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-e61a7047de7f4e138a9e806ad1918640
CCOC(=O)c1cn2c(C)nnc2c(Cl)c1Nc1ccc(Br)cc1Cl>>Cc1nnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12
[OH-].[Na+].C(C)OC(=O)C=1C(=C(C=2N(C1)C(=NN2)C)Cl)NC2=C(C=C(C=C2)Br)Cl.C1CCOC1.Cl>>BrC1=CC(=C(C=C1)NC1=C(C=2N(C=C1C(=O)O)C(=NN2)C)Cl)Cl
CC[O:21][C:19]([c:18]1[c:8]([NH:9][c:10]2[cH:11][cH:12][c:13]([Br:14])[cH:15][c:16]2[Cl:17])[c:6]([Cl:7])[c:5]2[n:4][n:3][c:2]([CH3:1])[n:23]2[cH:22]1)=[O:20]>>[CH3:1][c:2]1[n:3][n:4][c:5]2[c:6]([Cl:7])[c:8]([NH:9][c:10]3[cH:11][cH:12][c:13]([Br:14])[cH:15][c:16]3[Cl:17])[c:18]([C:19](=[O:20])[OH:21])[cH:22][n:23]12
CCOC(=O)c1cn2c(C)nnc2c(Cl)c1Nc1ccc(Br)cc1Cl
Cc1nnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12
null
null
O.[Cl-].[Na+].O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc(Nc2ccn3cnnc3c2)cc1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
null
[]
null
null
16
HOUR
Sodium hydroxide (715 μL of a 1 M solution) was added to a solution of 7-(4-bromo-2-chlorophenylamino)-8-chloro-3-methyl-[1,2,4]triazolo[4,3-a]pyridine-6-carboxylic acid ethyl ester (51a) (79 mg, 179 mmol) in 3:1 THF:water (4.5 mL). After 16 hours, the reaction mixture was poured into a separatory funnel, diluted with ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccn2cnnc2c1.c1ccccc1
Other
O.[Cl-].[Na+].O
null
16
CCOC(=O)c1cn2c(C)nnc2c(Cl)c1Nc1ccc(Br)cc1Cl>O.[Cl-].[Na+].O>Cc1nnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-b8f7129a11664ebdbf36985da2e2fa2e
CCOC(=O)c1cnc(NN)c(Cl)c1Nc1ccc(Br)cc1Cl.O=C(Cl)Cc1ccccc1>>COC(=O)c1cn2c(Cc3ccccc3)nnc2c(Cl)c1Nc1ccc(Br)cc1Cl
C1(=CC=CC=C1)CC(=O)Cl.C1(=CC=CC=C1)CC(=O)Cl.C(C)OC(C1=CN=C(C(=C1NC1=C(C=C(C=C1)Br)Cl)Cl)NN)=O.C(C)N(CC)CC.O=P(Cl)(Cl)Cl>>COC(=O)C=1C(=C(C=2N(C1)C(=NN2)CC2=CC=CC=C2)Cl)NC2=C(C=C(C=C2)Br)Cl
C[CH2:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][c:18]([NH:17][NH2:16])[c:19]([Cl:20])[c:21]1[NH:22][c:23]1[cH:24][cH:25][c:26]([Br:27])[cH:28][c:29]1[Cl:30].O=[C:8](Cl)[CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7]2[c:8]([CH2:9][c:10]3[cH:11][cH:12][cH:13][cH:14][cH:15]3)[n:1...
CCOC(=O)c1cnc(NN)c(Cl)c1Nc1ccc(Br)cc1Cl.O=C(Cl)Cc1ccccc1
COC(=O)c1cn2c(Cc3ccccc3)nnc2c(Cl)c1Nc1ccc(Br)cc1Cl
null
null
C(CCl)Cl.C(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
06ab74c60ce8ef6b39033ec039502ec63eb866bdf2ff8953b25e03708212c9f6
1cacea87a450fad028c3559617d303476857f6994646fcc16cab567f4ef1481c
c1ccc(Cc2nnc3cc(Nc4ccccc4)ccn23)cc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6]:[n;H0;D2;+0:7]:[c:8](-[NH;D2;+0:9]-[NH2;D1;+0:10]):[c:11].Cl-[C;H0;D3;+0:12](=O)-[C:13]-[c:14]>>[CH3;D1;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6]:[n;H0;D3;+0:7]1:[c:8](:[c:11]):[n;H0;D2;+0:9]:[n;H0;D2;+0:10]:[c;H0;D3;+0:12]:1-[C:13]-[c:14]
33.4
[{"value": 30.0, "product": "COC(=O)C=1C(=C(C=2N(C1)C(=NN2)CC2=CC=CC=C2)Cl)NC2=C(C=C(C=C2)Br)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 33.4, "product": "COC(=O)C=1C(=C(C=2N(C1)C(=NN2)CC2=CC=CC=C2)Cl)NC2=C(C=C(C=C2)Br)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
6
HOUR
Phenylacetyl chloride (152 μL, 1.148 mmol) was added to a solution of 4-(4-bromo-2-chlorophenylamino)-5-chloro-6-hydrazinonicotinic acid methyl ester (49) (0.233 g, 0.574 mmol) and triethylamine (160 μL, 1.148 mmol) in CH2Cl2 (5.7 mL) at 0° C. After warming to room temperature, an additional 75 μL phenylacetyl chloride...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Hydrazine.Ester
Ester
c1ccncc1
c1ccn2cnnc2c1
c1ccccc1.c1ccn2cnnc2c1.c1ccccc1
HCl
C(CCl)Cl.C(Cl)Cl
null
6
CCOC(=O)c1cnc(NN)c(Cl)c1Nc1ccc(Br)cc1Cl.O=C(Cl)Cc1ccccc1>C(CCl)Cl.C(Cl)Cl>COC(=O)c1cn2c(Cc3ccccc3)nnc2c(Cl)c1Nc1ccc(Br)cc1Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-db32bc23350740f1abb6cc7cce0f9309
COC(=O)c1cc(C(C)=O)c(F)c(F)c1Nc1ccccc1Cl>>COC(=O)c1cc2c(C)onc2c(F)c1Nc1ccccc1Cl
[N-]=[N+]=[N-].[Na+].COC(C1=C(C(=C(C(=C1)C(C)=O)F)F)NC1=C(C=CC=C1)Cl)=O.CC(=O)C>>COC(=O)C1=CC=2C(=NOC2C)C(=C1NC1=C(C=CC=C1)Cl)F
F[c:12]1[c:7]([C:8]([CH3:9])=[O:10])[cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[c:15]([NH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[Cl:23])[c:13]1[F:14]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7]2[c:8]([CH3:9])[o:10][n:11][c:12]2[c:13]([F:14])[c:15]1[NH:16][c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[Cl:23]
COC(=O)c1cc(C(C)=O)c(F)c(F)c1Nc1ccccc1Cl
COC(=O)c1cc2c(C)onc2c(F)c1Nc1ccccc1Cl
null
null
O.CCOC(=O)C
Aromatic Heterocycle Formation
OtherReaction
e5744ec146e9700a0e2ef8f4d6f9eca44bb1bfe137990d90f1ff3a1b5ad172fa
d7a14902b3a6abdab109b69c987d4859648c171877b79e6c5d2b5477595da891
c1ccc(Nc2ccc3conc3c2)cc1
F-[c;H0;D3;+0:1](:[c:2](-[F;D1;H0:3]):[c:4]):[c:5](-[C;H0;D3;+0:6](-[C;D1;H3:7])=[O;H0;D1;+0:8]):[c:9]>>[C;D1;H3:7]-[c;H0;D3;+0:6]1:[o;H0;D2;+0:8]:[#7;a:10]:[c;H0;D3;+0:1](:[c:2](-[F;D1;H0:3]):[c:4]):[c:5]:1:[c:9]
77
[{"value": 77.0, "product": "COC(=O)C1=CC=2C(=NOC2C)C(=C1NC1=C(C=CC=C1)Cl)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.0, "product": "COC(=O)C1=CC=2C(=NOC2C)C(=C1NC1=C(C=CC=C1)Cl)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
Sodium azide (128 mg, 1.95 mmol) was added to a mixture of 5-acetyl-2-(2-chlorophenylamino)-3,4-difluorobenzoic acid methyl ester (6) (601 mg, 1.59 mmol) in 3:1 acetone:water (16 ml) and heated to reflux. After 16 hours, the reaction mixture was cooled to room temperature, and diluted with EtOAc and water. The organic ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone
null
c1ccccc1
c1ccc2nocc2c1
c1ccc2nocc2c1.c1ccccc1
null
O.CCOC(=O)C
null
16
COC(=O)c1cc(C(C)=O)c(F)c(F)c1Nc1ccccc1Cl>O.CCOC(=O)C>COC(=O)c1cc2c(C)onc2c(F)c1Nc1ccccc1Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-cf6cf0cac0364cd59ba5c9d1ff16e067
COC(=O)c1cc2c(C)onc2c(F)c1Nc1ccccc1Cl>>Cc1onc2c(F)c(Nc3ccccc3Cl)c(C(=O)O)cc12
COC(=O)C1=CC=2C(=NOC2C)C(=C1NC1=C(C=CC=C1)Cl)F.C1CCOC1.[Li+].[OH-].Cl>>ClC1=C(C=CC=C1)NC=1C(=CC=2C(=NOC2C)C1F)C(=O)O
C[O:20][C:18]([c:17]1[c:8]([NH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[Cl:16])[c:6]([F:7])[c:5]2[n:4][o:3][c:2]([CH3:1])[c:22]2[cH:21]1)=[O:19]>>[CH3:1][c:2]1[o:3][n:4][c:5]2[c:6]([F:7])[c:8]([NH:9][c:10]3[cH:11][cH:12][cH:13][cH:14][c:15]3[Cl:16])[c:17]([C:18](=[O:19])[OH:20])[cH:21][c:22]12
COC(=O)c1cc2c(C)onc2c(F)c1Nc1ccccc1Cl
Cc1onc2c(F)c(Nc3ccccc3Cl)c(C(=O)O)cc12
null
null
O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc(Nc2ccc3conc3c2)cc1
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]
91
[{"value": 91.0, "product": "ClC1=C(C=CC=C1)NC=1C(=CC=2C(=NOC2C)C1F)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.7, "product": "ClC1=C(C=CC=C1)NC=1C(=CC=2C(=NOC2C)C1F)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 6-(2-chlorophenylamino)-7-fluoro-3-methyl-benzo[c]-isoxazole-5-carboxylic acid methyl ester (55) (100 mg, 0.299 mmol) in 6:1 THF:water (3.5 mL) was added LiOH (0.60 ml of a 1 M solution in water). After 1 hour, the reaction was acidified to pH 1 with 1 N HCl, diluted with water and extracted with EtOAc...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2nocc2c1.c1ccccc1
Other
O
null
1
COC(=O)c1cc2c(C)onc2c(F)c1Nc1ccccc1Cl>O>Cc1onc2c(F)c(Nc3ccccc3Cl)c(C(=O)O)cc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-07174ae39d004ca9a3623e64f59c121c
COC(=O)c1cnc(N)c(Cl)c1Nc1ccc(Br)cc1Cl.O=CC(Cl)C=O>>COC(=O)c1cn2c(C=O)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl
COC(C1=CN=C(C(=C1NC1=C(C=C(C=C1)Br)Cl)Cl)N)=O.ClC(C=O)C=O>>COC(=O)C=1C(=C(C=2N(C1)C(=CN2)C=O)Cl)NC2=C(C=C(C=C2)Br)Cl
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][c:13]([NH2:12])[c:14]([Cl:15])[c:16]1[NH:17][c:18]1[cH:19][cH:20][c:21]([Br:22])[cH:23][c:24]1[Cl:25].O=[CH:11][CH:8](Cl)[CH:9]=[O:10]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7]2[c:8]([CH:9]=[O:10])[cH:11][n:12][c:13]2[c:14]([Cl:15])[c:16]1[NH:17][c:18]1[cH:19][cH:20][c:21]([...
COC(=O)c1cnc(N)c(Cl)c1Nc1ccc(Br)cc1Cl.O=CC(Cl)C=O
COC(=O)c1cn2c(C=O)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl
null
null
null
Aromatic Heterocycle Formation
OtherReaction
aa2630788ad7f4b98b88a0bb6ce6643b41a4745823fcca8f38118ef044e276ec
777cfb7a0a90e330de341575c7c413a37b4b63909c3b8d37339ba538f80763a2
c1ccc(Nc2ccn3ccnc3c2)cc1
Cl-[CH;D3;+0:1](-[C:2]=[O;D1;H0:3])-[CH;D2;+0:4]=O.[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9]:[n;H0;D2;+0:10]:[c:11](-[NH2;D1;+0:12]):[c:13]>>[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9]:[n;H0;D3;+0:10]1:[c:11](:[c:13]):[n;H0;D2;+0:12]:[cH;D2;+0:4]:[c;H0;D3;+0:1]:1-[C:2]=[O;D1;H0:3]
null
[]
80
CELSIUS
null
null
A suspension of 6-amino-4-(4-bromo-2-chlorophenylamino)-5-chloro-nicotinic acid methyl ester (28) (1.06 g, 2.72 mmol) and 2-chloro-malonaldehyde (587 mg, 5.43 mmol) was heated to 80° C. for 45 minutes. The solution was allowed to cool to room temperature, and then washed with saturated aqueous NaHCO3, and brine. The or...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aldehyde.Aldehyde.Primary amine
Aldehyde
c1ccncc1
c1ccn2ccnc2c1
c1ccn2ccnc2c1.c1ccccc1
HCl
null
80
null
COC(=O)c1cnc(N)c(Cl)c1Nc1ccc(Br)cc1Cl.O=CC(Cl)C=O>>COC(=O)c1cn2c(C=O)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e60f1ee7c4654e0094c366fbd38ba4d6
CN.COC(=O)c1cn2c(C=O)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl>>CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)OC)cn12
C(C)(=O)O[BH-](OC(C)=O)OC(C)=O.[Na+].COC(=O)C=1C(=C(C=2N(C1)C(=CN2)C=O)Cl)NC2=C(C=C(C=C2)Br)Cl.C(C)(=O)O.CN>>COC(=O)C=1C(=C(C=2N(C1)C(=CN2)CNC)Cl)NC2=C(C=C(C=C2)Br)Cl
[CH3:1][NH2:2].O=[CH:3][c:4]1[cH:5][n:6][c:7]2[c:8]([Cl:9])[c:10]([NH:11][c:12]3[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]3[Cl:19])[c:20]([C:21](=[O:22])[O:23][CH3:24])[cH:25][n:26]12>>[CH3:1][NH:2][CH2:3][c:4]1[cH:5][n:6][c:7]2[c:8]([Cl:9])[c:10]([NH:11][c:12]3[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]3[Cl:19])[c:20](...
CN.COC(=O)c1cn2c(C=O)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl
CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)OC)cn12
null
null
null
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
c1ccc(Nc2ccn3ccnc3c2)cc1
O=[CH;D2;+0:1]-[c:2]1:[c:3]:[#7;a:4]:[c:5]:[#7;a:6]:1:[c:7].[C;D1;H3:8]-[NH2;D1;+0:9]>>[C;D1;H3:8]-[NH;D2;+0:9]-[CH2;D2;+0:1]-[c:2]1:[c:3]:[#7;a:4]:[c:5]:[#7;a:6]:1:[c:7]
46.8
[{"value": 46.0, "product": "COC(=O)C=1C(=C(C=2N(C1)C(=CN2)CNC)Cl)NC2=C(C=C(C=C2)Br)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 46.8, "product": "COC(=O)C=1C(=C(C=2N(C1)C(=CN2)CNC)Cl)NC2=C(C=C(C=C2)Br)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
0.5
HOUR
A suspension of 7-(4-bromo-2-chlorophenylamino)-8-chloro-3-formylimidazo[1,2-a]pyridine-6-carboxylic acid methyl ester (58) (25 mg, 0.056 mmol), acetic acid (7 μL, 0.11 mmol), and methylamine (2.0 M solution in THF, 56 μL, 0.11 mmol) was stirred for 0.5 hours. Sodium triacetoxyborohydride (36 mg, 0.17 mmol) was added a...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccn2ccnc2c1.c1ccccc1
Other
null
null
0.5
CN.COC(=O)c1cn2c(C=O)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl>>CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)OC)cn12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-effd8d1109d7499cbf3f109d0ae3e676
COC(=O)c1cn2c(CNCC(=O)OC(C)(C)C)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl>>CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12)C(=O)OC(C)(C)C
Cl.[OH-].[Na+].COC(=O)C=1C(=C(C=2N(C1)C(=CN2)CNCC(=O)OC(C)(C)C)Cl)NC2=C(C=C(C=C2)Br)Cl.CO.O>>BrC1=CC(=C(C=C1)NC1=C(C=2N(C=C1C(=O)O)C(=CN2)CN(C)C(=O)OC(C)(C)C)Cl)Cl
C[O:23][C:21]([c:20]1[c:10]([NH:11][c:12]2[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]2[Cl:19])[c:8]([Cl:9])[c:7]2[n:6][cH:5][c:4]([CH2:3][NH:2][CH2:1][C:26](=[O:27])[O:28][C:29]([CH3:30])([CH3:31])[CH3:32])[n:25]2[cH:24]1)=[O:22]>>[CH3:1][N:2]([CH2:3][c:4]1[cH:5][n:6][c:7]2[c:8]([Cl:9])[c:10]([NH:11][c:12]3[cH:13][cH:14...
COC(=O)c1cn2c(CNCC(=O)OC(C)(C)C)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl
CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12)C(=O)OC(C)(C)C
null
null
O
Miscellaneous
OtherReaction
1f73acab89b4d49cffa12bdd335b5b82dfc806de7b0f860018ca332cbad703ed
c69b5024139c8869fe89052e88181621aa4ee60a9d90514e6e13e7f94cbaf123
c1ccc(Nc2ccn3ccnc3c2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]:[c:7](-[C:8]-[NH;D2;+0:9]-[CH2;D2;+0:10]-[C;H0;D3;+0:11](=[O;D1;H0:12])-[#8:13]-[C:14](-[C;D1;H3:15])(-[C;D1;H3:16])-[C;D1;H3:17]):[c:18]:[#7;a:19]>>[#7;a:19]:[c:18]:[c:7](-[C:8]-[N;H0;D3;+0:9](-[CH3;D1;+0:10])-[C;H0;D3;+0:11](=[O;D1;H0:12])-[#8:13]-[C:14](-[C;D...
84
[{"value": 84.0, "product": "BrC1=CC(=C(C=C1)NC1=C(C=2N(C=C1C(=O)O)C(=CN2)CN(C)C(=O)OC(C)(C)C)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Sodium hydroxide (1.0 M aqueous solution, 0.16 mL, 0.16 mmol) is added to a solution of 7-(4-bromo-2-chlorophenylamino)-3-[(tert-butoxycarbonylmethylamino)-methyl]-8-chloroimidazo[1,2-a]pyridine-6-carboxylic acid methyl ester (60) (15 mg, 0.026 mmol) in 4:1 MeOH/water (5 mL). When the reaction was complete, the solutio...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Secondary amine
Carbamic ester.Carboxylic acid.Ether.Boc
null
null
c1ccn2ccnc2c1.c1ccccc1
Other
O
null
null
COC(=O)c1cn2c(CNCC(=O)OC(C)(C)C)cnc2c(Cl)c1Nc1ccc(Br)cc1Cl>O>CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12)C(=O)OC(C)(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-20dc90001c9a415da8c5a6b5eb7186bb
CC(C)(C)OC(=O)CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12.NOCC1CC1>>CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12)C(=O)OC(C)(C)C
C(C)(=O)OCC.CCN=C=NCCCN(C)C.Cl.C=1C=CC2=C(C1)N=NN2O.BrC1=CC(=C(C=C1)NC1=C(C=2N(C=C1C(=O)O)C(=CN2)CNCC(=O)OC(C)(C)C)Cl)Cl.C1(CC1)CON.C(C)N(CC)CC>>C(C)(C)(C)OC(N(C)CC1=CN=C2N1C=C(C(=C2Cl)NC2=C(C=C(C=C2)Br)Cl)C(NOCC2CC2)=O)=O
O[C:21]([c:20]1[c:10]([NH:11][c:12]2[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]2[Cl:19])[c:8]([Cl:9])[c:7]2[n:6][cH:5][c:4]([CH2:3][NH:2][CH2:1][C:31](=[O:32])[O:33][C:34]([CH3:35])([CH3:36])[CH3:37])[n:30]2[cH:29]1)=[O:22].[NH2:23][O:24][CH2:25][CH:26]1[CH2:27][CH2:28]1>>[CH3:1][N:2]([CH2:3][c:4]1[cH:5][n:6][c:7]2[c:8]...
CC(C)(C)OC(=O)CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12.NOCC1CC1
CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12)C(=O)OC(C)(C)C
null
null
CC(=O)N(C)C
Protection
OtherReaction
f1f1a0875c88a2b344cba15f2f501db951c6ebccf2691778c30417c6be5a4b11
6b150a32efa368c46804b091268c9a58239514c23099ef222410a1a27a975dff
O=C(NOCC1CC1)c1cn2ccnc2cc1Nc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[#7;a:6]1:[c:7]:[#7;a:8]:[c:9]:[c:10]:1-[C:11]-[NH;D2;+0:12]-[CH2;D2;+0:13]-[C;H0;D3;+0:14](=[O;D1;H0:15])-[#8:16]-[C:17](-[C;D1;H3:18])(-[C;D1;H3:19])-[C;D1;H3:20].[C:21]-[#8:22]-[NH2;D1;+0:23]>>[C:21]-[#8:22]-[NH;D2;+0:23]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[...
85
[{"value": 85.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
EDCl (6 mg, 0.033 mmol) and HOBt (5 mg, 0.033 mmol) were added to a solution of 7-(4-bromo-2-chlorophenylamino)-3-[(tert-butoxycarbonylmethylamino)-methyl]-8-chloro-imidazo[1,2-a]pyridine-6-carboxylic acid (61) in dimethylacetamide (0.4 mL). The yellow solution was allowed to stir at room temperature for 0.5 hours afte...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester.Primary amine.Secondary amine
Carbamic ester.Ether.Secondary amide.Boc
null
null
c1ccn2ccnc2c1.c1ccccc1.C1CC1
HO-
CC(=O)N(C)C
null
8
CC(C)(C)OC(=O)CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)O)cn12.NOCC1CC1>CC(=O)N(C)C>CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12)C(=O)OC(C)(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2c93b4d4fd2a452f83f81f842a2239f5
CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12)C(=O)OC(C)(C)C>>CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12
C(C)(C)(C)OC(N(C)CC1=CN=C2N1C=C(C(=C2Cl)NC2=C(C=C(C=C2)Br)Cl)C(NOCC2CC2)=O)=O.ClCCl.FC(C(=O)O)(F)F>>C1(CC1)CONC(=O)C=1C(=C(C=2N(C1)C(=CN2)CNC)Cl)NC2=C(C=C(C=C2)Br)Cl
CC(C)(C)OC(=O)[N:2]([CH3:1])[CH2:3][c:4]1[cH:5][n:6][c:7]2[c:8]([Cl:9])[c:10]([NH:11][c:12]3[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]3[Cl:19])[c:20]([C:21](=[O:22])[NH:23][O:24][CH2:25][CH:26]3[CH2:27][CH2:28]3)[cH:29][n:30]12>>[CH3:1][NH:2][CH2:3][c:4]1[cH:5][n:6][c:7]2[c:8]([Cl:9])[c:10]([NH:11][c:12]3[cH:13][cH:14]...
CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12)C(=O)OC(C)(C)C
CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12
null
null
null
Reduction
Boc amine deprotection
bbda4640db5f48af4538caded12fdadd56eacd6d4e5f7aefe46282d665df167e
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
O=C(NOCC1CC1)c1cn2ccnc2cc1Nc1ccccc1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[c:4](:[#7;a:5]):[c:6]:[#7;a:7]>>[#7;a:5]:[c:4](-[C:3]-[NH;D2;+0:1]-[C;D1;H3:2]):[c:6]:[#7;a:7]
83
[{"value": 83.0, "product": "C1(CC1)CONC(=O)C=1C(=C(C=2N(C1)C(=CN2)CNC)Cl)NC2=C(C=C(C=C2)Br)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of [7-(4-bromo-2-chlorophenylamino)-8-chloro-6-cyclopropylmethoxy-carbamoyl-imidazo[1,2-a]pyridin-3-ylmethyl]-methyl-carbamic acid tert-butyl ester (62) in 1:1 dichloromethane/trifluoroacetic acid was stirred for two hours. Solvent was removed under reduced pressure and the residue redissolved into ethyl ace...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
null
null
c1ccn2ccnc2c1.c1ccccc1.C1CC1
HO-
null
null
null
CN(Cc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12)C(=O)OC(C)(C)C>>CNCc1cnc2c(Cl)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCC3CC3)cn12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-4b9b6301407645a58c102b5f0a106557
CC(Cl)OC(=O)Cl.CCS>>CCSC(=O)OC(C)Cl
C(C)S.C(C)N(CC)CC.ClC(=O)OC(C)Cl>>C(OC(C)Cl)(SCC)=O
Cl[C:4](=[O:5])[O:6][CH:7]([CH3:8])[Cl:9].[CH3:1][CH2:2][SH:3]>>[CH3:1][CH2:2][S:3][C:4](=[O:5])[O:6][CH:7]([CH3:8])[Cl:9]
CC(Cl)OC(=O)Cl.CCS
CCSC(=O)OC(C)Cl
null
null
C(C)OCC
Acylation
thioether_nucl_sub
1e64d85185df227b30688cc91a7b5599fda55eef4d97baad42542d292c60862f
e25f8f686987a3d16d381c43fb269bbfe997b12f392a7cb69c3f21b45e42c5a6
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C;D1;H3:5]-[C:6]-[SH;D1;+0:7]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[S;H0;D2;+0:7]-[C:6]-[C;D1;H3:5]
89
[{"value": 89.0, "product": "C(OC(C)Cl)(SCC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.9, "product": "C(OC(C)Cl)(SCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A solution of 1-chloroethyl chloroformate (71.5 g, 0.5 mol) in diethyl ether (600 mL) was cooled to 0-4° C. in an ice-water bath and a solution of ethanethiol (37 mL, 0.5 mol) and triethylamine (69.3 mL, 0.5 mol) in diethyl ether (200 mL) was added dropwise over 1 h. The reaction mixture was removed from the ice bath a...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Aliphatic thiol
Ether.Monosulfide
null
null
null
HCl
C(C)OCC
null
4
CC(Cl)OC(=O)Cl.CCS>C(C)OCC>CCSC(=O)OC(C)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-aa1b1be5baa64a728d09278a5bd0313e
CC(C)(C)S.CC(Cl)OC(=O)Cl>>CC(Cl)OC(=O)SC(C)(C)C
C(C)(C)(C)S.ClC(=O)OC(C)Cl.CN1CCOCC1>>C(OC(C)Cl)(SC(C)(C)C)=O
[SH:7][C:8]([CH3:9])([CH3:10])[CH3:11].Cl[C:5]([O:4][CH:2]([CH3:1])[Cl:3])=[O:6]>>[CH3:1][CH:2]([Cl:3])[O:4][C:5](=[O:6])[S:7][C:8]([CH3:9])([CH3:10])[CH3:11]
CC(C)(C)S.CC(Cl)OC(=O)Cl
CC(Cl)OC(=O)SC(C)(C)C
null
null
C(Cl)Cl
Acylation
thioether_nucl_sub
1e64d85185df227b30688cc91a7b5599fda55eef4d97baad42542d292c60862f
e25f8f686987a3d16d381c43fb269bbfe997b12f392a7cb69c3f21b45e42c5a6
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C;D1;H3:5]-[C:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[SH;D1;+0:9]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[S;H0;D2;+0:9]-[C:6](-[C;D1;H3:5])(-[C;D1;H3:7])-[C;D1;H3:8]
89
[{"value": 89.0, "product": "C(OC(C)Cl)(SC(C)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.0, "product": "C(OC(C)Cl)(SC(C)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A solution of tert-butyl thiol (180 g, 2 mol) and 1-chloroethyl chloroformate (284 g, 2 mol) in CH2Cl2 (1 L) was cooled to 0° C. in an ice-water bath. N-Methylmorpholine (212.1 g, 2.1 mol) was added dropwise over a period of 1 h and the reaction mixture was allowed to stir at room temperature for 16 h. The reaction mix...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Aliphatic thiol
Ether.Monosulfide
null
null
null
HCl
C(Cl)Cl
null
16
CC(C)(C)S.CC(Cl)OC(=O)Cl>C(Cl)Cl>CC(Cl)OC(=O)SC(C)(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-097361bcf40b442c8d2dc604cdc92baa
CC(Cl)OC(=O)Cl.Sc1ccccc1>>CC(Cl)OC(=O)Sc1ccccc1
C(C)N(CC)CC.C1(=CC=CC=C1)S.ClC(=O)OC(C)Cl>>C(OC(C)Cl)(SC1=CC=CC=C1)=O
Cl[C:5]([O:4][CH:2]([CH3:1])[Cl:3])=[O:6].[SH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][CH:2]([Cl:3])[O:4][C:5](=[O:6])[S:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
CC(Cl)OC(=O)Cl.Sc1ccccc1
CC(Cl)OC(=O)Sc1ccccc1
null
null
ClCCl.C(Cl)Cl
Acylation
thioether_nucl_sub
3978f308f3250c89cbea32ce9713e8965cfa8792f1874ce54efdfd509c4dabe9
519bfe74e906772b61515a2291874fa5bdecca6886fffcbb6424325ea7e98e27
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[SH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[S;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]
98.5
[{"value": 98.5, "product": "C(OC(C)Cl)(SC1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.5, "product": "C(OC(C)Cl)(SC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
A solution of benzenethiol (50 g, 450 mmol) and 1-chloroethyl chloroformate (65 g, 450 mmol) in CH2Cl2 (300 mL) was cooled to 0-4° C. in an ice-water bath. To the mixture was added a solution of triethylamine (450 mmol) in dichloromethane (200 mL) dropwise over 30 min. The reaction was removed from the ice bath and sti...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Aromatic thiol
Ether.Monosulfide
null
null
c1ccccc1
HCl
ClCCl.C(Cl)Cl
null
12
CC(Cl)OC(=O)Cl.Sc1ccccc1>ClCCl.C(Cl)Cl>CC(Cl)OC(=O)Sc1ccccc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-78195199e32d4abaa861ba5154e7b4ae
CC(C)C(=O)O>>CC(C)C(=O)[O-]
[OH-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C(C)C)(=O)O>>C(C(C)C)(=O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[OH:6]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[O-:6]
CC(C)C(=O)O
CC(C)C(=O)[O-]
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
A 40 wt % solution of tetrabutylammonium hydroxide in water (250 mL, 99 g, 382 mmol), water (300 mL) and isobutyric acid (33.8 g, 382 mmol) was stirred at ambient temperature for 30 min. The solvent was removed in vacuo to afford the title compound (5) as a waxy solid, which was used without further purification. Condi...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CC(C)C(=O)O>O>CC(C)C(=O)[O-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-55b291c8e2044046a869b5ae58a39430
CC(C)C(=O)O>>CC(C)C(=O)[O-]
[OH-].C(CCC)[N+](CCCC)(CCCC)CCCC.CO.C(C(C)C)(=O)O>>C(C(C)C)(=O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[OH:6]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[O-:6]
CC(C)C(=O)O
CC(C)C(=O)[O-]
null
null
null
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Alternatively, a 1M solution of tetrabutylammonium hydroxide in methanol (1 L, 1 mol) and isobutyric acid (88.5 g, 1 mol) was stirred at ambient temperature for 30 min. The solvent was removed in vacuo to afford the title compound (5) as a waxy solid, which was used without further purification. Conditions: See reactio...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
null
null
null
CC(C)C(=O)O>>CC(C)C(=O)[O-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e5fa1c7500d9466d82c7315eebd7857c
CC(C)C(=O)O.CSC(=O)OC(C)Cl>>CSC(=O)OC(C)OC(=O)C(C)C
C(OC(C)Cl)(SC)=O.C(C(C)C)(=O)O.C(C(C)C)(=O)O.C(C)(C)N(CC)C(C)C>>C(OC(C)OC(C(C)C)=O)(SC)=O
[OH:8][C:9](=[O:10])[CH:11]([CH3:12])[CH3:13].Cl[CH:6]([O:5][C:3]([S:2][CH3:1])=[O:4])[CH3:7]>>[CH3:1][S:2][C:3](=[O:4])[O:5][CH:6]([CH3:7])[O:8][C:9](=[O:10])[CH:11]([CH3:12])[CH3:13]
CC(C)C(=O)O.CSC(=O)OC(C)Cl
CSC(=O)OC(C)OC(=O)C(C)C
null
null
CCOCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a1c78245a699a2d7f32afead5a272e9f9c3376384617cf46d1f41528c07c62a0
24a9dd2a1f5258889ba19b94426efe6fc90f5f9d7c761574387c6d65581f3783
null
Cl-[CH;D3;+0:1](-[C;D1;H3:2])-[#8:3]-[C:4](-[#16:5])=[O;D1;H0:6].[C:7]-[C:8](=[O;D1;H0:9])-[OH;D1;+0:10]>>[#16:5]-[C:4](=[O;D1;H0:6])-[#8:3]-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:10]-[C:8](-[C:7])=[O;D1;H0:9]
97
[{"value": 97.0, "product": "C(OC(C)OC(C(C)C)=O)(SC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.0, "product": "C(OC(C)OC(C(C)C)=O)(SC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
55
CELSIUS
null
null
Compound (1) (308 mg, 2 mmol) was dissolved in isobutyric acid (264 mg, 3 mmol). This mixture was slowly added to a pre-mixed solution of isobutyric acid (264 mg, 3 mmol) and diisopropylethylamine (387 mg, 3 mmol) and the reaction mixture heated to 55° C. for 16 h, diluted with ether (50 mL), washed with water (2×10 mL...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carboxylic acid
Ester
null
null
null
HCl
CCOCC
55
null
CC(C)C(=O)O.CSC(=O)OC(C)Cl>CCOCC>CSC(=O)OC(C)OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-28d3cce3be494893a4b299149ed1ce0e
CC(C)C(=O)[O-].CCSC(=O)OC(C)Cl>>CCSC(=O)OC(C)OC(=O)C(C)C
C(C(C)C)(=O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(OC(C)Cl)(SCC)=O>>C(OC(C)OC(C(C)C)=O)(SCC)=O
[O-:9][C:10](=[O:11])[CH:12]([CH3:13])[CH3:14].Cl[CH:7]([O:6][C:4]([S:3][CH2:2][CH3:1])=[O:5])[CH3:8]>>[CH3:1][CH2:2][S:3][C:4](=[O:5])[O:6][CH:7]([CH3:8])[O:9][C:10](=[O:11])[CH:12]([CH3:13])[CH3:14]
CC(C)C(=O)[O-].CCSC(=O)OC(C)Cl
CCSC(=O)OC(C)OC(=O)C(C)C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
c4b9f8f0e97e27b0b79018d7a91e67cd98aea96bf160fdfec2f05850d4093366
db536d01d4fbc476192b447c783c57fc0acdaf23478d7e09bd5fdb80ddf79bc8
null
Cl-[CH;D3;+0:1](-[C;D1;H3:2])-[#8:3]-[C:4](-[#16:5])=[O;D1;H0:6].[C:7]-[C:8](-[O-;H0;D1:9])=[O;D1;H0:10]>>[#16:5]-[C:4](=[O;D1;H0:6])-[#8:3]-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:9]-[C:8](-[C:7])=[O;D1;H0:10]
63
[{"value": 63.0, "product": "C(OC(C)OC(C(C)C)=O)(SCC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.0, "product": "C(OC(C)OC(C(C)C)=O)(SCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of tetrabutylammonium isobutyrate (5) (382 mmol) in tetrahydrofuran (500 mL) was added compound (2) (49 g, 288 mmol). The mixture was stirred at ambient temperature for 16 h then the solvent removed in vacuo. The residue was dissolved in diethyl ether (600 mL), washed with water (3×300 mL) and the organic...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ether
Ester
null
null
null
Other
O1CCCC1
null
16
CC(C)C(=O)[O-].CCSC(=O)OC(C)Cl>O1CCCC1>CCSC(=O)OC(C)OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-3bc65132c3dd477fa6d38a8141dd2485
CC(C)C(=O)O.CC(Cl)OC(=O)SC(C)(C)C>>CC(OC(=O)SC(C)(C)C)OC(=O)C(C)C
C(OC(C)Cl)(SC(C)(C)C)=O.C(C(C)C)(=O)O.C(C(C)C)(=O)O.C(C)(C)N(CC)C(C)C>>C(OC(C)OC(C(C)C)=O)(SC(C)(C)C)=O
[OH:11][C:12](=[O:13])[CH:14]([CH3:15])[CH3:16].Cl[CH:2]([CH3:1])[O:3][C:4](=[O:5])[S:6][C:7]([CH3:8])([CH3:9])[CH3:10]>>[CH3:1][CH:2]([O:3][C:4](=[O:5])[S:6][C:7]([CH3:8])([CH3:9])[CH3:10])[O:11][C:12](=[O:13])[CH:14]([CH3:15])[CH3:16]
CC(C)C(=O)O.CC(Cl)OC(=O)SC(C)(C)C
CC(OC(=O)SC(C)(C)C)OC(=O)C(C)C
null
null
CCOCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a1c78245a699a2d7f32afead5a272e9f9c3376384617cf46d1f41528c07c62a0
24a9dd2a1f5258889ba19b94426efe6fc90f5f9d7c761574387c6d65581f3783
null
Cl-[CH;D3;+0:1](-[C;D1;H3:2])-[#8:3]-[C:4](-[#16:5])=[O;D1;H0:6].[C:7]-[C:8](=[O;D1;H0:9])-[OH;D1;+0:10]>>[#16:5]-[C:4](=[O;D1;H0:6])-[#8:3]-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:10]-[C:8](-[C:7])=[O;D1;H0:9]
90.6
[{"value": 90.0, "product": "C(OC(C)OC(C(C)C)=O)(SC(C)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.6, "product": "C(OC(C)OC(C(C)C)=O)(SC(C)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
55
CELSIUS
null
null
Compound (3) (392 mg, 2 mmol) was dissolved in isobutyric acid (264 mg, 3 mmol) and the solution was slowly added to a pre-mixed solution of isobutyric acid (264 mg, 3 mmol) and diisopropylethylamine (387 mg, 3 mmol). The reaction mixture was heated to 55° C. for 16 h, then diluted with ether (50 mL), washed with water...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carboxylic acid
Ester
null
null
null
HCl
CCOCC
55
null
CC(C)C(=O)O.CC(Cl)OC(=O)SC(C)(C)C>CCOCC>CC(OC(=O)SC(C)(C)C)OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-9a51be63b2354a1997c8f41ee5285522
CC(C)C(=O)O.CC(Cl)OC(=O)Sc1ccccc1>>CC(OC(=O)Sc1ccccc1)OC(=O)C(C)C
C(OC(C)Cl)(SC1=CC=CC=C1)=O.C(C(C)C)(=O)O.C(C)N(CC)CC.[I-].[Na+]>>C(OC(C)OC(C(C)C)=O)(SC1=CC=CC=C1)=O
[OH:13][C:14](=[O:15])[CH:16]([CH3:17])[CH3:18].Cl[CH:2]([CH3:1])[O:3][C:4](=[O:5])[S:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][CH:2]([O:3][C:4](=[O:5])[S:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[O:13][C:14](=[O:15])[CH:16]([CH3:17])[CH3:18]
CC(C)C(=O)O.CC(Cl)OC(=O)Sc1ccccc1
CC(OC(=O)Sc1ccccc1)OC(=O)C(C)C
null
null
C(C)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a1c78245a699a2d7f32afead5a272e9f9c3376384617cf46d1f41528c07c62a0
24a9dd2a1f5258889ba19b94426efe6fc90f5f9d7c761574387c6d65581f3783
c1ccccc1
Cl-[CH;D3;+0:1](-[C;D1;H3:2])-[#8:3]-[C:4](-[#16:5])=[O;D1;H0:6].[C:7]-[C:8](=[O;D1;H0:9])-[OH;D1;+0:10]>>[#16:5]-[C:4](=[O;D1;H0:6])-[#8:3]-[CH;D3;+0:1](-[C;D1;H3:2])-[O;H0;D2;+0:10]-[C:8](-[C:7])=[O;D1;H0:9]
97
[{"value": 97.0, "product": "C(OC(C)OC(C(C)C)=O)(SC1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
A mixture of compound (4) (10 g, 46 mmol), isobutyric acid (30 mL), triethylamine (30 mL) and sodium iodide (2 g) was stirred and heated in an oil bath at 50° C. for 3 days. The reaction mixture was diluted with diethyl ether (200 mL) and washed successively with water (3×100 mL), saturated aqueous sodium bicarbonate (...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carboxylic acid
Ester
null
null
c1ccccc1
HCl
C(C)OCC
50
null
CC(C)C(=O)O.CC(Cl)OC(=O)Sc1ccccc1>C(C)OCC>CC(OC(=O)Sc1ccccc1)OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f5fdf094fbf64e4bbfad7efc41a84f83
CSC(=O)OC(C)OC(=O)C(C)C.O=C1CCC(=O)N1O>>CC(OC(=O)OC1CC(=O)NC1=O)OC(=O)C(C)C
C(OC(C)OC(C(C)C)=O)(SC)=O.ON1C(CCC1=O)=O.C(C)(=O)OO.C(C)(=O)O>>C(C(C)C)(=O)OC(C)OC(=O)OC1C(=O)NC(C1)=O
CS[C:4]([O:3][CH:2]([CH3:1])[O:14][C:15](=[O:16])[CH:17]([CH3:18])[CH3:19])=[O:5].[OH:6][N:11]1[C:9](=[O:10])[CH2:8][CH2:7][C:12]1=[O:13]>>[CH3:1][CH:2]([O:3][C:4](=[O:5])[O:6][CH:7]1[CH2:8][C:9](=[O:10])[NH:11][C:12]1=[O:13])[O:14][C:15](=[O:16])[CH:17]([CH3:18])[CH3:19]
CSC(=O)OC(C)OC(=O)C(C)C.O=C1CCC(=O)N1O
CC(OC(=O)OC1CC(=O)NC1=O)OC(=O)C(C)C
null
null
CCOCC.C(Cl)Cl
Acylation
OtherReaction
02135880cabf0520fe2823574725f3f8fc1c0bab0f84cd32266c3754d4ddc08a
acc814d6ee5ed8d60fec2d5fd5dfb0e09a3cffb805a07d7522f5fdeb2116a253
O=C1CCC(=O)N1
C-S-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[O;D1;H0:5]=[C:6]1-[C:7]-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[N;H0;D3;+0:11]-1-[OH;D1;+0:12]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:12]-[CH;D3;+0:8]1-[C:7]-[C:6](=[O;D1;H0:5])-[NH;D2;+0:11]-[C:9]-1=[O;D1;H0:10]
77
[{"value": 77.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
3
HOUR
To a solution of compound (6) (1 g, 4.8 mmol) in CH2Cl2 (10 mL) was added N-hydroxysuccinimide (1.1 g, 9.5 mmol) and the reaction mixture cooled to 0° C. A solution of 32% (v/v) peracetic acid in acetic acid (3.4 mL, 1.1 g, 14.4 mmol) was added dropwise over a period of 10 mm, then the solution allowed to stir at room ...
10.6084/m9.figshare.5104873.v1
null
Ether.Tertiary amide.Tertiary amide.Monosulfide
Carbonic Ester.Unsubstituted dicarboximide
C1CC[NH]C1
C1CCNC1
C1CCNC1
Other
CCOCC.C(Cl)Cl
0
3
CSC(=O)OC(C)OC(=O)C(C)C.O=C1CCC(=O)N1O>CCOCC.C(Cl)Cl>CC(OC(=O)OC1CC(=O)NC1=O)OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6d57c681b8834e76a2f56295c05a4671
O=C(OO)c1cccc(Cl)c1>>O=C(O)c1cccc(Cl)c1
C(C(C)C)(=O)OC(C)OC(=O)OC1C(=O)NC(C1)=O.ON1C(CCC1=O)=O.C(OC(C)OC(C(C)C)=O)(SC)=O.ClC1=CC(=CC=C1)C(=O)OO>>C(C(C)C)(=O)OC(C)OC(=O)OC1C(=O)NC(C1)=O.ClC=1C=C(C(=O)O)C=CC1
O[O:22][C:21](=[O:20])[c:23]1[cH:24][cH:25][cH:26][c:27]([Cl:28])[cH:29]1>>[O:20]=[C:21]([OH:22])[c:23]1[cH:24][cH:25][cH:26][c:27]([Cl:28])[cH:29]1
O=C(OO)c1cccc(Cl)c1
O=C(O)c1cccc(Cl)c1
null
null
CCOCC.C(Cl)Cl
Reduction
OtherReaction
a3a34f0a79d3ff42abf92863db20ba6c8958620c1c833b03092f42d83ad97bb6
531425a5a0d611c60dd4e710b59e4cf8c0bfa2d891e7bd03ed5bc1f943ee1b47
c1ccccc1
O-[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
16
HOUR
In an alternative synthesis of (10), N-hydroxysuccinimide (558 mg, 4.8 mmol) was added to a solution of compound (6) (500 mg, 2.4 mmol) in CH2Cl2 (10 mL) and the reaction mixture cooled to 0° C. m-Chloroperbenzoic acid (1.62 g, 7.2 mmol, commercial grade: 77% in water) was added over a period of 10 min and the mixture ...
10.6084/m9.figshare.5104873.v1
null
Peroxide
Carboxylic acid
null
null
c1ccccc1
Other
CCOCC.C(Cl)Cl
null
16
O=C(OO)c1cccc(Cl)c1>CCOCC.C(Cl)Cl>O=C(O)c1cccc(Cl)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5fd108b919624c62b4cb2d0c9160888a
O=C(OO)c1cccc(Cl)c1>>O=C(O)c1cccc(Cl)c1
C(C(C)C)(=O)OC(C)OC(=O)OC1C(=O)NC(C1)=O.ON1C(CCC1=O)=O.C(OC(C)OC(C(C)C)=O)(SC(C)(C)C)=O.ClC1=CC(=CC=C1)C(=O)OO>>C(C(C)C)(=O)OC(C)OC(=O)OC1C(=O)NC(C1)=O.ClC=1C=C(C(=O)O)C=CC1
O[O:22][C:21](=[O:20])[c:23]1[cH:24][cH:25][cH:26][c:27]([Cl:28])[cH:29]1>>[O:20]=[C:21]([OH:22])[c:23]1[cH:24][cH:25][cH:26][c:27]([Cl:28])[cH:29]1
O=C(OO)c1cccc(Cl)c1
O=C(O)c1cccc(Cl)c1
null
null
CCOCC.C(Cl)Cl
Reduction
OtherReaction
a3a34f0a79d3ff42abf92863db20ba6c8958620c1c833b03092f42d83ad97bb6
531425a5a0d611c60dd4e710b59e4cf8c0bfa2d891e7bd03ed5bc1f943ee1b47
c1ccccc1
O-[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
16
HOUR
In still another alternative synthesis of (10), N-hydroxysuccinimide (230 mg, 2 mmol) was added to a solution of compound (8) (248 mg, 1 mmol) in CH2Cl2 (10 mL) was added and the reaction mixture cooled to 0° C. m-Chloroperbenzoic acid (670 mg, 3 mmol, commercial grade: 77% in water) was added over a period of 10 min a...
10.6084/m9.figshare.5104873.v1
null
Peroxide
Carboxylic acid
null
null
c1ccccc1
Other
CCOCC.C(Cl)Cl
null
16
O=C(OO)c1cccc(Cl)c1>CCOCC.C(Cl)Cl>O=C(O)c1cccc(Cl)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-1934a0cf8729432495ba28b3d6194cc7
NCC1(CC(=O)O)CCCCC1>>NCC1(CC(=O)[O-])CCCCC1
C1CCC(CC1)(CC(=O)O)CN.[OH-].C(CCC)[N+](CCCC)(CCCC)CCCC>>NCC1(CCCCC1)CC(=O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
[NH2:18][CH2:19][C:20]1([CH2:21][C:22](=[O:23])[OH:24])[CH2:25][CH2:26][CH2:27][CH2:28][CH2:29]1>>[NH2:18][CH2:19][C:20]1([CH2:21][C:22](=[O:23])[O-:24])[CH2:25][CH2:26][CH2:27][CH2:28][CH2:29]1
NCC1(CC(=O)O)CCCCC1
NCC1(CC(=O)[O-])CCCCC1
null
null
CO
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
C1CCCCC1
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
A solution containing gabapentin (34.4 g, 200 mmol), a 1 M solution of tetrabutylammonium hydroxide in methanol (200 mL, 200 mmol), and additional methanol (200 mL) was stirred at ambient temperature for 14 h. The solvent was removed in vacuo, then toluene (200 mL) was added and evaporated under reduced pressure two ti...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
C1CCCCC1
null
CO
null
null
NCC1(CC(=O)O)CCCCC1>CO>NCC1(CC(=O)[O-])CCCCC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-cc9be9edf1b94d39b0517d0002587328
CC(OC(=O)OC1CC(=O)NC1=O)OC(=O)C(C)C.NCC1(CC(=O)O)CCCCC1>>CC(OC(=O)NCC1(CC(=O)O)CCCCC1)OC(=O)C(C)C
C1CCC(CC1)(CC(=O)O)CN.C([O-])(O)=O.[Na+].C(C(C)C)(=O)OC(C)OC(=O)OC1C(=O)NC(C1)=O>>C(C(C)C)(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O
O=C1CC(O[C:4]([O:3][CH:2]([CH3:1])[O:18][C:19](=[O:20])[CH:21]([CH3:22])[CH3:23])=[O:5])C(=O)N1.[NH2:6][CH2:7][C:8]1([CH2:9][C:10](=[O:11])[OH:12])[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[CH3:1][CH:2]([O:3][C:4](=[O:5])[NH:6][CH2:7][C:8]1([CH2:9][C:10](=[O:11])[OH:12])[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1)[O:18]...
