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-02ee2261663048188cf6d85d2cc96e3f
ord-cc6c87b9be304b508b4408d695432fd7
CC(C)(C)OC(=O)N1CC[N+](C)(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4nsc(N)n4)[C@H]3SC2)CC1>>C[N+]1(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4nsc(N)n4)[C@H]3SC2)CCNCC1
C(=O)O.FC(C(=O)O)(F)F.Cl.NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)OC(C)(C)C)C)C(=O)[O-])C1=O)=NOCC(=O)O>>NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCNCC2)C)C(=O)[O-])C1=O)=NOCC(=O)O
CC(C)(C)OC(=O)[N:34]1[CH2:33][CH2:32][N+:2]([CH3:1])([CH2:3][C:4]2=[C:5]([C:6](=[O:7])[O-:8])[N:9]3[C:10](=[O:11])[C@@H:12]([NH:13][C:14](=[O:15])[C:16](=[N:17][O:18][CH2:19][C:20](=[O:21])[OH:22])[c:23]4[n:24][s:25][c:26]([NH2:27])[n:28]4)[C@H:29]3[S:30][CH2:31]2)[CH2:36][CH2:35]1>>[CH3:1][N+:2]1([CH2:3][C:4]2=[C:5]([...
CC(C)(C)OC(=O)N1CC[N+](C)(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4nsc(N)n4)[C@H]3SC2)CC1
C[N+]1(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4nsc(N)n4)[C@H]3SC2)CCNCC1
null
null
C(C)(=O)OCC
Reduction
Boc amine deprotection
948da1202b15332e9a720370b2898a983e40f7f79e8dc94eb151be23c601d994
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCNCC3)CS[C@H]12)c1ncsn1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7;+:4]-[C:5]-[C:6]-1>>[#7;+:4]1-[C:3]-[C:2]-[NH;D2;+0:1]-[C:6]-[C:5]-1
33
[{"value": 33.0, "product": "NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCNCC2)C)C(=O)[O-])C1=O)=NOCC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
To a mixture of formic acid (10 ml) and trifluoroacetic acid (5 ml) was added 7β-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-carboxymethoxyiminoacetamido]-3-(1-methyl-4-tert-butoxycarbonyl-1-piperazinio)methyl-3-cephem-4-carboxylate hydrochloride (syn isomer) (5.7 g) at 20° C. under stirring. The stirring was continued for 1....
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
C1C[NH+]CC[NH]1
C1C[NH+]CCN1
C1=CN2CC[C@H]2SC1.c1ncsn1.C1C[NH+]CCN1
HO-
C(C)(=O)OCC
null
1.5
CC(C)(C)OC(=O)N1CC[N+](C)(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4nsc(N)n4)[C@H]3SC2)CC1>C(C)(=O)OCC>C[N+]1(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4nsc(N)n4)[C@H]3SC2)CCNCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6f6c5d046c9e4fcab21226b8290da43a
CN1CCN(C(=O)OC(C)(C)C)CC1.CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1nsc(N)n1>>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1
C(C)(=O)OCC.FC(C(=O)O)(F)F.NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)CCl)C(=O)O)C1=O)=NOC.CN1CCN(CC1)C(=O)OC(C)(C)C>>NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCNCC2)C)C(=O)[O-])C1=O)=NOC
CC(C)(C)OC(=O)[N:22]1[CH2:21][CH2:20][N:18]([CH3:19])[CH2:24][CH2:23]1.Cl[CH2:17][C:16]1=[C:12]([C:13](=[O:14])[OH:15])[N:11]2[C:9](=[O:10])[C@@H:8]([NH:7][C:5]([C:4](=[N:3][O:2][CH3:1])[c:28]3[n:29][s:30][c:31]([NH2:32])[n:33]3)=[O:6])[C@H:27]2[S:26][CH2:25]1>>[CH3:1][O:2][N:3]=[C:4]([C:5](=[O:6])[NH:7][C@@H:8]1[C:9](...
CN1CCN(C(=O)OC(C)(C)C)CC1.CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1nsc(N)n1
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
37ec5efd319715498aa716286cb5dbe164886d3b85a5337c2ffefe62bda054e7
01357b708f58664aeab786c7735bff696889ae4504065f45cfe2fc04b7ed3069
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCNCC3)CS[C@H]12)c1ncsn1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[N;H0;D3;+0:4](-[C;D1;H3:5])-[C:6]-[C:7]-1.Cl-[CH2;D2;+0:8]-[C:9](=[C:10](-[C:11](=[O;D1;H0:12])-[OH;D1;+0:13])-[#7:14]-[C:15]=[O;D1;H0:16])-[C:17]-[#16:18]>>[#16:18]-[C:17]-[C:9](-[CH2;D2;+0:8]-[N+;H0;D4:4]1(-[C;D1;H3:5])-[C:3]-[C:2]-[NH;D2;+0:1]-[C:7]-[C:6]-1)=[C:10](-[...
null
[]
null
null
30
MINUTE
To a solution of 7β-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-methoxyiminoacetamido]-3-chloromethyl-3-cephem-4-carboxylic acid trifluoroacetate (syn isomer) in N,N-dimethylformamide (150 ml) was added 1-methyl-4-tert-butoxycarbonylpiperazine (30 g). After being stirred at room temperature for 30 minutes, the mixture was add...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbamic ester.Carboxylic acid.Ether.Tertiary amine.Boc
Secondary amine
C1C[NH]CC[NH]1
C1C[NH+]CCN1
C1=CN2CC[C@H]2SC1.C1C[NH+]CCN1.c1ncsn1
HCl
CN(C=O)C
null
0.5
CN1CCN(C(=O)OC(C)(C)C)CC1.CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1nsc(N)n1>CN(C=O)C>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fb89a90e5efb421fbb23e563617fd178
CC(C)(C)OC(=O)CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)OC(C)(C)C)CC3)CS[C@H]12)c1csc(NC=O)n1>>C[N+]1(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4csc(N)n4)[C@H]3SC2)CCNCC1
Cl.C(=O)NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)OC(C)(C)C)C)C(=O)[O-])C1=O)=NOCC(=O)OC(C)(C)C.Cl.C(C)(=O)OCC>>NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCNCC2)C)C(=O)[O-])C1=O)=NOCC(=O)O
CC(C)(C)OC(=O)[N:34]1[CH2:33][CH2:32][N+:2]([CH3:1])([CH2:3][C:4]2=[C:5]([C:6](=[O:7])[O-:8])[N:9]3[C:10](=[O:11])[C@@H:12]([NH:13][C:14](=[O:15])[C:16](=[N:17][O:18][CH2:19][C:20](=[O:21])[O:22]C(C)(C)C)[c:23]4[cH:24][s:25][c:26]([NH:27]C=O)[n:28]4)[C@H:29]3[S:30][CH2:31]2)[CH2:36][CH2:35]1>>[CH3:1][N+:2]1([CH2:3][C:4...
CC(C)(C)OC(=O)CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)OC(C)(C)C)CC3)CS[C@H]12)c1csc(NC=O)n1
C[N+]1(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4csc(N)n4)[C@H]3SC2)CCNCC1
null
null
CO
Reduction
OtherReaction
bf9f37cb6352d975706fe0f05561dfa28add5a55ca2b6e731ff11a924eae65d8
0f151cf844bf1bb06ac48600a770444e4c8cc62144896aac3c26c07a465f07d0
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCNCC3)CS[C@H]12)c1cscn1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7;+:4]-[C:5]-[C:6]-1.C-C(-C)(-C)-[O;H0;D2;+0:7]-[C:8](-[C:9])=[O;D1;H0:10].O=C-[NH;D2;+0:11]-[c:12]1:[#16;a:13]:[c:14]:[c:15]:[#7;a:16]:1>>[#7;+:4]1-[C:3]-[C:2]-[NH;D2;+0:1]-[C:6]-[C:5]-1.[C:9]-[C:8](=[O;D1;H0:10])-[OH;D1;+0:7].[NH2;D1;+0:11]-[c:12]1:[#16;a:13]:[c:14]:[...
26.7
[{"value": 26.7, "product": "NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCNCC2)C)C(=O)[O-])C1=O)=NOCC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4.5
HOUR
To a suspension of 7β-[2-(2-formamidothiazol-4-yl)-2-tert-butoxycarbonylmethoxyiminoacetamido]-3-(1-methyl-4-tert-butoxycarbonyl-1-piperazinio)methyl-3-cephem-4-carboxylate hydrochloride (syn isomer) (4.02 g) in methanol (12 ml) was added conc. hydrochloric acid (4.4 ml) at 10° C. The resulting solution was warmed to r...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ester.Ether.Secondary amide.Boc.Boc
Carboxylic acid.Primary amine.Secondary amine
C1C[NH+]CC[NH]1
C1C[NH+]CCN1
C1=CN2CC[C@H]2SC1.c1cscn1.C1C[NH+]CCN1
HO-
CO
null
4.5
CC(C)(C)OC(=O)CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)OC(C)(C)C)CC3)CS[C@H]12)c1csc(NC=O)n1>CO>C[N+]1(CC2=C(C(=O)[O-])N3C(=O)[C@@H](NC(=O)C(=NOCC(=O)O)c4csc(N)n4)[C@H]3SC2)CCNCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-55ffa67baea94d4f88c43cf174843b6b
CN1CCN(C(=O)c2ccc(O)c(O)c2)CC1.CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1csc(NC=O)n1>>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(NC=O)n1
C(C)(=O)OCC.C(=O)NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)CCl)C(=O)O)C1=O)=NOC.CN1CCN(CC1)C(C1=CC(=C(C=C1)O)O)=O>>C(=O)NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(C2=CC(=C(C=C2)O)O)=O)C)C(=O)[O-])C1=O)=NOC
[N:18]1([CH3:19])[CH2:20][CH2:21][N:22]([C:23](=[O:24])[c:25]2[cH:26][cH:27][c:28]([OH:29])[c:30]([OH:31])[cH:32]2)[CH2:33][CH2:34]1.Cl[CH2:17][C:16]1=[C:12]([C:13](=[O:14])[OH:15])[N:11]2[C:9](=[O:10])[C@@H:8]([NH:7][C:5]([C:4](=[N:3][O:2][CH3:1])[c:38]3[cH:39][s:40][c:41]([NH:42][CH:43]=[O:44])[n:45]3)=[O:6])[C@H:37]...
CN1CCN(C(=O)c2ccc(O)c(O)c2)CC1.CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1csc(NC=O)n1
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(NC=O)n1
null
null
CN(C=O)C
Functional Group Interconversion
OtherReaction
511bf7d10783e9de01f4ae658b25b30801ba121b9d0efc2589106127c89aaa03
c8557186a9769d56d4131cf98797065b79da099d927f5093fc211d3e2ca1f543
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCN(C(=O)c4ccccc4)CC3)CS[C@H]12)c1cscn1
Cl-[CH2;D2;+0:1]-[C:2](=[C:3](-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6])-[#7:7]-[C:8]=[O;D1;H0:9])-[C:10]-[#16:11].[C;D1;H3:12]-[N;H0;D3;+0:13]1-[C:14]-[C:15]-[#7:16]-[C:17]-[C:18]-1>>[#16:11]-[C:10]-[C:2](-[CH2;D2;+0:1]-[N+;H0;D4:13]1(-[C;D1;H3:12])-[C:14]-[C:15]-[#7:16]-[C:17]-[C:18]-1)=[C:3](-[C:4](-[O-;H0;D1:6])=[O;D1;H0:5...
115.9
[{"value": 115.9, "product": "C(=O)NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(C2=CC(=C(C=C2)O)O)=O)C)C(=O)[O-])C1=O)=NOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
3.5
HOUR
To a solution of 7β-[2-(2-formamidothiazol-4-yl)-2-methoxyiminoacetamido]-3-chloromethyl-3-cephem-4-carboxylic acid (syn isomer) (920 mg) in N,N-dimethylformamide (5 ml) was added 1-methyl-4-(3,4-dihydroxybenzoyl)piperazine (945 mg) at 0° C. and the mixture was stirred at 0° C. for 3.5 hours. The mixture was added drop...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid.Tertiary amine
null
C1C[NH]CC[NH]1
C1C[NH+]CC[NH]1
C1=CN2CC[C@H]2SC1.C1C[NH+]CC[NH]1.c1ccccc1.c1cscn1
HCl
CN(C=O)C
0
3.5
CN1CCN(C(=O)c2ccc(O)c(O)c2)CC1.CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1csc(NC=O)n1>CN(C=O)C>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(NC=O)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1f2f42fc73044a5984d82eb3c72b03d5
C=CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1nsc(N)n1.CN1CCN(C(=O)c2cc(O)c(O)cn2)CC1>>C=CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
C(C)(=O)OCC.C(C)C(C(=O)[O-])CCCC.[Na+].CN1CCN(CC1)C(=O)C1=NC=C(C(=C1)O)O.FC(C(=O)O)(F)F.NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)CCl)C(=O)O)C1=O)=NOCC=C>>NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)C2=NC=C(C(=C2)O)O)C)C(=O)[O-])C1=O)=NOCC=C
Cl[CH2:19][C:18]1=[C:14]([C:15](=[O:16])[OH:17])[N:13]2[C:11](=[O:12])[C@@H:10]([NH:9][C:7]([C:6](=[N:5][O:4][CH2:3][CH:2]=[CH2:1])[c:40]3[n:41][s:42][c:43]([NH2:44])[n:45]3)=[O:8])[C@H:39]2[S:38][CH2:37]1.[N:20]1([CH3:21])[CH2:22][CH2:23][N:24]([C:25](=[O:26])[c:27]2[cH:28][c:29]([OH:30])[c:31]([OH:32])[cH:33][n:34]2)...
C=CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1nsc(N)n1.CN1CCN(C(=O)c2cc(O)c(O)cn2)CC1
C=CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
null
null
CS(=O)C
Functional Group Interconversion
OtherReaction
511bf7d10783e9de01f4ae658b25b30801ba121b9d0efc2589106127c89aaa03
c8557186a9769d56d4131cf98797065b79da099d927f5093fc211d3e2ca1f543
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCN(C(=O)c4ccccn4)CC3)CS[C@H]12)c1ncsn1
Cl-[CH2;D2;+0:1]-[C:2](=[C:3](-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6])-[#7:7]-[C:8]=[O;D1;H0:9])-[C:10]-[#16:11].[C;D1;H3:12]-[N;H0;D3;+0:13]1-[C:14]-[C:15]-[#7:16]-[C:17]-[C:18]-1>>[#16:11]-[C:10]-[C:2](-[CH2;D2;+0:1]-[N+;H0;D4:13]1(-[C;D1;H3:12])-[C:14]-[C:15]-[#7:16]-[C:17]-[C:18]-1)=[C:3](-[C:4](-[O-;H0;D1:6])=[O;D1;H0:5...
34.2
[{"value": 34.2, "product": "NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)C2=NC=C(C(=C2)O)O)C)C(=O)[O-])C1=O)=NOCC=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a suspension of 1-methyl-4-(4,5-dihydroxy-2-pyridylcarbonyl)piperazine (800 mg) in dimethyl sulfoxide (8 ml) was added sodium 2-ethylhexanoate (840 mg). The solution was added dropwise a solution of 7β-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-allyloxyiminoacetamido]-3-chloromethyl-3-cephem-4-carboxylate trifluoroacetate...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid.Tertiary amine
null
C1C[NH]CC[NH]1
C1C[NH+]CC[NH]1
C1=CN2CC[C@H]2SC1.C1C[NH+]CC[NH]1.c1ccncc1.c1ncsn1
HCl
CS(=O)C
null
4
C=CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(CCl)CS[C@H]12)c1nsc(N)n1.CN1CCN(C(=O)c2cc(O)c(O)cn2)CC1>CS(=O)C>C=CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-badf125e1b9643a4b3de78dd9442d0c1
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(NC=O)n1>>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(N)n1
C([O-])(O)=O.[Na+].Cl.C(=O)NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(C2=CC(=C(C=C2)O)O)=O)C)C(=O)[O-])C1=O)=NOC>>NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(C2=CC(=C(C=C2)O)O)=O)C)C(=O)[O-])C1=O)=NOC
O=C[NH:42][c:41]1[s:40][cH:39][c:38]([C:4](=[N:3][O:2][CH3:1])[C:5](=[O:6])[NH:7][C@@H:8]2[C:9](=[O:10])[N:11]3[C:12]([C:13](=[O:14])[O-:15])=[C:16]([CH2:17][N+:18]4([CH3:19])[CH2:20][CH2:21][N:22]([C:23](=[O:24])[c:25]5[cH:26][cH:27][c:28]([OH:29])[c:30]([OH:31])[cH:32]5)[CH2:33][CH2:34]4)[CH2:35][S:36][C@H:37]23)[n:4...
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(NC=O)n1
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(N)n1
null
null
CO
Reduction
Reduction of primary amides to amines
755df58c254dea764fdda078ffd678ec540bba057c83683be04c253f1270ac7b
025f7cefe51e71668ad5d09fca32df168e9b538347403e4d5c1748073e538adc
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCN(C(=O)c4ccccc4)CC3)CS[C@H]12)c1cscn1
O=C-[NH;D2;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1>>[NH2;D1;+0:1]-[c:2]1:[#16;a:3]:[c:4]:[c:5]:[#7;a:6]:1
37.7
[{"value": 37.7, "product": "NC=1SC=C(N1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(C2=CC(=C(C=C2)O)O)=O)C)C(=O)[O-])C1=O)=NOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a suspension of 7β-[2-(2-formamidothiazol-4-yl)-2-methoxyiminoacetamido]-3-[1-methyl-4-(3,4-dihydroxybenzoyl)-1-piperazinio]methyl-3-cephem-4-carboxylate (syn isomer) (1.52 g) in methanol (9 ml) was added concentrated hydrochloric acid (1.92 ml). After being stirred at room temperature for 4 hours, the solution was ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
Primary amine
null
null
C1=CN2CC[C@H]2SC1.C1C[NH+]CC[NH]1.c1ccccc1.c1cscn1
Other
CO
null
4
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(NC=O)n1>CO>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4ccc(O)c(O)c4)CC3)CS[C@H]12)c1csc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d576ec8dc5e942d7a4fd333adedd0dc3
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1.O=C(O)c1cc(O)c(O)cn1>>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
C(C)(C)OC(C)C.NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCNCC2)C)C(=O)[O-])C1=O)=NOC.C[Si](NC(C)=O)(C)C.OC1=CC(=NC=C1O)C(=O)O.ON1N=NC2=C1C=CC=C2.C1(CCCCC1)N=C=NC1CCCCC1>>NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)C2=NC=C(C(=C2)O)O)C)C(=O)[O-])C1=O)=NOC
[CH3:1][O:2][N:3]=[C:4]([C:5](=[O:6])[NH:7][C@@H:8]1[C:9](=[O:10])[N:11]2[C:12]([C:13](=[O:14])[O-:15])=[C:16]([CH2:17][N+:18]3([CH3:19])[CH2:20][CH2:21][NH:22][CH2:33][CH2:34]3)[CH2:35][S:36][C@H:37]12)[c:38]1[n:39][s:40][c:41]([NH2:42])[n:43]1.O[C:23](=[O:24])[c:25]1[cH:26][c:27]([OH:28])[c:29]([OH:30])[cH:31][n:32]1...
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1.O=C(O)c1cc(O)c(O)cn1
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
null
null
CS(=O)C
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
e47d96c9361a012293d76c3f121f4ccd40981f3fc68d72319df036f78dd5f08e
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCN(C(=O)c4ccccn4)CC3)CS[C@H]12)c1ncsn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6].[#7;+:7]1-[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[N;H0;D3;+0:10]1-[C:9]-[C:8]-[#7;+:7]-[C:12]-[C:11]-1)-[c:3](:[c:4]):[#7;a:5]:[c:6]
3.9
[{"value": 3.9, "product": "NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)C2=NC=C(C(=C2)O)O)C)C(=O)[O-])C1=O)=NOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 4,5-dihydroxy-2-pyridinecarboxylic acid (3.1 g) and 1-hydroxybenzotriazole (4.0 g) in dimethyl sulfoxide (30 ml) was added N,N'-dicyclohexylcarbodiimide (6.2 g). After being stirred at room temperature for 1 hour, the reaction mixture was added to a solution of 7β-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-m...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1C[NH+]CCN1
C1C[NH+]CC[NH]1
C1=CN2CC[C@H]2SC1.C1C[NH+]CC[NH]1.c1ccncc1.c1ncsn1
HO-
CS(=O)C
null
1
CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1.O=C(O)c1cc(O)c(O)cn1>CS(=O)C>CON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b271669b85e646cfaf401d72445f4700
CC(=O)Oc1cnc(C(=O)Cl)cc1OC(C)=O.CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1>>CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCNCC2)C)C(=O)[O-])C1=O)=NOCC.Cl.C(C)(=O)OC1=CC(=NC=C1OC(C)=O)C(=O)Cl.C([O-])(O)=O.[Na+]>>NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)C2=NC=C(C(=C2)O)O)C)C(=O)[O-])C1=O)=NOCC
CC(=O)[O:29][c:28]1[cH:27][c:26]([C:24](Cl)=[O:25])[n:33][cH:32][c:30]1[O:31]C(C)=O.[CH3:1][CH2:2][O:3][N:4]=[C:5]([C:6](=[O:7])[NH:8][C@@H:9]1[C:10](=[O:11])[N:12]2[C:13]([C:14](=[O:15])[O-:16])=[C:17]([CH2:18][N+:19]3([CH3:20])[CH2:21][CH2:22][NH:23][CH2:34][CH2:35]3)[CH2:36][S:37][C@H:38]12)[c:39]1[n:40][s:41][c:42]...
CC(=O)Oc1cnc(C(=O)Cl)cc1OC(C)=O.CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1
CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
null
null
O.CC(=O)C
Acylation
OtherReaction
cf01b5df9088496bd10db3298095e41d9d3cab861a1a6451d13c45e1f1ab45db
5214b83f6e2bb1b62d2ef28640d266abbdeda6fd4959fafbaca87c3fd32f11d7
N=C(C(=O)N[C@@H]1C(=O)N2C=C(C[NH+]3CCN(C(=O)c4ccccn4)CC3)CS[C@H]12)c1ncsn1
C-C(=O)-[O;H0;D2;+0:1]-[c:2]1:[c:3]:[c:4](-[C;H0;D3;+0:5](-Cl)=[O;D1;H0:6]):[#7;a:7]:[c:8]:[c:9]:1-[O;H0;D2;+0:10]-C(-C)=O.[#7;+:11]1-[C:12]-[C:13]-[NH;D2;+0:14]-[C:15]-[C:16]-1>>[O;D1;H0:6]=[C;H0;D3;+0:5](-[N;H0;D3;+0:14]1-[C:13]-[C:12]-[#7;+:11]-[C:16]-[C:15]-1)-[c:4]1:[#7;a:7]:[c:8]:[c:9](-[OH;D1;+0:10]):[c:2](-[OH;...
47.9
[{"value": 47.9, "product": "NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2(CCN(CC2)C(=O)C2=NC=C(C(=C2)O)O)C)C(=O)[O-])C1=O)=NOCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 7β-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-ethoxyiminoacetamido]-3-(1-methyl-1-piperazinio)methyl-3-cephem-4-carboxylate (syn isomer) (255 mg) in a mixture of water (5 ml) and acetone (5 ml) was added 4,5-diacetoxy-2-pyridinecarbonyl chloride hydrochloride (309 mg), with maintaining the pH of the solution...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ester.Ester.Secondary amine
Tertiary amide.Aromatic alcohol.Aromatic alcohol
C1C[NH+]CCN1
C1C[NH+]CC[NH]1
C1=CN2CC[C@H]2SC1.C1C[NH+]CC[NH]1.c1ccncc1.c1ncsn1
HCl
O.CC(=O)C
null
0.5
CC(=O)Oc1cnc(C(=O)Cl)cc1OC(C)=O.CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCNCC3)CS[C@H]12)c1nsc(N)n1>O.CC(=O)C>CCON=C(C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCN(C(=O)c4cc(O)c(O)cn4)CC3)CS[C@H]12)c1nsc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-470255b2b67b486898084bd101cb65db
Cl>>Cl
Cl.NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+](CC=2NC=C(C(C2)=O)O)(C)C)C(=O)[O-])C1=O)=NOC(C)(C)C(=O)O>>Cl.NC1=NC(=NS1)C(C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+](CC=2NC=C(C(C2)=O)O)(C)C)C(=O)[O-])C1=O)=NOC(C)(C)C(=O)O
[ClH:44]>>[ClH:44]
Cl
Cl
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
To 1N hydrochloric acid was added 7β-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[N,N-dimethyl-N-((5-hydroxy-4-oxo-1,4-dihydropyridin-2-yl)methyl}ammonio]methyl-3-cephem-4-carboxylate (syn isomer) (2.2 g). The mixture was stirred under ice-cooling for 3 hours. The resulting precipit...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
Cl>>Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fc2653c706e943b8b80ddf6fb2c55f7f
O=[N+]([O-])c1ccc(Cl)cc1.Sc1nsc(S)n1.[OH-]>>O=[N+]([O-])c1ccc(Sc2nsc(Sc3ccc([N+](=O)[O-])cc3)n2)cc1
ClC1=CC=C(C=C1)[N+](=O)[O-].[OH-].[Na+].SC1=NSC(=N1)S>>[N+](=O)([O-])C1=CC=C(C=C1)SC1=NSC(=N1)SC1=CC=C(C=C1)[N+](=O)[O-]
Cl[c:7]1[cH:6][cH:5][c:17]([N+:18](=[O:19])[O-:20])[cH:4][cH:24]1.[n:2]1[c:9]([SH:8])[n:10][s:11][c:12]1[SH:13].[OH-:1]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([S:8][c:9]2[n:10][s:11][c:12]([S:13][c:14]3[cH:15][cH:16][c:17]([N+:18](=[O:19])[O-:20])[cH:21][cH:22]3)[n:23]2)[cH:24][cH:25]1
O=[N+]([O-])c1ccc(Cl)cc1.Sc1nsc(S)n1.[OH-]
O=[N+]([O-])c1ccc(Sc2nsc(Sc3ccc([N+](=O)[O-])cc3)n2)cc1
null
null
CN(C)C=O.O
Aromatic Heterocycle Formation
OtherReaction
d6d1f72775c5d476329e874d98c360578641590005804cc329a91ba10ffc2b66
9ce8cecd24ca72e38fa1e8ac5a04feb7aa7ca915023db7e29a89863779f9a99d
c1ccc(Sc2nsc(Sc3ccccc3)n2)cc1
Cl-[c;H0;D3;+0:1]1:[c:2]:[cH;D2;+0:3]:[c;H0;D3;+0:4](-[#7;+:5](-[O;-;D1;H0:6])=[O;D1;H0:7]):[cH;D2;+0:8]:[cH;D2;+0:9]:1.[OH-;D0:10].[SH;D1;+0:11]-[c;H0;D3;+0:12]1:[#16;a:13]:[#7;a:14]:[c;H0;D3;+0:15](-[SH;D1;+0:16]):[n;H0;D2;+0:17]:1>>[O;-;D1;H0:6]-[#7;+:5](=[O;D1;H0:7])-[c;H0;D3;+0:4]1:[c:18]:[c:19]:[c:20](-[S;H0;D2;+...
