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-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b17219fcebd74ae7ac99426fccd85e3c
Nc1ccc(Cl)c(Cl)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1ccc(Cl)c(Cl)c1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(Cl)c(Cl)c1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.ClC=1C=C(N)C=CC1Cl>>ClC=1C=C(C=CC1Cl)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=C(C=C2)Cl)Cl)C=CC=C1)=O
[NH2:3][c:4]1[cH:5][cH:6][c:7]([Cl:8])[c:9]([Cl:10])[cH:11]1.[O:1]=[C:2]([c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18][S:19][c:20]1[cH:21][cH:22][cH:23][cH:24][c:25]1[C:26](=[O:27])[Cl:33])[Cl:35]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([Cl:8])[c:9]([Cl:10])[cH:11]1)[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18...
Nc1ccc(Cl)c(Cl)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1ccc(Cl)c(Cl)c1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(Cl)c(Cl)c1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
2f235573ea2831a0bfc0ca6a7a1d25e86fe9750de044d017cedf9966e87994b8
152f5a74588b671b90d31333a44ad79a10117acd8e5ede06fca5e8c644a4e2e7
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[Cl;H0;D1;+0:7]-[C;H0;D3;+0:8](=[O;D1;H0:9])-[c:10](:[c:11]):[c:12].[NH2;D1;+0:13]-[c:14](:[c:15]):[c:16]>>[Cl;H0;D1;+0:1]-[c:17](:[c:18]):[c:19](-[Cl;H0;D1;+0:7]):[c:20]:[c:21]-[#7:22]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[O;D1;H0:9]=[C;H0;D3...
10.2
[{"value": 10.2, "product": "ClC=1C=C(C=CC1Cl)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=C(C=C2)Cl)Cl)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (1.04 g, 3.03 mmol) in 25 mL of dichloromethane and 3,4-dichloroaniline (0.982 g, 6.06 mmol) in 8 mL of pyridine. The crude product was recrystallized from ethyl acetate-hexanes to yield 0.184 g of the title co...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Aromatic halide.Aromatic halide.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
ClCCl.N1=CC=CC=C1
null
null
Nc1ccc(Cl)c(Cl)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1ccc(Cl)c(Cl)c1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(Cl)c(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a52bb8c1753c453fa00de43f77a5ce8a
Nc1ccc(Cl)cc1Cl.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1ccc(Cl)cc1Cl)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(Cl)cc1Cl
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.ClC1=C(N)C=CC(=C1)Cl>>ClC1=C(C=CC(=C1)Cl)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=C(C=C2)Cl)Cl)C=CC=C1)=O
[NH2:3][c:4]1[cH:5][cH:6][c:7]([Cl:8])[cH:34][c:35]1[Cl:36].[O:1]=[C:2]([Cl:11])[c:12]1[cH:13][cH:14][cH:9][cH:16][c:17]1[S:18][S:19][c:20]1[cH:21][cH:22][cH:23][cH:24][c:25]1[C:26](=[O:27])[Cl:33]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([Cl:8])[cH:9][c:10]1[Cl:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18][S:...
Nc1ccc(Cl)cc1Cl.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1ccc(Cl)cc1Cl)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(Cl)cc1Cl
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
08f6fd1cc318cdb2fa23c9eb29a97032bbce3d4ed3ae3fdc6be78ee7a60521f7
ff709637114d139dc59366a7fc358c91f087a54b59bfe5b228e07ff4c733add3
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
[#16:1]-[c:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c:6]:[c:7]:1-[C;H0;D3;+0:8](-[Cl;H0;D1;+0:9])=[O;D1;H0:10].[Cl;H0;D1;+0:11]-[C;H0;D3;+0:12](=[O;D1;H0:13])-[c:14](:[c:15]):[c:16].[Cl;D1;H0:17]-[c;H0;D3;+0:18]1:[cH;D2;+0:19]:[c;H0;D3;+0:20](-[Cl;D1;H0:21]):[c:22]:[c:23]:[c;H0;D3;+0:24]:1-[NH2;D1;+0:25]>>[#16:1]-[c...
18.5
[{"value": 18.5, "product": "ClC1=C(C=CC(=C1)Cl)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=C(C=C2)Cl)Cl)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 2,4-dichloroaniline (1.89 g, 11.7 mmol) in 15 mL of pyridine. The crude product was triturated with a hot mixture of ethyl acetate, ethanol and methanol (1:1:...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Aromatic halide.Aromatic halide.Primary amine
Aromatic halide.Aromatic halide.Aromatic halide.Aromatic halide.Secondary amide.Secondary amide
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
ClCCl.N1=CC=CC=C1
null
null
Nc1ccc(Cl)cc1Cl.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1ccc(Cl)cc1Cl)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9c9e1e702e704b5496cf56b75362d6ea
Cc1ccc(N)cc1C.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(C)c(C)c2)cc1C
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.CC=1C=C(N)C=CC1C>>CC=1C=C(C=CC1C)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=C(C=C2)C)C)C=CC=C1)=O
[CH3:1][c:2]1[cH:3][cH:4][c:5]([NH2:6])[cH:34][c:35]1[CH3:36].Cl[C:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[S:15][S:16][c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[C:23](Cl)=[O:24]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([NH:6][C:7](=[O:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[S:15][S:16][c:17]2[cH:18][cH:19][cH:2...
Cc1ccc(N)cc1C.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(C)c(C)c2)cc1C
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
5e7dfe57baccae2b9f8237d28bb05b03f973be38ed0d1e13108e5b3f0bc6e511
71b0db43b87ed77f957cef6da658499ea92707aa5812cfa83af28fea1b8a9f46
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[#7:15]-[c:16])-[c:3](:[c:4]):[c:5].[O;D1;H0:7]=[C;H0;D3;+0:6](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:8](:[c:9]):[c:10]
16.8
[{"value": 16.8, "product": "CC=1C=C(C=CC1C)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=C(C=C2)C)C)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (1.12 g, 3.26 mmol) in 25 mL of dichloromethane and 3,4-dimethylaniline (0.79 g, 6.52 mmol) in 8 mL of pyridine. The crude product was triturated with ethyl ether and filtered to yield 0.28 g of the title compo...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
Cc1ccc(N)cc1C.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(C)c(C)c2)cc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-577baf93dbe446b29bfcb8fc756ce4c3
Nc1cc(Cl)cc(Cl)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1cc(Cl)cc(Cl)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cc(Cl)cc(Cl)c1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.ClC=1C=C(N)C=C(C1)Cl>>ClC=1C=C(C=C(C1)Cl)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC(=C2)Cl)Cl)C=CC=C1)=O
[NH2:3][c:4]1[cH:5][c:6]([Cl:7])[cH:33][c:34]([Cl:35])[cH:11]1.[O:1]=[C:2]([Cl:10])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18][S:19][c:20]1[cH:21][cH:22][cH:8][cH:24][c:25]1[C:26](=[O:27])[Cl:32]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][c:6]([Cl:7])[cH:8][c:9]([Cl:10])[cH:11]1)[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:1...
Nc1cc(Cl)cc(Cl)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1cc(Cl)cc(Cl)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cc(Cl)cc(Cl)c1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
08f6fd1cc318cdb2fa23c9eb29a97032bbce3d4ed3ae3fdc6be78ee7a60521f7
ff709637114d139dc59366a7fc358c91f087a54b59bfe5b228e07ff4c733add3
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
[Cl;D1;H0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[c:4](-[NH2;D1;+0:5]):[c:6]:[c;H0;D3;+0:7](-[Cl;D1;H0:8]):[cH;D2;+0:9]:1.[Cl;H0;D1;+0:10]-[C;H0;D3;+0:11](=[O;D1;H0:12])-[c:13](:[c:14]):[c:15].[Cl;H0;D1;+0:16]-[C;H0;D3;+0:17](=[O;D1;H0:18])-[c:19]1:[c:20]:[c:21]:[cH;D2;+0:22]:[cH;D2;+0:23]:[cH;D2;+0:24]:1>>[Cl;D1;H0:1]-[c;H0;...
22.5
[{"value": 22.5, "product": "ClC=1C=C(C=C(C1)Cl)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC(=C2)Cl)Cl)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 3,5-dichloroaniline (1.87 g, 11.7 mmol) in 15 mL of pyridine. The crude product was recrystallized from ethanol, then ethyl ether to yield 0.78 g of the title...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Aromatic halide.Aromatic halide.Primary amine
Aromatic halide.Aromatic halide.Aromatic halide.Aromatic halide.Secondary amide.Secondary amide
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
ClCCl.N1=CC=CC=C1
null
null
Nc1cc(Cl)cc(Cl)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1cc(Cl)cc(Cl)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cc(Cl)cc(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1e404142def44ea88cbeeff7e6caace1
Nc1ccc(F)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1ccc(F)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(F)cc1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.FC1=CC=C(N)C=C1>>FC1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)F)C=CC=C1)=O
[NH2:3][c:4]1[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]1.Cl[C:2](=[O:1])[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21][cH:22][cH:23][c:24]1[C:25](Cl)=[O:26]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([F:8])[cH:9][cH:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21]...
Nc1ccc(F)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1ccc(F)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(F)cc1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
0b7f4098d290755c90a886d0c252e496f0da36f344c58467b3815e0aa364cb08
c921e1c0b5b9c51b320d433f7de9030371670d372e19746642da538aefef62d9
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[#7:15]-[c:16])-[c:3](:[c:4]):[c:5].[O;D1;H0:7]=[C;H0;D3;+0:6](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:8](:[c:9]):[c:10]
9.7
[{"value": 9.7, "product": "FC1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)F)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (1.00 g, 2.92 mmol) in 20 mL of dichloromethane and 4-fluoroaniline (0.657 g, 5.91 mmol) in 5 mL of pyridine. The crude product was triturated with hot ethanol-ethyl acetate mixture, filtered, and recrystallize...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Aromatic halide.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1ccc(F)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1ccc(F)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2ee1555109fc4f4f898ac529b39d3c5b
Nc1cccc(C(F)(F)F)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1cccc(C(F)(F)F)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc(C(F)(F)F)c1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC=1C=C(C=CC1)C(F)(F)F>>FC(C=1C=C(C=CC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC=C2)C(F)(F)F)C=CC=C1)=O)(F)F
[NH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([C:9]([F:10])([F:12])[F:37])[cH:13]1.Cl[C:2](=[O:1])[c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[S:20][S:21][c:22]1[cH:23][cH:24][cH:25][cH:26][c:27]1[C:28](Cl)=[O:29]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13]1)[c:14]1[cH:15][cH:16][cH:17][cH...
Nc1cccc(C(F)(F)F)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1cccc(C(F)(F)F)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc(C(F)(F)F)c1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
ba094faccfda206d55221a88b09dbf39cf5aec45419b40567010e90901b5e999
9b195be506a1a77c1e22fa83b6e1bae8eb184b6ad68b5c3e4c30319262990215
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[F;D1;H0:11]-[C;H0;D4;+0:12](-[F;D1;H0:13])(-[F;H0;D1;+0:14])-[c:15](:[c:16]):[c:17]:[c:18](-[NH2;D1;+0:19]):[c:20]>>[F;D1;H0:11]-[C;H0;D4;+0:12](-[F;D1;H0:21])(-[F;D1;H0:13])-[c:15](:[c:16]):[c:17]:[c:18](-[NH;D2;+...
15.1
[{"value": 15.1, "product": "FC(C=1C=C(C=CC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC=C2)C(F)(F)F)C=CC=C1)=O)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 3-aminobenzotrifluoride (1.87 g, 11.6 mmol) in 15 mL of pyridine. The crude product was recrystallized from ethanol, then ethyl ether to yield 0.519 g of the ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Trifluoro group.Primary amine
Trifluoro group.Trifluoro group.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1cccc(C(F)(F)F)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1cccc(C(F)(F)F)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc(C(F)(F)F)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a6450132c7d642aaab511c2f2ec3bcb7
COc1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>COc1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1OC
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.COC=1C(=CC=CC1)N>>COC1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)OC)C=CC=C1)=O
[cH:7]1[c:8]([NH2:9])[c:34]([O:35][CH3:36])[cH:33][cH:32][cH:31]1.Cl[C:10](=[O:2])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18][S:19][c:20]1[cH:21][cH:1][cH:23][cH:24][c:25]1[C:26](Cl)=[O:27]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[NH:9][C:10](=[O:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18][S:19][...
COc1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
COc1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1OC
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
7a899fabf59db6681ca9e7bd4f2b39435b8652ebf37db403cb4d9ebcff19ad6c
1a6275414974c3f596ec292776f90484d83a560cecc1ad2212064aa4086df0c7
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[c:8]:1-[#16:9].Cl-[C;H0;D3;+0:10](=[O;H0;D1;+0:11])-[c:12](:[c:13]):[c:14].[C;D1;H3:15]-[#8:16]-[c;H0;D3;+0:17]1:[c:18]:[c:19]:[cH;D2;+0:20]:[cH;D2;+0:21]:[c;H0;D3;+0:22]:1-[NH2;D1;+0:23]>>[#16:9]-[c:8]1:[cH;D2;+0:7]:[c:24]:[cH;D2;+0:5...
21.3
[{"value": 21.3, "product": "COC1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)OC)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and o-anisidine (1.42 g, 11.5 mmol) in 10 mL of pyridine. The crude product was recrystallized from ethanol-ethyl acetate, then again from acetonitrile-DMF to yie...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Ether.Primary amine
Ether.Ether.Secondary amide.Secondary amide
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
COc1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>COc1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b718485e058f488da242388c9e90b503
COC(=O)c1sccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>COC(=O)c1sccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccsc1C(=O)OC
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=C(SC=C1)C(=O)OC>>C1(=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)NC1=C(SC=C1)C(=O)OC)C(=O)NC1=C(SC=C1)C(=O)OC
[NH2:10][c:30]1[cH:31][cH:32][s:33][c:34]1[C:35](=[O:36])[O:37][CH3:38].Cl[C:11](=[O:2])[c:13]1[cH:14][cH:15][cH:1][cH:17][c:18]1[S:19][S:6][c:21]1[cH:22][cH:23][cH:24][cH:25][c:26]1[C:27](Cl)=[O:28]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[s:6][cH:7][cH:8][c:9]1[NH:10][C:11](=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]1[...
COC(=O)c1sccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
COC(=O)c1sccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccsc1C(=O)OC
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
1abaa488e786db809080c2263cc57980c9cf7fb2cca818a69953e9baf68adb70
4a74bb4b1a11a78c14e69605ccf0912bf413a242d2df7d70e86626954e018c66
O=C(Nc1ccsc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccsc1
Cl-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3]1:[c:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[c:8]:1-[S;H0;D2;+0:9]-[S;H0;D2;+0:10]-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14](-[C;H0;D3;+0:15](-Cl)=[O;D1;H0:16]):[c:17].[C;D1;H3:18]-[#8:19]-[C:20](=[O;D1;H0:21])-[c:22]1:[#16;a:23]:[c:24]:[c:25]:[c;H0;D3;+0:26]:1-[NH2;D1;+0:27]>>[C...
59
[{"value": 59.0, "product": "C1(=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)NC1=C(SC=C1)C(=O)OC)C(=O)NC1=C(SC=C1)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
23
CELSIUS
18
HOUR
A solution of 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane was added to a solution of methyl 3-amino-2-thiophenecarboxylate (1.82 g, 11.6 mmol) in 14 mL of pyridine at 23° C. The reaction mixture was stirred for 18 hours at 23° C. under nitrogen atmosphere. The precipitate formed was c...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine.Disulfide
Ester.Secondary amide.Secondary amide.Disulfide
c1ccsc1.c1ccccc1.c1ccccc1
c1ccsc1.c1ccccc1.c1ccccc1.c1ccsc1
c1ccsc1.c1ccccc1.c1ccccc1.c1ccsc1
null
ClCCl.N1=CC=CC=C1
23
18
COC(=O)c1sccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>COC(=O)c1sccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccsc1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0f7687fce75f4342a1006eb952201a30
Nc1ccc(C(F)(F)F)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1ccc(C(F)(F)F)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(C(F)(F)F)cc1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=CC=C(C=C1)C(F)(F)F>>FC(C1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)C(F)(F)F)C=CC=C1)=O)(F)F
[NH2:3][c:4]1[cH:5][cH:6][c:7]([C:8]([F:9])([F:11])[F:36])[cH:12][cH:13]1.Cl[C:2](=[O:1])[c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[S:20][S:21][c:22]1[cH:23][cH:24][cH:25][cH:26][c:27]1[C:28](Cl)=[O:29]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([C:8]([F:9])([F:10])[F:11])[cH:12][cH:13]1)[c:14]1[cH:15][cH:16][cH:17][cH...
Nc1ccc(C(F)(F)F)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1ccc(C(F)(F)F)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(C(F)(F)F)cc1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
ba094faccfda206d55221a88b09dbf39cf5aec45419b40567010e90901b5e999
9b195be506a1a77c1e22fa83b6e1bae8eb184b6ad68b5c3e4c30319262990215
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[F;D1;H0:11]-[C;H0;D4;+0:12](-[F;D1;H0:13])(-[F;H0;D1;+0:14])-[c:15]1:[c:16]:[c:17]:[c:18](-[NH2;D1;+0:19]):[c:20]:[c:21]:1>>[F;D1;H0:22]-[C;H0;D4;+0:12](-[F;D1;H0:11])(-[F;D1;H0:13])-[c:15]1:[c:16]:[c:17]:[c:18](-[...
24.3
[{"value": 24.3, "product": "FC(C1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)C(F)(F)F)C=CC=C1)=O)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (1.12 g, 3.26 mmol) in 25 mL of dichloromethane and 4-aminobenzotrifluoride (1.05 g, 6.53 mmol) in 8 mL of pyridine. The crude product was recrystallized from water-DMF to yield 0.47 g of the title compound, mp...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Trifluoro group.Primary amine
Trifluoro group.Trifluoro group.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1ccc(C(F)(F)F)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1ccc(C(F)(F)F)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(C(F)(F)F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-95cacae25c9e40e49862ee7c1efd578d
Nc1ncc(Br)cn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1ncc(Br)cn1)c1ccccc1SSc1ccccc1C(=O)Nc1ncc(Br)cn1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=NC=C(C=N1)Br>>BrC=1C=NC(=NC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=NC=C(C=N2)Br)C=CC=C1)=O
[NH2:3][c:4]1[n:5][cH:6][c:7]([Br:8])[cH:9][n:10]1.Cl[C:2](=[O:1])[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21][cH:22][cH:23][c:24]1[C:25](Cl)=[O:26]>>[O:1]=[C:2]([NH:3][c:4]1[n:5][cH:6][c:7]([Br:8])[cH:9][n:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21][c...
Nc1ncc(Br)cn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1ncc(Br)cn1)c1ccccc1SSc1ccccc1C(=O)Nc1ncc(Br)cn1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
7f949b0f98d34899cd267e5eb2d06cf009ba7b2d60e613c9cd2591b03bc754fa
c921e1c0b5b9c51b320d433f7de9030371670d372e19746642da538aefef62d9
O=C(Nc1ncccn1)c1ccccc1SSc1ccccc1C(=O)Nc1ncccn1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[NH2;D1;+0:11]-[c:12](:[#7;a:13]:[c:14]):[#7;a:15]:[c:16]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[#7:17]-[c:18])-[c:3](:[c:4]):[c:5].[O;D1;H0:7]=[C;H0;D3;+0:6](-[NH;D2;+0:11]-[c:12](:[#7;a:13]:[c:14]):[#7;a:15]:[c:16])-[c:8](...
11.1
[{"value": 11.1, "product": "BrC=1C=NC(=NC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=NC=C(C=N2)Br)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 2-amino-5-bromopyrimidine (2.03 g, 11.7 mmol) in 16 mL of pyridine. The crude product was triturated with a hot mixture of ethyl acetate and ethanol, filtered...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Aromatic halide.Secondary amide.Secondary amide
null
c1cncnc1
c1cncnc1.c1ccccc1.c1ccccc1.c1cncnc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1ncc(Br)cn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1ncc(Br)cn1)c1ccccc1SSc1ccccc1C(=O)Nc1ncc(Br)cn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-11fa6b61f94248b8980e3d5948aa63fb
N#Cc1ccc(N)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>N#Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(C#N)cc2)cc1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=CC=C(C#N)C=C1>>C(#N)C1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)C#N)C=CC=C1)=O
[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:35][cH:36]1.Cl[C:8](=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16][S:17][c:18]1[cH:19][cH:20][cH:21][cH:22][c:23]1[C:24](Cl)=[O:25]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH:7][C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[S:16][S:17][c:18]2[cH:19][cH:20][c...
N#Cc1ccc(N)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
N#Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(C#N)cc2)cc1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
b6e30462973aab3da6f9362b407a7f6f56fd4f435d03bfe5f7b9cfc2aa626e56
c813481c121cec3c4d3841e0937d4ead02e5bd769a2a0f81aa76e63905a965b9
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[#7:15]-[c:16])-[c:3](:[c:4]):[c:5].[O;D1;H0:7]=[C;H0;D3;+0:6](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:8](:[c:9]):[c:10]
12.5
[{"value": 12.5, "product": "C(#N)C1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)C#N)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 4-aminobenzonitrile (1.38 g, 11.7 mmol) in 11 mL of pyridine. The crude product was triturated with a hot mixture of ethyl acetate and ethanol (1:1), filtered...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Nitrile.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
N#Cc1ccc(N)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>N#Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(C#N)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7da54477b90c42788a92fc7c0bf018be
CS(=O)(=O)c1ccc(N)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>CS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(S(C)(=O)=O)cc2)cc1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.CS(=O)(=O)C1=CC=C(C=C1)N>>CS(=O)(=O)C1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)C=CC=C1)=O
[O:3]=[S:33]([c:32]1[cH:6][cH:7][c:8]([NH2:9])[cH:39][cH:40]1)([CH3:34])=[O:35].Cl[C:10](=[O:11])[c:12]1[cH:13][cH:1][cH:15][cH:16][c:17]1[S:18][S:2][c:20]1[cH:21][cH:22][cH:23][cH:24][c:25]1[C:26](Cl)=[O:27]>>[CH3:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8]([NH:9][C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][c...
CS(=O)(=O)c1ccc(N)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
CS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(S(C)(=O)=O)cc2)cc1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
17aa62473bb616012597b840da7270c9d08a47da314ff3e256453ed1ac09f2b3
d3e4c27a17571d4b1804b7920121c68df73b33d6aa2a2f9ae2a99691a8d61071
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[cH;D2;+0:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[c:7]:[c:8]:1-[S;H0;D2;+0:9]-[S;H0;D2;+0:10]-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14](-[C;H0;D3;+0:15](-Cl)=[O;D1;H0:16]):[c:17].[C;D1;H3:18]-[S;H0;D4;+0:19](=[O;D1;H0:20])(=[O;H0;D1;+0:21])-[c;H0;D3;+0:22]1:[cH;D2;+0:23]:[c:24]:[c:25](-[NH2;D1...
56
[{"value": 56.0, "product": "CS(=O)(=O)C1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 4-aminophenyl methyl sulfone (2.00 g, 11.7 mmol) in 16 mL of pyridine. The crude product was recrystallized from acetonitrile-DMF to yield 2.0 g of the title ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine.Disulfide.Sulfone
Secondary amide.Secondary amide.Disulfide.Sulfone.Sulfone
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
CS(=O)(=O)c1ccc(N)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>CS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(S(C)(=O)=O)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-433c355fb94b481c9dee297890a544bc
Nc1cc(Cl)ncn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1cc(Cl)ncn1)c1ccccc1SSc1ccccc1C(=O)Nc1cc(Cl)ncn1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=NC=NC(=C1)Cl>>ClC1=CC(=NC=N1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=NC=NC(=C2)Cl)C=CC=C1)=O
[NH2:3][c:4]1[cH:5][c:6]([Cl:7])[n:8][cH:9][n:10]1.Cl[C:2](=[O:1])[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21][cH:22][cH:23][c:29]1[C:30](=[O:26])[Cl:31]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][c:6]([Cl:7])[n:8][cH:9][n:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:...
Nc1cc(Cl)ncn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1cc(Cl)ncn1)c1ccccc1SSc1ccccc1C(=O)Nc1cc(Cl)ncn1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
884eacce4242e627a95d5a5d354ec6923c10e46aa2cb7578ac5a93f339d94e94
c921e1c0b5b9c51b320d433f7de9030371670d372e19746642da538aefef62d9
O=C(Nc1ccncn1)c1ccccc1SSc1ccccc1C(=O)Nc1ccncn1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[#16:6]-[#16:7]-[c;H0;D3;+0:8]1:[c:9]:[c:10]:[c:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13]:1-[C;H0;D3;+0:14](-[Cl;D1;H0:15])=[O;H0;D1;+0:16].[NH2;D1;+0:17]-[c:18]1:[#7;a:19]:[c:20]:[#7;a:21]:[c:22]:[c:23]:1>>[Cl;D1;H0:15]-[c;H0;D3;+0:14]1:[#7;a:24]:[c:25]:[#7;a:26]:[c:27](-[#7...
12.3
[{"value": 12.3, "product": "ClC1=CC(=NC=N1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=NC=NC(=C2)Cl)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 90 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 4-amino-6-chloropyrimidine (1.51 g, 11.7 mmol) in 12 mL of pyridine. The crude product was triturated with a hot mixture of ethyl acetate and ethanol, filtere...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Aromatic halide.Secondary amide.Secondary amide
c1ccccc1
c1ccccc1.c1cncnc1
c1cncnc1.c1ccccc1.c1ccccc1.c1cncnc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1cc(Cl)ncn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1cc(Cl)ncn1)c1ccccc1SSc1ccccc1C(=O)Nc1cc(Cl)ncn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7c194310fbba4e8fa2c9c67981d2dbf3
Nc1ccc(I)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1ccc(I)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(I)cc1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.IC1=CC=C(N)C=C1>>IC1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)I)C=CC=C1)=O
[NH2:3][c:4]1[cH:5][cH:6][c:7]([I:8])[cH:9][cH:10]1.Cl[C:2](=[O:1])[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21][cH:22][cH:23][c:24]1[C:25](Cl)=[O:26]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][c:7]([I:8])[cH:9][cH:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21]...