CC(OC(=O)OC1CC(=O)NC1=O)OC(=O)C(C)C.NCC1(CC(=O)O)CCCCC1
CC(OC(=O)NCC1(CC(=O)O)CCCCC1)OC(=O)C(C)C
null
null
O.C(C)#N.C(C)OCC
Protection
OtherReaction
027d0fd8b951a171e70b3921f7d92c4a6800c5ef2d7b1bbadde0aa86898a31fc
f74d614cf84bcf20f6c6c1e8fa6e086089c89520408e8edf2b8e31f12242190c
C1CCCCC1
O=C1-C-C(-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-C(=O)-N-1.[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:6]-[C:5]
96
[{"value": 96.0, "product": "C(C(C)C)(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.0, "product": "C(C(C)C)(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of gabapentin (1.7 g, 10 mmol) and sodium bicarbonate (20 mmol) in water (40 mL) was added a solution of compound (10) (2.73 g, 10 mmol) in acetonitrile (20 mL) over 1 min. The reaction was stirred at ambient temperature for 16 h. The reaction mixture was diluted with diethyl ether (100 mL) and washed wit...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Unsubstituted dicarboximide.Primary amine
Carbamic ester
C1CCNC1
null
C1CCCCC1
HO-
O.C(C)#N.C(C)OCC
null
16
CC(OC(=O)OC1CC(=O)NC1=O)OC(=O)C(C)C.NCC1(CC(=O)O)CCCCC1>O.C(C)#N.C(C)OCC>CC(OC(=O)NCC1(CC(=O)O)CCCCC1)OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8aa22913bcad4306a3b567bf0203466f
CC(C)C(=O)O>>CC(C)C(=O)[O-]
C(C(C)C)(=O)O.[OH-].C[N+](C)(C)C>>C(C(C)C)(=O)[O-].C[N+](C)(C)C
[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[OH:6]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[O-:6]
CC(C)C(=O)O
CC(C)C(=O)[O-]
null
null
null
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
To a 20 L round bottom flask was added isobutyric acid (1300 mL, 14 mol), and an aqueous solution of 25% tetramethylammonium hydroxide (5 L, 14 mol). The water was removed under reduced pressure, and azeotroped with toluene (2×2 L) to leave the product (15) as an amber liquid, which was used without further purificatio...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
null
null
null
CC(C)C(=O)O>>CC(C)C(=O)[O-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-777faa7e89874a9282d528ed3c9f7d49
CC(C)C(=O)O.CSC(=O)OOC(Cl)C(C)C>>CSC(=O)OOC(OC(=O)C(C)C)C(C)C
C(C(C)C)(=O)[O-].C[N+](C)(C)C.C(C(C)C)(=O)O.C(OOC(C(C)C)Cl)(SC)=O>>C(OOC(C(C)C)OC(C(C)C)=O)(SC)=O
[OH:8][C:9](=[O:10])[CH:11]([CH3:12])[CH3:13].Cl[CH:7]([O:6][O:5][C:3]([S:2][CH3:1])=[O:4])[CH:14]([CH3:15])[CH3:16]>>[CH3:1][S:2][C:3](=[O:4])[O:5][O:6][CH:7]([O:8][C:9](=[O:10])[CH:11]([CH3:12])[CH3:13])[CH:14]([CH3:15])[CH3:16]
CC(C)C(=O)O.CSC(=O)OOC(Cl)C(C)C
CSC(=O)OOC(OC(=O)C(C)C)C(C)C
null
null
CCOC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a1c78245a699a2d7f32afead5a272e9f9c3376384617cf46d1f41528c07c62a0
24a9dd2a1f5258889ba19b94426efe6fc90f5f9d7c761574387c6d65581f3783
null
Cl-[CH;D3;+0:1](-[#8:2]-[#8:3]-[C:4]=[O;D1;H0:5])-[C:6](-[C;D1;H3:7])-[C;D1;H3:8].[C:9]-[C:10](=[O;D1;H0:11])-[OH;D1;+0:12]>>[C:9]-[C:10](=[O;D1;H0:11])-[O;H0;D2;+0:12]-[CH;D3;+0:1](-[#8:2]-[#8:3]-[C:4]=[O;D1;H0:5])-[C:6](-[C;D1;H3:7])-[C;D1;H3:8]
67.7
[{"value": 65.0, "product": "C(OOC(C(C)C)OC(C(C)C)=O)(SC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.7, "product": "C(OOC(C(C)C)OC(C(C)C)=O)(SC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
To a 3 L three neck round bottom flask equipped with a mechanical stirrer and teflon-coated thermocouple was added (15) (1672 g, 9 mol), isobutyric acid (264 g, 1.5 mol), and (14) (1050 g, 5.76 mol). The reaction mixture was heated to 80° C. for 12 h, monitoring the reaction progress by 1H NMR. The reaction mixture was...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carboxylic acid
Ester
null
null
null
HCl
CCOC(=O)C
80
null
CC(C)C(=O)O.CSC(=O)OOC(Cl)C(C)C>CCOC(=O)C>CSC(=O)OOC(OC(=O)C(C)C)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a1e5675904344e97b8bb7ba7e574b260
CSC(=O)OOC(OC(=O)C(C)C)C(C)C.O=C(O[C@@H]1C(=O)N(O)C(=O)[C@H]1OC(=O)c1ccccc1)c1ccccc1>>CC(C)C(=O)O[C@H](OC(=O)ON1C(=O)[C@@H](OC(=O)c2ccccc2)[C@H](OC(=O)c2ccccc2)C1=O)C(C)C
ON1C([C@H]([C@@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O.C(OOC(C(C)C)OC(C(C)C)=O)(SC)=O.C(C)(=O)OO.C(C)(=O)OO>>CC(C(=O)O[C@@H](C(C)C)OC(=O)ON1C([C@H]([C@@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O)C
CS[C:9](O[O:8][CH:7]([O:6][C:4]([CH:2]([CH3:1])[CH3:3])=[O:5])[CH:37]([CH3:38])[CH3:39])=[O:10].[OH:11][N:12]1[C:13](=[O:14])[C@@H:15]([O:16][C:17](=[O:18])[c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[C@H:25]([O:26][C:27](=[O:28])[c:29]2[cH:30][cH:31][cH:32][cH:33][cH:34]2)[C:35]1=[O:36]>>[CH3:1][CH:2]([CH3:3])[C:4](=[...
CSC(=O)OOC(OC(=O)C(C)C)C(C)C.O=C(O[C@@H]1C(=O)N(O)C(=O)[C@H]1OC(=O)c1ccccc1)c1ccccc1
CC(C)C(=O)O[C@H](OC(=O)ON1C(=O)[C@@H](OC(=O)c2ccccc2)[C@H](OC(=O)c2ccccc2)C1=O)C(C)C
null
null
ClCCl.C(C)(=O)O
Acylation
OtherReaction
1a0d65d95c03f609c9ba14e788b1ef64da345e59cee201a8100967aef66d4c98
b8c84c3e0ba8877f8793c358e95ebb320bfaabe7f65a860968c1a83a5d892903
O=C(O[C@@H]1C(=O)NC(=O)[C@H]1OC(=O)c1ccccc1)c1ccccc1
C-S-[C;H0;D3;+0:1](=[O;D1;H0:2])-O-[O;H0;D2;+0:3]-[CH;D3;+0:4](-[#8:5]-[C:6](-[C:7])=[O;D1;H0:8])-[C:9](-[C;D1;H3:10])-[C;D1;H3:11].[O;D1;H0:12]=[C:13]1-[C:14]-[C:15]-[C:16](=[O;D1;H0:17])-[#7:18]-1-[OH;D1;+0:19]>>[C:7]-[C:6](=[O;D1;H0:8])-[#8:5]-[C@H;D3;+0:4](-[O;H0;D2;+0:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:19...
25.7
[{"value": 25.0, "product": "CC(C(=O)O[C@@H](C(C)C)OC(=O)ON1C([C@H]([C@@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 25.7, "product": "CC(C(=O)O[C@@H](C(C)C)OC(=O)ON1C([C@H]([C@@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O)C", "details": "CALCULATEDPERC...
null
null
8
HOUR
To a stirred solution of compound (18) (35 g, 98.6 mmol) and thiocarbonate (13) (34.6 g, 148 mmol) in dichloromethane at 0° C. was dropwise added a 32% solution of peracetic acid (300 mmol) in acetic acid over 2 h. The reaction temperature was kept below 35° C. during the addition of peracetic acid. After the addition ...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Monosulfide
Ether
null
null
C1CC[NH]C1.c1ccccc1.c1ccccc1
Other
ClCCl.C(C)(=O)O
null
8
CSC(=O)OOC(OC(=O)C(C)C)C(C)C.O=C(O[C@@H]1C(=O)N(O)C(=O)[C@H]1OC(=O)c1ccccc1)c1ccccc1>ClCCl.C(C)(=O)O>CC(C)C(=O)O[C@H](OC(=O)ON1C(=O)[C@@H](OC(=O)c2ccccc2)[C@H](OC(=O)c2ccccc2)C1=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-bec25c2af5d04244be0f509c18c823c6
O=C(O[C@@H](C(=O)O)[C@@H](OC(=O)c1ccccc1)C(=O)O)c1ccccc1>>O=C(O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
C1=CC=C(C=C1)C(=O)O[C@H]([C@H](C(=O)O)OC(=O)C2=CC=CC=C2)C(=O)O.C(C)(=O)OC(C)=O>>O=C1OC([C@@H]([C@H]1OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O
O[C:5]([C@H:4]([O:3][C:2](=[O:1])[c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1)[C@H:10]([C:8]([OH:7])=[O:9])[O:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)=[O:6]>>[O:1]=[C:2]([O:3][C@H:4]1[C:5](=[O:6])[O:7][C:8](=[O:9])[C@@H:10]1[O:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[c:20]1[cH...
O=C(O[C@@H](C(=O)O)[C@@H](OC(=O)c1ccccc1)C(=O)O)c1ccccc1
O=C(O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
null
null
null
Miscellaneous
OtherReaction
dfa11c0c8b4511b7073a013bc90c6b8429c487af9f4101a7fcdad6ab1a1fd93d
22fb50577915472f1babb105381e408122dc09b3472eabb73e6e4daecfef90f6
O=C(O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[#8:4]-[C:5]=[O;D1;H0:6])-[C:7]-[C:8](=[O;D1;H0:9])-[OH;D1;+0:10]>>[O;D1;H0:6]=[C:5]-[#8:4]-[C:3]1-[C:7]-[C:8](=[O;D1;H0:9])-[O;H0;D2;+0:10]-[C;H0;D3;+0:1]-1=[O;D1;H0:2]
null
[]
85
CELSIUS
null
null
To a 3-necked 5 L round bottom flask fitted with a mechanical stirrer and a teflon coated thermocouple was added (−)-2,3-dibenzoyl-L-tartaric acid (1000 g, 2.79 mol) followed by acetic anhydride (2 L). The suspension was stirred and heated to 85° C. for 2 h during which time the starting material gradually dissolved. A...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid
Anhydride
null
C1CCOC1
C1CCOC1.c1ccccc1.c1ccccc1
HO-
null
85
null
O=C(O[C@@H](C(=O)O)[C@@H](OC(=O)c1ccccc1)C(=O)O)c1ccccc1>>O=C(O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d01879c487774bae935d5be782b66a84
NO.O=C(O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1>>O=C(O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
NO.O.O=C1OC([C@@H]([C@H]1OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O.C(C)#N>>ON1C([C@@H]([C@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O
[NH2:7][OH:8].O1[C:5](=[O:6])[C@H:4]([O:3][C:2](=[O:1])[c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[C@@H:11]([O:12][C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)[C:9]1=[O:10]>>[O:1]=[C:2]([O:3][C@H:4]1[C:5](=[O:6])[N:7]([OH:8])[C:9](=[O:10])[C@@H:11]1[O:12][C:13](=[O:14])[c:15]1[cH:16][cH:17][cH:18][cH:19]...
NO.O=C(O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
O=C(O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
ac5f63bba60d4a1d0330a86ebe6d3207e2dd9014985e5a45540d3ddb5de76511
f570959c6614f83205be0ddef7485420f00ece3dc52d54ad514eee7326c7fc88
O=C(O[C@H]1C(=O)NC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
[NH2;D1;+0:1]-[O;D1;H1:2].[O;D1;H0:3]=[C;H0;D3;+0:4]1-O-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C:7](-[#8:8]-[C:9]=[O;D1;H0:10])-[C:11]-1-[#8:12]-[C:13]=[O;D1;H0:14]>>[O;D1;H0:3]=[C;H0;D3;+0:4]1-[C:11](-[#8:12]-[C:13]=[O;D1;H0:14])-[C:7](-[#8:8]-[C:9]=[O;D1;H0:10])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:1]-1-[O;D1;H1:2]
87.1
[{"value": 87.0, "product": "ON1C([C@@H]([C@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.1, "product": "ON1C([C@@H]([C@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
4
CELSIUS
1
HOUR
To a 3-neck 5 L round bottom flask fitted with a mechanical stirrer and a teflon coated temperature probe was added (22) (2.79 mol) followed by acetonitrile (2 L). The suspension was cooled in an ice bath to 4° C., followed by the addition of 50% aqueous hydroxylamine (180 mL, 2.93 mol) over 1 h. The starting material ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Tertiary amide.Tertiary amide
C1CCOC1
C1CC[NH]C1
C1CC[NH]C1.c1ccccc1.c1ccccc1
HO-
C1(=CC=CC=C1)C
4
1
NO.O=C(O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1>C1(=CC=CC=C1)C>O=C(O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-152e443356ff434289acdc7b1da08d2d
CSC(=O)OOC(OC(=O)C(C)C)C(C)C.O=C(O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1>>CC(C)C(=O)O[C@@H](OC(=O)ON1C(=O)[C@H](OC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)C1=O)C(C)C
C(OOC(C(C)C)OC(C(C)C)=O)(SC)=O.ON1C([C@@H]([C@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O.C(C)(=O)OO.C(C)(=O)O>>CC(C(=O)O[C@H](C(C)C)OC(=O)ON1C([C@@H]([C@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O)C
CS[C:9](O[O:8][CH:7]([O:6][C:4]([CH:2]([CH3:1])[CH3:3])=[O:5])[CH:37]([CH3:38])[CH3:39])=[O:10].[OH:11][N:12]1[C:13](=[O:14])[C@H:15]([O:16][C:17](=[O:18])[c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[C@@H:25]([O:26][C:27](=[O:28])[c:29]2[cH:30][cH:31][cH:32][cH:33][cH:34]2)[C:35]1=[O:36]>>[CH3:1][CH:2]([CH3:3])[C:4](=[...
CSC(=O)OOC(OC(=O)C(C)C)C(C)C.O=C(O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
CC(C)C(=O)O[C@@H](OC(=O)ON1C(=O)[C@H](OC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)C1=O)C(C)C
null
null
ClCCCl
Acylation
OtherReaction
1a0d65d95c03f609c9ba14e788b1ef64da345e59cee201a8100967aef66d4c98
b8c84c3e0ba8877f8793c358e95ebb320bfaabe7f65a860968c1a83a5d892903
O=C(O[C@H]1C(=O)NC(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
C-S-[C;H0;D3;+0:1](=[O;D1;H0:2])-O-[O;H0;D2;+0:3]-[CH;D3;+0:4](-[#8:5]-[C:6](-[C:7])=[O;D1;H0:8])-[C:9](-[C;D1;H3:10])-[C;D1;H3:11].[O;D1;H0:12]=[C:13]1-[C:14]-[C:15]-[C:16](=[O;D1;H0:17])-[#7:18]-1-[OH;D1;+0:19]>>[C:7]-[C:6](=[O;D1;H0:8])-[#8:5]-[C@@H;D3;+0:4](-[O;H0;D2;+0:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:1...
25
[{"value": 25.0, "product": "CC(C(=O)O[C@H](C(C)C)OC(=O)ON1C([C@@H]([C@H](C1=O)OC(C1=CC=CC=C1)=O)OC(C1=CC=CC=C1)=O)=O)C", "details": "PERCENTYIELD", "is_desired": false}]
15
CELSIUS
null
null
A 3 L three necked round bottom flask fitted with a mechanical stirrer, teflon coated temperature probe and an addition funnel was charged with (13) (234 g, 1 mol), (23) (330 g, 0.95 mol), and 1,2-dichloroethane (2200 mL). The reaction mixture was cooled under a nitrogen atmosphere in an ice water bath to 15° C. To the...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Monosulfide
Ether
null
null
C1CC[NH]C1.c1ccccc1.c1ccccc1
Other
ClCCCl
15
null
CSC(=O)OOC(OC(=O)C(C)C)C(C)C.O=C(O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)c1ccccc1)c1ccccc1>ClCCCl>CC(C)C(=O)O[C@@H](OC(=O)ON1C(=O)[C@H](OC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)C1=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-bc9f4510ccde47d884e6fab83b6a1ae2
CC(C)C(=O)Cl.O=C(O)[C@H](O)[C@@H](O)C(=O)O>>CC(C)C(=O)O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)C(C)C
C([C@H](O)[C@@H](O)C(=O)O)(=O)O.C(C(C)C)(=O)Cl>>O=C1OC([C@@H]([C@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O
Cl[C:4]([CH:2]([CH3:1])[CH3:3])=[O:5].[OH:6][C@@H:19]([C:7](=[O:9])[OH:10])[C@@H:17]([OH:12])[C:15]([OH:14])=[O:16]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[O:6][C@H:7]1[C:8](=[O:9])[O:10][C:11](=[O:12])[C@@H:13]1[O:14][C:15](=[O:16])[CH:17]([CH3:18])[CH3:19]
CC(C)C(=O)Cl.O=C(O)[C@H](O)[C@@H](O)C(=O)O
CC(C)C(=O)O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)C(C)C
null
null
CCCCCC.CCOCC.C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
97e945862434d253355980141463740476b1aa5c4b8db8c31d16a34baf59ec6b
e0cfefbc9524ccf2e9a1480627bd015eb0fec489618391d800bcffef29909ee4
O=C1CCC(=O)O1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[C;D1;H3:5].[O;D1;H0:6]=[C:7](-[OH;D1;+0:8])-[C@H;D3;+0:9](-[OH;D1;+0:10])-[C@@H;D3;+0:11](-[OH;D1;+0:12])-[C;H0;D3;+0:13](=[O;H0;D1;+0:14])-[OH;D1;+0:15]>>[C;D1;H3:16]-[CH;D3;+0:9](-[CH3;D1;+0:11])-[C:7](=[O;D1;H0:6])-[O;H0;D2;+0:8]-[C:17]1-[C:18](=[O;H0;D1;+0:10])-[...
71
[{"value": 71.0, "product": "O=C1OC([C@@H]([C@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.6, "product": "O=C1OC([C@@H]([C@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
22
HOUR
To a suspension of L-tartaric acid (5.0 g, 33.3 mmol) in toluene (60 mL) was added isobutyryl chloride (11.3 mL, 107 mmol). The resulting suspension was heated to reflux and stirred for 22 h at reflux temperature. The reaction mixture was then concentrated in vacuo to afford a crystalline solid, which was suspended in ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Carboxylic acid.Carboxylic acid.Secondary alcohol.Secondary alcohol
Anhydride.Ester.Ester
null
C1CCOC1
C1CCOC1
null
CCCCCC.CCOCC.C1(=CC=CC=C1)C
null
22
CC(C)C(=O)Cl.O=C(O)[C@H](O)[C@@H](O)C(=O)O>CCCCCC.CCOCC.C1(=CC=CC=C1)C>CC(C)C(=O)O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6e46d3d6429541e5b8d2ad8aa41254d4
CC(C)C(=O)O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)C(C)C.NO>>CC(C)C(=O)O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)C(C)C
O=C1OC([C@@H]([C@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O.NO>>ON1C([C@@H]([C@H](C1=O)OC(C(C)C)=O)OC(C(C)C)=O)=O
O1[C:8](=[O:9])[C@H:7]([O:6][C:4]([CH:2]([CH3:1])[CH3:3])=[O:5])[C@@H:14]([O:15][C:16](=[O:17])[CH:18]([CH3:19])[CH3:20])[C:12]1=[O:13].[NH2:10][OH:11]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[O:6][C@H:7]1[C:8](=[O:9])[N:10]([OH:11])[C:12](=[O:13])[C@@H:14]1[O:15][C:16](=[O:17])[CH:18]([CH3:19])[CH3:20]
CC(C)C(=O)O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)C(C)C.NO
CC(C)C(=O)O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)C(C)C
null
null
C(C)(=O)OCC
Acylation
OtherReaction
ac5f63bba60d4a1d0330a86ebe6d3207e2dd9014985e5a45540d3ddb5de76511
f570959c6614f83205be0ddef7485420f00ece3dc52d54ad514eee7326c7fc88
O=C1CCC(=O)N1
[NH2;D1;+0:1]-[O;D1;H1:2].[O;D1;H0:3]=[C;H0;D3;+0:4]1-O-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C:7](-[#8:8]-[C:9]=[O;D1;H0:10])-[C:11]-1-[#8:12]-[C:13]=[O;D1;H0:14]>>[O;D1;H0:3]=[C;H0;D3;+0:4]1-[C:11](-[#8:12]-[C:13]=[O;D1;H0:14])-[C:7](-[#8:8]-[C:9]=[O;D1;H0:10])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:1]-1-[O;D1;H1:2]
99.7
[{"value": 99.7, "product": "ON1C([C@@H]([C@H](C1=O)OC(C(C)C)=O)OC(C(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a stirred solution of compound (27) (5.98 g, 22 mmol) in ethyl acetate (50 mL) at 0° C. was added a 50% aqueous solution of hydroxylamine (1.75 g, 26.4 mmol). The resulting mixture was stirred at room temperature for 3 h and washed successively with aqueous citric acid solution and brine, then dried over anhydrous s...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Tertiary amide.Tertiary amide
C1CCOC1
C1CC[NH]C1
C1CC[NH]C1
HO-
C(C)(=O)OCC
null
3
CC(C)C(=O)O[C@H]1C(=O)OC(=O)[C@@H]1OC(=O)C(C)C.NO>C(C)(=O)OCC>CC(C)C(=O)O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-4c6e1195c4934a40a35ac509c0a478ad
CC(C)C(=O)Cl.O=C(O)[C@@H](O)[C@H](O)C(=O)O>>CC(C)C(=O)O[C@@H]1C(=O)OC(=O)[C@H]1OC(=O)C(C)C
C([C@@H](O)[C@H](O)C(=O)O)(=O)O.C(C(C)C)(=O)Cl>>O=C1OC([C@H]([C@@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O
Cl[C:4]([CH:2]([CH3:1])[CH3:8])=[O:5].[OH:6][C@@H:17]([C@@H:13]([C:11]([OH:10])=[O:12])[OH:14])[C:15](=[O:9])[OH:16]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[O:6][C@@H:7]1[C:8](=[O:9])[O:10][C:11](=[O:12])[C@H:13]1[O:14][C:15](=[O:16])[CH:17]([CH3:18])[CH3:19]
CC(C)C(=O)Cl.O=C(O)[C@@H](O)[C@H](O)C(=O)O
CC(C)C(=O)O[C@@H]1C(=O)OC(=O)[C@H]1OC(=O)C(C)C
null
null
CCCCCC.CCOCC.C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
97e945862434d253355980141463740476b1aa5c4b8db8c31d16a34baf59ec6b
e0cfefbc9524ccf2e9a1480627bd015eb0fec489618391d800bcffef29909ee4
O=C1CCC(=O)O1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3](-[C;D1;H3:4])-[CH3;D1;+0:5].[O;D1;H0:6]=[C:7](-[OH;D1;+0:8])-[C@@H;D3;+0:9](-[OH;D1;+0:10])-[C@H;D3;+0:11](-[OH;D1;+0:12])-[C;H0;D3;+0:13](=[O;H0;D1;+0:14])-[OH;D1;+0:15]>>[C;D1;H3:16]-[CH;D3;+0:11](-[C;D1;H3:17])-[C;H0;D3;+0:13](=[O;H0;D1;+0:15])-[O;H0;D2;+0:10]-[C@@H;D3;+0...