92
[{"value": 92.0, "product": "[N+](=O)([O-])C1=CC=C(C=C1)SC1=NSC(=N1)SC1=CC=C(C=C1)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.7, "product": "[N+](=O)([O-])C1=CC=C(C=C1)SC1=NSC(=N1)SC1=CC=C(C=C1)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
3 g of NaOH were dissolved in 5 ml of water in a 250 ml three-necked flask, 3.8 g (25 mmol) of 3,5-dimer-capto-1,2,4-thiadiazole (preparation analogous to U.S. No. 3,899,502 or Z. Anorgan. Allgem. Chemie volume 486 (1982), pages 111-115) were added and the mixture was heated to 100° C. 79 g (50 mmol) of 1-chloro-4-nitr...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Nitro group.Aromatic thiol.Aromatic thiol
Nitro group.Nitro group.Monosulfide.Monosulfide
c1ccccc1.c1ncsn1
c1ccccc1.c1ncsn1.c1ccccc1
c1ccccc1.c1ncsn1.c1ccccc1
null
CN(C)C=O.O
100
null
O=[N+]([O-])c1ccc(Cl)cc1.Sc1nsc(S)n1.[OH-]>CN(C)C=O.O>O=[N+]([O-])c1ccc(Sc2nsc(Sc3ccc([N+](=O)[O-])cc3)n2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0d6c5b16d69b4534bf86c0fb3c59c329
BrCCCCBr.O=S(=O)(O)O.Oc1cccc(O)c1.[OH-]>>Oc1cccc(OCCCCOc2cccc(O)c2)c1
[OH-].[K+].C1(O)=CC(O)=CC=C1.S(O)(O)(=O)=O.BrCCCCBr>>OC=1C=C(OCCCCOC2=CC(=CC=C2)O)C=CC1
Br[CH2:8][CH2:9][CH2:2][CH2:20]Br.O=S(=O)(O)[OH:7].[OH:12][c:13]1[cH:14][cH:15][cH:16][c:17]([OH:18])[cH:19]1.[OH-:1]>>[OH:1][c:2]1[cH:3][cH:4][cH:5][c:6]([O:7][CH2:8][CH2:9][CH2:10][CH2:11][O:12][c:13]2[cH:14][cH:15][cH:16][c:17]([OH:18])[cH:19]2)[cH:20]1
BrCCCCBr.O=S(=O)(O)O.Oc1cccc(O)c1.[OH-]
Oc1cccc(OCCCCOc2cccc(O)c2)c1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
e6ffb2faee7dd6e7b0626caef33854c44061fa0c4984b3a90eb791d165d728d5
fdaa1813c7944a55b8970d6214b8c93d9eab4178705d897cc8ff86d898cadbe3
c1ccc(OCCCCOc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-Br.O-S(=O)(=O)-[OH;D1;+0:5].[OH-;D0:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[OH;D1;+0:6]-[c;H0;D3;+0:2]1:[c:11]:[c:12]:[c:13]:[c:14](-[O;H0;D2;+0:5]-[CH2;D2;+0:4]-[CH2;D2;+0:3]-[C:15]-[C:16]-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]):[cH;D2;+0:1]:1
null
[]
null
null
8
HOUR
A five neck five liter round bottom flask equipped with a mechanical stirrer, two condensers, and a dropping funnel is purged with nitrogen then charged under a nitrogen blanket with 1.5 kg (13.6 moles) resorcinol, 120 grams deionized water, and 138.75 grams (0.64 moles) 1,4-dibromobutane. The reaction slurry is slowly...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Aromatic alcohol
Ether.Ether.Aromatic alcohol
null
c1ccccc1
c1ccccc1.c1ccccc1
null
O
null
8
BrCCCCBr.O=S(=O)(O)O.Oc1cccc(O)c1.[OH-]>O>Oc1cccc(OCCCCOc2cccc(O)c2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-04e07f48769d45fb9b3405fdf6365184
BrCCCCBr.Oc1ccc(O)cc1.[OH-].[OH-]>>Oc1ccc(OCCCCOc2ccc(O)cc2)cc1
[OH-].[K+].C1(O)=CC=C(O)C=C1.BrCCCCBr.[OH-].[K+].[OH-].[K+]>>OC1=CC=C(OCCCCOC2=CC=C(C=C2)O)C=C1
Br[CH2:4][CH2:3][CH2:8][CH2:5]Br.[OH:1][c:2]1[cH:13][cH:14][c:15]([OH:16])[cH:17][cH:20]1.[OH-:11].[OH-:6]>>[OH:1][c:2]1[cH:3][cH:4][c:5]([O:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([OH:16])[cH:17][cH:18]2)[cH:19][cH:20]1
BrCCCCBr.Oc1ccc(O)cc1.[OH-].[OH-]
Oc1ccc(OCCCCOc2ccc(O)cc2)cc1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
a433113afb572656691553e0b9980eaa9212a47e371735e50c7ed3fa0d356e8f
fdaa1813c7944a55b8970d6214b8c93d9eab4178705d897cc8ff86d898cadbe3
c1ccc(OCCCCOc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-Br.[O;D1;H1:5]-[c:6]1:[c:7]:[cH;D2;+0:8]:[c;H0;D3;+0:9](-[O;D1;H1:10]):[cH;D2;+0:11]:[cH;D2;+0:12]:1.[OH-;D0:13].[OH-;D0:14]>>[O;D1;H1:5]-[c:6]1:[c:7]:[cH;D2;+0:8]:[c:15](-[O;H0;D2;+0:13]-[C:16]-[C:17]-[CH2;D2;+0:3]-[C:18]-[O;H0;D2;+0:14]-[c;H0;D3;+0:4]2:[c:19]...
46
[{"value": 46.0, "product": "OC1=CC=C(OCCCCOC2=CC=C(C=C2)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A five neck five liter round bottom flask equipped with a mechanical stirrer, two condensers, and a dropping funnel is purged with nitrogen then charged under a nitrogen blanket with 1.25 kg (11.36 moles) hydroquinone, 350 grams deionized water, and 231.25 grams (1.07 moles) 1,4-dibromobutane. The reaction mass becomes...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Aromatic alcohol
Ether.Ether.Aromatic alcohol
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Br-
O
null
8
BrCCCCBr.Oc1ccc(O)cc1.[OH-].[OH-]>O>Oc1ccc(OCCCCOc2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b21f5d35f68c4e3ead3485ab0ba70fbb
BrCCCCCCCCBr.Oc1ccc(O)cc1.[OH-].[OH-]>>Oc1ccc(OCCCCCCCCOc2ccc(O)cc2)cc1
C1(O)=CC=C(O)C=C1.[OH-].[K+].[OH-].[K+].[OH-].[K+].BrCCCCCCCCBr>>OC1=CC=C(OCCCCCCCCOC2=CC=C(C=C2)O)C=C1
Br[CH2:5][CH2:23][CH2:24][CH2:7][CH2:11][CH2:12][CH2:13][CH2:14]Br.[OH:1][c:2]1[cH:3][cH:4][c:19]([OH:20])[cH:21][cH:22]1.[OH-:6].[OH-:15]>>[OH:1][c:2]1[cH:3][cH:4][c:5]([O:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][c:16]2[cH:17][cH:18][c:19]([OH:20])[cH:21][cH:22]2)[cH:23][cH:24]1
BrCCCCCCCCBr.Oc1ccc(O)cc1.[OH-].[OH-]
Oc1ccc(OCCCCCCCCOc2ccc(O)cc2)cc1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
fe468b15bad24fc50ee155d266d9162241ea7aa8d8d56f38a6e9639e490d1b62
08134ccf30e746cd0aac5a54b51fcfee17628d21c85642ad552f88fc52be57f9
c1ccc(OCCCCCCCCOc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-Br.[O;D1;H1:9]-[c;H0;D3;+0:10]1:[c:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13](-[O;D1;H1:14]):[c:15]:[cH;D2;+0:16]:1.[OH-;D0:17].[OH-;D0:18]>>[O;D1;H1:9]-[c;H0;D3;+0:10]1:[c:11]:[cH;D2;+0:12]:[c;H0;D3;+0:8](-[O;H0;D2;+0:17]-[CH2;D2...
99
[{"value": 99.0, "product": "OC1=CC=C(OCCCCCCCCOC2=CC=C(C=C2)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
90
MINUTE
A five neck five liter round bottom flask equipped with a mechanical stirrer, two condensers, and a dropping funnel is purged with nitrogen then charged under a nitrogen blanket with 1.1 kg (10.0 moles) hydroquinone, 350 grams deionized water, and 272.0 grams (1.0 moles) 1,8-dibromooctane. The reaction mass becomes a s...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Aromatic alcohol.Aromatic alcohol
Ether.Ether.Aromatic alcohol.Aromatic alcohol
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Br-
O
null
1.5
BrCCCCCCCCBr.Oc1ccc(O)cc1.[OH-].[OH-]>O>Oc1ccc(OCCCCCCCCOc2ccc(O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d7ebeb5510864bf5a76d01a064162923
BrCCCCCCCCBr.Oc1cccc(O)c1.[OH-].[OH-]>>Oc1cccc(OCCCCCCCCOc2cccc(O)c2)c1
C1(O)=CC(O)=CC=C1.[OH-].[K+].[OH-].[K+].[OH-].[K+].BrCCCCCCCCBr>>OC=1C=C(OCCCCCCCCOC2=CC(=CC=C2)O)C=CC1
Br[CH2:2][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]Br.[OH:16][c:17]1[cH:18][cH:19][cH:20][c:21]([OH:22])[cH:23]1.[OH-:1].[OH-:7]>>[OH:1][c:2]1[cH:3][cH:4][cH:5][c:6]([O:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][O:16][c:17]2[cH:18][cH:19][cH:20][c:21]([OH:22])[cH:23]2)[cH:24]1
BrCCCCCCCCBr.Oc1cccc(O)c1.[OH-].[OH-]
Oc1cccc(OCCCCCCCCOc2cccc(O)c2)c1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
e6ffb2faee7dd6e7b0626caef33854c44061fa0c4984b3a90eb791d165d728d5
fdaa1813c7944a55b8970d6214b8c93d9eab4178705d897cc8ff86d898cadbe3
c1ccc(OCCCCCCCCOc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:3]-[C:4].Br-[CH2;D2;+0:5]-[C:6]-[C:7].[OH-;D0:8].[OH-;D0:9].[OH;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[C:4]-[C:3]-[CH2;D2;+0:2]-[C:14]-[O;H0;D2;+0:9]-[c:15]1:[c:16]:[c;H0;D3;+0:1](-[OH;D1;+0:8]):[c:17]:[c:18]:[c:19]:1.[C:7]-[C:6]-[CH2;D2;+0:5]-[O;H0;D2;+0:10]-[c:11](:[c:12]):[c:13]
27
[{"value": 27.0, "product": "OC=1C=C(OCCCCCCCCOC2=CC(=CC=C2)O)C=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
10
CELSIUS
null
null
A five neck five liter round bottom flask equipped with a mechanical stirrer, two condensers, and a dropping funnel is purged with nitrogen then charged under a nitrogen blanket with 1.6 kg (14.5 moles) resorcinol, 160 grams deionized water, and 296.7 grams (1.091 moles) 1,8-dibromooctane. The easily stirable reaction ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Aromatic alcohol
Ether.Ether.Aromatic alcohol
null
c1ccccc1
c1ccccc1.c1ccccc1
Br-
O
10
null
BrCCCCCCCCBr.Oc1cccc(O)c1.[OH-].[OH-]>O>Oc1cccc(OCCCCCCCCOc2cccc(O)c2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6a57ab6cf73c4e56abcc682a99f57c0a
CCCCCCCCCCCCC1(Cc2cc(O)ccc2O)COCCOCC(C)(C)COCCOC1>>CCCCCCCCCCCCC1(CC2=CC(=O)C=CC2=O)COCCOCC(C)(C)COCCOC1
C(CCCCCCCCCCC)C1(COCCOCC(COCCOC1)(C)C)CC1=C(C=CC(=C1)O)O>>C(CCCCCCCCCCC)C1(COCCOCC(COCCOC1)(C)C)CC1=CC(C=CC1=O)=O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][C:13]1([CH2:14][c:15]2[cH:16][c:17]([OH:18])[cH:19][cH:20][c:21]2[OH:22])[CH2:23][O:24][CH2:25][CH2:26][O:27][CH2:28][C:29]([CH3:30])([CH3:31])[CH2:32][O:33][CH2:34][CH2:35][O:36][CH2:37]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6]...
CCCCCCCCCCCCC1(Cc2cc(O)ccc2O)COCCOCC(C)(C)COCCOC1
CCCCCCCCCCCCC1(CC2=CC(=O)C=CC2=O)COCCOCC(C)(C)COCCOC1
null
[O-2].[O-2].[Mn+4]
ClCCl
Oxidation
OtherReaction
8e080e257c835909f04b22de1d62278b6e13d1c2ea092be950200c29bbf9740a
a6c6a9201eef9656e2a53a6d102761f5982be5a6ba4b17f7fdbbc6d73ced01df
O=C1C=CC(=O)C(CC2COCCOCCCOCCOC2)=C1
[C:1]-[C:2]-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[OH;D1;+0:6]):[cH;D2;+0:7]:[cH;D2;+0:8]:[c;H0;D3;+0:9]:1-[OH;D1;+0:10]>>[C:1]-[C:2]-[C;H0;D3;+0:3]1=[CH;D2;+0:4]-[C;H0;D3;+0:5](=[O;H0;D1;+0:6])-[CH;D2;+0:7]=[CH;D2;+0:8]-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]
null
[]
null
null
1
HOUR
A solution of 67.6 g (129.3 mmol) of Compound 6 in 600 mL of dichloromethane was mixed with 50.6 g (581.9 mmol) of activated manganese dioxide. The heterogeneous mixture was stirred at room temperature for 1 hour. The insolubles were removed by filtration through Celite diatomaceous earth and the solvent removed. The o...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Aromatic alcohol
Ketone.Ketone
c1ccccc1
C1=CCC=CC1
C1=CCC=CC1.C1COCCOCCCOCCOC1
null
[O-2].[O-2].[Mn+4].ClCCl
null
1
CCCCCCCCCCCCC1(Cc2cc(O)ccc2O)COCCOCC(C)(C)COCCOC1>[O-2].[O-2].[Mn+4].ClCCl>CCCCCCCCCCCCC1(CC2=CC(=O)C=CC2=O)COCCOCC(C)(C)COCCOC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6d9cce36bc1640beacc29f308680a163
CCCCCCCCCCCCC1(Cc2ccccc2O)COCCOCC(C)(C)COCCOC1.CS(=O)(=O)c1cc([N+](=O)[O-])ccc1[N+]#N>>CCCCCCCCCCCCC1(Cc2cc(N=Nc3ccc([N+](=O)[O-])cc3S(C)(=O)=O)ccc2O)COCCOCC(C)(C)COCCOC1
C(CCCCCCCCCCC)C1(COCCOCC(COCCOC1)(C)C)CC1=C(C=CC=C1)O.F[P-](F)(F)(F)(F)F.CS(=O)(=O)C1=C(C=CC(=C1)[N+](=O)[O-])[N+]#N>>C(CCCCCCCCCCC)C1(COCCOCC(COCCOC1)(C)C)CC1=C(C=CC(=C1)N=NC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)C)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][C:13]1([CH2:14][c:15]2[cH:16][cH:17][cH:33][cH:34][c:35]2[OH:36])[CH2:37][O:38][CH2:39][CH2:40][O:41][CH2:42][C:43]([CH3:44])([CH3:45])[CH2:46][O:47][CH2:48][CH2:49][O:50][CH2:51]1.[N:18]#[N+:19][c:20]1[cH:21][cH:22][c:23]([N+:24](=...
CCCCCCCCCCCCC1(Cc2ccccc2O)COCCOCC(C)(C)COCCOC1.CS(=O)(=O)c1cc([N+](=O)[O-])ccc1[N+]#N
CCCCCCCCCCCCC1(Cc2cc(N=Nc3ccc([N+](=O)[O-])cc3S(C)(=O)=O)ccc2O)COCCOCC(C)(C)COCCOC1
null
null
C(C)(=O)O.O.O1CCCC1
Functional Group Addition
OtherReaction
1806c1538219ad87d28be4617a67fcd9909e935b7ee0e5872f99c23fe8ccecff
2c6cd95d4efa78d9d3de76e13585ebc8f102df9229b31c028b4deed5aad0dd25
c1ccc(N=Nc2cccc(CC3COCCOCCCOCCOC3)c2)cc1
[N;H0;D1;+0:1]#[N+;H0;D2:2]-[c:3](:[c:4]):[c:5].[c:6]:[c:7]:[cH;D2;+0:8]:[c:9]:[c:10]>>[c:6]:[c:7]:[c;H0;D3;+0:8](-[N;H0;D2;+0:1]=[N;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]):[c:9]:[c:10]
4.9
[{"value": 4.7, "product": "C(CCCCCCCCCCC)C1(COCCOCC(COCCOC1)(C)C)CC1=C(C=CC(=C1)N=NC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 4.9, "product": "C(CCCCCCCCCCC)C1(COCCOCC(COCCOC1)(C)C)CC1=C(C=CC(=C1)N=NC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)C)O", "details": "CALCULAT...
null
null
16
HOUR
To a solution of 3.1 g (6.1 mmol) of Compound 15 in 50 cc acetic acid at 5° C. was added a solution of 3.0 g (8.0 mmol) of 2-methylsulfonyl-4-nitrophenyldiazonium hexafluorophosphate in 25 cc water and 75 cc tetrahydrofuran. The suspension was stirred at room temperature for 16 hours. The product was extracted into eth...
10.6084/m9.figshare.5104873.v1
null
null
Diazene
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.C1COCCOCCCOCCOC1
null
C(C)(=O)O.O.O1CCCC1
null
16
CCCCCCCCCCCCC1(Cc2ccccc2O)COCCOCC(C)(C)COCCOC1.CS(=O)(=O)c1cc([N+](=O)[O-])ccc1[N+]#N>C(C)(=O)O.O.O1CCCC1>CCCCCCCCCCCCC1(Cc2cc(N=Nc3ccc([N+](=O)[O-])cc3S(C)(=O)=O)ccc2O)COCCOCC(C)(C)COCCOC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9589a48d34f74be29e906b317fd0389c
Nc1ccc(-c2ccc(N)cc2)cc1.Nc1ccc(N)cc1>>Nc1ccc(N(c2ccc(N)cc2)c2ccc(-c3ccc(N(c4ccc(N)cc4)c4ccc(N)cc4)cc3)cc2)cc1
C1=CC(=CC=C1N)N.C1(=CC=C(N)C=C1)C1=CC=C(N)C=C1>>NC1=CC=C(C=C1)N(C1=CC=C(C2=CC=C(N(C3=CC=C(C=C3)N)C3=CC=C(C=C3)N)C=C2)C=C1)C1=CC=C(C=C1)N
[c:7]1(-[c:18]2[cH:17][cH:39][c:26]([NH2:27])[cH:14][cH:38]2)[cH:8][cH:9][c:10]([NH2:11])[cH:12][cH:13]1.[NH2:1][c:2]1[cH:3][cH:4][c:5]([NH2:6])[cH:41][cH:42]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([N:6]([c:7]2[cH:8][cH:9][c:10]([NH2:11])[cH:12][cH:13]2)[c:14]2[cH:15][cH:16][c:17](-[c:18]3[cH:19][cH:20][c:21]([N:22]([c:23]4[...
Nc1ccc(-c2ccc(N)cc2)cc1.Nc1ccc(N)cc1
Nc1ccc(N(c2ccc(N)cc2)c2ccc(-c3ccc(N(c4ccc(N)cc4)c4ccc(N)cc4)cc3)cc2)cc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
7b59445b9dbd16b3d7e64ce4888acd423405a9e02cdcf33e3f8f3be9cf8ad8fd
708aaf9b9308e90194297486ea8438895b5838a6d199d1df1fd3c78018c1732f
c1ccc(N(c2ccccc2)c2ccc(-c3ccc(N(c4ccccc4)c4ccccc4)cc3)cc2)cc1
[N;D1;H2:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[cH;D2;+0:11]:[cH;D2;+0:12]:1.[NH2;D1;+0:13]-[c:14](:[c:15]):[c:16]>>[N;D1;H2:1]-[c;H0;D3;+0:2](:[c:17]:[c:18]):[c:19]:[c:20].[c:8]:[c:7]:[c;H0;D3;+0:6](-[N;H0;D3;+0:13](-[c:14](:[c:15]):[c:16])-[c;H0;D3;+0:...
null
[]
null
null
null
null
The same reaction as in Synthesis example 1 was carried out except for changing p-phenylenediamine used in Synthesis example 1 to benzidine to obtain 12 parts of orange tetrakis (p-aminophenyl)benzidine. Conditions: See reaction.notes.procedure_details. Workup: The same reaction; as in Synthesis example 1
10.6084/m9.figshare.5104873.v1
null
Primary amine
Primary amine.Tertiary amine.Tertiary amine
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
null
null
null
Nc1ccc(-c2ccc(N)cc2)cc1.Nc1ccc(N)cc1>>Nc1ccc(N(c2ccc(N)cc2)c2ccc(-c3ccc(N(c4ccc(N)cc4)c4ccc(N)cc4)cc3)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f09896308b314dc9afd1bacf46b0ac34
CCOC(=O)Cl.NCCC1(O)CCc2ccccc2C12CCCC2>>CCOC(=O)NCCC1(O)CCc2ccccc2C12CCCC2
ClC(=O)OCC.NCCC1(C2(C3=CC=CC=C3CC1)CCCC2)O.C(C)N(CC)CC>>OC1(C2(C3=CC=CC=C3CC1)CCCC2)CCNC(OCC)=O
Cl[C:4]([O:3][CH2:2][CH3:1])=[O:5].[NH2:6][CH2:7][CH2:8][C:9]1([OH:10])[CH2:11][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[C:19]12[CH2:20][CH2:21][CH2:22][CH2:23]2>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[NH:6][CH2:7][CH2:8][C:9]1([OH:10])[CH2:11][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[C:19]12[CH2:20][CH2:21...
CCOC(=O)Cl.NCCC1(O)CCc2ccccc2C12CCCC2
CCOC(=O)NCCC1(O)CCc2ccccc2C12CCCC2
null
null
C(Cl)Cl
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
038720aa61a7efa0f2a9ee6f2e0adf63a9ffdc2be4697c11a6215baef34f97b2
205f353513ce9506ab61831799da8fb73ec2ef5cfa927664496d3ce72c438860
c1ccc2c(c1)CCCC21CCCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[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]
98
[{"value": 98.0, "product": "OC1(C2(C3=CC=CC=C3CC1)CCCC2)CCNC(OCC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.9, "product": "OC1(C2(C3=CC=CC=C3CC1)CCCC2)CCNC(OCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of the product from Example 9 (1.05 g, 4.28 mmol) and triethylamine (0.44 g, 4.35 mmol) in 10 mL of CH2Cl2 was cooled to 0° C. and ethyl chloroformate (0.47 g, 4.33 mmol) in 5 mL CH2Cl2 was added dropwise. The reaction was warmed to room temperature and washed with water. The aqueous phase was extracted with...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Carbamic ester
null
null
c1ccc2c(c1)CCCC21CCCC1
HCl
C(Cl)Cl
null
null
CCOC(=O)Cl.NCCC1(O)CCc2ccccc2C12CCCC2>C(Cl)Cl>CCOC(=O)NCCC1(O)CCc2ccccc2C12CCCC2
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-01efe08bb86845ba8cb6c06c77c689fa
NCCC1(O)CCc2ccccc2C12CCCC2.O=C(Cl)OCC(Cl)(Cl)Cl>>O=C(NCCC1(O)CCc2ccccc2C12CCCC2)OCC(Cl)(Cl)Cl
ClC(COC(=O)Cl)(Cl)Cl.NCCC1(C2(C3=CC=CC=C3CC1)CCCC2)O.C(C)N(CC)CC>>OC1(C2(C3=CC=CC=C3CC1)CCCC2)CCNC(OCC(Cl)(Cl)Cl)=O
[NH2:3][CH2:4][CH2:5][C:6]1([OH:7])[CH2:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[C:16]12[CH2:17][CH2:18][CH2:19][CH2:20]2.Cl[C:2](=[O:1])[O:21][CH2:22][C:23]([Cl:24])([Cl:25])[Cl:26]>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][C:6]1([OH:7])[CH2:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[C:16]12[CH2:17][CH2:18...
NCCC1(O)CCc2ccccc2C12CCCC2.O=C(Cl)OCC(Cl)(Cl)Cl
O=C(NCCC1(O)CCc2ccccc2C12CCCC2)OCC(Cl)(Cl)Cl
null
null
C(Cl)Cl
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
038720aa61a7efa0f2a9ee6f2e0adf63a9ffdc2be4697c11a6215baef34f97b2
205f353513ce9506ab61831799da8fb73ec2ef5cfa927664496d3ce72c438860
c1ccc2c(c1)CCCC21CCCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[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]
78.1
[{"value": 78.0, "product": "OC1(C2(C3=CC=CC=C3CC1)CCCC2)CCNC(OCC(Cl)(Cl)Cl)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.1, "product": "OC1(C2(C3=CC=CC=C3CC1)CCCC2)CCNC(OCC(Cl)(Cl)Cl)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
A solution of the product from Example 9 (0.88 g, 3.59 mmol) and triethylamine (0.40 g, 3.78 mmol) in 10 mL of CH2Cl2 was cooled to 0° C. and treated dropwise with 2,2,2-trichloroethylchloroformate (0.80 g, 3.78 mmol) in 2 mL CH2Cl2. The resulting solution was stirred at 0° C. for 30 minutes and warmed to room temperat...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Carbamic ester
null
null
c1ccc2c(c1)CCCC21CCCC1
HCl
C(Cl)Cl
0
0.5
NCCC1(O)CCc2ccccc2C12CCCC2.O=C(Cl)OCC(Cl)(Cl)Cl>C(Cl)Cl>O=C(NCCC1(O)CCc2ccccc2C12CCCC2)OCC(Cl)(Cl)Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-02b7b388594a45e995525bf702f7126b
Clc1ccc2c(Cl)ccnc2c1.Oc1ccc(F)cc1>>Fc1ccc(Oc2ccnc3cc(Cl)ccc23)cc1
ClC1=CC=NC2=CC(=CC=C12)Cl.FC1=CC=C(C=C1)O>>FC1=CC=C(OC2=CC=NC3=CC(=CC=C23)Cl)C=C1
Cl[c:7]1[cH:8][cH:9][n:10][c:11]2[cH:12][c:13]([Cl:14])[cH:15][cH:16][c:17]12.[F:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[cH:18][cH:19]1>>[F:1][c:2]1[cH:3][cH:4][c:5]([O:6][c:7]2[cH:8][cH:9][n:10][c:11]3[cH:12][c:13]([Cl:14])[cH:15][cH:16][c:17]23)[cH:18][cH:19]1
Clc1ccc2c(Cl)ccnc2c1.Oc1ccc(F)cc1
Fc1ccc(Oc2ccnc3cc(Cl)ccc23)cc1
null
null
C=1(C(=CC=CC1)C)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
499018af6792b58a137ac4495e0c20acdc548a3418ba695c815cb38084ffd839
27e9a6bab4e3ed54aeb6be4d84cb1c0170208288795e252a46e57e44ecc064f0
c1ccc(Oc2ccnc3ccccc23)cc1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5](:[c:6]):[c:7]:1:[c:8].[OH;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[c:6]:[c:5]1:[#7;a:4]:[c:3]:[c:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]):[c:7]:1:[c:8]
615.9
[{"value": 86.0, "product": "FC1=CC=C(OC2=CC=NC3=CC(=CC=C23)Cl)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 615.9, "product": "FC1=CC=C(OC2=CC=NC3=CC(=CC=C23)Cl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a 50 mL flask equipped with a condenser, drying tube and thermometer, was added 1.98 g (0.01 moles) of 4,7-dichloroquinoline, 1.07 g (0.0015 moles) of polyDMAP™and 20 mL of xylene. The mixture was stirred to reswell the polymer and 1.57 g (0.0014 moles) of 4-fluorophenol were added. The reaction mixure was heated to...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
Ether
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
HCl
C=1(C(=CC=CC1)C)C
null
null
Clc1ccc2c(Cl)ccnc2c1.Oc1ccc(F)cc1>C=1(C(=CC=CC1)C)C>Fc1ccc(Oc2ccnc3cc(Cl)ccc23)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-083e912021ea4636b30489d9253b9684
Clc1ccc2c(Cl)ccnc2c1.Oc1ccc(F)cc1>>Fc1ccc(Oc2ccnc3cc(Cl)ccc23)cc1
ClC1=CC=NC2=CC(=CC=C12)Cl.FC1=CC=C(C=C1)O.N1(CCCC1)C1=CC=NC=C1>>FC1=CC=C(OC2=CC=NC3=CC(=CC=C23)Cl)C=C1
Cl[c:7]1[cH:8][cH:9][n:10][c:11]2[cH:12][c:13]([Cl:14])[cH:15][cH:16][c:17]12.[F:1][c:2]1[cH:3][cH:4][c:5]([OH:6])[cH:18][cH:19]1>>[F:1][c:2]1[cH:3][cH:4][c:5]([O:6][c:7]2[cH:8][cH:9][n:10][c:11]3[cH:12][c:13]([Cl:14])[cH:15][cH:16][c:17]23)[cH:18][cH:19]1
Clc1ccc2c(Cl)ccnc2c1.Oc1ccc(F)cc1
Fc1ccc(Oc2ccnc3cc(Cl)ccc23)cc1
null
null
C=1(C(=CC=CC1)C)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
499018af6792b58a137ac4495e0c20acdc548a3418ba695c815cb38084ffd839
27e9a6bab4e3ed54aeb6be4d84cb1c0170208288795e252a46e57e44ecc064f0
c1ccc(Oc2ccnc3ccccc23)cc1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5](:[c:6]):[c:7]:1:[c:8].[OH;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[c:6]:[c:5]1:[#7;a:4]:[c:3]:[c:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[c:10](:[c:11]):[c:12]):[c:7]:1:[c:8]
649.9
[{"value": 91.0, "product": "FC1=CC=C(OC2=CC=NC3=CC(=CC=C23)Cl)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 649.9, "product": "FC1=CC=C(OC2=CC=NC3=CC(=CC=C23)Cl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a 50 mL flask equipped with a condenser, drying tube and thermometer, was added 1.98 g (0.01 moles) of 4,7-dichloroquinoline, 1.57 g (0.0014 moles) of 4-fluorophenol, 0.22 g (0.0015 moles) of 4-pyrrolidinopyridine and 20 mL of xylene. The reaction mixture was heated to reflux and reaction progress was monitored by T...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
Ether
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
HCl
C=1(C(=CC=CC1)C)C
null
18
Clc1ccc2c(Cl)ccnc2c1.Oc1ccc(F)cc1>C=1(C(=CC=CC1)C)C>Fc1ccc(Oc2ccnc3cc(Cl)ccc23)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e1035b9ffe964abea5e21dc8c9fb7b3c
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)F)CS[C@H]12>>C=CC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
C(=C)[Sn](CCCC)(CCCC)CCCC.O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)OS(=O)(=O)F)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O>>O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)C=C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O
CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)[CH:2]=[CH2:1].O=S(=O)(F)O[C:3]1=[C:4]([C:5](=[O:6])[O:7][CH:8]([c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)[N:21]2[C:22](=[O:23])[CH:24]([NH:25][C:26](=[O:27])[CH2:28][O:29][c:30]3[cH:31][cH:32][cH:33][cH:34][cH:35]3)[C@H:36]2[S:37][CH2:38]1>>[...
