procedure A...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2occc2c1.c1ccccc1
c1ccc2occc2c1
c1ccc2occc2c1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1c(C)oc2ccc(OCc3ccccc3)cc12.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1oc2ccc(OCc3ccccc3)cc2c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2755454004b444ccb71769aff67be485
CC(=O)c1ccc2c(c1)c1cc(Cl)ccc1n2C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cn1c2ccc(Cl)cc2c2cc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)ccc21
[OH-].[K+].ClC=1C=C2C=3C=C(C=CC3N(C2=CC1)C)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>ClC=1C=C2C=3C=C(C=CC3N(C2=CC1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)[c:12]1[cH:11][c:10]2[c:9]3[c:3]([n:2]([CH3:1])[c:43]2[cH:42][cH:41]1)[cH:4][cH:5][c:6]([Cl:7])[cH:8]3.Oc1ccc(Br)cc1-[c:13]1[cH:14][cH:15][c:16]2[cH:17][c:18](-[c:19]3[n:20][c:21]4[cH:22][c:23]([C:24](=[O:25])[OH:26])[cH:27][cH:28][c:29]4[n:30]3[CH:31]3[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36]3)[cH:37][cH:38][c:39...
CC(=O)c1ccc2c(c1)c1cc(Cl)ccc1n2C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cn1c2ccc(Cl)cc2c2cc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)ccc21
null
null
C(C)O
C-C Coupling
OtherReaction
725aef6ab8a30aa618ea5fc003b083d121adb959096e2e66fd47f40fc571d1f6
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5[nH]c6ccccc6c5c4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[c:9](:[#7;a:10]):[c:11]:[c:12]:1>>[#7;a:10]:[c:9]1:[c:8]:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:12]:[c:11]:1
12
[{"value": 12.0, "product": "ClC=1C=C2C=3C=C(C=CC3N(C2=CC1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(6-chloro-9-methyl-9H-carbazol-3-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (18 mg, 12% yield). MS: 585.21 (M+H+); HPLC Procedure A, ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2[nH]c3ccccc3c2c1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2[nH]c3ccccc3c2c1.c1ccc2ncccc2c1
c1ccc2[nH]c3ccccc3c2c1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc2c(c1)c1cc(Cl)ccc1n2C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cn1c2ccc(Cl)cc2c2cc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)ccc21
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5680b1d7af76442bab13c56201b4a54d
CC(=O)c1ccc2c(c1)CCO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCO5)ccc3c1)n2C1CCCCC1
[OH-].[K+].O1CCC2=C1C=CC(=C2)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=CC1=C(CCO1)C2
CC(=O)[c:18]1[cH:19][cH:20][c:21]2[c:22]([cH:23]1)[CH2:24][CH2:25][O:26]2.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:31]3[CH:32]3[CH2:33][CH2:34][CH2:35][CH2:36][CH2:37]3)[cH:30][c:29]2[cH:28][cH:27]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5]...
CC(=O)c1ccc2c(c1)CCO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCO5)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
2639e0145b47c7d851c30d3552031cd498be6de220ab3c05a72216e261182280
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCO5)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
28
[{"value": 28.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=CC1=C(CCO1)C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(2,3-dihydro-benzofuran-5-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in Ethanol (506 μL, 0.64 mmol) to produce the title compound (34 mg, 28% yield). MS: 490.19 (M+H+); HPLC Procedure A, retenti...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2c(c1)CCO2.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccc2c(c1)CCO2
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccc2c(c1)CCO2.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc2c(c1)CCO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc5c(c4)CCO5)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-978bee0078004e92a05619578dbbf7d6
CC(=O)c1cnn(-c2ccccc2)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cnn(-c5ccccc5)c4)ccc3c1)n2C1CCCCC1
[OH-].[K+].C1(=CC=CC=C1)N1N=CC(=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=NN(C2)C2=CC=CC=C2
CC(=O)[c:18]1[cH:19][n:20][n:21](-[c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)[cH:28]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:33]3[CH:34]3[CH2:35][CH2:36][CH2:37][CH2:38][CH2:39]3)[cH:32][c:31]2[cH:30][cH:29]1>>[O:1]=[C:2]([OH:3]...
CC(=O)c1cnn(-c2ccccc2)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cnn(-c5ccccc5)c4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
cc95b929fb804627d249ddb623f43c45e4fbdb1d580c792b60e158754e15fe1e
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-n2cc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cn2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[#7;a:8]:[#7;a:9](-[c:10]):[c:11]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[c:7]:[#7;a:8]:[#7;a:9](-[c:10]):[c:11]:1):[c:4]:[c:5]
51
[{"value": 51.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=NN(C2)C2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(1-phenyl-1H-pyrazol-4-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (69 mg, 51% yield). MS: 514.23 (M+H+); HPLC Procedure B, retention ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cn[nH]c1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1cn[nH]c1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1cn[nH]c1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cnn(-c2ccccc2)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cnn(-c5ccccc5)c4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d1c097dd2cd146e196d6b9a369c8f4a5
CC(=O)c1c(C)nn(-c2ccccc2)c1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1nn(-c2ccccc2)c(C)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].CC1=NN(C(=C1C(C)=O)C)C1=CC=CC=C1.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C(=NN(C2C)C2=CC=CC=C2)C
CC(=O)[c:13]1[c:2]([CH3:1])[n:3][n:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[c:11]1[CH3:12].Oc1ccc(Br)cc1-[c:14]1[cH:15][cH:16][c:17]2[cH:18][c:19](-[c:20]3[n:21][c:22]4[cH:23][c:24]([C:25](=[O:26])[OH:27])[cH:28][cH:29][c:30]4[n:31]3[CH:32]3[CH2:33][CH2:34][CH2:35][CH2:36][CH2:37]3)[cH:38][cH:39][c:40]2[n:41]1>>[CH3...
CC(=O)c1c(C)nn(-c2ccccc2)c1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1nn(-c2ccccc2)c(C)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
cc95b929fb804627d249ddb623f43c45e4fbdb1d580c792b60e158754e15fe1e
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-n2cc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cn2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7](-[C;D1;H3:8]):[#7;a:9](-[c:10]):[#7;a:11]:[c:12]:1-[C;D1;H3:13]>>[C;D1;H3:8]-[c:7]1:[#7;a:9](-[c:10]):[#7;a:11]:[c:12](-[C;D1;H3:13]):[c;H0;D3;+0:6]:1-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
37
[{"value": 37.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C(=NN(C2C)C2=CC=CC=C2)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (47 mg, 37% yield). Conditions: See reaction.notes.pro...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cn[nH]c1.c1ccccc1.c1ccc2ncccc2c1
c1cn[nH]c1.c1ccc2ncccc2c1
c1cn[nH]c1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1c(C)nn(-c2ccccc2)c1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1nn(-c2ccccc2)c(C)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-670b118e4ab741148e6a2752f946a6b4
CC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)no1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(-c5ccc(Cl)c(Cl)c5)no4)ccc3c1)n2C1CCCCC1
[OH-].[K+].ClC=1C=C(C=CC1Cl)C1=NOC(=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=NO2)C2=CC(=C(C=C2)Cl)Cl
CC(=O)[c:18]1[cH:19][c:20](-[c:21]2[cH:22][cH:23][c:24]([Cl:25])[c:26]([Cl:27])[cH:28]2)[n:29][o:30]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:35]3[CH:36]3[CH2:37][CH2:38][CH2:39][CH2:40][CH2:41]3)[cH:34][c:33]2[cH:32][cH:31]1>>[O:...
CC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)no1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(-c5ccc(Cl)c(Cl)c5)no4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
8b4b388453e9a0dc2e42ac24c2b3525cda3f10f82da404e7d5a83f0d31758d59
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2cc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)on2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#8;a:7]:[#7;a:8]:[c:9](-[c:10]):[c:11]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[#8;a:7]:[#7;a:8]:[c:9](-[c:10]):[c:11]:1):[c:4]:[c:5]
15
[{"value": 15.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=NO2)C2=CC(=C(C=C2)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-[3-(3,4-dichloro-phenyl)-isoxazol-5-yl]-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (21 mg, 15% yield). MS: 583.16 (M+H+); HPLC Procedure ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cnoc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1cnoc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1cnoc1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cc(-c2ccc(Cl)c(Cl)c2)no1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(-c5ccc(Cl)c(Cl)c5)no4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2a5ab8982e364511ad1f2a069c8b9e89
CC(=O)c1ccc(Oc2ccc(Cl)cc2)cc1Cl.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Oc5ccc(Cl)cc5)cc4Cl)ccc3c1)n2C1CCCCC1
[OH-].[K+].ClC1=C(C=CC(=C1)OC1=CC=C(C=C1)Cl)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>ClC1=C(C=CC(=C1)OC1=CC=C(C=C1)Cl)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)[c:18]1[cH:19][cH:20][c:21]([O:22][c:23]2[cH:24][cH:25][c:26]([Cl:27])[cH:28][cH:29]2)[cH:30][c:31]1[Cl:32].Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:37]3[CH:38]3[CH2:39][CH2:40][CH2:41][CH2:42][CH2:43]3)[cH:36][c:35]2[cH:34][...