71
[{"value": 71.0, "product": "O=C1OC([C@H]([C@@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.6, "product": "O=C1OC([C@H]([C@@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
22
HOUR
To a suspension of D-tartaric acid (5.0 g, 33.3 mmol) in toluene (60 mL) was added isobutyryl chloride (11.3 mL, 107 mmol). The resulting suspension was heated to reflux and stirred for 22 h at reflux temperature. The reaction mixture was then concentrated in vacuo to afford a crystalline solid, which was suspended in ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Carboxylic acid.Carboxylic acid.Secondary alcohol.Secondary alcohol
Anhydride.Ester.Ester
null
C1CCOC1
C1CCOC1
null
CCCCCC.CCOCC.C1(=CC=CC=C1)C
null
22
CC(C)C(=O)Cl.O=C(O)[C@@H](O)[C@H](O)C(=O)O>CCCCCC.CCOCC.C1(=CC=CC=C1)C>CC(C)C(=O)O[C@@H]1C(=O)OC(=O)[C@H]1OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-0ff82f6f7829463cb3550f7d496a4e54
CC(C)C(=O)O[C@@H]1C(=O)OC(=O)[C@H]1OC(=O)C(C)C.NO>>CC(C)C(=O)O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)C(C)C
O=C1OC([C@H]([C@@H]1OC(C(C)C)=O)OC(C(C)C)=O)=O.NO>>ON1C([C@@H]([C@H](C1=O)OC(C(C)C)=O)OC(C(C)C)=O)=O
O1[C:8](=[O:9])[C@@H:7]([O:6][C:4]([CH:2]([CH3:1])[CH3:3])=[O:5])[C@H:14]([O:15][C:16](=[O:17])[CH:18]([CH3:19])[CH3:20])[C:12]1=[O:13].[NH2:10][OH:11]>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[O:6][C@H:7]1[C:8](=[O:9])[N:10]([OH:11])[C:12](=[O:13])[C@@H:14]1[O:15][C:16](=[O:17])[CH:18]([CH3:19])[CH3:20]
CC(C)C(=O)O[C@@H]1C(=O)OC(=O)[C@H]1OC(=O)C(C)C.NO
CC(C)C(=O)O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)C(C)C
null
null
C(C)(=O)OCC
Acylation
OtherReaction
ac5f63bba60d4a1d0330a86ebe6d3207e2dd9014985e5a45540d3ddb5de76511
f570959c6614f83205be0ddef7485420f00ece3dc52d54ad514eee7326c7fc88
O=C1CCC(=O)N1
[NH2;D1;+0:1]-[O;D1;H1:2].[O;D1;H0:3]=[C;H0;D3;+0:4]1-O-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C:7](-[#8:8]-[C:9]=[O;D1;H0:10])-[C:11]-1-[#8:12]-[C:13]=[O;D1;H0:14]>>[O;D1;H0:3]=[C;H0;D3;+0:4]1-[C:11](-[#8:12]-[C:13]=[O;D1;H0:14])-[C:7](-[#8:8]-[C:9]=[O;D1;H0:10])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[N;H0;D3;+0:1]-1-[O;D1;H1:2]
99.7
[{"value": 99.7, "product": "ON1C([C@@H]([C@H](C1=O)OC(C(C)C)=O)OC(C(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a stirred solution of compound (30) (5.98 g, 22 mmol) in ethyl acetate (50 mL) at 0° C. was added a 50% aqueous solution of hydroxylamine (1.75 g, 26.4 mmol). The resulting mixture was stirred at room temperature for 3 h and washed successively with aqueous citric acid solution and brine, then dried over anhydrous s...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Tertiary amide.Tertiary amide
C1CCOC1
C1CC[NH]C1
C1CC[NH]C1
HO-
C(C)(=O)OCC
null
3
CC(C)C(=O)O[C@@H]1C(=O)OC(=O)[C@H]1OC(=O)C(C)C.NO>C(C)(=O)OCC>CC(C)C(=O)O[C@H]1C(=O)N(O)C(=O)[C@@H]1OC(=O)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-68d18f1c220342eb93c6beaf327191d9
CC(C)(C)OC(=O)N(CCCl)CCCl.N#CCc1ccc(Br)cc1>>CC(C)(C)OC(=O)N1CCC(C#N)(c2ccc(Br)cc2)CC1
C(C)(C)(C)OC(N(CCCl)CCCl)=O.BrC1=CC=C(C=C1)CC#N.[OH-].[Na+]>>C(C)(C)(C)OC(=O)N1CCC(CC1)(C#N)C1=CC=C(C=C1)Br
Cl[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:22][CH2:21]Cl.[CH2:11]([C:12]#[N:13])[c:14]1[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[CH2:9][CH2:10][C:11]([C:12]#[N:13])([c:14]2[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]2)[CH2:21][C...
CC(C)(C)OC(=O)N(CCCl)CCCl.N#CCc1ccc(Br)cc1
CC(C)(C)OC(=O)N1CCC(C#N)(c2ccc(Br)cc2)CC1
null
[Br-].C(CCCCCCCCCCCCCCC)[P+](CCCC)(CCCC)CCCC
O.C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
43554b849de36f518831bb4a87fa13a0a0525fa0929a0f498da9e7a024251318
7b68950fc1047c59bb49c25e850f5a51cbe91a99bb87839c4547aec123110e4b
c1ccc(C2CCNCC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#7:3](-[C:4]-[CH2;D2;+0:5]-Cl)-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[N;D1;H0:13]#[C:14]-[CH2;D2;+0:15]-[c:16](:[c:17]):[c:18]>>[C;D1;H3:10]-[C:9](-[C;D1;H3:11])(-[C;D1;H3:12])-[#8:8]-[C:6](=[O;D1;H0:7])-[#7:3]1-[C:4]-[CH2;D2;+0:5]-[C;H0;D4;+0:15](-[C:14]#[N...
51.7
[{"value": 51.7, "product": "C(C)(C)(C)OC(=O)N1CCC(CC1)(C#N)C1=CC=C(C=C1)Br", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
110
CELSIUS
null
null
To a mixture of bis-(2-chloro-ethyl)-carbamic acid tert-butyl ester from Step 1 (7.26 g, 30 mmol, 1 eq) and 4-bromophenylacetonitrile (5.88 g, 30 mmol, 1 eq) in 38 mL of toluene and 76 mL of H2O was added NaOH (45.6 g, 114 mmol, 10M solution) followed by hexadecyltributylphosphonium bromide (3.0 g, 6.0 mmol, 0.2 eq). T...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide
null
null
C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1
HCl
[Br-].C(CCCCCCCCCCCCCCC)[P+](CCCC)(CCCC)CCCC.O.C1(=CC=CC=C1)C
110
null
CC(C)(C)OC(=O)N(CCCl)CCCl.N#CCc1ccc(Br)cc1>[Br-].C(CCCCCCCCCCCCCCC)[P+](CCCC)(CCCC)CCCC.O.C1(=CC=CC=C1)C>CC(C)(C)OC(=O)N1CCC(C#N)(c2ccc(Br)cc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-26a28e9c09a047ae98dac8af6f50f05b
CC(C)(C)OC(=O)N1CCC(C#N)(c2ccc(Br)cc2)CC1.CO>>CC(C)(C)OC(=O)N1CCC(CC=O)(c2ccc(Br)cc2)CC1
CO.C(C)(C)(C)OC(=O)N1CCC(CC1)(C#N)C1=CC=C(C=C1)Br.CC(C)C[AlH]CC(C)C>>C(C)(C)(C)OC(=O)N1CCC(CC1)(CC=O)C1=CC=C(C=C1)Br
N#[C:12][C:11]1([c:15]2[cH:16][cH:17][c:18]([Br:19])[cH:20][cH:21]2)[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:23][CH2:22]1.[CH3:13][OH:14]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[CH2:9][CH2:10][C:11]([CH2:12][CH:13]=[O:14])([c:15]2[cH:16][cH:17][c:18]([Br:19])[cH:20][cH:...
CC(C)(C)OC(=O)N1CCC(C#N)(c2ccc(Br)cc2)CC1.CO
CC(C)(C)OC(=O)N1CCC(CC=O)(c2ccc(Br)cc2)CC1
null
null
ClCCl
Acylation
OtherReaction
45f1c96b0d061e9d88e0edbdf02ce532f16c290d610672bf6fe832ab076c9bba
1c846c445000d2e843d2685c5a5c58e2e39afe4a0a6abbc76e5e576879a32701
c1ccc(C2CCNCC2)cc1
N#[C;H0;D2;+0:1]-[C:2](-[c:3])(-[C:4])-[C:5].[CH3;D1;+0:6]-[OH;D1;+0:7]>>[C:4]-[C:2](-[c:3])(-[CH2;D2;+0:1]-[CH;D2;+0:6]=[O;H0;D1;+0:7])-[C:5]
null
[]
null
null
20
HOUR
To a solution of 4-(4-bromo-phenyl)-4-cyano-piperidine-1-carboxylic acid tert-butyl ester from Step 2 (5.67 g, 15.57 mmol, 1 eq) in 60 mL of dichloromethane was add a solution of DIBAL-H (1M in toluene, 23.36 mL, 23.36 mmol, 1.5 eq) in a drop-wise fashion. The resulting mixture was stirred at room temperature for 20 h ...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Methanol
Aldehyde
null
null
C1CC[NH]CC1.c1ccccc1
Other
ClCCl
null
20
CC(C)(C)OC(=O)N1CCC(C#N)(c2ccc(Br)cc2)CC1.CO>ClCCl>CC(C)(C)OC(=O)N1CCC(CC=O)(c2ccc(Br)cc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5eb68b1997cb44899342858bcb169ea0
CC(C)(C)OC(=O)N1CCC(CC=O)(c2ccc(Br)cc2)CC1>>CC(C)(C)OC(=O)N1CCC(CO)(c2ccc(Br)cc2)CC1
C(C)(C)(C)OC(=O)N1CCC(CC1)(CC=O)C1=CC=C(C=C1)Br.[BH4-].[Na+].C(C)(C)O>>C(C)(C)(C)OC(=O)N1CCC(CC1)(CO)C1=CC=C(C=C1)Br
C([CH2:12][C:11]1([c:14]2[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]2)[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:22][CH2:21]1)=[O:13]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[CH2:9][CH2:10][C:11]([CH2:12][OH:13])([c:14]2[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]2)[CH2:21]...
CC(C)(C)OC(=O)N1CCC(CC=O)(c2ccc(Br)cc2)CC1
CC(C)(C)OC(=O)N1CCC(CO)(c2ccc(Br)cc2)CC1
null
null
null
Miscellaneous
OtherReaction
165ea33990c9cff6d94955cdaafab084da8c9def01a31e920214b7759117f6ff
43cf4997d6e2488d8c69ca8bc684124ace6515563d3e08dcc47ef2a56dd17cc0
c1ccc(C2CCNCC2)cc1
[C:1]-[C:2](-[c:3])(-[CH2;D2;+0:4]-C=[O;H0;D1;+0:5])-[C:6]>>[C:1]-[C:2](-[c:3])(-[CH2;D2;+0:4]-[OH;D1;+0:5])-[C:6]
null
[]
null
null
20
HOUR
To a solution of 1.78 g of 4-(4-bromo-phenyl)-4-hydroxymethyl-piperidine-1-carboxylic acid tert-butyl ester from Step 3 (4.85 mmol, 1 eq) in 25 mL of isopropanol was added NaBH4 (0.201 g, 5.33 mmol, 1.1 eq). The mixture was stirred at room temperature for 20 h and then quenched by the addition of aqueous HCl (20 mL) to...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
C1CC[NH]CC1.c1ccccc1
Other
null
null
20
CC(C)(C)OC(=O)N1CCC(CC=O)(c2ccc(Br)cc2)CC1>>CC(C)(C)OC(=O)N1CCC(CO)(c2ccc(Br)cc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e63f3163b5de49a88ff24da4241e7ea5
CC(C)(C)OC(=O)N1CCC(c2ccc(Br)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1.N#Cc1cccc(B(O)O)c1>>CC(C)(C)OC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1
C(C)(C)(C)OC(=O)N1CCC(CC1)(C(COCC[Si](C)(C)C)OC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)Br.C(#N)C=1C=C(C=CC1)B(O)O.C1(=CC=CC=C1)C.C(=O)([O-])[O-].[Na+].[Na+]>>C(C)(C)(C)OC(=O)N1CCC(CC1)(C(COCC[Si](C)(C)C)OC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N
Br[c:15]1[cH:14][cH:13][c:12]([C:11]2([CH:26]([CH2:27][O:28][CH2:29][CH2:30][Si:31]([CH3:32])([CH3:33])[CH3:34])[O:35][c:36]3[n:37][c:38]4[cH:39][c:40]([Cl:41])[c:42]([Cl:43])[cH:44][c:45]4[nH:46]3)[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:48][CH2:47]2)[cH:25][cH:24]1.OB(O)[c:16]1[cH:17...
CC(C)(C)OC(=O)N1CCC(c2ccc(Br)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1.N#Cc1cccc(B(O)O)c1
CC(C)(C)OC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1
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
C(C)(=O)OCC.C(C)O
C-C Coupling
Suzuki coupling with boronic acids
d79a78c79f0c392f0911481acf5c300cc98205269acdb93c24fb610a61c4c868
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccc(C3(COc4nc5ccccc5[nH]4)CCNCC3)cc2)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:3]:[c:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
79.5
[{"value": 79.5, "product": "C(C)(C)(C)OC(=O)N1CCC(CC1)(C(COCC[Si](C)(C)C)OC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A mixture of 0.105 g of 4-(4-bromo-phenyl)-4-[5,6-dichloro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yloxymethyl]-piperidine-1-carboxylic acid tert-butyl ester 51 (0.144 mmol, 1 eq), 0.024 g of 3-cyanophenyl boronic acid (0.16 mmol, 1.1 eq), and 0.034 g of Pd(PPh3)4 (0.03 mmol, 20 mol %) was mixed with 3 m...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1ccc2[nH]cnc2c1
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.C(C)(=O)OCC.C(C)O
80
null
CC(C)(C)OC(=O)N1CCC(c2ccc(Br)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1.N#Cc1cccc(B(O)O)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.C(C)(=O)OCC.C(C)O>CC(C)(C)OC(=O)N1CCC(c2ccc(-c3c...
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-488c2532ff4e4cd5b0402a9995a20f8e
CC(C)(C)OC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1>>CC(C)(C)OC(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
C(C)(C)(C)OC(=O)N1CCC(CC1)(C(COCC[Si](C)(C)C)OC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N.CCCC[N+](CCCC)(CCCC)CCCC.[F-]>>C(C)(C)(C)OC(=O)N1CCC(CC1)(COC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N
C[Si](C)(C)CCOC[CH:12]([C:11]1([c:25]2[cH:26][cH:27][c:28](-[c:29]3[cH:30][cH:31][cH:32][c:33]([C:34]#[N:35])[cH:36]3)[cH:37][cH:38]2)[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:40][CH2:39]1)[O:13][c:14]1[n:15][c:16]2[cH:17][c:18]([Cl:19])[c:20]([Cl:21])[cH:22][c:23]2[nH:24]1>>[CH3:1][C:2...
CC(C)(C)OC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1
CC(C)(C)OC(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
null
null
O1CCCC1
Reduction
OtherReaction
d69c6d61640e32f10824c7c1514f3119c2d4874c1389751d2577a99972bf959d
9abd1fd0aee638213302f50e544d5b4119741bd519771ef99d13ceeb790018fc
c1ccc(-c2ccc(C3(COc4nc5ccccc5[nH]4)CCNCC3)cc2)cc1
C-[Si](-C)(-C)-C-C-O-C-[CH;D3;+0:1](-[#8:2]-[c:3](:[#7;a:4]):[#7;a:5])-[C:6](-[c:7])(-[C:8])-[C:9]>>[#7;a:4]:[c:3](-[#8:2]-[CH2;D2;+0:1]-[C:6](-[c:7])(-[C:8])-[C:9]):[#7;a:5]
52.7
[{"value": 52.7, "product": "C(C)(C)(C)OC(=O)N1CCC(CC1)(COC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a solution of 0.081 g of 4-(3′-cyano-biphenyl-4-yl)-4-[5,6-dichloro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yloxymethyl]-piperidine-1-carboxylic acid tert-butyl ester 52 (0.115 mmol) in 5 mL of tetrahydrofuran at room temperature was added 0.23 mL of a solution of TBAF (1M in THF, 0.23 mmol, 2 eq). Th...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Silyl protective group
Ether
null
null
C1CC[NH]CC1.c1ccc2[nH]cnc2c1.c1ccccc1.c1ccccc1
HO-
O1CCCC1
60
null
CC(C)(C)OC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1>O1CCCC1>CC(C)(C)OC(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-833505e716b6420083758a04c4baeb6d
CC(C)(C)OC(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1>>N#Cc1cccc(-c2ccc(C3(COc4nc5cc(Cl)c(Cl)cc5[nH]4)CCNCC3)cc2)c1
C(C)(C)(C)OC(=O)N1CCC(CC1)(COC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N.FC(C(=O)O)(F)F>>ClC1=CC2=C(NC(=N2)OCC2(CCNCC2)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl
CC(C)(C)OC(=O)[N:28]1[CH2:27][CH2:26][C:12]([c:11]2[cH:10][cH:9][c:8](-[c:7]3[cH:6][cH:5][cH:4][c:3]([C:2]#[N:1])[cH:33]3)[cH:32][cH:31]2)([CH2:13][O:14][c:15]2[n:16][c:17]3[cH:18][c:19]([Cl:20])[c:21]([Cl:22])[cH:23][c:24]3[nH:25]2)[CH2:30][CH2:29]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11](...
CC(C)(C)OC(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
N#Cc1cccc(-c2ccc(C3(COc4nc5cc(Cl)c(Cl)cc5[nH]4)CCNCC3)cc2)c1
null
null
ClCCl.C1(=CC=CC=C1)C
Reduction
Boc amine deprotection
bf3cd5dc3e17e694d8665c89f5d7e08e8763b18436a633eb66e9bf530b8b0316
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
c1ccc(-c2ccc(C3(COc4nc5ccccc5[nH]4)CCNCC3)cc2)cc1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C:5]>>[C:3]-[C:2]-[NH;D2;+0:1]-[C:4]-[C:5]
91
[{"value": 91.0, "product": "ClC1=CC2=C(NC(=N2)OCC2(CCNCC2)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
2
HOUR
To a solution of 0.015 g of 4-(3′-cyano-biphenyl-4-yl)-4-(5,6-dichloro-1H-benzoimidazol-2-yloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester 53 (0.026 mmol) in 3 mL of dichloromethane at 0° C. was added 1 mL of trifluoroacetic acid. The mixture was stirred at 0° C. for 2 h then diluted with 10 mL of toluene and...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
C1CC[NH]CC1
C1CCNCC1
c1ccccc1.c1ccccc1.c1ccc2[nH]cnc2c1.C1CCNCC1
HO-
ClCCl.C1(=CC=CC=C1)C
0
2
CC(C)(C)OC(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1>ClCCl.C1(=CC=CC=C1)C>N#Cc1cccc(-c2ccc(C3(COc4nc5cc(Cl)c(Cl)cc5[nH]4)CCNCC3)cc2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-1b2ab63d2f4d41b7b48473b6d268090e
CS(=O)(=O)Cl.C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1>>C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(S(C)(=O)=O)CC1
ClC1=CC2=C(NC(=N2)OC(COCC[Si](C)(C)C)C2(CCNCC2)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl.CS(=O)(=O)Cl.CCN(C(C)C)C(C)C>>ClC1=CC2=C(NC(=N2)OC(COCC[Si](C)(C)C)C2(CCN(CC2)S(=O)(=O)C)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl
Cl[S:40]([CH3:41])(=[O:42])=[O:43].[CH3:1][Si:2]([CH3:3])([CH3:4])[CH2:5][CH2:6][O:7][CH2:8][CH:9]([O:10][c:11]1[n:12][c:13]2[cH:14][c:15]([Cl:16])[c:17]([Cl:18])[cH:19][c:20]2[nH:21]1)[C:22]1([c:23]2[cH:24][cH:25][c:26](-[c:27]3[cH:28][cH:29][cH:30][c:31]([C:32]#[N:33])[cH:34]3)[cH:35][cH:36]2)[CH2:37][CH2:38][NH:39][...
CS(=O)(=O)Cl.C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1
C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(S(C)(=O)=O)CC1
null
null
ClCCl.C(C)(=O)OCC
Acylation
Sulfonamide synthesis (Schotten-Baumann) secondary amine
d63e07b47df62aebedb35134f6d0504cfcbed5ccfdec31c2c42bba6875c15fe7
b7aca5a5d690b0846685a854bc946849e1041bfc3965161290b5ffb2821af09e
c1ccc(-c2ccc(C3(COc4nc5ccccc5[nH]4)CCNCC3)cc2)cc1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4])-[C:8]-[C:9]
128.3
[{"value": 128.3, "product": "ClC1=CC2=C(NC(=N2)OC(COCC[Si](C)(C)C)C2(CCN(CC2)S(=O)(=O)C)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of 0.030 g of 4′-{4-[5,6-dichloro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yloxymethyl]-piperidin-4-yl}-biphenyl-3-carbonitrile (0.05 mmol) 55 in 1 mL of dichloromethane was added methanesulfonyl chloride (0.005 mL, 0.053 mmol, 1.1 eq) and DIEA (0.011 mL, 0.06 mmol, 1.2 eq). The resulting mi...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Sulfonyl halide
Tertiary amine
C1CCNCC1
C1CC[NH]CC1
c1ccc2[nH]cnc2c1.c1ccccc1.c1ccccc1.C1CC[NH]CC1
HCl
ClCCl.C(C)(=O)OCC
null
16
CS(=O)(=O)Cl.C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1>ClCCl.C(C)(=O)OCC>C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(S(C)(=O)=O)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-fb978749489047c8a4be6a0bfb025eb6
C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(S(C)(=O)=O)CC1>>CS(=O)(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
ClC1=CC2=C(NC(=N2)OC(COCC[Si](C)(C)C)C2(CCN(CC2)S(=O)(=O)C)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>ClC1=CC2=C(NC(=N2)OCC2(CCN(CC2)S(=O)(=O)C)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl
C[Si](C)(C)CCOC[CH:9]([C:8]1([c:22]2[cH:23][cH:24][c:25](-[c:26]3[cH:27][cH:28][cH:29][c:30]([C:31]#[N:32])[cH:33]3)[cH:34][cH:35]2)[CH2:7][CH2:6][N:5]([S:2]([CH3:1])(=[O:3])=[O:4])[CH2:37][CH2:36]1)[O:10][c:11]1[n:12][c:13]2[cH:14][c:15]([Cl:16])[c:17]([Cl:18])[cH:19][c:20]2[nH:21]1>>[CH3:1][S:2](=[O:3])(=[O:4])[N:5]1...
C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(S(C)(=O)=O)CC1
CS(=O)(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
null
null
O1CCCC1.C(C)(=O)OCC
Reduction
OtherReaction
d69c6d61640e32f10824c7c1514f3119c2d4874c1389751d2577a99972bf959d
9abd1fd0aee638213302f50e544d5b4119741bd519771ef99d13ceeb790018fc
c1ccc(-c2ccc(C3(COc4nc5ccccc5[nH]4)CCNCC3)cc2)cc1
C-[Si](-C)(-C)-C-C-O-C-[CH;D3;+0:1](-[#8:2]-[c:3](:[#7;a:4]):[#7;a:5])-[C:6](-[c:7])(-[C:8])-[C:9]>>[#7;a:4]:[c:3](-[#8:2]-[CH2;D2;+0:1]-[C:6](-[c:7])(-[C:8])-[C:9]):[#7;a:5]
44.9
[{"value": 44.9, "product": "ClC1=CC2=C(NC(=N2)OCC2(CCN(CC2)S(=O)(=O)C)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a solution of 0.044 g of crude 4′-{4-[5,6-dichloro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yloxymethyl]-1-methanesulfonyl-piperidin-4-yl}-biphenyl-3-carbonitrile from the previous step (˜0.05 mmol) in 2 mL of tetrahydrofuran was added tetrabutylammonium fluoride (1M in THF, 0.1 mL, 0.1 mmol, 2 eq) and...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Silyl protective group
Ether
null
null
C1CC[NH]CC1.c1ccc2[nH]cnc2c1.c1ccccc1.c1ccccc1
HO-
O1CCCC1.C(C)(=O)OCC
60
null
C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(S(C)(=O)=O)CC1>O1CCCC1.C(C)(=O)OCC>CS(=O)(=O)N1CCC(COc2nc3cc(Cl)c(Cl)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-964e54fb5eef4dc182fd8e148150cfcc
C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1.O=CC1CC1>>N#Cc1cccc(-c2ccc(C3(COc4nc5cc(Cl)c(Cl)cc5[nH]4)CCN(CC4CC4)CC3)cc2)c1
[F-].C(CCC)[N+](CCCC)(CCCC)CCCC.ClC1=CC2=C(NC(=N2)OC(COCC[Si](C)(C)C)C2(CCNCC2)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl.C1(CC1)C=O.[BH-](OC(=O)C)(OC(=O)C)OC(=O)C.[Na+]>>C1(CC1)CN1CCC(CC1)(COC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N
C[Si](C)(C)CCOC[CH:13]([C:12]1([c:11]2[cH:10][cH:9][c:8](-[c:7]3[cH:6][cH:5][cH:4][c:3]([C:2]#[N:1])[cH:37]3)[cH:36][cH:35]2)[CH2:26][CH2:27][NH:28][CH2:33][CH2:34]1)[O:14][c:15]1[n:16][c:17]2[cH:18][c:19]([Cl:20])[c:21]([Cl:22])[cH:23][c:24]2[nH:25]1.O=[CH:29][CH:30]1[CH2:31][CH2:32]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][cH...