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)F)CS[C@H]12
C=CC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
C(C)(=O)OCC.CN1C(CCC1)=O
C-C Coupling
OtherReaction
67eba8952d4464cae7e07121b203292d2b8bccb1e2dcaa174b0cb724fd226a44
8229f2e290a81d798706abc950f1fa9d9c98a7ca1d13c9b7fa6b9f580d9aa5a6
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=CCS[C@H]12
C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-C-C)-[CH;D2;+0:1]=[C;D1;H2:2].F-S(=O)(=O)-O-[C;H0;D3;+0:3]1=[C:4](-[C:5](=[O;D1;H0:6])-[#8:7]-[C:8])-[#7:9](-[C:10]=[O;D1;H0:11])-[C:12]-[#16:13]-[C:14]-1>>[C:8]-[#8:7]-[C:5](=[O;D1;H0:6])-[C:4]1=[C;H0;D3;+0:3](-[CH;D2;+0:1]=[C;D1;H2:2])-[C:14]-[#16:13]-[C:12]-[#7:9]-1-[C:10]=[O;...
88.8
[{"value": 85.0, "product": "O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)C=C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.8, "product": "O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)C=C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O", "details": "CALCULATEDPERCENTYIELD", "is_desir...
null
null
3
MINUTE
A solution of palladium (II) acetate (3.6 mg, 0.016 mmol, 0.1 eq.) in 1-methyl-2-pyrrolidinone (2 mL) was treated with vinyl tri-n-butylstannane (58.4 mL, 0.2 mmol, 1.2 eq.) under an inert atmosphere and allowed to stir for 3 minutes. The resulting dark suspension was then treated with diphenylmethyl 7-phenoxyacetamido...
10.6084/m9.figshare.5104873.v1
null
Enamine.Vinyl.Tin
Enamine.Vinyl
C1=CN2CC[C@H]2SC1
C1=CN2CC[C@H]2SC1
c1ccccc1.c1ccccc1.C1=CN2CC[C@H]2SC1.c1ccccc1
HF.Sn
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(C)(=O)OCC.CN1C(CCC1)=O
null
0.05
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)F)CS[C@H]12>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(C)(=O)OCC.CN1C(CCC1)=O>C=CC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c2b21fff05b941f38cbaf9f020481d88
C/C=[CH]\[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)F)CS[C@H]12>>C/C=C\C1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
C(=C/C)/[Sn](CCCC)(CCCC)CCCC.O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)OS(=O)(=O)F)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O>>O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)\C=C/C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O
CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)/[CH:3]=[CH:2]\[CH3:1].O=S(=O)(F)O[C:4]1=[C:5]([C:6](=[O:7])[O:8][CH:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[N:22]2[C:23](=[O:24])[CH:25]([NH:26][C:27](=[O:28])[CH2:29][O:30][c:31]3[cH:32][cH:33][cH:34][cH:35][cH:36]3)[C@H:37]2[S:38][CH...
C/C=[CH]\[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)F)CS[C@H]12
C/C=C\C1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
ClCCl
C-C Coupling
OtherReaction
160aa54afc0e5af3c669cf3c80740ad875eeafe71c85a27744301f82bbccbd15
a475964b87d2ef4c5698b1980466b9da951c3c0b64f664002f9d6da383a35778
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=CCS[C@H]12
C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-C-C)/[CH;D2;+0:1]=[C:2]\[C;D1;H3:3].F-S(=O)(=O)-O-[C;H0;D3;+0:4]1=[C:5](-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9])-[#7:10](-[C:11]=[O;D1;H0:12])-[C:13]-[#16:14]-[C:15]-1>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:5]1=[C;H0;D3;+0:4](/[CH;D2;+0:1]=[C:2]\[C;D1;H3:3])-[C:15]-[#16:14]-[C:13]-[#7:10...
92.9
[{"value": 89.0, "product": "O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)\\C=C/C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.9, "product": "O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)\\C=C/C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O", "details": "CALCULATEDPERCENTYIELD", "...
null
null
3
MINUTE
A solution of palladium (II) acetate (3.6 mg, 0.016 mmole, 0.1 eq.) in dichloromethane (2 mL) was treated with Z-1-propenyl tri-n-butylstannane (66.2 mg, 0.2 mmole, 1.2 eq.) under an inert atmosphere and allowed to stir for 3 minutes. The resulting dark suspension was then treated with diphenylmethyl 7-phenoxyacetamido...
10.6084/m9.figshare.5104873.v1
null
Enamine.Tin
Enamine
C1=CN2CC[C@H]2SC1
C1=CN2CC[C@H]2SC1
c1ccccc1.c1ccccc1.C1=CN2CC[C@H]2SC1.c1ccccc1
HF.Sn
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].ClCCl
null
0.05
C/C=[CH]\[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)F)CS[C@H]12>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].ClCCl>C/C=C\C1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8261f787d18e44569a78042ee44a9160
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(O)CS[C@H]12.O=S(=O)(Cl)c1ccc(Br)cc1>>O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)c3ccc(Br)cc3)CS[C@H]12
O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)O)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O.[H-].[Na+].BrC1=CC=C(C=C1)S(=O)(=O)Cl>>O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)OS(=O)(=O)C2=CC=C(C=C2)Br)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O
[O:1]=[C:2]([CH2:3][O:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[NH:11][CH:12]1[C:13](=[O:14])[N:15]2[C:16]([C:17](=[O:18])[O:19][CH:20]([c:21]3[cH:22][cH:23][cH:24][cH:25][cH:26]3)[c:27]3[cH:28][cH:29][cH:30][cH:31][cH:32]3)=[C:33]([OH:34])[CH2:45][S:46][C@H:47]12.Cl[S:35](=[O:36])(=[O:37])[c:38]1[cH:39][cH:40][c:41]([...
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(O)CS[C@H]12.O=S(=O)(Cl)c1ccc(Br)cc1
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)c3ccc(Br)cc3)CS[C@H]12
null
null
C(C)#N.[H][H]
Acylation
Formation of Sulfonic Esters
5da4d330816d41221dac5ccfcb17cc7283f159f991810d3234e183c971c877c4
a7be31b2844dda058c7c3aa56854ad4c914dd8646dc5e2d431f609f9ab031b83
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)c3ccccc3)CS[C@H]12
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#16:7]-[C:8]-[C:9](-[OH;D1;+0:10])=[C:11](-[C:12](-[#8:13])=[O;D1;H0:14])-[#7:15]-[C:16]=[O;D1;H0:17]>>[#16:7]-[C:8]-[C:9](-[O;H0;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6])=[C:11](-[C:12](-[#8:13])=[O;D1;H0:14])-[#7:15]-[C...
54.1
[{"value": 54.0, "product": "O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)OS(=O)(=O)C2=CC=C(C=C2)Br)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.1, "product": "O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)OS(=O)(=O)C2=CC=C(C=C2)Br)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O", "d...
0
CELSIUS
5
MINUTE
The title compound was prepared via a modification of the synthesis described in U.S. Pat. No. 3,985,737. A solution of 0.51 g (0.001 mole) of diphenylmethyl 7-phenoxyacetamido-3 -hydroxy-3-cephem- 4-carboxylate in 5 mL of acetonitrile was cooled to 0° C. under a nitrogen atmosphere. Then 0.030 g (0.001 mole) of sodium...
10.6084/m9.figshare.5104873.v1
null
Enol.Sulfonyl halide
Sulfonate
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.C1=CN2CC[C@H]2SC1
HCl
C(C)#N.[H][H]
0
0.083333
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(O)CS[C@H]12.O=S(=O)(Cl)c1ccc(Br)cc1>C(C)#N.[H][H]>O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)c3ccc(Br)cc3)CS[C@H]12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d423bb0af2d64620abf46421b8a2f7ef
C/C=[CH]\[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)c3ccc(Br)cc3)CS[C@H]12>>C/C=C\C1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)OS(=O)(=O)C2=CC=C(C=C2)Br)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O.C(=C/C)/[Sn](CCCC)(CCCC)CCCC.BrC1=CC=C(C=C1)S(=O)(=O)Cl>>O(C1=CC=CC=C1)CC(=O)NC1[C@@H]2N(C(=C(CS2)\C=C/C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O
CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)/[CH:3]=[CH:2]\[CH3:1].O=S(=O)(O[C:4]1=[C:5]([C:6](=[O:7])[O:8][CH:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[N:22]2[C:23](=[O:24])[CH:25]([NH:26][C:27](=[O:28])[CH2:29][O:30][c:31]3[cH:32][cH:33][cH:34][cH:35][cH:36]3)[C@H:37]2[S:38][CH2:...
C/C=[CH]\[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)c3ccc(Br)cc3)CS[C@H]12
C/C=C\C1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
CN1C(CCC1)=O
C-C Coupling
OtherReaction
37e41cffba8ac668bde391f540caf5d9c270d0ab2160981a195f860115c0841b
8383f8d0bbaf97131fcc20a8fb4f619058433745d77ec5ce8e207bc38c340c6d
O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=CCS[C@H]12
Br-c1:c:c:c(-S(=O)(=O)-O-[C;H0;D3;+0:1]2=[C:2](-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6])-[#7:7](-[C:8]=[O;D1;H0:9])-[C:10]-[#16:11]-[C:12]-2):c:c:1.C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-C-C)/[CH;D2;+0:13]=[C:14]\[C;D1;H3:15]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C:2]1=[C;H0;D3;+0:1](/[CH;D2;+0:13]=[C:14]\[C;D1;H3:15])-[C:12]-[...
null
[]
null
null
20
HOUR
To a mixture of 0.184 g (0.00025 mole) of the product of Procedure 6, 0.103 g (0.0003215 mole) of Z-1-propenyl-tri-n-butylstannane and 0.0064 g (0.000025 mole) of 4-bromobenzenesulfonyl chloride in 2.5 mL of 1-methyl-2-pyrrolidinone, under a nitrogen atmosphere, at room temperature was added 0.006 g (0.000025 mole) of ...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Sulfonate.Tin
Enamine
C1=CN2CC[C@H]2SC1.c1ccccc1
C1=CN2CC[C@H]2SC1
c1ccccc1.c1ccccc1.C1=CN2CC[C@H]2SC1.c1ccccc1
HBr.Sn
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].CN1C(CCC1)=O
null
20
C/C=[CH]\[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.O=C(COc1ccccc1)NC1C(=O)N2C(C(=O)OC(c3ccccc3)c3ccccc3)=C(OS(=O)(=O)c3ccc(Br)cc3)CS[C@H]12>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].CN1C(CCC1)=O>C/C=C\C1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)C(NC(=O)COc3ccccc3)[C@H]2SC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a5d5033460474ef09b7089853a326df4
CC(=O)c1ccco1.COc1ccc(C=O)c(OC)c1.[OH-]>>COc1ccc(C(CC(=O)c2ccco2)CC(=O)c2ccco2)c(OC)c1
COC1=C(C=O)C=CC(=C1)OC.[OH-].[K+].Cl.C(C)(=O)C=1OC=CC1>>O1C(=CC=C1)C(CC(CC(=O)C=1OC=CC1)C1=C(C=C(C=C1)OC)OC)=O
[CH3:16][C:17](=[O:18])[c:19]1[cH:20][cH:21][cH:22][o:23]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][c:11]([CH:9]=[O:10])[c:24]([O:25][CH3:26])[cH:27]1.[OH-:15]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([CH2:8][C:9](=[O:10])[c:11]2[cH:12][cH:13][cH:14][o:15]2)[CH2:16][C:17](=[O:18])[c:19]2[cH:20][cH:21][cH:22][o:23]2)[c:24]([O:...
CC(=O)c1ccco1.COc1ccc(C=O)c(OC)c1.[OH-]
COc1ccc(C(CC(=O)c2ccco2)CC(=O)c2ccco2)c(OC)c1
null
null
CO.O
Aromatic Heterocycle Formation
OtherReaction
a82a1b2f946051e542c74241fe5372a5417c3f7324ebfef97b00a6fc52877822
e1646497bb69536648e831497c90c3e74ad459ff066ba96f00e217e3294c42ff
O=C(CC(CC(=O)c1ccco1)c1ccccc1)c1ccco1
[#8;a:1]:[c:2]-[C:3](-[CH3;D1;+0:4])=[O;D1;H0:5].[C;D1;H3:6]-[#8:7]-[c;H0;D3;+0:8]1:[c:9]:[c:10]:[c:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13]:1-[CH;D2;+0:14]=[O;D1;H0:15].[OH-;D0:16]>>[#8;a:1]:[c:2]-[C:3](=[O;D1;H0:5])-[CH2;D2;+0:4]-[C:17](-[C:18]-[C;H0;D3;+0:14](=[O;D1;H0:15])-[c;H0;D3;+0:13]1:[c:19]:[c:20]:[c:21]:[o;H0;D2;+0...
null
[]
55
CELSIUS
8
HOUR
Following the general methods outlined by Weller and Luellen (see above), to a solution of 16.6 g (0.1 mole) of 2,4-dimethoxybenzaldehyde 1 and 20 ml (0.2 mole) of 2-acetylfuran 2 in 100 ml of methanol was added 5.5 g of potassium hydroxide previously dissolved in a small amount of methanol. The resulting mixture was h...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone.Ether
Ketone.Ketone.Ether
c1ccccc1
c1ccccc1.c1ccoc1
c1ccccc1.c1ccoc1.c1ccoc1
null
CO.O
55
8
CC(=O)c1ccco1.COc1ccc(C=O)c(OC)c1.[OH-]>CO.O>COc1ccc(C(CC(=O)c2ccco2)CC(=O)c2ccco2)c(OC)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-16c771509f2a408d9191b64cdb8e3d2d
CO.COc1cc(OCc2ccccc2)ccc1-c1cc(C(=O)O)nc(C(=O)O)c1>>COC(=O)c1cc(-c2ccc(OCc3ccccc3)cc2OC)cc(C(=O)OC)n1
COC1=C(C=CC(=C1)OCC1=CC=CC=C1)C1=CC(=NC(=C1)C(=O)O)C(=O)O.CO.C(C(=O)Cl)(=O)Cl.Cl>>COC(=O)C1=NC(=CC(=C1)C1=C(C=C(C=C1)OCC1=CC=CC=C1)OC)C(=O)OC
[CH3:1][OH:2].O[C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][cH:19]3)[cH:20][c:21]2[O:22][CH3:23])[cH:24][c:25]([C:26](=[O:27])[OH:28])[n:30]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][cH:17][c...
CO.COc1cc(OCc2ccccc2)ccc1-c1cc(C(=O)O)nc(C(=O)O)c1
COC(=O)c1cc(-c2ccc(OCc3ccccc3)cc2OC)cc(C(=O)OC)n1
null
CN(C)C=O
C(Cl)Cl.O
Protection
OtherReaction
822daae55a346743d1340292c63f5c3519896c50ea9bc191c797511ef8ade007
1610f4d027acc3a508af39670faf7c6ca77bca08137335192290f34a61822d56
c1ccc(COc2ccc(-c3ccncc3)cc2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]-[C:7](=[O;D1;H0:8])-[OH;D1;+0:9].[C;D1;H3:10]-[OH;D1;+0:11]>>[C;D1;H3:10]-[O;H0;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]-[C:7](=[O;D1;H0:8])-[O;H0;D2;+0:9]-[C;D1;H3:12]
65
[{"value": 65.0, "product": "COC(=O)C1=NC(=CC(=C1)C1=C(C=C(C=C1)OCC1=CC=CC=C1)OC)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a suspension of 10 g (0.026 mole) of the diacid 22 in 100 ml of CH2Cl2 and 7 drops of DMF was added, at 0° C., in a dropwise fashion 12 ml (0.138 mole) of oxalyl chloride. After addition the mixture was allowed to come to room temperature with vigorous evolution of HCl gas and stirred for 2 hours. The resulting homo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Methanol
Ester.Ester
null
null
c1ccncc1.c1ccccc1.c1ccccc1
null
CN(C)C=O.C(Cl)Cl.O
null
2
CO.COc1cc(OCc2ccccc2)ccc1-c1cc(C(=O)O)nc(C(=O)O)c1>CN(C)C=O.C(Cl)Cl.O>COC(=O)c1cc(-c2ccc(OCc3ccccc3)cc2OC)cc(C(=O)OC)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9b2830ab861241c3a58e06b4d4dabb73
COC(=O)c1cc(-c2ccc(OCc3ccccc3)cc2OC)cc(C(=O)OC)n1>>COC(=O)c1cc(-c2ccc(O)cc2OC)cc(C(=O)OC)n1
COC(=O)C1=NC(=CC(=C1)C1=C(C=C(C=C1)OCC1=CC=CC=C1)OC)C(=O)OC>>COC(=O)C1=NC(=CC(=C1)C1=C(C=C(C=C1)O)OC)C(=O)OC
c1ccc(C[O:12][c:11]2[cH:10][cH:9][c:8](-[c:7]3[cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[n:23][c:18]([C:19](=[O:20])[O:21][CH3:22])[cH:17]3)[c:14]([O:15][CH3:16])[cH:13]2)cc1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:13][c:14]2[O:15][CH3:16])[cH:17][c:18]([C:19](=[O:20])[O:21][CH3:2...
COC(=O)c1cc(-c2ccc(OCc3ccccc3)cc2OC)cc(C(=O)OC)n1
COC(=O)c1cc(-c2ccc(O)cc2OC)cc(C(=O)OC)n1
null
[Pd]
C(C)O
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc(-c2ccncc2)cc1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
89
[{"value": 89.0, "product": "COC(=O)C1=NC(=CC(=C1)C1=C(C=C(C=C1)O)OC)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 8.9, "product": "COC(=O)C1=NC(=CC(=C1)C1=C(C=C(C=C1)O)OC)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 7 g (0.174 mole) of the diester 23 in 200 ml of ethanol was added 1.0 g of 10% Pd/C. The container for the resulting suspension was evacuated and filled with H2 (repeated three times) and kept under a positive atomosphere by means of a hydrogen-filled rubber bladder for 60 hours with very rapid stirrin...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccncc1.c1ccccc1
Other
[Pd].C(C)O
null
null
COC(=O)c1cc(-c2ccc(OCc3ccccc3)cc2OC)cc(C(=O)OC)n1>[Pd].C(C)O>COC(=O)c1cc(-c2ccc(O)cc2OC)cc(C(=O)OC)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-728658d230cb49b7815fa4f092792817
BrCc1cc(CBr)cc(CBr)c1.O=[N+]=O>>O=[N+]([O-])c1c(CBr)cc(CBr)cc1CBr
BrCC1=CC(=CC(=C1)CBr)CBr.F[B-](F)(F)F.O=[N+]=O.O>>BrCC1=C(C(=CC(=C1)CBr)CBr)[N+](=O)[O-]
[cH:4]1[c:5]([CH2:6][Br:7])[cH:8][c:9]([CH2:10][Br:11])[cH:12][c:13]1[CH2:14][Br:15].[O:1]=[N+:2]=[O:3]>>[O:1]=[N+:2]([O-:3])[c:4]1[c:5]([CH2:6][Br:7])[cH:8][c:9]([CH2:10][Br:11])[cH:12][c:13]1[CH2:14][Br:15]
BrCc1cc(CBr)cc(CBr)c1.O=[N+]=O
O=[N+]([O-])c1c(CBr)cc(CBr)cc1CBr
null
null
CC#N
Functional Group Addition
OtherReaction
276ec2dfce0d9a25107ff9a7c7247f5a9b9ec7b55d27b2ac5d8644ca24f61ef2
5c75a9bf759be9717d985245c85c84dbfff904ea5287869736b84fdaa57f1e27
c1ccccc1
[C:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5](-[C:6]):[c:7].[O;D1;H0:8]=[N+;H0;D2:9]=[O;H0;D1;+0:10]>>[C:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[N+;H0;D3:9](-[O-;H0;D1:10])=[O;D1;H0:8]):[c:5](-[C:6]):[c:7]
86.4
[{"value": 86.0, "product": "BrCC1=C(C(=CC(=C1)CBr)CBr)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.4, "product": "BrCC1=C(C(=CC(=C1)CBr)CBr)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
To a solution of 5 g (0.014 mole) of the tribromide 8 in 100 ml of CH3CN was added, at room temperature and under argon atmosphere, in a dropwise fashion 3.72 g (0.028 mole) of nitronium tetrafluoroborate in 200 ml of CH3CN. The solution was then stirred for 20 minutes longer, poured into water and the mixture extracte...
10.6084/m9.figshare.5104873.v1
null
Nitroso.Nitroso
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
null
CC#N
null
0.333333
BrCc1cc(CBr)cc(CBr)c1.O=[N+]=O>CC#N>O=[N+]([O-])c1c(CBr)cc(CBr)cc1CBr
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1c4af60950e34e5ba3caea2d9484da0b
COC(=O)c1cc(-c2cc(S(=O)(=O)Cl)c(OC)cc2OC)cc(C(=O)OC)n1>>COc1ccc(-c2cc(C(=O)O)nc(C(=O)O)c2)c(OC)c1
CCN(CC)CC.BrCC1=CC(=CC(=C1)CBr)CBr.C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NCCO.BrCC1=CC(=CC(=C1)CBr)CBr.COC(=O)C1=NC(=CC(=C1)C1=C(C=C(C(=C1)S(=O)(=O)Cl)OC)OC)C(=O)OC>>COC1=C(C=CC(=C1)OC)C1=CC(=NC(=C1)C(=O)O)C(=O)O
C[O:12][C:10]([c:9]1[cH:8][c:7](-[c:6]2[cH:5][c:4](S(=O)(=O)Cl)[c:3]([O:2][CH3:1])[cH:22][c:19]2[O:20][CH3:21])[cH:18][c:14]([C:15](=[O:16])[O:17]C)[n:13]1)=[O:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([C:10](=[O:11])[OH:12])[n:13][c:14]([C:15](=[O:16])[OH:17])[cH:18]2)[c:19]([O:20][CH3:21])[cH:22]1
COC(=O)c1cc(-c2cc(S(=O)(=O)Cl)c(OC)cc2OC)cc(C(=O)OC)n1
COc1ccc(-c2cc(C(=O)O)nc(C(=O)O)c2)c(OC)c1
null
null
C(Cl)Cl.O.CO.C(Cl)(Cl)Cl
Reduction
OtherReaction
0d9bf8bfe7d0a18fada4bcbec94d4f089e8dee8ad16619ee01b3b7f91e8e0183
269b2949df4a35609cf974ee1cfd8107cfa459bdc781a6835ee994df4d13402b
c1ccc(-c2ccncc2)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[#7;a:5]:[c:6]-[C:7](=[O;D1;H0:8])-[O;H0;D2;+0:9]-C.Cl-S(=O)(=O)-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13](-[#8:14]):[c:15]>>[#8:14]-[c:13](:[c:15]):[cH;D2;+0:10]:[c:11]:[c:12].[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]:[#7;a:5]:[c:6]-[C:7](=[O;D1;H0:8])-[OH;D1;+0:9]
null
[]
null
null
30
MINUTE
To a suspension of 0.5 g (0.0008 mole) of the amine-hydrochloride 8 in 20 ml of CH2Cl2 was added all at once 1.4 ml (0.01 mole) of Et3N. The mixture was then cooled to 5°-10° C. and 1.4 g (0.0032 mole) of the sulfonyl chloride 39 in 20 ml of CH2Cl2 was slowly added in a dropwise fashion. The reaction was then allowed t...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Sulfonyl halide
Carboxylic acid.Carboxylic acid
c1ccccc1
c1ccccc1
c1ccccc1.c1ccncc1
HCl
C(Cl)Cl.O.CO.C(Cl)(Cl)Cl
null
0.5
COC(=O)c1cc(-c2cc(S(=O)(=O)Cl)c(OC)cc2OC)cc(C(=O)OC)n1>C(Cl)Cl.O.CO.C(Cl)(Cl)Cl>COc1ccc(-c2cc(C(=O)O)nc(C(=O)O)c2)c(OC)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cbb94c59df7b4764bd7a91e9ed9e8888
CCCC[C@@H](Br)C(=O)O.COCOC1CCN(C(=O)[C@@H](O)Cc2ccccc2)CC1>>CCCC[C@H](OCC[C@]1(C(=O)N2CCC(OCOC)CC2)C=CC=CC1)C(=O)O
COCOC1CCN(CC1)C(=O)[C@H](CC1=CC=CC=C1)O.[H-].[Na+].C1CCOC1.C1CCOC1.C1CCOC1.Br[C@@H](C(=O)O)CCCC.C1CCOC1>>COCOC1CCN(CC1)C(=O)[C@@]1(CC=CC=C1)CCO[C@H](C(=O)O)CCCC
Br[C@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[C:27](=[O:28])[OH:29].[OH:6][C@@H:9]([CH2:8][c:7]1[cH:22][cH:23][cH:24][cH:25][cH:26]1)[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][CH:15]([O:16][CH2:17][O:18][CH3:19])[CH2:20][CH2:21]1>>[CH3:1][CH2:2][CH2:3][CH2:4][C@H:5]([O:6][CH2:7][CH2:8][C@:9]1([C:10](=[O:11])[N:12]2[CH2:13][CH2:1...
CCCC[C@@H](Br)C(=O)O.COCOC1CCN(C(=O)[C@@H](O)Cc2ccccc2)CC1
CCCC[C@H](OCC[C@]1(C(=O)N2CCC(OCOC)CC2)C=CC=CC1)C(=O)O
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
f9986e1066abeec14926410b5ca286b88f8c775731227b44ed34901ada297548
9b5f806834b6f9c74cdf1cbb6fa2220ed02cfe05046870520204e39c58bb7b7b
O=C(C1C=CC=CC1)N1CCCCC1
Br-[C@H;D3;+0:1](-[C:2]-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[C:7]-[#7:8](-[C:9](=[O;D1;H0:10])-[C@@H;D3;+0:11](-[OH;D1;+0:12])-[C:13]-[c;H0;D3;+0:14]1:[cH;D2;+0:15]:[cH;D2;+0:16]:[cH;D2;+0:17]:[cH;D2;+0:18]:[cH;D2;+0:19]:1)-[C:20]>>[C:7]-[#7:8](-[C:9](=[O;D1;H0:10])-[C@;H0;D4;+0:11]1(-[C:13]-[CH2;D2;+0:14]-[O;H0;D2;...
60
[{"value": 60.0, "product": "COCOC1CCN(CC1)C(=O)[C@@]1(CC=CC=C1)CCO[C@H](C(=O)O)CCCC", "details": "PERCENTYIELD", "is_desired": false}]
45
CELSIUS
1
HOUR
1(S)-(4-(Methoxymethoxy)piperidin-1-yl-carbonyl)-2-phenylethanol (European Patent Application No. EP364804, published Apr. 25, 1991) (43.13 g, 147.2 mmol) in 200 mL dry THF was added dropwise to the suspension of sodium hydride (60% dispersion in oil, 12.36 g, 309.1 mmol) in 136 mL dry THF and 22.7 mL DMF at 45° C. oil...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary alcohol
Ether.Conjugated diene
c1ccccc1
C1=CCCC=C1
C1CC[NH]CC1.C1=CCCC=C1
Br-
CN(C)C=O
45
1
CCCC[C@@H](Br)C(=O)O.COCOC1CCN(C(=O)[C@@H](O)Cc2ccccc2)CC1>CN(C)C=O>CCCC[C@H](OCC[C@]1(C(=O)N2CCC(OCOC)CC2)C=CC=CC1)C(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9ef05d718e3f423da6bae4217b5ff8bd
NCCCN.O=C(OCc1ccccc1)ON1C(=O)CCC1=O>>NCCCNC(=O)OCc1ccccc1
NCCCN.C(C1=CC=CC=C1)OC(=O)ON1C(CCC1=O)=O>>C(C1=CC=CC=C1)OC(=O)NCCCN
[NH2:1][CH2:2][CH2:3][CH2:4][NH2:5].O=C1CCC(=O)N1O[C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1>>[NH2:1][CH2:2][CH2:3][CH2:4][NH:5][C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1
NCCCN.O=C(OCc1ccccc1)ON1C(=O)CCC1=O
NCCCNC(=O)OCc1ccccc1
null
null
C(Cl)(Cl)Cl
Protection
OtherReaction
90f1cd2cfb4916c247fdb0b8c4bcd653fe37fb375d251f3afd49969111cee737
f7ec1d72774a3155b06d1cf24e018b58f69117ddf4d9559df84efc3ecef0f4d7
c1ccccc1
O=C1-C-C-C(=O)-N-1-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]
80
[{"value": 80.0, "product": "C(C1=CC=CC=C1)OC(=O)NCCCN", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.0, "product": "C(C1=CC=CC=C1)OC(=O)NCCCN", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
8
HOUR
1,3-Diaminopropane (35.5 g, 0.48 mol) was dissolved in 300 mL CHCl3, and the solution was cooled to 0° C. A solution of N-(benzyloxycarbonyloxy)succinimide (4.5 g, 0.018 mol) in 150 mL CHCl3 was added dropwise over 6 h, with the internal temperature maintained below 10° C. After addition was complete, the reaction solu...
