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
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large_stringlengths
14
3.37k
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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
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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-0387783899c642a8b7eb4ba379bcdf5d
ord-c5d9bebb04b040e391a8be4021bce133
CNC.O=Cc1ccc(F)cc1Cl.O=[N+]([O-])c1cccc2[nH]ccc12>>CN(C)C(c1ccc(F)cc1Cl)c1c[nH]c2cccc([N+](=O)[O-])c12
[N+](=O)([O-])C1=C2C=CNC2=CC=C1.[Cl-].ClC1=C(C=[N+](C)C)C=CC(=C1)F.ClC1=C(C=O)C=CC(=C1)F.CNC>>ClC1=C(C=CC(=C1)F)C(C1=CNC2=CC=CC(=C12)[N+](=O)[O-])N(C)C
[CH3:1][NH:2][CH3:3].O=[CH:4][c:5]1[cH:6][cH:7][c:8]([F:9])[cH:10][c:11]1[Cl:12].[cH:13]1[cH:14][nH:15][c:16]2[cH:17][cH:18][cH:19][c:20]([N+:21](=[O:22])[O-:23])[c:24]12>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][c:8]([F:9])[cH:10][c:11]1[Cl:12])[c:13]1[cH:14][nH:15][c:16]2[cH:17][cH:18][cH:19][c:20]([N+:21](=[O:...
CNC.O=Cc1ccc(F)cc1Cl.O=[N+]([O-])c1cccc2[nH]ccc12
CN(C)C(c1ccc(F)cc1Cl)c1c[nH]c2cccc([N+](=O)[O-])c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 4-nitroindole and (2-chloro-4-fluoro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 2-chloro-4-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.O=Cc1ccc(F)cc1Cl.O=[N+]([O-])c1cccc2[nH]ccc12>>CN(C)C(c1ccc(F)cc1Cl)c1c[nH]c2cccc([N+](=O)[O-])c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9c25bc003cb249c8bfbc584f2f7916cd
CNC.Cc1cccc2[nH]ccc12.O=Cc1ccc(F)cc1Cl>>Cc1cccc2[nH]cc(C(c3ccc(F)cc3Cl)N(C)C)c12
CC1=C2C=CNC2=CC=C1.[Cl-].ClC1=C(C=[N+](C)C)C=CC(=C1)F.ClC1=C(C=O)C=CC(=C1)F.CNC>>ClC1=C(C=CC(=C1)F)C(C1=CNC2=CC=CC(=C12)C)N(C)C
[NH:19]([CH3:20])[CH3:21].[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[nH:7][cH:8][cH:9][c:22]12.O=[CH:10][c:11]1[cH:12][cH:13][c:14]([F:15])[cH:16][c:17]1[Cl:18]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[nH:7][cH:8][c:9]([CH:10]([c:11]3[cH:12][cH:13][c:14]([F:15])[cH:16][c:17]3[Cl:18])[N:19]([CH3:20])[CH3:21])[c:22]12
CNC.Cc1cccc2[nH]ccc12.O=Cc1ccc(F)cc1Cl
Cc1cccc2[nH]cc(C(c3ccc(F)cc3Cl)N(C)C)c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[cH;D2;+0:10]:[c:11]:[#7;a:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:10]1:[c:11]:[#7;a:12]:[c:13](:[c:14]):[c:9]:1:[c:8]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 4-methylindole and (2-chloro-4-fluoro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 2-chloro-4-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_de...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
null
null
null
CNC.Cc1cccc2[nH]ccc12.O=Cc1ccc(F)cc1Cl>>Cc1cccc2[nH]cc(C(c3ccc(F)cc3Cl)N(C)C)c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-024ef80f0453487d912adea4ad07485b
CNC.O=Cc1c(F)cccc1Cl.c1ccc(-c2cc3ccccc3[nH]2)cc1>>CN(C)C(c1c(F)cccc1Cl)c1c(-c2ccccc2)[nH]c2ccccc12
C1(=CC=CC=C1)C=1NC2=CC=CC=C2C1.[Cl-].ClC1=C(C=[N+](C)C)C(=CC=C1)F.ClC1=C(C=O)C(=CC=C1)F.CNC>>ClC1=C(C(=CC=C1)F)C(C1=C(NC2=CC=CC=C12)C1=CC=CC=C1)N(C)C
[CH3:1][NH:2][CH3:3].O=[CH:4][c:5]1[c:6]([F:7])[cH:8][cH:9][cH:10][c:11]1[Cl:12].[cH:13]1[c:14](-[c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)[nH:21][c:22]2[cH:23][cH:24][cH:25][cH:26][c:27]12>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[c:6]([F:7])[cH:8][cH:9][cH:10][c:11]1[Cl:12])[c:13]1[c:14](-[c:15]2[cH:16][cH:17][cH:18][cH:...
CNC.O=Cc1c(F)cccc1Cl.c1ccc(-c2cc3ccccc3[nH]2)cc1
CN(C)C(c1c(F)cccc1Cl)c1c(-c2ccccc2)[nH]c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c(-c3ccccc3)[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:9](-[c:8]):[#7;a:10]:[c:11](:[c:12]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-phenylindole and (2-chloro-6-fluoro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 2-chloro-6-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_de...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.O=Cc1c(F)cccc1Cl.c1ccc(-c2cc3ccccc3[nH]2)cc1>>CN(C)C(c1c(F)cccc1Cl)c1c(-c2ccccc2)[nH]c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-481423226194464382ed5e4c678c6fee
CNC.Clc1ccc(-c2cc3ccccc3[nH]2)cc1.O=Cc1c(F)cccc1Cl>>CN(C)C(c1c(F)cccc1Cl)c1c(-c2ccc(Cl)cc2)[nH]c2ccccc12
ClC1=CC=C(C=C1)C=1NC2=CC=CC=C2C1.[Cl-].ClC1=C(C=[N+](C)C)C(=CC=C1)F.ClC1=C(C=O)C(=CC=C1)F.CNC>>ClC1=C(C(=CC=C1)F)C(C1=C(NC2=CC=CC=C12)C1=CC=C(C=C1)Cl)N(C)C
[CH3:1][NH:2][CH3:3].[cH:13]1[c:14](-[c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][cH:21]2)[nH:22][c:23]2[cH:24][cH:25][cH:26][cH:27][c:28]12.O=[CH:4][c:5]1[c:6]([F:7])[cH:8][cH:9][cH:10][c:11]1[Cl:12]>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[c:6]([F:7])[cH:8][cH:9][cH:10][c:11]1[Cl:12])[c:13]1[c:14](-[c:15]2[cH:16][cH:17][c:...
CNC.Clc1ccc(-c2cc3ccccc3[nH]2)cc1.O=Cc1c(F)cccc1Cl
CN(C)C(c1c(F)cccc1Cl)c1c(-c2ccc(Cl)cc2)[nH]c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c(-c3ccccc3)[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:9](-[c:8]):[#7;a:10]:[c:11](:[c:12]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-(4-chlorophenyl)-indole and (2-chloro-6-fluoro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 2-chloro-6-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.p...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.Clc1ccc(-c2cc3ccccc3[nH]2)cc1.O=Cc1c(F)cccc1Cl>>CN(C)C(c1c(F)cccc1Cl)c1c(-c2ccc(Cl)cc2)[nH]c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f731be15c2084b7ab542d00f6022ab25
CNC.Cn1ccc2ccccc21.O=Cc1c(F)cccc1Cl>>CN(C)C(c1c(F)cccc1Cl)c1cn(C)c2ccccc12
CN1C=CC2=CC=CC=C12.[Cl-].ClC1=C(C=[N+](C)C)C(=CC=C1)F.ClC1=C(C=O)C(=CC=C1)F.CNC>>ClC1=C(C(=CC=C1)F)C(C1=CN(C2=CC=CC=C12)C)N(C)C
[CH3:1][NH:2][CH3:3].[cH:13]1[cH:14][n:15]([CH3:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12.O=[CH:4][c:5]1[c:6]([F:7])[cH:8][cH:9][cH:10][c:11]1[Cl:12]>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[c:6]([F:7])[cH:8][cH:9][cH:10][c:11]1[Cl:12])[c:13]1[cH:14][n:15]([CH3:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12
CNC.Cn1ccc2ccccc21.O=Cc1c(F)cccc1Cl
CN(C)C(c1c(F)cccc1Cl)c1cn(C)c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
05894bd812613f52cf9c1620f3154e6ca08db53b10e13d8864b239f8fa88e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[cH;D2;+0:8]:[c:9](:[c:10]):[c:11]:1:[c:12].[C;D1;H3:13]-[NH;D2;+0:14]-[C;D1;H3:15]>>[C;D1;H3:5]-[#7;a:6]1:[c:7]:[c;H0;D3;+0:8](-[CH;D3;+0:1](-[N;H0;D3;+0:14](-[C;D1;H3:13])-[C;D1;H3:15])-[c:2](:[c:3]):[c:4]):[c:9](:[c:10]):[c:11]:1:[c:12]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-methylindole and (2-chloro-6-fluoro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 2-chloro-6-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_de...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12
HO-
null
null
null
CNC.Cn1ccc2ccccc21.O=Cc1c(F)cccc1Cl>>CN(C)C(c1c(F)cccc1Cl)c1cn(C)c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a0d8c1eff92f4c29b36ecbd3a0dc11aa
CNC.Cn1ccc2ccccc21.O=Cc1cccc(Cl)c1>>CN(C)C(c1cccc(Cl)c1)c1cn(C)c2ccccc12
CN1C=CC2=CC=CC=C12.[Cl-].ClC=1C=C(C=[N+](C)C)C=CC1.ClC=1C=C(C=O)C=CC1.CNC>>ClC=1C=C(C=CC1)C(C1=CN(C2=CC=CC=C12)C)N(C)C
[CH3:1][NH:2][CH3:3].[cH:12]1[cH:13][n:14]([CH3:15])[c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]12.O=[CH:4][c:5]1[cH:6][cH:7][cH:8][c:9]([Cl:10])[cH:11]1>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][cH:8][c:9]([Cl:10])[cH:11]1)[c:12]1[cH:13][n:14]([CH3:15])[c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]12
CNC.Cn1ccc2ccccc21.O=Cc1cccc(Cl)c1
CN(C)C(c1cccc(Cl)c1)c1cn(C)c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
05894bd812613f52cf9c1620f3154e6ca08db53b10e13d8864b239f8fa88e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[cH;D2;+0:8]:[c:9](:[c:10]):[c:11]:1:[c:12].[C;D1;H3:13]-[NH;D2;+0:14]-[C;D1;H3:15]>>[C;D1;H3:5]-[#7;a:6]1:[c:7]:[c;H0;D3;+0:8](-[CH;D3;+0:1](-[N;H0;D3;+0:14](-[C;D1;H3:13])-[C;D1;H3:15])-[c:2](:[c:3]):[c:4]):[c:9](:[c:10]):[c:11]:1:[c:12]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-methylindole and (3-chloro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 3-chloro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12
HO-
null
null
null
CNC.Cn1ccc2ccccc21.O=Cc1cccc(Cl)c1>>CN(C)C(c1cccc(Cl)c1)c1cn(C)c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e628563da2734892a93257119bfd4b8e
CNC.C[N+](C)=Cc1cccc(Cl)c1Cl.Cn1ccc2ccccc21>>CN(C)C(c1cccc(Cl)c1Cl)c1cn(C)c2ccccc12
CN1C=CC2=CC=CC=C12.[Cl-].ClC1=C(C=[N+](C)C)C=CC=C1Cl.ClC1=C(C=O)C=CC=C1Cl.CNC>>ClC1=C(C=CC=C1Cl)C(C1=CN(C2=CC=CC=C12)C)N(C)C
[CH3:1][NH:2][CH3:3].C[N+](C)=[CH:4][c:5]1[cH:6][cH:7][cH:8][c:9]([Cl:10])[c:11]1[Cl:12].[cH:13]1[cH:14][n:15]([CH3:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][cH:8][c:9]([Cl:10])[c:11]1[Cl:12])[c:13]1[cH:14][n:15]([CH3:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12
CNC.C[N+](C)=Cc1cccc(Cl)c1Cl.Cn1ccc2ccccc21
CN(C)C(c1cccc(Cl)c1Cl)c1cn(C)c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
85aaf23583cdcf64b6fe54d87d17427b47bda7376efe96f2fd1dd9ad1df13e69
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[cH;D2;+0:8]:[c:9](:[c:10]):[c:11]:1:[c:12].[C;D1;H3:13]-[NH;D2;+0:14]-[C;D1;H3:15]>>[C;D1;H3:5]-[#7;a:6]1:[c:7]:[c;H0;D3;+0:8](-[CH;D3;+0:1](-[N;H0;D3;+0:14](-[C;D1;H3:13])-[C;D1;H3:15])-[c:2](:[c:3]):[c:4]):[c:9](:[c:10]):[c:11]:1:[c:12]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-methylindole and (2,3-dichloro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 2,3-dichloro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12
Other
null
null
null
CNC.C[N+](C)=Cc1cccc(Cl)c1Cl.Cn1ccc2ccccc21>>CN(C)C(c1cccc(Cl)c1Cl)c1cn(C)c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a77eb8032c0644bdbcdf6b13a2b295cc
CNC.Cn1ccc2ccccc21.O=Cc1ccc(Cl)cc1Cl>>CN(C)C(c1ccc(Cl)cc1Cl)c1cn(C)c2ccccc12
CN1C=CC2=CC=CC=C12.[Cl-].ClC1=C(C=[N+](C)C)C=CC(=C1)Cl.ClC1=C(C=O)C=CC(=C1)Cl.CNC>>ClC1=C(C=CC(=C1)Cl)C(C1=CN(C2=CC=CC=C12)C)N(C)C
[CH3:1][NH:2][CH3:3].[cH:13]1[cH:14][n:15]([CH3:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12.O=[CH:4][c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][c:11]1[Cl:12]>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][c:11]1[Cl:12])[c:13]1[cH:14][n:15]([CH3:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12
CNC.Cn1ccc2ccccc21.O=Cc1ccc(Cl)cc1Cl
CN(C)C(c1ccc(Cl)cc1Cl)c1cn(C)c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
05894bd812613f52cf9c1620f3154e6ca08db53b10e13d8864b239f8fa88e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[cH;D2;+0:8]:[c:9](:[c:10]):[c:11]:1:[c:12].[C;D1;H3:13]-[NH;D2;+0:14]-[C;D1;H3:15]>>[C;D1;H3:5]-[#7;a:6]1:[c:7]:[c;H0;D3;+0:8](-[CH;D3;+0:1](-[N;H0;D3;+0:14](-[C;D1;H3:13])-[C;D1;H3:15])-[c:2](:[c:3]):[c:4]):[c:9](:[c:10]):[c:11]:1:[c:12]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-methylindole and (2,4-dichloro-benzylidene)-dimethyl-ammonium chloride, which had been prepared in accordance with example 24 from 2,4-dichloro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12
HO-
null
null
null
CNC.Cn1ccc2ccccc21.O=Cc1ccc(Cl)cc1Cl>>CN(C)C(c1ccc(Cl)cc1Cl)c1cn(C)c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-599298268d6341939a695a9b3cc6a7f0
CC(C)(C)c1ccc(C=O)cc1.CCn1c(-c2ccccc2)cc2ccccc21.CNC>>CCn1c(-c2ccccc2)c(C(c2ccc(C(C)(C)C)cc2)N(C)C)c2ccccc21
C(C)N1C(=CC2=CC=CC=C12)C1=CC=CC=C1.[Cl-].C(C)(C)(C)C1=CC=C(C=[N+](C)C)C=C1.C(C)(C)(C)C1=CC=C(C=O)C=C1.CNC>>C(C)(C)(C)C1=CC=C(C=C1)C(C1=C(N(C2=CC=CC=C12)CC)C1=CC=CC=C1)N(C)C
O=[CH:12][c:13]1[cH:14][cH:15][c:16]([C:17]([CH3:18])([CH3:19])[CH3:20])[cH:21][cH:22]1.[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[cH:11][c:26]2[cH:27][cH:28][cH:29][cH:30][c:31]12.[NH:23]([CH3:24])[CH3:25]>>[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[c:11]([CH:12]([c:13]2...
CC(C)(C)c1ccc(C=O)cc1.CCn1c(-c2ccccc2)cc2ccccc21.CNC
CCn1c(-c2ccccc2)c(C(c2ccc(C(C)(C)C)cc2)N(C)C)c2ccccc21
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
bec24864ceecfec904d98640b3bb3caa9d35fa656dcbdac3c55c0dacb43b50eb
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c(-c3ccccc3)[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C:8]-[#7;a:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[cH;D2;+0:14]:[c:15]:1-[c:16]>>[C:8]-[#7;a:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[c;H0;D3;+0:14](-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]):[c:15]:1-[c:16]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-ethyl-2-phenyl-1H-indole and (4-tert-butyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 4-tert-butylbenzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_de...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1cc2ccccc2[nH]1
c1cc2ccccc2[nH]1
c1ccccc1.c1ccccc1.c1cc2ccccc2[nH]1
HO-
null
null
null
CC(C)(C)c1ccc(C=O)cc1.CCn1c(-c2ccccc2)cc2ccccc21.CNC>>CCn1c(-c2ccccc2)c(C(c2ccc(C(C)(C)C)cc2)N(C)C)c2ccccc21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f9cc66bc533c45fc829f8836d582b65f
CNC.Cc1cc2ccccc2[nH]1.O=Cc1ccc(F)cc1Cl>>Cc1[nH]c2ccccc2c1C(c1ccc(F)cc1Cl)N(C)C
CC=1NC2=CC=CC=C2C1.[Cl-].ClC1=C(C=[N+](C)C)C=CC(=C1)F.ClC1=C(C=O)C=CC(=C1)F.CNC>>ClC1=C(C=CC(=C1)F)C(C1=C(NC2=CC=CC=C12)C)N(C)C
[NH:20]([CH3:21])[CH3:22].[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[cH:10]1.O=[CH:11][c:12]1[cH:13][cH:14][c:15]([F:16])[cH:17][c:18]1[Cl:19]>>[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10]1[CH:11]([c:12]1[cH:13][cH:14][c:15]([F:16])[cH:17][c:18]1[Cl:19])[N:20]([CH3:21])[CH3:22]
CNC.Cc1cc2ccccc2[nH]1.O=Cc1ccc(F)cc1Cl
Cc1[nH]c2ccccc2c1C(c1ccc(F)cc1Cl)N(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[c;H0;D3;+0:15]:1-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-methyl-1H-indole and (2-chloro-4-fluoro-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-chloro-4-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
null
null
null
CNC.Cc1cc2ccccc2[nH]1.O=Cc1ccc(F)cc1Cl>>Cc1[nH]c2ccccc2c1C(c1ccc(F)cc1Cl)N(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f85e5808d5ab42c3a61017baad9dc05f
CNC.Cc1cc2ccccc2[nH]1.O=Cc1c(F)cccc1Cl>>Cc1[nH]c2ccccc2c1C(c1c(F)cccc1Cl)N(C)C
CC=1NC2=CC=CC=C2C1.[Cl-].ClC1=C(C=[N+](C)C)C(=CC=C1)F.ClC1=C(C=O)C(=CC=C1)F.CNC>>ClC1=C(C(=CC=C1)F)C(C1=C(NC2=CC=CC=C12)C)N(C)C
[NH:20]([CH3:21])[CH3:22].[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[cH:10]1.O=[CH:11][c:12]1[c:13]([F:14])[cH:15][cH:16][cH:17][c:18]1[Cl:19]>>[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10]1[CH:11]([c:12]1[c:13]([F:14])[cH:15][cH:16][cH:17][c:18]1[Cl:19])[N:20]([CH3:21])[CH3:22]
CNC.Cc1cc2ccccc2[nH]1.O=Cc1c(F)cccc1Cl
Cc1[nH]c2ccccc2c1C(c1c(F)cccc1Cl)N(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[c;H0;D3;+0:15]:1-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-methyl-1H-indole and (2-chloro-6-fluoro-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-chloro-6-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
null
null
null
CNC.Cc1cc2ccccc2[nH]1.O=Cc1c(F)cccc1Cl>>Cc1[nH]c2ccccc2c1C(c1c(F)cccc1Cl)N(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-587b5a90563d478ba07650bd7b8c540a
CNC.COc1cccc(C=O)c1OC.O=[N+]([O-])c1cccc2[nH]ccc12>>COc1cccc(C(c2c[nH]c3cccc([N+](=O)[O-])c23)N(C)C)c1OC
[N+](=O)([O-])C1=C2C=CNC2=CC=C1.[Cl-].COC1=C(C=[N+](C)C)C=CC=C1OC.COC1=C(C=O)C=CC=C1OC.CNC>>COC1=C(C=CC=C1OC)C(C1=CNC2=CC=CC(=C12)[N+](=O)[O-])N(C)C
[NH:21]([CH3:22])[CH3:23].O=[CH:8][c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:24]1[O:25][CH3:26].[cH:9]1[cH:10][nH:11][c:12]2[cH:13][cH:14][cH:15][c:16]([N+:17](=[O:18])[O-:19])[c:20]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH:8]([c:9]2[cH:10][nH:11][c:12]3[cH:13][cH:14][cH:15][c:16]([N+:17](=[O:18])[O-:19])[c:...
CNC.COc1cccc(C=O)c1OC.O=[N+]([O-])c1cccc2[nH]ccc12
COc1cccc(C(c2c[nH]c3cccc([N+](=O)[O-])c23)N(C)C)c1OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 4-nitro-1H-indole and (2,3-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2,3-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.COc1cccc(C=O)c1OC.O=[N+]([O-])c1cccc2[nH]ccc12>>COc1cccc(C(c2c[nH]c3cccc([N+](=O)[O-])c23)N(C)C)c1OC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-354e6617f7a94d3ab81859a0b3502e64
CNC.COc1cccc(C=[N+](C)C)c1OC.O=C(O)c1ccc2cc[nH]c2c1>>COc1cccc(C(c2c[nH]c3c2CC=C(C(=O)O)C3)N(C)C)c1OC
N1C=CC2=CC=C(C=C12)C(=O)O.[Cl-].COC1=C(C=[N+](C)C)C=CC=C1OC.COC1=C(C=O)C=CC=C1OC.CNC>>COC1=C(C=CC=C1OC)C(C1=CNC=2CC(=CCC12)C(=O)O)N(C)C
[NH:21]([CH3:22])[CH3:23].C[N+](C)=[CH:8][c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:24]1[O:25][CH3:26].[cH:9]1[cH:10][nH:11][c:12]2[c:13]1[cH:14][cH:15][c:16]([C:17](=[O:18])[OH:19])[cH:20]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH:8]([c:9]2[cH:10][nH:11][c:12]3[c:13]2[CH2:14][CH:15]=[C:16]([C:17](=[O:18])[OH:...
CNC.COc1cccc(C=[N+](C)C)c1OC.O=C(O)c1ccc2cc[nH]c2c1
COc1cccc(C(c2c[nH]c3c2CC=C(C(=O)O)C3)N(C)C)c1OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
3679d5ed704df7b735c63b1b3947eed592489fe8de1a08e47fd7328e6b27130f
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
C1=CCc2c(Cc3ccccc3)c[nH]c2C1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[O;D1;H0:8]=[C:9](-[O;D1;H1:10])-[c;H0;D3;+0:11]1:[cH;D2;+0:12]:[cH;D2;+0:13]:[c:14]2:[cH;D2;+0:15]:[c:16]:[#7;a:17]:[c:18]:2:[cH;D2;+0:19]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:...
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1H-indole-6-carboxylic acid and (2,3-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2,3-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedur...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
C1=CCc2[nH]ccc2C1
c1ccccc1.C1=CCc2[nH]ccc2C1
Other
null
null
null
CNC.COc1cccc(C=[N+](C)C)c1OC.O=C(O)c1ccc2cc[nH]c2c1>>COc1cccc(C(c2c[nH]c3c2CC=C(C(=O)O)C3)N(C)C)c1OC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-df37569297e741cf9e39494a4a08895e
CNC.COc1ccc(C=[N+](C)C)cc1OC.Cc1cc2ccccc2[nH]1>>COc1ccc(C(c2c(C)[nH]c3ccccc23)N(C)C)cc1OC
CC=1NC2=CC=CC=C2C1.[Cl-].COC=1C=C(C=[N+](C)C)C=CC1OC.COC=1C=C(C=O)C=CC1OC.CNC>>COC=1C=C(C=CC1OC)C(C1=C(NC2=CC=CC=C12)C)N(C)C
[NH:18]([CH3:19])[CH3:20].C[N+](C)=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:22]([O:23][CH3:24])[cH:21]1.[cH:8]1[c:9]([CH3:10])[nH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([c:8]2[c:9]([CH3:10])[nH:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]23)[N:18]([CH3:19])[CH3:2...
