dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-83cce351f7ce40fbbfb94ec6344ceae4
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCCN=C=S>>CCN(CC)CCCNC(=S)N(CCS(=O)(=O)c1ccccc1)C(C)C
C1(=CC=CC=C1)S(=O)(=O)CCNC(C)C.C(C)N(CC)CCCN=C=S>>C(C)N(CCCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=S)CC
[NH:12]([CH2:13][CH2:14][S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)[CH:24]([CH3:25])[CH3:26].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][CH2:8][N:9]=[C:10]=[S:11]>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][CH2:8][NH:9][C:10](=[S:11])[N:12]([CH2:13][CH2:14][S:15](=[O:16])(=[O:17])[...
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCCN=C=S
CCN(CC)CCCNC(=S)N(CCS(=O)(=O)c1ccccc1)C(C)C
null
null
C(C)#N
Heteroatom Alkylation and Arylation
thiourea
16b9dd18807f693b1cdd004c800af858aba15692e46e0e83fca1718f8bcadabb
48e0e6261e922bdea79c78ea511461d733cbd49c10100c782d86c83675c4be7c
c1ccccc1
[C:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[S;D1;H0:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9](-[C;D1;H3:10])-[C;D1;H3:11]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9](-[C;D1;H3:10])-[C;D1;H3:11])-[C;H0;D3;+0:4](=[S;D1;H0:5])-[NH;D2;+0:3]-[C:2]-[C:1]
76.9
[{"value": 76.9, "product": "C(C)N(CCCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=S)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 76.9, "product": "C(C)N(CCCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=S)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 5.0 g (0.022 mole) of N-[2-(phenylsulfonyl)ethyl]-2-propanamine and 4.30 g (0.025 mole) of 3-(N,N-diethylamino)propylisothiocyanate in 400 ml of acetonitrile was refluxed for 16 hr. The solvent was removed in vacuo and the residue was dissolved in ether. The solution was extracted with three portions of w...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Isothiocyanate
Thiourea
null
null
c1ccccc1
null
C(C)#N
null
null
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCCN=C=S>C(C)#N>CCN(CC)CCCNC(=S)N(CCS(=O)(=O)c1ccccc1)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-00fb66882c6644f8a3f0fc09bf6d44fa
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.S=C(n1ccnc1)n1ccnc1>>CCN(CC)CCNC(=S)N(CCS(=O)(=O)c1ccccc1)C(C)C
C1(=CC=CC=C1)S(=O)(=O)CCNC(C)C.C(C)N(CCN)CC.C(=S)(N1C=NC=C1)N1C=NC=C1>>C(C)N(CCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=S)CC
[NH:11]([CH2:12][CH2:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1)[CH:23]([CH3:24])[CH3:25].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH2:8].c1cn([C:9](n2ccnc2)=[S:10])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][C:9](=[S:10])[N:11]([CH2:12][CH2:13][S:14](=[O:15])(=[O:1...
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.S=C(n1ccnc1)n1ccnc1
CCN(CC)CCNC(=S)N(CCS(=O)(=O)c1ccccc1)C(C)C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
8f6639d4c1d8e74fe1edd589fbd0e52f490ad6c8933b6e3ee8c7c59b99e2905a
ac8bed454cbd32bb2d251ac3f635c69390732f28930050cdce90686f9b13ad73
c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7](-[C;D1;H3:8])-[C;D1;H3:9].[S;D1;H0:10]=[C;H0;D3;+0:11](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[C:7](-[C;D1;H3:8])-[C;D1;H3:9])-[C;H0;D3;+0:11](=[S;D1;H0:10])-[NH;D2;+0:3]-[C:2]-[C:1]
72.5
[{"value": 72.5, "product": "C(C)N(CCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=S)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.1, "product": "C(C)N(CCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=S)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 2.78 g (0.024 mole) of N,N-diethylethylenediamine and 4.82 g (0.027 mole) of 1,1'-thiocarbonyldiimidazole in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 5.00 g (0.022 mole) of N-[2-(phenylsulfonyl)ethyl]-2-propanamine in 100 ml of tetrahydrofuran was added, and the sol...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine.Thiocarbonyl
Thiourea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
O1CCCC1
null
1
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.S=C(n1ccnc1)n1ccnc1>O1CCCC1>CCN(CC)CCNC(=S)N(CCS(=O)(=O)c1ccccc1)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ef1535005443433a943b7d450a9fc636
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCCCN.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCCCNC(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C
C1(=CC=CC=C1)S(=O)(=O)CCNC(C)C.C(=O)(N1C=NC=C1)N1C=NC=C1.C(C)N(CCCCN)CC>>C(C)N(CCCCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC
[NH:13]([CH2:14][CH2:15][S:16](=[O:17])(=[O:18])[c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1)[CH:25]([CH3:26])[CH3:27].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][CH2:8][CH2:9][NH2:10].c1cn([C:11](n2ccnc2)=[O:12])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][CH2:8][CH2:9][NH:10][C:11](=[O:12])[N:13]([CH2:...
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCCCN.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCCCNC(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C
null
null
O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7](-[C;D1;H3:8])-[C;D1;H3:9].[O;D1;H0:10]=[C;H0;D3;+0:11](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[C:7](-[C;D1;H3:8])-[C;D1;H3:9])-[C;H0;D3;+0:11](=[O;D1;H0:10])-[NH;D2;+0:3]-[C:2]-[C:1]
26.2
[{"value": 26.2, "product": "C(C)N(CCCCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 26.2, "product": "C(C)N(CCCCNC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4.40 g (0.0272 mole) of 1,1'-carbonyldiimidazole and 3.46 g (0.024 mole) of N,N-diethyl-1,4-butanediamine in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 5.00 g (0.0220 mole) of N-[2-(phenylsulfonyl)ethyl]-2-propanamine in 50 ml of tetrahydrofuran was added, and the so...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
O1CCCC1
null
null
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CCCCN.O=C(n1ccnc1)n1ccnc1>O1CCCC1>CCN(CC)CCCCNC(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-676a05e13ec14819a379f9e941d94caf
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CC(C)N.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CC(C)NC(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C
C1(=CC=CC=C1)S(=O)(=O)CCNC(C)C.C(=O)(N1C=NC=C1)N1C=NC=C1.C(C)N(CC(C)N)CC>>C(C)N(CC(C)NC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC
[NH:12]([CH2:13][CH2:14][S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)[CH:24]([CH3:25])[CH3:26].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH:7]([CH3:8])[NH2:9].c1cn([C:10](n2ccnc2)=[O:11])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH:7]([CH3:8])[NH:9][C:10](=[O:11])[N:12]([CH2:13][CH2:14][S:...
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CC(C)N.O=C(n1ccnc1)n1ccnc1
CCN(CC)CC(C)NC(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C
null
null
O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
c1ccccc1
[C:1]-[C:2](-[C;D1;H3:3])-[NH2;D1;+0:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8](-[C;D1;H3:9])-[C;D1;H3:10].[O;D1;H0:11]=[C;H0;D3;+0:12](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[C:8](-[C;D1;H3:9])-[C;D1;H3:10])-[C;H0;D3;+0:12](=[O;D1;H0:11])-[NH;D2;+0:4]-[C:2](-[C:1])-[C;D1;H3:3]
59.5
[{"value": 59.5, "product": "C(C)N(CC(C)NC(N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 12.15 g (0.075 mole) of 1,1'-carbonyl diimidazole and 7.50 g (0.0476 mole) of 1-diethylamino-2-propanamine in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 12.26 g (0.054 mole) of N-[2-(phenylsulfonyl)ethyl]-2-propanamine in 50 ml of tetrahydrofuran was added, and the so...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
O1CCCC1
null
1
CC(C)NCCS(=O)(=O)c1ccccc1.CCN(CC)CC(C)N.O=C(n1ccnc1)n1ccnc1>O1CCCC1>CCN(CC)CC(C)NC(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f9350ef6ad3d4d59a6d8bded0cf293e3
CC(C)NCCS(=O)(=O)c1ccccc1.NCCCN1CCCCC1.O=C(n1ccnc1)n1ccnc1>>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCCN1CCCCC1
C1(=CC=CC=C1)S(=O)(=O)CCNC(C)C.C(=O)(N1C=NC=C1)N1C=NC=C1.NCCCN1CCCCC1>>CC(C)N(C(=O)NCCCN1CCCCC1)CCS(=O)(=O)C1=CC=CC=C1
[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[NH2:18][CH2:19][CH2:20][CH2:21][N:22]1[CH2:23][CH2:24][CH2:25][CH2:26][CH2:27]1.c1cn([C:16](n2ccnc2)=[O:17])cn1>>[CH3:1][CH:2]([CH3:3])[N:4]([CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][...
CC(C)NCCS(=O)(=O)c1ccccc1.NCCCN1CCCCC1.O=C(n1ccnc1)n1ccnc1
CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCCN1CCCCC1
null
null
O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
O=C(NCCCN1CCCCC1)NCCS(=O)(=O)c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7](-[C;D1;H3:8])-[C;D1;H3:9].[O;D1;H0:10]=[C;H0;D3;+0:11](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:11](=[O;D1;H0:10])-[N;H0;D3;+0:6](-[C:5]-[C:4])-[C:7](-[C;D1;H3:8])-[C;D1;H3:9]
27.1
[{"value": 27.1, "product": "CC(C)N(C(=O)NCCCN1CCCCC1)CCS(=O)(=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 27.1, "product": "CC(C)N(C(=O)NCCCN1CCCCC1)CCS(=O)(=O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 5.16 g (0.0319 mole) of 1,1'-carbonyldiimidazole and 4.16 g (0.029 mole) of N-(3-aminopropyl)piperidine in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 6.13 g (0.027 mole) of N-[2-(phenylsulfonyl)ethyl]-2-propanamine in 50 ml of tetrahydrofuran was added, and the mixtur...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1.C1CC[NH]CC1
Other
O1CCCC1
null
1
CC(C)NCCS(=O)(=O)c1ccccc1.NCCCN1CCCCC1.O=C(n1ccnc1)n1ccnc1>O1CCCC1>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCCN1CCCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9fc3086f133b4cb882634b634e570ee1
CC(C)NCCS(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCNC(=O)N(CCS(=O)c1ccccc1)C(C)C
C1(=CC=CC=C1)S(=O)CCNC(C)C.C(=O)(N1C=NC=C1)N1C=NC=C1.C(C)N(CCN)CC>>C(C)N(CCNC(N(CCS(=O)C1=CC=CC=C1)C(C)C)=O)CC
[NH:11]([CH2:12][CH2:13][S:14](=[O:15])[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[CH:22]([CH3:23])[CH3:24].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH2:8].c1cn([C:9](n2ccnc2)=[O:10])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][C:9](=[O:10])[N:11]([CH2:12][CH2:13][S:14](=[O:15])[c:16]1[cH:17][...
CC(C)NCCS(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCNC(=O)N(CCS(=O)c1ccccc1)C(C)C
null
null
O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7](-[C;D1;H3:8])-[C;D1;H3:9].[O;D1;H0:10]=[C;H0;D3;+0:11](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[C:7](-[C;D1;H3:8])-[C;D1;H3:9])-[C;H0;D3;+0:11](=[O;D1;H0:10])-[NH;D2;+0:3]-[C:2]-[C:1]
55.9
[{"value": 55.9, "product": "C(C)N(CCNC(N(CCS(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 55.9, "product": "C(C)N(CCNC(N(CCS(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 4.70 g (0.029 mole) of 1,1'-carbonyldiimidazole- and 3.07 g (0.0265 mole) of N,N-diethylethylenediamine in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 8.00 g (0.0245 mole) of N-[2-(phenylsulfinyl)ethyl]-2-propanamine in 50 ml of tetrahydrofuran was added, and the mixtu...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
O1CCCC1
null
1
CC(C)NCCS(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1>O1CCCC1>CCN(CC)CCNC(=O)N(CCS(=O)c1ccccc1)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b2b3cfe9a1a74be8888f94a8f751e180
CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1.O=S(=O)(CCNCc1ccccc1)c1ccccc1>>CCN(CC)CCNC(=O)N(CCS(=O)(=O)c1ccccc1)Cc1ccccc1
C(=O)(N1C=NC=C1)N1C=NC=C1.C(C)N(CCN)CC.C(C1=CC=CC=C1)NCCS(=O)(=O)C1=CC=CC=C1>>C(C)N(CCNC(N(CCS(=O)(=O)C1=CC=CC=C1)CC1=CC=CC=C1)=O)CC
[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH2:8].c1cn([C:9](n2ccnc2)=[O:10])cn1.[NH:11]([CH2:12][CH2:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1)[CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][C:9](=[O:10])[N:11]([CH2:12][CH...
CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1.O=S(=O)(CCNCc1ccccc1)c1ccccc1
CCN(CC)CCNC(=O)N(CCS(=O)(=O)c1ccccc1)Cc1ccccc1
null
null
O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
O=S(=O)(CCNCc1ccccc1)c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7]-[c:8].[O;D1;H0:9]=[C;H0;D3;+0:10](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[C:7]-[c:8])-[C;H0;D3;+0:10](=[O;D1;H0:9])-[NH;D2;+0:3]-[C:2]-[C:1]
69.98
[{"value": 69.98, "product": "C(C)N(CCNC(N(CCS(=O)(=O)C1=CC=CC=C1)CC1=CC=CC=C1)=O)CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 3.89 (0.024 mole) of 1,1'-carbonyldiimidazole and 2.55 g (0.022 mole) of N,N-diethylethylenediamine in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 5.70 g (0.0183 mole) of N-benzyl-2-phenylsulfonylethanamine in 50 ml of tetrahydrofuran was added, and the mixture was ref...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1.c1ccccc1
Other
O1CCCC1
null
1
CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1.O=S(=O)(CCNCc1ccccc1)c1ccccc1>O1CCCC1>CCN(CC)CCNC(=O)N(CCS(=O)(=O)c1ccccc1)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-55f9bf21ef824a7cb9d80cb03f44809d
CCN(CC)CCNC(C)C.NCCS(=O)(=O)c1ccccc1.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCN(C(=O)NCCS(=O)(=O)c1ccccc1)C(C)C
C(C)N(CCNC(C)C)CC.C1(=CC=CC=C1)S(=O)(=O)CCN.C(=O)(N1C=NC=C1)N1C=NC=C1>>C(C)N(CCN(C(=O)NCCS(=O)(=O)C1=CC=CC=C1)C(C)C)CC
[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][CH:23]([CH3:24])[CH3:25].[NH2:11][CH2:12][CH2:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1.c1cn([C:9](n2ccnc2)=[O:10])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][N:8]([C:9](=[O:10])[NH:11][CH2:12][CH2:13][S:14](=[O:15])(=[O:16]...
CCN(CC)CCNC(C)C.NCCS(=O)(=O)c1ccccc1.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCN(C(=O)NCCS(=O)(=O)c1ccccc1)C(C)C
null
null
O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7](-[C;D1;H3:8])-[C;D1;H3:9].[O;D1;H0:10]=[C;H0;D3;+0:11](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:11](=[O;D1;H0:10])-[N;H0;D3;+0:6](-[C:5]-[C:4])-[C:7](-[C;D1;H3:8])-[C;D1;H3:9]
null
[]
null
null
1
HOUR
A mixture of 6.96 g (0.0376 mole) of 2-phenylsulfonylethanamine and 6.64 g (0.041 mole) of 1,1'-carbonyldiimidazole in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 6.16 g (0.039 mole) of N-[2-(diethylamino)ethyl]-2-propanamine in 50 ml of tetrahydrofuran was added, and the mixture w...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
O1CCCC1
null
1
CCN(CC)CCNC(C)C.NCCS(=O)(=O)c1ccccc1.O=C(n1ccnc1)n1ccnc1>O1CCCC1>CCN(CC)CCN(C(=O)NCCS(=O)(=O)c1ccccc1)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-54b66e4802a3406cb2dc05cb341eaba1
CC(C)NCCS(=O)(=O)c1ccccc1.CN1CCN(CCCN)CC1.O=C(n1ccnc1)n1ccnc1>>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCCN1CCN(C)CC1
NCCCN1CCN(CC1)C.C(=O)(N1C=NC=C1)N1C=NC=C1.C(\C=C/C(=O)O)(=O)O.C1(=CC=CC=C1)S(=O)(=O)CCNC(C)C>>C(\C=C/C(=O)O)(=O)O.CC(C)N(C(=O)NCCCN1CCN(CC1)C)CCS(=O)(=O)C1=CC=CC=C1
[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[NH2:18][CH2:19][CH2:20][CH2:21][N:22]1[CH2:23][CH2:24][N:25]([CH3:26])[CH2:27][CH2:28]1.c1cn([C:16](n2ccnc2)=[O:17])cn1>>[CH3:1][CH:2]([CH3:3])[N:4]([CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][cH:13]...
CC(C)NCCS(=O)(=O)c1ccccc1.CN1CCN(CCCN)CC1.O=C(n1ccnc1)n1ccnc1
CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCCN1CCN(C)CC1
null
null
CO.O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
O=C(NCCCN1CCNCC1)NCCS(=O)(=O)c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7](-[C;D1;H3:8])-[C;D1;H3:9].[O;D1;H0:10]=[C;H0;D3;+0:11](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:11](=[O;D1;H0:10])-[N;H0;D3;+0:6](-[C:5]-[C:4])-[C:7](-[C;D1;H3:8])-[C;D1;H3:9]
68.8
[{"value": 68.8, "product": "C(\\C=C/C(=O)O)(=O)O.CC(C)N(C(=O)NCCCN1CCN(CC1)C)CCS(=O)(=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 6.00 g (0.035 mole) of 1-(3-aminopropyl)-4-methylpiperazine and 6.97 g (0.043 mole) of 1,1'-carbonyldiimidazole in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 8.17 g (0.036 mole) of N-(2-phenylsulfonylethyl)-2-propanamine in 100 ml of tetrahydrofuran was added, and the...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1.C1C[NH]CC[NH]1
Other
CO.O1CCCC1
null
1
CC(C)NCCS(=O)(=O)c1ccccc1.CN1CCN(CCCN)CC1.O=C(n1ccnc1)n1ccnc1>CO.O1CCCC1>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCCN1CCN(C)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-696537874e0c4dd5a445f74308693ec2
CC(C)NC(C)CS(=O)(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCNC(=O)N(C(C)C)C(C)CS(=O)(=O)c1ccccc1.O
C(C)N(CCN)CC.C(=O)(N1C=NC=C1)N1C=NC=C1.CC(C)NC(CS(=O)(=O)C1=CC=CC=C1)C>>O.C(C)N(CCNC(N(C(CS(=O)(=O)C1=CC=CC=C1)C)C(C)C)=O)CC
[NH:11]([CH:12]([CH3:13])[CH3:14])[CH:15]([CH3:16])[CH2:17][S:18](=[O:19])([c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1)=[O:27].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH2:8].c1cn([C:9](n2ccnc2)=[O:10])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][C:9](=[O:10])[N:11]([CH:12]([CH3:13])[CH3:14])[C...
CC(C)NC(C)CS(=O)(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCNC(=O)N(C(C)C)C(C)CS(=O)(=O)c1ccccc1.O
null
null
O1CCCC1
Acylation
OtherReaction
790fd9b6942665d99bc38ff775379891b82637e44650212952f5cedda0ed0eb1
013dbbbfd9d5d2d5efa0ece1df2d405de29fafa80f1f880bc16f7f746e690bb0
c1ccccc1
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])-[NH;D2;+0:4]-[C:5](-[C;D1;H3:6])-[C:7]-[S;H0;D4;+0:8](=[O;D1;H0:9])(=[O;H0;D1;+0:10])-[c:11](:[c:12]):[c:13].[C:14]-[C:15]-[NH2;D1;+0:16].[O;D1;H0:17]=[C;H0;D3;+0:18](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:14]-[C:15]-[NH;D2;+0:16]-[C;H0;D3;+0:18](=[O;D1;H0:17])-[N;H0;D3;+0:4](-[C:2](-[C;D1;H3:1...
null
[]
null
null
null
null
A solution of 3.71 g (0.032 mole) of N,N-diethylethylenediamine and 5.83 (0.036 mole) of 1,1'-carbonyldiimidazole in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 8.30 g (0.030 mole) of N-(2-propyl)-1-(phenylsulfonyl)-2-propanamine in 50 ml of tetrahydrofuran was added and the soluti...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine.Sulfone
Urea.Sulfone
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
O1CCCC1
null
null
CC(C)NC(C)CS(=O)(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1>O1CCCC1>CCN(CC)CCNC(=O)N(C(C)C)C(C)CS(=O)(=O)c1ccccc1.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1bbdfdf4f42246edb2dbfdf161a6a0b2
CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)Cl.CCN(CC)CCNC>>CCN(CC)CCN(C)C(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C.O
C(C)N(CCNC)CC.C(C)N(CC)CC.C(CC(O)(C(=O)O)CC(=O)O)(=O)O.CC(C)N(C(=O)Cl)CCS(=O)(=O)C1=CC=CC=C1>>O.C(CC(O)(C(=O)O)CC(=O)O)(=O)O.C(C)N(CCN(C(=O)N(CCS(=O)(=O)C1=CC=CC=C1)C(C)C)C)CC
Cl[C:10](=[O:11])[N:12]([CH2:13][CH2:14][S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)[CH:24]([CH3:25])[CH3:26].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][CH3:9]>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][N:8]([CH3:9])[C:10](=[O:11])[N:12]([CH2:13][CH2:14][S:15](=[O:16])(=[O:1...
CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)Cl.CCN(CC)CCNC
CCN(CC)CCN(C)C(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C.O
null
null
CCOCC.CO.O1CCCC1
Acylation
N-alkylation of secondary amines with alkyl halides
21141392b95d6b95cd118c7c0b595c90f08886f6a08d558238622ce18df3aa9b
353c6e1db25433862a8bcf26ca332f6abeb45cb685806584bc65f8cfcb712540
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3](-[C:4])-[C:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C;D1;H3:9]>>[C:4]-[#7:3](-[C:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:8](-[C;D1;H3:9])-[C:7]-[C:6]
null
[]
null
null
null
null
A mixture of 6.65 g (0.023 mole) of N-(1-methylethyl)-N-[2-(phenylsulfonyl)ethyl]carbamic chloride; 3.0 g (0.023 mole) of N,N-diethyl-N'-methylethylenediamine and triethylamine (2.7 g, 0.0267 mole) in 400 ml of tetrahydrofuran was stirred at room temperature for 10 hr. The solvent was removed in vacuo, and the residue ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Tertiary amide.Secondary amine
Urea
null
null
c1ccccc1
null
CCOCC.CO.O1CCCC1
null
null
CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)Cl.CCN(CC)CCNC>CCOCC.CO.O1CCCC1>CCN(CC)CCN(C)C(=O)N(CCS(=O)(=O)c1ccccc1)C(C)C.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f4da05c15f66425caadd5d8639eb6bb2
CC(C)NCCCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCNC(=O)N(CCCCS(=O)(=O)c1ccccc1)C(C)C.O
C(=O)(N1C=NC=C1)N1C=NC=C1.C(C)N(CCN)CC.CC(C)NCCCCS(=O)(=O)C1=CC=CC=C1>>O.C(C)N(CCNC(N(CCCCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC
[NH:11]([CH2:12][CH2:13][CH2:14][CH2:15][S:16](=[O:17])([c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1)=[O:28])[CH:25]([CH3:26])[CH3:27].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH2:8].c1cn([C:9](n2ccnc2)=[O:10])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][C:9](=[O:10])[N:11]([CH2:12][CH2:13][CH2:...
CC(C)NCCCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCNC(=O)N(CCCCS(=O)(=O)c1ccccc1)C(C)C.O
null
null
C(Cl)(Cl)Cl.O1CCCC1
Acylation
OtherReaction
790fd9b6942665d99bc38ff775379891b82637e44650212952f5cedda0ed0eb1
013dbbbfd9d5d2d5efa0ece1df2d405de29fafa80f1f880bc16f7f746e690bb0
c1ccccc1
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])-[NH;D2;+0:4]-[C:5]-[C:6]-[C:7]-[C:8]-[S;H0;D4;+0:9](=[O;D1;H0:10])(=[O;H0;D1;+0:11])-[c:12](:[c:13]):[c:14].[C:15]-[C:16]-[NH2;D1;+0:17].[O;D1;H0:18]=[C;H0;D3;+0:19](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:15]-[C:16]-[NH;D2;+0:17]-[C;H0;D3;+0:19](=[O;D1;H0:18])-[N;H0;D3;+0:4](-[C:5]-[C:6]-[C:7]-...
69.8
[{"value": 42.2, "product": "O.C(C)N(CCNC(N(CCCCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.8, "product": "O.C(C)N(CCNC(N(CCCCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 1,1'-carbonyldiimidazole (6.00 g, 0.037 mole) and N,N-diethylethylenediamine (4.00 g, 0.034 mole) was stirred at room temperature for 2 hours in 200 ml of tetrahydrofuran. A solution of N-(1-methylethyl)-4-(phenylsulfonyl]-1-butylamine (free base 7.99 g, 0.0313 mole) in 100 ml of tetrahydrofuran was added...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine.Sulfone
Urea.Sulfone
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
C(Cl)(Cl)Cl.O1CCCC1
null
null
CC(C)NCCCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.O=C(n1ccnc1)n1ccnc1>C(Cl)(Cl)Cl.O1CCCC1>CCN(CC)CCNC(=O)N(CCCCS(=O)(=O)c1ccccc1)C(C)C.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3bf903c0996240489547e5913b65a55e
CC(C)NCCCCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.CO.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCNC(=O)N(CCCCCS(=O)(=O)c1ccccc1)C(C)C.O
CO.C(=O)(N1C=NC=C1)N1C=NC=C1.C(C)N(CCN)CC.CC(C)NCCCCCS(=O)(=O)C1=CC=CC=C1>>O.C(C)N(CCNC(N(CCCCCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC
[NH:11]([CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][S:17](=[O:18])(=[O:19])[c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1)[CH:26]([CH3:27])[CH3:28].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH2:8].C[OH:29].c1cn([C:9](n2ccnc2)=[O:10])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][C:9](=[O:10])[N:11]([CH2...