C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1.O=CC1CC1
N#Cc1cccc(-c2ccc(C3(COc4nc5cc(Cl)c(Cl)cc5[nH]4)CCN(CC4CC4)CC3)cc2)c1
null
null
O1CCCC1.C(C)(=O)O.ClCCCl
Heteroatom Alkylation and Arylation
OtherReaction
e0f1d8750a019670f4994afcb1f27f4754623b9b5337e7e6204abafbfacdbec3
b742e0f5cea8d7b3d9fda93d9d894c14daa01ac5e15c5823be8f1ecad641ca82
c1ccc(-c2ccc(C3(COc4nc5ccccc5[nH]4)CCN(CC4CC4)CC3)cc2)cc1
C-[Si](-C)(-C)-C-C-O-C-[CH;D3;+0:1](-[#8:2]-[c:3](:[#7;a:4]):[#7;a:5])-[C:6]1(-[c:7])-[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]-1.O=[CH;D2;+0:13]-[C:14]1-[C:15]-[C:16]-1>>[#7;a:4]:[c:3](-[#8:2]-[CH2;D2;+0:1]-[C:6]1(-[c:7])-[C:8]-[C:9]-[N;H0;D3;+0:10](-[CH2;D2;+0:13]-[C:14]2-[C:15]-[C:16]-2)-[C:11]-[C:12]-1):[#7;a:5]
18
[{"value": 18.0, "product": "C1(CC1)CN1CCC(CC1)(COC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 0.045 g of 4′-{4-[5,6-dichloro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yloxymethyl]-piperidin-4-yl}-biphenyl-3-carbonitrile 55 (0.073 mmol, 1 eq) in 0.5 mL of 1,2-dichloroethane at room temperature was added 6.6 μL of cyclopropanecarboxaldehyde (0.088 mmol, 1.2 eq) and acetic acid (0.005...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ether.Ether.Secondary amine.Silyl protective group
Ether.Tertiary amine
C1CCNCC1
C1CC[NH]CC1
c1ccccc1.c1ccccc1.c1ccc2[nH]cnc2c1.C1CC[NH]CC1.C1CC1
HO-
O1CCCC1.C(C)(=O)O.ClCCCl
null
1
C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1.O=CC1CC1>O1CCCC1.C(C)(=O)O.ClCCCl>N#Cc1cccc(-c2ccc(C3(COc4nc5cc(Cl)c(Cl)cc5[nH]4)CCN(CC4CC4)CC3)cc2)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-63d2c51d78ef4c92b9fdbf9eed4b7d71
CCN=C=O.C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1>>CCNC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1
ClC1=CC2=C(NC(=N2)OC(COCC[Si](C)(C)C)C2(CCNCC2)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N)C=C1Cl.C(C)N=C=O.C(C)(C)N(CC)C(C)C>>C(C)NC(=O)N1CCC(CC1)(C(COCC[Si](C)(C)C)OC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N
[CH3:1][CH2:2][N:3]=[C:4]=[O:5].[NH:6]1[CH2:7][CH2:8][C:9]([c:10]2[cH:11][cH:12][c:13](-[c:14]3[cH:15][cH:16][cH:17][c:18]([C:19]#[N:20])[cH:21]3)[cH:22][cH:23]2)([CH:24]([CH2:25][O:26][CH2:27][CH2:28][Si:29]([CH3:30])([CH3:31])[CH3:32])[O:33][c:34]2[n:35][c:36]3[cH:37][c:38]([Cl:39])[c:40]([Cl:41])[cH:42][c:43]3[nH:44...
CCN=C=O.C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1
CCNC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1
null
null
ClCCl
Acylation
Urea synthesis via isocyanate and secondary amine
6a88f2fb12498f30b6ca536d46572ea3e28c2b70ddb4a5e5b0a05fe1e5e9bb8d
5272a383a93723269f1934f97993b0175b43cd993bcdf2f45add1dbb852d1e09
c1ccc(-c2ccc(C3(COc4nc5ccccc5[nH]4)CCNCC3)cc2)cc1
[C;D1;H3:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:3]-[C:2]-[C;D1;H3:1])-[C:9]-[C:10]
60.5
[{"value": 60.5, "product": "C(C)NC(=O)N1CCC(CC1)(C(COCC[Si](C)(C)C)OC1=NC2=C(N1)C=C(C(=C2)Cl)Cl)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a solution of 0.045 g of 4′-{4-[5,6-dichloro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-yloxymethyl]-piperidin-4-yl}-biphenyl-3-carbonitrile (0.073 mmol, 1 eq) in 0.7 mL of dichloromethane was added ethyl isocyanate (6.5 μL, 0.088 mmol, 1.2 eq) and 15.4 μL of diisopropylethyl amine (0.088 mmol, 1.2 eq) a...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Secondary amine
Urea
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1ccc2[nH]cnc2c1
null
ClCCl
null
16
CCN=C=O.C[Si](C)(C)CCOCC(Oc1nc2cc(Cl)c(Cl)cc2[nH]1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCNCC1>ClCCl>CCNC(=O)N1CCC(c2ccc(-c3cccc(C#N)c3)cc2)(C(COCC[Si](C)(C)C)Oc2nc3cc(Cl)c(Cl)cc3[nH]2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-aa810b331fbb4e18a986c0027bc5c8c1
Nc1ccc(F)c(F)c1N.O=C(O)CCl>>Fc1cc2nc(CCl)[nH]c2cc1F
FC=1C(=C(C=CC1F)N)N.ClCC(=O)O.[NH4+].[OH-]>>ClCC1=NC2=C(N1)C=C(C(=C2)F)F
[F:1][c:2]1[cH:3][cH:4][c:10]([NH2:9])[c:11]([NH2:5])[c:12]1[F:13].O=[C:6](O)[CH2:7][Cl:8]>>[F:1][c:2]1[cH:3][c:4]2[n:5][c:6]([CH2:7][Cl:8])[nH:9][c:10]2[cH:11][c:12]1[F:13]
Nc1ccc(F)c(F)c1N.O=C(O)CCl
Fc1cc2nc(CCl)[nH]c2cc1F
null
null
Cl
Aromatic Heterocycle Formation
OtherReaction
8409c8c0d4e4ea3a5ac4d357a90931cd25bdeaf070f3095e8e16fa38a40808ca
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
c1ccc2[nH]cnc2c1
O-[C;H0;D3;+0:1](=O)-[C:2]-[Cl;D1;H0:3].[F;D1;H0:4]-[c:5]1:[c:6]:[c:7]:[cH;D2;+0:8]:[c:9](-[NH2;D1;+0:10]):[c;H0;D3;+0:11]:1-[NH2;D1;+0:12]>>[Cl;D1;H0:3]-[C:2]-[c;H0;D3;+0:1]1:[n;H0;D2;+0:12]:[c;H0;D3;+0:8]2:[c:7]:[c:6]:[c:5](-[F;D1;H0:4]):[cH;D2;+0:11]:[c:9]:2:[nH;D2;+0:10]:1
null
[]
100
CELSIUS
null
null
A mixture of 1 g of 3,4-difluoro-1,2-phenylenediamine (6.94 mmol) and 0.983 g of chloro-acetic acid (10.41 mmol, 1.5 eq) in 13 mL of 4N aqueous HCl was heated to 100° C. for 3 h. The mixture was poured onto ice (10 g), neutralized by the addition of NH4OH and extracted with three 30 mL portions of ethyl acetate. The or...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
HO-
Cl
100
null
Nc1ccc(F)c(F)c1N.O=C(O)CCl>Cl>Fc1cc2nc(CCl)[nH]c2cc1F
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-55e345f3f73544e9a35091cfc8780b6a
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(Br)cc2)CC1.N#Cc1cccc(B(O)O)c1>>CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
C(C)(C)(C)OC(=O)N1CCC(CC1)(OCC1=NC2=C(N1COCC[Si](C)(C)C)C=C(C(=C2)F)F)C2=CC=C(C=C2)Br.C(#N)C=1C=C(C=CC1)B(O)O.C1(=CC=CC=C1)C.C(=O)([O-])[O-].[Na+].[Na+]>>C(C)(C)(C)OC(=O)N1CCC(CC1)(OCC1=NC2=C(N1COCC[Si](C)(C)C)C=C(C(=C2)F)F)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N
Br[c:36]1[cH:35][cH:34][c:33]([C:11]2([O:12][CH2:13][c:14]3[n:15][c:16]4[cH:17][c:18]([F:19])[c:20]([F:21])[cH:22][c:23]4[n:24]3[CH2:25][O:26][CH2:27][CH2:28][Si:29]([CH3:30])([CH3:31])[CH3:32])[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:48][CH2:47]2)[cH:46][cH:45]1.OB(O)[c:37]1[cH:38][cH...
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(Br)cc2)CC1.N#Cc1cccc(B(O)O)c1
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
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
C(C)(=O)OCC.C(C)O
C-C Coupling
Suzuki coupling with boronic acids
d79a78c79f0c392f0911481acf5c300cc98205269acdb93c24fb610a61c4c868
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccc(C3(OCc4nc5ccccc5[nH]4)CCNCC3)cc2)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:3]:[c:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
34.6
[{"value": 34.6, "product": "C(C)(C)(C)OC(=O)N1CCC(CC1)(OCC1=NC2=C(N1COCC[Si](C)(C)C)C=C(C(=C2)F)F)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A mixture of 0.116 g of 4-(4-bromo-phenyl)-4-[5,6-difluoro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-ylmethoxy]-piperidine-1-carboxylic acid tert-butyl ester 61 (˜0.18 mmol, 1 eq), 0.032 g of 3-cyanophenylboronic acid (0.215 mmol, 1.2 eq), and 0.040 g of Pd(PPh3)4 (0.036 mmol, 20 mol %) with 3 mL of toluen...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
C1CC[NH]CC1.c1ccc2[nH]cnc2c1.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.C(C)(=O)OCC.C(C)O
80
null
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(Br)cc2)CC1.N#Cc1cccc(B(O)O)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.C(C)(=O)OCC.C(C)O>CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)c...
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-7a22537c5391467097cb0b6136ff66c5
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(-c3cccc(C#N)c3)cc2)CC1>>CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
C(C)(C)(C)OC(=O)N1CCC(CC1)(OCC1=NC2=C(N1COCC[Si](C)(C)C)C=C(C(=C2)F)F)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>C(C)(C)(C)OC(=O)N1CCC(CC1)(OCC1=NC2=C(N1)C=C(C(=C2)F)F)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N
C[Si](C)(C)CCOC[n:24]1[c:14]([CH2:13][O:12][C:11]2([c:25]3[cH:26][cH:27][c:28](-[c:29]4[cH:30][cH:31][cH:32][c:33]([C:34]#[N:35])[cH:36]4)[cH:37][cH:38]3)[CH2:10][CH2:9][N:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:40][CH2:39]2)[n:15][c:16]2[cH:17][c:18]([F:19])[c:20]([F:21])[cH:22][c:23]21>>[CH3:1][C:2](...
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
null
null
O1CCCC1
Reduction
OtherReaction
8ce938c26df2ac3f48612e5a6fef893f0e283c99585c8225bd849efe3babbf31
d646edd3b1165ce8eea24b0587d24c565cf6371928b4879100704e7b3cd85ed9
c1ccc(-c2ccc(C3(OCc4nc5ccccc5[nH]4)CCNCC3)cc2)cc1
C-[Si](-C)(-C)-C-C-O-C-[n;H0;D3;+0:1]1:[c:2](-[C:3]):[#7;a:4]:[c:5](:[c:6]):[c:7]:1:[c:8]>>[C:3]-[c:2]1:[#7;a:4]:[c:5](:[c:6]):[c:7](:[c:8]):[nH;D2;+0:1]:1
91.8
[{"value": 91.8, "product": "C(C)(C)(C)OC(=O)N1CCC(CC1)(OCC1=NC2=C(N1)C=C(C(=C2)F)F)C2=CC=C(C=C2)C2=CC(=CC=C2)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
To a solution of 0.033 g of 4-(3′-cyano-biphenyl-4-yl)-4-[5,6-difluoro-1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzoimidazol-2-ylmethoxy]-piperidine-1-carboxylic acid tert-butyl ester 62 (0.05 mmol, 1 eq) in 2.5 mL of tetrahydrofuran was added 0.10 mL tetrabutylammonium fluoride (1M in THF, 0.1 mmol, 2 eq). The reaction...
10.6084/m9.figshare.5104873.v1
null
Ether.Silyl protective group
null
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
C1CC[NH]CC1.c1ccc2[nH]cnc2c1.c1ccccc1.c1ccccc1
HO-
O1CCCC1
null
20
CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3n2COCC[Si](C)(C)C)(c2ccc(-c3cccc(C#N)c3)cc2)CC1>O1CCCC1>CC(C)(C)OC(=O)N1CCC(OCc2nc3cc(F)c(F)cc3[nH]2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-931b01742a32446eb694fb362358701e
CN(C)C(=O)Nc1ccc(Cl)c(Cl)c1>>c1ccc2[nH]cnc2c1
[Na+].[Cl-].CN(C)C(=O)NC1=CC(=C(C=C1)Cl)Cl>>N1=CNC2=C1C=CC=C2
C[N:7](C)[C:6](=O)[NH:5][c:4]1[cH:3][cH:2][c:1](Cl)[c:9](Cl)[cH:8]1>>[cH:1]1[cH:2][cH:3][c:4]2[nH:5][cH:6][n:7][c:8]2[cH:9]1
CN(C)C(=O)Nc1ccc(Cl)c(Cl)c1
c1ccc2[nH]cnc2c1
null
null
C1CN(CCN1CCO)CCS(=O)(=O)O
Aromatic Heterocycle Formation
OtherReaction
4b372c4c7c90bef11a8b0c0147525f09ed44e0119c81816cf4f8dc873965ec8d
dca93e981fd4c868d915c45e7b938878dd6a6445868958886d6ebf14ffc0aeb1
c1ccc2[nH]cnc2c1
C-[N;H0;D3;+0:1](-C)-[C;H0;D3;+0:2](=O)-[NH;D2;+0:3]-[c:4]1:[c:5]:[c:6]:[c;H0;D3;+0:7](-Cl):[c;H0;D3;+0:8](-Cl):[cH;D2;+0:9]:1>>[c:6]1:[c:5]:[c:4]2:[nH;D2;+0:3]:[cH;D2;+0:2]:[n;H0;D2;+0:1]:[c;H0;D3;+0:9]:2:[cH;D2;+0:8]:[cH;D2;+0:7]:1
null
[]
null
null
2
HOUR
Membranes from CHO cells expressing the MCH receptor were prepared by lysing cells with 5 mM HEPES for 15 min at 4C. Cell lysates were centrifuged (12.5000×g, 15 min) and the pellet was resuspended in 5 mM HEPES. For each 96-well plate (Microlite, Dynex Technologies), 1 mg of cell membranes were incubated with 10 mg of...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Urea
null
c1ccccc1
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
HCl
C1CN(CCN1CCO)CCS(=O)(=O)O
null
2
CN(C)C(=O)Nc1ccc(Cl)c(Cl)c1>C1CN(CCN1CCO)CCS(=O)(=O)O>c1ccc2[nH]cnc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6d5bfc90160043f68888851e29fd8bec
COc1cccc([N+](=O)[O-])c1C>>COc1cccc(N)c1C
CC#N.O.CC1=C(C=CC=C1[N+](=O)[O-])OC.C(=O)(C(F)(F)F)O>>CC1=C(N)C=CC=C1OC
O=[N+:8]([O-])[c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:9]1[CH3:10]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[c:9]1[CH3:10]
COc1cccc([N+](=O)[O-])c1C
COc1cccc(N)c1C
null
[Pd]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
98
[{"value": 98.0, "product": "CC1=C(N)C=CC=C1OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 2-methyl-3-nitro anisole which is commercially available (1a1) (5.1 g; 30.33 mmol; requires ˜30 min. to dissolve) in absolute ethanol (85 mL) was added 10% Pd/C catalyst (500 mg). The solution was hydrogenated under a hydrogen filled balloon at atmospheric pressure and room temperature for 19 h. The re...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pd].C(C)O
null
null
COc1cccc([N+](=O)[O-])c1C>[Pd].C(C)O>COc1cccc(N)c1C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-74e9c1b9605a44ce85afd682f94646e1
Br.Nc1c(O)cccc1[N+](=O)[O-]>>O=[N+]([O-])c1cccc(O)c1Br
Br.NC1=C(C=CC=C1[N+](=O)[O-])O.Br.N(=O)[O-].[Na+]>>BrC1=C(C=CC=C1[N+](=O)[O-])O
[BrH:11].N[c:10]1[c:4]([N+:2](=[O:1])[O-:3])[cH:5][cH:6][cH:7][c:8]1[OH:9]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][cH:7][c:8]([OH:9])[c:10]1[Br:11]
Br.Nc1c(O)cccc1[N+](=O)[O-]
O=[N+]([O-])c1cccc(O)c1Br
null
null
O1CCOCC1.O
Miscellaneous
OtherReaction
976fb3f0996203ccf639edc3dd63ebf792dabe502fe07eb66206f5ee630d746b
1129c10513c603d2647e51dd9713063aaf10bd8a364ed275b9b93c32624e3ba4
c1ccccc1
N-[c;H0;D3;+0:1](:[c:2](-[#7;+:3]):[c:4]):[c:5](-[O;D1;H1:6]):[c:7].[BrH;D0;+0:8]>>[#7;+:3]-[c:2](:[c:4]):[c;H0;D3;+0:1](-[Br;H0;D1;+0:8]):[c:5](-[O;D1;H1:6]):[c:7]
null
[]
0
CELSIUS
15
MINUTE
2-Amino-3-nitrophenol 1b1 (5 g; 32.4 mmol) was dissolved in H2O (29.5 mL) and 1,4-dioxane (14.7 mL). The mixture was heated to reflux and hydrobromic acid (48%; 16.7 mL; 147 mmol) was added dropwise over a period of 20 min. Upon completion of the addition, the reflux was maintained an additional 15 min. The reaction wa...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
Other
O1CCOCC1.O
0
0.25
Br.Nc1c(O)cccc1[N+](=O)[O-]>O1CCOCC1.O>O=[N+]([O-])c1cccc(O)c1Br
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e9c9feaad4304b79a1b09618d00f1190
COc1cccc([N+](=O)[O-])c1Br>>COc1cccc(N)c1Br
BrC1=C(C=CC=C1[N+](=O)[O-])OC.C(=O)([O-])[O-].[Na+].[Na+]>>BrC1=C(N)C=CC=C1OC
O=[N+:8]([O-])[c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:9]1[Br:10]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[c:9]1[Br:10]
COc1cccc([N+](=O)[O-])c1Br
COc1cccc(N)c1Br
null
[Fe]
O.C(C)(=O)O.C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
2-Bromo-3-nitroanisole 1b3 (1.00 g; 4.31 mmol) was dissolved in glacial acetic acid (11.0 mL)/ethanol (11.0 mL) and to the solution was added iron powder (0.98 g; 17.5 mmol). The mixture was stirred at reflux for 3.5 hr and worked up. The reaction mixture was diluted with water (35 mL), neutralized with solid Na2CO3 an...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Fe].O.C(C)(=O)O.C(C)O
null
null
COc1cccc([N+](=O)[O-])c1Br>[Fe].O.C(C)(=O)O.C(C)O>COc1cccc(N)c1Br
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-894bea510080468f9d16eb64479f5a58
Cl.Nc1c(O)cccc1[N+](=O)[O-]>>O=[N+]([O-])c1cccc(O)c1Cl
Cl.N(=O)[O-].[Na+].NC1=C(C=CC=C1[N+](=O)[O-])O.Cl>>ClC1=C(C=CC=C1[N+](=O)[O-])O
[ClH:11].N[c:10]1[c:4]([N+:2](=[O:1])[O-:3])[cH:5][cH:6][cH:7][c:8]1[OH:9]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][cH:7][c:8]([OH:9])[c:10]1[Cl:11]
Cl.Nc1c(O)cccc1[N+](=O)[O-]
O=[N+]([O-])c1cccc(O)c1Cl
null
null
O1CCOCC1.O
Miscellaneous
OtherReaction
976fb3f0996203ccf639edc3dd63ebf792dabe502fe07eb66206f5ee630d746b
1129c10513c603d2647e51dd9713063aaf10bd8a364ed275b9b93c32624e3ba4
c1ccccc1
N-[c;H0;D3;+0:1](:[c:2](-[#7;+:3]):[c:4]):[c:5](-[O;D1;H1:6]):[c:7].[ClH;D0;+0:8]>>[#7;+:3]-[c:2](:[c:4]):[c;H0;D3;+0:1](-[Cl;H0;D1;+0:8]):[c:5](-[O;D1;H1:6]):[c:7]
null
[]
70
CELSIUS
15
MINUTE
2-Amino-3-nitrophenol 1b1 (5 g; 32.4 mmol) was dissolved in concentrated HCl (75 mL) and 1,4-dioxane (14.7 mL). The mixture was heated to 70° C. until most of the solids were in solution. The reaction mixture was cooled to 0° C. (ice bath), and sodium nitrite (2.23 g; 32.3 mmol) in H2O (5.4 mL) was added over a period ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
Other
O1CCOCC1.O
70
0.25
Cl.Nc1c(O)cccc1[N+](=O)[O-]>O1CCOCC1.O>O=[N+]([O-])c1cccc(O)c1Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-aee28bb42b424147965b597279f35827
COc1cccc([N+](=O)[O-])c1Cl>>COc1cccc(N)c1Cl
ClC1=C(C=CC=C1[N+](=O)[O-])OC.C(=O)([O-])[O-].[Na+].[Na+]>>ClC1=C(N)C=CC=C1OC
O=[N+:8]([O-])[c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:9]1[Cl:10]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[c:9]1[Cl:10]
COc1cccc([N+](=O)[O-])c1Cl
COc1cccc(N)c1Cl
null
[Fe]
O.C(C)(=O)O.C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
103.5
[{"value": 100.0, "product": "ClC1=C(N)C=CC=C1OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 103.5, "product": "ClC1=C(N)C=CC=C1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2-Chloro-3-nitroanisole 1c2 (1.38 g; 7.36 mmol) was dissolved in a mixture of glacial acetic acid (19 mL)/ethanol (19 mL). To this solution was added iron powder (1.64 g; 29.4 mmol). The mixture was stirred at reflux for 3.5 hr and worked up. The reaction mixture was diluted with water (70 mL), neutralized with solid N...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Fe].O.C(C)(=O)O.C(C)O
null
null
COc1cccc([N+](=O)[O-])c1Cl>[Fe].O.C(C)(=O)O.C(C)O>COc1cccc(N)c1Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-cb8575a7b29d4316add54ada91f35189
CCOC(C)=O.Nc1ccccc1.c1ccc(Oc2ccccc2)cc1>>COc1ccc2c(O)ccnc2c1C
C1(=CC=CC=C1)OC1=CC=CC=C1.NC1=CC=CC=C1.CCCCCC.CCOC(=O)C>>OC1=CC=NC2=C(C(=CC=C12)OC)C
[CH2:1]([O:2][C:3]([CH3:4])=[O:8])[CH3:14].[cH:5]1[cH:6][c:12]([NH2:11])[cH:13][cH:7][cH:9]1.c1ccc(Oc2cc[cH:10]cc2)cc1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([OH:8])[cH:9][cH:10][n:11][c:12]2[c:13]1[CH3:14]
CCOC(C)=O.Nc1ccccc1.c1ccc(Oc2ccccc2)cc1
COc1ccc2c(O)ccnc2c1C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
cef090c5bd97e780cab2d3ed8ad5652b8c9f5cec6204eb129e076255d355df89
dc0517de81a68d30734570298cb2d349ee8945c6caff5b6a241025d7c6c8628c
c1ccc2ncccc2c1
O(-c1:c:c:[cH;D2;+0:1]:c:c:1)-c1:c:c:c:c:c:1.[CH3;D1;+0:2]-[CH2;D2;+0:3]-[#8:4]-[C;H0;D3;+0:5](-[CH3;D1;+0:6])=[O;H0;D1;+0:7].[NH2;D1;+0:8]-[c:9]1:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:[cH;D2;+0:14]:1>>[CH3;D1;+0:2]-[c;H0;D3;+0:10]1:[c:9]2:[n;H0;D2;+0:8]:[cH;D2;+0:1]:[cH;D2;+0:12]:[c;H0;D3;+0:11](-[OH...
