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large_stringclasses
414 values
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large_stringlengths
36
36
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large_stringlengths
4
873
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large_stringlengths
19
1.07k
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large_stringlengths
14
3.37k
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large_stringlengths
1
581
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large_stringlengths
1
433
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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
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large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
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large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
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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-fae1bc17779a4c33ab6bacd79ee3ea5d
CCOC(=O)/C=C/c1cc(=O)c(OCc2ccccc2)c[nH]1>>O=C(O)/C=C/c1cc(=O)c(OCc2ccccc2)c[nH]1
O=C1C=C(NC=C1OCC1=CC=CC=C1)/C=C/C(=O)OCC.[OH-].[K+]>>O=C1C=C(NC=C1OCC1=CC=CC=C1)/C=C/C(=O)O
CC[O:3][C:2](=[O:1])/[CH:4]=[CH:5]/[c:6]1[cH:7][c:8](=[O:9])[c:10]([O:11][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][nH:20]1>>[O:1]=[C:2]([OH:3])/[CH:4]=[CH:5]/[c:6]1[cH:7][c:8](=[O:9])[c:10]([O:11][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][nH:20]1
CCOC(=O)/C=C/c1cc(=O)c(OCc2ccccc2)c[nH]1
O=C(O)/C=C/c1cc(=O)c(OCc2ccccc2)c[nH]1
null
null
C(C)O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1cc[nH]cc1OCc1ccccc1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])/[C:4]=[C:5]/[c:6]:[#7;a:7]>>[#7;a:7]:[c:6]/[C:5]=[C:4]/[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
null
[]
null
null
null
null
(E)-3-[1,4-Dihydro-4-oxo-5-(phenylmethoxy)-2-pyridinyl]-2-propenoic acid, ethyl ester (1.5 g) and 0.29 g of potassium hydroxide were stirred in 30 ml of ethanol for two hours at 50° C. After evaporating the solvent, the residue was dissolved in 100 ml of water and filtered. Hydrochloric acid (2N) was added to the filtr...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccncc1.c1ccccc1
Other
C(C)O
null
null
CCOC(=O)/C=C/c1cc(=O)c(OCc2ccccc2)c[nH]1>C(C)O>O=C(O)/C=C/c1cc(=O)c(OCc2ccccc2)c[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b1182f573e4048b888b6653ec0ae28f6
CC(C)(C)OC(=O)NN1CCNC1=O.O=C(Br)CBr>>CC(C)(C)OC(=O)NN1CCN(C(=O)CBr)C1=O
O=C1N(CCN1)NC(OC(C)(C)C)=O.N1=CC=CC=C1.BrCC(=O)Br>>BrCC(=O)N1C(N(CC1)NC(OC(C)(C)C)=O)=O
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][N:9]1[CH2:10][CH2:11][NH:12][C:17]1=[O:18].Br[C:13](=[O:14])[CH2:15][Br:16]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][N:9]1[CH2:10][CH2:11][N:12]([C:13](=[O:14])[CH2:15][Br:16])[C:17]1=[O:18]
CC(C)(C)OC(=O)NN1CCNC1=O.O=C(Br)CBr
CC(C)(C)OC(=O)NN1CCN(C(=O)CBr)C1=O
null
null
ClCCl
Acylation
N-alkylation of secondary amines with alkyl halides
c0d7cb275ad2aac32e9deba8fd2a7ffefbc279aaa29e792f49788aaa2d41eb1f
ed2e2a2113014ef864b0a3bd063f004647b373e1f6820e0fdd5587d12a0e8460
O=C1NCCN1
Br-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[Br;D1;H0:4].[C;D1;H3:5]-[C:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[#8:9]-[C:10](=[O;D1;H0:11])-[#7:12]-[#7:13]1-[C:14]-[C:15]-[NH;D2;+0:16]-[C:17]-1=[O;D1;H0:18]>>[Br;D1;H0:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:16]1-[C:15]-[C:14]-[#7:13](-[#7:12]-[C:10](=[O;D1;H0:11])-[#8:9]-[...
null
[]
0
CELSIUS
null
null
N-(2-Oxo-1-imidazolidinyl)carbamic acid, 1,1-dimethylethyl ester (12.0 g, 0.06 mmol) was dissolved in dichloromethane (75 ml) containing pyridine (5.2 g, 0.066 mol). The solution was cooled to 0° C. and treated slowly with bromoacetyl bromide (13.3 g, 0.066 mol). The solution was evaporated in vacuo to give a yellow oi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Urea
Urea.Substituted dicarboximide
C1CNC[NH]1
C1C[NH]C[NH]1
C1C[NH]C[NH]1
HBr
ClCCl
0
null
CC(C)(C)OC(=O)NN1CCNC1=O.O=C(Br)CBr>ClCCl>CC(C)(C)OC(=O)NN1CCN(C(=O)CBr)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-71dd9c746bed41b09c643f7528bb9407
CC(C)(C)OC(=O)NN1CCN(C(=O)CBr)C1=O.[I-]>>CC(C)(C)OC(=O)NN1CCN(C(=O)CI)C1=O
BrCC(=O)N1C(N(CC1)NC(OC(C)(C)C)=O)=O.[I-].[Na+]>>ICC(=O)N1C(N(CC1)NC(OC(C)(C)C)=O)=O
Br[CH2:15][C:13]([N:12]1[CH2:11][CH2:10][N:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[C:17]1=[O:18])=[O:14].[I-:16]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][N:9]1[CH2:10][CH2:11][N:12]([C:13](=[O:14])[CH2:15][I:16])[C:17]1=[O:18]
CC(C)(C)OC(=O)NN1CCN(C(=O)CBr)C1=O.[I-]
CC(C)(C)OC(=O)NN1CCN(C(=O)CI)C1=O
null
null
CC(=O)C
Functional Group Interconversion
OtherReaction
e944a2acb95a43a23818321f2ac2f96ba2f2b8d34f52c1cfd1e3802d2403177f
e2ca6f9fe1078a3836d617896a4e5cc310fb155ca459b021e2b549b3e61f1df7
O=C1NCCN1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#7:4](-[C:5])-[C:6](=[O;D1;H0:7])-[#7:8].[I-;H0;D0:9]>>[#7:8]-[C:6](=[O;D1;H0:7])-[#7:4](-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[I;H0;D1;+0:9])-[C:5]
null
[]
null
null
null
null
N-[3-(Bromoacetyl)-2-oxo-1-imidazolidinyl]carbamic acid, 1,1-dimethylethyl ester (20.9 g, 65 mmol) was dissolved in acetone (250 ml) containing sodium iodide (10.5 g, 70 mmol). The solution was stirred at reflux for three hours and filtered hot through Celite. The solution was evaporated in vacuo to give the title comp...
10.6084/m9.figshare.5104873.v1
null
Primary halide
Primary halide
null
null
C1C[NH]C[NH]1
Br-
CC(=O)C
null
null
CC(C)(C)OC(=O)NN1CCN(C(=O)CBr)C1=O.[I-]>CC(=O)C>CC(C)(C)OC(=O)NN1CCN(C(=O)CI)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-acf88472c2ef4cab9331b6f75454c6a6
C[C@H]1[C@H](NC(=O)OCc2ccccc2)C(=O)N1P(=O)(O)OCC(=O)N1CCN(NC(=O)OC(C)(C)C)C1=O>>C[C@H]1[C@H](NC(=O)OCc2ccccc2)C(=O)N1P(=O)(O)OCC(=O)N1CCN(N)C1=O
CC(C)(OC(=O)NN1C(N(CC1)C(COP(=O)(N1[C@H]([C@@H](C1=O)NC(OCC1=CC=CC=C1)=O)C)O)=O)=O)C.[K].C1(=CC=CC=C1)OC.FC(C(=O)O)(F)F.C([O-])(O)=O.[Na+]>>NN1C(N(CC1)C(COP(=O)(N1[C@H]([C@@H](C1=O)NC(OCC1=CC=CC=C1)=O)C)O)=O)=O
CC(C)(C)OC(=O)[NH:29][N:28]1[CH2:27][CH2:26][N:25]([C:23]([CH2:22][O:21][P:18]([N:17]2[C@@H:2]([CH3:1])[C@H:3]([NH:4][C:5](=[O:6])[O:7][CH2:8][c:9]3[cH:10][cH:11][cH:12][cH:13][cH:14]3)[C:15]2=[O:16])(=[O:19])[OH:20])=[O:24])[C:30]1=[O:31]>>[CH3:1][C@H:2]1[C@H:3]([NH:4][C:5](=[O:6])[O:7][CH2:8][c:9]2[cH:10][cH:11][cH:1...
C[C@H]1[C@H](NC(=O)OCc2ccccc2)C(=O)N1P(=O)(O)OCC(=O)N1CCN(NC(=O)OC(C)(C)C)C1=O
C[C@H]1[C@H](NC(=O)OCc2ccccc2)C(=O)N1P(=O)(O)OCC(=O)N1CCN(N)C1=O
null
null
O
Reduction
Reduction of primary amides to amines
dd5f1d5939749381406c2645d26610b15255d5a51ca846ff661f45d1c5e951db
b8e1e75e4199725018e8cff61fd2fde98c56b629bbf185579b99364e52c966a1
O=C(N[C@H]1CN([PH](=O)OCC(=O)N2CCNC2=O)C1=O)OCc1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[#7:2]1-[C:3]-[C:4]-[#7:5](-[C:6]=[O;D1;H0:7])-[C:8]-1=[O;D1;H0:9]>>[NH2;D1;+0:1]-[#7:2]1-[C:3]-[C:4]-[#7:5](-[C:6]=[O;D1;H0:7])-[C:8]-1=[O;D1;H0:9]
null
[]
null
null
6
HOUR
(2S-trans)[1-[[2-[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-oxo-1-imidazolidinyl]-2-oxoethoxy]hydroxyphosphinyl]-2-methyl-4-oxo-3-azetidinyl]carbamic acid, phenylmethyl ester, monopotassium salt (5.9 g, 10 mmol) was treated at 0° C. sequentially with anisole (25 ml) and trifluoroacetic acid (60 ml), and the solution w...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Acylhydrazine.Carbamic ester.Ether.Boc
Acylhydrazine
null
null
C1C[NH]C1.c1ccccc1.C1C[NH]C[NH]1
HO-
O
null
6
C[C@H]1[C@H](NC(=O)OCc2ccccc2)C(=O)N1P(=O)(O)OCC(=O)N1CCN(NC(=O)OC(C)(C)C)C1=O>O>C[C@H]1[C@H](NC(=O)OCc2ccccc2)C(=O)N1P(=O)(O)OCC(=O)N1CCN(N)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-81dc0c6c46c04f688c9e0a0ed9716418
CCC1CO1.Nc1ccccc1>>CCC(O)CNc1ccccc1
NC1=CC=CC=C1.O1CCOCC1.O1CC1CC.[F-].[K+]>>C1(=CC=CC=C1)NCC(CC)O
[CH3:1][CH2:2][CH:3]1[O:4][CH2:5]1.[NH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][CH2:2][CH:3]([OH:4])[CH2:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
CCC1CO1.Nc1ccccc1
CCC(O)CNc1ccccc1
null
null
C(Cl)Cl.O
Heteroatom Alkylation and Arylation
OtherReaction
f75f8fec78b0ee9c8e880101c8c57c2a3edaac070bc7ad0163a34826e2af8c65
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
c1ccccc1
[C:1]-[C:2]1-[CH2;D2;+0:3]-[O;H0;D2;+0:4]-1.[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C:1]-[C:2](-[OH;D1;+0:4])-[CH2;D2;+0:3]-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
null
null
null
null
Aniline, (102.3 g, 1.1 mole) was added to 50 ml of dioxane, 108 g of 1,2-epoxy butane and 1 g of potassium fluoride in 25 ml of water. The mixture heated to reflux for 30 hours. The mixture was poured into water, taken up in 200 ml of methylene chloride, dried over anhydrous magnesium sulfate and stripped under vacuum....
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
C1CO1
null
c1ccccc1
null
C(Cl)Cl.O
null
null
CCC1CO1.Nc1ccccc1>C(Cl)Cl.O>CCC(O)CNc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2606b9cbf440416d8f3e63a1500dbed7
CCC(O)CNc1ccc(F)c(C(F)(F)F)c1.O=Cc1cccc(Cl)c1>>CCC1CN(c2ccc(F)c(C(F)(F)F)c2)C(c2cccc(Cl)c2)O1
ClC=1C=C(C=O)C=CC1.FC(C=1C=C(C=CC1F)NCC(CC)O)(F)F>>ClC=1C=C(C=CC1)C1OC(CN1C1=CC(=C(C=C1)F)C(F)(F)F)CC
[CH3:1][CH2:2][CH:3]([CH2:4][NH:5][c:6]1[cH:7][cH:8][c:9]([F:10])[c:11]([C:12]([F:13])([F:14])[F:15])[cH:16]1)[OH:25].O=[CH:17][c:18]1[cH:19][cH:20][cH:21][c:22]([Cl:23])[cH:24]1>>[CH3:1][CH2:2][CH:3]1[CH2:4][N:5]([c:6]2[cH:7][cH:8][c:9]([F:10])[c:11]([C:12]([F:13])([F:14])[F:15])[cH:16]2)[CH:17]([c:18]2[cH:19][cH:20][...
CCC(O)CNc1ccc(F)c(C(F)(F)F)c1.O=Cc1cccc(Cl)c1
CCC1CN(c2ccc(F)c(C(F)(F)F)c2)C(c2cccc(Cl)c2)O1
null
CS(=O)(=O)O
null
Heteroatom Alkylation and Arylation
OtherReaction
ab3b4f808b07350acfd6d1e85757bbd6baa88d84a0ea16a460bf9c38c0c85e4e
95793bcca7dfdb9678898541206b5740e40b60c474970e6249c9e5d5ba1d0947
c1ccc(C2OCCN2c2ccccc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](-[OH;D1;+0:7])-[C:8]-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C:5]-[C:6]1-[C:8]-[N;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[O;H0;D2;+0:7]-1
null
[]
null
null
null
null
Meta-chlorobenzaldehyde (2.3 g, 0.016 mole) was combined with 5 g of 1-(3-trifluoromethyl-4-fluorophenylamino)-2-butanol and 3 drops of methane sulfonic acid was added. The mixture was heated on the steam bath for about one hour and stripped on the rotary evaporator. The product, a sticky, thick liquid, was characteriz...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary alcohol.Secondary amine
Ether.Tertiary amine
null
C1COC[NH]1
C1COC[NH]1.c1ccccc1.c1ccccc1
HO-
CS(=O)(=O)O
null
null
CCC(O)CNc1ccc(F)c(C(F)(F)F)c1.O=Cc1cccc(Cl)c1>CS(=O)(=O)O>CCC1CN(c2ccc(F)c(C(F)(F)F)c2)C(c2cccc(Cl)c2)O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-95fce6ee0fd6497e86db89788ce9af11
CCC(O)CNc1ccc(Cl)c(C(F)(F)F)c1.N#Cc1cccc(C=O)c1>>CCC1CN(c2ccc(Cl)c(C(F)(F)F)c2)C(c2cccc(C#N)c2)O1
C(#N)C=1C=C(C=O)C=CC1.FC(C=1C=C(C=CC1Cl)NCC(CC)O)(F)F.O>>C(#N)C=1C=C(C=CC1)C1OC(CN1C1=CC(=C(C=C1)Cl)C(F)(F)F)CC
[CH3:1][CH2:2][CH:3]([CH2:4][NH:5][c:6]1[cH:7][cH:8][c:9]([Cl:10])[c:11]([C:12]([F:13])([F:14])[F:15])[cH:16]1)[OH:26].O=[CH:17][c:18]1[cH:19][cH:20][cH:21][c:22]([C:23]#[N:24])[cH:25]1>>[CH3:1][CH2:2][CH:3]1[CH2:4][N:5]([c:6]2[cH:7][cH:8][c:9]([Cl:10])[c:11]([C:12]([F:13])([F:14])[F:15])[cH:16]2)[CH:17]([c:18]2[cH:19]...