CC(=O)c1ccc(Oc2ccc(Cl)cc2)cc1Cl.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Oc5ccc(Cl)cc5)cc4Cl)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(Oc2ccc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cc2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9](-[Cl;D1;H0:10]):[c:11]>>[Cl;D1;H0:10]-[c:9](:[c:11]):[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:7]:[c:8]
49
[{"value": 49.0, "product": "ClC1=C(C=CC(=C1)OC1=CC=C(C=C1)Cl)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (75 mg, 49% yield). MS: 608.17 (M+H+); HPLC Procedure B...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(Oc2ccc(Cl)cc2)cc1Cl.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Oc5ccc(Cl)cc5)cc4Cl)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-3ffb76ab3ccf49a4b063199ff614b595
CC(=O)c1cc(-c2ccc(Cl)cc2)oc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1oc(-c2ccc(Cl)cc2)cc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].ClC1=CC=C(C=C1)C1=CC(=C(O1)C)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>ClC1=CC=C(C=C1)C1=CC(=C(O1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)c1c[c:4](-[c:5]2[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]2)[o:3][c:2]1[CH3:1].Oc1ccc(Br)[cH:12][c:13]1-[c:14]1[cH:15][cH:16][c:17]2[cH:18][c:19](-[c:20]3[n:21][c:22]4[cH:23][c:24]([C:25](=[O:26])[OH:27])[cH:28][cH:29][c:30]4[n:31]3[CH:32]3[CH2:33][CH2:34][CH2:35][CH2:36][CH2:37]3)[cH:38][cH:39][c:40]2[n:41]1>>[CH3:...
CC(=O)c1cc(-c2ccc(Cl)cc2)oc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1oc(-c2ccc(Cl)cc2)cc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
Miscellaneous
OtherReaction
ff754d3c410dca834a2b7e1901e9aab845ad13b3e4145cab6f4a8111a1c7e45d
5d663a6f3250645b78580d7f1b46d37e7983f21b5145184e88099bc5e394410f
c1ccc(-c2cc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)co2)cc1
Br-c1:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):c(-O):c:c:1.C-C(=O)-c1:c:[c;H0;D3;+0:7](-[c:8](:[c:9]):[c:10]):[#8;a:11]:[c;H0;D3;+0:12]:1-[C;D1;H3:13]>>[C;D1;H3:13]-[c;H0;D3;+0:12]1:[#8;a:11]:[c;H0;D3;+0:7](-[c:8](:[c:9]):[c:10]):[cH;D2;+0:1]:[c;H0;D3;+0:2]:1-[c:3](:[c:4]):[#7;a:5]:[c:6]
59
[{"value": 59.0, "product": "ClC1=CC=C(C=C1)C1=CC(=C(O1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-[5-(4-chloro-phenyl)-2-methyl-furan-3-yl]-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (83 mg, 59% yield). MS: 562.21 (M+H+); HPLC Procedur...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccoc1.c1ccccc1
c1ccoc1
c1ccoc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cc(-c2ccc(Cl)cc2)oc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1oc(-c2ccc(Cl)cc2)cc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-7146818e4f0f44559a9ad70a49071ce0
CC(=O)c1c(-c2ccc(Cl)cc2)noc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1onc(-c2ccc(Cl)cc2)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].ClC1=CC=C(C=C1)C1=NOC(=C1C(C)=O)C.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>ClC1=CC=C(C=C1)C1=NOC(=C1C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)C
CC(=O)[c:13]1[c:2]([CH3:1])[o:3][n:4][c:5]1-[c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1.Oc1ccc(Br)cc1-[c:14]1[cH:15][cH:16][c:17]2[cH:18][c:19](-[c:20]3[n:21][c:22]4[cH:23][c:24]([C:25](=[O:26])[OH:27])[cH:28][cH:29][c:30]4[n:31]3[CH:32]3[CH2:33][CH2:34][CH2:35][CH2:36][CH2:37]3)[cH:38][cH:39][c:40]2[n:41]1>>[CH3:1...
CC(=O)c1c(-c2ccc(Cl)cc2)noc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1onc(-c2ccc(Cl)cc2)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
8b4b388453e9a0dc2e42ac24c2b3525cda3f10f82da404e7d5a83f0d31758d59
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2nocc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7](-[C;D1;H3:8]):[#8;a:9]:[#7;a:10]:[c:11]:1-[c:12]>>[C;D1;H3:8]-[c:7]1:[#8;a:9]:[#7;a:10]:[c:11](-[c:12]):[c;H0;D3;+0:6]:1-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
12
[{"value": 12.0, "product": "ClC1=CC=C(C=C1)C1=NOC(=C1C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-[3-(4-chloro-phenyl)-5-methyl-isoxazol-4-yl]-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (16 mg, 12% yield). Conditions: See reaction.note...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cnoc1.c1ccccc1.c1ccc2ncccc2c1
c1cnoc1.c1ccc2ncccc2c1
c1cnoc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1c(-c2ccc(Cl)cc2)noc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1onc(-c2ccc(Cl)cc2)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e6b83a0383664f9789a0c05c0c33737e
CC(=O)c1sc(-c2ccc(Cl)cc2)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1nc(-c2ccc(Cl)cc2)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].ClC1=CC=C(C=C1)C=1SC(=C(N1)C)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>ClC1=CC=C(C=C1)C=1SC(=C(N1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)[c:13]1[c:2]([CH3:1])[n:3][c:4](-[c:5]2[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]2)[s:12]1.Oc1ccc(Br)cc1-[c:14]1[cH:15][cH:16][c:17]2[cH:18][c:19](-[c:20]3[n:21][c:22]4[cH:23][c:24]([C:25](=[O:26])[OH:27])[cH:28][cH:29][c:30]4[n:31]3[CH:32]3[CH2:33][CH2:34][CH2:35][CH2:36][CH2:37]3)[cH:38][cH:39][c:40]2[n:41]1>>[CH3...
CC(=O)c1sc(-c2ccc(Cl)cc2)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1nc(-c2ccc(Cl)cc2)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
1d5c6f5b005ed70236ee338e17825f9573e4b8d5662849fd033a7cd4739092e7
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ncc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)s2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#16;a:7]:[c:8](-[c:9]):[#7;a:10]:[c:11]:1-[C;D1;H3:12]>>[C;D1;H3:12]-[c:11]1:[#7;a:10]:[c:8](-[c:9]):[#16;a:7]:[c;H0;D3;+0:6]:1-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
19
[{"value": 19.0, "product": "ClC1=CC=C(C=C1)C=1SC(=C(N1)C)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-[2-(4-chloro-phenyl)-4-methyl-thiazol-5-yl]-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (27 mg, 19% yield). MS: 580.19 (M+H+); HPLC Proced...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cscn1.c1ccccc1.c1ccc2ncccc2c1
c1cscn1.c1ccc2ncccc2c1
c1cscn1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1sc(-c2ccc(Cl)cc2)nc1C.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1nc(-c2ccc(Cl)cc2)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-863e45df0a9b457da6839281c85ec600
CC(=O)c1cc[nH]c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc[nH]c4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1C=C(C=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CNC=C2
CC(=O)[c:18]1[cH:19][cH:20][nH:21][cH:22]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:27]3[CH:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]3)[cH:26][c:25]2[cH:24][cH:23]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10...
CC(=O)c1cc[nH]c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc[nH]c4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
816e79feefe89602d7b2d905a921147b8cdf4b403c7ebb1cb51fc0135c0731fc
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4cc[nH]c4)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[#7;a:9]:[c:10]:1):[c:4]:[c:5]
8
[{"value": 8.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CNC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(1H-pyrrol-3-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (10 mg, 8% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cc[nH]c1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1cc[nH]c1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1cc[nH]c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cc[nH]c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc[nH]c4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2b8e0398f2774bbfb78cf923a33e6319
CC(=O)c1ccc[nH]1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc[nH]4)ccc3c1)n2C1CCCCC1
[OH-].[K+].N1C(=CC=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2NC=CC2
CC(=O)[c:18]1[cH:19][cH:20][cH:21][nH:22]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:27]3[CH:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]3)[cH:26][c:25]2[cH:24][cH:23]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[n:10...
CC(=O)c1ccc[nH]1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc[nH]4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
816e79feefe89602d7b2d905a921147b8cdf4b403c7ebb1cb51fc0135c0731fc
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1c[nH]c(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)c1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#7;a:7]:[c:8]:[c:9]:[c:10]:1>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[#7;a:7]:[c:8]:[c:9]:[c:10]:1):[c:4]:[c:5]
9
[{"value": 9.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2NC=CC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(1H-pyrrol-2-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (11 mg, 9% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1cc[nH]c1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1cc[nH]c1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1cc[nH]c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc[nH]1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc[nH]4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ae0e10489fd54c2eb3daf138afefde83
CC(=O)c1ccc2c(c1)NC(=O)CO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C1COc2ccc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)cc2N1
[OH-].[K+].C(C)(=O)C=1C=CC2=C(NC(CO2)=O)C1.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=CC1=C(NC(CO1)=O)C2
CC(=O)c1ccc2c(c1)[NH:39][C:2](=[O:1])[CH2:3][O:4]2.O[c:5]1[cH:6][cH:7][c:8](Br)[cH:37][c:38]1-[c:9]1[cH:10][cH:11][c:12]2[cH:13][c:14](-[c:15]3[n:16][c:17]4[cH:18][c:19]([C:20](=[O:21])[OH:22])[cH:23][cH:24][c:25]4[n:26]3[CH:27]3[CH2:28][CH2:29][CH2:30][CH2:31][CH2:32]3)[cH:33][cH:34][c:35]2[n:36]1>>[O:1]=[C:2]1[CH2:3]...