Nc1ccc(I)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1ccc(I)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(I)cc1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
0b7f4098d290755c90a886d0c252e496f0da36f344c58467b3815e0aa364cb08
c921e1c0b5b9c51b320d433f7de9030371670d372e19746642da538aefef62d9
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[#7:15]-[c:16])-[c:3](:[c:4]):[c:5].[O;D1;H0:7]=[C;H0;D3;+0:6](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:8](:[c:9]):[c:10]
36
[{"value": 36.0, "product": "IC1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC=C(C=C2)I)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 4-iodoaniline (2.54 g, 11.6 mmol) in 20 mL of pyridine. The crude product was recrystallized from water-DMF to yield 1.48 g of the title compound, mp 268°-271...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Aromatic halide.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1ccc(I)cc1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1ccc(I)cc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(I)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7d989fed42294e84a3366f42f847f891
CCc1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>CCc1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1CC
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.C(C)C1=C(N)C=CC=C1>>C(C)C1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)CC)C=CC=C1)=O
[cH:5]1[cH:6][cH:7][c:8]([NH2:9])[c:34]([CH2:35][CH3:36])[cH:33]1.Cl[C:10](=[O:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18][S:19][c:20]1[cH:21][cH:1][cH:23][cH:24][c:25]1[C:26](Cl)=[O:27]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[NH:9][C:10](=[O:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[S:18][S:1...
CCc1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
CCc1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1CC
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
49c984089c3266fdc90fd3e269b10a04d794c54780f8560852f5efac400661a8
71b0db43b87ed77f957cef6da658499ea92707aa5812cfa83af28fea1b8a9f46
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[c:13]:1-[#16:14].[C;D1;H3:15]-[C:16]-[c;H0;D3;+0:17]1:[cH;D2;+0:18]:[cH;D2;+0:19]:[c:20]:[c:21]:[c;H0;D3;+0:22]:1-[NH2;D1;+0:23]>>[#16:14]-[c:13]1:[cH;D2;+0:12]:[c:24]:[cH;D2;+0:10...
33.6
[{"value": 33.6, "product": "C(C)C1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)CC)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 90 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 2-ethylaniline (1.40 g, 11.6 mmol) in 12 mL of pyridine. The crude product was recrystallized from acetonitrile-DMF to yield 1.0 g of the title compound, mp 2...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Secondary amide.Secondary amide
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
CCc1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>CCc1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1CC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8b9c2430e1724400a4c74be58252de98
Nc1ccncn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1ccncn1)c1ccccc1SSc1ccccc1C(=O)Nc1ccncn1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=NC=NC=C1>>N1=CN=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=NC=NC=C2)C=CC=C1)=O
[n:3]1[cH:29][cH:28][c:27]([NH2:26])[n:32][cH:31]1.Cl[C:2](=[O:1])[c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16][S:17][c:18]1[cH:19][cH:20][cH:4][cH:22][c:23]1[C:24](Cl)=[O:25]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][n:7][cH:8][n:9]1)[c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16][S:17][c:18]1[cH:19][cH:20][cH:21][cH:...
Nc1ccncn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1ccncn1)c1ccccc1SSc1ccccc1C(=O)Nc1ccncn1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
f30f048d4d94488d1eed9939ac47c3f1423d2e6839e26f5bac1b9200646d6546
71b0db43b87ed77f957cef6da658499ea92707aa5812cfa83af28fea1b8a9f46
O=C(Nc1ccncn1)c1ccccc1SSc1ccccc1C(=O)Nc1ccncn1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[c:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:1.[NH2;D1;+0:14]-[c:15]1:[#7;a:16]:[cH;D2;+0:17]:[n;H0;D2;+0:18]:[cH;D2;+0:19]:[c:20]:1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:18]-[c;H0;D3;+0:12](:[#7;a:21]:[c:22]):[c:23]:[...
2
[{"value": 2.0, "product": "N1=CN=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=NC=NC=C2)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 90 using 2,2'-dithiobisbenzoyl chloride (3.00 g, 8.74 mmol) in 75 mL of dichloromethane and 4-aminopyrimidine (1.66 g, 17.5 mmol) in 14 mL of pyridine. The crude product was triturated with a hot mixture of acetonitrile and DMF, filtered, and recryst...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Secondary amide.Secondary amide
c1cncnc1.c1ccccc1
c1cncnc1.c1ccccc1.c1cncnc1
c1cncnc1.c1ccccc1.c1ccccc1.c1cncnc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1ccncn1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1ccncn1)c1ccccc1SSc1ccccc1C(=O)Nc1ccncn1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4a7cf2ad202e4c1397b6b815cf8ebc70
Nc1cccc([N+](=O)[O-])c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1cccc([N+](=O)[O-])c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc([N+](=O)[O-])c1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.[N+](=O)([O-])C=1C=C(N)C=CC1>>[N+](=O)([O-])C=1C=C(C=CC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC=C2)[N+](=O)[O-])C=CC=C1)=O
[NH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12]1.Cl[C:2](=[O:1])[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]1[S:19][S:20][c:21]1[cH:22][cH:23][cH:24][cH:25][c:26]1[C:27](Cl)=[O:28]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12]1)[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]...
Nc1cccc([N+](=O)[O-])c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1cccc([N+](=O)[O-])c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc([N+](=O)[O-])c1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
4472955bfa88478abba07a4cc7154c307fb81084178d69a517c77e496ac53b12
ad52e94667c28774f72157b153acd6400c4e6e1d52c0236ded1aefe4a3462786
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[#7:15]-[c:16])-[c:3](:[c:4]):[c:5].[O;D1;H0:7]=[C;H0;D3;+0:6](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:8](:[c:9]):[c:10]
24.9
[{"value": 24.9, "product": "[N+](=O)([O-])C=1C=C(C=CC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC=C2)[N+](=O)[O-])C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 3-nitroaniline (1.60 g, 11.6 mmol) in 13 mL of pyridine. The crude product was recrystallized once from ethanol-ether, then twice from acetonitrile-DMF-water ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Nitro group.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1cccc([N+](=O)[O-])c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1cccc([N+](=O)[O-])c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc([N+](=O)[O-])c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8758a287794b4b4db01fbda93c571355
Nc1ccccc1S(N)(=O)=O.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>NS(=O)(=O)c1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1S(N)(=O)=O
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=C(C=CC=C1)S(=O)(=O)N>>NS(=O)(=O)C1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)S(=O)(=O)N)C=CC=C1)=O
[NH2:1][c:31]1[cH:32][cH:33][cH:34][cH:35][c:36]1[S:37](=[O:3])(=[O:4])[NH2:38].Cl[C:12](=[O:13])[c:14]1[cH:5][cH:16][cH:17][cH:18][c:19]1[S:2][S:21][c:22]1[cH:23][cH:24][cH:25][cH:26][c:27]1[C:28](Cl)=[O:29]>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[NH:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][c...
Nc1ccccc1S(N)(=O)=O.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
NS(=O)(=O)c1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1S(N)(=O)=O
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
7ac7bc0cc5662ec00f4922bec048a5b26d4576545016181297e777317cc514df
237c94f9bfeb760408a4fe8675c80a8ef696736e818eb00c99939b94b6dc2129
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[cH;D2;+0:5]:[c:6]:[c:7]:[c;H0;D3;+0:8]:1-[S;H0;D2;+0:9]-[S;H0;D2;+0:10]-[c:11](:[c:12]):[c:13](-[C;H0;D3;+0:14](-Cl)=[O;D1;H0:15]):[c:16].[N;D1;H2:17]-[S;H0;D4;+0:18](=[O;H0;D1;+0:19])(=[O;H0;D1;+0:20])-[c:21](:[c:22]):[c;H0;D3;+0:23](-[NH2;D1;+0:24]):[c:25]...
19.6
[{"value": 19.6, "product": "NS(=O)(=O)C1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)S(=O)(=O)N)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
23
CELSIUS
6
DAY
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 2-aminobenzenesulfonamide (2.00 g, 11.6 mmol) in 16 mL of pyridine. The reaction mixture was stirred for 6 days at 23° C. under nitrogen atmosphere. The crude...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Sulfonamide.Primary amine.Disulfide
Sulfonamide.Sulfonamide.Secondary amide.Secondary amide.Disulfide
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
23
144
Nc1ccccc1S(N)(=O)=O.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>NS(=O)(=O)c1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1S(N)(=O)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0d887acf58894cdeab531ebdbbaba9ed
CC(C)c1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>CC(C)c1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1C(C)C
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.C(C)(C)C1=C(N)C=CC=C1>>CC(C)C1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)C(C)C)C=CC=C1)=O
[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[NH2:10].Cl[C:11](=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]1[S:19][S:20][c:21]1[cH:22][cH:23][cH:33][cH:34][c:35]1[C:36](Cl)=[O:28]>>[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[NH:10][C:11](=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]...
CC(C)c1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
CC(C)c1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1C(C)C
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
ad35fcc7b8c9e958b6441183e4e1bf74ea30caaf297bb377d3d908c17c91c784
71b0db43b87ed77f957cef6da658499ea92707aa5812cfa83af28fea1b8a9f46
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[#16:6]-[#16:7]-[c;H0;D3;+0:8]1:[c:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[c:12]:[c;H0;D3;+0:13]:1-[C;H0;D3;+0:14](-Cl)=[O;H0;D1;+0:15].[NH2;D1;+0:16]-[c:17](:[c:18]):[c:19]>>[C;D1;H3:20]-[CH;D3;+0:14](-[C;D1;H3:21])-[c;H0;D3;+0:13]1:[c:12]:[cH;D2;+0:11]:[c:22]:[c:23]:[c:24]:...
14.3
[{"value": 14.3, "product": "CC(C)C1=C(C=CC=C1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=C(C=CC=C2)C(C)C)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 90 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and 2-isopropylaniline (1.60 g, 11.6 mmol) in 13 mL of pyridine. The crude product was recrystallized twice from acetonitrile-DMF to yield 0.45 g of the title com...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Secondary amide.Secondary amide
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
CC(C)c1ccccc1N.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>CC(C)c1ccccc1NC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1C(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-820622bd6d264f8c8a3784a27744ca1b
Nc1cccc(I)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(Nc1cccc(I)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc(I)c1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.IC=1C=C(N)C=CC1>>IC=1C=C(C=CC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC=C2)I)C=CC=C1)=O
[NH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([I:9])[cH:10]1.Cl[C:2](=[O:1])[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21][cH:22][cH:23][c:24]1[C:25](Cl)=[O:26]>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][cH:7][c:8]([I:9])[cH:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[S:17][S:18][c:19]1[cH:20][cH:21]...
Nc1cccc(I)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(Nc1cccc(I)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc(I)c1
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
0b7f4098d290755c90a886d0c252e496f0da36f344c58467b3815e0aa364cb08
c921e1c0b5b9c51b320d433f7de9030371670d372e19746642da538aefef62d9
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[#7:15]-[c:16])-[c:3](:[c:4]):[c:5].[O;D1;H0:7]=[C;H0;D3;+0:6](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:8](:[c:9]):[c:10]
7.3
[{"value": 7.3, "product": "IC=1C=C(C=CC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2=CC(=CC=C2)I)C=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (3.00 g, 8.74 mmol) in 75 mL of dichloromethane and 3-iodoaniline (3.82 g, 17.5 mmol) in 17 mL of pyridine. The crude product was triturated with hot ethanol, filtered, and recrystallized first from water-DMF, ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Aromatic halide.Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
null
null
Nc1cccc(I)c1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>O=C(Nc1cccc(I)c1)c1ccccc1SSc1ccccc1C(=O)Nc1cccc(I)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9d750e19d8b4a39925f795da813a080
CCOP(=O)(Cc1ccc(N)cc1)OCC.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>CCOP(=O)(Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(CP(=O)(OCC)OCC)cc2)cc1)OCC
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.NC1=CC=C(CP(OCC)(OCC)=O)C=C1>>C(C)OP(OCC)(=O)CC1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(NC1=CC=C(C=C1)CP(=O)(OCC)OCC)=O)=O
[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][c:10]([NH2:11])[cH:46][cH:47]1)[O:48][CH2:49][CH3:31].Cl[C:12]([c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[S:20][S:21][c:22]1[cH:23][cH:24][cH:25][cH:26][c:27]1[C:28](Cl)=[O:29])=[O:37]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][c:7]1[cH:8][cH:9][c:10]([NH:11][C:...
CCOP(=O)(Cc1ccc(N)cc1)OCC.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
CCOP(=O)(Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(CP(=O)(OCC)OCC)cc2)cc1)OCC
null
null
ClCCl.N1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
5e7dfe57baccae2b9f8237d28bb05b03f973be38ed0d1e13108e5b3f0bc6e511
71b0db43b87ed77f957cef6da658499ea92707aa5812cfa83af28fea1b8a9f46
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1C(=O)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-[c:8](:[c:9]):[c:10].[#15:11]-[#8:12]-[CH2;D2;+0:13]-[CH3;D1;+0:14].[NH2;D1;+0:15]-[c:16](:[c:17]):[c:18]>>[#15:11]-[#8:12]-[CH2;D2;+0:13]-[C;D1;H3:19].[#8:20]-[#15:21](-[#8:22])(-[C:23])=[O;H0;D1;+0:7].[O;D1;H0:2]=[C;H0;D3;+0:1](-[#...
59.2
[{"value": 59.2, "product": "C(C)OP(OCC)(=O)CC1=CC=C(C=C1)NC(C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(NC1=CC=C(C=C1)CP(=O)(OCC)OCC)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
23
CELSIUS
3
DAY
This compound was prepared according to the general method of Example 77 using 2,2'-dithiobisbenzoyl chloride (2.00 g, 5.83 mmol) in 50 mL of dichloromethane and diethyl 4-aminobenzylphosphonate (2.90 g, 11.6 mmol) in 23 mL of pyridine. The reaction mixture was stirred for 3 days at 23° C. under nitrogen atmosphere. Th...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine
Secondary amide.Secondary amide
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
ClCCl.N1=CC=CC=C1
23
72
CCOP(=O)(Cc1ccc(N)cc1)OCC.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl.N1=CC=CC=C1>CCOP(=O)(Cc1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)Nc2ccc(CP(=O)(OCC)OCC)cc2)cc1)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3891158d65564d66834bcdc1c2f37155
CCN(CC)CC.NC1CC1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(NC1CC1)c1ccccc1SSc1ccccc1C(=O)NC1CC1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.C1(CC1)N.C(C)N(CC)CC.ClCCl.ClCCl>>C1(CC1)NC(C1=C(C=CC=C1)SSC1=C(C(=O)NC2CC2)C=CC=C1)=O
CC[N:3]([CH2:4]C)[CH2:6][CH3:5].[NH2:23][CH:24]1[CH2:25][CH2:26]1.Cl[C:2](=[O:1])[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[S:13][S:14][c:15]1[cH:16][cH:17][cH:18][cH:19][c:20]1[C:21](Cl)=[O:22]>>[O:1]=[C:2]([NH:3][CH:4]1[CH2:5][CH2:6]1)[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[S:13][S:14][c:15]1[cH:16][cH:17][cH:18][cH:19]...
CCN(CC)CC.NC1CC1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(NC1CC1)c1ccccc1SSc1ccccc1C(=O)NC1CC1
null
null
null
Acylation
OtherReaction
406c1d410511822e2c32fadbc4b9d0e0b66c76e5428cd1d7ed0d65ddb3d4516e
6bae7498e135285c9d695c8eebe8b4e8c6f211037b0a32e9828a1cf0341cfdf0
O=C(NC1CC1)c1ccccc1SSc1ccccc1C(=O)NC1CC1
C-C-[N;H0;D3;+0:1](-[CH2;D2;+0:2]-C)-[CH2;D2;+0:3]-[CH3;D1;+0:4].Cl-[C;H0;D3;+0:5](=[O;D1;H0:6])-[c:7](:[c:8]):[c:9].Cl-[C;H0;D3;+0:10](=[O;D1;H0:11])-[c:12](:[c:13]):[c:14].[NH2;D1;+0:15]-[C:16]1-[C:17]-[C:18]-1>>[O;D1;H0:11]=[C;H0;D3;+0:10](-[NH;D2;+0:1]-[CH;D3;+0:2]1-[CH2;D2;+0:4]-[CH2;D2;+0:3]-1)-[c:12](:[c:13]):[c...
null
[]
null
null
3
HOUR
A solution of 2,2'-dithiobisbenzoyl chloride (1.0 g, 3.0 mmol) in 20 mL of dichloromethane was added dropwise to a solution of cyclopropylamine (0.52 mL, 7.5 mmol) and triethylamine (1.2 mL, 9.0 mmol) in 20 mL of dichloromethane. A solid formed immediately, the mixture was stirred for 3 hours and then filtered. The sol...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary amine.Tertiary amine
Secondary amide.Secondary amide
null
C1CC1
C1CC1.c1ccccc1.c1ccccc1.C1CC1
HCl
null
null
3
CCN(CC)CC.NC1CC1.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(NC1CC1)c1ccccc1SSc1ccccc1C(=O)NC1CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ce2fac42f05a4292a71802d2a5aa59d9
C1CCNC1.CCN(CC)CC.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>>O=C(c1ccccc1SSc1ccccc1C(=O)N1CCCC1)N1CCCC1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.N1CCCC1.C(C)N(CC)CC>>N1(CCCC1)C(=O)C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)N1CCCC1
[NH:19]1[CH2:20][CH2:21][CH2:22][CH2:23]1.CC[N:24]([CH2:25][CH3:26])[CH2:28][CH3:27].Cl[C:2](=[O:1])[c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[S:9][S:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[C:17](Cl)=[O:18]>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[S:9][S:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[C:17](=[O:...
C1CCNC1.CCN(CC)CC.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl
O=C(c1ccccc1SSc1ccccc1C(=O)N1CCCC1)N1CCCC1
null
null
ClCCl
Acylation
OtherReaction
ea8ca56c36032f7821db62c41ccbf83211b61d9406fd5204e4c894ae1cb14783
53ffcfd2622b76ac9a654abbf10337346a70bce028c9c648756066334eefd291
O=C(c1ccccc1SSc1ccccc1C(=O)N1CCCC1)N1CCCC1
C-C-[N;H0;D3;+0:1](-[C:2]-[CH3;D1;+0:3])-[C:4]-[CH3;D1;+0:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].Cl-[C;H0;D3;+0:11](=[O;D1;H0:12])-[c:13](:[c:14]):[c:15].[C:16]1-[C:17]-[C:18]-[C:19]-[NH;D2;+0:20]-1>>[O;D1;H0:12]=[C;H0;D3;+0:11](-[N;H0;D3;+0:1]1-[C:2]-[CH2;D2;+0:3]-[CH2;D2;+0:5]-[C:4]-1)-[c:13](:[c:14]...
60.6
[{"value": 60.6, "product": "N1(CCCC1)C(=O)C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)N1CCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 112 using 2,2'-dithiobisbenzoyl chloride (1.0 g, 3.0 mmol) in 15 mL of dichloromethane and pyrrolidine (0.63 mL, 7.5 mmol) and triethylamine (1.2 mL, 9 mmol) in 20 mL of dichloromethane, to give 0.75 g of the title compound as a foam, mp 62°-63° C.; ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Secondary amine.Tertiary amine
Tertiary amide.Tertiary amide
C1CCNC1
C1CC[NH]C1.C1CC[NH]C1
c1ccccc1.c1ccccc1.C1CC[NH]C1.C1CC[NH]C1
HCl
ClCCl
null
null
C1CCNC1.CCN(CC)CC.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl>ClCCl>O=C(c1ccccc1SSc1ccccc1C(=O)N1CCCC1)N1CCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-90022719d27c459586f6b49166817b5d
CC(=O)N(C)[Si](C)(C)C.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl.O=C(O)C1CCNCC1>>O=C(O)C1CCN(C(=O)c2ccccc2SSc2ccccc2C(=O)N2CCC(C(=O)O)CC2)CC1
C(C1=C(C=CC=C1)SSC1=C(C(=O)Cl)C=CC=C1)(=O)Cl.N1CCC(C(=O)O)CC1.CN(C(C)=O)[Si](C)(C)C>>C1(=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)N1CCC(CC1)C(=O)O)C(=O)N1CCC(CC1)C(=O)O
[Si]([N:26]([CH3:27])[C:30]([CH3:29])=[O:31])([CH3:28])([CH3:33])[CH3:34].Cl[C:8](=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[S:16][S:17][c:18]1[cH:19][cH:20][cH:21][cH:22][c:23]1[C:24](Cl)=[O:25].[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][NH:7][CH2:35][CH2:36]1>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][N:7]([C:8](...
CC(=O)N(C)[Si](C)(C)C.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl.O=C(O)C1CCNCC1
O=C(O)C1CCN(C(=O)c2ccccc2SSc2ccccc2C(=O)N2CCC(C(=O)O)CC2)CC1
null
N1=CC=CC=C1
ClCCl
C-C Coupling
OtherReaction
bdfeab0ac9bf070110ff45deb052163efdc5c171b8bd808dd3b12b5bf4f50f9d
5986769fffda6caef634a288ef2bd834f11c82f4530b102cbf566cd6049b565e
O=C(c1ccccc1SSc1ccccc1C(=O)N1CCCCC1)N1CCCCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10].[CH3;D1;+0:11]-[N;H0;D3;+0:12](-[C;H0;D3;+0:13](-[CH3;D1;+0:14])=[O;D1;H0:15])-[Si](-[CH3;D1;+0:16])(-[CH3;D1;+0:17])-[CH3;D1;+0:18].[C:19]-[C:20]-[NH;D2;+0:21]-[C:22]-[C:23]>>[C:19]-[C:20]-[N;H0;D3;+0:21](-[C;H0;D3...
null
[]
null
null
24
HOUR
Isonipecotic acid (4-piperidinecarboxylic acid) (0.76 g, 6 mmol), N-methyl-N-trimethylsilylacetamide and 3 drops of pyridine were stirred at room temperature for 2 hours. This suspension was added to a filtered solution of 2,2'-dithiobisbenzoyl chloride (1.0 g, 3.0 mmol) in 15 mL of dichloromethane. The solvent was rem...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Tertiary amide.Secondary amine.Silyl protective group
Carboxylic acid.Tertiary amide.Tertiary amide
C1CCNCC1
C1CC[NH]CC1.C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1.c1ccccc1.C1CC[NH]CC1
HCl
N1=CC=CC=C1.ClCCl
null
24
CC(=O)N(C)[Si](C)(C)C.O=C(Cl)c1ccccc1SSc1ccccc1C(=O)Cl.O=C(O)C1CCNCC1>N1=CC=CC=C1.ClCCl>O=C(O)C1CCN(C(=O)c2ccccc2SSc2ccccc2C(=O)N2CCC(C(=O)O)CC2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d4f02f7260614e1283e973c416bc0d8e
CC(C)(C)OC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1SSc1ccccc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)OC(C)(C)C>>N=C(N)NCCC[C@H](NC(=O)c1ccccc1SSc1ccccc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(=O)O
CC(C)(C)OC([C@@H](NC(=O)C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)OC(C)(C)C)CCCNC(N)=N)=O>>C1(=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)O
CC(C)(C)[O:39][C:37]([C@@H:29]([NH:28][C:26]([c:25]1[c:20]([S:19][S:18][c:17]2[c:12]([C:10]([NH:9][C@@H:8]([CH2:7][CH2:6][CH2:5][NH:4][C:2](=[NH:1])[NH2:3])[C:40](=[O:41])[O:42]C(C)(C)C)=[O:11])[cH:13][cH:14][cH:15][cH:16]2)[cH:21][cH:22][cH:23][cH:24]1)=[O:27])[CH2:30][CH2:31][CH2:32][NH:33][C:34](=[NH:35])[NH2:36])=[...
CC(C)(C)OC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1SSc1ccccc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)OC(C)(C)C
N=C(N)NCCC[C@H](NC(=O)c1ccccc1SSc1ccccc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(=O)O
null
null
ClCCl.FC(C(=O)O)(F)F
Deprotection
OtherReaction
ca505900a12db9f5b5e9f03319157f3a1866191dca0d7b3ac3055953edad48a1
6963b6f47a0b0b5cff914a710e9b301204a20bd63f6727c47e40cb3bb5699806
c1ccc(SSc2ccccc2)cc1
C-C(-C)(-C)-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].C-C(-C)(-C)-[O;H0;D2;+0:5]-[C:6](-[C:7])=[O;D1;H0:8]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1].[C:7]-[C:6](=[O;D1;H0:8])-[OH;D1;+0:5]
59.8
[{"value": 59.8, "product": "C1(=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the general method of Example 122 using N,N'-[Dithiobis (2,1-phenylenecarbonyl)bis-L-arginine-bis(1,1-dimethylethyl) ester, (1.31 g, 2.0 mmol) from Example 127 in 15 mL of dichloromethane and 15 mL of trifluoroacetic acid. The residue was triturated with ethanol and 1N HCl to yie...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Boc.Boc
Carboxylic acid.Carboxylic acid
null
null
c1ccccc1.c1ccccc1
Other
ClCCl.FC(C(=O)O)(F)F
null
null
CC(C)(C)OC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1SSc1ccccc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)OC(C)(C)C>ClCCl.FC(C(=O)O)(F)F>N=C(N)NCCC[C@H](NC(=O)c1ccccc1SSc1ccccc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-85957d48a087410d9c293b7d5c14f82e
CC(=O)N[C@@H](CS)C(=O)O.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1>>CC(=O)NC(CSSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1)C(=O)O
O=C1N(SC2=C1C=CC=C2)C2=CC=C(C=C2)S(=O)(=O)N.C(C)(=O)N[C@@H](CS)C(=O)O>>C(C)(=O)NC(C(=O)O)CSSC1=C(C=CC=C1)C(NC1=CC=C(C=C1)S(N)(=O)=O)=O
[CH3:1][C:2](=[O:3])[NH:4][C@@H:5]([CH2:6][SH:7])[C:28](=[O:29])[OH:30].[s:8]1[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[c:15](=[O:16])[n:17]1-[c:18]1[cH:19][cH:20][c:21]([S:22]([NH2:23])(=[O:24])=[O:25])[cH:26][cH:27]1>>[CH3:1][C:2](=[O:3])[NH:4][CH:5]([CH2:6][S:7][S:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[C:15](=[...