null
[]
300
CELSIUS
20
MINUTE
A three-neck flask containing diphenyl ether (1.9 mL; 11.75 mmol) was placed into a preheated sand bath heated to ˜300° C. and the sand bath allowed to slowly heat further to ˜330° C. so as the internal temperature was between 245-250° C. The aniline derivative 1s1 was added portion-wise (immediately seeing gas evoluti...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Primary amine
Ether.Aromatic alcohol
c1ccccc1.c1ccccc1.c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HO-
null
300
0.333333
CCOC(C)=O.Nc1ccccc1.c1ccc(Oc2ccccc2)cc1>>COc1ccc2c(O)ccnc2c1C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a1acb0651e9f4126819cd5ea323804fc
CC(C)[C@H](N)C(=O)O>>CC(C)C(N)C(=O)[O-]
N[C@@H](C(C)C)C(=O)O.[OH-].[Na+]>>NC(C(=O)[O-])C(C)C.[Na+]
[CH3:1][CH:2]([CH3:3])[C@H:4]([NH2:5])[C:6](=[O:7])[OH:8]>>[CH3:1][CH:2]([CH3:3])[CH:4]([NH2:5])[C:6](=[O:7])[O-:8]
CC(C)[C@H](N)C(=O)O
CC(C)C(N)C(=O)[O-]
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 5.86 g (50 mmol) of Valine is dissolved in 200 ml of water. To this is added 55 ml of 1M sodium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carboxyla...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CC(C)[C@H](N)C(=O)O>O>CC(C)C(N)C(=O)[O-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e1d22e3799a5420585632407023d90b9
CC(C)C(N)C(=O)[O-].CCCC(=O)Cl>>CCCC(=O)OC(=O)C(N)C(C)C
C(CCC)(=O)Cl.NC(C(=O)[O-])C(C)C.[Na+].C(CCC)(=O)Cl>>C(CCC)(=O)OC(C(C(C)C)N)=O
[O-:6][C:7](=[O:8])[CH:9]([NH2:10])[CH:11]([CH3:12])[CH3:13].Cl[C:4]([CH2:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][CH2:3][C:4](=[O:5])[O:6][C:7](=[O:8])[CH:9]([NH2:10])[CH:11]([CH3:12])[CH3:13]
CC(C)C(N)C(=O)[O-].CCCC(=O)Cl
CCCC(=O)OC(=O)C(N)C(C)C
null
null
null
Acylation
OtherReaction
a277333969c51673a7c4bc3b7a1d27397572756db5225daff581114d737437ec
5fefc881dc234269fd51d1840a72dd88a62ba4ed6b7c2dfd03e5f64e328bf825
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C:6](-[C:5])=[O;D1;H0:8]
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 6.39 g (60 mmol) of the prepared butyryl chloride, and side arm water condenser fixed with a dry receiving flask, is placed 9.18 g (66 mmol) of sodium 2-amino-3-methylbutanoate. The round bottomed flask is placed in an ice bath...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Anhydride
null
null
null
Other
null
null
null
CC(C)C(N)C(=O)[O-].CCCC(=O)Cl>>CCCC(=O)OC(=O)C(N)C(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-7aa9ab214c114f08b80f4d34aebbfee4
CC[C@H](C)[C@H](N)C(=O)O>>CCC(C)C(N)C(=O)[O-]
N[C@@H]([C@@H](C)CC)C(=O)O.[OH-].[Na+]>>NC(C(=O)[O-])C(CC)C.[Na+]
[CH3:1][CH2:2][C@H:3]([CH3:4])[C@H:5]([NH2:6])[C:7](=[O:8])[OH:9]>>[CH3:1][CH2:2][CH:3]([CH3:4])[CH:5]([NH2:6])[C:7](=[O:8])[O-:9]
CC[C@H](C)[C@H](N)C(=O)O
CCC(C)C(N)C(=O)[O-]
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 6.56 g (50 mmol) of Isoleucine is dissolved in 200 ml of water. To this is added 55 ml of 1M sodium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carbo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CC[C@H](C)[C@H](N)C(=O)O>O>CCC(C)C(N)C(=O)[O-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-06008332fead487594dfab2b7e8eb607
CCC(C)C(N)C(=O)[O-].CCCCCC(=O)Br>>CCCCCC(=O)OC(=O)C(N)C(C)CC
C(CCCCC)(=O)Br.NC(C(=O)[O-])C(CC)C.[Na+].C(CCCCC)(=O)Br>>C(CCCCC)(=O)OC(C(C(CC)C)N)=O
[O-:8][C:9](=[O:10])[CH:11]([NH2:12])[CH:13]([CH3:14])[CH2:15][CH3:16].Br[C:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:7]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6](=[O:7])[O:8][C:9](=[O:10])[CH:11]([NH2:12])[CH:13]([CH3:14])[CH2:15][CH3:16]
CCC(C)C(N)C(=O)[O-].CCCCCC(=O)Br
CCCCCC(=O)OC(=O)C(N)C(C)CC
null
null
null
Acylation
OtherReaction
a277333969c51673a7c4bc3b7a1d27397572756db5225daff581114d737437ec
5fefc881dc234269fd51d1840a72dd88a62ba4ed6b7c2dfd03e5f64e328bf825
null
Br-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]>>[C:5]-[C:6](=[O;D1;H0:8])-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 10.81 g (60 mmol) of the prepared hexanoyl bromide, and side arm water condenser fixed with a dry receiving flask, is placed 11.03 g (72 mmol) of sodium 2-amino-3-methylpentanoate. The round bottomed flask is placed in an ice b...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Anhydride
null
null
null
Br-
null
null
null
CCC(C)C(N)C(=O)[O-].CCCCCC(=O)Br>>CCCCCC(=O)OC(=O)C(N)C(C)CC
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e74882c81c994186b3a5b592a2f17355
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCCCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCC)(=O)Cl
O[C:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:13].O=S(Cl)[Cl:14]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[Cl:14]
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl
CCCCCCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
45
CELSIUS
50
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 5.85 ml (80 mmol) of thionyl chloride, and a water condenser, is placed 10.02 g (50 mmol) of dodecanoic acid. Addition of the thionyl chloride is completed with heating to about 45° C. over the cours...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
45
0.833333
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCCCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-deb832ac8bfe4632baf579b126449788
N=C(N)NCCC[C@H](N)C(=O)O>>N=C(N)NCCCC(N)C(=O)[O-]
N[C@@H](CCCNC(N)=N)C(=O)O.[OH-].[NH4+]>>NC(C(=O)[O-])CCCNC(=N)N.[NH4+]
[NH:1]=[C:2]([NH2:3])[NH:4][CH2:5][CH2:6][CH2:7][C@H:8]([NH2:9])[C:10](=[O:11])[OH:12]>>[NH:1]=[C:2]([NH2:3])[NH:4][CH2:5][CH2:6][CH2:7][CH:8]([NH2:9])[C:10](=[O:11])[O-:12]
N=C(N)NCCC[C@H](N)C(=O)O
N=C(N)NCCCC(N)C(=O)[O-]
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 10.45 g (60 mmol) of Arginine is dissolved in 300 ml of water. To this is added 78 ml of 1M ammonium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carb...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
N=C(N)NCCC[C@H](N)C(=O)O>O>N=C(N)NCCCC(N)C(=O)[O-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5aeff84d06644da698fd1cedbb4780e1
CCCCCCCCCCCC(=O)Cl.N=C(N)NCCCC(N)C(=O)[O-]>>CCCCCCCCCCCC(=O)OC(=O)C(N)CCCNC(=N)N
C(CCCCCCCCCCC)(=O)Cl.NC(C(=O)[O-])CCCNC(=N)N.[NH4+].C(CCCCCCCCCCC)(=O)Cl>>C(CCCCCCCCCCC)(=O)OC(C(CCCNC(=N)N)N)=O
Cl[C:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:13].[O-:14][C:15](=[O:16])[CH:17]([NH2:18])[CH2:19][CH2:20][CH2:21][NH:22][C:23](=[NH:24])[NH2:25]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[O:14][C:15](=[O:16])[CH:17]([NH2...
CCCCCCCCCCCC(=O)Cl.N=C(N)NCCCC(N)C(=O)[O-]
CCCCCCCCCCCC(=O)OC(=O)C(N)CCCNC(=N)N
null
null
null
Protection
OtherReaction
28c2e4e4e899b53f47f26c928dd1e31ebef90e8fc1b5afe08cb871bc47f95bd3
d9986b0eedf845fc44f27353fb210fb36c2b2eb27a1b7c079579aaba5d804c30
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C:6](-[C:5])=[O;D1;H0:8]
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 15.31 g (70 mmol) of the prepared dodecanoyl chloride, and side arm water condenser fixed with a dry receiving flask, is placed 16.06 g (84 mmol) of ammonium 2-amino-5-guanidinopentanoate. The round bottomed flask is placed in ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Anhydride
null
null
null
Other
null
null
null
CCCCCCCCCCCC(=O)Cl.N=C(N)NCCCC(N)C(=O)[O-]>>CCCCCCCCCCCC(=O)OC(=O)C(N)CCCNC(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5d9ed55cfb244fc980f4735fb78cfebb
CCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCCCCCCCCCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCCCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCCCCCCCC)(=O)Cl
O[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19].O=S(Cl)[Cl:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[Cl:20]
CCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl
CCCCCCCCCCCCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
45
CELSIUS
45
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 4.81 ml (66 mmol) of thionyl chloride, and a water condenser, is placed 15.65 g (55 mmol) of stearic acid. Addition of the thionyl chloride is completed with heating to about 45° C. over the course o...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
45
0.75
CCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCCCCCCCCCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-345d0a27018043d1a770069557aa1330
CC(C)C[C@H](N)C(=O)O>>CC(C)CC(N)C(=O)[O-]
N[C@@H](CC(C)C)C(=O)O.[OH-].[K+]>>NC(C(=O)[O-])CC(C)C.[K+]
[CH3:1][CH:2]([CH3:3])[CH2:4][C@H:5]([NH2:6])[C:7](=[O:8])[OH:9]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH:5]([NH2:6])[C:7](=[O:8])[O-:9]
CC(C)C[C@H](N)C(=O)O
CC(C)CC(N)C(=O)[O-]
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 7.87 g (60 mmol) of Leucine is dissolved in 300 ml of water. To this is added 72 ml of 1 M potassium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carb...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CC(C)C[C@H](N)C(=O)O>O>CC(C)CC(N)C(=O)[O-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-79d913cc7ac74a02967425c33d1b82fd
CC(C)CC(N)C(=O)[O-].CCCCCCCCCCCCCCCCCC(=O)Cl>>CCCCCCCCCCCCCCCCCC(=O)OC(=O)C(N)CC(C)C
C(CCCCCCCCCCCCCCCCC)(=O)Cl.NC(C(=O)[O-])CC(C)C.[K+].C(CCCCCCCCCCCCCCCCC)(=O)Cl>>C(CCCCCCCCCCCCCCCCC)(=O)OC(C(CC(C)C)N)=O
[O-:20][C:21](=[O:22])[CH:23]([NH2:24])[CH2:25][CH:26]([CH3:27])[CH3:28].Cl[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:1...
CC(C)CC(N)C(=O)[O-].CCCCCCCCCCCCCCCCCC(=O)Cl
CCCCCCCCCCCCCCCCCC(=O)OC(=O)C(N)CC(C)C
null
null
null
Acylation
OtherReaction
a277333969c51673a7c4bc3b7a1d27397572756db5225daff581114d737437ec
5fefc881dc234269fd51d1840a72dd88a62ba4ed6b7c2dfd03e5f64e328bf825
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C:6](-[C:5])=[O;D1;H0:8]
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 21.27 g (70 mmol) of the prepared stearoyl chloride, and side arm water condenser fixed with a dry receiving flask, is placed 13.03 g (77 mmol) of potassium 2-amino-4-methylpentanoate. The round bottomed flask is placed in an i...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Anhydride
null
null
null
Other
null
null
null
CC(C)CC(N)C(=O)[O-].CCCCCCCCCCCCCCCCCC(=O)Cl>>CCCCCCCCCCCCCCCCCC(=O)OC(=O)C(N)CC(C)C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-80af1d69e9954dfa913604ecbf08a2fe
CCCCC/C=C\C/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCC\C=C/C\C=C/CCCCC)(=O)O>>C(CCCCCCC\C=C/C\C=C/CCCCC)(=O)Cl
O[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11]/[CH:10]=[CH:9]\[CH2:8]/[CH:7]=[CH:6]\[CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19].O=S(Cl)[Cl:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5]/[CH:6]=[CH:7]\[CH2:8]/[CH:9]=[CH:10]\[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[Cl:20]
CCCCC/C=C\C/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl
CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
40
CELSIUS
50
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 9.35 ml (128 mmol) of thionyl chloride, and a water condenser, is placed 24.90 ml (80 mmol) of linoleic acid. Addition of the thionyl chloride is completed with heating to about 40° C. over the cours...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
40
0.833333
CCCCC/C=C\C/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a4c3049184d5482a8a34391cdcb4880c
CC(N)C(=O)[O-].CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl.CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl>>CCCCC/C=C\C/C=C\CCCCCC(=O)OC(=O)CCCCC/C=C\C/C=C\CCCCC
C(CCCCCCC\C=C/C\C=C/CCCCC)(=O)Cl.NC(C(=O)[O-])C.[NH4+].C(CCCCCCC\C=C/C\C=C/CCCCC)(=O)Cl>>C(CCCCC\C=C/C\C=C/CCCCC)(=O)OC(CCCCC\C=C/C\C=C/CCCCC)=O
CC(N)C(=O)[O-:18].Cl[C:19](=[O:20])[CH2:21][CH2:22][CH2:23][CH2:24][CH2:25]CC/[CH:10]=[CH:9]\[CH2:8]/[CH:7]=[CH:6]\[CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].Cl[C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11]C[CH2:31]/[CH:30]=[CH:29]\[CH2:28]/[CH:27]=[CH:26]\C[CH2:32][CH2:33][CH2:34][CH3:35])=[O:17]>>[CH3:1][CH2:2][CH2:3][CH2:...
CC(N)C(=O)[O-].CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl.CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl
CCCCC/C=C\C/C=C\CCCCCC(=O)OC(=O)CCCCC/C=C\C/C=C\CCCCC
null
null
null
Acylation
OtherReaction
76480b7bb72821d3e774726a37d831593401301f426e09495a7f10deb9c3aded
f6372bc3afaa901ffa5cb4a5801eb88e4a808f6822f7883e1c1262c45daa5921
null
C-C(-N)-C(=O)-[O-;H0;D1:1].Cl-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]-[C:6]-[C:7]-[CH2;D2;+0:8]-C-C/[CH;D2;+0:9]=[C:10]\[C:11]/[C:12]=[C:13]\[C:14].Cl-[C;H0;D3;+0:15](=[O;D1;H0:16])-[C:17]-[C:18]-[C:19]-[C:20]-[CH2;D2;+0:21]-C-[CH2;D2;+0:22]/[C:23]=[C:24]\[C:25]/[C:26]=[CH;D2;+0:27]\C-[CH2;D2;+0:28]-[C:29]-[C:30]>>[C:...
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 17.93 g (60 mmol) of the prepared (9Z,12Z)-octadeca-9,12-dienoyl chloride, and side arm water condenser fixed with a dry receiving flask, is placed 7.64 g (72 mmol) of ammonium 2-aminopropanoate. The round bottomed flask is pla...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Anhydride
null
null
null
HCl
null
null
null
CC(N)C(=O)[O-].CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl.CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl>>CCCCC/C=C\C/C=C\CCCCCC(=O)OC(=O)CCCCC/C=C\C/C=C\CCCCC
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-58ce9951f10842119d4e46869554f4a8
CN(CC(=O)O)C(=N)N>>CN(CC(=O)[O-])C(=N)N
O=C(O)CN(C)C(N)=N.[OH-].[Na+]>>CN(C(=N)N)CC(=O)[O-].[Na+]
[CH3:1][N:2]([CH2:3][C:4](=[O:5])[OH:6])[C:7](=[NH:8])[NH2:9]>>[CH3:1][N:2]([CH2:3][C:4](=[O:5])[O-:6])[C:7](=[NH:8])[NH2:9]
CN(CC(=O)O)C(=N)N
CN(CC(=O)[O-])C(=N)N
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 6.56 g (50 mmol) of creatine is dissolved in 500 ml of water. To this is added 55 ml of 1M sodium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carboxy...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CN(CC(=O)O)C(=N)N>O>CN(CC(=O)[O-])C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f05d0779617340459ecd21e2d8bbbfea
CCCC(=O)Cl.CN(CC(=O)[O-])C(=N)N>>CN(CC(=O)OC(=O)CN(C)C(=N)N)C(=N)N
C(CCC)(=O)Cl.CN(C(=N)N)CC(=O)[O-].[Na+].C(CCC)(=O)Cl>>CN(C(=N)N)CC(=O)OC(CN(C(=N)N)C)=O
Cl[C:4]([CH2:3]C[CH3:1])=[O:5].[NH:2]=[C:12]([N:10]([CH2:9][C:7]([O-:6])=[O:8])[CH3:11])[NH2:17]>>[CH3:1][N:2]([CH2:3][C:4](=[O:5])[O:6][C:7](=[O:8])[CH2:9][N:10]([CH3:11])[C:12](=[NH:13])[NH2:14])[C:15](=[NH:16])[NH2:17]
CCCC(=O)Cl.CN(CC(=O)[O-])C(=N)N
CN(CC(=O)OC(=O)CN(C)C(=N)N)C(=N)N
null
null
null
Protection
OtherReaction
4e8a377bb3b8a9ec9f325a7ae963a97901b55ab63a5f830c6388ca9a6aea2c28
5b33930ec8bab92a3e3bea9235df5aba8b45e7c85a07488cc536714dab18306d
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-C-[CH3;D1;+0:4].[C;D1;H3:5]-[#7:6](-[C:7]-[C:8](-[O-;H0;D1:9])=[O;D1;H0:10])-[C;H0;D3;+0:11](-[NH2;D1;+0:12])=[NH;D1;+0:13]>>[C;D1;H3:5]-[#7:6](-[C:7]-[C:8](=[O;D1;H0:10])-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[N;H0;D3;+0:13](-[CH3;D1;+0:4])-[C:14](=[N;D...
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 6.39 g (60 mmol) of the prepared butyryl chloride, and side arm water condenser fixed with a dry receiving flask, is placed 12.08 g (66 mmol) of sodium 2-(1-methylguanidino)acetate. The round bottomed flask is placed in an ice ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Anhydride.Primary amine.Primary amine.Tertiary amine
null
null
null
null
null
null
null
CCCC(=O)Cl.CN(CC(=O)[O-])C(=N)N>>CN(CC(=O)OC(=O)CN(C)C(=N)N)C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-3419abdcfbd8463c93153c2bc3328298
CN(CC(=O)O)C(=N)N>>CN(CC(=O)[O-])C(=N)N
O=C(O)CN(C)C(N)=N.[OH-].[Na+]>>CN(C(=N)N)CC(=O)[O-].[Na+]
[CH3:1][N:2]([CH2:3][C:4](=[O:5])[OH:6])[C:7](=[NH:8])[NH2:9]>>[CH3:1][N:2]([CH2:3][C:4](=[O:5])[O-:6])[C:7](=[NH:8])[NH2:9]
CN(CC(=O)O)C(=N)N
CN(CC(=O)[O-])C(=N)N
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 6.56 g (50 mmol) of creatine is dissolved in 500 ml of water. To this is added 55 ml of 1M sodium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carboxy...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CN(CC(=O)O)C(=N)N>O>CN(CC(=O)[O-])C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8e672e2d6a704bb4adf23380a4afb362
CCCCCC(=O)Br.CN(CC(=O)[O-])C(=N)N>>CN(CC(=O)OC(=O)CN(C)C(=N)N)C(=N)N
C(CCCCC)(=O)Br.CN(C(=N)N)CC(=O)[O-].[Na+].C(CCCCC)(=O)Br>>CN(C(=N)N)CC(=O)OC(CN(C(=N)N)C)=O
Br[C:4]([CH2:3]CCC[CH3:1])=[O:5].[NH2:2][C:12]([N:10]([CH2:9][C:7]([O-:6])=[O:8])[CH3:11])=[NH:13]>>[CH3:1][N:2]([CH2:3][C:4](=[O:5])[O:6][C:7](=[O:8])[CH2:9][N:10]([CH3:11])[C:12](=[NH:13])[NH2:14])[C:15](=[NH:16])[NH2:17]
CCCCCC(=O)Br.CN(CC(=O)[O-])C(=N)N
CN(CC(=O)OC(=O)CN(C)C(=N)N)C(=N)N
null
null
null
Protection
OtherReaction
4e8a377bb3b8a9ec9f325a7ae963a97901b55ab63a5f830c6388ca9a6aea2c28
5b33930ec8bab92a3e3bea9235df5aba8b45e7c85a07488cc536714dab18306d
null
Br-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-C-C-C-[CH3;D1;+0:4].[C;D1;H3:5]-[#7:6](-[C:7]-[C:8](-[O-;H0;D1:9])=[O;D1;H0:10])-[C;H0;D3;+0:11](=[N;D1;H1:12])-[NH2;D1;+0:13]>>[C;D1;H3:5]-[#7:6](-[C:7]-[C:8](=[O;D1;H0:10])-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[N;H0;D3;+0:13](-[CH3;D1;+0:4])-[C:14](=[...
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 10.81 g (60 mmol) of the prepared hexanoyl bromide, and side arm water condenser fixed with a dry receiving flask, is placed 13.18 g (72 mmol) of sodium 2-(1-methylguanidino)acetate. The round bottomed flask is placed in an ice...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Anhydride.Primary amine.Primary amine.Tertiary amine
null
null
null
null
null
null
null
CCCCCC(=O)Br.CN(CC(=O)[O-])C(=N)N>>CN(CC(=O)OC(=O)CN(C)C(=N)N)C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-5c0a49985fdd4dd08228186d3b1aba59
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCCCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCC)(=O)Cl
O[C:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:13].O=S(Cl)[Cl:14]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[Cl:14]
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl
CCCCCCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
45
CELSIUS
50
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 5.85 ml (80 mmol) of thionyl chloride, and a water condenser, is placed 10.02 g (50 mmol) of dodecanoic acid. Addition of the thionyl chloride is completed with heating to about 45° C. over the cours...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
45
0.833333
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCCCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-6035ace7e84841c395d5c4d142ad3c75
CN(CC(=O)O)C(=N)N>>CN(CC(=O)[O-])C(=N)N
O=C(O)CN(C)C(N)=N.[OH-].[NH4+]>>CN(C(=N)N)CC(=O)[O-].[NH4+]
[CH3:1][N:2]([CH2:3][C:4](=[O:5])[OH:6])[C:7](=[NH:8])[NH2:9]>>[CH3:1][N:2]([CH2:3][C:4](=[O:5])[O-:6])[C:7](=[NH:8])[NH2:9]
CN(CC(=O)O)C(=N)N
CN(CC(=O)[O-])C(=N)N
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 7.87 g (60 mmol) of creatine is dissolved in 600 ml of water. To this is added 78 ml of 1M ammonium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carbo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CN(CC(=O)O)C(=N)N>O>CN(CC(=O)[O-])C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e51685ad3b0e4bb78719ec30d7f5f84a
CCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCCCCCCCCCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCCCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCCCCCCCC)(=O)Cl
O[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19].O=S(Cl)[Cl:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[Cl:20]
CCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl
CCCCCCCCCCCCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
45
CELSIUS
45
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 4.81 ml (66 mmol) of thionyl chloride, and a water condenser, is placed 15.65 g (55 mmol) of stearic acid. Addition of the thionyl chloride is completed with heating to about 45° C. over the course o...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
45
0.75
CCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCCCCCCCCCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ac017f4279f9458d9339f09d79516c97
CN(CC(=O)O)C(=N)N>>CN(CC(=O)[O-])C(=N)N
O=C(O)CN(C)C(N)=N.[OH-].[K+]>>CN(C(=N)N)CC(=O)[O-].[K+]
[CH3:1][N:2]([CH2:3][C:4](=[O:5])[OH:6])[C:7](=[NH:8])[NH2:9]>>[CH3:1][N:2]([CH2:3][C:4](=[O:5])[O-:6])[C:7](=[NH:8])[NH2:9]
CN(CC(=O)O)C(=N)N
CN(CC(=O)[O-])C(=N)N
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 7.87 g (60 mmol) of creatine is dissolved in 600 ml of water. To this is added 72 ml of 1M potassium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carb...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CN(CC(=O)O)C(=N)N>O>CN(CC(=O)[O-])C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-1980a97a10944bc7b3ebae6466e12b97
CCCCCCCCCCCCCCCCCC(=O)Cl.CN(CC(=O)[O-])C(=N)N>>CCCCCCCCCCCCCCCCCC(=O)OC(=O)CN(C)C(=N)N
C(CCCCCCCCCCCCCCCCC)(=O)Cl.CN(C(=N)N)CC(=O)[O-].[K+].C(CCCCCCCCCCCCCCCCC)(=O)Cl>>C(CCCCCCCCCCCCCCCCC)(=O)OC(CN(C(=N)N)C)=O
Cl[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19].[O-:20][C:21](=[O:22])[CH2:23][N:24]([CH3:25])[C:26](=[NH:27])[NH2:28]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14]...