CC(=O)c1ccc2c(c1)NC(=O)CO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C1COc2ccc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)cc2N1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
63267276b3feef59673eef8934ab934a3b106549020267a8b09ac43f43b98b96
fd9d01a3b72789dff10bb12c1092cbb5e4930ebb8892040ac09c3bdfbbddb82b
O=C1COc2ccc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)cc2N1
Br-[c;H0;D3;+0:1]1:[c:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:4](:[#7;a:5]:[c:6]):[c:7]:[c:8]):[c;H0;D3;+0:9](-O):[c:10]:[c:11]:1.C-C(=O)-c1:c:c:c2:c(:c:1)-[NH;D2;+0:12]-[C:13](=[O;D1;H0:14])-[C:15]-[O;H0;D2;+0:16]-2>>[O;D1;H0:14]=[C:13]1-[C:15]-[O;H0;D2;+0:16]-[c;H0;D3;+0:9]2:[c:10]:[c:11]:[c;H0;D3;+0:1](-[c;H0;D3;+0:4](:[#7;a...
8
[{"value": 8.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C=2C=CC1=C(NC(CO1)=O)C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 6-acetyl-4H-benzo[1,4]oxazin-3-one (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (11 mg, 8% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Ether.Secondary amide.Aromatic alcohol
Ether.Secondary amide
c1ccc2c(c1)NCCO2.c1ccccc1.c1ccc2ncccc2c1
c1ccc2c(c1)NCCO2.c1ccc2ncccc2c1
c1ccc2c(c1)NCCO2.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc2c(c1)NC(=O)CO2.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C1COc2ccc(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)cc2N1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d7aa1f1d49e348c096c6385ebccb7dcd
CC(=O)c1sc(-c2ccccc2)cc1N.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Nc1cc(-c2ccccc2)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].NC1=C(SC(=C1)C1=CC=CC=C1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>NC1=C(SC(=C1)C1=CC=CC=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)[c:12]1[c:2]([NH2:1])[cH:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[s:11]1.Oc1ccc(Br)cc1-[c:13]1[cH:14][cH:15][c:16]2[cH:17][c:18](-[c:19]3[n:20][c:21]4[cH:22][c:23]([C:24](=[O:25])[OH:26])[cH:27][cH:28][c:29]4[n:30]3[CH:31]3[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36]3)[cH:37][cH:38][c:39]2[n:40]1>>[NH2:1][c:2...
CC(=O)c1sc(-c2ccccc2)cc1N.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Nc1cc(-c2ccccc2)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
720f87d7df89fae5bee313ea8aae90dd7d141265b6e283e34e49e8dc216a5da5
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ccc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)s2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[#16;a:7]:[c:8]:[c:9]:[c:10]:1-[N;D1;H2:11]>>[N;D1;H2:11]-[c:10]1:[c:9]:[c:8]:[#16;a:7]:[c;H0;D3;+0:6]:1-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
14
[{"value": 14.0, "product": "NC1=C(SC(=C1)C1=CC=CC=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(3-amino-5-phenyl-thiophen-2-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (19 mg, 14% yield). MS: 545.24 (M+H+); HPLC Procedure B, rete...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccsc1.c1ccccc1.c1ccc2ncccc2c1
c1ccsc1.c1ccc2ncccc2c1
c1ccsc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1sc(-c2ccccc2)cc1N.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Nc1cc(-c2ccccc2)sc1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-22597246d1ff47819738715bf4c1607b
COc1ccc2occ(C(C)=O)c2c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>COc1ccc2occ(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)c2c1
[OH-].[K+].COC=1C=CC2=C(C(=CO2)C(C)=O)C1.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=COC1=C2C=C(C=C1)OC
CC(=O)[c:9]1[cH:8][o:7][c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:39][c:38]21.Oc1ccc(Br)cc1-[c:10]1[cH:11][cH:12][c:13]2[cH:14][c:15](-[c:16]3[n:17][c:18]4[cH:19][c:20]([C:21](=[O:22])[OH:23])[cH:24][cH:25][c:26]4[n:27]3[CH:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]3)[cH:34][cH:35][c:36]2[n:37]1>>[CH3:1][O:2][c:3]1[cH:...
COc1ccc2occ(C(C)=O)c2c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
COc1ccc2occ(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)c2c1
null
null
C(C)O
C-C Coupling
OtherReaction
6652b3d332750b9521edc9f82282db3de6903bc89164acd6b71bb882c727b5c6
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc2c(c1)nc(-c1ccc3nc(-c4coc5ccccc45)ccc3c1)n2C1CCCCC1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6]1:[c:7]:[#8;a:8]:[c:9](:[c:10]):[c:11]:1:[c:12]>>[c:5]:[c:4]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[c:7]:[#8;a:8]:[c:9](:[c:10]):[c:11]:1:[c:12]):[#7;a:2]:[c:3]
8
[{"value": 8.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=COC1=C2C=C(C=C1)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(5-methoxy-benzofuran-3-yl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (10 mg, 8% yield). MS: 518.24 (M+H+); HPLC Procedure B, retention ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccc2occc2c1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2occc2c1.c1ccc2ncccc2c1
c1ccc2occc2c1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
COc1ccc2occ(C(C)=O)c2c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>COc1ccc2occ(-c3ccc4cc(-c5nc6cc(C(=O)O)ccc6n5C5CCCCC5)ccc4n3)c2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-38b97266a3fd4f0495c8c608fcb0193f
CCOC(=O)c1ccc(Cl)c([N+](=O)[O-])c1.N[C@@H]1CCCC[C@H]1O>>CCOC(=O)c1ccc(N[C@@H]2CCCC[C@H]2O)c([N+](=O)[O-])c1
CO.C(C)OC(C1=CC(=C(C=C1)Cl)[N+](=O)[O-])=O.C(C)N(CC)CC.Cl.N[C@H]1[C@@H](CCCC1)O>>C(C)OC(C1=CC(=C(C=C1)N[C@H]1[C@@H](CCCC1)O)[N+](=O)[O-])=O
Cl[c:9]1[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:22][c:18]1[N+:19](=[O:20])[O-:21].[NH2:10][C@@H:11]1[CH2:12][CH2:13][CH2:14][CH2:15][C@H:16]1[OH:17]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([NH:10][C@@H:11]2[CH2:12][CH2:13][CH2:14][CH2:15][C@H:16]2[OH:17])[c:18]([N+:19](=[O:20])[O-:21])[c...
CCOC(=O)c1ccc(Cl)c([N+](=O)[O-])c1.N[C@@H]1CCCC[C@H]1O
CCOC(=O)c1ccc(N[C@@H]2CCCC[C@H]2O)c([N+](=O)[O-])c1
null
null
O.C(C)#N
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(NC2CCCCC2)cc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:9]-[C:8](-[C:7])-[C:10]):[c:2]:[c:3]
null
[]
null
null
null
null
Compound 9 (689 mg, 3 mmol) was suspended in acetonitrile (5 mL) and then triethylamine was added (1.3 mL, 9 mmol). trans-2-aminocyclohexanol hydrochloride (682 mg, 4.5 mmol) was then added and the reaction refluxed for 12 hours, 2 mL methanol was then added and the reaction further refluxed for another 24 hours. Water...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.C1CCCCC1
HCl
O.C(C)#N
null
null
CCOC(=O)c1ccc(Cl)c([N+](=O)[O-])c1.N[C@@H]1CCCC[C@H]1O>O.C(C)#N>CCOC(=O)c1ccc(N[C@@H]2CCCC[C@H]2O)c([N+](=O)[O-])c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-339bd8a048074752ac0329b6027b2e43
CCN(C(C)C)C(C)C.CCOC(=O)c1ccc(N[C@@H]2CCCC[C@H]2O)c(N)c1.CN(C)C(On1nnc2ccccc21)=[N+](C)C.CN(C)C=O>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2[C@@H]1CCCC[C@H]1O
C(C)OC(C1=CC(=C(C=C1)N[C@H]1[C@@H](CCCC1)O)N)=O.CN(C)C(=[N+](C)C)ON1C2=C(C=CC=C2)N=N1.[B-](F)(F)(F)F.CCN(C(C)C)C(C)C.CN(C)C=O>>O[C@H]1[C@@H](CCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1N=CC(=NC1=CC2)C2=CC=CC=C2
CC(C)N(C(C)C)[CH2:23][CH3:22].[O:1]=[C:2]([O:3][CH2:19][CH3:20])[c:4]1[cH:5][cH:6][c:7]([NH:28][C@@H:29]2[CH2:30][CH2:31][CH2:32][CH2:33][C@H:34]2[OH:35])[c:8]([NH2:10])[cH:9]1.C[N+](C)=[C:17](O[n:25]1n[n:16][c:15]2[cH:14][cH:13][cH:12][cH:27][c:26]21)N([CH3:21])[CH3:24].CN([CH:11]=O)[CH3:18]>>[O:1]=[C:2]([OH:3])[c:4]1...