CC(=O)N[C@@H](CS)C(=O)O.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1
CC(=O)NC(CSSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1)C(=O)O
null
null
null
Miscellaneous
OtherReaction
b009af05d472ccdcc7c275cf7d538d0fec35d7c49529303a2e355b9dd8798d3e
e8a16c39a4da768b069d0811166d9dd2e9252bf47af9bd7cebb79eb4280a5696
O=C(Nc1ccccc1)c1ccccc1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[C:4]-[C:5]-[SH;D1;+0:6].[O;D1;H0:7]=[c;H0;D3;+0:8]1:[c:9](:[c:10]):[c:11](:[c:12]):[s;H0;D2;+0:13]:[n;H0;D3;+0:14]:1-[c;H0;D3;+0:15](:[c:16]:[c:17]):[c:18]:[c:19]>>[O;D1;H0:7]=[C;H0;D3;+0:8](-[NH;D2;+0:14]-[c;H0;D3;+0:15](:[c:16]:[c:17]):[c:18]:[c:19])-[c:9](:[c:10]):[c:11](-[S;H0;D2;+0...
81.6
[{"value": 81.6, "product": "C(C)(=O)NC(C(=O)O)CSSC1=C(C=CC=C1)C(NC1=CC=C(C=C1)S(N)(=O)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the method of Example 132 using 0.8 g (2.4 mmol) of 4-(3-oxo-3H-benzo[d]isothiazol-2-yl)benzenesulfonamide and 0.39 g (2.4 mmol) of N-acetyl-L-cysteine. The product was washed with ether and dried in vacuo to give 0.92 g of the title compound, mp 218°-220° C. Conditions: See reac...
10.6084/m9.figshare.5104873.v1
null
Aliphatic thiol
Secondary amide.Disulfide
c1ccc2sncc2c1
c1ccccc1
c1ccccc1.c1ccccc1
null
null
null
null
CC(=O)N[C@@H](CS)C(=O)O.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1>>CC(=O)NC(CSSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4e6baa83df414e8490e7a223e4d371a6
CC(S)C(=O)NCC(=O)O.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1>>CC(SSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1)C(=O)NCC(=O)O
O=C1N(SC2=C1C=CC=C2)C2=CC=C(C=C2)S(=O)(=O)N.SC(C(=O)NCC(=O)O)C>>S(N)(=O)(=O)C1=CC=C(C=C1)NC(=O)C1=C(C=CC=C1)SSC(C(=O)NCC(=O)O)C
[CH3:1][CH:2]([SH:3])[C:24](=[O:25])[NH:26][CH2:27][C:28](=[O:29])[OH:30].[s:4]1[c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[c:11](=[O:12])[n:13]1-[c:14]1[cH:15][cH:16][c:17]([S:18]([NH2:19])(=[O:20])=[O:21])[cH:22][cH:23]1>>[CH3:1][CH:2]([S:3][S:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[C:11](=[O:12])[NH:13][c:14]1[cH:15][cH:1...
CC(S)C(=O)NCC(=O)O.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1
CC(SSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1)C(=O)NCC(=O)O
null
null
null
Miscellaneous
OtherReaction
b009af05d472ccdcc7c275cf7d538d0fec35d7c49529303a2e355b9dd8798d3e
e8a16c39a4da768b069d0811166d9dd2e9252bf47af9bd7cebb79eb4280a5696
O=C(Nc1ccccc1)c1ccccc1
[C;D1;H3:1]-[C:2](-[SH;D1;+0:3])-[C:4](=[O;D1;H0:5])-[#7:6]-[C:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10].[O;D1;H0:11]=[c;H0;D3;+0:12]1:[c:13](:[c:14]):[c:15](:[c:16]):[s;H0;D2;+0:17]:[n;H0;D3;+0:18]:1-[c;H0;D3;+0:19](:[c:20]:[c:21]):[c:22]:[c:23]>>[C;D1;H3:1]-[C:2](-[S;H0;D2;+0:3]-[S;H0;D2;+0:17]-[c:15](:[c:16]):[c:13](-[C;H...
92.3
[{"value": 92.3, "product": "S(N)(=O)(=O)C1=CC=C(C=C1)NC(=O)C1=C(C=CC=C1)SSC(C(=O)NCC(=O)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the method of Example 132 using 0.46 g (1.5 mmol) of 4-(3-oxo-3H-benzo[d]isothiazol-2-yl)benzenesulfonamide and 0.25 g (1.5 mmol) of 2-mercapto-propionylglycine. The product was washed with ether and dried in vacuo to give 0.65 g of the title compound, mp 254°-256° C. Conditions:...
10.6084/m9.figshare.5104873.v1
null
Aliphatic thiol
Secondary amide.Disulfide
c1ccc2sncc2c1
c1ccccc1
c1ccccc1.c1ccccc1
null
null
null
null
CC(S)C(=O)NCC(=O)O.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1>>CC(SSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1)C(=O)NCC(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-40ccfc0f214f4effb36ca78515638c20
NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1.O=C(O)c1ccccc1S>>NS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)O)cc1
O=C1N(SC2=C1C=CC=C2)C2=CC=C(C=C2)S(=O)(=O)N.C(C=1C(S)=CC=CC1)(=O)O>>S(N)(=O)(=O)C1=CC=C(C=C1)NC(=O)C1=C(C=CC=C1)SSC1=C(C(=O)O)C=CC=C1
[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8](-[n:9]2[c:10](=[O:11])[c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]3[s:18]2)[cH:29][cH:30]1.[SH:19][c:20]1[cH:21][cH:22][cH:23][cH:24][c:25]1[C:26](=[O:27])[OH:28]>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8]([NH:9][C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][cH:16...
NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1.O=C(O)c1ccccc1S
NS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)O)cc1
null
null
CO.O1CCCC1
Miscellaneous
OtherReaction
7156f34f0b223a21fe8e63830f3aca92fa983f2819e149259ffa96be70b7d466
2c5b5782f2989be8587a871e910ab32ac50067c6617ca6fd58b9c99c5fcadb6f
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[c:4]:[c:5](-[SH;D1;+0:6]):[c:7].[O;D1;H0:8]=[c;H0;D3;+0:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[s;H0;D2;+0:14]:[n;H0;D3;+0:15]:1-[c;H0;D3;+0:16](:[c:17]:[c:18]):[c:19]:[c:20]>>[O;D1;H0:8]=[C;H0;D3;+0:9](-[NH;D2;+0:15]-[c;H0;D3;+0:16](:[c:17]:[c:18]):[c:19]:[c:20])-[c:10](:[c:11]):[c:12](-[...
95.5
[{"value": 95.5, "product": "S(N)(=O)(=O)C1=CC=C(C=C1)NC(=O)C1=C(C=CC=C1)SSC1=C(C(=O)O)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the method of Example 132 using a suspension of 0.46 g (1.5 mmol) of 4-(3-oxo-3H-benzo[d]isothiazol-2-yl)benzene sulfonamide in a mixture of 15 mL of methanol and 15 mL of tetrahydrofuran, and 0.23 g (1.5 mmol) of thiosalicylic acid. The product was washed with ether and dried in...
10.6084/m9.figshare.5104873.v1
null
Aromatic thiol
Secondary amide.Disulfide
c1ccc2sncc2c1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
null
CO.O1CCCC1
null
null
NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1.O=C(O)c1ccccc1S>CO.O1CCCC1>NS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSc2ccccc2C(=O)O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-52d9d3961073476a8fa59d53b9462e89
COC(=O)c1ccccc1S.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1>>COC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1
O=C1N(SC2=C1C=CC=C2)C2=CC=C(C=C2)S(=O)(=O)N.C(C=1C(S)=CC=CC1)(=O)OC>>S(N)(=O)(=O)C1=CC=C(C=C1)NC(=O)C1=C(C=CC=C1)SSC1=C(C(=O)OC)C=CC=C1
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[SH:11].[s:12]1[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[c:19](=[O:20])[n:21]1-[c:22]1[cH:23][cH:24][c:25]([S:26]([NH2:27])(=[O:28])=[O:29])[cH:30][cH:31]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11][S:12][c:13]1[cH:14][cH:15][cH:1...
COC(=O)c1ccccc1S.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1
COC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1
null
null
CO.O1CCCC1
Miscellaneous
OtherReaction
7156f34f0b223a21fe8e63830f3aca92fa983f2819e149259ffa96be70b7d466
2c5b5782f2989be8587a871e910ab32ac50067c6617ca6fd58b9c99c5fcadb6f
O=C(Nc1ccccc1)c1ccccc1SSc1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5](-[SH;D1;+0:6]):[c:7].[O;D1;H0:8]=[c;H0;D3;+0:9]1:[c:10](:[c:11]):[c:12](:[c:13]):[s;H0;D2;+0:14]:[n;H0;D3;+0:15]:1-[c;H0;D3;+0:16](:[c:17]:[c:18]):[c:19]:[c:20]>>[#8:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5](-[S;H0;D2;+0:6]-[S;H0;D2;+0:14]-[c:12](:[c:13]):[c:10](-[C;H0;D3;+0:9](=[O;D1;H0...
92.7
[{"value": 92.7, "product": "S(N)(=O)(=O)C1=CC=C(C=C1)NC(=O)C1=C(C=CC=C1)SSC1=C(C(=O)OC)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared according to the method of Example 132 using a suspension of 0.46 g (1.5 mmol) of 4-(3-oxo-3H-benzo[d]isothiazol-2-yl)benzene sulfonamide in a mixture of 15 mL of methanol and 15 mL of tetrahydrofuran, and 0.27 g (1.6 mmol) of methyl thiosalicylate. The product was triturated with ether, filt...
10.6084/m9.figshare.5104873.v1
null
Aromatic thiol
Secondary amide.Disulfide
c1ccc2sncc2c1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
null
CO.O1CCCC1
null
null
COC(=O)c1ccccc1S.NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1>CO.O1CCCC1>COC(=O)c1ccccc1SSc1ccccc1C(=O)Nc1ccc(S(N)(=O)=O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-039c45d2d6ad447186631f36b49d7ebe
NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1.OCC(O)CS>>NS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSCC(O)CO)cc1
O=C1N(SC2=C1C=CC=C2)C2=CC=C(C=C2)S(=O)(=O)N.O1CCCC1.OC(CS)CO>>OC(CSSC1=C(C(=O)NC2=CC=C(C=C2)S(N)(=O)=O)C=CC=C1)CO
[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8](-[n:9]2[c:10](=[O:11])[c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]3[s:18]2)[cH:25][cH:26]1.[SH:19][CH2:20][CH:21]([OH:22])[CH2:23][OH:24]>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8]([NH:9][C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[S:18][S:19][CH2:...
NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1.OCC(O)CS
NS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSCC(O)CO)cc1
null
null
CO
Miscellaneous
OtherReaction
b009af05d472ccdcc7c275cf7d538d0fec35d7c49529303a2e355b9dd8798d3e
e8a16c39a4da768b069d0811166d9dd2e9252bf47af9bd7cebb79eb4280a5696
O=C(Nc1ccccc1)c1ccccc1
[C:1]-[C:2]-[SH;D1;+0:3].[O;D1;H0:4]=[c;H0;D3;+0:5]1:[c:6](:[c:7]):[c:8](:[c:9]):[s;H0;D2;+0:10]:[n;H0;D3;+0:11]:1-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]>>[C:1]-[C:2]-[S;H0;D2;+0:3]-[S;H0;D2;+0:10]-[c:8](:[c:9]):[c:6](-[C;H0;D3;+0:5](=[O;D1;H0:4])-[NH;D2;+0:11]-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16]):[c:7...
null
[]
null
null
null
null
This compound was prepared according to the method of Example 132 using a suspension of 0.46 g (1.5 mmol) of 4-(3-oxo-3H-benzo[d]isothiazol-2-yl) benzenesulfonamide in a mixture of 15 mL of methanol, and 15 mL of tetrahydrofuran and 2,3-dihydroxy-1-propanethiol. The product was washed with ether and dried in vacuo to g...
10.6084/m9.figshare.5104873.v1
null
Aliphatic thiol
Secondary amide.Disulfide
c1ccc2sncc2c1
c1ccccc1
c1ccccc1.c1ccccc1
null
CO
null
null
NS(=O)(=O)c1ccc(-n2sc3ccccc3c2=O)cc1.OCC(O)CS>CO>NS(=O)(=O)c1ccc(NC(=O)c2ccccc2SSCC(O)CO)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8b264e10282d462783a148a83796833e
CC(=O)N[C@@H](CS)C(=O)O.CCC(C)C(C(=O)O)n1sc2ccccc2c1=O>>CCC(C)C(NC(=O)c1ccccc1S[SH](CCC(=O)O)NC(C)=O)C(=O)O
CC(C(C(=O)O)N1SC2=C(C1=O)C=CC=C2)CC.C(C)(=O)N[C@@H](CS)C(=O)O>>C(C)(=O)NS(SC1=C(C(=O)NC(C(=O)O)C(CC)C)C=CC=C1)CCC(=O)O
[SH:16][CH2:17][C@@H:18]([C:19](=[O:20])[OH:21])[NH:22][C:23]([CH3:24])=[O:25].[CH3:1][CH2:2][CH:3]([CH3:4])[CH:5]([n:6]1[c:7](=[O:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[s:15]1)[C:26](=[O:27])[OH:28]>>[CH3:1][CH2:2][CH:3]([CH3:4])[CH:5]([NH:6][C:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[S:15][SH:16]([CH...
CC(=O)N[C@@H](CS)C(=O)O.CCC(C)C(C(=O)O)n1sc2ccccc2c1=O
CCC(C)C(NC(=O)c1ccccc1S[SH](CCC(=O)O)NC(C)=O)C(=O)O
null
null
CO
Miscellaneous
OtherReaction
af210ac592073827101a713c86f606364ea86b0e185a54e240864af93e67c70c
f1560323bad9af1dc55279d6e8cf7e6a1314dd20a0b0e11e3d2fbbb83e4fd24d
c1ccccc1
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[NH;D2;+0:4]-[C@@H;D3;+0:5](-[C:6]-[SH;D1;+0:7])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10].[C:11]-[C:12](-[C:13](=[O;D1;H0:14])-[O;D1;H1:15])-[n;H0;D3;+0:16]1:[s;H0;D2;+0:17]:[c:18](:[c:19]):[c:20](:[c:21]):[c;H0;D3;+0:22]:1=[O;D1;H0:23]>>[C:11]-[C:12](-[NH;D2;+0:16]-[C;H0;D3;+0:22](=[O;D1;H0:23]...
null
[]
null
null
18
HOUR
A solution of 0.58 g (2.2 mmol) of [S-(R*,R*)]-3-methyl-2-(3-oxo-3H-benzo[d]isothiazol-2-yl)pentanoic acid in 20 mL of methanol was treated with 0.36 g (2.2 mmol) of N-acetyl-L-cysteine and the reaction was stirred at room temperature for 18 hours. The solvent was removed in vacuo and the residue was triturated with 10...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Aliphatic thiol
Secondary amide.Secondary amide
c1ccc2sncc2c1
c1ccccc1
c1ccccc1
null
CO
null
18
CC(=O)N[C@@H](CS)C(=O)O.CCC(C)C(C(=O)O)n1sc2ccccc2c1=O>CO>CCC(C)C(NC(=O)c1ccccc1S[SH](CCC(=O)O)NC(C)=O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-950cfed0e8884a9ab3f2f0fdcbee3869
CCOC(=O)N=NC(=O)OCC.O=C(c1ccccc1)c1ccccc1S>>O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1
SC1=C(C(=O)C2=CC=CC=C2)C=CC=C1.N(=NC(=O)OCC)C(=O)OCC>>C(C1=CC=CC=C1)(=O)C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)C1=CC=CC=C1
O=[C:3](N=N[C:2](O[CH2:8][CH3:7])=[O:1])O[CH2:21][CH3:20].[c:9]1([C:23](=[O:24])[c:25]2[cH:26][cH:27][cH:28][cH:29][cH:30]2)[cH:10][cH:11][cH:12][cH:13][c:14]1[SH:15]>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[S:15][S:16][c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[C:23](...
CCOC(=O)N=NC(=O)OCC.O=C(c1ccccc1)c1ccccc1S
O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1
null
null
C1=CC=CC=C1.C(C)OCC
Aromatic Heterocycle Formation
OtherReaction
ae531ed1d67e6f3eff4e1aecb1c565f4851e348294c3b629df76efe8dc4172ca
50231886f82502b0a0a5c3927d4f2befa588a6f1d904da84171fca8b4ef3048c
O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1
O=[C;H0;D3;+0:1](-N=N-[C;H0;D3;+0:2](=[O;D1;H0:3])-O-[CH2;D2;+0:4]-[CH3;D1;+0:5])-O-[CH2;D2;+0:6]-[CH3;D1;+0:7].[O;D1;H0:8]=[C;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[c;H0;D3;+0:13](:[c:14]:[c:15]):[c:16](-[SH;D1;+0:17]):[c:18]>>[O;D1;H0:3]=[C;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[c:19]:[c:20]:[c:21]:[cH;D2;+0:5]:[cH;D2;+0:4]:1)...
50.7
[{"value": 50.0, "product": "C(C1=CC=CC=C1)(=O)C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.7, "product": "C(C1=CC=CC=C1)(=O)C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
To a solution of 2-mercaptobenzophenone (2.3 g, 7.4 mmol) in diethyl ether (10 mL) was added dropwise diethyl azodicarboxylate (0.65 g, 3.7 mmol). The solution was stirred for 5 minutes at room temperature, then diluted with benzene (40 mL) and refluxed for 16 hours. The solution was cooled and concentrated in vacuo le...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether.Ether.Diazene.Aromatic thiol
Ketone.Ketone.Disulfide
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
C1=CC=CC=C1.C(C)OCC
null
0.083333
CCOC(=O)N=NC(=O)OCC.O=C(c1ccccc1)c1ccccc1S>C1=CC=CC=C1.C(C)OCC>O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-169cfd162f7a4903b732bbd90fedb229
NO.O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1>>O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=NO)c1ccccc1
C(C)(=O)OCC.C(C1=CC=CC=C1)(=O)C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)C1=CC=CC=C1.Cl.NO.Cl>>ON=C(C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)C1=CC=CC=C1)C1=CC=CC=C1
[NH2:24][OH:25].O=[C:23]([c:22]1[c:17]([S:16][S:15][c:14]2[c:9]([C:2](=[O:1])[c:3]3[cH:4][cH:5][cH:6][cH:7][cH:8]3)[cH:10][cH:11][cH:12][cH:13]2)[cH:18][cH:19][cH:20][cH:21]1)[c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[S:15][S:...
NO.O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1
O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=NO)c1ccccc1
null
null
C(C)O.N1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
b5fd91d879f097d0ef2e8e2d3ef7d2ef0195968870a9602a47b8324c601790b9
1a0ef15294bdb221fb8888b5d4c7fcf00473b11e53da288791d32747daa48d23
N=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1
O=[C;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7].[NH2;D1;+0:8]-[O;D1;H1:9]>>[O;D1;H1:9]-[N;H0;D2;+0:8]=[C;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7]
35.9
[{"value": 32.0, "product": "ON=C(C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)C1=CC=CC=C1)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 35.9, "product": "ON=C(C1=C(C=CC=C1)SSC1=C(C=CC=C1)C(=O)C1=CC=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The [2-(2-benzoyl-phenyldisulfanyl)-phenyl]phenyl-methanone (0.55 g, 1.2 mmol) was diluted with ethanol (5 mL) and anhydrous pyridine (5 mL). Hydroxylamine hydrochloride (1 g, 14 mmol) was added and the solution was refluxed for 90 minutes. The solution was cooled and poured into cold aqueous HCl (1N). Ethyl acetate wa...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Oxime
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
C(C)O.N1=CC=CC=C1
null
null
NO.O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=O)c1ccccc1>C(C)O.N1=CC=CC=C1>O=C(c1ccccc1)c1ccccc1SSc1ccccc1C(=NO)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f05182efc7494917864a6ea459070b88
O=P(O)(O)O.O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].O=S(=O)(O)O>>O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3
N.[O-]P(=O)([O-])[O-].[O-]P(=O)([O-])[O-].[O-]P(=O)([O-])[O-].[F-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].P(O)(O)(O)=O.S(O)(O)(=O)=O>>O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3
[O:1]=[P:2]([OH:3])([OH:9])[OH:13].[O-][P:4]([O-])([O-])=[O:5].[O-][P:7]([O-])(=[O:6])[O-:8].[O-][P:11]([O-])([O-])=[O:12].O=S(=O)([OH:10])[OH:14]>>[O:1]=[P:2]12[O:3][P:4]3(=[O:5])[O:6][P:7](=[O:8])([O:9]1)[O:10][P:11](=[O:12])([O:13]2)[O:14]3
O=P(O)(O)O.O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].O=S(=O)(O)O
O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3
null
null
null
Miscellaneous
OtherReaction
bbf733c5cb49dcf8bae08bd465b7cb92c6362632f86a8f05af9849a1d176f723
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3
O=S(=O)(-[OH;D1;+0:1])-[OH;D1;+0:2].[O-;H0;D1:3]-[P;H0;D4;+0:4](-[O-])(-[O-])=[O;H0;D1;+0:5].[O-]-[P;H0;D4;+0:6](-[O-])(-[O-])=[O;D1;H0:7].[O-]-[P;H0;D4;+0:8](-[O-])(-[O-])=[O;D1;H0:9].[O;D1;H0:10]=[#15:11](-[OH;D1;+0:12])(-[OH;D1;+0:13])-[OH;D1;+0:14]>>[O;D1;H0:9]=[P;H0;D4;+0:8]12-[O;H0;D2;+0:1]-[P;H0;D4;+0:4]3(=[O;H0...
null
[]
null
null
null
null
In 1970, Richmond et al ('641 supra) reacted phosphate rock with phosphoric acid and then with sulfuric acid. The resulting acidulate was subsequently neutralized with anhydrous ammonia to produce a 7-21-0 (N--P2O5 --K2O) grade slurrey fertilizer. In later investigations Pottgiesser et al ('162 supra) produced a 13.5-6...
10.6084/m9.figshare.5104873.v1
null
null
null
null
O1P2OP3OP1OP(O2)O3
O1P2OP3OP1OP(O2)O3
HO-
null
null
null
O=P(O)(O)O.O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].O=S(=O)(O)O>>O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-97bc304407514ba8bc93cfbe5770416a
CC(=O)OO.CN(c1cccc(Cl)c1Cl)S(=O)(=O)c1ccccn1>>CN(c1cccc(Cl)c1Cl)S(=O)(=O)c1cccc[n+]1[O-]
CN(S(=O)(=O)C1=NC=CC=C1)C1=C(C(=CC=C1)Cl)Cl.C(C)(=O)OO>>CN(S(=O)(=O)C=1[N+](=CC=CC1)[O-])C1=C(C(=CC=C1)Cl)Cl
CC(=O)O[OH:20].[CH3:1][N:2]([c:3]1[cH:4][cH:5][cH:6][c:7]([Cl:8])[c:9]1[Cl:10])[S:11](=[O:12])(=[O:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][n:19]1>>[CH3:1][N:2]([c:3]1[cH:4][cH:5][cH:6][c:7]([Cl:8])[c:9]1[Cl:10])[S:11](=[O:12])(=[O:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][n+:19]1[O-:20]
CC(=O)OO.CN(c1cccc(Cl)c1Cl)S(=O)(=O)c1ccccn1
CN(c1cccc(Cl)c1Cl)S(=O)(=O)c1cccc[n+]1[O-]
null
null
null
Miscellaneous
OtherReaction
a6e542b06734899af4300a4d264aed7eb1e13d986216fa692ade3c6e81fedca9
c3ab83b3edcbc4bfd42c0a952aa2c988db0a3f4c3e00c1396c2ecfcd2e6940e6
O=S(=O)(Nc1ccccc1)c1cccc[nH+]1
C-C(=O)-O-[OH;D1;+0:1].[#16:2]-[c:3](:[c:4]):[n;H0;D2;+0:5]:[c:6]:[c:7]>>[#16:2]-[c:3](:[c:4]):[n+;H0;D3:5](-[O-;H0;D1:1]):[c:6]:[c:7]
null
[]
null
null
null
null
N-methyl-N-(2,3-dichlorophenyl)-2-pyridinesulfonamide (1.7 g, 5.3 mmol) is treated with 40% peracetic acid (approx. 12 ml) at 35°-45° under N2 for 14 hours. The excess peracetic acid is removed under vacuum, and the residue is diluted with methylene chloride, poured into water, neutralized with aq. sodium bicarbonate, ...
10.6084/m9.figshare.5104873.v1
null
Peroxide
null
c1ccncc1
C1=CC=[NH+]C=C1
c1ccccc1.C1=CC=[NH+]C=C1
HO-
null
null
null
CC(=O)OO.CN(c1cccc(Cl)c1Cl)S(=O)(=O)c1ccccn1>>CN(c1cccc(Cl)c1Cl)S(=O)(=O)c1cccc[n+]1[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-032d77276ec347c0b8611cfd56e26b51
C=CCBr.O=S(=O)(Nc1ccccc1C(F)(F)F)c1cccc[n+]1[O-]>>C=CCN(c1ccccc1C(F)(F)F)S(=O)(=O)c1cccc[n+]1[O-]
C(C=C)Br.FC(C1=C(C=CC=C1)NS(=O)(=O)C=1[N+](=CC=CC1)[O-])(F)F.[H-].[Na+]>>C(C=C)N(S(=O)(=O)C=1[N+](=CC=CC1)[O-])C1=C(C=CC=C1)C(F)(F)F
Br[CH2:3][CH:2]=[CH2:1].[NH:4]([c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[C:11]([F:12])([F:13])[F:14])[S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][cH:21][cH:22][n+:23]1[O-:24]>>[CH2:1]=[CH:2][CH2:3][N:4]([c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[C:11]([F:12])([F:13])[F:14])[S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][cH:21][c...