10.6084/m9.figshare.5104873.v1
null
Ether.Tertiary amide.Tertiary amide.Primary amine
Carbamic ester
C1CCNC1
null
c1ccccc1
HO-
C(Cl)(Cl)Cl
0
8
NCCCN.O=C(OCc1ccccc1)ON1C(=O)CCC1=O>C(Cl)(Cl)Cl>NCCCNC(=O)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-622c30d078094a8eb9dec49e03627d22
CCC(C)(CO)NC(=O)OCc1ccccc1.[N-]=[N+]=[N-]>>CCC(C)(CN=[N+]=[N-])NC(=O)OCc1ccccc1
N=[N+]=[N-].[O-]S(=O)(=O)[O-].[Mg+2].N(=NC(=O)OC(C)C)C(=O)OC(C)C.[N-]=[N+]=[N-].C(C1=CC=CC=C1)OC(=O)NC(CO)(CC)C.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>N(=[N+]=[N-])CC(CC)(C)NC(=O)OCC1=CC=CC=C1
O[CH2:5][C:3]([CH2:2][CH3:1])([CH3:4])[NH:9][C:10](=[O:11])[O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[N-:6]=[N+:7]=[N-:8]>>[CH3:1][CH2:2][C:3]([CH3:4])([CH2:5][N:6]=[N+:7]=[N-:8])[NH:9][C:10](=[O:11])[O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
CCC(C)(CO)NC(=O)OCc1ccccc1.[N-]=[N+]=[N-]
CCC(C)(CN=[N+]=[N-])NC(=O)OCc1ccccc1
null
null
CCOC(=O)C.CCCCCC.C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
b6ef7629d0f9b9d1438b20ee6805124558e67d10777a15184211800dd3e8b973
a446353c66aa2c48beeb0e3765234578855c107c1200bfc64cebc8b68d490616
c1ccccc1
O-[CH2;D2;+0:1]-[C:2](-[C:3])(-[C;D1;H3:4])-[#7:5]-[C:6]=[O;D1;H0:7].[N-;H0;D1:8]=[#7;+:9]=[N;-;D1;H0:10]>>[C:3]-[C:2](-[C;D1;H3:4])(-[#7:5]-[C:6]=[O;D1;H0:7])-[CH2;D2;+0:1]-[N;H0;D2;+0:8]=[#7;+:9]=[N;-;D1;H0:10]
null
[]
0
CELSIUS
1
HOUR
2-(Benyloxycarbonylamino)-2-methyl-1-butanol (1.358 g, 5.722 mmol) and triphenylphosphine (1.800 g, 6.86 mmol) were dissolved in 10 mL CH2Cl2, and the resulting solution was cooled to 0° C. A solution of hydrazoic acid (prepared from sodium azide (1.30 g, 20.0 mmol), 0.533 mL concentrated sulfuric acid and 1.3 mL water...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Azide
null
null
c1ccccc1
HO-
CCOC(=O)C.CCCCCC.C(Cl)Cl
0
1
CCC(C)(CO)NC(=O)OCc1ccccc1.[N-]=[N+]=[N-]>CCOC(=O)C.CCCCCC.C(Cl)Cl>CCC(C)(CN=[N+]=[N-])NC(=O)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-86be50e43ce8445287687f9a0c4a1bac
CC(C)=C1C[C@H](O)[C@H](CC2CCCCC2)NC1=O>>CC(C)[C@@H]1C[C@H](O)[C@H](C2CCCCC2)NC1=O
C1(CCCCC1)C[C@H]1[C@H](CC(C(N1)=O)=C(C)C)O>>C1(CCCCC1)[C@H]1[C@H](C[C@H](C(N1)=O)C(C)C)O
C1([CH2:9][C@H:8]2[C@@H:6]([OH:7])[CH2:5][C:4](=[C:2]([CH3:1])[CH3:3])[C:16](=[O:17])[NH:15]2)[CH2:10][CH2:11][CH2:12][CH2:13][CH2:14]1>>[CH3:1][CH:2]([CH3:3])[C@@H:4]1[CH2:5][C@H:6]([OH:7])[C@H:8]([CH:9]2[CH2:10][CH2:11][CH2:12][CH2:13][CH2:14]2)[NH:15][C:16]1=[O:17]
CC(C)=C1C[C@H](O)[C@H](CC2CCCCC2)NC1=O
CC(C)[C@@H]1C[C@H](O)[C@H](C2CCCCC2)NC1=O
null
[Pd]
C(C)(=O)OCC
Miscellaneous
OtherReaction
991a348c41662c029ddb376b9f1a188f98cd62eb88df9b000ea2621c824cd773
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1CCC[C@H](C2CCCCC2)N1
[C;D1;H3:1]-[C;H0;D3;+0:2](-[C;D1;H3:3])=[C;H0;D3;+0:4]1-[C:5]-[C:6]-[C:7](-[CH2;D2;+0:8]-C2-[CH2;D2;+0:9]-[C:10]-[C:11]-[C:12]-[CH2;D2;+0:13]-2)-[#7:14]-[C:15]-1=[O;D1;H0:16]>>[C;D1;H3:1]-[CH;D3;+0:2](-[C;D1;H3:3])-[C@@H;D3;+0:4]1-[C:5]-[C:6]-[C:7](-[CH;D3;+0:8]2-[CH2;D2;+0:9]-[C:10]-[C:11]-[C:12]-[CH2;D2;+0:13]-2)-[#...
null
[]
null
null
null
null
A solution of the product of Example 80e (24.7 g, 98.4 mmol) in 500 ml of ethyl acetate was treated with 2.5 g of dry Pd/C and hydrogenated at 4 atm for 4h at ambient temperature. The reaction mixture was filtered and concentrated to a white foamy solid which was taken on without further purification. mp 97°-99° C.; [α...
10.6084/m9.figshare.5104873.v1
null
null
null
C1CCNCC1.C1CCCCC1
C1CCNCC1.C1CCCCC1
C1CCNCC1.C1CCCCC1
Other
[Pd].C(C)(=O)OCC
null
null
CC(C)=C1C[C@H](O)[C@H](CC2CCCCC2)NC1=O>[Pd].C(C)(=O)OCC>CC(C)[C@@H]1C[C@H](O)[C@H](C2CCCCC2)NC1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6c6d592bcf1a42debe7854b152d5967a
CCC[CH2][Mg][Br].O=Cc1ccco1>>CCCCC(O)c1ccco1
C(C1=CC=CO1)=O.C(CCC)[Mg]Br.[NH4+].[Cl-]>>O1C(=CC=C1)C(CCCC)O
[Br][Mg][CH2:4][CH2:3][CH2:2][CH3:1].[CH:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][o:11]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([OH:6])[c:7]1[cH:8][cH:9][cH:10][o:11]1
CCC[CH2][Mg][Br].O=Cc1ccco1
CCCCC(O)c1ccco1
null
null
C1CCOC1
C-C Coupling
Grignard from aldehyde to alcohol
fec51c6fbcca146daa523566f7e8d93ddaee19549cd7ca45d0ef939f0a2ea2fd
38fa131ecaada942f85a297b49034b58ccef3f2e8ba6de5e28a59b5f4292ff1f
c1ccoc1
[Br]-[Mg]-[CH2;D2;+0:1]-[C:2]-[C:3].[O;H0;D1;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[#8;a:8]:[c:9]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:5](-[OH;D1;+0:4])-[c:6](:[c:7]):[#8;a:8]:[c:9]
null
[]
null
null
null
null
Freshly distilled furfural (233.5 g, 2.43 mol) was dissolved in 200 mL freshly distilled THF and added dropwise to a solution of butylmagnesium bromide (2.0 M in THF, 1460 mL, 2.92 mol) at 0° C. under dry nitrogen. After the addition was complete, the mixture was allowed to warm to room temperature overnight. The react...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Aldehyde
Secondary alcohol
null
null
c1ccoc1
Br-.Mg
C1CCOC1
null
null
CCC[CH2][Mg][Br].O=Cc1ccco1>C1CCOC1>CCCCC(O)c1ccco1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c3362f70087947e9a7caa72bda54863b
CCCCC(=O)c1ccco1>>CCCC[C@H](O)c1ccco1
B#B.C(CCCC)(=O)C=1OC=CC1.O1B=NC=C1.Cl>>O1C(=CC=C1)[C@H](CCCC)O
[CH3:1][CH2:2][CH2:3][CH2:4][C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][o:11]1>>[CH3:1][CH2:2][CH2:3][CH2:4][C@H:5]([OH:6])[c:7]1[cH:8][cH:9][cH:10][o:11]1
CCCCC(=O)c1ccco1
CCCC[C@H](O)c1ccco1
null
null
C1CCOC1.CO.CCOCC
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccoc1
[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5](:[c:6]):[#8;a:7]:[c:8]>>[C:1]-[C:2]-[C@H;D3;+0:3](-[OH;D1;+0:4])-[c:5](:[c:6]):[#8;a:7]:[c:8]
70
[{"value": 70.0, "product": "O1C(=CC=C1)[C@H](CCCC)O", "details": "PERCENTYIELD", "is_desired": false}]
10
CELSIUS
null
null
10.4 mmol (10.4 mL) of diborane (1 M solution in THF) was added dropwise in a period of 10 m at room temperature to a solution of 2-valeryl furan (2.62 g, 17.2 mmol) and 1.68 mmol (4.2 mL) of (3aR)-1,3,3-triphenyl pyrrolidino [1,2-c] [1,3,2] oxazaborole (see E. J. Corey et al. J. Am. Chem. Soc. 1987, 109, 7925-26, 0.4M...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccoc1
null
C1CCOC1.CO.CCOCC
10
null
CCCCC(=O)c1ccco1>C1CCOC1.CO.CCOCC>CCCC[C@H](O)c1ccco1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c6c1fca572fe4e32bea0275f2d8b6a26
CCCC[C@H](O)c1ccco1.O=C(O)CBr>>CCCCC(OCC(=O)O)c1ccco1
[H-].[Na+].O1C(=CC=C1)[C@H](CCCC)O.BrCC(=O)O>>O1C(=CC=C1)C(OCC(=O)O)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][C@H:5]([OH:6])[c:11]1[cH:12][cH:13][cH:14][o:15]1.Br[CH2:7][C:8](=[O:9])[OH:10]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([O:6][CH2:7][C:8](=[O:9])[OH:10])[c:11]1[cH:12][cH:13][cH:14][o:15]1
CCCC[C@H](O)c1ccco1.O=C(O)CBr
CCCCC(OCC(=O)O)c1ccco1
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
2e63de7b1f097c059f31781c5dec3b7812b761a1b3812b5238753f554cfa0846
9d3e82e8fa4f4bc62c1019e0bd869bdb0cf4748977f3c0b945b8ffdfc70126be
c1ccoc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[O;D1;H1:4].[C:5]-[C:6]-[C@H;D3;+0:7](-[OH;D1;+0:8])-[c:9](:[c:10]):[#8;a:11]:[c:12]>>[C:5]-[C:6]-[CH;D3;+0:7](-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[O;D1;H1:4])-[c:9](:[c:10]):[#8;a:11]:[c:12]
null
[]
0
CELSIUS
null
null
NaH (16.3 g, 680.9 mmol) and freshly distilled THF (170 mL) Were stirred at room temperature as (S)-1-(2-furyl)-1-pentanol ([α]25D -17.2°, 30.0 g, 46.0 mmol) in THF (170 mL) was added dropwise. After the addition was complete, the mixture was stirred for 15 m before cautiously heating to reflux for 1 h. The mixture was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary alcohol
Ether
null
null
c1ccoc1
HBr
C1CCOC1
0
null
CCCC[C@H](O)c1ccco1.O=C(O)CBr>C1CCOC1>CCCCC(OCC(=O)O)c1ccco1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-98ddb6a92a0a4ff7b45cdbe2ae30430c
CCCCC(OCC(=O)O)c1ccco1>>CCCCC(OCC(=O)OC)c1ccco1
[N+](=[N-])=C.O1C(=CC=C1)C(OCC(=O)O)CCCC.[OH-].[K+].CN(C(=N)N[N+](=O)[O-])N=O>>O1C(=CC=C1)C(OCC(=O)OC)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([O:6][CH2:7][C:8](=[O:9])[OH:10])[c:12]1[cH:13][cH:14][cH:15][o:16]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([O:6][CH2:7][C:8](=[O:9])[O:10][CH3:11])[c:12]1[cH:13][cH:14][cH:15][o:16]1
CCCCC(OCC(=O)O)c1ccco1
CCCCC(OCC(=O)OC)c1ccco1
null
null
CCOCC
Miscellaneous
OtherReaction
56520e0abb4535dce9a663824ca803b71c2c0dd72dfd246317d953596a987bd2
2ccc7a30191c2c171b49e8a0217bee87430687dd0f567141eca025a75b7e3136
c1ccoc1
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[C;D1;H3:5]
null
[]
null
null
null
null
Crude acid from example 84 (25 g, 118 mmol) was dissolved in ether and treated with excess diazomethane (generated by adding 1-methyl-3-nitro-1-nitrosoguanidine (MNNG) to a mixture of 40% KOH (aq) and ether at 0° C.). Excess diazomethane was quenched with acetic acid after 30 m. Vacuum distillation gave 18.8 g (70%): [...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1ccoc1
Other
CCOCC
null
null
CCCCC(OCC(=O)O)c1ccco1>CCOCC>CCCCC(OCC(=O)OC)c1ccco1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ad9cc210d01d4d0d92c70ab465fa4799
BrCc1ccccc1.CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1>>CCCC[C@H](O[C@@H](Cc1ccccc1)C(=O)OC(c1ccccc1)c1ccccc1)c1ccco1
C(C1=CC=CC=C1)Br.O1C(=CC=C1)C(OCC(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)CCCC.C[Si](C)(C)[N-][Si](C)(C)C.[Na+]>>C(C1=CC=CC=C1)[C@@H](C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)O[C@@H](CCCC)C=1OC=CC1
Br[CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([O:6][CH2:7][C:15](=[O:16])[O:17][CH:18]([c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1)[c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1)[c:31]1[cH:32][cH:33][cH:34][o:35]1>>[CH3:1][CH2:2][CH2:3][CH2:4][C@H:5]([O:6][C@@H:7]([CH2:8][c:9]1[cH:...
BrCc1ccccc1.CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1
CCCC[C@H](O[C@@H](Cc1ccccc1)C(=O)OC(c1ccccc1)c1ccccc1)c1ccco1
null
null
C1CCOC1.CN(C)P(=O)(N(C)C)N(C)C
C-C Coupling
OtherReaction
796fea58c3dd096157de0ee3a241534b729bfe3e21ae3e32235c219d66dae5fc
8ef4a7f3c2aa2c61ba42c1b7d8665a33daf968ae3eb9e2122661626a98ff3349
O=C(OC(c1ccccc1)c1ccccc1)[C@H](Cc1ccccc1)OCc1ccco1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[CH2;D2;+0:9]-[#8:10]-[C:11]>>[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C@@H;D3;+0:9](-[#8:10]-[C:11])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
0
CELSIUS
null
null
Benzhydryl 4-(2-furyl)-3-oxaoctanoate (2.0 g, 5.28 mmol) was dissolved in 20 mL freshly distilled THF and cooled to -80°±5° C. under dry argon. Sodium bis(trimethylsilyl)-amide (1.0M in THF, 5.6 mL, 5.6 mmol) was slowly added keeping the temperature at -80°±5° C. After 15 m, freshly distilled and filtered (through basi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ester.Ether
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccoc1
HBr
C1CCOC1.CN(C)P(=O)(N(C)C)N(C)C
0
null
BrCc1ccccc1.CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1>C1CCOC1.CN(C)P(=O)(N(C)C)N(C)C>CCCC[C@H](O[C@@H](Cc1ccccc1)C(=O)OC(c1ccccc1)c1ccccc1)c1ccco1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-85107b868f4343088910de19a024cbd4
BrCc1ccccc1.C1CCOC1.CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1.C[Si](C)(C)[N-][Si](C)(C)C>>CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1.CCCC[C@H](O[C@H](Cc1ccccc1)C(=O)OC(c1ccccc1)c1ccccc1)c1ccco1
C1CCOC1.C(C1=CC=CC=C1)Br.C[Si](C)(C)[N-][Si](C)(C)C.[Na+].O1C(=CC=C1)C(OCC(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)CCCC>>C(C1=CC=CC=C1)[C@H](C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)O[C@@H](CCCC)C=1OC=CC1.O1C(=CC=C1)C(OCC(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)CCCC
Br[CH2:36][c:37]1[cH:38][cH:39][cH:40][cH:41][cH:42]1.[O:10]1[CH2:35][CH2:43][CH2:60][CH2:59]1.[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([O:6][CH2:7][C:8](=[O:9])[O:45][CH:46]([c:47]1[cH:48][cH:49][cH:50][cH:51][cH:52]1)[c:53]1[cH:54][cH:55][cH:56][cH:57][cH:58]1)[c:24]1[cH:25][cH:26][cH:62][o:63]1.[N-]([Si]([CH3:11])([CH3:12...
BrCc1ccccc1.C1CCOC1.CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1.C[Si](C)(C)[N-][Si](C)(C)C
CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1.CCCC[C@H](O[C@H](Cc1ccccc1)C(=O)OC(c1ccccc1)c1ccccc1)c1ccco1
null
null
CN(C)P(=O)(N(C)C)N(C)C
Aromatic Heterocycle Formation
OtherReaction
7c60e600fc7752f5f072b648ee44370457581b73a772d9bd30ab1c7fcea689de
43f79a516217ddbf42d742f13759e3245ac5815b86c63e06b09cb7fc320df01d
O=C(COCc1ccco1)OC(c1ccccc1)c1ccccc1.O=C(OC(c1ccccc1)c1ccccc1)[C@@H](Cc1ccccc1)OCc1ccco1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH2;D2;+0:5]1-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-1.[CH3;D1;+0:10]-[Si](-[CH3;D1;+0:11])(-[CH3;D1;+0:12])-[N-]-[Si](-[CH3;D1;+0:13])(-[CH3;D1;+0:14])-[CH3;D1;+0:15].[C:16]-[C:17](-[#8:18]-[C:19]-[C;H0;D3;+0:20](=[O;D1;H0:21])-[O;H0;D2;+0:22]-[C:23](-[c:24])-[c:...
null
[]
null
null
null
null
Using the procedure in example 90 and (4S) benzhydryl 4-(2-furyl)-3-oxaoctanoate (5.0 g, 13.2 mmol), THF (50 mL), sodium bis(trimethylsilyl)amide (1.0M in THF, 14 mL, 14 mmol), and benzyl bromide (1.7 mL, 14 mmol) in 10 mL HMPA gave (2R,4S) benzhydryl 2-Benzyl-4-(2-furyl)-3-oxaoctanoate, 646.6 mg (10%) and 723 mg (12%)...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ether.Silyl protective group.Silyl protective group
Ester.Ester.Ether
C1CCOC1.c1ccoc1
c1ccccc1.c1ccccc1.c1ccoc1.c1ccoc1
c1ccccc1.c1ccccc1.c1ccoc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccoc1
HBr
CN(C)P(=O)(N(C)C)N(C)C
null
null
BrCc1ccccc1.C1CCOC1.CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1.C[Si](C)(C)[N-][Si](C)(C)C>CN(C)P(=O)(N(C)C)N(C)C>CCCCC(OCC(=O)OC(c1ccccc1)c1ccccc1)c1ccco1.CCCC[C@H](O[C@H](Cc1ccccc1)C(=O)OC(c1ccccc1)c1ccccc1)c1ccco1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c487bc368b6d4d0ab11ca0373808a940
COC(=O)CC(=O)OC.Cc1ccccc1>>CC(=O)C=Cc1ccc(C)cc1
C(CC(=O)OC)(=O)OC.C[O-].[Na+].C1(=CC=CC=C1)C>>CC1=CC=C(C=CC(C)=O)C=C1
CO[C:2]([CH2:1][C:4](=O)OC)=[O:3].[cH:6]1[cH:7][cH:8][c:9]([CH3:10])[cH:11][cH:12]1>>[CH3:1][C:2](=[O:3])[CH:4]=[CH:5][c:6]1[cH:7][cH:8][c:9]([CH3:10])[cH:11][cH:12]1
COC(=O)CC(=O)OC.Cc1ccccc1
CC(=O)C=Cc1ccc(C)cc1
null
null
null
C-C Coupling
OtherReaction
8d85ac46602381ac081b39162f9d8eca42fcb98834561ecff1ad0ba1cfdd62ee
53456c3e87e97f512921684f59b54573df1eee9d8c313db55cd612727f50bb31
c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[C;H0;D3;+0:4](=O)-O-C.[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[CH3;D1;+0:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D2;+0:4]=[C:10]-[c;H0;D3;+0:7](:[c:6]:[c:5]):[c:8]:[c:9]
null
[]
null
null
null
null
132 g of dimethyl malonate are introduced into 1 liter of toluene and 180 g of 30% strength sodium methylate solution are added at room temperature. A crystal slurry results, to which 160 g of p-methylbenzalacetone are added dropwise, with vigorous stirring. In the course of 3 hours, the reaction mixture is heated, wit...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
COC(=O)CC(=O)OC.Cc1ccccc1>>CC(=O)C=Cc1ccc(C)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c5320739ecb94875895071e346290d87
CC(=O)C=CC1CCCCC1.CCCC(=O)Cl.COC(=O)CC(=O)OC>>CCCC(=O)C1C(=O)CC(C2CCCCC2)CC1=O
[OH-].[Na+].C(CC(=O)OC)(=O)OC.C[O-].[Na+].C1(CCCCC1)C=CC(C)=O.C(CCC)(=O)Cl.Cl>>C(CCC)(=O)C1C(CC(CC1=O)C1CCCCC1)=O
[CH3:6][C:18]([CH:17]=[CH:10][CH:11]1[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]1)=[O:19].Cl[C:4]([CH2:3][CH2:2][CH3:1])=[O:5].COC(=O)[CH2:9][C:7](OC)=[O:8]>>[CH3:1][CH2:2][CH2:3][C:4](=[O:5])[CH:6]1[C:7](=[O:8])[CH2:9][CH:10]([CH:11]2[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]2)[CH2:17][C:18]1=[O:19]
CC(=O)C=CC1CCCCC1.CCCC(=O)Cl.COC(=O)CC(=O)OC
CCCC(=O)C1C(=O)CC(C2CCCCC2)CC1=O
null
null
C1(=CC=CC=C1)C.O
C-C Coupling
OtherReaction
e639475b924337c5181658d8a90a476ce491ff68027c341ba066aa3a55bb19e7
47470a729eeccda5bfeca983e4a619ea5fd51226dabbab763f38b7a3cc65932e
O=C1CC(=O)CC(C2CCCCC2)C1
C-O-C(=O)-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-O-C.Cl-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[C:7].[C:8]-[C:9](-[CH;D2;+0:10]=[CH;D2;+0:11]-[C:12](-[CH3;D1;+0:13])=[O;D1;H0:14])-[C:15]>>[C:8]-[C:9](-[CH;D3;+0:10]1-[CH2;D2;+0:11]-[C:12](=[O;D1;H0:14])-[CH;D3;+0:13](-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[C:7])-[C;H0;D3;+...
84.1
[{"value": 84.0, "product": "C(CCC)(=O)C1C(CC(CC1=O)C1CCCCC1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.1, "product": "C(CCC)(=O)C1C(CC(CC1=O)C1CCCCC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
4
HOUR
132 g of dimethyl malonate, 180 g of 30% strength sodium methylate, 152 g of 1-cyclohexylbut-1-en-3-one and 106.5 g of butyryl chloride are reacted in 1 liter of toluene, in a manner similar to that described in Example 1. 5 g of 4-N,N-dimethylaminopyridine are added to the reaction mixture thus obtained and the batch ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ketone.Ester.Ester
Ketone.Ketone.Ketone
null
C1CCCCC1
C1CCCCC1.C1CCCCC1
HCl
C1(=CC=CC=C1)C.O
100
4
CC(=O)C=CC1CCCCC1.CCCC(=O)Cl.COC(=O)CC(=O)OC>C1(=CC=CC=C1)C.O>CCCC(=O)C1C(=O)CC(C2CCCCC2)CC1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7b40b92986b142c0b4b761dffa4e4a2f
NNC(=O)c1ccc(O)cc1.Nc1ccccc1.O=C(Oc1ccccc1)c1ccc(O)cc1>>Oc1ccc(-c2nnc(-c3ccc(O)cc3)n2-c2ccccc2)cc1
Cl.NC1=CC=CC=C1.OC1=CC=C(C(=O)NN)C=C1.C1(=CC=CC=C1)OC(C1=CC=C(C=C1)O)=O.C1(=CC=CC=C1)O>>OC1=CC=C(C=C1)C1=NN=C(N1C1=CC=CC=C1)C1=CC=C(C=C1)O
O=[C:9]([NH:8][NH2:7])[c:10]1[cH:11][cH:12][c:13]([OH:14])[cH:15][cH:16]1.[NH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1.O=[C:6](Oc1ccccc1)[c:5]1[cH:4][cH:3][c:2]([OH:1])[cH:25][cH:24]1>>[OH:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][n:8][c:9](-[c:10]3[cH:11][cH:12][c:13]([OH:14])[cH:15][cH:16]3)[n:17]2-[c:18]2[cH:19]...
NNC(=O)c1ccc(O)cc1.Nc1ccccc1.O=C(Oc1ccccc1)c1ccc(O)cc1
Oc1ccc(-c2nnc(-c3ccc(O)cc3)n2-c2ccccc2)cc1
null
null
null
Miscellaneous
OtherReaction
3e9d0771548b24a3dc578df7b57aa1316c5a49b1e735951568a99ab9d6cf916b
e8af21e0f05f2b373585a67d65b8addb689f3c29b4af5933891ef079411717fe
c1ccc(-c2nnc(-c3ccccc3)n2-c2ccccc2)cc1
O=[C;H0;D3;+0:1](-O-c1:c:c:c:c:c:1)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].O=[C;H0;D3;+0:7](-[NH;D2;+0:8]-[NH2;D1;+0:9])-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14].[NH2;D1;+0:15]-[c;H0;D3;+0:16](:[c:17]:[c:18]):[c:19]:[c:20]>>[c:12]:[c:11]:[c;H0;D3;+0:10](-[c;H0;D3;+0:7]1:[n;H0;D2;+0:8]:[n;H0;D2;+0:9]:[c;H0;D3;+0:...
50
[{"value": 50.0, "product": "OC1=CC=C(C=C1)C1=NN=C(N1C1=CC=CC=C1)C1=CC=C(C=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.9, "product": "OC1=CC=C(C=C1)C1=NN=C(N1C1=CC=CC=C1)C1=CC=C(C=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
220
CELSIUS
2
HOUR
Into a 500 ml three neck round bottom flask equipped with a magnetic stirbar, nitrogen inlet, glass stopper, and distillation head was placed 4-hydroxybenzoic hydrazide (60.9 g, 0.4 mol) and phenyl-4-hydroxybenzoate (85.7 g, 0.4 mol). The mixture was heated to approximately 220° C. by use of a Wood's metal bath. The so...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Ester.Primary amine
null
c1ccccc1
c1nc[nH]n1
c1ccccc1.c1nc[nH]n1.c1ccccc1.c1ccccc1
HO-
null
220
2
NNC(=O)c1ccc(O)cc1.Nc1ccccc1.O=C(Oc1ccccc1)c1ccc(O)cc1>>Oc1ccc(-c2nnc(-c3ccc(O)cc3)n2-c2ccccc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-067a37df0148453b970f7e876cfd2a25
Nc1ccc(Oc2ccc(N)c(N)c2)cc1N.O=C(Oc1ccccc1)c1ccc(O)cc1>>Oc1ccc(-c2nc3ccc(Oc4ccc5nc(-c6ccc(O)cc6)[nH]c5c4)cc3[nH]2)cc1
NC=1C=C(C=CC1N)OC1=CC(=C(C=C1)N)N.C1(=CC=CC=C1)OC(C1=CC=C(C=C1)O)=O.C1(=CC=CC=C1)S(=O)(=O)C1=CC=CC=C1.C1(=CC=CC=C1)C>>O(C1=CC2=C(N=C(N2)C2=CC=C(C=C2)O)C=C1)C1=CC2=C(N=C(N2)C2=CC=C(C=C2)O)C=C1
[NH2:7][c:8]1[cH:9][cH:10][c:11]([O:12][c:13]2[cH:14][cH:15][c:16]([NH2:17])[c:27]([NH2:26])[cH:28]2)[cH:29][c:30]1[NH2:31].O=[C:18]([O:1][c:2]1[cH:3][cH:4][cH:5][cH:32][cH:33]1)[c:19]1[cH:20][cH:21][c:22]([OH:23])[cH:24][cH:25]1>>[OH:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][c:8]3[cH:9][cH:10][c:11]([O:12][c:13]4[cH:14][...
Nc1ccc(Oc2ccc(N)c(N)c2)cc1N.O=C(Oc1ccccc1)c1ccc(O)cc1
Oc1ccc(-c2nc3ccc(Oc4ccc5nc(-c6ccc(O)cc6)[nH]c5c4)cc3[nH]2)cc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
b911e48fe0a935f11d86453f9883acd47f0fc29a62d1c675eb70c867aec92c56
34a7f1192421a044c579c0d3f24e7e4d6654369b06ecfa22ca5e8f8321b21675
c1ccc(-c2nc3ccc(Oc4ccc5nc(-c6ccccc6)[nH]c5c4)cc3[nH]2)cc1
O=[C;H0;D3;+0:1](-[O;H0;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]:1)-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13].[NH2;D1;+0:14]-[c:15](:[c:16]):[c:17](-[NH2;D1;+0:18]):[c:19].[NH2;D1;+0:20]-[c:21](:[c:22]):[c:23](-[NH2;D1;+0:24]):[c:25]>>[OH;D1;+0:2]-[c:3]1:[c:4]:[c:5]:[c;H0;D3;+0:6](-[c:26]2:[n;H0;D2;+0:24...
