dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-915998a24bba4f2190531cc7ca53e3a6
COC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)OCc1ccccc1>>O=C(N[C@H](CO)Cc1ccc(OCc2ccccc2)cc1)OCc1ccccc1
[Cl-].[Na+].COC([C@@H](NC(=O)OCC1=CC=CC=C1)CC1=CC=C(C=C1)OCC1=CC=CC=C1)=O.[Cl-].[Li+].[BH4-].[Na+]>>C(C1=CC=CC=C1)OC1=CC=C(C[C@H](NC(=O)OCC2=CC=CC=C2)CO)C=C1
CO[C:5]([C@@H:4]([NH:3][C:2](=[O:1])[O:22][CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1)[CH2:7][c:8]1[cH:9][cH:10][c:11]([O:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[cH:20][cH:21]1)=[O:6]>>[O:1]=[C:2]([NH:3][C@H:4]([CH2:5][OH:6])[CH2:7][c:8]1[cH:9][cH:10][c:11]([O:12][CH2:13][c:14]2[cH:15][cH:16][cH...
COC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)OCc1ccccc1
O=C(N[C@H](CO)Cc1ccc(OCc2ccccc2)cc1)OCc1ccccc1
null
null
C(C)O.O1CCCC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
O=C(NCCc1ccc(OCc2ccccc2)cc1)OCc1ccccc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3](-[C:4])-[#7:5]-[C:6]=[O;D1;H0:7]>>[C:4]-[C:3](-[#7:5]-[C:6]=[O;D1;H0:7])-[CH2;D2;+0:1]-[OH;D1;+0:2]
99.9
[{"value": 99.9, "product": "C(C1=CC=CC=C1)OC1=CC=C(C[C@H](NC(=O)OCC2=CC=CC=C2)CO)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
27.25 g of O-benzyl-N-benzyloxycarbonyltyrosine methyl ester was dissolved in a mixed solvent of 185 ml of ethanol and 122 ml of tetrahydrofuran, and to the solution were added 5.8 g of lithium chloride and 5.2 g of sodium borohydride under ice cooling. The reaction mixture was stirred at a room temperature for 18 hour...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
C(C)O.O1CCCC1
null
18
COC(=O)[C@H](Cc1ccc(OCc2ccccc2)cc1)NC(=O)OCc1ccccc1>C(C)O.O1CCCC1>O=C(N[C@H](CO)Cc1ccc(OCc2ccccc2)cc1)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4e42a8b5fe4a46378087c9d3b246d21a
CN(C)C=O.COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C>>COCCOCOc1ccc(C[C@H](NC(=O)OC(C)(C)C)C(=O)OC)cc1
COC([C@@H](NC(=O)OC(C)(C)C)CC1=CC=C(C=C1)O)=O.[H-].[Na+].CN(C=O)C>>COC([C@@H](NC(=O)OC(C)(C)C)CC1=CC=C(C=C1)OCOCCOC)=O
N([CH3:1])([CH:3]=[O:2])[CH3:6].[CH3:4][C:18]([O:17][C:15]([NH:14][C@@H:13]([CH2:12][c:11]1[cH:10][cH:9][c:8]([OH:7])[cH:27][cH:26]1)[C:22](=[O:23])[O:24][CH3:25])=[O:16])([CH3:19])[CH3:21]>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[cH:9][cH:10][c:11]([CH2:12][C@H:13]([NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19]...
CN(C)C=O.COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C
COCCOCOc1ccc(C[C@H](NC(=O)OC(C)(C)C)C(=O)OC)cc1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
efafa0a6339c75bfa27dc36aebc157a1675075cd6c3754593e740058d44802c9
ea88b7c6ec4e4769f6c1d2c513fe7a03974fac7a6f46af80ffac0a032d1f27a2
c1ccccc1
[#7:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;H0;D4;+0:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[CH3;D1;+0:8].[OH;D1;+0:9]-[c:10](:[c:11]):[c:12].[CH3;D1;+0:13]-N(-[CH3;D1;+0:14])-[CH;D2;+0:15]=[O;H0;D1;+0:16]>>[#7:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;H0;D4;+0:5](-[C;D1;H3:6])(-[C;D1;H3:17])-[C;D1;H3:7].[CH3;D1;+0:13]-[O;H0;D2;+0:16]-[CH2;D2...
null
[]
null
null
null
null
13.39 g of N-tert-butoxycarbonyltyrosine methyl ester was dissolved in 65 ml of tetrahydrofuran and 65 ml of dimethylformamide, and to the solution was added 1.9 g of 60% sodium hydride with stirring in an ice bath. After removing from the ice bath, the mixture was stirred at a room temperature for 30 minutes, and afte...
10.6084/m9.figshare.5104873.v1
null
Ether.Tertiary amide.Aromatic alcohol.Boc
Ether.Ether.Ether.Ether.Boc
null
null
c1ccccc1
null
O1CCCC1
null
null
CN(C)C=O.COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C>O1CCCC1>COCCOCOc1ccc(C[C@H](NC(=O)OC(C)(C)C)C(=O)OC)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6fb0cb4113fb499eb4dfc30867774f34
O=C(N[C@@H](Cc1ccc(O)cc1)C(=O)O)OCc1ccccc1.c1ccc(N2CCNCC2)cc1>>O=C(N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCN(c2ccccc2)CC1)OCc1ccccc1
C(C1=CC=CC=C1)OC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)O.C1(=CC=CC=C1)N1CCNCC1.C1CCC(CC1)N=C=NC2CCCCC2>>C(C1=CC=CC=C1)OC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N1CCN(CC1)C1=CC=CC=C1
O[C:13]([C@@H:4]([NH:3][C:2](=[O:1])[O:27][CH2:28][c:29]1[cH:30][cH:31][cH:32][cH:33][cH:34]1)[CH2:5][c:6]1[cH:7][cH:8][c:9]([OH:10])[cH:11][cH:12]1)=[O:14].[NH:15]1[CH2:16][CH2:17][N:18]([c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[CH2:25][CH2:26]1>>[O:1]=[C:2]([NH:3][C@@H:4]([CH2:5][c:6]1[cH:7][cH:8][c:9]([OH:10])[cH...
O=C(N[C@@H](Cc1ccc(O)cc1)C(=O)O)OCc1ccccc1.c1ccc(N2CCNCC2)cc1
O=C(N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCN(c2ccccc2)CC1)OCc1ccccc1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
ed26ef5eea92a0cc433b3f89a34f4c61724425fa15a9d0ec83a0f7a903eec831
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(N[C@@H](Cc1ccccc1)C(=O)N1CCN(c2ccccc2)CC1)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6]=[O;D1;H0:7].[#7:8]1-[C:9]-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13]-1>>[C:4]-[C:3](-[#7:5]-[C:6]=[O;D1;H0:7])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:11]1-[C:10]-[C:9]-[#7:8]-[C:13]-[C:12]-1
58.6
[{"value": 58.6, "product": "C(C1=CC=CC=C1)OC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N1CCN(CC1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
12.3 g of N-benzyloxycarbonyltyrosine and 6.6 g of N-phenylpiperazine were dissolved in 150 ml of methylene chloride, and to the solution was added 8.4 g of DCC, and the mixture was stirred at a room temperature for 5 hours. Precipitated insoluble matter was filtered off and the filtrate was concentrated under a reduce...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
5
O=C(N[C@@H](Cc1ccc(O)cc1)C(=O)O)OCc1ccccc1.c1ccc(N2CCNCC2)cc1>C(Cl)Cl>O=C(N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCN(c2ccccc2)CC1)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dfeb66b2e0614f0e93caf3ee661eaf60
CI.O=C([C@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)NS(=O)(=O)c1cccc2cnccc12)N1CCN(c2ccccc2)CC1>>CN([C@@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)C(=O)N1CCN(c2ccccc2)CC1)S(=O)(=O)c1cccc2cnccc12
O.[H-].[Na+].C1=NC=CC=2C(=CC=CC12)S(=O)(=O)N[C@@H](CC1=CC=C(C=C1)OS(=O)(=O)C=1C=2C=CN=CC2C=CC1)C(=O)N1CCN(CC1)C1=CC=CC=C1.CI>>C1=NC=CC=2C(=CC=CC12)S(=O)(=O)N([C@@H](CC1=CC=C(C=C1)OS(=O)(=O)C=1C=2C=CN=CC2C=CC1)C(=O)N1CCN(CC1)C1=CC=CC=C1)C
I[CH3:1].[NH:2]([C@@H:3]([CH2:4][c:5]1[cH:6][cH:7][c:8]([O:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][c:17]3[cH:18][n:19][cH:20][cH:21][c:22]23)[cH:23][cH:24]1)[C:25](=[O:26])[N:27]1[CH2:28][CH2:29][N:30]([c:31]2[cH:32][cH:33][cH:34][cH:35][cH:36]2)[CH2:37][CH2:38]1)[S:39](=[O:40])(=[O:41])[c:42]1[cH:43][cH...
CI.O=C([C@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)NS(=O)(=O)c1cccc2cnccc12)N1CCN(c2ccccc2)CC1
CN([C@@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)C(=O)N1CCN(c2ccccc2)CC1)S(=O)(=O)c1cccc2cnccc12
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
c6ca050f6d67acb7bc6fc8b4d7848b3f349e4e8db81643cbb6d12b5a34cbf965
9d3dfd18cb6410898a6d822a6d80081d602cf34984cafbfa56b84aa4b38ddbf6
O=C([C@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)NS(=O)(=O)c1cccc2cnccc12)N1CCN(c2ccccc2)CC1
I-[CH3;D1;+0:1].[C:2]-[#7:3](-[C:4](=[O;D1;H0:5])-[C:6](-[C:7])-[NH;D2;+0:8]-[#16:9](=[O;D1;H0:10])(=[O;D1;H0:11])-[c:12])-[C:13]>>[C:2]-[#7:3](-[C:4](=[O;D1;H0:5])-[C:6](-[C:7])-[N;H0;D3;+0:8](-[CH3;D1;+0:1])-[#16:9](=[O;D1;H0:10])(=[O;D1;H0:11])-[c:12])-[C:13]
null
[]
null
null
90
MINUTE
2.27 g of the amorphous compound obtained in Example 108 was dissolved in 30 ml of dimethylformamide, to the solution were sequentially added 160 mg of 60% sodium hydride and 0.3 ml of methyl iodide with ice cooling, and the mixture was stirred for 90 minutes with ice cooling. After adding 80 ml of water, the reaction ...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Tertiary amine
null
null
c1ccccc1.c1ccc2cnccc2c1.C1C[NH]CC[NH]1.c1ccccc1.c1ccc2cnccc2c1
HI
CN(C=O)C
null
1.5
CI.O=C([C@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)NS(=O)(=O)c1cccc2cnccc12)N1CCN(c2ccccc2)CC1>CN(C=O)C>CN([C@@H](Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)C(=O)N1CCN(c2ccccc2)CC1)S(=O)(=O)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9210acb815974a8380d54b730e8abe69
C1CNCCNC1.O=C(Cl)OCc1ccccc1>>O=C(OCc1ccccc1)N1CCCNCC1
CN(C=O)C.N1CCNCCC1.C([O-])(O)=O.[Na+].C(C1=CC=CC=C1)OC(=O)Cl>>C(C1=CC=CC=C1)OC(=O)N1CCNCCC1
[NH:11]1[CH2:12][CH2:13][CH2:14][NH:15][CH2:16][CH2:17]1.Cl[C:2](=[O:1])[O:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[N:11]1[CH2:12][CH2:13][CH2:14][NH:15][CH2:16][CH2:17]1
C1CNCCNC1.O=C(Cl)OCc1ccccc1
O=C(OCc1ccccc1)N1CCCNCC1
null
null
O
Protection
N-alkylation of secondary amines with alkyl halides
466a90f5c0328778671e7ef9d1ad2a8b6e81fdc28f82b2a2f790befcf3020485
d86dc1e6d0e089b3444b62ddfcf4c4822bdac4b60e628553036562518c29adcd
O=C(OCc1ccccc1)N1CCCNCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#7:5]-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[#7:5]-[C:6]-[C:7]-[N;H0;D3;+0:8](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-[C:9]-[C:10]
65.5
[{"value": 65.5, "product": "C(C1=CC=CC=C1)OC(=O)N1CCNCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 230 ml of dimethylformamide were added 25 g of homopiperazine and 5.4 g of sodium bicarbonate and then 25 ml of water followed by dropwise addition of 10 g of benzyloxycarbonyl chloride with stirring under ice cooling, and the mixture was stirred at a room temperature overnight. After evaporating off dimethylformami...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Secondary amine
Carbamic ester
C1CNCCNC1
C1C[NH]CCNC1
c1ccccc1.C1C[NH]CCNC1
HCl
O
null
null
C1CNCCNC1.O=C(Cl)OCc1ccccc1>O>O=C(OCc1ccccc1)N1CCCNCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5e959f0c247e4beda9969377311282aa
CC(C)(C)OC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O.O=C(OCc1ccccc1)N1CCCNCC1>>CC(C)(C)OC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCCN(C(=O)OCc2ccccc2)CC1
C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)O.C(C1=CC=CC=C1)OC(=O)N1CCNCCC1.O.ON1N=NC2=C1C=CC=C2.C1CCC(CC1)N=C=NC2CCCCC2>>C(C1=CC=CC=C1)OC(=O)N1CCN(CCC1)C([C@@H](NC(=O)OC(C)(C)C)CC1=CC=C(C=C1)O)=O
O[C:18]([C@@H:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:10][c:11]1[cH:12][cH:13][c:14]([OH:15])[cH:16][cH:17]1)=[O:19].[NH:20]1[CH2:21][CH2:22][CH2:23][N:24]([C:25](=[O:26])[O:27][CH2:28][c:29]2[cH:30][cH:31][cH:32][cH:33][cH:34]2)[CH2:35][CH2:36]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[...
CC(C)(C)OC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O.O=C(OCc1ccccc1)N1CCCNCC1
CC(C)(C)OC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCCN(C(=O)OCc2ccccc2)CC1
null
null
O1CCCC1
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
fb7b4c9fc8ef266dfa5161dd684d02bd3bdb61458c00dd0f23100f34a6c5763c
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(CCc1ccccc1)N1CCCN(C(=O)OCc2ccccc2)CC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[#7:13]-[C:14]-[C:15]-[NH;D2;+0:16]-[C:17]-[C:18]>>[#7:13]-[C:14]-[C:15]-[N;H0;D3;+0:16](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;...
97.7
[{"value": 97.7, "product": "C(C1=CC=CC=C1)OC(=O)N1CCN(CCC1)C([C@@H](NC(=O)OC(C)(C)C)CC1=CC=C(C=C1)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
15.29 g of N-tert-butoxycarbonyltyrosine and 12.73 g of N-benzyloxycarbonylhomopiperazine were dissolved in 280 ml of tetrahydrofuran, to the solution were added 8.09 g of 1-hydroxybenzotriazole hydrate and 11.77 g of DCC at a room temperature with stirring, and the reaction mixture was stirred for 16 hours. The reacti...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CNCC[NH]C1
C1C[NH]CC[NH]C1
c1ccccc1.C1C[NH]CC[NH]C1.c1ccccc1
HO-
O1CCCC1
null
null
CC(C)(C)OC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O.O=C(OCc1ccccc1)N1CCCNCC1>O1CCCC1>CC(C)(C)OC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCCN(C(=O)OCc2ccccc2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fa570eec38af45bdaa6d75337b1e1aef
O=C(OCc1ccccc1)N1CCCN(C(=O)[C@H](Cc2ccc(OS(=O)(=O)c3cccc4cnccc34)cc2)NS(=O)(=O)c2cccc3cnccc23)CC1>>O=C(OCc1ccccc1)N1CCCN(C(=O)[C@H](Cc2ccc(O)cc2)NS(=O)(=O)c2cccc3cnccc23)CC1
C([O-])(O)=O.[Na+].C(C1=CC=CC=C1)OC(=O)N1CCN(CCC1)C([C@@H](NS(=O)(=O)C=1C=2C=CN=CC2C=CC1)CC1=CC=C(C=C1)OS(=O)(=O)C=1C=2C=CN=CC2C=CC1)=O.[OH-].[Na+].C(CC(O)(C(=O)O)CC(=O)O)(=O)O>>C(C1=CC=CC=C1)OC(=O)N1CCN(CCC1)C([C@@H](NS(=O)(=O)C=1C=2C=CN=CC2C=CC1)CC1=CC=C(C=C1)O)=O
O=S(=O)(c1cccc2cnccc12)[O:24][c:23]1[cH:22][cH:21][c:20]([CH2:19][C@@H:18]([C:16]([N:15]2[CH2:14][CH2:13][CH2:12][N:11]([C:2](=[O:1])[O:3][CH2:4][c:5]3[cH:6][cH:7][cH:8][cH:9][cH:10]3)[CH2:42][CH2:41]2)=[O:17])[NH:27][S:28](=[O:29])(=[O:30])[c:31]2[cH:32][cH:33][cH:34][c:35]3[cH:36][n:37][cH:38][cH:39][c:40]23)[cH:26][...
O=C(OCc1ccccc1)N1CCCN(C(=O)[C@H](Cc2ccc(OS(=O)(=O)c3cccc4cnccc34)cc2)NS(=O)(=O)c2cccc3cnccc23)CC1
O=C(OCc1ccccc1)N1CCCN(C(=O)[C@H](Cc2ccc(O)cc2)NS(=O)(=O)c2cccc3cnccc23)CC1
null
null
CO.O1CCCC1
Reduction
OtherReaction
8d3501a80697ea4890ac38f15ca267ef68b4b9c0548f46156239e85ec85dc664
755d4c7608355ba6558947cede05bc0a8af24b48bc69544e09fcab6bd629384a
O=C(OCc1ccccc1)N1CCCN(C(=O)[C@H](Cc2ccccc2)NS(=O)(=O)c2cccc3cnccc23)CC1
O=S(=O)(-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4])-c1:c:c:c:c2:c:n:c:c:c:1:2>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
74.7
[{"value": 74.7, "product": "C(C1=CC=CC=C1)OC(=O)N1CCN(CCC1)C([C@@H](NS(=O)(=O)C=1C=2C=CN=CC2C=CC1)CC1=CC=C(C=C1)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
5.50 g of the amorphous compound obtained in Example 122 was dissolved in 30 ml of methanol and 30 ml of tetrahydrofuran, to the solution was added 60 ml of 1N sodium hydroxide, and the mixture was refluxed for 2 hours and then cooled. The reaction mixture was acidified with citric acid and then alkalized with sodium b...
10.6084/m9.figshare.5104873.v1
null
Sulfonate
Aromatic alcohol
c1ccc2cnccc2c1
null
c1ccccc1.C1C[NH]CC[NH]C1.c1ccccc1.c1ccc2cnccc2c1
HO-
CO.O1CCCC1
null
null
O=C(OCc1ccccc1)N1CCCN(C(=O)[C@H](Cc2ccc(OS(=O)(=O)c3cccc4cnccc34)cc2)NS(=O)(=O)c2cccc3cnccc23)CC1>CO.O1CCCC1>O=C(OCc1ccccc1)N1CCCN(C(=O)[C@H](Cc2ccc(O)cc2)NS(=O)(=O)c2cccc3cnccc23)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-941e293f0a7c46e8b8635a04d61fecdf
CI.CN(C(Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)CN1CCC2(CC1)OCCO2)S(=O)(=O)c1cccc2cnccc12>>COc1ccc(CC(CN2CCC(=O)CC2)N(C)S(=O)(=O)c2cccc3cnccc23)cc1
CI.C([O-])([O-])=O.[K+].[K+].CN(C=O)C.O1CCCC1.Cl.C1OC2(CCN(CC2)CC(CC2=CC=C(C=C2)OS(=O)(=O)C=2C=3C=CN=CC3C=CC2)N(S(=O)(=O)C=2C=3C=CN=CC3C=CC2)C)OC1>>COC1=CC=C(CC(CN2CCC(CC2)=O)N(S(=O)(=O)C=2C=3C=CN=CC3C=CC2)C)C=C1
I[CH3:1].O=S(=O)(c1cccc2cnccc12)[O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH:8]([CH2:9][N:10]2[CH2:11][CH2:12][C:13]3(OCC[O:14]3)[CH2:15][CH2:16]2)[N:17]([CH3:18])[S:19](=[O:20])(=[O:21])[c:22]2[cH:23][cH:24][cH:25][c:26]3[cH:27][n:28][cH:29][cH:30][c:31]23)[cH:32][cH:33]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH:8](...
CI.CN(C(Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)CN1CCC2(CC1)OCCO2)S(=O)(=O)c1cccc2cnccc12
COc1ccc(CC(CN2CCC(=O)CC2)N(C)S(=O)(=O)c2cccc3cnccc23)cc1
null
null
null
Acylation
OtherReaction
99d28ed00b31ff0a902f97e2bddd045ff5f84e1e11411b2281454b5217be20b7
1691c310bf4574df6a9d9db1231c07fcb5dfb991f04b310ec3830fb6f6e98d3e
O=C1CCN(CC(Cc2ccccc2)NS(=O)(=O)c2cccc3cnccc23)CC1
C1-C-[O;H0;D2;+0:1]-[C;H0;D4;+0:2]2(-O-1)-[C:3]-[C:4]-[#7:5]-[C:6]-[C:7]-2.O=S(=O)(-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11])-c1:c:c:c:c2:c:n:c:c:c:1:2.I-[CH3;D1;+0:12]>>[CH3;D1;+0:12]-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11].[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[#7:5]-[C:6]-[C:7]-1
null
[]
null
null
null
null
The amorphous compound obtained in Example 94 was subjected to alkaline hydrolysis, methylation with methyl iodide and potassium carbonate in dimethylformamide/tetrahydrofuran (1:1), and reflux with 3N hydrochloric acid, to obtain N-{1-(p-methoxybenzyl)-2-(4-oxopiperidino)ethyl}-N-methyl-5-isoquinolinesulfonamide in a ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Sulfonate
Ketone.Ether
c1ccc2cnccc2c1.C1CC2(CC[NH]1)OCCO2
C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccc2cnccc2c1
HI
null
null
null
CI.CN(C(Cc1ccc(OS(=O)(=O)c2cccc3cnccc23)cc1)CN1CCC2(CC1)OCCO2)S(=O)(=O)c1cccc2cnccc12>>COc1ccc(CC(CN2CCC(=O)CC2)N(C)S(=O)(=O)c2cccc3cnccc23)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-18f979271f55488dada415f3d9cd2cc3
O=C(O)C=Cc1ccc(Cl)cc1>>COC(=O)C=Cc1ccc(Cl)cc1
ClC1=CC=C(C=CC(=O)O)C=C1.S(O)(O)(=O)=O.C([O-])(O)=O.[Na+]>>ClC1=CC=C(C=CC(=O)OC)C=C1
[OH:2][C:3](=[O:4])[CH:5]=[CH:6][c:7]1[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]=[CH:6][c:7]1[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]1
O=C(O)C=Cc1ccc(Cl)cc1
COC(=O)C=Cc1ccc(Cl)cc1
null
null
CO
Miscellaneous
Protection of carboxylic acid
56520e0abb4535dce9a663824ca803b71c2c0dd72dfd246317d953596a987bd2
2ccc7a30191c2c171b49e8a0217bee87430687dd0f567141eca025a75b7e3136
c1ccccc1
[O;D1;H0:1]=[C:2](-[OH;D1;+0:3])-[C:4]=[C:5]-[c:6]>>[C;D1;H3:7]-[O;H0;D2;+0:3]-[C:2](=[O;D1;H0:1])-[C:4]=[C:5]-[c:6]
null
[]
null
null
null
null
25.9 g of p-chlorocinnamic acid was dissolved in 250 ml of methanol, to the solution was added 1.5 ml of concentrated sulfuric acid, and the mixture was refluxed for 2 hours. The reaction mixture was poured on ice, and the mixture was alkalized with sodium bicarbonate and extracted twice with 1000 ml of chloroform. The...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1ccccc1
Other
CO
null
null
O=C(O)C=Cc1ccc(Cl)cc1>CO>COC(=O)C=Cc1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c09855ed64714736b79c8d5024c94a04
ClCC=Cc1ccc(Cl)cc1.Nc1ccccc1N>>Nc1ccccc1NCC=Cc1ccc(Cl)cc1
ClC1=CC=C(C=CCCl)C=C1.C([O-])([O-])=O.[K+].[K+].C1(=C(C=CC=C1)N)N.[Cl-].[Na+]>>ClC1=CC=C(C=CCNC2=C(C=CC=C2)N)C=C1
Cl[CH2:9][CH:10]=[CH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1.[NH2:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[NH2:8]>>[NH2:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[NH:8][CH2:9][CH:10]=[CH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1
ClCC=Cc1ccc(Cl)cc1.Nc1ccccc1N
Nc1ccccc1NCC=Cc1ccc(Cl)cc1
null
null
CN(C=O)C.O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
C(=Cc1ccccc1)CNc1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]=[C:3]-[c:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:4]-[C:3]=[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
82.2
[{"value": 82.2, "product": "ClC1=CC=C(C=CCNC2=C(C=CC=C2)N)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
19.6 g of 1,2-phenylenediamine was dissolved in 300 ml of dimethylformamide, to the solution were added 11.3 g of the above-prepared 4-chlorocinnamyl chloride crystals and 12.5 g of potassium carbonate at a room temperature with stirring, and the mixture was stirred for 48 hours under the same condition. After adding w...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccccc1
HCl
CN(C=O)C.O
null
null
ClCC=Cc1ccc(Cl)cc1.Nc1ccccc1N>CN(C=O)C.O>Nc1ccccc1NCC=Cc1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d4ee0e39c1e94258bf77463d69e44f83
ClCC=Cc1ccc(Cl)cc1.Nc1cccnc1N>>Nc1ncccc1NCC=Cc1ccc(Cl)cc1
O.ClC1=CC=C(C=CCCl)C=C1.NC1=NC=CC=C1N.C([O-])([O-])=O.[K+].[K+]>>NC1=NC=CC=C1NCC=CC1=CC=C(C=C1)Cl
Cl[CH2:9][CH:10]=[CH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1.[NH2:1][c:2]1[n:3][cH:4][cH:5][cH:6][c:7]1[NH2:8]>>[NH2:1][c:2]1[n:3][cH:4][cH:5][cH:6][c:7]1[NH:8][CH2:9][CH:10]=[CH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1
ClCC=Cc1ccc(Cl)cc1.Nc1cccnc1N
Nc1ncccc1NCC=Cc1ccc(Cl)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
C(=Cc1ccccc1)CNc1cccnc1
Cl-[CH2;D2;+0:1]-[C:2]=[C:3]-[c:4].[N;D1;H2:5]-[c:6](:[#7;a:7]:[c:8]):[c:9](-[NH2;D1;+0:10]):[c:11]>>[N;D1;H2:5]-[c:6](:[#7;a:7]:[c:8]):[c:9](-[NH;D2;+0:10]-[CH2;D2;+0:1]-[C:2]=[C:3]-[c:4]):[c:11]
42.2
[{"value": 42.2, "product": "NC1=NC=CC=C1NCC=CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
50
HOUR
7.71 g of p-chlorocinnamyl chloride and 13.5 g of 2,3-diaminopyridine were dissolved in 220 ml of dimethylformamide, and to the solution was added 8.6 g of potassium carbonate, and the mixture was stirred at a room temperature for 50 hours, and after adding 300 ml of water, extracted twice with 200 ml of chloroform. Th...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccncc1.c1ccccc1
HCl
CN(C=O)C
null
50
ClCC=Cc1ccc(Cl)cc1.Nc1cccnc1N>CN(C=O)C>Nc1ncccc1NCC=Cc1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-06bb6720d27140e6bd8fead9cef0ffdf
CN(C)c1ccccn1.Cl.O=S(=O)(Cl)c1cccc2cnccc12.c1ccncc1>>O=S(=O)(Nc1ncccc1NCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
N1=CC=CC=C1.Cl.C1=NC=CC=2C(=CC=CC12)S(=O)(=O)Cl.CN(C)C1=NC=CC=C1.O>>ClC1=CC=C(C=CCNC=2C(=NC=CC2)NS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1
[N:4]([c:5]1[n:6][cH:7][cH:8][cH:9][cH:10]1)([CH3:12])[CH3:15].[ClH:19].Cl[S:2](=[O:1])(=[O:3])[c:22]1[cH:23][cH:24][cH:25][c:26]2[cH:27][n:28][cH:29][cH:30][c:31]12.[n:11]1[cH:16][cH:17][cH:18][cH:20][cH:21]1>>[O:1]=[S:2](=[O:3])([NH:4][c:5]1[n:6][cH:7][cH:8][cH:9][c:10]1[NH:11][CH2:12][CH:13]=[CH:14][c:15]1[cH:16][cH...