CCC(O)CNc1ccc(Cl)c(C(F)(F)F)c1.N#Cc1cccc(C=O)c1
CCC1CN(c2ccc(Cl)c(C(F)(F)F)c2)C(c2cccc(C#N)c2)O1
null
CS(=O)(=O)O
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
ab3b4f808b07350acfd6d1e85757bbd6baa88d84a0ea16a460bf9c38c0c85e4e
95793bcca7dfdb9678898541206b5740e40b60c474970e6249c9e5d5ba1d0947
c1ccc(C2OCCN2c2ccccc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](-[OH;D1;+0:7])-[C:8]-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]>>[C:5]-[C:6]1-[C:8]-[N;H0;D3;+0:9](-[c:10](:[c:11]):[c:12])-[CH;D3;+0:1](-[c:2](:[c:3]):[c:4])-[O;H0;D2;+0:7]-1
null
[]
null
null
null
null
Meta-cyanobenzaldehyde (2.1 g, 0.016 mole) was added to 4.3 g of 1-(3-trifluoromethyl-4-chlorophenylamino)-2-butanol in 50 ml of toluene and 2-3 drops of methane sulfonic acid was added. The mixture was refluxed under a modified Dean-Stark apparatus until no more water came off and the mixture was stripped on a rotary ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary alcohol.Secondary amine
Ether.Tertiary amine
null
C1COC[NH]1
C1COC[NH]1.c1ccccc1.c1ccccc1
HO-
CS(=O)(=O)O.C1(=CC=CC=C1)C
null
null
CCC(O)CNc1ccc(Cl)c(C(F)(F)F)c1.N#Cc1cccc(C=O)c1>CS(=O)(=O)O.C1(=CC=CC=C1)C>CCC1CN(c2ccc(Cl)c(C(F)(F)F)c2)C(c2cccc(C#N)c2)O1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d3aa4ef6e7854887855a44c964e29706
CC(C)(C)C1(COc2ccc(Cl)cc2)CO1.c1nc[nH]n1>>CC(C)(C)C(O)(COc1ccc(Cl)cc1)Cn1cncn1
ClC1=CC=C(OCC2(OC2)C(C)(C)C)C=C1.N1N=CN=C1.C(C)(=O)OCC>>ClC1=CC=C(OCC(CN2N=CN=C2)(C(C)(C)C)O)C=C1
[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]1([CH2:7][O:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[O:6][CH2:16]1.[nH:17]1[cH:18][n:19][cH:20][n:21]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]([OH:6])([CH2:7][O:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1)[CH2:16][n:17]1[cH:18][n:19][cH:20][n:21]1
CC(C)(C)C1(COc2ccc(Cl)cc2)CO1.c1nc[nH]n1
CC(C)(C)C(O)(COc1ccc(Cl)cc1)Cn1cncn1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
28a0254009916c6c546927d7927691482e70d5ce5f7580284682740d091ca734
64c863766284618c8c914b50974c3faab567499928c69890adf3711c924533f0
c1ccc(OCCCn2cncn2)cc1
[#7;a:1]1:[c:2]:[nH;D2;+0:3]:[#7;a:4]:[c:5]:1.[C:6]-[C:7]1(-[C:8])-[CH2;D2;+0:9]-[O;H0;D2;+0:10]-1>>[C:6]-[C:7](-[C:8])(-[OH;D1;+0:10])-[CH2;D2;+0:9]-[n;H0;D3;+0:3]1:[#7;a:4]:[c:5]:[#7;a:1]:[c:2]:1
65
[{"value": 65.0, "product": "ClC1=CC=C(OCC(CN2N=CN=C2)(C(C)(C)C)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.8, "product": "ClC1=CC=C(OCC(CN2N=CN=C2)(C(C)(C)C)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
72.15 g (0.3 mole) of 2-(4-chlorophenoxy-methyl)-2-tert.-butyl-oxirane and 24.15 g (0.35 mole) of 1,2,4-triazole were heated under reflux in 120 ml of ethanol for 48 hours. The mixture was then concentrated, the residue was taken up in 200 ml of ethyl acetate and the ethyl acetate mixture was heated. It was then cooled...
10.6084/m9.figshare.5104873.v1
null
Ether
Tertiary alcohol
C1CO1.c1nc[nH]n1
c1nc[nH]n1
c1ccccc1.c1nc[nH]n1
null
C(C)O
null
null
CC(C)(C)C1(COc2ccc(Cl)cc2)CO1.c1nc[nH]n1>C(C)O>CC(C)(C)C(O)(COc1ccc(Cl)cc1)Cn1cncn1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b9a65196066a45deb5cb3baa21f1de1c
CC(C)(C)C(=O)COc1ccc(Cl)cc1.COS(=O)(=O)OC>>CC(C)(C)C1(COc2ccc(Cl)cc2)CO1
CSC.S(=O)(=O)(OC)OC.ClC1=CC=C(OCC(C(C)(C)C)=O)C=C1.C[O-].[Na+]>>ClC1=CC=C(OCC2(OC2)C(C)(C)C)C=C1
[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]([CH2:6][O:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1)=[O:16].COS(=O)(=O)O[CH3:15]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]1([CH2:6][O:7][c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]2)[CH2:15][O:16]1
CC(C)(C)C(=O)COc1ccc(Cl)cc1.COS(=O)(=O)OC
CC(C)(C)C1(COc2ccc(Cl)cc2)CO1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
8baa6edb5cd8bf6ac3a159f9a2c83da9850af70751cef9ef728836b2ad75fe75
65a8af0997ec9f56fa44fac9e6db8d8aeec07e535d6b4d216a6180693919dc05
c1ccc(OCC2CO2)cc1
C-O-S(=O)(=O)-O-[CH3;D1;+0:1].[#8:2]-[C:3]-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[C:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[C;D1;H3:9]>>[#8:2]-[C:3]-[C;H0;D4;+0:4]1(-[C:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[C;D1;H3:9])-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-1
84
[{"value": 84.0, "product": "ClC1=CC=C(OCC2(OC2)C(C)(C)C)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 83.9, "product": "ClC1=CC=C(OCC2(OC2)C(C)(C)C)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of 162 ml (2.2 moles) of dimethyl sulphide in 400 ml of absolute acetonitrile was added to a solution of 189 ml (2.0 moles) of dimethyl sulphate in 1,200 ml of absolute acetonitrile at room temperature. The reaction mixture was stirred overnight at room temperature. 118.8 g (2.2 moles) of sodium methylate we...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ether
null
C1CO1
c1ccccc1.C1CO1
HO-
C(C)#N
null
8
CC(C)(C)C(=O)COc1ccc(Cl)cc1.COS(=O)(=O)OC>C(C)#N>CC(C)(C)C1(COc2ccc(Cl)cc2)CO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-65ac7b4e119c45f7be18d6fb28021e3d
CC(C)(C)C1(C=Cc2ccc(Cl)cc2)CO1.CCO.c1nc[nH]n1>>CC(C)(C)C(O)(C=Cc1ccc(Cl)cc1)Cn1ccnc1
ClC1=CC=C(C=C1)C=CC1(OC1)C(C)(C)C.N1N=CN=C1.C(C)O>>ClC1=CC=C(C=C1)C=CC(C(C)(C)C)(O)CN1C=NC=C1
[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]1([CH:7]=[CH:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[O:6][CH2:16]1.OC[CH3:18].n1[nH:17][cH:21][n:20][cH:19]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]([OH:6])([CH:7]=[CH:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1)[CH2:16][n:17]1[cH:18][cH:19][n:20][cH:21]1
CC(C)(C)C1(C=Cc2ccc(Cl)cc2)CO1.CCO.c1nc[nH]n1
CC(C)(C)C(O)(C=Cc1ccc(Cl)cc1)Cn1ccnc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
5ea3783ebbd7096b13f1a1e72bf7085cb2d74cabf763792337323141dcbf5162
02cfabc6df4b8f83999e8e1bd949695f2480f50e3abb598c239092f7460dfe4f
C(=Cc1ccccc1)CCn1ccnc1
O-C-[CH3;D1;+0:1].[#7;a:2]1:[c:3]:[nH;D2;+0:4]:n:[cH;D2;+0:5]:1.[C:6]-[C:7]1(-[C:8]=[C:9]-[c:10])-[CH2;D2;+0:11]-[O;H0;D2;+0:12]-1>>[C:6]-[C:7](-[OH;D1;+0:12])(-[C:8]=[C:9]-[c:10])-[CH2;D2;+0:11]-[n;H0;D3;+0:4]1:[c:3]:[#7;a:2]:[cH;D2;+0:5]:[cH;D2;+0:1]:1
77
[{"value": 77.0, "product": "ClC1=CC=C(C=C1)C=CC(C(C)(C)C)(O)CN1C=NC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 17.75 g (0.075 mole) of 2-(4-chlorophenyl-ethenyl)-2-tert.-butyl-oxirane and 6.9 g (0.1 mole) of 1,2,4-triazole in 30 ml of ethanol was heated in a bomb tube at 150° C. for 20 hours. The reaction mixture was then concentrated and the crystalline residue was stirred with ether. The solid was then filtered ...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol
Tertiary alcohol
C1CO1.c1nc[nH]n1
c1c[nH]cn1
c1ccccc1.c1c[nH]cn1
HO-
null
null
null
CC(C)(C)C1(C=Cc2ccc(Cl)cc2)CO1.CCO.c1nc[nH]n1>>CC(C)(C)C(O)(C=Cc1ccc(Cl)cc1)Cn1ccnc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-31a19b8bc9484cb78d47d71464d3b4e3
CC(C)(C)C1(CCc2ccc(Cl)cc2)CO1.c1nc[nH]n1>>CC(C)(C)C(O)(CCc1ccc(Cl)cc1)Cn1cncn1
ClC1=CC=C(C=C1)CCC1(OC1)C(C)(C)C.N1N=CN=C1>>ClC1=CC=C(C=C1)CCC(C(C)(C)C)(O)CN1N=CN=C1
[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]1([CH2:7][CH2:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[O:6][CH2:16]1.[nH:17]1[cH:18][n:19][cH:20][n:21]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]([OH:6])([CH2:7][CH2:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1)[CH2:16][n:17]1[cH:18][n:19][cH:20][n:21]1
CC(C)(C)C1(CCc2ccc(Cl)cc2)CO1.c1nc[nH]n1
CC(C)(C)C(O)(CCc1ccc(Cl)cc1)Cn1cncn1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
28a0254009916c6c546927d7927691482e70d5ce5f7580284682740d091ca734
64c863766284618c8c914b50974c3faab567499928c69890adf3711c924533f0
c1ccc(CCCCn2cncn2)cc1
[#7;a:1]1:[c:2]:[nH;D2;+0:3]:[#7;a:4]:[c:5]:1.[C:6]-[C:7]1(-[C:8])-[CH2;D2;+0:9]-[O;H0;D2;+0:10]-1>>[C:6]-[C:7](-[C:8])(-[OH;D1;+0:10])-[CH2;D2;+0:9]-[n;H0;D3;+0:3]1:[#7;a:4]:[c:5]:[#7;a:1]:[c:2]:1
53.3
[{"value": 53.2, "product": "ClC1=CC=C(C=C1)CCC(C(C)(C)C)(O)CN1N=CN=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.3, "product": "ClC1=CC=C(C=C1)CCC(C(C)(C)C)(O)CN1N=CN=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 17.9 g (0.075 mole) of 2-(4-chlorophenylethyl)-2-tert.-butyl-oxirane and 6.9 g (0.1 mole) of 1,2,4-triazole in 30 ml of ethanol was heated in a bomb tube at 150° C. for 20 hours. The reaction solution was allowed to cool and was concentrated. The residue was dissolved in ether and the solution was washed ...
10.6084/m9.figshare.5104873.v1
null
Ether
Tertiary alcohol
C1CO1.c1nc[nH]n1
c1nc[nH]n1
c1ccccc1.c1nc[nH]n1
null
C(C)O
null
null
CC(C)(C)C1(CCc2ccc(Cl)cc2)CO1.c1nc[nH]n1>C(C)O>CC(C)(C)C(O)(CCc1ccc(Cl)cc1)Cn1cncn1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-aa9ed74e9a0d49428bacce5162b0c162
CC(C)C(C)(N)C(N)=O.CC1=C(C)C(=O)OC1=O>>C/C(C(=O)O)=C(\C)C(=O)NC(C)(C(N)=O)C(C)C
C/C/1=C(/C(=O)OC1=O)\C.NC(C(=O)N)(C(C)C)C>>C/C(/C(=O)NC(C(C)C)(C)C(=O)N)=C(/C(=O)O)\C
[NH2:10][C:11]([CH3:12])([C:13]([NH2:14])=[O:15])[CH:16]([CH3:17])[CH3:18].[CH3:1][C:2]1=[C:6]([CH3:7])[C:8](=[O:9])[O:5][C:3]1=[O:4]>>[CH3:1]/[C:2]([C:3](=[O:4])[OH:5])=[C:6](\[CH3:7])[C:8](=[O:9])[NH:10][C:11]([CH3:12])([C:13]([NH2:14])=[O:15])[CH:16]([CH3:17])[CH3:18]
CC(C)C(C)(N)C(N)=O.CC1=C(C)C(=O)OC1=O
C/C(C(=O)O)=C(\C)C(=O)NC(C)(C(N)=O)C(C)C
null
null
C(Cl)Cl
Protection
OtherReaction
5eeb1ad872b9f10501b37c5f8eee8f05cbb334b0ab6844e4f6b65e32b076e4ce
d83a5fe7c1575bfa4f6a9dc1cf7406e299c5c7ecfc75f13bc6d348857a70653f
null
[C;D1;H3:1]-[C:2]1=[C:3](-[C;D1;H3:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-[C:8]-1=[O;D1;H0:9].[C:10]-[C:11](-[C;D1;H3:12])(-[NH2;D1;+0:13])-[C:14](-[N;D1;H2:15])=[O;D1;H0:16]>>[C:10]-[C:11](-[C;D1;H3:12])(-[NH;D2;+0:13]-[C;H0;D3;+0:5](=[O;D1;H0:6])/[C:3](-[C;D1;H3:4])=[C:2](/[C;D1;H3:1])-[C:8](=[O;D1;H0:9])-[O...