30
[{"value": 30.0, "product": "O(C1=CC2=C(N=C(N2)C2=CC=C(C=C2)O)C=C1)C1=CC2=C(N=C(N2)C2=CC=C(C=C2)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
150
CELSIUS
null
null
A mixture of bis(3,4-diaminophenyl)ether (22.00 g, 0.096 mol), phenyl-4-hydroxybenzoate (41.00 g, 0.194 mol), diphenylsulfone (110.17 g), and toluene (135 ml) was heated under a nitrogen atmosphere for 3.5 hours at 150° C. The toluene was removed and the temperature increased to 250° C. and maintained for 1.5 hours. A ...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine.Primary amine.Primary amine.Primary amine
Aromatic alcohol
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccc2[nH]cnc2c1.c1ccc2[nH]cnc2c1
c1ccccc1.c1ccc2[nH]cnc2c1.c1ccc2[nH]cnc2c1.c1ccccc1
null
null
150
null
Nc1ccc(Oc2ccc(N)c(N)c2)cc1N.O=C(Oc1ccccc1)c1ccc(O)cc1>>Oc1ccc(-c2nc3ccc(Oc4ccc5nc(-c6ccc(O)cc6)[nH]c5c4)cc3[nH]2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cb39671eefbe47ab97af0a8c7bd6ff15
C[C@@H]1CNC[C@H]1NC(=O)OC(C)(C)C.O=C(Cl)c1ccccc1>>C[C@@H]1CN(C(=O)c2ccccc2)C[C@H]1NC(=O)OC(C)(C)C
C(C)N(CC)CC.C(C1=CC=CC=C1)(=O)Cl.C(C)(C)(C)OC(=O)N[C@@H]1CNC[C@H]1C>>C(C)(C)(C)OC(=O)N[C@@H]1CN(C[C@H]1C)C(C1=CC=CC=C1)=O
[CH3:1][C@@H:2]1[CH2:3][NH:4][CH2:13][C@H:14]1[NH:15][C:16](=[O:17])[O:18][C:19]([CH3:20])([CH3:21])[CH3:22].Cl[C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][C@@H:2]1[CH2:3][N:4]([C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[CH2:13][C@H:14]1[NH:15][C:16](=[O:17])[O:18][C:19]([CH3:20])([CH3:21])...
C[C@@H]1CNC[C@H]1NC(=O)OC(C)(C)C.O=C(Cl)c1ccccc1
C[C@@H]1CN(C(=O)c2ccccc2)C[C@H]1NC(=O)OC(C)(C)C
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
5ce41b3db1ff79b8dd0325761a92ce74d9b898070d3b61ae6f52ef2fb0fe31ed
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N1CCCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]1-[C:7]-[C:8]-[C:9]-[NH;D2;+0:10]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[N;H0;D3;+0:10]1-[C:6]-[C:7]-[C:8]-[C:9]-1)-[c:3](:[c:4]):[c:5]
97
[{"value": 97.0, "product": "C(C)(C)(C)OC(=O)N[C@@H]1CN(C[C@H]1C)C(C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In the presence of triethylamine, 59 g of benzoyl chloride was reacted at room temperature with 81.4 g of trans-3-tert-butoxycarbonylamino-4-methylpyrrolidine in methylene chloride, whereby 120 g of trans-3-tert-butoxycarbonylamino-4-methyl-1-benzoylpyrrolidine (a) was obtained. Hydrochloric acid was then reacted at ro...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
C1CCNC1
C1CC[NH]C1
C1CC[NH]C1.c1ccccc1
HCl
C(Cl)Cl
null
null
C[C@@H]1CNC[C@H]1NC(=O)OC(C)(C)C.O=C(Cl)c1ccccc1>C(Cl)Cl>C[C@@H]1CN(C(=O)c2ccccc2)C[C@H]1NC(=O)OC(C)(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2a852a07ea464fa89bf55a6c10dc6d5c
O=C(OCc1ccccc1)c1c(F)cc(F)c(F)c1F.OCc1ccccc1>>O=C(O)c1c(OCc2ccccc2)cc(F)c(F)c1F
C(C1=CC=CC=C1)O.FC1=C(C(=O)OCC2=CC=CC=C2)C(=CC(=C1F)F)F.O.[H-].[Na+]>>C(C1=CC=CC=C1)OC1=CC(=C(C(=C1C(=O)O)F)F)F
F[c:5]1[c:4]([C:2](=[O:1])[O:3]Cc2ccccc2)[c:19]([F:20])[c:17]([F:18])[c:15]([F:16])[cH:14]1.[OH:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[O:1]=[C:2]([OH:3])[c:4]1[c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][c:15]([F:16])[c:17]([F:18])[c:19]1[F:20]
O=C(OCc1ccccc1)c1c(F)cc(F)c(F)c1F.OCc1ccccc1
O=C(O)c1c(OCc2ccccc2)cc(F)c(F)c1F
null
null
C(C)(=O)O.CCCCCC.C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
9d48094a081436f4e8572ec04094de4d166599c746a684c9c817617474d08f02
8a16c79d9023d6e1eac34a7a6cb858d135b938d7ebe110172115bd21e9860078
c1ccc(COc2ccccc2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-C-c1:c:c:c:c:c:1):[c:8].[OH;D1;+0:9]-[C:10]-[c:11]>>[O;D1;H0:6]=[C:5](-[OH;D1;+0:7])-[c:4](:[c:8]):[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[C:10]-[c:11]):[c:2]:[c:3]
31.6
[{"value": 31.6, "product": "C(C1=CC=CC=C1)OC1=CC(=C(C(=C1C(=O)O)F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
6.5 g of benzyl alcohol was dissolved in 150 ml of benzene. While the resultant solution was cooled with water, 2.4 g of sodium hydride (60%) was added and reacted. To the reaction mixture was added 15 g of benzyl 2,3,4,6-tetrafluorobenzoate, and stirred at room temperature for 1 hour. 3.6 g of acetic acid was added, f...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Primary alcohol
Carboxylic acid.Ether
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HF
C(C)(=O)O.CCCCCC.C1=CC=CC=C1
null
1
O=C(OCc1ccccc1)c1c(F)cc(F)c(F)c1F.OCc1ccccc1>C(C)(=O)O.CCCCCC.C1=CC=CC=C1>O=C(O)c1c(OCc2ccccc2)cc(F)c(F)c1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-39ba3d3ec92e459f80ce36b757f83647
COC(=O)c1c(F)cc(F)c(F)c1F>>COC(=O)c1c(N)cc(F)c(F)c1F
FC1=C(C(=O)OC)C(=CC(=C1F)F)F.C(C1=CC=CC=C1)N>>NC1=CC(=C(C(=C1C(=O)OC)F)F)F
F[c:6]1[c:5]([C:3]([O:2][CH3:1])=[O:4])[c:13]([F:14])[c:11]([F:12])[c:9]([F:10])[cH:8]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([NH2:7])[cH:8][c:9]([F:10])[c:11]([F:12])[c:13]1[F:14]
COC(=O)c1c(F)cc(F)c(F)c1F
COC(=O)c1c(N)cc(F)c(F)c1F
null
null
C1=CC=CC=C1
Functional Group Interconversion
OtherReaction
0b3f36c6e96a844ac8c671a85ab317446ee29bfa735a32d39184f4616cac3a55
560c85d40afb1a57d77cf3258abf3be5bba829f35224f8687bf9a1d4c1f94bd9
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C:5](=[O;D1;H0:6])-[#8:7]-[C;D1;H3:8]):[c:9]>>[C;D1;H3:8]-[#8:7]-[C:5](=[O;D1;H0:6])-[c:4](:[c:9]):[c;H0;D3;+0:1](-[N;D1;H2:10]):[c:2]:[c:3]
null
[]
null
null
1.5
HOUR
60 g of methyl 2,3,4,6-tetrafluorobenzoate and 70 g of benzylamine were reacted under reflux for 1 hour in 400 ml of benzene. After the reaction mixture was allowed to cool down, it was washed successively with water, 1% hydrochloric acid and 1% aq. sodium carbonate, each in the amount of 600 ml. The reaction mixture w...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Primary amine
c1ccccc1
c1ccccc1
c1ccccc1
null
C1=CC=CC=C1
null
1.5
COC(=O)c1c(F)cc(F)c(F)c1F>C1=CC=CC=C1>COC(=O)c1c(N)cc(F)c(F)c1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bba1b398f5164b93b56a82edcd1f84ce
O=c1ccoc2ccc(OCCCNCC3COc4cc5c(cc4O3)OCO5)cc12>>c1cc2c(cc1OCCCNCC1COc3cc4c(cc3O1)OCO4)CCCO2
Cl.O1COC2=CC3=C(OCC(O3)CNCCCOC=3C=C4C(C=COC4=CC3)=O)C=C21.Cl.CC(C)O>>O1CCCC2=CC(=CC=C12)OCCCNCC1OC2=C(OC1)C=C1C(=C2)OCO1
O=[c:26]1[c:4]2[c:3]([cH:2][cH:1][c:6]([O:7][CH2:8][CH2:9][CH2:10][NH:11][CH2:12][CH:13]3[CH2:14][O:15][c:16]4[cH:17][c:18]5[c:19]([cH:20][c:21]4[O:22]3)[O:23][CH2:24][O:25]5)[cH:5]2)[o:29][cH:28][cH:27]1>>[cH:1]1[cH:2][c:3]2[c:4]([cH:5][c:6]1[O:7][CH2:8][CH2:9][CH2:10][NH:11][CH2:12][CH:13]1[CH2:14][O:15][c:16]3[cH:17...
O=c1ccoc2ccc(OCCCNCC3COc4cc5c(cc4O3)OCO5)cc12
c1cc2c(cc1OCCCNCC1COc3cc4c(cc3O1)OCO4)CCCO2
null
[Pd]
CO
Reduction
OtherReaction
6dad345603399266046e008fba48d21c660e0fe0e51569b1d41eae3180aa60d3
7ece147c6909fe307632f67c21e1517a1747c8ff389dff4b19e644c711d1d84d
c1cc2c(cc1OCCCNCC1COc3cc4c(cc3O1)OCO4)CCCO2
O=[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[o;H0;D2;+0:4]:[c:5](:[c:6]):[c:7]:1:[c:8]>>[c:6]:[c:5]1:[c:7](:[c:8])-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[O;H0;D2;+0:4]-1
56.3
[{"value": 56.3, "product": "O1CCCC2=CC(=CC=C12)OCCCNCC1OC2=C(OC1)C=C1C(=C2)OCO1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
6-[3-[[(6,7-Dihydro-1,3-dioxolo[4,5-g][1,4]benzodioxin-6-yl)methyl]amino]propoxy]chromen-4-one hydrochloride (0.9 g, 2.0 mmole), prepared in Example 5 above, was dissolved in 50 ml of methanol and 4N HCl/IPA (12.5 ml, 50 mmole) and 10% Palladium on Carbon (0.2 g) were added. The mixture was hydrogenated on a Parr appar...
10.6084/m9.figshare.5104873.v1
null
null
Ether
c1ccc2occcc2c1
c1ccc2c(c1)CCCO2
c1c2c(cc3c1OCO3)OCCO2.c1ccc2c(c1)CCCO2
Other
[Pd].CO
null
24
O=c1ccoc2ccc(OCCCNCC3COc4cc5c(cc4O3)OCO5)cc12>[Pd].CO>c1cc2c(cc1OCCCNCC1COc3cc4c(cc3O1)OCO4)CCCO2
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5865d24af6cd479aaec4ce67db420a22
COc1ccc2c(c1)OC(CN)CO2.O=c1ccoc2cc(OCCCBr)ccc12>>COc1ccc2c(c1)OC(CNCCCOc1ccc3c(=O)ccoc3c1)CO2
Cl.COC=1C=CC2=C(OC(CO2)CN)C1.BrCCCOC1=CC=C2C(C=COC2=C1)=O.C(C)(C)N(CC)C(C)C>>COC=1C=CC2=C(OC(CO2)CNCCCOC2=CC=C3C(C=COC3=C2)=O)C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[O:9][CH:10]([CH2:11][NH2:12])[CH2:28][O:29]2.Br[CH2:13][CH2:14][CH2:15][O:16][c:17]1[cH:18][cH:19][c:20]2[c:21](=[O:22])[cH:23][cH:24][o:25][c:26]2[cH:27]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[O:9][CH:10]([CH2:11][NH:12][CH2:13][CH2:14][CH2:15][O:16][c:1...
COc1ccc2c(c1)OC(CN)CO2.O=c1ccoc2cc(OCCCBr)ccc12
COc1ccc2c(c1)OC(CNCCCOc1ccc3c(=O)ccoc3c1)CO2
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
O=c1ccoc2cc(OCCCNCC3COc4ccccc4O3)ccc12
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]-[C:5]-[C:6]-[NH2;D1;+0:7]>>[#8:4]-[C:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[C:2]-[C:3]
4.4
[{"value": 4.4, "product": "COC=1C=CC2=C(OC(CO2)CNCCCOC2=CC=C3C(C=COC3=C2)=O)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
2,3-Dihydro-7-methoxy-1,4-benzodioxin-2-methanamine hydrochloride (4.0 g, 17 mmole), 7-(3-bromopropoxy)chromen-4-one (4.9 g, 17 mmole) and diisopropylethylamine (15.1 ml, 87 mmole) were combined in 150 ml of DMF and heated at 80° C. for 24 hours under a nitrogen atmosphere. The solvent was then removed and replaced wit...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2c(c1)OCCO2.c1ccc2cccoc2c1
HBr
CN(C)C=O
80
null
COc1ccc2c(c1)OC(CN)CO2.O=c1ccoc2cc(OCCCBr)ccc12>CN(C)C=O>COc1ccc2c(c1)OC(CNCCCOc1ccc3c(=O)ccoc3c1)CO2
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b5f1118b8c30426bbd0a88c29f75d946
NCC1COc2ccc(O)cc2O1.O=c1ccoc2cc(OCCCBr)ccc12>>O=c1ccoc2cc(OCCCNCC3COc4ccc(O)cc4O3)ccc12
Cl.OC=1C=CC2=C(OC(CO2)CN)C1.BrCCCOC1=CC=C2C(C=COC2=C1)=O.C(C)(C)N(CC)C(C)C>>OC=1C=CC2=C(OC(CO2)CNCCCOC2=CC=C3C(C=COC3=C2)=O)C1
[NH2:13][CH2:14][CH:15]1[CH2:16][O:17][c:18]2[cH:19][cH:20][c:21]([OH:22])[cH:23][c:24]2[O:25]1.Br[CH2:12][CH2:11][CH2:10][O:9][c:8]1[cH:7][c:6]2[o:5][cH:4][cH:3][c:2](=[O:1])[c:28]2[cH:27][cH:26]1>>[O:1]=[c:2]1[cH:3][cH:4][o:5][c:6]2[cH:7][c:8]([O:9][CH2:10][CH2:11][CH2:12][NH:13][CH2:14][CH:15]3[CH2:16][O:17][c:18]4[...
NCC1COc2ccc(O)cc2O1.O=c1ccoc2cc(OCCCBr)ccc12
O=c1ccoc2cc(OCCCNCC3COc4ccc(O)cc4O3)ccc12
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
O=c1ccoc2cc(OCCCNCC3COc4ccccc4O3)ccc12
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]-[C:5]-[C:6]-[NH2;D1;+0:7]>>[#8:4]-[C:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[C:2]-[C:3]
10.1
[{"value": 10.1, "product": "OC=1C=CC2=C(OC(CO2)CNCCCOC2=CC=C3C(C=COC3=C2)=O)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
2,3-Dihydro-7-hydroxy-1,4-benzodioxin-2-methanamine hydrochloride (4.7 g, 22 mmole), 7-(3-bromopropoxy)chromen-4-one (6.1 g, 22 mmole) and diisopropylethylamine (18.8 ml, 108 mmole) were combined in 200 ml of DMF and heated at 80° C. for 24 hours under a nitrogen atmosphere. The solvent was then removed and replaced wi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2cccoc2c1.c1ccc2c(c1)OCCO2
HBr
CN(C)C=O
80
null
NCC1COc2ccc(O)cc2O1.O=c1ccoc2cc(OCCCBr)ccc12>CN(C)C=O>O=c1ccoc2cc(OCCCNCC3COc4ccc(O)cc4O3)ccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f3e031aa403047fbaeb5992f3638bfd2
COc1ccc(CC(C)=O)cc1OC.NCC(O)c1cccc(Cl)c1>>COc1ccc(CC(C)NCC(O)c2cccc(Cl)c2)cc1OC
ClC=1C=C(C=CC1)C(CN)O.COC=1C=C(C=CC1OC)CC(C)=O.C(#N)[BH3-].[Na+]>>ClC=1C=C(C=CC1)C(O)CNC(CC1=CC(=C(C=C1)OC)OC)C
O=[C:8]([CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:22]([O:23][CH3:24])[cH:21]1)[CH3:9].[NH2:10][CH2:11][CH:12]([OH:13])[c:14]1[cH:15][cH:16][cH:17][c:18]([Cl:19])[cH:20]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH:8]([CH3:9])[NH:10][CH2:11][CH:12]([OH:13])[c:14]2[cH:15][cH:16][cH:17][c:18]([Cl:19])[cH:20]2)[cH...
COc1ccc(CC(C)=O)cc1OC.NCC(O)c1cccc(Cl)c1
COc1ccc(CC(C)NCC(O)c2cccc(Cl)c2)cc1OC
null
null
CO
Heteroatom Alkylation and Arylation
Reductive amination with ketone
4940e8ed9a0db9bde699fdcdc3aff2cff0409c19478aa0ed1acfd98213338adf
07faf85ffe990e88a1de7fd04a339bf226f78d8bfae9712ea59eebd76bb54b9f
c1ccc(CCNCCc2ccccc2)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[c:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3]-[c:4]
null
[]
null
null
null
null
In accordance with the above preferred reaction scheme 2-(3-chlorophenyl)-2-hydroxyethylamine 1, and 3,4-dimethoxyphenylacetone 2 are reacted with sodium cyanoborohydride in methanol, giving 3-chloroalpha-(((2-(3,4-dimethoxyphenyl)-1-methylethyl)amino)methyl) benzenemethanol 3 which is reacted with carbonyl diimidazole...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccccc1
Other
CO
null
null
COc1ccc(CC(C)=O)cc1OC.NCC(O)c1cccc(Cl)c1>CO>COc1ccc(CC(C)NCC(O)c2cccc(Cl)c2)cc1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-da519b35e805446ebee7f87ca244eb1f
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O>>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@@H](c4cccc(Cl)c4)OC3=O)cc2O1
ClC=1C=C(C=CC1)[C@@H]1CN(C(O1)=O)[C@@H](CC1=CC(=C(C=C1)O)O)C.BrC(C(=O)OCC)(C(=O)OCC)Br.C([O-])([O-])=O.[K+].[K+]>>ClC=1C=C(C=CC1)[C@@H]1CN(C(O1)=O)[C@@H](CC1=CC2=C(OC(O2)(C(=O)OCC)C(=O)OCC)C=C1)C
Br[C:6](Br)([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:7](=[O:8])[O:9][CH2:10][CH3:11].[OH:12][c:13]1[cH:14][cH:15][c:16]([CH2:17][C@@H:18]([CH3:19])[N:20]2[CH2:21][C@@H:22]([c:23]3[cH:24][cH:25][cH:26][c:27]([Cl:28])[cH:29]3)[O:30][C:31]2=[O:32])[cH:33][c:34]1[OH:35]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9]...
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@@H](c4cccc(Cl)c4)OC3=O)cc2O1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
af92e8ae1f27b7a1e6f478492a6f48fd98b71b8d2ef436c713fd3da904924b6f
661a42d0ac7fd9eb76e924a46e5fae3d564c0d30f9b9482dcc715291d9bc27ca
O=C1O[C@H](c2ccccc2)CN1CCc1ccc2c(c1)OCO2
Br-[C;H0;D4;+0:1](-Br)(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[OH;D1;+0:10]-[c:11](:[c:12]):[c:13](-[OH;D1;+0:14]):[c:15]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C;H0;D4;+0:1]1(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[O;H0;D2;+0:10]-[c:11](:[c:12]):[c:13](:[c:15])-[O;H0;D2;+0:14]-1
null
[]
null
null
null
null
In accordance with the above preferred reaction scheme 2-(3-chlorophenyl)-2-hydroxyethylamine 1, and 3,4-dimethoxyphenylacetone 2 are reacted with sodium cyanoborohydride in methanol, giving 3-chloroalpha-(((2-(3,4-dimethoxyphenyl)-1-methylethyl)amino)methyl) benzenemethanol 3 which is reacted with carbonyl diimidazole...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Ester.Ester.Aromatic alcohol.Aromatic alcohol
Ester.Ester.Ether.Ether
null
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2.C1COC[NH]1.c1ccccc1
HBr
CC(=O)C
null
null
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O>CC(=O)C>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@@H](c4cccc(Cl)c4)OC3=O)cc2O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cda2df2be4d44857bdab7b18d45916bd
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O>>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@@H](c4cccc(Cl)c4)OC3=O)cc2O1
ClC=1C=C(C=CC1)[C@@H]1CN(C(O1)=O)[C@@H](CC1=CC(=C(C=C1)O)O)C.BrC(C(=O)OCC)(C(=O)OCC)Br.C([O-])([O-])=O.[K+].[K+]>>ClC=1C=C(C=CC1)[C@@H]1CN(C(O1)=O)[C@@H](CC1=CC2=C(OC(O2)(C(=O)OCC)C(=O)OCC)C=C1)C
Br[C:6](Br)([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:7](=[O:8])[O:9][CH2:10][CH3:11].[OH:12][c:13]1[cH:14][cH:15][c:16]([CH2:17][C@@H:18]([CH3:19])[N:20]2[CH2:21][C@@H:22]([c:23]3[cH:24][cH:25][cH:26][c:27]([Cl:28])[cH:29]3)[O:30][C:31]2=[O:32])[cH:33][c:34]1[OH:35]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9]...
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@@H](c4cccc(Cl)c4)OC3=O)cc2O1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
af92e8ae1f27b7a1e6f478492a6f48fd98b71b8d2ef436c713fd3da904924b6f
661a42d0ac7fd9eb76e924a46e5fae3d564c0d30f9b9482dcc715291d9bc27ca
O=C1O[C@H](c2ccccc2)CN1CCc1ccc2c(c1)OCO2
Br-[C;H0;D4;+0:1](-Br)(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[OH;D1;+0:10]-[c:11](:[c:12]):[c:13](-[OH;D1;+0:14]):[c:15]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C;H0;D4;+0:1]1(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[O;H0;D2;+0:10]-[c:11](:[c:12]):[c:13](:[c:15])-[O;H0;D2;+0:14]-1
null
[]
null
null
null
null
More specifically, the chiral synthesis may be carried out by performing the synthetic reaction sequence outlined in Scheme III. L-DOPA 19 is treated with di-t-butyl-dicarbonate in dimethylformamide, giving (S)-N-(1-(1,1-dimethylethoxy)carbonyl)-3-hydroxy-L-tyrosine 20 which is reacted with methyl iodide and anhydrous ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Ester.Ester.Aromatic alcohol.Aromatic alcohol
Ester.Ester.Ether.Ether
null
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2.C1COC[NH]1.c1ccccc1
HBr
CC(=O)C
null
null
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O>CC(=O)C>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@@H](c4cccc(Cl)c4)OC3=O)cc2O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-463370cd2f4149d4a74c16289bb0ce5f
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O>>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@H](c4cccc(Cl)c4)OC3=O)cc2O1
ClC=1C=C(C=CC1)[C@@H]1CN(C(O1)=O)[C@H](CC1=CC(=C(C=C1)O)O)C.BrC(C(=O)OCC)(C(=O)OCC)Br.C([O-])([O-])=O.[K+].[K+]>>ClC=1C=C(C=CC1)[C@H]1CN(C(O1)=O)[C@@H](CC1=CC2=C(OC(O2)(C(=O)OCC)C(=O)OCC)C=C1)C
Br[C:6](Br)([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:7](=[O:8])[O:9][CH2:10][CH3:11].[OH:12][c:13]1[cH:14][cH:15][c:16]([CH2:17][C@H:18]([CH3:19])[N:20]2[CH2:21][C@@H:22]([c:23]3[cH:24][cH:25][cH:26][c:27]([Cl:28])[cH:29]3)[O:30][C:31]2=[O:32])[cH:33][c:34]1[OH:35]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9][...
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O
CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@H](c4cccc(Cl)c4)OC3=O)cc2O1
null
BrC(C(=O)OCC)(C(=O)OCC)Br
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
af92e8ae1f27b7a1e6f478492a6f48fd98b71b8d2ef436c713fd3da904924b6f
661a42d0ac7fd9eb76e924a46e5fae3d564c0d30f9b9482dcc715291d9bc27ca
O=C1O[C@@H](c2ccccc2)CN1CCc1ccc2c(c1)OCO2
Br-[C;H0;D4;+0:1](-Br)(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[OH;D1;+0:10]-[c:11](:[c:12]):[c:13](-[OH;D1;+0:14]):[c:15]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C;H0;D4;+0:1]1(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[O;H0;D2;+0:10]-[c:11](:[c:12]):[c:13](:[c:15])-[O;H0;D2;+0:14]-1
66.1
[{"value": 66.1, "product": "ClC=1C=C(C=CC1)[C@H]1CN(C(O1)=O)[C@@H](CC1=CC2=C(OC(O2)(C(=O)OCC)C(=O)OCC)C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 0.8 g of the above oxazolidinone, 0.74 g of diethyl dibromomalonate, 1.2 g of anhydrous potassium carbonate and 20 ml of acetone are stirred overnight with the addition of a few drops of diethyl dibromomalonate. The mixture is filtered, washed with acetone and the combined filtrate and wash are evaporated ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Ester.Ester.Aromatic alcohol.Aromatic alcohol
Ester.Ester.Ether.Ether
null
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2.C1COC[NH]1.c1ccccc1
HBr
BrC(C(=O)OCC)(C(=O)OCC)Br.CC(=O)C
null
null
CCOC(=O)C(Br)(Br)C(=O)OCC.C[C@@H](Cc1ccc(O)c(O)c1)N1C[C@@H](c2cccc(Cl)c2)OC1=O>BrC(C(=O)OCC)(C(=O)OCC)Br.CC(=O)C>CCOC(=O)C1(C(=O)OCC)Oc2ccc(C[C@@H](C)N3C[C@H](c4cccc(Cl)c4)OC3=O)cc2O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1c87a99897674504b9f67b900895e476
CC(C)=O.CCOC(=O)C(Br)C(=O)OCC.O=C1NCCO1>>CCOC(=O)C1(C(=O)OCC)Oc2ccccc2O1
O1C(NCC1)=O.BrC(C(=O)OCC)C(=O)OCC.C([O-])([O-])=O.[K+].[K+].CC(=O)C>>O1C(OC2=C1C=CC=C2)(C(=O)OCC)C(=O)OCC
C[C:15](=O)[CH3:14].Br[CH:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:7](=[O:8])[O:9][CH2:10][CH3:11].O=[C:18]1N[CH2:16][CH2:17][O:19]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9][CH2:10][CH3:11])[O:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[O:19]1
CC(C)=O.CCOC(=O)C(Br)C(=O)OCC.O=C1NCCO1
CCOC(=O)C1(C(=O)OCC)Oc2ccccc2O1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
94f07ca4b4604defe8f86efd1606f9449728efb37eea2bf833eda402a018515e
f0554a01e82e0f6e83f6b3f985aeef0a580a4d2833afa046490bc3fac37e3e64
c1ccc2c(c1)OCO2
Br-[CH;D3;+0:1](-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].C-[C;H0;D3;+0:10](=O)-[CH3;D1;+0:11].O=[C;H0;D3;+0:12]1-N-[CH2;D2;+0:13]-[CH2;D2;+0:14]-[O;H0;D2;+0:15]-1>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C;H0;D4;+0:1]1(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[#8:16]-[c:17]2:[cH;D2;+0:11]:[cH;D2;+0:10]:[...
null
[]
null
null
8
HOUR
A mixture of 240 mg of the above oxazolidinone, 234 mg of diethyl bromomalonate, 450 mg of anhydrous potassium carbonate and 10 ml of acetone is stirred overnight, filtered, washed with acetone and evaporated to a brown oil. The oil is purified by flash chromatography, eluting with 5 percent acetone in toluene. The pur...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carbamic ester.Ketone.Ester.Ester.Ether
Ester.Ester.Ether.Ether
C1COCN1
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
HBr
null
null
8
CC(C)=O.CCOC(=O)C(Br)C(=O)OCC.O=C1NCCO1>>CCOC(=O)C1(C(=O)OCC)Oc2ccccc2O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e5cdc5322a3f49ad962f9c48c672d656
CN(C)C1CCCNc2ccccc21.O=C(Cl)c1ccc([N+](=O)[O-])cc1>>CN(C)C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
CN(C1CCCNC2=C1C=CC=C2)C.C([O-])([O-])=O.[K+].[K+].[N+](=O)([O-])C1=CC=C(C(=O)Cl)C=C1>>CN(C1CCCN(C2=C1C=CC=C2)C(C2=CC=C(C=C2)[N+](=O)[O-])=O)C
[CH3:1][N:2]([CH3:3])[CH:4]1[CH2:5][CH2:6][CH2:7][NH:8][c:20]2[cH:21][cH:22][cH:23][cH:24][c:25]21.Cl[C:9](=[O:10])[c:11]1[cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][cH:19]1>>[CH3:1][N:2]([CH3:3])[CH:4]1[CH2:5][CH2:6][CH2:7][N:8]([C:9](=[O:10])[c:11]2[cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][cH:19]2...