CC(C)NCCCCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.CO.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCNC(=O)N(CCCCCS(=O)(=O)c1ccccc1)C(C)C.O
null
null
C(Cl)(Cl)Cl.O1CCCC1
Acylation
OtherReaction
3a9361bdbd95be6f6498be3f52a439bd7b3c42ac2343fcede959a771740be9b3
6079f211a2cccdac0f05b041613d4ae0d7c41f3cbc8e16635694efeef0e716e4
c1ccccc1
C-[OH;D1;+0:1].[C:2]-[C:3]-[NH2;D1;+0:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8](-[C;D1;H3:9])-[C;D1;H3:10].[O;D1;H0:11]=[C;H0;D3;+0:12](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[C:8](-[C;D1;H3:9])-[C;D1;H3:10])-[C;H0;D3;+0:12](=[O;D1;H0:11])-[NH;D2;+0:4]-[C:3]-[C:2].[OH2;D0;+0:1]
66.6
[{"value": 66.6, "product": "O.C(C)N(CCNC(N(CCCCCS(=O)(=O)C1=CC=CC=C1)C(C)C)=O)CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 1,1'-carbonyldiimidazole (4.54 g, 0.028 mole) and N,N-diethylethylenediamine (2.90 g, 0.025 mole) in tetrahydrofuran was stirred for 1 hr at room temperature. A solution of N-(1-methylethyl)-5-(phenylsulfonyl)-1-pentanamine (6.74 g, 0.025 mole) in tetrahydrofuran (dried over 4 A molecular sieves) was adde...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine.Methanol
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
C(Cl)(Cl)Cl.O1CCCC1
null
null
CC(C)NCCCCCS(=O)(=O)c1ccccc1.CCN(CC)CCN.CO.O=C(n1ccnc1)n1ccnc1>C(Cl)(Cl)Cl.O1CCCC1>CCN(CC)CCNC(=O)N(CCCCCS(=O)(=O)c1ccccc1)C(C)C.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-996cfb8dec7f4d15aaf706f5b8c366a3
O=[N+]([O-])c1cc(Cl)c(NS(=O)(=O)c2ccccc2)cc1Cl>>Nc1cc(Cl)c([N+](=O)[O-])cc1Cl
ClC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C(=C1)[N+](=O)[O-])Cl>>ClC1=C(N)C=C(C(=C1)[N+](=O)[O-])Cl
O=S(=O)(c1ccccc1)[NH:1][c:2]1[cH:3][c:4]([Cl:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[Cl:12]>>[NH2:1][c:2]1[cH:3][c:4]([Cl:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[Cl:12]
O=[N+]([O-])c1cc(Cl)c(NS(=O)(=O)c2ccccc2)cc1Cl
Nc1cc(Cl)c([N+](=O)[O-])cc1Cl
null
null
S(O)(O)(=O)=O
Reduction
OtherReaction
2e17a3c810032c9f14c9fec7e34afbbdc0ecfd09afc752c87a3897df8c7aa53a
a7ea9d81d4cfa76d8b5a506ce4b577cf1cb07ecc98efc32d6e49796f60cf3810
c1ccccc1
O=S(=O)(-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4])-c1:c:c:c:c:c:1>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
24
HOUR
0.44 mole (154 g) of 2,5-dichloro-4-nitro-N-benzenesulphonylaniline prepared in the previous stage is suspended in 600 ml of concentrated sulphuric acid. After 24 hours' stirring at ambient temperature the reaction mixture is poured onto 5 kg of ice. The expected product precipitates. After filtering, washing to neutra...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Primary amine
c1ccccc1
null
c1ccccc1
HO-
S(O)(O)(=O)=O
null
24
O=[N+]([O-])c1cc(Cl)c(NS(=O)(=O)c2ccccc2)cc1Cl>S(O)(O)(=O)=O>Nc1cc(Cl)c([N+](=O)[O-])cc1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-617bfdd769eb46abb48d202834543d87
O=S(=O)(Nc1cc(Br)ccc1Br)c1ccccc1.O=[N+]([O-])O>>O=[N+]([O-])c1cc(Br)c(NS(=O)(=O)c2ccccc2)cc1Br
C(C)(=O)O.N(=O)[O-].[Na+].BrC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C=C1)Br.[N+](=O)(O)[O-]>>BrC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C(=C1)[N+](=O)[O-])Br
[cH:4]1[cH:5][c:6]([Br:7])[c:8]([NH:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][c:20]1[Br:21].O[N+:2](=[O:1])[O-:3]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([Br:7])[c:8]([NH:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][c:20]1[Br:21]
O=S(=O)(Nc1cc(Br)ccc1Br)c1ccccc1.O=[N+]([O-])O
O=[N+]([O-])c1cc(Br)c(NS(=O)(=O)c2ccccc2)cc1Br
null
null
O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=S(=O)(Nc1ccccc1)c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Br;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[Br;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
null
[]
90
CELSIUS
null
null
To 250 ml of acetic acid, diluted with 130 ml of water, are added: 1.5 g of sodium nitrite, 0.13 mole of 2,5-dibromo-N-benzenesulphonylaniline prepared in the previous stage and 0.78 mole (32.5 ml) of nitric acid (d=1.52). The reaction mixture is heated for 1 hour at 90° C. The reaction mixture, cooled beforehand, is p...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
O
90
null
O=S(=O)(Nc1cc(Br)ccc1Br)c1ccccc1.O=[N+]([O-])O>O>O=[N+]([O-])c1cc(Br)c(NS(=O)(=O)c2ccccc2)cc1Br
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dbe92f0c312a4853a6a2bebab89efc08
O=[N+]([O-])c1cc(Br)c(NS(=O)(=O)c2ccccc2)cc1Br>>Nc1cc(Br)c([N+](=O)[O-])cc1Br
S(O)(O)(=O)=O.BrC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C(=C1)[N+](=O)[O-])Br>>BrC1=C(N)C=C(C(=C1)[N+](=O)[O-])Br
O=S(=O)(c1ccccc1)[NH:1][c:2]1[cH:3][c:4]([Br:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[Br:12]>>[NH2:1][c:2]1[cH:3][c:4]([Br:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[Br:12]
O=[N+]([O-])c1cc(Br)c(NS(=O)(=O)c2ccccc2)cc1Br
Nc1cc(Br)c([N+](=O)[O-])cc1Br
null
null
O
Reduction
OtherReaction
2e17a3c810032c9f14c9fec7e34afbbdc0ecfd09afc752c87a3897df8c7aa53a
a7ea9d81d4cfa76d8b5a506ce4b577cf1cb07ecc98efc32d6e49796f60cf3810
c1ccccc1
O=S(=O)(-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4])-c1:c:c:c:c:c:1>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
15 ml of water are added, with due care, to 115 ml of concentrated sulphuric acid; the temperature rises to 70° C. 0.105 mole (46 g) of 2,5-dibromo-4-nitro-N-benzenesulphonylaniline are then added. The temperature is maintained at 70°-78° C. for 2 hours. The reaction mixture is poured into 1 kg of ice and water; the ex...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Primary amine
c1ccccc1
null
c1ccccc1
HO-
O
null
null
O=[N+]([O-])c1cc(Br)c(NS(=O)(=O)c2ccccc2)cc1Br>O>Nc1cc(Br)c([N+](=O)[O-])cc1Br
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3dbdfcae709944628a41bf0158fca242
Nc1cc(F)ccc1F.O=S(=O)(Cl)c1ccccc1>>O=S(=O)(Nc1cc(F)ccc1F)c1ccccc1
Cl.FC1=C(N)C=C(C=C1)F.N1=CC=CC=C1.C1(=CC=CC=C1)S(=O)(=O)Cl>>FC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C=C1)F
[NH2:4][c:5]1[cH:6][c:7]([F:8])[cH:9][cH:10][c:11]1[F:12].Cl[S:2](=[O:1])(=[O:3])[c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[O:1]=[S:2](=[O:3])([NH:4][c:5]1[cH:6][c:7]([F:8])[cH:9][cH:10][c:11]1[F:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
Nc1cc(F)ccc1F.O=S(=O)(Cl)c1ccccc1
O=S(=O)(Nc1cc(F)ccc1F)c1ccccc1
null
null
O
Miscellaneous
Sulfonamide synthesis (Schotten-Baumann) primary amine
a86b0632821e188c0a5dc5a5a2aac298ab3eccaee8a52ba46078c3d5975a290d
50f8fbf3d327483c3eeff8f6cbd4065e4c7600bb501fbe08958a5c79a0926428
O=S(=O)(Nc1ccccc1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[O;D1;H0:2]=[S;H0;D4;+0:1](=[O;D1;H0:3])(-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10])-[c:4](:[c:5]):[c:6]
null
[]
40
CELSIUS
null
null
0.194 mole (25 g) of 2,5-difluoroaniline is added to 125 ml of pyridine. 0.2 mole (25.5 ml) of benzenesulphonyl chloride is added, while the temperature is between 35° C. and 45° C. The temperature is maintained at 40° C. for 1 hour after the addition is completed, and then the reaction mixture is poured onto 1 kg of i...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccccc1.c1ccccc1
HCl
O
40
null
Nc1cc(F)ccc1F.O=S(=O)(Cl)c1ccccc1>O>O=S(=O)(Nc1cc(F)ccc1F)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6690a163904649839ee51f83c59f74e3
O=S(=O)(Nc1cc(F)ccc1F)c1ccccc1.O=[N+]([O-])O>>O=[N+]([O-])c1cc(F)c(NS(=O)(=O)c2ccccc2)cc1F
C(C)(=O)O.N(=O)[O-].[Na+].FC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C=C1)F.[N+](=O)(O)[O-]>>FC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C(=C1)[N+](=O)[O-])F
[cH:4]1[cH:5][c:6]([F:7])[c:8]([NH:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][c:20]1[F:21].O[N+:2](=[O:1])[O-:3]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([F:7])[c:8]([NH:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][c:20]1[F:21]
O=S(=O)(Nc1cc(F)ccc1F)c1ccccc1.O=[N+]([O-])O
O=[N+]([O-])c1cc(F)c(NS(=O)(=O)c2ccccc2)cc1F
null
null
O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=S(=O)(Nc1ccccc1)c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[F;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[F;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
null
[]
96
CELSIUS
null
null
To 310 ml of acetic acid diluted with 160 ml of water are added: 1.5 g of sodium nitrite, 0.16 mole (42 g) of 2,5-difluoro-N-benzenesulphonylaniline prepared in the previous stage and 0.94 mole (39 ml) of nitric acid (d=1.52). The reaction mixture is heated to 96° C. for 1 hour. After cooling it is poured onto 1 kg of ...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
O
96
null
O=S(=O)(Nc1cc(F)ccc1F)c1ccccc1.O=[N+]([O-])O>O>O=[N+]([O-])c1cc(F)c(NS(=O)(=O)c2ccccc2)cc1F
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8734794de3904b748c5147f7f30b1fb2
O=[N+]([O-])c1cc(F)c(NS(=O)(=O)c2ccccc2)cc1F>>Nc1cc(F)c([N+](=O)[O-])cc1F
S(O)(O)(=O)=O.FC1=C(NS(=O)(=O)C2=CC=CC=C2)C=C(C(=C1)[N+](=O)[O-])F>>FC1=C(N)C=C(C(=C1)[N+](=O)[O-])F
O=S(=O)(c1ccccc1)[NH:1][c:2]1[cH:3][c:4]([F:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[F:12]>>[NH2:1][c:2]1[cH:3][c:4]([F:5])[c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]1[F:12]
O=[N+]([O-])c1cc(F)c(NS(=O)(=O)c2ccccc2)cc1F
Nc1cc(F)c([N+](=O)[O-])cc1F
null
null
O
Reduction
OtherReaction
2e17a3c810032c9f14c9fec7e34afbbdc0ecfd09afc752c87a3897df8c7aa53a
a7ea9d81d4cfa76d8b5a506ce4b577cf1cb07ecc98efc32d6e49796f60cf3810
c1ccccc1
O=S(=O)(-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4])-c1:c:c:c:c:c:1>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
70
CELSIUS
null
null
10 ml of water are added with due care to 75 ml of concentrated sulphuric acid; the temperature rises to 70° C. 0.105 mole (33 g) of 2,5-difluoro-4-nitro-N-benzenesulphonylaniline prepared in the previous stage is then added. The temperature is maintained at 70° C. for 2 hours. The reaction mixture is poured onto 1 kg ...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Primary amine
c1ccccc1
null
c1ccccc1
HO-
O
70
null
O=[N+]([O-])c1cc(F)c(NS(=O)(=O)c2ccccc2)cc1F>O>Nc1cc(F)c([N+](=O)[O-])cc1F
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b1ae56670021489c8b0a911be0cc61d1
NCCO.Nc1cc(Cl)c(Cl)cc1[N+](=O)[O-]>>Nc1cc(NCCO)c(Cl)cc1[N+](=O)[O-]
ClC1=CC(=C(N)C=C1Cl)[N+](=O)[O-].C(O)CN>>NC1=C(C=C(C(=C1)NCCO)Cl)[N+](=O)[O-]
[NH2:5][CH2:6][CH2:7][OH:8].Cl[c:4]1[cH:3][c:2]([NH2:1])[c:12]([N+:13](=[O:14])[O-:15])[cH:11][c:9]1[Cl:10]>>[NH2:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][CH2:7][OH:8])[c:9]([Cl:10])[cH:11][c:12]1[N+:13](=[O:14])[O-:15]
NCCO.Nc1cc(Cl)c(Cl)cc1[N+](=O)[O-]
Nc1cc(NCCO)c(Cl)cc1[N+](=O)[O-]
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[Cl;D1;H0:5]):[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[Cl;D1;H0:5]):[c:6]
null
[]
null
null
null
null
0.11 mole (22.8 g) of 4,5-dichloro-2-nitroaniline is added to a solution of 0.55 mole (33.3 ml) of ethanolamine in 70 ml of dioxane. The reaction mixture is heated for 6 hours in refluxing dioxane. After dilution with water and neutralization with concentrated hydrochloric acid, the expected product precipitates. Condi...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HCl
O1CCOCC1
null
null
NCCO.Nc1cc(Cl)c(Cl)cc1[N+](=O)[O-]>O1CCOCC1>Nc1cc(NCCO)c(Cl)cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b8234a4b6b1c4b76ac1f1dde36971aea
NCCN.O=[N+]([O-])c1cc(Cl)c(Cl)cc1Cl>>NCCNc1cc(Cl)c(Cl)cc1[N+](=O)[O-]
ClC1=C(C=C(C(=C1)Cl)Cl)[N+](=O)[O-].C(CN)N.C(C)O>>ClC1=CC(=C(NCCN)C=C1Cl)[N+](=O)[O-]
[NH2:1][CH2:2][CH2:3][NH2:4].Cl[c:5]1[cH:6][c:7]([Cl:8])[c:9]([Cl:10])[cH:11][c:12]1[N+:13](=[O:14])[O-:15]>>[NH2:1][CH2:2][CH2:3][NH:4][c:5]1[cH:6][c:7]([Cl:8])[c:9]([Cl:10])[cH:11][c:12]1[N+:13](=[O:14])[O-:15]
NCCN.O=[N+]([O-])c1cc(Cl)c(Cl)cc1Cl
NCCNc1cc(Cl)c(Cl)cc1[N+](=O)[O-]
null
null
O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:9]-[C:8]-[C:7]):[c:2]:[c:3]
null
[]
null
null
null
null
0.13 mole (30.6 g) of 2,4,5-trichloronitrobenzene is added to a solution of 78 g of ethylenediamine in 100 ml of 96° ethanol and 117 ml of water. After heating under reflux for 1 h 30 min, the reaction mixture is cooled. After dilution with iced water, the expected product precipitates. It melts as 84° C.-87° C. Condit...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HCl
O
null
null
NCCN.O=[N+]([O-])c1cc(Cl)c(Cl)cc1Cl>O>NCCNc1cc(Cl)c(Cl)cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4c54e3751d4842d7a5094d5ea6aa2e59
NCCNc1cc(Cl)c(Cl)cc1[N+](=O)[O-].NCCO>>NCCNc1cc(NCCO)c(Cl)cc1[N+](=O)[O-]
ClC1=CC(=C(NCCN)C=C1Cl)[N+](=O)[O-].C(O)CN>>ClC1=C(NCCO)C=C(C(=C1)[N+](=O)[O-])NCCN
Cl[c:7]1[cH:6][c:5]([NH:4][CH2:3][CH2:2][NH2:1])[c:15]([N+:16](=[O:17])[O-:18])[cH:14][c:12]1[Cl:13].[NH2:8][CH2:9][CH2:10][OH:11]>>[NH2:1][CH2:2][CH2:3][NH:4][c:5]1[cH:6][c:7]([NH:8][CH2:9][CH2:10][OH:11])[c:12]([Cl:13])[cH:14][c:15]1[N+:16](=[O:17])[O-:18]
NCCNc1cc(Cl)c(Cl)cc1[N+](=O)[O-].NCCO
NCCNc1cc(NCCO)c(Cl)cc1[N+](=O)[O-]
null
null
O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[Cl;D1;H0:5]):[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[Cl;D1;H0:5]):[c:6]
null
[]
null
null
null
null
0.04 mole (10 g) of 4,5-dichloro-2-nitro-N-β-aminoethylaniline prepared in the 1st stage is heated in 40 ml of monoethanolamine for 30 minutes to 100° C. The reaction mixture is diluted with 450 ml of iced water. An impurity is precipitated by adding hydrochloric acid and is removed by filtration. The filtrate is made ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HCl
O
null
null
NCCNc1cc(Cl)c(Cl)cc1[N+](=O)[O-].NCCO>O>NCCNc1cc(NCCO)c(Cl)cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-363bfb4003904efb8b5cf573bf65a281
NCCO.Nc1cc(Br)c([N+](=O)[O-])cc1Br>>Nc1cc(NCCO)c([N+](=O)[O-])cc1Br
BrC1=C(N)C=C(C(=C1)[N+](=O)[O-])Br.BrC1=C(N)C=C(C(=C1)[N+](=O)[O-])Br.C(O)CN>>OCCNC1=C(C=C(C(=C1)N)Br)[N+](=O)[O-]
[NH2:5][CH2:6][CH2:7][OH:8].Br[c:4]1[cH:3][c:2]([NH2:1])[c:14]([Br:15])[cH:13][c:9]1[N+:10](=[O:11])[O-:12]>>[NH2:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][CH2:7][OH:8])[c:9]([N+:10](=[O:11])[O-:12])[cH:13][c:14]1[Br:15]
NCCO.Nc1cc(Br)c([N+](=O)[O-])cc1Br
Nc1cc(NCCO)c([N+](=O)[O-])cc1Br
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[NH;D2;+0:9]-[C:8]-[C:7]):[c:2]:[c:3]
null
[]
null
null
null
null
0.02 mole (5.92 g) of 2,5-dibromo-4-nitroaniline (compound B) is added to 15 ml of 96° ethanol to which 12 ml of ethanolamine have been added. The mixture is heated in refluxing alcohol for 6 h 30 min. After cooling and dilution of the reaction mixture with 100 ml of iced water, the expected product precipitates. Condi...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HBr
C(C)O
null
null
NCCO.Nc1cc(Br)c([N+](=O)[O-])cc1Br>C(C)O>Nc1cc(NCCO)c([N+](=O)[O-])cc1Br
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4db7c84e1eb24c088f78a0ceb966e2c1
CSCCO.O=[N+]([O-])c1ccccc1F>>CSCCOc1ccccc1[N+](=O)[O-]
OCCSC.[H-].[Na+].FC1=C(C=CC=C1)[N+](=O)[O-]>>CSCCOC1=C(C=CC=C1)[N+](=O)[O-]
[CH3:1][S:2][CH2:3][CH2:4][OH:5].F[c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[N+:12](=[O:13])[O-:14]>>[CH3:1][S:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[N+:12](=[O:13])[O-:14]
CSCCO.O=[N+]([O-])c1ccccc1F
CSCCOc1ccccc1[N+](=O)[O-]
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[C:8]-[C:7]):[c:2]:[c:3]
null
[]
40
CELSIUS
20
MINUTE
16.3 g of 2-hydroxyethylmethyl sulfide are added dropwise at 20°-25° C. to 8.5 g of a 55% NaH suspension in 150 ml of absolute tetrahydrofuran. The mixture is stirred for 1 hour at 20° C. and for 20 minutes at 40° C., and 25 g of 1-fluoro-2-nitrobenzene are subsequently added at 20° C. After the suspension has been sti...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1
HF
O1CCCC1
40
0.333333
CSCCO.O=[N+]([O-])c1ccccc1F>O1CCCC1>CSCCOc1ccccc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-242fffddb7bc46a48d2d17eb9c1eb71e
CSCCOc1ccccc1[N+](=O)[O-]>>CSCCOc1ccccc1N
CSCCOC1=C(C=CC=C1)[N+](=O)[O-].[H][H]>>CSCCOC1=C(N)C=CC=C1
O=[N+:12]([O-])[c:11]1[c:6]([O:5][CH2:4][CH2:3][S:2][CH3:1])[cH:7][cH:8][cH:9][cH:10]1>>[CH3:1][S:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[NH2:12]
CSCCOc1ccccc1[N+](=O)[O-]
CSCCOc1ccccc1N
null
[Ni]
O1CCCC1
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
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
33.9 g of he oil obtained under (a) are hydrogenated in 100 ml of absolute tetrahydrofuran, with the addition of 13.6 g of Raney nickel, under normal pressure (hydrogen absorption=10.6 liters). After the catalyst has been filtered off, the filtrate is concentrated by evaporation, and then purified by means of chromatog...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Ni].O1CCCC1
null
null
CSCCOc1ccccc1[N+](=O)[O-]>[Ni].O1CCCC1>CSCCOc1ccccc1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8ff8d568cf1248518f7da91bcabe7759
CSCCOc1ccccc1N>>CSCCOc1ccccc1NN
O.O.Cl[Sn]Cl.NC1=CC=CC=C1.CSCCOC1=C(N)C=CC=C1.[OH-].[Na+].N(=O)[O-].[Na+]>>CSCCOC1=C(C=CC=C1)NN
[CH3:1][S:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[NH2:12]>>[CH3:1][S:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[NH:12][NH2:13]
CSCCOc1ccccc1N
CSCCOc1ccccc1NN
null
null
C(C)(=O)O.Cl.O.CCOCC
Miscellaneous
OtherReaction
c4079cd46dafde13b56adeac363106820ab4184dee8b1ca632594de2bba804bd
5c8e4e590249a630a16b10bd7a77b27600fffbea367a0b585a920dd877e5471b
c1ccccc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]>>[N;D1;H2:5]-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
4
HOUR
27.4 g of the aniline obtained under (b) are placed into 45 ml of glacial acetic acid and, with ice cooling, a mixture of 37 ml of concentrated HCl and 75 ml of H2O is added. The formed suspension is diazotised at 0°-5° C. with 10.3 g of NaNO2 in 22 ml of water. The diazonium solution is subsequently stirred at 0° C. f...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Hydrazine
null
null
c1ccccc1
Other
C(C)(=O)O.Cl.O.CCOCC
null
4
CSCCOc1ccccc1N>C(C)(=O)O.Cl.O.CCOCC>CSCCOc1ccccc1NN
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e8648a916c7c4fcfb8175365162e18a3
COC(=O)Cl.CSCCOc1ccccc1NN>>COC(=O)NNc1ccccc1OCCSC
COC(=O)Cl.CSCCOC1=C(C=CC=C1)NN.O>>COC(=O)NNC1=C(C=CC=C1)OCCSC
Cl[C:3]([O:2][CH3:1])=[O:4].[NH2:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[O:13][CH2:14][CH2:15][S:16][CH3:17]>>[CH3:1][O:2][C:3](=[O:4])[NH:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[O:13][CH2:14][CH2:15][S:16][CH3:17]
COC(=O)Cl.CSCCOc1ccccc1NN
COC(=O)NNc1ccccc1OCCSC
null
null
C(C)N(C(C)C)C(C)C.O1CCCC1
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
5be28d87ebf4e99b19d55116b9ee6a2de77dfa39d592d5f1181884aff5e22c5f
5fd6250903fa66c378faf3ffa4e2360187bf8e16b5a0c6900f15dfbc5082c0be
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[NH2;D1;+0:5]-[#7:6]-[c:7]>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[#7:6]-[c:7]
null
[]
20
CELSIUS
2
HOUR
5.6 ml of chloroformic acid methyl ester are added dropwise at 0° C. to 14.4 g of 2-(2-methylthioethoxy)-phenylhydrazine in 100 ml of tetrahydrofuran and 14 g of N-ethyldiisopropylamine. The reaction mixture is stirred at 20° C. for 2 hours; H2O is then added, and the mixture is repeatedly extracted with ethyl acetate....
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Hydrazine
Acylhydrazine
null
null
c1ccccc1
HCl
C(C)N(C(C)C)C(C)C.O1CCCC1
20
2
COC(=O)Cl.CSCCOc1ccccc1NN>C(C)N(C(C)C)C(C)C.O1CCCC1>COC(=O)NNc1ccccc1OCCSC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f06ba04cb6474d75ba73dea89e898e68
COC(=O)NNc1ccccc1OCCSC.O=C(Cl)Cl>>COC(=O)NN(C(=O)Cl)c1ccccc1OCCSC
C(=O)(Cl)Cl.COC(=O)NNC1=C(C=CC=C1)OCCSC>>COC(=O)NN(C1=C(C=CC=C1)OCCSC)C(=O)Cl
[CH3:1][O:2][C:3](=[O:4])[NH:5][NH:6][c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[O:16][CH2:17][CH2:18][S:19][CH3:20].Cl[C:7](=[O:8])[Cl:9]>>[CH3:1][O:2][C:3](=[O:4])[NH:5][N:6]([C:7](=[O:8])[Cl:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[O:16][CH2:17][CH2:18][S:19][CH3:20]
COC(=O)NNc1ccccc1OCCSC.O=C(Cl)Cl
COC(=O)NN(C(=O)Cl)c1ccccc1OCCSC
null
null
C1(=CC=CC=C1)C
Acylation
N-alkylation of secondary amines with alkyl halides
db2f2d9badbb4cb36546ceda2ff379720def5866cf636a6d826453d7aa31a0ea
bfae58b08a51df04e7066f096095322c7298aefc6db308d508a4f7157775bd3b
c1ccccc1
Cl-[C;H0;D3;+0:1](-[Cl;D1;H0:2])=[O;D1;H0:3].[C;D1;H3:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[#7:8]-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C;D1;H3:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[#7:8]-[N;H0;D3;+0:9](-[C;H0;D3;+0:1](-[Cl;D1;H0:2])=[O;D1;H0:3])-[c:10](:[c:11]):[c:12]
null
[]
90
CELSIUS
null
null
80 ml of a 20% solution of phosgene in toluene are added at 20° C. to 14.1 g of 2-[2-(2-methylthioethoxy)-phenyl]-hydrazinecarboxylic acid methyl ester in 130 ml of toluene. The reaction mixture is subsequently heated for 3 hours at 90° C., and the solvent is then removed. Recrystallisation of the residue in ethyl alco...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Acylhydrazine
Acyl halide.Acylhydrazine
null
null
c1ccccc1
HCl
C1(=CC=CC=C1)C
90
null
COC(=O)NNc1ccccc1OCCSC.O=C(Cl)Cl>C1(=CC=CC=C1)C>COC(=O)NN(C(=O)Cl)c1ccccc1OCCSC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f5275a19c7a34928b700f9075a50c3db
CC(=O)CC(C)=O.N#CNC(=N)N>>Cc1cc(C)nc(NC#N)n1
C(#N)NC(=N)N.CC(CC(C)=O)=O.Cl>>C(#N)NC1=NC(=CC(=N1)C)C
O=[C:2]([CH3:1])[CH2:3][C:4](=O)[CH3:5].[NH:6]=[C:7]([NH:8][C:9]#[N:10])[NH2:11]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[n:6][c:7]([NH:8][C:9]#[N:10])[n:11]1
CC(=O)CC(C)=O.N#CNC(=N)N
Cc1cc(C)nc(NC#N)n1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
13c4f8274b8a1498bbf21922aa6710f05b644e60bec8d6f0e0485988f777d70e
e8142154ce82c2e242e52c937b939f3fefdc51b29f1e30581e6f69472c9bf693
c1cncnc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[CH2;D2;+0:3]-[C;H0;D3;+0:4](=O)-[C;D1;H3:5].[N;D1;H0:6]#[C:7]-[#7:8]-[C;H0;D3;+0:9](-[NH2;D1;+0:10])=[NH;D1;+0:11]>>[C;D1;H3:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[c;H0;D3;+0:4](-[C;D1;H3:5]):[n;H0;D2;+0:11]:[c;H0;D3;+0:9](-[#7:8]-[C:7]#[N;D1;H0:6]):[n;H0;D2;+0:10]:1
70
[{"value": 70.0, "product": "C(#N)NC1=NC(=CC(=N1)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.9, "product": "C(#N)NC1=NC(=CC(=N1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
null
null
A mixture of 42 g (0.5 mol) of cyanoguanidine ("dicyanodiamide") and 50 g (0.5 mol) of 2,4-pentanedione ("acetylacetone") is heated to 120° C. for 15 hours. The reaction mixture is then cooled, after which 500 ml of water are added and the solution is acidified with hydrochloric acid at 0° C. to 10° C. The product obta...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Primary amine
null
null
c1cncnc1
c1cncnc1
HO-
O
120
null
CC(=O)CC(C)=O.N#CNC(=N)N>O>Cc1cc(C)nc(NC#N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-337e60123b3b4db0a8dbe09ecff88ae9
CC(=O)CC(C)=O.N#CNC(=N)N>>Cc1cc(C)nc(NC#N)n1
C(#N)NC(=N)N.CC(CC(C)=O)=O.Cl>>C(#N)NC1=NC(=CC(=N1)C)C
O=[C:2]([CH3:1])[CH2:3][C:4](=O)[CH3:5].[NH:6]=[C:7]([NH:8][C:9]#[N:10])[NH2:11]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[n:6][c:7]([NH:8][C:9]#[N:10])[n:11]1
CC(=O)CC(C)=O.N#CNC(=N)N
Cc1cc(C)nc(NC#N)n1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
13c4f8274b8a1498bbf21922aa6710f05b644e60bec8d6f0e0485988f777d70e
e8142154ce82c2e242e52c937b939f3fefdc51b29f1e30581e6f69472c9bf693
c1cncnc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[CH2;D2;+0:3]-[C;H0;D3;+0:4](=O)-[C;D1;H3:5].[N;D1;H0:6]#[C:7]-[#7:8]-[C;H0;D3;+0:9](-[NH2;D1;+0:10])=[NH;D1;+0:11]>>[C;D1;H3:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[c;H0;D3;+0:4](-[C;D1;H3:5]):[n;H0;D2;+0:11]:[c;H0;D3;+0:9](-[#7:8]-[C:7]#[N;D1;H0:6]):[n;H0;D2;+0:10]:1
70
[{"value": 70.0, "product": "C(#N)NC1=NC(=CC(=N1)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.9, "product": "C(#N)NC1=NC(=CC(=N1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
null
null
A mixture of 42 g (0.5 mol) of cyanoguanidine ("dicyanodiamide") and 50 g (0.5 mol) of 2,4-pentanedione ("acetylacetone") is heated to 120° C. for 15 hours. The reaction mixture is then cooled, after which 500 ml of water are added and the solution is acidified with hydrochloric acid at 0° C. to 10° C. The product obta...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Primary amine
null
null
c1cncnc1
c1cncnc1
HO-
O
120
null
CC(=O)CC(C)=O.N#CNC(=N)N>O>Cc1cc(C)nc(NC#N)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6d3bb0315e504c3db3692c33e7836381
OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O>>OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO
C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@@H]2[C@H](O[C@H]([C@@H]([C@H]2O)O)O)CO)O)O)O)O.[H][H]>>C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@H]([C@@H](CO)O)[C@@H]([C@H](CO)O)O)O)O)O)O
[OH:1][CH2:2][C@H:3]1[O:4][C@@H:22]([OH:23])[C@H:20]([OH:21])[C@@H:18]([OH:19])[C@@H:5]1[O:6][C@H:7]1[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12]([OH:13])[C@H:14]([OH:15])[C@H:16]1[OH:17]>>[OH:1][CH2:2][C@@H:3]([OH:4])[C@@H:5]([O:6][C@H:7]1[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12]([OH:13])[C@H:14]([OH:15])[C@H:16]1[OH:17])[C@H:...
OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O
OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO
null
[Ni]
null
Reduction
OtherReaction
93bad9e1481d9297027cc2205dbf9942d4ce365c281baf2a9085a614009c66b8
81b1ad4a7cad3c1b76b9a651363a849ef67dca7066b2c65cf8c797861273206f
C1CCOCC1
[C:1]-[C:2]1-[C:3]-[C:4]-[C:5](-[O;D1;H1:6])-[C@H;D3;+0:7](-[O;D1;H1:8])-[O;H0;D2;+0:9]-1>>[C:1]-[C:2](-[OH;D1;+0:9])-[C:3]-[C:4]-[C:5](-[O;D1;H1:6])-[CH2;D2;+0:7]-[O;D1;H1:8]
null
[]
null
null
null
null
A 50% aqueous solution of the highly-purified maltose was placed in an autoclave, and added with Raney nickel catalyst in an amount of 10%. Thereafter, the content was heated to 90°-125° C., and hydrogenation was effected at the temperature and a hydrogen pressure of 20-100 kg/cm2. After completion of the hydrogenation...
10.6084/m9.figshare.5104873.v1
null
Ether
Primary alcohol.Secondary alcohol
C1CCOCC1
null
C1CCOCC1
null
[Ni]
null
null
OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O>[Ni]>OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-876c8ad5813343f88cacf0ee9c0dee04
OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O>>OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO.OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO.OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](...
C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@@H]2[C@H](O[C@H]([C@@H]([C@H]2O)O)O)CO)O)O)O)O>>OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@H]([C@@H](CO)O)[C@@H]([C@H](CO)O)O)O)O)O)O.C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@@H]2[C@H](O[C@@H]([C@@H]([C@H]2O)O)O[C@H]([C@@H](CO)O)[C@@H]([C@H](C...
[OH:1][C@H:2]1[C@H:42]([OH:4])[O:43][C@H:21]([CH2:22][OH:23])[C@@H:47]([O:48][C@H:49]2[O:50][C@H:51]([CH2:52][OH:53])[C@@H:54]([OH:55])[C@H:56]([OH:57])[C@H:58]2[OH:59])[C@@H:60]1[OH:61]>>[OH:1][CH2:2][C@@H:3]([OH:4])[C@@H:5]([OH:6])[C@H:7]([OH:8])[C@@H:9]([OH:10])[CH2:11][OH:12].[OH:13][CH2:14][C@@H:15]([OH:16])[C@@H:...
OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O
OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO.OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO.OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO
null
[Ni]
null
Heteroatom Alkylation and Arylation
OtherReaction
d3a1656cd59da9f3f895c4de466f4ef60e84b8de5788edbd62c4fda36ca8a4d0
515bdaf89df1395d99a4348c18f1eae4dce256da814e2bf511d567890d844f9b
C1CCOCC1.C1CC[C@@H](O[C@H]2CCCOC2)OC1
[#8:1]-[C:2]-[#8:3]-[C@@H;D3;+0:4]1-[C@@H;D3;+0:5](-[C:6]-[O;D1;H1:7])-[O;H0;D2;+0:8]-[C@@H;D3;+0:9](-[OH;D1;+0:10])-[C@H;D3;+0:11](-[O;D1;H1:12])-[C@H;D3;+0:13]-1-[O;D1;H1:14]>>[#8:1]-[C:2]-[#8:3]-[C@@H;D3;+0:4]1-[C:15](-[C:16])-[O;H0;D2;+0:8]-[C@H;D3;+0:9](-[#8:17]-[C:18])-[C:19](-[O;D1;H1:20])-[C@H;D3;+0:13]-1-[O;D1...
null
[]
null
null
null
null
After adjusting the concentration of the maltose solution to 50%, to the concentrate was added Raney nickel catalyst in an amount of 10%, and the admixture was then heated to 90°-125° C. under stirring conditions, and hydrogenated at this temperature under a hydrogen pressure of 20-100 kg/cm2. After completion of the h...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Secondary alcohol.Secondary alcohol.Secondary alcohol
Ether.Ether.Ether.Ether.Ether.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcoho...
C1CCOCC1
C1CCOCC1.C1CCOCC1
C1CCOCC1.C1CCOCC1.C1CCOCC1
Other
[Ni]
null
null
OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O>[Ni]>OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO.OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO.OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@H](O)[C@H]1O)[C@H](O)[C@...
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fc92f46fd2df4e82ac255cb55bc6c991
Cc1ccccc1-n1[nH]c(C(N)=O)cc1=O>>Cc1ccccc1-n1[nH]c(C#N)cc1=O
P(=O)(Cl)(Cl)Cl.C(N)(=O)C=1NN(C(C1)=O)C1=C(C=CC=C1)C.C(C)#N>>C(#N)C=1NN(C(C1)=O)C1=C(C=CC=C1)C
O=[C:11]([c:10]1[nH:9][n:8](-[c:7]2[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]2)[c:14](=[O:15])[cH:13]1)[NH2:12]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1-[n:8]1[nH:9][c:10]([C:11]#[N:12])[cH:13][c:14]1=[O:15]
Cc1ccccc1-n1[nH]c(C(N)=O)cc1=O
Cc1ccccc1-n1[nH]c(C#N)cc1=O
null
null
CN(C=O)C
Miscellaneous
OtherReaction
5094e9d814705bbdc421edbf7e9198e499e70e93916e2cec6eefbc82d1ba5440
32b9893bcb5223559a9d02852f8392cf6473aacfb044a52ba4e9cb9c29edb170
O=c1cc[nH]n1-c1ccccc1
O=[C;H0;D3;+0:1](-[NH2;D1;+0:2])-[c:3]1:[#7;a:4]:[#7;a:5](-[c:6]):[c:7]:[c:8]:1>>[N;H0;D1;+0:2]#[C;H0;D2;+0:1]-[c:3]1:[#7;a:4]:[#7;a:5](-[c:6]):[c:7]:[c:8]:1
null
[]
null
null
null
null
22.5 g of 3-carbamoyl-1-(2-methylphenyl)-5-pyrazolone and 150 ml of acetonitrile were put into a 300 ml three-necked flask. A mixture solution of 35 ml of phosphorus oxychloride and 100 ml of N,N-dimethylformamide was added dropwise thereto at a temperature of 15° C. or below. After completion of the dropwise addition,...
10.6084/m9.figshare.5104873.v1
null
Primary amide
Nitrile
null
null
c1ccccc1.c1cn[nH]c1
HO-
CN(C=O)C
null
null
Cc1ccccc1-n1[nH]c(C(N)=O)cc1=O>CN(C=O)C>Cc1ccccc1-n1[nH]c(C#N)cc1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b37197377f3049a1b8bb4c506a8c3f2c
Cc1cc(S(=O)(=O)O)c(C)cc1N=Nc1c(C#N)[nH]n(-c2ccccc2C)c1=O.O=P(Cl)(Cl)Cl>>Cc1cc(S(=O)(=O)Cl)c(C)cc1N=Nc1c(C#N)[nH]n(-c2ccccc2C)c1=O
C(#N)C=1NN(C(C1N=NC1=C(C=C(C(=C1)C)S(=O)(=O)O)C)=O)C1=C(C=CC=C1)C.C(C)#N.P(=O)(Cl)(Cl)Cl>>ClS(=O)(=O)C1=CC(=C(C=C1C)N=NC1=C(NN(C1=O)C1=C(C=CC=C1)C)C#N)C
O[S:5]([c:4]1[cH:3][c:2]([CH3:1])[c:12]([N:13]=[N:14][c:15]2[c:16]([C:17]#[N:18])[nH:19][n:20](-[c:21]3[cH:22][cH:23][cH:24][cH:25][c:26]3[CH3:27])[c:28]2=[O:29])[cH:11][c:9]1[CH3:10])(=[O:6])=[O:7].O=P(Cl)(Cl)[Cl:8]>>[CH3:1][c:2]1[cH:3][c:4]([S:5](=[O:6])(=[O:7])[Cl:8])[c:9]([CH3:10])[cH:11][c:12]1[N:13]=[N:14][c:15]1...
Cc1cc(S(=O)(=O)O)c(C)cc1N=Nc1c(C#N)[nH]n(-c2ccccc2C)c1=O.O=P(Cl)(Cl)Cl
Cc1cc(S(=O)(=O)Cl)c(C)cc1N=Nc1c(C#N)[nH]n(-c2ccccc2C)c1=O
null
null
CN(C(C)=O)C
Functional Group Interconversion
OtherReaction
1d60417dbcce8291d459a7fb34824cf29ea6f69a30ac46aeb585ac8e7b69013e
4a93b4a9749514113cd3dffa44b64f21b1f88d26b8739299bcad711fe7a13a1b
O=c1c(N=Nc2ccccc2)c[nH]n1-c1ccccc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[S;H0;D4;+0:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5](:[c:6]):[c:7]>>[Cl;H0;D1;+0:1]-[S;H0;D4;+0:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5](:[c:6]):[c:7]
null
[]
null
null
30
MINUTE
8.6 g of the azo obtained in step (2) above, 35 ml of acetonitrile, and 8.6 ml of N,N-dimethylacetamide were put into a 100 ml three-necked flask and 8.6 ml of phosphorus oxychloride was added dropwise to the mixture at a temperature of 50° C. or below. After completion of the dropwise addition, the mixture was stirred...
10.6084/m9.figshare.5104873.v1
null
Sulfonic acid
Sulfonyl halide
null
null
c1ccccc1.c1cn[nH]c1.c1ccccc1
HCl
CN(C(C)=O)C
null
0.5
Cc1cc(S(=O)(=O)O)c(C)cc1N=Nc1c(C#N)[nH]n(-c2ccccc2C)c1=O.O=P(Cl)(Cl)Cl>CN(C(C)=O)C>Cc1cc(S(=O)(=O)Cl)c(C)cc1N=Nc1c(C#N)[nH]n(-c2ccccc2C)c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-10a5e567c3634c778989865c564fb6c3
COc1ccc(C)c(N)c1.NS(=O)(=O)O>>COc1cc(N)c(C)cc1S(=O)(=O)O
COC=1C=C(N)C(=CC1)C.S(N)(O)(=O)=O>>COC1=C(S(=O)(=O)O)C=C(C(=C1)N)C
[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[c:7]([CH3:8])[cH:9][cH:10]1.N[S:11](=[O:12])(=[O:13])[OH:14]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[c:7]([CH3:8])[cH:9][c:10]1[S:11](=[O:12])(=[O:13])[OH:14]
COc1ccc(C)c(N)c1.NS(=O)(=O)O
COc1cc(N)c(C)cc1S(=O)(=O)O
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
1bd69bda1d4654ef7571835d484654e43991922743754be44c6c12fd5f0fb8d1
ad1e84ed1c8a6e8f7849804ad9b2e13754d927e4c3c238c80d1249ced51d5be8
c1ccccc1
N-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[O;D1;H1:4].[#8:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[#8:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[O;D1;H1:4]):[c:9]:[c:10]
null
[]
null
null
2
HOUR
23.1 g of 3-methoxy-6-methylaniline and 16.4 g of sulfamic acid were put into a 100 ml egg-plant type flask and the mixture was heated to temperature of from 150° to 160° C. and maintained thereat for 2 hours. Acetonitrile was added to the reaction mixture and the crystals thus deposited were collected. The crystals we...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Sulfonic acid
c1ccccc1
c1ccccc1
c1ccccc1
Other
C(C)#N
null
2
COc1ccc(C)c(N)c1.NS(=O)(=O)O>C(C)#N>COc1cc(N)c(C)cc1S(=O)(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c6d9edc5bfb342979086cd16e1aa58ad
Nc1nc2c(ncn2[C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]1>>Nc1ncnc2c1ncn2[C@H]1C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O1
P(O)(=O)(OP(=O)(O)OP(=O)(O)O)OC[C@@H]1[C@H](C[C@@H](O1)N1C(=O)N=C(N)C=C1)O.P(O)(=O)(OP(=O)(O)OP(=O)(O)O)OC[C@@H]1[C@H](C[C@@H](O1)N1C=NC=2C(=O)NC(N)=NC12)O.OP(OP(O)(OP(O)(O)=O)=O)(OC[C@@H]1[C@@H](O)C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)=O>>C1=NC(=C2C(=N1)N(C=N2)[C@H]3C[C@@H]([C@H](O3)COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O)N
O=[c:2]1[nH:3][c:4]([NH2:1])[n:5][c:6]2[c:7]1[n:8][cH:9][n:10]2[C@H:11]1[CH2:12][C@H:13]([OH:14])[C@@H:15]([CH2:16][O:17][P:18](=[O:19])([OH:20])[O:21][P:22](=[O:23])([OH:24])[O:25][P:26](=[O:27])([OH:28])[OH:29])[O:30]1>>[NH2:1][c:2]1[n:3][cH:4][n:5][c:6]2[c:7]1[n:8][cH:9][n:10]2[C@H:11]1[CH2:12][C@H:13]([OH:14])[C@@H...
Nc1nc2c(ncn2[C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]1
Nc1ncnc2c1ncn2[C@H]1C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O1
null
null
null
Miscellaneous
OtherReaction
c51652fc80ac6d86c1af8f05954073530c62ebdbfbe33195e3f5b1ae43447cd0
c42d4a51b8decce845f4dd55a8ddb5af4c9af9d71e89c8422599c828a2d398e9
c1ncc2ncn([C@H]3CCCO3)c2n1
O=[c;H0;D3;+0:1]1:[nH;D2;+0:2]:[c;H0;D3;+0:3](-[NH2;D1;+0:4]):[#7;a:5]:[c:6]2:[#7;a:7](-[C:8]-[#8:9]):[c:10]:[#7;a:11]:[c:12]:2:1>>[#8:9]-[C:8]-[#7;a:7]1:[c:10]:[#7;a:11]:[c:12]2:[c:6]:1:[#7;a:5]:[cH;D2;+0:3]:[n;H0;D2;+0:2]:[c;H0;D3;+0:1]:2-[NH2;D1;+0:4]
null
[]
null
null
null
null
3.75 microliter 6.6 mM mix of dCTP, dGTP and dTTP Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amine
Primary amine
c1ncc2[nH]cnc2n1
c1ncnc2nc[nH]c12
c1ncnc2nc[nH]c12.C1CCOC1
Other
null
null
null
Nc1nc2c(ncn2[C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]1>>Nc1ncnc2c1ncn2[C@H]1C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ca4ebe883a8d4c61a09a581b5deadc24
O=S(=O)([O-])CC(S)CS>>O=S(=O)([O-])CC(S)CS
[S].CSSC.CSSC.C(C(CS(=O)(=O)[O-])S)S.[Na+]>>CSSC.C(C(CS(=O)(=O)[O-])S)S.[Na+]
[O:5]=[S:6](=[O:7])([O-:8])[CH2:9][CH:10]([SH:11])[CH2:12][SH:13]>>[O:5]=[S:6](=[O:7])([O-:8])[CH2:9][CH:10]([SH:11])[CH2:12][SH:13]
O=S(=O)([O-])CC(S)CS
O=S(=O)([O-])CC(S)CS
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
The procedure shown for DMDS above was repeated except that a 1:1 weight blend of DMDS and DMPS was used as the presulfiding agent and 55 g of the 1:1 blend was dissolved in 3905 g of diesel oil to give a solution containing 1.0 wt % sulfur contributed by the blend. The results are given in Table 1 below. Conditions: S...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
O=S(=O)([O-])CC(S)CS>>O=S(=O)([O-])CC(S)CS
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5281eca835b24f4999f7ce801feb6dce
CC(C)C[C@@H](C=O)NC(=O)OC(C)(C)C>>C=CC(O)[C@H](CC(C)C)NC(=O)OC(C)(C)C
C(=O)(OC(C)(C)C)N[C@@H](CC(C)C)C=O.C(=C)[Mg]Br>>C(C)(C)(C)OC(=O)N[C@H](C(C=C)O)CC(C)C
[CH:3](=[O:4])[C@H:5]([CH2:6][CH:7]([CH3:8])[CH3:9])[NH:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17]>>[CH2:1]=[CH:2][CH:3]([OH:4])[C@H:5]([CH2:6][CH:7]([CH3:8])[CH3:9])[NH:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17]
CC(C)C[C@@H](C=O)NC(=O)OC(C)(C)C
C=CC(O)[C@H](CC(C)C)NC(=O)OC(C)(C)C
null
null
O1CCCC1
Miscellaneous
OtherReaction
7c95c9d475b3e4739c4b4bffdb557ccc0332365664dc5f751958e7bb4139acbc
1cfdacde78204b273e664dc0eb50ffc4dc70522ea435514fcadd01e492b9b547
null
[C:1]-[C:2](-[#7:3]-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[C;D1;H3:10])-[CH;D2;+0:11]=[O;H0;D1;+0:12]>>[C:1]-[C:2](-[#7:3]-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[C;D1;H3:10])-[CH;D3;+0:11](-[OH;D1;+0:12])-[C:13]=[C;D1;H2:14]
65
[{"value": 65.0, "product": "C(C)(C)(C)OC(=O)N[C@H](C(C=C)O)CC(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
To a stirred 0° C. solution of Boc-leucinal (3.00 g, 13.9 mmol) in dry tetrahydrofuran (THF) (70 ml) was added vinyl magnesium bromide (35 ml of a 1.0M solution in THF). After 5 hours, the mixture was quenched with 1.0M NH4Cl (50 ml). Most of the THF was evaporated in vacuo and the residue was extracted with ether seve...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol.Vinyl
null
null
null
Other
O1CCCC1
null
5
CC(C)C[C@@H](C=O)NC(=O)OC(C)(C)C>O1CCCC1>C=CC(O)[C@H](CC(C)C)NC(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8c1f3451869a4ee29ada0d2769e0ba54
CC(C)C[CH2][Mg][Br].Cc1ccc(S(=O)(=O)N[C@@H](CC(C)C)C(=O)O)cc1>>Cc1ccccc1S(=O)(=O)N[C@@H](CC(C)C)C(=O)CCC(C)C
C(CC(C)C)[Mg]Br.Cl.N([C@@H](CC(C)C)C(=O)O)S(=O)(=O)C1=CC=C(C)C=C1.C(CCC)[Li]>>CC(C)C[C@@H](C(CCC(C)C)=O)NS(=O)(=O)C=1C(=CC=CC1)C
[Br][Mg][CH2:19][CH2:20][CH:21]([CH3:22])[CH3:23].O[C:17]([C@@H:12]([NH:11][S:8]([c:7]1[cH:4][cH:3][c:2]([CH3:1])[cH:5][cH:6]1)(=[O:9])=[O:10])[CH2:13][CH:14]([CH3:15])[CH3:16])=[O:18]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[S:8](=[O:9])(=[O:10])[NH:11][C@@H:12]([CH2:13][CH:14]([CH3:15])[CH3:16])[C:17](=[O:18])[CH...
CC(C)C[CH2][Mg][Br].Cc1ccc(S(=O)(=O)N[C@@H](CC(C)C)C(=O)O)cc1
Cc1ccccc1S(=O)(=O)N[C@@H](CC(C)C)C(=O)CCC(C)C
null
null
C1CCOC1.CCCCCC
C-C Coupling
OtherReaction
d940fd70b89cc2cc4be47412d1f6d0fafa3926c675fc36f0a31d78a298f1ecc6
640cebf51e15100e78116250be2508b04a71dccc1a9f5ef1e1c6773bcd660eb7
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[c;H0;D3;+0:9]1:[c:10]:[cH;D2;+0:11]:[c;H0;D3;+0:12](-[C;D1;H3:13]):[c:14]:[cH;D2;+0:15]:1.[Br]-[Mg]-[CH2;D2;+0:16]-[C:17]-[C:18]>>[C:4]-[C:3](-[#7:5]-[#16:6](=[O;D1;H0:7])(=[O;D1;H0:8])-[c;H0;D3;+0:9]1:[c:10]:[cH;D2;+0:11]:[cH;D2;+...
41
[{"value": 41.0, "product": "CC(C)C[C@@H](C(CCC(C)C)=O)NS(=O)(=O)C=1C(=CC=CC1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirred -78° C. solution of Ts-Leu (15 g, 53 mmol) in dry THF (240 ml) was added n-butyl lithium (57.8 ml of a 0.91M solution in hexane) followed 15 minutes later by isopentyl magnesium bromide (185 ml of a 0.8M solution in THF). The mixture was heated at reflux for 3 days, then cooled and poured into 0° C. 1M HCl...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Tosylate.Carboxylic acid
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HBr.Mg
C1CCOC1.CCCCCC
null
null
CC(C)C[CH2][Mg][Br].Cc1ccc(S(=O)(=O)N[C@@H](CC(C)C)C(=O)O)cc1>C1CCOC1.CCCCCC>Cc1ccccc1S(=O)(=O)N[C@@H](CC(C)C)C(=O)CCC(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-558929a71aa1437ba847c6cb70cee4f2
Cc1ccccc1S(=O)(=O)N[C@@H](CC(C)C)C(=O)CCC(C)C>>C=CC(O)(CCC(C)C)[C@H](CC(C)C)NS(=O)(=O)c1ccccc1C
CC(C)C[C@@H](C(CCC(C)C)=O)NS(=O)(=O)C=1C(=CC=CC1)C.C(=C)[Mg]Br>>CC(C)C[C@@H](C(CCC(C)C)(C=C)O)NS(=O)(=O)C=1C(=CC=CC1)C
[C:3](=[O:4])([CH2:5][CH2:6][CH:7]([CH3:8])[CH3:9])[C@H:10]([CH2:11][CH:12]([CH3:13])[CH3:14])[NH:15][S:16](=[O:17])(=[O:18])[c:19]1[cH:20][cH:21][cH:22][cH:23][c:24]1[CH3:25]>>[CH2:1]=[CH:2][C:3]([OH:4])([CH2:5][CH2:6][CH:7]([CH3:8])[CH3:9])[C@H:10]([CH2:11][CH:12]([CH3:13])[CH3:14])[NH:15][S:16](=[O:17])(=[O:18])[c:1...
Cc1ccccc1S(=O)(=O)N[C@@H](CC(C)C)C(=O)CCC(C)C
C=CC(O)(CCC(C)C)[C@H](CC(C)C)NS(=O)(=O)c1ccccc1C
null
null
C1CCOC1
Miscellaneous
OtherReaction
e4a1e0cd9d6dfd9db238e7c2c1de7c3e0737df0f5a991ca26c06602eed667e3f
2ce956c609b76ee2dc626ad09e785d954b7df9a7379fec6f4a0d038e8e2d1b2b
c1ccccc1
[#7:1]-[C:2](-[C:3])-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[C:6]-[C:7]>>[#7:1]-[C:2](-[C:3])-[C;H0;D4;+0:4](-[OH;D1;+0:5])(-[C:8]=[C;D1;H2:9])-[C:6]-[C:7]
95
[{"value": 95.0, "product": "CC(C)C[C@@H](C(CCC(C)C)(C=C)O)NS(=O)(=O)C=1C(=CC=CC1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirred 0° C. solution of the resultant compound of Example 5 (79 mg, 0.23 mmol) in dry THF (8 ml) was added vinyl magnesium bromide (1.5 ml of a 1.0M solution in THF) dropwise. The mixture was warmed (room temperature, 10 hours), quenched (8 ml H2O+2 ml brine), acidified with 0.1M H3PO4 (pH=7), and extracted with...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol.Vinyl
null
null
c1ccccc1
Other
C1CCOC1
null
null
Cc1ccccc1S(=O)(=O)N[C@@H](CC(C)C)C(=O)CCC(C)C>C1CCOC1>C=CC(O)(CCC(C)C)[C@H](CC(C)C)NS(=O)(=O)c1ccccc1C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8bab05ee85f7428ab7f581565106fcda
CC(C)C[C@@H](C=O)NC(=O)OC(C)(C)C>>C=CC(O)C(CC(C)C)NC(=O)OC(C)(C)C
C(=O)(OC(C)(C)C)N[C@@H](CC(C)C)C=O.C(=C)[Mg]Br>>C(C)(C)(C)OC(=O)NC(C(C=C)O)CC(C)C
[CH:3](=[O:4])[C@H:5]([CH2:6][CH:7]([CH3:8])[CH3:9])[NH:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17]>>[CH2:1]=[CH:2][CH:3]([OH:4])[CH:5]([CH2:6][CH:7]([CH3:8])[CH3:9])[NH:10][C:11](=[O:12])[O:13][C:14]([CH3:15])([CH3:16])[CH3:17]
CC(C)C[C@@H](C=O)NC(=O)OC(C)(C)C
C=CC(O)C(CC(C)C)NC(=O)OC(C)(C)C
null
null
C1CCOC1
Miscellaneous
OtherReaction
7c95c9d475b3e4739c4b4bffdb557ccc0332365664dc5f751958e7bb4139acbc
1cfdacde78204b273e664dc0eb50ffc4dc70522ea435514fcadd01e492b9b547
null
[C:1]-[C:2]-[C@H;D3;+0:3](-[#7:4]-[C:5](=[O;D1;H0:6])-[#8:7]-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[C;D1;H3:11])-[CH;D2;+0:12]=[O;H0;D1;+0:13]>>[C:1]-[C:2]-[CH;D3;+0:3](-[#7:4]-[C:5](=[O;D1;H0:6])-[#8:7]-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[C;D1;H3:11])-[CH;D3;+0:12](-[OH;D1;+0:13])-[C:14]=[C;D1;H2:15]
null
[]
null
null
5
HOUR
To a stirred 0° C. solution of Boc-leucinal (3.00 g, 13.9 mmol) in dry THF (70 ml) was added vinyl magnesium bromide (35 ml of a 1.0M solution in THF). After 5 hours, the mixture was quenched with 1.0M NH4Cl (50 ml). Most of the THF was evaporated in vacuo and the residue was extracted with ether several times. The com...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol.Vinyl
null
null
null
Other
C1CCOC1
null
5
CC(C)C[C@@H](C=O)NC(=O)OC(C)(C)C>C1CCOC1>C=CC(O)C(CC(C)C)NC(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-44f5f31ec6e3435b87b6de372f03caf8
CC(C)CC(=O)OC(I)C(C)C.CN(C)CCn1nnnc1SCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.Cl>>CC(C)CC(=O)OC(OC(=O)C1=C(CSc2nnnn2CCN(C)C)CS[C@@H]2[C@H](N)C(=O)N12)C(C)C.Cl
Cl.C(C)(=O)[O-].[K+].Cl.Cl.N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2CCN(C)C)C(=O)O)C1=O.CC(CC(=O)OC(C(C)C)I)C>>Cl.Cl.N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2CCN(C)C)C(=O)OC(C(C)C)OC(CC(C)C)=O)C1=O
I[CH:8]([O:7][C:5]([CH2:4][CH:2]([CH3:1])[CH3:3])=[O:6])[CH:34]([CH3:35])[CH3:36].[OH:9][C:10](=[O:11])[C:12]1=[C:13]([CH2:14][S:15][c:16]2[n:17][n:18][n:19][n:20]2[CH2:21][CH2:22][N:23]([CH3:24])[CH3:25])[CH2:26][S:27][C@@H:28]2[C@H:29]([NH2:30])[C:31](=[O:32])[N:33]12.[ClH:38]>>[CH3:1][CH:2]([CH3:3])[CH2:4][C:5](=[O:...
