dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
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large_stringlengths
14
3.37k
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large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
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-01dbb772c5e249108f0b191ed17a2c0c
ord-4cbd87311b894e64af3aedbc4e278737
ClCCCBr.c1ccc(CCN2CCNCC2)cc1>>Cl.Cl.ClCCCN1CCN(CCc2ccccc2)CC1
C(CC1=CC=CC=C1)N1CCNCC1.[OH-].[K+].BrCCCCl>>Cl.Cl.C(CC1=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][CH2:12][c:13]2[cH:14][cH:15][cH: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][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[CH2:19][CH2:20]1
ClCCCBr.c1ccc(CCN2CCNCC2)cc1
Cl.Cl.ClCCCN1CCN(CCc2ccccc2)CC1
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CCN2CCNCC2)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]
188.8
[{"value": 64.0, "product": "Cl.Cl.C(CC1=CC=CC=C1)N1CCN(CC1)CCCCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 188.8, "product": "Cl.Cl.C(CC1=CC=CC=C1)N1CCN(CC1)CCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(a) was followed, using 29.4 g of 1-phenethyl piperazine, 25.0 g of potassium hydroxide, 100 ml of dimethyl sulfoxide and 24.0 g of 1-bromo-3-chloropropane. Work-up, as described above, gave 32.6 g (64% of theory) of 1-phenethyl-4-(3-chloropropyl)piperazine dihydrochloride as an off-...
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.c1ccc(CCN2CCNCC2)cc1>CS(=O)C>Cl.Cl.ClCCCN1CCN(CCc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a12cdbab8eb74afc9c6c800abef1a068
Cl.ClCCCN1CCN(CCc2ccccc2)CC1.NC(N)=S>>Cl.SCCCN1CCN(CCc2ccccc2)CC1
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.C(CC1=CC=CC=C1)N1CCN(CC1)CCCCl>>Cl.Cl.C(CC1=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][CH2:12][c:13]2[cH:14][cH:15][cH: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][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[CH2:19][CH2:20]1
Cl.ClCCCN1CCN(CCc2ccccc2)CC1.NC(N)=S
Cl.SCCCN1CCN(CCc2ccccc2)CC1
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CCN2CCNCC2)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]
81.6
[{"value": 79.0, "product": "Cl.Cl.C(CC1=CC=CC=C1)N1CCN(CC1)CCCS", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.6, "product": "Cl.Cl.C(CC1=CC=CC=C1)N1CCN(CC1)CCCS", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 15.2 g of thiourea, 32.6 g of 1-phenethyl-4-(3-chloropropyl)piperazine dihydrochloride, 20.0 g of triethylamine and 250 ml of reagent ethanol. The hydrolysis was effected with 10.0 g of sodium hydroxide in 40 ml of water. Work-up, as described above, gave 26.4...
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(CCc2ccccc2)CC1.NC(N)=S>C(C)O.O>Cl.SCCCN1CCN(CCc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5ecfcbe5ec174867b5a9332b168281de
Cl.O=C=Nc1ccccc1.SCCCN1CCN(CCc2ccccc2)CC1>>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)CC1
C1(=CC=CC=C1)N=C=O.Cl.Cl.C(CC1=CC=CC=C1)N1CCN(CC1)CCCS.C(C)N(CC)CC>>O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCC1=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][CH2:22][c:23]2[cH:24][cH:25][cH:26][cH:27][cH:28]2)[CH2:29][CH2:30]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...
Cl.O=C=Nc1ccccc1.SCCCN1CCN(CCc2ccccc2)CC1
Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)CC1
null
null
C(Cl)Cl
Acylation
OtherReaction
3bf647ffd3af34283e2312f784edbca620c93d73a88c64f1c90f0c5841a13287
c6ec1d581e09757064752f97a5c83429292625d25a23d379af2b6feb108d2455
C(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)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]
67.9
[{"value": 35.0, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.9, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
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-phenethylpiperazin-1-yl)propanethiol dihydrochloride, 2.4 g of triethylamine and 50 ml of methylene chloride, to give 1.9 g (35% of theory) of N-phenyl-S-[3-(4-phenethylpiperazin-1-yl)propyl]thiocarbamate dihydrochloride ...
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(CCc2ccccc2)CC1>C(Cl)Cl>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3718907b4bb04353b2d6e7ee3e40a47d
ClCCCBr.Clc1ccc(CCN2CCNCC2)cc1>>Cl.Cl.ClCCCN1CCN(CCc2ccc(Cl)cc2)CC1
ClC1=CC=C(CCN2CCNCC2)C=C1.[OH-].[K+].BrCCCCl>>Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCCl)C=C1
Br[CH2:6][CH2:5][CH2:4][Cl:1].[NH:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][c:13]2[cH:14][cH:15][c:16]([Cl:17])[cH:18][cH:19]2)[CH2:20][CH2:21]1>>[ClH:1].[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][c:13]2[cH:14][cH:15][c:16]([Cl:17])[cH:18][cH:19]2)[CH2:20][CH2:21]1
ClCCCBr.Clc1ccc(CCN2CCNCC2)cc1
Cl.Cl.ClCCCN1CCN(CCc2ccc(Cl)cc2)CC1
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CCN2CCNCC2)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]
118.3
[{"value": 59.0, "product": "Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCCl)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 118.3, "product": "Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCCl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 17(a) was followed, using 6.5 g of 1-(4-chlorophenethyl)piperazine, 6.0 g of potassium hydroxide, 125 ml of dimethyl sulfoxide and 4.6 g of 1-bromo-3-chloropropane. Work-up, as described above, gave 6.4 g (59% of theory) of 1-(4-chlorophenethyl)-4-(3-chloropropyl)piperazine dihydrochl...
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(CCN2CCNCC2)cc1>CS(=O)C>Cl.Cl.ClCCCN1CCN(CCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5c4b8b9e101c4986b417b515edcf6735
Cl.ClCCCN1CCN(CCc2ccc(Cl)cc2)CC1.NC(N)=S>>Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCCl)C=C1>>Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1
[ClH:2].Cl[CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][c:13]2[cH:14][cH:15][c:16]([Cl:17])[cH:18][cH:19]2)[CH2:20][CH2:21]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][CH2:12][c:13]2[cH:14][cH:15][c:16]([Cl:17])[cH:18][cH:19]2)[CH2:20][CH2:21]1
Cl.ClCCCN1CCN(CCc2ccc(Cl)cc2)CC1.NC(N)=S
Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CCN2CCNCC2)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]
176.1
[{"value": 89.0, "product": "Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 176.1, "product": "Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 1.3 g of thiourea, 6.4 g of 1-(4-chlorophenethyl)-4-(3-chloropropyl)piperazine dihydrochloride, 1.6 g of triethylamine and 150 ml of reagent ethanol. The hydrolysis was effected with 3.5 g of sodium hydroxide and 40 ml of water. Work-up, as described above, ga...
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(CCc2ccc(Cl)cc2)CC1.NC(N)=S>C(C)O.O>Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c3adcdd7c4ee4836a73f889b5c888b78
Cl.O=C=Nc1ccccc1.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccc(Cl)cc2)CC1
C1(=CC=CC=C1)N=C=O.Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl
[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][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][cH:10][cH:11][cH:12]1)=[SH:13][CH2:14][CH2:15][CH2:16...
Cl.O=C=Nc1ccccc1.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccc(Cl)cc2)CC1
null
null
C(Cl)Cl
Acylation
OtherReaction
3bf647ffd3af34283e2312f784edbca620c93d73a88c64f1c90f0c5841a13287
c6ec1d581e09757064752f97a5c83429292625d25a23d379af2b6feb108d2455
C(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)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]
87.4
[{"value": 44.0, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.4, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCC1=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 phenyl isocyanate, 5.0 g of 3-[4-(4-chlorophenethyl)piperazin-1-yl]propanethiol dihydrochloride, 1.3 g of triethylamine and 50 ml of methylene chloride, to give 3.0 g (44% of theory) of N-phenyl-S-{3-[4-(4-chlorophenethyl)piperazin-1-yl]propyl}thiocarbam...
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(CCc2ccc(Cl)cc2)CC1>C(Cl)Cl>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-92cc679236af4645bac266887faa5c2d
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>>CCCCc1ccc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc1.Cl
C(CCC)C1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.C(CCC)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCC1=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:31][cH:32]1.[ClH:34].[SH:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][CH2:18][N:19]([CH2:20][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][CH2:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([NH:9][C:10]([OH:11])=[...
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
CCCCc1ccc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)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]
49.7
[{"value": 25.0, "product": "Cl.Cl.C(CCC)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.7, "product": "Cl.Cl.C(CCC)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.4 g of 4-n-butylphenyl isocyanate, 3.0 g of 3-[4-(4-chlorophenethyl)piperazin-1-yl]propanethiol dihydrochloride, 0.8 g of triethylamine and 50 ml of methylene chloride, to give 1.1 g (25% of theory) of N-(4-n-butylphenyl)-S-{3-[4-(4-chlorophenethyl)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
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>C(Cl)Cl>CCCCc1ccc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-524f4e4c964d4f9a84b265af1db184ef
COc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>>COc1ccc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc1.Cl
COC1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCC1=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:29][cH:30]1.[ClH:32].[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2:16][N:17]([CH2:18][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][c:6]([NH:7][C:8]([OH:9])=[SH:10][CH2:11][CH2:12][CH2:13][N:14]...
COc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
COc1ccc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)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]
49.8
[{"value": 25.0, "product": "Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.8, "product": "Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.7 g of 4-methoxyphenyl isocyanate, 4.0 g of 3-[4-(4-chlorophenethyl)piperazin-1-yl]propanethiol dihydrochloride, 1.1 g of triethylamine and 50 ml of methylene chloride, to give 1.4 g (25% of theory) of N-(4-methoxyphenyl)-S-{3-[4-(4-chlorophenethyl)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
COc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>C(Cl)Cl>COc1ccc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a578f973ce364f93924ecc2ae775a857
COc1cc(N=C=O)cc(OC)c1OC.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>>COc1cc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc(OC)c1OC.Cl
COC=1C=C(C=C(C1OC)OC)N=C=O.Cl.Cl.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>Cl.Cl.COC=1C=C(C=C(C1OC)OC)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl
[CH3:1][O:2][c:3]1[cH:4][c:5]([N:6]=[C:7]=[O:8])[cH:28][c:29]([O:30][CH3:31])[c:32]1[O:33][CH3:34].[ClH:36].[SH:9][CH2:10][CH2:11][CH2:12][N:13]1[CH2:14][CH2:15][N:16]([CH2:17][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][c:5]([NH:6][C:7]([OH:8])=[SH:9][CH2:10][...
COc1cc(N=C=O)cc(OC)c1OC.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
COc1cc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc(OC)c1OC.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(CCc2ccccc2)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]
46.4
[{"value": 23.0, "product": "Cl.Cl.COC=1C=C(C=C(C1OC)OC)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 46.4, "product": "Cl.Cl.COC=1C=C(C=C(C1OC)OC)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 2.5 g of 3,4,5-trimethoxyphenyl isocyanate, 4.4 g of 3-[4-(4-chlorophenethyl)piperazin-1-yl]propanethiol dihydrochloride, 1.2 g of triethylamine and 50 ml of methylene chloride, to give 1.6 g (23% of theory) of N-(3,4,5-trimethoxyphenyl)-S-{3-[4-(4-chlorophenethy...
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
COc1cc(N=C=O)cc(OC)c1OC.Cl.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>C(Cl)Cl>COc1cc(NC(O)=[SH]CCCN2CCN(CCc3ccc(Cl)cc3)CC2)cc(OC)c1OC.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-249a67ffce174364b0ae5c54cd4ac01c
ClCCCBr.c1ccc(CCCN2CCNCC2)cc1>>Cl.Cl.ClCCCN1CCN(CCCc2ccccc2)CC1
C1(=CC=CC=C1)CCCN1CCNCC1.[OH-].[K+].BrCCCCl>>Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCCl
Br[CH2:6][CH2:5][CH2:4][Cl:1].[NH:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]1>>[ClH:1].[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]1
ClCCCBr.c1ccc(CCCN2CCNCC2)cc1
Cl.Cl.ClCCCN1CCN(CCCc2ccccc2)CC1
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CCCN2CCNCC2)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]
219.3
[{"value": 73.0, "product": "Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 219.3, "product": "Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 17(a) was followed, using 36.0 g of (3-phenylpropyl)piperazine, 25.0 g of potassium hydroxide, 125 ml of dimethyl sulfoxide and 28.0 g of 1-bromo-3-chloropropane, to give 46.0 g (73% of theory) of 1-(3-phenylpropyl)-4-(3-chloropropyl)piperazine dihydrochloride. Conditions: See reactio...
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.c1ccc(CCCN2CCNCC2)cc1>CS(=O)C>Cl.Cl.ClCCCN1CCN(CCCc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-63495ea5d1234e62baec2879feb6bdcc
Cl.ClCCCN1CCN(CCCc2ccccc2)CC1.NC(N)=S>>Cl.SCCCN1CCN(CCCc2ccccc2)CC1
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCCl>>Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCS
[ClH:2].Cl[CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]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][CH2:12][CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]1
Cl.ClCCCN1CCN(CCCc2ccccc2)CC1.NC(N)=S
Cl.SCCCN1CCN(CCCc2ccccc2)CC1
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CCCN2CCNCC2)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]
82
[{"value": 82.0, "product": "Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCS", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.9, "product": "Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCS", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 19.0 g of thiourea, 44.0 g of 1-(3-phenylpropyl)-4-(3-chloropropyl)piperazine dihydrochloride, 25 g of triethylamine and 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...
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(CCCc2ccccc2)CC1.NC(N)=S>C(C)O.O>Cl.SCCCN1CCN(CCCc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-abf8bcdd1c6d4d7c97ff0a1a653f9a5d
Cl.O=C=Nc1ccccc1.SCCCN1CCN(CCCc2ccccc2)CC1>>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCCc2ccccc2)CC1
C1(=CC=CC=C1)N=C=O.Cl.Cl.C1(=CC=CC=C1)CCCN1CCN(CC1)CCCS.C(C)N(CC)CC>>O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=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][CH2:22][CH2:23][c:24]2[cH:25][cH:26][cH: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][cH:10][cH:11][cH:12]1)=[SH:13][CH2:14][CH2:15][CH2:16...
Cl.O=C=Nc1ccccc1.SCCCN1CCN(CCCc2ccccc2)CC1
Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCCc2ccccc2)CC1
null
null
C(Cl)Cl
Acylation
OtherReaction
3bf647ffd3af34283e2312f784edbca620c93d73a88c64f1c90f0c5841a13287
c6ec1d581e09757064752f97a5c83429292625d25a23d379af2b6feb108d2455
C(Nc1ccccc1)=[SH]CCCN1CCN(CCCc2ccccc2)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]
85
[{"value": 41.0, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.0, "product": "O.Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 1.2 g of phenyl isocyanate, 4.0 g of 3-[4-(3-phenylpropyl)piperazin-1-yl]propanethiol dihydrochloride, 2.2 g of triethylamine and 50 ml of methylene chloride, to give 2.1 g (41% of theory) of N-phenyl-S-{3-[4-(3-phenylpropyl)piperazin-1-yl]propyl}thiocarbamate di...
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(CCCc2ccccc2)CC1>C(Cl)Cl>Cl.O.OC(Nc1ccccc1)=[SH]CCCN1CCN(CCCc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ad02dc0d397f4092b422fb887e5d9b33
ClCCCBr.Clc1ccc(CCCN2CCNCC2)cc1>>Cl.Cl.ClCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
ClC1=CC=C(C=C1)CCCN1CCNCC1.[OH-].[K+].BrCCCCl>>Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCCl
Br[CH2:6][CH2:5][CH2:4][Cl:1].[NH:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]2)[CH2:21][CH2:22]1>>[ClH:1].[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]2)[CH2:21][CH2:22]1
ClCCCBr.Clc1ccc(CCCN2CCNCC2)cc1
Cl.Cl.ClCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CCCN2CCNCC2)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]
104.9
[{"value": 54.0, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 104.9, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 17(a) was followed, using 27.0 g of 3-(4-chlorophenyl)propyl piperazine, 22.0 g of potassium hydroxide, 250 ml of dimethyl sulfoxide and 17.7 g of 1-bromo-3-chloropropane to give 22.9 g (54% of theory) of 1-[3-(4-chlorophenyl)propyl]-4-(3-chloropropyl)piperazine dihydrochloride. 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(CCCN2CCNCC2)cc1>CS(=O)C>Cl.Cl.ClCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-25a33070dbbc46b2856cae32c57e7fb1
Cl.Clc1ccc(CCCN2CCN(c3cccc(Cl)c3)CC2)cc1.NC(N)=S>>Cl.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)C1=CC(=CC=C1)Cl>>Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCS
[ClH:2].Clc1cc[cH:5][c:6]([N:7]2[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][c:14]3[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]3)[CH2:21][CH2:22]2)c1.N[C:4](N)=[S:3]>>[ClH:2].[SH:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][c:14]2[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]2)[CH2:21][CH2:22...
Cl.Clc1ccc(CCCN2CCN(c3cccc(Cl)c3)CC2)cc1.NC(N)=S
Cl.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
null
null
C(C)O.O
C-C Coupling
OtherReaction
69195008f3ff4f25000daeb30917666f63686186c48877497716d23c84933d13
41a61ea33577e1fce20b89f6335d2850b4b949c2950a98f7fc57fc76dcf35289
c1ccc(CCCN2CCNCC2)cc1
Cl-c1:c:c:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[#7:3](-[C:4])-[C:5]):c:1.N-[C;H0;D3;+0:6](-N)=[S;H0;D1;+0:7]>>[C:4]-[#7:3](-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[CH2;D2;+0:6]-[SH;D1;+0:7])-[C:5]
134.8
[{"value": 65.0, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCS", "details": "PERCENTYIELD", "is_desired": false}, {"value": 134.8, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCS", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 7.6 g of thiourea, 22.9 g of 1-[3-(4-chlorophenyl)propyl]-4-(3-chlorophenyl)piperazine dihydrochloride, 5.8 g of triethylamine and 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 a...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Thiourea
Aliphatic thiol
c1ccccc1
null
C1C[NH]CC[NH]1.c1ccccc1
HCl
C(C)O.O
null
null
Cl.Clc1ccc(CCCN2CCN(c3cccc(Cl)c3)CC2)cc1.NC(N)=S>C(C)O.O>Cl.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fb6342854daa4ef9895b1e9cbc8b15ba
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1>>CCCCc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.Cl
C(CCC)C1=CC=C(C=C1)N=C=O.Cl.Cl.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCS.C(C)N(CC)CC>>Cl.Cl.C(CCC)C1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=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:32][cH:33]1.[ClH:34].[SH:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][CH2:18][N:19]([CH2:20][CH2:21][CH2:22][c:23]2[cH:24][cH:25][c:26]([Cl:27])[cH:28][cH:29]2)[CH2:30][CH2:31]1>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([NH:9][C:10]([O...
CCCCc1ccc(N=C=O)cc1.Cl.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
CCCCc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(Nc1ccccc1)=[SH]CCCN1CCN(CCCc2ccccc2)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]
null
[]
null
null
null
null
The procedure described in Example 2 was followed, using 2.5 g of 4-n-butylphenyl isocyanate, 5.0 g of 3-{4-[3-(4-chlorophenyl)propyl]piperazin-1-yl}propanethiol dihydrochloride, 1.4 g of triethylamine and 50 ml of methylene chloride, to give 2.7 g (34% of theory) of N-(4-n-butylphenyl-S-{3-[4-[3-(4-chlorophenyl)propyl...
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(CCCc2ccc(Cl)cc2)CC1>C(Cl)Cl>CCCCc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-734f4d7e69b04aab8269e26db78ea339
ClCCCBr.Fc1ccc(CN2CCNCC2)cc1>>Cl.Cl.Fc1ccc(CN2CCN(CCCCl)CC2)cc1
FC1=CC=C(CN2CCNCC2)C=C1.[OH-].[K+].BrCCCCl>>Cl.Cl.FC1=CC=C(CN2CCN(CC2)CCCCl)C=C1
Br[CH2:13][CH2:14][CH2:15][Cl:1].[F:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][N:9]2[CH2:10][CH2:11][NH:12][CH2:17][CH2:18]2)[cH:19][cH:20]1>>[ClH:1].[ClH:2].[F:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][N:9]2[CH2:10][CH2:11][N:12]([CH2:13][CH2:14][CH2:15][Cl:16])[CH2:17][CH2:18]2)[cH:19][cH:20]1
ClCCCBr.Fc1ccc(CN2CCNCC2)cc1
Cl.Cl.Fc1ccc(CN2CCN(CCCCl)CC2)cc1
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
8bb1dcdfb1ee6ce852f7a1c342bcd4b443f45e43cf7019fdcba041cd9c6ac04f
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]
179.2
[{"value": 61.0, "product": "Cl.Cl.FC1=CC=C(CN2CCN(CC2)CCCCl)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 179.2, "product": "Cl.Cl.FC1=CC=C(CN2CCN(CC2)CCCCl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(a) was followed, using 32.8 g of 1-(4-fluorobenzyl)piperazine, 30.0 g of potassium hydroxide, 100 ml of dimethyl sulfoxide and 27.0 g of 1-bromo-3-chloropropane. Work-up, as described above, gave 35.2 g (61% of theory) of 1-(4-fluorobenzyl)-4-(3-chloropropyl) piperazine dihydrochlor...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Secondary amine
Primary halide.Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1
Br-
CS(=O)C
null
null
ClCCCBr.Fc1ccc(CN2CCNCC2)cc1>CS(=O)C>Cl.Cl.Fc1ccc(CN2CCN(CCCCl)CC2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fb0f4206c10d4323b2412cb842391736
ClCCl.ClCCl.Fc1ccc(N2CCN(CCCS)CC2)cc1.O=C=Nc1ccccc1>>Cl.Cl.OC(Nc1ccccc1)=[SH]CCCN1CCN(c2ccc(F)cc2)CC1
C(Cl)Cl.C1(=CC=CC=C1)N=C=O.FC1=CC=C(C=C1)N1CCN(CC1)CCCS.C(Cl)Cl>>Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)C1=CC=C(C=C1)F
ClC[Cl:1].ClC[Cl:2].[SH:12][CH2:13][CH2:14][CH2:15][N:16]1[CH2:17][CH2:18][N:19]([c:20]2[cH:21][cH:22][c:23]([F:24])[cH:25][cH:26]2)[CH2:27][CH2:28]1.[O:3]=[C:4]=[N:5][c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1>>[ClH: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]...
ClCCl.ClCCl.Fc1ccc(N2CCN(CCCS)CC2)cc1.O=C=Nc1ccccc1
Cl.Cl.OC(Nc1ccccc1)=[SH]CCCN1CCN(c2ccc(F)cc2)CC1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
019a2e24e0358337607bf7b4ba58c5c6f3d418e1be5864dd8ac3426507a76549
ed477d17b3772485f3bf707e50ec8b6650cdbbfeb5890403e4ee7fb6adb0740e
C(Nc1ccccc1)=[SH]CCCN1CCN(c2ccccc2)CC1
Cl-C-[Cl;H0;D1;+0:1].Cl-C-[Cl;H0;D1;+0:2].[C:3]-[C:4]-[SH;D1;+0:5].[O;H0;D1;+0:6]=[C;H0;D2;+0:7]=[N;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[C:3]-[C:4]-[SH;D2;+0:5]=[C;H0;D3;+0:7](-[OH;D1;+0:6])-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11].[ClH;D0;+0:1].[ClH;D0;+0:2]
33
[{"value": 33.0, "product": "Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCCN1CCN(CC1)C1=CC=C(C=C1)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
1.2 g of phenyl isocyanate was added to a solution of 2.5 g of 3-[4-(4-fluorophenyl)piperazin-1-yl]propanethiol in 75 ml of methylene chloride, and the mixture was refluxed for four hours. After the further addition of 100 ml of methylene chloride the solution was washed with water, dried (sodium sulfate) and concentra...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Primary halide.Primary halide.Isocyanate.Aliphatic thiol
Secondary amine
null
null
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
Other
null
null
null
ClCCl.ClCCl.Fc1ccc(N2CCN(CCCS)CC2)cc1.O=C=Nc1ccccc1>>Cl.Cl.OC(Nc1ccccc1)=[SH]CCCN1CCN(c2ccc(F)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b5880115943c4665b571bee98c011ee9
ClCCBr.Clc1ccc(CN2CCNCC2)cc1>>Cl.Cl.ClCCN1CCN(Cc2ccc(Cl)cc2)CC1
ClC1=CC=C(CN2CCNCC2)C=C1.BrCCCl>>Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCl)C=C1
Br[CH2:5][CH2:4][Cl:1].[NH:6]1[CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1>>[ClH:1].[ClH:2].[Cl:3][CH2:4][CH2:5][N:6]1[CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1
ClCCBr.Clc1ccc(CN2CCNCC2)cc1
Cl.Cl.ClCCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
O1CCCC1
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CN2CCNCC2)cc1
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[Cl;H0;D1;+0:3].[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[Cl;D1;H0:10]-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1.[ClH;D0;+0:3]
112
[{"value": 56.0, "product": "Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCl)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 112.0, "product": "Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 15.0 g of 1-(4-chlorobenzyl)piperazine, 14.4 g of 1-bromo-2-chloroethane and 150 ml of tetrahydrofuran was refluxed for 8 hours. The solvent was removed in vacuo, and 2N sodium hydroxide was added to the residue. The product was extracted with methylene chloride, and the extract was dried (sodium sulfate) ...