C=CCBr.O=S(=O)(Nc1ccccc1C(F)(F)F)c1cccc[n+]1[O-]
C=CCN(c1ccccc1C(F)(F)F)S(=O)(=O)c1cccc[n+]1[O-]
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
4b716d2054b81e5a5a6e7964bd25a3d424d12bd268f271f58b49ac0e4ed91ee6
90c7a3d73a4d167431bb3c161f6525d0660b6b51ccf160c8c2113b2fb8ab28eb
O=S(=O)(Nc1ccccc1)c1cccc[nH+]1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[#7;a;+:4]:[c:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[#7;a;+:4]:[c:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[N;H0;D3;+0:9](-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3])-[c:10](:[c:11]):[c:12]
null
[]
null
null
30
MINUTE
To N-(2-trifluoromethylphenyl)-2-pyridinesulfonamide 1-oxide (compound 129, Table A) (1.0 g, 3.0 mmol) in 10 ml of DMF is added NaH (0.30 g, 6.2 mmol) under N2, and the mixture is stirred at RT for 30 minutes. Allyl bromide (0.82 g, 0.59 ml, 6.8 mmol) is added dropwise, and the mixture is stirred at RT for 48 hours. It...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Primary halide
Tertiary amine.Allyl
null
null
c1ccccc1.C1=CC=[NH+]C=C1
HBr
CN(C)C=O
null
0.5
C=CCBr.O=S(=O)(Nc1ccccc1C(F)(F)F)c1cccc[n+]1[O-]>CN(C)C=O>C=CCN(c1ccccc1C(F)(F)F)S(=O)(=O)c1cccc[n+]1[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6da5e6fc912a4f39abb42807db3359a7
CC(=O)OO.CN(c1ncc(Cl)cc1Cl)S(=O)(=O)c1ccccn1>>CN(c1ncc(Cl)cc1Cl)S(=O)(=O)c1cccc[n+]1[O-]
CN(S(=O)(=O)C1=NC=CC=C1)C1=NC=C(C=C1Cl)Cl.C(C)(=O)OO>>CN(S(=O)(=O)C=1[N+](=CC=CC1)[O-])C1=NC=C(C=C1Cl)Cl
CC(=O)O[OH:20].[CH3:1][N:2]([c:3]1[n:4][cH:5][c:6]([Cl:7])[cH:8][c:9]1[Cl:10])[S:11](=[O:12])(=[O:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][n:19]1>>[CH3:1][N:2]([c:3]1[n:4][cH:5][c:6]([Cl:7])[cH:8][c:9]1[Cl:10])[S:11](=[O:12])(=[O:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][n+:19]1[O-:20]
CC(=O)OO.CN(c1ncc(Cl)cc1Cl)S(=O)(=O)c1ccccn1
CN(c1ncc(Cl)cc1Cl)S(=O)(=O)c1cccc[n+]1[O-]
null
null
null
Miscellaneous
OtherReaction
a6e542b06734899af4300a4d264aed7eb1e13d986216fa692ade3c6e81fedca9
c3ab83b3edcbc4bfd42c0a952aa2c988db0a3f4c3e00c1396c2ecfcd2e6940e6
O=S(=O)(Nc1ccccn1)c1cccc[nH+]1
C-C(=O)-O-[OH;D1;+0:1].[#16:2]-[c:3](:[c:4]):[n;H0;D2;+0:5]:[c:6]:[c:7]>>[#16:2]-[c:3](:[c:4]):[n+;H0;D3:5](-[O-;H0;D1:1]):[c:6]:[c:7]
null
[]
null
null
null
null
Following the procedures of Example 1, N-methyl-N-(3,5-dichloro-2-pyridyl)-2-pyridinesulfonamide is oxidized with 40% peracetic acid to give the title compound, MS m/e 334.00 (M+). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Peroxide
null
c1ccncc1
C1=CC=[NH+]C=C1
c1ccncc1.C1=CC=[NH+]C=C1
HO-
null
null
null
CC(=O)OO.CN(c1ncc(Cl)cc1Cl)S(=O)(=O)c1ccccn1>>CN(c1ncc(Cl)cc1Cl)S(=O)(=O)c1cccc[n+]1[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a21c399ab50c44979c3f814313d13bd3
CI.O=S(=O)(Nc1cccnc1Cl)c1cccc[n+]1[O-]>>CN(c1cccnc1Cl)S(=O)(=O)c1cccc[n+]1[O-]
ClC1=NC=CC=C1NS(=O)(=O)C=1[N+](=CC=CC1)[O-].CI>>CN(S(=O)(=O)C=1[N+](=CC=CC1)[O-])C=1C(=NC=CC1)Cl
I[CH3:1].[NH:2]([c:3]1[cH:4][cH:5][cH:6][n:7][c:8]1[Cl:9])[S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][n+:18]1[O-:19]>>[CH3:1][N:2]([c:3]1[cH:4][cH:5][cH:6][n:7][c:8]1[Cl:9])[S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][n+:18]1[O-:19]
CI.O=S(=O)(Nc1cccnc1Cl)c1cccc[n+]1[O-]
CN(c1cccnc1Cl)S(=O)(=O)c1cccc[n+]1[O-]
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
c6ca050f6d67acb7bc6fc8b4d7848b3f349e4e8db81643cbb6d12b5a34cbf965
9d3dfd18cb6410898a6d822a6d80081d602cf34984cafbfa56b84aa4b38ddbf6
O=S(=O)(Nc1cccnc1)c1cccc[nH+]1
I-[CH3;D1;+0:1].[#7;a;+:2]:[c:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10](-[Cl;D1;H0:11]):[#7;a:12]:[c:13]>>[#7;a;+:2]:[c:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[N;H0;D3;+0:7](-[CH3;D1;+0:1])-[c:8](:[c:9]):[c:10](-[Cl;D1;H0:11]):[#7;a:12]:[c:13]
null
[]
null
null
null
null
The title compound of Example 5 above is reacted with methyl iodide (0.6 g, 0.26 ml, 4.2 mmol) to give N-methyl-N-(2-chloro-3-pyridyl)-2-pyridinesulfonamide 1-oxide, MS m/e 300.00 (M+ +1). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Tertiary amine
null
null
c1ccncc1.C1=CC=[NH+]C=C1
HI
null
null
null
CI.O=S(=O)(Nc1cccnc1Cl)c1cccc[n+]1[O-]>>CN(c1cccnc1Cl)S(=O)(=O)c1cccc[n+]1[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-acc451c6d71348d3baa782dc1cdfbe6d
C1CO1.CC(C)(C)CCCCC(=O)O>>CC(C)(C)CCCCC(=O)OCCO
C1CO1.C1CO1.C1CO1.C=C.C1CO1.C1CO1.C(CCCCC(C)(C)C)(=O)O.C1CO1.C1CO1.C1CO1>>C(CCCCC(C)(C)C)(=O)OCCO
[CH2:12]1[CH2:13][O:14]1.[CH3:1][C:2]([CH3:3])([CH3:4])[CH2:5][CH2:6][CH2:7][CH2:8][C:9](=[O:10])[OH:11]>>[CH3:1][C:2]([CH3:3])([CH3:4])[CH2:5][CH2:6][CH2:7][CH2:8][C:9](=[O:10])[O:11][CH2:12][CH2:13][OH:14]
C1CO1.CC(C)(C)CCCCC(=O)O
CC(C)(C)CCCCC(=O)OCCO
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
465f35bbfde0d5babd162017ed09f5142d87aedf8ed0abe047dfea06e57e4673
def7b1b7f2b04b0f2ff5ecfc0b043d7990825ab8ad8f99ebaf633c8077c610aa
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4].[C:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[CH2;D2;+0:6]-[C:5]-[OH;D1;+0:7]
null
[]
100
CELSIUS
20
MINUTE
To a one liter stainless steel autoclave, equipped with a mechanical stirrer, heater, cooling coils, automatic temperature controller, and a tared ethylene oxide cylinder, in a series of runs is added 500 grams neononanoic acid and 2.0 g of the selected catalyst. The reactor is heated to approximately 100° C. and a gas...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether
Ester.Primary alcohol
C1CO1
null
null
null
null
100
0.333333
C1CO1.CC(C)(C)CCCCC(=O)O>>CC(C)(C)CCCCC(=O)OCCO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d50e6d173a8247479425da3781712173
C1CO1.CC(C)(C)CCCCCC(=O)O>>CC(C)(C)CCCCCC(=O)OCCO
C1CO1.C(CCCCCC(C)(C)C)(=O)O>>C(CCCCCC(C)(C)C)(=O)OCCO
[CH2:13]1[CH2:14][O:15]1.[CH3:1][C:2]([CH3:3])([CH3:4])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C:10](=[O:11])[OH:12]>>[CH3:1][C:2]([CH3:3])([CH3:4])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C:10](=[O:11])[O:12][CH2:13][CH2:14][OH:15]
C1CO1.CC(C)(C)CCCCCC(=O)O
CC(C)(C)CCCCCC(=O)OCCO
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
465f35bbfde0d5babd162017ed09f5142d87aedf8ed0abe047dfea06e57e4673
def7b1b7f2b04b0f2ff5ecfc0b043d7990825ab8ad8f99ebaf633c8077c610aa
null
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4].[C:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[CH2;D2;+0:6]-[C:5]-[OH;D1;+0:7]
null
[]
100
CELSIUS
20
MINUTE
To a one liter stainless steel autoclave, equipped with a mechanical stirrer, heater, cooling coils, automatic temperature controller, and a tared ethylene oxide cylinder, in a series of runs is added 500 grams neodecanoic acid and 2.0 g of the selected catalyst. The reactor is heated to approximately 100° C. and a gas...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether
Ester.Primary alcohol
C1CO1
null
null
null
null
100
0.333333
C1CO1.CC(C)(C)CCCCCC(=O)O>>CC(C)(C)CCCCCC(=O)OCCO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8fea9f03fff34b1c8f6436c578cdb536
CCOC(=O)CCNC(=O)C(CSC(C)=O)Cc1ccccc1>>O=C(O)CCNC(=O)C(CS)Cc1ccccc1
[OH-].[Na+].C1(=CC=CC=C1)C.C(C)(=O)O.C(C)(=O)SCC(C(=O)NCCC(=O)OCC)CC1=CC=CC=C1.[OH-].[Na+]>>SCC(C(=O)NCCC(=O)O)CC1=CC=CC=C1
CC[O:3][C:2](=[O:1])[CH2:4][CH2:5][NH:6][C:7](=[O:8])[CH:9]([CH2:10][S:11]C(C)=O)[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][NH:6][C:7](=[O:8])[CH:9]([CH2:10][SH:11])[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
CCOC(=O)CCNC(=O)C(CSC(C)=O)Cc1ccccc1
O=C(O)CCNC(=O)C(CS)Cc1ccccc1
null
null
CO
Reduction
OtherReaction
1bcd8cbb2f136b4bcba1690e9ba45c4e43c89ba76f0e22de82a7d3fe318c82a9
5654c46fe4cb226f88ec3c899c7f9be1825c357673ea686958f9ef4883ee1db3
c1ccccc1
C-C(=O)-[S;H0;D2;+0:1]-[C:2]-[C:3]-[C:4](-[#7:5])=[O;D1;H0:6].C-C-[O;H0;D2;+0:7]-[C:8](-[C:9])=[O;D1;H0:10]>>[#7:5]-[C:4](=[O;D1;H0:6])-[C:3]-[C:2]-[SH;D1;+0:1].[C:9]-[C:8](=[O;D1;H0:10])-[OH;D1;+0:7]
null
[]
null
null
3
HOUR
A solution of the product from part (a) (1.02 g., 3.02 mmole) in methanol (6 ml.) is chilled (ice/methanol) and to it, under nitrogen, is added 1N sodium hydroxide (6.35 ml.) over 15 minutes. The mixture is stirred for 3 hours while warming to room temperature (TLC indicates incomplete reaction), and additional 1N sodi...
10.6084/m9.figshare.5104873.v1
null
Ester.Carbo-thioester
Carboxylic acid.Aliphatic thiol
null
null
c1ccccc1
HO-
CO
null
3
CCOC(=O)CCNC(=O)C(CSC(C)=O)Cc1ccccc1>CO>O=C(O)CCNC(=O)C(CS)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f14fe96832c846f8acc6375afbb7a901
CC(=O)SCC(Cc1ccccc1)C(=O)O.COC(=O)CCCN>>COC(=O)CCCNC(=O)C(CSC(C)=O)Cc1ccccc1
C(C(=O)Cl)(=O)Cl.C(C)(=O)SCC(C(=O)O)CC1=CC=CC=C1.Cl.NCCCC(=O)OC.C(C)(C)N(CC)C(C)C>>C(C)(=O)SCC(C(=O)NCCCC(=O)OC)CC1=CC=CC=C1
O[C:9](=[O:10])[CH:11]([CH2:12][S:13][C:14]([CH3:15])=[O:16])[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1.[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][CH2:7][NH2:8]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][CH2:7][NH:8][C:9](=[O:10])[CH:11]([CH2:12][S:13][C:14]([CH3:15])=[O:16])[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:...
CC(=O)SCC(Cc1ccccc1)C(=O)O.COC(=O)CCCN
COC(=O)CCCNC(=O)C(CSC(C)=O)Cc1ccccc1
null
CN(C=O)C
C(Cl)Cl.C(C)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])-[C:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:4]-[C:3](-[C:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C:7]-[C:6]
null
[]
null
null
1
HOUR
Oxalyl chloride (0.37 ml., 4.2 mmole) is added, under nitrogen, to a solution of (±)-2-[(acetylthio)methyl]-3-phenylpropanoic acid (0.95 g., 4.0 mmole) in ethyl ether (8 ml.). This mixture is cautiously treated with a catalytic amont of dimethylformamide (3 drops), and then stirred for one hour at room temperature. Aft...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
CN(C=O)C.C(Cl)Cl.C(C)OCC
null
1
CC(=O)SCC(Cc1ccccc1)C(=O)O.COC(=O)CCCN>CN(C=O)C.C(Cl)Cl.C(C)OCC>COC(=O)CCCNC(=O)C(CSC(C)=O)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-769057d21a9f49c2a23e796d958b008c
COC(=O)CCCCNC(=O)C(CSC(C)=O)Cc1ccccc1>>O=C(O)CCCCNC(=O)C(CS)Cc1ccccc1
[OH-].[Na+].C(C)(=O)SCC(C(=O)NCCCCC(=O)OC)CC1=CC=CC=C1>>SCC(C(=O)NCCCCC(=O)O)CC1=CC=CC=C1
CC(=O)[S:13][CH2:12][CH:11]([C:9]([NH:8][CH2:7][CH2:6][CH2:5][CH2:4][C:2](=[O:1])[O:3]C)=[O:10])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][CH2:7][NH:8][C:9](=[O:10])[CH:11]([CH2:12][SH:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
COC(=O)CCCCNC(=O)C(CSC(C)=O)Cc1ccccc1
O=C(O)CCCCNC(=O)C(CS)Cc1ccccc1
null
null
CO.C(C)(=O)OCC
Reduction
OtherReaction
1bcd8cbb2f136b4bcba1690e9ba45c4e43c89ba76f0e22de82a7d3fe318c82a9
5654c46fe4cb226f88ec3c899c7f9be1825c357673ea686958f9ef4883ee1db3
c1ccccc1
C-C(=O)-[S;H0;D2;+0:1]-[C:2]-[C:3]-[C:4](-[#7:5])=[O;D1;H0:6].C-[O;H0;D2;+0:7]-[C:8](-[C:9])=[O;D1;H0:10]>>[#7:5]-[C:4](=[O;D1;H0:6])-[C:3]-[C:2]-[SH;D1;+0:1].[C:9]-[C:8](=[O;D1;H0:10])-[OH;D1;+0:7]
null
[]
null
null
10
MINUTE
1N Sodium hydroxide (12.9 ml., 3.8 equiv.) is added dropwise over 10 minutes to a chilled solution (ice bath) of the product from part (b) (1.20 g., 3.41 mmole) dissolved in methanol (13 ml.) under a nitrogen atmosphere. The mixture is stirred at 0° for 10 minutes and then allowed to warm to room temperature and stirre...
10.6084/m9.figshare.5104873.v1
null
Ester.Carbo-thioester
Carboxylic acid.Aliphatic thiol
null
null
c1ccccc1
HO-
CO.C(C)(=O)OCC
null
0.166667
COC(=O)CCCCNC(=O)C(CSC(C)=O)Cc1ccccc1>CO.C(C)(=O)OCC>O=C(O)CCCCNC(=O)C(CS)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-878353b2e518459d97d4c3e89c51a6f3
COC(=O)CCCCCCNC(=O)C(CSC(C)=O)Cc1ccccc1>>COC(=O)CCCCCCNC(=O)C(CS)Cc1ccccc1
O.Cl.[OH-].[Na+].C(C)(=O)SCC(C(=O)NCCCCCCC(=O)OC)CC1=CC=CC=C1>>SCC(C(=O)NCCCCCCC(=O)OC)CC1=CC=CC=C1
CC(=O)[S:16][CH2:15][CH:14]([C:12]([NH:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][C:3]([O:2][CH3:1])=[O:4])=[O:13])[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][NH:11][C:12](=[O:13])[CH:14]([CH2:15][SH:16])[CH2:17][c:18]1[cH:19][cH:20][cH:2...
COC(=O)CCCCCCNC(=O)C(CSC(C)=O)Cc1ccccc1
COC(=O)CCCCCCNC(=O)C(CS)Cc1ccccc1
null
[Zn]
CO
Reduction
OtherReaction
7702cd666d5d9a9f1bdea3600e3b84cc62dd11d3f2cea261702317a39db4e581
18d802456fe85193570fdb3a00b25c8956a03b5a0210f708f961e42c1669d76e
c1ccccc1
C-C(=O)-[S;H0;D2;+0:1]-[C:2]-[C:3]-[C:4](-[#7:5])=[O;D1;H0:6]>>[#7:5]-[C:4](=[O;D1;H0:6])-[C:3]-[C:2]-[SH;D1;+0:1]
null
[]
null
null
null
null
(±)-7-[[2-[(Acetylthio)methyl]-1-oxo-3-phenylpropyl]amino]heptanoic acid, methyl ester (1.43 g., 3.77 mmole) is dissolved in methanol (30 ml.) by warming, and then chilled in an ice bath under nitrogen. 1N Sodium hydroxide (3.77 ml., 1.0 eq.) is added dropwise over 10 minutes to this solution. The mixture is stirred at...
10.6084/m9.figshare.5104873.v1
null
Carbo-thioester
Aliphatic thiol
null
null
c1ccccc1
HO-
[Zn].CO
null
null
COC(=O)CCCCCCNC(=O)C(CSC(C)=O)Cc1ccccc1>[Zn].CO>COC(=O)CCCCCCNC(=O)C(CS)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cd6c544d691047e28572b2af8207df9c
CC(C)(N)CNCCN.CCC(C)=O>>CCC(C)NCCNCC(C)(C)N
[H][H].NC(CNCCN)(C)C.CC(CC)=O>>CC(CC)NCCNCC(C)(C)N
[NH2:5][CH2:6][CH2:7][NH:8][CH2:9][C:10]([CH3:11])([CH3:12])[NH2:13].O=[C:3]([CH2:2][CH3:1])[CH3:4]>>[CH3:1][CH2:2][CH:3]([CH3:4])[NH:5][CH2:6][CH2:7][NH:8][CH2:9][C:10]([CH3:11])([CH3:12])[NH2:13]
CC(C)(N)CNCCN.CCC(C)=O
CCC(C)NCCNCC(C)(C)N
null
[Pt]
CO
Heteroatom Alkylation and Arylation
Reductive amination with ketone
4940e8ed9a0db9bde699fdcdc3aff2cff0409c19478aa0ed1acfd98213338adf
07faf85ffe990e88a1de7fd04a339bf226f78d8bfae9712ea59eebd76bb54b9f
null
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[C;D1;H3:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[CH;D3;+0:1](-[C;D1;H3:2])-[C:3]-[C;D1;H3:4]
69.5
[{"value": 69.5, "product": "CC(CC)NCCNCC(C)(C)N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 146 g (1.1 moles) of N-(2-amino-2-methylpropyl)-1,2-ethanediamine, 84.4 (1.17 moles) of 2-butanone, 300 ml methanol, and 3.0 g of 10% platinum on carbon were reacted in a 1 liter autoclave at 80° C. under 800 pounds per square inch (psi) hydrogen pressure. After two hours the reaction mixture was cooled, t...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Secondary amine
null
null
null
Other
[Pt].CO
null
null
CC(C)(N)CNCCN.CCC(C)=O>[Pt].CO>CCC(C)NCCNCC(C)(C)N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b296aa432e43463e8f3c1a0d26a6db83
CCC(C)NCCN1CC(C)(C)NC(C)(C)C1=O.Clc1nc(Cl)nc(Cl)n1>>CCC(C)N(CCN1CC(C)(C)NC(C)(C)C1=O)c1nc(Cl)nc(Cl)n1
C([O-])([O-])=O.[Na+].[Na+].N1=C(Cl)N=C(Cl)N=C1Cl.CC(CC)NCCN1C(C(NC(C1)(C)C)(C)C)=O>>ClC1=NC(=NC(=N1)Cl)N(CCN1C(C(NC(C1)(C)C)(C)C)=O)C(CC)C
[CH3:1][CH2:2][CH:3]([CH3:4])[NH:5][CH2:6][CH2:7][N:8]1[CH2:9][C:10]([CH3:11])([CH3:12])[NH:13][C:14]([CH3:15])([CH3:16])[C:17]1=[O:18].Cl[c:19]1[n:20][c:21]([Cl:22])[n:23][c:24]([Cl:25])[n:26]1>>[CH3:1][CH2:2][CH:3]([CH3:4])[N:5]([CH2:6][CH2:7][N:8]1[CH2:9][C:10]([CH3:11])([CH3:12])[NH:13][C:14]([CH3:15])([CH3:16])[C:...