CNC.COc1ccc(C=[N+](C)C)cc1OC.Cc1cc2ccccc2[nH]1
COc1ccc(C(c2c(C)[nH]c3ccccc23)N(C)C)cc1OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4aae3a4ea1be485aab9d544da9fceb1ce060e1d3dd462597adbb05c8cde19188
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[c;H0;D3;+0:15]:1-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-methyl-1H-indole and (3,4-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3,4-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
Other
null
null
null
CNC.COc1ccc(C=[N+](C)C)cc1OC.Cc1cc2ccccc2[nH]1>>COc1ccc(C(c2c(C)[nH]c3ccccc23)N(C)C)cc1OC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-26a3da5fe37a4979bafcc20f4b60700f
CNC.COc1ccc(C=[N+](C)C)cc1OC.Clc1ccc(-c2cc3ccccc3[nH]2)cc1>>COc1ccc(C(c2c(-c3ccc(Cl)cc3)[nH]c3ccccc23)N(C)C)cc1OC
ClC1=CC=C(C=C1)C=1NC2=CC=CC=C2C1.[Cl-].COC=1C=C(C=[N+](C)C)C=CC1OC.COC=1C=C(C=O)C=CC1OC.CNC>>ClC1=CC=C(C=C1)C=1NC2=CC=CC=C2C1C(C1=CC(=C(C=C1)OC)OC)N(C)C
[NH:24]([CH3:25])[CH3:26].C[N+](C)=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:28]([O:29][CH3:30])[cH:27]1.[cH:8]1[c:9](-[c:10]2[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]2)[nH:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([c:8]2[c:9](-[c:10]3[cH:11][cH:12][c:13]([Cl:14])[...
CNC.COc1ccc(C=[N+](C)C)cc1OC.Clc1ccc(-c2cc3ccccc3[nH]2)cc1
COc1ccc(C(c2c(-c3ccc(Cl)cc3)[nH]c3ccccc23)N(C)C)cc1OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4aae3a4ea1be485aab9d544da9fceb1ce060e1d3dd462597adbb05c8cde19188
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c(-c3ccccc3)[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:13](:[c:14]):[c:11](:[c:12]):[#7;a:10]:[c:9]:1-[c:8]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-(4-chloro-phenyl)-1H-indole and (3,4-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3,4-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.proced...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
Other
null
null
null
CNC.COc1ccc(C=[N+](C)C)cc1OC.Clc1ccc(-c2cc3ccccc3[nH]2)cc1>>COc1ccc(C(c2c(-c3ccc(Cl)cc3)[nH]c3ccccc23)N(C)C)cc1OC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8a5d2aadeeab4a9e83db1bfb5536dadd
CCn1c(-c2ccccc2)cc2ccccc21.CNC.COc1ccc(C=O)cc1OC>>CCn1c(-c2ccccc2)c(C(c2ccc(OC)c(OC)c2)N(C)C)c2ccccc21
C(C)N1C(=CC2=CC=CC=C12)C1=CC=CC=C1.[Cl-].COC=1C=C(C=[N+](C)C)C=CC1OC.COC=1C=C(C=O)C=CC1OC.CNC>>COC=1C=C(C=CC1OC)C(C1=C(N(C2=CC=CC=C12)CC)C1=CC=CC=C1)N(C)C
[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[cH:11][c:26]2[cH:27][cH:28][cH:29][cH:30][c:31]12.[NH:23]([CH3:24])[CH3:25].O=[CH:12][c:13]1[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([O:20][CH3:21])[cH:22]1>>[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[c:11]([CH:12]([c:13]2[cH:1...
CCn1c(-c2ccccc2)cc2ccccc21.CNC.COc1ccc(C=O)cc1OC
CCn1c(-c2ccccc2)c(C(c2ccc(OC)c(OC)c2)N(C)C)c2ccccc21
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
bec24864ceecfec904d98640b3bb3caa9d35fa656dcbdac3c55c0dacb43b50eb
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c(-c3ccccc3)[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C:8]-[#7;a:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[cH;D2;+0:14]:[c:15]:1-[c:16]>>[C:8]-[#7;a:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[c;H0;D3;+0:14](-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]):[c:15]:1-[c:16]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-ethyl-2-phenyl-1H-indole and (3,4-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3,4-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1cc2ccccc2[nH]1
c1cc2ccccc2[nH]1
c1ccccc1.c1ccccc1.c1cc2ccccc2[nH]1
HO-
null
null
null
CCn1c(-c2ccccc2)cc2ccccc21.CNC.COc1ccc(C=O)cc1OC>>CCn1c(-c2ccccc2)c(C(c2ccc(OC)c(OC)c2)N(C)C)c2ccccc21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e111e89002764368b426e6c6cee9123f
CCc1cccc2cc[nH]c12.CNC.COc1ccc(C=[N+](C)C)cc1OC>>CCc1cccc2c(C(c3ccc(OC)c(OC)c3)N(C)C)c[nH]c12
C(C)C=1C=CC=C2C=CNC12.[Cl-].COC=1C=C(C=[N+](C)C)C=CC1OC.COC=1C=C(C=O)C=CC1OC.CNC>>COC=1C=C(C=CC1OC)C(C1=CNC2=C(C=CC=C12)CC)N(C)C
[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[cH:8][cH:23][nH:24][c:25]12.[NH:20]([CH3:21])[CH3:22].C[N+](C)=[CH:9][c:10]1[cH:11][cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[cH:19]1>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]([CH:9]([c:10]3[cH:11][cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[cH:19]3)...
CCc1cccc2cc[nH]c12.CNC.COc1ccc(C=[N+](C)C)cc1OC
CCc1cccc2c(C(c3ccc(OC)c(OC)c3)N(C)C)c[nH]c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4aae3a4ea1be485aab9d544da9fceb1ce060e1d3dd462597adbb05c8cde19188
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 7-ethyl-1H-indole and (3,4-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3,4-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
Other
null
null
null
CCc1cccc2cc[nH]c12.CNC.COc1ccc(C=[N+](C)C)cc1OC>>CCc1cccc2c(C(c3ccc(OC)c(OC)c3)N(C)C)c[nH]c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0154d7bb83be47f2abfe9ae53b6686d5
CNC.COc1ccc(C=[N+](C)C)cc1OC.Cn1ccc2ccccc21>>COc1ccc(C(c2cn(C)c3ccccc23)N(C)C)cc1OC
CN1C=CC2=CC=CC=C12.[Cl-].COC=1C=C(C=[N+](C)C)C=CC1OC.COC=1C=C(C=O)C=CC1OC.CNC>>COC=1C=C(C=CC1OC)C(C1=CN(C2=CC=CC=C12)C)N(C)C
[NH:18]([CH3:19])[CH3:20].C[N+](C)=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:22]([O:23][CH3:24])[cH:21]1.[cH:8]1[cH:9][n:10]([CH3:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([c:8]2[cH:9][n:10]([CH3:11])[c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]23)[N:18]([CH3:19])[CH3:2...
CNC.COc1ccc(C=[N+](C)C)cc1OC.Cn1ccc2ccccc21
COc1ccc(C(c2cn(C)c3ccccc23)N(C)C)cc1OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
85aaf23583cdcf64b6fe54d87d17427b47bda7376efe96f2fd1dd9ad1df13e69
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[cH;D2;+0:8]:[c:9](:[c:10]):[c:11]:1:[c:12].[C;D1;H3:13]-[NH;D2;+0:14]-[C;D1;H3:15]>>[C;D1;H3:5]-[#7;a:6]1:[c:7]:[c;H0;D3;+0:8](-[CH;D3;+0:1](-[N;H0;D3;+0:14](-[C;D1;H3:13])-[C;D1;H3:15])-[c:2](:[c:3]):[c:4]):[c:9](:[c:10]):[c:11]:1:[c:12]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-methyl-1H-indole and (3,4-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3,4-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12
Other
null
null
null
CNC.COc1ccc(C=[N+](C)C)cc1OC.Cn1ccc2ccccc21>>COc1ccc(C(c2cn(C)c3ccccc23)N(C)C)cc1OC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-17043a3bab16407eb42e2bd7bcec8beb
CNC.COc1ccc(C=[N+](C)C)cc1OC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1>>COc1ccc(C(c2c(-c3ccc(F)cc3)[nH]c3ccccc23)N(C)C)cc1OC
FC1=CC=C(C=C1)C=1NC2=CC=CC=C2C1.[Cl-].COC=1C=C(C=[N+](C)C)C=CC1OC.COC=1C=C(C=O)C=CC1OC.CNC>>COC=1C=C(C=CC1OC)C(C1=C(NC2=CC=CC=C12)C1=CC=C(C=C1)F)N(C)C
[NH:24]([CH3:25])[CH3:26].C[N+](C)=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:28]([O:29][CH3:30])[cH:27]1.[cH:8]1[c:9](-[c:10]2[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]2)[nH:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([c:8]2[c:9](-[c:10]3[cH:11][cH:12][c:13]([F:14])[cH...
CNC.COc1ccc(C=[N+](C)C)cc1OC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1
COc1ccc(C(c2c(-c3ccc(F)cc3)[nH]c3ccccc23)N(C)C)cc1OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4aae3a4ea1be485aab9d544da9fceb1ce060e1d3dd462597adbb05c8cde19188
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c(-c3ccccc3)[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:13](:[c:14]):[c:11](:[c:12]):[#7;a:10]:[c:9]:1-[c:8]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-(4-fluoro-phenyl)-1H-indole and (3,4-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3,4-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.proced...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
Other
null
null
null
CNC.COc1ccc(C=[N+](C)C)cc1OC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1>>COc1ccc(C(c2c(-c3ccc(F)cc3)[nH]c3ccccc23)N(C)C)cc1OC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8fb4a0784c5e46a29b0b5a6f2dcabd3f
CNC.COc1ccc(C=[N+](C)C)cc1OC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1Cl>>COc1ccc(C(c2c(-c3ccc(F)c(Cl)c3)[nH]c3ccccc23)N(C)C)cc1OC
ClC=1C=C(C=CC1F)C=1NC2=CC=CC=C2C1.[Cl-].COC=1C=C(C=[N+](C)C)C=CC1OC.COC=1C=C(C=O)C=CC1OC.CNC>>ClC=1C=C(C=CC1F)C=1NC2=CC=CC=C2C1C(C1=CC(=C(C=C1)OC)OC)N(C)C
[NH:25]([CH3:26])[CH3:27].C[N+](C)=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:29]([O:30][CH3:31])[cH:28]1.[cH:8]1[c:9](-[c:10]2[cH:11][cH:12][c:13]([F:14])[c:15]([Cl:16])[cH:17]2)[nH:18][c:19]2[cH:20][cH:21][cH:22][cH:23][c:24]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([c:8]2[c:9](-[c:10]3[cH:11][cH:12][c:13]([F...
CNC.COc1ccc(C=[N+](C)C)cc1OC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1Cl
COc1ccc(C(c2c(-c3ccc(F)c(Cl)c3)[nH]c3ccccc23)N(C)C)cc1OC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4aae3a4ea1be485aab9d544da9fceb1ce060e1d3dd462597adbb05c8cde19188
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c(-c3ccccc3)[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:13](:[c:14]):[c:11](:[c:12]):[#7;a:10]:[c:9]:1-[c:8]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-(3-chloro-4-fluoro-phenyl)-1H-indole and (3,4-dimethoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3,4-dimethoxy-benzaldehyde and dimethylamine. Conditions: See reaction.not...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
Other
null
null
null
CNC.COc1ccc(C=[N+](C)C)cc1OC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1Cl>>COc1ccc(C(c2c(-c3ccc(F)c(Cl)c3)[nH]c3ccccc23)N(C)C)cc1OC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-050cdd945ea044439f3df802c5f31ea6
CNC.Clc1ccc2[nH]ccc2c1.O=Cc1ccccc1F>>CN(C)C(c1ccccc1F)c1c[nH]c2ccc(Cl)cc12
ClC=1C=C2C=CNC2=CC1.[Cl-].FC1=C(C=[N+](C)C)C=CC=C1.FC1=C(C=O)C=CC=C1.CNC>>ClC=1C=C2C(=CNC2=CC1)C(C1=C(C=CC=C1)F)N(C)C
[CH3:1][NH:2][CH3:3].[cH:12]1[cH:13][nH:14][c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][c:21]12.O=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[F:11]>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[F:11])[c:12]1[cH:13][nH:14][c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][c:21]12
CNC.Clc1ccc2[nH]ccc2c1.O=Cc1ccccc1F
CN(C)C(c1ccccc1F)c1c[nH]c2ccc(Cl)cc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 5-chloro-1H-indole and (2-fluoro-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.Clc1ccc2[nH]ccc2c1.O=Cc1ccccc1F>>CN(C)C(c1ccccc1F)c1c[nH]c2ccc(Cl)cc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e8415c5d0b5f45968db469e1e4e5f5f1
CNC.Cc1cccc2[nH]ccc12.O=Cc1ccc(F)cc1>>Cc1cccc2[nH]cc(C(c3ccc(F)cc3)N(C)C)c12
CC1=C2C=CNC2=CC=C1.[Cl-].FC1=CC=C(C=[N+](C)C)C=C1.FC1=CC=C(C=O)C=C1.CNC>>FC1=CC=C(C=C1)C(C1=CNC2=CC=CC(=C12)C)N(C)C
[NH:18]([CH3:19])[CH3:20].[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[nH:7][cH:8][cH:9][c:21]12.O=[CH:10][c:11]1[cH:12][cH:13][c:14]([F:15])[cH:16][cH:17]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[nH:7][cH:8][c:9]([CH:10]([c:11]3[cH:12][cH:13][c:14]([F:15])[cH:16][cH:17]3)[N:18]([CH3:19])[CH3:20])[c:21]12
CNC.Cc1cccc2[nH]ccc12.O=Cc1ccc(F)cc1
Cc1cccc2[nH]cc(C(c3ccc(F)cc3)N(C)C)c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[cH;D2;+0:10]:[c:11]:[#7;a:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:10]1:[c:11]:[#7;a:12]:[c:13](:[c:14]):[c:9]:1:[c:8]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 4-methyl-1H-indole and (4-fluoro-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 4-fluoro-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
null
null
null
CNC.Cc1cccc2[nH]ccc12.O=Cc1ccc(F)cc1>>Cc1cccc2[nH]cc(C(c3ccc(F)cc3)N(C)C)c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f851d4fe74e1437ea8d21be3e4172a3c
CCc1cccc2cc[nH]c12.CNC.COc1ccccc1C=O>>CCc1cccc2c(C(c3ccccc3OC)N(C)C)c[nH]c12
C(C)C=1C=CC=C2C=CNC12.[Cl-].COC1=C(C=[N+](C)C)C=CC=C1.COC1=C(C=O)C=CC=C1.CNC>>C(C)C=1C=CC=C2C(=CNC12)C(C1=C(C=CC=C1)OC)N(C)C
[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[cH:8][cH:21][nH:22][c:23]12.[NH:18]([CH3:19])[CH3:20].O=[CH:9][c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[O:16][CH3:17]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]([CH:9]([c:10]3[cH:11][cH:12][cH:13][cH:14][c:15]3[O:16][CH3:17])[N:18]([CH3:19])[CH3:20])[cH:21][nH:22][c...
CCc1cccc2cc[nH]c12.CNC.COc1ccccc1C=O
CCc1cccc2c(C(c3ccccc3OC)N(C)C)c[nH]c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 7-ethyl-1H-indole and (2-methoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-methoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CCc1cccc2cc[nH]c12.CNC.COc1ccccc1C=O>>CCc1cccc2c(C(c3ccccc3OC)N(C)C)c[nH]c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d2e25ad230874e0884226fde176b5733
Cc1cc2ccccc2[nH]1.Cc1ccccc1C=[N+](C)C>>Cc1ccccc1C(c1c(C)[nH]c2ccccc12)N(C)C
CC=1NC2=CC=CC=C2C1.[Cl-].CC1=C(C=[N+](C)C)C=CC=C1.CC1=C(C=O)C=CC=C1.CNC>>CN(C(C1=C(C=CC=C1)C)C1=C(NC2=CC=CC=C12)C)C
[cH:9]1[c:10]([CH3:11])[nH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12.[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH:8]=[N+:19]([CH3:20])[CH3:21]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH:8]([c:9]1[c:10]([CH3:11])[nH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12)[N:19]([CH3:20])[CH3:21]
Cc1cc2ccccc2[nH]1.Cc1ccccc1C=[N+](C)C
Cc1ccccc1C(c1c(C)[nH]c2ccccc12)N(C)C
null
null
null
C-C Coupling
OtherReaction
6f78ebae7a6e5f9c15e0d6ab78f58f64a17b670729ecfc39fbb9b9e11c788fae
5c03404e5740858973798689d4be0a8ed62608f5043e578ba3cd6de4363e2dbe
c1ccc(Cc2c[nH]c3ccccc23)cc1
[C;D1;H3:1]-[N+;H0;D3:2](-[C;D1;H3:3])=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[c;H0;D3;+0:15]:1-[CH;D3;+0:4](-[N;H0;D3;+0:2](-[C;D1;H3:1])-[C;D1;H3:3])-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-methyl-1H-indole and (2-methyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-methyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
null
null
null
null
Cc1cc2ccccc2[nH]1.Cc1ccccc1C=[N+](C)C>>Cc1ccccc1C(c1c(C)[nH]c2ccccc12)N(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-867d92e2aac34594979eadeda21ac344
CCc1cccc2cc[nH]c12.CNC.Cc1ccccc1C=O>>CCc1cccc2c(C(c3ccccc3C)N(C)C)c[nH]c12
C(C)C=1C=CC=C2C=CNC12.[Cl-].CC1=C(C=[N+](C)C)C=CC=C1.CC1=C(C=O)C=CC=C1.CNC>>C(C)C=1C=CC=C2C(=CNC12)C(C1=C(C=CC=C1)C)N(C)C
[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[cH:8][cH:20][nH:21][c:22]12.[NH:17]([CH3:18])[CH3:19].O=[CH:9][c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[CH3:16]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]([CH:9]([c:10]3[cH:11][cH:12][cH:13][cH:14][c:15]3[CH3:16])[N:17]([CH3:18])[CH3:19])[cH:20][nH:21][c:22]12
CCc1cccc2cc[nH]c12.CNC.Cc1ccccc1C=O
CCc1cccc2c(C(c3ccccc3C)N(C)C)c[nH]c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 7-ethyl-1H-indole and (2-methyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-methyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CCc1cccc2cc[nH]c12.CNC.Cc1ccccc1C=O>>CCc1cccc2c(C(c3ccccc3C)N(C)C)c[nH]c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9f30dee72cee4b8e950846dc191f7f87
CNC.Cc1ccccc1C=O.Cn1ccc2ccccc21>>Cc1ccccc1C(c1cn(C)c2ccccc12)N(C)C
CN1C=CC2=CC=CC=C12.[Cl-].CC1=C(C=[N+](C)C)C=CC=C1.CC1=C(C=O)C=CC=C1.CNC>>CN(C(C1=C(C=CC=C1)C)C1=CN(C2=CC=CC=C12)C)C
[NH:19]([CH3:20])[CH3:21].O=[CH:8][c:7]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]1.[cH:9]1[cH:10][n:11]([CH3:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH:8]([c:9]1[cH:10][n:11]([CH3:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12)[N:19]([CH3:20])[CH3:21]
CNC.Cc1ccccc1C=O.Cn1ccc2ccccc21
Cc1ccccc1C(c1cn(C)c2ccccc12)N(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
05894bd812613f52cf9c1620f3154e6ca08db53b10e13d8864b239f8fa88e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[cH;D2;+0:8]:[c:9](:[c:10]):[c:11]:1:[c:12].[C;D1;H3:13]-[NH;D2;+0:14]-[C;D1;H3:15]>>[C;D1;H3:5]-[#7;a:6]1:[c:7]:[c;H0;D3;+0:8](-[CH;D3;+0:1](-[N;H0;D3;+0:14](-[C;D1;H3:13])-[C;D1;H3:15])-[c:2](:[c:3]):[c:4]):[c:9](:[c:10]):[c:11]:1:[c:12]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-methyl-1H-indole and (2-methyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-methyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1c[nH]c2ccccc12
HO-
null
null
null
CNC.Cc1ccccc1C=O.Cn1ccc2ccccc21>>Cc1ccccc1C(c1cn(C)c2ccccc12)N(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2d8fffeb348e41d1964f1f9400476c80
CNC.Cc1ccccc1C=O.Clc1ccc2[nH]ccc2c1>>Cc1ccccc1C(c1c[nH]c2ccc(Cl)cc12)N(C)C
ClC=1C=C2C=CNC2=CC1.[Cl-].CC1=C(C=[N+](C)C)C=CC=C1.CC1=C(C=O)C=CC=C1.CNC>>ClC=1C=C2C(=CNC2=CC1)C(C1=C(C=CC=C1)C)N(C)C
[NH:19]([CH3:20])[CH3:21].O=[CH:8][c:7]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]1.[cH:9]1[cH:10][nH:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]12>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH:8]([c:9]1[cH:10][nH:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][c:18]12)[N:19]([CH3:20])[CH3:21]
CNC.Cc1ccccc1C=O.Clc1ccc2[nH]ccc2c1
Cc1ccccc1C(c1c[nH]c2ccc(Cl)cc12)N(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 5-chloro-1H-indole and (2-methyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-methyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.Cc1ccccc1C=O.Clc1ccc2[nH]ccc2c1>>Cc1ccccc1C(c1c[nH]c2ccc(Cl)cc12)N(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-76c370c1664845558d3cc239ce3bf4b9
CNC.Cc1cccc(C=O)c1.Clc1ccc2[nH]ccc2c1>>Cc1cccc(C(c2c[nH]c3ccc(Cl)cc23)N(C)C)c1
ClC=1C=C2C=CNC2=CC1.[Cl-].CC=1C=C(C=[N+](C)C)C=CC1.CC=1C=C(C=O)C=CC1.CNC>>ClC=1C=C2C(=CNC2=CC1)C(C=1C=C(C=CC1)C)N(C)C
[NH:18]([CH3:19])[CH3:20].O=[CH:7][c:6]1[cH:5][cH:4][cH:3][c:2]([CH3:1])[cH:21]1.[cH:8]1[cH:9][nH:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]12>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH:7]([c:8]2[cH:9][nH:10][c:11]3[cH:12][cH:13][c:14]([Cl:15])[cH:16][c:17]23)[N:18]([CH3:19])[CH3:20])[cH:21]1
CNC.Cc1cccc(C=O)c1.Clc1ccc2[nH]ccc2c1
Cc1cccc(C(c2c[nH]c3ccc(Cl)cc23)N(C)C)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 5-chloro-1H-indole and (3-methyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-methyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.Cc1cccc(C=O)c1.Clc1ccc2[nH]ccc2c1>>Cc1cccc(C(c2c[nH]c3ccc(Cl)cc23)N(C)C)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-64ec4af69c6f479089ad40c47495e9de
CNC.Cc1cc2ccccc2[nH]1.Cc1ccc(C=[N+](C)C)cc1>>Cc1ccc(C(c2c(C)[nH]c3ccccc23)N(C)C)cc1
CC=1NC2=CC=CC=C2C1.[Cl-].CC1=CC=C(C=[N+](C)C)C=C1.CC1=CC=C(C=O)C=C1.CNC>>CN(C(C1=CC=C(C=C1)C)C1=C(NC2=CC=CC=C12)C)C
[NH:17]([CH3:18])[CH3:19].[cH:7]1[c:8]([CH3:9])[nH:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]12.C[N+](C)=[CH:6][c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:21][cH:20]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH:6]([c:7]2[c:8]([CH3:9])[nH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]23)[N:17]([CH3:18])[CH3:19])[cH:20][cH:21]1
CNC.Cc1cc2ccccc2[nH]1.Cc1ccc(C=[N+](C)C)cc1
Cc1ccc(C(c2c(C)[nH]c3ccccc23)N(C)C)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4aae3a4ea1be485aab9d544da9fceb1ce060e1d3dd462597adbb05c8cde19188
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(Cc2c[nH]c3ccccc23)cc1
C-[N+](-C)=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:13](:[c:14]):[c:11](:[c:12]):[#7;a:10]:[c:9]:1-[C;D1;H3:8]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-methyl-1H-indole and (4-methyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 4-methyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
Other
null
null
null
CNC.Cc1cc2ccccc2[nH]1.Cc1ccc(C=[N+](C)C)cc1>>Cc1ccc(C(c2c(C)[nH]c3ccccc23)N(C)C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d55d366996404928a78cd09f61c25cca
CNC.Cc1ccc(C=O)cc1.Clc1ccc2[nH]ccc2c1>>Cc1ccc(C(c2c[nH]c3ccc(Cl)cc23)N(C)C)cc1
ClC=1C=C2C=CNC2=CC1.[Cl-].CC1=CC=C(C=[N+](C)C)C=C1.CC1=CC=C(C=O)C=C1.CNC>>ClC=1C=C2C(=CNC2=CC1)C(C1=CC=C(C=C1)C)N(C)C
[NH:17]([CH3:18])[CH3:19].O=[CH:6][c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:21][cH:20]1.[cH:7]1[cH:8][nH:9][c:10]2[cH:11][cH:12][c:13]([Cl:14])[cH:15][c:16]12>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH:6]([c:7]2[cH:8][nH:9][c:10]3[cH:11][cH:12][c:13]([Cl:14])[cH:15][c:16]23)[N:17]([CH3:18])[CH3:19])[cH:20][cH:21]1
CNC.Cc1ccc(C=O)cc1.Clc1ccc2[nH]ccc2c1
Cc1ccc(C(c2c[nH]c3ccc(Cl)cc23)N(C)C)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 5-chloro-1H-indole and (4-methyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 4-methyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.Cc1ccc(C=O)cc1.Clc1ccc2[nH]ccc2c1>>Cc1ccc(C(c2c[nH]c3ccc(Cl)cc23)N(C)C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-743e272d902a4863a523cebd7ee14efc
CNC.Cc1cc2ccccc2[nH]1.O=Cc1cccc(Oc2ccccc2)c1>>Cc1[nH]c2ccccc2c1C(c1cccc(Oc2ccccc2)c1)N(C)C
CC=1NC2=CC=CC=C2C1.[Cl-].O(C1=CC=CC=C1)C=1C=C(C=[N+](C)C)C=CC1.O(C1=CC=CC=C1)C=1C=C(C=O)C=CC1.CNC>>CN(C(C1=CC(=CC=C1)OC1=CC=CC=C1)C1=C(NC2=CC=CC=C12)C)C
[NH:25]([CH3:26])[CH3:27].[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[cH:10]1.O=[CH:11][c:12]1[cH:13][cH:14][cH:15][c:16]([O:17][c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[cH:24]1>>[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10]1[CH:11]([c:12]1[cH:13][cH:14][cH:15][c:16]([O:17][c:18]2[cH:19][...