CN(C)C1CCCNc2ccccc21.O=C(Cl)c1ccc([N+](=O)[O-])cc1
CN(C)C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
null
null
O.CC(=O)C
Acylation
N-alkylation of secondary amines with alkyl halides
64413dd180580e9c8f2736c3a8c0c162d266e6033cf64f74e0aa763b2659218c
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N1CCCCc2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[C:7]-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5])-[c:9](:[c:10]):[c:11]
97.1
[{"value": 97.1, "product": "CN(C1CCCN(C2=C1C=CC=C2)C(C2=CC=C(C=C2)[N+](=O)[O-])=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 5-dimethylamino-2,3,4,5-tetrahydro-1H-benzazepine (50 g) in a mixture of acetone (400 ml) and water (200 ml) is added potassium carbonate (38.8 g), and thereto is added p-nitrobenzoyl chloride (40 g) with stirring under ice-cooling, and the mixture is stirred at room temperature overnight. To the react...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
c1ccc2c(c1)CCCCN2
c1ccc2c(c1)CCCC[NH]2
c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HCl
O.CC(=O)C
null
null
CN(C)C1CCCNc2ccccc21.O=C(Cl)c1ccc([N+](=O)[O-])cc1>O.CC(=O)C>CN(C)C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5863f8a43c894049b8ad42ad0415ff02
CN(C)C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21>>CN(C)C1CCCN(C(=O)c2ccc(N)cc2)c2ccccc21
CN(C1CCCN(C2=C1C=CC=C2)C(C2=CC=C(C=C2)[N+](=O)[O-])=O)C>>CN(C1CCCN(C2=C1C=CC=C2)C(C2=CC=C(C=C2)N)=O)C
O=[N+:15]([O-])[c:14]1[cH:13][cH:12][c:11]([C:9]([N:8]2[CH2:7][CH2:6][CH2:5][CH:4]([N:2]([CH3:1])[CH3:3])[c:23]3[c:18]2[cH:19][cH:20][cH:21][cH:22]3)=[O:10])[cH:17][cH:16]1>>[CH3:1][N:2]([CH3:3])[CH:4]1[CH2:5][CH2:6][CH2:7][N:8]([C:9](=[O:10])[c:11]2[cH:12][cH:13][c:14]([NH2:15])[cH:16][cH:17]2)[c:18]2[cH:19][cH:20][cH...
CN(C)C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
CN(C)C1CCCN(C(=O)c2ccc(N)cc2)c2ccccc21
null
[Pd]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C(c1ccccc1)N1CCCCc2ccccc21
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
96
[{"value": 96.0, "product": "CN(C1CCCN(C2=C1C=CC=C2)C(C2=CC=C(C=C2)N)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In ethanol (500 ml) is dispersed 10% Pd-C (5 g), and thereto is added 5-dimethylamino-1-(4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-benzazepine (64.1 g), and the mixture is subjected to catalytic reduction at ordinary room temperature under atmospheric pressure. After reduction, 10% Pd-C is removed by filtration, and the fi...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccc2c(c1)CCCC[NH]2
Other
[Pd].C(C)O
null
null
CN(C)C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21>[Pd].C(C)O>CN(C)C1CCCN(C(=O)c2ccc(N)cc2)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c858891f9f9444f296084399c45e22a3
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(O)c2cc(Cl)ccc21.CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)O>>COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@H](CCSC)NC(=O)OC(C)(C)C)c2cc(Cl)ccc21
OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O.CN(C)C1=NC=CC=C1.Cl.CN(C)C1=NC=CC=C1.C(C)(C)(C)OC(=O)N[C@@H](CCSC)C(=O)O.C1(CCCCC1)N=C=NC1CCCCC1>>C(C)(C)(C)OC(=O)N[C@@H](CCSC)C(=O)OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O
[CH3:1][O:2][c:3]1[cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[CH3:15])[cH:16][cH:17][c:18]1[C:19](=[O:20])[N:21]1[CH2:22][CH2:23][CH2:24][CH:25]([OH:26])[c:42]2[cH:43][c:44]([Cl:45])[cH:46][cH:47][c:48]21.O[C:27](=[O:28])[C@H:29]([CH2:30][CH2:31][S:32][CH3:33])[NH:34][C:35](=[O:36])[O:37][C...
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(O)c2cc(Cl)ccc21.CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)O
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@H](CCSC)NC(=O)OC(C)(C)C)c2cc(Cl)ccc21
null
null
C(C)(=O)O.C(Cl)(Cl)Cl.CO
Acylation
Esterification of Carboxylic Acids
e916c5b009194e30c618975b40d7a233bfcf81339e65494c4e365f67cc5e011d
12ba7405a548c6b1674f05065819c74f53f1b6165cd54e84e1f2f208042fe660
O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[C:13]-[C:14](-[OH;D1;+0:15])-[c:16]>>[C:13]-[C:14](-[O;H0;D2;+0:15]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:1...
121.2
[{"value": 121.2, "product": "C(C)(C)(C)OC(=O)N[C@@H](CCSC)C(=O)OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
5-Hydroxy-7-chloro-1-[2-methoxy-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (0.7 g), dimethylaminopyridine (0.83 g) and dimethylaminopyridine hydrochloride (0.72 g) are dissolved in chloroform (15 ml), and thereto are added N-tert-butoxycarbonyl-L-methionine (0.56 g) and dicyclohexylcarbodiimide ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary alcohol
Ester
null
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
C(C)(=O)O.C(Cl)(Cl)Cl.CO
null
3
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(O)c2cc(Cl)ccc21.CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)O>C(C)(=O)O.C(Cl)(Cl)Cl.CO>COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@H](CCSC)NC(=O)OC(C)(C)C)c2cc(Cl)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3db121cfac504d159b1b06562cabf306
O=C(O)Cc1ccccc1Cl.O=S(Cl)Cl>>O=C(Cl)Cc1ccccc1Cl
ClC1=C(C=CC=C1)CC(=O)O.S(=O)(Cl)Cl>>ClC1=C(C=CC=C1)CC(=O)Cl
O[C:2](=[O:1])[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[Cl:11].O=S(Cl)[Cl:3]>>[O:1]=[C:2]([Cl:3])[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[Cl:11]
O=C(O)Cc1ccccc1Cl.O=S(Cl)Cl
O=C(Cl)Cc1ccccc1Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
c1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[c:5]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[c:5]
null
[]
null
null
2
HOUR
To 2-chlorophenylacetic acid (0.44 g) is added thionyl chloride (15 ml), and the mixture is stirred at room temperature for 2 hours. Thionyl chloride is distilled off, and the resultant is further distilled off by subjecting twice to azeotrophy with toluene. The resulting residue is dissolved in dichloromethane (10 ml)...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1
HCl
null
null
2
O=C(O)Cc1ccccc1Cl.O=S(Cl)Cl>>O=C(Cl)Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2aaa607f367b4114b06385b6e442d470
CCOC(=O)CP(=O)(OCC)OCC.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3cc(Cl)ccc32)c(C)c1>>CCOC(=O)C=C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21
[H-].[Na+].C(C)OP(=O)(OCC)CC(=O)OCC.O=C1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O>>C(C)OC(=O)C=C1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O
CCOP(=O)(OCC)[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].O=[C:7]1[CH2:8][CH2:9][CH2:10][N:11]([C:12](=[O:13])[c:14]2[cH:15][cH:16][c:17]([NH:18][C:19](=[O:20])[c:21]3[cH:22][cH:23][cH:24][cH:25][c:26]3[CH3:27])[cH:28][c:29]2[CH3:30])[c:31]2[cH:32][cH:33][c:34]([Cl:35])[cH:36][c:37]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]...
CCOC(=O)CP(=O)(OCC)OCC.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3cc(Cl)ccc32)c(C)c1
CCOC(=O)C=C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21
null
null
O1CCCC1
C-C Coupling
Wittig with Phosphonium
0f071c5d088734a3668468c108c63f4eebdb54435791854b689fbe85c99a4524
79a946b42eb7e7aee42e09efe41630192c1745e07085cd7f7f88cc7b599f9082
[CH]=C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3)cc2)c2ccccc21
C-C-O-P(=O)(-O-C-C)-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].O=[C;H0;D3;+0:6](-[C:7]-[C:8])-[c:9](:[c:10]):[c:11]-[#7:12]>>[#7:12]-[c:11]:[c:9](:[c:10])-[C;H0;D3;+0:6](=[CH;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:7]-[C:8]
null
[]
null
null
null
null
To tetrahydrofuran (200 ml) is added sodium hydride (60%, 0.85 g), and thereto is added dropwise ethyl diethylphosphonoacetate (4.68 ml) with stirring under ice-cooling, and the mixture is further stirred under ice-cooling for 10 minutes. To the reaction mixture is added 5-oxo-7-chloro-1-[2-methyl-4-(2-methylbenzoylami...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Ester
c1ccc2c(c1)CCCC[NH]2
c1ccc2c(c1)CCCC[NH]2
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
O1CCCC1
null
null
CCOC(=O)CP(=O)(OCC)OCC.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3cc(Cl)ccc32)c(C)c1>O1CCCC1>CCOC(=O)C=C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-be3698e1a0504a98b5ed49a7b8e68b9f
CCOC(=O)C=C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21>>CCOC(=O)CC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21
C(C)OC(=O)C=C1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O.[BH4-].[Na+]>>C(C)OC(=O)CC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]=[C:7]1[CH2:8][CH2:9][CH2:10][N:11]([C:12](=[O:13])[c:14]2[cH:15][cH:16][c:17]([NH:18][C:19](=[O:20])[c:21]3[cH:22][cH:23][cH:24][cH:25][c:26]3[CH3:27])[cH:28][c:29]2[CH3:30])[c:31]2[cH:32][cH:33][c:34]([Cl:35])[cH:36][c:37]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH:7]1[CH2:8][...
CCOC(=O)C=C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21
CCOC(=O)CC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21
null
O.O.O.O.O.O.[Ni](Cl)Cl
O1CCCC1.CO
Reduction
Hydrogenation (double to single)
65c294937a18f0bcd8c57100fa93b4fc8c207c3d98829714ec7712a3b8bd7de0
9a50abf8d2e4cd9195d7a0cadbe97483a261a81cf70b653cfddd5ecf76d383a6
O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1
[#7:1]-[c:2]:[c:3](:[c:4])-[C;H0;D3;+0:5](=[CH;D2;+0:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10])-[C:11]-[C:12]>>[#7:1]-[c:2]:[c:3](:[c:4])-[CH;D3;+0:5](-[CH2;D2;+0:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10])-[C:11]-[C:12]
43.2
[{"value": 43.2, "product": "C(C)OC(=O)CC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
5-Ethoxycarbonylmethylidene-7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (0.30 g) and nickel chloride hexahydrate (0.55 g) are dissolved in a mixture of tetrahydrofuran/methanol (1:1) (30 ml), and to the mixture is added slowly sodium borohydride (0.26 g) with stirring under i...
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
c1ccc2c(c1)CCCC[NH]2
c1ccc2c(c1)CCCC[NH]2
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
null
O.O.O.O.O.O.[Ni](Cl)Cl.O1CCCC1.CO
null
null
CCOC(=O)C=C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21>O.O.O.O.O.O.[Ni](Cl)Cl.O1CCCC1.CO>CCOC(=O)CC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dc7d68fa76f84aebbe68d0076ffab1c1
CC(C)[C@H](NC(=O)OCc1ccccc1)C(=O)O.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cc(Cl)ccc32)c(C)c1>>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(OC(=O)[C@@H](N)C(C)C)c3cc(Cl)ccc32)c(C)c1
OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O.CN(C)C1=NC=CC=C1.Cl.CN(C)C1=NC=CC=C1.C(C1=CC=CC=C1)OC(=O)N[C@@H](C(C)C)C(=O)O.C1(CCCCC1)N=C=NC1CCCCC1>>N[C@@H](C(C)C)C(=O)OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O
O=C(OCc1ccccc1)[NH:26][C@H:25]([C:23](O)=[O:24])[CH:27]([CH3:28])[CH3:29].[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[C:8](=[O:9])[NH:10][c:11]1[cH:12][cH:13][c:14]([C:15](=[O:16])[N:17]2[CH2:18][CH2:19][CH2:20][CH:21]([OH:22])[c:30]3[cH:31][c:32]([Cl:33])[cH:34][cH:35][c:36]32)[c:37]([CH3:38])[cH:39]1>>[CH3:1][c:2]1[c...
CC(C)[C@H](NC(=O)OCc1ccccc1)C(=O)O.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cc(Cl)ccc32)c(C)c1
Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(OC(=O)[C@@H](N)C(C)C)c3cc(Cl)ccc32)c(C)c1
null
[Pd]
C(C)(=O)O.C(Cl)(Cl)Cl.CO.C(C)(=O)OCC
Acylation
OtherReaction
2c76e343c45b7ee92c0bde24be04b20d4f03c30e0e1a1475114364c1d9034734
d049f62045e9c4fca1379cc1d9834b97ce2bdeaad5d7209d97ba9cb0d8edbebd
O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[NH;D2;+0:5]-C(=O)-O-C-c1:c:c:c:c:c:1.[C:6]-[C:7](-[OH;D1;+0:8])-[c:9]>>[C:6]-[C:7](-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[NH2;D1;+0:5])-[c:9]
38.5
[{"value": 38.5, "product": "N[C@@H](C(C)C)C(=O)OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
To a solution of 5-hydroxy-7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (1.0 g), dimethylaminopyridine (1.26 g) and dimethylaminopyridine hydrochloride (1.10 g) in chloroform (20 ml) are added N-benzyloxycarbonyl-L-valine (672 mg) and dicyclohexylcarbodiimide (1.42 g), and the...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid.Ether.Secondary alcohol
Ester.Primary amine
c1ccccc1
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
[Pd].C(C)(=O)O.C(Cl)(Cl)Cl.CO.C(C)(=O)OCC
null
7
CC(C)[C@H](NC(=O)OCc1ccccc1)C(=O)O.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cc(Cl)ccc32)c(C)c1>[Pd].C(C)(=O)O.C(Cl)(Cl)Cl.CO.C(C)(=O)OCC>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(OC(=O)[C@@H](N)C(C)C)c3cc(Cl)ccc32)c(C)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8b0e6b9d18174370a977ef82358fad31
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@H](CCSC)NC(=O)OC(C)(C)C)c2cc(Cl)ccc21>>COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@@H](N)CCSC)c2cc(Cl)ccc21
C(C)(C)(C)OC(=O)N[C@@H](CCSC)C(=O)OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O.FC(C(=O)O)(F)F.C1(=CC=CC=C1)OC>>N[C@@H](CCSC)C(=O)OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O
CC(C)(C)OC(=O)[NH:30][C@H:29]([C:27]([O:26][CH:25]1[CH2:24][CH2:23][CH2:22][N:21]([C:19]([c:18]2[c:3]([O:2][CH3:1])[cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[CH3:15])[cH:16][cH:17]2)=[O:20])[c:41]2[c:35]1[cH:36][c:37]([Cl:38])[cH:39][cH:40]2)=[O:28])[CH2:31][CH2:32][S:33][CH3:34]>>[CH3:1][...
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@H](CCSC)NC(=O)OC(C)(C)C)c2cc(Cl)ccc21
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@@H](N)CCSC)c2cc(Cl)ccc21
null
null
null
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7]>>[C:7]-[#8:6]-[C:4](=[O;D1;H0:5])-[C:2](-[C:3])-[NH2;D1;+0:1]
32.2
[{"value": 32.2, "product": "N[C@@H](CCSC)C(=O)OC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A uniform solution of 5-(N-tert-butoxycarbonyl-L-methionyloxy)-7-chloro-1-[2-methoxy-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (1.27 g), trifluoroacetic acid (2.5 ml) and anisole (0.6 ml) is stirred at room temperature for 2 hours. The trifluoroacetic acid is almost distilled off under reduced ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
null
null
null
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@H](CCSC)NC(=O)OC(C)(C)C)c2cc(Cl)ccc21>>COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OC(=O)[C@@H](N)CCSC)c2cc(Cl)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-95de830301e84a0d9f33eedda961e5bd
CN(C)CC(=O)O.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(CO)c3cc(Cl)ccc32)cc1>>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(COC(=O)CN(C)C)c3cc(Cl)ccc32)cc1
C1(CCCCC1)N=C=NC1CCCCC1.CN(C)C1=NC=CC=C1.Cl.CN(C)C1=NC=CC=C1.OCC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=CC=C(C=C2)NC(C2=C(C=CC=C2)C)=O)=O.C(O)([O-])=O.[Na+].Cl.CN(CC(=O)O)C>>Cl.CN(CC(=O)OCC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=CC=C(C=C2)NC(C2=C(C=CC=C2)C)=O)=O)C
O[C:24](=[O:25])[CH2:26][N:27]([CH3:28])[CH3:29].[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[C:8](=[O:9])[NH:10][c:11]1[cH:12][cH:13][c:14]([C:15](=[O:16])[N:17]2[CH2:18][CH2:19][CH2:20][CH:21]([CH2:22][OH:23])[c:30]3[cH:31][c:32]([Cl:33])[cH:34][cH:35][c:36]32)[cH:37][cH:38]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7...
CN(C)CC(=O)O.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(CO)c3cc(Cl)ccc32)cc1
Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(COC(=O)CN(C)C)c3cc(Cl)ccc32)cc1
null
null
C(C)(=O)O.C(Cl)(Cl)Cl.CO
Acylation
Esterification of Carboxylic Acids
d9bd78214ee7dbc907e499722ae01849a72d188753963443e5df9fe42c31c43b
3652e761944e8ef7ee40675a156c8ae39909c72166786934d88652debf2ec1ac
O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[#7:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C:6]-[C:5]
141.6
[{"value": 141.6, "product": "Cl.CN(CC(=O)OCC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=CC=C(C=C2)NC(C2=C(C=CC=C2)C)=O)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In a solution of 5-hydroxymethyl-7-chloro-1-[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (0.4 g) in chloroform (10 ml) are dissolved with heating dimethylaminopyridine (0.41 g) and dimethylaminopyridine hydrochloride (0.35 g), and thereto is added N,N-dimethylglycine hydrochloride (0.15 g) at roo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
C(C)(=O)O.C(Cl)(Cl)Cl.CO
null
null
CN(C)CC(=O)O.Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(CO)c3cc(Cl)ccc32)cc1>C(C)(=O)O.C(Cl)(Cl)Cl.CO>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(COC(=O)CN(C)C)c3cc(Cl)ccc32)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-afa3792d8ff0460690d319722a9ee47e
CCOC(=O)COC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccc(Cl)cc21>>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(OCCO)c3cc(Cl)ccc32)cc1
Cl.C(C)OC(=O)COC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=CC=C(C=C2)NC(C2=C(C=CC=C2)C)=O)=O.[BH4-].[Li+]>>OCCOC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=CC=C(C=C2)NC(C2=C(C=CC=C2)C)=O)=O
CCO[C:24]([CH2:23][O:22][CH:21]1[CH2:20][CH2:19][CH2:18][N:17]([C:15]([c:14]2[cH:13][cH:12][c:11]([NH:10][C:8]([c:7]3[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]3)=[O:9])[cH:34][cH:33]2)=[O:16])[c:32]2[c:26]1[cH:27][c:28]([Cl:29])[cH:30][cH:31]2)=[O:25]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[C:8](=[O:9])[NH:10][c:11]1[...
CCOC(=O)COC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccc(Cl)cc21
Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(OCCO)c3cc(Cl)ccc32)cc1
null
null
O1CCCC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3]-[#8:4]>>[#8:4]-[C:3]-[CH2;D2;+0:1]-[OH;D1;+0:2]
79.1
[{"value": 79.1, "product": "OCCOC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=CC=C(C=C2)NC(C2=C(C=CC=C2)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 5-ethoxycarbonylmethoxy-7-chloro-1-[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (2.2 g) in tetrahydrofuran (50 ml) is added with stirring lithium borohydride (0.28 g) at room temperature, and the mixture is refluxed for 30 minutes. The reaction solution is poured into diluted hyd...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
O1CCCC1
null
null
CCOC(=O)COC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccc(Cl)cc21>O1CCCC1>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(OCCO)c3cc(Cl)ccc32)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-09459eb81e7b4be98bb3082439814f71
CN1CCNCC1.COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OCCOS(=O)(=O)c2ccc(C)cc2)c2cc(F)ccc21>>COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OCCN2CCN(C)CC2)c2cc(F)ccc21
C1(=CC=C(C=C1)S(=O)(=O)OCCOC1CCCN(C2=C1C=C(C=C2)F)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O)C.CN1CCNCC1.[I-].[Na+]>>CN1CCN(CC1)CCOC1CCCN(C2=C1C=C(C=C2)F)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)OC)=O
[NH:29]1[CH2:30][CH2:31][N:32]([CH3:33])[CH2:34][CH2:35]1.Cc1ccc(S(=O)(=O)O[CH2:28][CH2:27][O:26][CH:25]2[CH2:24][CH2:23][CH2:22][N:21]([C:19]([c:18]3[c:3]([O:2][CH3:1])[cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]4[cH:10][cH:11][cH:12][cH:13][c:14]4[CH3:15])[cH:16][cH:17]3)=[O:20])[c:42]3[c:36]2[cH:37][c:38]([F:39])[cH:40][cH:...
CN1CCNCC1.COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OCCOS(=O)(=O)c2ccc(C)cc2)c2cc(F)ccc21
COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OCCN2CCN(C)CC2)c2cc(F)ccc21
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
883f55ad833601fa4f6fc3baadcfd9f1ad53f2d6935818c711f682845b8ecc58
71b4ac4449ece5e0df64e56caf0f1cbac76e83f802a92104cfb6c6c861b6a71c
O=C(Nc1ccc(C(=O)N2CCCC(OCCN3CCNCC3)c3ccccc32)cc1)c1ccccc1
C-c1:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]-[#8:3]):c:c:1.[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
null
[]
null
null
3
DAY
5-[2-(p-Toluenesulfonyloxy)ethoxy]-7-fluoro-1-[2-methoxy-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (0.4 g), N-methylpiperazine (0.38 ml) and sodium iodide (0.3 g) are dispersed in dimethylformamide (10 ml), and the mixture is stirred at room temperature for 3 days. The reaction mixture is conce...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Secondary amine
Tertiary amine
C1CNCC[NH]1.c1ccccc1
C1C[NH]CC[NH]1
c1ccccc1.c1ccccc1.C1C[NH]CC[NH]1.c1ccc2c(c1)CCCC[NH]2
TsOH.HO-
CN(C=O)C
null
72
CN1CCNCC1.COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OCCOS(=O)(=O)c2ccc(C)cc2)c2cc(F)ccc21>CN(C=O)C>COc1cc(NC(=O)c2ccccc2C)ccc1C(=O)N1CCCC(OCCN2CCN(C)CC2)c2cc(F)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-51fadc04c6db458b83e946b701fe0f2a
CC(=O)N1CCNCC1.Cc1ccc(S(=O)(=O)OCCC2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4C)cc3C)c3ccc(Cl)cc32)cc1>>CC(=O)N1CCN(CCC2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4C)cc3C)c3ccc(Cl)cc32)CC1
Cl.C1(=CC=C(C=C1)S(=O)(=O)OCCC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O)C.[I-].[Na+].C(C)(=O)N1CCNCC1>>Cl.C(C)(=O)N1CCN(CC1)CCC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O
[CH3:1][C:2](=[O:3])[N:4]1[CH2:5][CH2:6][NH:7][CH2:41][CH2:42]1.Cc1ccc(S(=O)(=O)O[CH2:8][CH2:9][CH:10]2[CH2:11][CH2:12][CH2:13][N:14]([C:15](=[O:16])[c:17]3[cH:18][cH:19][c:20]([NH:21][C:22](=[O:23])[c:24]4[cH:25][cH:26][cH:27][cH:28][c:29]4[CH3:30])[cH:31][c:32]3[CH3:33])[c:34]3[cH:35][cH:36][c:37]([Cl:38])[cH:39][c:4...