CN(C)c1ccccn1.Cl.O=S(=O)(Cl)c1cccc2cnccc12.c1ccncc1
O=S(=O)(Nc1ncccc1NCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
null
null
null
C-C Coupling
OtherReaction
e576e93b7dd529fcbe41d45e86cb0e44802fd9459a65fd894839606d16beacf5
347c6dd5e9f26f467f6591e9949b355e3b716dcfb02d962314646380ac72c472
O=S(=O)(Nc1ncccc1NCC=Cc1ccccc1)c1cccc2cnccc12
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[CH3;D1;+0:7]-[N;H0;D3;+0:8](-[CH3;D1;+0:9])-[c:10]1:[#7;a:11]:[c:12]:[c:13]:[c:14]:[cH;D2;+0:15]:1.[ClH;D0;+0:16].[c:17]1:[cH;D2;+0:18]:[n;H0;D2;+0:19]:[cH;D2;+0:20]:[c:21]:[cH;D2;+0:22]:1>>[Cl;H0;D1;+0:16]-[c;H0;D3;+0:22]1:[c:17]:[cH;D2;+0:18]:[c;H0;D3...
null
[]
null
null
18
HOUR
4.52 g of the crystals obtained in Reference Example 41 was dissolved in 50 ml of pyridine, to the solution were added 5.8 g of 5-isoquinolinesulfonyl chloride hydrochloride and 3 g of dimethylaminopyridine, and the mixture was stirred for 18 hours at a room temperature, after adding 150 ml of water, extracted twice wi...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine.Sulfonyl halide
Sulfonamide.Aromatic halide.Secondary amine
c1ccncc1.c1ccncc1
c1ccncc1.c1ccccc1
c1ccncc1.c1ccccc1.c1ccc2cnccc2c1
HCl
null
null
18
CN(C)c1ccccn1.Cl.O=S(=O)(Cl)c1cccc2cnccc12.c1ccncc1>>O=S(=O)(Nc1ncccc1NCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-02666c15032d4a23816abf9f01b6ac87
COC(=O)c1ccc(N)c(N)c1.ClCC=Cc1ccc(Cl)cc1>>COC(=O)c1ccc(N)c(NCC=Cc2ccc(Cl)cc2)c1
NC=1C=C(C(=O)OC)C=CC1N.C([O-])([O-])=O.[K+].[K+].ClC1=CC=C(C=CCCl)C=C1>>NC1=C(C=C(C(=O)OC)C=C1)NCC=CC1=CC=C(C=C1)Cl
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([NH2:9])[c:10]([NH2:11])[cH:22]1.Cl[CH2:12][CH:13]=[CH:14][c:15]1[cH:16][cH:17][c:18]([Cl:19])[cH:20][cH:21]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([NH2:9])[c:10]([NH:11][CH2:12][CH:13]=[CH:14][c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][cH:21]2)[cH:22]1
COC(=O)c1ccc(N)c(N)c1.ClCC=Cc1ccc(Cl)cc1
COC(=O)c1ccc(N)c(NCC=Cc2ccc(Cl)cc2)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
C(=Cc1ccccc1)CNc1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]=[C:3]-[c:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:4]-[C:3]=[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
63.2
[{"value": 63.2, "product": "NC1=C(C=C(C(=O)OC)C=C1)NCC=CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
5.0 g of methyl 3,4-diaminobenzoate was dissolved in 40 ml of dimethylformamide, and to the solution were added 2.07 g of potassium carbonate and 1.87 g of p-chlorocinnamyl chloride, and reaction was carried out according to the procedure in Reference Example 40, to obtain 2.0 g of the title compound as a light brown o...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccccc1
HCl
CN(C=O)C
null
null
COC(=O)c1ccc(N)c(N)c1.ClCC=Cc1ccc(Cl)cc1>CN(C=O)C>COC(=O)c1ccc(N)c(NCC=Cc2ccc(Cl)cc2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fe25518ea9ed4d34b2044f4a465444f9
ClCC=Cc1ccccc1.Nc1ccccc1N>>Nc1ccccc1NCC=Cc1ccccc1
C1(=C(C=CC=C1)N)N.C([O-])([O-])=O.[K+].[K+].C(C=CC1=CC=CC=C1)Cl>>C(C=CC1=CC=CC=C1)NC1=C(C=CC=C1)N
Cl[CH2:9][CH:10]=[CH:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[NH2:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[NH2:8]>>[NH2:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[NH:8][CH2:9][CH:10]=[CH:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
ClCC=Cc1ccccc1.Nc1ccccc1N
Nc1ccccc1NCC=Cc1ccccc1
null
null
O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
C(=Cc1ccccc1)CNc1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]=[C:3]-[c:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:4]-[C:3]=[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
89.5
[{"value": 89.5, "product": "C(C=CC1=CC=CC=C1)NC1=C(C=CC=C1)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
3.24 g of ortho-phenylenediamine was dissolved in 30 ml of dimithylformaide, to the solution were added 2.07 g of potassium carbonate and 1.52 g of cinnamyl chloride, and the mixture was stirred overnight at a room temperature. After adding 100 ml of water, the reaction mixture was extracted twice with 100 ml and 50 ml...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccccc1
HCl
O
null
8
ClCC=Cc1ccccc1.Nc1ccccc1N>O>Nc1ccccc1NCC=Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-09e583f252ac431594d8cdd55b9396bd
CC(=O)C=Cc1ccc(Cl)cc1.NCCNS(=O)(=O)c1cccc2cnccc12>>CC(=Cc1ccc(Cl)cc1)CNCCNS(=O)(=O)c1cccc2cnccc12
ClC1=CC=C(C=CC(C)=O)C=C1.NCCNS(=O)(=O)C=1C=2C=CN=CC2C=CC1.CO.[Na]>>ClC1=CC=C(C=C(CNCCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C)C=C1
O=[C:2]([CH3:1])[CH:11]=[CH:3][c:4]1[cH:5][cH:6][c:7]([Cl:8])[cH:9][cH:10]1.[NH2:12][CH2:13][CH2:14][NH:15][S:16](=[O:17])(=[O:18])[c:19]1[cH:20][cH:21][cH:22][c:23]2[cH:24][n:25][cH:26][cH:27][c:28]12>>[CH3:1][C:2](=[CH:3][c:4]1[cH:5][cH:6][c:7]([Cl:8])[cH:9][cH:10]1)[CH2:11][NH:12][CH2:13][CH2:14][NH:15][S:16](=[O:17...
CC(=O)C=Cc1ccc(Cl)cc1.NCCNS(=O)(=O)c1cccc2cnccc12
CC(=Cc1ccc(Cl)cc1)CNCCNS(=O)(=O)c1cccc2cnccc12
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4940e8ed9a0db9bde699fdcdc3aff2cff0409c19478aa0ed1acfd98213338adf
07faf85ffe990e88a1de7fd04a339bf226f78d8bfae9712ea59eebd76bb54b9f
O=S(=O)(NCCNCC=Cc1ccccc1)c1cccc2cnccc12
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[CH;D2;+0:3]=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:8]-[C:9]-[NH;D2;+0:10]-[CH2;D2;+0:3]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
36
HOUR
7.30 g of N-(2-aminoethyl)-5-isoquinolinesulfonamide was dissolved in 150 ml of methanol, to the solution was added 6.30 g of p-chlorobenzalacetone, and the mixture was stirred at a room temperature for 36 hours. After addition of 1.32 g of sodium tetrahydrideborate with ice-water cooling, the mixture was stirred for 3...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2cnccc2c1
Other
null
null
36
CC(=O)C=Cc1ccc(Cl)cc1.NCCNS(=O)(=O)c1cccc2cnccc12>>CC(=Cc1ccc(Cl)cc1)CNCCNS(=O)(=O)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-972b7e9615b641608f2fd7c85b62dfc9
NCCNS(=O)(=O)c1cccc2cnccc12.O=CC=Cc1ccc(Cl)cc1>>O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
C(C)(=O)OCC.ClC1=CC=C(C=CC=O)C=C1.NCCNS(=O)(=O)C=1C=2C=CN=CC2C=CC1.[Na]>>ClC1=CC=C(C=CCNCCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1
[O:1]=[S:2](=[O:3])([NH:4][CH2:5][CH2:6][NH2:7])[c:18]1[cH:19][cH:20][cH:21][c:22]2[cH:23][n:24][cH:25][cH:26][c:27]12.O=[CH:8][CH:9]=[CH:10][c:11]1[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]1>>[O:1]=[S:2](=[O:3])([NH:4][CH2:5][CH2:6][NH:7][CH2:8][CH:9]=[CH:10][c:11]1[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]1)[c:18]1...
NCCNS(=O)(=O)c1cccc2cnccc12.O=CC=Cc1ccc(Cl)cc1
O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
null
null
CO
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
O=S(=O)(NCCNCC=Cc1ccccc1)c1cccc2cnccc12
O=[CH;D2;+0:1]-[C:2]=[C:3]-[c:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[C:2]=[C:3]-[c:4]
71.5
[{"value": 71.5, "product": "ClC1=CC=C(C=CCNCCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2.01 g of N-(2-aminoethyl]-5-isoquinolinesulfonamide was dissolved in 30 ml of methanol, to the solution was added 1.60 g of p-chlorocinnamaldehyde, and the mixture was stirred for one hour at a room temperature. After an addition of 350 mg of sodium tetrahydrideborate in portions with ice cooling, the mixture was stir...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2cnccc2c1
Other
CO
null
1
NCCNS(=O)(=O)c1cccc2cnccc12.O=CC=Cc1ccc(Cl)cc1>CO>O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-06512ce644cf455d94b7605de32b603b
CI.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>>CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12
ClC1=CC=C(C=CCNCCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1.CI>>ClC1=CC=C(C=CCN(C)CCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1
I[CH3:1].[NH:2]([CH2:3][CH:4]=[CH:5][c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH2:13][CH2:14][NH:15][S:16](=[O:17])(=[O:18])[c:19]1[cH:20][cH:21][cH:22][c:23]2[cH:24][n:25][cH:26][cH:27][c:28]12>>[CH3:1][N:2]([CH2:3][CH:4]=[CH:5][c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH2:13][CH2:14][NH:15][S:16](=[O:17...
CI.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
e1587a52a1bca6a80c6048d43276d8bccf8d3e94e692e6b210e5fd3b22494187
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
O=S(=O)(NCCNCC=Cc1ccccc1)c1cccc2cnccc12
I-[CH3;D1;+0:1].[C:2]-[C:3]-[NH;D2;+0:4]-[C:5]-[C:6]=[C:7]-[c:8]>>[C:2]-[C:3]-[N;H0;D3;+0:4](-[CH3;D1;+0:1])-[C:5]-[C:6]=[C:7]-[c:8]
null
[]
null
null
40
MINUTE
1.50 g of the product of Example 172 was dissolved in 10 ml of chloroform, to the solution was added 3 ml of methyl iodide at a room temperature, and the mixture was stirred for 40 minutes. Excess methyl iodide was immediately evaporated off under a reduced pressure, and resulting residue was purified on a silica gel c...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
null
null
c1ccccc1.c1ccc2cnccc2c1
HI
C(Cl)(Cl)Cl
null
0.666667
CI.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>C(Cl)(Cl)Cl>CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-57a90189c8764512903a44bb9d37a3a5
O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>>O=S(=O)(c1cccc2cnccc12)N1CCN(CC=Cc2ccc(Cl)cc2)CC1
C(C)(=O)OCC.BrCCBr.C([O-])([O-])=O.[K+].[K+].ClC1=CC=C(C=CCNCCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1>>ClC1=CC=C(C=CCN2CCN(CC2)S(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1
[O:1]=[S:2](=[O:3])([c:4]1[cH:5][cH:6][cH:7][c:8]2[cH:9][n:10][cH:11][cH:12][c:13]12)[NH:14][CH2:15][CH2:16][NH:17][CH2:18][CH:19]=[CH:20][c:21]1[cH:22][cH:23][c:24]([Cl:25])[cH:26][cH:27]1>>[O:1]=[S:2](=[O:3])([c:4]1[cH:5][cH:6][cH:7][c:8]2[cH:9][n:10][cH:11][cH:12][c:13]12)[N:14]1[CH2:15][CH2:16][N:17]([CH2:18][CH:19...
O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
O=S(=O)(c1cccc2cnccc12)N1CCN(CC=Cc2ccc(Cl)cc2)CC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
1b33cc1f8e92e881af12e0e380d1a778ae5ef329639dfd7cb00ef69fd92a311f
161c3116a4374afd3332c7fbbdc4c4b8bc038020c5e2de722337ee190caa63bd
O=S(=O)(c1cccc2cnccc12)N1CCN(CC=Cc2ccccc2)CC1
[O;D1;H0:1]=[#16:2](=[O;D1;H0:3])(-[c:4])-[NH;D2;+0:5]-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]=[C:11]-[c:12]>>[O;D1;H0:1]=[#16:2](=[O;D1;H0:3])(-[c:4])-[N;H0;D3;+0:5]1-[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9]-[C:10]=[C:11]-[c:12])-[C:13]-[C:14]-1
25.5
[{"value": 25.5, "product": "ClC1=CC=C(C=CCN2CCN(CC2)S(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
1.31 g of the product of Example 172 was dissolved in 3 ml of dimethylformamide, to the solution were added 644 mg of 1,2-dibromoethane and 1.13 g of anhydrous potassium carbonate at a room temperature, and the mixture was stirred for 24 hours. After adding 100 ml of ethyl acetate, the ethyl acetate layer was sequentia...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Secondary amine
Tertiary amine.Tertiary amine
null
C1C[NH]CC[NH]1
c1ccc2cnccc2c1.C1C[NH]CC[NH]1.c1ccccc1
Other
CN(C=O)C
null
24
O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>CN(C=O)C>O=S(=O)(c1cccc2cnccc12)N1CCN(CC=Cc2ccc(Cl)cc2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bdd40074d9ed4c75ae6e98ec6d069c3c
O=CO.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>>O=CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12
C([O-])([O-])=O.[Na+].[Na+].C(=O)O.C(C)(=O)OC(C)=O.ClC1=CC=C(C=CCNCCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1>>ClC1=CC=C(C=CCN(C=O)CCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1
O[CH:2]=[O:1].[NH:3]([CH2:4][CH:5]=[CH:6][c:7]1[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]1)[CH2:14][CH2:15][NH:16][S:17](=[O:18])(=[O:19])[c:20]1[cH:21][cH:22][cH:23][c:24]2[cH:25][n:26][cH:27][cH:28][c:29]12>>[O:1]=[CH:2][N:3]([CH2:4][CH:5]=[CH:6][c:7]1[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]1)[CH2:14][CH2:15][NH:16][...
O=CO.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
O=CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12
null
null
C(C)(=O)OCC
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
ac72df6259d5d7baee7abdbd4706ef4b4627f86ead9dc94f0cefcfcb37c21def
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=S(=O)(NCCNCC=Cc1ccccc1)c1cccc2cnccc12
O-[CH;D2;+0:1]=[O;D1;H0:2].[C:3]-[C:4]-[NH;D2;+0:5]-[C:6]-[C:7]=[C:8]-[c:9]>>[C:3]-[C:4]-[N;H0;D3;+0:5](-[C:6]-[C:7]=[C:8]-[c:9])-[CH;D2;+0:1]=[O;D1;H0:2]
null
[]
null
null
null
null
3 ml of formic acid and 3 ml of acetic anhydride were mixed and stirred at a room temperature, and to the mixture was added 1.41 g of the product of Example 172, and the mixture was stirred for one hour. The reaction mixture was added to 50 ml of ethyl acetate and 30 ml of saturated sodium carbonate aqueous solution wi...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
null
null
c1ccccc1.c1ccc2cnccc2c1
HO-
C(C)(=O)OCC
null
null
O=CO.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>C(C)(=O)OCC>O=CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ad93cea3c46c4c05874b445fc5c954fd
O=Cc1ccc(O)cc1.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>>O=S(=O)(NCCN(CC=Cc1ccc(Cl)cc1)Cc1ccc(O)cc1)c1cccc2cnccc12
C(#N)[BH3-].[Na+].ClC1=CC=C(C=CCNCCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1.OC1=CC=C(C=O)C=C1>>ClC1=CC=C(C=CCN(CC2=CC=C(C=C2)O)CCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1
O=[CH:18][c:19]1[cH:20][cH:21][c:22]([OH:23])[cH:24][cH:25]1.[O:1]=[S:2](=[O:3])([NH:4][CH2:5][CH2:6][NH:7][CH2:8][CH:9]=[CH:10][c:11]1[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]1)[c:26]1[cH:27][cH:28][cH:29][c:30]2[cH:31][n:32][cH:33][cH:34][c:35]12>>[O:1]=[S:2](=[O:3])([NH:4][CH2:5][CH2:6][N:7]([CH2:8][CH:9]=[CH:10][...
O=Cc1ccc(O)cc1.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12
O=S(=O)(NCCN(CC=Cc1ccc(Cl)cc1)Cc1ccc(O)cc1)c1cccc2cnccc12
null
C(C)(=O)O
CO
Heteroatom Alkylation and Arylation
reductive amination
6d9c60e7c47e75322fc9565d992b855788f3516a27cb14d7f9ed299e190b30d3
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
O=S(=O)(NCCN(CC=Cc1ccccc1)Cc1ccccc1)c1cccc2cnccc12
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]=[C:10]-[c:11]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[C:8]-[C:9]=[C:10]-[c:11])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
59.3
[{"value": 59.3, "product": "ClC1=CC=C(C=CCN(CC2=CC=C(C=C2)O)CCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
DAY
0.2 g of the product of Example 172 and 0.13 g of p-hydroxybenzaldehyde were dissolved in 10 ml of methanol, to the solution were added 60 mg of sodium cyanoborohydride and two drops of acetic acid, and the mixture was stirred for 2 days at a room temperature. The reaction mixture was concentrated under a reduced press...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
null
null
c1ccccc1.c1ccccc1.c1ccc2cnccc2c1
Other
C(C)(=O)O.CO
null
48
O=Cc1ccc(O)cc1.O=S(=O)(NCCNCC=Cc1ccc(Cl)cc1)c1cccc2cnccc12>C(C)(=O)O.CO>O=S(=O)(NCCN(CC=Cc1ccc(Cl)cc1)Cc1ccc(O)cc1)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bb0f112c30d04259bcbd03fbf9a0c4bf
CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12.OCCN1CCCCC1>>CN(CC=Cc1ccc(Cl)cc1)CCN(CCN1CCCCC1)S(=O)(=O)c1cccc2cnccc12
ClC1=CC=C(C=CCN(C)CCNS(=O)(=O)C=2C=3C=CN=CC3C=CC2)C=C1.N1(CCCCC1)CCO.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.N(=NC(=O)OCC)C(=O)OCC>>ClC1=CC=C(C=CCN(C)CCN(S(=O)(=O)C=2C=3C=CN=CC3C=CC2)CCN2CCCCC2)C=C1
[CH3:1][N:2]([CH2:3][CH:4]=[CH:5][c:6]1[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]1)[CH2:13][CH2:14][NH:15][S:24](=[O:25])(=[O:26])[c:27]1[cH:28][cH:29][cH:30][c:31]2[cH:32][n:33][cH:34][cH:35][c:36]12.O[CH2:16][CH2:17][N:18]1[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]1>>[CH3:1][N:2]([CH2:3][CH:4]=[CH:5][c:6]1[cH:7][cH:8][c:...
CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12.OCCN1CCCCC1
CN(CC=Cc1ccc(Cl)cc1)CCN(CCN1CCCCC1)S(=O)(=O)c1cccc2cnccc12
null
null
C(C)(=O)OCC.O1CCCC1
Heteroatom Alkylation and Arylation
Mitsunobu_sulfonamide
0bda68210bc1a4edc8064b140a39ccb3ef813b89c5267469bd545dded6906cd4
2497efd1dadfa61592e966deb414dc4463866875b7ffd693ba98c7592e2a7ec2
O=S(=O)(c1cccc2cnccc12)N(CCNCC=Cc1ccccc1)CCN1CCCCC1
O-[CH2;D2;+0:1]-[C:2]-[#7:3].[C:4]-[C:5]-[NH;D2;+0:6]-[#16:7](=[O;D1;H0:8])(=[O;D1;H0:9])-[c:10]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C:5]-[C:4])-[#16:7](=[O;D1;H0:8])(=[O;D1;H0:9])-[c:10]
74.9
[{"value": 74.9, "product": "ClC1=CC=C(C=CCN(C)CCN(S(=O)(=O)C=2C=3C=CN=CC3C=CC2)CCN2CCCCC2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 0.39 g of the amorphous compound obtained in Example 190, 0.145 g of 1-piperidinethanol and 0.369 g of triphenylphosphine in 5 ml of tetrahydrofuran, was added dropwise a solution of 0.245 g of diethyl azodicarboxylate in 2 ml of tetrahydrofuran with stirring under ice cooling. The mixture was stirred ...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Primary alcohol
Tertiary amine
null
null
c1ccccc1.C1CC[NH]CC1.c1ccc2cnccc2c1
HO-
C(C)(=O)OCC.O1CCCC1
null
null
CN(CC=Cc1ccc(Cl)cc1)CCNS(=O)(=O)c1cccc2cnccc12.OCCN1CCCCC1>C(C)(=O)OCC.O1CCCC1>CN(CC=Cc1ccc(Cl)cc1)CCN(CCN1CCCCC1)S(=O)(=O)c1cccc2cnccc12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-98066fc44b1d4119929f1efebf1ad116
COc1ccc(N)cc1OC.O=S(=O)(Cl)c1cccc2cnccc12>>COc1ccc(NS(=O)(=O)c2cccc3cnccc23)cc1OC
COC=1C=C(N)C=CC1OC.C1=NC=CC=2C(=CC=CC12)S(=O)(=O)Cl.Cl>>COC=1C=C(C=CC1OC)NS(=O)(=O)C=1C=2C=CN=CC2C=CC1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:21][c:22]1[O:23][CH3:24].Cl[S:8](=[O:9])(=[O:10])[c:11]1[cH:12][cH:13][cH:14][c:15]2[cH:16][n:17][cH:18][cH:19][c:20]12>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][S:8](=[O:9])(=[O:10])[c:11]2[cH:12][cH:13][cH:14][c:15]3[cH:16][n:17][cH:18][cH:19][c:20]23)[cH:21][c:22]1[O...
COc1ccc(N)cc1OC.O=S(=O)(Cl)c1cccc2cnccc12
COc1ccc(NS(=O)(=O)c2cccc3cnccc23)cc1OC
null
null
N1=CC=CC=C1
Acylation
Sulfonamide synthesis (Schotten-Baumann) primary amine
4c44ef6d7646f6ef25dd125d2c32c713d8dcae7c603407faa5f0fb810631670e
8fce8115d8a725afa92eb3910ded29d4c852e5133eba78a425054f41f7142603
O=S(=O)(Nc1ccccc1)c1cccc2cnccc12
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[O;D1;H0:2]=[S;H0;D4;+0:1](=[O;D1;H0:3])(-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10])-[c:4](:[c:5]):[c:6]
82
[{"value": 82.0, "product": "COC=1C=C(C=CC1OC)NS(=O)(=O)C=1C=2C=CN=CC2C=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
3.06 g of 3,4-dimethoxyaniline was dissolved in 30 ml of pyridine, to the solution was added in small portions 5.28 g of 5-isoquinolinesulfonyl chloride.HCl with stirring under ice cooling, and the mixture was stirred for 30 minutes, and further stirred at a room temperature overnight. After evaporating off the pyridin...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccccc1.c1ccc2cnccc2c1
HCl
N1=CC=CC=C1
null
0.5
COc1ccc(N)cc1OC.O=S(=O)(Cl)c1cccc2cnccc12>N1=CC=CC=C1>COc1ccc(NS(=O)(=O)c2cccc3cnccc23)cc1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1bf8d60c367e45b9942d7471cdaae72c
N[C@@H](Cc1ccc(O)c(I)c1)C(=O)O>>N[C@@H](Cc1ccc(O)cc1)C(=O)O
[I-].IC=1C=C(C[C@H](N)C(=O)O)C=CC1O.[I-]>>N[C@@H](CC1=CC=C(C=C1)O)C(=O)O
I[c:9]1[c:7]([OH:8])[cH:6][cH:5][c:4]([CH2:3][C@H:2]([NH2:1])[C:11](=[O:12])[OH:13])[cH:10]1>>[NH2:1][C@@H:2]([CH2:3][c:4]1[cH:5][cH:6][c:7]([OH:8])[cH:9][cH:10]1)[C:11](=[O:12])[OH:13]
N[C@@H](Cc1ccc(O)c(I)c1)C(=O)O
N[C@@H](Cc1ccc(O)cc1)C(=O)O
null
null
null
Functional Group Interconversion
Aromatic dehalogenation
b66818d3926a4463fb8e1c3d4a89e94e47b4d46960d4bdb7bcfbeeec427cfd4e
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccccc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[O;D1;H1:5]):[c:6]>>[O;D1;H1:5]-[c:4](:[c:6]):[cH;D2;+0:1]:[c:2]:[c:3]
null
[]
null
null
null
null
Electrolysis was carried out using the same cell, anode, membrane and procedure as in Example 15, except that the pH of the anolyte and catholyte was 7.0. At 85% iodide conversion, the yield of 3-iodo-L-tyrosine was 58% based on initial iodide. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccccc1
c1ccccc1
c1ccccc1
I-
null
null
null
N[C@@H](Cc1ccc(O)c(I)c1)C(=O)O>>N[C@@H](Cc1ccc(O)cc1)C(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-faa192ddc81149e4a09422705fe2de84
OC[C@H]1O[C@@H]2O[C@H]3[C@H](O)[C@@H](O)[C@@H](O[C@H]4[C@H](O)[C@@H](O)[C@@H](O[C@H]5[C@H](O)[C@@H](O)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O[C@H]8[C@H](O)[C@@H](O)[C@@H](O[C@H]1[C@H](O)[C@H]2O)O[C@@H]8CO)O[C@@H]7CO)O[C@@H]6CO)O[C@@H]5CO)O[C@@H]4CO)O[C@@H]3CO>>OC[C@H]1O[C@@H]2O[C@H]3[C@H]...
CC(C)CC(C)(C#C)O.C([C@@H]1[C@@H]2[C@@H]([C@H]([C@H](O1)O[C@@H]3[C@H](O[C@@H]([C@@H]([C@H]3O)O)O[C@@H]4[C@H](O[C@@H]([C@@H]([C@H]4O)O)O[C@@H]5[C@H](O[C@@H]([C@@H]([C@H]5O)O)O[C@@H]6[C@H](O[C@@H]([C@@H]([C@H]6O)O)O[C@@H]7[C@H](O[C@@H]([C@@H]([C@H]7O)O)O[C@@H]8[C@H](O[C@H](O2)[C@@H]([C@H]8O)O)CO)CO)CO)CO)CO)CO)O)O)O>>C([C...
[OH:10][CH2:11][C@H:12]1[O:13][C@@H:14]2[O:15][C@H:16]3[C@H:17]([OH:18])[C@@H:19]([OH:20])[C@@H:21]([O:22][C@H:23]4[C@H:24]([OH:25])[C@@H:26]([OH:27])[C@@H:28]([O:29][C@H:30]5[C@H:31]([OH:32])[C@@H:33]([OH:34])[C@@H:35]([O:36][C@H:37]6[C@H:38]([OH:39])[C@@H:40]([OH:41])[C@@H:42]([O:43][C@H:44]7[C@H:45]([OH:46])[C@@H:47...