CC(C)CC(=O)OC(I)C(C)C.CN(C)CCn1nnnc1SCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.Cl
CC(C)CC(=O)OC(OC(=O)C1=C(CSc2nnnn2CCN(C)C)CS[C@@H]2[C@H](N)C(=O)N12)C(C)C.Cl
null
null
CN(C=O)C.C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
77b141d26ed5a7bde59d3b5f7a91610561531c64abebd7939b6101e4e6702cce
e0de5d8944748c8a8ff1e66140ca54f4b21d5de4aadb39226f32b2358b79ca36
O=C1C[C@H]2SCC(CSc3nnn[nH]3)=CN12
I-[CH;D3;+0:1](-[#8:2]-[C:3](-[C:4])=[O;D1;H0:5])-[C:6](-[C;D1;H3:7])-[C;D1;H3:8].[#16:9]-[C:10]-[C:11](-[C:12])=[C:13](-[C:14](=[O;D1;H0:15])-[OH;D1;+0:16])-[#7:17]-[C:18]=[O;D1;H0:19]>>[#16:9]-[C:10]-[C:11](-[C:12])=[C:13](-[C:14](=[O;D1;H0:15])-[O;H0;D2;+0:16]-[CH;D3;+0:1](-[#8:2]-[C:3](-[C:4])=[O;D1;H0:5])-[C:6](-[...
106
[{"value": 106.0, "product": "Cl.Cl.N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2CCN(C)C)C(=O)OC(C(C)C)OC(CC(C)C)=O)C1=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
To 60 ml of dimethylformamide solution containing 4.22 g of 7β-amino-3-[[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylic acid dihydrochloride is added 1.67 g of potassium acetate. The mixture is cooled to 0° C. With stirring, 5.0 g of 1-iodo-2-methylpropyl 3-methylbutyrate is added dropwis...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Carboxylic acid
Ester.Ester
null
null
c1nnn[nH]1.C1=CN2CC[C@H]2SC1
HI
CN(C=O)C.C(Cl)Cl
0
null
CC(C)CC(=O)OC(I)C(C)C.CN(C)CCn1nnnc1SCC1=C(C(=O)O)N2C(=O)[C@@H](N)[C@H]2SC1.Cl>CN(C=O)C.C(Cl)Cl>CC(C)CC(=O)OC(OC(=O)C1=C(CSc2nnnn2CCN(C)C)CS[C@@H]2[C@H](N)C(=O)N12)C(C)C.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-14d0b639897e4843a7bf6d6a18bfd472
CC(=O)CC(=O)OCC1=C(C(=O)[O-])N2C(=O)[C@@H](NC(=O)Cc3csc(N)n3)[C@H]2SC1.CC(C)CC(=O)OC(I)C(C)C>>CC(=O)CC(=O)OCC1=C(C(=O)OC(OC(=O)CC(C)C)C(C)C)N2C(=O)[C@@H](NC(=O)Cc3csc(N)n3)[C@H]2SC1
NC=1SC=C(N1)CC(=O)N[C@H]1[C@@H]2N(C(=C(CS2)COC(CC(=O)C)=O)C(=O)[O-])C1=O.[Na+].CC(CC(=O)OC(C(C)C)I)C>>NC=1SC=C(N1)CC(=O)N[C@H]1[C@@H]2N(C(=C(CS2)COC(CC(=O)C)=O)C(=O)OC(C(C)C)OC(CC(C)C)=O)C1=O
[CH3:1][C:2](=[O:3])[CH2:4][C:5](=[O:6])[O:7][CH2:8][C:9]1=[C:10]([C:11](=[O:12])[O-:13])[N:25]2[C:26](=[O:27])[C@@H:28]([NH:29][C:30](=[O:31])[CH2:32][c:33]3[cH:34][s:35][c:36]([NH2:37])[n:38]3)[C@H:39]2[S:40][CH2:41]1.I[CH:14]([O:15][C:16](=[O:17])[CH2:18][CH:19]([CH3:20])[CH3:21])[CH:22]([CH3:23])[CH3:24]>>[CH3:1][C...
CC(=O)CC(=O)OCC1=C(C(=O)[O-])N2C(=O)[C@@H](NC(=O)Cc3csc(N)n3)[C@H]2SC1.CC(C)CC(=O)OC(I)C(C)C
CC(=O)CC(=O)OCC1=C(C(=O)OC(OC(=O)CC(C)C)C(C)C)N2C(=O)[C@@H](NC(=O)Cc3csc(N)n3)[C@H]2SC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
ad601d2996b206a686c37882a286cf985a715f8c54c0bc9146c1f2c2ac0eb520
35ea08e89ab24be5344101bc972eb4bf72e9ff1d48154cb4bcd2eca6eda7c194
O=C(Cc1cscn1)N[C@@H]1C(=O)N2C=CCS[C@H]12
I-[CH;D3;+0:1](-[#8:2]-[C:3](-[C:4])=[O;D1;H0:5])-[C:6](-[C;D1;H3:7])-[C;D1;H3:8].[#16:9]-[C:10]-[C:11](-[C:12])=[C:13](-[C:14](-[O-;H0;D1:15])=[O;D1;H0:16])-[#7:17]-[C:18]=[O;D1;H0:19]>>[#16:9]-[C:10]-[C:11](-[C:12])=[C:13](-[C:14](=[O;D1;H0:16])-[O;H0;D2;+0:15]-[CH;D3;+0:1](-[#8:2]-[C:3](-[C:4])=[O;D1;H0:5])-[C:6](-[...
41
[{"value": 41.0, "product": "NC=1SC=C(N1)CC(=O)N[C@H]1[C@@H]2N(C(=C(CS2)COC(CC(=O)C)=O)C(=O)OC(C(C)C)OC(CC(C)C)=O)C1=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-5
CELSIUS
null
null
In 30 ml of N,N-dimethylformamide is dissolved 4.76 g of sodium 7β-[2-(2-aminothiazol-4-yl)acetamido]-3-acetoacetoxymethyl-ceph-3-em-4-carboxylate and the solution is cooled to -5° C. With stirring, 5.0 g of 1-iodo-2-methylpropyl 3-methylbutyrate is added dropwise, followed by stirring for further 5 minutes. Thereafter...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ester
Ester.Ester
null
null
C1=CN2CC[C@H]2SC1.c1cscn1
I-
CN(C=O)C
-5
null
CC(=O)CC(=O)OCC1=C(C(=O)[O-])N2C(=O)[C@@H](NC(=O)Cc3csc(N)n3)[C@H]2SC1.CC(C)CC(=O)OC(I)C(C)C>CN(C=O)C>CC(=O)CC(=O)OCC1=C(C(=O)OC(OC(=O)CC(C)C)C(C)C)N2C(=O)[C@@H](NC(=O)Cc3csc(N)n3)[C@H]2SC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d2b7c2cbd73f4fd7b71a3e7b4b6f8592
O=C(O)c1cc(F)c(F)c(Cl)c1F.O=S(Cl)Cl>>O=C(Cl)c1cc(F)c(F)c(Cl)c1F
FC1=C(C(=O)O)C=C(C(=C1)F)F.ClC=1C(=C(C(=O)O)C=C(C1F)F)F.S(=O)(Cl)Cl>>ClC=1C(=C(C(=O)Cl)C=C(C1F)F)F
O[C:2](=[O:1])[c:4]1[cH:5][c:6]([F:7])[c:8]([F:9])[c:10]([Cl:11])[c:12]1[F:13].O=S(Cl)[Cl:3]>>[O:1]=[C:2]([Cl:3])[c:4]1[cH:5][c:6]([F:7])[c:8]([F:9])[c:10]([Cl:11])[c:12]1[F:13]
O=C(O)c1cc(F)c(F)c(Cl)c1F.O=S(Cl)Cl
O=C(Cl)c1cc(F)c(F)c(Cl)c1F
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
c1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Chlorination of 2,4,5-trifluorobenzoic acid in chlorosulphonic acid leads to 3-chloro-2,4,5-trifluorobenzoic acid, which is reacted as a crude product with thionyl chloride to give 3-chloro-2,4,5-trifluorobenzoyl chloride (boiling point 94°/18 mbar; nD20 =1.5164): ##STR10## Conditions: See reaction.notes.procedure_deta...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1
HCl
null
null
null
O=C(O)c1cc(F)c(F)c(Cl)c1F.O=S(Cl)Cl>>O=C(Cl)c1cc(F)c(F)c(Cl)c1F
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fa8aee38ba2a46708a7c9d020ef29ebe
O=C(O)c1cc(F)c(Cl)cc1Cl.O=[N+]([O-])O>>O=C(O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
[N+](=O)(O)[O-].S(O)(O)(=O)=O.ClC1=C(C(=O)O)C=C(C(=C1)Cl)F>>ClC1=C(C(=O)O)C=C(C(=C1[N+](=O)[O-])Cl)F
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([F:7])[c:8]([Cl:9])[cH:10][c:14]1[Cl:15].O[N+:11](=[O:12])[O-:13]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([F:7])[c:8]([Cl:9])[c:10]([N+:11](=[O:12])[O-:13])[c:14]1[Cl:15]
O=C(O)c1cc(F)c(Cl)cc1Cl.O=[N+]([O-])O
O=C(O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Cl;D1;H0:4]-[c:5](:[c:6]-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]):[cH;D2;+0:10]:[c:11](-[Cl;D1;H0:12]):[c:13]>>[Cl;D1;H0:4]-[c:5](:[c:6]-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]):[c;H0;D3;+0:10](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:11](-[Cl;D1;H0:12]):[c:13]
null
[]
null
null
null
null
40 ml of concentrated nitric acid are added dropwise to 34 ml of concentrated sulphuric acid, while cooling with ice and stirring. 20.9 g of 2,4-dichloro-5-fluorobenzoic acid are introduced in portions into this nitration mixture, whereupon the temperature rises to 45°-50° C. The mixture is then heated at 90°-100° C. f...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
O=C(O)c1cc(F)c(Cl)cc1Cl.O=[N+]([O-])O>>O=C(O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-649c77e7ea1f4e54aff363d399cc7db7
CCOC(=O)CC(=O)OCC.O=C(Cl)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl>>CCOC(=O)C(C(=O)OCC)C(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
C(CC(=O)OCC)(=O)OCC.[Mg].ClC1=C(C(=O)Cl)C=C(C(=C1[N+](=O)[O-])Cl)F.[H][H].S(O)(O)(=O)=O>>ClC1=C(C(=O)C(C(=O)OCC)C(=O)OCC)C=C(C(=C1[N+](=O)[O-])Cl)F
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7](=[O:8])[O:9][CH2:10][CH3:11].Cl[C:12](=[O:13])[c:14]1[cH:15][c:16]([F:17])[c:18]([Cl:19])[c:20]([N+:21](=[O:22])[O-:23])[c:24]1[Cl:25]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([C:7](=[O:8])[O:9][CH2:10][CH3:11])[C:12](=[O:13])[c:14]1[cH:15][c:16]([F:17])[c:18]([Cl:19])[c:20](...
CCOC(=O)CC(=O)OCC.O=C(Cl)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
CCOC(=O)C(C(=O)OCC)C(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
null
C(Cl)(Cl)(Cl)Cl
C(C)O.C1(=CC=CC=C1)C.O
C-C Coupling
OtherReaction
872dd4ea89053916cf9ee557745988425973a0fb6c3fde7e681bde82864a0018
a7050091370b27e4945622bf444949c46249e49bd26e357ae44671cc72030a02
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH2;D2;+0:10]-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]>>[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH;D3;+0:10](-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
91
[{"value": 91.0, "product": "ClC1=C(C(=O)C(C(=O)OCC)C(=O)OCC)C=C(C(=C1[N+](=O)[O-])Cl)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2.1 g of carbon tetrachloride are added to 10.1 g of magnesium filings in 21 ml of ethanol and, when the evolution of hydrogen has started, a mixture of 66.6 g of diethyl malonate, 40 ml of ethanol and 150 ml of toluene is added dropwise at 50°-60° C. The mixture is subsequently stirred at this temperature for 1 hour a...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ester.Ester
Ketone
null
null
c1ccccc1
HCl
C(Cl)(Cl)(Cl)Cl.C(C)O.C1(=CC=CC=C1)C.O
null
1
CCOC(=O)CC(=O)OCC.O=C(Cl)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl>C(Cl)(Cl)(Cl)Cl.C(C)O.C1(=CC=CC=C1)C.O>CCOC(=O)C(C(=O)OCC)C(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cc19d9ec45394266839c589e505a7929
CCOC(=O)CC(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl.CCOC(OCC)OCC>>CCOC=C(C(=O)OCC)C(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
ClC1=C(C(=O)CC(=O)OCC)C=C(C(=C1[N+](=O)[O-])Cl)F.C(OCC)(OCC)OCC.C(C)(=O)OC(C)=O>>ClC1=C(C(=O)C(C(=O)OCC)=COCC)C=C(C(=C1[N+](=O)[O-])Cl)F
[CH2:5]([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[c:13]1[cH:14][c:15]([F:16])[c:17]([Cl:18])[c:19]([N+:20](=[O:21])[O-:22])[c:23]1[Cl:24].CCO[CH:4](OCC)[O:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][O:3][CH:4]=[C:5]([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[c:13]1[cH:14][c:15]([F:16])[c:17]([Cl:18])[c:19]([N+:20](...
CCOC(=O)CC(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl.CCOC(OCC)OCC
CCOC=C(C(=O)OCC)C(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
null
null
null
C-C Coupling
OtherReaction
7cfff3053680512afd8f3daf149645dfb2cfa4c9c32bf9b885b72097190aacf2
9164ecc9bc41a60ea056ee2b5a56d6c3899e2ff7c236ad9974338a128257f79c
c1ccccc1
C-C-O-[CH;D3;+0:1](-O-C-C)-[#8:2]-[C:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11]>>[C:3]-[#8:2]-[CH;D2;+0:1]=[C;H0;D3;+0:8](-[C:9](=[O;D1;H0:10])-[c:11])-[C:6](=[O;D1;H0:7])-[#8:5]-[C:4]
null
[]
null
null
null
null
244.8 g of ethyl (2,4-dichloro-5-fluoro-3-nitrobenzoyl)-acetate are heated at 150°-160° C. with 166 g of triethyl orthoformate and 185 g of acetic anhydride for 3 hours. The mixture is then concentrated in vacuo and 270 g of ethyl benzoyl-ethoxy-acrylate are obtained as an oily residue. Conditions: See reaction.notes.p...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Ether.Ether.Ether
Ketone.Ester.Ether
null
null
c1ccccc1
HO-
null
null
null
CCOC(=O)CC(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl.CCOC(OCC)OCC>>CCOC=C(C(=O)OCC)C(=O)c1cc(F)c(Cl)c([N+](=O)[O-])c1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6c47ed8b0d894cfb943cb4f2702a1e21
CC(=O)OC(C)=O.N#CCC(=O)c1cc(F)c(F)c(F)c1F>>COC=C(C#N)C(=O)c1cc(F)c(F)c(F)c1F
FC1=C(C(=O)CC#N)C=C(C(=C1F)F)F.C(C)(=O)OC(C)=O>>FC1=C(C(=O)C(C#N)=COC)C=C(C(=C1F)F)F
CC(=O)O[C:3]([CH3:1])=[O:2].[CH2:4]([C:5]#[N:6])[C:7](=[O:8])[c:9]1[cH:10][c:11]([F:12])[c:13]([F:14])[c:15]([F:16])[c:17]1[F:18]>>[CH3:1][O:2][CH:3]=[C:4]([C:5]#[N:6])[C:7](=[O:8])[c:9]1[cH:10][c:11]([F:12])[c:13]([F:14])[c:15]([F:16])[c:17]1[F:18]
CC(=O)OC(C)=O.N#CCC(=O)c1cc(F)c(F)c(F)c1F
COC=C(C#N)C(=O)c1cc(F)c(F)c(F)c1F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
22ff39feb71b498e65b9013c0acd77555446adc9e81686fa9880967369d0b854
4adcb9ae66fe3dc60ef78becfc80a25c7cd5002548129eda6bd7322d22f759a3
c1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[CH3;D1;+0:2])=[O;H0;D1;+0:3].[N;D1;H0:4]#[C:5]-[CH2;D2;+0:6]-[C:7](=[O;D1;H0:8])-[c:9]>>[CH3;D1;+0:2]-[O;H0;D2;+0:3]-[CH;D2;+0:1]=[C;H0;D3;+0:6](-[C:5]#[N;D1;H0:4])-[C:7](=[O;D1;H0:8])-[c:9]
95.3
[{"value": 95.3, "product": "FC1=C(C(=O)C(C#N)=COC)C=C(C(=C1F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
150
CELSIUS
null
null
A mixture of 16 g of 2,3,4,5-tetrafluorobenzoyl-acetonitrile, 15.6 g of trimethyl o-formate and 18.8 g of acetic anhydride is heated at 150° C. (bath temperature) for 3 hours. The solvent mixture is distilled off completely under a waterpump vacuum and finally under a high vacuum, at a bath temperature of 120° C. 18.2 ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ketone
Ketone.Ether
null
null
c1ccccc1
HO-
null
150
null
CC(=O)OC(C)=O.N#CCC(=O)c1cc(F)c(F)c(F)c1F>>COC=C(C#N)C(=O)c1cc(F)c(F)c(F)c1F
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-87003c6c45064e96a5879078c6f45037
O=C1c2cccnc2N(c2ccccc2)C2=NCCN12>>O=C1C2=C(NCCC2)N(c2ccccc2)C2=NCCN12
C1(=CC=CC=C1)N1C=2N(C(C3=C1N=CC=C3)=O)CCN2>>C1(=CC=CC=C1)N1C=2N(C(C3=C1NCCC3)=O)CCN2
[O:1]=[C:2]1[c:3]2[c:4]([n:5][cH:6][cH:7][cH:8]2)[N:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[C:16]2=[N:17][CH2:18][CH2:19][N:20]12>>[O:1]=[C:2]1[C:3]2=[C:4]([NH:5][CH2:6][CH2:7][CH2:8]2)[N:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[C:16]2=[N:17][CH2:18][CH2:19][N:20]12
O=C1c2cccnc2N(c2ccccc2)C2=NCCN12
O=C1C2=C(NCCC2)N(c2ccccc2)C2=NCCN12
null
[Pd]
C(C)(=O)O
Miscellaneous
OtherReaction
7fb15d0b3e0ba1f4ffb65b4c5bfa4220018fa4efb1003cbd41d7d701e4bbbf8d
202737ae2b4699d92d2248429bad18cbcc9b0d9df13a8e6ccc41e4e185dac3e3
O=C1C2=C(NCCC2)N(c2ccccc2)C2=NCCN12
[#7:1]=[C:2]1-[#7:3](-[C:4])-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:7]2:[cH;D2;+0:8]:[cH;D2;+0:9]:[cH;D2;+0:10]:[n;H0;D2;+0:11]:[c;H0;D3;+0:12]:2-[#7:13]-1-[c:14]>>[#7:1]=[C:2]1-[#7:3](-[C:4])-[C:5](=[O;D1;H0:6])-[C;H0;D3;+0:7]2=[C;H0;D3;+0:12](-[NH;D2;+0:11]-[CH2;D2;+0:10]-[CH2;D2;+0:9]-[CH2;D2;+0:8]-2)-[#7:13]-1-[c:14]
null
[]
null
null
null
null
Hydrogenate a mixture of 10% Pd/C (2.5 g), 10-phenyl-2,3-dihydroimidazo[1,2-a]pyrido[2,3-d]pyrimidin-5(10H)-one (5 g) and glacial acetic acid (125 ml) at 60 psi in a Paar apparatus for 24 hrs. at 25° C. Filter the mixture and evaporate the solvent of the filtrate. Dissolve the residue in 1N NaHCO3 (50 ml), neutralize w...
10.6084/m9.figshare.5104873.v1
null
null
Enamine.Enamine
c1cnc2c(c1)CN1CCN=C1[NH]2
C1CNC2=C(C1)CN1CCN=C1[NH]2
c1ccccc1.C1CNC2=C(C1)CN1CCN=C1[NH]2
null
[Pd].C(C)(=O)O
null
null
O=C1c2cccnc2N(c2ccccc2)C2=NCCN12>[Pd].C(C)(=O)O>O=C1C2=C(NCCC2)N(c2ccccc2)C2=NCCN12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1c1a49e7765a4431bc8ffdded835f413
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c(Cl)c(Cl)sc12>>COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
N1=CN=CC2=C1C=CS2=O.ClC1=C(C=2N=CNC(C2S1)=O)Cl.C[O-].[Na+].CO[C@H]1[C@@H](N(CCC1)C(=O)OC)CC(CBr)=O>>ClC1=C(C=2N=CN(C(C2S1)=O)CC(C[C@@H]1N(CCC[C@H]1OC)C(=O)OC)=O)Cl
Br[CH2:16][C:14]([CH2:13][C@@H:12]1[N:5]([C:3]([O:2][CH3:1])=[O:4])[CH2:6][CH2:7][CH2:8][C@H:9]1[O:10][CH3:11])=[O:15].[nH:17]1[cH:18][n:19][c:20]2[c:21]([Cl:22])[c:23]([Cl:24])[s:25][c:26]2[c:27]1=[O:28]>>[CH3:1][O:2][C:3](=[O:4])[N:5]1[CH2:6][CH2:7][CH2:8][C@@H:9]([O:10][CH3:11])[C@@H:12]1[CH2:13][C:14](=[O:15])[CH2:...
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c(Cl)c(Cl)sc12
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
null
null
CO
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
defcff97999181c881fe745fb7edf5f37965e4b434cb8b35499ced30efce9e33
0844e813fd6aa8a6f803ffd9d05cd5ff5272ddf69396b8c87d384d86e0562add
O=C(C[C@H]1CCCCN1)Cn1cnc2ccsc2c1=O
Br-[CH2;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[O;D1;H0:5]=[c:6]1:[nH;D2;+0:7]:[c:8]:[#7;a:9]:[c:10]:[c:11]:1:[#16;a:12]:[c:13]>>[C:3]-[C:2](=[O;D1;H0:4])-[CH2;D2;+0:1]-[n;H0;D3;+0:7]1:[c:8]:[#7;a:9]:[c:10]:[c:11](:[#16;a:12]:[c:13]):[c:6]:1=[O;D1;H0:5]
null
[]
null
null
2
HOUR
Under nitrogen in a flame dried round bottom flask with magnetic stirring, a solution of 0.440 g (0.002 moles) of 6,7-dichlorothieno[3,2-d]pyrimidin-4(3H)-one [M. Robba, J- M. Lecomte, and M. Cugnon de Sevricourt, Bull. soc. chim. France, 1970, 3630-3636], 5 ml of methanol, and 2.0 ml of 1.0N sodium methoxide in methan...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
c1cc2ncncc2s1
c1ncc2sccc2n1
C1CC[NH]CC1.c1ncc2sccc2n1
HBr
CO
null
2
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c(Cl)c(Cl)sc12>CO>COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bdb9779579ef468e9f8a5572939fe3c5
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O>>COC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
ClC1=C(C=2N=CN(C(C2S1)=O)CC(C[C@@H]1N(CCC[C@H]1OC)C(=O)OC)=O)Cl.B(Br)(Br)Br.C([O-])(O)=O.[Na+]>>ClC1=C(C=2N=CN(C(C2S1)=O)CC(C[C@@H]1N(CCC[C@H]1O)C(=O)OC)=O)Cl
C[O:10][C@@H:9]1[CH2:8][CH2:7][CH2:6][N:5]([C:3]([O:2][CH3:1])=[O:4])[C@H:11]1[CH2:12][C:13](=[O:14])[CH2:15][n:16]1[cH:17][n:18][c:19]2[c:20]([Cl:21])[c:22]([Cl:23])[s:24][c:25]2[c:26]1=[O:27]>>[CH3:1][O:2][C:3](=[O:4])[N:5]1[CH2:6][CH2:7][CH2:8][C@@H:9]([OH:10])[C@@H:11]1[CH2:12][C:13](=[O:14])[CH2:15][n:16]1[cH:17][...
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
COC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
dcaefb482d0d4070854ae2f21edb78f004963f26f985f41a9781ad20aca44e4e
32e9a9ca3191eb6608eee26da72fef0d2c2afd087eefdbcc65ce4c46772064f8
O=C(C[C@H]1CCCCN1)Cn1cnc2ccsc2c1=O
C-[O;H0;D2;+0:1]-[C:2](-[C:3])-[C:4]-[#7:5]>>[#7:5]-[C:4]-[C:2](-[OH;D1;+0:1])-[C:3]
null
[]
null
null
10
MINUTE
A 35 ml single neck round bottom flask equipped with a magnetic stirring bar was flame dried and then stoppered with a serum cap. Through a syringe needle the flask was evacuated and filled with dry nitrogen four times. A solution of 0.270 g (0.0006 mole) of methyl trans-2-[3-(6,7-dichloro-3,4-dihydro-4-oxothieno[3,2-d...
10.6084/m9.figshare.5104873.v1
null
Ether
Secondary alcohol
null
null
C1CC[NH]CC1.c1ncc2sccc2n1
Other
ClCCl
null
0.166667
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O>ClCCl>COC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-303909f3f84f4a05bac9039b7243a17c
COC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O>>Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
ClC1=C(C=2N=CN(C(C2S1)=O)CC(C[C@@H]1N(CCC[C@H]1O)C(=O)OC)=O)Cl.Br>>Br.Br.ClC1=C(C=2N=CN(C(C2S1)=O)CC(C[C@@H]1NCCC[C@H]1O)=O)Cl
COC(=O)[N:7]1[C@@H:6]([CH2:5][C:4](=[O:3])[CH2:13][n:14]2[cH:15][n:16][c:17]3[c:18]([Cl:19])[c:20]([Cl:21])[s:22][c:23]3[c:24]2=[O:25])[C@H:11]([OH:12])[CH2:10][CH2:9][CH2:8]1>>[BrH:2].[O:3]=[C:4]([CH2:5][C@@H:6]1[NH:7][CH2:8][CH2:9][CH2:10][C@H:11]1[OH:12])[CH2:13][n:14]1[cH:15][n:16][c:17]2[c:18]([Cl:19])[c:20]([Cl:2...