CCC(C)NCCN1CC(C)(C)NC(C)(C)C1=O.Clc1nc(Cl)nc(Cl)n1
CCC(C)N(CCN1CC(C)(C)NC(C)(C)C1=O)c1nc(Cl)nc(Cl)n1
null
null
O.CC(=O)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
1e1e3c2fd5a9e68e6b66ceb7f38ba57529dd1cfdb540b7a418aa13a9f2f6d698
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
O=C1CNCCN1CCNc1ncncn1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5](-[Cl;D1;H0:6]):[#7;a:7]:1.[C:8]-[C:9](-[C;D1;H3:10])-[NH;D2;+0:11]-[C:12]-[C:13]>>[C:8]-[C:9](-[C;D1;H3:10])-[N;H0;D3;+0:11](-[C:12]-[C:13])-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5](-[Cl;D1;H0:6]):[#7;a:7]:1
null
[]
null
null
30
MINUTE
In a 1 liter three-necked flask were placed 300 ml of water which was cooled to 1° C. 46.1 g (0.25 mole) of cyanuric chloride was dissolved in 240 ml acetone and added to the water in the flask. A white slurry formed which was stirred while adding to it dropwise, 63.9 g (0.25 mole) of 1-[2-(2-butylamino)ethyl]-3,3,5,5-...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ncncn1
c1ncncn1
C1C[NH]CCN1.c1ncncn1
HCl
O.CC(=O)C
null
0.5
CCC(C)NCCN1CC(C)(C)NC(C)(C)C1=O.Clc1nc(Cl)nc(Cl)n1>O.CC(=O)C>CCC(C)N(CCN1CC(C)(C)NC(C)(C)C1=O)c1nc(Cl)nc(Cl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-217b10af343044bfa5761f4da10eaeb8
COc1ccc(C(=O)Cl)c(OC)c1.NC1CN2CCC1CC2>>COc1ccc(C(=O)NC2CN3CCC2CC3)c(OC)c1
Cl.Cl.NC1CN2CCC1CC2.COC1=C(C(=O)Cl)C=CC(=C1)OC.C([O-])([O-])=O.[Na+].[Na+].O>>Cl.N12CC(C(CC1)CC2)NC(C2=C(C=C(C=C2)OC)OC)=O
Cl[C:7]([c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:21][c:18]1[O:19][CH3:20])=[O:8].[NH2:9][CH:10]1[CH2:11][N:12]2[CH2:13][CH2:14][CH:15]1[CH2:16][CH2:17]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[NH:9][CH:10]2[CH2:11][N:12]3[CH2:13][CH2:14][CH:15]2[CH2:16][CH2:17]3)[c:18]([O:19][CH3:20])[cH:21]1
COc1ccc(C(=O)Cl)c(OC)c1.NC1CN2CCC1CC2
COc1ccc(C(=O)NC2CN3CCC2CC3)c(OC)c1
null
null
C(Cl)(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NC1CN2CCC1CC2)c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[#7:6]-[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10]>>[#7:6]-[C:7]-[C:8](-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5])-[C:10]
23.7
[{"value": 23.7, "product": "Cl.N12CC(C(CC1)CC2)NC(C2=C(C=C(C=C2)OC)OC)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-aminoquinuclidine dihydrochloride, 6.95 g, (0.349), 2,4-dimethoxybenzoyl chloride, 700 g, (0.0349 mole), anhydrous sodium carbonate, 36.99 g, (0.349 mole), 175 ml water, and 175 ml chloroform was stirred rapidly to achieve good mixing of the 2 layers for 20 hrs. The chloroform layer was then separated, w...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.C1CN2CCC1CC2
HCl
C(Cl)(Cl)Cl
null
null
COc1ccc(C(=O)Cl)c(OC)c1.NC1CN2CCC1CC2>C(Cl)(Cl)Cl>COc1ccc(C(=O)NC2CN3CCC2CC3)c(OC)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-03d1b8f05e4141739d0b6c4cac54a2f6
CCCOc1ccccc1C(=O)Cl.NC1CN2CCC1CC2>>CCCOc1ccccc1C(=O)NC1CN2CCC1CC2
C(CC)OC1=C(C(=O)Cl)C=CC=C1.Cl.Cl.NC1CN2CCC1CC2.O.O.O.O.O.O.O.O.[OH-].[Ba+2].[OH-]>>Cl.N12CC(C(CC1)CC2)NC(C2=C(C=CC=C2)OCCC)=O
Cl[C:11]([c:10]1[c:5]([O:4][CH2:3][CH2:2][CH3:1])[cH:6][cH:7][cH:8][cH:9]1)=[O:12].[NH2:13][CH:14]1[CH2:15][N:16]2[CH2:17][CH2:18][CH:19]1[CH2:20][CH2:21]2>>[CH3:1][CH2:2][CH2:3][O:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[C:11](=[O:12])[NH:13][CH:14]1[CH2:15][N:16]2[CH2:17][CH2:18][CH:19]1[CH2:20][CH2:21]2
CCCOc1ccccc1C(=O)Cl.NC1CN2CCC1CC2
CCCOc1ccccc1C(=O)NC1CN2CCC1CC2
null
null
C(=O)=O.C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NC1CN2CCC1CC2)c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[#7:6]-[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10]>>[#7:6]-[C:7]-[C:8](-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5])-[C:10]
null
[]
null
null
null
null
To a solution of 3.82 g (0.0192 mole) of 3-amino quinuclidine dihydrochloride in about 25 ml of carbon dioxide-free water was added 8 g (0.025 mole) of barium hydroxide octahydrate. The mixture was warmed for 5 minutes and then dried to a powder on a rotary evaporator. While protecting from contamination with carbon di...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.C1CN2CCC1CC2
HCl
C(=O)=O.C(Cl)Cl
null
null
CCCOc1ccccc1C(=O)Cl.NC1CN2CCC1CC2>C(=O)=O.C(Cl)Cl>CCCOc1ccccc1C(=O)NC1CN2CCC1CC2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bc32b8c0b4ec4edd970f899e38ffb207
CNc1cc(OC)c(C(=O)NC2CN3CCC2CC3)cc1Cl.O=C([O-])/C=C/C(=O)[O-]>>CNc1cc(OC)c(C(=O)[NH+]([O-])C2CN3CCC2CC3)cc1Cl.Cl
N12CC(C(CC1)CC2)NC(C2=C(C=C(C(=C2)Cl)NC)OC)=O.C(\C=C\C(=O)[O-])(=O)[O-]>>Cl.N12CC(C(CC1)CC2)[NH+](C(C2=C(C=C(C(=C2)Cl)NC)OC)=O)[O-]
[CH3:1][NH:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[c:8]([C:9](=[O:10])[NH:11][CH:13]2[CH2:14][N:15]3[CH2:16][CH2:17][CH:18]2[CH2:19][CH2:20]3)[cH:21][c:22]1[Cl:23].O=C([O-])/C=C/C([O-])=[O:12]>>[CH3:1][NH:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[c:8]([C:9](=[O:10])[NH+:11]([O-:12])[CH:13]2[CH2:14][N:15]3[CH2:16][CH2:17][CH:18]2[CH2...
CNc1cc(OC)c(C(=O)NC2CN3CCC2CC3)cc1Cl.O=C([O-])/C=C/C(=O)[O-]
CNc1cc(OC)c(C(=O)[NH+]([O-])C2CN3CCC2CC3)cc1Cl.Cl
null
null
null
Miscellaneous
OtherReaction
258aaf9b783ac766ef04674a8049683ffe8fe0219b73c2d32e0bb4ecd173400f
a267a1d067671b1e552868d2a160d189ea3d111697964c07c12357f5fdb70c13
O=C([NH2+]C1CN2CCC1CC2)c1ccccc1
O=C(-[O-])/C=C/C(-[O-])=[O;H0;D1;+0:1].[#7:2]-[C:3]-[C:4](-[NH;D2;+0:5]-[C:6](=[O;D1;H0:7])-[c:8])-[C:9]>>[#7:2]-[C:3]-[C:4](-[NH+;D3:5](-[O-;H0;D1:1])-[C:6](=[O;D1;H0:7])-[c:8])-[C:9]
null
[]
null
null
null
null
N-(1-Azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide, fumarate [1:1] is converted to the free base by partitioning with aqueous sodium hydroxide and methylene chloride. Using the procedure of Example 1, the free base is reacted with peracetic acid to obtain the N-oxide and finally with hydrogen chl...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.C1CN2CCC1CC2
HO-
null
null
null
CNc1cc(OC)c(C(=O)NC2CN3CCC2CC3)cc1Cl.O=C([O-])/C=C/C(=O)[O-]>>CNc1cc(OC)c(C(=O)[NH+]([O-])C2CN3CCC2CC3)cc1Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d08bf726ee614cf79e621b0c1f4b7772
CC/C=C\C=C/CCCCCCCCCC=O>>C=CCCCCCCCCC/C=C\C=C/CC
C([O-])([O-])=O.C([O-])([O-])=O.[K+].[K+].O1CCOCC1.C(CCCCCCCCC\C=C/C=C\CC)=O>>C=CCCCCCCCCC\C=C/C=C\CC
O=[CH:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11]/[CH:12]=[CH:13]\[CH:14]=[CH:15]/[CH2:16][CH3:17]>>[CH2:1]=[CH:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11]/[CH:12]=[CH:13]\[CH:14]=[CH:15]/[CH2:16][CH3:17]
CC/C=C\C=C/CCCCCCCCCC=O
C=CCCCCCCCCC/C=C\C=C/CC
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
O
Functional Group Interconversion
OtherReaction
7702fabf33730b36d4194facf6bd167de8537ce3feabb6e16a2ab5a7eed012b1
327d0a428f3694bfca03537421df2e7fd8c75afd031319c50b8fe23cc3ad9de2
null
O=[CH;D2;+0:1]-[C:2]-[C:3]>>[C:3]-[C:2]-[CH;D2;+0:1]=[C;D1;H2:4]
null
[]
null
null
null
null
(Z,Z)-1,12,14-heptadecatriene (TRIENE) was synthesized conveniently from Wittig Salt and aldehyde in aqueous dioxidepotassium carbonate heterogeneous medium (Lechat 1982). A mixture of 3.57 g (0.01 mol) of methyl triphenylphosphonium bromide (Alfa Inorganics), 1.7 g (0.14 mol) of potassium carbonate, 10 ml of 1,4-dioxa...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Allyl
null
null
null
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.O
null
null
CC/C=C\C=C/CCCCCCCCCC=O>[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.O>C=CCCCCCCCCC/C=C\C=C/CC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-844bfa4964764092a84084123ac463f1
COCC(=O)c1ccccc1.[N-]=[N+]=Nc1ccc(C=O)cc1>>COc1ccccc1C(=O)C=Cc1ccc(N=[N+]=[N-])cc1
[OH-].[Na+].COCC(=O)C1=CC=CC=C1.N(=[N+]=[N-])C1=CC=C(C=O)C=C1.CO>>N(=[N+]=[N-])C1=CC=C(C=C1)C=CC(=O)C1=C(C=CC=C1)OC
[CH3:1][O:2][CH2:11][C:9]([c:8]1[cH:3][cH:4][cH:5][cH:6][cH:7]1)=[O:10].O=[CH:12][c:13]1[cH:14][cH:15][c:16]([N:17]=[N+:18]=[N-:19])[cH:20][cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[C:9](=[O:10])[CH:11]=[CH:12][c:13]1[cH:14][cH:15][c:16]([N:17]=[N+:18]=[N-:19])[cH:20][cH:21]1
COCC(=O)c1ccccc1.[N-]=[N+]=Nc1ccc(C=O)cc1
COc1ccccc1C(=O)C=Cc1ccc(N=[N+]=[N-])cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
cd8e70743afbaf8cc3e1648c822b76750ea4c274097b1fe30a5c4f36c14db898
1902fedd2f6f28e542a9d6629d43010d6b353c17fbfbb909c81a69c2aae0d321
O=C(C=Cc1ccccc1)c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[O;H0;D2;+0:6]-[CH2;D2;+0:7]-[C:8](=[O;D1;H0:9])-[c:10](:[c:11]):[cH;D2;+0:12]:[c:13]:[c:14]>>[C;D1;H3:5]-[O;H0;D2;+0:6]-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:10](-[C:8](=[O;D1;H0:9])-[CH;D2;+0:7]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:11]
null
[]
25
CELSIUS
24
HOUR
In a 500-ml flask were placed 15 g of 2-methoxyacetophenone (made by Aldrich Co., 99% purity), 15 g of p-azidobenzaldehyde (manufactured by Kanto Chemical Co., Ltd.), 50 g of 10% aqueous solution of NaOH, and 50 g of methanol. The mixture was stirred in a yellow light at 25° C. for 24 hours. After completion of the rea...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone.Ether
Ketone.Ether
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
null
25
24
COCC(=O)c1ccccc1.[N-]=[N+]=Nc1ccc(C=O)cc1>>COc1ccccc1C(=O)C=Cc1ccc(N=[N+]=[N-])cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-735299a0ef624d81b9ed5d77439bde1a
COc1ccc2occc(=O)c2c1>>COc1ccc2c(c1)C(O)CCO2
COC=1C=CC2=C(C(C=CO2)=O)C1.C(C)N(CC)CC>>COC=1C=CC2=C(C(CCO2)O)C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[c:9](=[O:10])[cH:11][cH:12][o:13]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH:9]([OH:10])[CH2:11][CH2:12][O:13]2
COc1ccc2occc(=O)c2c1
COc1ccc2c(c1)C(O)CCO2
null
[Pd]
C(C)O
Reduction
OtherReaction
e1dfc477dd91c2adbdb4bc7db294c9d008cf28766629c0b98080643a9de74bfe
0034de6654eff673c4919a40321b83463404d852b0929d3401429300290e8760
c1ccc2c(c1)CCCO2
[O;H0;D1;+0:1]=[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[o;H0;D2;+0:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[OH;D1;+0:1]-[CH;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]-1:[c:9]
null
[]
null
null
null
null
A solution of 6-methoxy-4-benzopyranone (31.6 g), triethylamine (4.9 ml) and 10% palladium on carbon (3.16 g) in absolute ethanol (1.7 l) is stirred under an atmosphere of hydrogen for 19 hours. The reaction mixture is filtered and evaporated in vacuo yielding the desired hydrogenated product as a pale yellow liquid. C...
10.6084/m9.figshare.5104873.v1
null
null
Ether.Secondary alcohol
c1ccc2occcc2c1
c1ccc2c(c1)CCCO2
c1ccc2c(c1)CCCO2
null
[Pd].C(C)O
null
null
COc1ccc2occc(=O)c2c1>[Pd].C(C)O>COc1ccc2c(c1)C(O)CCO2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-649ea945dd7e4b54ae14924d504966d6
C1CCNCC1.COc1ccc2c(c1)C(O)CCO2>>COc1ccc2c(c1)C(N1CCCCC1)CCO2
N1CCCCC1.CS(=O)(=O)Cl.COC=1C=CC2=C(C(CCO2)O)C1.C([O-])(O)=O.[Na+]>>COC=1C=CC2=C(C(CCO2)N2CCCCC2)C1
[NH:10]1[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]1.O[CH:9]1[c:7]2[c:6]([cH:5][cH:4][c:3]([O:2][CH3:1])[cH:8]2)[O:18][CH2:17][CH2:16]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH:9]([N:10]1[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]1)[CH2:16][CH2:17][O:18]2
C1CCNCC1.COc1ccc2c(c1)C(O)CCO2
COc1ccc2c(c1)C(N1CCCCC1)CCO2
null
null
C(Cl)Cl.C(C)N(CC)CC
Heteroatom Alkylation and Arylation
OtherReaction
f191075d01d8ca635ca442f38e41e9ed3fd1376be4d1b8e4347a724a27f399d5
540f526ef204b9f0fcb7b9bc2402af132d75c889d3e4a156b292e80c37384c80
c1ccc2c(c1)OCCC2N1CCCCC1
O-[CH;D3;+0:1]1-[C:2]-[C:3]-[#8:4]-[c:5]:[c:6]-1:[c:7].[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]>>[C:8]-[C:9]-[N;H0;D3;+0:10](-[CH;D3;+0:1]1-[C:2]-[C:3]-[#8:4]-[c:5]:[c:6]-1:[c:7])-[C:11]-[C:12]
null
[]
null
null
2
HOUR
Methane sulfonyl chloride (14.9 ml) is added dropwise to a stirred solution of the product obtained in Step 1. (31.6 g) and triethylamine (29.3 ml) in methylene chloride (750 ml) cooled to 0° C. under nitrogen. The reaction mixture is stirred at RT for 21/2 hours and cooled to 0° C. Piperidine (175 ml) is added to the ...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Secondary amine
Tertiary amine
C1CCNCC1.c1ccc2c(c1)CCCO2
C1CC[NH]CC1.c1ccc2c(c1)CCCO2
C1CC[NH]CC1.c1ccc2c(c1)CCCO2
HO-
C(Cl)Cl.C(C)N(CC)CC
null
2
C1CCNCC1.COc1ccc2c(c1)C(O)CCO2>C(Cl)Cl.C(C)N(CC)CC>COc1ccc2c(c1)C(N1CCCCC1)CCO2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-000cebf4787344f1bf7d418a9168b1b4
BrCCCBr.Oc1ccc2c(c1)C(N1CCCCC1)CCO2>>BrCCCOc1ccc2c(c1)C(N1CCCCC1)CCO2
[OH-].[K+].OC=1C=CC2=C(C(CCO2)N2CCCCC2)C1.BrCCCBr>>BrCCCOC=1C=CC2=C(C(CCO2)N2CCCCC2)C1
Br[CH2:4][CH2:3][CH2:2][Br:1].[OH:5][c:6]1[cH:7][cH:8][c:9]2[c:10]([cH:11]1)[CH:12]([N:13]1[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18]1)[CH2:19][CH2:20][O:21]2>>[Br:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]2[c:10]([cH:11]1)[CH:12]([N:13]1[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18]1)[CH2:19][CH2:20][O:21]2
BrCCCBr.Oc1ccc2c(c1)C(N1CCCCC1)CCO2
BrCCCOc1ccc2c(c1)C(N1CCCCC1)CCO2
null
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC
CCOCC.C(C)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2c(c1)OCCC2N1CCCCC1
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
48
HOUR
Crushed potassium hydroxide (1.15 g) and tetrabutyl ammonium chloride (0.61 g) are added to a solution of the product obtained in Step 3. (4.8 g) in 1,3-dibromopropane (21 ml). The reaction mixture is stirred under nitrogen at RT for 48 hours, diluted with diethyl ether, washed with water and extracted into 5% aq. HCl....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
C1CC[NH]CC1.c1ccc2c(c1)CCCO2
HBr
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.CCOCC.C(C)OCC
null
48
BrCCCBr.Oc1ccc2c(c1)C(N1CCCCC1)CCO2>[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.CCOCC.C(C)OCC>BrCCCOc1ccc2c(c1)C(N1CCCCC1)CCO2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2956eb50cd4a4f1bb50c59a5120211de
COc1cccc2c(=O)ccoc12>>COc1cccc2c1OCCC2O
COC1=CC=CC=2C(C=COC21)=O.C(C)N(CC)CC>>OC1CCOC2=C1C=CC=C2OC
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[o:9][cH:10][cH:11][c:12]2=[O:13]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[O:9][CH2:10][CH2:11][CH:12]2[OH:13]
COc1cccc2c(=O)ccoc12
COc1cccc2c1OCCC2O
null
[Pd]
C(C)O
Reduction
OtherReaction
75e7adcdbf2c81d6a6b8c6e0ffad15bb1e3e6ab17dc1e935c9e35b034caefa6e
0034de6654eff673c4919a40321b83463404d852b0929d3401429300290e8760
c1ccc2c(c1)CCCO2
[O;H0;D1;+0:1]=[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[o;H0;D2;+0:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[OH;D1;+0:1]-[CH;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]-1:[c:9]
null
[]
null
null
null
null
A solution of 8-methoxy-4-benzopyranone (31.6 g), triethylamine (4.9 ml) and 10% palladium on carbon (3.1 g) in absolute ethanol (1.7 l) is stirred under an atmosphere of hydrogen (P=52 lbs.) overnight. The resulting solid is filtered, washed with diethyl ether and evaporated in vacuo yielding the desired product as a ...
10.6084/m9.figshare.5104873.v1
null
null
Ether.Secondary alcohol
c1ccoc2ccccc12
c1ccc2c(c1)CCCO2
c1ccc2c(c1)CCCO2
null
[Pd].C(C)O
null
null
COc1cccc2c(=O)ccoc12>[Pd].C(C)O>COc1cccc2c1OCCC2O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-badde64ec33c4001be5240ae6f4f35f0
C1CCNCC1.COc1cccc2c1OCCC2O>>COc1cccc2c1OCCC2N1CCCCC1
CS(=O)(=O)Cl.OC1CCOC2=C1C=CC=C2OC.C(C)N(CC)CC.N1CCCCC1>>COC1=CC=CC=2C(CCOC21)N2CCCCC2
[NH:13]1[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18]1.O[CH:12]1[c:7]2[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:8]2[O:9][CH2:10][CH2:11]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[O:9][CH2:10][CH2:11][CH:12]2[N:13]1[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18]1
C1CCNCC1.COc1cccc2c1OCCC2O
COc1cccc2c1OCCC2N1CCCCC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
f191075d01d8ca635ca442f38e41e9ed3fd1376be4d1b8e4347a724a27f399d5
540f526ef204b9f0fcb7b9bc2402af132d75c889d3e4a156b292e80c37384c80
c1ccc2c(c1)OCCC2N1CCCCC1
O-[CH;D3;+0:1]1-[C:2]-[C:3]-[#8:4]-[c:5]:[c:6]-1:[c:7].[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]>>[C:8]-[C:9]-[N;H0;D3;+0:10](-[CH;D3;+0:1]1-[C:2]-[C:3]-[#8:4]-[c:5]:[c:6]-1:[c:7])-[C:11]-[C:12]
null
[]
null
null
2
HOUR
Methane sulfonyl chloride (14.9 ml) is added dropwise to a solution of the product obtained in Step 1. (31.6 g) and triethylamine (29.3 ml) in methylene chloride (750 ml) cooled to 0° C. under nitrogen. The reaction mixture is stirred for 11/2 hours; piperidine (175 ml) is added and the reaction mixture is stirred unde...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Secondary amine
Tertiary amine
C1CCNCC1.c1ccc2c(c1)CCCO2
c1ccc2c(c1)CCCO2.C1CC[NH]CC1
c1ccc2c(c1)CCCO2.C1CC[NH]CC1
HO-
C(Cl)Cl
null
2
C1CCNCC1.COc1cccc2c1OCCC2O>C(Cl)Cl>COc1cccc2c1OCCC2N1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-11041e93a6764496b437ae0e8552152e
BrCCCBr.Oc1cccc2c1OCCC2N1CCCCC1>>BrCCCOc1cccc2c1OCCC2N1CCCCC1
BrCCCBr.OC1=CC=CC=2C(CCOC21)N2CCCCC2.[OH-].[K+].O>>BrCCCOC1=CC=CC=2C(CCOC21)N2CCCCC2
Br[CH2:4][CH2:3][CH2:2][Br:1].[OH:5][c:6]1[cH:7][cH:8][cH:9][c:10]2[c:11]1[O:12][CH2:13][CH2:14][CH:15]2[N:16]1[CH2:17][CH2:18][CH2:19][CH2:20][CH2:21]1>>[Br:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][cH:9][c:10]2[c:11]1[O:12][CH2:13][CH2:14][CH:15]2[N:16]1[CH2:17][CH2:18][CH2:19][CH2:20][CH2:21]1
BrCCCBr.Oc1cccc2c1OCCC2N1CCCCC1
BrCCCOc1cccc2c1OCCC2N1CCCCC1
null
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC
C(C)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2c(c1)OCCC2N1CCCCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]-[c:5]:[c:6](-[OH;D1;+0:7]):[c:8]>>[#8:4]-[c:5]:[c:6](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[C:2]-[C:3]):[c:8]
null
[]
null
null
8
HOUR
Crushed potassium hydroxide (4.1 g) and tetrabutyl ammonium chloride (2.2 g) and H2O (5 ml) are added to a stirred mixture of the product obtained in Step 3. (17.2 g) and 1,3-dibromopropane (74.8 ml). The reaction mixture is stirred under nitrogen overnight, diluted with diethyl ether, and extracted with 5% aq. HCl. Th...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CCCO2.C1CC[NH]CC1
HBr
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C)OCC
null
8
BrCCCBr.Oc1cccc2c1OCCC2N1CCCCC1>[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C)OCC>BrCCCOc1cccc2c1OCCC2N1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5b26df7fe2534bf0910c119f65b7be7d
COc1cccc2c1OC(C)(C)C2=O>>COc1cccc2c1OC(C)(C)C2O
[BH4-].[Na+].COC1=CC=CC=2C(C(OC21)(C)C)=O>>COC1=CC=CC=2C(C(OC21)(C)C)O
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[O:9][C:10]([CH3:11])([CH3:12])[C:13]2=[O:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[O:9][C:10]([CH3:11])([CH3:12])[CH:13]2[OH:14]
COc1cccc2c1OC(C)(C)C2=O
COc1cccc2c1OC(C)(C)C2O
null
null
C(C)O.C(Cl)Cl
Reduction
Reduction of ketone to secondary alcohol
755c7bdda3ccaa9e2a097b82c386f43f2881f1d49e6c3707dce72c3ac00b51db
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccc2c(c1)CCO2
[C;D1;H3:1]-[C:2]1(-[C;D1;H3:3])-[#8:4]-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C;D1;H3:1]-[C:2]1(-[C;D1;H3:3])-[#8:4]-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
null
[]
null
null
null
null
An aqueous solution of sodium borohydride (8.2 g, 50 ml) is added to a stirred solution of the product obtained in Step 3. (41.8 g) in ethanol (1 l) and the mixture refluxed for 3 hours and evaporated in vacuo. The residue is taken up in water and toluene, the layers are separated and the organic phase washed, dried an...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2
null
C(C)O.C(Cl)Cl
null
null
COc1cccc2c1OC(C)(C)C2=O>C(C)O.C(Cl)Cl>COc1cccc2c1OC(C)(C)C2O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-29d226711096432384d0866c11b1dd4d
C1CCNCC1.COc1cccc2c1OC(C)(C)C2O>>COc1cccc2c1OC(C)(C)C2N1CCCCC1
N1CCCCC1.COC1=CC=CC=2C(C(OC21)(C)C)O.C([O-])(O)=O.[Na+].CS(=O)(=O)Cl>>COC1=CC=CC=2C(C(OC21)(C)C)N2CCCCC2
[NH:14]1[CH2:15][CH2:16][CH2:17][CH2:18][CH2:19]1.O[CH:13]1[c:7]2[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:8]2[O:9][C:10]1([CH3:11])[CH3:12]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[O:9][C:10]([CH3:11])([CH3:12])[CH:13]2[N:14]1[CH2:15][CH2:16][CH2:17][CH2:18][CH2:19]1
C1CCNCC1.COc1cccc2c1OC(C)(C)C2O
COc1cccc2c1OC(C)(C)C2N1CCCCC1
null
null
C(Cl)Cl.C(C)N(CC)CC
Heteroatom Alkylation and Arylation
OtherReaction
ff764035e14a0e265d5118c5ee8287c96fc78766bbde588c108e1e9046e67926
540f526ef204b9f0fcb7b9bc2402af132d75c889d3e4a156b292e80c37384c80
c1ccc2c(c1)OCC2N1CCCCC1
O-[CH;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[#8:5]-[C:6]-1(-[C;D1;H3:7])-[C;D1;H3:8].[C:9]-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13]>>[C:9]-[C:10]-[N;H0;D3;+0:11](-[CH;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[#8:5]-[C:6]-1(-[C;D1;H3:7])-[C;D1;H3:8])-[C:12]-[C:13]
null
[]
0
CELSIUS
3
HOUR
Triethylamine (29 ml) is added to a stirred solution of the product obtained in Step 4. (25.4 g) in methylene chloride (560 ml) at RT under nitrogen. Methanesulfonyl chloride (11.1 ml) is added dropwise to the mixture which is cooled to 0° C. The mixture is stirred for 3 hours at RT, cooled to 0° C., piperidine (128 ml...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Secondary amine
Tertiary amine
C1CCNCC1.c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2.C1CC[NH]CC1
c1ccc2c(c1)CCO2.C1CC[NH]CC1
HO-
C(Cl)Cl.C(C)N(CC)CC
0
3
C1CCNCC1.COc1cccc2c1OC(C)(C)C2O>C(Cl)Cl.C(C)N(CC)CC>COc1cccc2c1OC(C)(C)C2N1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-62c89f061fa24da181f2e8c2e39d52b5
COc1cccc2c1OC(C)(C)C2N1CCCCC1>>CC1(C)Oc2c(O)cccc2C1N1CCCCC1
COC1=CC=CC=2C(C(OC21)(C)C)N2CCCCC2.Br>>OC1=CC=CC=2C(C(OC21)(C)C)N2CCCCC2
C[O:7][c:6]1[c:5]2[c:11]([cH:10][cH:9][cH:8]1)[CH:12]([N:13]1[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18]1)[C:2]([CH3:1])([CH3:3])[O:4]2>>[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([OH:7])[cH:8][cH:9][cH:10][c:11]2[CH:12]1[N:13]1[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18]1
COc1cccc2c1OC(C)(C)C2N1CCCCC1
CC1(C)Oc2c(O)cccc2C1N1CCCCC1
null
null
C(C)(=O)O
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc2c(c1)OCC2N1CCCCC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]-[#8:5]>>[#8:5]-[c:4]:[c:2](-[OH;D1;+0:1]):[c:3]
null
[]
null
null
null
null
7-Methoxy-3-piperidino-2,2-dimethylbenzofuran (65.1 g) is added to a stirred mixture of glacial acetic acid (340 ml) and 48% HBr (340 ml) and the solution refluxed for 3 hours. The reaction mixture is poured into crushed ice/H2O and brought to a pH=8-10. The alkaline reaction mixture is extracted with methylene chlorid...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccc2c(c1)CCO2.C1CC[NH]CC1
Other
C(C)(=O)O
null
null
COc1cccc2c1OC(C)(C)C2N1CCCCC1>C(C)(=O)O>CC1(C)Oc2c(O)cccc2C1N1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f0acfd39ea7a462683b5b3c43269d05e
BrCCCBr.CC1(C)Oc2c(O)cccc2C1N1CCCCC1>>CC1(C)Oc2c(OCCCBr)cccc2C1N1CCCCC1
BrCCCBr.[OH-].[K+].O.OC1=CC=CC=2C(C(OC21)(C)C)N2CCCCC2>>BrCCCOC1=CC=CC=2C(C(OC21)(C)C)N2CCCCC2
Br[CH2:8][CH2:9][CH2:10][Br:11].[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([OH:7])[cH:12][cH:13][cH:14][c:15]2[CH:16]1[N:17]1[CH2:18][CH2:19][CH2:20][CH2:21][CH2:22]1>>[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([O:7][CH2:8][CH2:9][CH2:10][Br:11])[cH:12][cH:13][cH:14][c:15]2[CH:16]1[N:17]1[CH2:18][CH2:19][CH2:20][CH2:21][CH2:22...