CCN(C(C)C)C(C)C.CCOC(=O)c1ccc(N[C@@H]2CCCC[C@H]2O)c(N)c1.CN(C)C(On1nnc2ccccc21)=[N+](C)C.CN(C)C=O
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2[C@@H]1CCCC[C@H]1O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
d5224d3e39b5ea5e36ea115d5bbd42cdeb988ae706ebd58627c54fe64a28c596
477f657131ca4589b743a8a28b6796d63976298e2013be05ff0fa3589cec1ea5
c1ccc(-c2cnc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
C-C(-C)-N(-[CH2;D2;+0:1]-[CH3;D1;+0:2])-C(-C)-C.C-N(-[CH3;D1;+0:3])-[CH;D2;+0:4]=O.C-[N+](-C)=[C;H0;D3;+0:5](-O-[n;H0;D3;+0:6]1:n:[n;H0;D2;+0:7]:[c:8]2:[c:9]:[c:10]:[cH;D2;+0:11]:[c:12]:[c:13]:2:1)-N(-[CH3;D1;+0:14])-[CH3;D1;+0:15].[C:16]-[C:17](-[NH;D2;+0:18]-[c:19](:[c:20]):[c:21](-[NH2;D1;+0:22]):[c:23]:[c:24]-[C:25...
null
[]
null
null
20
HOUR
Compound 36A Y=Phenyl, (200 mg, 0.8 mmol) was activated in 8 mL DMF with TBTU (282 mg, 0.88 mmol) and DIEA (0.285 mL, 1.6 mmol) for 30 minutes at room temperature. This solution was then added to Compound 578b (230 mg, 0.83 mmol) and stirred at ambient temperature for 20 hours. The reaction was concentrated to a residu...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Ester.Tertiary amide.Primary amine.Secondary amine.Tertiary amine
Carboxylic acid
c1ccccc1.c1ccc2[nH]nnc2c1
c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2nccnc2c1.c1ccccc1.C1CCCCC1
HO-
null
null
20
CCN(C(C)C)C(C)C.CCOC(=O)c1ccc(N[C@@H]2CCCC[C@H]2O)c(N)c1.CN(C)C(On1nnc2ccccc21)=[N+](C)C.CN(C)C=O>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccccc4)cnc3c1)n2[C@@H]1CCCC[C@H]1O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-9c192dfdc6f54692b3f47d7b75654ab5
CC(=O)c1cc(Cl)c(N)c(Cl)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Nc1c(Cl)cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1Cl
[OH-].[K+].NC1=C(C=C(C=C1Cl)C(C)=O)Cl.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>NC1=C(C=C(C=C1Cl)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)Cl
CC(=O)c1c[c:3]([Cl:4])[c:2]([NH2:1])[c:36]([Cl:37])[cH:35]1.Oc1ccc(Br)[cH:5][c:6]1-[c:7]1[cH:8][cH:9][c:10]2[cH:11][c:12](-[c:13]3[n:14][c:15]4[cH:16][c:17]([C:18](=[O:19])[OH:20])[cH:21][cH:22][c:23]4[n:24]3[CH:25]3[CH2:26][CH2:27][CH2:28][CH2:29][CH2:30]3)[cH:31][cH:32][c:33]2[n:34]1>>[NH2:1][c:2]1[c:3]([Cl:4])[cH:5]...
CC(=O)c1cc(Cl)c(N)c(Cl)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Nc1c(Cl)cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1Cl
null
null
C(C)O
Miscellaneous
OtherReaction
6a309f5dd455d49d540fdde9d256250a05afc877ae1689368497529377020a76
a5f50b0757a934668f3fe20d1b59a66d0719baeb97c5ffdb5dc3bf9ea135698a
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):c(-O):c:c:1.C-C(=O)-c1:[cH;D2;+0:7]:[c:8](-[Cl;D1;H0:9]):[c:10](-[N;D1;H2:11]):[c;H0;D3;+0:12](-[Cl;D1;H0:13]):c:1>>[Cl;D1;H0:9]-[c:8]1:[cH;D2;+0:7]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):[cH;D2;+0:1]:[c;H0;D3;+0:12](-[Cl;D1;H0:13]):[c:10]:1-[N;D1;...
25
[{"value": 25.0, "product": "NC1=C(C=C(C=C1Cl)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(4-amino-3,5-dichloro-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (31 mg, 25% yield). Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Ketone.Aromatic alcohol
Aromatic halide
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cc(Cl)c(N)c(Cl)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Nc1c(Cl)cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-820f8c9b27db46b497cd74a95f2eba26
CC(=O)c1cccc(Br)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(Br)c4)ccc3c1)n2C1CCCCC1
[OH-].[K+].BrC=1C=C(C=CC1)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>BrC=1C=C(C=CC1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
CC(=O)[c:18]1[cH:19][cH:20][cH:21][c:22]([Br:23])[cH:24]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:29]3[CH:30]3[CH2:31][CH2:32][CH2:33][CH2:34][CH2:35]3)[cH:28][c:27]2[cH:26][cH:25]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8...
CC(=O)c1cccc(Br)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(Br)c4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
12
[{"value": 12.0, "product": "BrC=1C=C(C=CC1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(3-bromo-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (15 mg, 12% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cccc(Br)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(Br)c4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-215d7167ecab45e682b9ec273e8cbd0a
COc1cc(OC)cc(C(C)=O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>COc1cc(OC)cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
[OH-].[K+].COC=1C=C(C=C(C1)OC)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC(=C2)OC)OC
CC(=O)c1c[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH3:7])[cH:8]1.Oc1ccc(Br)[cH:38][c:9]1-[c:10]1[cH:11][cH:12][c:13]2[cH:14][c:15](-[c:16]3[n:17][c:18]4[cH:19][c:20]([C:21](=[O:22])[OH:23])[cH:24][cH:25][c:26]4[n:27]3[CH:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]3)[cH:34][cH:35][c:36]2[n:37]1>>[CH3:1][O:2][c:3]1[cH:4][c:...
COc1cc(OC)cc(C(C)=O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
COc1cc(OC)cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
C(C)O
Miscellaneous
OtherReaction
d2d0a69fbf4e3bd9ee03a6f0fc5f5013ffe449e61086d15d67619284d201f6ab
713eb02386e817c2cede100961151654d67d2b2ae5918ce33e70a9716d144b1b
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):c(-O):c:c:1.C-C(=O)-c1:[cH;D2;+0:7]:[c:8](-[#8:9]):[c:10]:[c;H0;D3;+0:11](-[#8:12]-[C;D1;H3:13]):c:1>>[#8:9]-[c:8]1:[c:10]:[c;H0;D3;+0:11](-[#8:12]-[C;D1;H3:13]):[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):[cH;D2;+0:7]:1
35
[{"value": 35.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC(=C2)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(3,5-dimethoxy-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (44 mg, 35% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Ether.Aromatic alcohol
Ether
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
COc1cc(OC)cc(C(C)=O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>COc1cc(OC)cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-15024a8393a3454f9146b84f9c03c218
CC(=O)c1ccc(Cl)c(Cl)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Cl)c(Cl)c4)ccc3c1)n2C1CCCCC1
[OH-].[K+].ClC=1C=C(C=CC1Cl)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=C(C=C2)Cl)Cl
CC(=O)[c:18]1[cH:19][cH:20][c:21]([Cl:22])[c:23]([Cl:24])[cH:25]1.Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:30]3[CH:31]3[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36]3)[cH:29][c:28]2[cH:27][cH:26]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c...
CC(=O)c1ccc(Cl)c(Cl)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Cl)c(Cl)c4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
10
[{"value": 10.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=C(C=C2)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(3,4-dichloro-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (12 mg, 10% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(Cl)c(Cl)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(Cl)c(Cl)c4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-4dacedd5040d4e699fc668470c3a21b4
CC(=O)c1ccc(O)cc1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(O)cc4O)ccc3c1)n2C1CCCCC1
[OH-].[K+].OC1=C(C=CC(=C1)O)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=C(C=C2)O)O
CC(=O)[c:18]1[cH:19][cH:20][c:21]([OH:22])[cH:23][c:24]1[OH:25].Oc1ccc(Br)cc1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:30]3[CH:31]3[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36]3)[cH:29][c:28]2[cH:27][cH:26]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7...
CC(=O)c1ccc(O)cc1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(O)cc4O)ccc3c1)n2C1CCCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9](-[O;D1;H1:10]):[c:11]>>[O;D1;H1:10]-[c:9](:[c:11]):[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:7]:[c:8]
8
[{"value": 8.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=C(C=C2)O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(2,4-dihydroxy-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (9.5 mg, 8% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1ccc(O)cc1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4ccc(O)cc4O)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-44615d37ce7345c4b5763a10d4aceb2f
CC(=O)c1cc(O)cc(O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(O)cc(O)c4)ccc3c1)n2C1CCCCC1
[OH-].[K+].OC=1C=C(C=C(C1)O)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC(=C2)O)O
CC(=O)c1c[c:20]([OH:21])[cH:22][c:23]([OH:24])[cH:25]1.Oc1ccc(Br)[cH:19][c:18]1-[c:17]1[n:16][c:15]2[cH:14][cH:13][c:12](-[c:11]3[n:10][c:8]4[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]4)[n:30]3[CH:31]3[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36]3)[cH:29][c:28]2[cH:27][cH:26]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c...