96.3
[{"value": 96.0, "product": "C/C(/C(=O)NC(C(C)C)(C)C(=O)N)=C(/C(=O)O)\\C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.3, "product": "C/C(/C(=O)NC(C(C)C)(C)C(=O)N)=C(/C(=O)O)\\C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 46 g of dimethylmaleic acid anhydride, 48 g of 2-amino-2,3-dimethylbutyric acid amide and 70 ml of methylene chloride was heated at its boiling point for 15 minutes. After some of the solvent had been distilled off, the residual mixture was stirred with 300 ml of diethyl ether, and the product precipitated...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Carboxylic acid.Secondary amide
C1=CCOC1
null
null
null
C(Cl)Cl
null
null
CC(C)C(C)(N)C(N)=O.CC1=C(C)C(=O)OC1=O>C(Cl)Cl>C/C(C(=O)O)=C(\C)C(=O)NC(C)(C(N)=O)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1726b250b80e416d94f4df3e349e6e44
CC(C)C(C)(N)C(N)=O>>CC(C)C(C)([NH-])C(N)=O
NC(C(=O)N)(C(C)C)C.C(C)N(CC)CC.[Cl-].C/C(/C(=O)OCC)=C(\C(=O)[O-])/C>>C(C)OC(\C(=C(\C(=O)[O-])/C)\C)=O.NC(=O)C(C(C)C)(C)[NH-]
[CH3:1][CH:2]([CH3:3])[C:4]([CH3:5])([NH2:6])[C:7]([NH2:8])=[O:9]>>[CH3:1][CH:2]([CH3:3])[C:4]([CH3:5])([NH-:6])[C:7]([NH2:8])=[O:9]
CC(C)C(C)(N)C(N)=O
CC(C)C(C)([NH-])C(N)=O
null
null
C(Cl)Cl
Reduction
OtherReaction
a4dec735d83c6848619f7be0a55460a7c8d55fc3ba038446e1223b4ec7329128
a4f16f822d2806606c05d0c4baa1761ad37a11006840dde863a01a253bdff5dd
null
[C:1]-[C:2](-[C;D1;H3:3])(-[NH2;D1;+0:4])-[C:5](-[N;D1;H2:6])=[O;D1;H0:7]>>[C:1]-[C:2](-[C;D1;H3:3])(-[NH-;D1:4])-[C:5](-[N;D1;H2:6])=[O;D1;H0:7]
42.3
[{"value": 41.0, "product": "C(C)OC(\\C(=C(\\C(=O)[O-])/C)\\C)=O.NC(=O)C(C(C)C)(C)[NH-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 42.3, "product": "C(C)OC(\\C(=C(\\C(=O)[O-])/C)\\C)=O.NC(=O)C(C(C)C)(C)[NH-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 13 g of monoethyl 2,3-dimethylfumarate chloride in 20 ml of methylene chloride was added dropwise, while stirring and cooling with ice, to a solution of 12 g of 2-amino-2,3-dimethyl-butyric acid amide and 12 ml of triethylamine in 80 ml of methylene chloride. The mixture was stirred for 2 hours at room te...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
null
null
null
null
C(Cl)Cl
null
null
CC(C)C(C)(N)C(N)=O>C(Cl)Cl>CC(C)C(C)([NH-])C(N)=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a4c6ac19a65248798aac4e008fbbaf15
Cc1cc(C)c(C#N)c(N)n1.O=C=NS(=O)(=O)c1ccccc1[N+](=O)[O-]>>Cc1cc(C)c(C#N)c(NC(=O)NS(=O)(=O)c2ccccc2[N+](=O)[O-])n1
NC1=NC(=CC(=C1C#N)C)C.[N+](=O)([O-])C1=C(C=CC=C1)S(=O)(=O)N=C=O>>C(#N)C=1C(=NC(=CC1C)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)[N+](=O)[O-]
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]([C:7]#[N:8])[c:9]([NH2:10])[n:26]1.[C:11](=[O:12])=[N:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[N+:23](=[O:24])[O-:25]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]([C:7]#[N:8])[c:9]([NH:10][C:11](=[O:12])[NH:13][S:14](=[O:15])(=[O:16])[c:17]2[cH:18][cH:19][c...
Cc1cc(C)c(C#N)c(N)n1.O=C=NS(=O)(=O)c1ccccc1[N+](=O)[O-]
Cc1cc(C)c(C#N)c(NC(=O)NS(=O)(=O)c2ccccc2[N+](=O)[O-])n1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ccccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5].[O;D1;H0:6]=[C;H0;D2;+0:7]=[N;H0;D2;+0:8]-[#16:9](=[O;D1;H0:10])(=[O;D1;H0:11])-[c:12]>>[O;D1;H0:6]=[C;H0;D3;+0:7](-[NH;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5])-[NH;D2;+0:8]-[#16:9](=[O;D1;H0:10])(=[O;D1;H0:11])-[c:12]
null
[]
null
null
8
HOUR
To a stirred suspension of 0.5 g (4.3 mmol) 2-amino-4,6-dimethyl-3-pyridinecarbonitrile [Archiv. Pharm., 288, 174 (1955)] in 20 ml of acetonitrile was added 1.3 g (5.7 mmol) o-nitrobenzenesulfonyl isocyanate. The mixture was then heated to reflux (80°) for four hours followed by stirring at ambient temperature overnigh...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccncc1.c1ccccc1
null
C(C)#N
null
8
Cc1cc(C)c(C#N)c(N)n1.O=C=NS(=O)(=O)c1ccccc1[N+](=O)[O-]>C(C)#N>Cc1cc(C)c(C#N)c(NC(=O)NS(=O)(=O)c2ccccc2[N+](=O)[O-])n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-78ad90bd69134387b5703ba1c2246b9a
COc1cc(N)nc(OC)n1.O=[N+]([O-])O>>COc1nc(N)c([N+](=O)[O-])c(OC)n1
S(O)(O)(=O)=O.COC1=NC(=CC(=N1)N)OC.[N+](=O)(O)[O-]>>COC1=NC(=C(C(=N1)N)[N+](=O)[O-])OC
[CH3:1][O:2][c:3]1[n:4][c:5]([NH2:6])[cH:7][c:11]([O:12][CH3:13])[n:14]1.O[N+:8](=[O:9])[O-:10]>>[CH3:1][O:2][c:3]1[n:4][c:5]([NH2:6])[c:7]([N+:8](=[O:9])[O-:10])[c:11]([O:12][CH3:13])[n:14]1
COc1cc(N)nc(OC)n1.O=[N+]([O-])O
COc1nc(N)c([N+](=O)[O-])c(OC)n1
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
17bd7245f9d737a6c07bbf84345ed5d1d53ccf508974b3db72c7e5633e72b7db
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1cncnc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[#8:4]-[c:5]1:[#7;a:6]:[c:7]:[#7;a:8]:[c:9](-[N;D1;H2:10]):[cH;D2;+0:11]:1>>[#8:4]-[c:5]1:[#7;a:6]:[c:7]:[#7;a:8]:[c:9](-[N;D1;H2:10]):[c;H0;D3;+0:11]:1-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]
null
[]
null
null
null
null
To a solution of 20 ml of concentrated nitric acid and 16 ml of concentrated sulfuric acid was added 3.9 g (0.025 mmol) of 2,6-dimethoxy-4-pyrimidinamine. The resulting solution was stirred at ambient temperature and pressure for thirty minutes and was then stirred at 50° for fifteen minutes. The solution was then cool...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1cncnc1
c1cncnc1
c1cncnc1
HO-
null
null
null
COc1cc(N)nc(OC)n1.O=[N+]([O-])O>>COc1nc(N)c([N+](=O)[O-])c(OC)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9ecd5cb885984a4aae7b8025b84f1e4f
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)c([N+](=O)[O-])c(OC)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)nc(OC)c1[N+](=O)[O-]
COC1=NC(=C(C(=N1)N)[N+](=O)[O-])OC.C(=O)(OC)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=C(C(=N1)NC(=O)NS(=O)(=O)C1=C(C(=O)OC)C=CC=C1)[N+](=O)[O-])OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][c:20]([O:21][CH3:22])[n:23][c:24]([O:25][CH3:26])[c:27]1[N+:28](=[O:29])[O-:30]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[N...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)c([N+](=O)[O-])c(OC)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)nc(OC)c1[N+](=O)[O-]
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ccncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1.[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[N;H0;D2;+0:12]=[C;H0;D2;+0:13]=[O;D1;H0:14]>>[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[NH;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1
90.6
[{"value": 90.6, "product": "COC1=NC(=C(C(=N1)NC(=O)NS(=O)(=O)C1=C(C(=O)OC)C=CC=C1)[N+](=O)[O-])OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
A solution of 0.2 g (1.0 mmol) of 2,6-dimethoxy-5-nitro-4-pyrimidinamine and 0.6 g (2.4 mmol) of 2-carbomethoxybenzenesulfonyl isocyanate in 15 ml of methylene chloride was stirred at ambient temperature and pressure for 12 hours under anhydrous conditions. The solvent was then evaporated under reduced pressure. The re...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cncnc1
null
C(Cl)Cl
null
12
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)c([N+](=O)[O-])c(OC)n1>C(Cl)Cl>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)nc(OC)c1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c4afe691e3a7425cae2c519da2b6103e
Cc1nc(C)c(C#N)c(N)n1.O=C=NS(=O)(=O)c1ccccc1Cl>>Cc1nc(C)c(C#N)c(NC(=O)NS(=O)(=O)c2ccccc2Cl)n1
ClC1=C(C=CC=C1)S(=O)(=O)N=C=O.NC1=NC(=NC(=C1C#N)C)C.N12CCN(CC1)CC2>>ClC1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=NC(=C1C#N)C)C
[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]#[N:8])[c:9]([NH2:10])[n:24]1.[C:11](=[O:12])=[N:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[Cl:23]>>[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]#[N:8])[c:9]([NH:10][C:11](=[O:12])[NH:13][S:14](=[O:15])(=[O:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]...
Cc1nc(C)c(C#N)c(N)n1.O=C=NS(=O)(=O)c1ccccc1Cl
Cc1nc(C)c(C#N)c(NC(=O)NS(=O)(=O)c2ccccc2Cl)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ccncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1.[O;D1;H0:8]=[C;H0;D2;+0:9]=[N;H0;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14]>>[O;D1;H0:8]=[C;H0;D3;+0:9](-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1)-[NH;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14]
71.2
[{"value": 71.2, "product": "ClC1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=NC(=C1C#N)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
DAY
4.35 g of 2-Chlorobenzenesulfonyl isocyanate was dissolved in 10 ml xylenes and 25 ml methylene chloride. To this was added 2.96 g of 4-amino-2,6-dimethyl-5-pyrimidine carbonitrile and a catalytic amount of 1,4-diazabicyclo-[2.2.2]octane. The reaction was stirred under a CaSO4 drying tube for three days. The reaction w...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1cncnc1.c1ccccc1
null
C(Cl)Cl
null
72
Cc1nc(C)c(C#N)c(N)n1.O=C=NS(=O)(=O)c1ccccc1Cl>C(Cl)Cl>Cc1nc(C)c(C#N)c(NC(=O)NS(=O)(=O)c2ccccc2Cl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6a5fb342034c427dadbea3f95a18e897
Cc1cc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(Cl)Cl>>Cc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(Cl)Cl)n1
NC1=NC(=CC(=N1)C)C.ClC(C1=C(C=CC=C1)S(=O)(=O)N=C=O)Cl>>ClC(C1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=CC(=N1)C)C)Cl
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[n:6][c:7]([NH2:8])[n:24]1.[C:9](=[O:10])=[N:11][S:12](=[O:13])(=[O:14])[c:15]1[cH:16][cH:17][cH:18][cH:19][c:20]1[CH:21]([Cl:22])[Cl:23]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[n:6][c:7]([NH:8][C:9](=[O:10])[NH:11][S:12](=[O:13])(=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[CH:21]([Cl...
Cc1cc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(Cl)Cl
Cc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(Cl)Cl)n1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;D1;H0:7]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[#16:10](=[O;D1;H0:11])(=[O;D1;H0:12])-[c:13]>>[O;D1;H0:7]=[C;H0;D3;+0:8](-[NH;D2;+0:9]-[#16:10](=[O;D1;H0:11])(=[O;D1;H0:12])-[c:13])-[NH;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
18
HOUR
2-(Dichloromethyl)benzenesulfonyl isocyanate, prepared from 10 mmol of sulfonamide as described in the synthesis of Example 1, was treated with acetonitrile and 2-amino-4,6-dimethylpyrimidine (1.23 g). The mixture was stirred at room temperature for 18 hrs, cooled, and filtered to provide 1.08 g of white solid, mp 195°...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1cncnc1.c1ccccc1
null
C(C)#N
null
18
Cc1cc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(Cl)Cl>C(C)#N>Cc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(Cl)Cl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a13c037be7c241d6a705a7e8083f6b1a
COc1nc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(Cl)Cl>>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(Cl)Cl)n1
NC1=NC(=NC(=N1)OC)C.ClC(C1=C(C=CC=C1)S(=O)(=O)N=C=O)Cl>>ClC(C1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=NC(=N1)OC)C)Cl
[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH2:9])[n:25]1.[C:10](=[O:11])=[N:12][S:13](=[O:14])(=[O:15])[c:16]1[cH:17][cH:18][cH:19][cH:20][c:21]1[CH:22]([Cl:23])[Cl:24]>>[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][S:13](=[O:14])(=[O:15])[c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[...
COc1nc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(Cl)Cl
COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(Cl)Cl)n1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[C;H0;D2;+0:9]=[N;H0;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14]>>[O;D1;H0:8]=[C;H0;D3;+0:9](-[NH;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1
null
[]
null
null
18
HOUR
2-(Dichloromethyl)benzenesulfonyl isocyanate prepared from 10 mmol of sulfonamide as described in the synthesis of Example 1, was treated with acetonitrile (15 ml) and 2-amino-4-methoxy-6-methyl-1,3,5-triazine (1.40 g). The mixture was stirred for 18 hrs. and filtered. The filtrate was evaporated and recrystallized fro...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ncncn1.c1ccccc1
null
C(C)#N
null
18
COc1nc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(Cl)Cl>C(C)#N>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(Cl)Cl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e3f81eb409d2431c8e14cd850aef493f
CO.C[O-].NS(=O)(=O)c1ccccc1CCl.O=C=Nc1nc(Cl)nc(Cl)n1>>COc1nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)nc(OC)n1
O.C[O-].[Na+].CO.ClC1=NC(=NC(=N1)Cl)N=C=O.ClCC1=C(C=CC=C1)S(=O)(=O)N>>ClCC1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=NC(=N1)OC)OC
[CH3:1][OH:2].[O-:23][CH3:24].[NH2:9][S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]1[CH2:19][Cl:20].Cl[c:3]1[n:4][c:5]([N:6]=[C:7]=[O:8])[n:21][c:22](Cl)[n:25]1>>[CH3:1][O:2][c:3]1[n:4][c:5]([NH:6][C:7](=[O:8])[NH:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[CH2:19][Cl:20])[n:...