CNC.Cc1cc2ccccc2[nH]1.O=Cc1cccc(Oc2ccccc2)c1
Cc1[nH]c2ccccc2c1C(c1cccc(Oc2ccccc2)c1)N(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Oc2cccc(Cc3c[nH]c4ccccc34)c2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[c;H0;D3;+0:15]:1-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-methyl-1H-indole and (3-phenoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-phenoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1.c1ccccc1
HO-
null
null
null
CNC.Cc1cc2ccccc2[nH]1.O=Cc1cccc(Oc2ccccc2)c1>>Cc1[nH]c2ccccc2c1C(c1cccc(Oc2ccccc2)c1)N(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e97e9aacf01447ff9cb577b2ed4fcc56
CCn1c(-c2ccccc2)cc2ccccc21.CNC.O=Cc1cccc(Oc2ccccc2)c1>>CCn1c(-c2ccccc2)c(C(c2cccc(Oc3ccccc3)c2)N(C)C)c2ccccc21
C(C)N1C(=CC2=CC=CC=C12)C1=CC=CC=C1.[Cl-].O(C1=CC=CC=C1)C=1C=C(C=[N+](C)C)C=CC1.O(C1=CC=CC=C1)C=1C=C(C=O)C=CC1.CNC>>C(C)N1C(=C(C2=CC=CC=C12)C(C1=CC(=CC=C1)OC1=CC=CC=C1)N(C)C)C1=CC=CC=C1
[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[cH:11][c:29]2[cH:30][cH:31][cH:32][cH:33][c:34]12.[NH:26]([CH3:27])[CH3:28].O=[CH:12][c:13]1[cH:14][cH:15][cH:16][c:17]([O:18][c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[cH:25]1>>[CH3:1][CH2:2][n:3]1[c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[c:11](...
CCn1c(-c2ccccc2)cc2ccccc21.CNC.O=Cc1cccc(Oc2ccccc2)c1
CCn1c(-c2ccccc2)c(C(c2cccc(Oc3ccccc3)c2)N(C)C)c2ccccc21
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
bec24864ceecfec904d98640b3bb3caa9d35fa656dcbdac3c55c0dacb43b50eb
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Oc2cccc(Cc3c(-c4ccccc4)[nH]c4ccccc34)c2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C:8]-[#7;a:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[cH;D2;+0:14]:[c:15]:1-[c:16]>>[C:8]-[#7;a:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[c;H0;D3;+0:14](-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]):[c:15]:1-[c:16]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-ethyl-2-phenyl-1H-indole and (3-phenoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-phenoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1cc2ccccc2[nH]1
c1cc2ccccc2[nH]1
c1ccccc1.c1ccccc1.c1ccccc1.c1cc2ccccc2[nH]1
HO-
null
null
null
CCn1c(-c2ccccc2)cc2ccccc21.CNC.O=Cc1cccc(Oc2ccccc2)c1>>CCn1c(-c2ccccc2)c(C(c2cccc(Oc3ccccc3)c2)N(C)C)c2ccccc21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e50db9293f9e4f3f9f2530c09171c21c
CCc1cccc2cc[nH]c12.CNC.O=Cc1cccc(Oc2ccccc2)c1>>CCc1cccc2c(C(c3cccc(Oc4ccccc4)c3)N(C)C)c[nH]c12
C(C)C=1C=CC=C2C=CNC12.[Cl-].O(C1=CC=CC=C1)C=1C=C(C=[N+](C)C)C=CC1.O(C1=CC=CC=C1)C=1C=C(C=O)C=CC1.CNC>>C(C)C=1C=CC=C2C(=CNC12)C(C1=CC(=CC=C1)OC1=CC=CC=C1)N(C)C
[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[cH:8][cH:26][nH:27][c:28]12.[NH:23]([CH3:24])[CH3:25].O=[CH:9][c:10]1[cH:11][cH:12][cH:13][c:14]([O:15][c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[cH:22]1>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]([CH:9]([c:10]3[cH:11][cH:12][cH:13][c:14]([O:15][c:16]4[cH:17][cH:18...
CCc1cccc2cc[nH]c12.CNC.O=Cc1cccc(Oc2ccccc2)c1
CCc1cccc2c(C(c3cccc(Oc4ccccc4)c3)N(C)C)c[nH]c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Oc2cccc(Cc3c[nH]c4ccccc34)c2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 7-ethyl-1H-indole and (3-phenoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-phenoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CCc1cccc2cc[nH]c12.CNC.O=Cc1cccc(Oc2ccccc2)c1>>CCc1cccc2c(C(c3cccc(Oc4ccccc4)c3)N(C)C)c[nH]c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e867fb0a3eb245aeb3eef62e76496d76
CNC.Cn1ccc2ccccc21.O=Cc1cccc(Oc2ccccc2)c1>>CN(C)C(c1cccc(Oc2ccccc2)c1)c1cn(C)c2ccccc12
CN1C=CC2=CC=CC=C12.[Cl-].O(C1=CC=CC=C1)C=1C=C(C=[N+](C)C)C=CC1.O(C1=CC=CC=C1)C=1C=C(C=O)C=CC1.CNC>>CN(C(C1=CC(=CC=C1)OC1=CC=CC=C1)C1=CN(C2=CC=CC=C12)C)C
[CH3:1][NH:2][CH3:3].[cH:18]1[cH:19][n:20]([CH3:21])[c:22]2[cH:23][cH:24][cH:25][cH:26][c:27]12.O=[CH:4][c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17]1>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17]1)[c:18]1[c...
CNC.Cn1ccc2ccccc21.O=Cc1cccc(Oc2ccccc2)c1
CN(C)C(c1cccc(Oc2ccccc2)c1)c1cn(C)c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
05894bd812613f52cf9c1620f3154e6ca08db53b10e13d8864b239f8fa88e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Oc2cccc(Cc3c[nH]c4ccccc34)c2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[cH;D2;+0:8]:[c:9](:[c:10]):[c:11]:1:[c:12].[C;D1;H3:13]-[NH;D2;+0:14]-[C;D1;H3:15]>>[C;D1;H3:13]-[N;H0;D3;+0:14](-[C;D1;H3:15])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:8]1:[c:7]:[#7;a:6](-[C;D1;H3:5]):[c:11](:[c:12]):[c:9]:1:[c:10]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 1-methyl-1H-indole and (3-phenoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-phenoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1ccccc1.c1ccccc1.c1c[nH]c2ccccc12
HO-
null
null
null
CNC.Cn1ccc2ccccc21.O=Cc1cccc(Oc2ccccc2)c1>>CN(C)C(c1cccc(Oc2ccccc2)c1)c1cn(C)c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8282e8e7abbb474d9be6f23017c76a92
CNC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1.O=Cc1cccc(Oc2ccccc2)c1>>CN(C)C(c1cccc(Oc2ccccc2)c1)c1c(-c2ccc(F)cc2)[nH]c2ccccc12
FC1=CC=C(C=C1)C=1NC2=CC=CC=C2C1.[Cl-].O(C1=CC=CC=C1)C=1C=C(C=[N+](C)C)C=CC1.O(C1=CC=CC=C1)C=1C=C(C=O)C=CC1.CNC>>FC1=CC=C(C=C1)C=1NC2=CC=CC=C2C1C(C1=CC(=CC=C1)OC1=CC=CC=C1)N(C)C
[CH3:1][NH:2][CH3:3].[cH:18]1[c:19](-[c:20]2[cH:21][cH:22][c:23]([F:24])[cH:25][cH:26]2)[nH:27][c:28]2[cH:29][cH:30][cH:31][cH:32][c:33]12.O=[CH:4][c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17]1>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][c:11]2[cH:12][cH:1...
CNC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1.O=Cc1cccc(Oc2ccccc2)c1
CN(C)C(c1cccc(Oc2ccccc2)c1)c1c(-c2ccc(F)cc2)[nH]c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Oc2cccc(Cc3c(-c4ccccc4)[nH]c4ccccc34)c2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:15]1:[c:9](-[c:8]):[#7;a:10]:[c:11](:[c:12]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-(4-fluoro-phenyl)-1H-indole and (3-phenoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-phenoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_deta...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.Fc1ccc(-c2cc3ccccc3[nH]2)cc1.O=Cc1cccc(Oc2ccccc2)c1>>CN(C)C(c1cccc(Oc2ccccc2)c1)c1c(-c2ccc(F)cc2)[nH]c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a3acf54bec8b45b7a82a1278ef642df9
Cn1c(-c2ccc(F)c(Cl)c2)cc2ccccc21.O=Cc1cccc(Oc2ccccc2)c1>>NC(c1cccc(Oc2ccccc2)c1)c1c(-c2ccc(F)c(Cl)c2)[nH]c2ccccc12
ClC=1C=C(C=CC1F)C=1N(C2=CC=CC=C2C1)C.[Cl-].O(C1=CC=CC=C1)C=1C=C(C=[N+](C)C)C=CC1.O(C1=CC=CC=C1)C=1C=C(C=O)C=CC1.CNC>>ClC=1C=C(C=CC1F)C=1NC2=CC=CC=C2C1C(C1=CC(=CC=C1)OC1=CC=CC=C1)N
C[n:26]1[c:17](-[c:18]2[cH:19][cH:20][c:21]([F:22])[c:23]([Cl:24])[cH:25]2)[cH:16][c:32]2[c:27]1[cH:28][cH:29][cH:30][cH:31]2.O=[CH:2][c:3]1[cH:4][cH:5][cH:6][c:7]([O:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[cH:15]1>>[NH2:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][c:7]([O:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[cH:15...
Cn1c(-c2ccc(F)c(Cl)c2)cc2ccccc21.O=Cc1cccc(Oc2ccccc2)c1
NC(c1cccc(Oc2ccccc2)c1)c1c(-c2ccc(F)c(Cl)c2)[nH]c2ccccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
a8afdafc7f0c759c2b4fc93e58f1765cda8faa3c8eae6dd29aba9ff10a17bf91
434eff7bf4fb77b67fd204a656cbb3f325fdb7557daa5d7ed8e2ca361ee90b8e
c1ccc(Oc2cccc(Cc3c(-c4ccccc4)[nH]c4ccccc34)c2)cc1
C-[n;H0;D3;+0:1]1:[c:2](-[c:3]):[cH;D2;+0:4]:[c:5](:[c:6]):[c:7]:1:[c:8].O=[CH;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[N;D1;H2:13]-[CH;D3;+0:9](-[c:10](:[c:11]):[c:12])-[c;H0;D3;+0:4]1:[c:2](-[c:3]):[nH;D2;+0:1]:[c:7](:[c:8]):[c:5]:1:[c:6]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-(3-chloro-4-fluoro-phenyl)-methyl-1H-indole and (3-phenoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-phenoxy-benzaldehyde and dimethylamine. Conditions: See reaction.note...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary amine
c1cc2ccccc2[nH]1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
Cn1c(-c2ccc(F)c(Cl)c2)cc2ccccc21.O=Cc1cccc(Oc2ccccc2)c1>>NC(c1cccc(Oc2ccccc2)c1)c1c(-c2ccc(F)c(Cl)c2)[nH]c2ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-687c0c1e420e46059158b481be04ab45
CNC.Cc1cccc2[nH]ccc12.O=Cc1cccc(Oc2ccccc2)c1>>Cc1cccc2[nH]cc(C(c3cccc(Oc4ccccc4)c3)N(C)C)c12
CC1=C2C=CNC2=CC=C1.[Cl-].O(C1=CC=CC=C1)C=1C=C(C=[N+](C)C)C=CC1.O(C1=CC=CC=C1)C=1C=C(C=O)C=CC1.CNC>>CN(C(C1=CC(=CC=C1)OC1=CC=CC=C1)C1=CNC2=CC=CC(=C12)C)C
[NH:24]([CH3:25])[CH3:26].[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[nH:7][cH:8][cH:9][c:27]12.O=[CH:10][c:11]1[cH:12][cH:13][cH:14][c:15]([O:16][c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[cH:23]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[nH:7][cH:8][c:9]([CH:10]([c:11]3[cH:12][cH:13][cH:14][c:15]([O:16][c:17]4[cH:18][cH:19][...
CNC.Cc1cccc2[nH]ccc12.O=Cc1cccc(Oc2ccccc2)c1
Cc1cccc2[nH]cc(C(c3cccc(Oc4ccccc4)c3)N(C)C)c12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Oc2cccc(Cc3c[nH]c4ccccc34)c2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[cH;D2;+0:10]:[c:11]:[#7;a:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:10]1:[c:11]:[#7;a:12]:[c:13](:[c:14]):[c:9]:1:[c:8]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 4-methyl-1H-indole and (3-phenoxy-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 3-phenoxy-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1.c1ccccc1
HO-
null
null
null
CNC.Cc1cccc2[nH]ccc12.O=Cc1cccc(Oc2ccccc2)c1>>Cc1cccc2[nH]cc(C(c3cccc(Oc4ccccc4)c3)N(C)C)c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-dc4ce530f30448019d635106dfd1829c
CNC.Clc1ccc2[nH]ccc2c1.O=Cc1ccccc1C(F)(F)F>>CN(C)C(c1ccccc1C(F)(F)F)c1c[nH]c2ccc(Cl)cc12
ClC=1C=C2C=CNC2=CC1.[Cl-].FC(C1=C(C=[N+](C)C)C=CC=C1)(F)F.FC(C1=C(C=O)C=CC=C1)(F)F.CNC>>ClC=1C=C2C(=CNC2=CC1)C(C1=C(C=CC=C1)C(F)(F)F)N(C)C
[CH3:1][NH:2][CH3:3].[cH:15]1[cH:16][nH:17][c:18]2[cH:19][cH:20][c:21]([Cl:22])[cH:23][c:24]12.O=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[C:11]([F:12])([F:13])[F:14]>>[CH3:1][N:2]([CH3:3])[CH:4]([c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[C:11]([F:12])([F:13])[F:14])[c:15]1[cH:16][nH:17][c:18]2[cH:19][cH:20][c:21]([Cl:22]...
CNC.Clc1ccc2[nH]ccc2c1.O=Cc1ccccc1C(F)(F)F
CN(C)C(c1ccccc1C(F)(F)F)c1c[nH]c2ccc(Cl)cc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:1:[c:14]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 5-chloro-1H-indole and (2-trifluoromethyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 2-trifluoromethyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccccc1.c1ccc2[nH]ccc2c1
HO-
null
null
null
CNC.Clc1ccc2[nH]ccc2c1.O=Cc1ccccc1C(F)(F)F>>CN(C)C(c1ccccc1C(F)(F)F)c1c[nH]c2ccc(Cl)cc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-4dfdeeb8dda1463f9bf2481d09e0218e
CNC.Cc1cc2ccccc2[nH]1.O=Cc1ccc(C(F)(F)F)cc1>>Cc1[nH]c2ccccc2c1C(c1ccc(C(F)(F)F)cc1)N(C)C
CC=1NC2=CC=CC=C2C1.[Cl-].FC(C1=CC=C(C=[N+](C)C)C=C1)(F)F.FC(C1=CC=C(C=O)C=C1)(F)F.CNC>>CN(C(C1=CC=C(C=C1)C(F)(F)F)C1=C(NC2=CC=CC=C12)C)C
[NH:22]([CH3:23])[CH3:24].[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[cH:10]1.O=[CH:11][c:12]1[cH:13][cH:14][c:15]([C:16]([F:17])([F:18])[F:19])[cH:20][cH:21]1>>[CH3:1][c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10]1[CH:11]([c:12]1[cH:13][cH:14][c:15]([C:16]([F:17])([F:18])[F:19])[cH:20][cH:21]1)[N:2...
CNC.Cc1cc2ccccc2[nH]1.O=Cc1ccc(C(F)(F)F)cc1
Cc1[nH]c2ccccc2c1C(c1ccc(C(F)(F)F)cc1)N(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1e887ffc9d31747076f97173ff8dc6f44b0480e2cfa9f6a88ab0a775ac92e3d5
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(Cc2c[nH]c3ccccc23)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[cH;D2;+0:15]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11](:[c:12]):[c:13](:[c:14]):[c;H0;D3;+0:15]:1-[CH;D3;+0:1](-[N;H0;D3;+0:6](-[C;D1;H3:5])-[C;D1;H3:7])-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
The preparation was carried out in accordance with general synthesis instructions 4 from 2-methyl-1H-indole and (4-trifluoromethyl-benzylidene)-dimethylammonium chloride, which had been prepared in accordance with example 44 from 4-trifluoromethyl-benzaldehyde and dimethylamine. Conditions: See reaction.notes.procedure...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
null
null
null
CNC.Cc1cc2ccccc2[nH]1.O=Cc1ccc(C(F)(F)F)cc1>>Cc1[nH]c2ccccc2c1C(c1ccc(C(F)(F)F)cc1)N(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1345b2679a1f4255af5f660665af3050
NOCc1ccccc1.O=C(O)CCCCCCCBr>>O=C(CCCCCCCBr)NOCc1ccccc1
O=C1OCCN1P(=O)(N1C(OCC1)=O)Cl.C(C)N(CC)CC.Cl.C(C1=CC=CC=C1)ON.BrCCCCCCCC(=O)O>>C(C1=CC=CC=C1)ONC(CCCCCCCBr)=O
[NH2:11][O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.O[C:2](=[O:1])[CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][Br:10]>>[O:1]=[C:2]([CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][Br:10])[NH:11][O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
NOCc1ccccc1.O=C(O)CCCCCCCBr
O=C(CCCCCCCBr)NOCc1ccccc1
null
null
ClCCl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[#8:6]-[NH2;D1;+0:7]>>[C:5]-[#8:6]-[NH;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
78
[{"value": 78.0, "product": "C(C1=CC=CC=C1)ONC(CCCCCCCBr)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.7, "product": "C(C1=CC=CC=C1)ONC(CCCCCCCBr)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
In an ice bath, 14 ml triethylamine was added to a suspension of 3.2 g (20 mmol) O-benzylhydroxylamine hydrochloride in 150 ml dichloromethane. Stirring was continued until the solution became clear. Then, 4.5 g (20 mmol) 8-bromo octanoic acid was added, followed by 5.6 g (22 mmol) bis-(2-oxo-3-oxazolidinyl)-phosphoryl...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
ClCCl
null
18
NOCc1ccccc1.O=C(O)CCCCCCCBr>ClCCl>O=C(CCCCCCCBr)NOCc1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2b702c2e3f184302b8ebff254e729685
O=C(CCCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NOCc1ccccc1>>O=C(CCCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NO
C(C1=CC=CC=C1)ONC(CCCCCCCN1S(C=2C3=C1C=CC=C3C=CC2)(=O)=O)=O>>ONC(CCCCCCCN1S(C=2C3=C1C=CC=C3C=CC2)(=O)=O)=O
c1ccc(C[O:25][NH:24][C:2](=[O:1])[CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][N:10]2[c:11]3[cH:12][cH:13][cH:14][c:15]4[cH:16][cH:17][cH:18][c:19]([c:20]34)[S:21]2(=[O:22])=[O:23])cc1>>[O:1]=[C:2]([CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][N:10]1[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][c:19]...
O=C(CCCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NOCc1ccccc1
O=C(CCCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NO
null
[Pd]
CO
Deprotection
OtherReaction
94fa5e5ed4a5b32c4aba0dd3c8151bfdd08491d1bc6453e9fd01d7dc3e51cd0f
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=S1(=O)Nc2cccc3cccc1c23
[C:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[O;H0;D2;+0:5]-C-c1:c:c:c:c:c:1>>[C:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[OH;D1;+0:5]
null
[]
null
null
null
null
8-(1,1-Dioxo-2H-naphtho[1,8-cd]isothiazol-2-yl)-octanoic acid benzyloxyamide (0.47 g) in methanol (30 ml) was hydrogenated for 1.5 h in the presence of palladium on barium sulfate at ambient temperature and pressure. The catalyst was removed by filtration and the solvent was evaporated. The residue was purified by colu...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1
null
c1cc2c3c(cccc3c1)S[NH]2
Other
[Pd].CO
null
null
O=C(CCCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NOCc1ccccc1>[Pd].CO>O=C(CCCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NO
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-190bbd673a414296bb77ded29b4d23dd
O=C(CCCCCCBr)NOCc1ccccc1.O=S1(=O)Nc2cccc3cccc1c23>>O=C(CCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NOCc1ccccc1
C(C1=CC=CC=C1)ONC(CCCCCCBr)=O.C1=CC2=C3C(=C1)NS(=O)(=O)C3=CC=C2.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)ONC(CCCCCCN1S(C=2C3=C1C=CC=C3C=CC2)(=O)=O)=O
Br[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][C:2](=[O:1])[NH:23][O:24][CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1.[NH:9]1[c:10]2[cH:11][cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][c:18]([c:19]23)[S:20]1(=[O:21])=[O:22]>>[O:1]=[C:2]([CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][N:9]1[c:10]2[cH:11][cH:12][cH:13][c:14]...