CC(=O)c1cc(O)cc(O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(O)cc(O)c4)ccc3c1)n2C1CCCCC1
null
null
C(C)O
Miscellaneous
OtherReaction
13d17d3ba2aab432715ff8895dcc7f34b9986951e91088a4bd02b1fd1fc5dcfe
826d5ed588669e06fdf43ab0d54c49b68fe5f7db98488b3f4628cb32a365c71c
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):c(-O):c:c:1.C-C(=O)-c1:[cH;D2;+0:7]:[c:8](-[O;D1;H1:9]):[c:10]:[c;H0;D3;+0:11](-[O;D1;H1:12]):c:1>>[O;D1;H1:12]-[c;H0;D3;+0:11]1:[c:10]:[c:8](-[O;D1;H1:9]):[cH;D2;+0:7]:[c;H0;D3;+0:2](-[c:3](:[c:4]):[#7;a:5]:[c:6]):[cH;D2;+0:1]:1
18
[{"value": 18.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC(=C2)O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(3,5-dihydroxy-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (22 mg, 18% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol.Aromatic alcohol
Aromatic alcohol
c1ccccc1.c1ccccc1
c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cc(O)cc(O)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(O)cc(O)c4)ccc3c1)n2C1CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-fb25cede22a5439ebe3be42255bb5afb
CC(=O)c1cc(C)cc([N+](=O)[O-])c1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>Cc1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(O)c([N+](=O)[O-])c1
[OH-].[K+].OC1=C(C=C(C=C1[N+](=O)[O-])C)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C(=CC(=C2)C)[N+](=O)[O-])O
CC(=O)c1[cH:3][c:2]([CH3:1])[cH:39][c:35]([N+:36](=[O:37])[O-:38])[c:33]1[OH:34].Oc1ccc(Br)c[c:4]1-[c:5]1[cH:6][cH:7][c:8]2[cH:9][c:10](-[c:11]3[n:12][c:13]4[cH:14][c:15]([C:16](=[O:17])[OH:18])[cH:19][cH:20][c:21]4[n:22]3[CH:23]3[CH2:24][CH2:25][CH2:26][CH2:27][CH2:28]3)[cH:29][cH:30][c:31]2[n:32]1>>[CH3:1][c:2]1[cH:3...
CC(=O)c1cc(C)cc([N+](=O)[O-])c1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
Cc1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(O)c([N+](=O)[O-])c1
null
null
C(C)O
Miscellaneous
OtherReaction
13d17d3ba2aab432715ff8895dcc7f34b9986951e91088a4bd02b1fd1fc5dcfe
826d5ed588669e06fdf43ab0d54c49b68fe5f7db98488b3f4628cb32a365c71c
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):[c;H0;D3;+0:1](-[c:2](:[c:3]):[#7;a:4]:[c:5]):c:1.C-C(=O)-c1:[cH;D2;+0:6]:[c:7](-[C;D1;H3:8]):[c:9]:[c:10](-[#7;+:11]):[c;H0;D3;+0:12]:1-[O;D1;H1:13]>>[#7;+:11]-[c:10]1:[c:9]:[c:7](-[C;D1;H3:8]):[cH;D2;+0:6]:[c;H0;D3;+0:1](-[c:2](:[c:3]):[#7;a:4]:[c:5]):[c;H0;D3;+0:12]:1-[O;D1;H1:13]
31
[{"value": 31.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C(=CC(=C2)C)[N+](=O)[O-])O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(2-hydroxy-5-methyl-3-nitro-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (40 mg, 31% yield). Conditions: See reaction.notes.procedu...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol.Aromatic alcohol
Aromatic alcohol
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
CC(=O)c1cc(C)cc([N+](=O)[O-])c1O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>Cc1cc(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(O)c([N+](=O)[O-])c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e22d17874ae84b2abaf5e64916ebecb4
COc1cccc(O)c1C(C)=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>COc1cccc(O)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
[OH-].[K+].OC1=C(C(=CC=C1)OC)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC=C2OC)O
CC(=O)[c:9]1[c:3]([O:2][CH3:1])[cH:4][cH:5][cH:6][c:7]1[OH:8].Oc1ccc(Br)cc1-[c:10]1[cH:11][cH:12][c:13]2[cH:14][c:15](-[c:16]3[n:17][c:18]4[cH:19][c:20]([C:21](=[O:22])[OH:23])[cH:24][cH:25][c:26]4[n:27]3[CH:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33]3)[cH:34][cH:35][c:36]2[n:37]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6]...
COc1cccc(O)c1C(C)=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
COc1cccc(O)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
null
null
C(C)O
C-C Coupling
OtherReaction
b0005d85f44f8fd2e5347e57b6d8612a6bcb7f2f6961e5711380421da946a83b
f34555a5c6bd5f7f28302c4b82e779fa0b15fb240c98b7acf87941b8ccbcbc8b
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):c(-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):c:1.C-C(=O)-[c;H0;D3;+0:6](:[c:7](-[#8:8]):[c:9]):[c:10](-[O;D1;H1:11]):[c:12]>>[#8:8]-[c:7](:[c:9]):[c;H0;D3;+0:6](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]):[c:10](-[O;D1;H1:11]):[c:12]
69
[{"value": 69.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC=C2OC)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with 1-(2-hydroxy-6-methoxy-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (75 mg, 69% yield). Conditions: See reaction.notes.procedure_deta...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
COc1cccc(O)c1C(C)=O.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>COc1cccc(O)c1-c1ccc2cc(-c3nc4cc(C(=O)O)ccc4n3C3CCCCC3)ccc2n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-bac94a5e2eea431691431af4792ad2f9
COc1cc(O)c(C(C)=O)c(OC)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>>COc1cc(O)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(OC)c1
[OH-].[K+].OC1=C(C(=CC(=C1)OC)OC)C(C)=O.BrC=1C=CC(=C(C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=C(C=C2OC)OC)O
CC(=O)c1[c:5]([OH:6])[cH:4][c:3]([O:2][CH3:1])[cH:39][c:36]1[O:37][CH3:38].Oc1ccc(Br)c[c:7]1-[c:8]1[cH:9][cH:10][c:11]2[cH:12][c:13](-[c:14]3[n:15][c:16]4[cH:17][c:18]([C:19](=[O:20])[OH:21])[cH:22][cH:23][c:24]4[n:25]3[CH:26]3[CH2:27][CH2:28][CH2:29][CH2:30][CH2:31]3)[cH:32][cH:33][c:34]2[n:35]1>>[CH3:1][O:2][c:3]1[cH...
COc1cc(O)c(C(C)=O)c(OC)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1
COc1cc(O)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(OC)c1
null
null
C(C)O
Miscellaneous
OtherReaction
f299fb44097350fa320651d0983e8ebd82ff762908ce3d8478bae97b0f2da916
0afcb6b3902647a00fcff3b908d1976f5faf335b657dea68fe2faec85b1ae7cc
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O):[c;H0;D3;+0:1](-[c:2](:[c:3]):[#7;a:4]:[c:5]):c:1.C-C(=O)-c1:[c;H0;D3;+0:6](-[#8:7]-[C;D1;H3:8]):[c:9]:[c:10]:[c:11]:[c;H0;D3;+0:12]:1-[O;D1;H1:13]>>[C;D1;H3:8]-[#8:7]-[c;H0;D3;+0:6]1:[c:9]:[c:10]:[c:11]:[c;H0;D3;+0:12](-[O;D1;H1:13]):[c;H0;D3;+0:1]:1-[c:2](:[c:3]):[#7;a:4]:[c:5]
65
[{"value": 65.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=C(C=C2OC)OC)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure and workup for Compound 354, Compound 354e (100 mg, 0.256 mmol) was reacted with -(2-hydroxy-4,6-dimethoxy-phenyl)-ethanone (0.256 mmol) in ethanol (2 mL) using 10% w/v KOH in ethanol (506 μL, 0.64 mmol) to produce the title compound (85 mg, 65% yield). Conditions: See reaction.notes.procedure_d...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Ether.Aromatic alcohol.Aromatic alcohol
Ether.Aromatic alcohol
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr
C(C)O
null
null
COc1cc(O)c(C(C)=O)c(OC)c1.O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(Br)ccc4O)ccc3c1)n2C1CCCCC1>C(C)O>COc1cc(O)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c(OC)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8b66773aa0bf407c865d37bd2c2576a1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(Br)c4)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)cc1>>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(-c5ccc(Cl)cc5)c4)ccc3c1)n2C1CCCCC1
BrC=1C=C(C=CC1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O.ClC1=CC=C(C=C1)B(O)O.C([O-])(O)=O.[Na+]>>ClC1=CC=C(C=C1)C1=CC(=CC=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O
Br[c:22]1[cH:21][cH:20][cH:19][c:18](-[c:17]2[n:16][c:15]3[cH:14][cH:13][c:12](-[c:11]4[n:10][c:8]5[c:7]([cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:9]5)[n:35]4[CH:36]4[CH2:37][CH2:38][CH2:39][CH2:40][CH2:41]4)[cH:34][c:33]3[cH:32][cH:31]2)[cH:30]1.OB(O)[c:23]1[cH:24][cH:25][c:26]([Cl:27])[cH:28][cH:29]1>>[O:1]=[C:2]([OH...
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(Br)c4)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)cc1
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(-c5ccc(Cl)cc5)c4)ccc3c1)n2C1CCCCC1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
O.C1(=CC=CC=C1)C.CO
C-C Coupling
Suzuki coupling with boronic acids
d79a78c79f0c392f0911481acf5c300cc98205269acdb93c24fb610a61c4c868
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2cccc(-c3ccc4cc(-c5nc6ccccc6n5C5CCCCC5)ccc4n3)c2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].O-B(-O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:5]:[c:4]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:2]:[c:3]
42.2
[{"value": 42.0, "product": "ClC1=CC=C(C=C1)C1=CC(=CC=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 42.2, "product": "ClC1=CC=C(C=C1)C1=CC(=CC=C1)C1=NC2=CC=C(C=C2C=C1)C1=NC2=C(N1C1CCCCC1)C=CC(=C2)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is...
90
CELSIUS
16
HOUR
In dried vial with a Teflon lined screw cap, a solution of Compound 482 (156 mg, 0.31 mmol), 4-chlorophenylboronic acid (73 mg, 0.465 mmol), and Palladium Tetrakis (37 mg, 0.031 mmol) in toluene (9 mL), methanol (2 mL), and saturated sodium bicarbonate in water (900 μL) was degassed, flushed with argon, and sealed. The...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccc2nc[nH]c2c1.c1ccc2ncccc2c1.c1ccccc1.c1ccccc1.C1CCCCC1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.C1(=CC=CC=C1)C.CO
90
16
O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(Br)c4)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)cc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.C1(=CC=CC=C1)C.CO>O=C(O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cccc(-c5ccc(Cl)c...