OC[C@H]1O[C@@H]2O[C@H]3[C@H](O)[C@@H](O)[C@@H](O[C@H]4[C@H](O)[C@@H](O)[C@@H](O[C@H]5[C@H](O)[C@@H](O)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O[C@H]8[C@H](O)[C@@H](O)[C@@H](O[C@H]1[C@H](O)[C@H]2O)O[C@@H]8CO)O[C@@H]7CO)O[C@@H]6CO)O[C@@H]5CO)O[C@@H]4CO)O[C@@H]3CO
OC[C@H]1O[C@@H]2O[C@H]3[C@H](O)[C@@H](O)[C@@H](O[C@H]4[C@H](O)[C@@H](O)[C@@H](O[C@H]5[C@H](O)[C@@H](O)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O[C@H]8[C@H](O)[C@@H](O)[C@@H](O[C@H]1[C@H](O)[C@H]2O)O[C@@H]8CO)O[C@@H]7CO)O[C@@H]6CO)O[C@@H]5CO)O[C@@H]4CO)O[C@@H]3CO
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
C1C[C@@H]2OC[C@H]1O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O2
null
null
[]
null
null
null
null
A mobile slurry is prepared by mixing about 410 g β-cyclodextrin and about 330 g deionized water (distilled water can be used) at about 25° C. in a stainless steel mixing bowl of a KitchenAid mixer using the flat beater mixing attachment. Mixing is continued while about 73 g of Perfume A is added rapidly. The low visco...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
C1C[C@@H]2OC[C@H]1O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O[C@@H]1CC[C@@H](CO1)O2
null
O
null
null
OC[C@H]1O[C@@H]2O[C@H]3[C@H](O)[C@@H](O)[C@@H](O[C@H]4[C@H](O)[C@@H](O)[C@@H](O[C@H]5[C@H](O)[C@@H](O)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@@H](O[C@H]7[C@H](O)[C@@H](O)[C@@H](O[C@H]8[C@H](O)[C@@H](O)[C@@H](O[C@H]1[C@H](O)[C@H]2O)O[C@@H]8CO)O[C@@H]7CO)O[C@@H]6CO)O[C@@H]5CO)O[C@@H]4CO)O[C@@H]3CO>O>OC[C@H]1O[C@@H]2O[C@H]3[C@H...
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c92cfeae8c76411db9a7c282c6b1f728
CCOC(=O)Cl.CCOC(=O)[O-].O=C([O-])OC(=O)[O-]>>CCOC(=O)OC(=O)OCC.[Cl-]
[O-]CC.[Na+].C(=O)=O.C(OCC)([O-])=O.[Na+].C(OCC)([O-])=O.[Na+].ClC(=O)OCC.C([O-])(=O)OC(=O)[O-].C([O-])([O-])=O.[Na].C(OCC)([O-])=O.[Na+]>>C(OCC)(=O)OC(=O)OCC.[Cl-].[Na+]
O=C(O[CH2:2][CH3:1])[Cl:12].O=C([O-])[O:9][CH2:10][CH3:11].[O-][C:7]([O:6][C:4]([O-:3])=[O:5])=[O:8]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[O:6][C:7](=[O:8])[O:9][CH2:10][CH3:11].[Cl-:12]
CCOC(=O)Cl.CCOC(=O)[O-].O=C([O-])OC(=O)[O-]
CCOC(=O)OC(=O)OCC.[Cl-]
null
null
C(C)O.C1(=CC=CC=C1)C
Protection
OtherReaction
264245ef874940b12fcb3c1294ae29c55a27433c0f41cdd2ebe1e2568c0c7f4e
93477ceed60da179b7bf7e05ad4ca2e1a66efe19a7f7f1f1ff21f2c63be4dd5c
null
O=C(-[Cl;H0;D1;+0:1])-O-[CH2;D2;+0:2]-[C;D1;H3:3].O=C(-[O-])-[O;H0;D2;+0:4]-[C:5]-[C;D1;H3:6].[O-;H0;D1:7]-[C:8](=[O;D1;H0:9])-[#8:10]-[C;H0;D3;+0:11](-[O-])=[O;D1;H0:12]>>[C;D1;H3:6]-[C:5]-[O;H0;D2;+0:4]-[C;H0;D3;+0:11](=[O;D1;H0:12])-[#8:10]-[C:8](=[O;D1;H0:9])-[O;H0;D2;+0:7]-[CH2;D2;+0:2]-[C;D1;H3:3].[Cl-;H0;D0:1]
null
[]
null
null
null
null
The organic pyrocarbonates may be prepared by reacting alkali metal organic carbonate, e.g., sodium ethyl carbonate, with organic halocarbonate, e.g., ethyl chlorocarbonate (ethyl chloroformate). The organo groups of the organic carbonate and halocarbonate are chosen to correspond to the organo groups desired for the p...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Anhydride.Carbonic Acid.Carbonic Acid.Carbonic Acid.Ether.Ether
Anhydride.Carbonic Ester.Carbonic Ester
null
null
null
Other
C(C)O.C1(=CC=CC=C1)C
null
null
CCOC(=O)Cl.CCOC(=O)[O-].O=C([O-])OC(=O)[O-]>C(C)O.C1(=CC=CC=C1)C>CCOC(=O)OC(=O)OCC.[Cl-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-07d855b37c5b4d328abc877c7bed7d1e
CO.N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O>>CN[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O
Cl.CO.[N+](=O)([O-])C1=CC=C(C[C@H](N)C(=O)O)C=C1>>Cl.CN[C@@H](CC1=CC=C(C=C1)[N+](=O)[O-])C(=O)O
O[CH3:1].[NH2:2][C@@H:3]([CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:14](=[O:15])[OH:16]>>[CH3:1][NH:2][C@@H:3]([CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:14](=[O:15])[OH:16]
CO.N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O
CN[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O
null
null
null
Functional Group Addition
Reductive amination with alcohol
7444d9f8c0b92d732b04381dfc7993e519351ad9ccf53db7c2f05a0bbe3a2866
7ff1f86b220c12721f9df74fb282088506a07c38583ba953e1688baf5ed2ad19
c1ccccc1
O-[CH3;D1;+0:1].[C:2]-[C:3](-[NH2;D1;+0:4])-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]>>[C:2]-[C:3](-[NH;D2;+0:4]-[CH3;D1;+0:1])-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]
null
[]
null
null
18
HOUR
Dry methanol (200 ml) was saturated with HCl(g) in a two-necked round bottom flask cooled to -10° C. p-Nitrophenylalanine (10.0 g, 47.6 mmol) was added in one portion and left to stir for about 18 hours, the solution was evaporated to near dryness on a rotary evaporator and the precipitated product collected in a Buchn...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Methanol
Secondary amine
null
null
c1ccccc1
HO-
null
null
18
CO.N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O>>CN[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-777c1fb9b65b4cdf9d3f220923205cdd
CC(=O)CN.CC(C)(C)OC(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O>>CC(=O)CNC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)OC(C)(C)C
C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=C(C=C1)[N+](=O)[O-])C(=O)O.Cl.NCC(C)=O.C(C)N(CC)CC.ON1N=NC2=C1C=CC=C2.C1(CCCCC1)N=C=NC1CCCCC1>>O=C(CNC([C@@H](NC(=O)OC(C)(C)C)CC1=CC=C(C=C1)[N+](=O)[O-])=O)C
[CH3:1][C:2](=[O:3])[CH2:4][NH2:5].O[C:6](=[O:7])[C@H:8]([CH2:9][c:10]1[cH:11][cH:12][c:13]([N+:14](=[O:15])[O-:16])[cH:17][cH:18]1)[NH:19][C:20](=[O:21])[O:22][C:23]([CH3:24])([CH3:25])[CH3:26]>>[CH3:1][C:2](=[O:3])[CH2:4][NH:5][C:6](=[O:7])[C@H:8]([CH2:9][c:10]1[cH:11][cH:12][c:13]([N+:14](=[O:15])[O-:16])[cH:17][cH:...
CC(=O)CN.CC(C)(C)OC(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O
CC(=O)CNC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)OC(C)(C)C
null
null
C(C)(=O)O.C(C)(=O)OCC
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])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[C;D1;H3:13]-[C:14](=[O;D1;H0:15])-[C:16]-[NH2;D1;+0:17]>>[C:4]-[C:3](-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+...
null
[]
0
CELSIUS
18
HOUR
t-Butyloxycarbonyl-p-nitrophenylalanine (4.42 g, 14.26 mmol, aminoacetone hydrochloride (1.56 g, 14.26 mmol), triethylamine (1.44 g, 14.26 mmol), 1-hydroxybenzotriazole (1.69 g, 12.55 mmol), were dissolved in ethyl acetate (400 ml). 1,3-Dicyclohexylcarbodiimide (3.23 g, 15.68 mmol) in ethyl acetate (25 ml) was added an...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
C(C)(=O)O.C(C)(=O)OCC
0
18
CC(=O)CN.CC(C)(C)OC(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)O>C(C)(=O)O.C(C)(=O)OCC>CC(=O)CNC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)OC(C)(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bae6517f0d0c4e2b88dc16d1d8fd4fb6
Nc1cccc(O)c1.O=C(O)c1ccc(O)cc1C(=O)O>>O=C1c2ccc(O)cc2C(=O)N1c1cccc(O)c1
NC=1C=C(C=CC1)O.OC=1C=C(C(C(=O)O)=CC1)C(=O)O>>OC=1C=C(C=CC1)N1C(C=2C(C1=O)=CC(=CC2)O)=O
[NH2:12][c:13]1[cH:14][cH:15][cH:16][c:17]([OH:18])[cH:19]1.O[C:2](=[O:1])[c:3]1[cH:4][cH:5][c:6]([OH:7])[cH:8][c:9]1[C:10](O)=[O:11]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][c:6]([OH:7])[cH:8][c:9]2[C:10](=[O:11])[N:12]1[c:13]1[cH:14][cH:15][cH:16][c:17]([OH:18])[cH:19]1
Nc1cccc(O)c1.O=C(O)c1ccc(O)cc1C(=O)O
O=C1c2ccc(O)cc2C(=O)N1c1cccc(O)c1
null
null
C(C)(=O)O
Acylation
OtherReaction
03989296fe7fd00d3061010c1aadbbfb4b9eaa9ca91856790fffb1e1bf4b4c50
b7eb222f11e89f2ccff57aab9a5106ae4173f0ba94ac518e1a9f3b22a378531d
O=C1c2ccccc2C(=O)N1c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5](-[C;H0;D3;+0:6](-O)=[O;D1;H0:7]):[c:8].[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[N;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:5](:[c:8]):[c:3]-1:[c:4]
80.5
[{"value": 80.5, "product": "OC=1C=C(C=CC1)N1C(C=2C(C1=O)=CC(=CC2)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
m-Aminophenol(13.23 g, 0.12 mol) and 4-hydroxyphthalic acid (16.98 g, 0.09 mol) are allowed to react in refluxing acetic acid as described above. The product (21.6 g, 91%), collected as a tan solid, is recrystallized from methanol to give 18.5 g of pale yellow powder [mp 270° C. differential scanning calorimetry] havin...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine
Substituted dicarboximide
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccccc1
HO-
C(C)(=O)O
null
null
Nc1cccc(O)c1.O=C(O)c1ccc(O)cc1C(=O)O>C(C)(=O)O>O=C1c2ccc(O)cc2C(=O)N1c1cccc(O)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1a0b05586da349f5b4252b3b31d4054d
BrCCCCCCCCCCBr.CCO.Oc1ccccc1N=Nc1ccccc1>>CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1
C(C)O.OC1=C(C=CC=C1)N=NC1=CC=CC=C1.BrCCCCCCCCCCBr.[OH-].[K+]>>BrCCCCCCCCCCOC1=CC=C(C=C1)N=NC1=CC=C(C=C1)CCCCCCCCCCCC
Br[CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][Br:34].O[CH2:2][CH3:1].[cH:13]1[cH:14][cH:15][c:16]([N:17]=[N:18][c:21]2[cH:20][cH:19][cH:36][cH:35][c:22]2[OH:23])[cH:37][cH:38]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:...
BrCCCCCCCCCCBr.CCO.Oc1ccccc1N=Nc1ccccc1
CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4b7ce20b118ba61230629b6c5ff630b0850500e59c3985d9d902320e7f981a37
a753faf74946b378a8f59b3e8d5ca05921b3f037160f49ab6eef7d3286a7016e
c1ccc(N=Nc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].O-[CH2;D2;+0:4]-[C;D1;H3:5].[OH;D1;+0:6]-[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:[c:11]:[c;H0;D3;+0:12]:1-[N;H0;D2;+0:13]=[#7:14]-[c:15]1:[c:16]:[c:17]:[cH;D2;+0:18]:[c:19]:[c:20]:1>>[C:21]-[C:22]-[CH2;D2;+0:4]-[C;D1;H3:5].[C:23]-[C:24]-[c;H0;D3;+0:18]1:[c:17]:[c:16]:[c:15](-[#7:14]=[N;H0;D2;+0:13...
null
[]
null
null
null
null
A 3000 ml three-necked round bottom flask was equipped with magnetic stirring, a heating mantle, a reflux condenser, and a nitrogen atmosphere. The flask was charged with 4-dodecyl-4,-hydroxyazobenzene (60.0 g, 0.164 mol), 1,10-dibromodecane, (66.95 g, 0.223 mol), potassium hydroxide (9.75 g, 0.174 mol), and ethanol (1...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Diazene.Primary alcohol.Aromatic alcohol
Ether.Diazene
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Br-
null
null
null
BrCCCCCCCCCCBr.CCO.Oc1ccccc1N=Nc1ccccc1>>CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-45d6e0e571fe4728804424dcef92127c
BrCCCCCCCCCCBr.CCCCCCCCCCCCc1ccc(N=Nc2ccc(O)cc2)cc1>>CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1
C(CCCCCCCCCCC)C1=CC=C(C=C1)N=NC1=CC=C(C=C1)O.BrCCCCCCCCCCBr.[OH-].[K+]>>BrCCCCCCCCCCOC1=CC=C(C=C1)N=NC1=CC=C(C=C1)CCCCCCCCCCCC
Br[CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][Br:34].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][c:16]([N:17]=[N:18][c:19]2[cH:20][cH:21][c:22]([OH:23])[cH:35][cH:36]2)[cH:37][cH:38]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:...
BrCCCCCCCCCCBr.CCCCCCCCCCCCc1ccc(N=Nc2ccc(O)cc2)cc1
CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(N=Nc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
A 3000 ml three-necked round bottom flask was equipped with magnetic stirring, a heating mantle, a reflux condenser, and a nitrogen atmosphere. The flask was charged with 4-dodecyl-4'-hydroxyazobenzene (60.0 g, 0.164 mol), 1,10-dibromodecane, (66.95 g, 0.223 mol), potassium hydroxide (9.75 g, 0.174 mol), and ethanol (1...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HBr
C(C)O
null
null
BrCCCCCCCCCCBr.CCCCCCCCCCCCc1ccc(N=Nc2ccc(O)cc2)cc1>C(C)O>CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1d8e39248edc4f098a636d77133a05dd
CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1.CN(C)CCO>>CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCC[N+](C)(C)CCO)cc2)cc1.[Br-]
BrCCCCCCCCCCOC1=CC=C(C=C1)N=NC1=CC=C(C=C1)CCCCCCCCCCCC.CN(CCO)C.O1CCCC1>>[Br-].C(CCCCCCCCCCC)C1=CC=C(C=C1)N=NC1=CC=C(OCCCCCCCCCC[N+](C)(C)CCO)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][c:16]([N:17]=[N:18][c:19]2[cH:20][cH:21][c:22]([O:23][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][Br:44])[cH:40][cH:41]2)[cH:42][cH:43]1.[N:34]([CH3:35])([CH3:36])[CH2:37][CH2...
CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1.CN(C)CCO
CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCC[N+](C)(C)CCO)cc2)cc1.[Br-]
null
null
CO
Functional Group Interconversion
OtherReaction
cf95568d208ea67162a1e8aa2ffc7c679479f5b8aaab2573599ff5258836e869
3d861fb9efedfc352e8049eef974a995ad6d89e50a2cf826c8f45bd07b1b8172
c1ccc(N=Nc2ccccc2)cc1
[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[C:3]-[C:4].[C:5]-[C:6]-[N;H0;D3;+0:7](-[C;D1;H3:8])-[C;D1;H3:9]>>[Br-;H0;D0:1].[C:4]-[C:3]-[CH2;D2;+0:2]-[N+;H0;D4:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[C:6]-[C:5]
null
[]
null
null
24
HOUR
A 3000 ml three-necked round bottom flask was equipped with magnetic stirring, a heating mantle, a reflux condenser, and a nitrogen atmosphere. The flask was charged with 4-(10-bromodecyloxy)-4'-dodecylazobenzene (40 g, 0.068 mol), dimethylethanolamine (95.2 g, 1.068 mole) and 1050 ml of tetrahydrofuran. The reaction m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Tertiary amine
null
null
null
c1ccccc1.c1ccccc1
null
CO
null
24
CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCCBr)cc2)cc1.CN(C)CCO>CO>CCCCCCCCCCCCc1ccc(N=Nc2ccc(OCCCCCCCCCC[N+](C)(C)CCO)cc2)cc1.[Br-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5d63c7e02326475d8934d8f39b40ad49
Nc1nc(N)nc(N)n1>>Nc1nc(N)nc(N)n1
N1=C(N)N=C(N)N=C1N.C=O>>C=O.N1=C(N)N=C(N)N=C1N
[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1>>[NH2:3][c:4]1[n:5][c:6]([NH2:7])[n:8][c:9]([NH2:10])[n:11]1
Nc1nc(N)nc(N)n1
Nc1nc(N)nc(N)n1
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ncncn1
null
null
[]
60
CELSIUS
30
MINUTE
Independently, to 31.5 g of melamine were added 52.2 g of 37% aqueous solution of formaldehyde and 170.3 g of distilled water, and the resulting mixture was stirred at 60° C. for 30 minutes to obtain a transparent melamine-formaldehyde precondensate. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ncncn1
null
O
60
0.5
Nc1nc(N)nc(N)n1>O>Nc1nc(N)nc(N)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8640071052634bebb681ae075425f7b2
CC(C)c1cccc(C(C)C)c1NC(=N)Nc1c(C(C)C)cccc1C(C)C.Cc1cccc(C(Cl)Cl)c1>>CC(C)c1cccc(C(C)C)c1NC(=NCc1cccc(CCl)c1)Nc1c(C(C)C)cccc1C(C)C
C(C)(C)C1=C(C(=CC=C1)C(C)C)NC(=N)NC1=C(C=CC=C1C(C)C)C(C)C.ClC(C1=CC(=CC=C1)C)Cl.C([O-])([O-])=O.[K+].[K+]>>C(C)(C)C1=C(C(=CC=C1)C(C)C)NC(=NCC1=CC(=CC=C1)CCl)NC1=C(C=CC=C1C(C)C)C(C)C
[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][c:8]([CH:9]([CH3:10])[CH3:11])[c:12]1[NH:13][C:14](=[NH:15])[NH:25][c:26]1[c:27]([CH:28]([CH3:29])[CH3:30])[cH:31][cH:32][cH:33][c:34]1[CH:35]([CH3:36])[CH3:37].Cl[CH:16]([c:17]1[cH:18][cH:19][cH:20][c:21]([CH3:22])[cH:24]1)[Cl:23]>>[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6]...
CC(C)c1cccc(C(C)C)c1NC(=N)Nc1c(C(C)C)cccc1C(C)C.Cc1cccc(C(Cl)Cl)c1
CC(C)c1cccc(C(C)C)c1NC(=NCc1cccc(CCl)c1)Nc1c(C(C)C)cccc1C(C)C
null
null
C=1(C(=CC=CC1)C)C
Functional Group Interconversion
OtherReaction
77c4006b61feafdadb38a3464a8de1ee490b61d0da0c13bca01b4c6c32c9e17b
6057d7fb75624930c9e41a46967dce14902ce53987bcfcd5587c4c1a79bea4df
c1ccc(CN=C(Nc2ccccc2)Nc2ccccc2)cc1
Cl-[CH;D3;+0:1](-[Cl;H0;D1;+0:2])-[c:3](:[c:4]):[c:5]:[c:6](-[CH3;D1;+0:7]):[c:8].[#7:9]-[C:10](-[#7:11])=[NH;D1;+0:12]>>[#7:9]-[C:10](-[#7:11])=[N;H0;D2;+0:12]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]:[c:6](-[CH2;D2;+0:7]-[Cl;H0;D1;+0:2]):[c:8]
32.8
[{"value": 32.8, "product": "C(C)(C)C1=C(C(=CC=C1)C(C)C)NC(=NCC1=CC(=CC=C1)CCl)NC1=C(C=CC=C1C(C)C)C(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
11.4 g (0.03 mole) of N,N'-bis-(2,6-diisopropylphenyl) guanidine, 5.7 g (0.033 mole) of α,α-dichloro-m-xylene and 2.1 g (0.015 mole) of anhydrous potassium carbonate were added to 50 ml of xylene. The thus-formed mixture was then refluxed under heating for 10 hours. After the mixture had been allowed to cool, the insol...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide
Primary halide
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HCl
C=1(C(=CC=CC1)C)C
null
null
CC(C)c1cccc(C(C)C)c1NC(=N)Nc1c(C(C)C)cccc1C(C)C.Cc1cccc(C(Cl)Cl)c1>C=1(C(=CC=CC1)C)C>CC(C)c1cccc(C(C)C)c1NC(=NCc1cccc(CCl)c1)Nc1c(C(C)C)cccc1C(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-da0c1141ff4a4a2e80f2daaa6a47cc27
CC(C)c1cccc(C(C)C)c1NC(=N)Nc1c(C(C)C)cccc1C(C)C.Cc1ccc(C(Br)Br)cc1>>CC(C)c1cccc(C(C)C)c1NC(=NCc1ccc(CBr)cc1)Nc1c(C(C)C)cccc1C(C)C
C(C)(C)C1=C(C(=CC=C1)C(C)C)NC(=N)NC1=C(C=CC=C1C(C)C)C(C)C.BrC(C1=CC=C(C=C1)C)Br.C([O-])([O-])=O.[K+].[K+]>>C(C)(C)C1=C(C(=CC=C1)C(C)C)NC(=NCC1=CC=C(C=C1)CBr)NC1=C(C=CC=C1C(C)C)C(C)C
[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][c:8]([CH:9]([CH3:10])[CH3:11])[c:12]1[NH:13][C:14](=[NH:15])[NH:25][c:26]1[c:27]([CH:28]([CH3:29])[CH3:30])[cH:31][cH:32][cH:33][c:34]1[CH:35]([CH3:36])[CH3:37].Br[CH:16]([c:17]1[cH:18][cH:19][c:20]([CH3:21])[cH:23][cH:24]1)[Br:22]>>[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6]...
CC(C)c1cccc(C(C)C)c1NC(=N)Nc1c(C(C)C)cccc1C(C)C.Cc1ccc(C(Br)Br)cc1
CC(C)c1cccc(C(C)C)c1NC(=NCc1ccc(CBr)cc1)Nc1c(C(C)C)cccc1C(C)C
null
null
C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
77c4006b61feafdadb38a3464a8de1ee490b61d0da0c13bca01b4c6c32c9e17b
6057d7fb75624930c9e41a46967dce14902ce53987bcfcd5587c4c1a79bea4df
c1ccc(CN=C(Nc2ccccc2)Nc2ccccc2)cc1
Br-[CH;D3;+0:1](-[Br;H0;D1;+0:2])-[c:3]1:[c:4]:[c:5]:[c:6](-[CH3;D1;+0:7]):[c:8]:[c:9]:1.[#7:10]-[C:11](-[#7:12])=[NH;D1;+0:13]>>[#7:10]-[C:11](-[#7:12])=[N;H0;D2;+0:13]-[CH2;D2;+0:1]-[c:3]1:[c:4]:[c:5]:[c:6](-[CH2;D2;+0:7]-[Br;H0;D1;+0:2]):[c:8]:[c:9]:1
39.1
[{"value": 39.1, "product": "C(C)(C)C1=C(C(=CC=C1)C(C)C)NC(=NCC1=CC=C(C=C1)CBr)NC1=C(C=CC=C1C(C)C)C(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
11.4 g (0.03 mole) of N,N'-bis-(2,6-diisopropylphenyl) guanidine, 8.7 g (0.03 mole) of α,α-dibromo-p-xylene and 2.1 g (0.015 mole) of anhydrous potassium carbonate were added to 50 ml of toluene. The thus-formed mixture was then refluxed under heating for 10 hours. After the mixture had been allowed to cool, the insolu...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide
Primary halide
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HBr
C1(=CC=CC=C1)C
null
null
CC(C)c1cccc(C(C)C)c1NC(=N)Nc1c(C(C)C)cccc1C(C)C.Cc1ccc(C(Br)Br)cc1>C1(=CC=CC=C1)C>CC(C)c1cccc(C(C)C)c1NC(=NCc1ccc(CBr)cc1)Nc1c(C(C)C)cccc1C(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6fb2d39ee99944cc9f9143eb8ab5677c
CCc1cccc(CC)c1NC(=N)Nc1c(CC)cccc1CC.Cc1cccc(C(Cl)Cl)c1>>CCc1cccc(CC)c1NC(=NCc1cccc(CCl)c1)Nc1c(CC)cccc1CC
C(C)C1=C(C(=CC=C1)CC)NC(=N)NC1=C(C=CC=C1CC)CC.ClC(C1=CC(=CC=C1)C)Cl.C([O-])([O-])=O.[K+].[K+]>>C(C)C1=C(C(=CC=C1)CC)NC(=NCC1=CC(=CC=C1)CCl)NC1=C(C=CC=C1CC)CC
[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][CH3:9])[c:10]1[NH:11][C:12](=[NH:13])[NH:23][c:24]1[c:25]([CH2:26][CH3:27])[cH:28][cH:29][cH:30][c:31]1[CH2:32][CH3:33].Cl[CH:14]([c:15]1[cH:16][cH:17][cH:18][c:19]([CH3:20])[cH:22]1)[Cl:21]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][CH3:9])[c:10]1[NH:11][C:...
CCc1cccc(CC)c1NC(=N)Nc1c(CC)cccc1CC.Cc1cccc(C(Cl)Cl)c1
CCc1cccc(CC)c1NC(=NCc1cccc(CCl)c1)Nc1c(CC)cccc1CC
null
null
C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
77c4006b61feafdadb38a3464a8de1ee490b61d0da0c13bca01b4c6c32c9e17b
6057d7fb75624930c9e41a46967dce14902ce53987bcfcd5587c4c1a79bea4df
c1ccc(CN=C(Nc2ccccc2)Nc2ccccc2)cc1
Cl-[CH;D3;+0:1](-[Cl;H0;D1;+0:2])-[c:3](:[c:4]):[c:5]:[c:6](-[CH3;D1;+0:7]):[c:8].[#7:9]-[C:10](-[#7:11])=[NH;D1;+0:12]>>[#7:9]-[C:10](-[#7:11])=[N;H0;D2;+0:12]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]:[c:6](-[CH2;D2;+0:7]-[Cl;H0;D1;+0:2]):[c:8]
32.5
[{"value": 32.5, "product": "C(C)C1=C(C(=CC=C1)CC)NC(=NCC1=CC(=CC=C1)CCl)NC1=C(C=CC=C1CC)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
9.7 g (0.03 mole) of N,N'-bis-(2,6-diethylphenyl) guanidine, 5.7 g (0.033 mole) of α,α-dichloro-m-xylene and 2.1 g (0.015 mole) of anhydrous potassium carbonate were added to 50 ml of toluene. The thus-formed mixture was then refluxed under heating for 10 hours. After the mixture had been allowed to cool, the insoluble...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide
Primary halide
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HCl
C1(=CC=CC=C1)C
null
null
CCc1cccc(CC)c1NC(=N)Nc1c(CC)cccc1CC.Cc1cccc(C(Cl)Cl)c1>C1(=CC=CC=C1)C>CCc1cccc(CC)c1NC(=NCc1cccc(CCl)c1)Nc1c(CC)cccc1CC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6b289f54e6794a3998880c4a3d4f3dbc
Cc1ccc(C(Cl)Cl)cc1.N=C(Nc1ccccc1-c1ccccc1)Nc1ccccc1-c1ccccc1>>ClCc1ccc(CN=C(Nc2ccccc2-c2ccccc2)Nc2ccccc2-c2ccccc2)cc1
C1(=CC=CC=C1)C1=C(C=CC=C1)NC(=N)NC1=C(C=CC=C1)C1=CC=CC=C1.ClC(C1=CC=C(C=C1)C)Cl.C([O-])([O-])=O.[K+].[K+]>>C1(=CC=CC=C1)C1=C(C=CC=C1)NC(=NCC1=CC=C(C=C1)CCl)NC1=C(C=CC=C1)C1=CC=CC=C1
Cl[CH:2]([Cl:1])[c:3]1[cH:4][cH:5][c:6]([CH3:7])[cH:36][cH:37]1.[NH:8]=[C:9]([NH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1-[c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1)[NH:23][c:24]1[cH:25][cH:26][cH:27][cH:28][c:29]1-[c:30]1[cH:31][cH:32][cH:33][cH:34][cH:35]1>>[Cl:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][N:8]=[C:9...