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-
O1CCCC1
null
null
ClCCBr.Clc1ccc(CN2CCNCC2)cc1>O1CCCC1>Cl.Cl.ClCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a44d77395f1c48f3a29b906d95127ca1
Cl.ClCCN1CCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S>>Cl.SCCN1CCN(Cc2ccc(Cl)cc2)CC1
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCl)C=C1>>Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCS)C=C1
[ClH:2].Cl[CH2:4][CH2:5][N:6]1[CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1.NC(N)=[S:3]>>[ClH:2].[SH:3][CH2:4][CH2:5][N:6]1[CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1
Cl.ClCCN1CCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S
Cl.SCCN1CCN(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]-[#7:3].N-C(-N)=[S;H0;D1;+0:4]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[SH;D1;+0:4]
97.8
[{"value": 62.0, "product": "Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCS)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.8, "product": "Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCS)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 6.1 g of thiourea, 13.8 g of 1-(4-chlorobenzyl)-4-(2-chloroethyl)piperazine dihydrochloride, 4.1 g of triethylamine and 150 ml of reagent ethanol. The hydrolysis was effected with 7.0 g of sodium hydroxide and 50 ml of water. Work-up, as described above, gave ...
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.ClCCN1CCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S>C(C)O.O>Cl.SCCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fcef17e19b204f38a565811b3b58d7ad
O=C=Nc1ccccc1.SCCN1CCN(Cc2ccc(Cl)cc2)CC1>>Cl.Cl.OC(Nc1ccccc1)=[SH]CCN1CCN(Cc2ccc(Cl)cc2)CC1
C1(=CC=CC=C1)N=C=O.ClC1=CC=C(CN2CCN(CC2)CCS)C=C1>>Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[O:3]=[C:4]=[N:5][c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1.[Cl:1][c:23]1[cH:22][cH:21][c:20]([CH2:19][N:18]2[CH2:17][CH2:16][N:15]([CH2:14][CH2:13][SH:12])[CH2:28][CH2:27]2)[cH:26][cH:25]1>>[ClH: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][N:15]1[CH2:16][CH2:17][N:18]([CH2...
O=C=Nc1ccccc1.SCCN1CCN(Cc2ccc(Cl)cc2)CC1
Cl.Cl.OC(Nc1ccccc1)=[SH]CCN1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
9ddf29a0add694314a86de0a39264129a9713962546a4ec140d50667e08753fd
126df213390631efc30fe64ae8364e595ba3d5d450128f642d2c5ebbd6a2ca21
C(Nc1ccccc1)=[SH]CCN1CCN(Cc2ccccc2)CC1
[C:1]-[C:2]-[SH;D1;+0:3].[Cl;H0;D1;+0:4]-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9].[O;H0;D1;+0:10]=[C;H0;D2;+0:11]=[N;H0;D2;+0:12]-[c:13](:[c:14]):[c:15]>>[C:1]-[C:2]-[SH;D2;+0:3]=[C;H0;D3;+0:11](-[OH;D1;+0:10])-[NH;D2;+0:12]-[c:13](:[c:14]):[c:15].[Cl;D1;H0:16]-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9].[ClH;D0;+0:4]
128.2
[{"value": 43.0, "product": "Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 128.2, "product": "Cl.Cl.C1(=CC=CC=C1)NC(O)=SCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 35 was followed, using 1.3 g of phenyl isocyanate, 3.0 g of 2-[4-(4-chlorobenzyl)piperazin-1-yl]ethanethiol and 100 ml of methylene chloride, to give 2.2 g (43% of theory) of N-phenyl-S-{2-[4-(4-chlorobenzyl)piperazin-1-yl]ethyl}thiocarbamate dihydrochloride as a white crystalline sol...
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
null
O=C=Nc1ccccc1.SCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>Cl.Cl.OC(Nc1ccccc1)=[SH]CCN1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a34cebc025d14918a8b53e7fb7577a4a
O=C=NC1CCCCC1.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>>Cl.Cl.OC(NC1CCCCC1)=[SH]CCCN1CCN(CCc2ccc(Cl)cc2)CC1
C1(CCCCC1)N=C=O.ClC1=CC=C(CCN2CCN(CC2)CCCS)C=C1>>Cl.Cl.C1(CCCCC1)NC(O)=SCCCN1CCN(CC1)CCC1=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:25]1[cH:24][cH:23][c:22]([CH2:21][CH2:20][N:19]2[CH2:18][CH2:17][N:16]([CH2:15][CH2:14][CH2:13][SH:12])[CH2:30][CH2:29]2)[cH:28][cH:27]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][CH2:1...
O=C=NC1CCCCC1.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1
Cl.Cl.OC(NC1CCCCC1)=[SH]CCCN1CCN(CCc2ccc(Cl)cc2)CC1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
9ddf29a0add694314a86de0a39264129a9713962546a4ec140d50667e08753fd
126df213390631efc30fe64ae8364e595ba3d5d450128f642d2c5ebbd6a2ca21
C(NC1CCCCC1)=[SH]CCCN1CCN(CCc2ccccc2)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]
170.7
[{"value": 58.0, "product": "Cl.Cl.C1(CCCCC1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 170.7, "product": "Cl.Cl.C1(CCCCC1)NC(O)=SCCCN1CCN(CC1)CCC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 35 was followed, using 1.7 g of cyclohexyl isocyanate, 4.0 g of 3-[4-(4-chlorophenethyl)piperazin-1-yl]propanethiol and 100 ml of methylene chloride, to give 3.8 g (58% of theory) of N-cyclohexyl-S-{3-[4-(4-chlorophenethyl)piperazin-1-yl]propyl}thiocarbamate dihydrochloride as a white...
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
null
O=C=NC1CCCCC1.SCCCN1CCN(CCc2ccc(Cl)cc2)CC1>C(Cl)Cl>Cl.Cl.OC(NC1CCCCC1)=[SH]CCCN1CCN(CCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0346a80a37094debaa473c96709fc5a5
COc1ccc(N=C=O)cc1.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1>>COc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.COc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.Cl.Cl.Cl.Cl.O
COC1=CC=C(C=C1)N=C=O.ClC1=CC=C(C=C1)CCCN1CCN(CC1)CCCS>>O.Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=CC=C(C=C1)Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=CC=C(C=C1)Cl.Cl.Cl
[CH3:1][O:2][c:3]1[cH:31][cH:4][c:6]([N:7]=[C:8]=[O:9])[cH:57][cH:58]1.[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2:47][N:48]([CH2:49][CH2:50][CH2:51][c:52]2[cH:27][cH:26][c:24]([Cl:25])[cH:23][cH:53]2)[CH2:59][CH2:60]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]...
COc1ccc(N=C=O)cc1.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1
COc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.COc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.Cl.Cl.Cl.Cl.O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
269f1633e2ea877d9658f087c771fdd064531e4fcb63915701a286aa807c71eb
4615a94198e052f6fbe6c3d4f017aa5c788848cac6fab2700239215f52926247
C(Nc1ccccc1)=[SH]CCCN1CCN(CCCc2ccccc2)CC1.C(Nc1ccccc1)=[SH]CCCN1CCN(CCCc2ccccc2)CC1
[C;D1;H3:1]-[#8:2]-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[N;H0;D2;+0:7]=[C;H0;D2;+0:8]=[O;H0;D1;+0:9]):[cH;D2;+0:10]:[cH;D2;+0:11]:1.[Cl;D1;H0:12]-[c:13]1:[c:14]:[cH;D2;+0:15]:[c;H0;D3;+0:16](-[C:17]-[C:18]-[C:19]-[#7:20]2-[C:21]-[CH2;D2;+0:22]-[N;H0;D3;+0:23](-[C:24]-[C:25]-[C:26]-[SH;D1;+0:27])-[C...
146.1
[{"value": 48.0, "product": "O.Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=CC=C(C=C1)Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=CC=C(C=C1)Cl.Cl.Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 146.1, "product": "O.Cl.Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1CCN(CC1)CCCC1=CC=C(C=C1)Cl.COC1=CC=C(C=C1)NC(O)=SCCCN1...
null
null
null
null
The procedure described in Example 35 was followed, using 2.0 g of 4-methoxyphenyl isocyanate, 4.0 g of 3-{4-[3-(4-chlorophenyl)propyl]piperazin-1-yl}propanethiol and 100 ml of methylene chlorine to give 3.4 g (48% of theory) of N-(4-methoxyphenyl)-S-{3-[4-[3-(4-chlorophenyl)propyl]piperazin-1-yl]propyl}thiocarbamate d...
10.6084/m9.figshare.5104873.v1
null
Ether.Isocyanate.Tertiary amine.Aliphatic thiol
Aromatic halide.Ether.Ether.Secondary amine.Secondary amine.Tertiary amine.Tertiary amine.Tertiary amine
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.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
null
null
null
COc1ccc(N=C=O)cc1.SCCCN1CCN(CCCc2ccc(Cl)cc2)CC1>>COc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.COc1ccc(NC(O)=[SH]CCCN2CCN(CCCc3ccc(Cl)cc3)CC2)cc1.Cl.Cl.Cl.Cl.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b3cce434c6ef4afc85c9dbb95a837744
CCCCCCN=C=O.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>CCCCCCNC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl
C(CCCCC)N=C=O.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1>>Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][N:7]=[C:8]=[O:9].[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][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][NH:7][C:8]([OH:9])=[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2:16][N:1...
CCCCCCN=C=O.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
CCCCCCNC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
c1ccc(CN2CCNCC2)cc1
[C:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;H0;D1;+0:5].[C:6]-[C:7]-[SH;D1;+0:8]>>[C:6]-[C:7]-[SH;D2;+0:8]=[C;H0;D3;+0:4](-[OH;D1;+0:5])-[NH;D2;+0:3]-[C:2]-[C:1]
157.9
[{"value": 51.0, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 157.9, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 35 was followed, using 1.4 g of n-hexyl isocyanate, 3.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol and 100 ml of methylene chloride, to give 2.7 g (51% of theory) of N-(n-hexyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]propyl}thiocarbamate dihydrochloride as a white crystalli...
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
CCCCCCN=C=O.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CCCCCCNC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3a99d50f95d64431bf061d9f3353a09f
ClCCCBr.Clc1ccc(CCCCN2CCNCC2)cc1>>Cl.Cl.ClCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1
ClC1=CC=C(C=C1)CCCCN1CCNCC1.BrCCCCl.[OH-].[K+]>>Cl.Cl.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCCl
Br[CH2:6][CH2:5][CH2:4][Cl:1].[NH:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][CH2:14][c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][cH:21]2)[CH2:22][CH2:23]1>>[ClH:1].[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][CH2:14][c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][cH:21]2)[CH2:...
ClCCCBr.Clc1ccc(CCCCN2CCNCC2)cc1
Cl.Cl.ClCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1
null
null
CS(=O)C
Functional Group Interconversion
N-alkylation of secondary amines with alkyl halides
0403b0fd8876264587fe8aac393e426a627a9dbc8cbe88cf6818c920cd0399bd
a4ff305a4a016f4677b6596bbb229eed668b787eedc9bb50407db4321ec4925c
c1ccc(CCCCN2CCNCC2)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]
125.7
[{"value": 82.0, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 125.7, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(a) was followed, using 10.0 g of 4-(4-chlorophenyl)butyl piperazine, 47.2 g of 1-bromo-3-chloropropane, 150 ml of dimethyl sulfoxide and 11.2 g of potassium hydroxide, to give 10.0 g (82% of theory) of 1-[4-(4-chlorophenyl)butyl]-4-(3-chloropropyl)piperazine dihydrochloride as a whi...
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(CCCCN2CCNCC2)cc1>CS(=O)C>Cl.Cl.ClCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bf5cd469793a4ce49e0abb6aa996f1d7
Cl.ClCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1.NC(N)=S>>Cl.SCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1
C(C)O.NC(=S)N.Cl.Cl.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCCl.[OH-].[Na+]>>Cl.Cl.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCS
[ClH:2].Cl[CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][CH2:14][c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][cH:21]2)[CH2:22][CH2:23]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][CH2:12][CH2:13][CH2:14][c:15]2[cH:16][cH:17][c:18]([Cl:19])[cH:20][cH:21]2)[...
Cl.ClCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1.NC(N)=S
Cl.SCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CCCCN2CCNCC2)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]
30.2
[{"value": 16.0, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCS", "details": "PERCENTYIELD", "is_desired": false}, {"value": 30.2, "product": "Cl.Cl.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCS", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 1.0 g of thiourea, 4.0 g of 1-[4-(4-chlorophenyl)butyl]-4-(3-chloropropyl)piperazine dihydrochloride and 50 ml of reagent ethanol. The hydrolysis was effected with 4.0 g of sodium hydroxide in 50 ml of water. Work-up of the free base, as described above follow...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
C1C[NH]CC[NH]1.c1ccccc1
HCl
O
null
null
Cl.ClCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1.NC(N)=S>O>Cl.SCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-79c508329b5d4f1d8bd9e814f1079ea1
CCCCCCN=C=O.SCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1>>CCCCCCNC(O)=[SH]CCCN1CCN(CCCCc2ccc(Cl)cc2)CC1.Cl.Cl
C(CCCCC)N=C=O.ClC1=CC=C(C=C1)CCCCN1CCN(CC1)CCCS>>Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CCCCC1=CC=C(C=C1)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][N:7]=[C:8]=[O:9].[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2:16][N:17]([CH2:18][CH2:19][CH2:20][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][CH2:3][CH2:4][CH2:5][CH2:6][NH:7][C:8]([OH:9])=[SH:10][CH2:11][CH2:12][CH2:13][N:...
CCCCCCN=C=O.SCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1
CCCCCCNC(O)=[SH]CCCN1CCN(CCCCc2ccc(Cl)cc2)CC1.Cl.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
c1ccc(CCCCN2CCNCC2)cc1
[C:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;H0;D1;+0:5].[C:6]-[C:7]-[SH;D1;+0:8]>>[C:6]-[C:7]-[SH;D2;+0:8]=[C;H0;D3;+0:4](-[OH;D1;+0:5])-[NH;D2;+0:3]-[C:2]-[C:1]
99.8
[{"value": 32.0, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CCCCC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.8, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CCCCC1=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 n-hexyl isocyanate, 2.6 g of 3-{4-[4-(4-chlorophenyl)butyl]piperazin-1-yl}propanethiol and 25 ml of methylene chloride, to give 1.4 g (32% of theory) of N-(n-hexyl)-S-{3-[4-[4-(4-chlorophenyl)butyl]piperazin-1-yl]propyl}thiocarbamate dihydrochloride as a...
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
CCCCCCN=C=O.SCCCN1CCN(CCCCc2ccc(Cl)cc2)CC1>C(Cl)Cl>CCCCCCNC(O)=[SH]CCCN1CCN(CCCCc2ccc(Cl)cc2)CC1.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d30d8a19d77a43a283a0480973ee3168
BrCC=Cc1ccccc1.Cl.ClCCCN1CCNCC1>>Cl.ClCCCN1CCN(CC=Cc2ccccc2)CC1
C(C=CC1=CC=CC=C1)Br.O.Cl.Cl.ClCCCN1CCNCC1.ClCCCN1CCNCC1.Cl.Cl.C(C)N(CC)CC>>Cl.Cl.C(C=CC1=CC=CC=C1)N1CCN(CC1)CCCCl
Br[CH2:11][CH:12]=[CH:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][NH:10][CH2:20][CH2:21]1>>[ClH:2].[Cl:3][CH2:4][CH2:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH2:11][CH:12]=[CH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]1
BrCC=Cc1ccccc1.Cl.ClCCCN1CCNCC1
Cl.ClCCCN1CCN(CC=Cc2ccccc2)CC1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
b703623ddc3b029d4716c15f5414f41773434bcc7e3f3853faf62273596bed77
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
C(=Cc1ccccc1)CN1CCNCC1
Br-[CH2;D2;+0:1]-[C:2]=[C:3]-[c:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[c:4]-[C:3]=[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1
278.1
[{"value": 70.0, "product": "Cl.Cl.C(C=CC1=CC=CC=C1)N1CCN(CC1)CCCCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 278.1, "product": "Cl.Cl.C(C=CC1=CC=CC=C1)N1CCN(CC1)CCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
6.0 g of cinnamyl bromide were added to a mixture of 7.4 g of 1-(3-chloropropyl)piperazine dihydrochloride hemihydrate, 6.1 g of triethylamine and 100 ml of reagent ethanol. The mixture was refluxed for 4 hours and then stirred overnight. After removal of the solvent in vacuo, water was added to the residue. The produc...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccccc1
HBr
C(C)O
null
8
BrCC=Cc1ccccc1.Cl.ClCCCN1CCNCC1>C(C)O>Cl.ClCCCN1CCN(CC=Cc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c7de0e9fa1d24e82a534bc829b4771d1
Cl.ClCCCN1CCN(CC=Cc2ccccc2)CC1.NC(N)=S>>Cl.SCCCN1CCN(CC=Cc2ccccc2)CC1
NC(=S)N.[OH-].[Na+].C(C)N(CC)CC.Cl.Cl.C(C=CC1=CC=CC=C1)N1CCN(CC1)CCCCl>>Cl.Cl.C(C=CC1=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][CH:12]=[CH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]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][CH:12]=[CH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[CH2:20][CH2:21]1
Cl.ClCCCN1CCN(CC=Cc2ccccc2)CC1.NC(N)=S
Cl.SCCCN1CCN(CC=Cc2ccccc2)CC1
null
null
C(C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
C(=Cc1ccccc1)CN1CCNCC1
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]
52
[{"value": 52.0, "product": "Cl.Cl.C(C=CC1=CC=CC=C1)N1CCN(CC1)CCCS", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.0, "product": "Cl.Cl.C(C=CC1=CC=CC=C1)N1CCN(CC1)CCCS", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 1(b) was followed, using 3.1 g of thiourea, 7.4 g of 1-cinnamyl-4-(3-chloropropyl)piperazine dihydrochloride, 4,1 g of triethylamine and 100 ml of reagent ethanol. The hydrolysis was effected with 3.0 g of sodium hydroxide in 30 ml of water. Work-up, as described above, gave 3.6 g (52...
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(CC=Cc2ccccc2)CC1.NC(N)=S>C(C)O.O>Cl.SCCCN1CCN(CC=Cc2ccccc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ed77c6d5e9bf4296bf37b6996aa0f6d8
CCCCCCN=C=O.Cl.SCCCN1CCN(CC=Cc2ccccc2)CC1>>CCCCCCNC(O)=[SH]CCCN1CCN(CC=Cc2ccccc2)CC1.Cl
C(CCCCC)N=C=O.Cl.Cl.C(C=CC1=CC=CC=C1)N1CCN(CC1)CCCS.C(C)N(CC)CC>>Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CC=CC1=CC=CC=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][N:7]=[C:8]=[O:9].[ClH:30].[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2:16][N:17]([CH2:18][CH:19]=[CH:20][c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[CH2:27][CH2:28]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][NH:7][C:8]([OH:9])=[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2...
CCCCCCN=C=O.Cl.SCCCN1CCN(CC=Cc2ccccc2)CC1
CCCCCCNC(O)=[SH]CCCN1CCN(CC=Cc2ccccc2)CC1.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
C(=Cc1ccccc1)CN1CCNCC1
[C:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;H0;D1;+0:5].[C:6]-[C:7]-[SH;D1;+0:8]>>[C:6]-[C:7]-[SH;D2;+0:8]=[C;H0;D3;+0:4](-[OH;D1;+0:5])-[NH;D2;+0:3]-[C:2]-[C:1]
64.2
[{"value": 31.0, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CC=CC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.2, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CC1)CC=CC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure described in Example 2 was followed, using 0.4 g of n-hexyl isocyanate, 1.0 g of 3-(4-cinnamylpiperazin-1-yl)propanethiol dihydrochloride, 0.6 g of triethylamine and 50 ml of methylene chloride, to give 0.44 g (31% of theory) of N-(n-hexyl)-S-[3-(4-cinnamylpiperazin-1-yl)propyl]thiocarbamate dihydrochlori...
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
CCCCCCN=C=O.Cl.SCCCN1CCN(CC=Cc2ccccc2)CC1>C(Cl)Cl>CCCCCCNC(O)=[SH]CCCN1CCN(CC=Cc2ccccc2)CC1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0956ad0caa5041f28456e5e148238e1e
ClCCCBr.Clc1ccc(CN2CCCNCC2)cc1>>ClCCCN1CCCN(Cc2ccc(Cl)cc2)CC1
BrCCCCl.ClC1=CC=C(CN2CCNCCC2)C=C1.[OH-].[K+]>>ClC1=CC=C(CN2CCN(CCC2)CCCCl)C=C1
Br[CH2:4][CH2:3][CH2:2][Cl:1].[NH:5]1[CH2:6][CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1>>[Cl:1][CH2:2][CH2:3][CH2:4][N:5]1[CH2:6][CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1
ClCCCBr.Clc1ccc(CN2CCCNCC2)cc1
ClCCCN1CCCN(Cc2ccc(Cl)cc2)CC1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
a53bdae9df4a04e07ad93d60984a5afd70715f5d49f2f60eb64dc34064ff0da2
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CN2CCCNCC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#7:4]-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[#7:4]-[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:8]-[C:9]
42
[{"value": 42.0, "product": "ClC1=CC=C(CN2CCN(CCC2)CCCCl)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 41.8, "product": "ClC1=CC=C(CN2CCN(CCC2)CCCCl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
15.7 g of 1-bromo-3-chloropropane were added to a cooled solution of 15.0 g of 1-(4-chlorobenzyl)homopiperazine and 12.0 g of potassium hydroxide in 50 ml of dimethyl sulfoxide. The mixture was stirred at 5°-10° C. for one hour, and then an additional 30 minutes at room temperature. After the addition of ice water, the...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CNCC[NH]C1
C1C[NH]CC[NH]C1
C1C[NH]CC[NH]C1.c1ccccc1
HBr
CS(=O)C
null
1
ClCCCBr.Clc1ccc(CN2CCCNCC2)cc1>CS(=O)C>ClCCCN1CCCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-73e545c91cc447a8af0c692a3811aa45
ClCCCN1CCCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S>>SCCCN1CCCN(Cc2ccc(Cl)cc2)CC1
[OH-].[Na+].NC(=S)N.ClC1=CC=C(CN2CCN(CCC2)CCCCl)C=C1.C(C)O>>ClC1=CC=C(CN2CCN(CCC2)CCCS)C=C1
Cl[CH2:2][CH2:3][CH2:4][N:5]1[CH2:6][CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1.NC(N)=[S:1]>>[SH:1][CH2:2][CH2:3][CH2:4][N:5]1[CH2:6][CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]([Cl:15])[cH:16][cH:17]2)[CH2:18][CH2:19]1
ClCCCN1CCCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S
SCCCN1CCCN(Cc2ccc(Cl)cc2)CC1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccc(CN2CCCNCC2)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]
39.1
[{"value": 39.0, "product": "ClC1=CC=C(CN2CCN(CCC2)CCCS)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 39.1, "product": "ClC1=CC=C(CN2CCN(CCC2)CCCS)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
4.1 g of thiourea were added to a mixture of 8.0 g of 1-(4-chlorobenzyl)-4-(3-chloropropyl)homopiperazine and 100 ml of reagent ethanol. The mixture was refluxed for 6 hours and then stirred overnight at room temperature. A solution of 5.0 g of sodium hydroxide in 30 ml of water was added, and the resulting solution wa...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
C1C[NH]CC[NH]C1.c1ccccc1
HCl
O
null
8
ClCCCN1CCCN(Cc2ccc(Cl)cc2)CC1.NC(N)=S>O>SCCCN1CCCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-111c8594f1d44a3f8495a7a4086c6573
CCCCCCN=C=O.SCCCN1CCCN(Cc2ccc(Cl)cc2)CC1>>CCCCCCNC(O)=[SH]CCCN1CCCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl
C(CCCCC)N=C=O.ClC1=CC=C(CN2CCN(CCC2)CCCS)C=C1>>Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CCC1)CC1=CC=C(C=C1)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][N:7]=[C:8]=[O:9].[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][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][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][NH:7][C:8]([OH:9])=[SH:10][CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2...
CCCCCCN=C=O.SCCCN1CCCN(Cc2ccc(Cl)cc2)CC1
CCCCCCNC(O)=[SH]CCCN1CCCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
d231144fa8916ec255ee403916a9da3c3f1c5088a3508df700953f4bb7ee4232
975aa459e325ce46eb7c0448bba281ba869acd2dcf1407dbdcac2da9a164e0c9
c1ccc(CN2CCCNCC2)cc1
[C:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;H0;D1;+0:5].[C:6]-[C:7]-[SH;D1;+0:8]>>[C:6]-[C:7]-[SH;D2;+0:8]=[C;H0;D3;+0:4](-[OH;D1;+0:5])-[NH;D2;+0:3]-[C:2]-[C:1]
77.6
[{"value": 33.0, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CCC1)CC1=CC=C(C=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.6, "product": "Cl.Cl.C(CCCCC)NC(O)=SCCCN1CCN(CCC1)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 n-hexyl isocyanate, 3.0 g of 3-[4-(4-chlorobenzyl)homopiperazin-1-yl]propanethiol and 75 ml of methylene chloride, to give 1.3 g (33% of theory) of N-(n-hexyl)-S-{3-[4-(4-chlorobenzyl)homopiperazin-1-yl]propyl}thiocarbamate dihydrochloride as a tan powde...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Aliphatic thiol
Secondary amine
null
null
C1C[NH]CC[NH]C1.c1ccccc1
null
C(Cl)Cl
null
null
CCCCCCN=C=O.SCCCN1CCCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CCCCCCNC(O)=[SH]CCCN1CCCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5a4a048975d74124980c61747a711e76
CC(C)(C)N=C=O.CCN(CC)CC.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>>CC(C)(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.CC(C)(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl.Cl.O.O.O
C(C)(C)(C)N=C=O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)CCCS)C=C1.C(C)N(CC)CC>>O.Cl.Cl.C(C)(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl.O.O.C(C)(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl.Cl.Cl
[CH3:1][C:2]([CH3:3])([N:5]=[C:6]=[O:7])[CH3:44].[CH3:4][CH2:36][N:15]([CH2:16][CH3:17])[CH2:34][CH3:35].[ClH:46].[SH:8][CH2:9][CH2:10][CH2:11][N:12]1[CH2:13][CH2:39][N:40]([CH2:41][c:42]2[cH:18][cH:19][c:20]([Cl:21])[cH:47][cH:48]2)[CH2:24][CH2:25]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[NH:5][C:6]([OH:7])=[SH:8][CH2:9][CH2:...