CC(=O)N1CCNCC1.Cc1ccc(S(=O)(=O)OCCC2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4C)cc3C)c3ccc(Cl)cc32)cc1
CC(=O)N1CCN(CCC2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4C)cc3C)c3ccc(Cl)cc32)CC1
null
null
CN(C=O)C.C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
9d271698b0c48162ad18ec9c479844bc505434e9294038bc9af6d1140123fb4f
71b4ac4449ece5e0df64e56caf0f1cbac76e83f802a92104cfb6c6c861b6a71c
O=C(Nc1ccc(C(=O)N2CCCC(CCN3CCNCC3)c3ccccc32)cc1)c1ccccc1
C-c1:c:c:c(-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]-[C:3]):c:c:1.[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
121.5
[{"value": 121.5, "product": "Cl.C(C)(=O)N1CCN(CC1)CCC1CCCN(C2=C1C=C(C=C2)Cl)C(C2=C(C=C(C=C2)NC(C2=C(C=CC=C2)C)=O)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 5-[2-(p-toluenesulfonyloxy)ethyl]-7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine (0.25 g) in dry dimethylformamide (20 ml) are added sodium iodide (0.178 g) and 4-acetylpiperazine (0.152 g), and the mixture is stirred at room temperature for one hour. The mixtur...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Secondary amine
Tertiary amine
C1C[NH]CCN1.c1ccccc1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
TsOH.HO-
CN(C=O)C.C(C)OCC
null
1
CC(=O)N1CCNCC1.Cc1ccc(S(=O)(=O)OCCC2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4C)cc3C)c3ccc(Cl)cc32)cc1>CN(C=O)C.C(C)OCC>CC(=O)N1CCN(CCC2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4C)cc3C)c3ccc(Cl)cc32)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f062401e98454d87bfd0d4d5cf3629c0
C=C(C)C(=O)OCC(O)CCl.ClCC1CO1>>C=C(C)C(=O)OCC1CO1.[Cl-]
C(C(=C)C)(=O)OCC(CCl)O.[OH-].[Na+].[OH-].[K+].C(Cl)C1CO1.[OH-].[K+].C(C(=C)C)(=O)OCC(CCl)O>>C(C(=C)C)(=O)OCC1CO1.[Cl-].[K+]
OC(CCl)C[O:6][C:4]([C:2](=[CH2:1])[CH3:3])=[O:5].[CH2:7]([CH:8]1[CH2:9][O:10]1)[Cl:11]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH:8]1[CH2:9][O:10]1.[Cl-:11]
C=C(C)C(=O)OCC(O)CCl.ClCC1CO1
C=C(C)C(=O)OCC1CO1.[Cl-]
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
32c99f0eb08f47b81bb647b50a09f600dfa27c1940971aad8c430600820adde6
94555e253b0dd09ee7a50d5bf9af8bd561b2f56eac7bb8692ecea93d4f41b3cc
C1CO1
Cl-C-C(-O)-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4](=[C;D1;H2:5])-[C;D1;H3:6].[Cl;H0;D1;+0:7]-[CH2;D2;+0:8]-[C:9]1-[#8:10]-[C:11]-1>>[C;D1;H2:5]=[C:4](-[C;D1;H3:6])-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:1]-[CH2;D2;+0:8]-[C:9]1-[#8:10]-[C:11]-1.[Cl-;H0;D0:7]
null
[]
null
null
null
null
A feed with 3-chloro-2-hydroxypropyl methacrylate (CHPMA), epichlorohydrln, and minor amounts of by-products (GMA and heavies such as polymer by-product materials) flows into an epoxidation reactor to which aqueous alkali metal hydroxides such as sodium hydroxide (NaOH) or potassium hydroxide (KOH) and additional epich...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ester.Secondary alcohol
Ester
null
null
C1CO1
HCl
O
null
null
C=C(C)C(=O)OCC(O)CCl.ClCC1CO1>O>C=C(C)C(=O)OCC1CO1.[Cl-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6e955e2991c44b43badb9a9ccdf6b729
ClCc1ccccc1.c1ccc2[nH]ccc2c1>>c1ccc(Cn2ccc3ccccc32)cc1
N.C(C1=CC=CC=C1)Cl.[NH2-].[Na+].[Na].N.N1C=CC2=CC=CC=C12>>C(C1=CC=CC=C1)N1C=CC2=CC=CC=C12
Cl[CH2:5][c:4]1[cH:3][cH:2][cH:1][cH:16][cH:15]1.[nH:6]1[cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]12>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][n:6]2[cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[cH:15][cH:16]1
ClCc1ccccc1.c1ccc2[nH]ccc2c1
c1ccc(Cn2ccc3ccccc32)cc1
null
null
CCOCC
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
92cc004fc3e2a92f5c9aa0385cdf93f1126e35d5aa485f4f5fe9240c9543c8fe
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccc3ccccc32)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]1:[c:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[c:5]:[c:6]1:[c:7]:[c:8]:[c:9]:[n;H0;D3;+0:10]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
30
MINUTE
To a stirred mixture of sodium amide (prepared from 19.6 g, 0.85 mole of sodium and a few mg of Fe(NO3)3 -9H2O) and 800 mL of liquid NH3 (a dry ice condenser was used) was added a solution of 100 g (0.85 mole) of indole in 250 mL of dry ether during 15 minutes. The mixture was stirred for 30 minutes and then a solution...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HCl
CCOCC
null
0.5
ClCc1ccccc1.c1ccc2[nH]ccc2c1>CCOCC>c1ccc(Cn2ccc3ccccc32)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0aa88ee7cb854783bfc493ea25668c80
ClCc1ccc(Cl)cc1.c1ccc2[nH]ccc2c1>>Clc1ccc(Cn2ccc3ccccc32)cc1
N1C=CC2=CC=CC=C12.ClC1=CC=C(CCl)C=C1.[OH-].[K+]>>ClC1=CC=C(CN2C=CC3=CC=CC=C23)C=C1
Cl[CH2:6][c:5]1[cH:4][cH:3][c:2]([Cl:1])[cH:17][cH:16]1.[nH:7]1[cH:8][cH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]12>>[Cl:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][n:7]2[cH:8][cH:9][c:10]3[cH:11][cH:12][cH:13][cH:14][c:15]23)[cH:16][cH:17]1
ClCc1ccc(Cl)cc1.c1ccc2[nH]ccc2c1
Clc1ccc(Cn2ccc3ccccc32)cc1
null
null
C1(=CC=CC=C1)C.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
92cc004fc3e2a92f5c9aa0385cdf93f1126e35d5aa485f4f5fe9240c9543c8fe
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccc3ccccc32)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]1:[c:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[c:5]:[c:6]1:[c:7]:[c:8]:[c:9]:[n;H0;D3;+0:10]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
84.1
[{"value": 84.0, "product": "ClC1=CC=C(CN2C=CC3=CC=CC=C23)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.1, "product": "ClC1=CC=C(CN2C=CC3=CC=CC=C23)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 11.72 g (0.1 mole) of indole, 17.71 g (0.11 mole) of 4-chlorobenzyl chloride, 33 g (0.5 mole) of 85% KOH, 14 mL of H2O, 2.5 g (2.5 mmoles) of PEG-1000 and 100 mL of toluene was stirred and heated at 55°-65° for 22 hours. After cooling to room temperature, 50 mL of H2O was added. The layers were separated. ...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HCl
C1(=CC=CC=C1)C.O
null
null
ClCc1ccc(Cl)cc1.c1ccc2[nH]ccc2c1>C1(=CC=CC=C1)C.O>Clc1ccc(Cn2ccc3ccccc32)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9e54ac87e6cd4333953c4b9787bd6f06
Brc1ccccc1.c1ccc2[nH]ccc2c1>>c1ccc(-n2ccc3ccccc32)cc1
N1C=CC2=CC=CC=C12.BrC1=CC=CC=C1.C([O-])([O-])=O.[K+].[K+].CN(C)C=O>>C1(=CC=CC=C1)N1C=CC2=CC=CC=C12
Br[c:4]1[cH:3][cH:2][cH:1][cH:15][cH:14]1.[nH:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]12>>[cH:1]1[cH:2][cH:3][c:4](-[n:5]2[cH:6][cH:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]23)[cH:14][cH:15]1
Brc1ccccc1.c1ccc2[nH]ccc2c1
c1ccc(-n2ccc3ccccc32)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
85a6484ae5d3889901774194dcc76ef1462fff5cf0c72d425fcc6d34b5fde5ee
e3660767655c50df0f92afc78c794dd2af7cf646bf1430960eafd30c23bf3fa7
c1ccc(-n2ccc3ccccc32)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[c:6]:[c:7]1:[c:8]:[c:9]:[c:10]:[nH;D2;+0:11]:1>>[c:6]:[c:7]1:[c:8]:[c:9]:[c:10]:[n;H0;D3;+0:11]:1-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
20.2
[{"value": 20.0, "product": "C1(=CC=CC=C1)N1C=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 20.2, "product": "C1(=CC=CC=C1)N1C=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 17.57 g (0.15 mole) of indole, 23.55 g (0.15 mole) of bromobenzene, 21 g of anhydrous potassium carbonate, 0.75 g of CuO, and 30 mL of DMF was stirred and heated under reflux for 43 hours. The cooled mixture was diluted with 200 mL of H2O and extracted with 150 mL of ether. The extract was washed with H2O ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccccc1.c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HBr
O
null
null
Brc1ccccc1.c1ccc2[nH]ccc2c1>O>c1ccc(-n2ccc3ccccc32)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3ef121dbf1f0400b85825dd9302cc9ce
ClCc1ccccc1.c1ccc(-c2cc3ccccc3[nH]2)cc1>>c1ccc(Cn2c(-c3ccccc3)cc3ccccc32)cc1
C1(=CC=CC=C1)C=1NC2=CC=CC=C2C1.C(C1=CC=CC=C1)Cl.[OH-].[K+]>>C(C1=CC=CC=C1)N1C(=CC2=CC=CC=C12)C1=CC=CC=C1
Cl[CH2:5][c:4]1[cH:3][cH:2][cH:1][cH:22][cH:21]1.[nH:6]1[c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]12>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][n:6]2[c:7](-[c:8]3[cH:9][cH:10][cH:11][cH:12][cH:13]3)[cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]23)[cH:21][cH:22]1
ClCc1ccccc1.c1ccc(-c2cc3ccccc3[nH]2)cc1
c1ccc(Cn2c(-c3ccccc3)cc3ccccc32)cc1
null
null
C1(=CC=CC=C1)C.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
16b46a8af20339f7ff0b611b4ac5dd01fe35ba577361e893c359dfa478dc1974
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2c(-c3ccccc3)cc3ccccc32)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]1:[c:7]:[c:8]:[c:9](-[c:10]):[nH;D2;+0:11]:1>>[c:5]:[c:6]1:[c:7]:[c:8]:[c:9](-[c:10]):[n;H0;D3;+0:11]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
13.2
[{"value": 13.0, "product": "C(C1=CC=CC=C1)N1C(=CC2=CC=CC=C12)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 13.2, "product": "C(C1=CC=CC=C1)N1C(=CC2=CC=CC=C12)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 19.33 g (0.1 mole) of 2-phenylindole, 13.92 g (0.11 mole) of benzyl chloride, 33 g (0.5 mole) of 85% KOH, 14 mL of H2O, 2.5 g (2.5 mmoles) of PEG-1000, and 100 mL of toluene was stirred and heated at 55°-60° for 24 hours. After cooling to room temperature, 100 mL of H2O was added. The layers were separated...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1cc2ccccc2[nH]1
c1ccccc1.c1ccccc1.c1cc2ccccc2[nH]1
HCl
C1(=CC=CC=C1)C.O
null
null
ClCc1ccccc1.c1ccc(-c2cc3ccccc3[nH]2)cc1>C1(=CC=CC=C1)C.O>c1ccc(Cn2c(-c3ccccc3)cc3ccccc32)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0121012381ad40bb9bdeb58d7a76e8eb
BrCc1ccccc1.Clc1ccc2[nH]ccc2c1>>Clc1ccc2c(ccn2Cc2ccccc2)c1
ClC=1C=C2C=CNC2=CC1.C(C1=CC=CC=C1)Br.C1COCCOCCOCCOCCOCCO1.CC(C)([O-])C.[K+]>>C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)Cl
Br[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1.[Cl:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7][cH:8][nH:9]2)[cH:17]1>>[Cl:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7][cH:8][n:9]2[CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17]1
BrCc1ccccc1.Clc1ccc2[nH]ccc2c1
Clc1ccc2c(ccn2Cc2ccccc2)c1
null
null
CCOCC.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
92cc004fc3e2a92f5c9aa0385cdf93f1126e35d5aa485f4f5fe9240c9543c8fe
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccc3ccccc32)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]1:[c:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[n;H0;D3;+0:10]1:[c:9]:[c:8]:[c:7]:[c:6]:1:[c:5]):[c:4]
90
[{"value": 90.0, "product": "C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.6, "product": "C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
0.5
HOUR
To a solution of 0.8 g (3.03 mmoles) of 18-crown-6 in 100 mL of dry ether was added 4.39 g (39.12 mmoles) potassium tert-butoxide. The mixture was stirred while 5.08 g (33.51 mmoles) of 5-chloroindole was added. The stirring was continued for 0.5 hour. Most of the solid dissolved. Then 6.69 g (39.11 mmoles) of benzyl b...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HBr
CCOCC.O
null
0.5
BrCc1ccccc1.Clc1ccc2[nH]ccc2c1>CCOCC.O>Clc1ccc2c(ccn2Cc2ccccc2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1e9c28188ba44ba1b3e90f556b1d3cd8
Cc1cc2ccccc2[nH]1.ClCc1ccccc1>>Cc1cc2ccccc2n1Cc1ccccc1
CC=1NC2=CC=CC=C2C1.C(C1=CC=CC=C1)Cl.[OH-].[K+]>>C(C1=CC=CC=C1)N1C(=CC2=CC=CC=C12)C
[CH3:1][c:2]1[cH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[nH:10]1.Cl[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[CH3:1][c:2]1[cH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[n:10]1[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
Cc1cc2ccccc2[nH]1.ClCc1ccccc1
Cc1cc2ccccc2n1Cc1ccccc1
null
null
C1(=CC=CC=C1)C.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
16b46a8af20339f7ff0b611b4ac5dd01fe35ba577361e893c359dfa478dc1974
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccc3ccccc32)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[c:9](:[c:10]):[nH;D2;+0:11]:1>>[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[c:9](:[c:10]):[n;H0;D3;+0:11]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
9.4
[{"value": 9.0, "product": "C(C1=CC=CC=C1)N1C(=CC2=CC=CC=C12)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 9.4, "product": "C(C1=CC=CC=C1)N1C(=CC2=CC=CC=C12)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 13.11 g (0.1 mole) of 2-methylindole, 13.92 g (0.11 mole) of benzyl chloride, 33 g (0.5 mole) of 85% KOH, 14 mL of H2O, 2.5 g (2.5 mmoles) of PEG-1000, and 100 mL of toluene was stirred and heated at 60° for 23 hours. After cooling to room temperature, 100 mL of H2O was added. The layers were separated. Th...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1cc2ccccc2[nH]1
c1cc2ccccc2[nH]1.c1ccccc1
HCl
C1(=CC=CC=C1)C.O
null
null
Cc1cc2ccccc2[nH]1.ClCc1ccccc1>C1(=CC=CC=C1)C.O>Cc1cc2ccccc2n1Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b299b94d41124dd7b4f6bdbadde51879
Cc1cc2ccccc2[nH]1.ClCc1ccccc1>>Cc1cc2ccccc2n1Cc1ccccc1
CC=1NC2=CC=CC=C2C1.C(C1=CC=CC=C1)Cl.C1COCCOCCOCCOCCOCCO1.CC(C)([O-])C.[K+]>>C(C1=CC=CC=C1)N1C(=CC2=CC=CC=C12)C
[CH3:1][c:2]1[cH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[nH:10]1.Cl[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[CH3:1][c:2]1[cH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[n:10]1[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
Cc1cc2ccccc2[nH]1.ClCc1ccccc1
Cc1cc2ccccc2n1Cc1ccccc1
null
null
CCOCC.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
16b46a8af20339f7ff0b611b4ac5dd01fe35ba577361e893c359dfa478dc1974
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccc3ccccc32)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[c:9](:[c:10]):[nH;D2;+0:11]:1>>[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[c:9](:[c:10]):[n;H0;D3;+0:11]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
0.5
HOUR
To a solution of 2.39 g (9.04 mmoles) of 18-crown-6 in 250 mL of dry ether was added 13.1 g (116.7 mmoles) of potassium tert-butoxide. The mixture was stirred while 13.11 g (100 mmoles) of 2-methylindole was added. The stirring was continued for 0.5 hour. Most of the solid dissolved. Then 20 g (116.9 mmoles) of benzyl ...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1cc2ccccc2[nH]1
c1cc2ccccc2[nH]1.c1ccccc1
HCl
CCOCC.O
null
0.5
Cc1cc2ccccc2[nH]1.ClCc1ccccc1>CCOCC.O>Cc1cc2ccccc2n1Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a27889ee44e040db9dcdb94b80457c09
C=CCBr.c1ccc2[nH]ccc2c1>>C=CCn1ccc2ccccc21
N1C=CC2=CC=CC=C12.C(C=C)Br.C1COCCOCCOCCOCCOCCO1.CC(C)([O-])C.[K+]>>C(C=C)N1C=CC2=CC=CC=C12
Br[CH2:3][CH:2]=[CH2:1].[nH:4]1[cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12>>[CH2:1]=[CH:2][CH2:3][n:4]1[cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12
C=CCBr.c1ccc2[nH]ccc2c1
C=CCn1ccc2ccccc21
null
null
CCOCC.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2090660879279eaab8ecde544313a56fd80d46bfd3ea06a7bc9e63018902ce70
4c606dc54eac846ef90c7b3255999ceff93277747e7c2b0ddd37ccf25562b7c5
c1ccc2[nH]ccc2c1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[c:4]:[c:5]1:[c:6]:[c:7]:[c:8]:[nH;D2;+0:9]:1>>[C;D1;H2:3]=[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:9]1:[c:8]:[c:7]:[c:6]:[c:5]:1:[c:4]
74
[{"value": 74.0, "product": "C(C=C)N1C=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.8, "product": "C(C=C)N1C=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a solution of 2.39 g (9.04 mmoles) of 18-crown-6 in 250 ml of dry ether was added 13.1 g (116.7 mmoles) of potassium tert-butoxide. The mixture was stirred while 11.72 g (100 mmoles) indole was added. The stirring was continued for 3 hours. All of the solid did not dissolve. Then 14.1 g (116.5 mmoles) of allyl bromi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Allyl
Allyl
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
HBr
CCOCC.O
null
3
C=CCBr.c1ccc2[nH]ccc2c1>CCOCC.O>C=CCn1ccc2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d138d27f7a2240c7b892e2313bc78ca3
Cc1ccc2[nH]ccc2c1.ClCc1ccccc1>>Cc1ccc2c(ccn2Cc2ccccc2)c1
[NH2-].[Na+].N.C(C1=CC=CC=C1)Cl.CC=1C=C2C=CNC2=CC1.N>>C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)C
[CH3:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7][cH:8][nH:9]2)[cH:17]1.Cl[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7][cH:8][n:9]2[CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17]1
Cc1ccc2[nH]ccc2c1.ClCc1ccccc1
Cc1ccc2c(ccn2Cc2ccccc2)c1
null
null
CCOCC
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
92cc004fc3e2a92f5c9aa0385cdf93f1126e35d5aa485f4f5fe9240c9543c8fe
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccc3ccccc32)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]1:[c:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[n;H0;D3;+0:10]1:[c:9]:[c:8]:[c:7]:[c:6]:1:[c:5]):[c:4]
53
[{"value": 53.0, "product": "C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.7, "product": "C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
To a stirred mixture of sodium amide (prepared from 0.9 g 39.13 mmoles of sodium) and ca 100 ml of liquid ammonia was added a solution of 5.08 g (38.73 mmoles) of 5-methylindole in 100 ml of ether during 5 minutes. The mixture was stirred for 1.5 hours. Then a solution of 5.15 g (40.68 mmoles) of benzyl chloride in 100...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HCl
CCOCC
null
1.5
Cc1ccc2[nH]ccc2c1.ClCc1ccccc1>CCOCC>Cc1ccc2c(ccn2Cc2ccccc2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d0c9152d9e564c87bc2c916dccd31853
ClCc1ccccc1.Fc1ccc2[nH]ccc2c1>>Fc1ccc2c(ccn2Cc2ccccc2)c1
C(C1=CC=CC=C1)Cl.FC=1C=C2C=CNC2=CC1.C1COCCOCCOCCOCCOCCO1.CC(C)([O-])C.[K+]>>C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)F
Cl[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1.[F:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7][cH:8][nH:9]2)[cH:17]1>>[F:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7][cH:8][n:9]2[CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17]1
ClCc1ccccc1.Fc1ccc2[nH]ccc2c1
Fc1ccc2c(ccn2Cc2ccccc2)c1
null
null
CCOCC.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
92cc004fc3e2a92f5c9aa0385cdf93f1126e35d5aa485f4f5fe9240c9543c8fe
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccc3ccccc32)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6]1:[c:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[n;H0;D3;+0:10]1:[c:9]:[c:8]:[c:7]:[c:6]:1:[c:5]):[c:4]
14.1
[{"value": 14.0, "product": "C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 14.1, "product": "C(C1=CC=CC=C1)N1C=CC2=CC(=CC=C12)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
0.5
HOUR
To a solution of 0.8 g (3.03 mmoles) of 18-crown-6 in 100 ml of dry ether was added 3.27 g (29.14 mmoles) of potassium tert-butoxide. The mixture was stirred while a solution of 3.75 g (27.75 mmoles) of 5-fluoroindole in 80 ml of ether was added. The stirring was continued for 0.5 hour. Solid was present. Then 3.69 g (...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HCl
CCOCC.O
null
0.5
ClCc1ccccc1.Fc1ccc2[nH]ccc2c1>CCOCC.O>Fc1ccc2c(ccn2Cc2ccccc2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a2f03c228cfc4a80915bffdae99800be
CCOC(=O)C(OCC)OCC.[NH4+]>>CCOC(OCC)C(N)=O
C(C)OC(C(=O)OCC)OCC.[OH-].[NH4+]>>C(C)OC(C(=O)N)OCC
CCO[C:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])=[O:10].[NH4+:9]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[C:8]([NH2:9])=[O:10]
CCOC(=O)C(OCC)OCC.[NH4+]
CCOC(OCC)C(N)=O
null
null
C(Cl)Cl
Acylation
OtherReaction
d5b10d4f469e7a196a3b04a6a9e159a7d90514b6df5b50c1197d4b1b774c04e1
adc0ef6f6c1340dd2dbab737c85bf17fc842769181c5db1a2b4f82b391b28f9f
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[#8:4])-[#8:5].[NH4+;D0:6]>>[#8:4]-[C:3](-[#8:5])-[C;H0;D3;+0:1](-[NH2;D1;+0:6])=[O;D1;H0:2]
87
[{"value": 87.0, "product": "C(C)OC(C(=O)N)OCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
A mixture of 24.85 g of ethyl diethoxyacetate and 140 ml of concentrated ammonium hydroxide was stirred for 3 hours. The ammonia and H2O were evaporated under reduced pressure on a water bath at 50°-60° leaving a wet solid. The wet solid was dried in a vacuum oven at 53° for 18 hours giving a dark pink solid. The solid...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary amide
null
null
null
HO-
C(Cl)Cl
null
3
CCOC(=O)C(OCC)OCC.[NH4+]>C(Cl)Cl>CCOC(OCC)C(N)=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1e607e457e3c44ccb98525fa715b1116
CO.O=C(O)Cc1cccc(C(F)(F)F)c1>>COC(=O)Cc1cccc(C(F)(F)F)c1
FC(C=1C=C(C=CC1)CC(=O)O)(F)F.CO>>COC(CC1=CC(=CC=C1)C(F)(F)F)=O
[CH3:1][OH:2].O[C:3](=[O:4])[CH2:5][c:6]1[cH:7][cH:8][cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][c:6]1[cH:7][cH:8][cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15]1
CO.O=C(O)Cc1cccc(C(F)(F)F)c1
COC(=O)Cc1cccc(C(F)(F)F)c1
null
null
CCOC(=O)C
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C;D1;H3:5]-[OH;D1;+0:6]>>[C;D1;H3:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
89
[{"value": 89.0, "product": "COC(CC1=CC(=CC=C1)C(F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Into a solution of 3-trifluoromethylphenylacetic acid (20.0 g. 98 mmol) in MeOH (100 mL), cooled in an ice-water bath, was bubbled HCl (g) for 15 min. The mixture was allowed to warm to room temperature and was then concentrated in vacuo to furnish a clear, yellow-green liquid which was diluted with EtOAc (0.25L) and w...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
CCOC(=O)C
null
null
CO.O=C(O)Cc1cccc(C(F)(F)F)c1>CCOC(=O)C>COC(=O)Cc1cccc(C(F)(F)F)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-117b19d4882f4413bce8c78046c64c8c
O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>>O=C([O-])C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
FC(C=1C=C(CNC(C(=O)O)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F.[OH-].[Na+]>>FC(C=1C=C(CNC(C(=O)[O-])C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F.[Na+]
[O:1]=[C:2]([OH:3])[CH:4]([NH:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([C:12]([F:13])([F:14])[F:15])[cH:16]1)[c:17]1[cH:18][n:19]([CH2:20][c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[c:27]2[cH:28][cH:29][cH:30][cH:31][c:32]12>>[O:1]=[C:2]([O-:3])[CH:4]([NH:5][CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([C:12]([F:13])([F:14])...
O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
O=C([O-])C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
null
null
CO
Oxidation
Carboxylic acid to carboxylate
af9382a4a3fca177895c8a400271aa22025197fc08b983f9d71150044c1e6777
b3097057beeca787f1d4960a7ee432572ee7aecad541233195b0dbbc0f674e9c
c1ccc(CNCc2cn(Cc3ccccc3)c3ccccc23)cc1
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]>>[C:1]-[C:2](-[O-;H0;D1:4])=[O;D1;H0:3]
86
[{"value": 86.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3 g (6.84 mmoles) of α-[3-(trifluoromethyl)benzylamino]-1-benzylindole 3-acetic acid, 3.4 ml (6.80 mmoles) of 2N NaOH, and 100 ml of MeOH was warmed until a solution was obtained (one to two hours). The solvent was evaporated. The residue was dried in a vacuum oven at 66° for 70 hours giving 2.70 (86%) of ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
null
null
null
c1ccccc1.c1ccccc1.c1c[nH]c2ccccc12
null
CO
null
null
O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>CO>O=C([O-])C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5e05af3e4327470e88c75d53a7f6a7c7
CCI.O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>>CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
CN(C=O)C.FC(C=1C=C(CNC(C(=O)O)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F.C[O-].[Na+].C(C)I>>FC(C=1C=C(CNC(C(=O)OCC)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F
I[CH2:2][CH3:1].[OH:3][C:4](=[O:5])[CH:6]([NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]([C:14]([F:15])([F:16])[F:17])[cH:18]1)[c:19]1[cH:20][n:21]([CH2:22][c:23]2[cH:24][cH:25][cH:26][cH:27][cH:28]2)[c:29]2[cH:30][cH:31][cH:32][cH:33][c:34]12>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([NH:7][CH2:8][c:9]1[cH:10][cH:11][cH...
CCI.O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
null
null
[Cl-].[Na+].O.CO.CCOCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
c1ccc(CNCc2cn(Cc3ccccc3)c3ccccc23)cc1
I-[CH2;D2;+0:1]-[C;D1;H3:2].[C:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6]>>[C:3]-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C;D1;H3:2]
null
[]
null
null
2
HOUR
To a magnetically stirred suspension of α-[3-(trifluoromethyl)benzylamino)-1-benzylindole-3-acetic acid (21.9 g, 0.05 mol) in 250 mL of methanol at room temperature was treated with 11.34 g of sodium methoxide (25% in methanol) at once. The resulting solution was stirred for two hours, concentrated directly on a rotary...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1ccccc1.c1ccccc1.c1c[nH]c2ccccc12
HI
[Cl-].[Na+].O.CO.CCOCC
null
2
CCI.O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>[Cl-].[Na+].O.CO.CCOCC>CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-37e9705164da464eb5088a85a9aeda49
CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccccc12.CCOC(=O)Cl>>CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(C(=O)OCC)c2ccccc12.Cl
ClC(=O)OCC.FC(C=1C=C(CNC(C(=O)OCC)C2=CNC3=CC=CC=C23)C=CC1)(F)F.[H-].[Na+]>>Cl.FC(C=1C=C(CNC(C(=O)OCC)C2=CN(C3=CC=CC=C23)C(=O)OCC)C=CC1)(F)F
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]([C:14]([F:15])([F:16])[F:17])[cH:18]1)[c:19]1[cH:20][nH:21][c:27]2[cH:28][cH:29][cH:30][cH:31][c:32]12.[C:22](=[O:23])([O:24][CH2:25][CH3:26])[Cl:33]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:1...
CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccccc12.CCOC(=O)Cl
CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(C(=O)OCC)c2ccccc12.Cl
null
null
CN(C)C=O
Acylation
N-alkylation of secondary amines with alkyl halides
33124901c27cb4c2fff33775c779f3741fa39355cb89bbb8a4cc6f24b1c52834
d03c43b1eb3e007d0a26c663cd0f6b51f594c27d1ade9616fb1640d35a60bddb
c1ccc(CNCc2c[nH]c3ccccc23)cc1
[C:1]-[#8:2]-[C;H0;D3;+0:3](-[Cl;H0;D1;+0:4])=[O;D1;H0:5].[c:6]:[c:7]1:[c:8]:[c:9]:[c:10]:[nH;D2;+0:11]:1>>[C:1]-[#8:2]-[C;H0;D3;+0:3](=[O;D1;H0:5])-[n;H0;D3;+0:11]1:[c:10]:[c:9]:[c:8]:[c:7]:1:[c:6].[ClH;D0;+0:4]
66.4
[{"value": 66.4, "product": "Cl.FC(C=1C=C(CNC(C(=O)OCC)C2=CN(C3=CC=CC=C23)C(=O)OCC)C=CC1)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To a magnetically stirred solution of ethyl α-[3(trifluoromethyl)-benzylamino]-indole-3-acetate (1.00 g, 2.66 mmol) in 15 mL of DMF was added under nitrogen 0.112 g (2.79 mmol) of sodium hydride (60% oil dispersion). After stirring at room temperature for 10 minutes, 0.26 ml (2.79 mmol) of ethyl chloroformate was added...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether
Ether
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12
null
CN(C)C=O
null
0.166667
CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccccc12.CCOC(=O)Cl>CN(C)C=O>CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(C(=O)OCC)c2ccccc12.Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f5076b126f9c44638f9cffe98c7e0417
CC(=O)Cl.O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>>COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
C(C)(=O)Cl.FC(C=1C=C(CNC(C(=O)O)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F.C(=O)(O)[O-].[Na+].C(=O)(O)[O-].[Na+].Cl>>FC(C=1C=C(CNC(C(=O)OC)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F
O=C(Cl)[CH3:1].[OH:2][C:3](=[O:4])[CH:5]([NH:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1)[c:18]1[cH:19][n:20]([CH2:21][c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)[c:28]2[cH:29][cH:30][cH:31][cH:32][c:33]12>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([NH:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][c:12]...
CC(=O)Cl.O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
null
null
CO
Heteroatom Alkylation and Arylation
O-methylation
e4e418517831e68b0ae6eff0e20954e6373d72ef6db8a62429d10c826be6ea2e
b1bbfb03e48869c16300667505b58de6f6c5a435aa2a615a319deee7cf33326a
c1ccc(CNCc2cn(Cc3ccccc3)c3ccccc23)cc1
Cl-C(=O)-[CH3;D1;+0:1].[C:2]-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]>>[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH3;D1;+0:1]
null
[]
null
null
45
MINUTE
To a magnetically stirred solution of 100 ml of methanol cooled in an ice-acetone bath at ca. -15° C., was treated dropwise with acetyl chloride (27.3 g, 350 mmol, 35 eq) over a six-minute period as a convenient way to generate HCl in situ. The solution was stirred at ambient temperature for 45 minutes, then solid α-[3...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Carboxylic acid
Ester
null
null
c1ccccc1.c1ccccc1.c1c[nH]c2ccccc12
HCl
CO
null
0.75
CC(=O)Cl.O=C(O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>CO>COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9d6b4639e61f428789f790c938140d8e
COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>>CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
Cl.FC(C=1C=C(CNC(C(=O)OC)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F.C[O-].[Na+]>>FC(C=1C=C(CNC(C(=O)OCC)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F
[CH3:2][O:3][C:4](=[O:5])[CH:6]([NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]([C:14]([F:15])([F:16])[F:17])[cH:18]1)[c:19]1[cH:20][n:21]([CH2:22][c:23]2[cH:24][cH:25][cH:26][cH:27][cH:28]2)[c:29]2[cH:30][cH:31][cH:32][cH:33][c:34]12>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]...
COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
null
null
C(C)O.CO
Miscellaneous
Methylation
797948efc8975454230354c6926ef43459a60311d668503c7a6b6bcdb3eafe50
6ad95641ddc9be155108cd2297ce15bcd8cb0ca25c68bfc4fce3cbf5009a236a
c1ccc(CNCc2cn(Cc3ccccc3)c3ccccc23)cc1
[C:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[CH3;D1;+0:5]>>[C:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[CH2;D2;+0:5]-[C;D1;H3:6]
null
[]
null
null
2
HOUR
To a magnetically stirred solution of methyl α-[3-(trifluoromethyl)benzylamino-]-1-benzylindole-3-acetate hydrochloride (100 mg) in 8 mL of ethanol was added 70 μL of 25% sodium methoxide in methanol. After stirring at room temperature for two hours, TLC analysis showed 90% conversion to the title compound. Conditions:...
10.6084/m9.figshare.5104873.v1
null
Ester
Ester
null
null
c1ccccc1.c1ccccc1.c1c[nH]c2ccccc12
Other
C(C)O.CO
null
2
COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12>C(C)O.CO>CCOC(=O)C(NCc1cccc(C(F)(F)F)c1)c1cn(Cc2ccccc2)c2ccccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-60b3074aefe344eab4ea2ade849112af
Cl>>Cl
FC(C=1C=C(CNC(C(=O)OC)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F.Cl>>Cl.FC(C=1C=C(CNC(C(=O)OC)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F
[ClH:34]>>[ClH:34]
Cl
Cl
null
null
CCOCC
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
95
[{"value": 95.0, "product": "Cl.FC(C=1C=C(CNC(C(=O)OC)C2=CN(C3=CC=CC=C23)CC2=CC=CC=C2)C=CC1)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A magnetically stirred solution of methyl α-[3-(trifluoromethyl)benzylamino]-1-benzylindole-3-acetate (4.07 g, 9.0 mmol) in 65 mL of ether cooled at 0°-5° C. was treated dropwise over a four-minute period with a stock solution of hydrogen chloride in ether (3.8 mL, 11.71 mmol, 1.3 eq, 3.1 mmol per mL). The cooling bath...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
CCOCC
null
8
Cl>CCOCC>Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-21c30be098ec4f848e781425f347ffe0
Cl>>Cl
FC(C=1C=C(CNC(C(=O)OCC)C2=CN(C3=CC=CC=C23)CC)C=CC1)(F)F.Cl>>Cl.FC(C=1C=C(CNC(C(=O)OCC)C2=CN(C3=CC=CC=C23)CC)C=CC1)(F)F
[ClH:30]>>[ClH:30]
Cl
Cl
null
null
CCOCC
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
30
MINUTE
Ethyl α-[3-(trifluoromethyl)benzylamino]-1-ethylindole-3-acetate (1.50 g, 3.70 mmol) was placed in 25 mL of ether, saturated with HCl gas and stirred under nitrogen for 30 minutes. The contents were concentrated to dryness in vacuo and the resulting solid recrystallized from acetone-ether (1:5) to give 1.30 g of the ti...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
CCOCC
null
0.5
Cl>CCOCC>Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3f8581bc16ea4d41a3c766acc9b0ade0
CCCCCC.COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccccc12.ClCc1ccc(Cl)cc1>>COC(=O)C(c1cn(Cc2ccc(Cl)cc2)c2ccccc12)N(C)Cc1cccc(C(F)(F)F)c1
CCCCCC.C(C)(=O)OCC.ClC1=CC=C(CCl)C=C1.[H-].[Na+].FC(C=1C=C(CNC(C(=O)OC)C2=CNC3=CC=CC=C23)C=CC1)(F)F>>CN(C(C(=O)OC)C1=CN(C2=CC=CC=C12)CC1=CC=C(C=C1)Cl)CC1=CC(=CC=C1)C(F)(F)F
CCCCC[CH3:24].[CH3:1][O:2][C:3](=[O:4])[CH:5]([c:6]1[cH:7][nH:8][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12)[NH:23][CH2:25][c:26]1[cH:27][cH:28][cH:29][c:30]([C:31]([F:32])([F:33])[F:34])[cH:35]1.Cl[CH2:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([c:6]1[cH:7][n:8]([CH2:9][c:10...