CCCCCCCCCCCCCCCCCC(=O)Cl.CN(CC(=O)[O-])C(=N)N
CCCCCCCCCCCCCCCCCC(=O)OC(=O)CN(C)C(=N)N
null
null
null
Protection
OtherReaction
28c2e4e4e899b53f47f26c928dd1e31ebef90e8fc1b5afe08cb871bc47f95bd3
d9986b0eedf845fc44f27353fb210fb36c2b2eb27a1b7c079579aaba5d804c30
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C:6](-[C:5])=[O;D1;H0:8]
null
[]
null
null
null
null
Finally, in a dry 2-necked, round bottomed flask, fixed with a separatory funnel, containing 21.27 g (70 mmol) of the prepared stearoyl chloride, and side arm water condenser fixed with a dry receiving flask, is placed 23.40 g (77 mmol) of potassium 2-(1-methylguanidino)acetate. The round bottomed flask is placed in an...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Anhydride
null
null
null
Other
null
null
null
CCCCCCCCCCCCCCCCCC(=O)Cl.CN(CC(=O)[O-])C(=N)N>>CCCCCCCCCCCCCCCCCC(=O)OC(=O)CN(C)C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-0bcb3d1cf9254d19a95a3cdda43b531b
CCCCC/C=C\C/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCC\C=C/C\C=C/CCCCC)(=O)O>>C(CCCCCCC\C=C/C\C=C/CCCCC)(=O)Cl
O[C:18]([CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11]/[CH:10]=[CH:9]\[CH2:8]/[CH:7]=[CH:6]\[CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:19].O=S(Cl)[Cl:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5]/[CH:6]=[CH:7]\[CH2:8]/[CH:9]=[CH:10]\[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[Cl:20]
CCCCC/C=C\C/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl
CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
40
CELSIUS
50
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 9.35 ml (128 mmol) of thionyl chloride, and a water condenser, is placed 24.90 ml (80 mmol) of linoleic acid. Addition of the thionyl chloride is completed with heating to about 40° C. over the cours...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
40
0.833333
CCCCC/C=C\C/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCC/C=C\C/C=C\CCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-738c7e9edb764a9ab8ad87a2e28f310a
CN(CC(=O)O)C(=N)N>>CN(CC(=O)[O-])C(=N)N
O=C(O)CN(C)C(N)=N.[OH-].[NH4+]>>CN(C(=N)N)CC(=O)[O-].[NH4+]
[CH3:1][N:2]([CH2:3][C:4](=[O:5])[OH:6])[C:7](=[NH:8])[NH2:9]>>[CH3:1][N:2]([CH2:3][C:4](=[O:5])[O-:6])[C:7](=[NH:8])[NH2:9]
CN(CC(=O)O)C(=N)N
CN(CC(=O)[O-])C(=N)N
null
null
O
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
null
[]
null
null
null
null
Separately, in a single-necked, round bottomed flask, equipped with a magnetic stirrer, 7.87 g (60 mmol) of creatine is dissolved in 600 ml of water. To this is added 78 ml of 1M ammonium hydroxide with vigorous stirring, until heat production ceases. At this point the water is removed by evaporation to yield the carbo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
null
null
O
null
null
CN(CC(=O)O)C(=N)N>O>CN(CC(=O)[O-])C(=N)N
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ec3c00d00aa44b628bdbec3d60bafcbe
CCCCCCCC(=O)O.O=S(Br)Br>>CCCCCCCC(=O)Br
S(=O)(Br)Br.S(=O)(Br)Br.S(=O)(Br)Br.C(CCCCCCC)(=O)O>>C(CCCCCCC)(=O)Br
O[C:8]([CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:9].O=S(Br)[Br:10]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][C:8](=[O:9])[Br:10]
CCCCCCCC(=O)O.O=S(Br)Br
CCCCCCCC(=O)Br
null
null
O
Functional Group Interconversion
OtherReaction
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Br-S(=O)-[Br;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[Br;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]
null
[]
50
CELSIUS
null
null
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 10.07 ml (130 mmol) of thionyl bromide, and a water condenser, is placed 10.30 ml (65 mmol) of octanoic acid. Addition of the thionyl bromide is completed with heating to about 50° C. over the course...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HBr
O
50
null
CCCCCCCC(=O)O.O=S(Br)Br>O>CCCCCCCC(=O)Br
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-81defff891a547b3a96824b36a52363b
CCCCCCCC(=O)Br.CN(CC(=O)O)C(=N)N>>CCCCCCCC(=O)NC(=N)N(C)CC(=O)O
C(CCCCCCC)(=O)Br.N1=CC=CC=C1.C(CCCCCCC)(=O)Br.O=C(O)CN(C)C(N)=N.C(CCCCCCC)(=O)Br.C(=O)=O.C(CCCCCCC)(=O)Br>>CN(C(=N)NC(CCCCCCC)=O)CC(=O)O
Br[C:8]([CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:9].[NH2:10][C:11](=[NH:12])[N:13]([CH3:14])[CH2:15][C:16](=[O:17])[OH:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][C:8](=[O:9])[NH:10][C:11](=[NH:12])[N:13]([CH3:14])[CH2:15][C:16](=[O:17])[OH:18]
CCCCCCCC(=O)Br.CN(CC(=O)O)C(=N)N
CCCCCCCC(=O)NC(=N)N(C)CC(=O)O
null
null
ClCCl.CC(=O)C
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
null
Br-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[#7:5]-[C:6](=[N;D1;H1:7])-[NH2;D1;+0:8]>>[#7:5]-[C:6](=[N;D1;H1:7])-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
null
[]
null
null
null
null
In a dry 3-necked, round bottomed flask, equipped with a magnetic stirrer, a thermometer, a nitrogen inlet tube and the dropping funnel containing the octanoyl bromide solution, 7.08 g (54 mmol) of creatine is suspended, with stirring, in 50 ml of dry dichloromethane. To this suspension a catalytic amount (0.1 mmol) of...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
null
HBr
ClCCl.CC(=O)C
null
null
CCCCCCCC(=O)Br.CN(CC(=O)O)C(=N)N>ClCCl.CC(=O)C>CCCCCCCC(=O)NC(=N)N(C)CC(=O)O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-19ddd728dc474a718f53529edd1d687b
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCCCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCC)(=O)Cl
O[C:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:13].O=S(Cl)[Cl:14]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[Cl:14]
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl
CCCCCCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
45
CELSIUS
45
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 13.13 ml (180 mmol) of thionyl chloride, and a water condenser, is placed 20.03 g (100 mmol) of dodecanoic acid. Addition of the thionyl chloride is completed with heating to about 45° C. over the co...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
45
0.75
CCCCCCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCCCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f97a24765fae4e6bb2fa83918acd3402
CCCCCCCCCCCC(=O)Cl.CN(CC(=O)O)C(=N)N>>CCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
C(CCCCCCCCCCC)(=O)Cl.N1=CC=CC=C1.C(CCCCCCCCCCC)(=O)Cl.O=C(O)CN(C)C(N)=N.C(CCCCCCCCCCC)(=O)Cl.C(=O)=O.C(CCCCCCCCCCC)(=O)Cl>>C(CCCCCCCCCCC)(=O)NC(N(C)CC(=O)O)=N
Cl[C:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:13].[NH2:14][C:15](=[NH:16])[N:17]([CH3:18])[CH2:19][C:20](=[O:21])[OH:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[NH:14][C:15](=[NH:16])[N:17]([CH3:18])[CH2:19][C:20](=[O...
CCCCCCCCCCCC(=O)Cl.CN(CC(=O)O)C(=N)N
CCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
null
null
ClCCl.CC(=O)C
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[#7:5]-[C:6](=[N;D1;H1:7])-[NH2;D1;+0:8]>>[#7:5]-[C:6](=[N;D1;H1:7])-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
null
[]
null
null
null
null
In a dry 3-necked, round bottomed flask, equipped with a magnetic stirrer, a thermometer, a nitrogen inlet tube and the dropping funnel containing the dodecanoyl chloride solution, 7.34 g (56 mmol) of creatine is suspended, with stirring, in 50 ml of dry dichloromethane. To this suspension a catalytic amount (0.1 mmol)...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
null
HCl
ClCCl.CC(=O)C
null
null
CCCCCCCCCCCC(=O)Cl.CN(CC(=O)O)C(=N)N>ClCCl.CC(=O)C>CCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-c4dff51e1d564cf88832a0296a2750b7
CCCCCCCCCCCCCCCC(=O)O.O=S(Br)Br>>CCCCCCCCCCCCCCCC(=O)Br
S(=O)(Br)Br.S(=O)(Br)Br.S(=O)(Br)Br.C(CCCCCCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCCCCCC)(=O)Br
O[C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:17].O=S(Br)[Br:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][C:16](=[O:17])[Br:18]
CCCCCCCCCCCCCCCC(=O)O.O=S(Br)Br
CCCCCCCCCCCCCCCC(=O)Br
null
null
O
Functional Group Interconversion
OtherReaction
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Br-S(=O)-[Br;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[Br;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]
null
[]
50
CELSIUS
null
null
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 7.75 ml (100 mmol) of thionyl bromide, and a water condenser, is placed 12.82 g (50 mmol) of palmitic acid. Addition of the thionyl bromide is completed with heating to about 50° C. over the course o...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HBr
O
50
null
CCCCCCCCCCCCCCCC(=O)O.O=S(Br)Br>O>CCCCCCCCCCCCCCCC(=O)Br
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-c7baff985f1c4b459347dff42e8198b7
CCCCCCCCCCCCCCCC(=O)Br.CN(CC(=O)O)C(=N)N>>CCCCCCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
C(CCCCCCCCCCCCCCC)(=O)Br.N1=CC=CC=C1.C(CCCCCCCCCCCCCCC)(=O)Br.O=C(O)CN(C)C(N)=N.C(CCCCCCCCCCCCCCC)(=O)Br.C(=O)=O.C(CCCCCCCCCCCCCCC)(=O)Br>>CN(C(=N)NC(CCCCCCCCCCCCCCC)=O)CC(=O)O
Br[C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:17].[NH2:18][C:19](=[NH:20])[N:21]([CH3:22])[CH2:23][C:24](=[O:25])[OH:26]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][C:16](=...
CCCCCCCCCCCCCCCC(=O)Br.CN(CC(=O)O)C(=N)N
CCCCCCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
null
null
ClCCl.CC(=O)C
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
null
Br-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[#7:5]-[C:6](=[N;D1;H1:7])-[NH2;D1;+0:8]>>[#7:5]-[C:6](=[N;D1;H1:7])-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
null
[]
null
null
null
null
In a dry 3-necked, round bottomed flask, equipped with a magnetic stirrer, a thermometer, a nitrogen inlet tube and the dropping funnel containing the palmitoyl bromide solution, 10.99 g (60 mmol) of creatine is suspended, with stirring, in 100 ml of dry dichloromethane. To this suspension a catalytic amount (0.1 mmol)...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
null
HBr
ClCCl.CC(=O)C
null
null
CCCCCCCCCCCCCCCC(=O)Br.CN(CC(=O)O)C(=N)N>ClCCl.CC(=O)C>CCCCCCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-010e4c3b4b894d4f82a7584883310830
CCCCCCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCCCCCCCCCCCCCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCCCCCCCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCCCCCCCCCCCC)(=O)Cl
O[C:22]([CH2:21][CH2:20][CH2:19][CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:23].O=S(Cl)[Cl:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][...
CCCCCCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl
CCCCCCCCCCCCCCCCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
45
CELSIUS
70
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 7.88 ml (108 mmol) of thionyl chloride, and a water condenser, is placed 20.44 g (60 mmol) of docosanoic acid. Addition of the thionyl chloride is completed with heating to about 45° C. over the cour...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
45
1.166667
CCCCCCCCCCCCCCCCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCCCCCCCCCCCCCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f510a0453e704f45b9eea93c4e2fb61b
CCCCCCCCCCCCCCCCCCCCCC(=O)Cl.CN(CC(=O)O)C(=N)N>>CCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
C(CCCCCCCCCCCCCCCCCCCCC)(=O)Cl.N1=CC=CC=C1.C(CCCCCCCCCCCCCCCCCCCCC)(=O)Cl.O=C(O)CN(C)C(N)=N.C(CCCCCCCCCCCCCCCCCCCCC)(=O)Cl.C(=O)=O.C(CCCCCCCCCCCCCCCCCCCCC)(=O)Cl>>C(CCCCCCCCCCC)(=O)NC(N(C)CC(=O)O)=N
CCCCCCCCCC[CH2:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](Cl)=[O:13].[NH2:14][C:15](=[NH:16])[N:17]([CH3:18])[CH2:19][C:20](=[O:21])[OH:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[NH:14][C:15](=[NH:16])[N:17]([CH3:18])[CH2:19]...
CCCCCCCCCCCCCCCCCCCCCC(=O)Cl.CN(CC(=O)O)C(=N)N
CCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
null
null
ClCCl.CC(=O)C
Acylation
OtherReaction
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
null
C-C-C-C-C-C-C-C-C-C-[CH2;D2;+0:1]-[C:2]-[C:3].Cl-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[C:7].[#7:8]-[C:9](=[N;D1;H1:10])-[NH2;D1;+0:11]>>[#7:8]-[C:9](=[N;D1;H1:10])-[NH;D2;+0:11]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[C:7].[C:3]-[C:2]-[CH3;D1;+0:1]
null
[]
null
null
null
null
In a dry 3-necked, round bottomed flask, equipped with a magnetic stirrer, a thermometer, a nitrogen inlet tube and the dropping funnel containing the docosanoyl chloride solution, 12.59 g (96 mmol) of creatine is suspended, with stirring, in 100 ml of dry dichloromethane. To this suspension a catalytic amount (0.1 mmo...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
null
HCl
ClCCl.CC(=O)C
null
null
CCCCCCCCCCCCCCCCCCCCCC(=O)Cl.CN(CC(=O)O)C(=N)N>ClCCl.CC(=O)C>CCCCCCCCCCCC(=O)NC(=N)N(C)CC(=O)O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f633fdfc486c446da53f2012bb61b1c9
CCCCCC/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl>>CCCCCC/C=C\CCCCCCCC(=O)Cl
S(=O)(Cl)Cl.S(=O)(Cl)Cl.S(=O)(Cl)Cl.C(CCCCCCC\C=C/CCCCCC)(=O)O>>C(CCCCCCC\C=C/CCCCCC)(=O)Cl
O[C:16]([CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9]/[CH:8]=[CH:7]\[CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:17].O=S(Cl)[Cl:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6]/[CH:7]=[CH:8]\[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][C:16](=[O:17])[Cl:18]
CCCCCC/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl
CCCCCC/C=C\CCCCCCCC(=O)Cl
null
null
O
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
40
CELSIUS
55
MINUTE
In a dry 2-necked, round bottomed flask, equipped with a magnetic stirrer and fixed with a separatory funnel, containing 13.15 ml (180 mmol) of thionyl chloride, and a water condenser, is placed 28.45 ml (100 mmol) of palmitoleic acid. Addition of the thionyl chloride is completed with heating to about 40° C. over the ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
O
40
0.916667
CCCCCC/C=C\CCCCCCCC(=O)O.O=S(Cl)Cl>O>CCCCCC/C=C\CCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-34c2f1a97cd04a1eb04c0d7754254a54
NN=C(c1ccccc1)c1ccccc1.O=C(Cl)CCCCl>>O=C(CCCCl)NN=C(c1ccccc1)c1ccccc1
O.ClCCCC(=O)Cl.C(C1=CC=CC=C1)(C1=CC=CC=C1)=NN.N1=CC=CC=C1>>C(C1=CC=CC=C1)(C1=CC=CC=C1)=NNC(CCCCl)=O
[NH2:7][N:8]=[C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1.Cl[C:2](=[O:1])[CH2:3][CH2:4][CH2:5][Cl:6]>>[O:1]=[C:2]([CH2:3][CH2:4][CH2:5][Cl:6])[NH:7][N:8]=[C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
NN=C(c1ccccc1)c1ccccc1.O=C(Cl)CCCCl
O=C(CCCCl)NN=C(c1ccccc1)c1ccccc1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
e1e032c84f30f6c93cf688039f3cc62747a034583f6175d60f7a0e21b27b6064
863011cce7fa0c660ac34aaac93028d203ff6ffc4b5a2233660e564db26255d2
N=C(c1ccccc1)c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[NH2;D1;+0:5]-[#7:6]=[C:7](-[c:8])-[c:9]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[#7:6]=[C:7](-[c:8])-[c:9]
null
[]
null
null
0.5
HOUR
4-Chlorobutyryl chloride (57 mL, 510 mmol) is added to a solution of benzophenone hydrazone (100 g, 510 mmol) and pyridine (41 mL, 510 mmol) in anhydrous CH2Cl2 (520 mL) under nitrogen at a rate that maintained a gentle reflux throughout the addition. The mixture is stirred for 0.5 h and poured into water (1 L). The la...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Hydrazone
Hydrazone amide
null
null
c1ccccc1.c1ccccc1
HCl
C(Cl)Cl
null
0.5
NN=C(c1ccccc1)c1ccccc1.O=C(Cl)CCCCl>C(Cl)Cl>O=C(CCCCl)NN=C(c1ccccc1)c1ccccc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-cf9535f6b3cf4b6b98d9b139abe041d0
CO.Cc1cccc(C(=O)O)n1>>COC(=O)c1cccc(C)n1
CC1=CC=CC(=N1)C(=O)O.CO.C(CCl)Cl>>COC(=O)C1=NC(=CC=C1)C
O[CH3:1].[OH:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH3:10])[n:11]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH3:10])[n:11]1
CO.Cc1cccc(C(=O)O)n1
COC(=O)c1cccc(C)n1
null
CN(C1=CC=NC=C1)C
C(Cl)Cl
Heteroatom Alkylation and Arylation
Esterification of Carboxylic Acids
961bfcd5802efbb4a2d5a1e38cbfb6654b5b78f769c3570df49b858a6f105ab6
0a622556a49b258b9020bd3a5bdd1fa9237e7093cf9b09de3a6b575ffe935dcd
c1ccncc1
O-[CH3;D1;+0:1].[#7;a:2]:[c:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6]>>[#7;a:2]:[c:3]-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[CH3;D1;+0:1]
null
[]
0
CELSIUS
6
HOUR
To a suspension of 6-methyl-pyridine-2-carboxylic Acid (10 g, 72.9 mmol) in CH2Cl2 (200 mL) cooled to 0° C. is added MeOH (10 mL), 4-dimethylaminopyridine (11.6 g, 94.8 mmol), and EDC (18.2 g, 94.8 mmol). The mixture is stirred at RT for 6 h, washed with water and brine, and dried over Na2SO4. The mixture is filtered a...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccncc1
HO-
CN(C1=CC=NC=C1)C.C(Cl)Cl
0
6
CO.Cc1cccc(C(=O)O)n1>CN(C1=CC=NC=C1)C.C(Cl)Cl>COC(=O)c1cccc(C)n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8f57fa29e9ac49ff89af3b6a105da1ce
C=CC(C)=O.Nc1cccc(Br)c1>>Cc1ccnc2cc(Br)ccc12
C(=C)C(=O)C.OS(=O)(=O)O.BrC=1C=C(N)C=CC1>>BrC1=CC=C2C(=CC=NC2=C1)C
O=[C:2]([CH3:1])[CH:3]=[CH2:4].[NH2:5][c:6]1[cH:7][c:8]([Br:9])[cH:10][cH:11][cH:12]1>>[CH3:1][c:2]1[cH:3][cH:4][n:5][c:6]2[cH:7][c:8]([Br:9])[cH:10][cH:11][c:12]12
C=CC(C)=O.Nc1cccc(Br)c1
Cc1ccnc2cc(Br)ccc12
null
null
O1CCOCC1
Aromatic Heterocycle Formation
OtherReaction
7d164ccd2a961120aaa0574a88528d2776564b1fb1b3cf378b67e98287524e77
e8439cfe055023d9132dc0595e690b94c7d2d437ab1f19554009dc0b9bd47b59
c1ccc2ncccc2c1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[CH;D2;+0:3]=[CH2;D1;+0:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[C;D1;H3:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[n;H0;D2;+0:5]:[c:6](:[c:7]):[c;H0;D3;+0:8]:1:[c:9]:[c:10]
null
[]
null
null
1
HOUR
H2SO4 (14.4 mL, 270 mmol) is added to a solution of 3-bromoaniline (Aldrich, 30.0 g, 174 mmol) in 1,4-dioxane (1 L) at RT. The mixture is heated to reflux and treated with methyl vinyl ketone (Aldrich, 19.5 mL, 270 mmol) in 1,4-dioxane (50 mL) dropwise over 3 h. Heating is continued for 1 h after the addition, followed...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine.Vinyl
null
c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HO-
O1CCOCC1
null
1
C=CC(C)=O.Nc1cccc(Br)c1>O1CCOCC1>Cc1ccnc2cc(Br)ccc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d53f2e58c9774e8984be8aeaf795a267
CO.O=C(O)CCc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1>>COC(=O)CCc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
N1=C(C=CC=C1)C=1C(=C2N(N1)CCC2)C2=CC=NC1=CC(=CC=C21)C2=CC=C(C=C2)CCC(=O)O.Cl.CO>>COC(CCC1=CC=C(C=C1)C1=CC=C2C(=CC=NC2=C1)C1=C2N(N=C1C1=NC=CC=C1)CCC2)=O
[CH3:1][OH:2].O[C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10](-[c:11]2[cH:12][cH:13][c:14]3[c:15](-[c:16]4[c:17](-[c:18]5[cH:19][cH:20][cH:21][cH:22][n:23]5)[n:24][n:25]5[c:26]4[CH2:27][CH2:28][CH2:29]5)[cH:30][cH:31][n:32][c:33]3[cH:34]2)[cH:35][cH:36]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c...
CO.O=C(O)CCc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
COC(=O)CCc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C;D1;H3:5]-[OH;D1;+0:6]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:6]-[C;D1;H3:5]
null
[]
null
null
null
null
Into a 100 mL roundbottom flask is placed 3-{4-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl]phenyl}propionic Acid (Example 30 before reverse phase purification) (160 mg, 0.35 mmol), 20 mL of MeOH, and 1.5 mL of conc HCl solution. The mixture is refluxed 3 h, and solvent removed under reduc...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1.c1ccncc1.c1cc2n(n1)CCC2.c1ccc2ncccc2c1
HO-
null
null
null
CO.O=C(O)CCc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1>>COC(=O)CCc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-9c29f6f8319341f29ceb15208efbf7dd
O=S(=O)(OCC(F)(F)F)C(F)(F)F.Oc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1>>FC(F)(F)COc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1.O=C(O)C(F)(F)F
[H-].[Na+].N1=C(C=CC=C1)C=1C(=C2N(N1)CCC2)C2=CC=NC1=CC(=CC=C21)C2=CC=C(C=C2)O.FC(COS(=O)(=O)C(F)(F)F)(F)F>>FC(C(=O)O)(F)F.N1=C(C=CC=C1)C=1C(=C2N(N1)CCC2)C2=CC=NC1=CC(=CC=C21)C2=CC=C(C=C2)OCC(F)(F)F
O=S(=[O:37])([O:39][CH2:5][C:2]([F:1])([F:3])[F:4])[C:40]([F:41])([F:42])[F:43].[OH:6][c:7]1[cH:8][cH:9][c:10](-[c:11]2[cH:12][cH:13][c:14]3[c:15](-[c:16]4[c:17](-[c:18]5[cH:19][cH:20][cH:21][cH:22][n:23]5)[n:24][n:25]5[c:26]4[CH2:27][CH2:28][CH2:29]5)[cH:30][cH:31][n:32][c:33]3[cH:34]2)[cH:35][cH:36]1>>[F:1][C:2]([F:3...