CC(C)(C)N=C=O.CCN(CC)CC.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1
CC(C)(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.CC(C)(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl.Cl.O.O.O
null
null
C(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
170d291efa68874c42c5544601aab6c0edfcfd06ec7e7a4139e7efdccfe2cde2
4d3b6a868bf49165ce96d9965938fb5717fddaeab7e13b62dac1602bc9e82d12
c1ccc(CN2CCNCC2)cc1.c1ccc(CN2CCNCC2)cc1
[C;D1;H3:1]-[C;H0;D4;+0:2](-[C;D1;H3:3])(-[CH3;D1;+0:4])-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[O;H0;D1;+0:7].[CH3;D1;+0:8]-[C:9]-[N;H0;D3;+0:10](-[CH2;D2;+0:11]-[CH3;D1;+0:12])-[CH2;D2;+0:13]-[CH3;D1;+0:14].[Cl;D1;H0:15]-[c;H0;D3;+0:16]1:[c:17]:[cH;D2;+0:18]:[c;H0;D3;+0:19](-[C:20]-[N;H0;D3;+0:21]2-[CH2;D2;+0:22]-[C:23]-[#7:2...
140.2
[{"value": 60.0, "product": "O.Cl.Cl.C(C)(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl.O.O.C(C)(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl.Cl.Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 140.2, "product": "O.Cl.Cl.C(C)(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl.O.O.C(C)(C)(C)NC(O)=SCCCN1CCN(CC1)CC1=CC=C(C...
null
null
null
null
The procedure described in Example 2 was followed, using 0.8 g of t-butyl isocyanate, 3.0 g of 3-[4-(4-chlorobenzyl)piperazin-1-yl]propanethiol dihydrochloride, 1.6 g of triethylamine and 75 ml of methylene chloride, to give 2.2 g (60% of theory) of N-(t-butyl)-S-{3-[4-(4-chlorobenzyl)piperazin-1-yl]propyl}thiocarbamat...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Isocyanate.Tertiary amine.Tertiary amine.Aliphatic thiol
Aromatic halide.Aromatic halide.Secondary amine.Secondary amine.Tertiary amine.Tertiary amine.Tertiary amine
C1C[NH]CC[NH]1.c1ccccc1
C1C[NH]CC[NH]1.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
C1C[NH]CC[NH]1.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(Cl)Cl
null
null
CC(C)(C)N=C=O.CCN(CC)CC.Cl.SCCCN1CCN(Cc2ccc(Cl)cc2)CC1>C(Cl)Cl>CC(C)(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.CC(C)(C)NC(O)=[SH]CCCN1CCN(Cc2ccc(Cl)cc2)CC1.Cl.Cl.Cl.O.O.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e5f252377ae24090a434bf5416e54651
COc1cc(SC)ccc1C(=O)O.Nc1cn[nH]c(=O)c1N>>COc1cc(SC)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
COC1=C(C(=O)O)C=CC(=C1)SC.NC=1C(NN=CC1N)=O>>COC1=C(C=CC(=C1)SC)C=1N=C2C(=CNNC2=O)N1
O=[C:11](O)[c:10]1[c:3]([O:2][CH3:1])[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9]1.[NH2:12][c:13]1[cH:14][n:15][nH:16][c:17](=[O:18])[c:19]1[NH2:20]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9][c:10]1-[c:11]1[n:12][c:13]2[cH:14][nH:15][nH:16][c:17](=[O:18])[c:19]-2[n:20]1
COc1cc(SC)ccc1C(=O)O.Nc1cn[nH]c(=O)c1N
COc1cc(SC)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
96109e218d24fb14479892243bf7b2a5f05e386416ab27902ec0f9172e3e4a04
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
O=c1[nH][nH]cc2nc(-c3ccccc3)nc1-2
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5](-[#8:6]):[c:7].[NH2;D1;+0:8]-[c;H0;D3;+0:9]1:[c:10]:[n;H0;D2;+0:11]:[#7;a:12]:[c:13](=[O;D1;H0:14]):[c;H0;D3;+0:15]:1-[NH2;D1;+0:16]>>[#8:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:8]:[c;H0;D3;+0:9]2:[c:10]:[nH;D2;+0:11]:[#7;a:12]:[c:13](=[O;D1;H...
null
[]
50
CELSIUS
null
null
Two grams of 2-methoxy-4-methylmercapto-benzoic acid are suspended in 20 ml of polyphosphoric acid, and 1.2 gm of 4,5-diamino-2H-pyridazin-3-one are added thereto with stirring at 50° C. The mixture is heated for 90 minutes to 100°-110° C. and then poured onto ice water, and the product which is precipitated on stirrin...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1ccnnc1
c1nc2cnncc2[nH]1
c1ccccc1.c1nc2cnncc2[nH]1
HO-
null
50
null
COc1cc(SC)ccc1C(=O)O.Nc1cn[nH]c(=O)c1N>>COc1cc(SC)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-11a5b9119d9941618a2c6738f74ed215
COc1cc(SC)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.OO>>COc1cc(S(C)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
COC1=C(C=CC(=C1)SC)C=1N=C2C(=CNNC2=O)N1.OO>>COC1=C(C=CC(=C1)S(=O)C)C=1N=C2C(=CNNC2=O)N1
[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6][CH3:7])[cH:9][cH:10][c:11]1-[c:12]1[n:13][c:14]2[cH:15][nH:16][nH:17][c:18](=[O:19])[c:20]-2[n:21]1.O[OH:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6]([CH3:7])=[O:8])[cH:9][cH:10][c:11]1-[c:12]1[n:13][c:14]2[cH:15][nH:16][nH:17][c:18](=[O:19])[c:20]-2[n:21]1
COc1cc(SC)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.OO
COc1cc(S(C)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
null
null
C(C)(=O)O
Oxidation
Sulfanyl to sulfinyl_H2O2
3f94fa67dce0f9d1622f25c2f6b679e0a2528e6d5c5559b15aed37456745a4b5
099322fb111e24ec324e6fad75d493a762ca0cd5af0df8c6f3bfd25c910b45a8
O=c1[nH][nH]cc2nc(-c3ccccc3)nc1-2
O-[OH;D1;+0:1].[C;D1;H3:2]-[S;H0;D2;+0:3]-[c:4](:[c:5]):[c:6]>>[C;D1;H3:2]-[S;H0;D3;+0:3](=[O;H0;D1;+0:1])-[c:4](:[c:5]):[c:6]
null
[]
null
null
24
HOUR
An amount of 0.21 gm of 2-(2-methoxy-4-methylmercapto-phenyl)-5H-imidazo[4,5-d]pyridazin-4-one is suspended in 10 ml of glacial acetic acid and mixed with 0.08 ml of 30% hydrogen peroxide. The mixture is stirred for 24 hours at ambient temperature and poured onto 20 ml of ice water. It is then stirred until a precipita...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Monosulfide
Sulfoxide
null
null
c1ccccc1.c1nc2cnncc2[nH]1
HO-
C(C)(=O)O
null
24
COc1cc(SC)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.OO>C(C)(=O)O>COc1cc(S(C)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-033061a22a0d4381887b3730bf5da3c7
COc1cc(S(C)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.OO>>COc1cc(S(C)(=O)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
COC1=C(C=CC(=C1)S(=O)C)C=1N=C2C(=CNNC2=O)N1.OO.OO>>COC1=C(C=CC(=C1)S(=O)(=O)C)C=1N=C2C(=CNNC2=O)N1
[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6]([CH3:7])=[O:8])[cH:10][cH:11][c:12]1-[c:13]1[n:14][c:15]2[cH:16][nH:17][nH:18][c:19](=[O:20])[c:21]-2[n:22]1.O[OH:9]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6]([CH3:7])(=[O:8])=[O:9])[cH:10][cH:11][c:12]1-[c:13]1[n:14][c:15]2[cH:16][nH:17][nH:18][c:19](=[O:20])[c:21]-2[n:22]1
COc1cc(S(C)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.OO
COc1cc(S(C)(=O)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
null
null
C(C)(=O)O
Oxidation
OtherReaction
82eeb432cea55e49dd1e612c513601ecda8b69f66d62f31cabaae14486674ab1
cbb05648c84536652b4eef951a389695d3f3bef8ba19ea253e8a66fff9ee4d44
O=c1[nH][nH]cc2nc(-c3ccccc3)nc1-2
O-[OH;D1;+0:1].[C;D1;H3:2]-[S;H0;D3;+0:3](=[O;D1;H0:4])-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[S;H0;D4;+0:3](=[O;D1;H0:4])(=[O;H0;D1;+0:1])-[c:5](:[c:6]):[c:7]
null
[]
null
null
55
MINUTE
A quantity of 0.07 gm of 2-(2-methoxy-4-methylsulfinyl-phenyl)-5H-imidazo[4,5-d]pyridazin-4-one is dissolved in 5 ml of glacial acetic acid, mixed with 0.05 ml of 30% hydrogen peroxide, and stirred first for 55 minutes at ambient temperature then for two hours at 40°-50° C., Then, a further 0.05 ml of hydrogen peroxide...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Sulfoxide
Sulfone
null
null
c1ccccc1.c1nc2cnncc2[nH]1
HO-
C(C)(=O)O
null
0.916667
COc1cc(S(C)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.OO>C(C)(=O)O>COc1cc(S(C)(=O)=O)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ed32d25e0c7c45dfb2b09ee2c01e0cd2
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)O.COc1ccc(N)c(N)n1>>COc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2N(C)C)c(N)n1
N.CN(C1=C(C(=O)O)C=CC(=C1)[N+](=O)[O-])C.Cl.Cl.NC1=NC(=CC=C1N)OC.O>>CN(C1=C(C(=O)NC=2C(=NC(=CC2)OC)N)C=CC(=C1)[N+](=O)[O-])C
O[C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13]([N+:14](=[O:15])[O-:16])[cH:17][c:18]1[N:19]([CH3:20])[CH3:21].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[c:22]([NH2:23])[n:24]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][C:8](=[O:9])[c:10]2[cH:11][cH:12][c:13]([N+:14](=[O:15])[O-:16])[cH:17][c:18]2[N:19]([CH3:20])[CH3:21])...
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)O.COc1ccc(N)c(N)n1
COc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2N(C)C)c(N)n1
null
null
P(=O)(Cl)(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Nc1cccnc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[N;D1;H2:6]-[c:7](:[#7;a:8]:[c:9]):[c:10](-[NH2;D1;+0:11]):[c:12]>>[N;D1;H2:6]-[c:7](:[#7;a:8]:[c:9]):[c:10](-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]):[c:12]
null
[]
null
null
null
null
An amount of 1.05 gm of 2-dimethylamino-4-nitro-benzoic acid is suspended in 35 ml of phosphorus oxychloride, and 1.05 gm of 2,3-diamino-6-methoxy-pyridine dihydrochloride are added thereto. The mixture is refluxed for 5 minutes, left to cool for 15 minutes with stirring, and finally decomposed with water. The solution...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccncc1.c1ccccc1
HO-
P(=O)(Cl)(Cl)Cl
null
null
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)O.COc1ccc(N)c(N)n1>P(=O)(Cl)(Cl)Cl>COc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2N(C)C)c(N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-072da412b7c74d68ae2b0cbe80cf9367
COc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2N(C)C)c(N)n1>>COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1
CN(C1=C(C(=O)NC=2C(=NC(=CC2)OC)N)C=CC(=C1)[N+](=O)[O-])C>>CN(C1=C(C=CC(=C1)[N+](=O)[O-])C=1NC=2C(=NC(=CC2)OC)N1)C
O=[C:8]([NH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[n:23][c:22]1[NH2:21])[c:9]1[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]1[N:18]([CH3:19])[CH3:20]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][c:8](-[c:9]3[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]3[N:18]([CH3:19])[CH3:20])[n:21][c:22]2[n:2...
COc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2N(C)C)c(N)n1
COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1
null
null
P(=O)(Cl)(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
e4e19e3354cf9a80f944e2a2a196231b02ba3b66651d07863abe72917fd317c6
a079090652d9d6c0e17c70eeab94f6d7afea064f52cf5fa9036d5feedd14143a
c1ccc(-c2nc3ncccc3[nH]2)cc1
O=[C;H0;D3;+0:1](-[NH;D2;+0:2]-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[#7;a:7]:[c:8])-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12](-[#7:13]):[c:14]>>[#7:13]-[c:12](:[c:14]):[c;H0;D3;+0:9](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:6]:[c:5](:[#7;a:7]:[c:8]):[c:3](:[c:4]):[nH;D2;+0:2]:1):[c:10]:[c:11]
null
[]
null
null
null
null
A suspension of 1.4 gm of 3-[(2-dimethylamino-4-nitro-benzoyl)-amino]-2-amino-6-methoxy-pyridine in 40 ml of phosphorus oxychloride is refluxed for three hours. The phosphorus oxychloride is evaporated off by about two-thirds, and the residue is poured into water. The solution obtained is made ammoniacal, and the produ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine
null
c1ccncc1
c1cnc2nc[nH]c2c1
c1cnc2nc[nH]c2c1.c1ccccc1
HO-
P(=O)(Cl)(Cl)Cl
null
null
COc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2N(C)C)c(N)n1>P(=O)(Cl)(Cl)Cl>COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2a7e3c04034f4962805f2b8605f567fe
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)O.COc1ccc(N)c(N)n1>>COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1
CN(C1=C(C(=O)O)C=CC(=C1)[N+](=O)[O-])C.Cl.Cl.NC1=NC(=CC=C1N)OC>>CN(C1=C(C=CC(=C1)[N+](=O)[O-])C=1NC=2C(=NC(=CC2)OC)N1)C
O=[C:8](O)[c:9]1[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]1[N:18]([CH3:19])[CH3:20].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[c:22]([NH2:21])[n:23]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][c:8](-[c:9]3[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]3[N:18]([CH3:19])[CH3:20])[n:21][c:22]...
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)O.COc1ccc(N)c(N)n1
COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1
null
null
P(=O)(Cl)(Cl)Cl
Aromatic Heterocycle Formation
OtherReaction
732e0ce9e0b11ff0dfc685a4702602ca2b8a50d1240d37c421f2ec2dce5e88c1
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
c1ccc(-c2nc3ncccc3[nH]2)cc1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5](-[#7:6]):[c:7].[NH2;D1;+0:8]-[c:9](:[#7;a:10]:[c:11]):[c:12](-[NH2;D1;+0:13]):[c:14]>>[#7:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:8]:[c:9](:[#7;a:10]:[c:11]):[c:12](:[c:14]):[nH;D2;+0:13]:1):[c:3]:[c:4]
null
[]
null
null
null
null
An amount of 0.45 gm of 2-dimethylamino-4-nitro-benzoic acid is suspended in 15 ml of phosphorus oxychloride, and 0.45 gm of 2,3-diamino-6-methoxy-pyridine dihydrochloride are added. The mixture is refluxed for two hours and after cooling poured onto water. The aqueous solution is made ammoniacal with cooling, and the ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1ccncc1
c1cnc2nc[nH]c2c1
c1cnc2nc[nH]c2c1.c1ccccc1
HO-
P(=O)(Cl)(Cl)Cl
null
null
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)O.COc1ccc(N)c(N)n1>P(=O)(Cl)(Cl)Cl>COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-32e3d902264f4bcabd1c60500c9ad7ca
COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1>>CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=CCC(=O)NC2=N1
CN(C1=C(C=CC(=C1)[N+](=O)[O-])C=1NC=2C(=NC(=CC2)OC)N1)C.Cl>>CN(C1=C(C=CC(=C1)[N+](=O)[O-])C1=NC=2C(NC(CC2)=O)=N1)C
C[O:19][c:18]1[cH:17][cH:16][c:15]2[nH:14][c:13](-[c:12]3[c:4]([N:2]([CH3:1])[CH3:3])[cH:5][c:6]([N+:7](=[O:8])[O-:9])[cH:10][cH:11]3)[n:22][c:21]2[n:20]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][c:6]([N+:7](=[O:8])[O-:9])[cH:10][cH:11][c:12]1[C:13]1=[N:14][C:15]2=[CH:16][CH2:17][C:18](=[O:19])[NH:20][C:21]2=[N:22]1
COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=CCC(=O)NC2=N1
null
null
null
Reduction
OtherReaction
1d9952418bd03299fc209d71ff471e1f9e7efb202810a53a913ea8369ea77e1f
2aeb8b29862491232763337fc29cdbaeebf7c7f0fe8fc7b3a932e164064ec89c
O=C1CC=C2N=C(c3ccccc3)N=C2N1
C-[O;H0;D2;+0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5]2:[nH;D2;+0:6]:[c;H0;D3;+0:7](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](-[#7:12]):[c:13]):[n;H0;D2;+0:14]:[c;H0;D3;+0:15]:2:[n;H0;D2;+0:16]:1>>[#7:12]-[c:11](:[c:13]):[c;H0;D3;+0:8](-[C;H0;D3;+0:7]1=[N;H0;D2;+0:6]-[C;H0;D3;+0:5]2=[CH;D2;+0:4]-[CH2;D2;...
null
[]
null
null
null
null
A quantity of 0.2 gm of 2-(2-dimethylamino-4-nitro-phenyl)-5-methoxy-imidazo[4,5-b]pyridine is heated in a bomb tube to 100° C. for three hours with 5 ml of concentrated hydrochloric acid. The reaction mixture is poured onto about 20 ml of ice, neutralized, and extracted with ethyl acetate. After washing with water and...
10.6084/m9.figshare.5104873.v1
null
Ether
Secondary amide
c1cnc2nc[nH]c2c1
C1=NC2=CCCNC2=N1
c1ccccc1.C1=NC2=CCCNC2=N1
Other
null
null
null
COc1ccc2[nH]c(-c3ccc([N+](=O)[O-])cc3N(C)C)nc2n1>>CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=CCC(=O)NC2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-635cfe2f33674766827bc3eaf4c9f1ef
COc1cc(SC)ccc1C(=O)Nc1[nH]c(=O)ccc1[N+](=O)[O-]>>COc1cc(SC)ccc1C1=NC2=CCC(=O)NC2=N1
COC1=C(C(=O)NC=2NC(C=CC2[N+](=O)[O-])=O)C=CC(=C1)SC>>COC1=C(C=CC(=C1)SC)C1=NC=2C(NC(CC2)=O)=N1
O=[C:11]([c:10]1[c:3]([O:2][CH3:1])[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9]1)[NH:12][c:13]1[nH:18][c:16](=[O:17])[cH:15][cH:14][c:19]1[N+:20](=O)[O-]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9][c:10]1[C:11]1=[N:12][C:13]2=[CH:14][CH2:15][C:16](=[O:17])[NH:18][C:19]2=[N:20]1
COc1cc(SC)ccc1C(=O)Nc1[nH]c(=O)ccc1[N+](=O)[O-]
COc1cc(SC)ccc1C1=NC2=CCC(=O)NC2=N1
null
[Pd]
C(C)(=O)O.[H][H]
Functional Group Interconversion
OtherReaction
097fc0ee2c46913ac4696174b943d22ba6c02de85f4d1e046db3addb5981cdbd
5165cb7328f1a36fd7fbe60c5a38f86cf63e94d5d06f686e3ec068783b31cb00
O=C1CC=C2N=C(c3ccccc3)N=C2N1
O=[C;H0;D3;+0:1](-[NH;D2;+0:2]-[c;H0;D3;+0:3]1:[nH;D2;+0:4]:[c;H0;D3;+0:5](=[O;D1;H0:6]):[cH;D2;+0:7]:[cH;D2;+0:8]:[c;H0;D3;+0:9]:1-[N+;H0;D3:10](=O)-[O-])-[c:11](:[c:12]):[c:13]>>[O;D1;H0:6]=[C;H0;D3;+0:5]1-[CH2;D2;+0:7]-[CH;D2;+0:8]=[C;H0;D3;+0:3]2-[N;H0;D2;+0:2]=[C;H0;D3;+0:1](-[c:11](:[c:12]):[c:13])-[N;H0;D2;+0:10...
null
[]
null
null
null
null
An amount of 6.2 gm of 2-[(2-methoxy-4-methylmercapto-benzoyl)-amino]-3-nitro-1H-pyridin-6-one is dissolved in 370 ml of glacial acetic acid and hydrogenated with hydrogen in the presence of 6 gm of 10% palladium charcoal at ambient temperature under 5 bars of pressure (duration of reaction: two hours). The catalyst is...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Secondary amide
Secondary amide
c1cnccc1
C1=NC2=CCCNC2=N1
c1ccccc1.C1=NC2=CCCNC2=N1
Other
[Pd].C(C)(=O)O.[H][H]
null
null
COc1cc(SC)ccc1C(=O)Nc1[nH]c(=O)ccc1[N+](=O)[O-]>[Pd].C(C)(=O)O.[H][H]>COc1cc(SC)ccc1C1=NC2=CCC(=O)NC2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-eed20875f89042a78eaca70db7681c77
COc1ccc(-c2nc3c(ccc[n+]3[O-])[nH]2)c(OC)c1>>COc1ccc(C2=NC3=CCC(=O)NC3=N2)c(OC)c1
O.COC1=C(C=CC(=C1)OC)C=1NC=2C(=[N+](C=CC2)[O-])N1.Cl>>COC1=C(C=CC(=C1)OC)C1=NC=2C(NC(CC2)=O)=N1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[nH:8][c:9]3[cH:10][cH:11][cH:12][n+:14]([O-:13])[c:15]3[n:16]2)[c:17]([O:18][CH3:19])[cH:20]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2=[N:8][C:9]3=[CH:10][CH2:11][C:12](=[O:13])[NH:14][C:15]3=[N:16]2)[c:17]([O:18][CH3:19])[cH:20]1
COc1ccc(-c2nc3c(ccc[n+]3[O-])[nH]2)c(OC)c1
COc1ccc(C2=NC3=CCC(=O)NC3=N2)c(OC)c1
null
null
C(C)(=O)OC(C)=O
Reduction
OtherReaction
f2c2fc23baa26f196552837bc874de3c071e518b7de1f37d2a5ae017bb507d87
0bc6e593e557e498d898fea24a080f55573b56d80aeb59ee40dc96af16ebee15
O=C1CC=C2N=C(c3ccccc3)N=C2N1
[#8:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[c;H0;D3;+0:5]1:[n;H0;D2;+0:6]:[c;H0;D3;+0:7]2:[c;H0;D3;+0:8](:[cH;D2;+0:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[n+;H0;D3:12]:2-[O-;H0;D1:13]):[nH;D2;+0:14]:1):[c:15]:[c:16]>>[#8:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[C;H0;D3;+0:5]1=[N;H0;D2;+0:14]-[C;H0;D3;+0:8]2=[CH;D2;+0:9]-[CH2;D2;+0:10]-[C;...
null
[]
120
CELSIUS
30
MINUTE
Four grams of 2-(2,4-dimethoxy-phenyl)-imidazo[4,5-b]pyridin-4-oxide is suspended in 40 ml of acetic anhydride and refluxed for 2.75 hours. After cooling the mixture is poured onto 150 ml of ice, 25 ml of 6N hydrochloric acid are added, and the mixture is stirred at 120° C. for 30 minutes. It is cooled to ambient tempe...