CO.C[O-].NS(=O)(=O)c1ccccc1CCl.O=C=Nc1nc(Cl)nc(Cl)n1
COc1nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)nc(OC)n1
null
null
C(C)#N
Acylation
OtherReaction
5cdd877a8ea4ad7f77e0b58a5aa98d7b3adfbfbb456325612b5171f9a3531a5c
e436601634444b82a56ec7862cb8244a75bca7f9b265f2a0e3614cb21c0195bb
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[N;H0;D2;+0:4]=[C;H0;D2;+0:5]=[O;D1;H0:6]):[#7;a:7]:[c;H0;D3;+0:8](-Cl):[#7;a:9]:1.[C;D1;H3:10]-[O-;H0;D1:11].[C;D1;H3:12]-[OH;D1;+0:13].[NH2;D1;+0:14]-[#16:15](=[O;D1;H0:16])(=[O;D1;H0:17])-[c:18]>>[C;D1;H3:12]-[O;H0;D2;+0:13]-[c;H0;D3;+0:8]1:[#7;a:9]:[c;H0;D3;+0:1](-[O;H0;D2;+0:11]-...
null
[]
null
null
20
HOUR
A solution of 4,6-dichloro-1,3,5-triazin-2-yl isocyanate (3.10 g, 16.2 mmol) in acetonitrile (15 ml) was contacted with 2-(chloromethyl)benzene sulfonamide (3.34 g, 16.2 mmol) and stirred for 20 hrs at 25°. The mixture was heated at 50° for 2 hrs, cooled and filtered to provide 3.86 g, mp 162°-170°, which was contacted...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Aromatic halide.Aromatic halide.Isocyanate.Methanol
Sulfonamide.Ether.Ether.Urea
c1ncncn1
c1ncncn1
c1ncncn1.c1ccccc1
HCl
C(C)#N
null
20
CO.C[O-].NS(=O)(=O)c1ccccc1CCl.O=C=Nc1nc(Cl)nc(Cl)n1>C(C)#N>COc1nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)nc(OC)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7101f12d796b4a7697ca6546a96de61b
COc1cc(OC)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1CCl>>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)n1
S(=O)(=O)(N=C=O)N=C=O.ClCC1=C(C=CC=C1)S(=O)(=O)N=C=O.C(=O)(Cl)Cl.NC1=NC(=CC(=N1)OC)OC.ClCC1=C(C=CC=C1)S(=O)(=O)NC(=O)NCCCC>>ClCC1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=CC(=N1)OC)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[n:8][c:9]([NH2:10])[n:25]1.[C:11](=[O:12])=[N:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[CH2:23][Cl:24]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][S:14](=[O:15])(=[O:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c...
COc1cc(OC)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1CCl
COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)n1
null
N12NCC(CC1)CC2
C(C)#N.C=1(C(=CC=CC1)C)C
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;D1;H0:7]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[#16:10](=[O;D1;H0:11])(=[O;D1;H0:12])-[c:13]>>[O;D1;H0:7]=[C;H0;D3;+0:8](-[NH;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6])-[NH;D2;+0:9]-[#16:10](=[O;D1;H0:11])(=[O;D1;H0:12])-[c:13]
69.6
[{"value": 69.6, "product": "ClCC1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=CC(=N1)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A solution of 2-(chloromethyl)-N-(butylaminocarbonyl)benzene sulfonamide (1.33 g, 4.38 mmol) and diazabicyclo[2.2.2]octane (5 mg) in xylene (12 ml) was heated at reflux and contacted in portions with phosgene (1.0 ml. condensed phase). After 2.0 hrs at reflux, the mixture was cooled to room temperature, decanted, and v...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1cncnc1.c1ccccc1
null
N12NCC(CC1)CC2.C(C)#N.C=1(C(=CC=CC1)C)C
null
16
COc1cc(OC)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1CCl>N12NCC(CC1)CC2.C(C)#N.C=1(C(=CC=CC1)C)C>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-849b814f85c74b4ea52ba55f26ec47fb
C1CCNC1.COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)n1>>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CN2CCCC2)n1.Cl
ClCC1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=CC(=N1)OC)OC.N1CCCC1.[K+].[Br-]>>Cl.N1(CCCC1)CC1=C(C=CC=C1)S(=O)(=O)NC(=O)NC1=NC(=CC(=N1)OC)OC
[NH:24]1[CH2:25][CH2:26][CH2:27][CH2:28]1.[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][S:14](=[O:15])(=[O:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[CH2:23][Cl:30])[n:29]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][S:14](=[O:15])(=[O:1...
C1CCNC1.COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)n1
COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CN2CCCC2)n1.Cl
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
19b442dc26882f89f7423416f5e0a16bdb8e48776df57991434a0634e21f0505
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1CN1CCCC1
[C:1]1-[C:2]-[C:3]-[C:4]-[NH;D2;+0:5]-1.[Cl;H0;D1;+0:6]-[CH2;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[ClH;D0;+0:6].[c:9]:[c:8](-[CH2;D2;+0:7]-[N;H0;D3;+0:5]1-[C:1]-[C:2]-[C:3]-[C:4]-1):[c:10]
null
[]
null
null
3.5
HOUR
A slurry of 2-(chloromethyl)-N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]benzenesulfonamide (1.00 g) in dimethylformamide (5 ml) was contacted with pyrrolidine (0.45 ml) and stirred for 3.5 hrs. Volatiles were removed under vacuum and the residue was taken up in methanol. Solvent was removed and the water (15 ml) was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNC1
C1CC[NH]C1
c1cncnc1.c1ccccc1.C1CC[NH]C1
null
CN(C=O)C
null
3.5
C1CCNC1.COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CCl)n1>CN(C=O)C>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2ccccc2CN2CCCC2)n1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5a26a82ee29e4183bd849568dc3c6a8f
CCc1ccccc1S(=O)(=O)Cl.ClOCl>>CC(Cl)c1ccccc1S(=O)(=O)Cl
C(C)C1=C(C=CC=C1)S(=O)(=O)Cl.O(Cl)Cl>>ClC(C)C1=C(C=CC=C1)S(=O)(=O)Cl
[CH3:1][CH2:2][c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[S:10](=[O:11])(=[O:12])[Cl:13].ClO[Cl:3]>>[CH3:1][CH:2]([Cl:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[S:10](=[O:11])(=[O:12])[Cl:13]
CCc1ccccc1S(=O)(=O)Cl.ClOCl
CC(Cl)c1ccccc1S(=O)(=O)Cl
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Chlorination
fb976bf1eab8c62577a847af299a41a3ccb21dd6033b1d12da0fc75ebe4f95a0
0c353a1260488c22c3ffb72de5623420c3ec35470a0b3a2045b11c29224f458e
c1ccccc1
Cl-O-[Cl;H0;D1;+0:1].[C;D1;H3:2]-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6]>>[C;D1;H3:2]-[CH;D3;+0:3](-[Cl;H0;D1;+0:1])-[c:4](:[c:5]):[c:6]
83.9
[{"value": 83.9, "product": "ClC(C)C1=C(C=CC=C1)S(=O)(=O)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-ethylbenzenesulfonyl chloride (obtained by chlorosulfonation of ethylbenzene) (7.78 g) in carbon tetrachloride (5.0 ml) was contacted with a solution of dichlorine monoxide (82 mmol) in carbon tetrachloride (100 ml) and the mixture was heated in a closed system at 50°-60° for 16 hrs. The mixture was dri...
10.6084/m9.figshare.5104873.v1
null
null
Secondary halide
null
null
c1ccccc1
HCl
C(Cl)(Cl)(Cl)Cl
null
null
CCc1ccccc1S(=O)(=O)Cl.ClOCl>C(Cl)(Cl)(Cl)Cl>CC(Cl)c1ccccc1S(=O)(=O)Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-27141d7cdd0949518f09952f7124156b
N.O=S(=O)(Cl)c1ccccc1CCl>>NS(=O)(=O)c1ccccc1CCl
N.ClCC1=C(C=CC=C1)S(=O)(=O)Cl>>ClCC1=C(C=CC=C1)S(=O)(=O)N
[NH3:1].Cl[S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[CH2:11][Cl:12]>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[CH2:11][Cl:12]
N.O=S(=O)(Cl)c1ccccc1CCl
NS(=O)(=O)c1ccccc1CCl
null
null
O1CCCC1
Miscellaneous
OtherReaction
419151dfc49d0719bc8d3fc5b23cdd08248d27df18761ee59c11624194c4c5ab
ae33b93faeb632e8ec1263862cc7a6f628747ed893339f281ddf88c6e380b60a
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[NH3;D0;+0:7]>>[NH2;D1;+0:7]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
A solution of ammonia (5.2 ml) in tetrahydrofuran (250 ml) at -70° was contacted rapidly with a solution of 2-(chloromethyl)benzenesulfonyl chloride (21.8 g) in tetrahydrofuran (125 ml). The stirred mixture was allowed to warm to 0° and volatiles were removed under vacuum. The residue was contacted with ethyl acetate a...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonamide
null
null
c1ccccc1
HCl
O1CCCC1
null
null
N.O=S(=O)(Cl)c1ccccc1CCl>O1CCCC1>NS(=O)(=O)c1ccccc1CCl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-81369e951b824169a8227c813fb01c19
CC(Cl)c1ccccc1S(=O)(=O)Cl.N>>CC(Cl)c1ccccc1S(N)(=O)=O
N.ClC(C)C1=C(C=CC=C1)S(=O)(=O)Cl>>ClC(C)C1=C(C=CC=C1)S(=O)(=O)N
Cl[S:10]([c:9]1[c:4]([CH:2]([CH3:1])[Cl:3])[cH:5][cH:6][cH:7][cH:8]1)(=[O:12])=[O:13].[NH3:11]>>[CH3:1][CH:2]([Cl:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[S:10]([NH2:11])(=[O:12])=[O:13]
CC(Cl)c1ccccc1S(=O)(=O)Cl.N
CC(Cl)c1ccccc1S(N)(=O)=O
null
null
O1CCCC1
Miscellaneous
OtherReaction
419151dfc49d0719bc8d3fc5b23cdd08248d27df18761ee59c11624194c4c5ab
ae33b93faeb632e8ec1263862cc7a6f628747ed893339f281ddf88c6e380b60a
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[NH3;D0;+0:7]>>[NH2;D1;+0:7]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
A solution of ammonia (1.2 ml) in tetrahydrofuran (100 ml) at -70° was contacted rapidly with a solution of 2-(1-chloroethyl)benzenesulfonyl chloride (4.32 g, 18.1 mmol) in tetrahydrofuran (50 ml). The stirred mixture was allowed to warm to 0° and volatiles were removed under reduced pressure. The residue was taken up ...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonamide
null
null
c1ccccc1
HCl
O1CCCC1
null
null
CC(Cl)c1ccccc1S(=O)(=O)Cl.N>O1CCCC1>CC(Cl)c1ccccc1S(N)(=O)=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e0b6a4d4050747dd9fd78e33c2ece435
N.O=S(=O)(Cl)c1ccccc1CBr>>NS(=O)(=O)c1ccccc1CBr
N.BrCC1=C(C=CC=C1)S(=O)(=O)Cl.BrCC1=CC=C(C=C1)S(=O)(=O)Cl>>BrCC1=C(C=CC=C1)S(=O)(=O)N
[NH3:1].Cl[S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[CH2:11][Br:12]>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[CH2:11][Br:12]
N.O=S(=O)(Cl)c1ccccc1CBr
NS(=O)(=O)c1ccccc1CBr
null
null
O1CCCC1
Miscellaneous
OtherReaction
419151dfc49d0719bc8d3fc5b23cdd08248d27df18761ee59c11624194c4c5ab
ae33b93faeb632e8ec1263862cc7a6f628747ed893339f281ddf88c6e380b60a
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[NH3;D0;+0:7]>>[NH2;D1;+0:7]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
A solution of ammonia (1.0 ml) in tetrahydrofuran (50 ml) at -78° was contacted dropwise with a solution of a 60/40 mixture of 2-(bromomethyl)benzenesulfonyl chloride/4-(bromomethyl)benzenesulfonyl chloride (4.52 g) in tetrahydrofuran (20 ml). The stirred mixture was allowed to warm to 0° and volatiles were removed in ...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonamide
null
null
c1ccccc1
HCl
O1CCCC1
null
null
N.O=S(=O)(Cl)c1ccccc1CBr>O1CCCC1>NS(=O)(=O)c1ccccc1CBr