COC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
null
null
C(C)O
Miscellaneous
Hydrogenolysis of tertiary amines
393e5d874f317ec1155203f17eea0a123929a5fcf273863e84fbd79bfa0739cd
ce1d20ece0ee3db84a8954171912e0cc035fe478f2082f416fe209b2e3984b26
O=C(C[C@H]1CCCCN1)Cn1cnc2ccsc2c1=O
C-O-C(=O)-[N;H0;D3;+0:1](-[C:2]-[C:3])-[C:4](-[C:5]-[C:6]=[O;D1;H0:7])-[C:8]>>[C:8]-[C:4](-[C:5]-[C:6]=[O;D1;H0:7])-[NH;D2;+0:1]-[C:2]-[C:3]
null
[]
null
null
3
MINUTE
In a 15 ml single-neck round bottom flask equipped with a reflux condenser, a solution of 0.190 g (0.00044 mole) of methyl trans-2-[3-(6,7-dichloro-3,4-dihydro-4-oxothieno[3,2-d]pyrimidin-3-yl)-2-oxopropyl]-3-hydroxy-1-piperidinecarboxylate and 6.2 ml of 48% aqueous hydrobromic acid was immersed in an oil bath preheate...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether
Secondary amine
C1CC[NH]CC1
C1CCNCC1
C1CCNCC1.c1ncc2sccc2n1
HO-
C(C)O
null
0.05
COC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2c(Cl)c(Cl)sc2c1=O>C(C)O>Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2c(Cl)c(Cl)sc2c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-28268398841145ef80593572bb765ce9
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2cc(Cl)sc12>>C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2cc(Cl)sc2c1=O
ClC1=CC=2N=CNC(C2S1)=O.C[O-].[Na+].CO[C@H]1[C@@H](N(CCC1)C(=O)OCC=C)CC(CBr)=O>>ClC1=CC=2N=CN(C(C2S1)=O)CC(C[C@@H]1N(CCC[C@H]1OC)C(=O)OCC=C)=O
Br[CH2:18][C:16]([CH2:15][C@@H:14]1[N:7]([C:5]([O:4][CH2:3][CH:2]=[CH2:1])=[O:6])[CH2:8][CH2:9][CH2:10][C@H:11]1[O:12][CH3:13])=[O:17].[nH:19]1[cH:20][n:21][c:22]2[cH:23][c:24]([Cl:25])[s:26][c:27]2[c:28]1=[O:29]>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[N:7]1[CH2:8][CH2:9][CH2:10][C@@H:11]([O:12][CH3:13])[C@@H:14]1[CH2...
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2cc(Cl)sc12
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2cc(Cl)sc2c1=O
null
null
CO
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
defcff97999181c881fe745fb7edf5f37965e4b434cb8b35499ced30efce9e33
0844e813fd6aa8a6f803ffd9d05cd5ff5272ddf69396b8c87d384d86e0562add
O=C(C[C@H]1CCCCN1)Cn1cnc2ccsc2c1=O
Br-[CH2;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[O;D1;H0:5]=[c:6]1:[nH;D2;+0:7]:[c:8]:[#7;a:9]:[c:10]:[c:11]:1:[#16;a:12]:[c:13]>>[C:3]-[C:2](=[O;D1;H0:4])-[CH2;D2;+0:1]-[n;H0;D3;+0:7]1:[c:8]:[#7;a:9]:[c:10]:[c:11](:[#16;a:12]:[c:13]):[c:6]:1=[O;D1;H0:5]
null
[]
null
null
8
HOUR
Under a nitrogen atmosphere in a flame dried flask and with magnetic stirring, a solution of 0.80 g (0.0043 mole) of 6-chlorothieno[3,2-d]pyrimidin-4(3H)-one, 3.52 ml of 1.22N sodium methoxide in methanol, and 20 ml of methanol was treated with 1.86 g (0.0056 mole) of allyl trans-3-methoxy-2-(3-bromo-2-oxopropyl)-1-pip...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
c1cc2ncncc2s1
c1ncc2sccc2n1
C1CC[NH]CC1.c1ncc2sccc2n1
HBr
CO
null
8
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2cc(Cl)sc12>CO>C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2cc(Cl)sc2c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0a4cb4e545e64cc5b3c6911886f99a0d
C=CCOC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2cc(Cl)sc2c1=O>>Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2cc(Cl)sc2c1=O
ClC1=CC=2N=CN(C(C2S1)=O)CC(C[C@@H]1N(CCC[C@H]1O)C(=O)OCC=C)=O.Br>>Br.Br.ClC1=CC=2N=CN(C(C2S1)=O)CC(C[C@@H]1NCCC[C@H]1O)=O
C=CCOC(=O)[N:7]1[C@@H:6]([CH2:5][C:4](=[O:3])[CH2:13][n:14]2[cH:15][n:16][c:17]3[cH:18][c:19]([Cl:20])[s:21][c:22]3[c:23]2=[O:24])[C@H:11]([OH:12])[CH2:10][CH2:9][CH2:8]1>>[BrH:2].[O:3]=[C:4]([CH2:5][C@@H:6]1[NH:7][CH2:8][CH2:9][CH2:10][C@H:11]1[OH:12])[CH2:13][n:14]1[cH:15][n:16][c:17]2[cH:18][c:19]([Cl:20])[s:21][c:2...
C=CCOC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2cc(Cl)sc2c1=O
Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2cc(Cl)sc2c1=O
null
null
null
Miscellaneous
Hydrogenolysis of tertiary amines
5ff8911a6b43572b9beb59978ab6f79b27754a7f46f3374df3680f737ecfb56e
dc79cadbf5b0b7e63ff6b048e333711cda1fe9e54b6e666841c0c26e8bed1f97
O=C(C[C@H]1CCCCN1)Cn1cnc2ccsc2c1=O
C=C-C-O-C(=O)-[N;H0;D3;+0:1](-[C:2]-[C:3])-[C:4](-[C:5]-[C:6]=[O;D1;H0:7])-[C:8]>>[C:8]-[C:4](-[C:5]-[C:6]=[O;D1;H0:7])-[NH;D2;+0:1]-[C:2]-[C:3]
null
[]
null
null
7
MINUTE
In a 15 ml single-neck round bottom flask equipped with a reflux condenser, a solution of 0.69 g (0.00162 mole) of allyl trans-2-[3-(6-chloro-3,4-dihydro-4-oxothieno[3,2-d]pyrimidin-3-yl)-2-oxopropyl]-3-hydroxy-1-piperidinecarboxylate and 6 ml of 48% aqueous hydrobromic acid was immersed in an oil bath preheated to 100...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Allyl
Secondary amine
C1CC[NH]CC1
C1CCNCC1
C1CCNCC1.c1ncc2sccc2n1
HO-
null
null
0.116667
C=CCOC(=O)N1CCC[C@@H](O)[C@@H]1CC(=O)Cn1cnc2cc(Cl)sc2c1=O>>Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2cc(Cl)sc2c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7e66be7c0e9d4c90b088462789db9336
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c(Br)c(Cl)sc12>>C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Br)c(Cl)sc2c1=O
BrC1=C(SC2=C1N=CNC2=O)Cl.CO[C@H]1[C@@H](N(CCC1)C(=O)OCC=C)CC(CBr)=O>>BrC1=C(SC2=C1N=CN(C2=O)CC(C[C@@H]2N(CCC[C@H]2OC)C(=O)OCC=C)=O)Cl
Br[CH2:18][C:16]([CH2:15][C@@H:14]1[N:7]([C:5]([O:4][CH2:3][CH:2]=[CH2:1])=[O:6])[CH2:8][CH2:9][CH2:10][C@H:11]1[O:12][CH3:13])=[O:17].[nH:19]1[cH:20][n:21][c:22]2[c:23]([Br:24])[c:25]([Cl:26])[s:27][c:28]2[c:29]1=[O:30]>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[N:7]1[CH2:8][CH2:9][CH2:10][C@@H:11]([O:12][CH3:13])[C@@H:...
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c(Br)c(Cl)sc12
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Br)c(Cl)sc2c1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
defcff97999181c881fe745fb7edf5f37965e4b434cb8b35499ced30efce9e33
0844e813fd6aa8a6f803ffd9d05cd5ff5272ddf69396b8c87d384d86e0562add
O=C(C[C@H]1CCCCN1)Cn1cnc2ccsc2c1=O
Br-[CH2;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[O;D1;H0:5]=[c:6]1:[nH;D2;+0:7]:[c:8]:[#7;a:9]:[c:10]:[c:11]:1:[#16;a:12]:[c:13]>>[C:3]-[C:2](=[O;D1;H0:4])-[CH2;D2;+0:1]-[n;H0;D3;+0:7]1:[c:8]:[#7;a:9]:[c:10]:[c:11](:[#16;a:12]:[c:13]):[c:6]:1=[O;D1;H0:5]
null
[]
null
null
null
null
According to the method of Example 4, 0.662 g (0.0025 mole) of 7-bromo-6-chlorothieno[3,2-d]pyrimidin-4(3H)-one and 1.24 g (0.0037 mole) of allyl trans-3-methoxy-2-(3-bromo-2-oxopropyl)-1-piperidinecarboxylate were combined to give the title compound: yield 0.90 g (69%); 1H-nmr (CDCl3) delta 1.3-2.1 ppm (multiplet, 4H,...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
c1cc2ncncc2s1
c1ncc2sccc2n1
C1CC[NH]CC1.c1ncc2sccc2n1
HBr
null
null
null
C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c(Br)c(Cl)sc12>>C=CCOC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(Br)c(Cl)sc2c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0dbed953e7ea41bf9d9c0da06739cec1
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c1oc1ccccc12>>COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(oc3ccccc32)c1=O
N1=CNC(C2=C1C1=C(O2)C=CC=C1)=O.CO[C@H]1[C@@H](N(CCC1)C(=O)OC)CC(CBr)=O>>O=C1C2=C(N=CN1CC(C[C@@H]1N(CCC[C@H]1OC)C(=O)OC)=O)C1=C(O2)C=CC=C1
Br[CH2:16][C:14]([CH2:13][C@@H:12]1[N:5]([C:3]([O:2][CH3:1])=[O:4])[CH2:6][CH2:7][CH2:8][C@H:9]1[O:10][CH3:11])=[O:15].[nH:17]1[cH:18][n:19][c:20]2[c:21]([o:22][c:23]3[cH:24][cH:25][cH:26][cH:27][c:28]23)[c:29]1=[O:30]>>[CH3:1][O:2][C:3](=[O:4])[N:5]1[CH2:6][CH2:7][CH2:8][C@@H:9]([O:10][CH3:11])[C@@H:12]1[CH2:13][C:14]...
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c1oc1ccccc12
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(oc3ccccc32)c1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
18cb901ea1a7041f60b07e0a7eb806cc3ad6eb5b85db9f97a2701be9b90609a8
0844e813fd6aa8a6f803ffd9d05cd5ff5272ddf69396b8c87d384d86e0562add
O=C(C[C@H]1CCCCN1)Cn1cnc2c(oc3ccccc32)c1=O
Br-[CH2;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[O;D1;H0:5]=[c:6]1:[nH;D2;+0:7]:[c:8]:[#7;a:9]:[c:10]:[c:11]:1:[#8;a:12]:[c:13]>>[C:3]-[C:2](=[O;D1;H0:4])-[CH2;D2;+0:1]-[n;H0;D3;+0:7]1:[c:8]:[#7;a:9]:[c:10]:[c:11](:[#8;a:12]:[c:13]):[c:6]:1=[O;D1;H0:5]
null
[]
null
null
null
null
According to the method of Example 1, 1.22 g (0.0066 mole) of benzofuro[3,2-d]pyrimidin-4(3H)-one [S. S. Sangapure and Y. S. Agasimundin, Indian J. Chem., 14B, 688-691 (1976)] and 0.0066 moles of methyl trans-3-methoxy-2-(3-bromo-2-oxopropyl)-1-piperidinecarboxylate were combined to give the title compound: yield 0.627...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
c1ncnc2c1oc1ccccc12
c1ccc2c(c1)oc1cncnc12
C1CC[NH]CC1.c1ccc2c(c1)oc1cncnc12
HBr
null
null
null
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)CBr.O=c1[nH]cnc2c1oc1ccccc12>>COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(oc3ccccc32)c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e73b22e82350428eb477a670f319f5f9
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(oc3ccccc32)c1=O>>Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2c(oc3ccccc32)c1=O
O=C1C2=C(N=CN1CC(C[C@@H]1N(CCC[C@H]1OC)C(=O)OC)=O)C1=C(O2)C=CC=C1.Br>>Br.Br.O[C@H]1[C@@H](NCCC1)CC(CN1C=NC2=C(C1=O)OC1=C2C=CC=C1)=O
COC(=O)[N:7]1[C@@H:6]([CH2:5][C:4](=[O:3])[CH2:13][n:14]2[cH:15][n:16][c:17]3[c:18]([o:19][c:20]4[cH:21][cH:22][cH:23][cH:24][c:25]34)[c:26]2=[O:27])[C@H:11]([O:12]C)[CH2:10][CH2:9][CH2:8]1>>[BrH:2].[O:3]=[C:4]([CH2:5][C@@H:6]1[NH:7][CH2:8][CH2:9][CH2:10][C@H:11]1[OH:12])[CH2:13][n:14]1[cH:15][n:16][c:17]2[c:18]([o:19]...
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(oc3ccccc32)c1=O
Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2c(oc3ccccc32)c1=O
null
null
C(C)O
Miscellaneous
OtherReaction
f876fc69bce4686ec83597e83d01503a38ea8758fb4ebd928b1eeaac3eab6dff
dfd47adcccbf1a90279005b45b2f6771d2817194b0ad76c2f3a09e6a22d954eb
O=C(C[C@H]1CCCCN1)Cn1cnc2c(oc3ccccc32)c1=O
C-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5](-[O;H0;D2;+0:6]-C)-[C:7]-1-[C:8]-[C:9]=[O;D1;H0:10]>>[O;D1;H0:10]=[C:9]-[C:8]-[C:7]1-[NH;D2;+0:1]-[C:2]-[C:3]-[C:4]-[C:5]-1-[OH;D1;+0:6]
null
[]
null
null
12
MINUTE
A solution of 0.600 g (0.00145 mole) of methyl trans-2-[3-(3,4-dihydro-4-oxobenzofuro[3,2-d]pyrimidin-3-yl)-2-oxopropyl]-3-methoxy-1-piperidinecarboxylate and 30 ml of 48% hydrobromic acid in a 100 ml round bottom flask was immersed in a bath preheated to 150° C. and held there for 12 minutes. Upon cooling to room temp...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Ether
Secondary alcohol.Secondary amine
C1CC[NH]CC1
C1CCNCC1
C1CCNCC1.c1ccc2c(c1)oc1cncnc12
HO-
C(C)O
null
0.2
COC(=O)N1CCC[C@@H](OC)[C@@H]1CC(=O)Cn1cnc2c(oc3ccccc32)c1=O>C(C)O>Br.O=C(C[C@@H]1NCCC[C@H]1O)Cn1cnc2c(oc3ccccc32)c1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9620239eddff4d22a6ab98be1c6bb71f
C=COCC.CC(=O)C(CCl)=NO>>CCOC1CCC(C(C)=O)=NO1
C([O-])([O-])=O.[Na+].[Na+].C(=C)OCC.ClCC(C(C)=O)=NO>>C(C)OC1CCC(=NO1)C(C)=O
[CH3:1][CH2:2][O:3][CH:4]=[CH2:5].Cl[CH2:6][C:7]([C:8]([CH3:9])=[O:10])=[N:11][OH:12]>>[CH3:1][CH2:2][O:3][CH:4]1[CH2:5][CH2:6][C:7]([C:8]([CH3:9])=[O:10])=[N:11][O:12]1
C=COCC.CC(=O)C(CCl)=NO
CCOC1CCC(C(C)=O)=NO1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
734e6f2cdfe6a0dff13fac705e648d41fd9cf21a751c1bba66a3fc5458ee449a
5604d9e685f8090034f972d4694e4198c7a13624f8e6d7666087c9f4e12ace64
C1=NOCCC1
Cl-[CH2;D2;+0:1]-[C:2](=[#7:3]-[OH;D1;+0:4])-[C:5](-[C;D1;H3:6])=[O;D1;H0:7].[C:8]-[#8:9]-[CH;D2;+0:10]=[CH2;D1;+0:11]>>[C:8]-[#8:9]-[CH;D3;+0:10]1-[CH2;D2;+0:11]-[CH2;D2;+0:1]-[C:2](-[C:5](-[C;D1;H3:6])=[O;D1;H0:7])=[#7:3]-[O;H0;D2;+0:4]-1
98
[{"value": 98.0, "product": "C(C)OC1CCC(=NO1)C(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.9, "product": "C(C)OC1CCC(=NO1)C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
21
HOUR
A 1000 ml three-neck flask equipped with a mechanical stirrer, a reflux condenser, and a nitrogen inlet adapter was heat dried and charged with nitrogen. When the flask was at room temperature, it was loaded in order: 39.5 g (0.37 mole) of anhydrous sodium carbonate; (with stirring) 132 g (1.83 mole) of ethyl vinyl eth...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Vinyl.Oxime
Ether
null
C1=NOCCC1
C1=NOCCC1
HCl
null
null
21
C=COCC.CC(=O)C(CCl)=NO>>CCOC1CCC(C(C)=O)=NO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8c00c59e6a604b8aaf1f1980523d636b
COc1ccc[n+]([O-])c1C>>COc1cccnc1C
[OH-].[Na+].[OH-].[Na+].COC=1C(=[N+](C=CC1)[O-])C.C(Cl)(Cl)Cl.P(Cl)(Cl)Cl.C(Cl)(Cl)Cl>>COC=1C(=NC=CC1)C
[O-][n+:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:8]1[CH3:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][n:7][c:8]1[CH3:9]
COc1ccc[n+]([O-])c1C
COc1cccnc1C
null
null
O
Functional Group Interconversion
OtherReaction
8660dc08f9c4d3b8c6814ee1b12714454b2bd6ddbe4d55cbaaeb274a83637cea
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
c1ccncc1
[C;D1;H3:1]-[c:2](:[c:3]):[n+;H0;D3:4](-[O-]):[c:5]:[c:6]>>[C;D1;H3:1]-[c:2](:[c:3]):[n;H0;D2;+0:4]:[c:5]:[c:6]
null
[]
null
null
20
MINUTE
Under a nitrogen atmosphere, a magnetically stirred solution of 25.8 g (0.185 mole) of 3-methoxy-2-methylpyridine 1-oxide and 200 ml of chloroform cooled to 0° C. was treated dropwise a solution of 75.6 g (0.556 mole) of phosphorus trichloride and 50 ml of chloroform. The temperature was maintained at <10° C. during th...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=CC=[NH+]C=C1
c1ccncc1
c1ccncc1
Other
O
null
0.333333
COc1ccc[n+]([O-])c1C>O>COc1cccnc1C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6e4b65d842a24b1fb016b47316612e80
COC(=O)CS.N#CC=C(Cl)Cl>>COC(=O)c1sc(Cl)cc1N
C(CS)(=O)OC.[Na].ClC(=CC#N)Cl>>NC1=C(SC(=C1)Cl)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[CH2:5][SH:6].Cl[C:7]([Cl:8])=[CH:9][C:10]#[N:11]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[s:6][c:7]([Cl:8])[cH:9][c:10]1[NH2:11]
COC(=O)CS.N#CC=C(Cl)Cl
COC(=O)c1sc(Cl)cc1N
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
572f3af6ed732dd565c44e5540bbf9696e221e49e641738804d0125b2ba60245
c6e202d7ab98aff5fe00b144ad3e840d360bb1662b4e877c3dc15d79ccfaa037
c1ccsc1
Cl-[C;H0;D3;+0:1](-[Cl;D1;H0:2])=[CH;D2;+0:3]-[C;H0;D2;+0:4]#[N;H0;D1;+0:5].[C;D1;H3:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH2;D2;+0:10]-[SH;D1;+0:11]>>[C;D1;H3:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[c;H0;D3;+0:10]1:[s;H0;D2;+0:11]:[c;H0;D3;+0:1](-[Cl;D1;H0:2]):[cH;D2;+0:3]:[c;H0;D3;+0:4]:1-[NH2;D1;+0:5]
null
[]
null
null
null
null
In a flame dried flask under a nitrogen atmosphere, and with mechanical stirring, a solution of about 1.2 g (0.05 mole) of sodium metal dissolved in 30 ml of dry methanol was treated dropwise with 2.35 g (1.98 ml, 0.022 mole) of methyl thioglycolate while maintaining the temperature below 25° C. A solution of 2.70 g (0...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Ester.Nitrile.Aliphatic thiol
Aromatic halide.Ester.Primary amine
null
c1ccsc1
c1ccsc1
HCl
CO
null
null
COC(=O)CS.N#CC=C(Cl)Cl>CO>COC(=O)c1sc(Cl)cc1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cfc067ec972b42689c43ec1a5ef3a03e
BrBr.O=c1[nH]cnc2cc(Cl)sc12>>O=c1[nH]cnc2c(Br)c(Cl)sc12
ClC1=CC=2N=CNC(C2S1)=O.BrBr>>BrC1=C(SC2=C1N=CNC2=O)Cl
Br[Br:8].[O:1]=[c:2]1[nH:3][cH:4][n:5][c:6]2[cH:7][c:9]([Cl:10])[s:11][c:12]12>>[O:1]=[c:2]1[nH:3][cH:4][n:5][c:6]2[c:7]([Br:8])[c:9]([Cl:10])[s:11][c:12]12
BrBr.O=c1[nH]cnc2cc(Cl)sc12
O=c1[nH]cnc2c(Br)c(Cl)sc12
null
null
C(C)(=O)O
Functional Group Interconversion
Bromination
8d37b11a43d310b2ffdc4474e084c26188cb26c3957270a92d4c5d02a0646cc0
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
O=c1[nH]cnc2ccsc12
Br-[Br;H0;D1;+0:1].[Cl;D1;H0:2]-[c:3]1:[#16;a:4]:[c:5]2:[c:6]:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:2:[cH;D2;+0:11]:1>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:11]1:[c:10]2:[#7;a:9]:[c:8]:[#7;a:7]:[c:6]:[c:5]:2:[#16;a:4]:[c:3]:1-[Cl;D1;H0:2]
44
[{"value": 44.0, "product": "BrC1=C(SC2=C1N=CNC2=O)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 43.9, "product": "BrC1=C(SC2=C1N=CNC2=O)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2.5
HOUR
A solution of 1.12 g (0.006 mole) of 6-chlorothieno[3,2-d]pyrimidin-4(3H)-one and 15 ml of acetic acid at 80° C. was treated with 2.88 g (0.92 ml, 0.018 mole) of bromine. Heating was continued for 2.5 hours during which time solids precipitated. After cooling to room temperature, the mixture was filtered and washed wit...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1cc2ncncc2s1
c1cc2ncncc2s1
c1cc2ncncc2s1
HBr
C(C)(=O)O
null
2.5
BrBr.O=c1[nH]cnc2cc(Cl)sc12>C(C)(=O)O>O=c1[nH]cnc2c(Br)c(Cl)sc12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-06fbe5b3f1e34d95a302135ea4df5b48
COc1cccc(CC(=O)O)c1.ClI>>COc1ccc(I)c(CC(=O)O)c1
COC=1C=C(C=CC1)CC(=O)O.ICl.O>>IC1=C(C=C(C=C1)OC)CC(=O)O
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:8]([CH2:9][C:10](=[O:11])[OH:12])[cH:13]1.Cl[I:7]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([I:7])[c:8]([CH2:9][C:10](=[O:11])[OH:12])[cH:13]1
COc1cccc(CC(=O)O)c1.ClI
COc1ccc(I)c(CC(=O)O)c1
null
II
C(C)(=O)O
Functional Group Interconversion
OtherReaction
f6effe61353895b318215d8bd9b6bb1105cafbf7be8c217d748df587260b32c3
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccccc1
Cl-[I;H0;D1;+0:1].[O;D1;H0:2]=[C:3](-[O;D1;H1:4])-[C:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[I;H0;D1;+0:1]-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:6](-[C:5]-[C:3](=[O;D1;H0:2])-[O;D1;H1:4]):[c:7]
65
[{"value": 65.0, "product": "IC1=C(C=C(C=C1)OC)CC(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.7, "product": "IC1=C(C=C(C=C1)OC)CC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 45 g (0.27 mole) of 3-methoxybenzeneacetic acid, 52.6 g (0.32 mole) of iodine monochloride and 1 g of iodine was allowed to stand in 500 ml of glacial acetic acid for six days at room temperature. The reaction was poured into water and the solid collected. It was recrystallized from toluene to give 51 g o...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
HCl
II.C(C)(=O)O
null
null
COc1cccc(CC(=O)O)c1.ClI>II.C(C)(=O)O>COc1ccc(I)c(CC(=O)O)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-986aa5b3e849477ab861a73561ebea06
COc1cccc(CCC(C)=O)c1.II>>COc1ccc(I)c(CCC(C)=O)c1
II.COC=1C=C(C=CC1)CCC(C)=O>>IC1=C(C=C(C=C1)OC)CCC(C)=O
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:8]([CH2:9][CH2:10][C:11]([CH3:12])=[O:13])[cH:14]1.I[I:7]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([I:7])[c:8]([CH2:9][CH2:10][C:11]([CH3:12])=[O:13])[cH:14]1
COc1cccc(CCC(C)=O)c1.II
COc1ccc(I)c(CCC(C)=O)c1
null
C(C)(=O)[O-].[Ag+]
C(C)(=O)O
Functional Group Interconversion
OtherReaction
f6effe61353895b318215d8bd9b6bb1105cafbf7be8c217d748df587260b32c3
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccccc1
I-[I;H0;D1;+0:1].[C:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6]:[c:7]>>[C:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[I;H0;D1;+0:1]):[c:6]:[c:7]
82.3
[{"value": 82.0, "product": "IC1=C(C=C(C=C1)OC)CCC(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.3, "product": "IC1=C(C=C(C=C1)OC)CCC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Samples of iodine (42.4 g, 0.167 mole) and silver acetate (27.87 g, 0.167 mole) were added in portions to a solution of 29.8 g (0.167 mole) of 1-(3-methoxyphenyl)butane-3-one in 167 ml of glacial acetic acid. The mixture was stirred one hour. The silver iodide was removed by filtration and washed with acetic acid. The ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
HI
C(C)(=O)[O-].[Ag+].C(C)(=O)O
null
1
COc1cccc(CCC(C)=O)c1.II>C(C)(=O)[O-].[Ag+].C(C)(=O)O>COc1ccc(I)c(CCC(C)=O)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-376b3b80298747838d4894a89b3c46a4
CNC.COc1ccc(I)c(CC(=O)O)c1>>COc1ccc(I)c(CC(=O)N(C)C)c1
C(Cl)Cl.C(C(=O)Cl)(=O)Cl.IC1=C(C=C(C=C1)OC)CC(=O)O.CNC>>CN(C(CC1=C(C=CC(=C1)OC)I)=O)C
[NH:12]([CH3:13])[CH3:14].O[C:10]([CH2:9][c:8]1[c:6]([I:7])[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:15]1)=[O:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([I:7])[c:8]([CH2:9][C:10](=[O:11])[N:12]([CH3:13])[CH3:14])[cH:15]1
CNC.COc1ccc(I)c(CC(=O)O)c1
COc1ccc(I)c(CC(=O)N(C)C)c1
null
null
CN(C)C=O.C1(=CC=CC=C1)C
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
ac72df6259d5d7baee7abdbd4706ef4b4627f86ead9dc94f0cefcfcb37c21def
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C;D1;H3:5]-[NH;D2;+0:6]-[C;D1;H3:7]>>[C;D1;H3:5]-[N;H0;D3;+0:6](-[C;D1;H3:7])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
null
[]
null
null
16
HOUR
A 16.7 g (0.19 mole) sample of oxalyl chloride was added dropwise at 0° C. to a solution of 50.0 g (0.17 mole) of 2-iodo-5-methoxybenzeneacetic acid in 310 ml dry toluene and 31.7 ml of DMF. The mixture was allowed to warm to room temperature and stir for 16 hours. The solution was cooled to 0° C. and dimethylamine gas...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
null
null
c1ccccc1
HO-
CN(C)C=O.C1(=CC=CC=C1)C
null
16
CNC.COc1ccc(I)c(CC(=O)O)c1>CN(C)C=O.C1(=CC=CC=C1)C>COc1ccc(I)c(CC(=O)N(C)C)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-214ecc35b1464ace9fcae69c7d4277a7
COc1cccc(C=CC(C)=O)c1>>COc1cccc(CCC(C)=O)c1
COC=1C=C(C=CC1)C=CC(C)=O>>COC=1C=C(C=CC1)CCC(C)=O
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH:8]=[CH:9][C:10]([CH3:11])=[O:12])[cH:13]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([CH2:8][CH2:9][C:10]([CH3:11])=[O:12])[cH:13]1
COc1cccc(C=CC(C)=O)c1
COc1cccc(CCC(C)=O)c1
null
[Pd]
CO
Reduction
Hydrogenation (double to single)
6556ac5f7a00160b061cac263043ece7ea2394a4006031c4a0b899c0ea4ccfef
0e0db21233797ec1d2a9464a1f32cef94e53e6a41f96d680fa1307067bbf01f2
c1ccccc1
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8]
99.2
[{"value": 99.2, "product": "COC=1C=C(C=CC1)CCC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 30.1 g of 4-(3-methoxyphenyl)-3-buten-2-one in 200 ml of MeOH was hydrogenated over 200 mg of 10% palladium on carbon for two hours. The catalyst was filtered and the solvent evaporated in vacuo to give 30.2 g of yellow oily 4-(3-methoxyphenyl)-2-butanone. Conditions: See reaction.notes.procedure_details....