10.6084/m9.figshare.5104873.v1
null
null
Secondary amide
C1=C[NH+]=c2nc[nH]c2=C1
C1=NC2=CCCNC2=N1
c1ccccc1.C1=NC2=CCCNC2=N1
null
C(C)(=O)OC(C)=O
120
0.5
COc1ccc(-c2nc3c(ccc[n+]3[O-])[nH]2)c(OC)c1>C(C)(=O)OC(C)=O>COc1ccc(C2=NC3=CCC(=O)NC3=N2)c(OC)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ef123c04d995491aa3822ca7748bf055
CC(=O)O.COc1ccc(-c2nc3ncnc(Cl)c3[nH]2)c(OC)c1>>COc1ccc(-c2nc3nc[nH]c(=O)c3[nH]2)c(OC)c1
COC1=C(C=CC(=C1)OC)C1=NC2=NC=NC(=C2N1)Cl.C(C)(=O)O>>COC1=C(C=CC(=C1)OC)C1=NC=2N=CNC(C2N1)=O
CC(O)=[O:14].Cl[c:13]1[n:12][cH:11][n:10][c:9]2[n:8][c:7](-[c:6]3[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:20][c:17]3[O:18][CH3:19])[nH:16][c:15]21>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[n:8][c:9]3[n:10][cH:11][nH:12][c:13](=[O:14])[c:15]3[nH:16]2)[c:17]([O:18][CH3:19])[cH:20]1
CC(=O)O.COc1ccc(-c2nc3ncnc(Cl)c3[nH]2)c(OC)c1
COc1ccc(-c2nc3nc[nH]c(=O)c3[nH]2)c(OC)c1
null
null
[OH-].[Na+]
Miscellaneous
OtherReaction
9377ccc63c37898d5c04b2c0b12e6c58f02a4daaf315adef4f55845fc1e74f96
3fbb180061815c1a91daf750f59d95354663c01e4c6076719644d5369bdccd52
O=c1[nH]cnc2nc(-c3ccccc3)[nH]c12
C-C(-O)=[O;H0;D1;+0:1].Cl-[c;H0;D3;+0:2]1:[n;H0;D2;+0:3]:[c:4]:[#7;a:5]:[c:6]2:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:2:1>>[O;H0;D1;+0:1]=[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c:4]:[#7;a:5]:[c:6]2:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:2:1
null
[]
null
null
null
null
One-half gram of 8-(2,4-dimethoxy-phenyl)-6-chloro-purine is refluxed for seven hours in 30 ml of 2N sodium hydroxide solution. The mixture is acidified with glacial acetic acid, and the precipitate obtained is recrystallized from methanol. Conditions: See reaction.notes.procedure_details. Workup: the precipitate obtai...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carboxylic acid
null
c1ncc2nc[nH]c2n1
c1nc2cncnc2[nH]1
c1ccccc1.c1nc2cncnc2[nH]1
HCl
[OH-].[Na+]
null
null
CC(=O)O.COc1ccc(-c2nc3ncnc(Cl)c3[nH]2)c(OC)c1>[OH-].[Na+]>COc1ccc(-c2nc3nc[nH]c(=O)c3[nH]2)c(OC)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1710e5d8571f49e99991ce847c7586f7
COc1ccc(SC)cc1-c1nc2ncnc(Cl)c2[nH]1.[OH-]>>COc1ccc(SC)cc1C1=NC2=NC=NC(=O)C2=N1
ClC1=C2NC(=NC2=NC=N1)C1=C(C=CC(=C1)SC)OC.[OH-].[K+]>>COC1=C(C=C(C=C1)SC)C1=NC2=NC=NC(C2=N1)=O
Cl[c:17]1[n:16][cH:15][n:14][c:13]2[n:12][c:11](-[c:10]3[c:3]([O:2][CH3:1])[cH:4][cH:5][c:6]([S:7][CH3:8])[cH:9]3)[nH:20][c:19]21.[OH-:18]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([S:7][CH3:8])[cH:9][c:10]1[C:11]1=[N:12][C:13]2=[N:14][CH:15]=[N:16][C:17](=[O:18])[C:19]2=[N:20]1
COc1ccc(SC)cc1-c1nc2ncnc(Cl)c2[nH]1.[OH-]
COc1ccc(SC)cc1C1=NC2=NC=NC(=O)C2=N1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
327533abca4f49f12126eb122dcca5190e8fa70809992fbb7584ad35f80bddab
91d49c9e42f397efc3bc857ca7ed897b28f3c235ee6bb61b057a5ee9eee70a95
O=C1N=CN=C2N=C(c3ccccc3)N=C12
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[cH;D2;+0:3]:[n;H0;D2;+0:4]:[c;H0;D3;+0:5]2:[n;H0;D2;+0:6]:[c;H0;D3;+0:7](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](-[#8:12]):[c:13]):[nH;D2;+0:14]:[c;H0;D3;+0:15]:2:1.[OH-;D0:16]>>[#8:12]-[c:11](:[c:13]):[c;H0;D3;+0:8](-[C;H0;D3;+0:7]1=[N;H0;D2;+0:6]-[C;H0;D3;+0:5]2=[N;H0;D2;+0:4]-[CH;D2;...
null
[]
null
null
null
null
Prepared analogously to Example 16 from 6-chloro-8-(2-methoxy-5-methylmercapto-phenyl)-purine by reaction with 20% potassium hydroxide solution. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Substituted imine
c1ncc2nc[nH]c2n1
C1=NCC2=NC=NC2=N1
c1ccccc1.C1=NCC2=NC=NC2=N1
HCl
null
null
null
COc1ccc(SC)cc1-c1nc2ncnc(Cl)c2[nH]1.[OH-]>>COc1ccc(SC)cc1C1=NC2=NC=NC(=O)C2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2a4c687c874b41f689e1af3834786261
COc1cc(OC)c(-c2nc3ncnc(Cl)c3[nH]2)cc1Br.[OH-]>>COc1cc(OC)c(C2=NC3=NC=NC(=O)C3=N2)cc1Br
ClC1=C2NC(=NC2=NC=N1)C1=C(C=C(C(=C1)Br)OC)OC.[OH-].[K+]>>BrC=1C(=CC(=C(C1)C1=NC2=NC=NC(C2=N1)=O)OC)OC
Cl[c:15]1[n:14][cH:13][n:12][c:11]2[n:10][c:9](-[c:8]3[c:5]([O:6][CH3:7])[cH:4][c:3]([O:2][CH3:1])[c:20]([Br:21])[cH:19]3)[nH:18][c:17]21.[OH-:16]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[c:8]([C:9]2=[N:10][C:11]3=[N:12][CH:13]=[N:14][C:15](=[O:16])[C:17]3=[N:18]2)[cH:19][c:20]1[Br:21]
COc1cc(OC)c(-c2nc3ncnc(Cl)c3[nH]2)cc1Br.[OH-]
COc1cc(OC)c(C2=NC3=NC=NC(=O)C3=N2)cc1Br
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
327533abca4f49f12126eb122dcca5190e8fa70809992fbb7584ad35f80bddab
91d49c9e42f397efc3bc857ca7ed897b28f3c235ee6bb61b057a5ee9eee70a95
O=C1N=CN=C2N=C(c3ccccc3)N=C12
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[cH;D2;+0:3]:[n;H0;D2;+0:4]:[c;H0;D3;+0:5]2:[n;H0;D2;+0:6]:[c;H0;D3;+0:7](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](-[#8:12]):[c:13]):[nH;D2;+0:14]:[c;H0;D3;+0:15]:2:1.[OH-;D0:16]>>[#8:12]-[c:11](:[c:13]):[c;H0;D3;+0:8](-[C;H0;D3;+0:7]1=[N;H0;D2;+0:6]-[C;H0;D3;+0:5]2=[N;H0;D2;+0:4]-[CH;D2;...
null
[]
null
null
null
null
Prepared analogously to Example 16 from 6-chloro-8-(5-bromo-2,4-dimethoxy-phenyl)-purine by reaction with 20% potassium hydroxide solution. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Substituted imine
c1ncc2nc[nH]c2n1
C1=NCC2=NC=NC2=N1
c1ccccc1.C1=NCC2=NC=NC2=N1
HCl
null
null
null
COc1cc(OC)c(-c2nc3ncnc(Cl)c3[nH]2)cc1Br.[OH-]>>COc1cc(OC)c(C2=NC3=NC=NC(=O)C3=N2)cc1Br
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5e0c07233f644f10933c6296392a0863
CNS(=O)(=O)c1cc(-c2nc(Cl)c3[nH]cnc3n2)c(OC)cc1Cl>>CNS(=O)c1cc(C2=NC3=NC=NC(=O)C3=N2)c(OC)cc1Cl
ClC1=C2NC=NC2=NC(=N1)C1=C(C=C(C(=C1)S(=O)(=O)NC)Cl)OC.[OH-].[K+]>>ClC1=CC(=C(C=C1S(=O)NC)C1=NC2=NC=NC(C2=N1)=O)OC
Cl[c:14]1[c:16]2[c:10]([n:9][c:8](-[c:7]3[cH:6][c:5]([S:3]([NH:2][CH3:1])(=[O:4])=[O:15])[c:22]([Cl:23])[cH:21][c:18]3[O:19][CH3:20])[n:17]1)[n:11][cH:12][nH:13]2>>[CH3:1][NH:2][S:3](=[O:4])[c:5]1[cH:6][c:7]([C:8]2=[N:9][C:10]3=[N:11][CH:12]=[N:13][C:14](=[O:15])[C:16]3=[N:17]2)[c:18]([O:19][CH3:20])[cH:21][c:22]1[Cl:2...
CNS(=O)(=O)c1cc(-c2nc(Cl)c3[nH]cnc3n2)c(OC)cc1Cl
CNS(=O)c1cc(C2=NC3=NC=NC(=O)C3=N2)c(OC)cc1Cl
null
null
null
Reduction
OtherReaction
3e4cf9df2c9f742f263371e855ee29cdf6de22aa47b48f9d571faca5570cf50b
8cd35126ae40bb2bce2484e3c67bcf4ba838ff3c539e79634188717dbe42a6b6
O=C1N=CN=C2N=C(c3ccccc3)N=C12
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c;H0;D3;+0:3](-[c;H0;D3;+0:4]2:[c:5]:[c:6](-[S;H0;D4;+0:7](=[O;D1;H0:8])(=[O;H0;D1;+0:9])-[#7:10]-[C;D1;H3:11]):[c:12]:[c:13]:[c:14]:2-[#8:15]):[n;H0;D2;+0:16]:[c;H0;D3;+0:17]2:[n;H0;D2;+0:18]:[cH;D2;+0:19]:[nH;D2;+0:20]:[c;H0;D3;+0:21]:2:1>>[#8:15]-[c:14]1:[c:13]:[c:12]:[c:6](-[S;H0;...
null
[]
null
null
null
null
Prepared analogously to Example 16 from 6-chloro-(4-chloro-2-methoxy-5-methylaminosulfonyl-phenyl)-purine with 20% potassium hydroxide solution. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Aromatic halide
Substituted imine
c1ncc2nc[nH]c2n1
C1=NCC2=NC=NC2=N1
c1ccccc1.C1=NCC2=NC=NC2=N1
HCl
null
null
null
CNS(=O)(=O)c1cc(-c2nc(Cl)c3[nH]cnc3n2)c(OC)cc1Cl>>CNS(=O)c1cc(C2=NC3=NC=NC(=O)C3=N2)c(OC)cc1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bb53e3adbf81433d844364e852ee7c9c
COc1cc(SC)ccc1C(=O)O.Nc1[nH]c(=O)[nH]c(=O)c1N>>COc1cc(SC)ccc1C(=O)Nc1c(N)[nH]c(=O)[nH]c1=O
O.COC1=C(C(=O)O)C=CC(=C1)SC.NC=1NC(NC(C1N)=O)=O>>NC=1NC(NC(C1NC(C1=C(C=C(C=C1)SC)OC)=O)=O)=O
O[C:11]([c:10]1[c:3]([O:2][CH3:1])[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9]1)=[O:12].[NH2:13][c:14]1[c:15]([NH2:16])[nH:17][c:18](=[O:19])[nH:20][c:21]1=[O:22]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9][c:10]1[C:11](=[O:12])[NH:13][c:14]1[c:15]([NH2:16])[nH:17][c:18](=[O:19])[nH:20][c:21]1=[O:22]
COc1cc(SC)ccc1C(=O)O.Nc1[nH]c(=O)[nH]c(=O)c1N
COc1cc(SC)ccc1C(=O)Nc1c(N)[nH]c(=O)[nH]c1=O
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Nc1c[nH]c(=O)[nH]c1=O)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[N;D1;H2:6]-[c:7]1:[#7;a:8]:[c:9]:[#7;a:10]:[c:11](=[O;D1;H0:12]):[c:13]:1-[NH2;D1;+0:14]>>[N;D1;H2:6]-[c:7]1:[#7;a:8]:[c:9]:[#7;a:10]:[c:11](=[O;D1;H0:12]):[c:13]:1-[NH;D2;+0:14]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
30
MINUTE
Twenty grams of 2-methoxy-4-methylmercapto-benzoic acid is dissolved in 260 ml of dimethylformamide, mixed with 13 gm of N,N'-carbonyl-diimidazole, and stirred for 30 minutes at ambient temperature. Then, 13 gm of 4,5-diamino-pyrimidin-2,6-dione are added, and the reaction mixture is refluxed for three hours with stirr...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1cncnc1
HO-
CN(C=O)C
null
0.5
COc1cc(SC)ccc1C(=O)O.Nc1[nH]c(=O)[nH]c(=O)c1N>CN(C=O)C>COc1cc(SC)ccc1C(=O)Nc1c(N)[nH]c(=O)[nH]c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-88ccc828c8c445c7842b8cfe8e1ea814
COc1cc(SC)ccc1C(=O)Nc1c(N)[nH]c(=O)[nH]c1=O>>COc1cc(SC)ccc1C1=NC2=NC(=O)NC(=O)C2=N1
NC=1NC(NC(C1NC(C1=C(C=C(C=C1)SC)OC)=O)=O)=O.[OH-].[Na+]>>COC1=C(C=CC(=C1)SC)C1=NC2=NC(NC(C2=N1)=O)=O
O=[C:11]([c:10]1[c:3]([O:2][CH3:1])[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9]1)[NH:21][c:20]1[c:13]([NH2:12])[nH:14][c:15](=[O:16])[nH:17][c:18]1=[O:19]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6][CH3:7])[cH:8][cH:9][c:10]1[C:11]1=[N:12][C:13]2=[N:14][C:15](=[O:16])[NH:17][C:18](=[O:19])[C:20]2=[N:21]1
COc1cc(SC)ccc1C(=O)Nc1c(N)[nH]c(=O)[nH]c1=O
COc1cc(SC)ccc1C1=NC2=NC(=O)NC(=O)C2=N1
null
null
C(C)O
Oxidation
OtherReaction
f19b00b783c8668bdd897adbf9f0a492f75ec8ff374f905495560e889f5ad6dd
8094e487c6679f2b9c623ceccf688ef9bd51c882e09a5e50b6df3f985c6c390b
O=C1N=C2N=C(c3ccccc3)N=C2C(=O)N1
O=[C;H0;D3;+0:1](-[NH;D2;+0:2]-[c;H0;D3;+0:3]1:[c;H0;D3;+0:4](-[NH2;D1;+0:5]):[nH;D2;+0:6]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[nH;D2;+0:9]:[c;H0;D3;+0:10]:1=[O;D1;H0:11])-[c:12](:[c:13]):[c:14]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[N;H0;D2;+0:6]=[C;H0;D3;+0:4]2-[N;H0;D2;+0:5]=[C;H0;D3;+0:1](-[c:12](:[c:13]):[c:14])-[N;H0;D2;+0:2]=[C...
null
[]
null
null
15
MINUTE
Two grams of 4-amino-5-(2-methoxy-4-methylmercapto-benzoylamino)-pyrimidin-2,6-dione are refluxed for 21 hours with 50 ml of ethanol and 50 ml of 2N sodium hydroxide solution. After about 15 minutes, a solution is formed. After cooling, the solution is suction filtered with glacial acetic acid, washed with water, and d...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine
Substituted imine.Unsubstituted dicarboximide
c1cncnc1
C1=NC2=NCNCC2=N1
c1ccccc1.C1=NC2=NCNCC2=N1
HO-
C(C)O
null
0.25
COc1cc(SC)ccc1C(=O)Nc1c(N)[nH]c(=O)[nH]c1=O>C(C)O>COc1cc(SC)ccc1C1=NC2=NC(=O)NC(=O)C2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cd16ce517d74444e9c3738b0eac46728
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)Nc1nc[nH]c(=O)c1N>>CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=NC=NC(=O)C2=N1
NC1=C(N=CNC1=O)NC(C1=C(C=C(C=C1)[N+](=O)[O-])N(C)C)=O>>CN(C1=C(C=CC(=C1)[N+](=O)[O-])C1=NC2=NC=NC(C2=N1)=O)C
O=[C:13]([c:12]1[c:4]([N:2]([CH3:1])[CH3:3])[cH:5][c:6]([N+:7](=[O:8])[O-:9])[cH:10][cH:11]1)[NH:14][c:15]1[n:16][cH:17][nH:18][c:19](=[O:20])[c:21]1[NH2:22]>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][c:6]([N+:7](=[O:8])[O-:9])[cH:10][cH:11][c:12]1[C:13]1=[N:14][C:15]2=[N:16][CH:17]=[N:18][C:19](=[O:20])[C:21]2=[N:22]1
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)Nc1nc[nH]c(=O)c1N
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=NC=NC(=O)C2=N1
null
null
C(C)(=O)O
Oxidation
OtherReaction
d1086c143044236faf9cf27747cb243342e0b462dafd8d56bc6d7c348e0f7406
1a44b30fbd9836f37983c1becc2bcb0cab0f1034333aa4a97c7d041f13ef2d97
O=C1N=CN=C2N=C(c3ccccc3)N=C12
O=[C;H0;D3;+0:1](-[NH;D2;+0:2]-[c;H0;D3;+0:3]1:[n;H0;D2;+0:4]:[cH;D2;+0:5]:[nH;D2;+0:6]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[c;H0;D3;+0:9]:1-[NH2;D1;+0:10])-[c:11](:[c:12]):[c:13]>>[O;D1;H0:8]=[C;H0;D3;+0:7]1-[N;H0;D2;+0:6]=[CH;D2;+0:5]-[N;H0;D2;+0:4]=[C;H0;D3;+0:3]2-[N;H0;D2;+0:2]=[C;H0;D3;+0:1](-[c:11](:[c:12]):[c:13])-[N;H...
null
[]
null
null
null
null
One gram of 5-amino-4-(2-dimethylamino-4-nitro-benzoylamino)pyrimidin-6-one is refluxed for two hours in 50 ml of glacial acetic acid. The mixture is evaporated to dryness, and the residue is stirred out with ethanol in the warm. Conditions: See reaction.notes.procedure_details. Workup: The mixture is evaporated to dry...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine
Substituted imine
c1cncnc1
C1=NCC2=NC=NC2=N1
c1ccccc1.C1=NCC2=NC=NC2=N1
HO-
C(C)(=O)O
null
null
CN(C)c1cc([N+](=O)[O-])ccc1C(=O)Nc1nc[nH]c(=O)c1N>C(C)(=O)O>CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=NC=NC(=O)C2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7272044c980b48afb3322c501ec35ccc
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=NC=NC(=O)C2=N1>>CN(C)c1cc(N)ccc1C1=NC2=NC=NC(=O)C2=N1
CN(C1=C(C=CC(=C1)[N+](=O)[O-])C1=NC2=NC=NC(C2=N1)=O)C.[H][H]>>NC1=CC(=C(C=C1)C1=NC2=NC=NC(C2=N1)=O)N(C)C
O=[N+:7]([O-])[c:6]1[cH:5][c:4]([N:2]([CH3:1])[CH3:3])[c:10]([C:11]2=[N:12][C:13]3=[N:14][CH:15]=[N:16][C:17](=[O:18])[C:19]3=[N:20]2)[cH:9][cH:8]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][c:6]([NH2:7])[cH:8][cH:9][c:10]1[C:11]1=[N:12][C:13]2=[N:14][CH:15]=[N:16][C:17](=[O:18])[C:19]2=[N:20]1
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=NC=NC(=O)C2=N1
CN(C)c1cc(N)ccc1C1=NC2=NC=NC(=O)C2=N1
null
[Ni]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C1N=CN=C2N=C(c3ccccc3)N=C12
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
An amount of 0.9 gm of 8-(2-dimethylamino-4-nitro-phenyl)purin-6-one is hydrogenated in 50 ml of methanol in the presence of 0.5 gm of Raney nickel at ambient temperature and under 5 bars of pressure with hydrogen for three hours until the calculated quantity has been taken up. After the catalyst has been subjected to ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.C1=NCC2=NC=NC2=N1
Other
[Ni].CO
null
null
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=NC=NC(=O)C2=N1>[Ni].CO>CN(C)c1cc(N)ccc1C1=NC2=NC=NC(=O)C2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-639397261a4c4c98b76a12db25b2c876
CC(=O)OC(C)=O.CN(C)c1cc(N)ccc1C1=NC2=NC=NC(=O)C2=N1>>CC(=O)Nc1ccc(C2=NC3=NC=NC(=O)C3=N2)c(N(C)C)c1
NC1=CC(=C(C=C1)C1=NC2=NC=NC(C2=N1)=O)N(C)C.C(C)(=O)OC(C)=O>>C(C)(=O)NC1=CC(=C(C=C1)C1=NC2=NC=NC(C2=N1)=O)N(C)C
CC(=O)O[C:2]([CH3:1])=[O:3].[NH2:4][c:5]1[cH:6][cH:7][c:8]([C:9]2=[N:10][C:11]3=[N:12][CH:13]=[N:14][C:15](=[O:16])[C:17]3=[N:18]2)[c:19]([N:20]([CH3:21])[CH3:22])[cH:23]1>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]([C:9]2=[N:10][C:11]3=[N:12][CH:13]=[N:14][C:15](=[O:16])[C:17]3=[N:18]2)[c:19]([N:20]([CH3:21])[C...
CC(=O)OC(C)=O.CN(C)c1cc(N)ccc1C1=NC2=NC=NC(=O)C2=N1
CC(=O)Nc1ccc(C2=NC3=NC=NC(=O)C3=N2)c(N(C)C)c1
null
null
null
Acylation
Aminolysis of esters
87d35e51b477fc9a658a6f307eb56d84c8879182772c9dd3a42ec0d584fd2684
627cbc0550c9f51ad0105d9fcf46677e8c93bed87ee95bfe69292a82550c95b7
O=C1N=CN=C2N=C(c3ccccc3)N=C12
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
A quantity of 0.6 gm of 8-(4-amino-2-dimethylamino-phenyl)purin-6-one is heated to 150° C. in 5 ml of acetic anhydride for one hour. The mixture is evaporated to dryness in vacuo and recrystallized from acetone/ether. Conditions: See reaction.notes.procedure_details. Workup: The mixture is evaporated to dryness in vacu...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Secondary amide
null
null
c1ccccc1.C1=NCC2=NC=NC2=N1
HO-
null
null
null
CC(=O)OC(C)=O.CN(C)c1cc(N)ccc1C1=NC2=NC=NC(=O)C2=N1>>CC(=O)Nc1ccc(C2=NC3=NC=NC(=O)C3=N2)c(N(C)C)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7c71ace40aec4481bedb5ae26a19e76f
COc1cc(OCc2ccccc2)ccc1-c1nc2ncnc(Cl)c2[nH]1.[OH-]>>COc1cc(OCc2ccccc2)ccc1C1=NC2=NC=NC(=O)C2=N1
C(C1=CC=CC=C1)OC1=CC(=C(C=C1)C1=NC2=NC=NC(=C2N1)Cl)OC.[OH-].[K+]>>C(C1=CC=CC=C1)OC1=CC(=C(C=C1)C1=NC2=NC=NC(C2=N1)=O)OC
Cl[c:23]1[n:22][cH:21][n:20][c:19]2[n:18][c:17](-[c:16]3[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH2:7][c:8]4[cH:9][cH:10][cH:11][cH:12][cH:13]4)[cH:14][cH:15]3)[nH:26][c:25]21.[OH-:24]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15][c:16]1[C:17]1=[N:18][C:19]2=[N:20][CH:...
COc1cc(OCc2ccccc2)ccc1-c1nc2ncnc(Cl)c2[nH]1.[OH-]
COc1cc(OCc2ccccc2)ccc1C1=NC2=NC=NC(=O)C2=N1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
327533abca4f49f12126eb122dcca5190e8fa70809992fbb7584ad35f80bddab
91d49c9e42f397efc3bc857ca7ed897b28f3c235ee6bb61b057a5ee9eee70a95
O=C1N=CN=C2N=C(c3ccc(OCc4ccccc4)cc3)N=C12
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[cH;D2;+0:3]:[n;H0;D2;+0:4]:[c;H0;D3;+0:5]2:[n;H0;D2;+0:6]:[c;H0;D3;+0:7](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](-[#8:12]):[c:13]):[nH;D2;+0:14]:[c;H0;D3;+0:15]:2:1.[OH-;D0:16]>>[#8:12]-[c:11](:[c:13]):[c;H0;D3;+0:8](-[C;H0;D3;+0:7]1=[N;H0;D2;+0:6]-[C;H0;D3;+0:5]2=[N;H0;D2;+0:4]-[CH;D2;...
null
[]
null
null
null
null
Prepared analogously to Example 16 from 8-(4-benzyloxy-2-methoxy-phenyl)-6-chloro-purine by reaction with 40% potassium hydroxide solution. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Substituted imine
c1ncc2nc[nH]c2n1
C1=NCC2=NC=NC2=N1
c1ccccc1.c1ccccc1.C1=NCC2=NC=NC2=N1
HCl
null
null
null
COc1cc(OCc2ccccc2)ccc1-c1nc2ncnc(Cl)c2[nH]1.[OH-]>>COc1cc(OCc2ccccc2)ccc1C1=NC2=NC=NC(=O)C2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9bb33ecc109041f0a8377bc723501737
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=CCC(=O)NC2=N1>>CN(C)c1cc(N)ccc1C1=NC2=CCC(=O)NC2=N1
O.CN(C1=C(C=CC(=C1)[N+](=O)[O-])C1=NC=2C(NC(CC2)=O)=N1)C.[H][H].Cl>>Cl.CN(C1=C(C=CC(=C1)N)C1=NC=2C(NC(CC2)=O)=N1)C
O=[N+:7]([O-])[c:6]1[cH:5][c:4]([N:2]([CH3:1])[CH3:3])[c:10]([C:11]2=[N:12][C:13]3=[CH:14][CH2:15][C:16](=[O:17])[NH:18][C:19]3=[N:20]2)[cH:9][cH:8]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][c:6]([NH2:7])[cH:8][cH:9][c:10]1[C:11]1=[N:12][C:13]2=[CH:14][CH2:15][C:16](=[O:17])[NH:18][C:19]2=[N:20]1
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=CCC(=O)NC2=N1
CN(C)c1cc(N)ccc1C1=NC2=CCC(=O)NC2=N1
null
[Pd]
CN(C=O)C
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C1CC=C2N=C(c3ccccc3)N=C2N1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
An amount of 1.7 gm of 2-(2-dimethylamino-4-nitro-phenyl)-4H-imidazo[4,5-b]pyridin-5-one is dissolved in 20 ml of dimethylformamide and mixed with 0.2 gm of 10% palladium/charcoal. The mixture is hydrogenated for three hours with hydrogen at ambient temperature under 5 bars of pressure. The mixture is filtered off from...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.C1=NC2=CCCNC2=N1
Other
[Pd].CN(C=O)C
null
null
CN(C)c1cc([N+](=O)[O-])ccc1C1=NC2=CCC(=O)NC2=N1>[Pd].CN(C=O)C>CN(C)c1cc(N)ccc1C1=NC2=CCC(=O)NC2=N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f2c701250f51434a8eabd6294b537cef
CC(=O)OC(C)=O.CN(C)c1cc(N)ccc1C1=NC2=NC(=O)C=CC2=N1>>CC(=O)Nc1ccc(C2=NC3=CCC(=O)NC3=N2)c(N(C)C)c1
CN(C1=C(C=CC(=C1)N)C=1N=C2C(=NC(C=C2)=O)N1)C.C(C)(=O)OC(C)=O>>CN(C1=C(C=CC(=C1)NC(=O)C)C1=NC=2C(NC(CC2)=O)=N1)C
CC(=O)O[C:2]([CH3:1])=[O:3].[NH2:4][c:5]1[cH:6][cH:7][c:8]([C:9]2=[N:18][C:17]3=[N:16][C:14](=[O:15])[CH:13]=[CH:12][C:11]3=[N:10]2)[c:19]([N:20]([CH3:21])[CH3:22])[cH:23]1>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]([C:9]2=[N:10][C:11]3=[CH:12][CH2:13][C:14](=[O:15])[NH:16][C:17]3=[N:18]2)[c:19]([N:20]([CH3:21]...