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-eab0fe71e0cc43c3893df4095261d255
C1CCNC1.NS(=O)(=O)c1ccccc1CCl>>NS(=O)(=O)c1ccccc1CN1CCCC1
ClCC1=C(C=CC=C1)S(=O)(=O)N.N1CCCC1>>N1(CCCC1)CC1=C(C=CC=C1)S(=O)(=O)N
[NH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1.Cl[CH2:11][c:10]1[c:5]([S:2]([NH2:1])(=[O:3])=[O:4])[cH:6][cH:7][cH:8][cH:9]1>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[CH2:11][N:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1
C1CCNC1.NS(=O)(=O)c1ccccc1CCl
NS(=O)(=O)c1ccccc1CN1CCCC1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
19b442dc26882f89f7423416f5e0a16bdb8e48776df57991434a0634e21f0505
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(CN2CCCC2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]1-[C:6]-[C:7]-[C:8]-[NH;D2;+0:9]-1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:9]1-[C:5]-[C:6]-[C:7]-[C:8]-1):[c:4]
92.8
[{"value": 92.8, "product": "N1(CCCC1)CC1=C(C=CC=C1)S(=O)(=O)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 2-(chloromethyl)benzenesulfonamide (2.00 g, 10 mmol) in acetonitrile (20 ml) was contacted with pyrrolidine (1.6 ml, 20 mmol). After 1.0 hr at ambient temperature, the volatiles were removed under vacuum and the residue was treated with water (40 ml) and chilled. The resulting solid was pulverized, filter...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CCNC1
C1CC[NH]C1
c1ccccc1.C1CC[NH]C1
HCl
C(C)#N
null
1
C1CCNC1.NS(=O)(=O)c1ccccc1CCl>C(C)#N>NS(=O)(=O)c1ccccc1CN1CCCC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a1d6ecf5affe4cdc9339c195051b4e6a
CI.NS(=O)(=O)c1ccccc1CN1CCCC1>>CNS(=O)(=O)c1ccccc1CN1CCCC1.[I-]
N1(CCCC1)CC1=C(C=CC=C1)S(=O)(=O)N.CI>>[I-].N1(CCCC1)CC1=C(C=CC=C1)S(=O)(=O)NC
[CH3:1][I:18].[NH2:2][S:3](=[O:4])(=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[CH2:12][N:13]1[CH2:14][CH2:15][CH2:16][CH2:17]1>>[CH3:1][NH:2][S:3](=[O:4])(=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[CH2:12][N:13]1[CH2:14][CH2:15][CH2:16][CH2:17]1.[I-:18]
CI.NS(=O)(=O)c1ccccc1CN1CCCC1
CNS(=O)(=O)c1ccccc1CN1CCCC1.[I-]
null
null
C(C)#N
Functional Group Addition
N-alkylation of primary amines with alkyl halides
976de1015d989c0c5f36a699555d436cf203ed2f06f91b0acbfa101a293d3eeb
6a5d85c8f0ea70e5fce45998d00e869aa529bdae85ab86c721877b1dc53f883d
c1ccc(CN2CCCC2)cc1
[CH3;D1;+0:1]-[I;H0;D1;+0:2].[NH2;D1;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]>>[CH3;D1;+0:1]-[NH;D2;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7].[I-;H0;D0:2]
null
[]
null
null
null
null
A solution of 2-(pyrrolidinomethyl)benzenesulfonamide (0.8 g) in acetonitrile (10 ml) was contacted with methyl iodide (3 ml) and heated to reflux for 2.0 hrs. Solvent was removed and the residue was treated with acetone and ether. The solid was filtered, digested with acetone (20 ml), chilled and collected. There was ...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Sulfonamide
null
null
c1ccccc1.C1CC[NH]C1
null
C(C)#N
null
null
CI.NS(=O)(=O)c1ccccc1CN1CCCC1>C(C)#N>CNS(=O)(=O)c1ccccc1CN1CCCC1.[I-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-96b36f56b2bf4e2fa59c2f023ae48e35
CCCCN=C=O.NS(=O)(=O)c1ccccc1CCl>>CCCCNC(=O)NS(=O)(=O)c1ccccc1CCl
ClCC1=C(C=CC=C1)S(=O)(=O)N.C(CCC)N=C=O>>ClCC1=C(C=CC=C1)S(=O)(=O)NC(=O)NCCCC
[CH3:1][CH2:2][CH2:3][CH2:4][N:5]=[C:6]=[O:7].[NH2:8][S:9](=[O:10])(=[O:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[CH2:18][Cl:19]>>[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][C:6](=[O:7])[NH:8][S:9](=[O:10])(=[O:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[CH2:18][Cl:19]
CCCCN=C=O.NS(=O)(=O)c1ccccc1CCl
CCCCNC(=O)NS(=O)(=O)c1ccccc1CCl
null
N12NCC(CC1)CC2
C=1(C(=CC=CC1)C)C
Acylation
OtherReaction
5e91197373c0e9b04f4abef28663b2a5340491c55a6757f9a5f8cf7ca2e4aefe
0fe1082098d61e5130a83440c9351817ede5cdd433bfc65ee308ef6fab351022
c1ccccc1
[C:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[NH2;D1;+0:6]-[#16:7](=[O;D1;H0:8])(=[O;D1;H0:9])-[c:10]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[#16:7](=[O;D1;H0:8])(=[O;D1;H0:9])-[c:10]
74.8
[{"value": 74.8, "product": "ClCC1=C(C=CC=C1)S(=O)(=O)NC(=O)NCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-(chloromethyl)benzenesulfonamide (13.2 g, 64 mmol) and butyl isocyanate (7.0 g, 71 mmol) in xylene (80 ml) was contacted with diazabicyclo[2.2.2]octane (0.25 g) and heated to reflux for 5.0 hrs. Volatiles were removed under vacuum and the residue was treated with 0.5N NaOH (200 ml) and extracted with eth...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Isocyanate
Sulfonamide.Urea
null
null
c1ccccc1
null
N12NCC(CC1)CC2.C=1(C(=CC=CC1)C)C
null
null
CCCCN=C=O.NS(=O)(=O)c1ccccc1CCl>N12NCC(CC1)CC2.C=1(C(=CC=CC1)C)C>CCCCNC(=O)NS(=O)(=O)c1ccccc1CCl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d41592ac9b864e5fa8d5045e4e4bc7fb
C=CCc1cc(C)c(OCC2CO2)c(C)c1.CC(=O)OO>>Cc1cc(CC2CO2)cc(C)c1OCC1CO1
C(C1CO1)OC1=C(C=C(C=C1C)CC=C)C.C(C)(=O)[O-].[Na+].C(C)(=O)OO>>C(C1CO1)OC1=C(C=C(C=C1C)CC1CO1)C
[CH3:1][c:2]1[cH:3][c:4]([CH2:5][CH:6]=[CH2:7])[cH:9][c:10]([CH3:11])[c:12]1[O:13][CH2:14][CH:15]1[CH2:16][O:17]1.CC(=O)O[OH:8]>>[CH3:1][c:2]1[cH:3][c:4]([CH2:5][CH:6]2[CH2:7][O:8]2)[cH:9][c:10]([CH3:11])[c:12]1[O:13][CH2:14][CH:15]1[CH2:16][O:17]1
C=CCc1cc(C)c(OCC2CO2)c(C)c1.CC(=O)OO
Cc1cc(CC2CO2)cc(C)c1OCC1CO1
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
173f96f965e916bc74678202d36f5d0142af5230a7d483e540b63ebc1e6f47ae
cf4df6d170df9662664f9744161f06baeb1f4777cb3701fb34820ed0286c62f4
c1cc(OCC2CO2)ccc1CC1CO1
C-C(=O)-O-[OH;D1;+0:1].[CH2;D1;+0:2]=[CH;D2;+0:3]-[C:4]-[c:5]>>[c:5]-[C:4]-[CH;D3;+0:3]1-[CH2;D2;+0:2]-[O;H0;D2;+0:1]-1
863.5
[{"value": 863.5, "product": "C(C1CO1)OC1=C(C=C(C=C1C)CC1CO1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A 350 ml sulfurating flask equipped with thermometer, stirrer, cooler and drip funnel is charged with 46.30 g (0.21 mole) of 4-allyl-2,6-dimethylphenyl glycidyl ether, 1.93 g of sodium acetate and 160 ml of chloroform, and the batch is heated to 35°-40° C. At this temperature, 52.3 g (0.28 mole) of 40% peracetic acid a...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Allyl
Ether
null
C1CO1
c1ccccc1.C1CO1.C1CO1
HO-
C(Cl)(Cl)Cl
null
4
C=CCc1cc(C)c(OCC2CO2)c(C)c1.CC(=O)OO>C(Cl)(Cl)Cl>Cc1cc(CC2CO2)cc(C)c1OCC1CO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2a2a0d78cbcc499984b40bbe74b117a2
C=CCc1cc(C)c(OCC2CO2)c(C)c1.OO>>Cc1cc(CC2CO2)cc(C)c1OCC1CO1
C(C1CO1)OC1=C(C=C(C=C1C)CC=C)C.C(=O)O.OO>>C(C1CO1)OC1=C(C=C(C=C1C)CC1CO1)C
[CH3:1][c:2]1[cH:3][c:4]([CH2:5][CH:6]=[CH2:7])[cH:9][c:10]([CH3:11])[c:12]1[O:13][CH2:14][CH:15]1[CH2:16][O:17]1.O[OH:8]>>[CH3:1][c:2]1[cH:3][c:4]([CH2:5][CH:6]2[CH2:7][O:8]2)[cH:9][c:10]([CH3:11])[c:12]1[O:13][CH2:14][CH:15]1[CH2:16][O:17]1
C=CCc1cc(C)c(OCC2CO2)c(C)c1.OO
Cc1cc(CC2CO2)cc(C)c1OCC1CO1
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
173f96f965e916bc74678202d36f5d0142af5230a7d483e540b63ebc1e6f47ae
cf4df6d170df9662664f9744161f06baeb1f4777cb3701fb34820ed0286c62f4
c1cc(OCC2CO2)ccc1CC1CO1
O-[OH;D1;+0:1].[CH2;D1;+0:2]=[CH;D2;+0:3]-[C:4]-[c:5]>>[c:5]-[C:4]-[CH;D3;+0:3]1-[CH2;D2;+0:2]-[O;H0;D2;+0:1]-1
85.5
[{"value": 80.5, "product": "C(C1CO1)OC1=C(C=C(C=C1C)CC1CO1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.5, "product": "C(C1CO1)OC1=C(C=C(C=C1C)CC1CO1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 350 ml sulfurating flask equipped with thermometer, stirrer, cooler and drip funnel is charged with 21.8 g (0.10 mole) of 4-allyl-2,6-dimethylphenyl glycidyl ether, 10.9 g (0.24 mole) of formic acid and 135 ml of chloroform. At room temperature, 23.2 g (0.47 mole) of hydrogen peroxide are then added dropise over 4 ho...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Allyl
Ether
null
C1CO1
c1ccccc1.C1CO1.C1CO1
HO-
C(Cl)(Cl)Cl
null
null
C=CCc1cc(C)c(OCC2CO2)c(C)c1.OO>C(Cl)(Cl)Cl>Cc1cc(CC2CO2)cc(C)c1OCC1CO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-652355d8c729482398cb6fea03dd1456
C=CCc1cc(Cl)c(OCC2CO2)c(Cl)c1.CC(=O)OO>>Clc1cc(CC2CO2)cc(Cl)c1OCC1CO1
C(C1CO1)OC1=C(C=C(C=C1Cl)CC=C)Cl.C(C)(=O)OO>>C(C1CO1)OC1=C(C=C(C=C1Cl)CC1CO1)Cl
[Cl:1][c:2]1[cH:3][c:4]([CH2:5][CH:6]=[CH2:7])[cH:9][c:10]([Cl:11])[c:12]1[O:13][CH2:14][CH:15]1[CH2:16][O:17]1.CC(=O)O[OH:8]>>[Cl:1][c:2]1[cH:3][c:4]([CH2:5][CH:6]2[CH2:7][O:8]2)[cH:9][c:10]([Cl:11])[c:12]1[O:13][CH2:14][CH:15]1[CH2:16][O:17]1
C=CCc1cc(Cl)c(OCC2CO2)c(Cl)c1.CC(=O)OO
Clc1cc(CC2CO2)cc(Cl)c1OCC1CO1
null
null
C1(=CC=CC=C1)C.C(C)(=O)[O-].[Na+]
Heteroatom Alkylation and Arylation
OtherReaction
173f96f965e916bc74678202d36f5d0142af5230a7d483e540b63ebc1e6f47ae
cf4df6d170df9662664f9744161f06baeb1f4777cb3701fb34820ed0286c62f4
c1cc(OCC2CO2)ccc1CC1CO1
C-C(=O)-O-[OH;D1;+0:1].[CH2;D1;+0:2]=[CH;D2;+0:3]-[C:4]-[c:5]>>[c:5]-[C:4]-[CH;D3;+0:3]1-[CH2;D2;+0:2]-[O;H0;D2;+0:1]-1
92.3
[{"value": 92.3, "product": "C(C1CO1)OC1=C(C=C(C=C1Cl)CC1CO1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.3, "product": "C(C1CO1)OC1=C(C=C(C=C1Cl)CC1CO1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A 100 ml sulfurating flask equipped with stirrer, cooler, thermometer and drip funnel is charged with 13.0 g (0.05 mole) of 4-allyl-2,6-dichlorophenyl glycidyl ether in 40 ml of toluene and 0.5 g of sodium acetate. Over 2 hours, 14.0 g (0.07 mole) of 10% peracetic acid are then added dropwise at 30°-50° C. After the dr...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Allyl
Ether
null
C1CO1
c1ccccc1.C1CO1.C1CO1
HO-
C1(=CC=CC=C1)C.C(C)(=O)[O-].[Na+]
null
2
C=CCc1cc(Cl)c(OCC2CO2)c(Cl)c1.CC(=O)OO>C1(=CC=CC=C1)C.C(C)(=O)[O-].[Na+]>Clc1cc(CC2CO2)cc(Cl)c1OCC1CO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a11e6358c0444cb68a62cdc6256a2d8a
C=CCc1cc(-c2ccccc2)c(OCC2CO2)c(-c2ccccc2)c1.CC(=O)OO>>c1ccc(-c2cc(CC3CO3)cc(-c3ccccc3)c2OCC2CO2)cc1
C(C1CO1)OC1=C(C=C(C=C1C1=CC=CC=C1)CC=C)C1=CC=CC=C1.C(C)(=O)OO>>C(C1CO1)OC1=C(C=C(C=C1C1=CC=CC=C1)CC1CO1)C1=CC=CC=C1
[cH:1]1[cH:2][cH:3][c:4](-[c:5]2[cH:6][c:7]([CH2:8][CH:9]=[CH2:10])[cH:12][c:13](-[c:14]3[cH:15][cH:16][cH:17][cH:18][cH:19]3)[c:20]2[O:21][CH2:22][CH:23]2[CH2:24][O:25]2)[cH:26][cH:27]1.CC(=O)O[OH:11]>>[cH:1]1[cH:2][cH:3][c:4](-[c:5]2[cH:6][c:7]([CH2:8][CH:9]3[CH2:10][O:11]3)[cH:12][c:13](-[c:14]3[cH:15][cH:16][cH:17]...