Cc1ccc(C(Cl)Cl)cc1.N=C(Nc1ccccc1-c1ccccc1)Nc1ccccc1-c1ccccc1
ClCc1ccc(CN=C(Nc2ccccc2-c2ccccc2)Nc2ccccc2-c2ccccc2)cc1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
3ced70ac43dd5799bc4b89314ebb5482ef8918317df37c036f8f155a8aca8aa0
498fc9fa63817756d78172f2f80442d316dac1e36623b01cda3447ffb87955c4
c1ccc(CN=C(Nc2ccccc2-c2ccccc2)Nc2ccccc2-c2ccccc2)cc1
Cl-[CH;D3;+0:1](-[Cl;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[c:6](-[CH3;D1;+0:7]):[c:8]:[c:9]:1.[#7:10]-[C:11](-[#7:12])=[NH;D1;+0:13]>>[#7:10]-[C:11](-[#7:12])=[N;H0;D2;+0:13]-[CH2;D2;+0:7]-[c:6]1:[c:5]:[c:4]:[c:3](-[CH2;D2;+0:1]-[Cl;D1;H0:2]):[c:9]:[c:8]:1
20.6
[{"value": 20.6, "product": "C1(=CC=CC=C1)C1=C(C=CC=C1)NC(=NCC1=CC=C(C=C1)CCl)NC1=C(C=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
10.9 g (0.03 mole) of N,N'-bis-(2-phenylphenyl) guanidine, 5.7 g (0.033 mole) of α,α-dichloro-p-xylene and 2.1 g (0.015 mole) of anhydrous potassium carbonate were added to 50 ml of toluene. The thus-formed mixture was then refluxed under heating for 10 hours. After the mixture had been allowed to cool, the insoluble s...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide
Primary halide
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HCl
C1(=CC=CC=C1)C
null
null
Cc1ccc(C(Cl)Cl)cc1.N=C(Nc1ccccc1-c1ccccc1)Nc1ccccc1-c1ccccc1>C1(=CC=CC=C1)C>ClCc1ccc(CN=C(Nc2ccccc2-c2ccccc2)Nc2ccccc2-c2ccccc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f252bc5bba1b49918808b53ec81978dd
O=c1ccn(C2OC(COP(=O)(O)OC3C(CO)OC(n4ccc(=O)[nH]c4=O)C3O)C(O)C2O)c(=O)[nH]1>>O=c1[nH]c(=O)c2[nH]c(=O)[nH]c2[nH]1
CC1=C(C(=O)N(N1C)C=2C=CC=CC2)N.C1=CN(C(=O)NC1=O)C2C(C(C(O2)COP(=O)(O)OC3C(OC(C3O)N4C=CC(=O)NC4=O)CO)O)O.N>>N1C(=O)NC=2NC(=O)NC2C1=O
O=c1cc[n:7](C2OC(COP(=O)(O)OC3C(CO)OC([n:12]4[c:2](=[O:1])[nH:3][c:4](=[O:5])[cH:6][cH:11]4)C3O)C(O)C2O)[c:8](=[O:9])[nH:10]1>>[O:1]=[c:2]1[nH:3][c:4](=[O:5])[c:6]2[nH:7][c:8](=[O:9])[nH:10][c:11]2[nH:12]1
O=c1ccn(C2OC(COP(=O)(O)OC3C(CO)OC(n4ccc(=O)[nH]c4=O)C3O)C(O)C2O)c(=O)[nH]1
O=c1[nH]c(=O)c2[nH]c(=O)[nH]c2[nH]1
null
null
P(=O)([O-])([O-])[O-]
Functional Group Interconversion
OtherReaction
85ffbf903c3a7a465c7bbb22aef288016ddcce6c379e1317c2e84434d04b76b9
6ffcbc09efa9f7952582a4dec70b5e9a5b2c89d9b165136680d1e196c76fddc4
O=c1[nH]c(=O)c2[nH]c(=O)[nH]c2[nH]1
O-C-C1-O-C(-[n;H0;D3;+0:1]2:[cH;D2;+0:2]:[cH;D2;+0:3]:[c:4](=[O;D1;H0:5]):[#7;a:6]:[c:7]:2=[O;D1;H0:8])-C(-O)-C-1-O-P(-O)(=O)-O-C-C1-O-C(-[n;H0;D3;+0:9]2:c:c:c(=O):[nH;D2;+0:10]:[c:11]:2=[O;D1;H0:12])-C(-O)-C-1-O>>[O;D1;H0:8]=[c:7]1:[#7;a:6]:[c:4](=[O;D1;H0:5]):[c;H0;D3;+0:3]2:[nH;D2;+0:9]:[c:11](=[O;D1;H0:12]):[nH;D2;...
null
[]
37
CELSIUS
null
null
To each of the mixtures was added a reagent prepared by dissolving 1 μmol 4-aminoantipyrine and 2 units of uricase in 1.5 ml of 0.1M phosphate buffer (pH 6.5). After the resulting mixtures were maintained in a thermostat at 37° C. for about 5 minutes, the absorbance was measured at a wavelength of 555 nm with a spectro...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
null
c1ncccn1.C1CCOC1.C1CCOC1.c1ccncn1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HO-
P(=O)([O-])([O-])[O-]
37
null
O=c1ccn(C2OC(COP(=O)(O)OC3C(CO)OC(n4ccc(=O)[nH]c4=O)C3O)C(O)C2O)c(=O)[nH]1>P(=O)([O-])([O-])[O-]>O=c1[nH]c(=O)c2[nH]c(=O)[nH]c2[nH]1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-de9085482ee942acb56e459381852f84
O=S(=O)(O)O.[Ga]>>O.O=S(=O)([O-])[O-].O=S(=O)([O-])[O-].O=S(=O)([O-])[O-].[Ga+3].[Ga+3]
[Ga].OS(=O)(=O)O>>O.S(=O)(=O)([O-])[O-].[Ga+3].S(=O)(=O)([O-])[O-].S(=O)(=O)([O-])[O-].[Ga+3]
[OH:1][S:3](=[O:2])(=[O:4])[OH:11].[Ga:17]>>[OH2:1].[O:2]=[S:3](=[O:4])([O-:5])[O-:6].[O:7]=[S:8](=[O:9])([O-:10])[O-:11].[O:12]=[S:13](=[O:14])([O-:15])[O-:16].[Ga+3:17].[Ga+3:18]
O=S(=O)(O)O.[Ga]
O.O=S(=O)([O-])[O-].O=S(=O)([O-])[O-].O=S(=O)([O-])[O-].[Ga+3].[Ga+3]
null
null
C(C)O.O
Functional Group Interconversion
OtherReaction
42af6cdfb86a130c92365e01a31b50705eea7bdf12f67dc370bf24402f7ceedc
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
null
[Ga;H0;D0;+0:1].[O;D1;H0:2]=[S;H0;D4;+0:3](=[O;D1;H0:4])(-[OH;D1;+0:5])-[OH;D1;+0:6]>>[Ga+3;H0;D0:1].[O-;H0;D1:5]-[#16:7](-[O;-;D1;H0:8])(=[O;D1;H0:9])=[O;D1;H0:10].[O;-;D1;H0:11]-[S;H0;D4;+0:3](-[O;-;D1;H0:12])(=[O;D1;H0:2])=[O;D1;H0:4].[OH2;D0;+0:6]
null
[]
null
null
null
null
4.1 g of gallium sulphate hydrate (the H2O/Ga2 (SO4)3 molar ratio is close to 25) are dissolved in 3.7 g of distilled water. The sulphate is obtained by dissolving gallium (Grade 1 from Johnson Matthey) in hot concentrated H2SO4, in excess, taking up the suspension obtained in ethanol at a concentration of 60% in water...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
C(C)O.O
null
null
O=S(=O)(O)O.[Ga]>C(C)O.O>O.O=S(=O)([O-])[O-].O=S(=O)([O-])[O-].O=S(=O)([O-])[O-].[Ga+3].[Ga+3]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6c9c4dc14ecb42679eca1006ffa0ee05
[Al+3].[Mg+2]>>[Al+3].[Mg+2]
P(=O)([O-])([O-])[O-].[NH4+].[NH4+].[NH4+].[N+](=O)([O-])[O-].[Al+3].[N+](=O)([O-])[O-].[N+](=O)([O-])[O-].[Cl-].[Mg+2].[Cl-].[OH-].[NH4+].Cl[Ti](Cl)(Cl)Cl.Cl[Ti](Cl)(Cl)Cl>>P(=O)([O-])([O-])[O-].[Mg+2].[Al+3].Cl[Ti](Cl)(Cl)Cl
[Al+3:6].[Mg+2:12]>>[Al+3:6].[Mg+2:12]
[Al+3].[Mg+2]
[Al+3].[Mg+2]
null
null
CCCCCCC
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
A series of catalysts comprising TiCl4 and a particulate cogelled xerogel of aluminum-magnesium phosphate was prepared at a pH of about 6-10 by combining aqueous solutions of aluminum nitrate, magnesium chloride, monobasic ammonium phosphate and ammonium hydroxide. Generally, each catalyst was made by slurrying the gel...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
CCCCCCC
null
null
[Al+3].[Mg+2]>CCCCCCC>[Al+3].[Mg+2]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e4e95021117a431db55e0845d2ecf3fd
Cc1ccccc1S(=O)(=O)N=C=O.Nc1ccccc1>>Cc1ccc(S(=O)(=O)NC(=O)Nc2ccccc2)cc1
NC1=CC=CC=C1.NC1=CC=CC=C1.C1(=CC=CC=C1)C.C=1(C(=CC=CC1)S(=O)(=O)N=C=O)C>>C1(=CC=C(C=C1)S(=O)(=O)NC(=O)NC1=CC=CC=C1)C
[CH3:1][c:2]1[c:5]([S:6](=[O:7])(=[O:8])[N:9]=[C:10]=[O:11])[cH:4][cH:3][cH:19][cH:20]1.[NH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([S:6](=[O:7])(=[O:8])[NH:9][C:10](=[O:11])[NH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][cH:20]1
Cc1ccccc1S(=O)(=O)N=C=O.Nc1ccccc1
Cc1ccc(S(=O)(=O)NC(=O)Nc2ccccc2)cc1
null
null
null
Acylation
OtherReaction
8dc8740a6cf6305b28543404dca4a41e9db54610b035fd636d4198fbeab524f4
24cba6b128cf13377717dc3857354238fb483e0cd1cd012e69813867b2abb802
O=C(Nc1ccccc1)NS(=O)(=O)c1ccccc1
[C;D1;H3:1]-[c;H0;D3;+0:2]1:[c:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c:6]:[c;H0;D3;+0:7]:1-[#16:8](=[O;D1;H0:9])(=[O;D1;H0:10])-[N;H0;D2;+0:11]=[C;H0;D2;+0:12]=[O;D1;H0:13].[NH2;D1;+0:14]-[c:15](:[c:16]):[c:17]>>[C;D1;H3:1]-[c;H0;D3;+0:2]1:[c:3]:[cH;D2;+0:4]:[c;H0;D3;+0:7](-[#16:8](=[O;D1;H0:9])(=[O;D1;H0:10])-[NH;D2;+0:11]-[C...
null
[]
90
CELSIUS
null
null
A three-necked flask equipped with a dropping funnel, a thermometer, and a reflux condenser was charged with 18.6 g of aniline and the aniline was dissolved in 200 ml of toluene. While the resultant reaction solution was stirred with a magnetic stirrer, 42.0 g of toluenesulfonylisocyanate were added dropwise from the d...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Tosylate.Urea
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
null
null
90
null
Cc1ccccc1S(=O)(=O)N=C=O.Nc1ccccc1>>Cc1ccc(S(=O)(=O)NC(=O)Nc2ccccc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-07d878beecdd42a5b96e75782c8b11ad
COC(=O)CBr.COc1ccc2c(c1)C(N)CCC2>>COC(=O)CNC1CCCc2ccc(OC)cc21
NC1CCCC2=CC=C(C=C12)OC.COC(CBr)=O>>COC(CNC1CCCC2=CC=C(C=C12)OC)=O
Br[CH2:5][C:3]([O:2][CH3:1])=[O:4].[NH2:6][CH:7]1[CH2:8][CH2:9][CH2:10][c:11]2[cH:12][cH:13][c:14]([O:15][CH3:16])[cH:17][c:18]21>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][CH:7]1[CH2:8][CH2:9][CH2:10][c:11]2[cH:12][cH:13][c:14]([O:15][CH3:16])[cH:17][c:18]21
COC(=O)CBr.COc1ccc2c(c1)C(N)CCC2
COC(=O)CNC1CCCc2ccc(OC)cc21
null
null
C(C)OCC
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
308780347cfd56717124ea78bf2bc5de380db774d7ce948246e279dfd7d8998b
d2327a8d30a39f085182e5e2f77f5b022ac99c077866b86103acfec639a8f73d
c1ccc2c(c1)CCCC2
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].[C:6]-[C:7](-[NH2;D1;+0:8])-[c:9]>>[C:6]-[C:7](-[NH;D2;+0:8]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5])-[c:9]
null
[]
null
null
70
HOUR
367.0 g of 1-amino-7-methoxy-1,2,3,4-tetrahydronaphthalene are solved in 1500 ml of diethyl ether. To this solution is dropwise added a solution of 158.3 g of bromoacetic acid methyl ester in 450 ml of diethyl ether. The mixture is stirred at room temperature for 70 hours. The precipitate is separated and the solution ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Primary amine
Ester.Secondary amine
null
null
c1ccc2c(c1)CCCC2
HBr
C(C)OCC
null
70
COC(=O)CBr.COc1ccc2c(c1)C(N)CCC2>C(C)OCC>COC(=O)CNC1CCCc2ccc(OC)cc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d331a1f9455242ecbaaee3d7cbdb816e
CC(=O)OC(C)=O.COC(=O)CNC1CCCc2ccc(OC)cc21>>COC(=O)CN(C=O)C1CCCc2ccc(OC)cc21
COC(CNC1CCCC2=CC=C(C=C12)OC)=O.C(C)(=O)OC(C)=O>>COC(CN(C1CCCC2=CC=C(C=C12)OC)C=O)=O
CC(=O)O[C:7](C)=[O:8].[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][CH:9]1[CH2:10][CH2:11][CH2:12][c:13]2[cH:14][cH:15][c:16]([O:17][CH3:18])[cH:19][c:20]21>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][N:6]([CH:7]=[O:8])[CH:9]1[CH2:10][CH2:11][CH2:12][c:13]2[cH:14][cH:15][c:16]([O:17][CH3:18])[cH:19][c:20]21
CC(=O)OC(C)=O.COC(=O)CNC1CCCc2ccc(OC)cc21
COC(=O)CN(C=O)C1CCCc2ccc(OC)cc21
null
null
C(=O)O
Acylation
OtherReaction
72a6d1966b6b15ac7195d4682af251dc9ffac857f784a4242970ab5c7a529369
6593c6062585994f02076cd3c86920ae7244b86659eab65c21b5a8628c6d4bb8
c1ccc2c(c1)CCCC2
C-C(=O)-O-[C;H0;D3;+0:1](-C)=[O;D1;H0:2].[C:3]-[C:4](-[NH;D2;+0:5]-[C:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10])-[c:11]>>[C:3]-[C:4](-[N;H0;D3;+0:5](-[C:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10])-[CH;D2;+0:1]=[O;D1;H0:2])-[c:11]
101.1
[{"value": 97.0, "product": "COC(CN(C1CCCC2=CC=C(C=C12)OC)C=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 101.1, "product": "COC(CN(C1CCCC2=CC=C(C=C12)OC)C=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
70
HOUR
2.40 g of N-(7-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)glycine methyl ester are added dropwise with cooling to 5° C. to 5.52 g of formic acid. Additionally 1.79 g of acetic anhydride are added, and the mixture is kept at room temperature for 70 hours. Destillation under vacuum affords 2.7 g (97% of theory) of N-formy...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amine
Tertiary amide
null
null
c1ccc2c(c1)CCCC2
HO-
C(=O)O
null
70
CC(=O)OC(C)=O.COC(=O)CNC1CCCc2ccc(OC)cc21>C(=O)O>COC(=O)CN(C=O)C1CCCc2ccc(OC)cc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7700c29acc3b4bd1902fd09ff1183544
COC(=O)C(C=O)N(C=O)C1CCCc2ccccc21.[NH4+]>>COC(=O)c1cncn1C1CCCc2ccccc21
C([O-])([O-])=O.[NH4+].[NH4+].COC(C(N(C1CCCC2=CC=CC=C12)C=O)C=O)=O>>COC(=O)C1=CN=CN1C1CCCC2=CC=CC=C12
O=[CH:6][CH:5]([C:3]([O:2][CH3:1])=[O:4])[N:9]([CH:8]=O)[CH:10]1[CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21.[NH4+:7]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21
COC(=O)C(C=O)N(C=O)C1CCCc2ccccc21.[NH4+]
COC(=O)c1cncn1C1CCCc2ccccc21
null
null
C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
OtherReaction
1a481ad88f8384c14db36618e609a6265b383027caf03124ea737d7c71ca43d1
33a99fda60914bd5ae296afe9e7947aa8e075ab24e2116a7c1687ab31c7abbeb
c1ccc2c(c1)CCCC2n1ccnc1
O=[CH;D2;+0:1]-[CH;D3;+0:2](-[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6])-[N;H0;D3;+0:7](-[CH;D2;+0:8]=O)-[C:9](-[C:10])-[c:11].[NH4+;D0:12]>>[C:10]-[C:9](-[n;H0;D3;+0:7]1:[cH;D2;+0:8]:[n;H0;D2;+0:12]:[cH;D2;+0:1]:[c;H0;D3;+0:2]:1-[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6])-[c:11]
null
[]
70
CELSIUS
null
null
33.0 g of ammonium carbonate are added at room temperature to a solution of 15.5 g of N,α-bis-formyl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)glycine methyl ester in 300 ml of xylene. The mixture is heated to 70° C. for 1 hour then the temperature is raised to 120° C. for 3 hours. After concentration the 1-(1,2,3,4-tetrahy...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Tertiary amide
Ester
null
c1c[nH]cn1
c1c[nH]cn1.c1ccc2c(c1)CCCC2
HO-
C=1(C(=CC=CC1)C)C
70
null
COC(=O)C(C=O)N(C=O)C1CCCc2ccccc21.[NH4+]>C=1(C(=CC=CC1)C)C>COC(=O)c1cncn1C1CCCc2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f57d7a6d780c4a4a823cce69c82616b4
COC(=O)C(C=O)N(C=O)C1CCCc2ccccc21.[NH4+]>>COC(=O)c1cncn1C1CCCc2ccccc21
C(C)(=O)[O-].[NH4+].COC(C(N(C1CCCC2=CC=CC=C12)C=O)C=O)=O.C(C)(=O)[O-].[NH4+].C(C)(=O)O>>COC(=O)C1=CN=CN1C1CCCC2=CC=CC=C12
O=[CH:6][CH:5]([C:3]([O:2][CH3:1])=[O:4])[N:9]([CH:8]=O)[CH:10]1[CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21.[NH4+:7]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21
COC(=O)C(C=O)N(C=O)C1CCCc2ccccc21.[NH4+]
COC(=O)c1cncn1C1CCCc2ccccc21
null
null
O
Aromatic Heterocycle Formation
OtherReaction
1a481ad88f8384c14db36618e609a6265b383027caf03124ea737d7c71ca43d1
33a99fda60914bd5ae296afe9e7947aa8e075ab24e2116a7c1687ab31c7abbeb
c1ccc2c(c1)CCCC2n1ccnc1
O=[CH;D2;+0:1]-[CH;D3;+0:2](-[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6])-[N;H0;D3;+0:7](-[CH;D2;+0:8]=O)-[C:9](-[C:10])-[c:11].[NH4+;D0:12]>>[C:10]-[C:9](-[n;H0;D3;+0:7]1:[cH;D2;+0:8]:[n;H0;D2;+0:12]:[cH;D2;+0:1]:[c;H0;D3;+0:2]:1-[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6])-[c:11]
null
[]
null
null
4
HOUR
A mixture of 16.5 g of N,α-bis-formyl-N-(1,2,3,4-tetrahydronaphthalen-1-yl) glycine methyl ester, 65.0 g of ammonium acetate and 100 ml of acetic acid are refluxed for 8 hours. Then additional 50 g ammonium acetate are added and the refluxing is continued for further 4 hours. The solution is diluted with 300 ml of wate...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Tertiary amide
Ester
null
c1c[nH]cn1
c1c[nH]cn1.c1ccc2c(c1)CCCC2
HO-
O
null
4
COC(=O)C(C=O)N(C=O)C1CCCc2ccccc21.[NH4+]>O>COC(=O)c1cncn1C1CCCc2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-803d1399dfd7461184d0632b8742a4e8
CC1(C)CCc2ccccc2C1N.COC(=O)CBr>>COC(=O)CNC1c2ccccc2CCC1(C)C
NC1C(CCC2=CC=CC=C12)(C)C.COC(CBr)=O>>COC(CNC1C(CCC2=CC=CC=C12)(C)C)=O
[NH2:6][CH:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH2:14][CH2:15][C:16]1([CH3:17])[CH3:18].Br[CH2:5][C:3]([O:2][CH3:1])=[O:4]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][CH:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH2:14][CH2:15][C:16]1([CH3:17])[CH3:18]
CC1(C)CCc2ccccc2C1N.COC(=O)CBr
COC(=O)CNC1c2ccccc2CCC1(C)C
null
null
C(C)OCC
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
308780347cfd56717124ea78bf2bc5de380db774d7ce948246e279dfd7d8998b
d2327a8d30a39f085182e5e2f77f5b022ac99c077866b86103acfec639a8f73d
c1ccc2c(c1)CCCC2
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].[C:6]-[C:7](-[NH2;D1;+0:8])-[c:9]>>[C:6]-[C:7](-[NH;D2;+0:8]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5])-[c:9]
null
[]
null
null
70
HOUR
65.2 g of 1-amino-2,2-dimethyl-1,2,3,4-tetrahydronaphthalene are solved in 250 ml of diethyl ether. To this solution is dropwise added a solution of 28.5 g of bromoacetic acid methyl ester in 150 ml of diethyl ether. The mixture is stirred at room temperature for 70 hours. The precipitate is separated and the solution ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Primary amine
Ester.Secondary amine
null
null
c1ccc2c(c1)CCCC2
HBr
C(C)OCC
null
70
CC1(C)CCc2ccccc2C1N.COC(=O)CBr>C(C)OCC>COC(=O)CNC1c2ccccc2CCC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-16ccefa01c1e42bcac9d0c141776cc38
CC(=O)OC(C)=O.COC(=O)CNC1c2ccccc2CCC1(C)C>>COC(=O)CN(C=O)C1c2ccccc2CCC1(C)C
COC(CNC1C(CCC2=CC=CC=C12)(C)C)=O.C(C)(=O)OC(C)=O>>COC(CN(C1C(CCC2=CC=CC=C12)(C)C)C=O)=O
CC(=O)O[C:7](C)=[O:8].[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][CH:9]1[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[CH2:16][CH2:17][C:18]1([CH3:19])[CH3:20]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][N:6]([CH:7]=[O:8])[CH:9]1[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[CH2:16][CH2:17][C:18]1([CH3:19])[CH3:20]
CC(=O)OC(C)=O.COC(=O)CNC1c2ccccc2CCC1(C)C
COC(=O)CN(C=O)C1c2ccccc2CCC1(C)C
null
null
C(=O)O
Acylation
OtherReaction
72a6d1966b6b15ac7195d4682af251dc9ffac857f784a4242970ab5c7a529369
6593c6062585994f02076cd3c86920ae7244b86659eab65c21b5a8628c6d4bb8
c1ccc2c(c1)CCCC2
C-C(=O)-O-[C;H0;D3;+0:1](-C)=[O;D1;H0:2].[C:3]-[C:4](-[NH;D2;+0:5]-[C:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10])-[c:11]>>[C:3]-[C:4](-[N;H0;D3;+0:5](-[C:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10])-[CH;D2;+0:1]=[O;D1;H0:2])-[c:11]
null
[]
null
null
70
HOUR
The complete yield of N-(2,2-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)glycine methyl ester of the process a) is added dropwise with cooling to 5° C. to 67.8 ml of formic acid. Additionally 24.9 ml of acetic anhydride are added, and the mixture is kept at room temperature for 70 hours. Destillation under vacuum afford...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amine
Tertiary amide
null
null
c1ccc2c(c1)CCCC2
HO-
C(=O)O
null
70
CC(=O)OC(C)=O.COC(=O)CNC1c2ccccc2CCC1(C)C>C(=O)O>COC(=O)CN(C=O)C1c2ccccc2CCC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-90f241a6026441e4b5bbd36ef857d8ed
CC(=O)OC(C)=O.COC(=O)CNC1c2ccccc2CC1(C)C>>COC(=O)CN(C=O)C1c2ccccc2CC1(C)C
COC(CNC1C(CC2=CC=CC=C12)(C)C)=O.C(C)(=O)OC(C)=O>>COC(CN(C1C(CC2=CC=CC=C12)(C)C)C=O)=O
CC(=O)O[C:7](C)=[O:8].[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][CH:9]1[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[CH2:16][C:17]1([CH3:18])[CH3:19]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][N:6]([CH:7]=[O:8])[CH:9]1[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[CH2:16][C:17]1([CH3:18])[CH3:19]
CC(=O)OC(C)=O.COC(=O)CNC1c2ccccc2CC1(C)C
COC(=O)CN(C=O)C1c2ccccc2CC1(C)C
null
null
C(=O)O
Acylation
OtherReaction
72a6d1966b6b15ac7195d4682af251dc9ffac857f784a4242970ab5c7a529369
6593c6062585994f02076cd3c86920ae7244b86659eab65c21b5a8628c6d4bb8
c1ccc2c(c1)CCC2
C-C(=O)-O-[C;H0;D3;+0:1](-C)=[O;D1;H0:2].[C:3]-[C:4](-[NH;D2;+0:5]-[C:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10])-[c:11]>>[C:3]-[C:4](-[N;H0;D3;+0:5](-[C:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10])-[CH;D2;+0:1]=[O;D1;H0:2])-[c:11]
null
[]
null
null
18.5
HOUR
936 g of N-(2,2-dimethyl-indan-1-yl)glycine methyl ester are added dropwise with cooling to 5° C. to 1817 ml of formic acid. Additionally 664 ml of acetic anhydride are added, and the mixture is kept at room temperature for 18.5 hours. Destillation under vacuum affords 1015 g of N-formyl-N-(2,2-dimethyl-indan-1-yl)glyc...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amine
Tertiary amide
null
null
c1ccc2c(c1)CCC2
HO-
C(=O)O
null
18.5
CC(=O)OC(C)=O.COC(=O)CNC1c2ccccc2CC1(C)C>C(=O)O>COC(=O)CN(C=O)C1c2ccccc2CC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-13f80b85ece745a599e02367384e39e8
COC(=O)c1cnc(S)n1C1c2ccccc2CC1(C)C>>COC(=O)c1cncn1C1c2ccccc2CC1(C)C
[OH-].[Na+].N(=O)[O-].[Na+].[N+](=O)(O)[O-].COC(=O)C1=CN=C(N1C1C(CC2=CC=CC=C12)(C)C)S>>COC(=O)C1=CN=CN1C1C(CC2=CC=CC=C12)(C)C
S[c:8]1[n:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[CH2:17][C:18]1([CH3:19])[CH3:20]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[CH2:17][C:18]1([CH3:19])[CH3:20]
COC(=O)c1cnc(S)n1C1c2ccccc2CC1(C)C
COC(=O)c1cncn1C1c2ccccc2CC1(C)C
null
null
O
Reduction
OtherReaction
eae27167089e95faf7ce5ed478321b2a0cf6e27101b71987c0c66ed8073c81f6
6dfa579c3c25232785e7dcb34dfc1e7688e0474e6615711d0e6a05188bc6f710
c1ccc2c(c1)CCC2n1ccnc1
S-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4](-[C:5](-[#8:6])=[O;D1;H0:7]):[#7;a:8]:1-[C:9]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]1:[c:3]:[#7;a:2]:[cH;D2;+0:1]:[#7;a:8]:1-[C:9]
96.7
[{"value": 96.7, "product": "COC(=O)C1=CN=CN1C1C(CC2=CC=CC=C12)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
2 g of sodium nitrite and 17.4 ml of nitric acid are solved in 140 ml of deionisized water. Within 20 min. 28 g of 1-(2,2-dimethyl-indan-1-yl)-2-mercapto-5-imidazolecarboxylic acid methyl ester are added portionwise at a temperature between 30° C. and 50° C. The reaction mixture is treated with conc. aqueous sodium hyd...