CC(=O)OC(C)=O.CN(C)c1cc(N)ccc1C1=NC2=NC(=O)C=CC2=N1
CC(=O)Nc1ccc(C2=NC3=CCC(=O)NC3=N2)c(N(C)C)c1
null
null
null
Acylation
OtherReaction
51e2bda446ba4c8c5a1d914db33e90c108810c5753ada7e402d7668ec0fabb8f
4268bb9edae8244adfa3b7b9a65f5aaf238c4d88c54c190675bc60f475d85d78
O=C1CC=C2N=C(c3ccccc3)N=C2N1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[NH2;D1;+0:4]-[c:5]1:[c:6]:[c:7]:[c:8](-[C;H0;D3;+0:9]2=[N;H0;D2;+0:10]-[C;H0;D3;+0:11]3=[N;H0;D2;+0:12]-[C:13](=[O;D1;H0:14])-[CH;D2;+0:15]=[CH;D2;+0:16]-[C;H0;D3;+0:17]-3=[N;H0;D2;+0:18]-2):[c:19]:[c:20]:1>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[NH;D2;+0:4]-[c:5]1...
null
[]
null
null
null
null
A quantity of 0.6 gm of 2-(2-dimethylamino-4-amino-phenyl)imidazo[4,5-b]pyridin-5-one is refluxed with 20 ml of acetic anhydride for 30 minutes. After evaporation, 10 ml of concentrated ammnoia and then 20 ml of ice are added. The product precipitated is suction filtered and washed with water. Conditions: See reaction....
10.6084/m9.figshare.5104873.v1
null
Anhydride.Substituted imine.Primary amine
Secondary amide.Secondary amide
C1=CC2=NC=NC2=NC1
C1=NC2=CCCNC2=N1
c1ccccc1.C1=NC2=CCCNC2=N1
HO-
null
null
null
CC(=O)OC(C)=O.CN(C)c1cc(N)ccc1C1=NC2=NC(=O)C=CC2=N1>>CC(=O)Nc1ccc(C2=NC3=CCC(=O)NC3=N2)c(N(C)C)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1cb12684952945bc8c6d959e38d194f3
COc1cc(OCc2ccccc2)ccc1C(=O)O.Nc1cnc(Cl)nc1N>>COc1cc(OCc2ccccc2)ccc1-c1nc2nc(Cl)ncc2[nH]1
ClC1=NC=C(C(=N1)N)N.COC1=C(C(=O)O)C=CC(=C1)OCC1=CC=CC=C1>>COC1=C(C=CC(=C1)OCC1=CC=CC=C1)C1=NC2=NC(=NC=C2N1)Cl
O=[C:17](O)[c:16]1[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15]1.[NH2:18][c:19]1[n:20][c:21]([Cl:22])[n:23][cH:24][c:25]1[NH2:26]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15][c:16]1-[c:17]1[n:18][c:19]2[n:20][c:...
COc1cc(OCc2ccccc2)ccc1C(=O)O.Nc1cnc(Cl)nc1N
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(Cl)ncc2[nH]1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
e7e72999864bfebc9719cc1ba22dd1cfcb4276023277f918059872106fb5d875
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
c1ccc(COc2ccc(-c3nc4ncncc4[nH]3)cc2)cc1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5](-[#8:6]):[c:7].[NH2;D1;+0:8]-[c:9]1:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:1-[NH2;D1;+0:15]>>[#8:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:8]:[c:9]2:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:2:[nH;D2;+0:15]:1):[c:3]:[c:4]
null
[]
null
null
null
null
Prepared analogously to Example 5 from 2-chloro-4,5-diaminopyrimidine and 2-methoxy-4-benzyloxy benzoic acid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1cncnc1
c1ncc2nc[nH]c2n1
c1ccccc1.c1ccccc1.c1ncc2nc[nH]c2n1
HO-
null
null
null
COc1cc(OCc2ccccc2)ccc1C(=O)O.Nc1cnc(Cl)nc1N>>COc1cc(OCc2ccccc2)ccc1-c1nc2nc(Cl)ncc2[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-18a6059416844248a8ba411c923fd244
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(Cl)ncc2[nH]1.[OH-]>>COc1cc(OCc2ccccc2)ccc1-c1nc2nc(OCc3ccccc3)ncc2[nH]1
[OH-].[K+].COC1=C(C=CC(=C1)OCC1=CC=CC=C1)C1=NC2=NC(=NC=C2N1)Cl>>COC1=C(C=CC(=C1)OCC1=CC=CC=C1)C1=NC2=NC(=NC=C2N1)OCC1=CC=CC=C1
Cl[c:21]1[n:20][c:19]2[n:18][c:17](-[c:16]3[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH2:7][c:8]4[cH:9][cH:10][cH:11][cH:12][cH:13]4)[cH:14][cH:15]3)[nH:33][c:32]2[cH:31][n:30]1.[OH-:22]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15][c:16]1-[c:17]1[n:18][c:19]2[n:20][c:21...
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(Cl)ncc2[nH]1.[OH-]
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(OCc3ccccc3)ncc2[nH]1
null
null
C(C1=CC=CC=C1)O
Aromatic Heterocycle Formation
OtherReaction
03a5998335ffb596af27d8aab0922ef9f1874f8bb28364cc91b165295431030a
a4840aa8bdfd6f728c7dfa6c00c462c0316cfea6c6529f068981467c19c289cb
c1ccc(COc2ccc(-c3nc4nc(OCc5ccccc5)ncc4[nH]3)cc2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](:[#7;a:4]):[c:5](:[#7;a:6]):[c:7]:[#7;a:8]:1.[OH-;D0:9]>>[#7;a:4]:[c:3]1:[#7;a:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[C:10]-[c:11]):[#7;a:8]:[c:7]:[c:5]:1:[#7;a:6]
null
[]
150
CELSIUS
null
null
An amount of 4.5 gm of powdered potassium hydroxide is dissolved in 70 ml of benzyl alcohol, and then 7.2 gm of 8-(2-methoxy-4-benzyloxy-phenyl)-2-chloro-purine are added. The mixture is heated to 150° C. for three hours, cooled, and filtered, the filtrate is mixed with ether, and the precipitate obtained is purified b...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Ether
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1.c1ccccc1
c1ccccc1.c1ccccc1.c1ncc2nc[nH]c2n1.c1ccccc1
null
C(C1=CC=CC=C1)O
150
null
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(Cl)ncc2[nH]1.[OH-]>C(C1=CC=CC=C1)O>COc1cc(OCc2ccccc2)ccc1-c1nc2nc(OCc3ccccc3)ncc2[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-31404deb6e244db4997f5de822a83ec7
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(OCc3ccccc3)ncc2[nH]1>>COc1cc(O)ccc1-c1nc2[nH]c(=O)ncc2[nH]1
O.[OH-].[Na+].COC1=C(C=CC(=C1)OCC1=CC=CC=C1)C1=NC2=NC(=NC=C2N1)OCC1=CC=CC=C1.[H][H]>>COC1=C(C=CC(=C1)O)C1=NC=2NC(N=CC2N1)=O
c1ccc(C[O:6][c:5]2[cH:4][c:3]([O:2][CH3:1])[c:9](-[c:10]3[n:11][c:12]4[n:13][c:14]([O:15]Cc5ccccc5)[n:16][cH:17][c:18]4[nH:19]3)[cH:8][cH:7]2)cc1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([OH:6])[cH:7][cH:8][c:9]1-[c:10]1[n:11][c:12]2[nH:13][c:14](=[O:15])[n:16][cH:17][c:18]2[nH:19]1
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(OCc3ccccc3)ncc2[nH]1
COc1cc(O)ccc1-c1nc2[nH]c(=O)ncc2[nH]1
null
[Pd]
C(C)O
Miscellaneous
OtherReaction
1f81964fd141b4682692af25f8f498cdff8427eef37d8c7223b62fbb154873cd
97b700253a515732e056bebfec7d29d55492867916f45a12199b66c78e6a3460
O=c1ncc2[nH]c(-c3ccccc3)nc2[nH]1
C(-[O;H0;D2;+0:1]-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[#7;a:8]:[c:9]:2:[n;H0;D2;+0:10]:1)-c1:c:c:c:c:c:1.[c:11]:[c:12](-[O;H0;D2;+0:13]-C-c1:c:c:c:c:c:1):[c:14]>>[O;H0;D1;+0:1]=[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[#7;a:8]:[c:9]:2:[nH;D2;+0:10]:1.[OH;D1;+0:13]-[c:12](:[c:11]):[c:14]
null
[]
null
null
null
null
Three grams of 8-(2-methoxy-4-benzyloxy-phenyl)-2-benzyloxypurine are dissolved in 100 ml of ethanol and hydrogenated in the presence of 1 gm of 20% palladium/charcoal for two hours at 50° C. with hydrogen at 5 bar. The catalyst is filtered off and washed with hot ethanol. The filtrates are evaporated, and the residue ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
c1ccccc1.c1ncc2nc[nH]c2n1.c1ccccc1
c1ncc2nc[nH]c2n1
c1ccccc1.c1ncc2nc[nH]c2n1
Other
[Pd].C(C)O
null
null
COc1cc(OCc2ccccc2)ccc1-c1nc2nc(OCc3ccccc3)ncc2[nH]1>[Pd].C(C)O>COc1cc(O)ccc1-c1nc2[nH]c(=O)ncc2[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f3d5d152d9a34241b654d7e6361c94bd
COc1ccc2[nH]c(-c3cc([N+](=O)[O-])c(N4C(=O)c5cc([N+](=O)[O-])ccc5C(C)(C)C4=O)cc3OC)nc2n1>>COc1ccc2[nH]c(-c3cc([N+](=O)[O-])c(N)cc3OC)nc2n1
COC1=C(C=C(C(=C1)N1C(C2=CC(=CC=C2C(C1=O)(C)C)[N+](=O)[O-])=O)[N+](=O)[O-])C=1NC=2C(=NC(=CC2)OC)N1.O.NN>>COC1=C(C=C(C(=C1)N)[N+](=O)[O-])C=1NC=2C(=NC(=CC2)OC)N1
CC1(C)C(=O)[N:16]([c:15]2[c:11]([N+:12](=[O:13])[O-:14])[cH:10][c:9](-[c:8]3[nH:7][c:6]4[cH:5][cH:4][c:3]([O:2][CH3:1])[n:23][c:22]4[n:21]3)[c:18]([O:19][CH3:20])[cH:17]2)C(=O)c2cc([N+](=O)[O-])ccc21>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][c:8](-[c:9]3[cH:10][c:11]([N+:12](=[O:13])[O-:14])[c:15]([NH2:16])[cH:17][c:...
COc1ccc2[nH]c(-c3cc([N+](=O)[O-])c(N4C(=O)c5cc([N+](=O)[O-])ccc5C(C)(C)C4=O)cc3OC)nc2n1
COc1ccc2[nH]c(-c3cc([N+](=O)[O-])c(N)cc3OC)nc2n1
null
null
C(C)(C)O
Reduction
OtherReaction
be2562881ed0428f65a7738b6bdfc3bb79b65abb4fb65b1370a2b2057af1cfc1
b30a79a18555d000c53b56d2dc755cec2380a4d4f2c61e07cb571d58c9e343b2
c1ccc(-c2nc3ncccc3[nH]2)cc1
C-C1(-C)-C(=O)-[N;H0;D3;+0:1](-[c:2](:[c:3]):[c:4])-C(=O)-c2:c:c(-[N+](=O)-[O-]):c:c:c:2-1>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
One half gram of 2-[2-methoxy-5-nitro-4-(4,4-dimethyl-7-nitro-2H,4H-isoquinolin-1,3-dione-2-yl)-phenyl]-5-methoxy-imidazo[4,5-b]pyridine is suspended in 10 ml of isopropanol, mixed with 0.5 ml of 80% hydrazine hydrate, and refluxed for 1.75 hours with stirring. The reaction mixture is concentrated by evaporation, the r...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide.Nitro group
Primary amine
c1ccc2c(c1)CC[NH]C2
null
c1cnc2nc[nH]c2c1.c1ccccc1
HO-
C(C)(C)O
null
null
COc1ccc2[nH]c(-c3cc([N+](=O)[O-])c(N4C(=O)c5cc([N+](=O)[O-])ccc5C(C)(C)C4=O)cc3OC)nc2n1>C(C)(C)O>COc1ccc2[nH]c(-c3cc([N+](=O)[O-])c(N)cc3OC)nc2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ac149cd0f9424d489ae8f7b30a738b68
COc1cc(N)ccc1C(=O)O.Nc1cn[nH]c(=O)c1N>>COc1cc(N)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
NC=1C(NN=CC1N)=O.COC1=C(C(=O)O)C=CC(=C1)N>>COC1=C(C=CC(=C1)N)C=1N=C2C(=CNNC2=O)N1
O=[C:10](O)[c:9]1[c:3]([O:2][CH3:1])[cH:4][c:5]([NH2:6])[cH:7][cH:8]1.[NH2:11][c:12]1[cH:13][n:14][nH:15][c:16](=[O:17])[c:18]1[NH2:19]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[cH:7][cH:8][c:9]1-[c:10]1[n:11][c:12]2[cH:13][nH:14][nH:15][c:16](=[O:17])[c:18]-2[n:19]1
COc1cc(N)ccc1C(=O)O.Nc1cn[nH]c(=O)c1N
COc1cc(N)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
96109e218d24fb14479892243bf7b2a5f05e386416ab27902ec0f9172e3e4a04
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
O=c1[nH][nH]cc2nc(-c3ccccc3)nc1-2
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5](-[#8:6]):[c:7].[NH2;D1;+0:8]-[c;H0;D3;+0:9]1:[c:10]:[n;H0;D2;+0:11]:[#7;a:12]:[c:13](=[O;D1;H0:14]):[c;H0;D3;+0:15]:1-[NH2;D1;+0:16]>>[#8:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:8]:[c;H0;D3;+0:9]2:[c:10]:[nH;D2;+0:11]:[#7;a:12]:[c:13](=[O;D1;H...
null
[]
null
null
null
null
Prepared analogously to Example 1 from 4,5-diamino-2H-pyridazin-3-one and 2-methoxy-4-amino-benzoic acid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1ccnnc1
c1nc2cnncc2[nH]1
c1ccccc1.c1nc2cnncc2[nH]1
HO-
null
null
null
COc1cc(N)ccc1C(=O)O.Nc1cn[nH]c(=O)c1N>>COc1cc(N)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-42289bdb3bd249a6a417937c8b9e169e
CCCOc1cc(SC)ccc1C(=O)O.COc1ccc(N)c(N)n1>>CCCOc1cc(SC)ccc1-c1nc2nc(OC)ccc2[nH]1
Cl.Cl.NC1=NC(=CC=C1N)OC.C(CC)OC1=C(C(=O)O)C=CC(=C1)SC>>Cl.C(CC)OC1=C(C=CC(=C1)SC)C=1NC=2C(=NC(=CC2)OC)N1
O=[C:13](O)[c:12]1[c:5]([O:4][CH2:3][CH2:2][CH3:1])[cH:6][c:7]([S:8][CH3:9])[cH:10][cH:11]1.[NH2:14][c:15]1[n:16][c:17]([O:18][CH3:19])[cH:20][cH:21][c:22]1[NH2:23]>>[CH3:1][CH2:2][CH2:3][O:4][c:5]1[cH:6][c:7]([S:8][CH3:9])[cH:10][cH:11][c:12]1-[c:13]1[n:14][c:15]2[n:16][c:17]([O:18][CH3:19])[cH:20][cH:21][c:22]2[nH:23...
CCCOc1cc(SC)ccc1C(=O)O.COc1ccc(N)c(N)n1
CCCOc1cc(SC)ccc1-c1nc2nc(OC)ccc2[nH]1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
a9a94f4ec3c76aeed619fd0cb32af4fac024911d5bce22bc3a860e6b5d9190bc
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
c1ccc(-c2nc3ncccc3[nH]2)cc1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5](-[#8:6]):[c:7].[NH2;D1;+0:8]-[c:9](:[#7;a:10]:[c:11]):[c:12](-[NH2;D1;+0:13]):[c:14]>>[#8:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:8]:[c:9](:[#7;a:10]:[c:11]):[c:12](:[c:14]):[nH;D2;+0:13]:1):[c:3]:[c:4]
null
[]
null
null
null
null
Prepared analogously to Example 5 from 2,3-diamino-6-methoxypyridine dihydrochloride and 2-propoxy-4-methylmercapto-benzoic acid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1ccncc1
c1cnc2[nH]cnc2c1
c1ccccc1.c1cnc2[nH]cnc2c1
HO-
null
null
null
CCCOc1cc(SC)ccc1C(=O)O.COc1ccc(N)c(N)n1>>CCCOc1cc(SC)ccc1-c1nc2nc(OC)ccc2[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8c990ec368674a9a9a4163d3dd8c972f
COc1cc(N)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.Cl>>COc1cc(Cl)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
COC1=C(C=CC(=C1)N)C=1N=C2C(=CNNC2=O)N1.N(=O)[O-].[Na+].Cl>>COC1=C(C=CC(=C1)Cl)C=1N=C2C(=CNNC2=O)N1
N[c:5]1[cH:4][c:3]([O:2][CH3:1])[c:9](-[c:10]2[n:11][c:12]3[cH:13][nH:14][nH:15][c:16](=[O:17])[c:18]-3[n:19]2)[cH:8][cH:7]1.[ClH:6]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([Cl:6])[cH:7][cH:8][c:9]1-[c:10]1[n:11][c:12]2[cH:13][nH:14][nH:15][c:16](=[O:17])[c:18]-2[n:19]1
COc1cc(N)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.Cl
COc1cc(Cl)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
null
null
O
Miscellaneous
OtherReaction
976fb3f0996203ccf639edc3dd63ebf792dabe502fe07eb66206f5ee630d746b
1129c10513c603d2647e51dd9713063aaf10bd8a364ed275b9b93c32624e3ba4
O=c1[nH][nH]cc2nc(-c3ccccc3)nc1-2
N-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[ClH;D0;+0:6]>>[Cl;H0;D1;+0:6]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
40
MINUTE
An amount of 1.05 gm of 2-(2-methoxy-4-amino-phenyl)-5H-imidazo[4,5-d]pyridazin-4-one is suspended in 20 ml of 6N hydrochloric acid. The suspension is cooled to 0° to -3° C., and 0.28 gm of sodium nitrite, dissolved in 2 ml of water, are added dropwise thereto. The mixture is stirred for a further 40 minutes and then h...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1.c1nc2cnncc2[nH]1
Other
O
null
0.666667
COc1cc(N)ccc1-c1nc2c[nH][nH]c(=O)c-2n1.Cl>O>COc1cc(Cl)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c7a439da589547019f39681016779e11
COc1cc(C#N)ccc1-c1nc2[nH]c(=O)ncc2[nH]1.O=S(=O)(O)O>>COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)ncc2[nH]1
COC1=C(C=CC(=C1)C#N)C1=NC=2NC(N=CC2N1)=O.S(O)(O)(=O)=O>>COC1=C(C=CC(=C1)C(=O)N)C1=NC=2NC(N=CC2N1)=O
[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]#[N:7])[cH:9][cH:10][c:11]1-[c:12]1[n:13][c:14]2[nH:15][c:16](=[O:17])[n:18][cH:19][c:20]2[nH:21]1.O=S(=O)(O)[OH:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([NH2:7])=[O:8])[cH:9][cH:10][c:11]1-[c:12]1[n:13][c:14]2[nH:15][c:16](=[O:17])[n:18][cH:19][c:20]2[nH:21]1
COc1cc(C#N)ccc1-c1nc2[nH]c(=O)ncc2[nH]1.O=S(=O)(O)O
COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)ncc2[nH]1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1d1793919e847ed86dcb16487e62464531560dbf4782f9a5875bfe7e0477a3ec
d6f9d146e8ef95e62f1a3ab55a7e3b4ceec8856a5f71b6dccd4ad850f945b658
O=c1ncc2[nH]c(-c3ccccc3)nc2[nH]1
O-S(=O)(=O)-[OH;D1;+0:1].[N;H0;D1;+0:2]#[C;H0;D2;+0:3]-[c:4](:[c:5]):[c:6]>>[NH2;D1;+0:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:1])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Prepared by partial saponification of 8-(2-methoxy-4-cyanophenyl)-3H-purin-2-one with concentrated sulfuric acid at ambient temperature. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amide
null
null
c1ccccc1.c1ncc2nc[nH]c2n1
Other
null
null
null
COc1cc(C#N)ccc1-c1nc2[nH]c(=O)ncc2[nH]1.O=S(=O)(O)O>>COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)ncc2[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6a823073ab7c4f51901f88aec89eb947
COc1cc(C(=O)O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1.N>>COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1
C(C)(=O)O.COC1=C(C=CC(=C1)C(=O)O)C1=NC=2NC(NC(C2N1)=O)=O.N.O>>COC1=C(C=CC(=C1)C(=O)N)C1=NC=2NC(NC(C2N1)=O)=O
O[C:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:11](-[c:12]2[n:13][c:14]3[nH:15][c:16](=[O:17])[nH:18][c:19](=[O:20])[c:21]3[nH:22]2)[cH:10][cH:9]1)=[O:8].[NH3:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([NH2:7])=[O:8])[cH:9][cH:10][c:11]1-[c:12]1[n:13][c:14]2[nH:15][c:16](=[O:17])[nH:18][c:19](=[O:20])[c:21]2[nH:22]1
COc1cc(C(=O)O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1.N
COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1
null
CN(C=O)C
CN(C=O)C.S(=O)(Cl)Cl
Acylation
Carboxylic acid to amide conversion
1283aef55d7ee699f097a8e5267689198c76ba671644401547f902657820236d
cb0a71c3fb37a76e96fbd81aae6f95a28398a03d1ad2c8e877085e735efb98f1
O=c1[nH]c(=O)c2[nH]c(-c3ccccc3)nc2[nH]1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH3;D0;+0:6]>>[NH2;D1;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A quantity of 2.3 gm of 8-(2-methoxy-4-carboxy-phenyl)-1H,-3H-purin-2,6-dione are refluxed for one hour in 50 ml of thionyl chloride with the addition of 1 drop of dimethylformamide. The excess thionyl chloride is drawn off, and the residue is stirred for 16 hours at ambient temperature with a solution of ammonia in di...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary amide
null
null
c1ccccc1.c1ncc2nc[nH]c2n1
HO-
CN(C=O)C.CN(C=O)C.S(=O)(Cl)Cl
null
null
COc1cc(C(=O)O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1.N>CN(C=O)C.CN(C=O)C.S(=O)(Cl)Cl>COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-659dfef79a1345f9a27aa0d9cf9068c9
COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1>>COc1cc(C#N)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1
COC1=C(C=CC(=C1)C(=O)N)C1=NC=2NC(NC(C2N1)=O)=O>>COC1=C(C=CC(=C1)C#N)C1=NC=2NC(NC(C2N1)=O)=O
O=[C:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:10](-[c:11]2[n:12][c:13]3[nH:14][c:15](=[O:16])[nH:17][c:18](=[O:19])[c:20]3[nH:21]2)[cH:9][cH:8]1)[NH2:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]#[N:7])[cH:8][cH:9][c:10]1-[c:11]1[n:12][c:13]2[nH:14][c:15](=[O:16])[nH:17][c:18](=[O:19])[c:20]2[nH:21]1
COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1
COc1cc(C#N)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1
null
null
P(=O)(Cl)(Cl)Cl
Miscellaneous
OtherReaction
5094e9d814705bbdc421edbf7e9198e499e70e93916e2cec6eefbc82d1ba5440
32b9893bcb5223559a9d02852f8392cf6473aacfb044a52ba4e9cb9c29edb170
O=c1[nH]c(=O)c2[nH]c(-c3ccccc3)nc2[nH]1
O=[C;H0;D3;+0:1](-[NH2;D1;+0:2])-[c:3](:[c:4]):[c:5]>>[N;H0;D1;+0:2]#[C;H0;D2;+0:1]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
Prepared by boiling 0.7 gm of 8-(2-methoxy-4-aminocarbonylphenyl)-1H,3H-purin-2,6-dione in 10 ml of phosphorus oxychloride for 24 hours. The compound crystallizes as the hemihydrate. Conditions: See reaction.notes.procedure_details. Workup: Prepared; for 24 hours; The compound crystallizes as the hemihydrate
10.6084/m9.figshare.5104873.v1
null
Primary amide
Nitrile
null
null
c1ccccc1.c1ncc2nc[nH]c2n1
HO-
P(=O)(Cl)(Cl)Cl
null
null
COc1cc(C(N)=O)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1>P(=O)(Cl)(Cl)Cl>COc1cc(C#N)ccc1-c1nc2[nH]c(=O)[nH]c(=O)c2[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-07ba6e5f908b4ae49ca949e471af2338
CN.COc1ncc2[nH]c(-c3cc(S(=O)(=O)Cl)c(Cl)cc3OC)nc2n1>>CNS(=O)(=O)c1cc(-c2nc3nc(OC)ncc3[nH]2)c(OC)cc1Cl
COC1=NC=C2NC(=NC2=N1)C1=C(C=C(C(=C1)S(=O)(=O)Cl)Cl)OC.CN>>COC1=NC=C2NC(=NC2=N1)C1=C(C=C(C(=C1)S(=O)(=O)NC)Cl)OC
[CH3:1][NH2:2].Cl[S:3](=[O:4])(=[O:5])[c:6]1[cH:7][c:8](-[c:9]2[n:10][c:11]3[n:12][c:13]([O:14][CH3:15])[n:16][cH:17][c:18]3[nH:19]2)[c:20]([O:21][CH3:22])[cH:23][c:24]1[Cl:25]>>[CH3:1][NH:2][S:3](=[O:4])(=[O:5])[c:6]1[cH:7][c:8](-[c:9]2[n:10][c:11]3[n:12][c:13]([O:14][CH3:15])[n:16][cH:17][c:18]3[nH:19]2)[c:20]([O:21]...