BrCCCBr.CC1(C)Oc2c(O)cccc2C1N1CCCCC1
CC1(C)Oc2c(OCCCBr)cccc2C1N1CCCCC1
null
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC
CCOCC.C(C)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2c(c1)OCC2N1CCCCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]-[c:5]:[c:6](-[OH;D1;+0:7]):[c:8]>>[#8:4]-[c:5]:[c:6](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[C:2]-[C:3]):[c:8]
null
[]
null
null
20
HOUR
Potassium hydroxide (1.47 g), tetrabutyl ammonium chloride (0.77 g) and H2O (1 ml) are added to a solution of the product obtained in Step 6. (6.6 g) in 1,3-dibromopropane (27 ml). The reaction mixture is stirred for 20 hours and diluted with diethyl ether and washed with 5% aq. HCl. The acidic solution is washed with ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CCO2.C1CC[NH]CC1
HBr
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.CCOCC.C(C)OCC
null
20
BrCCCBr.CC1(C)Oc2c(O)cccc2C1N1CCCCC1>[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.CCOCC.C(C)OCC>CC1(C)Oc2c(OCCCBr)cccc2C1N1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e1cc7aae472c4f0e89601c6881976e37
BrCCCCBr.CC1(C)Oc2c(O)cccc2C1N1CCCCC1>>CC1(C)Oc2c(OCCCCBr)cccc2C1N1CCCCC1
[OH-].[K+].OC1=CC=CC=2C(C(OC21)(C)C)N2CCCCC2.BrCCCCBr>>BrCCCCOC1=CC=CC=2C(C(OC21)(C)C)N2CCCCC2
Br[CH2:8][CH2:9][CH2:10][CH2:11][Br:12].[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([OH:7])[cH:13][cH:14][cH:15][c:16]2[CH:17]1[N:18]1[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]1>>[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([O:7][CH2:8][CH2:9][CH2:10][CH2:11][Br:12])[cH:13][cH:14][cH:15][c:16]2[CH:17]1[N:18]1[CH2:19][CH2:20][CH2:21...
BrCCCCBr.CC1(C)Oc2c(O)cccc2C1N1CCCCC1
CC1(C)Oc2c(OCCCCBr)cccc2C1N1CCCCC1
null
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC
CCOCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2c(c1)OCC2N1CCCCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]-[c:5]:[c:6](-[OH;D1;+0:7]):[c:8]>>[#8:4]-[c:5]:[c:6](-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[C:2]-[C:3]):[c:8]
null
[]
null
null
5
HOUR
Crushed potassium hydroxide (19.6 g) and tetrabutyl ammonium chloride (1.7 g) are added to a solution of 7-hydroxy-3-piperidino-2,2-dimethylbenzofuran (14.4 g) in 1,4-dibromobutane (69.4 ml) and the mixture stirred at RT under nitrogen for 5 hours. The reaction mixture is diluted with ether, washed with water, extracte...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CCO2.C1CC[NH]CC1
HBr
[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.CCOCC
null
5
BrCCCCBr.CC1(C)Oc2c(O)cccc2C1N1CCCCC1>[Cl-].C(CCC)[N+](CCCC)(CCCC)CCCC.CCOCC>CC1(C)Oc2c(OCCCCBr)cccc2C1N1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3d9fe4eea0d14c78998610d953418f18
COc1ccc(COC(=O)N[C@H](CO)C(=O)OCc2ccccc2)cc1>>COC[C@@H](NC(=O)OCc1ccc(OC)cc1)C(=O)OCc1ccccc1
[N+](=[N-])=C.C(=O)=O.CC(=O)C.C(C1=CC=CC=C1)OC([C@H](NC(=O)OCC1=CC=C(C=C1)OC)CO)=O.B(F)(F)F.CCOCC>>C(C1=CC=CC=C1)OC([C@H](NC(=O)OCC1=CC=C(C=C1)OC)COC)=O
[OH:2][CH2:3][C@@H:4]([NH:5][C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][c:13]([O:14][CH3:15])[cH:16][cH:17]1)[C:18](=[O:19])[O:20][CH2:21][c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1>>[CH3:1][O:2][CH2:3][C@@H:4]([NH:5][C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][c:13]([O:14][CH3:15])[cH:16][cH:17]1)[C:18](=[O:19])[...
COc1ccc(COC(=O)N[C@H](CO)C(=O)OCc2ccccc2)cc1
COC[C@@H](NC(=O)OCc1ccc(OC)cc1)C(=O)OCc1ccccc1
null
null
ClCCl
Miscellaneous
OtherReaction
70208f2708ef916b87826db62bd559464d026f06571e7efe1ab0d84891b316f6
e85669534439e6064e577a50279050476a21ceb3b9ce2038de4518b5b972fb94
O=C(CNC(=O)OCc1ccccc1)OCc1ccccc1
[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5]-[OH;D1;+0:6]>>[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5]-[O;H0;D2;+0:6]-[C;D1;H3:7]
70
[{"value": 70.0, "product": "C(C1=CC=CC=C1)OC([C@H](NC(=O)OCC1=CC=C(C=C1)OC)COC)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The N-p-methoxybenzyloxycarbonyl-D-serine benzyl ester (720 mg, 2.00 mmol) is dissolved in dry dichloromethane (20 ml) and the solution cooled to dry ice/acetone. Boron trifluoride etherate (100 μl) is added followed by the portionwise addition of diazomethane (30 mmol in 20 ml CH2Cl2). After about 30 minutes the solut...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Ether
null
null
c1ccccc1.c1ccccc1
Other
ClCCl
null
null
COc1ccc(COC(=O)N[C@H](CO)C(=O)OCc2ccccc2)cc1>ClCCl>COC[C@@H](NC(=O)OCc1ccc(OC)cc1)C(=O)OCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c71b9f3cdcad49d1b3a53a42a03aed7c
Nc1cccc2c1OC(F)(F)O2.O=[N+]([O-])c1cc([N+](=O)[O-])c(Cl)c(C(F)(F)F)c1>>O=[N+]([O-])c1cc([N+](=O)[O-])c(Nc2cccc3c2OC(F)(F)O3)c(C(F)(F)F)c1
Cl.O[Li].O.FC1(OC2=C(O1)C=CC=C2N)F.[N+](=O)([O-])C1=C(C(=CC(=C1)[N+](=O)[O-])C(F)(F)F)Cl>>FC1(OC2=C(O1)C=CC=C2NC2=C(C=C(C=C2C(F)(F)F)[N+](=O)[O-])[N+](=O)[O-])F
[NH2:11][c:12]1[cH:13][cH:14][cH:15][c:16]2[c:17]1[O:18][C:19]([F:20])([F:21])[O:22]2.Cl[c:10]1[c:6]([N+:7](=[O:8])[O-:9])[cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:28][c:23]1[C:24]([F:25])([F:26])[F:27]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([N+:7](=[O:8])[O-:9])[c:10]([NH:11][c:12]2[cH:13][cH:14][cH:15][c:16]3[c:17]2[O:18]...
Nc1cccc2c1OC(F)(F)O2.O=[N+]([O-])c1cc([N+](=O)[O-])c(Cl)c(C(F)(F)F)c1
O=[N+]([O-])c1cc([N+](=O)[O-])c(Nc2cccc3c2OC(F)(F)O3)c(C(F)(F)F)c1
null
null
CS(=O)C.O
Heteroatom Alkylation and Arylation
Goldberg coupling aryl amine-aryl chloride
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(Nc2cccc3c2OCO3)cc1
Cl-[c;H0;D3;+0:1](:[c:2](-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[F;D1;H0:6]):[c:7]):[c:8](-[#7;+:9]):[c:10].[#8:11]-[c:12]:[c:13](-[NH2;D1;+0:14]):[c:15]>>[#7;+:9]-[c:8](:[c:10]):[c;H0;D3;+0:1](-[NH;D2;+0:14]-[c:13](:[c:15]):[c:12]-[#8:11]):[c:2](-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[F;D1;H0:6]):[c:7]
null
[]
null
null
20
MINUTE
20.8 g of LiOH.H2O are added at 0° C. to a solution of 24.5 g of 2,2-difluoro-4-amino-1,3-benzodioxole in 70 ml of dimethyl sulfoxide. The mixture is then stirred for 20 minutes. Subsequently, a solution of 38.3 g of 2,4-dinitro-6-trifluoromethylchlorobenzene in 70 ml of dimethyl sulfoxide is added, and the resultant r...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2c(c1)OCO2
HCl
CS(=O)C.O
null
0.333333
Nc1cccc2c1OC(F)(F)O2.O=[N+]([O-])c1cc([N+](=O)[O-])c(Cl)c(C(F)(F)F)c1>CS(=O)C.O>O=[N+]([O-])c1cc([N+](=O)[O-])c(Nc2cccc3c2OC(F)(F)O3)c(C(F)(F)F)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-38fb1d06294f4f07968ae0a46176877a
CCOC(=S)NNC(=O)C(C)Oc1ccc(Oc2ccc(Cl)cc2)cc1>>CCOc1nnc(C(C)Oc2ccc(Oc3ccc(Cl)cc3)cc2)s1
C(C)OC(NNC(C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)Cl)=O)=S>>C(C)OC=1SC(=NN1)C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)Cl
O=[C:7]([NH:6][NH:5][C:4]([O:3][CH2:2][CH3:1])=[S:25])[CH:8]([CH3:9])[O:10][c:11]1[cH:12][cH:13][c:14]([O:15][c:16]2[cH:17][cH:18][c:19]([Cl:20])[cH:21][cH:22]2)[cH:23][cH:24]1>>[CH3:1][CH2:2][O:3][c:4]1[n:5][n:6][c:7]([CH:8]([CH3:9])[O:10][c:11]2[cH:12][cH:13][c:14]([O:15][c:16]3[cH:17][cH:18][c:19]([Cl:20])[cH:21][cH...
CCOC(=S)NNC(=O)C(C)Oc1ccc(Oc2ccc(Cl)cc2)cc1
CCOc1nnc(C(C)Oc2ccc(Oc3ccc(Cl)cc3)cc2)s1
null
null
S(O)(O)(=O)=O
Aromatic Heterocycle Formation
OtherReaction
ff34a009045b5c9adf9fb943f11b38be8f1350c0755ea4ec5e2842f930b046f9
5caf0fd195797c78f794bcf8d12286f6659d5c73f87eedb48b36b62a76260df7
c1ccc(Oc2ccc(OCc3nncs3)cc2)cc1
O=[C;H0;D3;+0:1](-[NH;D2;+0:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[S;H0;D1;+0:5])-[#8:6]-[C:7])-[C:8](-[#8:9])-[C;D1;H3:10]>>[#8:9]-[C:8](-[C;D1;H3:10])-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[n;H0;D2;+0:3]:[c;H0;D3;+0:4](-[#8:6]-[C:7]):[s;H0;D2;+0:5]:1
52.4
[{"value": 52.4, "product": "C(C)OC=1SC(=NN1)C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 10 ml of concentrated sulfuric acid cooled to -5° C. was added, with stirring, 2.0 g of 3-[2-[4-(4-chlorophenoxy)phenoxy]-propionyl]-thiocarbazic acid-O-ethyl ester gradually. After stirring at the same temperature for 10 minutes, the reaction mixture was poured over 100 g of ice followed by extracting with ethyl ac...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Ether.Thioamide
Ether
null
c1nncs1
c1nncs1.c1ccccc1.c1ccccc1
HO-
S(O)(O)(=O)=O
null
null
CCOC(=S)NNC(=O)C(C)Oc1ccc(Oc2ccc(Cl)cc2)cc1>S(O)(O)(=O)=O>CCOc1nnc(C(C)Oc2ccc(Oc3ccc(Cl)cc3)cc2)s1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dedcc622a9794abe8181ef0f7412474d
CCOC(=S)NNC(=O)C(C)Oc1ccc(Oc2ccc(C(F)(F)F)cc2)cc1>>CCOc1nnc(C(C)Oc2ccc(Oc3ccc(C(F)(F)F)cc3)cc2)s1
C(C)OC(NNC(C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)C(F)(F)F)=O)=S>>C(C)OC=1SC(=NN1)C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)C(F)(F)F
O=[C:7]([NH:6][NH:5][C:4]([O:3][CH2:2][CH3:1])=[S:28])[CH:8]([CH3:9])[O:10][c:11]1[cH:12][cH:13][c:14]([O:15][c:16]2[cH:17][cH:18][c:19]([C:20]([F:21])([F:22])[F:23])[cH:24][cH:25]2)[cH:26][cH:27]1>>[CH3:1][CH2:2][O:3][c:4]1[n:5][n:6][c:7]([CH:8]([CH3:9])[O:10][c:11]2[cH:12][cH:13][c:14]([O:15][c:16]3[cH:17][cH:18][c:1...
CCOC(=S)NNC(=O)C(C)Oc1ccc(Oc2ccc(C(F)(F)F)cc2)cc1
CCOc1nnc(C(C)Oc2ccc(Oc3ccc(C(F)(F)F)cc3)cc2)s1
null
null
S(O)(O)(=O)=O
Aromatic Heterocycle Formation
OtherReaction
ff34a009045b5c9adf9fb943f11b38be8f1350c0755ea4ec5e2842f930b046f9
5caf0fd195797c78f794bcf8d12286f6659d5c73f87eedb48b36b62a76260df7
c1ccc(Oc2ccc(OCc3nncs3)cc2)cc1
O=[C;H0;D3;+0:1](-[NH;D2;+0:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[S;H0;D1;+0:5])-[#8:6]-[C:7])-[C:8](-[#8:9])-[C;D1;H3:10]>>[#8:9]-[C:8](-[C;D1;H3:10])-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[n;H0;D2;+0:3]:[c;H0;D3;+0:4](-[#8:6]-[C:7]):[s;H0;D2;+0:5]:1
57.4
[{"value": 57.4, "product": "C(C)OC=1SC(=NN1)C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)C(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 10 ml of concentrated sulfuric acid cooled to -5° C. was added, with stirring, 2.0 g of 3-[2-[4-(4-trifluoromethylphenoxy)phenoxy]-propionyl]-thiocarbazic acid-O-ethyl ester gradually. After stirring at the same temperature for 10 minutes, the reaction mixture was poured over 100 g of ice followed by extracting with...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Ether.Thioamide
Ether
null
c1nncs1
c1nncs1.c1ccccc1.c1ccccc1
HO-
S(O)(O)(=O)=O
null
null
CCOC(=S)NNC(=O)C(C)Oc1ccc(Oc2ccc(C(F)(F)F)cc2)cc1>S(O)(O)(=O)=O>CCOc1nnc(C(C)Oc2ccc(Oc3ccc(C(F)(F)F)cc3)cc2)s1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f72db97d8ce54dbba8cafdb5ed72d91d
CCOc1nnc(CBr)s1.Oc1ccc(Oc2ccccc2)cc1>>CCOC1=NN=C(Oc2ccc(Oc3ccccc3)cc2)[SH]1C
C(C)(=O)OCC.C([O-])([O-])=O.[K+].[K+].BrCC=1SC(=NN1)OCC.O(C1=CC=CC=C1)C1=CC=C(C=C1)O>>C(C)OC=1S(C(=NN1)OC1=CC=C(C=C1)OC1=CC=CC=C1)C
Br[CH2:23][c:7]1[n:6][n:5][c:4]([O:3][CH2:2][CH3:1])[s:22]1.[OH:8][c:9]1[cH:10][cH:11][c:12]([O:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[cH:20][cH:21]1>>[CH3:1][CH2:2][O:3][C:4]1=[N:5][N:6]=[C:7]([O:8][c:9]2[cH:10][cH:11][c:12]([O:13][c:14]3[cH:15][cH:16][cH:17][cH:18][cH:19]3)[cH:20][cH:21]2)[SH:22]1[CH3:23]
CCOc1nnc(CBr)s1.Oc1ccc(Oc2ccccc2)cc1
CCOC1=NN=C(Oc2ccc(Oc3ccccc3)cc2)[SH]1C
null
null
CC(=O)C
Acylation
OtherReaction
8f406dc626aae18297683d0b62d3d601ac9366fdba7a91cf80dd60f751fe5c84
54efcbe8e120567f454985a52b84b5c2743f8a3bfcd524048dd0be68629ab022
C1=NN=C(Oc2ccc(Oc3ccccc3)cc2)S1
Br-[CH2;D2;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:3]:[n;H0;D2;+0:4]:[c;H0;D3;+0:5](-[#8:6]-[C:7]):[s;H0;D2;+0:8]:1.[OH;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C:7]-[#8:6]-[C;H0;D3;+0:5]1=[N;H0;D2;+0:4]-[N;H0;D2;+0:3]=[C;H0;D3;+0:2](-[O;H0;D2;+0:9]-[c:10](:[c:11]):[c:12])-[SH;D3;+0:8]-1-[CH3;D1;+0:1]
74.2
[{"value": 74.2, "product": "C(C)OC=1S(C(=NN1)OC1=CC=C(C=C1)OC1=CC=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.76 g of 4-phenoxy phenol was dissolved in 10 ml of acetone followed by adding 0.6 g of anhydrous potassium carbonate and 1.0 g of 2-bromomethyl-5-ethoxy-1,3,4-thiadiazole. The resulting mixture was refluxed with stirring and heated for 2 hours. After cooling, 100 ml of ethyl acetate was added followed by washing with...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Aromatic alcohol
Ether.Ether
c1nncs1
C1=NN=C[SH]1
C1=NN=C[SH]1.c1ccccc1.c1ccccc1
Br-
CC(=O)C
null
null
CCOc1nnc(CBr)s1.Oc1ccc(Oc2ccccc2)cc1>CC(=O)C>CCOC1=NN=C(Oc2ccc(Oc3ccccc3)cc2)[SH]1C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-08f23e697a564844a42b9eee52f2f3d1
CCOc1nnc(C(C)Br)s1.Cc1ccc(Oc2ccc(O)cc2)cc1>>CCOc1nnc(C(C)Oc2ccc(Oc3ccc(C)cc3)cc2)s1
CC1=CC=C(OC2=CC=C(C=C2)O)C=C1.C([O-])([O-])=O.[K+].[K+].BrC(C)C=1SC(=NN1)OCC>>C(C)OC=1SC(=NN1)C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)C
Br[CH:8]([c:7]1[n:6][n:5][c:4]([O:3][CH2:2][CH3:1])[s:25]1)[CH3:9].[OH:10][c:11]1[cH:12][cH:13][c:14]([O:15][c:16]2[cH:17][cH:18][c:19]([CH3:20])[cH:21][cH:22]2)[cH:23][cH:24]1>>[CH3:1][CH2:2][O:3][c:4]1[n:5][n:6][c:7]([CH:8]([CH3:9])[O:10][c:11]2[cH:12][cH:13][c:14]([O:15][c:16]3[cH:17][cH:18][c:19]([CH3:20])[cH:21][c...
CCOc1nnc(C(C)Br)s1.Cc1ccc(Oc2ccc(O)cc2)cc1
CCOc1nnc(C(C)Oc2ccc(Oc3ccc(C)cc3)cc2)s1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
bff4876be49b448135c783dd3eeeb68ab3cc5bdc91beadda8a9095106cd5c747
cf768afb66ed5041aefdce1fa6d1e40995a1ab7c4b4a4ca47544fe49ee1e629f
c1ccc(Oc2ccc(OCc3nncs3)cc2)cc1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[c:3]1:[#16;a:4]:[c:5]:[#7;a:6]:[#7;a:7]:1.[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[C;D1;H3:2]-[CH;D3;+0:1](-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11])-[c:3]1:[#16;a:4]:[c:5]:[#7;a:6]:[#7;a:7]:1
73.6
[{"value": 73.6, "product": "C(C)OC=1SC(=NN1)C(C)OC1=CC=C(C=C1)OC1=CC=C(C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.84 g of 4-(4-methylphenoxy)phenol was dissolved in 5 ml of acetone followed by adding 0.87 g of anhydrous potassium carbonate and 1.0 g of 2-(1-bromoethyl)-5-ethoxy-1,3,4-thiadiazole. The resulting mixture was refluxed with stirring and heating for 2 hours. After cooling, insoluble salts were filtered off, and aceton...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol
Ether
null
null
c1nncs1.c1ccccc1.c1ccccc1
HBr
CC(=O)C
null
null
CCOc1nnc(C(C)Br)s1.Cc1ccc(Oc2ccc(O)cc2)cc1>CC(=O)C>CCOc1nnc(C(C)Oc2ccc(Oc3ccc(C)cc3)cc2)s1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-35eabf0f8e394ae3b362808c91e10ea1
CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)O.COC(=O)CCCCN>>COC(=O)CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C
CN1CCOCC1.C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)O.CN1CCOCC1.Cl.NCCCCC(=O)OC.C(C(C)C)OC(=O)Cl>>C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCC(=O)OC
O[C:10](=[O:11])[C@H:12]([CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[NH:20][C:21](=[O:22])[O:23][C:24]([CH3:25])([CH3:26])[CH3:27].[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][CH2:7][CH2:8][NH2:9]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][CH2:7][CH2:8][NH:9][C:10](=[O:11])[C@H:12]([CH2:13][c:14]1[cH:15][cH:16][cH:17...
CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)O.COC(=O)CCCCN
COC(=O)CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C
null
null
CN(C=O)C
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:13]-[C:14]-[NH2;D1;+0:15]>>[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;+0:15]-[C:14]-[C:13]
96.2
[{"value": 96.2, "product": "C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCC(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a cold (ca -30° ), stirred solution of 26.5 g (0.1 mole) of t-butoxycarbonylphenylalanine (BOC-Phe) and 11.2 g (0.1 mole) of N-methylmorpholine in 150 ml of dimethylformamide (DMF) was added dropwise 13.2 ml (0.1 mole) of isobutylchloroformate. After warming and then holding the temperature at ca. -15° for about ten...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
CN(C=O)C
null
8
CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)O.COC(=O)CCCCN>CN(C=O)C>COC(=O)CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dfc940d1027e4824b71c811ac0ae7fe4
COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C>>COC(=O)CCCCCNC(=O)[C@@H](N)Cc1ccccc1
C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCCC(=O)OC.Cl.O1CCOCC1>>Cl.COC(CCCCCNC([C@@H](N)CC1=CC=CC=C1)=O)=O
CC(C)(C)OC(=O)[NH:14][C@H:13]([C:11]([NH:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][C:3]([O:2][CH3:1])=[O:4])=[O:12])[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][NH:10][C:11](=[O:12])[C@@H:13]([NH2:14])[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C
COC(=O)CCCCCNC(=O)[C@@H](N)Cc1ccccc1
null
null
O1CCOCC1
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
c1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#7:6]-[C:7]>>[C:3]-[C:2](-[NH2;D1;+0:1])-[C:4](=[O;D1;H0:5])-[#7:6]-[C:7]
null
[]
null
null
null
null
To a solution of the title compound of Example 2 (43.1 g, 0.11 mole) in 100 ml of dioxane was added 100 ml of 6M hydrogen chloride/dioxane. After about 30 min. the solution was concentrated in vacuo to dryness and the residue triturated thoroughly with diethyl ether. The solid was collected and washed well with diethyl...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1
HO-
O1CCOCC1
null
null
COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C>O1CCOCC1>COC(=O)CCCCCNC(=O)[C@@H](N)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-df3ebfe50c8c461e85592be41123da00
COC(=O)CN.CSCC[C@@H](NC(=O)OC(C)(C)C)C(=O)O>>COC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C
C(C)(C)(C)OC(=O)N[C@H](CCSC)C(=O)O.Cl.COC(CN)=O>>COC(CNC([C@H](NC(=O)OC(C)(C)C)CCSC)=O)=O
[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH2:6].O[C:7](=[O:8])[C@@H:9]([CH2:10][CH2:11][S:12][CH3:13])[NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][C:7](=[O:8])[C@@H:9]([CH2:10][CH2:11][S:12][CH3:13])[NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21]
COC(=O)CN.CSCC[C@@H](NC(=O)OC(C)(C)C)C(=O)O
COC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C
null
null
null
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
null
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]-[#8:14]-[C:15](=[O;D1;H0:16])-[C:17]-[NH2;D1;+0:18]>>[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])-...
null
[]
null
null
null
null
The title compound was prepared by the general method of Example 1 using 24.9 g (0.1 mole) of t-butoxycarbonyl-D-methionine (BOC-D-Met) and 13.8 g (0.11 mole) of glycine methyl ester hydrochloride. The crude product was recrystallized from ethyl acetate/Skellysolve B to give the title compound, which was used in subseq...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
null
HO-
null
null
null
COC(=O)CN.CSCC[C@@H](NC(=O)OC(C)(C)C)C(=O)O>>COC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-37b5bfcf3c62463e96183b6c7a43b894
COC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C>>CSCC[C@@H](NC(=O)OC(C)(C)C)C(=O)NCC(=O)O
COC(CNC([C@H](NC(=O)OC(C)(C)C)CCSC)=O)=O.[OH-].[K+]>>C(C)(C)(C)OC(=O)N[C@H](CCSC)C(=O)NCC(=O)O
C[O:20][C:18]([CH2:17][NH:16][C:14]([C@@H:5]([CH2:4][CH2:3][S:2][CH3:1])[NH:6][C:7](=[O:8])[O:9][C:10]([CH3:11])([CH3:12])[CH3:13])=[O:15])=[O:19]>>[CH3:1][S:2][CH2:3][CH2:4][C@@H:5]([NH:6][C:7](=[O:8])[O:9][C:10]([CH3:11])([CH3:12])[CH3:13])[C:14](=[O:15])[NH:16][CH2:17][C:18](=[O:19])[OH:20]
COC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C
CSCC[C@@H](NC(=O)OC(C)(C)C)C(=O)NCC(=O)O
null
null
CO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
null
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
null
null
null
null
The title compound of Example 8 (32.0 g, 0.1 mole) was dissolved in 200 ml of methanol to which was added 200 ml of 2M potassium hydroxide. After ca. 5 min. at room temperature the solution was concentrated to about half volume and diluted with ethyl acetate. The solution was neutralized by washing with two portions of...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
null
Other
CO
null
null
COC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C>CO>CSCC[C@@H](NC(=O)OC(C)(C)C)C(=O)NCC(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5cde0d6b47b04ae18f76dd684a697a17
C1COCCO1.COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C>>COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](N)CCSC.COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](N)CCSC.Cl.O
C(C)(C)(C)OC(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCCC(=O)OC.Cl.O1CCOCC1>>O.Cl.N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCCC(=O)OC.N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCCC(OC)=O.Cl
[CH2:6]1[CH2:7][O:60][CH2:9][CH2:55][O:56]1.[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:39][CH2:40][CH2:41][CH2:42][NH:43][C:44](=[O:45])[C@@H:46]([NH:21][C:22](=[O:23])[CH2:24][NH:25][C:26](=[O:27])[C@H:28]([NH:10][C:11](=[O:12])[O:35][C:20]([CH3:8])([CH3:19])[CH3:64])[CH2:30][CH2:31][S:32][CH3:33])[CH2:47][c:48]1[cH:49][cH:...
C1COCCO1.COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C
COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](N)CCSC.COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](N)CCSC.Cl.O
null
null
O1CCOCC1
Aromatic Heterocycle Formation
OtherReaction
1eb9f9bad8df2ed4a5013c42562dfad69178cfdd17cf7123774db00e33167a9a
83bb2cfddad31ecdb1957349ae1a47c1f8a1d56fcdea61bfe359f575971cab76
c1ccccc1.c1ccccc1
[CH2;D2;+0:1]1-[CH2;D2;+0:2]-[O;H0;D2;+0:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[O;H0;D2;+0:6]-1.[C:7]-[C:8]-[C@@H;D3;+0:9](-[NH;D2;+0:10]-[C;H0;D3;+0:11](=[O;D1;H0:12])-[O;H0;D2;+0:13]-[C;H0;D4;+0:14](-[CH3;D1;+0:15])(-[CH3;D1;+0:16])-[CH3;D1;+0:17])-[C:18](=[O;D1;H0:19])-[#7:20]-[C:21]-[C:22](=[O;D1;H0:23])-[NH;D2;+0:24]-[C@...
null
[]
null
null
1
HOUR
The title compound of Example 10 (12.0 g) was dissolved in 50 ml of dioxane to which was added 50 ml of 6M hydrogen chloride/dioxane. After about one hour, the volatiles were removed in vacuo and the residue triturated thoroughly with diethyl ether. The title compound (10.9 g) was collected as an analytically pure hydr...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ester.Ether.Ether.Ether.Secondary amide.Boc
Ester.Ester.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Primary amine.Primary amine.Monosulfide
C1COCCO1
c1ccccc1
c1ccccc1.c1ccccc1
Other
O1CCOCC1
null
1
C1COCCO1.COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CCSC)NC(=O)OC(C)(C)C>O1CCOCC1>COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](N)CCSC.COC(=O)CCCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](N)CCSC.Cl.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7110aa93414d4664b7879c9e173b8a54
CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(OC(=O)OCC(C)C)cc1)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCCCC(=O)OC.ClCCl.O=C([O-])[O-].O=S(=O)([O-])O>>CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCCCC(=O)OC.CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCSC)C(=O)N...
ClCCl.S([O-])(O)(=O)=O.[K+].C(C)(C)(C)OC(=O)N([C@@H](CC1=CC=C(C=C1)OC(=O)OCC(C)C)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCCC(=O)OC)CC.C([O-])([O-])=O.[K+].[K+]>>O.Cl.C(C)(C)(C)OC(=O)N([C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCCCCCC(=O)OC)CC.C(C)(C)(C)OC(=O)N([C@@...
[CH3:1][CH2:2][N:3]([C:4](=[O:5])[O:6][C:7]([CH3:8])([CH3:56])[CH3:66])[C@@H:11]([CH2:12][c:13]1[cH:14][cH:15][c:16]([O:17][C:51](=[O:52])[O:53][CH2:31][CH:32]([CH3:48])[CH3:50])[cH:18][cH:19]1)[C:20](=[O:21])[NH:22][C@H:23]([CH2:24][CH2:25][S:26][CH3:27])[C:82](=[O:83])[NH:84][CH2:85][C:86](=[O:87])[NH:88][C@@H:89]([C...
CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(OC(=O)OCC(C)C)cc1)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCCCC(=O)OC.ClCCl.O=C([O-])[O-].O=S(=O)([O-])O
CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCCCC(=O)OC.CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCCCC(=O)OC.Cl.Cl.O
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
9cb59a237f03cec0f6065f95c0bce58d49ea6ca2e2e826e2b3188b08090421b5
2654ea69a5122c8288d135ec1f252cd8535ebaf6d52bf1338c76182c65f32e29
O=C(CCc1ccccc1)NCC(=O)NCC(=O)NCCc1ccccc1.O=C(CCc1ccccc1)NCC(=O)NCC(=O)NCCc1ccccc1
[CH3;D1;+0:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-[C;H0;D3;+0:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11].[C:12]-[C:13]-[CH2;D2;+0:14]-[NH;D2;+0:15]-[C;H0;D3;+0:16](=[O;D1;H0:17])-[C:18](-[C:19])-[#7:20]-[C:21](=[O;D1;H0:22])-[C:23]-[#7:24]-[C;H0;D3;+0:25](=[O;D1;H0:26])-[C@H;D3;+0:27](-...
null
[]
null
null
null
null
To a stirred mixture of 1.7 g (1.9 mmole) of the title product of Example 52 in 40 ml of methanol was added 10 ml of 10% aqueous potassium carbonate. After about 75 minutes the resultant solution was poured into a mixture of 150 ml of dichloromethane and 100 ml of 0.5M potassium bisulfate. The organic phase (containing...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ether.Ether.Ether.Secondary amide.Secondary amide.Boc
Carbamic ester.Ester.Ether.Ether.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Aromatic alcohol.Aromatic alcohol.Monosulfide.Boc.Boc
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
CO
null
null
CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(OC(=O)OCC(C)C)cc1)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCCCC(=O)OC.ClCCl.O=C([O-])[O-].O=S(=O)([O-])O>CO>CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCSC)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCCCC(=O)OC.CCN(C(=O)OC(C)(C)C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCSC)C(=O...
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-93fa51c8f7084cf4905f1b5a5619a265
ClCCCBr.c1ccc(CN2CCNCC2)cc1>>Cl.Cl.ClCCCN1CCN(Cc2ccccc2)CC1
BrCCCCl.C(C1=CC=CC=C1)N1CCNCC1.CS(=O)C.[OH-].[K+]>>Cl.Cl.C(C1=CC=CC=C1)N1CCN(CC1)CCCCl
Br[CH2:6][CH2:5][CH2:4][Cl:1].[NH:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[CH2:18][CH2:19]1>>[ClH:1].[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[CH2:18][CH2:19]1
ClCCCBr.c1ccc(CN2CCNCC2)cc1
Cl.Cl.ClCCCN1CCN(Cc2ccccc2)CC1
null
null
O
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CN2CCNCC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[CH2;D2;+0:3]-[Cl;H0;D1;+0:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[Cl;D1;H0:11]-[CH2;D2;+0:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1.[ClH;D0;+0:4]
163.9
[{"value": 55.0, "product": "Cl.Cl.C(C1=CC=CC=C1)N1CCN(CC1)CCCCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 163.9, "product": "Cl.Cl.C(C1=CC=CC=C1)N1CCN(CC1)CCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
31.5 g of 1-bromo-3-chloropropane were added to a mixture of 35 g of 1-benzylpiperazine, 150 ml of dimethyl sulfoxide and 25 g of potassium hydroxide. The resulting mixture was stirred at room temperature for 3 hours. Water was added to the resulting solution, the reaction product was extracted with ether, dried (magne...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Secondary amine
Primary halide.Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccccc1
Br-
O
null
3
ClCCCBr.c1ccc(CN2CCNCC2)cc1>O>Cl.Cl.ClCCCN1CCN(Cc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4a99484645cc4c6ca8fde2874eaff9ec
Cl.ClCCCN1CCN(Cc2ccccc2)CC1.NC(N)=S>>Cl.SCCCN1CCN(Cc2ccccc2)CC1
NC(=S)N.Cl.Cl.C(C1=CC=CC=C1)N1CCN(CC1)CCCCl.C(C)N(CC)CC.[OH-].[Na+]>>Cl.Cl.C(C1=CC=CC=C1)N1CCN(CC1)CCCS
[ClH:2].Cl[CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[CH2:18][CH2:19]1.NC(N)=[S:3]>>[ClH:2].[SH:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[CH2:18][CH2:19]1
Cl.ClCCCN1CCN(Cc2ccccc2)CC1.NC(N)=S
Cl.SCCCN1CCN(Cc2ccccc2)CC1
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CN2CCNCC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].N-C(-N)=[S;H0;D1;+0:4]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[SH;D1;+0:4]
78
[{"value": 78.0, "product": "Cl.Cl.C(C1=CC=CC=C1)N1CCN(CC1)CCCS", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
15 g of thiourea were added to a solution of 35 g of -benzyl-4-(3-chloropropyl)piperazine dihydrochloride, 20 g of triethylamine and 250 ml of reagent ethanol, and the mixture was refluxed for 8 hours. After the addition of a solution of 10 g of sodium hydroxide in 50 ml of water, the resulting mixture was refluxed for...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
C1C[NH]CC[NH]1.c1ccccc1
HCl
C(C)O.O
null
null
Cl.ClCCCN1CCN(Cc2ccccc2)CC1.NC(N)=S>C(C)O.O>Cl.SCCCN1CCN(Cc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e0666140f18d4bf7be07a753ad3f837c
Cl.O=C=Nc1ccccc1.SCCCN1CCN(Cc2ccccc2)CC1>>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
C1(=CC=CC=C1)N=C=O.Cl.Cl.C(C1=CC=CC=C1)N1CCN(CC1)CCCS.C(C)N(CC)CC>>O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=CC=C1
[ClH:2].[O:3]=[C:5]=[N:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1.[SH:13][CH2:14][CH2:15][CH2:16][N:17]1[CH2:18][CH2:19][N:20]([CH2:21][c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)[CH2:28][CH2:29]1>>[ClH:2].[OH2:3].[OH:4][C:5]([NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)=[SH:13][CH2:14][CH2:15][CH2:16][N:17]1[CH2:18]...
Cl.O=C=Nc1ccccc1.SCCCN1CCN(Cc2ccccc2)CC1
Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
null
null
C(Cl)Cl
Acylation
OtherReaction
3bf647ffd3af34283e2312f784edbca620c93d73a88c64f1c90f0c5841a13287
c6ec1d581e09757064752f97a5c83429292625d25a23d379af2b6feb108d2455
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[O;D1;H1:10])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9].[OH2;D0;+0:4]
41.9
[{"value": 20.0, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 41.9, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.6 g of phenyl isocyanate were added to a solution of 4.0 g of 3-(4-benzylpiperazin-1-yl)propanethiol dihydrochloride and 2.6 g of triethylamine in 50 ml of methylene chloride. The mixture was refluxed for four hours, washed with water and dried (sodium sulfate). Precipitation of the salt with ethereal hydrochloric ac...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
Cl.O=C=Nc1ccccc1.SCCCN1CCN(Cc2ccccc2)CC1>C(Cl)Cl>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2696e8dc20db40a1b56b86bc942054c8
ClCCCBr.Clc1ccc(CN2CCNCC2)cc1>>Cl.Cl.ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1
ClC1=CC=C(CN2CCNCC2)C=C1.[OH-].[K+].BrCCCCl>>Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCCl)C=C1
Br[CH2:6][CH2:5][CH2:4][Cl:1].[NH:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]2)[CH2:19][CH2:20]1>>[ClH:1].[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]2)[CH2:19][CH2:20]1
ClCCCBr.Clc1ccc(CN2CCNCC2)cc1
Cl.Cl.ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CN2CCNCC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[CH2;D2;+0:3]-[Cl;H0;D1;+0:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[Cl;D1;H0:11]-[CH2;D2;+0:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1.[ClH;D0;+0:4]
74
[{"value": 74.0, "product": "Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCCl)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Utilizing the procedure described in Example 1(a), 20.0 g of 1-(4-chlorobenzyl)piperazine, 100 ml of dimethyl sulfoxide, 15.0 g of potassium hydroxide and 15.0 of 1-bromo-3-chloropropane yielded 25.1 g (74% of theory) of 1-(4-chlorobenzyl)-4-(3-chloropropyl)piperazine dihydrochloride as a white crystalline solid. Condi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Secondary amine
Primary halide.Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccccc1
Br-
CS(=O)C
null
null
ClCCCBr.Clc1ccc(CN2CCNCC2)cc1>CS(=O)C>Cl.Cl.ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dd78e8a69cf04d3fa6ac7e292bbcdfdd
Cl.ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S>>Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCCl)C=C1.C(C)N(CC)CC.[OH-].[Na+].NC(=S)N>>Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1
[ClH:2].Cl[CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]2)[CH2:19][CH2:20]1.NC(N)=[S:3]>>[ClH:2].[SH:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]2)[CH2:19][CH2:20]1
Cl.ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S
Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CN2CCNCC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].N-C(-N)=[S;H0;D1;+0:4]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[SH;D1;+0:4]
75
[{"value": 75.0, "product": "Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Utilizing the procedure described in Example 1(b), 6.0 g of thiourea, was reacted with 25.2 g of 1-(4-chlorobenzyl-4-(3-chloropropyl)piperazine dihydrochloride and 8.7 g of triethylamine in 200 ml of reagent ethanol. The hydrolysis was effected with 5.0 g of sodium hydroxide in 50 ml of water. Work-up as described abov...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
C1C[NH]CC[NH]1.c1ccccc1
HCl
C(C)O.O
null
null
Cl.ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S>C(C)O.O>Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3d2e024e70544f24ae5de4bfff5d6753
CN=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>CNC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl
CN=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.CNC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][N:2]=[C:3]=[O:4].[ClH:24].[SH:5][CH2:6][CH2:7][CH2:8][N:9]1[CH2:10][CH2:11][N:12]([CH2:13][c:14]2[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]2)[CH2:21][CH2:22]1>>[CH3:1][NH:2][C:3]([OH:4])=[SH:5][CH2:6][CH2:7][CH2:8][N:9]1[CH2:10][CH2:11][N:12]([CH2:13][c:14]2[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]2)[CH2:21]...
CN=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
CNC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
c1ccc(CN2CCNCC2)cc1
[C;D1;H3:1]-[N;H0;D2;+0:2]=[C;H0;D2;+0:3]=[O;H0;D1;+0:4].[C:5]-[C:6]-[SH;D1;+0:7]>>[C:5]-[C:6]-[SH;D2;+0:7]=[C;H0;D3;+0:3](-[OH;D1;+0:4])-[NH;D2;+0:2]-[C;D1;H3:1]
64.4
[{"value": 32.0, "product": "Cl.Cl.CNC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.4, "product": "Cl.Cl.CNC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 0.4 g of methyl isocyanate, 2.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.7 g of triethylamine and 50 ml of methylene chloride, to give 0.75 g (32% of theory) of N-methyl-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]propyl}thiocarbamate d...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CN=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CNC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2a06c362448a46898ee87d972b4b0e1c
CC(C)N=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>CC(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl
C(C)(C)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.C(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][CH:2]([CH3:3])[N:4]=[C:5]=[O:6].[ClH:26].[SH:7][CH2:8][CH2:9][CH2:10][N:11]1[CH2:12][CH2:13][N:14]([CH2:15][c:16]2[cH:17][cH:18][c:19]([Cl:20])[cH:21][cH:22]2)[CH2:23][CH2:24]1>>[CH3:1][CH:2]([CH3:3])[NH:4][C:5]([OH:6])=[SH:7][CH2:8][CH2:9][CH2:10][N:11]1[CH2:12][CH2:13][N:14]([CH2:15][c:16]2[cH:17][cH:18][c:19...
CC(C)N=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
CC(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
c1ccc(CN2CCNCC2)cc1
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])-[N;H0;D2;+0:4]=[C;H0;D2;+0:5]=[O;H0;D1;+0:6].[C:7]-[C:8]-[SH;D1;+0:9]>>[C:7]-[C:8]-[SH;D2;+0:9]=[C;H0;D3;+0:5](-[OH;D1;+0:6])-[NH;D2;+0:4]-[C:2](-[C;D1;H3:1])-[C;D1;H3:3]
56.3
[{"value": 28.0, "product": "Cl.Cl.C(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.3, "product": "Cl.Cl.C(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 0.5 g of isopropyl isocyanate, 2.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.7 g of triethylamine and 50 ml of methylene chloride, to give 0.7 g (28% of theory) of N-isopropyl-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]propyl}thiocarbam...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CC(C)N=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CC(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9d1937c896e54cb4b8977e4368ead391
O=C=NC1CCCCC1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>Cl.Cl.OC(NC1CCCCC1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
C1(CCCCC1)N=C=O.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1>>Cl.Cl.C1(CCCCC1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[O:3]=[C:4]=[N:5][CH:6]1[CH2:7][CH2:8][CH2:9][CH2:10][CH2:11]1.[Cl:1][c:24]1[cH:23][cH:22][c:21]([CH2:20][N:19]2[CH2:18][CH2:17][N:16]([CH2:15][CH2:14][CH2:13][SH:12])[CH2:29][CH2:28]2)[cH:27][cH:26]1>>[ClH:1].[ClH:2].[OH:3][C:4]([NH:5][CH:6]1[CH2:7][CH2:8][CH2:9][CH2:10][CH2:11]1)=[SH:12][CH2:13][CH2:14][CH2:15][N:16]...
O=C=NC1CCCCC1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
Cl.Cl.OC(NC1CCCCC1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
9ddf29a0add694314a86de0a39264129a9713962546a4ec140d50667e08753fd
126df213390631efc30fe64ae8364e595ba3d5d450128f642d2c5ebbd6a2ca21
C(NC1CCCCC1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2](-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;H0;D1;+0:5])-[C:6].[C:7]-[C:8]-[SH;D1;+0:9].[Cl;H0;D1;+0:10]-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]>>[C:1]-[C:2](-[NH;D2;+0:3]-[C;H0;D3;+0:4](-[OH;D1;+0:5])=[SH;D2;+0:9]-[C:8]-[C:7])-[C:6].[Cl;D1;H0:16]-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15].[ClH;D0;+0:10]
100.7
[{"value": 30.0, "product": "Cl.Cl.C1(CCCCC1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.7, "product": "Cl.Cl.C1(CCCCC1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A mixture of 1.0 g of cyclohexyl isocyanate, 2.1 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol and 10 ml of methylene chloride was stirred at room temperature overnight and then concentrated in vacuo. The residue crystallized upon standing. The product was recrystallized from aqueous ethanol, dissolved in ether...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Isocyanate.Aliphatic thiol
Aromatic halide.Secondary amine
c1ccccc1
c1ccccc1
C1CCCCC1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
8
O=C=NC1CCCCC1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>Cl.Cl.OC(NC1CCCCC1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1915446d4e914e9ba2cead88cca852e5
Cl.O=C=Nc1ccccc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>Cl.OC(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
C1(=CC=CC=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[ClH:2].[O:3]=[C:4]=[N:5][c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1.[SH:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][CH2:18][N:19]([CH2:20][c:21]2[cH:22][cH:23][c:24]([Cl:25])[cH:26][cH:27]2)[CH2:28][CH2:29]1>>[ClH:2].[OH:3][C:4]([NH:5][c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)=[SH:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][C...
Cl.O=C=Nc1ccccc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
Cl.OC(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
107.1
[{"value": 53.0, "product": "Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 107.1, "product": "Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 4.3 g of phenyl isocyanate, 12.7 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 7.3 g of triethylamine and 100 ml of methylene chloride, to give 9.1 g (53% of theory) of N-phenyl-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]propyl}thiocarbamate ...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
Cl.O=C=Nc1ccccc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>Cl.OC(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fcb401d798df4579a0d7b003226aee98
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>CCCCc1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl
C(CCC)C1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.C(CCC)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([N:9]=[C:10]=[O:11])[cH:30][cH:31]1.[ClH:33].[SH:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][CH2:18][N:19]([CH2:20][c:21]2[cH:22][cH:23][c:24]([Cl:25])[cH:26][cH:27]2)[CH2:28][CH2:29]1>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([NH:9][C:10]([OH:11])=[SH:12][C...
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
CCCCc1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
56.8
[{"value": 28.0, "product": "Cl.Cl.C(CCC)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.8, "product": "Cl.Cl.C(CCC)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.0 g of 4-n-butylphenyl isocyanate, 2.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.7 g of triethylamine and 50 ml of methylene chloride, to give 0.85 g (28% of theory) of N-(4-n-butylphenyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]pr...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CCCCc1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-191ac2eaae9442b6b59ea19756714b3f
Cl.O=C=Nc1ccc(F)cc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>Cl.OC(Nc1ccc(F)cc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
FC1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.FC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[ClH:2].[O:3]=[C:4]=[N:5][c:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][cH:12]1.[SH:13][CH2:14][CH2:15][CH2:16][N:17]1[CH2:18][CH2:19][N:20]([CH2:21][c:22]2[cH:23][cH:24][c:25]([Cl:26])[cH:27][cH:28]2)[CH2:29][CH2:30]1>>[ClH:2].[OH:3][C:4]([NH:5][c:6]1[cH:7][cH:8][c:9]([F:10])[cH:11][cH:12]1)=[SH:13][CH2:14][CH2:15][CH2:16][N:...
Cl.O=C=Nc1ccc(F)cc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
Cl.OC(Nc1ccc(F)cc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
92.3
[{"value": 47.0, "product": "Cl.Cl.FC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.3, "product": "Cl.Cl.FC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 0.8 g of 4-fluorophenyl isocyanate, 2.2 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.6 g of triethylamine and 25 ml of methylene chloride, to give 1.41 g (47% of theory) of N-(4-fluorophenyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]prop...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
Cl.O=C=Nc1ccc(F)cc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>Cl.OC(Nc1ccc(F)cc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d33367d8f1b54a0ba584c0599674b958
Cl.O=C=Nc1ccc(Cl)cc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>Cl.O.OC(Nc1ccc(Cl)cc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
ClC1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.CCl>>O.Cl.Cl.ClC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[ClH:2].[O:3]=[C:5]=[N:6][c:7]1[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]1.[SH:14][CH2:15][CH2:16][CH2:17][N:18]1[CH2:19][CH2:20][N:21]([CH2:22][c:23]2[cH:24][cH:25][c:26]([Cl:27])[cH:28][cH:29]2)[CH2:30][CH2:31]1>>[ClH:2].[OH2:3].[OH:4][C:5]([NH:6][c:7]1[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]1)=[SH:14][CH2:15][CH2:16...
Cl.O=C=Nc1ccc(Cl)cc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
Cl.O.OC(Nc1ccc(Cl)cc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(C)N(CC)CC
Acylation
OtherReaction
3bf647ffd3af34283e2312f784edbca620c93d73a88c64f1c90f0c5841a13287
c6ec1d581e09757064752f97a5c83429292625d25a23d379af2b6feb108d2455
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[O;D1;H1:10])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9].[OH2;D0;+0:4]
42.4
[{"value": 21.0, "product": "O.Cl.Cl.ClC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 42.4, "product": "O.Cl.Cl.ClC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.5 g of 4-chlorophenyl isocyanate, 3.5 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 1.2 g of triethylamine and 50 ml of methyl chloride, to give 1.1 g (21% of theory) of N-(4-chlorophenyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]propyl}t...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(C)N(CC)CC
null
null
Cl.O=C=Nc1ccc(Cl)cc1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(C)N(CC)CC>Cl.O.OC(Nc1ccc(Cl)cc1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-326edc7cd8db46ef8ec72874e2c49ab5
Cl.O=C=Nc1ccc(Cl)c(Cl)c1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>Cl.OC(Nc1ccc(Cl)c(Cl)c1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
ClC=1C=C(C=CC1Cl)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.ClC=1C=C(C=CC1Cl)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[ClH:2].[O:3]=[C:4]=[N:5][c:6]1[cH:7][cH:8][c:9]([Cl:10])[c:11]([Cl:12])[cH:13]1.[SH:14][CH2:15][CH2:16][CH2:17][N:18]1[CH2:19][CH2:20][N:21]([CH2:22][c:23]2[cH:24][cH:25][c:26]([Cl:27])[cH:28][cH:29]2)[CH2:30][CH2:31]1>>[ClH:2].[OH:3][C:4]([NH:5][c:6]1[cH:7][cH:8][c:9]([Cl:10])[c:11]([Cl:12])[cH:13]1)=[SH:14][CH2:15][...