10.6084/m9.figshare.5104873.v1
null
Aromatic thiol
null
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2c(c1)CCC2
Other
O
null
0.333333
COC(=O)c1cnc(S)n1C1c2ccccc2CC1(C)C>O>COC(=O)c1cncn1C1c2ccccc2CC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-37a0638f1dc84d4298b53e5aaef50245
COC(=O)c1cncn1C1c2ccccc2CCC1(C)C.[OH-]>>COC(=O)c1cncn1C1c2ccccc2C(=O)CC1(C)C
COC(=O)C1=CN=CN1C1C(CCC2=CC=CC=C12)(C)C.[OH-].[Na+]>>COC(=O)C1=CN=CN1C1C(CC(C2=CC=CC=C12)=O)(C)C
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[CH2:17][CH2:19][C:20]1([CH3:21])[CH3:22].[OH-:18]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[C:17](=[O:18])[CH2:19][C:20]1([CH3:21])[CH3:22]
COC(=O)c1cncn1C1c2ccccc2CCC1(C)C.[OH-]
COC(=O)c1cncn1C1c2ccccc2C(=O)CC1(C)C
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
17ac1d8e8ffb91d08f39e971f0bcfc22ee244df26ff57dd988bb7232a176ede7
a196f7191876ee39420290ab9d6c2b9eeb3251b37ae345fc435efba1949a85d9
O=C1CCC(n2ccnc2)c2ccccc21
[C:1]-[C:2]-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6].[OH-;D0:7]>>[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:7])-[c:4](:[c:5]):[c:6]
28.2
[{"value": 28.2, "product": "COC(=O)C1=CN=CN1C1C(CC(C2=CC=CC=C12)=O)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
142 g of 1-(2,2-dimethyl-tetralin-1-yl)-5-imidazolecarboxylic acid methyl ester are dispersed in 1 liter of deionisized water. The suspension is heated to +87° C., and within a period of 1.5 hours a total of 335 g of ammoniaperoxodisulfate is added portionwise in such a manner, that the temperature does not exceed +90°...
10.6084/m9.figshare.5104873.v1
null
null
Ketone
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1c[nH]cn1.c1ccc2c(c1)CCCC2
null
O
null
null
COC(=O)c1cncn1C1c2ccccc2CCC1(C)C.[OH-]>O>COC(=O)c1cncn1C1c2ccccc2C(=O)CC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d340505be6cf4a148cb1322f1bc7b740
CC1(C)C(=O)N(Br)C(=O)N1Br.COC(=O)c1cncn1C1c2ccccc2CCC1(C)C>>COC(=O)c1cncn1C1c2ccccc2C(Br)=CC1(C)C
COC(=O)C1=CN=CN1C1C(CCC2=CC=CC=C12)(C)C.BrN1C(=O)N(C(=O)C1(C)C)Br>>COC(=O)C1=CN=CN1C1C(C=C(C2=CC=CC=C12)Br)(C)C
CC1(C)C(=O)N(Br)C(=O)N1[Br:18].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[CH2:17][CH2:19][C:20]1([CH3:21])[CH3:22]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[C:17]([Br:18])=[CH:19][C:20]1([CH3:21...
CC1(C)C(=O)N(Br)C(=O)N1Br.COC(=O)c1cncn1C1c2ccccc2CCC1(C)C
COC(=O)c1cncn1C1c2ccccc2C(Br)=CC1(C)C
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
OtherReaction
e505f7c41876ffbb88c042e3c5c1b11785785d2fa8ff6a1328717c49a2b88c29
17cbffb6a81e2a92eac972329bd87d2c6ed7c1b3f29193aa2663709d2f8ac83f
C1=Cc2ccccc2C(n2ccnc2)C1
Br-N1-C(=O)-N(-[Br;H0;D1;+0:1])-C(-C)(-C)-C-1=O.[C;D1;H3:2]-[C:3]1(-[C;D1;H3:4])-[C:5]-[c:6]:[c:7](:[c:8])-[CH2;D2;+0:9]-[CH2;D2;+0:10]-1>>[Br;H0;D1;+0:1]-[C;H0;D3;+0:9]1=[CH;D2;+0:10]-[C:3](-[C;D1;H3:2])(-[C;D1;H3:4])-[C:5]-[c:6]:[c:7]-1:[c:8]
51.9
[{"value": 51.9, "product": "COC(=O)C1=CN=CN1C1C(C=C(C2=CC=CC=C12)Br)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 8.5 g of 1-(2,2-dimethyltetralin-1-yl)-5-imidazolecarboxylic acid methyl ester in 100 ml of carbon tetrachloride is treated with 8.6 g of 1,3-dibromo-5,5-dimethylhydantoin and heated to reflux for 1 hour, while the reaction vessel is exposed to a 100W-irradiation lamp. The mixture is cooled to room temper...
10.6084/m9.figshare.5104873.v1
null
Urea.Tertiary amide
Alkenyl halide
C1CNCN1.c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
c1c[nH]cn1.C1=Cc2ccccc2CC1
HBr
C(Cl)(Cl)(Cl)Cl
null
null
CC1(C)C(=O)N(Br)C(=O)N1Br.COC(=O)c1cncn1C1c2ccccc2CCC1(C)C>C(Cl)(Cl)(Cl)Cl>COC(=O)c1cncn1C1c2ccccc2C(Br)=CC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5e6d61be575e48c1b3148f75190618fb
COC(=O)c1cncn1C1c2ccccc2CC1(C)C.O=S(=O)(O)O>>COC(=O)c1cncn1C1c2ccccc2C(=O)C1(C)C
[OH-].[Na+].COC(=O)C1=CN=CN1C1C(CC2=CC=CC=C12)(C)C.S(O)(O)(=O)=O>>COC(=O)C1=CN=CN1C1C(C(C2=CC=CC=C12)=O)(C)C
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[CH2:17][C:19]1([CH3:20])[CH3:21].O=S(O)(O)=[O:18]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[C:17](=[O:18])[C:19]1([CH3:20])[CH3:21]
COC(=O)c1cncn1C1c2ccccc2CC1(C)C.O=S(=O)(O)O
COC(=O)c1cncn1C1c2ccccc2C(=O)C1(C)C
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
32ab24ed955b97edb4307c2f3e4046b88d7a3304f9d6f8e3f49a6ef57e022b90
a196f7191876ee39420290ab9d6c2b9eeb3251b37ae345fc435efba1949a85d9
O=C1CC(n2ccnc2)c2ccccc21
O-S(-O)(=O)=[O;H0;D1;+0:1].[C;D1;H3:2]-[C:3]1(-[C;D1;H3:4])-[C:5]-[c:6]:[c:7](:[c:8])-[CH2;D2;+0:9]-1>>[C;D1;H3:2]-[C:3]1(-[C;D1;H3:4])-[C:5]-[c:6]:[c:7](:[c:8])-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:1]
60.2
[{"value": 60.2, "product": "COC(=O)C1=CN=CN1C1C(C(C2=CC=CC=C12)=O)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 30 g of 1-(2,2-dimethyl-indan-1-yl)-5-imidazolecarboxylic acid methyl ester, 150 ml of water and 17 g of sulfuric acid is heated to +80° C. Within a period of 1.5 hours an aqueous solution of 114 g of ammoniaperoxodisulfate is added dropwise. The reaction mixture is cooled to +7° C. and the pH-value is adj...
10.6084/m9.figshare.5104873.v1
null
null
Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1c[nH]cn1.c1ccc2c(c1)CCC2
HO-
O
null
null
COC(=O)c1cncn1C1c2ccccc2CC1(C)C.O=S(=O)(O)O>O>COC(=O)c1cncn1C1c2ccccc2C(=O)C1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-48e222cb04ad453db4f252afa1c90d91
COC(=O)c1cncn1C1c2ccccc2C(=O)C1(C)C.FS(F)(F)F>>COC(=O)c1cncn1C1c2ccccc2C(F)(F)C1(C)C
COC(=O)C1=CN=CN1C1C(C(C2=CC=CC=C12)=O)(C)C.S(F)(F)(F)F.F>>COC(=O)C1=CN=CN1C1C(C(C2=CC=CC=C12)(F)F)(C)C
O=[C:17]1[c:16]2[c:11]([cH:12][cH:13][cH:14][cH:15]2)[CH:10]([n:9]2[c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:6][n:7][cH:8]2)[C:20]1([CH3:21])[CH3:22].FS(F)([F:18])[F:19]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[C:17]([F:18])([F:19])[C:20]1([CH3:21])[CH3:22]
COC(=O)c1cncn1C1c2ccccc2C(=O)C1(C)C.FS(F)(F)F
COC(=O)c1cncn1C1c2ccccc2C(F)(F)C1(C)C
null
null
null
Functional Group Interconversion
OtherReaction
c04761b116f8f1d87ea7ec401f8b69cf89b1bacf0f356541b04c249a65ea80ad
2296f264e64b8bfbfcbc70726e7ebb990eb0ff1d1f55dd16887952425668883a
c1ccc2c(c1)CCC2n1ccnc1
F-S(-F)(-[F;H0;D1;+0:1])-[F;H0;D1;+0:2].O=[C;H0;D3;+0:3]1-[c:4](:[c:5]):[c:6]-[C:7]-[C:8]-1(-[C;D1;H3:9])-[C;D1;H3:10]>>[C;D1;H3:9]-[C:8]1(-[C;D1;H3:10])-[C:7]-[c:6]:[c:4](:[c:5])-[C;H0;D4;+0:3]-1(-[F;H0;D1;+0:1])-[F;H0;D1;+0:2]
68.4
[{"value": 68.4, "product": "COC(=O)C1=CN=CN1C1C(C(C2=CC=CC=C12)(F)F)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 11.4 g of 1-(2,2-dimethyl-3-oxo-indan-1-yl)-5-imidazolecarboxylic acid methyl ester, 43 g of sulfur tetrafluoride and 160 g of hydrogen fluoride is heated for 24 hours to +50° C. in an acid-resistant autoclave. The pressure is about 7 bars. The unreacted hydrogen fluoride is removed and the residue is take...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary halide.Tertiary halide
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1c[nH]cn1.c1ccc2c(c1)CCC2
Other
null
null
null
COC(=O)c1cncn1C1c2ccccc2C(=O)C1(C)C.FS(F)(F)F>>COC(=O)c1cncn1C1c2ccccc2C(F)(F)C1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-65d806fc62d34034938ca2f29c783c94
CI.CI.O=C1CCc2c(Cl)cccc21>>CC1(C)Cc2c(Cl)cccc2C1=O
[OH-].[K+].ClC1=C2CCC(C2=CC=C1)=O.CI.CN(C=O)C.O.CI>>CC1(C(C2=CC=CC(=C2C1)Cl)=O)C
I[CH3:1].I[CH3:3].[CH2:2]1[CH2:4][c:5]2[c:6]([Cl:7])[cH:8][cH:9][cH:10][c:11]2[C:12]1=[O:13]>>[CH3:1][C:2]1([CH3:3])[CH2:4][c:5]2[c:6]([Cl:7])[cH:8][cH:9][cH:10][c:11]2[C:12]1=[O:13]
CI.CI.O=C1CCc2c(Cl)cccc21
CC1(C)Cc2c(Cl)cccc2C1=O
null
null
null
C-C Coupling
OtherReaction
05f10ef4d1ab771e97c7b7be0989d91b62b233a8c3db90531562574485d68797
6c72a64362b644ff7380f8d0c7bdda962edffb1f22535d7f0916fcd367b6b992
O=C1CCc2ccccc21
I-[CH3;D1;+0:1].I-[CH3;D1;+0:2].[O;D1;H0:3]=[C:4]1-[CH2;D2;+0:5]-[C:6]-[c:7]:[c:8]-1>>[CH3;D1;+0:1]-[C;H0;D4;+0:5]1(-[CH3;D1;+0:2])-[C:6]-[c:7]:[c:8]-[C:4]-1=[O;D1;H0:3]
null
[]
null
null
0.5
HOUR
22.4 g of pulverized potassium hydroxide and 0.1 g of 18-dibenzocrown-6 are added portionwise to a solution of 25 g of 4-chloroindanone and 56.7 g of methyl iodide in 120 ml of dimethylformamide in such a manner that the temperature is kept below +70° C. When the exothermic reaction is over, 5.6 g of methyl iodide are ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HI
null
null
0.5
CI.CI.O=C1CCc2c(Cl)cccc21>>CC1(C)Cc2c(Cl)cccc2C1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-085932d48bf14331abdf9a25304a46c5
CC1(C)Cc2c(Cl)cccc2C1N=CNC#N.COC(=O)CBr>>COC(=O)c1cncn1C1c2cccc(Cl)c2CC1(C)C
C([O-])([O-])=O.[K+].[K+].C([O-])([O-])=O.[K+].[K+].C(#N)NC=NC1C(CC2=C(C=CC=C12)Cl)(C)C.BrCC(=O)OC>>COC(=O)C1=CN=CN1C1C(CC2=C(C=CC=C12)Cl)(C)C
N#[C:6][NH:7][CH:8]=[N:9][CH:10]1[c:11]2[cH:12][cH:13][cH:14][c:15]([Cl:16])[c:17]2[CH2:18][C:19]1([CH3:20])[CH3:21].Br[CH2:5][C:3]([O:2][CH3:1])=[O:4]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[c:11]2[cH:12][cH:13][cH:14][c:15]([Cl:16])[c:17]2[CH2:18][C:19]1([CH3:20])[CH3:21]
CC1(C)Cc2c(Cl)cccc2C1N=CNC#N.COC(=O)CBr
COC(=O)c1cncn1C1c2cccc(Cl)c2CC1(C)C
null
null
CN(C=O)C
Aromatic Heterocycle Formation
OtherReaction
db02dc5dfb17181a055b24a942b62fc5275836628b97c95a452453eeef19bfc6
5d337f1b3dd397171244b5ace24da000a36b300a6429db4e96009e07843a18d8
c1ccc2c(c1)CCC2n1ccnc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].N#[C;H0;D2;+0:6]-[NH;D2;+0:7]-[CH;D2;+0:8]=[N;H0;D2;+0:9]-[C:10](-[C:11])-[c:12]>>[C:11]-[C:10](-[n;H0;D3;+0:9]1:[cH;D2;+0:8]:[n;H0;D2;+0:7]:[cH;D2;+0:6]:[c;H0;D3;+0:1]:1-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5])-[c:12]
49.2
[{"value": 49.2, "product": "COC(=O)C1=CN=CN1C1C(CC2=C(C=CC=C12)Cl)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
12.7 g of potassium carbonate are added to a solution of 21 g of N-cyano-N'-(2,2-dimethyl-4-chloroindan-1-yl)formamidine in 80 ml of dimethylformamide. 14.1 g of methyl bromoacetate are added dropwise. After the exothermic reaction has ceased the mixture is agitated for 1.5 hours at +50° C. another portion of 12.7 g of...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Cyanamide.Ester
Ester
null
c1c[nH]cn1
c1c[nH]cn1.c1ccc2c(c1)CCC2
HBr
CN(C=O)C
null
18
CC1(C)Cc2c(Cl)cccc2C1N=CNC#N.COC(=O)CBr>CN(C=O)C>COC(=O)c1cncn1C1c2cccc(Cl)c2CC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e1764cad45a24269bfb95b0d00a282b2
CC1CC(=O)c2ccccc21.COC(=O)CN>>CC1CC(N(C)CC(=O)O)c2ccccc21
CC1CC(C2=CC=CC=C12)=O.NCC(=O)OC.S1C=CC=C1.C(=O)[O-].[Na+]>>CN(CC(=O)O)C1CC(C2=CC=CC=C12)C
O=[C:4]1[CH2:3][CH:2]([CH3:1])[c:16]2[c:11]1[cH:12][cH:13][cH:14][cH:15]2.C[O:10][C:8]([CH2:7][NH2:5])=[O:9]>>[CH3:1][CH:2]1[CH2:3][CH:4]([N:5]([CH3:6])[CH2:7][C:8](=[O:9])[OH:10])[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]21
CC1CC(=O)c2ccccc21.COC(=O)CN
CC1CC(N(C)CC(=O)O)c2ccccc21
null
[Pd]
CO
Heteroatom Alkylation and Arylation
OtherReaction
2bc4eaa73f23ffd8d982e8944fe469fcba8b9dee744e421bad001b3fc257f848
df47b4fe566332b22ca06efbaad8d3ee4806fcbd642480aefc26d5d77242391e
c1ccc2c(c1)CCC2
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[NH2;D1;+0:5].O=[C;H0;D3;+0:6]1-[C:7]-[C:8]-[c:9]:[c:10]-1:[c:11]>>[C;D1;H3:12]-[N;H0;D3;+0:5](-[C:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1])-[CH;D3;+0:6]1-[C:7]-[C:8]-[c:9]:[c:10]-1:[c:11]
54.1
[{"value": 54.1, "product": "CN(CC(=O)O)C1CC(C2=CC=CC=C12)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 21 parts of 2,3-dihydro-3-methyl-1H-inden-1-one, 25 parts of methyl 2-aminoacetate, 2 parts of a solution of thiophene in methanol 4%, 25 parts of sodium formate and 480 parts of methanol is hydrogenated in a Parr-apparatus and at 50° C. with 5 parts of palladium-on-charcoal catalyst 10%. The reaction mixt...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Primary amine
Carboxylic acid.Tertiary amine
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
Other
[Pd].CO
null
null
CC1CC(=O)c2ccccc21.COC(=O)CN>[Pd].CO>CC1CC(N(C)CC(=O)O)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a873420835704421bdbe4d1c155cadc8
CC1CC(N(C)CC(=O)O)c2ccccc21.O=CO>>CC1CC(N(C=O)C(C)C(=O)O)c2ccccc21
CN(CC(=O)O)C1CC(C2=CC=CC=C12)C.C(C)(=O)OC(C)=O.C(=O)O>>CC(N(C=O)C1CC(C2=CC=CC=C12)C)C(=O)O
[CH3:1][CH:2]1[CH2:3][CH:4]([N:5]([CH2:8][C:10](=[O:11])[OH:12])[CH3:9])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]21.O[CH:6]=[O:7]>>[CH3:1][CH:2]1[CH2:3][CH:4]([N:5]([CH:6]=[O:7])[CH:8]([CH3:9])[C:10](=[O:11])[OH:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]21
CC1CC(N(C)CC(=O)O)c2ccccc21.O=CO
CC1CC(N(C=O)C(C)C(=O)O)c2ccccc21
null
null
null
C-C Coupling
OtherReaction
e4fb14ba8d9fa2f7234edf0d64af7f50d102f78c1ee2361f849352db9a0089c6
e56af770732f724a4446b034cf73b7c95d8ca0204a8c1cd008a666e4b19159c2
c1ccc2c(c1)CCC2
O-[CH;D2;+0:1]=[O;D1;H0:2].[C:3]-[C:4](-[N;H0;D3;+0:5](-[CH3;D1;+0:6])-[CH2;D2;+0:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10])-[c:11]>>[C:3]-[C:4](-[N;H0;D3;+0:5](-[CH;D2;+0:1]=[O;D1;H0:2])-[CH;D3;+0:7](-[CH3;D1;+0:6])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10])-[c:11]
78.7
[{"value": 78.7, "product": "CC(N(C=O)C1CC(C2=CC=CC=C12)C)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 17 parts of methyl N-(2,3-dihydro-3-methyl-1H-inden-1-yl)glycine in 60 parts of formic acid and 20 parts of acetic acid anhydride is stirred overnight at room temperature. The reaction mixture is evaporated in vacuo and the residue is taken up in 1,1'-oxybisethane. The organic layer is washed with a sodiu...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amine
Tertiary amide
null
null
c1ccc2c(c1)CCC2
HO-
null
null
null
CC1CC(N(C)CC(=O)O)c2ccccc21.O=CO>>CC1CC(N(C=O)C(C)C(=O)O)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a725ac383d3d49d4a25d7e2303a9b53c
COC(=O)c1cnc(S)n1C1CC(C)c2ccccc21>>COC(=O)c1cncn1C1CC(C)c2ccccc21
[OH-].[Na+].CC1CC(C2=CC=CC=C12)N1C(=NC=C1C(=O)OC)S.[N+](=O)(O)[O-]>>[N+](=O)(O)[O-].CC1CC(C2=CC=CC=C12)N1C=NC=C1C(=O)OC
S[c:8]1[n:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[n:9]1[CH:10]1[CH2:11][CH:12]([CH3:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][n:7][cH:8][n:9]1[CH:10]1[CH2:11][CH:12]([CH3:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]21
COC(=O)c1cnc(S)n1C1CC(C)c2ccccc21
COC(=O)c1cncn1C1CC(C)c2ccccc21
null
null
null
Reduction
OtherReaction
eae27167089e95faf7ce5ed478321b2a0cf6e27101b71987c0c66ed8073c81f6
6dfa579c3c25232785e7dcb34dfc1e7688e0474e6615711d0e6a05188bc6f710
c1ccc2c(c1)CCC2n1ccnc1
S-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4](-[C:5](-[#8:6])=[O;D1;H0:7]):[#7;a:8]:1-[C:9]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]1:[c:3]:[#7;a:2]:[cH;D2;+0:1]:[#7;a:8]:1-[C:9]
62.6
[{"value": 62.6, "product": "[N+](=O)(O)[O-].CC1CC(C2=CC=CC=C12)N1C=NC=C1C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A mixture of 10 parts of methyl 1-(2,3-dihydro-3-methyl-1H-inden-1-yl)-2-mercapto-1H-imidazole-5-carboxylate and 120 parts of a nitric acid solution 30% is stirred for 30 minutes at room temperature (intense reaction). The reaction mixture is poured into crushed ice and treated with a sodium hydroxide solution. The pro...
10.6084/m9.figshare.5104873.v1
null
Aromatic thiol
null
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccc2c(c1)CCC2
Other
null
null
0.5
COC(=O)c1cnc(S)n1C1CC(C)c2ccccc21>>COC(=O)c1cncn1C1CC(C)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a31b6d4ef7e040b1a5ea277dc09e088c
COC(=O)c1cncn1C1CC(C)c2ccccc21>>CC1CC(n2cncc2C(=O)O)c2ccccc21
[N+](=O)(O)[O-].CC1CC(C2=CC=CC=C12)N1C=NC=C1C(=O)OC.[OH-].[Na+]>>CC1CC(C2=CC=CC=C12)N1C=NC=C1C(=O)O
C[O:12][C:10]([c:9]1[n:5]([CH:4]2[CH2:3][CH:2]([CH3:1])[c:18]3[c:13]2[cH:14][cH:15][cH:16][cH:17]3)[cH:6][n:7][cH:8]1)=[O:11]>>[CH3:1][CH:2]1[CH2:3][CH:4]([n:5]2[cH:6][n:7][cH:8][c:9]2[C:10](=[O:11])[OH:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]21
COC(=O)c1cncn1C1CC(C)c2ccccc21
CC1CC(n2cncc2C(=O)O)c2ccccc21
null
null
C(C)(=O)O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc2c(c1)CCC2n1ccnc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4](:[#7;a:5]):[c:6]:[#7;a:7]>>[#7;a:5]:[c:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]):[c:6]:[#7;a:7]
90
[{"value": 90.0, "product": "CC1CC(C2=CC=CC=C12)N1C=NC=C1C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 3.6 parts of methyl 1-(2,3-dihydro-3-methyl-1H-inden-1-yl)-1H-imidazole-5-carboxylate mononitrate in 50 parts of a sodium hydroxide solution 20% is stirred for 1.5 hours at reflux temperature. After cooling, the reaction mixture is neutralized with acetic acid. The product is extracted with 1,1'-oxybiseth...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cnc[nH]1.c1ccc2c(c1)CCC2
Other
C(C)(=O)O
null
null
COC(=O)c1cncn1C1CC(C)c2ccccc21>C(C)(=O)O>CC1CC(n2cncc2C(=O)O)c2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4af060a23de24f8e80acbb43ee1a8a58
COCCCl.O=C(O)c1cncn1C1CCCc2ccccc21>>COCCOC(=O)c1cncn1C1CCCc2ccccc21
C1(CCCC2=CC=CC=C12)N1C=NC=C1C(=O)O.[H-].[Na+].ClCCOC>>C1(CCCC2=CC=CC=C12)N1C=NC=C1C(=O)OCCOC
Cl[CH2:4][CH2:3][O:2][CH3:1].[OH:5][C:6](=[O:7])[c:8]1[cH:9][n:10][cH:11][n:12]1[CH:13]1[CH2:14][CH2:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]21>>[CH3:1][O:2][CH2:3][CH2:4][O:5][C:6](=[O:7])[c:8]1[cH:9][n:10][cH:11][n:12]1[CH:13]1[CH2:14][CH2:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]21
COCCCl.O=C(O)c1cncn1C1CCCc2ccccc21
COCCOC(=O)c1cncn1C1CCCc2ccccc21
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
c1ccc2c(c1)CCCC2n1ccnc1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[#7;a:4]:[c:5]:[c:6](-[C:7](=[O;D1;H0:8])-[OH;D1;+0:9]):[#7;a:10]>>[#7;a:4]:[c:5]:[c:6](-[C:7](=[O;D1;H0:8])-[O;H0;D2;+0:9]-[CH2;D2;+0:1]-[C:2]-[#8:3]):[#7;a:10]
46.7
[{"value": 46.7, "product": "C1(CCCC2=CC=CC=C12)N1C=NC=C1C(=O)OCCOC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
4.8 Parts of 1-(1,2,3,4-tetrahydro-1-naphthalenyl)-1H-imidazole-5-carboxylic acid are dissolved in 94 parts of warm N,N-dimethylformamide. 0.96 Parts of a sodium hydride dispersion 50% are added portionwise to the thus obtained reaction mixture. Upon complete addition, stirring is continued for 1 hour at room temperatu...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1c[nH]cn1.c1ccc2c(c1)CCCC2
HCl
CN(C=O)C
null
1
COCCCl.O=C(O)c1cncn1C1CCCc2ccccc21>CN(C=O)C>COCCOC(=O)c1cncn1C1CCCc2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9fc75b912d0046a3a872e761ace84d22
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1.CN1CCNCC1>>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCN(C)CC2)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)N=C=S)N2CCC(CC2)C.CN1CCNCC1>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)N2CCN(CC2)C)N2CCC(CC2)C
[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[N:19]=[C:20]=[S:21])[CH2:29][CH2:30]1.[NH:22]1[CH2:23][CH2:24][N:25]([CH3:26])[CH2:27][CH2:28]1>>[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:1...