CN.COc1ncc2[nH]c(-c3cc(S(=O)(=O)Cl)c(Cl)cc3OC)nc2n1
CNS(=O)(=O)c1cc(-c2nc3nc(OC)ncc3[nH]2)c(OC)cc1Cl
null
null
null
Acylation
Sulfonamide synthesis (Schotten-Baumann) primary amine
4c44ef6d7646f6ef25dd125d2c32c713d8dcae7c603407faa5f0fb810631670e
8fce8115d8a725afa92eb3910ded29d4c852e5133eba78a425054f41f7142603
c1ccc(-c2nc3ncncc3[nH]2)cc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C;D1;H3:7]-[NH2;D1;+0:8]>>[C;D1;H3:7]-[NH;D2;+0:8]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Prepared analogously to Example 11 from 2-methoxy-8-(2-methoxy-4-chloro-5-chlorosulfonyl-phenyl)-purine and aqueous methylamine solution. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccccc1.c1ncc2nc[nH]c2n1
HCl
null
null
null
CN.COc1ncc2[nH]c(-c3cc(S(=O)(=O)Cl)c(Cl)cc3OC)nc2n1>>CNS(=O)(=O)c1cc(-c2nc3nc(OC)ncc3[nH]2)c(OC)cc1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-75a79419a651472b8e61ac37752ac50b
CNC.COc1cc(S(=O)(=O)Cl)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C>>COc1cc(S(=O)(=O)N(C)C)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C
CN1C(N(C=2N=C(NC2C1=O)C1=C(C=C(C=C1)S(=O)(=O)Cl)OC)C)=O.CNC>>CN1C(N(C=2N=C(NC2C1=O)C1=C(C=C(C=C1)S(=O)(=O)N(C)C)OC)C)=O
[NH:9]([CH3:10])[CH3:11].Cl[S:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:14](-[c:15]2[n:16][c:17]3[c:18]([nH:19]2)[c:20](=[O:21])[n:22]([CH3:23])[c:24](=[O:25])[n:26]3[CH3:27])[cH:13][cH:12]1)(=[O:7])=[O:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([S:6](=[O:7])(=[O:8])[N:9]([CH3:10])[CH3:11])[cH:12][cH:13][c:14]1-[c:15]1[n:16][c:17]2[...
CNC.COc1cc(S(=O)(=O)Cl)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C
COc1cc(S(=O)(=O)N(C)C)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C
null
null
null
Acylation
Sulfonamide synthesis (Schotten-Baumann) secondary amine
abeb6d9a0c70fe5baef0a8e555c2cd55ac2317f763ce7a0831775db7a04777d8
b7aca5a5d690b0846685a854bc946849e1041bfc3965161290b5ffb2821af09e
O=c1[nH]c(=O)c2[nH]c(-c3ccccc3)nc2[nH]1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C;D1;H3:7]-[NH;D2;+0:8]-[C;D1;H3:9]>>[C;D1;H3:7]-[N;H0;D3;+0:8](-[C;D1;H3:9])-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Prepared analogously to Example 11 from 1,3-dimethyl-8-(2-methoxy-4-chlorosulfonyl-phenyl)-1H,3H-purin-2,6-dione and dimethylamine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Sulfonyl halide
Tertiary amine
null
null
c1ccccc1.c1ncc2nc[nH]c2n1
HCl
null
null
null
CNC.COc1cc(S(=O)(=O)Cl)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C>>COc1cc(S(=O)(=O)N(C)C)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-66ffec08e9f549e2bbc01b436836183e
COc1cc(OCc2ccccc2)ccc1C(=O)O.Cn1c(N)c(N)c(=O)n(C)c1=O>>COc1cc(OCc2ccccc2)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C
CN1C(N(C(=C(C1=O)N)N)C)=O.COC1=C(C(=O)O)C=CC(=C1)OCC1=CC=CC=C1>>CN1C(N(C=2N=C(NC2C1=O)C1=C(C=C(C=C1)OCC1=CC=CC=C1)OC)C)=O
O=[C:17](O)[c:16]1[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15]1.[NH2:18][c:19]1[c:20]([NH2:21])[c:22](=[O:23])[n:24]([CH3:25])[c:26](=[O:27])[n:28]1[CH3:29]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15][c:16]1-[...
COc1cc(OCc2ccccc2)ccc1C(=O)O.Cn1c(N)c(N)c(=O)n(C)c1=O
COc1cc(OCc2ccccc2)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C
null
null
null
Aromatic Heterocycle Formation
OtherReaction
e7e72999864bfebc9719cc1ba22dd1cfcb4276023277f918059872106fb5d875
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
O=c1[nH]c(=O)c2[nH]c(-c3ccc(OCc4ccccc4)cc3)nc2[nH]1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5](-[#8:6]):[c:7].[C;D1;H3:8]-[#7;a:9]1:[c:10]:[#7;a:11](-[C;D1;H3:12]):[c:13](-[NH2;D1;+0:14]):[c:15](-[NH2;D1;+0:16]):[c:17]:1=[O;D1;H0:18]>>[#8:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:14]:[c:13]2:[#7;a:11](-[C;D1;H3:12]):[c:10]:[#7;a:9](-[C;D1...
null
[]
null
null
null
null
Prepared analogously to Example 14 from 1,3-dimethyl-4,5-diamino-1H,3H-pyrimidin-2,6-dione and 2-methoxy-4-benzyloxybenzoic acid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1cncnc1
c1ncc2nc[nH]c2n1
c1ccccc1.c1ccccc1.c1ncc2nc[nH]c2n1
HO-
null
null
null
COc1cc(OCc2ccccc2)ccc1C(=O)O.Cn1c(N)c(N)c(=O)n(C)c1=O>>COc1cc(OCc2ccccc2)ccc1-c1nc2c([nH]1)c(=O)n(C)c(=O)n2C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-812dd49b20de4a6eb087670e6fda7435
COc1cc(OC)c(C(=O)O)cc1Br.Nc1ncnc(Cl)c1N>>COc1cc(OC)c(-c2nc3ncnc(Cl)c3[nH]2)cc1Br
NC1=NC=NC(=C1N)Cl.COC1=C(C(=O)O)C=C(C(=C1)OC)Br>>ClC1=C2NC(=NC2=NC=N1)C1=C(C=C(C(=C1)Br)OC)OC
O=[C:9](O)[c:8]1[c:5]([O:6][CH3:7])[cH:4][c:3]([O:2][CH3:1])[c:20]([Br:21])[cH:19]1.[NH2:10][c:11]1[n:12][cH:13][n:14][c:15]([Cl:16])[c:17]1[NH2:18]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[c:8](-[c:9]2[n:10][c:11]3[n:12][cH:13][n:14][c:15]([Cl:16])[c:17]3[nH:18]2)[cH:19][c:20]1[Br:21]
COc1cc(OC)c(C(=O)O)cc1Br.Nc1ncnc(Cl)c1N
COc1cc(OC)c(-c2nc3ncnc(Cl)c3[nH]2)cc1Br
null
null
null
Aromatic Heterocycle Formation
OtherReaction
e7e72999864bfebc9719cc1ba22dd1cfcb4276023277f918059872106fb5d875
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
c1ccc(-c2nc3ncncc3[nH]2)cc1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5](-[#8:6]):[c:7].[Cl;D1;H0:8]-[c:9]1:[#7;a:10]:[c:11]:[#7;a:12]:[c:13](-[NH2;D1;+0:14]):[c:15]:1-[NH2;D1;+0:16]>>[#8:6]-[c:5](:[c:7]):[c;H0;D3;+0:2](-[c;H0;D3;+0:1]1:[n;H0;D2;+0:14]:[c:13]2:[#7;a:12]:[c:11]:[#7;a:10]:[c:9](-[Cl;D1;H0:8]):[c:15]:2:[nH;D2;+0:16]:1):[c...
null
[]
null
null
null
null
Prepared analogously to Example 14 from 4,5-diamino-6-chloropyrimidine and 2,4-dimethoxy-5-bromo-benzoic acid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1cncnc1
c1ncc2nc[nH]c2n1
c1ccccc1.c1ncc2nc[nH]c2n1
HO-
null
null
null
COc1cc(OC)c(C(=O)O)cc1Br.Nc1ncnc(Cl)c1N>>COc1cc(OC)c(-c2nc3ncnc(Cl)c3[nH]2)cc1Br
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1bcc2a3d16bb4766b58a295e2fc2fc6b
CC(Cl)Cl.COc1cc(C#N)ccc1C(=O)O.COc1nccc(N)c1N>>COC(=O)c1ccc(C2=NC3=CCNC(=O)C3=N2)c(OC)c1.Cl
COC1=NC=CC(=C1N)N.COC1=C(C(=O)O)C=CC(=C1)C#N.ClC(C)Cl.C(C)O>>Cl.COC1=C(C=CC(=C1)C(=O)OC)C1=NC=2C(C(NCC2)=O)=N1
CC(Cl)[Cl:23].N#[C:3][c:5]1[cH:6][cH:7][c:8]([C:9]([OH:2])=[O:4])[c:19]([O:20][CH3:21])[cH:22]1.[CH3:1][O:16][c:15]1[n:14][cH:13][cH:12][c:11]([NH2:10])[c:17]1[NH2:18]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([C:9]2=[N:10][C:11]3=[CH:12][CH2:13][NH:14][C:15](=[O:16])[C:17]3=[N:18]2)[c:19]([O:20][CH3:21])[cH:22...
CC(Cl)Cl.COc1cc(C#N)ccc1C(=O)O.COc1nccc(N)c1N
COC(=O)c1ccc(C2=NC3=CCNC(=O)C3=N2)c(OC)c1.Cl
null
null
null
Acylation
OtherReaction
59e74931176ca11a8b3b012f0820490ff7c59ac2f16614b65abe297b7bd42286
4e50644f8d1e19addfaa3e366597a746b1101627eaa0a56d85c5e91fb60a0ee9
O=C1NCC=C2N=C(c3ccccc3)N=C12
C-C(-Cl)-[Cl;H0;D1;+0:1].N#[C;H0;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[c:6](-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[OH;D1;+0:9]):[c:10]:[c:11]:1.[CH3;D1;+0:12]-[O;H0;D2;+0:13]-[c;H0;D3;+0:14]1:[n;H0;D2;+0:15]:[cH;D2;+0:16]:[cH;D2;+0:17]:[c;H0;D3;+0:18](-[NH2;D1;+0:19]):[c;H0;D3;+0:20]:1-[NH2;D1;+0:21]>>[CH3;D1;+0:12]-[O;H0;D2;+0:9]-[...
null
[]
null
null
null
null
Prepared analogously to Example 1 from 2-methoxy-3,4-diaminopyridine and 2-methoxy-4-cyano-benzoic acid. The product mixture obtained is digested with dichloroethane/ethanol (3:1). The undissolved material is filtered off, and the solution is evaporated and boiled with methanolic hydrochloric acid. On cooling, the prod...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Carboxylic acid.Ether.Nitrile.Primary amine.Primary amine
Ester.Substituted imine.Secondary amide
c1ccncc1
C1=NC2=CCNCC2=N1
c1ccccc1.C1=NC2=CCNCC2=N1
HCl
null
null
null
CC(Cl)Cl.COc1cc(C#N)ccc1C(=O)O.COc1nccc(N)c1N>>COC(=O)c1ccc(C2=NC3=CCNC(=O)C3=N2)c(OC)c1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e60e9f255ff64e7190309e64e3d68715
CN.COc1cc(S(=O)(=O)Cl)ccc1-c1nc2c[nH][nH]c(=O)c-2n1>>CNS(=O)(=O)c1ccc(-c2nc3c[nH][nH]c(=O)c-3n2)c(OC)c1
COC1=C(C=CC(=C1)S(=O)(=O)Cl)C=1N=C2C(=CNNC2=O)N1.CN>>COC1=C(C=CC(=C1)S(=O)(=O)NC)C=1N=C2C(=CNNC2=O)N1
[CH3:1][NH2:2].Cl[S:3](=[O:4])(=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[n:11][c:12]3[cH:13][nH:14][nH:15][c:16](=[O:17])[c:18]-3[n:19]2)[c:20]([O:21][CH3:22])[cH:23]1>>[CH3:1][NH:2][S:3](=[O:4])(=[O:5])[c:6]1[cH:7][cH:8][c:9](-[c:10]2[n:11][c:12]3[cH:13][nH:14][nH:15][c:16](=[O:17])[c:18]-3[n:19]2)[c:20]([O:21][CH3:22])...
CN.COc1cc(S(=O)(=O)Cl)ccc1-c1nc2c[nH][nH]c(=O)c-2n1
CNS(=O)(=O)c1ccc(-c2nc3c[nH][nH]c(=O)c-3n2)c(OC)c1
null
null
null
Acylation
Sulfonamide synthesis (Schotten-Baumann) primary amine
4c44ef6d7646f6ef25dd125d2c32c713d8dcae7c603407faa5f0fb810631670e
8fce8115d8a725afa92eb3910ded29d4c852e5133eba78a425054f41f7142603
O=c1[nH][nH]cc2nc(-c3ccccc3)nc1-2
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C;D1;H3:7]-[NH2;D1;+0:8]>>[C;D1;H3:7]-[NH;D2;+0:8]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Prepared analogously to Example 11 from 2-(2-methoxy-4-chlorosulfonyl-phenyl)-5-H-imidazo[4,5-d]pyridazin-4-one and aqueous methylamine solution Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccccc1.c1nc2cnncc2[nH]1
HCl
null
null
null
CN.COc1cc(S(=O)(=O)Cl)ccc1-c1nc2c[nH][nH]c(=O)c-2n1>>CNS(=O)(=O)c1ccc(-c2nc3c[nH][nH]c(=O)c-3n2)c(OC)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b9ccee3c2bf64ab8b2bb177fb8f8050b
BrCc1ccc2ccccc2c1.O=C(NC(=O)c1ccccc1)NC1CCNCC1>>O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1
O.C(C1=CC=CC=C1)(=O)NC(NC1CCNCC1)=O.BrCC1=CC2=CC=CC=C2C=C1.C(C)N(CC)CC>>C(C1=CC=CC=C1)(=O)NC(=O)NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1
Br[CH2:17][c:18]1[cH:19][cH:20][c:21]2[cH:22][cH:23][cH:24][cH:25][c:26]2[cH:27]1.[O:1]=[C:2]([NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)[NH:12][CH:13]1[CH2:14][CH2:15][NH:16][CH2:28][CH2:29]1>>[O:1]=[C:2]([NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)[NH:12][CH:13]1[CH2:14][CH2:15][N:16]([...
BrCc1ccc2ccccc2c1.O=C(NC(=O)c1ccccc1)NC1CCNCC1
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0240b8450ff2c489d02f5f0d90bc953079d7a3ab239d35a03f26392fc248b4ef
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:8]-[C:9]
null
[]
null
null
null
null
4-Benzoylureidopiperidine (1.28 g, 0.005 m), 2-(bromomethyl)naphthalene (1.1 g, 0.005 m) and triethylamine (0.6 g, 0.006 m) in dimethylformamide (25 cm3) were stirred at room temperature for 23 hours. Water was added and the precipitated solid filtered off and washed well with water. The solid was suspended in warm eth...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNCC1
C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccc2ccccc2c1
HBr
CN(C=O)C
null
null
BrCc1ccc2ccccc2c1.O=C(NC(=O)c1ccccc1)NC1CCNCC1>CN(C=O)C>O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6c695e0fc6704fb0ad8fd2c49b74c803
ClCc1cccc2ccccc12.O=C(NC(=O)c1ccccc1)NC1CCNCC1>>O=C(NC(=O)c1ccccc1)NC1CCN(Cc2cccc3ccccc23)CC1
O.ClCC1=CC=CC2=CC=CC=C12.C(C1=CC=CC=C1)(=O)NC(NC1CCNCC1)=O.C(C)N(CC)CC>>C(C1=CC=CC=C1)(=O)NC(=O)NC1CCN(CC1)CC1=CC=CC2=CC=CC=C12
Cl[CH2:17][c:18]1[cH:19][cH:20][cH:21][c:22]2[cH:23][cH:24][cH:25][cH:26][c:27]12.[O:1]=[C:2]([NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)[NH:12][CH:13]1[CH2:14][CH2:15][NH:16][CH2:28][CH2:29]1>>[O:1]=[C:2]([NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)[NH:12][CH:13]1[CH2:14][CH2:15][N:16]([...
ClCc1cccc2ccccc12.O=C(NC(=O)c1ccccc1)NC1CCNCC1
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2cccc3ccccc23)CC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0240b8450ff2c489d02f5f0d90bc953079d7a3ab239d35a03f26392fc248b4ef
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2cccc3ccccc23)CC1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:8]-[C:9]
null
[]
null
null
null
null
1-Chloromethylnaphthalene (0.88 g, 0.005 m), 4-benzoylureidopiperidine (1.28 g, 0.005 m) and triethylamine (0.6 g) in dimethylformamide (25 cm3) were stirred at room temperature for 24 hours. Water was added and the precipitated solid filtered off. The solid was suspended in isopropylalcohol and acidified with ethanoli...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNCC1
C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccc2ccccc2c1
HCl
CN(C=O)C
null
null
ClCc1cccc2ccccc12.O=C(NC(=O)c1ccccc1)NC1CCNCC1>CN(C=O)C>O=C(NC(=O)c1ccccc1)NC1CCN(Cc2cccc3ccccc23)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-35a5faba84b5422a9a52f12017701c29
CC(C)c1ccc(CCl)cc1.O=C(NC(=O)c1ccccc1)NC1CCNCC1>>CC(C)c1ccc(CN2CCC(NC(=O)NC(=O)c3ccccc3)CC2)cc1
O.C(C)(C)C1=CC=C(CCl)C=C1.C(C1=CC=CC=C1)(=O)NC(NC1CCNCC1)=O.C(C)N(CC)CC>>C(C1=CC=CC=C1)(=O)NC(=O)NC1CCN(CC1)CC1=CC=C(C=C1)C(C)C
Cl[CH2:8][c:7]1[cH:6][cH:5][c:4]([CH:2]([CH3:1])[CH3:3])[cH:28][cH:27]1.[NH:9]1[CH2:10][CH2:11][CH:12]([NH:13][C:14](=[O:15])[NH:16][C:17](=[O:18])[c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[CH2:25][CH2:26]1>>[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7]([CH2:8][N:9]2[CH2:10][CH2:11][CH:12]([NH:13][C:14](=[O:15])[NH:1...
CC(C)c1ccc(CCl)cc1.O=C(NC(=O)c1ccccc1)NC1CCNCC1
CC(C)c1ccc(CN2CCC(NC(=O)NC(=O)c3ccccc3)CC2)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0240b8450ff2c489d02f5f0d90bc953079d7a3ab239d35a03f26392fc248b4ef
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:8]-[C:9]
null
[]
null
null
null
null
4-Isopropylbenzyl chloride (0.84 g, 0.005 m), 4-benzoylureidopiperidine (1.28 g, 0.005 m) and triethylamine (0.6 g) in dimethylformamide (25 cm3) were stirred at room temperature for 24 hours. Water was added and the precipitated solid filtered off. The solid was suspended in isopropylalcohol and acidified with ethanol...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNCC1
C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccccc1
HCl
CN(C=O)C
null
null
CC(C)c1ccc(CCl)cc1.O=C(NC(=O)c1ccccc1)NC1CCNCC1>CN(C=O)C>CC(C)c1ccc(CN2CCC(NC(=O)NC(=O)c3ccccc3)CC2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-229294ec89824edba85133b93bb6a360
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2cccc([N+](=O)[O-])c2)CC1>>Nc1cccc(CN2CCC(NC(=O)NC(=O)c3ccccc3)CC2)c1
C(C1=CC=CC=C1)(=O)NC(=O)NC1CCN(CC1)CC1=CC(=CC=C1)[N+](=O)[O-].[H][H]>>C(C1=CC=CC=C1)(=O)NC(=O)NC1CCN(CC1)CC1=CC(=CC=C1)N
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][cH:5][c:6]([CH2:7][N:8]2[CH2:9][CH2:10][CH:11]([NH:12][C:13](=[O:14])[NH:15][C:16](=[O:17])[c:18]3[cH:19][cH:20][cH:21][cH:22][cH:23]3)[CH2:24][CH2:25]2)[cH:26]1>>[NH2:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH2:7][N:8]2[CH2:9][CH2:10][CH:11]([NH:12][C:13](=[O:14])[NH:15][C:16](=[O:17])[c:18]3...
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2cccc([N+](=O)[O-])c2)CC1
Nc1cccc(CN2CCC(NC(=O)NC(=O)c3ccccc3)CC2)c1
null
[Pd]
null
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
46.1
[{"value": 46.1, "product": "C(C1=CC=CC=C1)(=O)NC(=O)NC1CCN(CC1)CC1=CC(=CC=C1)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1-Benzoyl-3-[1-(3-nitrobenzyl)piperid-4-yl]urea 4.47 g (from Example 13) was hydrogenated with 5% Pd/C (0.5 g) at atmospheric pressure and room temperature until no more hydrogen was taken up. The catalyst was filtered and the filtrate evaporated. The residue was dissolved in water and basified with 0.880 ammonia. The ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1
Other
[Pd]
null
null
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2cccc([N+](=O)[O-])c2)CC1>[Pd]>Nc1cccc(CN2CCC(NC(=O)NC(=O)c3ccccc3)CC2)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-abd517df60204610939cf68a6c24b096
NC1CCN(Cc2ccc3ccccc3c2)CC1.O=C(N=C=S)c1ccccc1>>O=C(NC(=S)NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1
NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1.C(C1=CC=CC=C1)(=O)N=C=S>>C(C1=CC=CC=C1)(=O)NC(=S)NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1
[NH2:6][CH:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[cH:21]2)[CH2:22][CH2:23]1.[O:1]=[C:2]([N:3]=[C:4]=[S:5])[c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1>>[O:1]=[C:2]([NH:3][C:4](=[S:5])[NH:6][CH:7]1[CH2:8][CH2:9][N:10]([CH2:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:...
NC1CCN(Cc2ccc3ccccc3c2)CC1.O=C(N=C=S)c1ccccc1
O=C(NC(=S)NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
thiourea
9037f368cdf8e91fcd9f93f4d9cf27991f85fa921c9d19c7875d3a77561f439b
0fbf3d6c8cd704ac451c2cf111f32090de5e76a9d41cce326e212c758f4ed46f
O=C(NC(=S)NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1
[C:1]-[C:2](-[NH2;D1;+0:3])-[C:4].[O;D1;H0:5]=[C:6](-[c:7])-[N;H0;D2;+0:8]=[C;H0;D2;+0:9]=[S;D1;H0:10]>>[C:1]-[C:2](-[NH;D2;+0:3]-[C;H0;D3;+0:9](=[S;D1;H0:10])-[NH;D2;+0:8]-[C:6](=[O;D1;H0:5])-[c:7])-[C:4]
null
[]
null
null
null
null
4-Amino-1-(naphth-2-ylmethyl)piperidine (1.0 g, 0.0042 m) and benzoylisothiocyanate (0.69 g, 0.0042 m) in toluene (120 cm3) was stirred at room temperature for 6 hours. The solvent was evaporated and the gum dissolved in isopropyl alcohol and acidified with ethanolic HCl. The solvent was evaporated and the residue diss...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Isothiocyanate
Thiourea
null
null
C1CC[NH]CC1.c1ccc2ccccc2c1.c1ccccc1
null
C1(=CC=CC=C1)C
null
null
NC1CCN(Cc2ccc3ccccc3c2)CC1.O=C(N=C=S)c1ccccc1>C1(=CC=CC=C1)C>O=C(NC(=S)NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b9261355c50f45a3ac126c2d60770352
NC(=O)NC(=O)c1cccs1.NC1CCN(Cc2ccc3ccccc3c2)CC1>>O=C(NC(=O)c1cccs1)NC1CCN(Cc2ccc3ccccc3c2)CC1
NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1.C(=O)(C1=CC=CS1)NC(=O)N>>C1=C(C=CC2=CC=CC=C12)CN1CCC(CC1)NC(=O)NC(=O)C1=CC=CS1
N[C:2](=[O:1])[NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][s:10]1.[NH2:11][CH:12]1[CH2:13][CH2:14][N:15]([CH2:16][c:17]2[cH:18][cH:19][c:20]3[cH:21][cH:22][cH:23][cH:24][c:25]3[cH:26]2)[CH2:27][CH2:28]1>>[O:1]=[C:2]([NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][s:10]1)[NH:11][CH:12]1[CH2:13][CH2:14][N:15]([CH2:16][c:17]2[...