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-147c10f1b8ef4deabab477614815e219
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1>>COc1ccc(-c2ccc(C(N)=O)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
[OH-].[K+].COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.C([O-])(O)=O.[Na+].O>>C(N)(=O)C1=CC=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=C1
Br[c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:45][c:16]1-[c:17]1[cH:18][cH:19][c:20]2[cH:21][c:22](-[c:23]3[n:12][c:25]4[cH:26][c:27]([C:28](=[O:29])[O:30][CH3:7])[cH:31][cH:32][c:33]4[n:34]3[CH:35]3[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]3)[cH:41][cH:42][c:43]2[n:44]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1
COc1ccc(-c2ccc(C(N)=O)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
C1(=CC=CC=C1)C.CO
Aromatic Heterocycle Formation
OtherReaction
3f7edad97709d4bd5d44566bb7179d840b74c5299eb1373f73c2ff159ea5009c
faa5f70adcaec17880da4b509384bb36ded18d7fda4ad0119b5c36e3e1980dbc
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].[C:8]-[#7;a:9]1:[c:10](:[c:11]):[c;H0;D3;+0:12](:[c:13]:[c:14]-[C:15](=[O;D1;H0:16])-[O;H0;D2;+0:17]-[CH3;D1;+0:18]):[n;H0;D2;+0:19]:[c;H0;D3;+0:20]:1-[c:21](:[c:22]):[c:23]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:18]1:[c:24]:[c:25]:[c:26](-...
null
[]
90
CELSIUS
16
HOUR
In a flame dried vial with a Teflon lined screw cap, a solution of Compound 365b (100 mg, 0.175 mmol), 4-amidophenylboronic acid (31 mg, 0.2625 mmol), and Palladium Tetrakis (20 mg, 0.0175 mmol) in toluene (6.5 mL), methanol (1.6 mL), and saturated sodium bicarbonate in water (800 ul) was degassed, flushed with argon, ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester
Carboxylic acid.Primary amide
c1ccccc1.c1ccc2nc[nH]c2c1
c1ccccc1.c1ccccc1.c1ccc2nc[nH]c2c1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
Br-
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C.CO
90
16
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C.CO>COc1ccc(-c2ccc(C(N)=O)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCC...
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f7ff849513b44655869091b850785528
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(F)c(Cl)c1>>COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
[OH-].[K+].COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.FC1=C(C=C(C=C1)B(O)O)Cl.C([O-])(O)=O.[Na+]>>ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F
C[O:29][C:27]([c:26]1[cH:25][c:24]2[n:23][c:22](-[c:21]3[cH:20][c:19]4[cH:18][cH:17][c:16](-[c:15]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:44]5)[n:43][c:42]4[cH:41][cH:40]3)[n:33]([CH:34]3[CH2:35][CH2:36][CH2:37][CH2:38][CH2:39]3)[c:32]2[cH:31][cH:30]1)=[O:28].OB(O)[c:7]1[cH:8][cH:9][c:10]([F:11])[c:12]([Cl:13])[cH...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(F)c(Cl)c1
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
O.C1(=CC=CC=C1)C.CO
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
7
[{"value": 7.0, "product": "ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 6.6, "product": "ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F", "details": "CALCULATEDPERCENTYIELD",...
90
CELSIUS
16
HOUR
In dried vial with a Teflon lined screw cap, a solution of Compound 365b (100 mg, 0.175 mmol), 4-fluoro-3-chlorophenylboronic acid (61 mg, 0.2625 mmol), and Palladium Tetrakis (20 mg, 0.0175 mmol) in toluene (6.5 mL), methanol (1.6 mL), and saturated sodium bicarbonate in water (800 ul) was degassed, flushed with argon...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.C1(=CC=CC=C1)C.CO
90
16
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(F)c(Cl)c1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.C1(=CC=CC=C1)C.CO>COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5...
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a90125c0ee144210b3381874be655e30
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.O=[N+]([O-])c1ccc(B(O)O)cc1>>COc1ccc(-c2ccc([N+](=O)[O-])cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.[N+](=O)([O-])C1=CC=C(C=C1)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)[N+](=O)[O-])OC
Fc1ccc(-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:45][c:16]2-[c:17]2[cH:18][cH:19][c:20]3[cH:21][c:22](-[c:23]4[n:24][c:25]5[cH:26][c:27]([C:28](=[O:29])[OH:30])[cH:31][cH:32][c:33]5[n:34]4[CH:35]4[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]4)[cH:41][cH:42][c:43]3[n:44]2)cc1Cl.OB(O)[c:7]1[cH:8][cH:9][c:10]([N+:11](=[O:12])[...
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.O=[N+]([O-])c1ccc(B(O)O)cc1
COc1ccc(-c2ccc([N+](=O)[O-])cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
32c6d9e04f426e2be7276d51def4545d9be5d98cffa0b1b76a196565e6617362
b431b00445693c7ae33759145152dfe407ee85c3562148bfc9cb7e8a06213bb6
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Cl-c1:c:c(-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7]):c:c:c:1-F.O-B(-O)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]):[c:2]:[c:3]
14.3
[{"value": 14.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)[N+](=O)[O-])OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 14.3, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)[N+](=O)[O-])OC", "details": "...
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 4-nitrophenylboronic acid (62 mg, 0.2625 mmol) to produce the title compound (15 mg, 14% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HF.B
null
null
null
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.O=[N+]([O-])c1ccc(B(O)O)cc1>>COc1ccc(-c2ccc([N+](=O)[O-])cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-1825744e8a6c407a8e7b798d3a65e5fe
CN(C)c1ccc(B(O)O)cc1.COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1>>COc1ccc(-c2ccc(N(C)C)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.CN(C1=CC=C(C=C1)B(O)O)C>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)N(C)C)OC
OB(O)[c:7]1[cH:8][cH:9][c:10]([N:11]([CH3:12])[CH3:13])[cH:14][cH:15]1.C[O:30][C:28]([c:27]1[cH:26][c:25]2[n:24][c:23](-[c:22]3[cH:21][c:20]4[cH:19][cH:18][c:17](-[c:16]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:45]5)[n:44][c:43]4[cH:42][cH:41]3)[n:34]([CH:35]3[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]3)[c:33]2[cH:32][...
CN(C)c1ccc(B(O)O)cc1.COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1
COc1ccc(-c2ccc(N(C)C)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
26
[{"value": 26.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)N(C)C)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 4-dimethylaminophenylboronic acid (44 mg, 0.2625 mmol) to produce the title compound (27 mg, 26% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
CN(C)c1ccc(B(O)O)cc1.COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1>>COc1ccc(-c2ccc(N(C)C)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e5cbc77d5254481ca690a470d7a938e0
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.O=[N+]([O-])c1cccc(B(O)O)c1>>COc1ccc(-c2cccc([N+](=O)[O-])c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.[N+](=O)([O-])C=1C=C(C=CC1)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC(=CC=C2)[N+](=O)[O-])OC
Fc1ccc(-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:45][c:16]2-[c:17]2[cH:18][cH:19][c:20]3[cH:21][c:22](-[c:23]4[n:24][c:25]5[cH:26][c:27]([C:28](=[O:29])[OH:30])[cH:31][cH:32][c:33]5[n:34]4[CH:35]4[CH2:36][CH2:37][CH2:38][CH2:39][CH2:40]4)[cH:41][cH:42][c:43]3[n:44]2)cc1Cl.OB(O)[c:7]1[cH:8][cH:9][cH:10][c:11]([N+:12](=[...
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.O=[N+]([O-])c1cccc(B(O)O)c1
COc1ccc(-c2cccc([N+](=O)[O-])c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
32c6d9e04f426e2be7276d51def4545d9be5d98cffa0b1b76a196565e6617362
b431b00445693c7ae33759145152dfe407ee85c3562148bfc9cb7e8a06213bb6
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Cl-c1:c:c(-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7]):c:c:c:1-F.O-B(-O)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]):[c:2]:[c:3]
7
[{"value": 7.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC(=CC=C2)[N+](=O)[O-])OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 3-nitrophenylboronic acid (44 mg, 0.2625 mmol) to produce the title compound (7 mg, 7% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HF.B
null
null
null
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.O=[N+]([O-])c1cccc(B(O)O)c1>>COc1ccc(-c2cccc([N+](=O)[O-])c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ae30255c8e3b42fa867c623833b9b378
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(C(F)(F)F)cc1>>COc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.FC(C1=CC=C(C=C1)B(O)O)(F)F>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)C(F)(F)F)OC
C[O:31][C:29]([c:28]1[cH:27][c:26]2[n:25][c:24](-[c:23]3[cH:22][c:21]4[cH:20][cH:19][c:18](-[c:17]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:46]5)[n:45][c:44]4[cH:43][cH:42]3)[n:35]([CH:36]3[CH2:37][CH2:38][CH2:39][CH2:40][CH2:41]3)[c:34]2[cH:33][cH:32]1)=[O:30].OB(O)[c:7]1[cH:8][cH:9][c:10]([C:11]([F:12])([F:13])[F:...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(C(F)(F)F)cc1
COc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
12
[{"value": 12.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)C(F)(F)F)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 4-trifluoromethylphenylboronic acid (50 mg, 0.2625 mmol) to produce the title compound (14 mg, 12% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(C(F)(F)F)cc1>>COc1ccc(-c2ccc(C(F)(F)F)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d51ab9a3caea428780a298ad2cc96de6
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.OB(O)c1ccco1>>COc1ccc(-c2ccco2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.O1C(=CC=C1)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC(=C2)OC)C=2OC=CC2
Fc1ccc(-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:41][c:12]2-[c:13]2[cH:14][cH:15][c:16]3[cH:17][c:18](-[c:19]4[n:20][c:21]5[cH:22][c:23]([C:24](=[O:25])[OH:26])[cH:27][cH:28][c:29]5[n:30]4[CH:31]4[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36]4)[cH:37][cH:38][c:39]3[n:40]2)cc1Cl.OB(O)[c:7]1[cH:8][cH:9][cH:10][o:11]1>>[CH3:1][...