O=C(CCCCCCBr)NOCc1ccccc1.O=S1(=O)Nc2cccc3cccc1c23
O=C(CCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NOCc1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
ed85001971e6b69caaa4e6ac714726e893cc7ff8ac09362f619ddbe41bb0c27c
0b054affe7e4bb904ceae512aabc19d89c93551cb46dfbc6f220fc85e5eeff75
O=C(CCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NOCc1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[O;D1;H0:4]=[#16:5]1(=[O;D1;H0:6])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]:[c:11]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[c:8](:[c:9]):[c:10]:[c:11]-[#16:5]-1(=[O;D1;H0:4])=[O;D1;H0:6]
null
[]
null
null
null
null
In a manner analogous to that of example 1(b), 7-bromo-heptanoic acid benzyloxyamide 0.46 g, 1.5 mmol) was reacted with 1,8-naphthalenesultam (0.3 g, 1.5 mmol) in the presence of potassium carbonate (0.2 g, 1.4 mmol) to give 7-(1,1-dioxo-2H-naphtho[1,8-cd]isothiazol-2-yl)-heptanoic acid benzyloxyamide as an amorphous s...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Primary halide
Tertiary amine
c1cc2c3c(cccc3c1)SN2
c1cc2c3c(cccc3c1)S[NH]2
c1cc2c3c(cccc3c1)S[NH]2.c1ccccc1
HBr
null
null
null
O=C(CCCCCCBr)NOCc1ccccc1.O=S1(=O)Nc2cccc3cccc1c23>>O=C(CCCCCCN1c2cccc3cccc(c23)S1(=O)=O)NOCc1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-dce42a25d6154aac814679c0cf4274dc
O=C(CCCCCCCBr)NOCc1ccccc1.O=C1Nc2cccc3cccc1c23>>O=C(CCCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
C(C1=CC=CC=C1)ONC(CCCCCCCBr)=O.N1C(C2=C3C(C=CC=C13)=CC=C2)=O.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)ONC(CCCCCCCN1C(C2=C3C(C=CC=C13)=CC=C2)=O)=O
Br[CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][C:2](=[O:1])[NH:23][O:24][CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1.[NH:10]1[C:11](=[O:12])[c:13]2[cH:20][cH:19][cH:18][c:17]3[cH:16][cH:15][cH:14][c:21]1[c:22]23>>[O:1]=[C:2]([CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][N:10]1[C:11](=[O:12])[c:13]2[cH:1...
O=C(CCCCCCCBr)NOCc1ccccc1.O=C1Nc2cccc3cccc1c23
O=C(CCCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
57898719c69ec2e691a59084e883c7c6aecb533a494f23939bacaf45212e2c94
4a6c1e88c9e8bed487b746792f88d478ff36cc235f9a217d4632e6babdebdc9a
O=C(CCCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[O;D1;H0:4]=[C:5]1-[NH;D2;+0:6]-[c;H0;D3;+0:7]2:[cH;D2;+0:8]:[c:9]:[c:10]:[c:11]3:[c:12]:[c:13]:[cH;D2;+0:14]:[c;H0;D3;+0:15]-1:[c:16]:3:2>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6]1-[C:5](=[O;D1;H0:4])-[c;H0;D3;+0:15]2:[cH;D2;+0:8]:[c:9]:[c:10]:[c:11]3:[c:12]:[c:13]:[cH;D2;+0:14]:[c;H0;D3;+...
null
[]
null
null
null
null
In a manner analogous to that of example 1(b), 8-bromo-octanoic acid benzyloxyamide 0.49 g, 1.5 mmol) was reacted with benzo[cd]indol-2(1H)-one (0.25 g, 1.5 mmol) in the presence of potassium carbonate (0.2 g, 1.4 mmol) to give 8-(2-oxo-2H-benzo[cd]indol-1-yl)-octanoic acid benzyloxyamide as an amorphous solid (yield 0...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amide
Tertiary amide
c1cc2c3c(cccc3c1)NC2
c1cc2c3c(cccc3c1)[NH]C2
c1cc2c3c(cccc3c1)[NH]C2.c1ccccc1
HBr
null
null
null
O=C(CCCCCCCBr)NOCc1ccccc1.O=C1Nc2cccc3cccc1c23>>O=C(CCCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-10c22954f0c8489195af41f93b71e584
O=C(CCCCCCBr)NOCc1ccccc1.O=C1Nc2cccc3cccc1c23>>O=C(CCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
C(C1=CC=CC=C1)ONC(CCCCCCBr)=O.N1C(C2=C3C(C=CC=C13)=CC=C2)=O.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)ONC(CCCCCCN1C(C2=C3C(C=CC=C13)=CC=C2)=O)=O
Br[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][C:2](=[O:1])[NH:22][O:23][CH2:24][c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1.[NH:9]1[C:10](=[O:11])[c:12]2[cH:19][cH:18][cH:17][c:16]3[cH:15][cH:14][cH:13][c:20]1[c:21]23>>[O:1]=[C:2]([CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][N:9]1[C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15]...
O=C(CCCCCCBr)NOCc1ccccc1.O=C1Nc2cccc3cccc1c23
O=C(CCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
57898719c69ec2e691a59084e883c7c6aecb533a494f23939bacaf45212e2c94
4a6c1e88c9e8bed487b746792f88d478ff36cc235f9a217d4632e6babdebdc9a
O=C(CCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[O;D1;H0:4]=[C:5]1-[NH;D2;+0:6]-[c;H0;D3;+0:7]2:[cH;D2;+0:8]:[c:9]:[c:10]:[c:11]3:[c:12]:[c:13]:[cH;D2;+0:14]:[c;H0;D3;+0:15]-1:[c:16]:3:2>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6]1-[C:5](=[O;D1;H0:4])-[c;H0;D3;+0:15]2:[cH;D2;+0:8]:[c:9]:[c:10]:[c:11]3:[c:12]:[c:13]:[cH;D2;+0:14]:[c;H0;D3;+...
null
[]
null
null
null
null
In a manner analogous to that of example 2(b), 7-bromo-heptanoic acid benzyloxy-amide 0.46 g, 1.5 mmol) was reacted with benzo[cd]indol-2(1H)-one (0.25 g, 1.5 mmol) in the presence of potassium carbonate (0.2 g, 1.4 mmol) to give 7-(2-oxo-2H-benzo[cd]indol-1-yl)-heptanoic acid benzyloxyamide as an amorphous solid (yiel...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amide
Tertiary amide
c1cc2c3c(cccc3c1)NC2
c1cc2c3c(cccc3c1)[NH]C2
c1cc2c3c(cccc3c1)[NH]C2.c1ccccc1
HBr
null
null
null
O=C(CCCCCCBr)NOCc1ccccc1.O=C1Nc2cccc3cccc1c23>>O=C(CCCCCCN1C(=O)c2cccc3cccc1c23)NOCc1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-388534def69443b5861bd8642778f4f5
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1sc(N)nc1C>>CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
C(C)OC(=O)C1=C(N=C(S1)N)C.C(C)(C)(C)OC(=O)OC(=O)OC(C)(C)C>>C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C
CC(C)(C)OC(=O)[O:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17].[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH2:9])[n:18][c:19]1[CH3:20]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH:9][O:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17])[n:18][c:19]1[CH3:20]
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1sc(N)nc1C
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
null
CN(C1=CC=NC=C1)C
O1CCCC1
Miscellaneous
OtherReaction
573d4841f3c12e78e6b12cf91f4d399dc4182819414ba565cbb5ba4d94db2872
6534c82b6e71666d74191826a188dd640b31790e5c8329ff0e4034ba8a3022e5
c1cscn1
C-C(-C)(-C)-O-C(=O)-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].[#8:9]-[C:10](=[O;D1;H0:11])-[c:12]1:[#16;a:13]:[c:14](-[NH2;D1;+0:15]):[#7;a:16]:[c:17]:1>>[#8:9]-[C:10](=[O;D1;H0:11])-[c:12]1:[#16;a:13]:[c:14](-[NH;D2;+0:15]-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[...
72
[{"value": 72.0, "product": "C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.1, "product": "C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
A suspension of ethyl-2-amino-4-methyl-thiazole-5-carboxylate (18.6 g, 100 mmol), di-t-butyldicarbonate (26.2 g, 120 mmol) and 4-dimethylaminopyridine (800 mg, 6.55 mmol) in dry tetrahydrofuran (300 mL) was stirred under nitrogen for 18 h. The solvent was evaporated in vacuo. The residue was suspended in dichloromethan...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Carbonic Ester.Carbonic Ester.Primary amine.Boc
Secondary amine
null
null
c1cscn1
HO-
CN(C1=CC=NC=C1)C.O1CCCC1
null
18
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1sc(N)nc1C>CN(C1=CC=NC=C1)C.O1CCCC1>CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8e2c9bc4dca442bda6037a7be6b1f8b6
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C>>Cc1nc(NOC(=O)OC(C)(C)C)sc1C(=O)O
Cl.C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C.[OH-].[K+]>>C(C)(C)(C)OC(=O)ONC=1SC(=C(N1)C)C(=O)O
CC[O:18][C:16]([c:15]1[c:2]([CH3:1])[n:3][c:4]([NH:5][O:6][C:7](=[O:8])[O:9][C:10]([CH3:11])([CH3:12])[CH3:13])[s:14]1)=[O:17]>>[CH3:1][c:2]1[n:3][c:4]([NH:5][O:6][C:7](=[O:8])[O:9][C:10]([CH3:11])([CH3:12])[CH3:13])[s:14][c:15]1[C:16](=[O:17])[OH:18]
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
Cc1nc(NOC(=O)OC(C)(C)C)sc1C(=O)O
null
null
O1C(CCC1)CCO
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1cscn1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#16;a:5]):[c:6]:[#7;a:7]>>[#16;a:5]:[c:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]):[c:6]:[#7;a:7]
null
[]
55
CELSIUS
null
null
A stirred solution of ethyl-2-tert-butoxycarbonyloxyamino-4-methyl-thiazole-5-carboxylate (10 g, 34.95 mmol) in tetrahydrofuran-ethanol (250 mL, 2:3) was treated with a 6N KOH solution (250 mL). The mixture was heated to 55° C. overnight. The solution was cooled to 0° C. and acidified with concd. HCl to pH 1. The solve...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cscn1
Other
O1C(CCC1)CCO
55
null
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C>O1C(CCC1)CCO>Cc1nc(NOC(=O)OC(C)(C)C)sc1C(=O)O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-95939283827b413aa59601d91194e5dd
Cc1cc(C)c(NC(=O)c2sc(NC(=O)OC(C)(C)C)nc2C)c(C)c1>>Cc1cc(C)c(NC(=O)c2sc(N)nc2C)c(C)c1
CC1=C(C(=CC(=C1)C)C)NC(=O)C1=C(N=C(S1)NC(OC(C)(C)C)=O)C>>NC=1SC(=C(N1)C)C(=O)NC1=C(C=C(C=C1C)C)C
CC(C)(C)OC(=O)[NH:13][c:12]1[s:11][c:10]([C:8]([NH:7][c:6]2[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:19][c:17]2[CH3:18])=[O:9])[c:15]([CH3:16])[n:14]1>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]([NH:7][C:8](=[O:9])[c:10]2[s:11][c:12]([NH2:13])[n:14][c:15]2[CH3:16])[c:17]([CH3:18])[cH:19]1
Cc1cc(C)c(NC(=O)c2sc(NC(=O)OC(C)(C)C)nc2C)c(C)c1
Cc1cc(C)c(NC(=O)c2sc(N)nc2C)c(C)c1
null
null
FC(C(=O)O)(F)F
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=C(Nc1ccccc1)c1cncs1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[c:2]1:[#16;a:3]:[c:4](-[C:5](-[#7:6])=[O;D1;H0:7]):[c:8]:[#7;a:9]:1>>[#7:6]-[C:5](=[O;D1;H0:7])-[c:4]1:[#16;a:3]:[c:2](-[NH2;D1;+0:1]):[#7;a:9]:[c:8]:1
91.4
[{"value": 91.0, "product": "NC=1SC(=C(N1)C)C(=O)NC1=C(C=C(C=C1C)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.4, "product": "NC=1SC(=C(N1)C)C(=O)NC1=C(C=C(C=C1C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of [5-[[(2,4,6-Trimethylphenyl)amino]carbonyl]-4-methyl-2-thiazolyl]carbamic acid, 1,1-dimethylethyl ester (10 g, 26.63 mmol) in trifluoroacetic acid (100 mL) was stirred at rt for 3 h. The solution was concentrated under reduced pressure and the residue was diluted with EtOAc (700 mL), washed with 5% aq. KH...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1.c1cscn1
HO-
FC(C(=O)O)(F)F
null
null
Cc1cc(C)c(NC(=O)c2sc(NC(=O)OC(C)(C)C)nc2C)c(C)c1>FC(C(=O)O)(F)F>Cc1cc(C)c(NC(=O)c2sc(N)nc2C)c(C)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1489de592ed543aead9b9b3cc9eda428
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1sc(N)nc1C(F)(F)F>>CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C(F)(F)F
C(C)OC(=O)C1=C(N=C(S1)N)C(F)(F)F.C(C)(C)(C)OC(=O)OC(=O)OC(C)(C)C>>C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C(F)(F)F
CC(C)(C)OC(=O)[O:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17].[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH2:9])[n:18][c:19]1[C:20]([F:21])([F:22])[F:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH:9][O:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17])[n:18][c:19]1[C:20]([F:21])...
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1sc(N)nc1C(F)(F)F
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C(F)(F)F
null
CN(C1=CC=NC=C1)C
ClCCl
Miscellaneous
OtherReaction
573d4841f3c12e78e6b12cf91f4d399dc4182819414ba565cbb5ba4d94db2872
6534c82b6e71666d74191826a188dd640b31790e5c8329ff0e4034ba8a3022e5
c1cscn1
C-C(-C)(-C)-O-C(=O)-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].[#8:9]-[C:10](=[O;D1;H0:11])-[c:12]1:[#16;a:13]:[c:14](-[NH2;D1;+0:15]):[#7;a:16]:[c:17]:1>>[#8:9]-[C:10](=[O;D1;H0:11])-[c:12]1:[#16;a:13]:[c:14](-[NH;D2;+0:15]-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[...
92
[{"value": 92.0, "product": "C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C(F)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.7, "product": "C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
A suspension of ethyl-2-amino-4-trifluoromethyl-thiazole-5-carboxylate (5.05 g, 21.02 mmol), di-t-butyldicarbonate (4.82 g, 22.07 mmol) and 4-dimethylaminopyridine (260 mg, 2.1 mmol) in dichloromethane (209 mL) was stirred under nitrogen for 1.5 h. The solvent was evaporated in vacuo. The residue was chromatographed on...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Carbonic Ester.Carbonic Ester.Primary amine.Boc
Secondary amine
null
null
c1cscn1
HO-
CN(C1=CC=NC=C1)C.ClCCl
null
1.5
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1sc(N)nc1C(F)(F)F>CN(C1=CC=NC=C1)C.ClCCl>CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C(F)(F)F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9428c79723c14198955b974363dbc33e
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C(F)(F)F>>CC(C)(C)OC(=O)ONc1nc(C(F)(F)F)c(C(=O)O)s1
Cl.C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C(F)(F)F.[OH-].[Na+]>>C(C)(C)(C)OC(=O)ONC=1SC(=C(N1)C(F)(F)F)C(=O)O
CC[O:20][C:18]([c:17]1[c:12]([C:13]([F:14])([F:15])[F:16])[n:11][c:10]([NH:9][O:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[s:21]1)=[O:19]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[O:8][NH:9][c:10]1[n:11][c:12]([C:13]([F:14])([F:15])[F:16])[c:17]([C:18](=[O:19])[OH:20])[s:21]1
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C(F)(F)F
CC(C)(C)OC(=O)ONc1nc(C(F)(F)F)c(C(=O)O)s1
null
null
CO
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1cscn1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#16;a:5]):[c:6]:[#7;a:7]>>[#16;a:5]:[c:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]):[c:6]:[#7;a:7]
null
[]
null
null
8
HOUR
A stirred solution of ethyl-2-tert-butoxycarbonyloxyamino-4-trifluoromethyl-thiazole-5-carboxylate (6.5 g, 19.1 mmol) in methanol (100 mL) was treated with a 1N aq. NaOH solution (573 mL). The mixture was stirred at rt overnight. The solution was cooled to 0° C. and acidified with a 6 M aq. HCl solution to pH 1 and ext...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cscn1
Other
CO
null
8
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C(F)(F)F>CO>CC(C)(C)OC(=O)ONc1nc(C(F)(F)F)c(C(=O)O)s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f75c4e99532d4a508cd22f8965bec48f
CCOC(=O)c1sc(N)nc1C.O=C(Cl)OCc1ccccc1>>CCOC(=O)c1sc(NOC(=O)OCc2ccccc2)nc1C
ClC(=O)OCC1=CC=CC=C1.C(=O)(O)[O-].[Na+].C(C)OC(=O)C1=C(N=C(S1)N)C.ClC(=O)OCC1=CC=CC=C1>>C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OCC1=CC=CC=C1)C
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH2:9])[n:21][c:22]1[CH3:23].Cl[C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH:9][O:10][C:11](=[O:12])[O:13][CH2:14][c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)[n:21][c:22]1[CH3:23]
CCOC(=O)c1sc(N)nc1C.O=C(Cl)OCc1ccccc1
CCOC(=O)c1sc(NOC(=O)OCc2ccccc2)nc1C
null
null
ClCCl.C1CCOC1.O
Acylation
OtherReaction
45b9b0e25c597562683452adce8466688667b23f75e19af296c1a5a031c98ee1
464a9ef6461bb6ec6a8915b72ac7ce5008d5625d8040f6a6c7cc16c6435e26ae
O=C(OCc1ccccc1)ONc1nccs1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[#16;a:9]:[c:10](-[NH2;D1;+0:11]):[#7;a:12]:[c:13]:1>>[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[#16;a:9]:[c:10](-[NH;D2;+0:11]-[#8:14]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]):[#7;a:12]:[c:13]:1
48
[{"value": 48.0, "product": "C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OCC1=CC=CC=C1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A 3 M aq. NaHCO3 solution (10 mL, 30 mmol) was added to a stirred solution of ethyl-2-amino-4-methyl-thiazole-5-carboxylate (372 mg, 2 mmol) in THF (20 mL) at 0–5° C. Benzyl chloroformate (500 μL) was added. After 2 h, additional benzyl chloroformate (500 μL) and the biphasic solution was stirred for an additional 2 h ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Ether.Secondary amine
null
null
c1cscn1.c1ccccc1
null
ClCCl.C1CCOC1.O
null
2
CCOC(=O)c1sc(N)nc1C.O=C(Cl)OCc1ccccc1>ClCCl.C1CCOC1.O>CCOC(=O)c1sc(NOC(=O)OCc2ccccc2)nc1C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8e323e0dfaa24bf8871d0a446d323fd4
CCOC(=O)c1sc(N)nc1C.CS(=O)(=O)Cl>>CCOC(=O)c1sc(NS(C)(=O)=O)nc1C
C(C)OC(=O)C1=C(N=C(S1)N)C.CS(=O)(=O)Cl>>C(C)OC(=O)C1=C(N=C(S1)NS(=O)(=O)C)C
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH2:9])[n:14][c:15]1[CH3:16].Cl[S:10]([CH3:11])(=[O:12])=[O:13]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH:9][S:10]([CH3:11])(=[O:12])=[O:13])[n:14][c:15]1[CH3:16]
CCOC(=O)c1sc(N)nc1C.CS(=O)(=O)Cl
CCOC(=O)c1sc(NS(C)(=O)=O)nc1C
null
null
ClCCl.N1=CC=CC=C1
Acylation
Sulfonamide synthesis (Schotten-Baumann) primary amine
4c44ef6d7646f6ef25dd125d2c32c713d8dcae7c603407faa5f0fb810631670e
8fce8115d8a725afa92eb3910ded29d4c852e5133eba78a425054f41f7142603
c1cscn1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[#16;a:9]:[c:10](-[NH2;D1;+0:11]):[#7;a:12]:[c:13]:1>>[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[#16;a:9]:[c:10](-[NH;D2;+0:11]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]):[#7;a:12]:[c:13]:1
87
[{"value": 87.0, "product": "C(C)OC(=O)C1=C(N=C(S1)NS(=O)(=O)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.6, "product": "C(C)OC(=O)C1=C(N=C(S1)NS(=O)(=O)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred solution of ethyl-2-amino-4-methyl-thiazole-5-carboxylate (558 mg, 3 mmol) in dichloromethane (15 mL) and pyridine (5 mL) was treated with methanesulfonyl chloride (687 mg, 6 mmol) at rt overnight. The solution was diluted with dichloromethane (50 mL) and washed with 2N aq. HCl solution (15 mL, 3×), dried (Mg...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1cscn1
HCl
ClCCl.N1=CC=CC=C1
null
null
CCOC(=O)c1sc(N)nc1C.CS(=O)(=O)Cl>ClCCl.N1=CC=CC=C1>CCOC(=O)c1sc(NS(C)(=O)=O)nc1C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-59e03f216bec45e885b78045a0b57aed
CCOC(=O)c1sc(NS(C)(=O)=O)nc1C>>Cc1nc(NS(C)(=O)=O)sc1C(=O)O
Cl.C(C)OC(=O)C1=C(N=C(S1)NS(=O)(=O)C)C.[OH-].[Na+]>>CS(=O)(=O)NC=1SC(=C(N1)C)C(=O)O
CC[O:14][C:12]([c:11]1[c:2]([CH3:1])[n:3][c:4]([NH:5][S:6]([CH3:7])(=[O:8])=[O:9])[s:10]1)=[O:13]>>[CH3:1][c:2]1[n:3][c:4]([NH:5][S:6]([CH3:7])(=[O:8])=[O:9])[s:10][c:11]1[C:12](=[O:13])[OH:14]
CCOC(=O)c1sc(NS(C)(=O)=O)nc1C
Cc1nc(NS(C)(=O)=O)sc1C(=O)O
null
null
CO
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1cscn1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#16;a:5]):[c:6]:[#7;a:7]>>[#16;a:5]:[c:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]):[c:6]:[#7;a:7]
null
[]
null
null
8
HOUR
A stirred solution of Ethyl-2-[(methylsulfonyl)amino]-4-methyl-thiazole-5-carboxylate (300 mg, 1.14 mmol) in methanol (9 mL) was treated with a 1N NaOH solution (28.4 mL, 28.4 mmol). The mixture was stirred at rt overnight. The solution was cooled to 0° C. and acidified with 6N aq. HCl solution to pH 1. The solution wa...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cscn1
Other
CO
null
8
CCOC(=O)c1sc(NS(C)(=O)=O)nc1C>CO>Cc1nc(NS(C)(=O)=O)sc1C(=O)O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-7b8cb11dcdcf4486a625205a9d01af52
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1cnc(N)s1>>CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
C(C)OC(=O)C1=CN=C(S1)N.C(C)(C)(C)OC(=O)OC(=O)OC(C)(C)C.O1CCCC1>>C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C
CC(C)(C)OC(=O)[O:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17].[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH2:9])[n:18][cH:19]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[s:7][c:8]([NH:9][O:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17])[n:18][c:19]1[CH3:20]
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1cnc(N)s1
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
null
CN(C1=CC=NC=C1)C
null
C-C Coupling
OtherReaction
fc103691cbf8d10076de901c3ed38b08dd9e349f2a648885626a9e90fb13bfe5
718843329b9c43fc61f59e89f6a61edd702695d27eaeeab096d4a7bcb6000080
c1cscn1
C-C(-C)(-C)-O-C(=O)-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].[C:9]-[#8:10]-[C:11](=[O;D1;H0:12])-[c:13]1:[#16;a:14]:[c:15](-[NH2;D1;+0:16]):[#7;a:17]:[cH;D2;+0:18]:1>>[C:9]-[#8:10]-[C:11](=[O;D1;H0:12])-[c:13]1:[#16;a:14]:[c:15](-[NH;D2;+0:16]-[O;H0;D2;+0:1]-[C:2](=[O;D1;H...