Cl.O=C=Nc1ccc(Cl)c(Cl)c1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
Cl.OC(Nc1ccc(Cl)c(Cl)c1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
52.2
[{"value": 26.0, "product": "Cl.Cl.ClC=1C=C(C=CC1Cl)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.2, "product": "Cl.Cl.ClC=1C=C(C=CC1Cl)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.6 g of 3,4-dichlorophenyl isocyanate, 3.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.9 g of triethylamine and 50 ml of methylene chloride, to give 1.2 g (26% of theory) of N-(3,4-dichlorophenyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
Cl.O=C=Nc1ccc(Cl)c(Cl)c1.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>Cl.OC(Nc1ccc(Cl)c(Cl)c1)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cf45e59bdef54089b629c31b7412880d
CCN(CC)CC.COc1ccccc1N=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>COc1ccccc1NC(O)=[SH]CCCN1CCN(C(Cl)c2ccccc2)CC1.COc1ccccc1NC(O)=[SH]CCCN1CCN(C(Cl)c2ccccc2)CC1.Cl.Cl.Cl.O.O.O
COC1=C(C=CC=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>O.Cl.Cl.COC1=C(C=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C1=CC=CC=C1)Cl.O.O.COC1=C(C=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C1=CC=CC=C1)Cl.Cl.Cl
[CH2:18]([N:19]([CH2:20][CH3:22])[CH2:44][CH3:43])[CH3:23].[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[N:9]=[C:10]=[O:11].[ClH:61].[SH:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][CH2:47][N:48]([CH2:49][c:51]2[cH:27][cH:26][c:54]([Cl:21])[cH:53][cH:52]2)[CH2:57][CH2:58]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c...
CCN(CC)CC.COc1ccccc1N=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
COc1ccccc1NC(O)=[SH]CCCN1CCN(C(Cl)c2ccccc2)CC1.COc1ccccc1NC(O)=[SH]CCCN1CCN(C(Cl)c2ccccc2)CC1.Cl.Cl.Cl.O.O.O
null
null
C(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
28033e2d67866b16340c76bc9501d8fe873ef33747a77835ac25a8f39fd65bd5
4749bac01e6e887a02951c249ccae0b96f7479ff629d0210328fb7b10470049c
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1.C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[CH3;D1;+0:1]-[CH2;D2;+0:2]-[N;H0;D3;+0:3](-[CH2;D2;+0:4]-[CH3;D1;+0:5])-[CH2;D2;+0:6]-[CH3;D1;+0:7].[Cl;H0;D1;+0:8]-[c;H0;D3;+0:9]1:[c:10]:[c:11]:[c;H0;D3;+0:12](-[CH2;D2;+0:13]-[#7:14]2-[C:15]-[CH2;D2;+0:16]-[N;H0;D3;+0:17](-[C:18]-[C:19]-[C:20]-[SH;D1;+0:21])-[CH2;D2;+0:22]-[CH2;D2;+0:23]-2):[cH;D2;+0:24]:[cH;D2;+0:...
48.2
[{"value": 20.0, "product": "O.Cl.Cl.COC1=C(C=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C1=CC=CC=C1)Cl.O.O.COC1=C(C=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C1=CC=CC=C1)Cl.Cl.Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.2, "product": "O.Cl.Cl.COC1=C(C=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C1=CC=CC=C1)Cl.O.O.COC1=C(C=CC=C1)NC(O)=SCCCN...
null
null
null
null
The procedure described in Example 2 was followed, using 1.3 g of 2-methoxyphenyl isocyanate, 3.0 g of 3-[4-(4-chlorobenzyl)piperazin--yl]propanethiol dihydrochloride, 0.9 g of triethylamine and 50 ml of methylene chloride, to give 0.9 g (20% of theory) of N-(2-methoxyphenyl)-S-{3-[4-(chlorobenzyl)piperazin-1-yl]propyl...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Isocyanate.Tertiary amine.Tertiary amine.Aliphatic thiol
Secondary halide.Secondary halide.Ether.Secondary amine.Secondary amine.Tertiary amine.Tertiary amine.Tertiary amine
C1C[NH]CC[NH]1.c1ccccc1
C1C[NH]CC[NH]1.c1ccccc1.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CCN(CC)CC.COc1ccccc1N=C=O.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>COc1ccccc1NC(O)=[SH]CCCN1CCN(C(Cl)c2ccccc2)CC1.COc1ccccc1NC(O)=[SH]CCCN1CCN(C(Cl)c2ccccc2)CC1.Cl.Cl.Cl.O.O.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c50c30503cc343a3939f9f57a5d8d133
COc1cccc(N=C=O)c1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>COc1cccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1.Cl
COC=1C=C(C=CC1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.COC=1C=C(C=CC1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([N:8]=[C:9]=[O:10])[cH:29]1.[ClH:31].[SH:11][CH2:12][CH2:13][CH2:14][N:15]1[CH2:16][CH2:17][N:18]([CH2:19][c:20]2[cH:21][cH:22][c:23]([Cl:24])[cH:25][cH:26]2)[CH2:27][CH2:28]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH:8][C:9]([OH:10])=[SH:11][CH2:12][CH2:13][CH2:14][N:15]2...
COc1cccc(N=C=O)c1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
COc1cccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
63.3
[{"value": 32.0, "product": "Cl.Cl.COC=1C=C(C=CC1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.3, "product": "Cl.Cl.COC=1C=C(C=CC1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.3 g of 3-methoxyphenyl isocyanate, 3.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.9 g of triethylamine and 50 ml of methylene chloride, to give 1.35 g (32% of theory) of N-(3-methoxyphenyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]pr...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
COc1cccc(N=C=O)c1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>COc1cccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7f2d634825de4fb38e53460cd8c87fba
COc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>COc1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl.O
COC1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>O.Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([N:7]=[C:8]=[O:9])[cH:28][cH:29]1.[ClH:31].[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2:16][N:17]([CH2:18][c:19]2[cH:20][cH:21][c:22]([Cl:23])[cH:24][cH:25]2)[CH2:26][CH2:27]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][C:8]([OH:9])=[SH:10][CH2:11][CH2:12][CH2:13][N:14]2[CH2:15...
COc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
COc1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl.O
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
d8c9c1a89d54a4cd76e63eccb394ecc0c920cdad853402e3a087dd7621e6fd3e
bc4576d342715dde5eb26e659c67b11b56a595de68edf5b187c45e442919e403
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
48.9
[{"value": 25.0, "product": "O.Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.9, "product": "O.Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 0.9 g of 4-methoxyphenyl isocyanate, 2.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.7 g of triethylamine and 50 ml of methylene chloride, to give 0.72 g (25% of theory) of N-(4-methoxyphenyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]pr...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
COc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>COc1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cc89c78e3c7641519d60f0df07730851
CC(=O)c1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>CC(=O)c1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl.O
C(C)(=O)C1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>O.Cl.Cl.C(C)(=O)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([N:8]=[C:9]=[O:10])[cH:29][cH:30]1.[ClH:32].[SH:11][CH2:12][CH2:13][CH2:14][N:15]1[CH2:16][CH2:17][N:18]([CH2:19][c:20]2[cH:21][cH:22][c:23]([Cl:24])[cH:25][cH:26]2)[CH2:27][CH2:28]1>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([NH:8][C:9]([OH:10])=[SH:11][CH2:12][CH2:13][CH2...
CC(=O)c1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
CC(=O)c1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl.O
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
d8c9c1a89d54a4cd76e63eccb394ecc0c920cdad853402e3a087dd7621e6fd3e
bc4576d342715dde5eb26e659c67b11b56a595de68edf5b187c45e442919e403
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
55.1
[{"value": 29.0, "product": "O.Cl.Cl.C(C)(=O)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 55.1, "product": "O.Cl.Cl.C(C)(=O)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.0 g of 4-acetylphenyl isocyanate, 2.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.7 g of triethylamine and 50 ml of methylene chloride, to give 0.83 g (29% of theory) of N-(4-acetylphenyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]prop...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CC(=O)c1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CC(=O)c1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ca1b8ca8d82f487c9acd52ad82720fa7
CCOC(=O)c1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>CCOC(=O)c1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl
C(C)OC(=O)C1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.C(C)OC(=O)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([N:10]=[C:11]=[O:12])[cH:31][cH:32]1.[ClH:34].[SH:13][CH2:14][CH2:15][CH2:16][N:17]1[CH2:18][CH2:19][N:20]([CH2:21][c:22]2[cH:23][cH:24][c:25]([Cl:26])[cH:27][cH:28]2)[CH2:29][CH2:30]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([NH:10][C:11]([OH:12])...
CCOC(=O)c1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
CCOC(=O)c1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
55.2
[{"value": 28.0, "product": "Cl.Cl.C(C)OC(=O)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 55.2, "product": "Cl.Cl.C(C)OC(=O)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.1 g of 4-ethoxycarbonylphenyl isocyanate, 2.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 0.7 g of triethylamine and 50 ml of methylene chloride, to give 0.85 g (28% of theory) of N-(4-ethoxycarbonylphenyl)-S-{3-[4-(4-chlorobenzyl)pip...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CCOC(=O)c1ccc(N=C=O)cc1.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CCOC(=O)c1ccc(NC(O)=[SH]CCCN2CCN(Cc3ccc(Cl)cc3)CC2)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-077a49be5a59401b8abfc287ca092333
Cc1ccc(CN2CCNCC2)cc1.ClCCCBr>>Cc1ccc(CN2CCN(CCCCl)CC2)cc1.Cl.Cl
BrCCCCl.CC1=CC=C(CN2CCNCC2)C=C1.[OH-].[K+].CS(=O)C>>Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCCl)C=C1
[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][N:7]2[CH2:8][CH2:9][NH:10][CH2:15][CH2:16]2)[cH:17][cH:18]1.Br[CH2:11][CH2:12][CH2:13][Cl:14]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][N:7]2[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][Cl:14])[CH2:15][CH2:16]2)[cH:17][cH:18]1.[ClH:19].[ClH:20]
Cc1ccc(CN2CCNCC2)cc1.ClCCCBr
Cc1ccc(CN2CCN(CCCCl)CC2)cc1.Cl.Cl
null
null
O
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
ace038913084fcdf81b35aa8057c48e144f1d774d55e84580611fa34db8b1552
da87afc172ebd302d462893afe878066c210a24130312f3acba00f6d41a889fd
c1ccc(CN2CCNCC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
274.5
[{"value": 94.0, "product": "Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCCl)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 274.5, "product": "Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCCl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
45
MINUTE
A mixture of 14.0 g of 1-(4-methylbenzyl)piperazine, 8.0 g of potassium hydroxide and 125 ml of dimethyl sulfoxide was stirred for 45 minutes. 11.8 g of 1-bromo-3-chloropropane were then added, and the mixture was stirred for an additional hour. Water was added, and the product was extracted with ether, and the extract...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1
Br-
O
null
0.75
Cc1ccc(CN2CCNCC2)cc1.ClCCCBr>O>Cc1ccc(CN2CCN(CCCCl)CC2)cc1.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-76581291372d4210a560be5a42ab7838
Cc1ccc(CN2CCN(CCCCl)CC2)cc1.Cl.NC(N)=S>>Cc1ccc(CN2CCN(CCCS)CC2)cc1.Cl
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCCl)C=C1>>Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCS)C=C1
Cl[CH2:13][CH2:12][CH2:11][N:10]1[CH2:9][CH2:8][N:7]([CH2:6][c:5]2[cH:4][cH:3][c:2]([CH3:1])[cH:18][cH:17]2)[CH2:16][CH2:15]1.[ClH:20].NC(N)=[S:14]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][N:7]2[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][SH:14])[CH2:15][CH2:16]2)[cH:17][cH:18]1.[ClH:20]
Cc1ccc(CN2CCN(CCCCl)CC2)cc1.Cl.NC(N)=S
Cc1ccc(CN2CCN(CCCS)CC2)cc1.Cl
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CN2CCNCC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].N-C(-N)=[S;H0;D1;+0:4]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[SH;D1;+0:4]
72
[{"value": 72.0, "product": "Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCS)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.8, "product": "Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCS)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 7.7 g of thiourea, 23.0 g of 1-(4-methylbenzyl)-4-(3-chloropropyl)piperazine dihydrochloride, 6.5 g of triethylamine and 250 ml of reagent ethanol. The hydrolysis was effected with 6.0 g of sodium hydroxide in 40 ml of water. Work-up, as described above, gave ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
c1ccccc1.C1C[NH]CC[NH]1
HCl
C(C)O.O
null
null
Cc1ccc(CN2CCN(CCCCl)CC2)cc1.Cl.NC(N)=S>C(C)O.O>Cc1ccc(CN2CCN(CCCS)CC2)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1a29534138cf42879b452e139d3dd015
CCN(CC)CC.Cc1ccc(CN2CCN(CCCS)CC2)cc1.Cl.O=C=Nc1ccccc1>>Cc1ccc(CN2CCN(CCC[SH]=C(O)Nc3ccccc3)CC2)cc1.Cc1ccc(CN2CCN(CCC[SH]=C(O)Nc3ccccc3)CC2)cc1.Cl.Cl.Cl.O.O.O
C1(=CC=CC=C1)N=C=O.Cl.Cl.CC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)C.O.O.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)C.Cl.Cl
[CH3:1][CH2:8][N:7]([CH2:6][CH3:5])[CH2:38][CH3:39].[CH2:9]1[N:10]([CH2:11][CH2:12][CH2:13][SH:14])[CH2:24][CH2:25][N:34]([CH2:33][c:32]2[cH:31][cH:30][c:29]([CH3:28])[cH:54][cH:53]2)[CH2:35]1.[ClH:58].[C:15](=[O:16])=[N:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][N:7]2[CH2:8]...
CCN(CC)CC.Cc1ccc(CN2CCN(CCCS)CC2)cc1.Cl.O=C=Nc1ccccc1
Cc1ccc(CN2CCN(CCC[SH]=C(O)Nc3ccccc3)CC2)cc1.Cc1ccc(CN2CCN(CCC[SH]=C(O)Nc3ccccc3)CC2)cc1.Cl.Cl.Cl.O.O.O
null
null
C(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
8101f5def4764d3a464ace49dcd811a6b5a64aaa086c4febacde1faa81e5ff91
6c59d446178fa8326efe9e6fcc7fe762e06c74f526449b4f57ac008c79818102
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1.C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[CH3;D1;+0:1]-[CH2;D2;+0:2]-[N;H0;D3;+0:3](-[C:4]-[CH3;D1;+0:5])-[CH2;D2;+0:6]-[CH3;D1;+0:7].[O;H0;D1;+0:8]=[C;H0;D2;+0:9]=[N;H0;D2;+0:10]-[c:11](:[c:12]):[c:13].[SH;D1;+0:14]-[C:15]-[C:16]-[C:17]-[#7:18]1-[C:19]-[CH2;D2;+0:20]-[N;H0;D3;+0:21](-[C:22]-[c:23])-[CH2;D2;+0:24]-[CH2;D2;+0:25]-1>>[#16:26]-[C:27]-[CH2;D2;+0:...
48.2
[{"value": 20.0, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)C.O.O.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)C.Cl.Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.2, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)C.O.O.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CC...
null
null
null
null
The procedure described in Example 2 was followed, using 1.4 g of phenyl isocyanate, 4.0 g of 3-[4-(4-methylbenzyl)piperazin-1-yl]propanethiol dihydrochloride, 1.2 g of triethylamine and 50 ml of methylene chloride, to give 1.1 g (20% of theory) of N-phenyl-S-{3-[4-(4-methylbenzyl)piperazin-1-yl]propyl}thiocarbamate di...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Tertiary amine.Tertiary amine.Aliphatic thiol
Secondary amine.Secondary amine.Tertiary amine.Tertiary amine.Tertiary amine
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.C1C[NH]CC[NH]1.c1ccccc1
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CCN(CC)CC.Cc1ccc(CN2CCN(CCCS)CC2)cc1.Cl.O=C=Nc1ccccc1>C(Cl)Cl>Cc1ccc(CN2CCN(CCC[SH]=C(O)Nc3ccccc3)CC2)cc1.Cc1ccc(CN2CCN(CCC[SH]=C(O)Nc3ccccc3)CC2)cc1.Cl.Cl.Cl.O.O.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-73dfc2a4ed354bdeacc95510bbfc783d
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1.ClCCCBr>>CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCCl
BrCCCCl.ClC1=CC=C(CN2C(CNC(C2)C)C)C=C1.[OH-].[K+].CS(=O)C>>ClC1=CC=C(CN2C(CN(C(C2)C)CCCCl)C)C=C1
[CH3:1][CH:2]1[CH2:3][N:4]([CH2:5][c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH:13]([CH3:14])[CH2:15][NH:16]1.Br[CH2:17][CH2:18][CH2:19][Cl:20]>>[CH3:1][CH:2]1[CH2:3][N:4]([CH2:5][c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH:13]([CH3:14])[CH2:15][N:16]1[CH2:17][CH2:18][CH2:19][Cl:20]
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1.ClCCCBr
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCCl
null
null
O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
bad6b7d8e43c3debef0c262d60564e43415b41bcee72e526419c8c16be18fec1
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CN2CCNCC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[C:5]1-[C:6]-[#7:7]-[C:8]-[C:9]-[NH;D2;+0:10]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:10]1-[C:9]-[C:8]-[#7:7]-[C:6]-[C:5]-1-[C;D1;H3:4]
58
[{"value": 58.0, "product": "ClC1=CC=C(CN2C(CN(C(C2)C)CCCCl)C)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
22.0 g g of 1-bromo-3-chloropropane were added to a mixture of 33.0 g of 4-chlorobenzyl-2,5-dimethylpiperazine, 25.0 g of potassium hydroxide and 125 ml of dimethyl sulfoxide. After stirring the solution for 3 hours at room temperature, water was added, the product was extracted with ether, and the extract was dried (m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccccc1
HBr
O
null
3
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1.ClCCCBr>O>CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCCl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ac25165bc3e44b80977c05d9becefbc7
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCCl.NC(N)=S>>CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCS.Cl.Cl
[OH-].[Na+].NC(=S)N.ClC1=CC=C(CN2C(CN(C(C2)C)CCCCl)C)C=C1.C(C)O>>Cl.Cl.ClC1=CC=C(CN2CC(N(CC2C)CCCS)C)C=C1
[CH3:1][CH:2]1[CH2:3][N:4]([CH2:5][c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH:13]([CH3:14])[CH2:15][N:16]1[CH2:17][CH2:18][CH2:19][Cl:21].NC(N)=[S:20]>>[CH3:1][CH:2]1[CH2:3][N:4]([CH2:5][c:6]2[cH:7][cH:8][c:9]([Cl:10])[cH:11][cH:12]2)[CH:13]([CH3:14])[CH2:15][N:16]1[CH2:17][CH2:18][CH2:19][SH:20].[ClH:21].[ClH:...
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCCl.NC(N)=S
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCS.Cl.Cl
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CN2CCNCC2)cc1
N-C(-N)=[S;H0;D1;+0:1].[C:2]-[C:3]-[CH2;D2;+0:4]-[Cl;H0;D1;+0:5]>>[C:2]-[C:3]-[CH2;D2;+0:4]-[SH;D1;+0:1].[ClH;D0;+0:5]
249.9
[{"value": 83.0, "product": "Cl.Cl.ClC1=CC=C(CN2CC(N(CC2C)CCCS)C)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 249.9, "product": "Cl.Cl.ClC1=CC=C(CN2CC(N(CC2C)CCCS)C)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 12.7 g of thiourea and 26.0 g of 1-(4-chlorobenzyl)-2,5-dimethyl-4-(3-chloropropyl)piperazine in 250 ml of reagent ethanol. The hydrolysis was effected with 10.0 g of sodium hydroxide in 50 ml of water. Work-up, as described above, gave 26.5 g (83% of theory) ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
C1C[NH]CC[NH]1.c1ccccc1
Other
O
null
null
CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCCl.NC(N)=S>O>CC1CN(Cc2ccc(Cl)cc2)C(C)CN1CCCS.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-93cf949e00b544a7b8fbd151bc44a719
CC(c1ccccc1)N1CCNCC1.ClCCCBr>>CC(c1ccccc1)N1CCN(CCCCl)CC1.Cl.Cl
C1(=CC=CC=C1)C(C)N1CCNCC1.[OH-].[K+].BrCCCCl>>Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCCl
[CH3:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]1[CH2:10][CH2:11][NH:12][CH2:17][CH2:18]1.Br[CH2:13][CH2:14][CH2:15][Cl:16]>>[CH3:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]1[CH2:10][CH2:11][N:12]([CH2:13][CH2:14][CH2:15][Cl:16])[CH2:17][CH2:18]1.[ClH:19].[ClH:20]
CC(c1ccccc1)N1CCNCC1.ClCCCBr
CC(c1ccccc1)N1CCN(CCCCl)CC1.Cl.Cl
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
ace038913084fcdf81b35aa8057c48e144f1d774d55e84580611fa34db8b1552
da87afc172ebd302d462893afe878066c210a24130312f3acba00f6d41a889fd
c1ccc(CN2CCNCC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
409.8
[{"value": 96.0, "product": "Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 409.8, "product": "Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 17(a) was followed, using 16.5 g of 1-(1-phenylethyl)piperazine, 8.0 g of potassium hydroxide, 125 ml of dimethyl sulfoxide and 9.5 g of 1-bromo-3-chloropropane. Work-up, as described above, gave 28.0 g (96% of theory) of 1-(1-phenylethyl)-4-(3-chloropropyl)piperazine dihydrochloride ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1
Br-
CS(=O)C
null
null
CC(c1ccccc1)N1CCNCC1.ClCCCBr>CS(=O)C>CC(c1ccccc1)N1CCN(CCCCl)CC1.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d017d716638549a595ea280009b45216
CC(c1ccccc1)N1CCN(CCCCl)CC1.Cl.NC(N)=S>>CC(c1ccccc1)N1CCN(CCCS)CC1.Cl
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCCl>>Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCS
Cl[CH2:15][CH2:14][CH2:13][N:12]1[CH2:11][CH2:10][N:9]([CH:2]([CH3:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][cH:8]2)[CH2:18][CH2:17]1.[ClH:20].NC(N)=[S:16]>>[CH3:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]1[CH2:10][CH2:11][N:12]([CH2:13][CH2:14][CH2:15][SH:16])[CH2:17][CH2:18]1.[ClH:20]
CC(c1ccccc1)N1CCN(CCCCl)CC1.Cl.NC(N)=S
CC(c1ccccc1)N1CCN(CCCS)CC1.Cl
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CN2CCNCC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].N-C(-N)=[S;H0;D1;+0:4]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[SH;D1;+0:4]
51
[{"value": 51.0, "product": "Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCS", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.4, "product": "Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCS", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 9.8 g of thiourea, 29.0 g of 1-(1-phenylethyl)-4-(3-chloropropyl)piperazine dihydrochloride, 8.3 g of triethylamine and 250 ml of reagent ethanol. The hydrolysis was effected with 6.0 g of sodium hydroxide in 40 ml of water. Work-up, as above, gave 14.5 g (51%...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
c1ccccc1.C1C[NH]CC[NH]1
HCl
C(C)O.O
null
null
CC(c1ccccc1)N1CCN(CCCCl)CC1.Cl.NC(N)=S>C(C)O.O>CC(c1ccccc1)N1CCN(CCCS)CC1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d4976450c77348398a9bbdba85a55e9b
CC(c1ccccc1)N1CCN(CCCS)CC1.Cl.O=C=Nc1ccccc1>>CC(c1ccccc1)N1CCN(CCC[SH]=C(O)Nc2ccccc2)CC1.Cl.O.O
C1(=CC=CC=C1)N=C=O.Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCS.C(C)N(CC)CC>>O.O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C)C1=CC=CC=C1
[CH3:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]1[CH2:10][CH2:11][N:12]([CH2:13][CH2:14][CH2:15][SH:16])[CH2:26][CH2:27]1.[ClH:29].[C:17](=[O:18])=[N:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1>>[CH3:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]1[CH2:10][CH2:11][N:12]([CH2:13][CH2:14][CH2:15][SH:16]=...
CC(c1ccccc1)N1CCN(CCCS)CC1.Cl.O=C=Nc1ccccc1
CC(c1ccccc1)N1CCN(CCC[SH]=C(O)Nc2ccccc2)CC1.Cl.O.O
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[O;H0;D1;+0:4]=[C;H0;D2;+0:5]=[N;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:5](-[OH;D1;+0:4])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
94.8
[{"value": 38.0, "product": "O.O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.8, "product": "O.O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)C(C)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.6 g of phenyl isocyanate, 4.5 g of 3-[4-(1-phenylethyl)piperazin-1-yl]propanethiol dihydrochloride, 1.3 g of triethylamine and 50 ml of methylene chloride, to give 2.1 g (38% of theory) of N-phenyl-S-{3-[4-(1-phenylethyl)piperazin-1-yl]propyl}thiocarbamate dihy...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CC(c1ccccc1)N1CCN(CCCS)CC1.Cl.O=C=Nc1ccccc1>C(Cl)Cl>CC(c1ccccc1)N1CCN(CCC[SH]=C(O)Nc2ccccc2)CC1.Cl.O.O