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1.CN1CCNCC1
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCN(C)CC2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
thiourea
ffc0a97fbb7803c8ffec3d1f54c2fb07d25092ebf582a6d00ebbacbd14015afa
48e0e6261e922bdea79c78ea511461d733cbd49c10100c782d86c83675c4be7c
S=C(Nc1cc2scnc2cc1N1CCCCC1)N1CCNCC1
[#16;a:1]:[c:2]:[c:3]:[c:4](-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[S;D1;H0:7]):[c:8].[#7:9]1-[C:10]-[C:11]-[NH;D2;+0:12]-[C:13]-[C:14]-1>>[#16;a:1]:[c:2]:[c:3]:[c:4](-[NH;D2;+0:5]-[C;H0;D3;+0:6](=[S;D1;H0:7])-[N;H0;D3;+0:12]1-[C:11]-[C:10]-[#7:9]-[C:14]-[C:13]-1):[c:8]
95.1
[{"value": 95.1, "product": "C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)N2CCN(CC2)C)N2CCC(CC2)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a stirred solution of 90 g of 2-tert-butyl-6-isothiocyanato-5-(4-methylpiperidin-1-yl)benzothiazole in 900 ml of methylene chloride is added dropwise 26 g of N-methylpiperazine. The solution is stirred for 1 hour, washed with water, dried over anhydrous sodium sulphate and evaporated to give 110 g of 2-tert-butyl-6-...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Isothiocyanate
Thiourea
C1CNCC[NH]1
C1C[NH]CC[NH]1
C1CC[NH]CC1.c1ccc2scnc2c1.C1C[NH]CC[NH]1
null
C(Cl)Cl
null
1
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1.CN1CCNCC1>C(Cl)Cl>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCN(C)CC2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-269df9c1e534472b9cb72738c8208fee
CC(C)(C)c1nc2cc(Cl)c([N+](=O)[O-])cc2s1.CC1CCNCC1>>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
O.C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)[N+](=O)[O-])Cl.CC1CCNCC1.C([O-])([O-])=O.[K+].[K+]>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)[N+](=O)[O-])N2CCC(CC2)C
Cl[c:6]1[cH:7][c:8]2[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]2[cH:17][c:18]1[N+:19](=[O:20])[O-:21].[CH3:1][CH:2]1[CH2:3][CH2:4][NH:5][CH2:22][CH2:23]1>>[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[N+:19](=[O:20])[O-:21]...
CC(C)(C)c1nc2cc(Cl)c([N+](=O)[O-])cc2s1.CC1CCNCC1
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
null
null
C(Cl)(Cl)Cl.CS(=O)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
23940903aa7aade562a2a6bb5bb712c644c4ccfd92817133b79b0dc88344f250
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1nc2cc(N3CCCCC3)ccc2s1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3]2:[#7;a:4]:[c:5]:[#16;a:6]:[c:7]:2:[c:8]:[c:9]:1-[#7;+:10].[C:11]-[C:12]-[NH;D2;+0:13]-[C:14]-[C:15]>>[#7;+:10]-[c:9]1:[c:8]:[c:7]2:[#16;a:6]:[c:5]:[#7;a:4]:[c:3]:2:[c:2]:[c;H0;D3;+0:1]:1-[N;H0;D3;+0:13](-[C:12]-[C:11])-[C:14]-[C:15]
null
[]
null
null
null
null
A solution of 32,4 g of 2-tert-butyl-5-chloro-6-nitrobenzothiazole, (described in European patent application 85810418.5 published under No. 0175650) in 300 ml of dimethylsulphoxide, is stirred and heated at 140° for 6 hours with 12.8 g of 4-methylpiperidine and 35.8 g of anhydrous potassium carbonate, cooled and poure...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccc2scnc2c1.C1CCNCC1
C1CC[NH]CC1.c1ccc2scnc2c1
C1CC[NH]CC1.c1ccc2scnc2c1
HCl
C(Cl)(Cl)Cl.CS(=O)C
null
null
CC(C)(C)c1nc2cc(Cl)c([N+](=O)[O-])cc2s1.CC1CCNCC1>C(Cl)(Cl)Cl.CS(=O)C>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d2d2589cd1d140879dce79874d0e6100
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1>>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)[N+](=O)[O-])N2CCC(CC2)C>>NC1=CC2=C(N=C(S2)C(C)(C)C)C=C1N1CCC(CC1)C
O=[N+:19]([O-])[c:18]1[c:6]([N:5]2[CH2:4][CH2:3][CH:2]([CH3:1])[CH2:21][CH2:20]2)[cH:7][c:8]2[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]2[cH:17]1>>[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[NH2:19])[CH2:20][CH2:21]1
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1
null
[Ni]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1nc2cc(N3CCCCC3)ccc2s1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]:[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]:[c:4]:[c:2](-[NH2;D1;+0:1]):[c:3]
null
[]
null
null
null
null
A solution of 15.2 g of 2-tert-butyl-5-(4-methyl-piperidin-1-yl)-6-nitrobenzothiazole in 600 ml of methanol is hydrogenated in presence of 6.5 g of Raney Nickel at room temperature. After removing the catalyst the solution is concentrated and the solid filtered to give 6-amino-2-tert-butyl-5-(4-methylpiperidin-1-yl)ben...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
C1CC[NH]CC1.c1ccc2scnc2c1
Other
[Ni].CO
null
null
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1>[Ni].CO>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6cc07c4d63d84829877b5eb5f5957d9d
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1.S=C(Cl)Cl>>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
C(=S)(Cl)Cl.NC1=CC2=C(N=C(S2)C(C)(C)C)C=C1N1CCC(CC1)C.C([O-])(O)=O.[K+]>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)N=C=S)N2CCC(CC2)C
[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[NH2:19])[CH2:22][CH2:23]1.Cl[C:20](Cl)=[S:21]>>[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[N:19]=[C:20]=[S:21]...
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1.S=C(Cl)Cl
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
Amine and thiophosgene to isothiocyanate
1226380c52141f79542a4f85564c11e38ca245efc80be1557b635219a638388c
e5752ca9983a57ab07a0b76a5c8a57a6667ab2cd460616b960134623ec0fce31
c1nc2cc(N3CCCCC3)ccc2s1
Cl-[C;H0;D3;+0:1](-Cl)=[S;D1;H0:2].[#16;a:3]:[c:4]:[c:5]:[c:6](-[NH2;D1;+0:7]):[c:8]>>[#16;a:3]:[c:4]:[c:5]:[c:6](-[N;H0;D2;+0:7]=[C;H0;D2;+0:1]=[S;D1;H0:2]):[c:8]
null
[]
null
null
2
HOUR
To a cooled mixture of 2.1 g of 6-amino-2-tert-butyl-5-(4-methylpiperidin-1-yl)benzothiazole and 2.8 g of potassium bicarbonate in 20 ml of chloroform is added dropwise 1.6 g of thiophosgene in 5 ml of chloroform under stirring. The stirring is continued for 2 hours maintaining the temperature at 0°-2° . The solid is f...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Primary amine
Isothiocyanate
null
null
C1CC[NH]CC1.c1ccc2scnc2c1
HCl
C(Cl)(Cl)Cl
null
2
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1.S=C(Cl)Cl>C(Cl)(Cl)Cl>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c586dd8d365640deae3890d8575254f9
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1.CN1CCNCC1>>CN1CCN(C(=S)Nc2cc3sc(C(C)(C)C)nc3cc2N2CCN(C)CC2)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)N=C=S)N2CCN(CC2)C.CN1CCNCC1>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)N2CCN(CC2)C)N2CCN(CC2)C
[C:6](=[S:7])=[N:8][c:9]1[cH:10][c:11]2[s:12][c:13]([C:14]([CH3:15])([CH3:16])[CH3:17])[n:18][c:19]2[cH:20][c:21]1[N:22]1[CH2:23][CH2:24][N:25]([CH3:26])[CH2:27][CH2:28]1.[CH3:1][N:2]1[CH2:3][CH2:4][NH:5][CH2:29][CH2:30]1>>[CH3:1][N:2]1[CH2:3][CH2:4][N:5]([C:6](=[S:7])[NH:8][c:9]2[cH:10][c:11]3[s:12][c:13]([C:14]([CH3:...
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1.CN1CCNCC1
CN1CCN(C(=S)Nc2cc3sc(C(C)(C)C)nc3cc2N2CCN(C)CC2)CC1
null
null
null
Heteroatom Alkylation and Arylation
thiourea
beb066691ff40a37c26bc4234840e891c6843c6d14f49542e84576855b81b429
48e0e6261e922bdea79c78ea511461d733cbd49c10100c782d86c83675c4be7c
S=C(Nc1cc2scnc2cc1N1CCNCC1)N1CCNCC1
[#16;a:1]:[c:2]:[c:3]:[c:4](-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[S;D1;H0:7]):[c:8].[#7:9]1-[C:10]-[C:11]-[NH;D2;+0:12]-[C:13]-[C:14]-1>>[#16;a:1]:[c:2]:[c:3]:[c:4](-[NH;D2;+0:5]-[C;H0;D3;+0:6](=[S;D1;H0:7])-[N;H0;D3;+0:12]1-[C:11]-[C:10]-[#7:9]-[C:14]-[C:13]-1):[c:8]
null
[]
null
null
null
null
Using the procedure described in Example 1 by reaction of 2-tert-butyl-6-isothiocyanato-5-(4-methyl-piperazin-1-yl)benzothiazole with 4-methylpiperazine is obtained 2-tert-butyl-6[(4-methylpiperazin-1-yl)thiocarbonylamino]-5-(4-methyl-piperazin-1-yl)benzothiazole, melting at 190°-193°. Conditions: See reaction.notes.pr...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Isothiocyanate
Thiourea
C1C[NH]CCN1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccc2scnc2c1.C1C[NH]CC[NH]1
null
null
null
null
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1.CN1CCNCC1>>CN1CCN(C(=S)Nc2cc3sc(C(C)(C)C)nc3cc2N2CCN(C)CC2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8d6c5e55a6af4dfdb2e2e90fcdc60967
CC(C)(C)C(=S)Nc1cc(Cl)c([N+](=O)[O-])cc1Cl.CN1CCNCC1>>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
C(C)(C)(C)C(=S)NC1=C(C=C(C(=C1)Cl)[N+](=O)[O-])Cl.CN1CCNCC1.O>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)[N+](=O)[O-])N2CCN(CC2)C
Cl[c:6]1[cH:7][c:8]([NH:9][C:10]([C:11]([CH3:12])([CH3:13])[CH3:14])=[S:15])[c:16](Cl)[cH:17][c:18]1[N+:19](=[O:20])[O-:21].[CH3:1][N:2]1[CH2:3][CH2:4][NH:5][CH2:22][CH2:23]1>>[CH3:1][N:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[N+:19](=[O:20])[O-...
CC(C)(C)C(=S)Nc1cc(Cl)c([N+](=O)[O-])cc1Cl.CN1CCNCC1
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
null
null
CS(=O)C
Aromatic Heterocycle Formation
OtherReaction
297f82e651599316300ea4f144d833ce40a1bbc8b8cc5d293abe23ff11a6a397
3d6aed948203792cde1994139fdaf33ee119c39bdeb5518dc010f2535b646762
c1nc2cc(N3CCNCC3)ccc2s1
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[#7;+:4]):[c;H0;D3;+0:5](-Cl):[c:6]:[c:7]:1-[NH;D2;+0:8]-[C;H0;D3;+0:9](=[S;H0;D1;+0:10])-[C:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[C;D1;H3:14].[#7:15]1-[C:16]-[C:17]-[NH;D2;+0:18]-[C:19]-[C:20]-1>>[#7;+:4]-[c:3]1:[c:2]:[c;H0;D3;+0:1]2:[s;H0;D2;+0:10]:[c;H0;D3;+0:9](-[C:11](-[C;D1;H3:12])(-[...
null
[]
null
null
null
null
A solution of 171 g of N-tert-butylthiocarbonyl-2,5-dichloro-4-nitroaniline (described in European patent application No. 85810418.5 published under No. 0175650) and 605 ml of N-methylpiperazine in 1700 ml of dimethylsulphoxide is heated at 140° for 8 hours, cooled and poured into water. The solid is filtered, washed w...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Thioamide.Secondary amine
Tertiary amine
c1ccccc1.C1C[NH]CCN1
C1C[NH]CC[NH]1.c1ccc2scnc2c1
C1C[NH]CC[NH]1.c1ccc2scnc2c1
HCl
CS(=O)C
null
null
CC(C)(C)C(=S)Nc1cc(Cl)c([N+](=O)[O-])cc1Cl.CN1CCNCC1>CS(=O)C>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c4b9469cd7684e858e4abf2ec83970cc
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1>>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)[N+](=O)[O-])N2CCN(CC2)C>>NC1=CC2=C(N=C(S2)C(C)(C)C)C=C1N1CCN(CC1)C
O=[N+:19]([O-])[c:18]1[c:6]([N:5]2[CH2:4][CH2:3][N:2]([CH3:1])[CH2:21][CH2:20]2)[cH:7][c:8]2[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]2[cH:17]1>>[CH3:1][N:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[NH2:19])[CH2:20][CH2:21]1
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1
null
[Ni]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1nc2cc(N3CCNCC3)ccc2s1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]:[c:5]:[#16;a:6]>>[#16;a:6]:[c:5]:[c:4]:[c:2](-[NH2;D1;+0:1]):[c:3]
null
[]
null
null
null
null
A solution of 86 g of the above nitro compound in 150 ml of ethanol is hydrogenated in presence of 30 g of Raney nickel at 45°. The solution is filtered to give 6-amino-2-tert-butyl-5-(4-methylpiperazin-1-yl)benzothiazole, melting at 130° C. Conditions: See reaction.notes.procedure_details. Workup: The solution is filt...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
C1C[NH]CC[NH]1.c1ccc2scnc2c1
Other
[Ni].C(C)O
null
null
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2[N+](=O)[O-])CC1>[Ni].C(C)O>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a9b6c5936caf4afa829011ebb019f26e
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1.S=C(Cl)Cl>>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
[OH-].[Na+].NC1=CC2=C(N=C(S2)C(C)(C)C)C=C1N1CCN(CC1)C.C([O-])(O)=O.[Na+].C(=S)(Cl)Cl>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)N=C=S)N2CCN(CC2)C
[CH3:1][N:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[NH2:19])[CH2:22][CH2:23]1.Cl[C:20](Cl)=[S:21]>>[CH3:1][N:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[N:19]=[C:20]=[S:21])[...
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1.S=C(Cl)Cl
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
null
null
C(Cl)(Cl)Cl.O
Heteroatom Alkylation and Arylation
Amine and thiophosgene to isothiocyanate
1226380c52141f79542a4f85564c11e38ca245efc80be1557b635219a638388c
e5752ca9983a57ab07a0b76a5c8a57a6667ab2cd460616b960134623ec0fce31
c1nc2cc(N3CCNCC3)ccc2s1
Cl-[C;H0;D3;+0:1](-Cl)=[S;D1;H0:2].[#16;a:3]:[c:4]:[c:5]:[c:6](-[NH2;D1;+0:7]):[c:8]>>[#16;a:3]:[c:4]:[c:5]:[c:6](-[N;H0;D2;+0:7]=[C;H0;D2;+0:1]=[S;D1;H0:2]):[c:8]
null
[]
null
null
4
HOUR
To a stirred mixture of 75 g of 6-Amino-2-tert-butyl-5-(4-methylpiperazin-1-yl)benzothiazole and 29 g of sodium bicarbonate in 1100 ml of chloroform at 0° is added 41 g of thiophosgene and the mixture stirred at 10° for 4 hours. After filtering off the solid, the solution is evaporated to get a yellow solid which is di...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Primary amine
Isothiocyanate
null
null
C1C[NH]CC[NH]1.c1ccc2scnc2c1
HCl
C(Cl)(Cl)Cl.O
null
4
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N)CC1.S=C(Cl)Cl>C(Cl)(Cl)Cl.O>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-498a7819ece24228b5eb4b4daeed8749
C1CCNCC1.CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1>>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCCCC2)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)N=C=S)N2CCN(CC2)C.N1CCCCC1>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)N2CCCCC2)N2CCN(CC2)C
[NH:22]1[CH2:23][CH2:24][CH2:25][CH2:26][CH2:27]1.[CH3:1][N:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[N:19]=[C:20]=[S:21])[CH2:28][CH2:29]1>>[CH3:1][N:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][...
C1CCNCC1.CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCCCC2)CC1
null
null
null
Heteroatom Alkylation and Arylation
thiourea
22c0be506eba558bc623a80aec10790e7277d2acd89004b822814260d768b6ca
48e0e6261e922bdea79c78ea511461d733cbd49c10100c782d86c83675c4be7c
S=C(Nc1cc2scnc2cc1N1CCNCC1)N1CCCCC1
[#16;a:1]:[c:2]:[c:3]:[c:4](-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[S;D1;H0:7]):[c:8].[C:9]-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13]>>[#16;a:1]:[c:2]:[c:3]:[c:4](-[NH;D2;+0:5]-[C;H0;D3;+0:6](=[S;D1;H0:7])-[N;H0;D3;+0:11](-[C:10]-[C:9])-[C:12]-[C:13]):[c:8]
null
[]
null
null
null
null
Reaction of 2-tert-butyl-6-isothiocyanato-5-(4-methyl-piperazin-1-yl)benzothiazole described in Example 2 with piperidine under conditions described in Example 1 gives 2-tert-butyl-6-[(piperidin-1-yl)thiocarbonylamino]-5-(4-methyl-piperazin-1-yl)benzothiazole, melting at 202°-206°. Conditions: See reaction.notes.proced...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Isothiocyanate
Thiourea
C1CCNCC1
C1CC[NH]CC1
C1C[NH]CC[NH]1.c1ccc2scnc2c1.C1CC[NH]CC1
null
null
null
null
C1CCNCC1.CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1>>CN1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCCCC2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0021d0cc1d434e90be2099cbc1a36c49
C1CNCCN1.CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1>>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCNCC2)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)N=C=S)N2CCC(CC2)C.N1CCNCC1>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)N2CCNCC2)N2CCC(CC2)C
[NH:22]1[CH2:23][CH2:24][NH:25][CH2:26][CH2:27]1.[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17][c:18]2[N:19]=[C:20]=[S:21])[CH2:28][CH2:29]1>>[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15]...
C1CNCCN1.CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCNCC2)CC1
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
thiourea
0ffd0e1a6ff3ac1a0669a3464c502b065eb1f716362b6957d50d08a7f94ff96f
48e0e6261e922bdea79c78ea511461d733cbd49c10100c782d86c83675c4be7c
S=C(Nc1cc2scnc2cc1N1CCCCC1)N1CCNCC1
[#16;a:1]:[c:2]:[c:3]:[c:4](-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[S;D1;H0:7]):[c:8].[#7:9]1-[C:10]-[C:11]-[NH;D2;+0:12]-[C:13]-[C:14]-1>>[#16;a:1]:[c:2]:[c:3]:[c:4](-[NH;D2;+0:5]-[C;H0;D3;+0:6](=[S;D1;H0:7])-[N;H0;D3;+0:12]1-[C:11]-[C:10]-[#7:9]-[C:14]-[C:13]-1):[c:8]
69.6
[{"value": 69.6, "product": "C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)N2CCNCC2)N2CCC(CC2)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
A solution of 3.45 g of 2-tert-butyl-6-isothiocyanato-5-(4-methylpiperidin-1-yl)benzothiazole, described in Example 1, and 8.6 g of anhydrous piperazine in 30 ml of chloroform is stirred for 3 hours, washed with water, dried over anhydrous sodium sulphate and evaporated to get a sticky residue which is triturated with ...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Isothiocyanate
Thiourea
C1CNCCN1
C1C[NH]CCN1
C1CC[NH]CC1.c1ccc2scnc2c1.C1C[NH]CCN1
null
C(Cl)(Cl)Cl
null
3
C1CNCCN1.CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1>C(Cl)(Cl)Cl>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCNCC2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c1cccb7f4ab14334a9142cd6bd51341b
CC(=O)N1CCNCC1.CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1>>CC(=O)N1CCN(C(=S)Nc2cc3sc(C(C)(C)C)nc3cc2N2CCC(C)CC2)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)N=C=S)N2CCC(CC2)C.C(C)(=O)N1CCNCC1>>C(C)(=O)N1CCN(CC1)C(=S)NC1=CC2=C(N=C(S2)C(C)(C)C)C=C1N1CCC(CC1)C
[CH3:1][C:2](=[O:3])[N:4]1[CH2:5][CH2:6][NH:7][CH2:31][CH2:32]1.[C:8](=[S:9])=[N:10][c:11]1[cH:12][c:13]2[s:14][c:15]([C:16]([CH3:17])([CH3:18])[CH3:19])[n:20][c:21]2[cH:22][c:23]1[N:24]1[CH2:25][CH2:26][CH:27]([CH3:28])[CH2:29][CH2:30]1>>[CH3:1][C:2](=[O:3])[N:4]1[CH2:5][CH2:6][N:7]([C:8](=[S:9])[NH:10][c:11]2[cH:12][...
CC(=O)N1CCNCC1.CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1
CC(=O)N1CCN(C(=S)Nc2cc3sc(C(C)(C)C)nc3cc2N2CCC(C)CC2)CC1
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
thiourea
beb066691ff40a37c26bc4234840e891c6843c6d14f49542e84576855b81b429
48e0e6261e922bdea79c78ea511461d733cbd49c10100c782d86c83675c4be7c
S=C(Nc1cc2scnc2cc1N1CCCCC1)N1CCNCC1
[#16;a:1]:[c:2]:[c:3]:[c:4](-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[S;D1;H0:7]):[c:8].[#7:9]1-[C:10]-[C:11]-[NH;D2;+0:12]-[C:13]-[C:14]-1>>[#16;a:1]:[c:2]:[c:3]:[c:4](-[NH;D2;+0:5]-[C;H0;D3;+0:6](=[S;D1;H0:7])-[N;H0;D3;+0:12]1-[C:11]-[C:10]-[#7:9]-[C:14]-[C:13]-1):[c:8]
null
[]
null
null
null
null
A solution of 2.0 g of 2-tert-butyl-6-isothiocyanato-5-(4-methylpiperidin-1-yl)benzothiazole and 0.78 g of 1-acetyl-piperazine in 30 ml of chloroform is stirred for 30 minutes and the product triturated with petroleum ether to obtain 6-[(4-acetyl-piperazin-1-yl)thiocarbonylamino]-2-tert-butyl-5-(4-methylpiperidin-1-yl)...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Isothiocyanate
Thiourea
C1C[NH]CCN1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccc2scnc2c1.C1CC[NH]CC1
null
C(Cl)(Cl)Cl
null
null
CC(=O)N1CCNCC1.CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2N=C=S)CC1>C(Cl)(Cl)Cl>CC(=O)N1CCN(C(=S)Nc2cc3sc(C(C)(C)C)nc3cc2N2CCC(C)CC2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-31d1f67ee9ff459da6d1d62523ee490c
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)Oc2ccccc2)CC1.CN1CCNCC1>>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCN(C)CC2)CC1
C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)OC2=CC=CC=C2)N2CCC(CC2)C.CN1CCNCC1>>C(C)(C)(C)C=1SC2=C(N1)C=C(C(=C2)NC(=S)N2CCN(CC2)C)N2CCC(CC2)C
c1ccc(O[C:20]([NH:19][c:18]2[c:6]([N:5]3[CH2:4][CH2:3][CH:2]([CH3:1])[CH2:30][CH2:29]3)[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[s:15][c:16]3[cH:17]2)=[S:21])cc1.[NH:22]1[CH2:23][CH2:24][N:25]([CH3:26])[CH2:27][CH2:28]1>>[CH3:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[cH:7][c:8]3[n:9][c:10]([C:11]([CH3:12])(...
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)Oc2ccccc2)CC1.CN1CCNCC1
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCN(C)CC2)CC1
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
f203caeb853ec2a5d06ef14ace71f92aa0cf64e04c1926993a6e02783752f4c4
a7203ce657e7d6b42383ef88862a35a277cf8306602c3faf7b8bbf0a1e9adfe3
S=C(Nc1cc2scnc2cc1N1CCCCC1)N1CCNCC1
[#7:1]1-[C:2]-[C:3]-[NH;D2;+0:4]-[C:5]-[C:6]-1.[S;D1;H0:7]=[C;H0;D3;+0:8](-O-c1:c:c:c:c:c:1)-[#7:9]-[c:10]>>[S;D1;H0:7]=[C;H0;D3;+0:8](-[#7:9]-[c:10])-[N;H0;D3;+0:4]1-[C:3]-[C:2]-[#7:1]-[C:6]-[C:5]-1
null
[]
null
null
null
null
A solution of 0.5 g of 2-tert-butyl-5-(4-methyl-piperidin-1-yl)-6-phenoxythiocarbonylaminobenzothiazole and 0.11 g of 4-methylpiperazine in 20 ml of dioxane is refluxed for 16 hours. Evaporation of the solvent and chromatography of the residue over silica gel and elution with methylene dichloride-methanol (98:2) gives ...