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.OB(O)c1ccco1
COc1ccc(-c2ccco2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
0e0253b66decd7d74d1a1f97a0c8fe92b35f6d02bfe7317498d3b5459234f4f4
b431b00445693c7ae33759145152dfe407ee85c3562148bfc9cb7e8a06213bb6
c1coc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)c1
Cl-c1:c:c(-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7]):c:c:c:1-F.O-B(-O)-[c;H0;D3;+0:8]1:[#8;a:9]:[c:10]:[c:11]:[c:12]:1>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:8]1:[#8;a:9]:[c:10]:[c:11]:[c:12]:1):[c:2]:[c:3]
5
[{"value": 5.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC(=C2)OC)C=2OC=CC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 2-furanboronic acid (30 mg, 0.2625 mmol) to produce the title compound (5 mg, 5% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1.c1ccoc1
c1ccccc1.c1ccoc1
c1ccccc1.c1ccoc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HF.B
null
null
null
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.OB(O)c1ccco1>>COc1ccc(-c2ccco2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2b1343f3b8d943b2a98e378b1d72deef
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(B(O)O)cc1>>COc1ccc(-c2ccc(OC)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.COC1=CC=C(C=C1)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)OC)OC
C[O:28][C:26]([c:25]1[cH:24][c:23]2[n:22][c:21](-[c:20]3[cH:19][c:18]4[cH:17][cH:16][c:15](-[c:14]5[c:7](Br)[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13]5)[n:42][c:41]4[cH:40][cH:39]3)[n:32]([CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[c:31]2[cH:30][cH:29]1)=[O:27].OB(O)[c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:44][cH...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(B(O)O)cc1
COc1ccc(-c2ccc(OC)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
15
[{"value": 15.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 4-methoxyphenylboronic acid (40 mg, 0.2625 mmol) to produce the title compound (15 mg, 15% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(B(O)O)cc1>>COc1ccc(-c2ccc(OC)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2723f4bee31647beb62e1df971549d8e
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1>>COc1ccc(-c2cccc(C(=O)O)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1>>C(=O)(O)C=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1
COc1ccc(Br)c(-c2ccc3cc(-c4nc5c(n4C4CCCCC4)[cH:9][cH:10][c:11]([C:12](=[O:13])[O:14]C)[cH:15]5)ccc3n2)c1.Fc1c[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:45][c:16]2-[c:17]2[cH:18][cH:19][c:20]3[cH:21][c:22](-[c:23]4[n:24][c:25]5[cH:26][c:27]([C:28](=[O:29])[OH:30])[cH:31][cH:32][c:33]5[n:34]4[CH:35]4[CH2:36][CH...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
COc1ccc(-c2cccc(C(=O)O)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
Miscellaneous
OtherReaction
7b44631509d7b2c3d68f050efb14ee329debb5a841ec6fdcf1402f4d0a7dce09
f35c9d72ec193f2e381c4d42cb243062a5caa8c3ad0413d2a6200b6b5dd7eec3
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-O-C):c:c:1-c1:c:c:c2:c:c(-c3:n:c4:[cH;D2;+0:1]:[c:2](-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-C):[c:6]:[cH;D2;+0:7]:c:4:n:3-C3-C-C-C-C-C-3):c:c:c:2:n:1.Cl-c1:c:[c;H0;D3;+0:8](-[c:9](:[c:10]):[c:11]):[cH;D2;+0:12]:c:c:1-F>>[O;D1;H0:4]=[C:3](-[OH;D1;+0:5])-[c:2]1:[c:6]:[cH;D2;+0:7]:[cH;D2;+0:12]:[c;H0;D3;+0:8](-[...
23
[{"value": 23.0, "product": "C(=O)(O)C=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with ethyl 3-boronic acid benzoate (51 mg, 0.2625 mmol) to produce the title compound (26 mg, 23% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Ester.Ether
Carboxylic acid
c1ccccc1.c1ccc2ncccc2c1.C1CCCCC1.c1ccc2nc[nH]c2c1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HF.Br-
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1>>COc1ccc(-c2cccc(C(=O)O)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-cf988f9c625644d7a04b04f9cdfba449
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1>>COc1ccc(-c2ccc(O)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)O)OC
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc([O:11]C)ccc4Br)ccc3c1)n2C1CCCCC1.F[c:10]1[cH:9][cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:43][c:14]2-[c:15]2[cH:16][cH:17][c:18]3[cH:19][c:20](-[c:21]4[n:22][c:23]5[cH:24][c:25]([C:26](=[O:27])[OH:28])[cH:29][cH:30][c:31]5[n:32]4[CH:33]4[CH2:34][CH2:35][CH2:36][CH2:37][CH...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
COc1ccc(-c2ccc(O)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
f30117c431a2592965204599aa4c028643efc650df21031e46a71a6eff6364c2
96757a10f94e51057570c37db8198b2450e6ebfdc9332f472ca09eb028b6aa59
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-c1:c:c:c(-[O;H0;D2;+0:1]-C):c:c:1-c1:c:c:c2:c:c(-c3:n:c4:c:c(-C(=O)-O-C):c:c:c:4:n:3-C3-C-C-C-C-C-3):c:c:c:2:n:1.Cl-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[c:5]:[c:6]:[c;H0;D3;+0:7]:1-F>>[OH;D1;+0:1]-[c;H0;D3;+0:7]1:[c:6]:[c:5]:[c:4]:[c:3]:[cH;D2;+0:2]:1
8
[{"value": 8.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 4-phenolboronic acid (36 mg, 0.2625 mmol) to produce the title compound (10 mg, 8% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Ester.Ether
Aromatic alcohol
c1ccc2[nH]cnc2c1.c1ccc2ncccc2c1.c1ccccc1.C1CCCCC1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HF.Br-
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1>>COc1ccc(-c2ccc(O)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6a6328dcf0164138af0f9e9fe1e9d067
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)c(Cl)c1>>COc1ccc(-c2ccc(Cl)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.ClC=1C=C(C=CC1Cl)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC(=C(C=C2)Cl)Cl)OC
C[O:29][C:27]([c:26]1[cH:25][c:24]2[n:23][c:22](-[c:21]3[cH:20][c:19]4[cH:18][cH:17][c:16](-[c:15]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:44]5)[n:43][c:42]4[cH:41][cH:40]3)[n:33]([CH:34]3[CH2:35][CH2:36][CH2:37][CH2:38][CH2:39]3)[c:32]2[cH:31][cH:30]1)=[O:28].OB(O)[c:7]1[cH:8][cH:9][c:10]([Cl:11])[c:12]([Cl:13])[c...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)c(Cl)c1
COc1ccc(-c2ccc(Cl)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
4
[{"value": 4.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC(=C(C=C2)Cl)Cl)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 3,4-dichlorophenylboronic acid (50 mg, 0.2625 mmol) to produce the title compound (5 mg, 4% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1ccc(Cl)c(Cl)c1>>COc1ccc(-c2ccc(Cl)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ac7b8470b97e4ed69ebcda8897d794e2
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1cccc(Cl)c1>>COc1ccc(-c2cccc(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.ClC=1C=C(C=CC1)B(O)O>>ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1
C[O:28][C:26]([c:25]1[cH:24][c:23]2[n:22][c:21](-[c:20]3[cH:19][c:18]4[cH:17][cH:16][c:15](-[c:14]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:43]5)[n:42][c:41]4[cH:40][cH:39]3)[n:32]([CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[c:31]2[cH:30][cH:29]1)=[O:27].OB(O)[c:7]1[cH:8][cH:9][cH:10][c:11]([Cl:12])[cH:13]1>>...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1cccc(Cl)c1
COc1ccc(-c2cccc(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
17
[{"value": 17.0, "product": "ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 3-chlorophenylboronic acid (41 mg, 0.2625 mmol) to produce the title compound (20 mg, 17% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.OB(O)c1cccc(Cl)c1>>COc1ccc(-c2cccc(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2cee28962f824527a7804f82b1d870e9
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.Cc1ccc(B(O)O)cc1>>COc1ccc(-c2ccc(C)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.B(C=1C=CC(=CC1)C)(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)C)OC
C[O:28][C:26]([c:25]1[cH:24][c:23]2[n:22][c:21](-[c:20]3[cH:19][c:18]4[cH:17][cH:16][c:15](-[c:14]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:43]5)[n:42][c:41]4[cH:40][cH:39]3)[n:32]([CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[c:31]2[cH:30][cH:29]1)=[O:27].OB(O)[c:7]1[cH:8][cH:9][c:10]([CH3:11])[cH:12][cH:13]1>...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.Cc1ccc(B(O)O)cc1
COc1ccc(-c2ccc(C)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
12
[{"value": 12.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)C)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with p-tolylboronic acid (36 mg, 0.2625 mmol) to produce the title compound (12 mg, 12% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.Cc1ccc(B(O)O)cc1>>COc1ccc(-c2ccc(C)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-7fa46e71435c4562962a37bc739e725a
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.Cc1cccc(B(O)O)c1>>COc1ccc(-c2cccc(C)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.C1(=CC(=CC=C1)B(O)O)C>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC(=CC=C2)C)OC
C[O:28][C:26]([c:25]1[cH:24][c:23]2[n:22][c:21](-[c:20]3[cH:19][c:18]4[cH:17][cH:16][c:15](-[c:14]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:43]5)[n:42][c:41]4[cH:40][cH:39]3)[n:32]([CH:33]3[CH2:34][CH2:35][CH2:36][CH2:37][CH2:38]3)[c:31]2[cH:30][cH:29]1)=[O:27].OB(O)[c:7]1[cH:8][cH:9][cH:10][c:11]([CH3:12])[cH:13]1>...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.Cc1cccc(B(O)O)c1
COc1ccc(-c2cccc(C)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
27
[{"value": 27.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC(=CC=C2)C)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with m-tolylboronic acid (36 mg, 0.2625 mmol) to produce the title compound (27 mg, 27% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.Cc1cccc(B(O)O)c1>>COc1ccc(-c2cccc(C)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8350caabb43a419a964d0c03037cf9b0
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.NCc1ccc(B(O)O)cc1>>COc1ccc(-c2ccc(CN)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.NCC1=CC=C(C=C1)B(O)O>>NCC1=CC=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=C1
Fc1ccc(-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:44][c:15]2-[c:16]2[cH:17][cH:18][c:19]3[cH:20][c:21](-[c:22]4[n:23][c:24]5[cH:25][c:26]([C:27](=[O:28])[OH:29])[cH:30][cH:31][c:32]5[n:33]4[CH:34]4[CH2:35][CH2:36][CH2:37][CH2:38][CH2:39]4)[cH:40][cH:41][c:42]3[n:43]2)cc1Cl.OB(O)[c:7]1[cH:8][cH:9][c:10]([CH2:11][NH2:12])...