O=S(=O)(OCC(F)(F)F)C(F)(F)F.Oc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
FC(F)(F)COc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1.O=C(O)C(F)(F)F
null
null
CN(C)C=O
Acylation
OtherReaction
2d3fe6bfc9e5d1c85305db82870e16e2eb4a5b7417da03f96414efa97cc8afe5
7e6d092a6a905cf2ea3fa6e2722443d9dc2b97b08244e142b4e8ebcd7bcd451f
c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
O=S(=[O;H0;D1;+0:1])(-[O;H0;D2;+0:2]-[CH2;D2;+0:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[F;D1;H0:7])-[C;H0;D4;+0:8](-[F;D1;H0:9])(-[F;D1;H0:10])-[F;D1;H0:11].[OH;D1;+0:12]-[c:13](:[c:14]):[c:15]>>[F;D1;H0:9]-[C;H0;D4;+0:8](-[F;D1;H0:10])(-[F;D1;H0:11])-[C:16](=[O;H0;D1;+0:1])-[OH;D1;+0:2].[F;D1;H0:5]-[C:4](-[F;D1;H0:6])(-...
null
[]
70
CELSIUS
null
null
Into a 25 mL glass pressure tube fitted with Teflon screw cap and magnetic bar is placed 4-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl]phenol (Example 7 before reverse phase HPLC purification); 0.100 g, 0.25 mmol), DMF (2 mL), trifluoro-methanesulfonic acid 2,2,2-trifluoroethyl ester (0.0...
10.6084/m9.figshare.5104873.v1
null
Triflate.Aromatic alcohol
Trifluoro group.Carboxylic acid.Ether
null
null
c1ccccc1.c1ccncc1.c1cc2n(n1)CCC2.c1ccc2ncccc2c1
Other
CN(C)C=O
70
null
O=S(=O)(OCC(F)(F)F)C(F)(F)F.Oc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1>CN(C)C=O>FC(F)(F)COc1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1.O=C(O)C(F)(F)F
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f998128849b945c88d02b7863ec5f63c
CC(C)(C)OC(=O)NCCN.O=C(O)c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1>>CC(C)(C)OC(=O)NCCNC(=O)c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
N1=C(C=CC=C1)C=1C(=C2N(N1)CCC2)C2=CC=NC1=CC(=CC=C21)C2=CC=C(C(=O)O)C=C2.C(C)(C)(C)OC(NCCN)=O.CN(C)C(=[N+](C)C)ON1C2=C(C=CC=C2)N=N1.F[P-](F)(F)(F)(F)F>>C(C)(C)(C)OC(NCCNC(C1=CC=C(C=C1)C1=CC=C2C(=CC=NC2=C1)C1=C2N(N=C1C1=NC=CC=C1)CCC2)=O)=O
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH2:9][CH2:10][NH2:11].O[C:12](=[O:13])[c:14]1[cH:15][cH:16][c:17](-[c:18]2[cH:19][cH:20][c:21]3[c:22](-[c:23]4[c:24](-[c:25]5[cH:26][cH:27][cH:28][cH:29][n:30]5)[n:31][n:32]5[c:33]4[CH2:34][CH2:35][CH2:36]5)[cH:37][cH:38][n:39][c:40]3[cH:41]2)[cH:42][cH:43]1>>[CH3...
CC(C)(C)OC(=O)NCCN.O=C(O)c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
CC(C)(C)OC(=O)NCCNC(=O)c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
null
null
CN(C)C=O.CCOC(=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
8
HOUR
4-[4-(2-Pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolin-7-yl]-benzoic acid (Example 41 before reverse phase chromatography, 0.08 g, 0.185 mmol), (2-aminoethyl)-carbamic acid tert-butyl ester (0.036 g, 0.2 mmol), N—N-Diisopropylethylamine (0.08 mL, 0.46 mmol) and HBTU (0.076 g, 0.2 mmol) are mixed in 10...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccncc1.c1cc2n(n1)CCC2.c1ccc2ncccc2c1
HO-
CN(C)C=O.CCOC(=O)C
null
8
CC(C)(C)OC(=O)NCCN.O=C(O)c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1>CN(C)C=O.CCOC(=O)C>CC(C)(C)OC(=O)NCCNC(=O)c1ccc(-c2ccc3c(-c4c(-c5ccccn5)nn5c4CCC5)ccnc3c2)cc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-fb29c5481180486292375ef17481b9f6
CCCCCCCCCCCC(=O)c1ccc2cc(O)ccc2c1.CN>>CCCCCCCCCCCC(=O)c1ccc2cc(NC)ccc2c1
CN.Cl.OC1=CC2=CC=C(C=C2C=C1)C(CCCCCCCCCCC)=O.[OH-].[Na+]>>C(CCCCCCCCCCC)(=O)C=1C=C2C=CC(=CC2=CC1)NC
O[c:19]1[cH:18][c:17]2[cH:16][cH:15][c:14]([C:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:13])[cH:25][c:24]2[cH:23][cH:22]1.[NH2:20][CH3:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][c:17]2[cH:18][c:19...
CCCCCCCCCCCC(=O)c1ccc2cc(O)ccc2c1.CN
CCCCCCCCCCCC(=O)c1ccc2cc(NC)ccc2c1
null
null
O
Heteroatom Alkylation and Arylation
Reductive amination with alcohol
de3f59587802c5fbb12e4a6a2c857c24b6ffebe3ab2996064124a48d15e13249
d1ce63afd91e9f43d522aac919284b7f154a7b1ed206dc2b146286d54897dcb1
c1ccc2ccccc2c1
O-[c;H0;D3;+0:1](:[c: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](:[c:2]:[c:3]):[c:4]:[c:5]
67
[{"value": 67.0, "product": "C(CCCCCCCCCCC)(=O)C=1C=C2C=CC(=CC2=CC1)NC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.0, "product": "C(CCCCCCCCCCC)(=O)C=1C=C2C=CC(=CC2=CC1)NC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
140
CELSIUS
48
HOUR
MeNH2.HCl (11.0 g, 0.13 mol) was added to a mixture of 2-hydroxy-6-dodecanoylnaphthalene (8.0 g, 25 mmol), Na2S2O5 (12 g, 61 mmol), NaOH (5.2 g, 0.13 mol) and water (100 ml) in a high-pressure tube. The resulting mixture was stirred at 140° C. for 48 hours, followed by filtration to collect a solid. The solid was suffi...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Primary amine
Secondary amine
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
HO-
O
140
48
CCCCCCCCCCCC(=O)c1ccc2cc(O)ccc2c1.CN>O>CCCCCCCCCCCC(=O)c1ccc2cc(NC)ccc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a91725a931084092b21bc00e3cae7e72
CNc1ccc2cc(Br)ccc2c1>>CNc1ccc2cc(C#N)ccc2c1
BrC=1C=C2C=CC(=CC2=CC1)NC.[Cu]C#N>>CNC=1C=C2C=CC(=CC2=CC1)C#N
Br[c:8]1[cH:7][c:6]2[cH:5][cH:4][c:3]([NH:2][CH3:1])[cH:14][c:13]2[cH:12][cH:11]1>>[CH3:1][NH:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][c:8]([C:9]#[N:10])[cH:11][cH:12][c:13]2[cH:14]1
CNc1ccc2cc(Br)ccc2c1
CNc1ccc2cc(C#N)ccc2c1
null
null
N1=CC=CC=C1
Miscellaneous
OtherReaction
6b2e76ea725bec0f478425d10a420e3873896604ae33af70efc4c0461fad2cf4
73a96fe5e833259ca394a42f82d6cc2ee7231bcde92d95030d2893b90c3fef76
c1ccc2ccccc2c1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]>>[N;D1;H0:6]#[C:7]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
71
[{"value": 71.0, "product": "CNC=1C=C2C=CC(=CC2=CC1)C#N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.0, "product": "CNC=1C=C2C=CC(=CC2=CC1)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
220
CELSIUS
4
HOUR
A solution of 6-bromo-N-methyl-2-naphthylamine (2.0 g, 8.5 mmol) in pyridine (50 ml) was added to copper (I) cyanide (1.1 g, 12.3 mmol). The mixture was stirred at 220° C. for 4 hours. The reaction mixture was allowed to cool to room temperature, extracted with dichloromethane, washed with an aqueous solution of hethyl...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Nitrile
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
Br-
N1=CC=CC=C1
220
4
CNc1ccc2cc(Br)ccc2c1>N1=CC=CC=C1>CNc1ccc2cc(C#N)ccc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2e260b1673e6470d921969f0b18aab52
CNc1ccc2cc(C#N)ccc2c1.O=S(=O)(O)O>>CNc1ccc2cc(C=O)ccc2c1
S(O)(O)(=O)=O.[H-].C(C(C)C)[Al+]CC(C)C.CNC=1C=C2C=CC(=CC2=CC1)C#N.[Cl-].[NH4+]>>C(=O)C=1C=C2C=CC(=CC2=CC1)NC
N#[C:9][c:8]1[cH:7][c:6]2[cH:5][cH:4][c:3]([NH:2][CH3:1])[cH:14][c:13]2[cH:12][cH:11]1.O=S(O)(O)=[O:10]>>[CH3:1][NH:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][c:8]([CH:9]=[O:10])[cH:11][cH:12][c:13]2[cH:14]1
CNc1ccc2cc(C#N)ccc2c1.O=S(=O)(O)O
CNc1ccc2cc(C=O)ccc2c1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
26082e4725cd2a7c1eb6362fc44981286c2087c015aba2f1b570103659ffb41e
e783d65987caa6ceae095ff666413e4c8d25ead96c003eb4f99d66fc68c0b0bb
c1ccc2ccccc2c1
N#[C;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].O-S(-O)(=O)=[O;H0;D1;+0:5]>>[O;H0;D1;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
89
[{"value": 89.0, "product": "C(=O)C=1C=C2C=CC(=CC2=CC1)NC", "details": "PERCENTYIELD", "is_desired": false}]
-78
CELSIUS
4
HOUR
A solution of 6-methylamino-2-naphthonitrile (0.84 g, 4.6 mmol) prepared above in toluene (50 ml) was mixed with diisobutylaluminum hydride (9 ml, 1.0M (in toluene)) under a nitrogen atmosphere at −70° C. The mixture was stirred at −78° C. for 30 minutes and at room temperature for 4 hours. The mixture was added to a s...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Aldehyde
null
null
c1ccc2ccccc2c1
HO-
C1(=CC=CC=C1)C
-78
4
CNc1ccc2cc(C#N)ccc2c1.O=S(=O)(O)O>C1(=CC=CC=C1)C>CNc1ccc2cc(C=O)ccc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-29af8fcf6b5d4a7ebf5b3ffd1d149c60
CCCCCCCCCCCCCl.COc1ccc2ccccc2c1.O=[N+]([O-])c1ccccc1>>CCCCCCCCCCCC(=O)c1ccc2cc(OC)ccc2c1
Cl.COC1=CC2=CC=CC=C2C=C1.[Cl-].[Al+3].[Cl-].[Cl-].[N+](=O)([O-])C1=CC=CC=C1.C(CCCCCCCCCCC)Cl>>COC1=CC2=CC=C(C=C2C=C1)C(CCCCCCCCCCC)=O
Cl[CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[cH:14]1[cH:15][cH:16][c:17]2[cH:18][c:19]([O:20][CH3:21])[cH:22][cH:23][c:24]2[cH:25]1.[O-][N+](c1ccccc1)=[O:13]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[c:14]1[cH:15][cH:16]...
CCCCCCCCCCCCCl.COc1ccc2ccccc2c1.O=[N+]([O-])c1ccccc1
CCCCCCCCCCCC(=O)c1ccc2cc(OC)ccc2c1
null
null
null
Functional Group Interconversion
OtherReaction
a9128a0af2a4286c9286039fe20650f14721e9388d501c4cbd9e7e604a639916
70f17c63a4b7105b0ea445fe2f2d68b2827b89eef89e402d0e06628e53d5c930
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[O-]-[N+](=[O;H0;D1;+0:4])-c1:c:c:c:c:c:1.[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[C:3]-[C:2]-[C;H0;D3;+0:1](=[O;H0;D1;+0:4])-[c;H0;D3;+0:7](:[c:6]:[c:5]):[c:8]:[c:9]
64.2
[{"value": 64.2, "product": "COC1=CC2=CC=C(C=C2C=C1)C(CCCCCCCCCCC)=O", "details": "PERCENTYIELD", "is_desired": false}]
5
CELSIUS
12
HOUR
2-Methoxynaphthalene (30.1 g, 0.19 mol) was added to a solution of aluminum chloride (32.9 g, 0.25 mol) in anhydrous nitrobenzene under a nitrogen atmosphere. To the mixture was slowly added dropwise lauryl chloride (41.6 g, 0.19 mol) at 10-13° C. over 15 minutes. The resulting mixture was stirred at 5° C. for 2 hours ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Nitro group
Ketone
c1ccc2ccccc2c1.c1ccccc1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
HCl
null
5
12
CCCCCCCCCCCCCl.COc1ccc2ccccc2c1.O=[N+]([O-])c1ccccc1>>CCCCCCCCCCCC(=O)c1ccc2cc(OC)ccc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-a0f61b78c625438bb6a9ed18d1ebb3d2
CCCCCCCCCCCC(=O)c1ccc2cc(OC)ccc2c1.CNC>>CCCCCCCCCCCC(=O)c1ccc2cc(N(C)C)ccc2c1
CNC.CN(C)P(=O)(N(C)C)N(C)C.COC1=CC2=CC=C(C=C2C=C1)C(CCCCCCCCCCC)=O>>CCCCCCCCCCCC(=O)C1=CC2=C(C=C1)C=C(C=C2)N(C)C
CO[c:19]1[cH:18][c:17]2[cH:16][cH:15][c:14]([C:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:13])[cH:26][c:25]2[cH:24][cH:23]1.[NH:20]([CH3:21])[CH3:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][c:17]2[c...
CCCCCCCCCCCC(=O)c1ccc2cc(OC)ccc2c1.CNC
CCCCCCCCCCCC(=O)c1ccc2cc(N(C)C)ccc2c1
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
Displacement of ethoxy group by secondary amine
6326e1db93c48a78fa64ccca67243ca05322ff7c1916e72f48454573b2cf23b4
f41a0ac1ece338534be38b696cb3541e6003cebbbc2e76e91361a568e6946ab0
c1ccc2ccccc2c1
C-O-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C;D1;H3:6]-[NH;D2;+0:7]-[C;D1;H3:8]>>[C;D1;H3:6]-[N;H0;D3;+0:7](-[C;D1;H3:8])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
66
[{"value": 66.0, "product": "CCCCCCCCCCCC(=O)C1=CC2=C(C=C1)C=C(C=C2)N(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Li (0.5 g, 70 mmol) was added to HMPA (20 ml) and benzene (30 ml), and then dimethylamine (3.5 g, 78 mmol) was added dropwise thereto. The mixture was violently stirred for one hour. To the resulting mixture was added 2-methoxy-6-dodecanoylnaphthalene (7.3 g, 22 mmol) prepared in Comparative Example 1-(1) all at one ti...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Tertiary amine
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
HO-
C1=CC=CC=C1
null
1
CCCCCCCCCCCC(=O)c1ccc2cc(OC)ccc2c1.CNC>C1=CC=CC=C1>CCCCCCCCCCCC(=O)c1ccc2cc(N(C)C)ccc2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-69b8d738db8e4760bc17caad85c5f98d
Cc1ccc(Cl)cc1.Cc1ccc(S(=O)c2ccc(C)cc2)cc1>>Cc1ccc([S+](c2ccc(C)cc2)c2ccc(C)cc2)cc1.[Cl-]
CC1=CC=C(C=C1)S(=O)C1=CC=C(C=C1)C.ClC1=CC=C(C=C1)C>>[Cl-].CC1=CC=C(C=C1)[S+](C1=CC=C(C=C1)C)C1=CC=C(C=C1)C
[c:14]1([Cl:23])[cH:15][cH:16][c:17]([CH3:18])[cH:19][cH:20]1.O=[S:6]([c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:22][cH:21]1)[c:7]1[cH:8][cH:9][c:10]([CH3:11])[cH:12][cH:13]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([S+:6]([c:7]2[cH:8][cH:9][c:10]([CH3:11])[cH:12][cH:13]2)[c:14]2[cH:15][cH:16][c:17]([CH3:18])[cH:19][cH:20]2)[cH:21][cH...
Cc1ccc(Cl)cc1.Cc1ccc(S(=O)c2ccc(C)cc2)cc1
Cc1ccc([S+](c2ccc(C)cc2)c2ccc(C)cc2)cc1.[Cl-]
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
b7fca8eeb731d381e222beb473d8e55fa6d5f2f0a2f48cd3a0fb40a9c5698a75
31d32474c31cc1c196190b139dce413ab579369dcdb12c0b32f09d6175566440
c1ccc([S+](c2ccccc2)c2ccccc2)cc1
O=[S;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7].[Cl;H0;D1;+0:8]-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]>>[Cl-;H0;D0:8].[c:6]:[c:5](-[S+;H0;D3:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]):[c:7]
null
[]
null
null
null
null
The target compound was obtained by following the procedure of Synthesis Example 1 aside from using bis(4-methylphenyl)sulfoxide instead of the diphenyl sulfoxide and 4-chlorotoluene instead of the chlorobenzene in Synthesis Example 1, and increasing the amount of water for extraction. Conditions: See reaction.notes.pr...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Sulfoxide
null
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
Other
O
null
null
Cc1ccc(Cl)cc1.Cc1ccc(S(=O)c2ccc(C)cc2)cc1>O>Cc1ccc([S+](c2ccc(C)cc2)c2ccc(C)cc2)cc1.[Cl-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-952cf908abad47d3bc945c1b45e936dc
CC(C)(C)c1ccc(Br)cc1.CC(C)(C)c1ccc(S(=O)c2ccc(C(C)(C)C)cc2)cc1>>CC(C)(C)c1ccc([S+](c2ccc(C(C)(C)C)cc2)c2ccc(C(C)(C)C)cc2)cc1.[Br-]
C(C)(C)(C)C1=CC=C(C=C1)S(=O)C1=CC=C(C=C1)C(C)(C)C.C(C)(C)(C)C1=CC=C(C=C1)Br>>[Br-].C(C)(C)(C)C1=CC=C(C=C1)[S+](C1=CC=C(C=C1)C(C)(C)C)C1=CC=C(C=C1)C(C)(C)C
[c:10]1([Br:32])[cH:11][cH:12][c:13]([C:14]([CH3:15])([CH3:16])[CH3:17])[cH:18][cH:19]1.O=[S:9]([c:8]1[cH:7][cH:6][c:5]([C:2]([CH3:1])([CH3:3])[CH3:4])[cH:31][cH:30]1)[c:20]1[cH:21][cH:22][c:23]([C:24]([CH3:25])([CH3:26])[CH3:27])[cH:28][cH:29]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][cH:7][c:8]([S+:9]([c:10]2[cH:1...
CC(C)(C)c1ccc(Br)cc1.CC(C)(C)c1ccc(S(=O)c2ccc(C(C)(C)C)cc2)cc1
CC(C)(C)c1ccc([S+](c2ccc(C(C)(C)C)cc2)c2ccc(C(C)(C)C)cc2)cc1.[Br-]
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
b7fca8eeb731d381e222beb473d8e55fa6d5f2f0a2f48cd3a0fb40a9c5698a75
31d32474c31cc1c196190b139dce413ab579369dcdb12c0b32f09d6175566440
c1ccc([S+](c2ccccc2)c2ccccc2)cc1
O=[S;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7].[Br;H0;D1;+0:8]-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]>>[Br-;H0;D0:8].[c:11]:[c:10]:[c;H0;D3;+0:9](-[S+;H0;D3:1](-[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7]):[c:12]:[c:13]
null
[]
null
null
null
null
The target compound was obtained by following the procedure of Synthesis Example 1 aside from using bis(4-tert-butylphenyl)sulfoxide instead of the diphenyl sulfoxide and 4-tert-butylbromobenzene instead of the chlorobenzene in Synthesis Example 1, and increasing the amount of water for extraction. Conditions: See reac...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Sulfoxide
null
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
Other
O
null
null
CC(C)(C)c1ccc(Br)cc1.CC(C)(C)c1ccc(S(=O)c2ccc(C(C)(C)C)cc2)cc1>O>CC(C)(C)c1ccc([S+](c2ccc(C(C)(C)C)cc2)c2ccc(C(C)(C)C)cc2)cc1.[Br-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-49dfe19fd3e547f8a63a6c386e43abce
C1CCSC1.O=C(CBr)c1ccccc1>>O=C(C[S+]1CCCC1)c1ccccc1.[Br-]
C(C(=O)C1=CC=CC=C1)Br.S1CCCC1.O.C(C)OCC>>[Br-].C(C(=O)C1=CC=CC=C1)[S+]1CCCC1
[S:4]1[CH2:5][CH2:6][CH2:7][CH2:8]1.[O:1]=[C:2]([CH2:3][Br:15])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[O:1]=[C:2]([CH2:3][S+:4]1[CH2:5][CH2:6][CH2:7][CH2:8]1)[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[Br-:15]
C1CCSC1.O=C(CBr)c1ccccc1
O=C(C[S+]1CCCC1)c1ccccc1.[Br-]
null
null
[N+](=O)([O-])C
Functional Group Interconversion
OtherReaction
85f24012cc235dcc2174546a7acc1a27fcb95f75402893a368fc99d3ab479d23
243e6d69a1ef4217446cfc3f9974b61aa23bfb74648883a134f35ef9c12f90f1
O=C(C[S+]1CCCC1)c1ccccc1
[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[C:3](=[O;D1;H0:4])-[c:5].[C:6]1-[C:7]-[C:8]-[C:9]-[S;H0;D2;+0:10]-1>>[Br-;H0;D0:1].[O;D1;H0:4]=[C:3](-[c:5])-[CH2;D2;+0:2]-[S+;H0;D3:10]1-[C:6]-[C:7]-[C:8]-[C:9]-1
null
[]
null
null
4
HOUR
88.2 g (0.44 mole) of phenacyl bromide and 39.1 g (0.44 mole) of tetrahydrothiophene were dissolved in 220 g of nitromethane, which was stirred for 4 hours at room temperature. 800 g of water and 400 g of diethyl ether were added to the reaction solution whereupon the mixture separated into two layers. The aqueous laye...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Monosulfide
Ketone
C1CCSC1
C1CC[S+]C1
C1CC[S+]C1.c1ccccc1
null
[N+](=O)([O-])C
null
4
C1CCSC1.O=C(CBr)c1ccccc1>[N+](=O)([O-])C>O=C(C[S+]1CCCC1)c1ccccc1.[Br-]
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d3b0e7f48d424e0781af1e3bf1e69ea3
COS(=O)(=O)OC.CSc1ccccc1>>C[S+](C)c1ccccc1.O=S(=O)([O-])O
C1(=CC=CC=C1)SC.S(=O)(=O)(OC)OC.O>>S(=O)(=O)(O)[O-].C[S+](C1=CC=CC=C1)C
C[O:13][S:11](=[O:10])(=[O:12])[O:14][CH3:3].[CH3:1][S:2][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1>>[CH3:1][S+:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1.[O:10]=[S:11](=[O:12])([O-:13])[OH:14]
COS(=O)(=O)OC.CSc1ccccc1
C[S+](C)c1ccccc1.O=S(=O)([O-])O
null
null
C(C)OCC
Protection
OtherReaction
a27abd92746860a3a2d8385da23c5a6d6da58ebae8a1f56d03eb57f286c2ced2
fd6f5097e6b4b848368a6acbac5c2fc1c3716ca071296766b72a424c32f5899c
c1ccccc1
C-[O;H0;D2;+0:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH3;D1;+0:6].[C;D1;H3:7]-[S;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[C;D1;H3:7]-[S+;H0;D3:8](-[CH3;D1;+0:6])-[c:9](:[c:10]):[c:11].[O-;H0;D1:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[OH;D1;+0:5]
null
[]
null
null
null
null
6.2 g (0.05 mole) of thioanisole and 6.9 g (0.055 mole) of dimethyl sulfate were stirred for 12 hours at room temperature. 100 g of water and 50 ml of diethyl ether were added to the reaction solution whereupon the mixture separated into two layers. The aqueous layer was taken out, which was an aqueous solution of the ...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
null
null
null
c1ccccc1
Other
C(C)OCC
null
null
COS(=O)(=O)OC.CSc1ccccc1>C(C)OCC>C[S+](C)c1ccccc1.O=S(=O)([O-])O