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
null
null
c1ccccc1
null
[Pd].CO
null
null
COc1cccc(C=CC(C)=O)c1>[Pd].CO>COc1cccc(CCC(C)=O)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7271bcbdc29044d1993bceb145ad2cb2
CCCCCC(=O)C=Cc1cccc(OC)c1>>CCCCCC(=O)CCc1cccc(OC)c1
COC=1C=C(C=CC1)C=CC(CCCCC)=O.COC=1C=C(C=CC1)C=CC(C)=O>>COC=1C=C(C=CC1)CCC(CCCCC)=O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6](=[O:7])[CH:8]=[CH:9][c:10]1[cH:11][cH:12][cH:13][c:14]([O:15][CH3:16])[cH:17]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6](=[O:7])[CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][c:14]([O:15][CH3:16])[cH:17]1
CCCCCC(=O)C=Cc1cccc(OC)c1
CCCCCC(=O)CCc1cccc(OC)c1
null
null
null
Reduction
Hydrogenation (double to single)
6556ac5f7a00160b061cac263043ece7ea2394a4006031c4a0b899c0ea4ccfef
0e0db21233797ec1d2a9464a1f32cef94e53e6a41f96d680fa1307067bbf01f2
c1ccccc1
[C:1]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[C:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
null
null
null
null
Following the procedure of Example 15 and substituting an equivalent quantity of 1-(3-methoxyphenyl)-1-octen-3-one for 4-(3-methoxyphenyl)-3-buten-2-one there was obtained as the product 1-(3-methoxyphenyl)octan-3-one as a colorless oil. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
null
null
c1ccccc1
null
null
null
null
CCCCCC(=O)C=Cc1cccc(OC)c1>>CCCCCC(=O)CCc1cccc(OC)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4b5a38fe3955401aa0ddf3e185732936
CCCCCC(=O)Cc1cc(OC)ccc1I.CNC.CNC>>CCCCCC(CCc1cc(OC)ccc1I)N(C)C
IC1=C(C=C(C=C1)OC)CC(CCCCC)=O.CNC.Cl.CNC.C(#N)[BH3-].[Na+].Cl>>Cl.IC1=C(C=C(C=C1)OC)CCC(N(C)C)CCCCC
O=[C:7]([CH2:6][CH2:5][CH2:4][CH2:3][CH3:2])[CH2:8][c:9]1[cH:10][c:11]([O:12][CH3:13])[cH:14][cH:15][c:16]1[I:17].[NH:18]([CH3:19])[CH3:20].CN[CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]([CH2:7][CH2:8][c:9]1[cH:10][c:11]([O:12][CH3:13])[cH:14][cH:15][c:16]1[I:17])[N:18]([CH3:19])[CH3:20]
CCCCCC(=O)Cc1cc(OC)ccc1I.CNC.CNC
CCCCCC(CCc1cc(OC)ccc1I)N(C)C
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
ef7c79135e297dfd2538d1b5aff73e623d0318673162ff6faa0976fc32092ae3
392f4bf36c5dce5fac128c91895ac6331ef01e9645f5108b22ed0b00d3833c53
c1ccccc1
C-N-[CH3;D1;+0:1].O=[C;H0;D3;+0:2](-[C:3]-[c:4])-[CH2;D2;+0:5]-[C:6]-[C:7]-[C:8]-[CH3;D1;+0:9].[C;D1;H3:10]-[NH;D2;+0:11]-[C;D1;H3:12]>>[C;D1;H3:10]-[N;H0;D3;+0:11](-[C;D1;H3:12])-[CH;D3;+0:5](-[C:6]-[C:7]-[C:8]-[CH2;D2;+0:9]-[CH3;D1;+0:1])-[CH2;D2;+0:2]-[C:3]-[c:4]
null
[]
null
null
8
HOUR
A mixture of 13.0 g (0.036 mole) of 1-(2-iodo-5-methoxyphenyl)heptan-2-one, 46.6 ml (0.18 mole) of a solution of 3.86 M dimethylamine in methanol, 8.24 g (0.101 mole) of dimethylamine hydrochloride, 100 ml of methanol and 1.82 g (0.029 mole) of sodium cyanoborohydride was stirred overnight under an atmosphere of nitrog...
10.6084/m9.figshare.5104873.v1
null
Ketone.Secondary amine.Secondary amine
Tertiary amine
null
null
c1ccccc1
HO-
CO
null
8
CCCCCC(=O)Cc1cc(OC)ccc1I.CNC.CNC>CO>CCCCCC(CCc1cc(OC)ccc1I)N(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c233d3f7474f4b86a95a4c7f7873d8ec
C#CCCCC.COc1ccc(I)c(CCN(C)C)c1>>CCCCC#Cc1ccc(OC)cc1CCN(C)C
Cl.[Li]CCCC.IC1=C(C=C(C=C1)OC)CCN(C)C.C#CCCCC>>Cl.C(#CCCCC)C1=C(C=C(C=C1)OC)CCN(C)C
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]#[CH:6].I[c:7]1[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13][c:14]1[CH2:15][CH2:16][N:17]([CH3:18])[CH3:19]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]#[C:6][c:7]1[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13][c:14]1[CH2:15][CH2:16][N:17]([CH3:18])[CH3:19]
C#CCCCC.COc1ccc(I)c(CCN(C)C)c1
CCCCC#Cc1ccc(OC)cc1CCN(C)C
null
[Cl-].[Zn+2].[Cl-].[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
O.O1CCCC1
C-C Coupling
Sonogashira alkyne_aryl halide
15c08902746c61a960c314898ce6bb5fcc5e189f9e057388c59dba9ec9d0c81c
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
c1ccccc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C:5]):[c:6].[C:7]-[C:8]#[CH;D1;+0:9]>>[C:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[C;H0;D2;+0:9]#[C:8]-[C:7]):[c:2]:[c:3]
27
[{"value": 27.0, "product": "Cl.C(#CCCCC)C1=C(C=C(C=C1)OC)CCN(C)C", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
20
MINUTE
A solution of 2.7 ml (0.027 mole) 1-hexyne in 10 ml dry (4 A sieves) tetrahydrofuran was cooled to 0° C. in an ice bath. Argon was passed over the solution 10.4 ml (0.027 mole) 2.69 M n-BuLi was added slowly via syringe through a serum cap. The resulting solution was stirred 20 minutes under argon. During this time, a ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1
HI
[Cl-].[Zn+2].[Cl-].[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.O1CCCC1
0
0.333333
C#CCCCC.COc1ccc(I)c(CCN(C)C)c1>[Cl-].[Zn+2].[Cl-].[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.O1CCCC1>CCCCC#Cc1ccc(OC)cc1CCN(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5738c90848c14330a8109484a074deed
O=C(O)C=Cc1cccc([N+](=O)[O-])c1>>Nc1cccc(CCC(=O)O)c1
[N+](=O)([O-])C=1C=C(C=CC(=O)O)C=CC1.[H][H]>>NC=1C=C(C=CC1)CCC(=O)O
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][cH:5][c:6]([CH:7]=[CH:8][C:9](=[O:10])[OH:11])[cH:12]1>>[NH2:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH2:7][CH2:8][C:9](=[O:10])[OH:11])[cH:12]1
O=C(O)C=Cc1cccc([N+](=O)[O-])c1
Nc1cccc(CCC(=O)O)c1
null
[Pd]
C(C)(=O)O.CO
Reduction
OtherReaction
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]:[c:5](-[CH;D2;+0:6]=[CH;D2;+0:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]):[c:11]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]:[c:5](-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]):[c:11]
null
[]
null
null
null
null
A suspension of 100 g (0.52 moles) of 3-nitrocinnamic acid in 800 ml glacial acetic acid and 100 ml of methanol was hydrogenated at 50 pounds per square inch over 2.5 g 10% palladium on carbon until four equivalents of hydrogen were absorbed. The catalyst was filtered off, the filtrates combined and the solvent was con...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pd].C(C)(=O)O.CO
null
null
O=C(O)C=Cc1cccc([N+](=O)[O-])c1>[Pd].C(C)(=O)O.CO>Nc1cccc(CCC(=O)O)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cd3f0cac90124ff0adb84e6417ad574b
C#CCC(O)C(C)=O.Cc1ccc(S(=O)(=O)Cl)cc1>>C#CCC(OS(=O)(=O)c1ccc(C)cc1)C(C)=O
S(=O)(=O)(C1=CC=C(C)C=C1)Cl.OC(C(C)=O)CC#C.C(C)N(CC)CC>>S(=O)(=O)(C1=CC=C(C)C=C1)OC(C(C)=O)CC#C
[CH:1]#[C:2][CH2:3][CH:4]([OH:5])[C:16]([CH3:17])=[O:18].Cl[S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][c:12]([CH3:13])[cH:14][cH:15]1>>[CH:1]#[C:2][CH2:3][CH:4]([O:5][S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][c:12]([CH3:13])[cH:14][cH:15]1)[C:16]([CH3:17])=[O:18]
C#CCC(O)C(C)=O.Cc1ccc(S(=O)(=O)Cl)cc1
C#CCC(OS(=O)(=O)c1ccc(C)cc1)C(C)=O
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
ad3deb6f5d4dc7823aa3ad2bfe24985be1f3e6860ff8cc0ba215d7624074ef69
ec645297cfd3107bffb1a4753ac125e48856598e58005e939bb2f0e91bf5e57c
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C;D1;H1:7]#[C:8]-[C:9]-[C:10](-[OH;D1;+0:11])-[C:12](-[C;D1;H3:13])=[O;D1;H0:14]>>[C;D1;H1:7]#[C:8]-[C:9]-[C:10](-[O;H0;D2;+0:11]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6])-[C:12](-[C;D1;H3:13])=[O;D1;H0:14]
55.3
[{"value": 55.3, "product": "S(=O)(=O)(C1=CC=C(C)C=C1)OC(C(C)=O)CC#C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2.5
HOUR
Tosyl chloride (3.81 g) was added to a solution of 3-hydroxy-5-hexyn-2-one (2.24 g) and triethylamine (2.424 g) in methylene chloride (20 ml) under ice-cooling. After being stirred for 2.5 hours, the mixture was washed with water, dried over magnesium sulfate and evaporated in vacuo. The oily residue was purified by co...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Secondary alcohol.Sulfonyl halide
Tosylate
null
null
c1ccccc1
HCl
C(Cl)Cl
null
2.5
C#CCC(O)C(C)=O.Cc1ccc(S(=O)(=O)Cl)cc1>C(Cl)Cl>C#CCC(OS(=O)(=O)c1ccc(C)cc1)C(C)=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fb1b8a9a3abb43df9bafa1d48884824e
C#CCC(O)C(=C)OC.CS(=O)(=O)Cl>>C#CCC(OS(C)(=O)=O)C(=C)OC
S(=O)(=O)(C)Cl.OC(C(=C)OC)CC#C.C(C)N(CC)CC>>S(=O)(=O)(C)OC(C(=C)OC)CC#C
[CH:1]#[C:2][CH2:3][CH:4]([OH:5])[C:10](=[CH2:11])[O:12][CH3:13].Cl[S:6]([CH3:7])(=[O:8])=[O:9]>>[CH:1]#[C:2][CH2:3][CH:4]([O:5][S:6]([CH3:7])(=[O:8])=[O:9])[C:10](=[CH2:11])[O:12][CH3:13]
C#CCC(O)C(=C)OC.CS(=O)(=O)Cl
C#CCC(OS(C)(=O)=O)C(=C)OC
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
641955d0081c80f158ce2aacd31873a3f3301c87ca0800cf263e288ba8390217
4f9373df8a11470603daf885a5777cebf95940370e32739263d35df0f171a0dd
null
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[#8:5]-[C:6](=[C;D1;H2:7])-[C:8](-[OH;D1;+0:9])-[C:10]-[C:11]#[C;D1;H1:12]>>[#8:5]-[C:6](=[C;D1;H2:7])-[C:8](-[C:10]-[C:11]#[C;D1;H1:12])-[O;H0;D2;+0:9]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]
null
[]
null
null
48
HOUR
Mesyl chloride (1.73 ml) was added dropwise to a solution of 3-hydroxy-2-methoxy-1-hexen-5-yne (2 g) and triethylamine (3.32 ml) in methylene chloride (20 ml) under ice-cooling over a period of 10 minutes. After being stirred for 48 hours at room temperature the mixture was washed successively with water, aqueous sodiu...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Sulfonyl halide
Mesylate
null
null
null
HCl
C(Cl)Cl
null
48
C#CCC(O)C(=C)OC.CS(=O)(=O)Cl>C(Cl)Cl>C#CCC(OS(C)(=O)=O)C(=C)OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b8f160543fa44baea176707de4dac95e
C#CCC(OS(C)(=O)=O)C(=C)OC>>C#CCC(OS(C)(=O)=O)C(C)=O
S(=O)(=O)(C)OC(C(=C)OC)CC#C.S(O)(O)(=O)=O>>S(=O)(=O)(C)OC(C(C)=O)CC#C
C[O:12][C:10]([CH:4]([CH2:3][C:2]#[CH:1])[O:5][S:6]([CH3:7])(=[O:8])=[O:9])=[CH2:11]>>[CH:1]#[C:2][CH2:3][CH:4]([O:5][S:6]([CH3:7])(=[O:8])=[O:9])[C:10]([CH3:11])=[O:12]
C#CCC(OS(C)(=O)=O)C(=C)OC
C#CCC(OS(C)(=O)=O)C(C)=O
null
null
CC(=O)C
Miscellaneous
OtherReaction
3e02cda7ca3208f28d8355e2c059d63c9e4eb2c7eba0cae088d693f3c74db23e
215582e9637166736070a53bb588f4e45b0dfc6c974d1df4c97ac5a98451627c
null
C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2](=[CH2;D1;+0:3])-[C:4](-[#8:5])-[C:6]-[C:7]#[C;D1;H1:8]>>[#8:5]-[C:4](-[C:6]-[C:7]#[C;D1;H1:8])-[C;H0;D3;+0:2](-[CH3;D1;+0:3])=[O;H0;D1;+0:1]
88
[{"value": 88.0, "product": "S(=O)(=O)(C)OC(C(C)=O)CC#C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
To a solution of 3-mesyloxy-2-methoxy-1-hexen-5-yne (0.5 g) in acetone (1.5 ml) was added 20% sulfuric acid (1.5 ml) under ice-cooling and the mixture was stirred for 1.5 hours under the same conditions and then for 1.5 hours at room temperature. Acetone was evaporated in vacuo and the residue was extracted with methyl...
10.6084/m9.figshare.5104873.v1
null
Ether.Vinyl
Ketone
null
null
null
Other
CC(=O)C
null
1.5
C#CCC(OS(C)(=O)=O)C(=C)OC>CC(=O)C>C#CCC(OS(C)(=O)=O)C(C)=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4a0ab28d099d4c989edf76e5c61389c1
Cc1ccccc1CCl.Nc1ncccc1O>>Cc1ccccc1COc1cccnc1N
NC1=NC=CC=C1O.CC1=C(CCl)C=CC=C1>>NC1=NC=CC=C1OCC1=C(C=CC=C1)C
Cl[CH2:8][c:7]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]1.[OH:9][c:10]1[cH:11][cH:12][cH:13][n:14][c:15]1[NH2:16]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][O:9][c:10]1[cH:11][cH:12][cH:13][n:14][c:15]1[NH2:16]
Cc1ccccc1CCl.Nc1ncccc1O
Cc1ccccc1COc1cccnc1N
null
CCCCCCCC[N+](C)(CCCCCCCC)CCCCCCCC.[Cl-]
[OH-].[Na+].C(Cl)Cl
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2cccnc2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[N;D1;H2:5]-[c:6](:[#7;a:7]:[c:8]):[c:9](-[OH;D1;+0:10]):[c:11]>>[N;D1;H2:5]-[c:6](:[#7;a:7]:[c:8]):[c:9](-[O;H0;D2;+0:10]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:11]
null
[]
null
null
24
HOUR
To a mixture of 2-amino-3-hydroxypyridine (7 g) and Adogen 464 (Trademark: prepared by Aldrich Chemical Co.) (0.4 g) in 40% aqueous sodium hydroxide (32 ml) and methylene chloride (32 ml) was added 2-methylbenzyl chloride (8.42 ml) at ambient temperature. After being stirred for 24 hours, the organic layer was separate...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccncc1
HCl
CCCCCCCC[N+](C)(CCCCCCCC)CCCCCCCC.[Cl-].[OH-].[Na+].C(Cl)Cl
null
24
Cc1ccccc1CCl.Nc1ncccc1O>CCCCCCCC[N+](C)(CCCCCCCC)CCCCCCCC.[Cl-].[OH-].[Na+].C(Cl)Cl>Cc1ccccc1COc1cccnc1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8afe18d01bb54bda9ec3d89b8bd7890e
Cc1ccccc1C=O.Nc1cccnc1N>>Cc1ccccc1CNc1cccnc1N
C([O-])(O)=O.[Na+].NC1=NC=CC=C1N.CC1=C(C=O)C=CC=C1.C(#N)[BH3-].[Na+]>>NC1=NC=CC=C1NCC1=C(C=CC=C1)C
O=[CH:8][c:7]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]1.[NH2:9][c:10]1[cH:11][cH:12][cH:13][n:14][c:15]1[NH2:16]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][NH:9][c:10]1[cH:11][cH:12][cH:13][n:14][c:15]1[NH2:16]
Cc1ccccc1C=O.Nc1cccnc1N
Cc1ccccc1CNc1cccnc1N
null
null
C(C)(=O)O.CO
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
c1ccc(CNc2cccnc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[N;D1;H2:5]-[c:6](:[#7;a:7]:[c:8]):[c:9](-[NH2;D1;+0:10]):[c:11]>>[N;D1;H2:5]-[c:6](:[#7;a:7]:[c:8]):[c:9](-[NH;D2;+0:10]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:11]
34.4
[{"value": 34.4, "product": "NC1=NC=CC=C1NCC1=C(C=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
96
HOUR
Molecular Sieves (16 g) was added to a solution of 2,3-diaminopyridine (8 g), 2-methylbenzaldehyde (8.81 g), and acetic acid (4.2 ml) in methanol (160 ml) and the mixture was stirred for 96 hours at room temperature. Sodium cyanoborohydride (4.61 g) was added portionwise to the mixture with stirring under ice-cooling o...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccncc1
Other
C(C)(=O)O.CO
null
96
Cc1ccccc1C=O.Nc1cccnc1N>C(C)(=O)O.CO>Cc1ccccc1CNc1cccnc1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-163ac3e349334314939c73ed51b57929
Cc1ccccc1CO.Nc1nccnc1Cl>>Cc1ccccc1COc1nccnc1N
NC1=NC=CN=C1Cl.CC1=C(CO)C=CC=C1.[H-].[Na+]>>NC1=NC=CN=C1OCC1=C(C=CC=C1)C
[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][OH:9].Cl[c:10]1[n:11][cH:12][cH:13][n:14][c:15]1[NH2:16]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][O:9][c:10]1[n:11][cH:12][cH:13][n:14][c:15]1[NH2:16]
Cc1ccccc1CO.Nc1nccnc1Cl
Cc1ccccc1COc1nccnc1N
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
8088ac3623a2ee47f375f73ca665bec9cf80b1384463e6e2f03125aecbcea517
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccc(COc2cnccn2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1-[N;D1;H2:7].[OH;D1;+0:8]-[C:9]-[c:10]>>[N;D1;H2:7]-[c:6]1:[#7;a:5]:[c:4]:[c:3]:[#7;a:2]:[c;H0;D3;+0:1]:1-[O;H0;D2;+0:8]-[C:9]-[c:10]
41.5
[{"value": 41.5, "product": "NC1=NC=CN=C1OCC1=C(C=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
30
MINUTE
To a solution of 2-methylbenzyl alcohol (0.985 g) in N,N-dimethylformamide (10 ml) was added 62.8% sodium hydride (0.308 g) under a nitrogen atmosphere and then stirred for 30 minutes. 2-Amino-3-chloropyrazine (0.87 g) was added to the solution and the mixture was heated at 65° C. for 2 hours and poured onto crushed ic...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1cnccn1
c1cnccn1
c1ccccc1.c1cnccn1
HCl
CN(C=O)C
65
0.5
Cc1ccccc1CO.Nc1nccnc1Cl>CN(C=O)C>Cc1ccccc1COc1nccnc1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9d28aa19805e4a3182693ceb169ad3c2
Cc1ccccc1CN.Nc1nccnc1Cl>>Cc1ccccc1CNc1nccnc1N
NC1=NC=CN=C1Cl.CC1=C(CN)C=CC=C1.C([O-])([O-])=O.[K+].[K+].[I-].[K+]>>NC1=NC=CN=C1NCC1=C(C=CC=C1)C
[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][NH2:9].Cl[c:10]1[n:11][cH:12][cH:13][n:14][c:15]1[NH2:16]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][NH:9][c:10]1[n:11][cH:12][cH:13][n:14][c:15]1[NH2:16]
Cc1ccccc1CN.Nc1nccnc1Cl
Cc1ccccc1CNc1nccnc1N
null
null
CN(C=O)C.O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
d8d76a4347a32a5acf79894f48887cf8d745ba4ca5f91e54084ebdbe25f43c75
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(CNc2cnccn2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1-[N;D1;H2:7].[NH2;D1;+0:8]-[C:9]-[c:10]>>[N;D1;H2:7]-[c:6]1:[#7;a:5]:[c:4]:[c:3]:[#7;a:2]:[c;H0;D3;+0:1]:1-[NH;D2;+0:8]-[C:9]-[c:10]
19.7
[{"value": 19.7, "product": "NC1=NC=CN=C1NCC1=C(C=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-amino-3-chloropyrazine (4.3 g), 2-methylbenzylamine (4.6 g), potassium carbonate (5.5 g), and potassium iodide (0.4 g) in N,N-dimethylformamide (43 ml) was refluxed for 24 hours under a nitrogen atmosphere and allowed to stand at room temperature. The mixture was poured into water and extracted with ethy...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1cnccn1
c1cnccn1
c1ccccc1.c1cnccn1
HCl
CN(C=O)C.O
null
null
Cc1ccccc1CN.Nc1nccnc1Cl>CN(C=O)C.O>Cc1ccccc1CNc1nccnc1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d1e537d445bf410db0fd0a5741375d9f
Cc1cn2cccc(O)c2n1.ClCc1ccccc1Cl>>Cc1cn2cccc(OCc3ccccc3Cl)c2n1
ClC1=C(CCl)C=CC=C1.O.[H-].[Na+].OC=1C=2N(C=CC1)C=C(N2)C>>ClC1=C(COC=2C=3N(C=CC2)C=C(N3)C)C=CC=C1
[CH3:1][c:2]1[cH:3][n:4]2[cH:5][cH:6][cH:7][c:8]([OH:9])[c:18]2[n:19]1.Cl[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[Cl:17]>>[CH3:1][c:2]1[cH:3][n:4]2[cH:5][cH:6][cH:7][c:8]([O:9][CH2:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[Cl:17])[c:18]2[n:19]1
Cc1cn2cccc(O)c2n1.ClCc1ccccc1Cl
Cc1cn2cccc(OCc3ccccc3Cl)c2n1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2cccn3ccnc23)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]1:[#7;a:9]:[c:10]:[c:11]:[#7;a:12]:1:[c:13]>>[c:3]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]1:[#7;a:9]:[c:10]:[c:11]:[#7;a:12]:1:[c:13]):[c:4]
66.8
[{"value": 66.8, "product": "ClC1=C(COC=2C=3N(C=CC2)C=C(N3)C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A 60% dispersion of sodium hydride in mineral oil (1.87 g) was added portionwise to a suspension of 8-hydroxy-2-methylimidazo[1,2-a]pyridine (6.3 g) in dimethyl sulfoxide (63 ml) at room temperature over a period of 15 minutes. After being stirred for 30 minutes, 2-chlorobenzyl chloride (7.54 g) was added in one portio...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccn2ccnc2c1.c1ccccc1
HCl
CS(=O)C
null
0.5
Cc1cn2cccc(O)c2n1.ClCc1ccccc1Cl>CS(=O)C>Cc1cn2cccc(OCc3ccccc3Cl)c2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-022e022fa6a34c4ca3ba0dec5c804a5d
CC(=O)CCl.Cc1ccccc1CNc1cccnc1N>>Cc1cn2cccc(NCc3ccccc3C)c2n1
NC1=NC=CC=C1NCC1=C(C=CC=C1)C.ClCC(C)=O>>CC1=C(CNC=2C=3N(C=CC2)C=C(N3)C)C=CC=C1
O=[C:2]([CH3:1])[CH2:3]Cl.[n:4]1[cH:5][cH:6][cH:7][c:8]([NH:9][CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[CH3:17])[c:18]1[NH2:19]>>[CH3:1][c:2]1[cH:3][n:4]2[cH:5][cH:6][cH:7][c:8]([NH:9][CH2:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[CH3:17])[c:18]2[n:19]1
CC(=O)CCl.Cc1ccccc1CNc1cccnc1N
Cc1cn2cccc(NCc3ccccc3C)c2n1
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
98b9b4632b0457bc035e4a4d36e0a1658474c53cb0def2f4c4d097bbd0d48009
9e77d52183fdbe84f0d2ab96039aaf521caea9340e743bdc6436175f1a3bbdb6
c1ccc(CNc2cccn3ccnc23)cc1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[C;D1;H3:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[n;H0;D2;+0:7]:[c:8]:[c:9]>>[C;D1;H3:3]-[c;H0;D3;+0:2]1:[cH;D2;+0:1]:[n;H0;D3;+0:7](:[c:8]:[c:9]):[c:5](:[c:6]):[n;H0;D2;+0:4]:1
null
[]
null
null
null
null
A solution of 2-amino-3-(2-methylbenzylamino)pyridine (3.25 g) and chloroacetone (1.26 ml) in ethanol (65 ml) was refluxed for 18 hours and then evaporated in vacuo. To the residue was added aqueous sodium bicarbonate solution and the mixture was extracted with methylene chloride. The extract was washed with brine, dri...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Primary amine
null
c1ccncc1
c1ccn2ccnc2c1
c1ccn2ccnc2c1.c1ccccc1
HCl
C(C)O
null
null
CC(=O)CCl.Cc1ccccc1CNc1cccnc1N>C(C)O>Cc1cn2cccc(NCc3ccccc3C)c2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-92e60f8984b44a1db9d8ae0442b210af
C=O.CNC.Cc1cn2cccc(OCc3ccccc3Cl)c2n1>>Cc1nc2c(OCc3ccccc3Cl)cccn2c1CN(C)C
ClC1=C(COC=2C=3N(C=CC2)C=C(N3)C)C=CC=C1.C=O.CNC>>ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)CN(C)C)C=CC=C1
O=[CH2:23].[CH3:20][NH:21][CH3:22].[CH3:1][c:2]1[n:3][c:4]2[c:5]([O:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[Cl:14])[cH:15][cH:16][cH:17][n:18]2[cH:19]1>>[CH3:1][c:2]1[n:3][c:4]2[c:5]([O:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[Cl:14])[cH:15][cH:16][cH:17][n:18]2[c:19]1[CH2:20][N:21]([CH3:22])[CH3:23]
C=O.CNC.Cc1cn2cccc(OCc3ccccc3Cl)c2n1
Cc1nc2c(OCc3ccccc3Cl)cccn2c1CN(C)C
null
null
C(C)(=O)O
Heteroatom Alkylation and Arylation
OtherReaction
991ddcf1933c85b5de89c8220fc08fceb03a8dd4087543d85e8a78c13bfec399
e1fdef8fde1c506d7c9deb8fd5e6f322eceea2abce3167abcf412a1fa4fd5443
c1ccc(COc2cccn3ccnc23)cc1
O=[CH2;D1;+0:1].[C;D1;H3:2]-[NH;D2;+0:3]-[CH3;D1;+0:4].[C;D1;H3:5]-[c:6]1:[#7;a:7]:[c:8](:[c:9]):[#7;a:10](:[c:11]):[cH;D2;+0:12]:1>>[C;D1;H3:5]-[c:6]1:[#7;a:7]:[c:8](:[c:9]):[#7;a:10](:[c:11]):[c;H0;D3;+0:12]:1-[CH2;D2;+0:4]-[N;H0;D3;+0:3](-[C;D1;H3:2])-[CH3;D1;+0:1]
85.4
[{"value": 85.4, "product": "ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)CN(C)C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To a solution of 37% aqueous formaldehyde (2.38 g) in acetic acid (38 ml) was added dropwise 50% aqueous dimethylamine (2.63 g) with ice-cooling over a period of 10 minutes and the mixture was stirred for an additional 10 minutes. The mixture was heated at 50°-55° C. for 2 hours after an addition of 8-(2-chlorobenzylox...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Secondary amine
Tertiary amine
c1ccn2ccnc2c1
c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
HO-
C(C)(=O)O
null
0.166667
C=O.CNC.Cc1cn2cccc(OCc3ccccc3Cl)c2n1>C(C)(=O)O>Cc1nc2c(OCc3ccccc3Cl)cccn2c1CN(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-91c2eee7c15b45b0a59d06a37df37e76
CI.Cc1nc2c(OCc3ccccc3Cl)cccn2c1CN(C)C>>Cc1nc2c(OCc3ccccc3Cl)cccn2c1C[N+](C)(C)C.[I-]
CI.ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)CN(C)C)C=CC=C1>>[I-].ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)C[N+](C)(C)C)C=CC=C1
[CH3:22][I:25].[CH3:1][c:2]1[n:3][c:4]2[c:5]([O:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[Cl:14])[cH:15][cH:16][cH:17][n:18]2[c:19]1[CH2:20][N:21]([CH3:23])[CH3:24]>>[CH3:1][c:2]1[n:3][c:4]2[c:5]([O:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[Cl:14])[cH:15][cH:16][cH:17][n:18]2[c:19]1[CH2:20][N+:21]([CH3:...