70
[{"value": 70.0, "product": "C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of ethyl-2-amino-thiazole-5-carboxylate (972 mg, 6 mmol, B. Plouvler, C. Bailly, R. Houssin, j-P. Henlchart Heterocyles 32(4), 693–701, 1991 and H. J. Becker, J. de Jonge Rec. Trav. Chim, 61, 463, 1942), di-t-butyldicarbonate (1.94 g, 9 mmol) and 4-dimethylaminopyridine (73 mg, 0.6 mmol) in dry tetrahydrof...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Carbonic Ester.Carbonic Ester.Primary amine.Boc
Secondary amine
c1cscn1
c1cscn1
c1cscn1
HO-
CN(C1=CC=NC=C1)C
null
null
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C.CCOC(=O)c1cnc(N)s1>CN(C1=CC=NC=C1)C>CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f30f6fee1bf24541893678b7a7c2463b
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C>>CC(C)(C)OC(=O)ONc1ncc(C(=O)O)s1
C(C)OC(=O)C1=C(N=C(S1)NOC(=O)OC(C)(C)C)C.[OH-].[Na+]>>C(C)(C)(C)OC(=O)ONC=1SC(=CN1)C(=O)O
CC[O:16][C:14]([c:13]1[c:12](C)[n:11][c:10]([NH:9][O:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[s:17]1)=[O:15]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[O:8][NH:9][c:10]1[n:11][cH:12][c:13]([C:14](=[O:15])[OH:16])[s:17]1
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C
CC(C)(C)OC(=O)ONc1ncc(C(=O)O)s1
null
null
O1C(CCC1)CO
Deprotection
OtherReaction
0daaaff4e26641512f45c4a3a3599acca9d94cce9b964eb5e9d934cefb85f4c2
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1cscn1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]1:[#16;a:5]:[c:6]:[#7;a:7]:[c;H0;D3;+0:8]:1-C>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]1:[#16;a:5]:[c:6]:[#7;a:7]:[cH;D2;+0:8]:1
null
[]
null
null
24
HOUR
A stirred solution of ethyl-2-tert-butoxycarbonyloxyamino-4-methyl-thiazole-5-carboxylate (1.1 g, 4.2 mmol) in tetrahydrofuran-methanol (80 mL, 1:1) was treated with a 6N aq. NaOH solution (20 mL, 120 mmol). The mixture was stirred at rt for 24 h. Most of THF and methanol were removed by distillation under reduced pres...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1cscn1
c1cscn1
c1cscn1
Other
O1C(CCC1)CO
null
24
CCOC(=O)c1sc(NOC(=O)OC(C)(C)C)nc1C>O1C(CCC1)CO>CC(C)(C)OC(=O)ONc1ncc(C(=O)O)s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-4cce3d012348490bb45fe8a36bc03cd3
O=[N+]([O-])c1cccc(O)c1>>O=[N+]([O-])c1ccccc1
[N+](=O)([O-])C=1C=C(C=CC1)O.C(=O)([O-])[O-].[K+].[K+].[Na+].[I-]>>[N+](=O)([O-])C1=CC=CC=C1
O[c:8]1[cH:7][cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:9]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1
O=[N+]([O-])c1cccc(O)c1
O=[N+]([O-])c1ccccc1
null
null
CN(C)C=O
Reduction
OtherReaction
0b15258bc3b0efb75716a15093f26f3ade1fb35d0d50493dcb65925b9449d16a
27ebe27a5e17883303ac9a42d30f2cb918c0044de7ff3c79776e1ddb80cc53d9
c1ccccc1
O-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]>>[c:5]:[c:4]:[cH;D2;+0:1]:[c:2]:[c:3]
null
[]
120
CELSIUS
null
null
A suspension of 3-nitrophenol (837 mg, 6.02 mmole), 1-chloro-3-[imidazo-1-yl]-propane (871 mg, 1 eq), K2CO3 (3.3 gm, 4 eq) and NaI (1.0 gm, 1.1 eq) in DMF was heated at 120° C. for 6 hr. After cooling to RT, the reaction was filtered and the filter cake was washed with DMF. The solvent was removed from the filtrate and...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
null
c1ccccc1
c1ccccc1
c1ccccc1
Other
CN(C)C=O
120
null
O=[N+]([O-])c1cccc(O)c1>CN(C)C=O>O=[N+]([O-])c1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-68f4737b6c484d558c81c99a24e5ed31
CCN=C=O.Nc1nc2ccc(Cl)cc2s1>>CCNC(=O)Nc1nc2ccc(Cl)cc2s1
ClC1=CC2=C(N=C(S2)N)C=C1.C(C)N=C=O.C(C)N(CC)CC>>ClC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][N:3]=[C:4]=[O:5].[NH2:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][c:15]2[s:16]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][c:15]2[s:16]1
CCN=C=O.Nc1nc2ccc(Cl)cc2s1
CCNC(=O)Nc1nc2ccc(Cl)cc2s1
null
null
CN(C)C=O
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
c1ccc2scnc2c1
[C;D1;H3:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[NH2;D1;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1>>[C;D1;H3:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1
null
[]
null
null
null
null
Three grams of 6-chloro-1,3-benzothiazol-2-amine was dissolved in about 50 mL DMF. Next, about 2.5 mL of EtNCO was added followed by about 3.2 mL of triethylamine. The solution was allowed to react at about 80° C. for about 8 hours. The reaction solvent was then removed in vacuo and the crude oil was taken up in ether....
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccc2scnc2c1
null
CN(C)C=O
null
null
CCN=C=O.Nc1nc2ccc(Cl)cc2s1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(Cl)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8fdf60b6ede54c5a9ab0db4f301291f1
CCNC(=O)Nc1nc2ccc(Cl)cc2s1.O=[N+]([O-])O>>CCNC(=O)Nc1nc2cc([N+](=O)[O-])c(Cl)cc2s1
ClC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.[N+](=O)(O)[O-]>>ClC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1[N+](=O)[O-]
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:15]([Cl:16])[cH:17][c:18]2[s:19]1.O[N+:12](=[O:13])[O-:14]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][c:11]([N+:12](=[O:13])[O-:14])[c:15]([Cl:16])[cH:17][c:18]2[s:19]1
CCNC(=O)Nc1nc2ccc(Cl)cc2s1.O=[N+]([O-])O
CCNC(=O)Nc1nc2cc([N+](=O)[O-])c(Cl)cc2s1
null
null
S(O)(O)(=O)=O
Functional Group Addition
Aromatic nitration with HNO3
668b9c8f526506609a3c1bae67dc3186759376057ca0511251a32d7865e504f8
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccc2scnc2c1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Cl;D1;H0:4]-[c:5]1:[c:6]:[c:7]2:[#16;a:8]:[c:9]:[#7;a:10]:[c:11]:2:[c:12]:[cH;D2;+0:13]:1>>[Cl;D1;H0:4]-[c:5]1:[c:6]:[c:7]2:[#16;a:8]:[c:9]:[#7;a:10]:[c:11]:2:[c:12]:[c;H0;D3;+0:13]:1-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]
null
[]
null
null
1
HOUR
Three grams of N-(6-chloro-1,3-benzothiazol-2-yl)-N′-ethylurea was dissolved in about 15 mL of concentrated sulfuric acid (about 92–94%). The solution was cooled to about 0–5° C. About 1.5 g of ice cooled nitric acid (70% concentration was used, though this is not necessary) was added dropwise. The reaction was held at...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
HO-
S(O)(O)(=O)=O
null
1
CCNC(=O)Nc1nc2ccc(Cl)cc2s1.O=[N+]([O-])O>S(O)(O)(=O)=O>CCNC(=O)Nc1nc2cc([N+](=O)[O-])c(Cl)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6eca5615015f4ce68df2769bea908bce
N#C[S-].N#Cc1ccc(N)cc1>>N#Cc1ccc2nc(N)sc2c1
C(C1=CC=CC=C1)#N.[S-]C#N.[K+].NC1=CC=C(C#N)C=C1.BrBr>>NC=1SC2=C(N1)C=CC(=C2)C#N
[C:8](#[N:9])[S-:10].[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:11][cH:12]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[n:7][c:8]([NH2:9])[s:10][c:11]2[cH:12]1
N#C[S-].N#Cc1ccc(N)cc1
N#Cc1ccc2nc(N)sc2c1
null
null
O.C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
09d23668c864254f076a396c221fe470e495edd36b92b7e2edc27fa4162c1052
c7c78474f6971eeaa7d180c68d4a8af29cb23110025e531bca1233dc3931475c
c1ccc2scnc2c1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[S-;H0;D1:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[NH2;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:4]:[c:5](:[c:6]):[c;H0;D3;+0:7](:[c:8]:[c:9]):[s;H0;D2;+0:3]:1
null
[]
null
null
16
HOUR
4-Aminobenzonitrile is dissolved in acetic acid (or a weak protic acid) and the solution is cooled to about 16–30° C., preferably 16–18° C. Potassium thiocyanate is added and the flask is then equipped with an addition funnel. The addition funnel is charged with bromine and acetic acid. This dark solution is then added...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary amine
Primary amine
c1ccccc1
c1ccc2scnc2c1
c1ccc2scnc2c1
null
O.C(C)(=O)O
null
16
N#C[S-].N#Cc1ccc(N)cc1>O.C(C)(=O)O>N#Cc1ccc2nc(N)sc2c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0c848bca2734433db737a84e3267c158
CCN(CC)CC.CN(C)C=O.N#Cc1ccc2nc(N)sc2c1>>CCNC(=O)Nc1nc2ccc(C#N)cc2s1
C(C)N(CC)CC.NC=1SC2=C(N1)C=CC(=C2)C#N.CN(C=O)C>>C(#N)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
CC[N:3](CC)[CH2:2][CH3:1].CN(C)[CH:4]=[O:5].[NH2:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[N:14])[cH:15][c:16]2[s:17]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[N:14])[cH:15][c:16]2[s:17]1
CCN(CC)CC.CN(C)C=O.N#Cc1ccc2nc(N)sc2c1
CCNC(=O)Nc1nc2ccc(C#N)cc2s1
null
null
null
Acylation
OtherReaction
e77d698eff83e8794b05b3ce5fedd9ef96c82455e86eba1122b49fc0626d6db2
bcb50edc2d59fe372b4cfb78843db7d4062ca25f84556b960638045f86f9e947
c1ccc2scnc2c1
C-C-[N;H0;D3;+0:1](-C-C)-[C:2]-[C;D1;H3:3].C-N(-C)-[CH;D2;+0:4]=[O;D1;H0:5].[NH2;D1;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1>>[C;D1;H3:3]-[C:2]-[NH;D2;+0:1]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1
null
[]
80
CELSIUS
4
HOUR
2-Amino-1,3-benzothiazole-6-carbonitrile is dissolved in a polar aprotic solvent, preferrably dimethylformamide. R3NCO is added, followed by an alkyl amine base, preferably triethylamine and the solution is heated to about 70–90° C., preferably about 80° C., under good agitation. The solution is allowed to stir for abo...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Primary amine.Tertiary amine
Urea
null
null
c1ccc2scnc2c1
Other
null
80
4
CCN(CC)CC.CN(C)C=O.N#Cc1ccc2nc(N)sc2c1>>CCNC(=O)Nc1nc2ccc(C#N)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-5037c9c33a5a49e9b0b5c20797e25f9c
N#C[S-].N#Cc1ccc(N)cc1>>N#Cc1ccc2nc(N)sc2c1
C(C1=CC=CC=C1)#N.[S-]C#N.[K+].NC1=CC=C(C#N)C=C1.BrBr>>NC=1SC2=C(N1)C=CC(=C2)C#N
[C:8](#[N:9])[S-:10].[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:11][cH:12]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[n:7][c:8]([NH2:9])[s:10][c:11]2[cH:12]1
N#C[S-].N#Cc1ccc(N)cc1
N#Cc1ccc2nc(N)sc2c1
null
null
O.C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
09d23668c864254f076a396c221fe470e495edd36b92b7e2edc27fa4162c1052
c7c78474f6971eeaa7d180c68d4a8af29cb23110025e531bca1233dc3931475c
c1ccc2scnc2c1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[S-;H0;D1:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[NH2;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:4]:[c:5](:[c:6]):[c;H0;D3;+0:7](:[c:8]:[c:9]):[s;H0;D2;+0:3]:1
67.4
[{"value": 67.4, "product": "NC=1SC2=C(N1)C=CC(=C2)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
16
CELSIUS
16
HOUR
Two grams of 4-aminobenzonitrile was dissolved in about 40 mL acetic acid and the solution was cooled to about 16° C. About 3.3 g of potassium thiocyanate was added and the flask was equipped with an addition funnel. The addition funnel was charged with about 2.7 g bromine and about 5 mL acetic acid. This dark solution...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary amine
Primary amine
c1ccccc1
c1ccc2scnc2c1
c1ccc2scnc2c1
null
O.C(C)(=O)O
16
16
N#C[S-].N#Cc1ccc(N)cc1>O.C(C)(=O)O>N#Cc1ccc2nc(N)sc2c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-4bb201544c5043cd978fe2b16f5062ab
CCN=C=O.N#Cc1ccc2nc(N)sc2c1>>CCNC(=O)Nc1nc2ccc(C#N)cc2s1
NC=1SC2=C(N1)C=CC(=C2)C#N.C(C)N=C=O.C(C)N(CC)CC>>C(#N)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][N:3]=[C:4]=[O:5].[NH2:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[N:14])[cH:15][c:16]2[s:17]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[N:14])[cH:15][c:16]2[s:17]1
CCN=C=O.N#Cc1ccc2nc(N)sc2c1
CCNC(=O)Nc1nc2ccc(C#N)cc2s1
null
null
CN(C=O)C
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
c1ccc2scnc2c1
[C;D1;H3:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[NH2;D1;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1>>[C;D1;H3:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1
null
[]
80
CELSIUS
4
HOUR
2-Amino-1,3-benzothiazole-6-carbonitrile (0.2 g) was dissolved in about 5 mL dimethylformamide. About 0.2 mL of ethylisocyanate was added, followed by about 0.3 mL triethylamine and the solution was heated to about 80° C. under good agitation. The solution was allowed to stir for about 4 hours then cooled to room tempe...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccc2scnc2c1
null
CN(C=O)C
80
4
CCN=C=O.N#Cc1ccc2nc(N)sc2c1>CN(C=O)C>CCNC(=O)Nc1nc2ccc(C#N)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e8b7ee04ec75448d86e69b5a0568d5fc
C=O.CCN1CN(C)CN(c2nc3ccc([N+](=O)[O-])cc3s2)C1=O.CCNC(=O)Nc1nc2ccc([N+](=O)[O-])cc2s1.CN>>N#Cc1ccc2nc(NC(=O)NCc3cccnc3)sc2c1
CN1CCOCC1.C(C)N1C(N(CN(C1)C)C=1SC2=C(N1)C=CC(=C2)[N+](=O)[O-])=O.C(C)NC(=O)NC=1SC2=C(N1)C=CC(=C2)[N+](=O)[O-].C=O.CN>>C(#N)C1=CC2=C(N=C(S2)NC(=O)NCC=2C=NC=CC2)C=C1
O=[CH2:2].CC[N:18]1[C:17](=O)N(c2nc3c(cc([N+](=O)[O-])[cH:16][cH:15]3)s2)CN(C)[CH2:19]1.O=[N+]([O-])[c:3]1[cH:4][cH:5][c:6]2[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][CH2:13][CH3:14])[s:20][c:21]2[cH:22]1.C[NH2:1]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][CH2:13][c:14]3[cH:15][cH:16][cH:1...
C=O.CCN1CN(C)CN(c2nc3ccc([N+](=O)[O-])cc3s2)C1=O.CCNC(=O)Nc1nc2ccc([N+](=O)[O-])cc2s1.CN
N#Cc1ccc2nc(NC(=O)NCc3cccnc3)sc2c1
null
null
CO.CCO.O
Functional Group Interconversion
OtherReaction
5131c57603f6750f0299e6e79c282d38f1ab637874a31291b2d136aedfeeef39
d624d8d96fc6f2378b9c81de01f9c2535d63f3cc0df91d45260c67c5efe7890e
O=C(NCc1cccnc1)Nc1nc2ccccc2s1
C-C-[N;H0;D3;+0:1]1-[CH2;D2;+0:2]-N(-C)-C-N(-c2:n:c3:[cH;D2;+0:3]:[cH;D2;+0:4]:c(-[N+](=O)-[O-]):c:c:3:s:2)-[C;H0;D3;+0:5]-1=O.C-[NH2;D1;+0:6].O=[CH2;D1;+0:7].O=[N+](-[O-])-[c;H0;D3;+0:8]1:[c:9]:[c:10]2:[#16;a:11]:[c:12](-[#7:13]-[C:14](=[O;D1;H0:15])-[#7:16]-[C:17]-[CH3;D1;+0:18]):[#7;a:19]:[c:20]:2:[c:21]:[c:22]:1>>[...
null
[]
80
CELSIUS
4
HOUR
General procedure for synthesizing 1-ethyl-5-methyl-3-(6-nitro-1,3-benzothiazol-2-yl)-1,3,5-triazinan-2-one: N-Ethyl-N′-(6-nitro-1,3-benzothiazol-2-yl)urea is suspended in an alkanol/water mixture, preferably 1:1 EtOH/H2O at room temperature. A 37% aqueous solution of formaldehyde is added followed by addition of a 2M ...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Urea.Nitro group.Nitro group.Primary amine.Tertiary amine
Nitrile
C1NCNC[NH]1.c1ccc2scnc2c1.c1ccc2scnc2c1
c1ccc2scnc2c1.c1ccncc1
c1ccc2scnc2c1.c1ccncc1
Other
CO.CCO.O
80
4
C=O.CCN1CN(C)CN(c2nc3ccc([N+](=O)[O-])cc3s2)C1=O.CCNC(=O)Nc1nc2ccc([N+](=O)[O-])cc2s1.CN>CO.CCO.O>N#Cc1ccc2nc(NC(=O)NCc3cccnc3)sc2c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3d6f07f08bd342b498abd6f7a943c2cb
C=O.CCNC(=O)Nc1nc2ccc([N+](=O)[O-])cc2s1.CN>>CCN1CN(C)CN(c2nc3ccc([N+](=O)[O-])cc3s2)C1=O
CN1CCOCC1.C(C)NC(=O)NC=1SC2=C(N1)C=CC(=C2)[N+](=O)[O-].C=O.CN>>C(C)N1C(N(CN(C1)C)C=1SC2=C(N1)C=CC(=C2)[N+](=O)[O-])=O
O=[CH2:7].[CH3:1][CH2:2][NH:3][C:21]([NH:8][c:9]1[n:10][c:11]2[cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][c:19]2[s:20]1)=[O:22].[NH2:5][CH3:6]>>[CH3:1][CH2:2][N:3]1[CH2:4][N:5]([CH3:6])[CH2:7][N:8]([c:9]2[n:10][c:11]3[cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18][c:19]3[s:20]2)[C:21]1=[O:22]
C=O.CCNC(=O)Nc1nc2ccc([N+](=O)[O-])cc2s1.CN
CCN1CN(C)CN(c2nc3ccc([N+](=O)[O-])cc3s2)C1=O
null
null
CO.CCO.O
Heteroatom Alkylation and Arylation
OtherReaction
bdea82356d1d675fe90b0ec07e79d17a706b5b14db216d1856803977c01f0274
2bbb8aef114a0ee542edb20042bb6d63f1fdf5f603b0aa000dfbb71b18ea52a0
O=C1NCNCN1c1nc2ccccc2s1
O=[CH2;D1;+0:1].[C;D1;H3:2]-[C:3]-[NH;D2;+0:4]-[C:5](=[O;D1;H0:6])-[NH;D2;+0:7]-[c:8]1:[#16;a:9]:[c:10]:[c:11]:[#7;a:12]:1.[C;D1;H3:13]-[NH2;D1;+0:14]>>[C;D1;H3:2]-[C:3]-[N;H0;D3;+0:4]1-[C:15]-[N;H0;D3;+0:14](-[C;D1;H3:13])-[CH2;D2;+0:1]-[N;H0;D3;+0:7](-[c:8]2:[#16;a:9]:[c:10]:[c:11]:[#7;a:12]:2)-[C:5]-1=[O;D1;H0:6]
null
[]
80
CELSIUS
16
HOUR
N-Ethyl-N′-(6-nitro-1,3-benzothiazol-2-yl)urea (2.8 g) was suspended in about 100 mL 1:1 EtOH/H2O at room temperature. About 8 mL of a 37% aqueous solution of formaldehyde is added followed by addition of about 15 mL of a 2M solution of MeNH2 in MeOH, then about 2.2 mL of N-methylmorpholine. The solution was warmed to ...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Urea.Primary amine
Urea.Tertiary amine
null
C1[NH]C[NH]C[NH]1
C1[NH]C[NH]C[NH]1.c1ccc2scnc2c1
null
CO.CCO.O
80
16
C=O.CCNC(=O)Nc1nc2ccc([N+](=O)[O-])cc2s1.CN>CO.CCO.O>CCN1CN(C)CN(c2nc3ccc([N+](=O)[O-])cc3s2)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0f07a300f177487084962573f64fed09
CCN=C=O.Nc1nc2c(s1)C(=O)CCC2>>CCNC(=O)Nc1nc2c(s1)C(=O)CCC2
CCOCC.NC=1SC2=C(N1)CCCC2=O.C(C)N(CC)CC.C(C)N=C=O>>O=C1CCCC=2N=C(SC21)NC(=O)NCC
[CH3:1][CH2:2][N:3]=[C:4]=[O:5].[NH2:6][c:7]1[n:8][c:9]2[c:10]([s:11]1)[C:12](=[O:13])[CH2:14][CH2:15][CH2:16]2>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[c:10]([s:11]1)[C:12](=[O:13])[CH2:14][CH2:15][CH2:16]2
CCN=C=O.Nc1nc2c(s1)C(=O)CCC2
CCNC(=O)Nc1nc2c(s1)C(=O)CCC2
null
null
CN(C)C=O
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
O=C1CCCc2ncsc21
[C;D1;H3:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[NH2;D1;+0:6]-[c:7]1:[#16;a:8]:[c:9](:[c:10]:[#7;a:11]:1)-[C:12]=[O;D1;H0:13]>>[C;D1;H3:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[c:7]1:[#16;a:8]:[c:9](:[c:10]:[#7;a:11]:1)-[C:12]=[O;D1;H0:13]
85
[{"value": 85.0, "product": "O=C1CCCC=2N=C(SC21)NC(=O)NCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.0, "product": "O=C1CCCC=2N=C(SC21)NC(=O)NCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
3
HOUR
A solution of 2-amino-7-oxo-4,5,6,7-tetrahydro-benzothiazole 3 (11.56 g, 68.7 mmol) in anhydrous DMF (200 mL) was treated with triethylamine (19.2 mL, 137 mmol, 2.0 eq) and ethyl isocyanate (10.9 nL, 137 mmol, 2.0 eq). The reaction mixture was heated at about 90° C. with stirring for about 3 hours. The DMF solvent was ...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1nc2c(s1)CCCC2
null
CN(C)C=O
90
3
CCN=C=O.Nc1nc2c(s1)C(=O)CCC2>CN(C)C=O>CCNC(=O)Nc1nc2c(s1)C(=O)CCC2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-514fddbecd104874be43c28786f03d53
BrBr.CCNC(=O)Nc1nc2c(s1)C(=O)CCC2>>CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2
O=C1CCCC=2N=C(SC21)NC(=O)NCC.Br.BrBr>>BrC1(C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O)Br
[Br:15][Br:16].[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[c:10]([s:11]1)[C:12](=[O:13])[CH2:14][CH2:17][CH2:18]2>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[c:10]([s:11]1)[C:12](=[O:13])[C:14]([Br:15])([Br:16])[CH2:17][CH2:18]2
BrBr.CCNC(=O)Nc1nc2c(s1)C(=O)CCC2
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2
null
null
CC(=O)O
Miscellaneous
OtherReaction
de7f1ef5007cd3b0cdd78b2b3829c93be31702b6b016757b5ad2ec7c305af598
d7e0cb4138f465d209584b403eade9ac08ac7b78b08c53cd9ba80f59a0761110
O=C1CCCc2ncsc21
[#16;a:1]:[c:2]1:[c:3](:[#7;a:4])-[C:5]-[C:6]-[CH2;D2;+0:7]-[C:8]-1=[O;D1;H0:9].[Br;H0;D1;+0:10]-[Br;H0;D1;+0:11]>>[#16;a:1]:[c:2]1:[c:3](:[#7;a:4])-[C:5]-[C:6]-[C;H0;D4;+0:7](-[Br;H0;D1;+0:10])(-[Br;H0;D1;+0:11])-[C:8]-1=[O;D1;H0:9]
937.5
[{"value": 94.0, "product": "BrC1(C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O)Br", "details": "PERCENTYIELD", "is_desired": false}, {"value": 937.5, "product": "BrC1(C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O)Br", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
45
CELSIUS
null
null
A solution of 1-(7-oxo-4,5,6,7-tetrahydro-2-benzothiazolyl)-3-ethyl-urea 4 (5.00 g, 20.9 mmol), 48% HBr (aq) (1.20 mL, 2.09 mmol, 0.1 eq) and AcOH (451 mL) was treated dropwise with a solution of Br2 (2.21 mL, 42.8 mmol, 2.05 eq) in AcOH (5 mL) with stirring. The reaction mixture was heated at about 45° C. with stirrin...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary halide.Tertiary halide
c1nc2c(s1)CCCC2
c1nc2c(s1)CCCC2
c1nc2c(s1)CCCC2
null
CC(=O)O
45
null
BrBr.CCNC(=O)Nc1nc2c(s1)C(=O)CCC2>CC(=O)O>CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-4f2e74aefc354a3f8e93f452a584a7ad
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2>>CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1
BrC1(C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O)Br.C1CCC2=NCCCN2CC1.C1CCC2=NCCCN2CC1>>BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O
Br[C:12]1([Br:13])[CH2:11][CH2:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:17][c:16]2[C:14]1=[O:15]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([OH:15])[c:16]2[s:17]1
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1
null
null
C1CCOC1
Functional Group Interconversion
OtherReaction
182ebab0a44dcfaa96f2549e00b7a0898ae20a92e3eb7bd3780b196f3b0a5fb9
d41de2414b2cfa6a39168b2591625983cd73933a93e7987f54fa6db9b391c613
c1ccc2scnc2c1