NC(=O)NC(=O)c1cccs1.NC1CCN(Cc2ccc3ccccc3c2)CC1
O=C(NC(=O)c1cccs1)NC1CCN(Cc2ccc3ccccc3c2)CC1
null
null
N1=CC=CC=C1
Acylation
OtherReaction
ee88c85dd0298c7570ff891f0a63d5ba74c10c53d8b511286ccf5ed6d0220803
85c12bcb6a376caef505909a73a2892ca05bfb0340f2644fc218cdee9c5187ab
O=C(NC(=O)c1cccs1)NC1CCN(Cc2ccc3ccccc3c2)CC1
N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3]-[C:4](=[O;D1;H0:5])-[c:6]:[#16;a:7].[C:8]-[C:9](-[NH2;D1;+0:10])-[C:11]>>[#16;a:7]:[c:6]-[C:4](=[O;D1;H0:5])-[#7:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9](-[C:8])-[C:11]
null
[]
null
null
null
null
4-Amino-1-(naphth-2-ylmethyl)piperidine (1.0 g, 0.0047 m) and 1-(then-2-oyl)urea (0.65 g, 0.0042 m) in pyridine (5 cm3) was refluxed for 9.5 hours. The solvent was evaporated, water added, and the precipitated title compound filtered and washed well with water. This was recrystallised from ethanol, converted to the hyd...
10.6084/m9.figshare.5104873.v1
null
Urea.Unsubstituted dicarboximide.Primary amine
Urea
null
null
c1ccsc1.C1CC[NH]CC1.c1ccc2ccccc2c1
Other
N1=CC=CC=C1
null
null
NC(=O)NC(=O)c1cccs1.NC1CCN(Cc2ccc3ccccc3c2)CC1>N1=CC=CC=C1>O=C(NC(=O)c1cccs1)NC1CCN(Cc2ccc3ccccc3c2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f835042249204abe88c806390379a6a4
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1>>NC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1
C(C1=CC=CC=C1)(=O)NC(=O)NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1>>C1=C(C=CC2=CC=CC=C12)CN1CCC(CC1)NC(=O)N
O=C(c1ccccc1)[NH:1][C:2](=[O:3])[NH:4][CH:5]1[CH2:6][CH2:7][N:8]([CH2:9][c:10]2[cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]3[cH:19]2)[CH2:20][CH2:21]1>>[NH2:1][C:2](=[O:3])[NH:4][CH:5]1[CH2:6][CH2:7][N:8]([CH2:9][c:10]2[cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]3[cH:19]2)[CH2:20][CH2:21]1
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1
NC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1
null
null
[OH-].[Na+]
Reduction
Hydrogenolysis of amides/imides/carbamates
cef6d282debf67869b4ff7117425f8a9682536ad0cfda16621a004d70e3c594b
bd99c049ef764d527dcd2e7b23a61d65d845df2ddd7efd5a187ffda1670906e4
c1ccc2cc(CN3CCCCC3)ccc2c1
O=C(-[NH;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5])-c1:c:c:c:c:c:1>>[C:5]-[#7:4]-[C:2](-[NH2;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
null
null
1-Benzoyl-3-[1-(naphth-2-ylmethyl)piperid-4-yl]urea (prepared acccording to Example 1) is hydrolysed by refluxing in 2N sodium hydroxide to give [1-(naphth-2-ylmethyl)piperid-4-yl]urea(m.p. 183°-5° C.). The product is acylated by reaction with 4-methoxybenzoyl chloride to give the title compound, m.p. of HCL, quarterhy...
10.6084/m9.figshare.5104873.v1
null
Urea.Unsubstituted dicarboximide
Urea
c1ccccc1
null
C1CC[NH]CC1.c1ccc2ccccc2c1
HO-
[OH-].[Na+]
null
null
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1>[OH-].[Na+]>NC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-eded3f07bc674eab884909ce377e9ea4
CNC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1.O=C(Cl)c1ccccc1>>CN(C(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1)C(=O)c1ccccc1
CNC(=O)NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1.C(C1=CC=CC=C1)(=O)Cl.N1=CC=CC=C1>>C(C1=CC=CC=C1)(=O)N(C(=O)NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1)C
[CH3:1][NH:2][C:3](=[O:4])[NH:5][CH:6]1[CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[cH:20]2)[CH2:21][CH2:22]1.Cl[C:23](=[O:24])[c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1>>[CH3:1][N:2]([C:3](=[O:4])[NH:5][CH:6]1[CH2:7][CH2:8][N:9]([CH2:10][c:11]2[cH:12][cH:13][c:14]3[cH:15...
CNC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1.O=C(Cl)c1ccccc1
CN(C(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1)C(=O)c1ccccc1
null
null
C1(=CC=CC=C1)C
Acylation
N-alkylation of secondary amines with alkyl halides
996e0ddf2d6b57ad6b8e08b45c57ed86da0355f61815643564e670f244fe345b
ed2e2a2113014ef864b0a3bd063f004647b373e1f6820e0fdd5587d12a0e8460
O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccc3ccccc3c2)CC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[#7:7]-[C:8](=[O;D1;H0:9])-[NH;D2;+0:10]-[C;D1;H3:11]>>[C:6]-[#7:7]-[C:8](=[O;D1;H0:9])-[N;H0;D3;+0:10](-[C;D1;H3:11])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
1-Methyl-3-[1-(naphth-2-ylmethyl)piperid-4-yl]urea (1.4 g.) (prepared by reacting 4-amino-1-(naphth-2-ylmethyl)piperidine with methyl isocyanate) in toluene (30 cm3) was acylated using benzoyl chloride (0.92 g) in presence of pyridine (0.6 g) to give the title compound: m.p. of HCl, hemihydrate salt =164°-166° C. Condi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Urea
Urea.Substituted dicarboximide
null
null
C1CC[NH]CC1.c1ccc2ccccc2c1.c1ccccc1
HCl
C1(=CC=CC=C1)C
null
null
CNC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1.O=C(Cl)c1ccccc1>C1(=CC=CC=C1)C>CN(C(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1)C(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fab15c502e684fbfa88cc582949b25fa
NC(=O)NC(=O)c1ccco1.NC1CCN(Cc2ccc3ccccc3c2)CC1>>NC(=O)c1occc1C(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1
NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1.O1C(=CC=C1)C(=O)NC(=O)N.N1=CC=CC=C1.O>>C1=C(C=CC2=CC=CC=C12)CN1CCC(CC1)NC(=O)C1=C(OC=C1)C(=O)N
N[C:9]([NH:1][C:2](=[O:3])[c:4]1[o:5][cH:6][cH:7][cH:8]1)=[O:10].[NH2:11][CH:12]1[CH2:13][CH2:14][N:15]([CH2:16][c:17]2[cH:18][cH:19][c:20]3[cH:21][cH:22][cH:23][cH:24][c:25]3[cH:26]2)[CH2:27][CH2:28]1>>[NH2:1][C:2](=[O:3])[c:4]1[o:5][cH:6][cH:7][c:8]1[C:9](=[O:10])[NH:11][CH:12]1[CH2:13][CH2:14][N:15]([CH2:16][c:17]2[...
NC(=O)NC(=O)c1ccco1.NC1CCN(Cc2ccc3ccccc3c2)CC1
NC(=O)c1occc1C(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1
null
null
null
Acylation
OtherReaction
d0db0d4804d1c375f5ead5a4a1a61bcf24028b76ee97b6a753b32886cc0ef1ab
5417ebfa0c4325e1c6fd3a05ca94f7d3810bb9ccad2a0aceda9b79146542a78b
O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccoc1
N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[c:6]1:[#8;a:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1.[C:11]-[C:12](-[NH2;D1;+0:13])-[C:14]>>[C:11]-[C:12](-[NH;D2;+0:13]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:10]1:[c:9]:[c:8]:[#8;a:7]:[c:6]:1-[C:4](-[NH2;D1;+0:3])=[O;D1;H0:5])-[C:14]
null
[]
null
null
null
null
4-Amino-1-(naphth-2-ylmethyl)piperidine (1.2 g, 0.005 m) and 2-furoylurea (0.7 g) in pyridine (5 ml) was refluxed for 6 hours, then cooled. Water was added and the precipitate collected by filtration. The solid was dissolved in chloroform with a little methanol and filtered. The solvent was removed under reduced pressu...
10.6084/m9.figshare.5104873.v1
null
Urea.Unsubstituted dicarboximide.Primary amine
Primary amide.Secondary amide
c1ccoc1
c1ccoc1
c1ccoc1.C1CC[NH]CC1.c1ccc2ccccc2c1
Other
null
null
null
NC(=O)NC(=O)c1ccco1.NC1CCN(Cc2ccc3ccccc3c2)CC1>>NC(=O)c1occc1C(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5a710b5c50314be3848a9b1928e8c6b3
CCOC(=O)c1ccccn1.NC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1>>O=C(NC(=O)c1ccccn1)NC1CCN(Cc2ccc3ccccc3c2)CC1
N.N.N1=C(C=CC=C1)C(=O)OCC.[Na].N.C1=C(C=CC2=CC=CC=C12)CN1CCC(CC1)NC(=O)N>>N1=C(C=CC=C1)C(=O)NC(=O)NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1
CCO[C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][n:11]1.[O:1]=[C:2]([NH2:3])[NH:12][CH:13]1[CH2:14][CH2:15][N:16]([CH2:17][c:18]2[cH:19][cH:20][c:21]3[cH:22][cH:23][cH:24][cH:25][c:26]3[cH:27]2)[CH2:28][CH2:29]1>>[O:1]=[C:2]([NH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][n:11]1)[NH:12][CH:13]1[CH2:14][CH2:15][N:16](...
CCOC(=O)c1ccccn1.NC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1
O=C(NC(=O)c1ccccn1)NC1CCN(Cc2ccc3ccccc3c2)CC1
null
null
null
Acylation
Aminolysis of esters
0330f4993bddb0991bb489c6979d77406cc1a28c3b8a210251333bf0843c59df
3e0cd27ef7f0f0adedddcc27920abb1de1e606dd69fa301eb6865b7fac89ec4a
O=C(NC(=O)c1ccccn1)NC1CCN(Cc2ccc3ccccc3c2)CC1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6].[C:7]-[#7:8]-[C:9](-[NH2;D1;+0:10])=[O;D1;H0:11]>>[C:7]-[#7:8]-[C:9](=[O;D1;H0:11])-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#7;a:5]:[c:6]
32.5
[{"value": 32.5, "product": "N1=C(C=CC=C1)C(=O)NC(=O)NC1CCN(CC1)CC1=CC2=CC=CC=C2C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
DAY
Sodium (0.1 g, 4.35 mmol) in liquid ammonia (100-150 cm3) was stirred until the blue colour was discharged. A bomb was charged with [1-(Naphth-2-yl-methyl)piperid-4-yl]urea (0.83 g, 2.93 mmol) and the liquid ammonia solution was added. The mixture was stirred at room temperature for 2 days then the bomb was cooled to -...
10.6084/m9.figshare.5104873.v1
null
Ester.Urea
Urea.Unsubstituted dicarboximide
null
null
c1ccncc1.C1CC[NH]CC1.c1ccc2ccccc2c1
HO-
null
null
48
CCOC(=O)c1ccccn1.NC(=O)NC1CCN(Cc2ccc3ccccc3c2)CC1>>O=C(NC(=O)c1ccccn1)NC1CCN(Cc2ccc3ccccc3c2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0255eb3447734ab3a76de421c8683068
Br>>[Br-]
CC1=C(C(CCC1)(C)C)/C=C/C(=C/C=C/C(=C/CO)/C)/C.Br.C1(=CC=CC=C1)[PH+](C1=CC=CC=C1)C1=CC=CC=C1>>[Br-].C1(=CC=CC=C1)[PH+](C1=CC=CC=C1)C1=CC=CC=C1
[BrH:1]>>[Br-:1]
Br
[Br-]
null
null
C1(=CC=CC=C1)C
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[BrH;D0;+0:1]>>[Br-;H0;D0:1]
null
[]
60
CELSIUS
2
HOUR
Retinol (2 g, 7 mmol) is dissolved in 50 ml of toluene and 2.4 g (7 mmol) of triphenylphosphonium hydrobromide is added. The mixture is stirred for 18 hours at room temperature and 2 hours at 60° C., then cooled and the toluene separated. The viscous sediment is digested four times with 25 ml of dry toluene. The final ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C1(=CC=CC=C1)C
60
2
Br>C1(=CC=CC=C1)C>[Br-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-76f548fb96d24dc298bc9940f96eeedc
CCOC(=O)C(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C>>CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO
C(C)OC(C(=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C)C)=O.[H-].[H-].[H-].[H-].[Li+].[Al+3]>>CC(CO)=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C
CCO[C:23]([C:21](=[CH:20][CH:19]=[C:17]([CH:16]=[CH:15][CH:14]=[C:2]([CH3:1])[CH:3]=[CH:4][C:5]1=[C:6]([CH3:7])[CH2:8][CH2:9][CH2:10][C:11]1([CH3:12])[CH3:13])[CH3:18])[CH3:22])=[O:24]>>[CH3:1][C:2]([CH:3]=[CH:4][C:5]1=[C:6]([CH3:7])[CH2:8][CH2:9][CH2:10][C:11]1([CH3:12])[CH3:13])=[CH:14][CH:15]=[CH:16][C:17]([CH3:18])...
CCOC(=O)C(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO
null
null
C1CCOC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
C1=CCCCC1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3](-[C;D1;H3:4])=[C:5]-[C:6]=[C:7]>>[C:7]=[C:6]-[C:5]=[C:3](-[C;D1;H3:4])-[CH2;D2;+0:1]-[OH;D1;+0:2]
null
[]
null
null
4
HOUR
A solution of 2,5,9-trimethyl-11-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8,10-undecapentaenoic acid ethyl ester (1.85 g, 5 mmol) in 25 ml of anhydrous THF is cooled to -10° C. and 0.19 g (5 mmol) of LAH is added in portions. The resulting mixture is stirred for 4 hours and quenched carefully with 0.4 ml of water. The...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
C1=CCCCC1
HO-
C1CCOC1
null
4
CCOC(=O)C(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C>C1CCOC1>CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-16b2bb9cea4a43ed8b1c6f70818936f9
CC(=O)Cl.CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO>>CC(=O)OCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
C(C)(=O)Cl.CC(CO)=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C.N1=CC=CC=C1>>C(C)(=O)OCC(=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C)C
Cl[C:2]([CH3:1])=[O:3].[OH:4][CH2:5][C:6]([CH3:7])=[CH:8][CH:9]=[C:10]([CH3:11])[CH:12]=[CH:13][CH:14]=[C:15]([CH3:16])[CH:17]=[CH:18][C:19]1=[C:20]([CH3:21])[CH2:22][CH2:23][CH2:24][C:25]1([CH3:26])[CH3:27]>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][C:6]([CH3:7])=[CH:8][CH:9]=[C:10]([CH3:11])[CH:12]=[CH:13][CH:14]=[C:15]([CH3:...
CC(=O)Cl.CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO
CC(=O)OCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
null
null
CCOCC.C(Cl)Cl
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
C1=CCCCC1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]=[C:5]-[C:6]=[C:7](-[C;D1;H3:8])-[C:9]-[OH;D1;+0:10]>>[C:4]=[C:5]-[C:6]=[C:7](-[C;D1;H3:8])-[C:9]-[O;H0;D2;+0:10]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
0
CELSIUS
2
HOUR
A solution of 2,5,9-trimethyl-11-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8,10-undecapentaene-1-ol (1.6 g, 5 mmol) and pyridine (9.6 ml, 7.3 mmol) in 15 ml of anhydrous methylene chloride is stirred in an ice bath and a solution of acetyl chloride (0.37 ml, 5.25 mmol) in 5 ml of anhydrous methylene chloride is added d...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
C1=CCCCC1
HCl
CCOCC.C(Cl)Cl
0
2
CC(=O)Cl.CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO>CCOCC.C(Cl)Cl>CC(=O)OCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-32560364bc2c4583929e9619527c24ce
CC(=O)OCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C.[S-]c1ccccc1>>CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CSc1ccccc1
C(C)(=O)OCC(=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C)C.[S-]C1=CC=CC=C1.[Na+]>>C1(=CC=CC=C1)SCC(=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C)C
CC(=O)O[CH2:23][C:21](=[CH:20][CH:19]=[C:17]([CH:16]=[CH:15][CH:14]=[C:2]([CH3:1])[CH:3]=[CH:4][C:5]1=[C:6]([CH3:7])[CH2:8][CH2:9][CH2:10][C:11]1([CH3:12])[CH3:13])[CH3:18])[CH3:22].[S-:24][c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1>>[CH3:1][C:2]([CH:3]=[CH:4][C:5]1=[C:6]([CH3:7])[CH2:8][CH2:9][CH2:10][C:11]1([CH3:12])...
CC(=O)OCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C.[S-]c1ccccc1
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CSc1ccccc1
null
null
C1CCOC1.CN(C)P(=O)(N(C)C)N(C)C.C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
5733dbf3fa3c89f36c04baccc93170809e2644bb7f231de1b5858a1113f0eb5f
d5aadbfeb774ee97265b01254dc5b32931df6322312658654ed230582a36a6e5
C(=CC=CC=CC1=CCCCC1)C=CC=CCSc1ccccc1
C-C(=O)-O-[CH2;D2;+0:1]-[C:2](-[C;D1;H3:3])=[C:4]-[C:5]=[C:6].[S-;H0;D1:7]-[c:8](:[c:9]):[c:10]>>[C:6]=[C:5]-[C:4]=[C:2](-[C;D1;H3:3])-[CH2;D2;+0:1]-[S;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]
null
[]
null
null
18
HOUR
To a solution of 1.85 g (5 mmol) of 2,5,9-trimethyl-11-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8,10-undecapentaenyl acetate in 25 ml of anhydrous THF and 8 ml of HMPA is added in portions 0.68 g (5.2 mmol) of sodium thiophenoxide. The resulting mixture is stirred at room temperature for 18 hours and then taken up in ...
10.6084/m9.figshare.5104873.v1
null
Ester
Monosulfide
null
null
C1=CCCCC1.c1ccccc1
HO-
C1CCOC1.CN(C)P(=O)(N(C)C)N(C)C.C(C)OCC
null
18
CC(=O)OCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C.[S-]c1ccccc1>C1CCOC1.CN(C)P(=O)(N(C)C)N(C)C.C(C)OCC>CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CSc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c01cb519f753417099bc0730fcf1a233
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO>>CNCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
CC(CO)=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.BrN1C(CCC1=O)=O>>CNCC(=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C)C
O[CH2:3][C:4]([CH3:5])=[CH:6][CH:7]=[C:8]([CH3:9])[CH:10]=[CH:11][CH:12]=[C:13]([CH3:14])[CH:15]=[CH:16][C:17]1=[C:18]([CH3:19])[CH2:20][CH2:21][CH2:22][C:23]1([CH3:24])[CH3:25]>>[CH3:1][NH:2][CH2:3][C:4]([CH3:5])=[CH:6][CH:7]=[C:8]([CH3:9])[CH:10]=[CH:11][CH:12]=[C:13]([CH3:14])[CH:15]=[CH:16][C:17]1=[C:18]([CH3:19])[...
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO
CNCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
null
null
C1CCOC1
Miscellaneous
OtherReaction
48dad0f5b231c0d740a50fd8810c796a0b51f24cdb89b976c9df81724489b664
1da3d050763f9c56998cc752e2b3f224578fac5a94a0c6233507a69672a2b533
C1=CCCCC1
O-[CH2;D2;+0:1]-[C:2](-[C;D1;H3:3])=[C:4]-[C:5]=[C:6]>>[C:6]=[C:5]-[C:4]=[C:2](-[C;D1;H3:3])-[CH2;D2;+0:1]-[#7:7]-[C;D1;H3:8]
null
[]
null
null
18
HOUR
A solution of 2,5,9-trimethyl-11-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8,10-undecapentaene-1-ol (3.2 g, 10 mmol) and triphenylphosphine (2.88 g, 11 mmol) in 20 ml of THF is stirred in an ice bath and 1.78 g (10 mmol) of N-bromosuccinimide is added in small portions over a period of one hour. After addition, the coo...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Secondary amine
null
null
C1=CCCCC1
null
C1CCOC1
null
18
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO>C1CCOC1>CNCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-881c5b03087e4b6fa8b661db36b63481
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO.CO>>COCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
C(=O)(O)[O-].[Na+].CC(CO)=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C.C(OC)(OC)OC.CO.FC(C(=O)O)(F)F>>COCC(=CC=C(C=CC=C(C=CC1=C(CCCC1(C)C)C)C)C)C
[OH:2][CH2:3][C:4]([CH3:5])=[CH:6][CH:7]=[C:8]([CH3:9])[CH:10]=[CH:11][CH:12]=[C:13]([CH3:14])[CH:15]=[CH:16][C:17]1=[C:18]([CH3:19])[CH2:20][CH2:21][CH2:22][C:23]1([CH3:24])[CH3:25].O[CH3:1]>>[CH3:1][O:2][CH2:3][C:4]([CH3:5])=[CH:6][CH:7]=[C:8]([CH3:9])[CH:10]=[CH:11][CH:12]=[C:13]([CH3:14])[CH:15]=[CH:16][C:17]1=[C:1...
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO.CO
COCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
Alcohol to ether
c873da657d50d2833a5f2666591cb755f50dd7890d803ad948097f1a9004ed92
6598fea024a5fbd71aab93259b9b6cb0238901bd1731856222fcfdfc0bdff95d
C1=CCCCC1
O-[CH3;D1;+0:1].[C:2]=[C:3]-[C:4]=[C:5](-[C;D1;H3:6])-[C:7]-[OH;D1;+0:8]>>[C:2]=[C:3]-[C:4]=[C:5](-[C;D1;H3:6])-[C:7]-[O;H0;D2;+0:8]-[CH3;D1;+0:1]
null
[]
null
null
8
HOUR
To a solution of 2,5,9-trimethyl-11-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8,10-undecapentaene-1-ol (1.6 g, 5 mmol), 106 g (10 mmol) of trimethyl orthoformate and 160 mg (5 mmol) of dry methanol in 5 ml of dry THF is added dropwise a solution of 40 μL of trifluoroacetic acid in 1 ml of dry THF over a 1 minute period...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Methanol
Ether
null
null
C1=CCCCC1
HO-
C1CCOC1
null
8
CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC=C(C)CO.CO>C1CCOC1>COCC(C)=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8f678bfe64a843f0a9a23754ecb07be3
c1ccc([Se][Se]c2ccccc2)cc1>>[Se]=[SeH-]
O1CCCC1.[PH2](=O)O.C1(=CC=CC=C1)C(C[Se]CC(C1=CC=CC=C1)N)N.C1(=CC=CC=C1)[Se][Se]C1=CC=CC=C1.O1CCCC1>>C1(=CC=CC=C1)C(C[Se]CC(C1=CC=CC=C1)N)N.[SeH-]=[Se]
c1ccc([Se:20][Se:21]c2ccccc2)cc1>>[Se:20]=[SeH-:21]
c1ccc([Se][Se]c2ccccc2)cc1
[Se]=[SeH-]
null
null
CCOCC
Miscellaneous
OtherReaction
c7270c048ee5b92f11aec509cd1fcec9f72e573bd2e78bc92bb00ad72ceb64c9
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[Se;H0;D2;+0:1](-[Se;H0;D2;+0:2]-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[Se;H0;D1;+0:1]=[SeH-;D1:2]
null
[]
null
null
null
null
A preferred compound is phenyl-2-aminoethyl selenide and salts thereof. Phenyl-2-aminoethyl selenide (PAESe) was synthesized by employing the following procedure. Diphenyl diselenide, 24.707 g (79.16 mmol) was dissolved into 100 ml of tetrahydrofuran (THF) with steam heating. To the intensely dark red THF solution was ...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1.c1ccccc1
null
null
Other
CCOCC
null
null
c1ccc([Se][Se]c2ccccc2)cc1>CCOCC>[Se]=[SeH-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-582897d5e0ee4beea88f45c69a6bdd13
ClCc1cccc2c1CC2.c1ccc(P(c2ccccc2)c2ccccc2)cc1>>C1=Cc2cc(C[P+](c3ccccc3)(c3ccccc3)c3ccccc3)ccc21.[Cl-]
ClCC1=C2C(CC2)=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(C)OCC>>[Cl-].C1(=CC=CC=C1)[P+](CC1=CC2=C(C=C2)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1
[CH2:1]1[CH2:2][c:3]2[c:4]1[c:5]([CH2:6][Cl:29])[cH:26][cH:27][cH:28]2.[P:7]([c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)([c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1>>[CH:1]1=[CH:2][c:3]2[cH:4][c:5]([CH2:6][P+:7]([c:8]3[cH:9][cH:10][cH:11][cH:12][cH:13]3)([c:14]3[cH:15][cH:16][...