CI.Cc1nc2c(OCc3ccccc3Cl)cccn2c1CN(C)C
Cc1nc2c(OCc3ccccc3Cl)cccn2c1C[N+](C)(C)C.[I-]
null
null
CC(=O)C
Functional Group Interconversion
OtherReaction
c1c361ee4cbadaf5c6784ce94893dc199b85d8bd1f54519979f4b44d8dfd8b3e
5a8d30abc7481f1c446ec3891ae2e6d38df9cf7a08165b843f1d24fc50c4b9cd
c1ccc(COc2cccn3ccnc23)cc1
[#7;a:1]:[c:2](-[C:3]-[N;H0;D3;+0:4](-[C;D1;H3:5])-[C;D1;H3:6]):[c:7]:[#7;a:8].[CH3;D1;+0:9]-[I;H0;D1;+0:10]>>[#7;a:1]:[c:2](-[C:3]-[N+;H0;D4:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[CH3;D1;+0:9]):[c:7]:[#7;a:8].[I-;H0;D0:10]
101.7
[{"value": 101.7, "product": "[I-].ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)C[N+](C)(C)C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
Methyl iodide (3.48 g) was added dropwise to a solution of 8-(2-chlorobenzyloxy)-3-dimethylaminomethyl-2-methylimidazo[1,2-a]pyridine (7.8 g) in acetone (100 ml) at room temperature and the mixture was stirred for 24 hours. The resulting precipitate was collected by filtration, washed with acetone, and dried in a desic...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
null
null
null
c1ccccc1.c1ccn2ccnc2c1
null
CC(=O)C
null
24
CI.Cc1nc2c(OCc3ccccc3Cl)cccn2c1CN(C)C>CC(=O)C>Cc1nc2c(OCc3ccccc3Cl)cccn2c1C[N+](C)(C)C.[I-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-185e83baf0c3403dab14950827063d22
C=CCC(Cl)C(C)=O.Nc1ncccc1OCc1ccccc1>>C=CCc1c(C)nc2c(OCc3ccccc3)cccn12
NC1=NC=CC=C1OCC1=CC=CC=C1.ClC(C(C)=O)CC=C>>C(C1=CC=CC=C1)OC=1C=2N(C=CC1)C(=C(N2)C)CC=C
O=[C:5]([CH:4](Cl)[CH2:3][CH:2]=[CH2:1])[CH3:6].[NH2:7][c:8]1[c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19][cH:20][n:21]1>>[CH2:1]=[CH:2][CH2:3][c:4]1[c:5]([CH3:6])[n:7][c:8]2[c:9]([O:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)[cH:18][cH:19][cH:20][n:21]12
C=CCC(Cl)C(C)=O.Nc1ncccc1OCc1ccccc1
C=CCc1c(C)nc2c(OCc3ccccc3)cccn12
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
68f76555483972bc3db5d3d4b5e479a66c1f89ab1b71b2a0fb941126aa9c191a
235fd48cd394ba1137abde2ba7484c051be6ffcae187060d6065fe5adf0e90a3
c1ccc(COc2cccn3ccnc23)cc1
Cl-[CH;D3;+0:1](-[C:2]-[C:3]=[C;D1;H2:4])-[C;H0;D3;+0:5](=O)-[C;D1;H3:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[n;H0;D2;+0:10]:[c:11]:[c:12]>>[C;D1;H2:4]=[C:3]-[C:2]-[c;H0;D3;+0:1]1:[c;H0;D3;+0:5](-[C;D1;H3:6]):[n;H0;D2;+0:7]:[c:8](:[c:9]):[n;H0;D3;+0:10]:1:[c:11]:[c:12]
7.4
[{"value": 7.4, "product": "C(C1=CC=CC=C1)OC=1C=2N(C=CC1)C(=C(N2)C)CC=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-amino-3-benzyloxypyridine (3 g) and 3-chloro-5-hexen-2-one (2.981 g) in ethanol (15 ml) was stirred and refluxed for 45 hours and then evaporated in vacuo. To the residue was added an aqueous solution of sodium bicarbonate and the mixture was extracted with ethyl acetate. The extract was washed with wat...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ketone.Primary amine
null
c1ccncc1
c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
HCl
C(C)O
null
null
C=CCC(Cl)C(C)=O.Nc1ncccc1OCc1ccccc1>C(C)O>C=CCc1c(C)nc2c(OCc3ccccc3)cccn12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-30e0a8c847e3408db73ba26ed7bed814
C#CCC(OS(=O)(=O)c1ccc(C)cc1)C(C)=O.Nc1ncccc1OCc1ccccc1>>C#CCc1c(C)nc2c(OCc3ccccc3)cccn12
NC1=NC=CC=C1OCC1=CC=CC=C1.S(=O)(=O)(C1=CC=C(C)C=C1)OC(C(C)=O)CC#C>>C(C1=CC=CC=C1)OC=1C=2N(C=CC1)C(=C(N2)C)CC#C
Cc1ccc(S(=O)(=O)O[CH:4]([CH2:3][C:2]#[CH:1])[C:5](=O)[CH3:6])cc1.[NH2:7][c:8]1[c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19][cH:20][n:21]1>>[CH:1]#[C:2][CH2:3][c:4]1[c:5]([CH3:6])[n:7][c:8]2[c:9]([O:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)[cH:18][cH:19][cH:20][n:21]12
C#CCC(OS(=O)(=O)c1ccc(C)cc1)C(C)=O.Nc1ncccc1OCc1ccccc1
C#CCc1c(C)nc2c(OCc3ccccc3)cccn12
null
null
C(C)O
Functional Group Interconversion
OtherReaction
05c332a02d21c1a0dc368986a4cd1766ba670505a7c33ce9a4e6613de9ab3a70
b3fe639a14cda8cf395bb492e10e6f982c6df5a0f3702dac7bbaa7704cd5b4d9
c1ccc(COc2cccn3ccnc23)cc1
C-c1:c:c:c(-S(=O)(=O)-O-[CH;D3;+0:1](-[C:2]-[C:3]#[C;D1;H1:4])-[C;H0;D3;+0:5](=O)-[C;D1;H3:6]):c:c:1.[NH2;D1;+0:7]-[c:8](:[c:9]):[n;H0;D2;+0:10]:[c:11]:[c:12]>>[C;D1;H1:4]#[C:3]-[C:2]-[c;H0;D3;+0:1]1:[c;H0;D3;+0:5](-[C;D1;H3:6]):[n;H0;D2;+0:7]:[c:8](:[c:9]):[n;H0;D3;+0:10]:1:[c:11]:[c:12]
31
[{"value": 31.0, "product": "C(C1=CC=CC=C1)OC=1C=2N(C=CC1)C(=C(N2)C)CC#C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-amino-3-benzyloxypyridine (2 g) and 3-tosyloxy-5-hexyn-2-one (2.66 g) in ethanol (15 ml) was stirred and refluxed for 24 hours and then evaporated in vacuo. To the residue was added an aqueous solution of sodium bicarbonate and the mixture was extracted with ethyl acetate. The extract was washed with wa...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Ketone.Primary amine
null
c1ccccc1.c1ccncc1
c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
TsOH.HO-
C(C)O
null
null
C#CCC(OS(=O)(=O)c1ccc(C)cc1)C(C)=O.Nc1ncccc1OCc1ccccc1>C(C)O>C#CCc1c(C)nc2c(OCc3ccccc3)cccn12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-02f0036534674dbdbf7bb937e43757ec
C#CCC(OS(C)(=O)=O)C(C)=O.Cc1ccccc1CNc1cccnc1N>>C#CCc1c(C)nc2c(NCc3ccccc3C)cccn12
NC1=NC=CC=C1NCC1=C(C=CC=C1)C.S(=O)(=O)(C)OC(C(C)=O)CC#C>>CC1=C(CNC=2C=3N(C=CC2)C(=C(N3)C)CC#C)C=CC=C1
CS(=O)(=O)O[CH:4]([CH2:3][C:2]#[CH:1])[C:5](=O)[CH3:6].[NH2:7][c:8]1[c:9]([NH:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[CH3:18])[cH:19][cH:20][cH:21][n:22]1>>[CH:1]#[C:2][CH2:3][c:4]1[c:5]([CH3:6])[n:7][c:8]2[c:9]([NH:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]3[CH3:18])[cH:19][cH:20][cH:21][n:22]1...
C#CCC(OS(C)(=O)=O)C(C)=O.Cc1ccccc1CNc1cccnc1N
C#CCc1c(C)nc2c(NCc3ccccc3C)cccn12
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
77a56b54cbecae5bd21ceb645c55e500764965636e673cfcf991bf32c16bcf53
bd0bab184c57def941fa6a922e349010f6f49341eb09c2fb9a172d2e8e4d8443
c1ccc(CNc2cccn3ccnc23)cc1
C-S(=O)(=O)-O-[CH;D3;+0:1](-[C:2]-[C:3]#[C;D1;H1:4])-[C;H0;D3;+0:5](=O)-[C;D1;H3:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[n;H0;D2;+0:10]:[c:11]:[c:12]>>[C;D1;H1:4]#[C:3]-[C:2]-[c;H0;D3;+0:1]1:[c;H0;D3;+0:5](-[C;D1;H3:6]):[n;H0;D2;+0:7]:[c:8](:[c:9]):[n;H0;D3;+0:10]:1:[c:11]:[c:12]
30.3
[{"value": 30.3, "product": "CC1=C(CNC=2C=3N(C=CC2)C(=C(N3)C)CC#C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-amino-3-(2-methylbenzylamino)pyridine (2 g) and 3-mesyloxy-5-hexyn-2-one (1.78 g) in ethanol (40 ml) was refluxed for 31.5 hours and then evaporated in vacuo. The residue was treated with aqueous sodium bicarbonate solution and extracted with methylene chloride. The extract was washed with water, dried ...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Ketone.Primary amine
null
c1ccncc1
c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
MsOH.HO-
C(C)O
null
null
C#CCC(OS(C)(=O)=O)C(C)=O.Cc1ccccc1CNc1cccnc1N>C(C)O>C#CCc1c(C)nc2c(NCc3ccccc3C)cccn12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5a47df5726014329923daab875341450
C#CCC(OS(C)(=O)=O)C(C)=O.Cc1ccccc1COc1nccnc1N>>C#CCc1c(C)nc2c(OCc3ccccc3C)nccn12
C([O-])(O)=O.[Na+].C([O-])(O)=O.[Na+].NC1=NC=CN=C1OCC1=C(C=CC=C1)C.S(=O)(=O)(C)OC(C(C)=O)CC#C>>CC1=C(COC=2C=3N(C=CN2)C(=C(N3)C)CC#C)C=CC=C1
CS(=O)(=O)O[CH:4]([CH2:3][C:2]#[CH:1])[C:5](=O)[CH3:6].[NH2:7][c:8]1[c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[CH3:18])[n:19][cH:20][cH:21][n:22]1>>[CH:1]#[C:2][CH2:3][c:4]1[c:5]([CH3:6])[n:7][c:8]2[c:9]([O:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]3[CH3:18])[n:19][cH:20][cH:21][n:22]12
C#CCC(OS(C)(=O)=O)C(C)=O.Cc1ccccc1COc1nccnc1N
C#CCc1c(C)nc2c(OCc3ccccc3C)nccn12
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
0b4115faa1b55129bb90c6c55ba81741c5593609c021552a032b4f0dd0725876
bd0bab184c57def941fa6a922e349010f6f49341eb09c2fb9a172d2e8e4d8443
c1ccc(COc2nccn3ccnc23)cc1
C-S(=O)(=O)-O-[CH;D3;+0:1](-[C:2]-[C:3]#[C;D1;H1:4])-[C;H0;D3;+0:5](=O)-[C;D1;H3:6].[#8:7]-[c:8]1:[#7;a:9]:[c:10]:[c:11]:[n;H0;D2;+0:12]:[c:13]:1-[NH2;D1;+0:14]>>[#8:7]-[c:8]1:[#7;a:9]:[c:10]:[c:11]:[n;H0;D3;+0:12]2:[c:13]:1:[n;H0;D2;+0:14]:[c;H0;D3;+0:5](-[C;D1;H3:6]):[c;H0;D3;+0:1]:2-[C:2]-[C:3]#[C;D1;H1:4]
3.8
[{"value": 3.8, "product": "CC1=C(COC=2C=3N(C=CN2)C(=C(N3)C)CC#C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Sodium bicarbonate (2.73 g) was added to a solution of 2-amino-3-(2-methylbenzyloxy)pyrazine (3.5 g) and 3-mesyloxy-5-hexyn-2-one (6.18 g) in ethanol (35 ml) and the mixture was refluxed for 12 hours. The mixture was poured into an aqueous solution of sodium bicarbonate and extracted with chloroform. The extract was wa...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Ketone.Primary amine
null
c1cnccn1
c1cn2ccnc2cn1
c1ccccc1.c1cn2ccnc2cn1
MsOH.HO-
C(C)O
null
null
C#CCC(OS(C)(=O)=O)C(C)=O.Cc1ccccc1COc1nccnc1N>C(C)O>C#CCc1c(C)nc2c(OCc3ccccc3C)nccn12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ebc91131d5f547cb8a0bb15bdb77240c
C#CCc1c(C)nc2c(OCc3ccccc3C)cccn12>>C=C=Cc1c(C)nc2c(OCc3ccccc3C)cccn12
CC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)CC#C)C=CC=C1.[OH-].[Na+]>>CC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)C=C=C)C=CC=C1
[CH:1]#[C:2][CH2:3][c:4]1[c:5]([CH3:6])[n:7][c:8]2[c:9]([O:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]3[CH3:18])[cH:19][cH:20][cH:21][n:22]12>>[CH2:1]=[C:2]=[CH:3][c:4]1[c:5]([CH3:6])[n:7][c:8]2[c:9]([O:10][CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]3[CH3:18])[cH:19][cH:20][cH:21][n:22]12
C#CCc1c(C)nc2c(OCc3ccccc3C)cccn12
C=C=Cc1c(C)nc2c(OCc3ccccc3C)cccn12
null
null
CO
Miscellaneous
OtherReaction
2f13f6ad84546451f3d01481775a52c4098398348b523c935b8104d01b87fd5f
a396e5546fe76b7265b1c53702233ee449ddd085280941b2992883e25d48851e
c1ccc(COc2cccn3ccnc23)cc1
[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5](:[c:6]):[c:7]:1-[CH2;D2;+0:8]-[C;H0;D2;+0:9]#[CH;D1;+0:10]>>[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5](:[c:6]):[c:7]:1-[CH;D2;+0:8]=[C;H0;D2;+0:9]=[CH2;D1;+0:10]
27.3
[{"value": 27.3, "product": "CC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)C=C=C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 8-(2-methylbenzyloxy)-3-(2-propynyl)-2-methylimidazo[1,2-a]pyridine (0.99 g) and 1N-sodium hydroxide solution (5.65 ml) in methanol (50 ml) was stirred for 72 hours at room temperature. The mixture was evaporated in vacuo and the residue was dissolved in chloroform. The solution was washed with brine, dri...
10.6084/m9.figshare.5104873.v1
null
Alkyne
Allene
null
null
c1ccccc1.c1ccn2ccnc2c1
null
CO
null
null
C#CCc1c(C)nc2c(OCc3ccccc3C)cccn12>CO>C=C=Cc1c(C)nc2c(OCc3ccccc3C)cccn12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ff349a1b204b4c2aab891a575c293bf5
Cc1ccccc1COc1cccn2c(C[N+](C)(C)C)c(C)nc12>>C#CCOCc1c(C)nc2c(OCc3ccccc3C)cccn12
[H-].[Na+].[I-].CC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)C[N+](C)(C)C)C=CC=C1>>CC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)COCC#C)C=CC=C1
[N+]([CH3:1])([CH3:2])([CH3:3])[CH2:5][c:6]1[c:7]([CH3:8])[n:9][c:10]2[c:11]([O:4][CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[CH3:20])[cH:21][cH:22][cH:23][n:24]12>>[CH:1]#[C:2][CH2:3][O:4][CH2:5][c:6]1[c:7]([CH3:8])[n:9][c:10]2[c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[CH3:20])[cH:21][cH:22...
Cc1ccccc1COc1cccn2c(C[N+](C)(C)C)c(C)nc12
C#CCOCc1c(C)nc2c(OCc3ccccc3C)cccn12
null
null
C(C#C)O
Functional Group Interconversion
OtherReaction
482318f577acf49c86cbbb7e098cb729667daafa70f29010a70e72298356abb3
5c0da6dbcd390e2c3349103c81f82cc550c05f4a0fd872aee3b671caf307c53d
c1ccc(COc2cccn3ccnc23)cc1
[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]2:[#7;a:5](:[c:6]:[c:7]:[c:8]:[c;H0;D3;+0:9]:2-[O;H0;D2;+0:10]-[CH2;D2;+0:11]-[c:12](:[c:13]):[c:14]):[c:15]:1-[CH2;D2;+0:16]-[N+](-[CH3;D1;+0:17])(-[CH3;D1;+0:18])-[CH3;D1;+0:19]>>[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]2:[#7;a:5](:[c:6]:[c:7]:[c:8]:[c;H0;D3;+0:9]:2-[#8:20]-[CH2;D2;+0:11]-[c:...
110.8
[{"value": 110.8, "product": "CC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)COCC#C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of sodium hydride (63.6% in mineral oil dispersion, 0.285 g) in 2-propynyl alcohol (12 ml) was added 8-(2-methylbenzyloxy)-3-trimethylammoniomethyl-2-methylimidazo[1,2-a]pyridine iodide (3 g) and the mixture was heated at 85°-100° C. for 1.5 hours. After being cooled, the mixture was poured into ice-water...
10.6084/m9.figshare.5104873.v1
null
Ether
Ether.Ether.Alkyne
c1ccn2ccnc2c1
c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
null
C(C#C)O
null
null
Cc1ccccc1COc1cccn2c(C[N+](C)(C)C)c(C)nc12>C(C#C)O>C#CCOCc1c(C)nc2c(OCc3ccccc3C)cccn12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b00092430ac54cc19a9bd1a0f1697fff
Cc1nc2c(OCc3ccccc3Cl)cccn2c1C[N+](C)(C)C>>C#CCOCc1c(C)nc2c(OCc3ccccc3Cl)cccn12
[H-].[Na+].[I-].ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)C[N+](C)(C)C)C=CC=C1>>ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)COCC#C)C=CC=C1
[N+]([CH3:1])([CH3:2])([CH3:3])[CH2:5][c:6]1[c:7]([CH3:8])[n:9][c:10]2[c:11]([O:4][CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[Cl:20])[cH:21][cH:22][cH:23][n:24]12>>[CH:1]#[C:2][CH2:3][O:4][CH2:5][c:6]1[c:7]([CH3:8])[n:9][c:10]2[c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[Cl:20])[cH:21][cH:22][...
Cc1nc2c(OCc3ccccc3Cl)cccn2c1C[N+](C)(C)C
C#CCOCc1c(C)nc2c(OCc3ccccc3Cl)cccn12
null
null
C(C#C)O
Functional Group Interconversion
OtherReaction
482318f577acf49c86cbbb7e098cb729667daafa70f29010a70e72298356abb3
5c0da6dbcd390e2c3349103c81f82cc550c05f4a0fd872aee3b671caf307c53d
c1ccc(COc2cccn3ccnc23)cc1
[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]2:[#7;a:5](:[c:6]:[c:7]:[c:8]:[c;H0;D3;+0:9]:2-[O;H0;D2;+0:10]-[CH2;D2;+0:11]-[c:12](:[c:13]):[c:14]):[c:15]:1-[CH2;D2;+0:16]-[N+](-[CH3;D1;+0:17])(-[CH3;D1;+0:18])-[CH3;D1;+0:19]>>[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]2:[#7;a:5](:[c:6]:[c:7]:[c:8]:[c;H0;D3;+0:9]:2-[#8:20]-[CH2;D2;+0:11]-[c:...
124.6
[{"value": 124.6, "product": "ClC1=C(COC=2C=3N(C=CC2)C(=C(N3)C)COCC#C)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of sodium hydride (60% in mineral oil dispersion, 0.186 g) in 2-propynyl alcohol (8 ml) was added 8-(2-chlorobenzyloxy)-3-trimethylammoniomethyl-2-methylimidazo[1,2-a]pyridine iodide (2 g) and the mixture was heated at 90°-95° C. with stirring for 1 hour. After being cooled, the mixture was poured into ic...
10.6084/m9.figshare.5104873.v1
null
Ether
Ether.Ether.Alkyne
c1ccn2ccnc2c1
c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
null
C(C#C)O
null
1
Cc1nc2c(OCc3ccccc3Cl)cccn2c1C[N+](C)(C)C>C(C#C)O>C#CCOCc1c(C)nc2c(OCc3ccccc3Cl)cccn12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3372c0ca9f334c538c916228292e2cfe
C#CCOCc1c(C)nc2c(OCc3ccccc3)cccn12.O=C=O>>Cc1nc2c(OCc3ccccc3)cccn2c1COCC#CC(=O)O
C(=O)=O.C(C1=CC=CC=C1)OC=1C=2N(C=CC1)C(=C(N2)C)COCC#C.C(CCC)[Li].C(C)(=O)O>>C(C1=CC=CC=C1)OC=1C=2N(C=CC1)C(=C(N2)C)COCC#CC(=O)O
[CH3:1][c:2]1[n:3][c:4]2[c:5]([O:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][cH:13]3)[cH:14][cH:15][cH:16][n:17]2[c:18]1[CH2:19][O:20][CH2:21][C:22]#[CH:23].[C:24](=[O:25])=[O:26]>>[CH3:1][c:2]1[n:3][c:4]2[c:5]([O:6][CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][cH:13]3)[cH:14][cH:15][cH:16][n:17]2[c:18]1[CH2:19][O:20][CH2:21...