C=CCc1cc(-c2ccccc2)c(OCC2CO2)c(-c2ccccc2)c1.CC(=O)OO
c1ccc(-c2cc(CC3CO3)cc(-c3ccccc3)c2OCC2CO2)cc1
null
null
C1(=CC=CC=C1)C.C(C)(=O)[O-].[Na+]
Heteroatom Alkylation and Arylation
OtherReaction
173f96f965e916bc74678202d36f5d0142af5230a7d483e540b63ebc1e6f47ae
cf4df6d170df9662664f9744161f06baeb1f4777cb3701fb34820ed0286c62f4
c1ccc(-c2cc(CC3CO3)cc(-c3ccccc3)c2OCC2CO2)cc1
C-C(=O)-O-[OH;D1;+0:1].[CH2;D1;+0:2]=[CH;D2;+0:3]-[C:4]-[c:5]>>[c:5]-[C:4]-[CH;D3;+0:3]1-[CH2;D2;+0:2]-[O;H0;D2;+0:1]-1
86.9
[{"value": 86.5, "product": "C(C1CO1)OC1=C(C=C(C=C1C1=CC=CC=C1)CC1CO1)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.9, "product": "C(C1CO1)OC1=C(C=C(C=C1C1=CC=CC=C1)CC1CO1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A 100 ml sulfurating flask equipped with stirrer, cooler, thermometer and drip funnel is charged with 13.7 g (0.04 mole) of 4-allyl-2,6-diphenylphenyl glycidyl ether in 20 ml of toluene and 0.7 g of sodium acetate. Over 2 hours, 9.13 g (0.048 mole) of 40% peracetic acid are added at a temperature in the range from 30° ...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Allyl
Ether
null
C1CO1
c1ccccc1.c1ccccc1.C1CO1.c1ccccc1.C1CO1
HO-
C1(=CC=CC=C1)C.C(C)(=O)[O-].[Na+]
null
2
C=CCc1cc(-c2ccccc2)c(OCC2CO2)c(-c2ccccc2)c1.CC(=O)OO>C1(=CC=CC=C1)C.C(C)(=O)[O-].[Na+]>c1ccc(-c2cc(CC3CO3)cc(-c3ccccc3)c2OCC2CO2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-72f2082343ba44e69fe8adf60a87217c
CCOc1ccc(C(=O)O)c(O)c1.CO>>CCOc1ccc(C(=O)OC)c(O)c1
Cl.C(C)OC1=CC(=C(C(=O)O)C=C1)O.CO>>C(C)OC1=CC(=C(C(=O)OC)C=C1)O
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[OH:10])[c:12]([OH:13])[cH:14]1.O[CH3:11]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[O:10][CH3:11])[c:12]([OH:13])[cH:14]1
CCOc1ccc(C(=O)O)c(O)c1.CO
CCOc1ccc(C(=O)OC)c(O)c1
null
null
null
Heteroatom Alkylation and Arylation
Esterification of Carboxylic Acids
961bfcd5802efbb4a2d5a1e38cbfb6654b5b78f769c3570df49b858a6f105ab6
0a622556a49b258b9020bd3a5bdd1fa9237e7093cf9b09de3a6b575ffe935dcd
c1ccccc1
O-[CH3;D1;+0:1].[O;D1;H0:2]=[C:3](-[OH;D1;+0:4])-[c:5]>>[CH3;D1;+0:1]-[O;H0;D2;+0:4]-[C:3](=[O;D1;H0:2])-[c:5]
null
[]
15
CELSIUS
null
null
Hydrogen chloride was bubbled into a stirred solution of 4-ethoxy-2-hydroxybenzoic acid (10.10 g, 0.554 mol) in methanol (2000 mL) until the solution was saturated. The solution was heated under reflux for 3 days and then cooled to 15° C. This caused the product to crystallize out. The crystals were collected, rinsed w...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
null
15
null
CCOc1ccc(C(=O)O)c(O)c1.CO>>CCOc1ccc(C(=O)OC)c(O)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f3c65c892c17444ab3d7195abd66c222
CCOc1ccc(C(=O)OC)c(SC(=O)N(C)C)c1>>CCOc1ccc(C(=O)OC)c(S)c1
C[O-].[Na+].CN(C(=O)SC1=C(C(=O)OC)C=CC(=C1)OCC)C>>C(C)OC1=CC(=C(C(=O)OC)C=C1)S
CN(C)C(=O)[S:13][c:12]1[c:7]([C:8](=[O:9])[O:10][CH3:11])[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[cH:14]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[O:10][CH3:11])[c:12]([SH:13])[cH:14]1
CCOc1ccc(C(=O)OC)c(SC(=O)N(C)C)c1
CCOc1ccc(C(=O)OC)c(S)c1
null
null
CO
Reduction
OtherReaction
b8de7c0dd998c42f71fbae789bd47547a8833f1078d4106e4c6eaba466ea8b96
616235514d65b822291e24d80df126c1e4bd115c2e4fc6cf16de0cb196278e81
c1ccccc1
C-N(-C)-C(=O)-[S;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](-[#8:6])=[O;D1;H0:7]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]:[c:2](-[SH;D1;+0:1]):[c:3]
86.7
[{"value": 86.7, "product": "C(C)OC1=CC(=C(C(=O)OC)C=C1)S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Methanolic sodium methoxide (4.9M, 22.4 mL, 0.11 mol) was added via syringe to a solution of methyl 2-[(dimethylamino)carbonylthio]-4-ethoxybenzoate (crude, ca. 28.3 g, 0.10 mol) in methanol (100 mL) under nitrogen. The reaction mixture was heated at reflux for 30 minutes, then cooled with the aid of a water bath. Rota...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide
Aromatic thiol
null
null
c1ccccc1
HO-
CO
null
null
CCOc1ccc(C(=O)OC)c(SC(=O)N(C)C)c1>CO>CCOc1ccc(C(=O)OC)c(S)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5b7d4e41ceb24f3f9e9e577756bacd06
CCOc1ccc(C(=O)OC)c(S(=O)(=O)Cl)c1.N>>CCOc1ccc(C(=O)OC)c(S(N)(=O)=O)c1
O.N.ClS(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)OCC.O>>NS(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)OCC
Cl[S:13]([c:12]1[c:7]([C:8](=[O:9])[O:10][CH3:11])[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[cH:17]1)(=[O:15])=[O:16].[NH3:14]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[O:10][CH3:11])[c:12]([S:13]([NH2:14])(=[O:15])=[O:16])[cH:17]1
CCOc1ccc(C(=O)OC)c(S(=O)(=O)Cl)c1.N
CCOc1ccc(C(=O)OC)c(S(N)(=O)=O)c1
null
null
ClCCl
Acylation
OtherReaction
672a14b4f1ef0b966898e1b4c118f241f21df1d6e087372155b9d0c840dac61f
29e1633db8f1f00444181a0bcac91d574ed806fddf9165be4c8478fc32a80994
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]-[C:7](-[#8:8])=[O;D1;H0:9].[NH3;D0;+0:10]>>[#8:8]-[C:7](=[O;D1;H0:9])-[c:6]:[c:4](-[S;H0;D4;+0:1](-[NH2;D1;+0:10])(=[O;D1;H0:2])=[O;D1;H0:3]):[c:5]
74.4
[{"value": 74.4, "product": "NS(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-10
CELSIUS
30
MINUTE
Liquified ammonia (4.4 mL, 180 mmol) was added to a stirred solution of methyl 2-(chlorosulfonyl)-4-ethoxybenzoate (22.1 g, 79.3 mmol) in dichloromethane (221 mL) at -70° C. The reaction mixture was allowed to warm to -10° C. and was held at this temperature for 30 minutes. The mixture was then poured into water (221 m...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonamide
null
null
c1ccccc1
HCl
ClCCl
-10
0.5
CCOc1ccc(C(=O)OC)c(S(=O)(=O)Cl)c1.N>ClCCl>CCOc1ccc(C(=O)OC)c(S(N)(=O)=O)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-afb1397756f348c8aace29697e67d299
CCCCN=C=O.CCOc1ccc(C(=O)OC)c(S(N)(=O)=O)c1>>CCOc1ccc(C(=O)OC)c(S(=O)(=O)N=C=O)c1
C(=O)(Cl)Cl.NS(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)OCC.C(CCC)N=C=O>>C(C)OC1=CC(=C(C(=O)OC)C=C1)S(=O)(=O)N=C=O
CCCCN=[C:17]=[O:18].[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[O:10][CH3:11])[c:12]([S:13](=[O:14])(=[O:15])[NH2:16])[cH:19]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[O:10][CH3:11])[c:12]([S:13](=[O:14])(=[O:15])[N:16]=[C:17]=[O:18])[cH:19]1
CCCCN=C=O.CCOc1ccc(C(=O)OC)c(S(N)(=O)=O)c1
CCOc1ccc(C(=O)OC)c(S(=O)(=O)N=C=O)c1
null
null
null
Functional Group Interconversion
OtherReaction
d6c69f89b87c5c421a628563544ee2b8b0164ec4561bcd29a2cbba0dce4075ac
5df9e857f75ada60baf9e936007533a18389016451154bd1ed26e91b5babd844
c1ccccc1
C-C-C-C-N=[C;H0;D2;+0:1]=[O;D1;H0:2].[NH2;D1;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]>>[O;D1;H0:5]=[#16:4](=[O;D1;H0:6])(-[c:7])-[N;H0;D2;+0:3]=[C;H0;D2;+0:1]=[O;D1;H0:2]
98.4
[{"value": 98.4, "product": "C(C)OC1=CC(=C(C(=O)OC)C=C1)S(=O)(=O)N=C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of methyl 2-(aminosulfonyl)-4-ethoxybenzoate (7.56 g, 29.2 mmol), n-butyl isocyanate (3.29 mL, 29.2 mmol), and 1,4-diaza[2.2.2]bicyclooctane (0.13 g, 1.2 mmol) in mixed xylenes was heated at reflux for 10 minutes. Phosgene was then added at such a rate that the internal temperature stayed at 133° C. or above...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Isocyanate
null
null
null
c1ccccc1
Other
null
null
null
CCCCN=C=O.CCOc1ccc(C(=O)OC)c(S(N)(=O)=O)c1>>CCOc1ccc(C(=O)OC)c(S(=O)(=O)N=C=O)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-efea6328e97c41fda837d753a6815718
COC(=O)c1ccc(SC)cc1[N+](=O)[O-]>>COC(=O)c1ccc(SC)cc1N
CSC1=CC(=C(C(=O)OC)C=C1)[N+](=O)[O-].[H][H]>>NC1=C(C(=O)OC)C=CC(=C1)SC
O=[N+:13]([O-])[c:12]1[c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:6][cH:7][c:8]([S:9][CH3:10])[cH:11]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([S:9][CH3:10])[cH:11][c:12]1[NH2:13]
COC(=O)c1ccc(SC)cc1[N+](=O)[O-]
COC(=O)c1ccc(SC)cc1N
null
[Pt]=S
C(C)(=O)OC
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[C:5](-[#8:6])=[O;D1;H0:7]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]:[c:2](-[NH2;D1;+0:1]):[c:3]
null
[]
null
null
null
null
A mixture of methyl 4-(methylthio)-2-nitrobenzoate (11.3 g, 49.7 mmol) and 5% platinum sulfide on carbon catalyst (0.7 g) in methyl acetate (40 mL) was hydrogenated at 750 psi and 75° C. until hydrogen uptake ceased. The mixture was filtered through Celite®, and the filtrate solvent was rotary evaporated, leaving methy...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pt]=S.C(C)(=O)OC
null
null
COC(=O)c1ccc(SC)cc1[N+](=O)[O-]>[Pt]=S.C(C)(=O)OC>COC(=O)c1ccc(SC)cc1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2b6185ff48f74872a4d4707ac892d99d
CCCCN=C=O.COC(=O)c1ccc(SC)cc1S(N)(=O)=O>>COC(=O)c1ccc(SC)cc1S(=O)(=O)N=C=O
C(=O)(Cl)Cl.NS(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)SC.C(CCC)N=C=O>>N(=C=O)S(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)SC
CCCCN=[C:17]=[O:18].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([S:9][CH3:10])[cH:11][c:12]1[S:13](=[O:14])(=[O:15])[NH2:16]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([S:9][CH3:10])[cH:11][c:12]1[S:13](=[O:14])(=[O:15])[N:16]=[C:17]=[O:18]
CCCCN=C=O.COC(=O)c1ccc(SC)cc1S(N)(=O)=O
COC(=O)c1ccc(SC)cc1S(=O)(=O)N=C=O
null
null
null
Functional Group Interconversion
OtherReaction
d6c69f89b87c5c421a628563544ee2b8b0164ec4561bcd29a2cbba0dce4075ac
5df9e857f75ada60baf9e936007533a18389016451154bd1ed26e91b5babd844
c1ccccc1
C-C-C-C-N=[C;H0;D2;+0:1]=[O;D1;H0:2].[NH2;D1;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]>>[O;D1;H0:5]=[#16:4](=[O;D1;H0:6])(-[c:7])-[N;H0;D2;+0:3]=[C;H0;D2;+0:1]=[O;D1;H0:2]
111.4
[{"value": 111.4, "product": "N(=C=O)S(=O)(=O)C1=C(C(=O)OC)C=CC(=C1)SC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of methyl 2-(aminosulfonyl)-4-(methylthio)benzoate (5.23 g, 20.0 mmol), n-butyl isocyanate (2.25 mL, 20.0 mmol), and 1,4-diaza[2.2.2]bicyclooctane (0.09 g, 0.8 mmol) in mixed xylenes (50 mL) was heated at reflux for 10 minutes. Phosgene was then added at such a rate that the internal temperature stayed at 13...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Isocyanate
null
null
null
c1ccccc1
Other
null
null
null
CCCCN=C=O.COC(=O)c1ccc(SC)cc1S(N)(=O)=O>>COC(=O)c1ccc(SC)cc1S(=O)(=O)N=C=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-41d0738c14934a8d8d2f0c0151409174
CCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>>CCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCC)cc3)CN(Nc3ccc(C(=O)OCC)cc3)C2)cc1
NC1=CC=C(C(=O)OCC)C=C1.N1=C(Cl)N=C(Cl)N=C1Cl.Cl>>C(C)OC(=O)C1=CC=C(NN2CN(CN(C2)NC2=CC=C(C=C2)C(=O)OCC)NC2=CC=C(C=C2)C(=O)OCC)C=C1
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([NH2:10])[cH:41][cH:38]1.Cl[c:12]1[n:11][c:16](Cl)[n:13][c:19](Cl)[n:28]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([NH:10][N:11]2[CH2:12][N:13]([NH:14][c:15]3[cH:16][cH:17][c:18]([C:19](=[O:20])[O:21][CH2:22][CH3:23])[cH:24][cH:25]3)[CH2:26][N:27](...
CCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1
CCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCC)cc3)CN(Nc3ccc(C(=O)OCC)cc3)C2)cc1
null
null
C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
OtherReaction
ed9b4e3f7d9fcf59802d9282dfba25cd158ad6444611b9c9e892d87f4f4ad2f1
89c26d060a9b2ad6ff892ab2cb3f2d3dd04eecda2432a97bc7079f40dd16fe84
c1ccc(NN2CN(Nc3ccccc3)CN(Nc3ccccc3)C2)cc1
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c;H0;D3;+0:3](-Cl):[n;H0;D2;+0:4]:[c;H0;D3;+0:5](-Cl):[n;H0;D2;+0:6]:1.[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[c;H0;D3;+0:11]1:[c:12]:[c:13]:[c:14](-[NH2;D1;+0:15]):[cH;D2;+0:16]:[cH;D2;+0:17]:1>>[C:18]-[#8:19]-[C;H0;D3;+0:5](=[O;D1;H0:20])-[c:21]1:[c:22]:[cH;D2;+0:3]:[c:23](-[#7:24]-[N;H0...
97
[{"value": 97.0, "product": "C(C)OC(=O)C1=CC=C(NN2CN(CN(C2)NC2=CC=C(C=C2)C(=O)OCC)NC2=CC=C(C=C2)C(=O)OCC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
82.6 g of ethyl p-aminobenzoate and 30.75 g of cyanuric chloride in 1,500 ml of xylene were refluxed for 8 hours, hydrogen chloride escaping during this procedure. Thereafter, 1 liter of xylene was added, and the suspension, at 80°-90° C., was washed neutral with saturated sodium bicarbonate solution and then cooled to...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Ester.Primary amine
Hydrazine.Hydrazine.Hydrazine.Ester.Ester.Ester
c1ccccc1.c1ncncn1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
null
C=1(C(=CC=CC1)C)C
null
null
CCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>C=1(C(=CC=CC1)C)C>CCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCC)cc3)CN(Nc3ccc(C(=O)OCC)cc3)C2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-848069fa4f1f477c85839d23e4203cc5
CCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>>CCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCC)cc3)C2)cc1
NC1=CC=C(C(=O)OCCCCCCCC)C=C1.N1=C(Cl)N=C(Cl)N=C1Cl.Cl>>C(CCCCCCC)OC(=O)C1=CC=C(NN2CN(CN(C2)NC2=CC=C(C=C2)C(=O)OCCCCCCCC)NC2=CC=C(C=C2)C(=O)OCCCCCCCC)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:45]([c:44]1[cH:43][cH:42][c:15]([NH2:16])[cH:59][cH:56]1)=[O:46].Cl[c:10]1[n:17][c:25](Cl)[n:20][c:24](Cl)[n:39]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[c:12]1[cH:13][cH:14][c:15]([NH:16][N:17]2[CH2:18][N:19]([NH:20][...
CCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1
CCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCC)cc3)C2)cc1
null
null
C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
OtherReaction
ed9b4e3f7d9fcf59802d9282dfba25cd158ad6444611b9c9e892d87f4f4ad2f1
89c26d060a9b2ad6ff892ab2cb3f2d3dd04eecda2432a97bc7079f40dd16fe84
c1ccc(NN2CN(Nc3ccccc3)CN(Nc3ccccc3)C2)cc1
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c;H0;D3;+0:3](-Cl):[n;H0;D2;+0:4]:[c;H0;D3;+0:5](-Cl):[n;H0;D2;+0:6]:1.[C:7]-[C:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[c:12]1:[c:13]:[cH;D2;+0:14]:[c;H0;D3;+0:15](-[NH2;D1;+0:16]):[cH;D2;+0:17]:[cH;D2;+0:18]:1>>[C:19]-[#8:20]-[C;H0;D3;+0:3](=[O;D1;H0:21])-[c;H0;D3;+0:5]1:[c...
null
[]
90
CELSIUS
null
null
75 g of octyl p-aminobenzoate and 18.5 g of cyanuric chloride in 1,000 ml of xylene were heated at 140° C. for 8 hours. After the evolution of hydrogen chloride was complete, the reaction solution was cooled to 90° C., washed twice with saturated sodium bicarbonate solution and once with water and then cooled to room t...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Ester.Primary amine
Hydrazine.Hydrazine.Hydrazine.Ester.Ester.Ester
c1ccccc1.c1ncncn1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
null
C=1(C(=CC=CC1)C)C
90
null
CCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>C=1(C(=CC=CC1)C)C>CCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCC)cc3)C2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d7ec7c5243894addb439002cd6f1f99a
CCCCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>>CCCCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCCCC)cc3)C2)cc1
NC1=CC=C(C(=O)OCCCCCCCCCC)C=C1.N1=C(Cl)N=C(Cl)N=C1Cl.Cl>>C(CCCCCCCCC)OC(=O)C1=CC=C(NN2CN(CN(C2)NC2=CC=C(C=C2)C(=O)OCCCCCCCCCC)NC2=CC=C(C=C2)C(=O)OCCCCCCCCCC)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][C:27]([c:26]1[cH:25][cH:24][c:17]([NH2:18])[cH:65][cH:40]1)=[O:28].Cl[c:12]1[n:19][c:64](Cl)[n:43][c:42](Cl)[n:21]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][C:12](=[O:13])[c:14]1[cH:15][cH:16][c:17]([NH:1...
CCCCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1
CCCCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCCCC)cc3)C2)cc1
null
null
C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
OtherReaction
ed9b4e3f7d9fcf59802d9282dfba25cd158ad6444611b9c9e892d87f4f4ad2f1
89c26d060a9b2ad6ff892ab2cb3f2d3dd04eecda2432a97bc7079f40dd16fe84
c1ccc(NN2CN(Nc3ccccc3)CN(Nc3ccccc3)C2)cc1
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c;H0;D3;+0:3](-Cl):[n;H0;D2;+0:4]:[c;H0;D3;+0:5](-Cl):[n;H0;D2;+0:6]:1.[C:7]-[C:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[c:12]1:[c:13]:[cH;D2;+0:14]:[c;H0;D3;+0:15](-[NH2;D1;+0:16]):[cH;D2;+0:17]:[cH;D2;+0:18]:1>>[C:19]-[#8:20]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[c:12]1:[c:13]:[c...
null
[]
90
CELSIUS
null
null
83 g of decyl p-aminobenzoate and 18.5 g of cyanuric chloride in 1,000 ml of xylene were heated at 140° C. for 8 hours. After the evolution of hydrogen chloride was complete, the reaction solution was cooled to 90° C., washed twice with saturated sodium bicarbonate solution and once with water, and then cooled to room ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Ester.Primary amine
Hydrazine.Hydrazine.Hydrazine.Ester.Ester.Ester
c1ccccc1.c1ncncn1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
null
C=1(C(=CC=CC1)C)C
90
null
CCCCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>C=1(C(=CC=CC1)C)C>CCCCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCCCC)cc3)C2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6b8bf34c051a47799634f0478cd59831
CCCCCCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>>CCCCCCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCCCCCC)cc3)C2)cc1
N1=C(Cl)N=C(Cl)N=C1Cl.NC1=CC=C(C(=O)OCCCCCCCCCCCC)C=C1.Cl>>C(CCCCCCCCCCC)OC(=O)C1=CC=C(NN2CN(CN(C2)NC2=CC=C(C=C2)C(=O)OCCCCCCCCCCCC)NC2=CC=C(C=C2)C(=O)OCCCCCCCCCCCC)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][C:53]([c:52]1[cH:51][cH:50][c:19]([NH2:20])[cH:71][cH:68]1)=[O:54].Cl[c:14]1[n:21][c:29](Cl)[n:47][c:28](Cl)[n:48]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][C:14](=[O:15])[...
CCCCCCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1
CCCCCCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCCCCCC)cc3)C2)cc1
null
null
C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
OtherReaction
ed9b4e3f7d9fcf59802d9282dfba25cd158ad6444611b9c9e892d87f4f4ad2f1
89c26d060a9b2ad6ff892ab2cb3f2d3dd04eecda2432a97bc7079f40dd16fe84
c1ccc(NN2CN(Nc3ccccc3)CN(Nc3ccccc3)C2)cc1
Cl-[c;H0;D3;+0:1]1:[n;H0;D2;+0:2]:[c;H0;D3;+0:3](-Cl):[n;H0;D2;+0:4]:[c;H0;D3;+0:5](-Cl):[n;H0;D2;+0:6]:1.[C:7]-[C:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[c:12]1:[c:13]:[cH;D2;+0:14]:[c;H0;D3;+0:15](-[NH2;D1;+0:16]):[cH;D2;+0:17]:[cH;D2;+0:18]:1>>[C:19]-[#8:20]-[C;H0;D3;+0:3](=[O;D1;H0:21])-[c;H0;D3;+0:5](:[c...
null
[]
80
CELSIUS
8
HOUR
18.5 g of cyanuric chloride and 92 g of dodecyl p-aminobenzoate in 1,000 ml of xylene were heated at 140° C. until HCl gas was no longer evolved. After 8 hours, the reaction solution was cooled to 80° C., washed twice with saturated sodium bicarbonate solution and once with water, and then cooled to room temperature. T...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Ester.Primary amine
Hydrazine.Hydrazine.Hydrazine.Ester.Ester.Ester
c1ccccc1.c1ncncn1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
c1ccccc1.C1[NH]C[NH]C[NH]1.c1ccccc1.c1ccccc1
null
C=1(C(=CC=CC1)C)C
80
8
CCCCCCCCCCCCOC(=O)c1ccc(N)cc1.Clc1nc(Cl)nc(Cl)n1>C=1(C(=CC=CC1)C)C>CCCCCCCCCCCCOC(=O)c1ccc(NN2CN(Nc3ccc(C(=O)OCCCCCCCCCCCC)cc3)CN(Nc3ccc(C(=O)OCCCCCCCCCCCC)cc3)C2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-51d04ddc18b345bfacbd8eb04a8a2685
c1ccc(C2CO2)cc1>>c1ccc(C2CO2)cc1
C(CCCCCCC\C=C/CCCCCCCC)N.C1C(C2=CC=CC=C2)O1.C1(=CC=CC=C1)C.[B]>>C(CCCCCCC\C=C/CCCCCCCC)N.C1C(C2=CC=CC=C2)O1
[cH:20]1[cH:21][cH:22][c:23]([CH:24]2[CH2:25][O:26]2)[cH:27][cH:28]1>>[cH:20]1[cH:21][cH:22][c:23]([CH:24]2[CH2:25][O:26]2)[cH:27][cH:28]1
c1ccc(C2CO2)cc1
c1ccc(C2CO2)cc1
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccc(C2CO2)cc1
null
null
[]
null
null
null
null
A sulfurized, boron-containing, heterocyclic compound is prepared by mixing 12 grams of oleylamine, 9.6 grams of styrene oxide and 200 ml of toluene for 30 minutes at room temperature (25° C.) in a single-necked one-liter round-bottomed flask. The flask is placed in a heating mantle and equipped with a water-cooled con...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.C1CO1
null
O
null
null
c1ccc(C2CO2)cc1>O>c1ccc(C2CO2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-91b5da6b753c4d87a85d7b0c1e08baeb
Nc1ccc(NNC=O)cc1.O=C(O)c1cccc(-n2nnnc2S)c1>>O=CNNc1ccc(NC(=O)c2cccc(-n3nnnc3S)c2)cc1
C1(CCCCC1)N=C=NC1CCCCC1.C(=O)(O)C=1C=C(C=CC1)N1N=NN=C1S.C(=O)NNC1=CC=C(N)C=C1>>SC1=NN=NN1C1=CC(=CC=C1)C(NC1=CC=C(C=C1)NNC=O)=O
[O:1]=[CH:2][NH:3][NH:4][c:5]1[cH:6][cH:7][c:8]([NH2:9])[cH:24][cH:25]1.O[C:10](=[O:11])[c:12]1[cH:13][cH:14][cH:15][c:16](-[n:17]2[n:18][n:19][n:20][c:21]2[SH:22])[cH:23]1>>[O:1]=[CH:2][NH:3][NH:4][c:5]1[cH:6][cH:7][c:8]([NH:9][C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][c:16](-[n:17]3[n:18][n:19][n:20][c:21]3[SH:22])[...
Nc1ccc(NNC=O)cc1.O=C(O)c1cccc(-n2nnnc2S)c1
O=CNNc1ccc(NC(=O)c2cccc(-n3nnnc3S)c2)cc1
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Nc1ccccc1)c1cccc(-n2cnnn2)c1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
25.4
[{"value": 25.4, "product": "SC1=NN=NN1C1=CC(=CC=C1)C(NC1=CC=C(C=C1)NNC=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
In 50 ml of dimethylformamide were dissolved 11.1 g of 1-(3-carboxyphenyl)-5-mercaptotetrazole and 7.6 g of 4-(2-formylhydrazino)aniline, and a solution of 10.3 g of dicyclohexylcarbodiimide in 10 ml of dimethylformamide was added dropwise to the solution at 0° C. in a nitrogeneous atmosphere over about 30 minutes. Aft...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.c1nnn[nH]1
HO-
CN(C=O)C
null
3
Nc1ccc(NNC=O)cc1.O=C(O)c1cccc(-n2nnnc2S)c1>CN(C=O)C>O=CNNc1ccc(NC(=O)c2cccc(-n3nnnc3S)c2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-03c19910184945d28d0037efcffa7194
O=C(O)CBr.Sc1nnc(S)s1>>O=C(O)CSc1nnc(S)s1
BrCC(=O)O.SC=1SC(=NN1)S.[OH-].[K+]>>C(=O)(O)CSC=1SC(=NN1)S
Br[CH2:4][C:2](=[O:1])[OH:3].[SH:5][c:6]1[n:7][n:8][c:9]([SH:10])[s:11]1>>[O:1]=[C:2]([OH:3])[CH2:4][S:5][c:6]1[n:7][n:8][c:9]([SH:10])[s:11]1
O=C(O)CBr.Sc1nnc(S)s1
O=C(O)CSc1nnc(S)s1
null
null
O
Heteroatom Alkylation and Arylation
thioether_nucl_sub
26df88c6a3f5f203c89584658be4e126cb42994c98a2e16bc812e1036cdae857
8b2f52296c3a93039174c980b6042ba15754e04d6892a1284c3a32985220b214
c1nncs1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[O;D1;H1:4].[SH;D1;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[#7;a:9]:[#7;a:10]:1>>[O;D1;H0:3]=[C:2](-[O;D1;H1:4])-[CH2;D2;+0:1]-[S;H0;D2;+0:5]-[c:6]1:[#16;a:7]:[c:8]:[#7;a:9]:[#7;a:10]:1
86.6
[{"value": 86.6, "product": "C(=O)(O)CSC=1SC(=NN1)S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
1
HOUR
In 200 ml of water were dissolved 15.0 g of 2,5-dimercapto-1,3,4-thiadiazole and 69 g of potassium hydroxide, and a solution of 13.9 g of bromoacetic acid in 30 ml of water was added thereto dropwise at room temperature. After the addition, the mixture was stirred at 60° C. for 1 hour, followed by allowing to cool to r...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic thiol
Monosulfide
null
null
c1nncs1
HBr
O
60
1
O=C(O)CBr.Sc1nnc(S)s1>O>O=C(O)CSc1nnc(S)s1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ade2fb49e10c41c6b4889a7c288bd378
O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N=C=S)cc21>>O=C(O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12
C1=CC2=C(C=C1N=C=S)C(=O)OC23C4=C(C=C(C=C4)O)OC5=C3C=CC(=C5)O.C([O-])([O-])=O.C1=CC2=C(C=C1N=C=S)C(=O)OC23C4=C(C=C(C=C4)O)OC5=C3C=CC(=C5)O>>C=1C=CC(=C(C1)C2=C3C=CC(=O)C=C3OC4=C2C=CC(=C4)O)C(=O)O
S=C=N[c:6]1[cH:5][c:4]2[c:9]([cH:8][cH:7]1)[C:10]1([O:3][C:2]2=[O:1])[c:11]2[cH:12][cH:13][c:14]([OH:15])[cH:16][c:17]2[O:18][c:19]2[cH:20][c:21]([OH:22])[cH:23][cH:24][c:25]21>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1-[c:10]1[c:11]2[cH:12][cH:13][c:14](=[O:15])[cH:16][c:17]-2[o:18][c:19]2[cH:20][c:21]([...
O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N=C=S)cc21
O=C(O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12
null
null
C(C)O
Functional Group Interconversion
OtherReaction
2bdf19f895cccba6c6602b312223931295ab2b9d32ef41313b16970e6181726d
e6f7e6efa036edd9dd5bbb1c3bf5fdd9a5ca0cde297a4f028b8d6746b1b615fd
O=c1ccc2c(-c3ccccc3)c3ccccc3oc-2c1
S=C=N-[c;H0;D3;+0:1]1:[c:2]:[c:3]2:[c;H0;D3;+0:4](:[c:5]:[c:6]:1)-[C;H0;D4;+0:7]1(-[O;H0;D2;+0:8]-[C:9]-2=[O;D1;H0:10])-[c:11](:[c:12]):[c:13](:[c:14])-[O;H0;D2;+0:15]-[c;H0;D3;+0:16]2:[c:17]:[c;H0;D3;+0:18](-[OH;D1;+0:19]):[c:20]:[c:21]:[c;H0;D3;+0:22]:2-1>>[O;D1;H0:10]=[C:9](-[OH;D1;+0:8])-[c:3]1:[c:2]:[cH;D2;+0:1]:[...
null
[]
null
null
null
null
Fluoresceinisothiocyanate (FITC) is dissolved in ethanol (5 mg solid/ml). To 2 ml of a 5 mg/ml protein solution from (I), 0.5 ml carbonate buffer (1M NaHCO3 --Na2CO3 buffer pH 9) is added, followed by 50 μl FITC solution. The mixture is shaken well and the free FITC is chromatographically separated from the bound molec...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Aromatic alcohol.Isothiocyanate
Carboxylic acid
c1ccc2c(c1)COC21c2ccccc2Oc2ccccc21
c1ccccc1.c1ccc2cc3ccccc3oc2c1
c1ccccc1.c1ccc2cc3ccccc3oc2c1
Other
C(C)O
null
null
O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N=C=S)cc21>C(C)O>O=C(O)c1ccccc1-c1c2ccc(=O)cc-2oc2cc(O)ccc12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6c256a247ecb4bdb8cf60a7f89a63e98
CC(C)C[C@H](N)C(=O)O.CC(C)C[C@H](N)C(=O)O.O=c1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)[nH]1>>O=c1ccn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]1.O=c1ccn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]1
[C@@H]1([C@H](O)[C@H](O)[C@@H](CO)O1)N1C(=O)NC(=O)C=C1.N[C@@H](CC(C)C)C(=O)O.N[C@@H](CC(C)C)C(=O)O>>C1[C@@H]([C@H](O[C@H]1N2C=CC(=O)NC2=O)CO)O.[C@@H]1(C[C@H](O)[C@@H](CO)O1)N1C(=O)NC(=O)C=C1
C[CH:27]([CH2:19][C@@H:20]([C:18](=[O:17])[OH:29])[NH2:32])[CH3:26].C[CH:24](C)[CH2:23][C@H:22]([NH2:21])[C:30]([OH:28])=[O:31].[O:1]=[c:2]1[cH:3][cH:4][n:5]([C@H:6]2[C@H:7]([OH:25])[C@H:8]([OH:9])[C@@H:10]([CH2:11][OH:12])[O:13]2)[c:14](=[O:15])[nH:16]1>>[O:1]=[c:2]1[cH:3][cH:4][n:5]([C@H:6]2[CH2:7][C@H:8]([OH:9])[C@@...