ClCc1cccc2c1CC2.c1ccc(P(c2ccccc2)c2ccccc2)cc1
C1=Cc2cc(C[P+](c3ccccc3)(c3ccccc3)c3ccccc3)ccc21.[Cl-]
null
null
C(Cl)(Cl)Cl
C-C Coupling
OtherReaction
127f8013fd832f07dba9c227580ae1d03fe917a64b25bf9f7f4f72f6647c370e
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
C1=Cc2cc(C[P+](c3ccccc3)(c3ccccc3)c3ccccc3)ccc21
[Cl;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]2:[c;H0;D3;+0:8]:1-[CH2;D2;+0:9]-[CH2;D2;+0:10]-2.[c:11]:[c:12](-[P;H0;D3;+0:13](-[c:14](:[c:15]):[c:16])-[c:17](:[c:18]):[c:19]):[c:20]>>[Cl-;H0;D0:1].[c:11]:[c:12](-[P+;H0;D4:13](-[CH2;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[c;H0;D3;+0:6]2:[c:7](:[cH;D2;+0:8]:1)...
null
[]
null
null
null
null
A solution of 4-chloromethylbenzocyclobutene (24.4 g, 160 mmol) and triphenylphosphine (41.9 g, 160 mmol) in 120 ml of chloroform was heated at reflux for 24 h. Addition of diethyl ether followed by filtration gave tripheny(4-benzocyclobutenyl)methyl phosphonium chloride as a white powder: 1H NMR (CDCl3) δ3.03 (m, 4H),...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2c(c1)CC2
C1=Cc2ccccc21
C1=Cc2ccccc21.c1ccccc1.c1ccccc1.c1ccccc1
null
C(Cl)(Cl)Cl
null
null
ClCc1cccc2c1CC2.c1ccc(P(c2ccccc2)c2ccccc2)cc1>C(Cl)(Cl)Cl>C1=Cc2cc(C[P+](c3ccccc3)(c3ccccc3)c3ccccc3)ccc21.[Cl-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c8ad3021517e47849a4ef0618fa4b5f1
CC(C)=O.C[Si](C)(C)Cl.FC(F)(F)C(c1ccc(Br)cc1)(c1ccc(Br)cc1)C(F)(F)F>>C[Si](C)(C)c1ccc(C(c2ccc([Si](C)(C)C)cc2)(C(F)(F)F)C(F)(F)F)cc1
C(=O)=O.CC(=O)C.BrC1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)C1=CC=C(C=C1)Br.C(CCC)[Li].Cl[Si](C)(C)C>>C[Si](C1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)C1=CC=C(C=C1)[Si](C)(C)C)(C)C
O=C([CH3:15])[CH3:16].Cl[Si:2]([CH3:1])([CH3:3])[CH3:4].Br[c:5]1[cH:6][cH:7][c:8]([C:9]([c:10]2[cH:11][cH:12][c:13](Br)[cH:18][cH:19]2)([C:20]([F:21])([F:22])[F:23])[C:24]([F:25])([F:26])[F:27])[cH:28][cH:29]1>>[CH3:1][Si:2]([CH3:3])([CH3:4])[c:5]1[cH:6][cH:7][c:8]([C:9]([c:10]2[cH:11][cH:12][c:13]([Si:14]([CH3:15])([C...
CC(C)=O.C[Si](C)(C)Cl.FC(F)(F)C(c1ccc(Br)cc1)(c1ccc(Br)cc1)C(F)(F)F
C[Si](C)(C)c1ccc(C(c2ccc([Si](C)(C)C)cc2)(C(F)(F)F)C(F)(F)F)cc1
null
null
CCCCCC.O1CCCC1
Miscellaneous
OtherReaction
d9c0813edfd655437e0619c276031b87485ac244e3a31e4a6d0b649d0faaaaba
400c69d416533a42d629d44e8f6638def1c96e24296888dc3d74d06a33e92041
c1ccc(Cc2ccccc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].Br-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10].Cl-[Si;H0;D4;+0:11](-[C;D1;H3:12])(-[C;D1;H3:13])-[C;D1;H3:14].O=C(-[CH3;D1;+0:15])-[CH3;D1;+0:16]>>[C;D1;H3:17]-[#14:18](-[CH3;D1;+0:15])(-[CH3;D1;+0:16])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C;D1;H3:12]-[Si;H0;D4;+0:11](-[C;...
null
[]
-78
CELSIUS
16
HOUR
To a solution of 4.62 g (0.1 mole) 2,2-bis(4-bromophenyl)hexafluoropropane in 75 ml of anhydrous tetrahydrofuran was added dropwise 28 ml (0.4 moles) of a 1.4 molar solution of n-butyllithium in hexane while the reaction mixture was cooled in a dry ice-acetone slush. The reaction mixture was stirred for one half hour a...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Ketone.Silyl protective group
Silyl protective group.Silyl protective group
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Br-
CCCCCC.O1CCCC1
-78
16
CC(C)=O.C[Si](C)(C)Cl.FC(F)(F)C(c1ccc(Br)cc1)(c1ccc(Br)cc1)C(F)(F)F>CCCCCC.O1CCCC1>C[Si](C)(C)c1ccc(C(c2ccc([Si](C)(C)C)cc2)(C(F)(F)F)C(F)(F)F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1df2989375bc46478b5ee78beb16d265
CCCCCl.c1ccccc1>>CCCCc1ccccc1
ClCCCC.NC(=O)N.S(O)(O)(=O)=O.C1=CC=CC=C1.NC(=O)N.S(O)(O)(=O)=O.NC(=O)N.S(O)(O)(=O)=O>>C(CCC)C1=CC=CC=C1
Cl[CH2:4][CH2:3][CH2:2][CH3:1].[cH:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1
CCCCCl.c1ccccc1
CCCCc1ccccc1
null
null
null
C-C Coupling
Friedel-Crafts alkylation with halide
abd82b32c15853d5913cc8f5d51923ff8cee2c9e5cfc2628ece51b84576c3f2d
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:5]:[c:4]
null
[]
null
null
10
MINUTE
Normal-butylbenzene is prepared by heating equal molar amounts of 1-chlorobutane and benzene in a molten urea-sulfuric acid component containing 42.6 weight percent urea and 75.4 weight percent sulfuric acid having a urea/sulfuric acid molar ratio of 1.2 at a temperature of 140° F. and a pressure of 100 psig. for a per...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccccc1
c1ccccc1
c1ccccc1
HCl
null
null
0.166667
CCCCCl.c1ccccc1>>CCCCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cb342278cc67421d861b38254858d7ca
N=C(N)N.O=C1CC(Cl)(CCl)O1>>Nc1nc(O)cc(CCl)n1
ClC1(CC(O1)=O)CCl.Cl.NC(=N)N.Cl>>NC1=NC(=CC(=N1)CCl)O
[NH2:1][C:2]([NH2:3])=[NH:10].Cl[C:7]1([CH2:8][Cl:9])O[C:4](=[O:5])[CH2:6]1>>[NH2:1][c:2]1[n:3][c:4]([OH:5])[cH:6][c:7]([CH2:8][Cl:9])[n:10]1
N=C(N)N.O=C1CC(Cl)(CCl)O1
Nc1nc(O)cc(CCl)n1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
0696bdbf97c9bf9861014eae451ad11c18128202bdc40d43b11a076939b2d145
129990a0b56fe349b93ca8731b8ff9a7cfaf015afb641b0852728d0f92224b5a
c1cncnc1
Cl-[C;H0;D4;+0:1]1(-[C:2]-[Cl;D1;H0:3])-O-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[CH2;D2;+0:6]-1.[N;D1;H2:7]-[C;H0;D3;+0:8](-[NH2;D1;+0:9])=[NH;D1;+0:10]>>[Cl;D1;H0:3]-[C:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:6]:[c;H0;D3;+0:4](-[OH;D1;+0:5]):[n;H0;D2;+0:9]:[c;H0;D3;+0:8](-[N;D1;H2:7]):[n;H0;D2;+0:10]:1
null
[]
120
CELSIUS
null
null
620 parts of 4-chloro-4-chloromethyloxetan-2-one and 440 parts of guanidine hydrochloride were charged to a reaction flask and the mixture was stirred and heated under nitrogen purge as the bath temperature was gradually raised to 120° C. When the bath temperature approached 100° C., reaction commenced accompanied by e...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Ester.Primary amine
Aromatic alcohol
C1COC1
c1cncnc1
c1cncnc1
HCl
O
120
null
N=C(N)N.O=C1CC(Cl)(CCl)O1>O>Nc1nc(O)cc(CCl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bd220c185fdc4f29a50c93efa6db59de
N=C(N)N.O=C1CC(Cl)(CC(Cl)(Cl)Cl)O1>>Nc1nc(O)cc(C=C(Cl)Cl)n1
ClC1(CC(O1)=O)CC(Cl)(Cl)Cl.Cl.NC(=N)N.Cl>>NC1=NC(=CC(=N1)C=C(Cl)Cl)O
[NH2:1][C:2]([NH2:3])=[NH:12].O=[C:4]1[O:5][C:7](Cl)([CH2:8][C:9](Cl)([Cl:10])[Cl:11])[CH2:6]1>>[NH2:1][c:2]1[n:3][c:4]([OH:5])[cH:6][c:7]([CH:8]=[C:9]([Cl:10])[Cl:11])[n:12]1
N=C(N)N.O=C1CC(Cl)(CC(Cl)(Cl)Cl)O1
Nc1nc(O)cc(C=C(Cl)Cl)n1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
f6e8b6c016c264d65a00ac2c1b3c0e2e7c0f17cf4fe88b866e901fc8f9bbef9f
7b2bd2e2424b24297e7c6fcfa0019ee4773825ace42c090d742953d12c1e6bbf
c1cncnc1
Cl-[C;H0;D4;+0:1]1(-[CH2;D2;+0:2]-[C;H0;D4;+0:3](-Cl)(-[Cl;D1;H0:4])-[Cl;D1;H0:5])-[CH2;D2;+0:6]-[C;H0;D3;+0:7](=O)-[O;H0;D2;+0:8]-1.[N;D1;H2:9]-[C;H0;D3;+0:10](-[NH2;D1;+0:11])=[NH;D1;+0:12]>>[Cl;D1;H0:4]-[C;H0;D3;+0:3](-[Cl;D1;H0:5])=[CH;D2;+0:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:6]:[c;H0;D3;+0:7](-[OH;D1;+0:8]):[n;H0;D2;+0:...
null
[]
140
CELSIUS
45
MINUTE
119 Parts of 4-chloro-4-(2,2,2-trichloroethyl)-oxetan-2-one and 95.5 parts of guanidine hydrochloride were charged to a reaction flask and heated in an oil bath at 140° C. for 15 minutes. The solid dissolved and HCl gas was evolved. The oil bath temperature was raised to 160° C. and heating was continued for a further ...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Tertiary halide.Ester.Primary amine
Alkenyl halide.Alkenyl halide.Aromatic alcohol
C1COC1
c1cncnc1
c1cncnc1
HCl
null
140
0.75
N=C(N)N.O=C1CC(Cl)(CC(Cl)(Cl)Cl)O1>>Nc1nc(O)cc(C=C(Cl)Cl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c5ccdb6526a343d180e97ac51b4a58da
Nc1nc(O)cc(CCl)n1.O=P(Cl)(Cl)Cl>>Nc1nc(Cl)cc(CCl)n1
NC1=NC(=CC(=N1)CCl)O.P(=O)(Cl)(Cl)Cl>>NC1=NC(=CC(=N1)Cl)CCl
O[c:4]1[n:3][c:2]([NH2:1])[n:10][c:7]([CH2:8][Cl:9])[cH:6]1.O=P(Cl)(Cl)[Cl:5]>>[NH2:1][c:2]1[n:3][c:4]([Cl:5])[cH:6][c:7]([CH2:8][Cl:9])[n:10]1
Nc1nc(O)cc(CCl)n1.O=P(Cl)(Cl)Cl
Nc1nc(Cl)cc(CCl)n1
null
null
null
Functional Group Interconversion
Alcohol to chloride_POCl3_ortho
c34cc3a735ba90a6ebc3a31af86c6a0085713d9dcab569055caa3b8d444bb07d
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1cncnc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6](-[C:7]):[c:8]:1>>[C:7]-[c:6]1:[#7;a:5]:[c:4]:[#7;a:3]:[c;H0;D3;+0:2](-[Cl;H0;D1;+0:1]):[c:8]:1
null
[]
null
null
10
MINUTE
47.9 Parts of 2-amino-4-chloromethyl-6-hydroxypyrimidine was added portionwise to 410 parts of phosphorus oxychloride with stirring. The mixture was placed in an oil bath at 130° C. and stirred until all the solid had dissolved and then for a further 10 minutes. The solution was cooled and the excess of phosphorus oxyc...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Aromatic halide
c1cncnc1
c1cncnc1
c1cncnc1
HCl
null
null
0.166667
Nc1nc(O)cc(CCl)n1.O=P(Cl)(Cl)Cl>>Nc1nc(Cl)cc(CCl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2d0c936e376d46a4a7dfb16b647c8164
Nc1nc(O)cc(C=C(Cl)Cl)n1.O=P(Cl)(Cl)Cl>>Nc1nc(Cl)cc(C=C(Cl)Cl)n1
NC1=NC(=CC(=N1)C=C(Cl)Cl)O.P(=O)(Cl)(Cl)Cl>>NC1=NC(=CC(=N1)Cl)C=C(Cl)Cl
O[c:4]1[n:3][c:2]([NH2:1])[n:12][c:7]([CH:8]=[C:9]([Cl:10])[Cl:11])[cH:6]1.O=P(Cl)(Cl)[Cl:5]>>[NH2:1][c:2]1[n:3][c:4]([Cl:5])[cH:6][c:7]([CH:8]=[C:9]([Cl:10])[Cl:11])[n:12]1
Nc1nc(O)cc(C=C(Cl)Cl)n1.O=P(Cl)(Cl)Cl
Nc1nc(Cl)cc(C=C(Cl)Cl)n1
null
null
null
Functional Group Interconversion
Alcohol to chloride_POCl3_ortho
c34cc3a735ba90a6ebc3a31af86c6a0085713d9dcab569055caa3b8d444bb07d
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1cncnc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6](-[C:7]=[C:8]):[c:9]:1>>[C:8]=[C:7]-[c:6]1:[#7;a:5]:[c:4]:[#7;a:3]:[c;H0;D3;+0:2](-[Cl;H0;D1;+0:1]):[c:9]:1
null
[]
null
null
null
null
10 Parts of 2-amino-4-(2,2-dichlorovinyl)-6-hydroxypyrimidine and 66 parts of phosphorus oxychloride were heated together under reflux for 1 hour with stirring. The solution was cooled and excess phosphorus oxychloride was removed in vacuo on a rotary evaporator. The residual viscous oil was poured onto ice, with stirr...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Aromatic halide
c1cncnc1
c1cncnc1
c1cncnc1
HCl
null
null
null
Nc1nc(O)cc(C=C(Cl)Cl)n1.O=P(Cl)(Cl)Cl>>Nc1nc(Cl)cc(C=C(Cl)Cl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c486bd8087ef4bc39cbd7955c7ea7c4c
C[O-].Nc1nc(Cl)cc(C=C(Cl)Cl)n1>>COc1cc(C=C(Cl)Cl)nc(N)n1
[Na].NC1=NC(=CC(=N1)Cl)C=C(Cl)Cl.C[O-].[Na+]>>NC1=NC(=CC(=N1)C=C(Cl)Cl)OC
[CH3:1][O-:2].Cl[c:3]1[cH:4][c:5]([CH:6]=[C:7]([Cl:8])[Cl:9])[n:10][c:11]([NH2:12])[n:13]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]=[C:7]([Cl:8])[Cl:9])[n:10][c:11]([NH2:12])[n:13]1
C[O-].Nc1nc(Cl)cc(C=C(Cl)Cl)n1
COc1cc(C=C(Cl)Cl)nc(N)n1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
f4c4542ecb881e89239e5ab87f858188051f8469235d618ac5a349648125ce56
51fd03eb6a688046e417b9ed09ea0e72062396d005af1318b9b5f376a97da959
c1cncnc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[N;D1;H2:4]):[#7;a:5]:[c:6](-[C:7]=[C:8]):[c:9]:1.[C;D1;H3:10]-[O-;H0;D1:11]>>[C:8]=[C:7]-[c:6]1:[#7;a:5]:[c:3](-[N;D1;H2:4]):[#7;a:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:11]-[C;D1;H3:10]):[c:9]:1
null
[]
null
null
4
HOUR
22.0 Parts of 2-amino-4-chloro-6-(2,2-dichlorovinyl)pyrimidine was dissolved in 500 parts of dry methanol and stirred whilst a solution of sodium methoxide, prepared by dissolving 4.6 parts of sodium in 200 parts of dry methanol, was added dropwise, over 30 minutes at ambient temperature. The resulting solution was sti...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Ether
c1cncnc1
c1cncnc1
c1cncnc1
Other
CO
null
4
C[O-].Nc1nc(Cl)cc(C=C(Cl)Cl)n1>CO>COc1cc(C=C(Cl)Cl)nc(N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-49bd71cf48ae45fcbb90a9526cdec8dd
CNC.Nc1nc(Cl)cc(CCl)n1>>CN(C)c1cc(CCl)nc(N)n1
Cl.CNC.[Na].NC1=NC(=CC(=N1)Cl)CCl>>NC1=NC(=CC(=N1)CCl)N(C)C
[CH3:1][NH:2][CH3:3].Cl[c:4]1[cH:5][c:6]([CH2:7][Cl:8])[n:9][c:10]([NH2:11])[n:12]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][c:6]([CH2:7][Cl:8])[n:9][c:10]([NH2:11])[n:12]1
CNC.Nc1nc(Cl)cc(CCl)n1
CN(C)c1cc(CCl)nc(N)n1
null
null
CO
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
8a13b42f4b06102b68f4963e65202071bf1d0630fbad1b11bbd8e99b9f9c8f34
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1cncnc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[N;D1;H2:4]):[#7;a:5]:[c:6](-[C:7]):[c:8]:1.[C;D1;H3:9]-[NH;D2;+0:10]-[C;D1;H3:11]>>[C:7]-[c:6]1:[#7;a:5]:[c:3](-[N;D1;H2:4]):[#7;a:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:10](-[C;D1;H3:9])-[C;D1;H3:11]):[c:8]:1
null
[]
null
null
null
null
8.1 Parts of dimethylamine hydrochloride was added to a solution of 2.3 parts of sodium in 20 parts of methanol. The resulting mixture was added dropwise with stirring over about 10 minutes to a solution of 9.9 parts of 2-amino-4-chloro-6-chloromethylpyrimidine in 50 parts of methanol. The reaction was monitored by TLC...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1cncnc1
c1cncnc1
c1cncnc1
HCl
CO
null
null
CNC.Nc1nc(Cl)cc(CCl)n1>CO>CN(C)c1cc(CCl)nc(N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-57c87955e9ed4a11aa4e6f98c7716c2b
COc1cc(CCl)nc(N)n1.[F-]>>COc1cc(CF)nc(N)n1
NC1=NC(=CC(=N1)CCl)OC.[F-].[Cs+]>>NC1=NC(=CC(=N1)CF)OC
Cl[CH2:6][c:5]1[cH:4][c:3]([O:2][CH3:1])[n:11][c:9]([NH2:10])[n:8]1.[F-:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH2:6][F:7])[n:8][c:9]([NH2:10])[n:11]1
COc1cc(CCl)nc(N)n1.[F-]
COc1cc(CF)nc(N)n1
null
null
CN(C=O)C
Functional Group Interconversion
OtherReaction
e944a2acb95a43a23818321f2ac2f96ba2f2b8d34f52c1cfd1e3802d2403177f
e2ca6f9fe1078a3836d617896a4e5cc310fb155ca459b021e2b549b3e61f1df7
c1cncnc1
Cl-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1.[F-;H0;D0:8]>>[F;H0;D1;+0:8]-[CH2;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1
null
[]
null
null
null
null
A mixture of 17.0 parts of 2-amino-4-chloromethyl-6-methoxypyrimidine, 59.5 parts of caesium fluoride and 130 parts of dry dimethylformamide was stirred under reflux for 2 hours. The mixture was cooled and evaporated in vacuo. The residue was taken up in ethyl acetate and the solution was washed four times with water. ...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Primary halide
null
null
c1cncnc1
Other
CN(C=O)C
null
null
COc1cc(CCl)nc(N)n1.[F-]>CN(C=O)C>COc1cc(CF)nc(N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2890b78e01af42029f6cf55bc787a012
CS.Nc1nc(F)cc(CF)n1>>CSc1cc(CF)nc(N)n1
NC1=NC(=CC(=N1)F)CF.CS.O1CCCC1.[Na]>>NC1=NC(=CC(=N1)CF)SC
[CH3:1][SH:2].F[c:3]1[cH:4][c:5]([CH2:6][F:7])[n:8][c:9]([NH2:10])[n:11]1>>[CH3:1][S:2][c:3]1[cH:4][c:5]([CH2:6][F:7])[n:8][c:9]([NH2:10])[n:11]1
CS.Nc1nc(F)cc(CF)n1
CSc1cc(CF)nc(N)n1
null
null
CO
Heteroatom Alkylation and Arylation
thioether_nucl_sub
270d69d232cba6e3d197f50ba299db6b74c94a769bfdb5d3c28eabf0ce3253f9
b7fe376f7aad2517725eef26ab981e4baa6c31c5f38fdf89e7c52a4a2c6cc1d2
c1cncnc1
F-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[N;D1;H2:4]):[#7;a:5]:[c:6](-[C:7]):[c:8]:1.[C;D1;H3:9]-[SH;D1;+0:10]>>[C:7]-[c:6]1:[#7;a:5]:[c:3](-[N;D1;H2:4]):[#7;a:2]:[c;H0;D3;+0:1](-[S;H0;D2;+0:10]-[C;D1;H3:9]):[c:8]:1
null
[]
null
null
1
HOUR
A mixture of 1.0 part of 2-amino-4-fluoro-6-fluoromethylpyrimidine, 3.0 parts of methanethiol and 50 parts of dry tetrahydrofuran was stirred at 5° C. whilst a solution of 0.16 parts of sodium in 20 parts of dry methanol was added dropwise. The temperature was kept below 10° C. with ice-bath cooling. When the addition ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aliphatic thiol
Monosulfide
c1cncnc1
c1cncnc1
c1cncnc1
HF
CO
null
1
CS.Nc1nc(F)cc(CF)n1>CO>CSc1cc(CF)nc(N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c5c4f3d95a07449791cf3a5bbb4138ec
CCCCO.Nc1nc(Cl)cc(CCl)n1>>CCCCOc1cc(CCl)nc(N)n1
NC1=NC(=CC(=N1)Cl)CCl.CC(C)([O-])C.[K+].C(CCC)O>>NC1=NC(=CC(=N1)OCCCC)CCl
[CH3:1][CH2:2][CH2:3][CH2:4][OH:5].Cl[c:6]1[cH:7][c:8]([CH2:9][Cl:10])[n:11][c:12]([NH2:13])[n:14]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][c:8]([CH2:9][Cl:10])[n:11][c:12]([NH2:13])[n:14]1
CCCCO.Nc1nc(Cl)cc(CCl)n1
CCCCOc1cc(CCl)nc(N)n1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a445000eb5ed501274d93689ad5b9d45095af02deca02b6b541c8a834890a276
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1cncnc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[N;D1;H2:4]):[#7;a:5]:[c:6](-[C:7]):[c:8]:1.[C:9]-[C:10]-[OH;D1;+0:11]>>[C:9]-[C:10]-[O;H0;D2;+0:11]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[N;D1;H2:4]):[#7;a:5]:[c:6](-[C:7]):[c:8]:1
null
[]
50
CELSIUS
null
null
3,56 Parts of 2-amino-4-chloro-6-chloromethylpyrimidine and 2.24 parts of potassium t-butoxide were dissolved in 60 parts of n-butanol at room temperature then the solution was heated at 50° C. for 2 hours, with stirring. After this time, the solution was cooled and evaporated in vacuo. The residue was partitioned betw...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1cncnc1
c1cncnc1
c1cncnc1
HCl
null
50
null
CCCCO.Nc1nc(Cl)cc(CCl)n1>>CCCCOc1cc(CCl)nc(N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f606e875095f482a95b954389719a17c
C=CCNCC=C.Nc1nc(Cl)cc(CCl)n1>>C=CCN(CC=C)c1cc(CCl)nc(N)n1
NC1=NC(=CC(=N1)Cl)CCl.C(C=C)NCC=C>>NC1=NC(=CC(=N1)CCl)N(CC=C)CC=C
[CH2:1]=[CH:2][CH2:3][NH:4][CH2:5][CH:6]=[CH2:7].Cl[c:8]1[cH:9][c:10]([CH2:11][Cl:12])[n:13][c:14]([NH2:15])[n:16]1>>[CH2:1]=[CH:2][CH2:3][N:4]([CH2:5][CH:6]=[CH2:7])[c:8]1[cH:9][c:10]([CH2:11][Cl:12])[n:13][c:14]([NH2:15])[n:16]1
C=CCNCC=C.Nc1nc(Cl)cc(CCl)n1
C=CCN(CC=C)c1cc(CCl)nc(N)n1
null
null
null
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
8a13b42f4b06102b68f4963e65202071bf1d0630fbad1b11bbd8e99b9f9c8f34
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1cncnc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[N;D1;H2:4]):[#7;a:5]:[c:6](-[C:7]):[c:8]:1.[C;D1;H2:9]=[C:10]-[C:11]-[NH;D2;+0:12]-[C:13]-[C:14]=[C;D1;H2:15]>>[C:7]-[c:6]1:[#7;a:5]:[c:3](-[N;D1;H2:4]):[#7;a:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:12](-[C:11]-[C:10]=[C;D1;H2:9])-[C:13]-[C:14]=[C;D1;H2:15]):[c:8]:1
null
[]
null
null
null
null
3.56 Parts of 2-amino-4-chloro-6-chloromethylpyrimidine and 3.9 parts of diallylamine were reacted together according to the method of Example 15 to give 2-amino-4-chloromethyl-6-diallylaminopyrimidine m.p. 53°-55° C. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1cncnc1
c1cncnc1
c1cncnc1
HCl
null
null
null
C=CCNCC=C.Nc1nc(Cl)cc(CCl)n1>>C=CCN(CC=C)c1cc(CCl)nc(N)n1