Br-[C;H0;D4;+0:1]1(-[Br;D1;H0:2])-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[c:5]2:[#7;a:6]:[c:7]:[#16;a:8]:[c:9]:2-[C;H0;D3;+0:10]-1=[O;H0;D1;+0:11]>>[Br;D1;H0:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5]2:[#7;a:6]:[c:7]:[#16;a:8]:[c:9]:2:[c;H0;D3;+0:10]:1-[OH;D1;+0:11]
78
[{"value": 78.0, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.9, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
18
HOUR
A suspension of 1-(6,6-dibromo-7-oxo-4,5,6,7-tetrahydro-2-benzothiazolyl)-3-ethyl-urea 5 (7.78 g, 19.6 mmol) in THF (50 mL) was treated with DBU (8.79 mL, 58.8 mmol, 3.0 eq) dropwise at about 20° C. A dark green suspension was obtained while heat was generated upon addition of DBU. It was stirred at about 20° C. for ab...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Ketone
Aromatic halide.Aromatic alcohol
c1nc2c(s1)CCCC2
c1ccc2scnc2c1
c1ccc2scnc2c1
HBr
C1CCOC1
20
18
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2>C1CCOC1>CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-091d1065bf6a4e45857801ca9cde86da
BrBr.CCNC(=O)Nc1nc2c(s1)C(=O)CCC2>>CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)CC2
O=C1CCCC=2N=C(SC21)NC(=O)NCC.Br.BrBr>>BrC1C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O
Br[Br:15].[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[c:10]([s:11]1)[C:12](=[O:13])[CH2:14][CH2:16][CH2:17]2>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[c:10]([s:11]1)[C:12](=[O:13])[CH:14]([Br:15])[CH2:16][CH2:17]2
BrBr.CCNC(=O)Nc1nc2c(s1)C(=O)CCC2
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)CC2
null
null
CC(=O)O
Functional Group Interconversion
Bromination
c1da30deb3c2b1d2b15808c016938f0e62d86bb3f9dfee9bd96f482ea3a67ece
fe149a07f370bdd2ea40b2dff4f3462711fb34a60b8733c443efdeb5ab4d5c53
O=C1CCCc2ncsc21
Br-[Br;H0;D1;+0:1].[#16;a:2]:[c:3]1:[c:4](:[#7;a:5])-[C:6]-[C:7]-[CH2;D2;+0:8]-[C:9]-1=[O;D1;H0:10]>>[#16;a:2]:[c:3]1:[c:4](:[#7;a:5])-[C:6]-[C:7]-[CH;D3;+0:8](-[Br;H0;D1;+0:1])-[C:9]-1=[O;D1;H0:10]
166.9
[{"value": 83.0, "product": "BrC1C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 166.9, "product": "BrC1C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
45
CELSIUS
null
null
A solution of 1-(7-oxo-4,5,6,7-tetrahydro-2-benzothiazolyl)-3-ethyl-urea 4 (1.00 g, 4.18 mmol) and 48% HBr (aq) (0.24 mL, 2.09 mmol, 0.5 eq) in AcOH (18 mL) was treated dropwise with a solution of Br2 (0.23 mL, 4.39 mmol, 1.05 eq) in AcOH (1 mL) with stirring. The reaction mixture was heated at about 45° C. with stirri...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary halide
c1nc2c(s1)CCCC2
c1nc2c(s1)CCCC2
c1nc2c(s1)CCCC2
HBr
CC(=O)O
45
null
BrBr.CCNC(=O)Nc1nc2c(s1)C(=O)CCC2>CC(=O)O>CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)CC2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f28c76dea7f44a58b87eb28465351440
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2>>CCNC(=O)Nc1nc2cccc(O)c2s1
BrC1(C(C2=C(N=C(S2)NC(=O)NCC)CC1)=O)Br.C1CCC2=NCCCN2CC1.C1CCC2=NCCCN2CC1>>OC1=CC=CC=2N=C(SC21)NC(=O)NCC
Br[C:12]1(Br)[CH2:11][CH2:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:16][c:15]2[C:13]1=[O:14]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][cH:12][c:13]([OH:14])[c:15]2[s:16]1
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2
CCNC(=O)Nc1nc2cccc(O)c2s1
null
null
C1CCOC1
Miscellaneous
OtherReaction
ae229ce338b8acc1177e28dc753f0d19e887ebbc1f31e2eebcb619dbd23b7878
fc192a81bb1b5ef7110cb68881e9a7f5a22c45e549875dffdc37c7a80468b788
c1ccc2scnc2c1
Br-[C;H0;D4;+0:1]1(-Br)-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]>>[OH;D1;+0:10]-[c;H0;D3;+0:9]1:[cH;D2;+0:1]:[cH;D2;+0:2]:[cH;D2;+0:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:1
32.2
[{"value": 32.0, "product": "OC1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 32.2, "product": "OC1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
18
HOUR
To a suspension of 1-(6-bromo-7-oxo-4,5,6,7-tetrahydro-2-benzothiazolyl)-3-ethyl-urea 5 (0.100 g, 0.314 mmol) in THF (1.0 mL) was added DBU (0.141 mL, 0.94 mmol, 3 eq) dropwise at about 20° C. A dark green suspension was obtained while heat was generated upon addition of DBU. It was stirred at about 20° C. for about 18...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Ketone
Aromatic alcohol
c1nc2c(s1)CCCC2
c1ccc2scnc2c1
c1ccc2scnc2c1
Br-
C1CCOC1
20
18
CCNC(=O)Nc1nc2c(s1)C(=O)C(Br)(Br)CC2>C1CCOC1>CCNC(=O)Nc1nc2cccc(O)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b7720941bb934e35991fd79ffdaedd76
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>>CCNC(=O)Nc1nc2cccc(O)c2s1
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.C([O-])([O-])=O.[K+].[K+].CO>>OC1=CC=CC=2N=C(SC21)NC(=O)NCC
Br[c:12]1[cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:16][c:15]2[c:13]1[OH:14]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][cH:12][c:13]([OH:14])[c:15]2[s:16]1
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1
CCNC(=O)Nc1nc2cccc(O)c2s1
null
null
CN(C)C=O
Functional Group Interconversion
Aromatic dehalogenation
776c7f75e87bb735c9b3cad39517ab7ffb5754e38a78c449a72d14189b4df482
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccc2scnc2c1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1-[O;D1;H1:10]>>[O;D1;H1:10]-[c:9]1:[cH;D2;+0:1]:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:1:2
null
[]
20
CELSIUS
0.5
HOUR
General Procedure for 1-(6-bromo-7-alkoxy-2-benzothiazolyl)-3-ethyl-urea compounds 9–13. A mixture of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea 6 and potassium carbonate (1.05 eq) in anhydrous DMF was stirred at about 20° C. for about 0.5 hour, and was cooled down to about 0° C. The mixture was treated with a...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
Br-
CN(C)C=O
20
0.5
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>CN(C)C=O>CCNC(=O)Nc1nc2cccc(O)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c5baa1466eb64f28875bdeda9757c685
BrCc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>>CCNC(=O)Nc1nc2ccc(Br)c(OCc3ccccc3)c2s1
CO.BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)Br>>BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OCC1=CC=CC=C1
Br[CH2:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1.[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([OH:15])[c:23]2[s:24]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([O:15][CH2:16][c:17]3[cH:18][cH:19][cH:20][cH:21][cH:22]3)...
BrCc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1
CCNC(=O)Nc1nc2ccc(Br)c(OCc3ccccc3)c2s1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2cccc3ncsc23)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]1:[#16;a:9]:[c:10]:[#7;a:11]:[c:12]:1>>[c:7]:[c:6](-[O;H0;D2;+0:5]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:8]1:[#16;a:9]:[c:10]:[#7;a:11]:[c:12]:1
45
[{"value": 45.0, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.6, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
0.5
HOUR
A mixture of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea 6 (0.050 g, 0.16 mmol) and potassium carbonate (0.023 g, 0.17 mmol, 1.05 eq) in anhydrous DMF (1.6 mL) was stirred at about 20° C. for about 0.5 hour, and was cooled down to about 0° C. The reaction mixture was treated with benzyl bromide (0.019 mL, 0.16 ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2scnc2c1.c1ccccc1
HBr
CN(C)C=O
20
0.5
BrCc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(Br)c(OCc3ccccc3)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-12cf03b2e2304f0c877426f44e1029ac
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.CI>>CCNC(=O)Nc1nc2ccc(Br)c(OC)c2s1
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.C([O-])([O-])=O.[K+].[K+].IC>>BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OC
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([OH:15])[c:17]2[s:18]1.I[CH3:16]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([O:15][CH3:16])[c:17]2[s:18]1
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.CI
CCNC(=O)Nc1nc2ccc(Br)c(OC)c2s1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
b8b041187bac58376aae824630608e7deb49a01db3d652291f8b379c10d4e434
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
c1ccc2scnc2c1
I-[CH3;D1;+0:1].[OH;D1;+0:2]-[c:3](:[c:4]):[c:5]1:[#16;a:6]:[c:7]:[#7;a:8]:[c:9]:1>>[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]1:[#16;a:6]:[c:7]:[#7;a:8]:[c:9]:1
2
[{"value": 2.0, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea 6, potassium carbonate and iodomethane in DMF was reacted to give 0.0034 g (2%) of the desired compound 10. 1H NMR (DMSO) δ 10.88 (br s, 1H, NH), 7.55 (d, 1H, J=8.5 Hz, ArH), 7.33 (d, 1H, J=8.5 Hz, ArH), 6.82 (br s, 1H, NH), 3.93 (s, 3H, CH3), 3.18 (m, 2H...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
null
null
c1ccc2scnc2c1
HI
CN(C)C=O
null
null
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.CI>CN(C)C=O>CCNC(=O)Nc1nc2ccc(Br)c(OC)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a370cc9a12cf48bda09d8ac2cf6359f2
CC(C)Br.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>>CCNC(=O)Nc1nc2ccc(Br)c(OC(C)C)c2s1
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.C([O-])([O-])=O.[K+].[K+].BrC(C)C>>BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OC(C)C
Br[CH:16]([CH3:17])[CH3:18].[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([OH:15])[c:19]2[s:20]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([O:15][CH:16]([CH3:17])[CH3:18])[c:19]2[s:20]1
CC(C)Br.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1
CCNC(=O)Nc1nc2ccc(Br)c(OC(C)C)c2s1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
bff4876be49b448135c783dd3eeeb68ab3cc5bdc91beadda8a9095106cd5c747
cf768afb66ed5041aefdce1fa6d1e40995a1ab7c4b4a4ca47544fe49ee1e629f
c1ccc2scnc2c1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C;D1;H3:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]1:[#16;a:8]:[c:9]:[#7;a:10]:[c:11]:1>>[C;D1;H3:2]-[CH;D3;+0:1](-[C;D1;H3:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]1:[#16;a:8]:[c:9]:[#7;a:10]:[c:11]:1
81
[{"value": 81.0, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OC(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea 6, potassium carbonate and 2-bromopropane in DMF was reacted to give 0.046 g (81%) of the desired compound 11. 1H NMR (DMSO) δ 10.83 (br s, 1H, NH), 7.55 (d, 1H, J=8.5 Hz, ArH), 7.31 (d, 1H, J=8.6 Hz, ArH), 6.71 (br s, 1H, NH), 4.69 (hept, 1H, J=6.0 Hz, C...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol
Ether
null
null
c1ccc2scnc2c1
HBr
CN(C)C=O
null
null
CC(C)Br.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(Br)c(OC(C)C)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6994d4027fca4d73947eb9301277e302
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.COCCOCCBr>>CCNC(=O)Nc1nc2ccc(Br)c(OCCOCCOC)c2s1
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.C([O-])([O-])=O.[K+].[K+].COCCOCCBr>>BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OCCOCCOC
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([OH:15])[c:23]2[s:24]1.Br[CH2:16][CH2:17][O:18][CH2:19][CH2:20][O:21][CH3:22]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([O:15][CH2:16][CH2:17][O:18][CH2:19][CH2:20][O:21][CH3:22...
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.COCCOCCBr
CCNC(=O)Nc1nc2ccc(Br)c(OCCOCCOC)c2s1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2scnc2c1
Br-[CH2;D2;+0:1]-[C:2]-[#8:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]1:[#16;a:8]:[c:9]:[#7;a:10]:[c:11]:1>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]1:[#16;a:8]:[c:9]:[#7;a:10]:[c:11]:1
39
[{"value": 39.0, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OCCOCCOC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea 6, potassium carbonate and 2-(2-methoxyethoxy)ethyl bromide in DMF was reacted to give 0.026 g (39%) of the desired compound 12. 1H NMR (DMSO) δ 10.65 (br s, 1H, NH), 7.54 (d, 1H, J=8.5 Hz, ArH), 7.32 (d, 1H, J=8.6 Hz, ArH), 6.73 (br s, 1H, NH), 4.24 (d, ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2scnc2c1
HBr
CN(C)C=O
null
null
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.COCCOCCBr>CN(C)C=O>CCNC(=O)Nc1nc2ccc(Br)c(OCCOCCOC)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6778be28994349a58c0ea43b72428dba
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.Fc1ccc(CBr)cc1>>CCNC(=O)Nc1nc2ccc(Br)c(OCc3ccc(F)cc3)c2s1
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.C([O-])([O-])=O.[K+].[K+].FC1=CC=C(CBr)C=C1>>BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OCC1=CC=C(C=C1)F
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([OH:15])[c:24]2[s:25]1.Br[CH2:16][c:17]1[cH:18][cH:19][c:20]([F:21])[cH:22][cH:23]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([O:15][CH2:16][c:17]3[cH:18][cH:19][c:20]([F:21])[c...
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.Fc1ccc(CBr)cc1
CCNC(=O)Nc1nc2ccc(Br)c(OCc3ccc(F)cc3)c2s1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2cccc3ncsc23)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]1:[#16;a:9]:[c:10]:[#7;a:11]:[c:12]:1>>[c:7]:[c:6](-[O;H0;D2;+0:5]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:8]1:[#16;a:9]:[c:10]:[#7;a:11]:[c:12]:1
19
[{"value": 19.0, "product": "BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OCC1=CC=C(C=C1)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea 6, potassium carbonate and p-fluoro-benzyl-bromide in DMF was reacted to give 0.013 g (19%) of the desired compound 13. 1H NMR (DMSO) δ 1.08 (t, 3H, J=8 Hz CH2CH3), 3.18 (m, 2H, CH2), 5.16 (s, 2H, OCH2Ar), 6.73 (br s, 1H, NH), 7.26 (dd, 2H, J=4, 4 Hz, ArH...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2scnc2c1.c1ccccc1
HBr
CN(C)C=O
null
null
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.Fc1ccc(CBr)cc1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(Br)c(OCc3ccc(F)cc3)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-871ba8cd3b864435860dd69669537659
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.O=S(=O)(OS(=O)(=O)C(F)(F)F)C(F)(F)F>>CCNC(=O)Nc1nc2ccc(Br)c(S(=O)(=O)C(F)(F)F)c2s1
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.O(S(=O)(=O)C(F)(F)F)S(=O)(=O)C(F)(F)F>>BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)S(=O)(=O)C(F)(F)F
O[c:14]1[c:12]([Br:13])[cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:23][c:22]21.O=S(=O)(O[S:15](=[O:16])(=[O:17])[C:18]([F:19])([F:20])[F:21])C(F)(F)F>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[c:14]([S:15](=[O:16])(=[O:17])[C:18]([F:19])([F:20])[...
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.O=S(=O)(OS(=O)(=O)C(F)(F)F)C(F)(F)F
CCNC(=O)Nc1nc2ccc(Br)c(S(=O)(=O)C(F)(F)F)c2s1
null
null
N1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
7674ed2e5f64ab8fff3f27a750a5930306ccf9e2d3f773d1ecbf4ee9d29858d2
5f0ac2514d72d3f96bd6091be4d08699e506de1e84622ae8bde68f2cee9ab5d6
c1ccc2scnc2c1
F-C(-F)(-F)-S(=O)(=O)-O-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[F;D1;H0:7].O-[c;H0;D3;+0:8]1:[c:9](-[Br;D1;H0:10]):[c:11]:[c:12]:[c:13]2:[#7;a:14]:[c:15]:[#16;a:16]:[c:17]:2:1>>[Br;D1;H0:10]-[c:9]1:[c:11]:[c:12]:[c:13]2:[#7;a:14]:[c:15]:[#16;a:16]:[c:17]:2:[c;H0;D3;+0:8]:1-[S;H0;D4...
null
[]
35
CELSIUS
3
HOUR
To a solution of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea (50 mg, 0.158 mmol) in pyridine (1 mL) were added 3 portions of (CF3SO2)2O (29 μL, 0.174 mmol) about 45 minutes apart. The reaction mixture was stirred for about 3 hours at about 35° C. The solvent was then evaporated. The crude material was purified ...
10.6084/m9.figshare.5104873.v1
null
Triflate.Triflate.Aromatic alcohol
Sulfone
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
TfOH.HO-
N1=CC=CC=C1
35
3
CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1.O=S(=O)(OS(=O)(=O)C(F)(F)F)C(F)(F)F>N1=CC=CC=C1>CCNC(=O)Nc1nc2ccc(Br)c(S(=O)(=O)C(F)(F)F)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c336b764197e420a978d946859501796
CCNC(=O)Nc1nc2cccc(O)c2s1.O=[N+]=O>>CCNC(=O)Nc1nc2ccc([N+](=O)[O-])c(O)c2s1
OC1=CC=CC=2N=C(SC21)NC(=O)NCC.F[B-](F)(F)F.O=[N+]=O>>OC1=C(C=CC=2N=C(SC21)NC(=O)NCC)[N+](=O)[O-]
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][cH:12][c:16]([OH:17])[c:18]2[s:19]1.[N+:13](=[O:14])=[O:15]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[c:16]([OH:17])[c:18]2[s:19]1
CCNC(=O)Nc1nc2cccc(O)c2s1.O=[N+]=O
CCNC(=O)Nc1nc2ccc([N+](=O)[O-])c(O)c2s1
null
null
C(C)OCC.C(C)#N
Functional Group Addition
OtherReaction
3db8a56438dbfcd47114c5d6aa6c6bdcd06ee8af429447c5f40cfdd0f6b6476a
5c75a9bf759be9717d985245c85c84dbfff904ea5287869736b84fdaa57f1e27
c1ccc2scnc2c1
[O;D1;H0:1]=[N+;H0;D2:2]=[O;H0;D1;+0:3].[O;D1;H1:4]-[c:5]1:[cH;D2;+0:6]:[c:7]:[c:8]:[c:9]2:[#7;a:10]:[c:11]:[#16;a:12]:[c:13]:1:2>>[O-;H0;D1:3]-[N+;H0;D3:2](=[O;D1;H0:1])-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[c:9]2:[#7;a:10]:[c:11]:[#16;a:12]:[c:13]:2:[c:5]:1-[O;D1;H1:4]
10.4
[{"value": 10.0, "product": "OC1=C(C=CC=2N=C(SC21)NC(=O)NCC)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 10.4, "product": "OC1=C(C=CC=2N=C(SC21)NC(=O)NCC)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
5
MINUTE
To a solution of 2-methylpyridone (0.020 mL, 0.20 mmol, 1.2 eq) in anhydrous acetonitrile (0.5 mL), nitronium tetrafluoroborate (0.045 g, 0.32 mmol, 1.9 eq) was added. The suspension was stirred at about 20° C. for about 5 minutes to get an orange solution. The solution was then transferred to a suspension of 1-(7-hydr...
10.6084/m9.figshare.5104873.v1
null
Nitroso.Nitroso
Nitro group
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
null
C(C)OCC.C(C)#N
20
0.083333
CCNC(=O)Nc1nc2cccc(O)c2s1.O=[N+]=O>C(C)OCC.C(C)#N>CCNC(=O)Nc1nc2ccc([N+](=O)[O-])c(O)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2f5cc1a1e92a4c30a33e6ae5e6746e67
BrBr.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>>CCNC(=O)Nc1nc2c(Br)cc(Br)c(O)c2s1
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)O.BrBr.C1(=CC=CC=C1)C>>BrC1=CC(=C(C2=C1N=C(S2)NC(=O)NCC)O)Br
Br[Br:11].[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:12][c:13]([Br:14])[c:15]([OH:16])[c:17]2[s:18]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[c:10]([Br:11])[cH:12][c:13]([Br:14])[c:15]([OH:16])[c:17]2[s:18]1
BrBr.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1
CCNC(=O)Nc1nc2c(Br)cc(Br)c(O)c2s1
null
null
CC(=O)O
Functional Group Interconversion
Bromination
42ba26ec59d66e34c4ffd51d0bc49d29a4fe2f80ce47b015ee1e31fc90c660cd
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2scnc2c1
Br-[Br;H0;D1;+0:1].[#16;a:2]1:[c:3]:[#7;a:4]:[c:5]2:[cH;D2;+0:6]:[c:7]:[c:8]:[c:9]:[c:10]:1:2>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[c:9]:[c:10]2:[#16;a:2]:[c:3]:[#7;a:4]:[c:5]:2:1
null
[]
20
CELSIUS
15
MINUTE
To a suspension of 1-(6-bromo-7-hydroxy-2-benzothiazolyl)-3-ethyl-urea (50 mg, 0.158 mmol) in AcOH (2 mL) at about 20° C. was added Br2 (9 μl, 0.174 mmol). The reaction mixture was stirred at about 20° C. for about 15 minutes. Toluene (10 mL) was added and the solvents evaporated. The crude material was purified by pre...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
HBr
CC(=O)O
20
0.25
BrBr.CCNC(=O)Nc1nc2ccc(Br)c(O)c2s1>CC(=O)O>CCNC(=O)Nc1nc2c(Br)cc(Br)c(O)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1a6875afea914c3fb284eeb3add847f4
C#C[Si](C)(C)C.CCNC(=O)Nc1nc2cccc(S(=O)(=O)C(F)(F)F)c2s1>>CCNC(=O)Nc1nc2cccc(C#C[Si](C)(C)C)c2s1
FC(S(=O)(=O)C1=CC=CC=2N=C(SC21)NC(=O)NCC)(F)F.C(C)N(CC)CC.C[Si](C)(C)C#C>>C[Si](C)(C)C#CC1=CC=CC=2N=C(SC21)NC(=O)NCC
[CH:14]#[C:15][Si:16]([CH3:17])([CH3:18])[CH3:19].O=S(=O)(C(F)(F)F)[c:13]1[cH:12][cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:21][c:20]21>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][cH:12][c:13]([C:14]#[C:15][Si:16]([CH3:17])([CH3:18])[CH3:19])[c:20]2[s:21]1
C#C[Si](C)(C)C.CCNC(=O)Nc1nc2cccc(S(=O)(=O)C(F)(F)F)c2s1
CCNC(=O)Nc1nc2cccc(C#C[Si](C)(C)C)c2s1
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CO.CN(C)C=O
C-C Coupling
OtherReaction
b089807d2270da66e4017f883e8fc70aa59f7eb4c69322f959c73f607cbaa1f3
4e971c26e411eb96e6bdc2680fd74feac55fede1a4ae64a25e6a61867967b471
c1ccc2scnc2c1
F-C(-F)(-F)-S(=O)(=O)-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[#16;a:8]:[c:9]:2:1.[C;D1;H3:10]-[#14:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[C:14]#[CH;D1;+0:15]>>[C;D1;H3:10]-[#14:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[C:14]#[C;H0;D2;+0:15]-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[#16;a:8]:[c:9]:2...