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.NCc1ccc(B(O)O)cc1
COc1ccc(-c2ccc(CN)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
32c6d9e04f426e2be7276d51def4545d9be5d98cffa0b1b76a196565e6617362
b431b00445693c7ae33759145152dfe407ee85c3562148bfc9cb7e8a06213bb6
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Cl-c1:c:c(-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7]):c:c:c:1-F.O-B(-O)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]):[c:2]:[c:3]
46
[{"value": 46.0, "product": "NCC1=CC=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 4-aminomethylphenylboronic acid (49 mg, 0.2625 mmol) to produce the title compound (48 mg, 46% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HF.B
null
null
null
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.NCc1ccc(B(O)O)cc1>>COc1ccc(-c2ccc(CN)cc2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-addf8a4775ce43b588fd76124ba7beb4
CCOc1ccc(B(O)O)cc1.COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1>>CCOc1ccc(-c2ccc(OC)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.C(C)OC1=CC=C(C=C1)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)OCC)OC
OB(O)[c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[cH:45][cH:44]1.C[O:29][C:27]([c:26]1[cH:25][c:24]2[n:23][c:22](-[c:21]3[cH:20][c:19]4[cH:18][cH:17][c:16](-[c:15]5[c:8](Br)[cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]5)[n:43][c:42]4[cH:41][cH:40]3)[n:33]([CH:34]3[CH2:35][CH2:36][CH2:37][CH2:38][CH2:39]3)[c:32]2[cH:31][cH...
CCOc1ccc(B(O)O)cc1.COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1
CCOc1ccc(-c2ccc(OC)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
null
null
null
C-C Coupling
OtherReaction
04157bef51d5543c035526858b11d2af2b78e75d38cd85edf56b617e6aebc946
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:2]:[c:3].[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:11]
16
[{"value": 16.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=CC(=CC=C2C2=CC=C(C=C2)OCC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 4-ethoxyphenylboronic acid (44 mg, 0.2625 mmol) to produce the title compound (17 mg, 16% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
CCOc1ccc(B(O)O)cc1.COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1>>CCOc1ccc(-c2ccc(OC)cc2-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-69cce5cf2758402fa1fa9ae09f52f727
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.OB(O)c1cccs1>>COc1ccc(-c2cccs2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.S1C(=CC=C1)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC(=C2)OC)C=2SC=CC2
Fc1ccc(-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:41][c:12]2-[c:13]2[cH:14][cH:15][c:16]3[cH:17][c:18](-[c:19]4[n:20][c:21]5[cH:22][c:23]([C:24](=[O:25])[OH:26])[cH:27][cH:28][c:29]5[n:30]4[CH:31]4[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36]4)[cH:37][cH:38][c:39]3[n:40]2)cc1Cl.OB(O)[c:7]1[cH:8][cH:9][cH:10][s:11]1>>[CH3:1][...
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.OB(O)c1cccs1
COc1ccc(-c2cccs2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
43c61b81957e5d103120d30884b9edaab0a7a61161f36389d85bcd0a6cb56cf7
b431b00445693c7ae33759145152dfe407ee85c3562148bfc9cb7e8a06213bb6
c1csc(-c2ccccc2-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)c1
Cl-c1:c:c(-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7]):c:c:c:1-F.O-B(-O)-[c;H0;D3;+0:8]1:[#16;a:9]:[c:10]:[c:11]:[c:12]:1>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:8]1:[#16;a:9]:[c:10]:[c:11]:[c:12]:1):[c:2]:[c:3]
27
[{"value": 27.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC(=C2)OC)C=2SC=CC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 2-thiopheneboronic acid (34 mg, 0.2625 mmol) to produce the title compound (26 mg, 27% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1.c1ccsc1
c1ccccc1.c1ccsc1
c1ccccc1.c1ccsc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HF.B
null
null
null
COc1ccc(-c2ccc(F)c(Cl)c2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1.OB(O)c1cccs1>>COc1ccc(-c2cccs2)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-39fad7e43001435c9baa4847ee94145c
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ncc(B(O)O)c(OC)n1>>COc1ccc(-c2cnc(OC)nc2OC)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
ClC=1C=C(C2=CC=C(C=C2C2=NC3=CC=C(C=C3C=C2)C2=NC3=C(N2C2CCCCC2)C=CC(=C3)C(=O)O)OC)C=CC1F.COC(=O)C1=CC2=C(N(C(=N2)C=2C=C3C=CC(=NC3=CC2)C2=C(C=CC(=C2)OC)Br)C2CCCCC2)C=C1.COC1=NC=C(C(=N1)OC)B(O)O>>C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC(=C2)OC)C=2C(=NC(=NC2)OC)OC
C[O:31][C:29]([c:28]1[cH:27][c:26]2[n:25][c:24](-[c:23]3[cH:22][c:21]4[cH:20][cH:19][c:18](-[c:17]5[c:6](Br)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:46]5)[n:45][c:44]4[cH:43][cH:42]3)[n:35]([CH:36]3[CH2:37][CH2:38][CH2:39][CH2:40][CH2:41]3)[c:34]2[cH:33][cH:32]1)=[O:30].OB(O)[c:7]1[cH:8][n:9][c:10]([O:11][CH3:12])[n:13][c:14...
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ncc(B(O)O)c(OC)n1
COc1ccc(-c2cnc(OC)nc2OC)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1
null
null
null
C-C Coupling
OtherReaction
e4889be329320133de905898c8e49409b08273a08be014191d1c84d85b74afc8
5af41468c321f267448297a8abdded64f3cc5543e523be88c60c8574c327b358
c1ccc(-c2ccc3cc(-c4nc5ccccc5n4C4CCCCC4)ccc3n2)c(-c2cncnc2)c1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[c:5]:[#7;a:6]):[c:7].C-[O;H0;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11].O-B(-O)-[c;H0;D3;+0:12]1:[c:13]:[#7;a:14]:[c:15]:[#7;a:16]:[c:17]:1-[#8:18]>>[#7;a:6]:[c:5]-[c:4](:[c:7]):[c;H0;D3;+0:1](-[c;H0;D3;+0:12]1:[c:13]:[#7;a:14]:[c:15]:[#7;a:16]:[c:17]:1-[#8:18]):[c:2]:[c:3].[O;D1;H0:10...
7
[{"value": 7.0, "product": "C1(CCCCC1)N1C(=NC2=C1C=CC(=C2)C(=O)O)C=2C=C1C=CC(=NC1=CC2)C2=C(C=CC(=C2)OC)C=2C(=NC(=NC2)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the full procedure and workup for Compound 366, Compound 365b (100 mg, 0.175 mmol) was reacted with 2,4-dimethoxypyrimidine-5-boronic acid (34 mg, 0.2625 mmol) to produce the title compound (8 mg, 7% yield). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Carboxylic acid
c1ccccc1.c1cncnc1
c1ccccc1.c1cncnc1
c1ccccc1.c1cncnc1.c1ccc2ncccc2c1.c1ccc2nc[nH]c2c1.C1CCCCC1
HBr.B
null
null
null
COC(=O)c1ccc2c(c1)nc(-c1ccc3nc(-c4cc(OC)ccc4Br)ccc3c1)n2C1CCCCC1.COc1ncc(B(O)O)c(OC)n1>>COc1ccc(-c2cnc(OC)nc2OC)c(-c2ccc3cc(-c4nc5cc(C(=O)O)ccc5n4C4CCCCC4)ccc3n2)c1