CCCCCC.COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccccc12.ClCc1ccc(Cl)cc1
COC(=O)C(c1cn(Cc2ccc(Cl)cc2)c2ccccc12)N(C)Cc1cccc(C(F)(F)F)c1
null
null
CN(C=O)C.CCOCC
Heteroatom Alkylation and Arylation
OtherReaction
c6ee39ced5d4143298d1037a6764569d0214d9628a7df282055ec75108f5a438
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CNCc2cn(Cc3ccccc3)c3ccccc23)cc1
C-C-C-C-C-[CH3;D1;+0:1].Cl-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[C:10](-[NH;D2;+0:11]-[C:12]-[c:13])-[c:14]1:[c:15]:[c:16](:[c:17]):[nH;D2;+0:18]:[c:19]:1>>[C;D1;H3:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[C:10](-[N;H0;D3;+0:11](-[CH3;D1;+0:1])-[C:12]-[c:13])-[c:14]1:[c:15]:[c:16](:[c:17]):[n;...
null
[]
null
null
10
MINUTE
To a magnetically stirred suspension of sodium hydride (60% oil dispersion washed two times with hexane, 80 mg, 2.0 mmol) in 5 mL of dimethylformamide (DMF) under nitrogen was added methyl α-[3-(trifluoromethyl)benzylamino]-indole-3acetate (752 mg, 2.0 mmol) dissolved in 2 mL DMF. Stirring was continued at room tempera...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12.c1ccccc1
HCl
CN(C=O)C.CCOCC
null
0.166667
CCCCCC.COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccccc12.ClCc1ccc(Cl)cc1>CN(C=O)C.CCOCC>COC(=O)C(c1cn(Cc2ccc(Cl)cc2)c2ccccc12)N(C)Cc1cccc(C(F)(F)F)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2ab8d445b07a4216a285e80f012a3dfa
COc1ccc2[nH]ccc2c1.NCc1cccc(C(F)(F)F)c1.O=CC(=O)O>>COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccc(OC)cc12
COC=1C=C2C=CNC2=CC1.FC(C=1C=C(CN)C=CC1)(F)F.C(C)(=O)O.O.C(C=O)(=O)O>>FC(C=1C=C(C=CC1)CNC(C(=O)OC)C1=CNC2=CC=C(C=C12)OC)(F)F
[cH:18]1[cH:19][nH:20][c:21]2[cH:22][cH:23][c:24]([O:25][CH3:26])[cH:27][c:28]12.[NH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1.O=[CH:5][C:3]([OH:2])=[O:4]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([NH:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1)[c:18]1[c...
COc1ccc2[nH]ccc2c1.NCc1cccc(C(F)(F)F)c1.O=CC(=O)O
COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccc(OC)cc12
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
1ad28a17916661faa13d1595f9601d2e5842ade24e08e8306fdd72a883053031
97dbaca91fbe46a7e0670cff222de61ac85a7fcf864bf14fca6123c5a1a3812c
c1ccc(CNCc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4].[NH2;D1;+0:5]-[C:6]-[c:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:15]-[O;H0;D2;+0:4]-[C:2](=[O;D1;H0:3])-[CH;D3;+0:1](-[NH;D2;+0:5]-[C:6]-[c:7])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
3
DAY
To a stirred solution of 7.24 g (41.34 mmoles) of 3-(trifluoromethyl)benzylamine and 4 mL (4.2 g, 69.88 mmoles) of acetic acid in 50 mL of MeOH was added a solution of 3.65 g (41.34 mmoles) of glyoxylic acid monohydrate in 50 mL of MeOH followed by 5.07 g (34.45 mmoles) of 5-methoxyindole. The resulting solution was al...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Carboxylic acid.Primary amine
Ester.Secondary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
null
CO
null
72
COc1ccc2[nH]ccc2c1.NCc1cccc(C(F)(F)F)c1.O=CC(=O)O>CO>COC(=O)C(NCc1cccc(C(F)(F)F)c1)c1c[nH]c2ccc(OC)cc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-69fd0f6486c34ef8b949897a3d4dc910
CCOC(=O)C(N)c1c[nH]c2ccccc12>>NC(C(=O)O)c1c[nH]c2ccccc12
NC(C(=O)OCC)C1=CNC2=CC=CC=C12.[OH-].[Na+].CO>>NC(C(=O)O)C1=CNC2=CC=CC=C12
CC[O:5][C:3]([CH:2]([NH2:1])[c:6]1[cH:7][nH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]12)=[O:4]>>[NH2:1][CH:2]([C:3](=[O:4])[OH:5])[c:6]1[cH:7][nH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]12
CCOC(=O)C(N)c1c[nH]c2ccccc12
NC(C(=O)O)c1c[nH]c2ccccc12
null
null
C(C)(=O)O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc2[nH]ccc2c1
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
null
null
50
MINUTE
A mixture of 2 g of ethyl α-aminoindole-3-acetate, excess dilute NaOH solution, and a few mL of MeOH was stirred occasionally for 25 minutes. Since a solution had not been obtained, the mixture was heated on a steam bath for ten minutes. The resulting solution was allowed to stand at ambient temperature for 50 minutes....
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2[nH]ccc2c1
Other
C(C)(=O)O
null
0.833333
CCOC(=O)C(N)c1c[nH]c2ccccc12>C(C)(=O)O>NC(C(=O)O)c1c[nH]c2ccccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-07edbbd2cd764d6591514470ed57cfaa
COC(=O)C=O.NCCc1ccc(S(N)(=O)=O)cc1.c1ccc2[nH]ccc2c1>>NS(=O)(=O)c1ccc(CCNC(C(=O)O)c2c[nH]c3ccccc23)cc1.O
N1C=CC2=CC=CC=C12.NCCC1=CC=C(C=C1)S(=O)(=O)N.C(C)(=O)O.C(C=O)(=O)OC>>O.NS(=O)(=O)C1=CC=C(C=C1)CCNC(C(=O)O)C1=CNC2=CC=CC=C12
C[O:15][C:13]([CH:12]=[O:27])=[O:14].[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH2:9][CH2:10][NH2:11])[cH:25][cH:26]1.[cH:16]1[cH:17][nH:18][c:19]2[cH:20][cH:21][cH:22][cH:23][c:24]12>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH2:9][CH2:10][NH:11][CH:12]([C:13](=[O:14])[OH:15])[c:16]2[cH:17][nH:1...
COC(=O)C=O.NCCc1ccc(S(N)(=O)=O)cc1.c1ccc2[nH]ccc2c1
NS(=O)(=O)c1ccc(CCNC(C(=O)O)c2c[nH]c3ccccc23)cc1.O
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
a80af25249377d1b42548b94d6e944681d1777120ac835628ebb2925ed11199d
4be68a8f2d238730b7d84250aa75cdaa35366d05903de952015a33135d01500f
c1ccc(CCNCc2c[nH]c3ccccc23)cc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[O;H0;D1;+0:5].[C:6]-[C:7]-[NH2;D1;+0:8].[c:9]:[c:10]1:[#7;a:11]:[c:12]:[cH;D2;+0:13]:[c:14]:1:[c:15]>>[C:6]-[C:7]-[NH;D2;+0:8]-[CH;D3;+0:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1])-[c;H0;D3;+0:13]1:[c:12]:[#7;a:11]:[c:10](:[c:9]):[c:14]:1:[c:15].[OH2;D0;+0:5]
63,355.6
[{"value": 38.0, "product": "O.NS(=O)(=O)C1=CC=C(C=C1)CCNC(C(=O)O)C1=CNC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63355.6, "product": "O.NS(=O)(=O)C1=CC=C(C=C1)CCNC(C(=O)O)C1=CNC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
DAY
To a stirred solution of 6.01 g (0.03 mmole) of 4-(2-aminoethyl)benzenesulfonamide and 2.5 mL (2.62 g 0.044 mole) of acetic acid in 150 mL of MeOH was added a solution of 2.64 g (0.03 mole) of methyl glyoxylate in 50 mL of MeOH followed by 2.93 g (0.025 mole) of indole. Initially a solution was obtained. Soon solid beg...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Primary amine
Carboxylic acid.Secondary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
Other
CO
null
96
COC(=O)C=O.NCCc1ccc(S(N)(=O)=O)cc1.c1ccc2[nH]ccc2c1>CO>NS(=O)(=O)c1ccc(CCNC(C(=O)O)c2c[nH]c3ccccc23)cc1.O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-69d35a3bb1bc42339ef1b49a84e23b5f
COC(=O)C=O.NCc1ccccc1.c1ccc2[nH]ccc2c1>>COC(=O)C(NCc1ccccc1)c1c[nH]c2ccccc12
N1C=CC2=CC=CC=C12.C(C1=CC=CC=C1)N.C(C)(=O)O.C(C=O)(=O)OC>>C1(=CC=CC=C1)CNC(C(=O)OC)C1=CNC2=CC=CC=C12
O=[CH:5][C:3]([O:2][CH3:1])=[O:4].[NH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.[cH:14]1[cH:15][nH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([NH:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[c:14]1[cH:15][nH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12
COC(=O)C=O.NCc1ccccc1.c1ccc2[nH]ccc2c1
COC(=O)C(NCc1ccccc1)c1c[nH]c2ccccc12
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
5595146384c598279112ebd7ba0cf5386a231bbdc1f289220bf12fba7cc91e05
58e20d8df59c2495160850d53d072962f7ab0829c937d9b002a0dd2d82d92775
c1ccc(CNCc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].[NH2;D1;+0:6]-[C:7]-[c:8].[c:9]:[c:10]1:[#7;a:11]:[c:12]:[cH;D2;+0:13]:[c:14]:1:[c:15]>>[C;D1;H3:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH;D3;+0:1](-[NH;D2;+0:6]-[C:7]-[c:8])-[c;H0;D3;+0:13]1:[c:12]:[#7;a:11]:[c:10](:[c:9]):[c:14]:1:[c:15]
86.3
[{"value": 86.3, "product": "C1(=CC=CC=C1)CNC(C(=O)OC)C1=CNC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
69
HOUR
To a stirred solution of 6.43 g (0.06 mole) of benzylamine and 5 mL (5.25 g, 0.09 mole) of acetic acid in 50 mL of MeOH was added a solution of 5.28 g (0.06 mole) of methyl glyoxylate in 50 mL of MeOH followed by 5.86 g (0.05 mole) of indole. The resulting solution was allowed to stand for 69 hours. The solvent was eva...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Primary amine
Ester.Secondary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
CO
null
69
COC(=O)C=O.NCc1ccccc1.c1ccc2[nH]ccc2c1>CO>COC(=O)C(NCc1ccccc1)c1c[nH]c2ccccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c456b7da73ac4e6ca23b379fc52bb58b
COC(=O)CNc1ccccc1.O=Cc1cn(Cc2ccccc2)c2ccccc12>>COC(=O)C(NCc1cn(Cc2ccccc2)c2ccccc12)c1ccccc1
[BH3-]C#N.[Na+].C1(=CC=CC=C1)CN1C=C(C2=CC=CC=C12)C=O.Cl.C1(=CC=CC=C1)NCC(=O)OC.CC(=O)O.CO>>C1(=CC=CC=C1)CN1C=C(C2=CC=CC=C12)CNC(C(=O)OC)C1=CC=CC=C1
[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1.O=[CH:7][c:8]1[cH:9][n:10]([CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]12>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([NH:6][CH2:7][c:8]1[cH:9][n:10]([CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]...
COC(=O)CNc1ccccc1.O=Cc1cn(Cc2ccccc2)c2ccccc12
COC(=O)C(NCc1cn(Cc2ccccc2)c2ccccc12)c1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2394dddb06f5e80eb63aa57cb341e545bca55094f537ccd3ceb95ddec7356af1
345fa7989b6c7bd18d53834597527cc4f3089a81ee246a4b80121bb910b114a0
c1ccc(CNCc2cn(Cc3ccccc3)c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5](-[C:6]):[c:7]:1.[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[CH2;D2;+0:12]-[NH;D2;+0:13]-[c;H0;D3;+0:14](:[c:15]:[c:16]):[c:17]:[c:18]>>[C:6]-[#7;a:5]1:[c:4]:[c:3]:[c:2](-[CH2;D2;+0:1]-[NH;D2;+0:13]-[CH;D3;+0:12](-[C:10](=[O;D1;H0:11])-[#8:9]-[C;D1;H3:8])-[c;H0;D3;+0:14](:[c:15]:...
43
[{"value": 43.0, "product": "C1(=CC=CC=C1)CN1C=C(C2=CC=CC=C12)CNC(C(=O)OC)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
To a suspension of methyl (+/-)-phenylglycinate hydrochloride (4.00 g, 19.8 mmol) in MeOH (50 mL), and HOAc (4 mL) was added 1-phenylmethyl-indole-3-carboxaldehyde (2.85 g, 12.1 mmol). The resulting mixture was allowed to stir at room temperature for 20 minutes; then NaBH3CN (1.98 g, 31.5 mmol) was added in one portion...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Secondary amine
Ester.Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1c[nH]c2ccccc12.c1ccccc1
Other
null
null
0.333333
COC(=O)CNc1ccccc1.O=Cc1cn(Cc2ccccc2)c2ccccc12>>COC(=O)C(NCc1cn(Cc2ccccc2)c2ccccc12)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c1c083a6f395481abe3df8731345c900
C[Si](C)(Cl)Cl.N>>C[Si]1(C)N[Si](C)(C)N[Si](C)(C)N1
C[Si](Cl)(Cl)C.N>>C[Si]1(N[Si](N[Si](N1)(C)C)(C)C)C
Cl[Si:2](Cl)([CH3:1])[CH3:7].[NH3:4]>>[CH3:1][Si:2]1([CH3:3])[NH:4][Si:5]([CH3:6])([CH3:7])[NH:8][Si:9]([CH3:10])([CH3:11])[NH:12]1
C[Si](C)(Cl)Cl.N
C[Si]1(C)N[Si](C)(C)N[Si](C)(C)N1
null
null
C1=CC=CC=C1
Protection
OtherReaction
14143e77eb8e0d2e8640f64675f2937ce6536749cb929538870537b809701eb3
69f9623d70f8449fc8a053886a4509e0600bee582fe9a4cd1a5c5e2782e4232a
N1[SiH2]N[SiH2]N[SiH2]1
Cl-[Si;H0;D4;+0:1](-Cl)(-[C;D1;H3:2])-[CH3;D1;+0:3].[NH3;D0;+0:4]>>[C;D1;H3:2]-[Si;H0;D4;+0:1]1(-[C;D1;H3:5])-[#7:6]-[#14:7]-[#7:8]-[#14:9](-[C;D1;H3:10])(-[CH3;D1;+0:3])-[NH;D2;+0:4]-1
null
[]
null
null
null
null
This method involves reacting dimethyldichlorosilane with ammonia in benzene at 30° C., removing ammonia chloride by-product by filtration through a glass filter or the like, and distilling the reaction product to isolate hexamethylcyclotrisilazane. Conditions: See reaction.notes.procedure_details. Workup: at 30° C.; r...
10.6084/m9.figshare.5104873.v1
null
Silyl protective group
Secondary amine.Secondary amine.Secondary amine.Silyl protective group.Silyl protective group.Silyl protective group
null
N1[Si]N[Si]N[Si]1
N1[Si]N[Si]N[Si]1
null
C1=CC=CC=C1
null
null
C[Si](C)(Cl)Cl.N>C1=CC=CC=C1>C[Si]1(C)N[Si](C)(C)N[Si](C)(C)N1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8e84db8ce536415d96651b7838d19504
C[Si](C)(Cl)Cl.N>>C[Si]1(C)N[Si](C)(C)N[Si](C)(C)N1
C[Si](Cl)(Cl)C.N>>C[Si]1(N[Si](N[Si](N1)(C)C)(C)C)C
Cl[Si:2](Cl)([CH3:1])[CH3:7].[NH3:4]>>[CH3:1][Si:2]1([CH3:3])[NH:4][Si:5]([CH3:6])([CH3:7])[NH:8][Si:9]([CH3:10])([CH3:11])[NH:12]1
C[Si](C)(Cl)Cl.N
C[Si]1(C)N[Si](C)(C)N[Si](C)(C)N1
null
null
C1(=CC=CC=C1)C
Protection
OtherReaction
14143e77eb8e0d2e8640f64675f2937ce6536749cb929538870537b809701eb3
69f9623d70f8449fc8a053886a4509e0600bee582fe9a4cd1a5c5e2782e4232a
N1[SiH2]N[SiH2]N[SiH2]1
Cl-[Si;H0;D4;+0:1](-Cl)(-[C;D1;H3:2])-[CH3;D1;+0:3].[NH3;D0;+0:4]>>[C;D1;H3:2]-[Si;H0;D4;+0:1]1(-[C;D1;H3:5])-[#7:6]-[#14:7]-[#7:8]-[#14:9](-[C;D1;H3:10])(-[CH3;D1;+0:3])-[NH;D2;+0:4]-1
42.1
[{"value": 42.0, "product": "C[Si]1(N[Si](N[Si](N1)(C)C)(C)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 42.1, "product": "C[Si]1(N[Si](N[Si](N1)(C)C)(C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 500-ml, four-necked flask equipped with a stirrer, dry ice/acetone condenser, thermometer, and gas inlet tube was charged with 64.5 grams (0.5 mol) of dimethyldichlorosilane and 150 grams of toluene. Into the solution at 30° C., 52 grams (3.06 mol) of ammonia was blown over 2 hours for effecting reaction. At the end ...
10.6084/m9.figshare.5104873.v1
null
Silyl protective group
Secondary amine.Secondary amine.Secondary amine.Silyl protective group.Silyl protective group.Silyl protective group
null
N1[Si]N[Si]N[Si]1
N1[Si]N[Si]N[Si]1
null
C1(=CC=CC=C1)C
null
null
C[Si](C)(Cl)Cl.N>C1(=CC=CC=C1)C>C[Si]1(C)N[Si](C)(C)N[Si](C)(C)N1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fabc61b31cd147d983caa87d8e7474d5
CCCCCCBr.COC(=O)CC(C)=O>>CCCCCCC(C(C)=O)C(=O)OC
C(CC(=O)C)(=O)OC.C[O-].[Na+].BrCCCCCC>>C(C)(=O)C(C(=O)OC)CCCCCC
Br[CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[CH2:7]([C:8]([CH3:9])=[O:10])[C:11](=[O:12])[O:13][CH3:14]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH:7]([C:8]([CH3:9])=[O:10])[C:11](=[O:12])[O:13][CH3:14]
CCCCCCBr.COC(=O)CC(C)=O
CCCCCCC(C(C)=O)C(=O)OC
null
null
CO
C-C Coupling
OtherReaction
eb3faf2a43700925ab4f46cf65072b7145e4e060dba25a917e6b7428f38e349e
61bad66347ae366bfd0a2cd3779dd3d0c29125e97564b97243e11258be3b2a9f
null
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[C:9](-[C;D1;H3:10])=[O;D1;H0:11]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:8](-[C:6](=[O;D1;H0:7])-[#8:5]-[C;D1;H3:4])-[C:9](-[C;D1;H3:10])=[O;D1;H0:11]
62.3
[{"value": 62.3, "product": "C(C)(=O)C(C(=O)OC)CCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
465 g of methyl acetoacetate were added dropwise under nitrogen and stirring to 720 g of 30% sodium methylate solution in 1200 ml of methanol. Then, 727 g of 1-bromohexane were added and the reaction mixture was boiled at reflux for 20 hours. The majority of the methanol was distilled off and the residue was poured on ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone.Ester
null
null
null
HBr
CO
null
null
CCCCCCBr.COC(=O)CC(C)=O>CO>CCCCCCC(C(C)=O)C(=O)OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3394f386594347eeac4f17cc00376730
Cc1ccccc1.O=C(OC(=O)c1ccccc1)c1ccccc1.[O-][Cl+3]([O-])([O-])O>>CCCCCCCCCCCC1CC(OC(=O)c2ccccc2)C(CCCCCC)C(=O)O1
C1(=CC=CC=C1)C.C(C1=CC=CC=C1)(=O)OC(C1=CC=CC=C1)=O.Cl(=O)(=O)(=O)O>>C(C1=CC=CC=C1)(=O)OC1C(C(=O)OC(C1)CCCCCCCCCCC)CCCCCC
[cH:1]1[cH:2][cH:13][c:12]([CH3:11])[cH:29][cH:30]1.[cH:14]1[c:24]([C:31]([O:15][C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)=[O:33])[cH:25][cH:26][cH:27][cH:28]1.[O-][Cl+3]([O-])(O)[O-:32]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH:12]1[CH2:13][CH:14]([O:15][C:16]...
Cc1ccccc1.O=C(OC(=O)c1ccccc1)c1ccccc1.[O-][Cl+3]([O-])([O-])O
CCCCCCCCCCCC1CC(OC(=O)c2ccccc2)C(CCCCCC)C(=O)O1
null
null
null
C-C Coupling
OtherReaction
c9cfa63c20444de92fcef08b02d1254bf21ad8bd4547a1cfeebe9628108651e7
f4f0e4933e28ad003609fc57514057fc8dd4673f5e354908bb247868372e8d2b
O=C1CC(OC(=O)c2ccccc2)CCO1
O-[Cl+3](-[O-;H0;D1:1])(-[O-])-[O-].[CH3;D1;+0:2]-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:1.[O;D1;H0:9]=[C:10](-[c:11])-[O;H0;D2;+0:12]-[C;H0;D3;+0:13](=[O;H0;D1;+0:14])-[c;H0;D3;+0:15]1:[cH;D2;+0:16]:[cH;D2;+0:17]:[cH;D2;+0:18]:[cH;D2;+0:19]:[cH;D2;+0:20]:1>>[C:21]-[C:22]-[CH2;...
103.4
[{"value": 103.4, "product": "C(C1=CC=CC=C1)(=O)OC1C(C(=O)OC(C1)CCCCCCCCCCC)CCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
177.3 g of the δ-lactone from c) were suspended in 1250 ml of toluene while stirring. After the addition of 138.6 g of benzoic anhydride the mixture was stirred for 10 minutes. Then, 2.5 ml of perchloric acid were added. The mixture was stirred for a further 2.5 hours. The reaction solution was extracted in toluene wit...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester
Ester.Ester
c1ccccc1.c1ccccc1
C1CCOCC1
C1CCOCC1.c1ccccc1
null
null
null
null
Cc1ccccc1.O=C(OC(=O)c1ccccc1)c1ccccc1.[O-][Cl+3]([O-])([O-])O>>CCCCCCCCCCCC1CC(OC(=O)c2ccccc2)C(CCCCCC)C(=O)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7aa6ea05ad5f4e639b91d1a44ecf298b
CCCCCCCCCCC[C@@H](O)CC(=O)OC.N=C(OCc1ccccc1)C(Cl)(Cl)Cl>>CCCCCCCCCCC[C@H](CC(=O)OC)OCc1ccccc1
O[C@@H](CC(=O)OC)CCCCCCCCCCC.ClC(C(OCC1=CC=CC=C1)=N)(Cl)Cl.FC(S(=O)(=O)O)(F)F>>C(C1=CC=CC=C1)O[C@@H](CC(=O)OC)CCCCCCCCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C@H:12]([CH2:13][C:14](=[O:15])[O:16][CH3:17])[OH:18].N=C(O[CH2:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1)C(Cl)(Cl)Cl>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C@H:12]([CH2:13][C:14](=[O:15])[O:16...
CCCCCCCCCCC[C@@H](O)CC(=O)OC.N=C(OCc1ccccc1)C(Cl)(Cl)Cl
CCCCCCCCCCC[C@H](CC(=O)OC)OCc1ccccc1
null
null
C1CCCCC1
Heteroatom Alkylation and Arylation
OtherReaction
e1602c7639e9590c57e1f519302834b854314fa06b50f2e00792e7923548c28a
9939e71487b269001d097fe9b7393354dcb141bf54208fca597f111e50af4454
c1ccccc1
Cl-C(-Cl)(-Cl)-C(=N)-O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]-[C:9](-[C:10])-[OH;D1;+0:11]>>[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]-[C:9](-[C:10])-[O;H0;D2;+0:11]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
112.8
[{"value": 112.8, "product": "C(C1=CC=CC=C1)O[C@@H](CC(=O)OC)CCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 206.7 g of methyl (R)-3-hydroxytetradecanoate in 1000 ml of cyclohexane was treated under nitrogen and while stirring with 214.2 g of benzyl trichloroacetimidate and dissolved at 20°. 10 ml of trifluoromethanesulphonic acid were added dropwise while cooling in an ice/water bath in such a manner that the...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Ether.Secondary alcohol
Ether
null
null
c1ccccc1
HCl
C1CCCCC1
null
null
CCCCCCCCCCC[C@@H](O)CC(=O)OC.N=C(OCc1ccccc1)C(Cl)(Cl)Cl>C1CCCCC1>CCCCCCCCCCC[C@H](CC(=O)OC)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3778de4bf8bd4957a0ab8fe7b5d88d63
CCCCCCCCCCC[C@@H](O)CC(=O)OC>>CCCCCCCCCCC[C@@H](O)CC(=O)O
O[C@@H](CC(=O)OC)CCCCCCCCCCC.O1CCOCC1.[OH-].[Na+]>>O[C@@H](CC(=O)O)CCCCCCCCCCC
C[O:17][C:15]([CH2:14][C@@H:12]([CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[OH:13])=[O:16]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][C@@H:12]([OH:13])[CH2:14][C:15](=[O:16])[OH:17]
CCCCCCCCCCC[C@@H](O)CC(=O)OC
CCCCCCCCCCC[C@@H](O)CC(=O)O
null
null
CO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
null
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
98
[{"value": 98.0, "product": "O[C@@H](CC(=O)O)CCCCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.9, "product": "O[C@@H](CC(=O)O)CCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Under nitrogen and while stirring there were added dropwise to a solution of 129.2 g of methyl (R)-3-hydroxytetradecanoate, 1033 ml of dioxan and 122.9 g of 28 percent sodium hydroxide solution. 77.5 ml of methanol were added dropwise to the solution. After stirring for a further 1.5 hours the resulting suspension was ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
null
Other
CO
null
null
CCCCCCCCCCC[C@@H](O)CC(=O)OC>CO>CCCCCCCCCCC[C@@H](O)CC(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-355ce15f03e04745bfb0f379e76f61c0
CCCCCCBr.COC(=O)CC(=O)OC>>CCCCCCC(C(=O)OC)C(=O)OC
O.C[O-].[Na+].C(CC(=O)OC)(=O)OC.BrCCCCCC>>C(CCCCC)C(C(=O)OC)C(=O)OC
Br[CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[CH2:7]([C:8](=[O:9])[O:10][CH3:11])[C:12](=[O:13])[O:14][CH3:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH:7]([C:8](=[O:9])[O:10][CH3:11])[C:12](=[O:13])[O:14][CH3:15]
CCCCCCBr.COC(=O)CC(=O)OC
CCCCCCC(C(=O)OC)C(=O)OC
null
null
CO
C-C Coupling
OtherReaction
8175b6573d6439ec7ccc45bf6b48843ab56b46dccfc6504384c4766d09f35cc7
d1817e44576d3a158547867a56245217a593d4f828a6d6dfaa8ed11276894e44
null
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[#8:11]-[C;D1;H3:12]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:8](-[C:9](=[O;D1;H0:10])-[#8:11]-[C;D1;H3:12])-[C:6](=[O;D1;H0:7])-[#8:5]-[C;D1;H3:4]
78.3
[{"value": 78.3, "product": "C(CCCCC)C(C(=O)OC)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.3, "product": "C(CCCCC)C(C(=O)OC)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
350.1 g of 30 percent sodium methylate solution in methanol were diluted with 550 ml of methanol under nitrogen and while stirring. 264.2 g of dimethyl malonate were added dropwise. After warming the suspension to 40° 321.0 g of 1-bromohexane were added dropwise. After stirring at 40° for 1 hour, under reflux for 2 hou...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ester
Ester.Ester
null
null
null
HBr
CO
null
null
CCCCCCBr.COC(=O)CC(=O)OC>CO>CCCCCCC(C(=O)OC)C(=O)OC