93
[{"value": 93.0, "product": "C[Si](C)(C)C#CC1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.6, "product": "C[Si](C)(C)C#CC1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
18
HOUR
A mixture of 1-(7-trifluoromethylsulfonyl-2-benzothiazolyl)-3-ethylurea (0.080 g, 80% pure, 0.17 mmol), Pd(PPh3)2Cl2 (0.010 g, 0.014 mmol, 0.08 eq), and triethylamine (0.102 mL, 0.73 mmol, 4.3 eq) in 1 mL of anhydrous DMF was bubbled with nitrogen gas for 5 minutes, followed by the addition of trimethylsilyl acetylene ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Sulfone.Alkyne
Alkyne
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
HF
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO.CN(C)C=O
100
18
C#C[Si](C)(C)C.CCNC(=O)Nc1nc2cccc(S(=O)(=O)C(F)(F)F)c2s1>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO.CN(C)C=O>CCNC(=O)Nc1nc2cccc(C#C[Si](C)(C)C)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8abe128357e5495cb8583bed1bcfdda2
CCNC(=O)Nc1nc2cccc(C#C[Si](C)(C)C)c2s1>>C#Cc1cccc2nc(NC(=O)NCC)sc12
C[Si](C)(C)C#CC1=CC=CC=2N=C(SC21)NC(=O)NCC.[OH-].[K+].CN(C)C=O.CO>>C(#C)C1=CC=CC=2N=C(SC21)NC(=O)NCC
C[Si](C)(C)[C:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][CH2:14][CH3:15])[s:16][c:17]12>>[CH:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][CH2:14][CH3:15])[s:16][c:17]12
CCNC(=O)Nc1nc2cccc(C#C[Si](C)(C)C)c2s1
C#Cc1cccc2nc(NC(=O)NCC)sc12
null
null
CO.CCCCCCC
Deprotection
TMS deprotection from alkyne
e85676bb81da384790c9c858d44f182cdd01e3a79f77f7a239fe38487234cb96
56d526d7c9cb1bd7bee4940e216a9b1dd4597fd025a186b8d6e4675d8f4db26b
c1ccc2scnc2c1
C-[Si](-C)(-C)-[C;H0;D2;+0:1]#[C:2]-[c:3]:[c:4]:[#16;a:5]>>[#16;a:5]:[c:4]:[c:3]-[C:2]#[CH;D1;+0:1]
15.3
[{"value": 15.0, "product": "C(#C)C1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 15.3, "product": "C(#C)C1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A mixture of 1-(7-trimethylsilylacetylenyl-2-benzothiazolyl)-3-ethylurea 2 (0.050 g, 0.16 mmol) and 1M aqueous KOH solution (0.16 mL, 0.16 mmol, 1.0 eq) in 1.5 mL of 2/1 mixture of DMF/MeOH was stirred at room temperature for about 2 hours. The mixture was taken up in 10 mL MeOH and the precipitation was filtered off. ...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Silyl protective group
Alkyne
null
null
c1ccc2scnc2c1
Other
CO.CCCCCCC
null
2
CCNC(=O)Nc1nc2cccc(C#C[Si](C)(C)C)c2s1>CO.CCCCCCC>C#Cc1cccc2nc(NC(=O)NCC)sc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9a4c0e1c1fc94c6586402782e0c32725
CCNC(=O)Nc1nc2ccc(Br)c(OC(C)C)c2s1>>CCNC(=O)Nc1nc2cccc(OC(C)C)c2s1
[Li]CCCC.BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)OC(C)C.ClN1C(CCC1=O)=O>>C(C)(C)OC1=CC=CC=2N=C(SC21)NC(=O)NCC
Br[c:12]1[cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:19][c:18]2[c:13]1[O:14][CH:15]([CH3:16])[CH3:17]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][cH:12][c:13]([O:14][CH:15]([CH3:16])[CH3:17])[c:18]2[s:19]1
CCNC(=O)Nc1nc2ccc(Br)c(OC(C)C)c2s1
CCNC(=O)Nc1nc2cccc(OC(C)C)c2s1
null
null
CO.COCCOC
Functional Group Interconversion
Aromatic dehalogenation
776c7f75e87bb735c9b3cad39517ab7ffb5754e38a78c449a72d14189b4df482
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccc2scnc2c1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1-[#8:10]>>[#8:10]-[c:9]1:[cH;D2;+0:1]:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:1:2
25.1
[{"value": 25.0, "product": "C(C)(C)OC1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 25.1, "product": "C(C)(C)OC1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
20
MINUTE
A solution of 1-(6-bromo-7-isopropoxy-2-benzothiazolyl)-3-ethylurea (0.036 g, 0.10 mmol) in 0.5 mL DME was cooled down to about −78° C., and was treated with a solution of 1.6 M n-BuLi in hexanes (0.16 mL, 0.26 mmol, 2.6 eq). It was stirred at the temperature for about 20 min, then a solution of N-chlorosuccinimide (NC...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
Br-
CO.COCCOC
0
0.333333
CCNC(=O)Nc1nc2ccc(Br)c(OC(C)C)c2s1>CO.COCCOC>CCNC(=O)Nc1nc2cccc(OC(C)C)c2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1b2a9a1d73d34afbbad146c0399680cb
C=[CH][Sn]([CH]=C)([CH]=C)[CH]=C.CCNC(=O)Nc1nc2cccc(S(=O)(=O)C(F)(F)F)c2s1>>C=Cc1cccc2nc(NC(=O)NCC)sc12
FC(S(=O)(=O)C1=CC=CC=2N=C(SC21)NC(=O)NCC)(F)F.[Cl-].[Li+].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(=C)[Sn](C=C)(C=C)C=C>>C(=C)C1=CC=CC=2N=C(SC21)NC(=O)NCC
C=[CH][Sn]([CH]=C)([CH]=C)[CH:2]=[CH2:1].O=S(=O)(C(F)(F)F)[c:3]1[cH:4][cH:5][cH:6][c:7]2[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][CH2:14][CH3:15])[s:16][c:17]12>>[CH2:1]=[CH:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][CH2:14][CH3:15])[s:16][c:17]12
C=[CH][Sn]([CH]=C)([CH]=C)[CH]=C.CCNC(=O)Nc1nc2cccc(S(=O)(=O)C(F)(F)F)c2s1
C=Cc1cccc2nc(NC(=O)NCC)sc12
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
null
C-C Coupling
OtherReaction
3497ccc5b3feccb81acd801312140b9382eb1d91628704ea2f1b20a31f06a7d4
442c6cecbfc241ab3f8437ed659158a1c002809445f8019bc11d84c4a025a81d
c1ccc2scnc2c1
C=[CH]-[Sn](-[CH;D2;+0:1]=[C;D1;H2:2])(-[CH]=C)-[CH]=C.F-C(-F)(-F)-S(=O)(=O)-[c;H0;D3;+0:3]1:[c:4]:[c:5]:[c:6]:[c:7]2:[#7;a:8]:[c:9]:[#16;a:10]:[c:11]:2:1>>[C;D1;H2:2]=[CH;D2;+0:1]-[c;H0;D3;+0:3]1:[c:4]:[c:5]:[c:6]:[c:7]2:[#7;a:8]:[c:9]:[#16;a:10]:[c:11]:2:1
24.5
[{"value": 14.0, "product": "C(=C)C1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 24.5, "product": "C(=C)C1=CC=CC=2N=C(SC21)NC(=O)NCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
Similar to the synthesis of Example 203, a mixture of 1-(7-trifluoromethylsulfonyl-2-benzothiazolyl)-3-ethylurea (0.050 g, 80% pure, 0.11 mmol), lithium chloride (0.039 g, 0.92 mmol, 8.4 eq), triphenylphosphine (0.017 g, 0.066 mmol, 0.6 eq), Pd(PPh3)2Cl2 (0.009 g, 0.013 mmol, 0.12 eq), tetravinyltin (0.040 mL, 0.22 mmo...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Sulfone.Vinyl.Vinyl.Vinyl.Vinyl.Tin
Vinyl
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
HF.Sn
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
100
null
C=[CH][Sn]([CH]=C)([CH]=C)[CH]=C.CCNC(=O)Nc1nc2cccc(S(=O)(=O)C(F)(F)F)c2s1>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl>C=Cc1cccc2nc(NC(=O)NCC)sc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-43344259a13143f2b751032583d652d5
C=[CH][Sn]([CH]=C)([CH]=C)[CH]=C.CCNC(=O)Nc1nc2ccc(Br)c(S(=O)(=O)C(F)(F)F)c2s1>>C=Cc1ccc2nc(NC(=O)NCC)sc2c1C=C
BrC1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)S(=O)(=O)C(F)(F)F.[Cl-].[Li+].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(=C)[Sn](C=C)(C=C)C=C.[Sn]>>C(=C)C1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)C=C
C=[CH][Sn]([CH]=C)([CH:2]=[CH2:1])[CH:18]=[CH2:19].O=S(=O)(C(F)(F)F)[c:17]1[c:3](Br)[cH:4][cH:5][c:6]2[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][CH2:13][CH3:14])[s:15][c:16]21>>[CH2:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]2[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][CH2:13][CH3:14])[s:15][c:16]2[c:17]1[CH:18]=[CH2:19]
C=[CH][Sn]([CH]=C)([CH]=C)[CH]=C.CCNC(=O)Nc1nc2ccc(Br)c(S(=O)(=O)C(F)(F)F)c2s1
C=Cc1ccc2nc(NC(=O)NCC)sc2c1C=C
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CO
C-C Coupling
OtherReaction
1148c4f7a7eb27ea822712bcb7856d412139833bcbe1012c1bdb4acd80153df0
dd54cc01242eb3808113b5ff0843c27c76ad02e5faff96f50dec9c764e22c4a5
c1ccc2scnc2c1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c;H0;D3;+0:9]:1-S(=O)(=O)-C(-F)(-F)-F.C=[CH]-[Sn](-[CH;D2;+0:10]=[C;D1;H2:11])(-[CH;D2;+0:12]=[C;D1;H2:13])-[CH]=C>>[C;D1;H2:11]=[CH;D2;+0:10]-[c;H0;D3;+0:9]1:[c:8]2:[#16;a:7]:[c:6]:[#7;a:5]:[c:4]:2:[c:3]:[c:2]:[c;H0;D3;+0:1]:1-[CH;D2;+0:12]=[C;D1;...
39.4
[{"value": 23.0, "product": "C(=C)C1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)C=C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 39.4, "product": "C(=C)C1=C(C2=C(N=C(S2)NC(=O)NCC)C=C1)C=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
Similar to the synthesis of Example 203, a mixture of 1-(6-bromo-7-trifluoromethylsulfonyl-2-benzothiazolyl)-3-ethylurea (0.100 g, 0.22 mmol), lithium chloride (0.078 g, 1.84 mmol, 8.4 eq), triphenylphosphine (0.034 g, 0.13 mmol, 0.6 eq), Pd(PPh3)2Cl2 (0.018 g, 0.026 mmol, 0.12 eq), tetravinyltin (0.080 mL, 0.44 mmol, ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Tertiary halide.Tertiary halide.Tertiary halide.Sulfone.Vinyl.Vinyl.Vinyl.Vinyl.Tin
Vinyl.Vinyl
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
HF.Br-.Sn
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO
100
null
C=[CH][Sn]([CH]=C)([CH]=C)[CH]=C.CCNC(=O)Nc1nc2ccc(Br)c(S(=O)(=O)C(F)(F)F)c2s1>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO>C=Cc1ccc2nc(NC(=O)NCC)sc2c1C=C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-74007a0173b8457e84bcfc9f8de348a6
N#C[S-].Nc1ccc(Cc2ccccc2)cc1>>Nc1nc2ccc(Cc3ccccc3)cc2s1
BrBr.C(C1=CC=CC=C1)C1=CC=C(N)C=C1.C(#N)[S-].[K+]>>NC=1SC2=C(N1)C=CC(=C2)CC2=CC=CC=C2
[N:1]#[C:2][S-:17].[NH2:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][cH:14]2)[cH:15][cH:16]1>>[NH2:1][c:2]1[n:3][c:4]2[cH:5][cH:6][c:7]([CH2:8][c:9]3[cH:10][cH:11][cH:12][cH:13][cH:14]3)[cH:15][c:16]2[s:17]1
N#C[S-].Nc1ccc(Cc2ccccc2)cc1
Nc1nc2ccc(Cc3ccccc3)cc2s1
null
null
C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
09d23668c864254f076a396c221fe470e495edd36b92b7e2edc27fa4162c1052
c7c78474f6971eeaa7d180c68d4a8af29cb23110025e531bca1233dc3931475c
c1ccc(Cc2ccc3ncsc3c2)cc1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[S-;H0;D1:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[NH2;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:4]:[c:5](:[c:6]):[c;H0;D3;+0:7](:[c:8]:[c:9]):[s;H0;D2;+0:3]:1
88.2
[{"value": 88.0, "product": "NC=1SC2=C(N1)C=CC(=C2)CC2=CC=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.2, "product": "NC=1SC2=C(N1)C=CC(=C2)CC2=CC=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 4-benzylaniline (0.916 g, 5.00 mmol) and KSCN (0.97 g, 10.0 mmol, 2.0 eq) in 10 mL acetic acid was cooled at about 5° C., and was treated dropwise with a solution of bromine (0.258 mL, 5.00 mmol, 1.0 eq) in 2 mL acetic acid. The mixture was stirred at room temperature for about 1 hour. The precipitate was...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary amine
Primary amine
c1ccccc1
c1ccc2scnc2c1
c1ccc2scnc2c1.c1ccccc1
null
C(C)(=O)O
null
1
N#C[S-].Nc1ccc(Cc2ccccc2)cc1>C(C)(=O)O>Nc1nc2ccc(Cc3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-507cd915806547c7b328f3dffb50e852
CCN=C=O.Nc1nc2ccc(Cc3ccccc3)cc2s1>>CCNC(=O)Nc1nc2ccc(Cc3ccccc3)cc2s1
NC=1SC2=C(N1)C=CC(=C2)CC2=CC=CC=C2.C(C)N(CC)CC.C(C)N=C=O>>C(C1=CC=CC=C1)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][N:3]=[C:4]=[O:5].[NH2:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][cH:19]3)[cH:20][c:21]2[s:22]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][cH:19]3)[cH:20][c:21]2[s:22]1
CCN=C=O.Nc1nc2ccc(Cc3ccccc3)cc2s1
CCNC(=O)Nc1nc2ccc(Cc3ccccc3)cc2s1
null
null
C1(=CC=CC=C1)C
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
c1ccc(Cc2ccc3ncsc3c2)cc1
[C;D1;H3:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[NH2;D1;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1>>[C;D1;H3:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1
56
[{"value": 56.0, "product": "C(C1=CC=CC=C1)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.8, "product": "C(C1=CC=CC=C1)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
95
CELSIUS
null
null
A suspension of 2-amino-6-benzyl-benzothiazole (0.040 g, 0.17 mmol), triethylamine (0.104 mL, 0.77 mmol, 4.5 eq), and ethyl isocyanate (0.049 mL, 0.64 mmol, 3.8 eq) in 1 mL toluene was heated at about 95° C. for about 16 hours. The precipitate was filtered off, washed with Et2O and MeOH, and dried under vacuum to give ...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccc2scnc2c1.c1ccccc1
null
C1(=CC=CC=C1)C
95
null
CCN=C=O.Nc1nc2ccc(Cc3ccccc3)cc2s1>C1(=CC=CC=C1)C>CCNC(=O)Nc1nc2ccc(Cc3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-39cabe140ee74440b053a8e259355b3d
N#C[S-].Nc1ccc(Oc2ccc(F)cc2)cc1>>Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1
BrBr.FC1=CC=C(OC2=CC=C(N)C=C2)C=C1.C(#N)[S-].[K+]>>NC=1SC2=C(N1)C=CC(=C2)OC2=CC=C(C=C2)F
[N:1]#[C:2][S-:18].[NH2:3][c:4]1[cH:5][cH:6][c:7]([O:8][c:9]2[cH:10][cH:11][c:12]([F:13])[cH:14][cH:15]2)[cH:16][cH:17]1>>[NH2:1][c:2]1[n:3][c:4]2[cH:5][cH:6][c:7]([O:8][c:9]3[cH:10][cH:11][c:12]([F:13])[cH:14][cH:15]3)[cH:16][c:17]2[s:18]1
N#C[S-].Nc1ccc(Oc2ccc(F)cc2)cc1
Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1
null
null
C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
09d23668c864254f076a396c221fe470e495edd36b92b7e2edc27fa4162c1052
c7c78474f6971eeaa7d180c68d4a8af29cb23110025e531bca1233dc3931475c
c1ccc(Oc2ccc3ncsc3c2)cc1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[S-;H0;D1:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[NH2;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:4]:[c:5](:[c:6]):[c;H0;D3;+0:7](:[c:8]:[c:9]):[s;H0;D2;+0:3]:1
103.2
[{"value": 90.0, "product": "NC=1SC2=C(N1)C=CC(=C2)OC2=CC=C(C=C2)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 103.2, "product": "NC=1SC2=C(N1)C=CC(=C2)OC2=CC=C(C=C2)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of 4-(4′-fluorophenoxy)aniline (0.305 g, 1.50 mmol) and KSCN (0.29 g, 3.00 mmol, 2.0 eq) in 3 mL acetic acid was cooled at about 5° C., and was treated dropwise with a solution of bromine (0.077 mL, 1.50 mmol, 1.0 eq) in 2 mL acetic acid. The mixture was stirred at room temperature for about 2 hours. The pre...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary amine
Primary amine
c1ccccc1
c1ccc2scnc2c1
c1ccc2scnc2c1.c1ccccc1
null
C(C)(=O)O
null
2
N#C[S-].Nc1ccc(Oc2ccc(F)cc2)cc1>C(C)(=O)O>Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b5f2f4212b8240a4b4901953e91f7565
CCN=C=O.Nc1nc2ccc(Br)cc2s1>>CCNC(=O)Nc1nc2ccc(Br)cc2s1
NC=1SC2=C(N1)C=CC(=C2)Br.C(C)N(CC)CC.C(C)N=C=O>>BrC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][N:3]=[C:4]=[O:5].[NH2:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[cH:14][c:15]2[s:16]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[cH:14][c:15]2[s:16]1
CCN=C=O.Nc1nc2ccc(Br)cc2s1
CCNC(=O)Nc1nc2ccc(Br)cc2s1
null
null
C1(=CC=CC=C1)C
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
c1ccc2scnc2c1
[C;D1;H3:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[NH2;D1;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1>>[C;D1;H3:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[c:7]1:[#16;a:8]:[c:9]:[c:10]:[#7;a:11]:1
94
[{"value": 94.0, "product": "BrC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.0, "product": "BrC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
null
null
A suspension of 2-amino-6-bromo-benzothiazole (6.12 g, 26.2 mmol), triethylamine (7.30 mL, 52.4 mmol, 2.0 eq), and ethyl isocyanate (4.15 mL, 52.4 mmol, 2.0 eq) in 50 mL toluene was heated at about 90° C. for about 15 hours. The precipitate was filtered off, washed with Et2O, and dried under vacuum to give the desired ...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccc2scnc2c1
null
C1(=CC=CC=C1)C
90
null
CCN=C=O.Nc1nc2ccc(Br)cc2s1>C1(=CC=CC=C1)C>CCNC(=O)Nc1nc2ccc(Br)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-257621e7b77e496c8a6049834742adcb
C#C[Si](C)(C)C.CCNC(=O)Nc1nc2ccc(Br)cc2s1>>CCNC(=O)Nc1nc2ccc(C#C[Si](C)(C)C)cc2s1
BrC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C(C)N(CC)CC.C[Si](C)(C)C#C>>C[Si](C)(C)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH:13]#[C:14][Si:15]([CH3:16])([CH3:17])[CH3:18].Br[c:12]1[cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:21][c:20]2[cH:19]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[C:14][Si:15]([CH3:16])([CH3:17])[CH3:18])[cH:19][c:20]2[s:21]1
C#C[Si](C)(C)C.CCNC(=O)Nc1nc2ccc(Br)cc2s1
CCNC(=O)Nc1nc2ccc(C#C[Si](C)(C)C)cc2s1
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CO.CN(C)C=O
C-C Coupling
Sonogashira alkyne_aryl halide
81a8d0200d6382de35d744789f5ef14526aa97a1d031cda8081b95243d0e45dd
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
c1ccc2scnc2c1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1.[C;D1;H3:10]-[#14:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[C:14]#[CH;D1;+0:15]>>[C;D1;H3:10]-[#14:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[C:14]#[C;H0;D2;+0:15]-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1
89
[{"value": 89.0, "product": "C[Si](C)(C)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.8, "product": "C[Si](C)(C)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
15
HOUR
A mixture of 1-(6-bromo-2-benzothiazolyl)-3-ethylurea (0.100 g, 0.33 mmol), Pd(PPh3)2Cl2 (0.012 g, 0.017 mmol, 0.05 eq), and triethylamine (0.20 mL, 1.42 mmol, 4.3 eq) in 1 mL of anhydrous DMF was bubbled with nitrogen gas for about 5 minutes, followed by the addition of trimethylsilyl acetylene (0.23 mL, 1.65 mmol, 5....