C#CCOCc1c(C)nc2c(OCc3ccccc3)cccn12.O=C=O
Cc1nc2c(OCc3ccccc3)cccn2c1COCC#CC(=O)O
null
null
CCCCCC.O1CCCC1
Acylation
OtherReaction
79750b25e2e891222a6213659b9b96213d6cfd615f193dc07d015f66fa42c61b
d91f4325df4c0a97d921e50d724781c1eb02533a0e976122bbd0b1dc69cfd2e7
c1ccc(COc2cccn3ccnc23)cc1
[C:1]-[C:2]#[CH;D1;+0:3].[O;D1;H0:4]=[C;H0;D2;+0:5]=[O;H0;D1;+0:6]>>[C:1]-[C:2]#[C;H0;D2;+0:3]-[C;H0;D3;+0:5](=[O;D1;H0:4])-[OH;D1;+0:6]
58.6
[{"value": 58.6, "product": "C(C1=CC=CC=C1)OC=1C=2N(C=CC1)C(=C(N2)C)COCC#CC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To a solution of 8-benzyloxy-3-(2-propynyloxymethyl)-2-methylimidazo[1,2-a]pyridine (1 g) in tetrahydrofuran (10 ml) was added dropwise 10% solution of n-butyllithium in n-hexane (2.09 ml) at -60° C. under a nitrogen atmosphere. After being stirred for 10 minutes the solution was treated with dry ice (1.4 g), allowed t...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Carbon dioxide
Carboxylic acid.Alkyne
null
null
c1ccccc1.c1ccn2ccnc2c1
null
CCCCCC.O1CCCC1
null
0.166667
C#CCOCc1c(C)nc2c(OCc3ccccc3)cccn12.O=C=O>CCCCCC.O1CCCC1>Cc1nc2c(OCc3ccccc3)cccn2c1COCC#CC(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-374e80436b6f4dea998738769e836db4
O=C(Cn1c(S)nc2ccccc21)c1ccccn1>>c1ccc(-c2cn3c(nc4ccccc43)s2)nc1
SC1=NC2=C(N1CC(C1=NC=CC=C1)=O)C=CC=C2.C(=O)([O-])[O-].[Na+].[Na+]>>N1=C(C=CC=C1)C1=CN2C(=NC3=C2C=CC=C3)S1
O=[C:5]([c:4]1[cH:3][cH:2][cH:1][cH:18][n:17]1)[CH2:6][n:7]1[c:8]([SH:16])[n:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]12>>[cH:1]1[cH:2][cH:3][c:4](-[c:5]2[cH:6][n:7]3[c:8]([n:9][c:10]4[cH:11][cH:12][cH:13][cH:14][c:15]34)[s:16]2)[n:17][cH:18]1
O=C(Cn1c(S)nc2ccccc21)c1ccccn1
c1ccc(-c2cn3c(nc4ccccc43)s2)nc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
9d1596ab3913372e735f11645b8fe1732fad7a35a5ee22cad45f2cb93f68875c
7015f9bd646bfe69b891dc9cb85114e2d8c209a7ff8bee5e1ff5903b86ef8580
c1ccc(-c2cn3c(nc4ccccc43)s2)nc1
O=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[#7;a:3]1:[c:4]:[c:5]:[#7;a:6]:[c:7]:1-[SH;D1;+0:8])-[c;H0;D3;+0:9](:[#7;a:10]:[c:11]):[c:12]:[c:13]>>[c:11]:[#7;a:10]:[c;H0;D3;+0:9](-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[#7;a:3]2:[c:4]:[c:5]:[#7;a:6]:[c:7]:2:[s;H0;D2;+0:8]:1):[c:12]:[c:13]
37.5
[{"value": 37.5, "product": "N1=C(C=CC=C1)C1=CN2C(=NC3=C2C=CC=C3)S1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-mercapto-1-[2-oxo-2-(2-pyridyl)ethyl]benzimidazole (1 g.) in polyphosphoric acid was heated at 140° C. for 1 hour. The solution was neutralised with Na2CO3 solution and extracted into EtOAc (700 ml). The extracts were dried (MgSO4) and evaporated to give a solid which was recrystallised from EtOAc/EtOH ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Aromatic thiol
null
c1nc2ccccc2[nH]1
c1ccc2c(c1)nc1sccn12
c1ccncc1.c1ccc2c(c1)nc1sccn12
HO-
null
null
null
O=C(Cn1c(S)nc2ccccc21)c1ccccn1>>c1ccc(-c2cn3c(nc4ccccc43)s2)nc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e54381d6a37d4ac89c8f8f5dc9dbc8ea
COc1ccnc(C(=O)CBr)c1>>CC(C)O.CC(C)OC(C)C
C(=O)([O-])[O-].[K+].[K+].BrCC(=O)C1=NC=CC(=C1)OC.ClC=1NC2=C(N1)C=CC=C2.O>>CC(C)O.C(C)(C)OC(C)C
O=[C:5]([c:6]1nc[cH:1][c:2]([O:4][CH3:7])[cH:3]1)[CH2:11]Br>>[CH3:1][CH:2]([CH3:3])[OH:4].[CH3:5][CH:6]([CH3:7])[O:8][CH:9]([CH3:10])[CH3:11]
COc1ccnc(C(=O)CBr)c1
CC(C)O.CC(C)OC(C)C
null
null
CN(C=O)C
Miscellaneous
OtherReaction
f35c709fea588031a645ddcbbe2fffed2ee75bd6c97ae4d6538342ad677e37bc
97ee76a97823cae0ae8db273bb9cacc344d3c41821358baf271f1fb7c5df9370
null
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[O;H0;D2;+0:6]-[CH3;D1;+0:7]):[cH;D2;+0:8]:c:n:1>>[C;D1;H3:9]-[C:10](-[CH3;D1;+0:1])-[#8:11]-[CH;D3;+0:3](-[CH3;D1;+0:2])-[CH3;D1;+0:7].[CH3;D1;+0:8]-[CH;D3;+0:5](-[CH3;D1;+0:4])-[OH;D1;+0:6]
null
[]
2
CELSIUS
0.5
HOUR
2-Bromoacetyl-4-methoxypyridine (11.5 g, 0.05) and 2-chlorobenzimidazole (7.5 g, 0.05 mole) were dissolved in dimethylformamide (75 ml) and cooled to 2° C. K2CO3 (12 g, 0.08 mole) was added and the temperature rose to 9° C. as the suspension was stirred for 1/2 hour. The mixture was added to H2O (200 ml) giving a solid...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Ether
Ether.Secondary alcohol
c1ccncc1
null
null
Br-
CN(C=O)C
2
0.5
COc1ccnc(C(=O)CBr)c1>CN(C=O)C>CC(C)O.CC(C)OC(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-39008d9572cc46a1a61451fb05242526
Clc1nc2ccccc2[nH]1>>c1ccc2[nH]cnc2c1
ClC=1NC2=C(N1)C=CC=C2.BrCC(=O)C1=NC=CC(=C1C)SCC.C(=O)([O-])[O-].[K+].[K+]>>N1=CNC2=C1C=CC=C2
Cl[c:6]1[nH:5][c:4]2[cH:3][cH:2][cH:1][cH:9][c:8]2[n:7]1>>[cH:1]1[cH:2][cH:3][c:4]2[nH:5][cH:6][n:7][c:8]2[cH:9]1
Clc1nc2ccccc2[nH]1
c1ccc2[nH]cnc2c1
null
null
null
Functional Group Interconversion
Aromatic dehalogenation
ca1ff206ba5e3245a070477a37dade787c5ff5e118fea1cc6b950980a4e5b17a
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccc2[nH]cnc2c1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[#7;a:5]:1>>[#7;a:2]1:[c:3]:[c:4]:[#7;a:5]:[cH;D2;+0:1]:1
null
[]
null
null
null
null
2-Chlorobenzimidazole is reacted with 2-bromoacetyl-4-ethylthio-3-methylpyridine in the presence of K2CO3 to give 2-chloro-1-[2-[4-ethylthio-3-methylpyridyl])-2-oxoethyl]benzimidazole. This is reacted with thiourea and treated with NH4OH to give 2-mercapto-1-(2-(2-(4-ethylthio-3-methylpyridyl))-2-oxoethyl)benzimidazole...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1
Other
null
null
null
Clc1nc2ccccc2[nH]1>>c1ccc2[nH]cnc2c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a0df9816cf51486da9d534d6342d0836
CCSc1ccnc(-c2cn3c(nc4ccccc43)s2)c1C.O=C(OO)c1cccc(Cl)c1>>CCSc1ccnc(C2=Cn3c(nc4ccccc43)S2=O)c1C
C(C)SC1=C(C(=NC=C1)C1=CN2C(=NC3=C2C=CC=C3)S1)C.ClC=1C=C(C(=O)OO)C=CC1>>C(C)SC1=C(C(=NC=C1)C1=CN2C(=NC3=C2C=CC=C3)S1=O)C
[CH3:1][CH2:2][S:3][c:4]1[cH:5][cH:6][n:7][c:8](-[c:9]2[cH:10][n:11]3[c:12]([n:13][c:14]4[cH:15][cH:16][cH:17][cH:18][c:19]34)[s:20]2)[c:22]1[CH3:23].O=C(O[OH:21])c1cccc(Cl)c1>>[CH3:1][CH2:2][S:3][c:4]1[cH:5][cH:6][n:7][c:8]([C:9]2=[CH:10][n:11]3[c:12]([n:13][c:14]4[cH:15][cH:16][cH:17][cH:18][c:19]34)[S:20]2=[O:21])[c...
CCSc1ccnc(-c2cn3c(nc4ccccc43)s2)c1C.O=C(OO)c1cccc(Cl)c1
CCSc1ccnc(C2=Cn3c(nc4ccccc43)S2=O)c1C
null
null
C(Cl)Cl
Oxidation
OtherReaction
3af9ed32602f5852fad4d7bddcb7110cf8597d7ff387aa22f73409d6e758b38e
081bebe60ef12ca80072327af69d872c987a74a66ca947b1bdb982ac71fd1052
O=S1C(c2ccccn2)=Cn2c1nc1ccccc12
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C;D1;H3:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[c;H0;D3;+0:6]1:[cH;D2;+0:7]:[#7;a:8]2:[c:9]:[c:10]:[#7;a:11]:[c:12]:2:[s;H0;D2;+0:13]:1):[#7;a:14]:[c:15]>>[C;D1;H3:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[C;H0;D3;+0:6]1=[CH;D2;+0:7]-[#7;a:8]2:[c:9]:[c:10]:[#7;a:11]:[c:12]:2-[S;H0;D3;+0:13]-...
null
[]
null
null
null
null
A solution of 2-(4-ethylthio-3-methylpyrid-2-yl)-thiazolo[3,2-a]benzimidazole (0.01 mole) is dissolved in CH2Cl2 solution (100 ml) at 0° C. and treated with m-chloroperoxybenzoic acid (0.01 mole) for 0.5 hours. The solution is then washed with sodium carbonate solution and dried (MgSO4). Purification by chromatography ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide
Sulfoxide
c1ccc2c(c1)nc1sccn12.c1ccccc1
c1ccc2c(c1)nc1sccn12
c1ccncc1.c1ccc2c(c1)nc1sccn12
HCl
C(Cl)Cl
null
null
CCSc1ccnc(-c2cn3c(nc4ccccc43)s2)c1C.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>CCSc1ccnc(C2=Cn3c(nc4ccccc43)S2=O)c1C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-adafda2f10aa459986df317fa2d32be6
COc1ccc2[nH]ccc2c1.N#CCCl.NC(N)=S>>COc1ccc2[nH]cc(SCC#N)c2c1
ClCC#N.COC=1C=C2C=CNC2=CC1.NC(=S)N.II>>COC=1C=C2C(=CNC2=CC1)SCC#N
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][cH:8][cH:9][c:14]2[cH:15]1.Cl[CH2:11][C:12]#[N:13].NC(N)=[S:10]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][cH:8][c:9]([S:10][CH2:11][C:12]#[N:13])[c:14]2[cH:15]1
COc1ccc2[nH]ccc2c1.N#CCCl.NC(N)=S
COc1ccc2[nH]cc(SCC#N)c2c1
null
null
CO.O.C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
6eca71f48de78b8f1122f33a4f563f3ae4d8df6bf08c897e78e7ec4233dc53a4
304c94f4367e24c71f550ef55805048586c03c416bc00e3c48114269d0abdd01
c1ccc2[nH]ccc2c1
Cl-[CH2;D2;+0:1]-[C:2]#[N;D1;H0:3].N-C(-N)=[S;H0;D1;+0:4].[c:5]:[c:6]1:[cH;D2;+0:7]:[c:8]:[#7;a:9]:[c:10]:1:[c:11]>>[N;D1;H0:3]#[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:4]-[c;H0;D3;+0:7]1:[c:8]:[#7;a:9]:[c:10](:[c:11]):[c:6]:1:[c:5]
42
[{"value": 42.0, "product": "COC=1C=C2C(=CNC2=CC1)SCC#N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a solution of 50 g (0.34 mole) of 5-methoxyindole and 25.8 (0.34 mole) of thiourea in 1700 ml of 50% aqueous methanol was added 340 ml of KI/I2 in water over a 5 minute period and the reaction mixture was allowed to stir at room temperature for 3 hours. The reaction mixture was then evaporated in vacuo to about 1100...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Monosulfide
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
HCl
CO.O.C(C)OCC
null
3
COc1ccc2[nH]ccc2c1.N#CCCl.NC(N)=S>CO.O.C(C)OCC>COc1ccc2[nH]cc(SCC#N)c2c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e1d5c8532bfa4e83949fd6e9d0c8900e
Cc1cccc2c(SCC#N)c[nH]c12>>Cc1cccc2c(SCCN)c[nH]c12
CC=1C=CC=C2C(=CNC12)SCC#N.[H-].[Al+3].[Li+].[H-].[H-].[H-].[Al+3].[Cl-].[Cl-].[Cl-]>>NCCSC1=CNC2=C(C=CC=C12)C
[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[c:7]([S:8][CH2:9][C:10]#[N:11])[cH:12][nH:13][c:14]12>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[c:7]([S:8][CH2:9][CH2:10][NH2:11])[cH:12][nH:13][c:14]12
Cc1cccc2c(SCC#N)c[nH]c12
Cc1cccc2c(SCCN)c[nH]c12
null
null
CCOCC
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
c1ccc2[nH]ccc2c1
[#16:1]-[C:2]-[C;H0;D2;+0:3]#[N;H0;D1;+0:4]>>[#16:1]-[C:2]-[CH2;D2;+0:3]-[NH2;D1;+0:4]
null
[]
null
null
null
null
The ether solution was separated and dried over MgSO4. The filtered solution was evaporated in vacuo to give 24.4 g (66%) of 7-methylindol-3-ylthioacetonitrile as a tan solid. An ether solution of 14.1 g (70 mmole) of the nitrile was treated with 2.7 g (70 mmole) of lithium aluminum hydride and 9.5 g (70 mmole) of AlCl...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
c1ccc2[nH]ccc2c1
null
CCOCC
null
null
Cc1cccc2c(SCC#N)c[nH]c12>CCOCC>Cc1cccc2c(SCCN)c[nH]c12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3ac68fcac968481094ca4e6ef976f341
C1CNCCN1.Fc1ccc(CCl)cc1>>Fc1ccc(CN2CCNCC2)cc1
FC1=CC=C(CCl)C=C1.C(C)O.N1CCNCC1.C(C)O>>FC1=CC=C(CN2CCNCC2)C=C1
[NH:7]1[CH2:8][CH2:9][NH:10][CH2:11][CH2:12]1.Cl[CH2:6][c:5]1[cH:4][cH:3][c:2]([F:1])[cH:14][cH:13]1>>[F:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][N:7]2[CH2:8][CH2:9][NH:10][CH2:11][CH2:12]2)[cH:13][cH:14]1
C1CNCCN1.Fc1ccc(CCl)cc1
Fc1ccc(CN2CCNCC2)cc1
null
null
CCOCC
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
61ec49e5207aa33ebff7094bb66b1d997d4af14524931a8b3643ef7a94219a9a
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CN2CCNCC2)cc1
Cl-[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:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1):[c:4]
55.7
[{"value": 55.7, "product": "FC1=CC=C(CN2CCNCC2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
2
HOUR
A solution of 29 g of p-fluorobenzyl chloride in 50 g of reagent ethanol was added dropwise to a stirred solution of 34.5 g of piperazine in 150 g of reagent ethanol. A cold water bath was used to maintain the reaction temperature at 20° C. during the addition. The reaction mixture was stirred for an additional 11/2 ho...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CNCCN1
C1C[NH]CCN1
c1ccccc1.C1C[NH]CCN1
HCl
CCOCC
20
2
C1CNCCN1.Fc1ccc(CCl)cc1>CCOCC>Fc1ccc(CN2CCNCC2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9e8e1e68cd8c457689d598080df4296f
ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1.O=C(CN1CCNCC1)c1ccccc1>>O=C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1
C(C(=O)C1=CC=CC=C1)N1CCNCC1.ClCCCN1CCN(CC1)CC1=CC=C(C=C1)Cl.C(C)N(CC)CC>>ClC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC(=O)C2=CC=CC=C2)C=C1
Cl[CH2:8][CH2:9][CH2:10][N:11]1[CH2:12][CH2:13][N:14]([CH2:15][c:16]2[cH:17][cH:18][c:19]([Cl:20])[cH:21][cH:22]2)[CH2:23][CH2:24]1.[O:1]=[C:2]([CH2:3][N:4]1[CH2:5][CH2:6][NH:7][CH2:25][CH2:26]1)[c:27]1[cH:28][cH:29][cH:30][cH:31][cH:32]1>>[O:1]=[C:2]([CH2:3][N:4]1[CH2:5][CH2:6][N:7]([CH2:8][CH2:9][CH2:10][N:11]2[CH2:1...
ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1.O=C(CN1CCNCC1)c1ccccc1
O=C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b703623ddc3b029d4716c15f5414f41773434bcc7e3f3853faf62273596bed77
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C(CN1CCN(CCCN2CCN(Cc3ccccc3)CC2)CC1)c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
77.5
[{"value": 50.0, "product": "ClC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC(=O)C2=CC=CC=C2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.5, "product": "ClC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC(=O)C2=CC=CC=C2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4.1 g of 1-phenacylpiperazine, 5.7 g of 1-chloro-3-[4-(4-chlorobenzyl)-1-piperazinyl]propane, 2.6 g of triethylamine and 35 ml of reagent ethanol was refluxed for 5 hours. The solvent was removed by rotary evaporation, 150 ml of water were added, and the mixture was extracted with ether (3×150 ml). The eth...
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.C1C[NH]CC[NH]1.c1ccccc1.c1ccccc1
HCl
C(C)O
null
null
ClCCCN1CCN(Cc2ccc(Cl)cc2)CC1.O=C(CN1CCNCC1)c1ccccc1>C(C)O>O=C(CN1CCN(CCCN2CCN(Cc3ccc(Cl)cc3)CC2)CC1)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5fbf8b934342464383a21037ee00b589
ClCCl.Clc1ccc(CN2CCNCC2)cc1.O=C(Cl)CC(=O)Cl.[OH-]>>Cl.Cl.O.O=C(CC(=O)N1CCN(Cc2ccc(Cl)cc2)CC1)N1CCN(Cc2ccc(Cl)cc2)CC1
[OH-].[Na+].ClC1=CC=C(CN2CCNCC2)C=C1.C(CC(=O)Cl)(=O)Cl.C(Cl)Cl>>O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)C(CC(=O)N2CCN(CC2)CC2=CC=C(C=C2)Cl)=O)C=C1
Cl[CH2:35][Cl:32].[NH:9]1[CH2:10][CH2:11][N:12]([CH2:13][c:14]2[cH:15][cH:16][c:17]([Cl:18])[cH:19][cH:20]2)[CH2:21][CH2:22]1.[Cl:1][C:36]([CH2:6][C:5]([Cl:2])=[O:4])=[O:8].[OH-:3]>>[ClH:1].[ClH:2].[OH2:3].[O:4]=[C:5]([CH2:6][C:7](=[O:8])[N:9]1[CH2:10][CH2:11][N:12]([CH2:13][c:14]2[cH:15][cH:16][c:17]([Cl:18])[cH:19][c...
ClCCl.Clc1ccc(CN2CCNCC2)cc1.O=C(Cl)CC(=O)Cl.[OH-]
Cl.Cl.O.O=C(CC(=O)N1CCN(Cc2ccc(Cl)cc2)CC1)N1CCN(Cc2ccc(Cl)cc2)CC1
null
null
C(C)N(CC)CC
Aromatic Heterocycle Formation
OtherReaction
ac379cbfa9f2e1769d6f1c27fb3ebb1edfecdf976ffc21a437ef9644b50637c7
41623b51c86655a69083ebffce0dd73032f5ac63ff2ccd2898fe0580e61913f7
O=C(CC(=O)N1CCN(Cc2ccccc2)CC1)N1CCN(Cc2ccccc2)CC1
Cl-[CH2;D2;+0:1]-[Cl;H0;D1;+0:2].[#7:3]1-[C:4]-[C:5]-[NH;D2;+0:6]-[C:7]-[C:8]-1.[Cl;H0;D1;+0:9]-[C;H0;D3;+0:10](=[O;H0;D1;+0:11])-[CH2;D2;+0:12]-[C;H0;D3;+0:13](-[Cl;H0;D1;+0:14])=[O;D1;H0:15].[OH-;D0:16]>>[C:17]-[#7:18]1-[C:19]-[C:20]-[#7:21](-[C;H0;D3;+0:13](=[O;D1;H0:15])-[CH2;D2;+0:12]-[C:22](=[O;H0;D1;+0:11])-[N;H...
45.1
[{"value": 22.0, "product": "O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)C(CC(=O)N2CCN(CC2)CC2=CC=C(C=C2)Cl)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 45.1, "product": "O.Cl.Cl.ClC1=CC=C(CN2CCN(CC2)C(CC(=O)N2CCN(CC2)CC2=CC=C(C=C2)Cl)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
60
HOUR
A mixture of 4.2 g of 1-(4-chlorobenzyl)piperazine, 1.4 g of malonyl dichloride, 10 g of methylene chloride and 2.0 g of triethylamine was stirred for 60 hours. The reaction mixture was made basic with 2N sodium hydroxide. The organic layer was separated, and the aqueous phase was extracted with three 50 ml portions of...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Primary halide.Primary halide.Secondary amine
Aromatic halide.Tertiary amide.Tertiary amide.Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1.C1C[NH]CC[NH]1.c1ccccc1
C1C[NH]CC[NH]1.c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
null
C(C)N(CC)CC
null
60
ClCCl.Clc1ccc(CN2CCNCC2)cc1.O=C(Cl)CC(=O)Cl.[OH-]>C(C)N(CC)CC>Cl.Cl.O.O=C(CC(=O)N1CCN(Cc2ccc(Cl)cc2)CC1)N1CCN(Cc2ccc(Cl)cc2)CC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-17ee4450157049288fbf93d876e000e4
CC(c1ccccc1)N1CCNCC1.ClCCCBr>>CC(c1ccccc1)N1CCN(CCCN2CCN(C(C)c3ccccc3)CC2)CC1.Cl.Cl.Cl.Cl
C1(=CC=CC=C1)C(C)N1CCNCC1.BrCCCCl>>Cl.Cl.Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCN1CCN(CC1)C(C)C1=CC=CC=C1
[NH:9]1[CH2:17][CH2:18][N:19]([CH:20]([CH3:21])[c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)[CH2:28][CH2:29]1.Br[CH2:2][CH2:14][CH2:1][Cl:32]>>[CH3:1][CH:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]1[CH2:10][CH2:11][N:12]([CH2:13][CH2:14][CH2:15][N:16]2[CH2:17][CH2:18][N:19]([CH:20]([CH3:21])[c:22]3[cH:23][cH:24][cH:2...
CC(c1ccccc1)N1CCNCC1.ClCCCBr
CC(c1ccccc1)N1CCN(CCCN2CCN(C(C)c3ccccc3)CC2)CC1.Cl.Cl.Cl.Cl
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
6e158a54a631fccf88355586f2945a2595f247424e72404e0ad4bd3708ba00d6
c7e09259e1b5abfe3121d0f0f4968272fe438d5dd27de348d3ddb2af70014c90
c1ccc(CN2CCN(CCCN3CCN(Cc4ccccc4)CC3)CC2)cc1
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[Cl;H0;D1;+0:4].[C:5]-[#7:6]1-[C:7]-[CH2;D2;+0:8]-[NH;D2;+0:9]-[CH2;D2;+0:10]-[C:11]-1>>[C:5]-[#7:6]1-[C:7]-[CH2;D2;+0:8]-[#7:12](-[C:13]-[CH2;D2;+0:2]-[C:14]-[#7:15]2-[C:16]-[C:17]-[N;H0;D3;+0:9](-[CH;D3;+0:1](-[CH3;D1;+0:3])-[c:18](:[c:19]):[c:20])-[C:21]-[C:22]-2)-[CH2;D2...
211.9
[{"value": 51.0, "product": "Cl.Cl.Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCN1CCN(CC1)C(C)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 211.9, "product": "Cl.Cl.Cl.Cl.C1(=CC=CC=C1)C(C)N1CCN(CC1)CCCN1CCN(CC1)C(C)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 7.6 g of 1-(1-phenylethyl)piperazine, 3.2 g of 1-bromo-3-chloropropane and 50 ml of reagent ethanol was refluxed for 5 hours. The solvent was then removed under vacuum, 75 ml of water were added, and the mixture was extracted with ether (3×150 ml). The ether extract was evaporated to an oil and chromatogra...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Secondary amine
Tertiary amine.Tertiary amine.Tertiary amine
C1CNCC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.C1C[NH]CC[NH]1.c1ccccc1
Br-
C(C)O
null
null
CC(c1ccccc1)N1CCNCC1.ClCCCBr>C(C)O>CC(c1ccccc1)N1CCN(CCCN2CCN(C(C)c3ccccc3)CC2)CC1.Cl.Cl.Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7341df2adb3541c79cb658048cb382de
CO.ClCCCBr.ClCCl.Clc1cccc(CN2CCNCC2)c1.[NH4+].[OH-]>>Cl.Clc1cccc(CN2CCN(CCCN3CCN(Cc4cccc(Cl)c4)CC3)CC2)c1.O
C(Cl)Cl.CO.[OH-].[NH4+].ClC=1C=C(CN2CCNCC2)C=CC1.BrCCCCl.Cl>>O.Cl.Cl.ClC=1C=C(CN2CCN(CC2)CCCN2CCN(CC2)CC2=CC(=CC=C2)Cl)C=CC1
O[CH3:28].Br[CH2:30][CH2:15][CH2:14][Cl:27].Cl[CH2:21][Cl:1].[Cl:3][c:4]1[cH:5][cH:6][cH:7][c:8]([CH2:9][N:10]2[CH2:11][CH2:12][NH:13][CH2:31][CH2:32]2)[cH:33]1.[NH4+:17].[OH-:34]>>[ClH:1].[Cl:3][c:4]1[cH:5][cH:6][cH:7][c:8]([CH2:9][N:10]2[CH2:11][CH2:12][N:13]([CH2:14][CH2:15][CH2:16][N:17]3[CH2:18][CH2:19][N:20]([CH2...
CO.ClCCCBr.ClCCl.Clc1cccc(CN2CCNCC2)c1.[NH4+].[OH-]
Cl.Clc1cccc(CN2CCN(CCCN3CCN(Cc4cccc(Cl)c4)CC3)CC2)c1.O
null
null
C(C)O.O.C(C)N(CC)CC
Aromatic Heterocycle Formation
OtherReaction
aa370d01081fc4e3cf6d3649b69e93c12fb8744fad75b2065fbda06b71b922b3
53faa84b34b0ef284a224692dfeee7f31714383e2d662b7a0243dcf1398f2ce0
c1ccc(CN2CCN(CCCN3CCN(Cc4ccccc4)CC3)CC2)cc1
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[Cl;H0;D1;+0:4].Cl-[CH2;D2;+0:5]-[Cl;H0;D1;+0:6].O-[CH3;D1;+0:7].[#7:8]1-[C:9]-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13]-1.[NH4+;D0:14].[OH-;D0:15]>>[Cl;H0;D1;+0:4]-[c:16](:[c:17]):[cH;D2;+0:7]:[c:18](-[CH2;D2;+0:5]-[#7:19]1-[C:20]-[C:21]-[N;H0;D3;+0:14](-[C:22]-[CH2;D2;+0:2]-[CH2;...
68
[{"value": 68.0, "product": "O.Cl.Cl.ClC=1C=C(CN2CCN(CC2)CCCN2CCN(CC2)CC2=CC(=CC=C2)Cl)C=CC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 6.3 g of 1-(3-chlorobenzyl)piperazine, 2.4 g of 1-bromo-3-chloropropane, 50 ml of reagent ethanol and 3.0 g of triethylamine was refluxed for 4 hours. Water (70 ml) was added, and the mixture was concentrated under vacuum to about 70 ml. The resulting aqueous mixture was extracted with ether (3×150 ml), an...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Primary halide.Primary halide.Secondary amine.Methanol
Aromatic halide.Tertiary amine.Tertiary amine.Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1.C1C[NH]CC[NH]1.c1ccccc1
c1ccccc1.C1C[NH]CC[NH]1.C1C[NH]CC[NH]1.c1ccccc1
Br-
C(C)O.O.C(C)N(CC)CC
null
null
CO.ClCCCBr.ClCCl.Clc1cccc(CN2CCNCC2)c1.[NH4+].[OH-]>C(C)O.O.C(C)N(CC)CC>Cl.Clc1cccc(CN2CCN(CCCN3CCN(Cc4cccc(Cl)c4)CC3)CC2)c1.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-35f81a39a06a45d1ab9c40a8e88e5022
COc1ccc(CN2CCN(CCCN3CCN(Cc4ccc(OC)cc4)CC3)CC2)cc1>>Oc1ccc(CN2CCN(CCCN3CCN(Cc4ccc(O)cc4)CC3)CC2)cc1
COC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC2=CC=C(C=C2)OC)C=C1.Br>>OC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC2=CC=C(C=C2)O)C=C1
C[O:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][N:7]2[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][N:14]3[CH2:15][CH2:16][N:17]([CH2:18][c:19]4[cH:20][cH:21][c:22]([O:23]C)[cH:24][cH:25]4)[CH2:26][CH2:27]3)[CH2:28][CH2:29]2)[cH:30][cH:31]1>>[OH:1][c:2]1[cH:3][cH:4][c:5]([CH2:6][N:7]2[CH2:8][CH2:9][N:10]([CH2:11][CH2:12][CH2:13][...
COc1ccc(CN2CCN(CCCN3CCN(Cc4ccc(OC)cc4)CC3)CC2)cc1
Oc1ccc(CN2CCN(CCCN3CCN(Cc4ccc(O)cc4)CC3)CC2)cc1
null
null
O
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
c1ccc(CN2CCN(CCCN3CCN(Cc4ccccc4)CC3)CC2)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].C-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]
31
[{"value": 31.0, "product": "OC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC2=CC=C(C=C2)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 30.8, "product": "OC1=CC=C(CN2CCN(CC2)CCCN2CCN(CC2)CC2=CC=C(C=C2)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4.5 g of 1,3-bis[4-(4-methoxybenzyl)-1-piperazinyl]propane from Example 19 and 125 ml of 49% hydrobromic acid was refluxed for 2 hours and was then cooled and diluted with 125 ml of water. After filtration the aqueous solution was neutralized with 2N sodium hydroxide to adjust the pH to 8. The resulting mi...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1.C1C[NH]CC[NH]1.C1C[NH]CC[NH]1.c1ccccc1
Other
O
null
null
COc1ccc(CN2CCN(CCCN3CCN(Cc4ccc(OC)cc4)CC3)CC2)cc1>O>Oc1ccc(CN2CCN(CCCN3CCN(Cc4ccc(O)cc4)CC3)CC2)cc1