10.6084/m9.figshare.5104873.v1
null
Ether.Thioamide.Secondary amine
Thiourea
c1ccccc1.C1CNCC[NH]1
C1C[NH]CC[NH]1
C1CC[NH]CC1.c1ccc2scnc2c1.C1C[NH]CC[NH]1
HO-
O1CCOCC1
null
null
CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)Oc2ccccc2)CC1.CN1CCNCC1>O1CCOCC1>CC1CCN(c2cc3nc(C(C)(C)C)sc3cc2NC(=S)N2CCN(C)CC2)CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-776b6e04372e48e3ab61b37e552959a1
CC1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>>CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
N.NC1=CC=C(C=C1)C=1C(CC(NN1)=O)C.O1C=CC(C=C1)=O.Cl>>CC1CC(NN=C1C1=CC=C(C=C1)N1C=CC(C=C1)=O)=O
[CH3:1][CH:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12]([NH2:13])[cH:20][cH:21]1.o1[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]1>>[CH3:1][CH:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
CC1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1
CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A stirred mixture of 6-(4-aminophenyl)-5-methyl-4,5-dihydro-3(2H)-pyridazinone (1.0 g), 4H-pyran-4-one (0.52 g), water (20 ml), and concentrated hydrochloric acid (0.41 ml) was heated under reflux for 31/2 hours. The resultant solid was dissolved in the minimum of hot water and the solution was neutralised with aqueous...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
C1=NNCCC1.c1ccccc1.c1ccncc1
HO-
O
null
null
CC1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>O>CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-485e041677a3458f8860e1c73bcd36fb
Nc1ccc(C2=NNC(=O)CC2)cc1.O=c1ccocc1>>O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
Cl.NC1=CC=C(C=C1)C=1CCC(NN1)=O.O1C=CC(C=C1)=O.N>>O=C1C=CN(C=C1)C1=CC=C(C=C1)C=1CCC(NN1)=O
[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9]([NH2:10])[cH:17][cH:18]2)=[N:19][NH:20]1.o1[cH:11][cH:12][c:13](=[O:14])[cH:15][cH:16]1>>[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([c:6]2[cH:7][cH:8][c:9](-[n:10]3[cH:11][cH:12][c:13](=[O:14])[cH:15][cH:16]3)[cH:17][cH:18]2)=[N:19][NH:20]1
Nc1ccc(C2=NNC(=O)CC2)cc1.O=c1ccocc1
O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A stirred mixture of 6-(4-aminophenyl)-4,5-dihydro-3(2H)-pyridazinone hydrochloride (1.5 g), 4H-pyran-4-one (0.7 g), and water (20 ml), was heated under reflux for 41/2 hours. The resultant solid was dissolved in the minimum of hot water and the solution was neutralised with ammonia to give the crude product. Recrystal...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
C1=NNCCC1.c1ccccc1.c1ccncc1
HO-
O
null
null
Nc1ccc(C2=NNC(=O)CC2)cc1.O=c1ccocc1>O>O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2e0927e1207d4f81994448ab79173b02
Nc1ccc(-c2ccc(=O)[nH]n2)cc1.O=c1ccocc1>>O=c1ccn(-c2ccc(-c3ccc(=O)[nH]n3)cc2)cc1
Cl.NC1=CC=C(C=C1)C=1C=CC(NN1)=O.O1C=CC(C=C1)=O.N>>O=C1C=CN(C=C1)C1=CC=C(C=C1)C=1C=CC(NN1)=O
[NH2:5][c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][cH:12][c:13](=[O:14])[nH:15][n:16]2)[cH:17][cH:18]1.o1[cH:4][cH:3][c:2](=[O:1])[cH:20][cH:19]1>>[O:1]=[c:2]1[cH:3][cH:4][n:5](-[c:6]2[cH:7][cH:8][c:9](-[c:10]3[cH:11][cH:12][c:13](=[O:14])[nH:15][n:16]3)[cH:17][cH:18]2)[cH:19][cH:20]1
Nc1ccc(-c2ccc(=O)[nH]n2)cc1.O=c1ccocc1
O=c1ccn(-c2ccc(-c3ccc(=O)[nH]n3)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=c1ccn(-c2ccc(-c3ccc(=O)[nH]n3)cc2)cc1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A stirred mixture of 6-(4-aminophenyl)-3(2H)-pyridazinone hydrochloride (1.5 g), 4H-pyran-4-one (0.71 g), and water (20 ml), was heated under reflux for 2 hours. The pH of the hot solution was adjusted to 8 with aqueous ammonia and the mixture was cooled to give the crude product, 1.84 g, m.p. 338°-340° C. Recrystallis...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
c1ccncc1.c1ccccc1.c1cccnn1
HO-
O
null
null
Nc1ccc(-c2ccc(=O)[nH]n2)cc1.O=c1ccocc1>O>O=c1ccn(-c2ccc(-c3ccc(=O)[nH]n3)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4206414e65394297bb38130b22a09378
Nc1ccc(C2=NNC(=O)CS2)cc1.O=c1ccocc1>>O=C1CSC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
N.NC1=CC=C(C=C1)C=1SCC(NN1)=O.O1C=CC(C=C1)=O.Cl>>O=C1C=CN(C=C1)C1=CC=C(C=C1)C=1SCC(NN1)=O
[O:1]=[C:2]1[CH2:3][S:4][C:5]([c:6]2[cH:7][cH:8][c:9]([NH2:10])[cH:17][cH:18]2)=[N:19][NH:20]1.o1[cH:11][cH:12][c:13](=[O:14])[cH:15][cH:16]1>>[O:1]=[C:2]1[CH2:3][S:4][C:5]([c:6]2[cH:7][cH:8][c:9](-[n:10]3[cH:11][cH:12][c:13](=[O:14])[cH:15][cH:16]3)[cH:17][cH:18]2)=[N:19][NH:20]1
Nc1ccc(C2=NNC(=O)CS2)cc1.O=c1ccocc1
O=C1CSC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=C1CSC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A stirred mixture of 2-(4-aminophenyl)-4H,6H-1,3,4-thiadiazin-5-one (1.0 g), 4H-pyran-4-one (0.51 g), water (20 ml) and concentrated hydrochloric acid (0.42 ml), was heated under reflux for 3 hours. The warm solution was neutralised with concentrated aqueous ammonia and cooled to give a solid, 1.33 g. Recrystallisation...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
C1=NNCCS1.c1ccccc1.c1ccncc1
HO-
O
null
null
Nc1ccc(C2=NNC(=O)CS2)cc1.O=c1ccocc1>O>O=C1CSC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2f8234d22a2e4c56b954a52e13ae7222
CC1SC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>>CC1SC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
NC1=CC=C(C=C1)C1=NNC(SC1C)=O.O1C=CC(C=C1)=O.C(C)(=O)O>>O=C1C=CN(C=C1)C1=CC=C(C=C1)C1=NNC(SC1C)=O
[CH3:1][CH:2]1[S:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12]([NH2:13])[cH:20][cH:21]1.o1[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]1>>[CH3:1][CH:2]1[S:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
CC1SC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1
CC1SC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=C1NN=C(c2ccc(-n3ccc(=O)cc3)cc2)CS1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A stirred mixture of 5-(4-aminophenyl)-6-methyl-3H,6H-1,3,4-thiadiazine-2-one (0.54 g), 4H-pyran-4-one (0.26 g), glacial acetic acid (0.15 g) and water (20 ml) was heated under reflux for 24 hours to give a solid, 0.54 g. Recrystallisation from aqueous ethanol gave the title compound, 0.28 g, which darkened at 265° C. ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
C1=NNCSC1.c1ccccc1.c1ccncc1
HO-
O
null
null
CC1SC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>O>CC1SC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-acfd563acf594497a8d324ed74eb0b8c
Nc1ccc(-c2c[nH]c(=O)cn2)cc1.O=c1ccocc1>>O=c1ccn(-c2ccc(-c3c[nH]c(=O)cn3)cc2)cc1
Cl.NC1=CC=C(C=C1)C=1N=CC(NC1)=O.Cl.O1C=CC(C=C1)=O>>O=C1C=CN(C=C1)C1=CC=C(C=C1)C=1N=CC(NC1)=O
[NH2:5][c:6]1[cH:7][cH:8][c:9](-[c:10]2[cH:11][nH:12][c:13](=[O:14])[cH:15][n:16]2)[cH:17][cH:18]1.o1[cH:4][cH:3][c:2](=[O:1])[cH:20][cH:19]1>>[O:1]=[c:2]1[cH:3][cH:4][n:5](-[c:6]2[cH:7][cH:8][c:9](-[c:10]3[cH:11][nH:12][c:13](=[O:14])[cH:15][n:16]3)[cH:17][cH:18]2)[cH:19][cH:20]1
Nc1ccc(-c2c[nH]c(=O)cn2)cc1.O=c1ccocc1
O=c1ccn(-c2ccc(-c3c[nH]c(=O)cn3)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=c1ccn(-c2ccc(-c3c[nH]c(=O)cn3)cc2)cc1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A stirred mixture of 5-(4-aminophenyl)-2(1H)pyrazinone hydrochloride (1.5 g, from hydrolysis of the corresponding acetamido derivative with hydrochloric acid), 4H-pyran-4-one (0.71 g) and water (15 ml) was heated under reflux for 21/2 hours under a nitrogen atmosphere. The resultant solution was neutralised to give a s...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
c1ccncc1.c1ccccc1.c1cnccn1
HO-
O
null
null
Nc1ccc(-c2c[nH]c(=O)cn2)cc1.O=c1ccocc1>O>O=c1ccn(-c2ccc(-c3c[nH]c(=O)cn3)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f6081b4f6c874294b9305d5620438d99
Nc1ccc2c(c1)Cc1cc(=O)[nH]nc1-2.O=c1ccocc1>>O=c1ccn(-c2ccc3c(c2)Cc2cc(=O)[nH]nc2-3)cc1
Cl.NC=1C=C2CC=3C(=NNC(C3)=O)C2=CC1.O1C=CC(C=C1)=O.N>>O=C1C=CN(C=C1)C=1C=C2CC=3C(=NNC(C3)=O)C2=CC1
[NH2:5][c:6]1[cH:7][cH:8][c:9]2[c:10]([cH:11]1)[CH2:12][c:13]1[cH:14][c:15](=[O:16])[nH:17][n:18][c:19]1-2.o1[cH:4][cH:3][c:2](=[O:1])[cH:21][cH:20]1>>[O:1]=[c:2]1[cH:3][cH:4][n:5](-[c:6]2[cH:7][cH:8][c:9]3[c:10]([cH:11]2)[CH2:12][c:13]2[cH:14][c:15](=[O:16])[nH:17][n:18][c:19]2-3)[cH:20][cH:21]1
Nc1ccc2c(c1)Cc1cc(=O)[nH]nc1-2.O=c1ccocc1
O=c1ccn(-c2ccc3c(c2)Cc2cc(=O)[nH]nc2-3)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=c1ccn(-c2ccc3c(c2)Cc2cc(=O)[nH]nc2-3)cc1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A stirred mixture of 7-amino-[5H]indeno[1,2-c]pyridazin-3(2H)-one hydrochloride (1.0 g) and 4H-pyran-4-one (0.48 g) in water (10 ml) was heated under reflux for 1 hour in a nitrogen atmosphere. The warm mixture was neutralised with aqueous ammonia to give a solid, 0.9 g, m.p. >300° C. This solid was triturated with war...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
c1ccncc1.c1ccc2c(c1)Cc1ccnnc12
HO-
O
null
null
Nc1ccc2c(c1)Cc1cc(=O)[nH]nc1-2.O=c1ccocc1>O>O=c1ccn(-c2ccc3c(c2)Cc2cc(=O)[nH]nc2-3)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-59c565222c524969851c7e1b747f4739
Nc1ccc2c(c1)CCC1CC(=O)NN=C21.O=c1ccocc1>>O=C1CC2CCc3cc(-n4ccc(=O)cc4)ccc3C2=NN1
Cl.NC=1C=CC2=C(CCC3CC(NN=C23)=O)C1.O1C=CC(C=C1)=O>>O=C1C=CN(C=C1)C=1C=CC2=C(CCC3CC(NN=C23)=O)C1
[O:1]=[C:2]1[CH2:3][CH:4]2[CH2:5][CH2:6][c:7]3[cH:8][c:9]([NH2:10])[cH:17][cH:18][c:19]3[C:20]2=[N:21][NH:22]1.o1[cH:11][cH:12][c:13](=[O:14])[cH:15][cH:16]1>>[O:1]=[C:2]1[CH2:3][CH:4]2[CH2:5][CH2:6][c:7]3[cH:8][c:9](-[n:10]4[cH:11][cH:12][c:13](=[O:14])[cH:15][cH:16]4)[cH:17][cH:18][c:19]3[C:20]2=[N:21][NH:22]1
Nc1ccc2c(c1)CCC1CC(=O)NN=C21.O=c1ccocc1
O=C1CC2CCc3cc(-n4ccc(=O)cc4)ccc3C2=NN1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=C1CC2CCc3cc(-n4ccc(=O)cc4)ccc3C2=NN1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
10.3
[{"value": 10.3, "product": "O=C1C=CN(C=C1)C=1C=CC2=C(CCC3CC(NN=C23)=O)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred mixture of 8-amino-4,4a,5,6-tetrahydrobenzo[h]cinnolin-3(2H)-one hydrochloride (1.5 g) and 4H-pyran-4-one (0.84 g) in water (40 ml) was heated under reflux for 2 hours in a nitrogen atmosphere. The resultant solid was washed with dilute hydrochloric acid to give a crude product, 0.5 g. Purification by column ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
c1ccc2c(c1)CCC1CCNN=C21.c1ccncc1
HO-
O
null
null
Nc1ccc2c(c1)CCC1CC(=O)NN=C21.O=c1ccocc1>O>O=C1CC2CCc3cc(-n4ccc(=O)cc4)ccc3C2=NN1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5b3edb5c38374dab95408851f226d3f9
Nc1ccc(-c2n[nH]c(=O)s2)cc1.O=c1ccocc1>>O=c1ccn(-c2ccc(-c3n[nH]c(=O)s3)cc2)cc1
Cl.NC1=CC=C(C=C1)C1=NNC(S1)=O.O1C=CC(C=C1)=O.C(C)O>>O=C1C=CN(C=C1)C1=CC=C(C=C1)C1=NNC(S1)=O
[NH2:5][c:6]1[cH:7][cH:8][c:9](-[c:10]2[n:11][nH:12][c:13](=[O:14])[s:15]2)[cH:16][cH:17]1.o1[cH:4][cH:3][c:2](=[O:1])[cH:19][cH:18]1>>[O:1]=[c:2]1[cH:3][cH:4][n:5](-[c:6]2[cH:7][cH:8][c:9](-[c:10]3[n:11][nH:12][c:13](=[O:14])[s:15]3)[cH:16][cH:17]2)[cH:18][cH:19]1
Nc1ccc(-c2n[nH]c(=O)s2)cc1.O=c1ccocc1
O=c1ccn(-c2ccc(-c3n[nH]c(=O)s3)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=c1ccn(-c2ccc(-c3n[nH]c(=O)s3)cc2)cc1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A mixture of 5-(4-aminophenyl)-1,3,4-thiadiazol-2(3H)-one hydrochloride (1.25 g), 4H-pyran-4-one (0.58 g), ethanol (10 ml) and water (50 ml) was stirred under reflux under nitrogen for 31/2 hours. The cooled reaction mixture was filtered and the collected orange solid was washed with aqueous potassium hydrogen carbonat...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
c1ccncc1.c1ccccc1.c1nncs1
HO-
O
null
null
Nc1ccc(-c2n[nH]c(=O)s2)cc1.O=c1ccocc1>O>O=c1ccn(-c2ccc(-c3n[nH]c(=O)s3)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d3f1608a6b4f44cb9da8fc4248faeacd
O=c1[nH]nc(-c2ccc([N+](=O)[O-])cc2)o1>>Nc1ccc(-c2n[nH]c(=O)o2)cc1
[N+](=O)([O-])C1=CC=C(C=C1)C1=NNC(O1)=O>>NC1=CC=C(C=C1)C1=NNC(O1)=O
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][nH:8][c:9](=[O:10])[o:11]2)[cH:12][cH:13]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][nH:8][c:9](=[O:10])[o:11]2)[cH:12][cH:13]1
O=c1[nH]nc(-c2ccc([N+](=O)[O-])cc2)o1
Nc1ccc(-c2n[nH]c(=O)o2)cc1
null
[Pd]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=c1[nH]nc(-c2ccccc2)o1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
5-(4-nitrophenyl)-1,3,4-oxadiazol-2(3H)-one, (0.65 g) in ethanol (100 ml) was hydrogenated at 276 kPa (40 p.s.i.) in the presence of palladium on carbon at room temperature for one hour. The reaction mixture was filtered, the filtrate was evaporated to dryness and the resultant yellow solid was recrystallised from etha...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1nnco1
Other
[Pd].C(C)O
null
null
O=c1[nH]nc(-c2ccc([N+](=O)[O-])cc2)o1>[Pd].C(C)O>Nc1ccc(-c2n[nH]c(=O)o2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c091a3ddf3114d9bb84a4a03518b6901
Nc1ccc(-c2n[nH]c(=O)o2)cc1.O=c1ccocc1>>O=c1ccn(-c2ccc(-c3n[nH]c(=O)o3)cc2)cc1
N.NC1=CC=C(C=C1)C1=NNC(O1)=O.O1C=CC(C=C1)=O.Cl>>O=C1C=CN(C=C1)C1=CC=C(C=C1)C1=NNC(O1)=O
[NH2:5][c:6]1[cH:7][cH:8][c:9](-[c:10]2[n:11][nH:12][c:13](=[O:14])[o:15]2)[cH:16][cH:17]1.o1[cH:4][cH:3][c:2](=[O:1])[cH:19][cH:18]1>>[O:1]=[c:2]1[cH:3][cH:4][n:5](-[c:6]2[cH:7][cH:8][c:9](-[c:10]3[n:11][nH:12][c:13](=[O:14])[o:15]3)[cH:16][cH:17]2)[cH:18][cH:19]1
Nc1ccc(-c2n[nH]c(=O)o2)cc1.O=c1ccocc1
O=c1ccn(-c2ccc(-c3n[nH]c(=O)o3)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=c1ccn(-c2ccc(-c3n[nH]c(=O)o3)cc2)cc1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A mixture of 5-(4-aminophenyl)-1,3,4-oxadiazol-2(3H)-one (0.41 g), 4H-pyran-4-one (0.24 g), and hydrochloric acid (2N, 1.15 ml) in water (25 ml) was stirred under reflux for 3 hours to afford a yellow solid. This solid was added to hot water with stirring and the resulting suspension was made alkaline (pH 8) with aqueo...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
c1ccncc1.c1ccccc1.c1nnco1
HO-
O
null
null
Nc1ccc(-c2n[nH]c(=O)o2)cc1.O=c1ccocc1>O>O=c1ccn(-c2ccc(-c3n[nH]c(=O)o3)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1945fdf2a7b44ef385a20f3f04cdd9c1
C[C@@H]1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>>C[C@@H]1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
N.NC1=CC=C(C=C1)C=1[C@@H](CC(NN1)=O)C.O1C=CC(C=C1)=O.Cl>>C[C@@H]1CC(NN=C1C1=CC=C(C=C1)N1C=CC(C=C1)=O)=O
[CH3:1][C@@H:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12]([NH2:13])[cH:20][cH:21]1.o1[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]1>>[CH3:1][C@@H:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
C[C@@H]1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1
C[C@@H]1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A mixture of (R)-6-(4-aminophenyl)-5-methyl-4,5-dihydro-3(2H)-pyridazinone (100 mg), 4H-pyran-4-one (52 mg) and hydrochloric acid (0.1N, 1 ml) in water (1.3 ml) was stirred under reflux under nitrogen for 3 hours. Aqueous ammonia (880, 0.01 ml) was added to the cooled reaction mixture to afford the title compound which...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
C1=NNCCC1.c1ccccc1.c1ccncc1
HO-
O
null
null
C[C@@H]1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>O>C[C@@H]1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-99bfe2d0d774438586d35308dbb80cd3
C[C@H]1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>>C[C@H]1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
NC1=CC=C(C=C1)C=1[C@H](CC(NN1)=O)C.O1C=CC(C=C1)=O.Cl>>C[C@H]1CC(NN=C1C1=CC=C(C=C1)N1C=CC(C=C1)=O)=O
[CH3:1][C@H:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12]([NH2:13])[cH:20][cH:21]1.o1[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]1>>[CH3:1][C@H:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
C[C@H]1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1
C[C@H]1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
null
null
O
Miscellaneous
OtherReaction
820fdf5c7d90563efa4f0fcdced261f60cc5772161039256cfa8cd4dfa87d9f6
74f861e099b6420f2f6d4f3094b402eaca1d0baec018283dff42a39bacc23c31
O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
[NH2;D1;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[c:7]1:[c:8]:[c:9]:[cH;D2;+0:10]:o:[cH;D2;+0:11]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](-[n;H0;D3;+0:1]1:[cH;D2;+0:11]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1):[c:5]:[c:6]
null
[]
null
null
null
null
A mixture of (S)-6-(4-aminophenyl)-5-methyl-4,5-dihydro-3(2H)-pyridazinone (147 mg), 4H-pyran-4-one (78 mg) and hydrochloric acid (0.1N, 1.5 ml) in water (2 ml) was stirred under reflux under nitrogen for 3 hours. The reaction mixture was cooled to afford the title compound, which was collected, washed with water and d...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccocc1
c1ccncc1
C1=NNCCC1.c1ccccc1.c1ccncc1
HO-
O
null
null
C[C@H]1CC(=O)NN=C1c1ccc(N)cc1.O=c1ccocc1>O>C[C@H]1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6a06c5f7ca494a2a99419033715c3d96
CC(Cl)C(=O)Cl.Fc1ccccc1>>CC(Cl)C(=O)c1ccc(F)cc1
ClC(C(=O)Cl)C.[Cl-].[Cl-].[Cl-].[Al+3].FC1=CC=CC=C1>>ClC(C(=O)C1=CC=C(C=C1)F)C
Cl[C:4]([CH:2]([CH3:1])[Cl:3])=[O:5].[cH:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][cH:12]1>>[CH3:1][CH:2]([Cl:3])[C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][cH:12]1
CC(Cl)C(=O)Cl.Fc1ccccc1
CC(Cl)C(=O)c1ccc(F)cc1
null
null
ClCCl
C-C Coupling
Friedel-Crafts acylation
55541449ad4f182ef3dc0497085b282b1dcb76e0fb5ed140dc4eab4973eacb28
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[Cl;D1;H0:5].[c:6]:[c:7]:[cH;D2;+0:8]:[c:9]:[c:10]>>[C;D1;H3:4]-[C:3](-[Cl;D1;H0:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:8](:[c:7]:[c:6]):[c:9]:[c:10]
null
[]
null
null
10
MINUTE
A solution of 2-chloropropionyl chloride (49 ml) in dichloromethane (50 ml) was added to a mixture of anhydrous aluminium trichloride (55.5 g) in dichloromethane (120 ml). The mixture was stirred for 10 minutes at room temperature and then a solution of fluorobenzene (39.5 ml) in dichloromethane (30 ml) was added dropw...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HCl
ClCCl
null
0.166667
CC(Cl)C(=O)Cl.Fc1ccccc1>ClCCl>CC(Cl)C(=O)c1ccc(F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d092b65cc0c947de9cedeff753e34adf
CC(Cl)C(=O)c1ccc(F)cc1.CCOC(=O)CC(=O)OCC>>CCOC(=O)C(C(=O)OCC)C(C)C(=O)c1ccc(F)cc1
O.[H-].[Na+].C(CC(=O)OCC)(=O)OCC.ClC(C(=O)C1=CC=C(C=C1)F)C>>C(C)OC(=O)C(C(=O)OCC)C(C)C(C1=CC=C(C=C1)F)=O
Cl[CH:12]([CH3:13])[C:14](=[O:15])[c:16]1[cH:17][cH:18][c:19]([F:20])[cH:21][cH:22]1.[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7](=[O:8])[O:9][CH2:10][CH3:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([C:7](=[O:8])[O:9][CH2:10][CH3:11])[CH:12]([CH3:13])[C:14](=[O:15])[c:16]1[cH:17][cH:18][c:19]([F:20])[cH:21][cH:22]1
CC(Cl)C(=O)c1ccc(F)cc1.CCOC(=O)CC(=O)OCC
CCOC(=O)C(C(=O)OCC)C(C)C(=O)c1ccc(F)cc1
null
null
CN(C=O)C
C-C Coupling
OtherReaction
ddbfd093676894631592cc1860a2cf8bbaf94b988b30cd6f1e79f06ccf4b2a83
ee836fe12c6e6643596973ababf2df399dc694362c1c015f4160fe4381ae5166
c1ccccc1
Cl-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3](=[O;D1;H0:4])-[c:5].[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH2;D2;+0:10]-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]>>[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH;D3;+0:10](-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14])-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3](=[O;D1;H0:4])-[c:5]
null
[]
null
null
2
HOUR
Sodium hydride (50% oil dispersion, 3.5 g) was added with caution to a cooled solution of diethyl malonate (11.85 ml) in dimethylformamide (10 ml). The reaction mixture was stirred at room temperature for 30 minutes before a solution of 2-chloro-1-(4-fluorophenyl)-1-propanone (12.13 g) in dimethylformamide (50 ml) was ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ketone.Ester.Ester
Ketone.Ester.Ester
null
null
c1ccccc1
HCl
CN(C=O)C
null
2
CC(Cl)C(=O)c1ccc(F)cc1.CCOC(=O)CC(=O)OCC>CN(C=O)C>CCOC(=O)C(C(=O)OCC)C(C)C(=O)c1ccc(F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-25e67d7e720b442a8e013d9e9df27485
CC(CC(=O)O)C(=O)c1ccc(F)cc1.Oc1ccncc1>>CC(CC(=O)O)C(=O)c1ccc(-n2ccc(=O)cc2)cc1
Cl.FC1=CC=C(C(=O)C(CC(=O)O)C)C=C1.OC1=CC=NC=C1.[OH-].[Na+]>>O=C1C=CN(C=C1)C1=CC=C(C(=O)C(CC(=O)O)C)C=C1
F[c:12]1[cH:11][cH:10][c:9]([C:7]([CH:2]([CH3:1])[CH2:3][C:4](=[O:5])[OH:6])=[O:8])[cH:21][cH:20]1.[n:13]1[cH:14][cH:15][c:16]([OH:17])[cH:18][cH:19]1>>[CH3:1][CH:2]([CH2:3][C:4](=[O:5])[OH:6])[C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
CC(CC(=O)O)C(=O)c1ccc(F)cc1.Oc1ccncc1
CC(CC(=O)O)C(=O)c1ccc(-n2ccc(=O)cc2)cc1
null
null
O
Acylation
OtherReaction
4308b383a3710ca54de2d883c53ac81bae07d58b1e4603761dc4ccecde83005c
9fb0a4734c628f8028aa0d8a5f3520861ccd6e9f72791fbc28874467838ebc37
O=c1ccn(-c2ccccc2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[OH;D1;+0:6]-[c;H0;D3;+0:7]1:[c:8]:[c:9]:[n;H0;D2;+0:10]:[c:11]:[c:12]:1>>[O;H0;D1;+0:6]=[c;H0;D3;+0:7]1:[c:8]:[c:9]:[n;H0;D3;+0:10](-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]):[c:11]:[c:12]:1
null
[]
null
null
null
null
A solution of 3-(4-fluorobenzoyl)butanoic acid (8 g), 4-hydroxypridine (8 g) and sodium hydroxide (4.6 g) in water (80 ml) was heated in an autoclave at 140° C. for 20 hours. The reaction mixture was cooled and on acidification to pH3 with dilute hydrochloric acid afforded as a white crystalline precipitate 3-[4-(4-oxo...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol
null
c1ccccc1.c1ccncc1
c1ccccc1.c1ccncc1
c1ccccc1.c1ccncc1
HF
O
null
null
CC(CC(=O)O)C(=O)c1ccc(F)cc1.Oc1ccncc1>O>CC(CC(=O)O)C(=O)c1ccc(-n2ccc(=O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9082b80c2ce84f57abe9c9a2c56ec958
CC(CC(=O)O)C(=O)c1ccc(-n2ccc(=O)cc2)cc1.NN>>CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
O.NN.O=C1C=CN(C=C1)C1=CC=C(C(=O)C(CC(=O)O)C)C=C1>>CC1CC(NN=C1C1=CC=C(C=C1)N1C=CC(C=C1)=O)=O
O=[C:8]([CH:2]([CH3:1])[CH2:3][C:4](O)=[O:5])[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1.[NH2:6][NH2:7]>>[CH3:1][CH:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
CC(CC(=O)O)C(=O)c1ccc(-n2ccc(=O)cc2)cc1.NN
CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
null
null
O
Acylation
OtherReaction
16e715242dd5e92f711d46176c552652cef6c6f4fed9bc9a09a311d5b0b86cea
30de68c4dde17a0553a43eee47b1b865b8390bb08557512a59e6e71e0ed0ad51
O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[C;D1;H3:5])-[C;H0;D3;+0:6](=O)-[c:7](:[c:8]):[c:9].[NH2;D1;+0:10]-[NH2;D1;+0:11]>>[C;D1;H3:5]-[C:4]1-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[N;H0;D2;+0:11]=[C;H0;D3;+0:6]-1-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
Hydrazine hydrate (1.8 g) was added to a suspension of 3-[4-(4-oxo-1,4-dihydropyridin-1-yl)benzoyl]butanoic acid (5 g) in water (60 ml). The resulting solution was stirred under reflux for 2 hours and cooled to afford the title compound as a pale yellow solid, 4.45 g, m.p. 255°-258° C. Conditions: See reaction.notes.pr...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid.Ketone
Hydrazone amide
null
C1=NNCCC1
C1=NNCCC1.c1ccccc1.c1ccncc1
HO-
O
null
null
CC(CC(=O)O)C(=O)c1ccc(-n2ccc(=O)cc2)cc1.NN>O>CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c82a189b0657442b9a6978acdd19952a
CC1CC(=O)NN=C1c1ccc(N)cc1.CN(C)C=CC(=O)C=CN(C)C>>CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
Cl.NC1=CC=C(C=C1)C=1C(CC(NN1)=O)C.CN(C=CC(C=CN(C)C)=O)C.Cl>>CC1CC(NN=C1C1=CC=C(C=C1)N1C=CC(C=C1)=O)=O
[CH3:1][CH:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12]([NH2:13])[cH:20][cH:21]1.CN(C)[CH:14]=[CH:15][C:16](=[O:17])[CH:18]=[CH:19]N(C)C>>[CH3:1][CH:2]1[CH2:3][C:4](=[O:5])[NH:6][N:7]=[C:8]1[c:9]1[cH:10][cH:11][c:12](-[n:13]2[cH:14][cH:15][c:16](=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
CC1CC(=O)NN=C1c1ccc(N)cc1.CN(C)C=CC(=O)C=CN(C)C
CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
d7fdb9b56dbbdcfbb3cd6327379e4f0b769c4b1fbcc6777beb6ca87209d9f4f3
0e3cef2991b5837f847176871737a49d675b557a92368f3fc16324e7aa459279
O=C1CCC(c2ccc(-n3ccc(=O)cc3)cc2)=NN1
C-N(-C)-[CH;D2;+0:1]=[CH;D2;+0:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[CH;D2;+0:5]=[CH;D2;+0:6]-N(-C)-C.[NH2;D1;+0:7]-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]>>[O;D1;H0:4]=[c;H0;D3;+0:3]1:[cH;D2;+0:2]:[cH;D2;+0:1]:[n;H0;D3;+0:7](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]):[cH;D2;+0:6]:[cH;D2;+0:5]:1
null
[]
null
null
4
HOUR
A mixture of 6-(4-aminophenyl)-5-methyl-4,5-dihydro-3(2H)-pyridazinone (101 mg), 1,5-bis(dimethylamino)-1,4-pentadien-3-one (84 mg) and hydrochloric acid (1N, 0.5 ml) in water (1.5 ml) was stirred at room temperature for 4 hours. More hydrochloric acid (1N, 0.5 ml) was added and the reaction mixture was stirred at room...