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1
HBr
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO.CN(C)C=O
80
15
C#C[Si](C)(C)C.CCNC(=O)Nc1nc2ccc(Br)cc2s1>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO.CN(C)C=O>CCNC(=O)Nc1nc2ccc(C#C[Si](C)(C)C)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6e34ac8687504305874573b2b52188a8
C#Cc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)cc2s1>>CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1
BrC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C(C)N(CC)CC.C1(=CC=CC=C1)C#C>>C1(=CC=CC=C1)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH:13]#[C:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1.Br[c:12]1[cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:23][c:22]2[cH:21]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[C:14][c:15]3[cH:16][cH:17][cH:18][cH:19][cH:20]3)[cH:21][c:22]2[s:23]1
C#Cc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)cc2s1
CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CN(C)C=O
C-C Coupling
Sonogashira alkyne_aryl halide
81a8d0200d6382de35d744789f5ef14526aa97a1d031cda8081b95243d0e45dd
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
C(#Cc1ccc2ncsc2c1)c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1.[CH;D1;+0:10]#[C:11]-[c:12]>>[c:12]-[C:11]#[C;H0;D2;+0:10]-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1
8
[{"value": 8.0, "product": "C1(=CC=CC=C1)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-(6-bromo-2-benzothiazolyl)-3-ethylurea, Pd(PPh3)2Cl2, triethylamine, and phenylacetylene in 1 mL of anhydrous DMF was reacted according to the procedure of Example 213 to give 0.008 g (8%) of the desired compound. LC/MS 322 (M+1); LC retention time 3.65 min. Conditions: See reaction.notes.procedure_detai...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1.c1ccccc1
HBr
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C)C=O
null
null
C#Cc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)cc2s1>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C)C=O>CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e28f5a27454f477e9bdcf8a67a519fdf
CCNC(=O)Nc1nc2ccc(C#C[Si](C)(C)C)cc2s1>>C#Cc1ccc2nc(NC(=O)NCC)sc2c1
C[Si](C)(C)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.[OH-].[K+].Cl>>C(#C)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
C[Si](C)(C)[C:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][CH2:13][CH3:14])[s:15][c:16]2[cH:17]1>>[CH:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][CH2:13][CH3:14])[s:15][c:16]2[cH:17]1
CCNC(=O)Nc1nc2ccc(C#C[Si](C)(C)C)cc2s1
C#Cc1ccc2nc(NC(=O)NCC)sc2c1
null
null
CO.CCOC(=O)C
Deprotection
TMS deprotection from alkyne
e85676bb81da384790c9c858d44f182cdd01e3a79f77f7a239fe38487234cb96
56d526d7c9cb1bd7bee4940e216a9b1dd4597fd025a186b8d6e4675d8f4db26b
c1ccc2scnc2c1
C-[Si](-C)(-C)-[C;H0;D2;+0:1]#[C:2]-[c:3]>>[CH;D1;+0:1]#[C:2]-[c:3]
5.6
[{"value": 5.0, "product": "C(#C)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 5.6, "product": "C(#C)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A mixture of 1-(6-trimethylsilylacetylenyl-2-benzothiazolyl)-3-ethylurea (0.0710 g, 0.22 mmol) and 1M aqueous KOH solution (1.22 mL, 1.22 mmol, 5.5 eq) in 1.5 mL MeOH was stirred at room temperature for about 2 hours. The mixture acidified with 1 M HCl, then taken up in 20 mL AcOEt, and the aqueous phase was extracted ...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Silyl protective group
Alkyne
null
null
c1ccc2scnc2c1
Other
CO.CCOC(=O)C
null
2
CCNC(=O)Nc1nc2ccc(C#C[Si](C)(C)C)cc2s1>CO.CCOC(=O)C>C#Cc1ccc2nc(NC(=O)NCC)sc2c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-95e95ae24cd64ca5ba5ab0c7319f2bfb
CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1>>CCNC(=O)Nc1nc2ccc(CCc3ccccc3)cc2s1
C1(=CC=CC=C1)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1>>C1(=CC=CC=C1)CCC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[C:14][c:15]3[cH:16][cH:17][cH:18][cH:19][cH:20]3)[cH:21][c:22]2[s:23]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([CH2:13][CH2:14][c:15]3[cH:16][cH:17][cH:18][cH:19][cH:20]3)[cH:21][c:22]2[s:23]1
CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1
CCNC(=O)Nc1nc2ccc(CCc3ccccc3)cc2s1
null
[Pd]
C(C)O
Reduction
OtherReaction
2bb8d5b532a2781e0a7c069a5cd3e8a7e8d44660c0ec1d9e17c04d8ba2cb383b
1990560e9c55934bde8ca0feaed9c61d80f37f94f0cf240a9929dc374d0a33aa
c1ccc(CCc2ccc3ncsc3c2)cc1
[#16;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D2;+0:5]#[C;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]):[c:10]>>[#16;a:1]:[c:2]:[c:3]:[c:4](-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[c:7](:[c:8]):[c:9]):[c:10]
76
[{"value": 76.0, "product": "C1(=CC=CC=C1)CCC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.8, "product": "C1(=CC=CC=C1)CCC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A suspension of 1-(6-phenylacetylenyl-2-benzothiazolyl)-3-ethylurea (0.048 g, 0.15 mmol) and 10% palladium on carbon (0.016 g, 10% weight purity, 0.015 mmol, 0.10 eq) in 2 mL ethanol was purged with nitrogen gas, followed by bubbling of hydrogen gas. It was stirred under hydrogen atmosphere for about 16 hours. The mixt...
10.6084/m9.figshare.5104873.v1
null
Alkyne
null
null
null
c1ccc2scnc2c1.c1ccccc1
null
[Pd].C(C)O
null
16
CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1>[Pd].C(C)O>CCNC(=O)Nc1nc2ccc(CCc3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b034843c1eae49b58ee346d1b1960c87
CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1>>CCNC(=O)Nc1nc2ccc(/C=C\c3ccccc3)cc2s1
C1(=CC=CC=C1)C#CC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1>>C1(=CC=CC=C1)\C=C/C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13]#[C:14][c:15]3[cH:16][cH:17][cH:18][cH:19][cH:20]3)[cH:21][c:22]2[s:23]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12](/[CH:13]=[CH:14]\[c:15]3[cH:16][cH:17][cH:18][cH:19][cH:20]3)[cH:21][c:22]2[s:23]1
CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1
CCNC(=O)Nc1nc2ccc(/C=C\c3ccccc3)cc2s1
null
[Pd].CC(=O)[O-].CC(=O)[O-].[Pb+2]
C(C)O
Reduction
Hydrogenation (triple to double)
2bb8d5b532a2781e0a7c069a5cd3e8a7e8d44660c0ec1d9e17c04d8ba2cb383b
1990560e9c55934bde8ca0feaed9c61d80f37f94f0cf240a9929dc374d0a33aa
C(=C\c1ccc2ncsc2c1)\c1ccccc1
[#16;a:1]:[c:2]:[c:3]:[c:4](-[C;H0;D2;+0:5]#[C;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]):[c:10]>>[#16;a:1]:[c:2]:[c:3]:[c:4](/[CH;D2;+0:5]=[CH;D2;+0:6]\[c:7](:[c:8]):[c:9]):[c:10]
41
[{"value": 41.0, "product": "C1(=CC=CC=C1)\\C=C/C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 41.0, "product": "C1(=CC=CC=C1)\\C=C/C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
36
HOUR
A suspension of 1-(6-phenylacetylenyl-2-benzothiazolyl)-3-ethylurea (0.032 g, 83% purity by weight, 0.083 mmol) and Lindlar catalyst (0.030 g, 5% weight purity, 0.012 mmol, 0.15 eq) in 2 mL ethanol was purged with nitrogen gas, followed by bubbling of hydrogen gas. It was stirred under hydrogen atmosphere for about 36 ...
10.6084/m9.figshare.5104873.v1
null
Alkyne
null
null
null
c1ccc2scnc2c1.c1ccccc1
null
[Pd].CC(=O)[O-].CC(=O)[O-].[Pb+2].C(C)O
null
36
CCNC(=O)Nc1nc2ccc(C#Cc3ccccc3)cc2s1>[Pd].CC(=O)[O-].CC(=O)[O-].[Pb+2].C(C)O>CCNC(=O)Nc1nc2ccc(/C=C\c3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e3c1889fcfaf4fb982b73eceaea5d2bc
C=Cc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)cc2s1>>CCNC(=O)Nc1nc2ccc(/C=C/c3ccccc3)cc2s1
BrC1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C=1C=CC(=CC1)P(CCCP(C=2C=CC=CC2)C=3C=CC=CC3)C=4C=CC=CC4.C(C)N(CC)CC.C=CC1=CC=CC=C1>>C1(=CC=CC=C1)/C=C/C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH2:13]=[CH:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1.Br[c:12]1[cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:23][c:22]2[cH:21]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12](/[CH:13]=[CH:14]/[c:15]3[cH:16][cH:17][cH:18][cH:19][cH:20]3)[cH:21][c:22]2[s:23...
C=Cc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)cc2s1
CCNC(=O)Nc1nc2ccc(/C=C/c3ccccc3)cc2s1
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CN(C)C=O
C-C Coupling
Heck terminal vinyl
75ca16f9fb0fbd5ca837ac801a3bf869050db64700b139faf9efed8ef9e02537
4b186811a4930853b446d93d9faa39b267bddb9ce0b8021bda5c5a3b2bc69f0b
C(=C/c1ccc2ncsc2c1)\c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1.[CH2;D1;+0:10]=[C:11]-[c:12]>>[c:12]/[C:11]=[CH;D2;+0:10]/[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[#16;a:7]:[c:8]:2:[c:9]:1
62
[{"value": 62.0, "product": "C1(=CC=CC=C1)/C=C/C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-(6-bromo-2-benzothiazolyl)-3-ethylurea, Pd(PPh3)2Cl2, dppp, triethylamine, styrene, and two crystals of BHT in anhydrous DMF was reacted according to the procedure of Example 225 to give the desired compound 0.201 g (62%). LC/MS 324.2 (M+1); LC retention time 2.87 min. Conditions: See reaction.notes.proc...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Vinyl
null
c1ccc2scnc2c1
c1ccc2scnc2c1
c1ccc2scnc2c1.c1ccccc1
HBr
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C)C=O
null
null
C=Cc1ccccc1.CCNC(=O)Nc1nc2ccc(Br)cc2s1>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C)C=O>CCNC(=O)Nc1nc2ccc(/C=C/c3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-740e84ce00124f83a802a02af18c14b6
COC(=S)Cl.Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1>>CCOC(=S)Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1
Cl.ClC(=S)OC.NC=1SC2=C(N1)C=CC(=C2)OC2=CC=C(C=C2)F.N1=CC=CC=C1>>FC1=CC=C(OC2=CC3=C(N=C(S3)NC(OCC)=S)C=C2)C=C1
Cl[C:4]([O:3][CH3:2])=[S:5].[NH2:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([O:13][c:14]3[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]3)[cH:21][c:22]2[s:23]1>>[CH3:1][CH2:2][O:3][C:4](=[S:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([O:13][c:14]3[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]3)[cH:21][c:22]2[s:23]1
COC(=S)Cl.Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1
CCOC(=S)Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
0a23a66795ec4b7fa0bd30742fc813ad896e669d9d6489e05f50db8a591c6b07
373750671fa9bcc9f846e7098fb90c60e0ea9e513d59381135c62cc38d06816d
c1ccc(Oc2ccc3ncsc3c2)cc1
Cl-[C;H0;D3;+0:1](=[S;D1;H0:2])-[#8:3]-[CH3;D1;+0:4].[NH2;D1;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1>>[C;D1;H3:11]-[CH2;D2;+0:4]-[#8:3]-[C;H0;D3;+0:1](=[S;D1;H0:2])-[NH;D2;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1
65
[{"value": 65.0, "product": "FC1=CC=C(OC2=CC3=C(N=C(S3)NC(OCC)=S)C=C2)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A suspension of 2-amino-6-(4′-fluorophenoxy)-benzothiazole (associated with 2.0 eq of KBr salt, 2.50 g, 5.02 mmol) in 10 mL pyridine was treated dropwise with methyl chlorothioformate (0.65 mL, 7.53 mmol, 01.5 eq). It was stirred at room temperature for about 1 hour, and was poured into 40 mL ice water. The mixture was...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Ether.Primary amine
Ether.Thioamide
null
null
c1ccc2scnc2c1.c1ccccc1
null
null
null
1
COC(=S)Cl.Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1>>CCOC(=S)Nc1nc2ccc(Oc3ccc(F)cc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-193af041f89c4a718cbabf830a9304dc
CCNC(=O)Nc1nc2ccc(Cc3ccccc3)cc2s1.CCOC(=O)c1ccc2nc(N)sc2c1>>CCNC(=O)Nc1nc2ccc(C(=O)OCC)cc2s1
C(C1=CC=CC=C1)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.NC=1SC2=C(N1)C=CC(=C2)C(=O)OCC.C(C)N(CC)CC.C(C)N=C=O>>C(C)OC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
c1ccc(Cc2ccc3nc(N[C:4]([NH:3][CH2:2][CH3:1])=[O:5])sc3c2)cc1.[NH2:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[O:15][CH2:16][CH3:17])[cH:18][c:19]2[s:20]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[O:15][CH2:16][CH3:17])[cH:18][c:19]2[s:20]1
CCNC(=O)Nc1nc2ccc(Cc3ccccc3)cc2s1.CCOC(=O)c1ccc2nc(N)sc2c1
CCNC(=O)Nc1nc2ccc(C(=O)OCC)cc2s1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
ba60c90fe4fc8b1bce2e75337f9f3b3b4a82100ebf9cf0bdc0393fc79ed9c761
f17cc9fc6250903fc236407915f5767fca8f6b6242f886ce02918cf1cdfcba61
c1ccc2scnc2c1
[C:1]-[#7:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-N-c1:n:c2:c:c:c(-C-c3:c:c:c:c:c:3):c:c:2:s:1.[NH2;D1;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1>>[C:1]-[#7:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1
82
[{"value": 82.0, "product": "C(C)OC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
According to the General Procedure for 1-(6-substituted-2-benzothiazolyl)-3-ethylurea compounds, and similar to the synthesis of 1-(6-benzyl-2-benzothiazolyl)-3-ethylurea, a mixture of 2-amino-6-ethoxycarbonyl-benzothiazole, triethylamine and ethyl isocyanate in toluene was reacted to give the desired compound 2.40 g (...
10.6084/m9.figshare.5104873.v1
null
Urea.Primary amine
Urea
c1ccccc1.c1ccc2scnc2c1
null
c1ccc2scnc2c1
Other
C1(=CC=CC=C1)C
null
null
CCNC(=O)Nc1nc2ccc(Cc3ccccc3)cc2s1.CCOC(=O)c1ccc2nc(N)sc2c1>C1(=CC=CC=C1)C>CCNC(=O)Nc1nc2ccc(C(=O)OCC)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8549526be9da42f8b9e0ee50ad49b065
CC#N.CCNC(=O)Nc1nc2ccc(C(=O)OCC)cc2s1>>CCNC(=O)Nc1nc2ccc(C(=O)CC#N)cc2s1
C1CCOC1.C(C)OC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C(C)#N.[Li+].C[Si](C)(C)[N-][Si](C)(C)C.[Li+].C[Si](C)(C)[N-][Si](C)(C)C>>C(#N)CC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:15][C:16]#[N:17].CCO[C:13]([c:12]1[cH:11][cH:10][c:9]2[n:8][c:7]([NH:6][C:4]([NH:3][CH2:2][CH3:1])=[O:5])[s:20][c:19]2[cH:18]1)=[O:14]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][C:16]#[N:17])[cH:18][c:19]2[s:20]1
CC#N.CCNC(=O)Nc1nc2ccc(C(=O)OCC)cc2s1
CCNC(=O)Nc1nc2ccc(C(=O)CC#N)cc2s1
null
null
CN(C)C=O
C-C Coupling
OtherReaction
8ce89878f5db9b98fa4633d16adf2407dbf79d96925d930c608f1ce0756e674e
f80cbbd7f2bfc042e62829b7de30498cf0880b808f2adad888ffdfe089982722
c1ccc2scnc2c1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[c:6]:[#16;a:7].[CH3;D1;+0:8]-[C:9]#[N;D1;H0:10]>>[#16;a:7]:[c:6]:[c:5]:[c:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:8]-[C:9]#[N;D1;H0:10]):[c:4]
54
[{"value": 54.0, "product": "C(#N)CC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
0.5
HOUR
A solution of 1-(6-ethoxycarbonyl-2-benzothiazolyl)-3-ethylurea (1.20 g, 4.09 mmol) in 5 mL of anhydrous DMF was treated with 2 mL of acetonitrile, cooled down to about 0° C., followed by treatment with 1 M LiHMDS in THF (13.1 mL, 13.1 mmol, 3.2 eq). It was stirred at the temperature for about 0.5 hour, then warmed up ...
10.6084/m9.figshare.5104873.v1
null
Ester
Ketone
null
null
c1ccc2scnc2c1
HO-
CN(C)C=O
0
0.5
CC#N.CCNC(=O)Nc1nc2ccc(C(=O)OCC)cc2s1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(C(=O)CC#N)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ec7552d657b74d9cb90ee4e75ae57522
CCNC(=O)Nc1nc2ccc(C(=O)CC#N)cc2s1>>CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1
C(#N)CC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.CO>>NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][C:16]#[N:17])[cH:18][c:19]2[s:20]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][CH2:16][NH2:17])[cH:18][c:19]2[s:20]1
CCNC(=O)Nc1nc2ccc(C(=O)CC#N)cc2s1
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1
null
[Pt](=O)=O
C(Cl)(Cl)Cl
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
c1ccc2scnc2c1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[C:3]-[C:4](=[O;D1;H0:5])-[c:6]>>[NH2;D1;+0:1]-[CH2;D2;+0:2]-[C:3]-[C:4](=[O;D1;H0:5])-[c:6]
121.5
[{"value": 121.5, "product": "NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
DAY
A suspension of 1-(6-(2-cyanoacetyl)-2-benzothiazolyl)-3-ethylurea (0.56 g, 1.94 mmol) and platinum (IV) oxide (0.176 g, 0.78 mmol, 0.40 eq) in 50 mL of 2/3 mixture of MeOH and chloroform was purged and bubbled with hydrogen gas. It was stirred under hydrogen gas for about 2 days. The mixture was filtered and concentra...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
c1ccc2scnc2c1
null
[Pt](=O)=O.C(Cl)(Cl)Cl
null
48
CCNC(=O)Nc1nc2ccc(C(=O)CC#N)cc2s1>[Pt](=O)=O.C(Cl)(Cl)Cl>CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d4a430f6fb924fac95a71637b5597afc
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.O=C(Cl)c1ccccc1>>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)c3ccccc3)cc2s1
C(C1=CC=CC=C1)(=O)Cl.NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C(C)N(CC)CC>>C(C)NC(=O)NC=1SC2=C(N1)C=CC(=C2)C(CCNC(C2=CC=CC=C2)=O)=O
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][CH2:16][NH2:17])[cH:26][c:27]2[s:28]1.Cl[C:18](=[O:19])[c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][CH2:16][NH:17][C:1...
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.O=C(Cl)c1ccccc1
CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)c3ccccc3)cc2s1
null
null
CN(C)C=O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(CCNC(=O)c1ccccc1)c1ccc2ncsc2c1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[C:7]-[C:8]-[C:9]=[O;D1;H0:10]>>[O;D1;H0:10]=[C:9]-[C:8]-[C:7]-[NH;D2;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
28
[{"value": 28.0, "product": "C(C)NC(=O)NC=1SC2=C(N1)C=CC(=C2)C(CCNC(C2=CC=CC=C2)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 27.7, "product": "C(C)NC(=O)NC=1SC2=C(N1)C=CC(=C2)C(CCNC(C2=CC=CC=C2)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
A solution of 1-(6-(3-aminopropanoyl)-2-benzothiazolyl)-3-ethylurea (0.033 g, 0.10 mmol) in 1 mL anhydrous DMF was treated with triethylamine (0.028 mL, 0.20 mmol, 2.0 eq) at room temperature. It was stirred for about 5 min, followed by the addition of benzoyl chloride (0.014 mL, 0.12 mmol, 1.2 eq). It was stirred for ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccc2scnc2c1.c1ccccc1
HCl
CN(C)C=O
null
0.083333
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.O=C(Cl)c1ccccc1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)c3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-7c11d59354d54b46b7c009458d9fc655
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.O=C=Nc1ccccc1>>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)Nc3ccccc3)cc2s1
C1(=CC=CC=C1)N=C=O.NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C(C)N(CC)CC>>C1(=CC=CC=C1)NC(=O)NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][CH2:16][NH2:17])[cH:27][c:28]2[s:29]1.[C:18](=[O:19])=[N:20][c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][CH2:16][NH:17...
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.O=C=Nc1ccccc1
CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)Nc3ccccc3)cc2s1
null
null
CN(C)C=O
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
O=C(NCCC(=O)c1ccc2ncsc2c1)Nc1ccccc1
[NH2;D1;+0:1]-[C:2]-[C:3]-[C:4]=[O;D1;H0:5].[O;D1;H0:6]=[C;H0;D2;+0:7]=[N;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[O;D1;H0:5]=[C:4]-[C:3]-[C:2]-[NH;D2;+0:1]-[C;H0;D3;+0:7](=[O;D1;H0:6])-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]
22
[{"value": 22.0, "product": "C1(=CC=CC=C1)NC(=O)NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 21.9, "product": "C1(=CC=CC=C1)NC(=O)NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
A solution of 1-(6-(3-aminopropanoyl)-2-benzothiazolyl)-3-ethylurea (0.033 g, 0.10 mmol) in 1 mL anhydrous DMF was treated with triethylamine (0.028 mL, 0.20 mmol, 2.0 eq) at room temperature. It was stirred for about 5 min, followed by the addition of phenyl isocyanate (0.013 mL, 0.12 mmol, 1.2 eq). It was stirred for...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccc2scnc2c1.c1ccccc1
null
CN(C)C=O
null
0.083333
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.O=C=Nc1ccccc1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)Nc3ccccc3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3b86cf3eeca34ce7947e49ad0db3feaf
CCN(CC)CC.CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.[N-]=C=O>>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)Nc3cccc(C)c3)cc2s1
NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C(C)N(CC)CC.[N-]=C=O>>CC=1C=C(C=CC1)NC(=O)NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1
N([CH2:21][CH3:22])([CH2:25][CH3:26])[CH2:27][CH3:23].[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][CH2:16][NH2:17])[cH:28][c:29]2[s:30]1.[C:18](=[O:19])=[N-:20]>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][C...
CCN(CC)CC.CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.[N-]=C=O
CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)Nc3cccc(C)c3)cc2s1
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
ceeef5fff04fe6a7f7ce23912c40c6b56c48ab10b532da4166f49e27ddc6de5e
442a18545a92795a137ffa2717869d0ab7cb2b1c39aa88d4f3af549ee08fea76
O=C(NCCC(=O)c1ccc2ncsc2c1)Nc1ccccc1
[C;D1;H3:1]-[CH2;D2;+0:2]-N(-[CH2;D2;+0:3]-[CH3;D1;+0:4])-[CH2;D2;+0:5]-[CH3;D1;+0:6].[N-;H0;D1:7]=[C;H0;D2;+0:8]=[O;D1;H0:9].[NH2;D1;+0:10]-[C:11]-[C:12]-[C:13]=[O;D1;H0:14]>>[C;D1;H3:1]-[c;H0;D3;+0:2]1:[c:15]:[cH;D2;+0:6]:[cH;D2;+0:4]:[c;H0;D3;+0:3](-[NH;D2;+0:7]-[C;H0;D3;+0:8](=[O;D1;H0:9])-[NH;D2;+0:10]-[C:11]-[C:1...
25
[{"value": 25.0, "product": "CC=1C=C(C=CC1)NC(=O)NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Similar to the synthesis of Example 249, a mixture of 1-(6-(3-aminopropanoyl)-2-benzothiazolyl)-3-ethylurea, triethylamine and 3-methylphenhyl isocyanate in DMF was reacted to give the desired compound 0.021 g (25%). LC/MS 426.1 (M+1); LC retention time 2.94 min. Conditions: See reaction.notes.procedure_details. Workup...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Tertiary amine
Urea
null
c1ccccc1
c1ccc2scnc2c1.c1ccccc1
null
CN(C)C=O
null
null
CCN(CC)CC.CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.[N-]=C=O>CN(C)C=O>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)Nc3cccc(C)c3)cc2s1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6922b5b487d84e03beb86b2f7f9581c3
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.CN(C)c1ccc(C(=O)Cl)cc1>>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)c3ccc(N(C)C)cc3)cc2s1
C(C)(=O)O.NCCC(=O)C1=CC2=C(N=C(S2)NC(=O)NCC)C=C1.C(C)N(CC)CC.CN(C1=CC=C(C(=O)Cl)C=C1)C>>C(C)NC(=O)NC=1SC2=C(N1)C=CC(=C2)C(CCNC(C2=CC=C(C=C2)N(C)C)=O)=O
[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[CH2:15][CH2:16][NH2:17])[cH:29][c:30]2[s:31]1.Cl[C:18](=[O:19])[c:20]1[cH:21][cH:22][c:23]([N:24]([CH3:25])[CH3:26])[cH:27][cH:28]1>>[CH3:1][CH2:2][NH:3][C:4](=[O:5])[NH:6][c:7]1[n:8][c:9]2[cH:10][cH:11][c:12]([C:13](=[O:14])[C...
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.CN(C)c1ccc(C(=O)Cl)cc1
CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)c3ccc(N(C)C)cc3)cc2s1
null
null
CN(C)C=O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(CCNC(=O)c1ccccc1)c1ccc2ncsc2c1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[C:7]-[C:8]-[C:9]=[O;D1;H0:10]>>[O;D1;H0:10]=[C:9]-[C:8]-[C:7]-[NH;D2;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
25
[{"value": 25.0, "product": "C(C)NC(=O)NC=1SC2=C(N1)C=CC(=C2)C(CCNC(C2=CC=C(C=C2)N(C)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Similar to the synthesis of Example 248, a mixture of 1-(6-(3-aminopropanoyl)-2-benzothiazolyl)-3-ethylurea, triethylamine and 4-dimethylaminobenzoyl chloride in DMF was reacted to give the desired compound 0.025 g (25%) as an acetic acid salt. LC/MS 440.1 (M+1); LC retention time 2.86 min. Conditions: See reaction.not...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccc2scnc2c1.c1ccccc1
HCl
CN(C)C=O
null
null
CCNC(=O)Nc1nc2ccc(C(=O)CCN)cc2s1.CN(C)c1ccc(C(=O)Cl)cc1>CN(C)C=O>CCNC(=O)Nc1nc2ccc(C(=O)CCNC(=O)c3ccc(N(C)C)cc3)cc2s1