10.6084/m9.figshare.5104873.v1
null
Enamine.Enamine.Ketone.Primary amine
null
null
c1ccncc1
C1=NNCCC1.c1ccccc1.c1ccncc1
Other
O
null
4
CC1CC(=O)NN=C1c1ccc(N)cc1.CN(C)C=CC(=O)C=CN(C)C>O>CC1CC(=O)NN=C1c1ccc(-n2ccc(=O)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9399f232cbbb4b3389dd35141f07ec6e
CN(C)OC(=O)c1c(O)cccc1-c1cc[nH]n1.COc1cc(OC)nc(S(C)(=O)=O)n1>>COc1cc(OC)nc(Oc2cccc(-c3cc[nH]n3)c2C(=O)ON(C)C)n1
P(O)(O)(O)=O.[H-].[Na+].N1N=C(C=C1)C=1C(=C(C=CC1)O)C(=O)ON(C)C.CS(=O)(=O)C1=NC(=CC(=N1)OC)OC>>N1N=C(C=C1)C1=CC=CC(=C1C(=O)ON(C)C)OC1=NC(=CC(=N1)OC)OC
[OH:10][c:11]1[cH:12][cH:13][cH:14][c:15](-[c:16]2[cH:17][cH:18][nH:19][n:20]2)[c:21]1[C:22](=[O:23])[O:24][N:25]([CH3:26])[CH3:27].CS(=O)(=O)[c:9]1[n:8][c:5]([O:6][CH3:7])[cH:4][c:3]([O:2][CH3:1])[n:28]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[n:8][c:9]([O:10][c:11]2[cH:12][cH:13][cH:14][c:15](-[c:16]3[cH:17][cH:...
CN(C)OC(=O)c1c(O)cccc1-c1cc[nH]n1.COc1cc(OC)nc(S(C)(=O)=O)n1
COc1cc(OC)nc(Oc2cccc(-c3cc[nH]n3)c2C(=O)ON(C)C)n1
null
null
CN(C=O)C.O.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
1c345af4a3df0f977c6c030350153f590996fc7a2b6ceaf9fe6cff27648ed228
5df75ac15caf6173d8206dd70d45a57321a6ccb2169690bfa04f02c58252d4f1
c1cnc(Oc2cccc(-c3cc[nH]n3)c2)nc1
C-S(=O)(=O)-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5].[#8:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10](-[OH;D1;+0:11]):[c:12]>>[#8:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10](-[O;H0;D2;+0:11]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5]):[c:12]
null
[]
30
CELSIUS
3
HOUR
At 10° C., 0.30 g (0.01 mol) of sodium hydride (80% strength) is added to a solution of 2.47 g (10 mmol) of 3-pyrazolyl-2-(N,N-dimethylaminooxycarbonyl)-phenol in 25 ml of anhydrous dimethylformamide, and the reaction mixture is stirred for 3 hours at 30° C. 2.18 g (0.01 mol) of 2-methylsulfonyl-4,6-dimethoxypyrimidine...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Sulfone
Ether
c1cncnc1
c1cncnc1
c1cncnc1.c1ccccc1.c1cn[nH]c1
HO-
CN(C=O)C.O.C(C)(=O)OCC
30
3
CN(C)OC(=O)c1c(O)cccc1-c1cc[nH]n1.COc1cc(OC)nc(S(C)(=O)=O)n1>CN(C=O)C.O.C(C)(=O)OCC>COc1cc(OC)nc(Oc2cccc(-c3cc[nH]n3)c2C(=O)ON(C)C)n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-876c69db2b8146499f39252eada8512a
CON1CN(Cl)CN(OC)C1.O=C(O)c1c(O)cccc1-c1ncc[nH]1.On1cccn1>>CON1CN(OC)CN(Oc2cccc(-c3ncc[nH]3)c2C(=O)On2cccn2)C1
[H-].[Na+].P(O)(O)(O)=O.N1C(=NC=C1)C=1C=CC=C(C1C(=O)O)O.ClN1CN(CN(C1)OC)OC.ON1N=CC=C1>>N1C(=NC=C1)C1=CC=CC(=C1C(=O)ON1N=CC=C1)ON1CN(CN(C1)OC)OC
Cl[N:9]1[CH2:8][N:5]([O:6][CH3:7])[CH2:4][N:3]([O:2][CH3:1])[CH2:30]1.O[C:22]([c:21]1[c:11]([OH:10])[cH:12][cH:13][cH:14][c:15]1-[c:16]1[n:17][cH:18][cH:19][nH:20]1)=[O:23].[OH:24][n:25]1[cH:26][cH:27][cH:28][n:29]1>>[CH3:1][O:2][N:3]1[CH2:4][N:5]([O:6][CH3:7])[CH2:8][N:9]([O:10][c:11]2[cH:12][cH:13][cH:14][c:15](-[c:1...
CON1CN(Cl)CN(OC)C1.O=C(O)c1c(O)cccc1-c1ncc[nH]1.On1cccn1
CON1CN(OC)CN(Oc2cccc(-c3ncc[nH]3)c2C(=O)On2cccn2)C1
null
null
O1CCCC1
Acylation
OtherReaction
08455edd162739111984b8a1914303a6c0284315761e8cf3e5624a1ddcc7dbe0
f4525ecd0571b2e0c099853d5f1894c98844f63a04a7bcf4433c9de4b57a1c02
O=C(On1cccn1)c1c(ON2CNCNC2)cccc1-c1ncc[nH]1
Cl-[N;H0;D3;+0:1]1-[C:2]-[#7:3](-[#8:4])-[C:5]-[#7:6](-[#8:7])-[C:8]-1.O-[C;H0;D3;+0:9](=[O;D1;H0:10])-[c:11](:[c:12]):[c:13](-[OH;D1;+0:14]):[c:15].[#7;a:16]:[#7;a:17](-[OH;D1;+0:18]):[c:19]>>[#7;a:16]:[#7;a:17](-[O;H0;D2;+0:18]-[C;H0;D3;+0:9](=[O;D1;H0:10])-[c:11](:[c:12]):[c:13](-[O;H0;D2;+0:14]-[N;H0;D3;+0:1]1-[C:2...
null
[]
null
null
30
MINUTE
1.75 g (10.8 mmol) of N,N'-carbonylbisimidazole is added to a solution of 1.88 g (10 mmol) of 6-imidazolylsalicylic acid in 30 ml of tetrahydrofuran. After the mixture has been stirred for 30 minutes at room temperature, 9.9 mmol of N-hydroxypyrazole is added and the mixture is stirred for a further 14 hours. The react...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol.Tertiary amine
Tertiary amine
C1[NH]C[NH]C[NH]1
C1[NH]C[NH]C[NH]1
C1[NH]C[NH]C[NH]1.c1ccccc1.c1c[nH]cn1.c1cn[nH]c1
HCl
O1CCCC1
null
0.5
CON1CN(Cl)CN(OC)C1.O=C(O)c1c(O)cccc1-c1ncc[nH]1.On1cccn1>O1CCCC1>CON1CN(OC)CN(Oc2cccc(-c3ncc[nH]3)c2C(=O)On2cccn2)C1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-774ce888c2ae4a3eb24f6b6510e760c5
Clc1cnc2ccccc2n1.[SH-]>>Sc1cnc2ccccc2n1
ClC1=NC2=CC=CC=C2N=C1.[SH-].[Na+]>>SC1=NC2=CC=CC=C2N=C1
Cl[c:2]1[cH:3][n:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11]1.[SH-:1]>>[SH:1][c:2]1[cH:3][n:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[n:11]1
Clc1cnc2ccccc2n1.[SH-]
Sc1cnc2ccccc2n1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
618526068c98548f3e33251e238323468f68913857bd4da8b171e44c07719770
5acfc94bcb91f90cc14ddd9f791d64cf2f45381ebe181eac63cc3d2843bb00cd
c1ccc2nccnc2c1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1.[SH-;D0:7]>>[SH;D1;+0:7]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1
157.3
[{"value": 157.3, "product": "SC1=NC2=CC=CC=C2N=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
3
HOUR
2-Chloroquinoxaline (2 g) and sodium hydrosulphide (1.23 g) were stirred together in 25 ml of dimethylformamide and heated to 100° C. After 3 hours the reaction mixture was allowed to cool and then partitioned between 70 ml of water and 30 ml of ethyl acetate. The organic layer was separated and the aqueous layer extra...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Aromatic thiol
c1ccc2nccnc2c1
c1ccc2nccnc2c1
c1ccc2nccnc2c1
Other
CN(C=O)C
100
3
Clc1cnc2ccccc2n1.[SH-]>CN(C=O)C>Sc1cnc2ccccc2n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7070d8bc971546909aeafe6e08288d5c
Cc1nc2ccccc2nc1O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>Cc1nc2ccccc2nc1S
OC1=NC2=CC=CC=C2N=C1C.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>SC1=NC2=CC=CC=C2N=C1C
O[c:11]1[c:2]([CH3:1])[n:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[n:10]1.S=P12SP3(=S)SP(=S)(S1)SP(=[S:12])(S2)S3>>[CH3:1][c:2]1[n:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[n:10][c:11]1[SH:12]
Cc1nc2ccccc2nc1O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
Cc1nc2ccccc2nc1S
null
null
N1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
6b70c18a601c3d520a3f9bcb8a7122f0554a354c356ace9bcfabb77b02d4a672
5064cd713f52475d9702bad414c4e5aaac7fac3150d286577c363bca18bdbe15
c1ccc2nccnc2c1
O-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1-[C;D1;H3:7].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:8])(-S-2)-S-3>>[C;D1;H3:7]-[c:6]1:[#7;a:5]:[c:4]:[c:3]:[#7;a:2]:[c;H0;D3;+0:1]:1-[SH;D1;+0:8]
null
[]
null
null
null
null
2-Hydroxy-3-methylquinoxaline (2 g) and phosphorus pentasulphide (3.05 g) were stirred together in 40 ml of pyridine and the reaction mixture heated to reflux. Conditions: See reaction.notes.procedure_details. Workup: the reaction mixture heated to reflux
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Aromatic thiol
c1ccc2nccnc2c1.S1P2SP3SP1SP(S2)S3
c1ccc2nccnc2c1
c1ccc2nccnc2c1
Other
N1=CC=CC=C1
null
null
Cc1nc2ccccc2nc1O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>N1=CC=CC=C1>Cc1nc2ccccc2nc1S
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d5edec4fc25d4165a206856d008fcc0a
CCOC(=O)CBr.Nc1ccc(F)cc1>>CCN(CC(=O)O)c1ccc(F)cc1
FC1=CC=C(N)C=C1.C([O-])([O-])=O.[K+].[K+].C1COCCOCCOCCOCCOCCO1.C(C)OC(CBr)=O>>C(C)N(CC(=O)O)C1=CC=C(C=C1)F
Br[CH2:4][C:5](=[O:6])[O:7][CH2:2][CH3:1].[NH2:3][c:8]1[cH:9][cH:10][c:11]([F:12])[cH:13][cH:14]1>>[CH3:1][CH2:2][N:3]([CH2:4][C:5](=[O:6])[OH:7])[c:8]1[cH:9][cH:10][c:11]([F:12])[cH:13][cH:14]1
CCOC(=O)CBr.Nc1ccc(F)cc1
CCN(CC(=O)O)c1ccc(F)cc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
3d32c7244697cf6aa13f97f5b44e896f7d6e28dca4be367d4c8a70a634f7354e
8557e77f434d58647556c853429bbd1304f785e81ed25dd3b19413e60d2746ad
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[CH2;D2;+0:5]-[C;D1;H3:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H3:6]-[CH2;D2;+0:5]-[N;H0;D3;+0:7](-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4])-[c:8](:[c:9]):[c:10]
null
[]
null
null
null
null
4-Fluoroaniline (5 g), potassium carbonate (3.11 g) and a catalytic amount of 18-Crown-6 were stirred together in 50 ml of ethanol. A solution of ethylbromoacetate (7.52 g) in 25 ml of ethanol was added dropwise and the reaction was heated to reflux. Conditions: See reaction.notes.procedure_details. Workup: the reactio...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Primary amine
Carboxylic acid.Tertiary amine
null
null
c1ccccc1
HBr
C(C)O
null
null
CCOC(=O)CBr.Nc1ccc(F)cc1>C(C)O>CCN(CC(=O)O)c1ccc(F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a3390456313144aa978257dac6d1ec7e
CS(=O)(=O)c1nc(N)n2nc(-c3ccco3)nc2n1.Nc1nc(NCCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12>>Nc1nc(NCCc2ccc(Oc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc2nc(-c3ccco3)nn12
C(Cl)Cl.CO.NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)NCCC2=CC=C(C=C2)O.N12CCCCCC2=NCCC1.NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)S(=O)(=O)C>>NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)OC2=CC=C(C=C2)CCNC2=NC=1N(C(=N2)N)N=C(N1)C=1OC=CC1
CS(=O)(=O)[c:13]1[n:14][c:15]([NH2:16])[n:17]2[n:18][c:19](-[c:20]3[cH:21][cH:22][cH:23][o:24]3)[n:25][c:26]2[n:27]1.[NH2:1][c:2]1[n:3][c:4]([NH:5][CH2:6][CH2:7][c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:28][cH:29]2)[n:30][c:31]2[n:32][c:33](-[c:34]3[cH:35][cH:36][cH:37][o:38]3)[n:39][n:40]12>>[NH2:1][c:2]1[n:3][c:4]([NH:5]...
CS(=O)(=O)c1nc(N)n2nc(-c3ccco3)nc2n1.Nc1nc(NCCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12
Nc1nc(NCCc2ccc(Oc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc2nc(-c3ccco3)nn12
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
4f28b727ad8941dcd3a706875a7132829b3fbbba254eec3154abc670bf3ca2d6
5df75ac15caf6173d8206dd70d45a57321a6ccb2169690bfa04f02c58252d4f1
c1coc(-c2nc3nc(NCCc4ccc(Oc5ncn6nc(-c7ccco7)nc6n5)cc4)ncn3n2)c1
C-S(=O)(=O)-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]2:[#7;a:5]:[c:6]:[#7;a:7]:[c:8]:2:[#7;a:9]:1.[OH;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[c:12]:[c:11](-[O;H0;D2;+0:10]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]2:[#7;a:5]:[c:6]:[#7;a:7]:[c:8]:2:[#7;a:9]:1):[c:13]
null
[]
null
null
null
null
7-amino-2-(2-furyl)-5-[2-(4-hydroxyphenyl)ethyl]amino[1,2,4]-triazolo[1,5-a][1,3,5]triazine (0.91 g) and 1,8-diazabicyclo[5,4,0]undec-7-ene (DBU, 0.37 ml) were added to a suspension of 7-amino-2-(2-furyl)-5-methylsulphonyl-[1,2,4]triazolo[1,5-a][1,3,5]triazine (0.82 g) in acetonitrile (50 ml) and the resulting mixture ...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Sulfone
Ether
c1ncn2ncnc2n1
c1ncn2ncnc2n1
c1ccccc1.c1ncn2ncnc2n1.c1ccoc1.c1ncn2ncnc2n1.c1ccoc1
HO-
C(C)#N
null
null
CS(=O)(=O)c1nc(N)n2nc(-c3ccco3)nc2n1.Nc1nc(NCCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12>C(C)#N>Nc1nc(NCCc2ccc(Oc3nc(N)n4nc(-c5ccco5)nc4n3)cc2)nc2nc(-c3ccco3)nn12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-263a470489eb4f31aa2b7a9416d2c743
CSC(=NC#N)SC.Nc1n[nH]c(-c2ccco2)n1>>CSc1nc(N)n2nc(-c3ccco3)nc2n1
NC1=NNC(=N1)C=1OC=CC1.CSC(=NC#N)SC>>NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)SC
CS[C:3]([S:2][CH3:1])=[N:4][C:5]#[N:6].[n:7]1[nH:8][c:9](-[c:10]2[cH:11][cH:12][cH:13][o:14]2)[n:15][c:16]1[NH2:17]>>[CH3:1][S:2][c:3]1[n:4][c:5]([NH2:6])[n:7]2[n:8][c:9](-[c:10]3[cH:11][cH:12][cH:13][o:14]3)[n:15][c:16]2[n:17]1
CSC(=NC#N)SC.Nc1n[nH]c(-c2ccco2)n1
CSc1nc(N)n2nc(-c3ccco3)nc2n1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
566500fbfb455ebdfa23274308e3d530174cbc8eff3f50b1f36552a70387f76f
81955634976ddffb98b1dc0b18f40adc0b0fe8c65fec77cb19d2966e57d60ed0
c1coc(-c2nc3ncncn3n2)c1
C-S-[C;H0;D3;+0:1](-[#16:2]-[C;D1;H3:3])=[N;H0;D2;+0:4]-[C;H0;D2;+0:5]#[N;H0;D1;+0:6].[#8;a:7]:[c:8]-[c:9]1:[#7;a:10]:[c:11](-[NH2;D1;+0:12]):[n;H0;D2;+0:13]:[nH;D2;+0:14]:1>>[#8;a:7]:[c:8]-[c:9]1:[#7;a:10]:[c:11]2:[n;H0;D2;+0:12]:[c;H0;D3;+0:1](-[#16:2]-[C;D1;H3:3]):[n;H0;D2;+0:4]:[c;H0;D3;+0:5](-[NH2;D1;+0:6]):[n;H0;...
20.3
[{"value": 20.3, "product": "NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)SC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
170
CELSIUS
null
null
An intimate mixture of 3-amino-5-(2-furyl)-1,2,4-triazole (33.0 g) and dimethyl N-cyanodithioiminocarbonate (33.0 g) was heated at 170° C. for 1 hour, under a slow stream of argon. After cooling, the resulting solid was purified by column chromatography on silica (600 g) eluting with an increasing amount of ethyl aceta...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary amine.Monosulfide.Monosulfide
Primary amine.Monosulfide
c1nc[nH]n1
c1ncn2ncnc2n1
c1ncn2ncnc2n1.c1ccoc1
Other
null
170
null
CSC(=NC#N)SC.Nc1n[nH]c(-c2ccco2)n1>>CSc1nc(N)n2nc(-c3ccco3)nc2n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-77c7e60be0494129bd4ab11177e4baf3
Nc1nc(NCc2ccc(OCc3ccccc3)cc2)nc2nc(-c3ccco3)nn12>>Nc1nc(NCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12
NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)NCC2=CC=C(C=C2)OCC2=CC=CC=C2>>NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)NCC2=CC=C(C=C2)O
c1ccc(C[O:11][c:10]2[cH:9][cH:8][c:7]([CH2:6][NH:5][c:4]3[n:3][c:2]([NH2:1])[n:24]4[c:15]([n:14]3)[n:16][c:17](-[c:18]3[cH:19][cH:20][cH:21][o:22]3)[n:23]4)[cH:13][cH:12]2)cc1>>[NH2:1][c:2]1[n:3][c:4]([NH:5][CH2:6][c:7]2[cH:8][cH:9][c:10]([OH:11])[cH:12][cH:13]2)[n:14][c:15]2[n:16][c:17](-[c:18]3[cH:19][cH:20][cH:21][o...
Nc1nc(NCc2ccc(OCc3ccccc3)cc2)nc2nc(-c3ccco3)nn12
Nc1nc(NCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12
null
[Pd]
CO.C(C)(=O)OCC
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc(CNc2ncn3nc(-c4ccco4)nc3n2)cc1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
null
[]
null
null
null
null
A solution of 7-amino-5-[(4-benzyloxyphenyl)methyl]amino-2-(2-furyl)-[1,2,4]triazolo[1,5-a][1,3,5]triazine (2.37 g) in ethyl acetate (150 ml) and methanol (150 ml) was treated with 10% palladium on carbon (3.0 g) and hydrogenated at atmospheric pressure for 2.5 hours. The catalyst was filtered through diatomaceous eart...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccccc1.c1ncn2ncnc2n1.c1ccoc1
Other
[Pd].CO.C(C)(=O)OCC
null
null
Nc1nc(NCc2ccc(OCc3ccccc3)cc2)nc2nc(-c3ccco3)nn12>[Pd].CO.C(C)(=O)OCC>Nc1nc(NCc2ccc(O)cc2)nc2nc(-c3ccco3)nn12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b75301676eb1424c9eacfe2ac252c8f5
Nc1nc(NCCc2ccccc2OCc2ccccc2)nc2nc(-c3ccco3)nn12>>Nc1nc(NCCc2ccccc2O)nc2nc(-c3ccco3)nn12
NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)NCCC2=C(C=CC=C2)OCC2=CC=CC=C2.[H][H]>>NC1=NC(=NC=2N1N=C(N2)C=2OC=CC2)NCCC2=C(C=CC=C2)O
c1ccc(C[O:14][c:13]2[c:8]([CH2:7][CH2:6][NH:5][c:4]3[n:3][c:2]([NH2:1])[n:25]4[c:16]([n:15]3)[n:17][c:18](-[c:19]3[cH:20][cH:21][cH:22][o:23]3)[n:24]4)[cH:9][cH:10][cH:11][cH:12]2)cc1>>[NH2:1][c:2]1[n:3][c:4]([NH:5][CH2:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[OH:14])[n:15][c:16]2[n:17][c:18](-[c:19]3[cH:20][c...
Nc1nc(NCCc2ccccc2OCc2ccccc2)nc2nc(-c3ccco3)nn12
Nc1nc(NCCc2ccccc2O)nc2nc(-c3ccco3)nn12
null
[Pd]
CO
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc(CCNc2ncn3nc(-c4ccco4)nc3n2)cc1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
null
[]
null
null
null
null
A solution of the product of step (1) (0.9g) in methanol (150 ml) was hydrogenated at room-temperature and pressure using 10% palladium on carbon (0.9 g) catalyst. After the uptake of hydrogen was complete, the catalyst was filtered off and the solvent evaporated. The residue was crystallised from ethanol, and gave 7-a...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccccc1.c1ncn2ncnc2n1.c1ccoc1
Other
[Pd].CO
null
null
Nc1nc(NCCc2ccccc2OCc2ccccc2)nc2nc(-c3ccco3)nn12>[Pd].CO>Nc1nc(NCCc2ccccc2O)nc2nc(-c3ccco3)nn12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ac2c06d7cbfb4525b6d01a68903c4d4b
O=C1Nc2ccccc2SC1c1ccc(F)cc1>>Fc1ccc(C2CNc3ccccc3S2)cc1
FC1=CC=C(C=C1)C1SC2=C(NC1=O)C=CC=C2.[BH4-].[Na+].C([O-])([O-])=O.[K+].[K+].Cl>>FC1=CC=C(C=C1)C1SC2=C(NC1)C=CC=C2
O=[C:7]1[CH:6]([c:5]2[cH:4][cH:3][c:2]([F:1])[cH:17][cH:16]2)[S:15][c:14]2[c:9]([cH:10][cH:11][cH:12][cH:13]2)[NH:8]1>>[F:1][c:2]1[cH:3][cH:4][c:5]([CH:6]2[CH2:7][NH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[S:15]2)[cH:16][cH:17]1
O=C1Nc2ccccc2SC1c1ccc(F)cc1
Fc1ccc(C2CNc3ccccc3S2)cc1
null
null
O1CCCC1
Reduction
Reduction of secondary amides to amines
1dcd93b688ffb5a97304eaeb9d3e97c68c92ef37b3351d43b5078fead2422b3b
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(C2CNc3ccccc3S2)cc1
O=[C;H0;D3;+0:1]1-[#7:2]-[c:3]:[c:4]-[#16:5]-[C:6]-1-[c:7]>>[c:7]-[C:6]1-[#16:5]-[c:4]:[c:3]-[#7:2]-[CH2;D2;+0:1]-1
91.2
[{"value": 91.0, "product": "FC1=CC=C(C=C1)C1SC2=C(NC1)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.2, "product": "FC1=CC=C(C=C1)C1SC2=C(NC1)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 2-(4-fluorophenyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazine (4.0 g), sodium borohydride (2.91 g) and tetrahydrofuran (100 ml) is added dropwise with stirring boron trifluoride etherate complex (12. 5 ml) at room temperature, and the mixture is refluxed for 1.5 hour. After cooling, to the mixture is added ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
c1ccc2c(c1)NCCS2
c1ccc2c(c1)NCCS2
c1ccccc1.c1ccc2c(c1)NCCS2
Other
O1CCCC1
null
null
O=C1Nc2ccccc2SC1c1ccc(F)cc1>O1CCCC1>Fc1ccc(C2CNc3ccccc3S2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d89b6b0a42ba47e2b52fd965ff8e6b9b
C=CC(=O)Cl.Clc1ccc(C2CNc3ccccc3S2)cc1>>C=CC(=O)N1CC(c2ccc(Cl)cc2)Sc2ccccc21
C(C=C)(=O)Cl.ClC1=CC=C(C=C1)C1SC2=C(NC1)C=CC=C2.C(O)([O-])=O.[Na+].O>>ClC1=CC=C(C=C1)C1SC2=C(N(C1)C(C=C)=O)C=CC=C2
Cl[C:3]([CH:2]=[CH2:1])=[O:4].[NH:5]1[CH2:6][CH:7]([c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]2)[S:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]21>>[CH2:1]=[CH:2][C:3](=[O:4])[N:5]1[CH2:6][CH:7]([c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]2)[S:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]21
C=CC(=O)Cl.Clc1ccc(C2CNc3ccccc3S2)cc1
C=CC(=O)N1CC(c2ccc(Cl)cc2)Sc2ccccc21
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
4ce9986a2e7f31aa9eaa0925622c2cb2cd91fbaa9d58585e0420c051b9143356
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
c1ccc(C2CNc3ccccc3S2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4].[c:5]:[c:6]1:[c:7]-[#16:8]-[C:9]-[C:10]-[NH;D2;+0:11]-1>>[C;D1;H2:4]=[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:11]1-[C:10]-[C:9]-[#16:8]-[c:7]:[c:6]-1:[c:5]
93
[{"value": 93.0, "product": "ClC1=CC=C(C=C1)C1SC2=C(N(C1)C(C=C)=O)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.7, "product": "ClC1=CC=C(C=C1)C1SC2=C(N(C1)C(C=C)=O)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a mixture of 2-(4-chlorophenyl)-3,4-dihydro-2H-1,4-benzothiazine (9.62 g), sodium hydrogen carbonate (6.0 g), methylene chloride (100 ml) and water (50 ml) is added dropwise with stirring a solution of acryloyl chloride (5.0 g) in methylene chloride (20 ml) under ice cooling over a period of about 30 minutes. The mi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
c1ccc2c(c1)NCCS2
c1ccc2c(c1)[NH]CCS2
c1ccccc1.c1ccc2c(c1)[NH]CCS2
HCl
C(Cl)Cl
null
3
C=CC(=O)Cl.Clc1ccc(C2CNc3ccccc3S2)cc1>C(Cl)Cl>C=CC(=O)N1CC(c2ccc(Cl)cc2)Sc2ccccc21