CC(C)C[C@H](N)C(=O)O.CC(C)C[C@H](N)C(=O)O.O=c1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)[nH]1
O=c1ccn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]1.O=c1ccn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
c4b81035e98988b0bda725ca7fddc63bba64117299484e9ac7ac3e4e4482c668
69613725106b233a9d33d53844819b260ebce100f3446af9f0222e8b950247eb
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1.O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
C-[CH;D3;+0:1](-C)-[C:2]-[C@H;D3;+0:3](-[NH2;D1;+0:4])-[C;H0;D3;+0:5](=[O;D1;H0:6])-[OH;D1;+0:7].C-[CH;D3;+0:8](-[CH3;D1;+0:9])-[CH2;D2;+0:10]-[C@H;D3;+0:11](-[NH2;D1;+0:12])-[C;H0;D3;+0:13](=[O;D1;H0:14])-[OH;D1;+0:15].[#7;a:16]-[C:17]1-[#8:18]-[C:19]-[C:20](-[O;D1;H1:21])-[C@H;D3;+0:22]-1-[OH;D1;+0:23]>>[#7;a:16]-[C:...
null
[]
null
null
null
null
Urd-uridine; Leu-L-leucine. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Secondary alcohol.Primary amine.Primary amine
Ether.Primary alcohol.Secondary alcohol
C1CCOC1
C1CCOC1.c1ccncn1.C1CCOC1
c1ccncn1.C1CCOC1.c1ccncn1.C1CCOC1
Other
null
null
null
CC(C)C[C@H](N)C(=O)O.CC(C)C[C@H](N)C(=O)O.O=c1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(=O)[nH]1>>O=c1ccn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]1.O=c1ccn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a74d48ae4860473095f955cf805e25c4
Cc1cn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]c1=O>>Cc1cn2c(nc1=O)O[C@H]1C[C@H]2O[C@@H]1CO
[C@@H]1(C[C@H](O)[C@@H](CO)O1)N1C(=O)NC(=O)C(C)=C1.ClC(C(F)(F)N(CC)CC)F.C(C)O>>CC1=CN2[C@H]3C[C@@H]([C@H](O3)CO)OC2=NC1=O
O=[c:5]1[n:4]([C@H:12]2[CH2:11][C@H:10]([OH:9])[C@@H:14]([CH2:15][OH:16])[O:13]2)[cH:3][c:2]([CH3:1])[c:7](=[O:8])[nH:6]1>>[CH3:1][c:2]1[cH:3][n:4]2[c:5]([n:6][c:7]1=[O:8])[O:9][C@H:10]1[CH2:11][C@H:12]2[O:13][C@@H:14]1[CH2:15][OH:16]
Cc1cn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]c1=O
Cc1cn2c(nc1=O)O[C@H]1C[C@H]2O[C@@H]1CO
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
7216ae954245743aa450156cb863eb127cb9ec1e3bba6623b2e49580a2a0c455
08f7221cae607d413f579138dcaa6997bebcad2bbb42d2f1b3b2a2d886befb37
O=c1ccn2c(n1)O[C@@H]1CO[C@@H]2C1
O=[c;H0;D3;+0:1]1:[nH;D2;+0:2]:[c:3](=[O;D1;H0:4]):[c:5]:[c:6]:[#7;a:7]:1-[C:8]1-[#8:9]-[C:10]-[C:11](-[OH;D1;+0:12])-[C:13]-1>>[O;D1;H0:4]=[c:3]1:[c:5]:[c:6]:[#7;a:7]2:[c;H0;D3;+0:1](:[n;H0;D2;+0:2]:1)-[O;H0;D2;+0:12]-[C:11]1-[C:13]-[C:8]-2-[#8:9]-[C:10]-1
60.3
[{"value": 60.3, "product": "CC1=CN2[C@H]3C[C@@H]([C@H](O3)CO)OC2=NC1=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.3, "product": "CC1=CN2[C@H]3C[C@@H]([C@H](O3)CO)OC2=NC1=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
null
null
Thymidine (85.4 g; 0.353 mol) was dissolved in 500 mL dry DMF (dimethyl formamide) and added to N-(2-chloro-1,1,2-trifluoroethyl)diethylamine (100.3 g; 0.529 mol) [prepared according to the method of D. E. Ayer, J. Med. Chem. 6, 608 (1963)]. This solution was heated at 70° C. for 30 minutes then poured into 950 mL etha...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ether
c1cncnc1
c1cnc2n(c1)[C@H]1C[C@@H](CO1)O2
c1cnc2n(c1)[C@H]1C[C@@H](CO1)O2
HO-
CN(C=O)C
70
null
Cc1cn([C@H]2C[C@H](O)[C@@H](CO)O2)c(=O)[nH]c1=O>CN(C=O)C>Cc1cn2c(nc1=O)O[C@H]1C[C@H]2O[C@@H]1CO
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-74fbee929e784564bd98215859d583b0
C#CCCC(=O)Cl.O=C1Nc2cccnc2Nc2ccccc21>>C#CCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21
C(CCC)[Li].C(CCC#C)(=O)Cl.N1=CC=CC2=C1NC1=C(C(N2)=O)C=CC=C1>>O=C(CCC#C)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2
Cl[C:5]([CH2:4][CH2:3][C:2]#[CH:1])=[O:6].[NH:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[NH:16][c:17]2[cH:18][cH:19][cH:20][n:21][c:22]21>>[CH:1]#[C:2][CH2:3][CH2:4][C:5](=[O:6])[N:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[NH:16][c:17]2[cH:18][cH:19][cH:20][n:21][c:22]21
C#CCCC(=O)Cl.O=C1Nc2cccnc2Nc2ccccc21
C#CCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21
null
null
CCCCCC.C(C)(=O)OCC.O1CCCC1
Acylation
N-alkylation of secondary amines with alkyl halides
46c0938aafd554a4057df12dbebe677cf04009fa5bed51927bc1d071fff7b2b6
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C1Nc2cccnc2Nc2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[C:5]#[C;D1;H1:6].[O;D1;H0:7]=[C:8]1-[#7:9]-[c:10]:[c:11](:[#7;a:12]:[c:13])-[NH;D2;+0:14]-[c:15](:[c:16]):[c:17]-1>>[C;D1;H1:6]#[C:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:14]1-[c:11](:[#7;a:12]:[c:13]):[c:10]-[#7:9]-[C:8](=[O;D1;H0:7])-[c:17]:[c:15]-1:[c:16]
null
[]
30
CELSIUS
30
MINUTE
22.4 ml of a 1.6 molar solution of n-butyl-lithium in n-hexane are added dropwise with stirring, at 0° C., to a suspension of 3.7 g (0.017 mol) of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one in 150 ml of absolute tetrahydrofuran. After it has all been added, the mixture is stirred for a further 30 minutes and...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
c1ccc2c(c1)CNc1cccnc1N2
c1ccc2c(c1)CNc1cccnc1[NH]2
c1ccc2c(c1)CNc1cccnc1[NH]2
HCl
CCCCCC.C(C)(=O)OCC.O1CCCC1
30
0.5
C#CCCC(=O)Cl.O=C1Nc2cccnc2Nc2ccccc21>CCCCCC.C(C)(=O)OCC.O1CCCC1>C#CCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-da6aacba240a48b7804ec076824d5006
C#CCN.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21>>C#CCNC(=O)N1c2ccccc2C(=O)Nc2cccnc21
C(C#C)N.ClC(=O)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2.C(C)N(CC)CC>>C(C#C)NC(=O)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2
[CH:1]#[C:2][CH2:3][NH2:4].Cl[C:5](=[O:6])[N:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[NH:16][c:17]2[cH:18][cH:19][cH:20][n:21][c:22]21>>[CH:1]#[C:2][CH2:3][NH:4][C:5](=[O:6])[N:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[NH:16][c:17]2[cH:18][cH:19][cH:20][n:21][c:22]21
C#CCN.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21
C#CCNC(=O)N1c2ccccc2C(=O)Nc2cccnc21
null
null
C(Cl)(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
b81fefae7607aa106605114867756af2924064950a2aea97200543849613e96a
406c5893488430105533c87dfb5d625d8382e709e047cda9cfdc2235e742a9cf
O=C1Nc2cccnc2Nc2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3](-[c:4])-[c:5]:[#7;a:6].[C;D1;H1:7]#[C:8]-[C:9]-[NH2;D1;+0:10]>>[#7;a:6]:[c:5]-[#7:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9]-[C:8]#[C;D1;H1:7])-[c:4]
null
[]
40
CELSIUS
30
MINUTE
5.5 g (0.1 mol) of propargylamine were added dropwise with stirring at ambient temperature to a suspension of 27.3 g (0.1 mol) of 11-chlorocarbonyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one and 10.0 g (0.1 mol) of triethylamine in 500 ml of chloroform, whereupon the temperature rises to 35° C. The mixture i...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Tertiary amide.Primary amine
Urea
null
null
c1ccc2c(c1)CNc1cccnc1[NH]2
HCl
C(Cl)(Cl)Cl
40
0.5
C#CCN.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21>C(Cl)(Cl)Cl>C#CCNC(=O)N1c2ccccc2C(=O)Nc2cccnc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-40ce053f6f454522aede5b77a4a32553
C#CCNC.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21>>C#CCN(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
ClC(=O)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2.CNCC#C>>CN(C(=O)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2)CC#C
[CH:1]#[C:2][CH2:3][NH:4][CH3:5].Cl[C:6](=[O:7])[N:8]1[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15](=[O:16])[NH:17][c:18]2[cH:19][cH:20][cH:21][n:22][c:23]21>>[CH:1]#[C:2][CH2:3][N:4]([CH3:5])[C:6](=[O:7])[N:8]1[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15](=[O:16])[NH:17][c:18]2[cH:19][cH:20][cH:21][n:22][c:23]21
C#CCNC.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21
C#CCN(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
null
null
null
Acylation
N-alkylation of secondary amines with alkyl halides
21141392b95d6b95cd118c7c0b595c90f08886f6a08d558238622ce18df3aa9b
353c6e1db25433862a8bcf26ca332f6abeb45cb685806584bc65f8cfcb712540
O=C1Nc2cccnc2Nc2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3](-[c:4])-[c:5]:[#7;a:6].[C;D1;H1:7]#[C:8]-[C:9]-[NH;D2;+0:10]-[C;D1;H3:11]>>[#7;a:6]:[c:5]-[#7:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:10](-[C;D1;H3:11])-[C:9]-[C:8]#[C;D1;H1:7])-[c:4]
null
[]
null
null
null
null
Analogously to Example C, using 27.3 g (0.1 mol) of 11-chlorocarbonyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one and 7.0 g (0.1 mol) of N-methyl-propargylamine, 27 g (88% of theory) of the desired compound are obtained. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Tertiary amide.Secondary amine
Urea
null
null
c1ccc2c(c1)CNc1cccnc1[NH]2
HCl
null
null
null
C#CCNC.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21>>C#CCN(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b62934e97d654247b2961e7c9f60d869
C#CCO.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21>>C#CCOC(=O)N1c2ccccc2C(=O)Nc2cccnc21
C(CCC)[Li].C(C#C)O.ClC(=O)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2>>C(C#C)OC(=O)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2
[CH:1]#[C:2][CH2:3][OH:4].Cl[C:5](=[O:6])[N:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[NH:16][c:17]2[cH:18][cH:19][cH:20][n:21][c:22]21>>[CH:1]#[C:2][CH2:3][O:4][C:5](=[O:6])[N:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[NH:16][c:17]2[cH:18][cH:19][cH:20][n:21][c:22]21
C#CCO.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21
C#CCOC(=O)N1c2ccccc2C(=O)Nc2cccnc21
null
null
CCCCCC.O1CCCC1
Protection
Schotten-Baumann to ester
597fa7ba4ca169ec9e1d3b8730fbab27757ccde00143c31019a679c09b7b2b7f
562b6a5118cb63cbe5ff058f35135dc3f085de8b8ec7fa4ac4de518324eb826a
O=C1Nc2cccnc2Nc2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3](-[c:4])-[c:5]:[#7;a:6].[C;D1;H1:7]#[C:8]-[C:9]-[OH;D1;+0:10]>>[#7;a:6]:[c:5]-[#7:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:10]-[C:9]-[C:8]#[C;D1;H1:7])-[c:4]
null
[]
null
null
30
MINUTE
At 15° to 20° C., 3.08 g (0.048 mol) of n-butyl-lithium in 30 ml of n-hexane are added dropwise to a solution of 2.24 g (0.04 mol) of propargyl alcohol in 120 ml of tetrahydrofuran. After it has all been added, the mixture is stirred for a further 30 minutes at ambient temperature and then mixed with a suspension of 10...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Tertiary amide.Primary alcohol
Carbamic ester
null
null
c1ccc2c(c1)CNc1cccnc1[NH]2
HCl
CCCCCC.O1CCCC1
null
0.5
C#CCO.O=C1Nc2cccnc2N(C(=O)Cl)c2ccccc21>CCCCCC.O1CCCC1>C#CCOC(=O)N1c2ccccc2C(=O)Nc2cccnc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7887cac5bd37464998c4050ed1a73ce5
C#CCBr.CCOC(=O)C(C)C(=O)OCC>>C#CCC(C)(C(=O)OCC)C(=O)OCC
CC(C(=O)OCC)C(=O)OCC.C(C#C)Br.[Br-].[Na+]>>CC(C(=O)OCC)(C(=O)OCC)CC#C
Br[CH2:3][C:2]#[CH:1].[CH:4]([CH3:5])([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[O:13][CH2:14][CH3:15]>>[CH:1]#[C:2][CH2:3][C:4]([CH3:5])([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[O:13][CH2:14][CH3:15]
C#CCBr.CCOC(=O)C(C)C(=O)OCC
C#CCC(C)(C(=O)OCC)C(=O)OCC
null
null
null
C-C Coupling
OtherReaction
8175b6573d6439ec7ccc45bf6b48843ab56b46dccfc6504384c4766d09f35cc7
d1817e44576d3a158547867a56245217a593d4f828a6d6dfaa8ed11276894e44
null
Br-[CH2;D2;+0:1]-[C:2]#[C;D1;H1:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH;D3;+0:8](-[C;D1;H3:9])-[C:10](=[O;D1;H0:11])-[#8:12]-[C:13]>>[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[C;H0;D4;+0:8](-[C;D1;H3:9])(-[CH2;D2;+0:1]-[C:2]#[C;D1;H1:3])-[C:10](=[O;D1;H0:11])-[#8:12]-[C:13]
null
[]
null
null
null
null
At 35° to 40° to C., with stirring, 174 g (1.0 ml) of diethyl methylmalonate are added dropwise to an alkoxide solution (prepared from 23 g of sodium and 800 ml of absolute ethanol), the mixture is stirred for a further hour and then at 45° C. 130.8 g (1.1 mol) of propargyl bromide are added dropwise. The mixture is re...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ester
Ester.Ester
null
null
null
HBr
null
null
null
C#CCBr.CCOC(=O)C(C)C(=O)OCC>>C#CCC(C)(C(=O)OCC)C(=O)OCC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f675b34133534fd2ad6348d7c4b67760
C#CCC(C)(C(=O)OCC)C(=O)OCC>>C#CCC(C)(C(=O)O)C(=O)O
CC(C(=O)OCC)(C(=O)OCC)CC#C.[OH-].[K+]>>CC(C(=O)O)(C(=O)O)CC#C
CC[O:8][C:6]([C:4]([CH2:3][C:2]#[CH:1])([CH3:5])[C:9](=[O:10])[O:11]CC)=[O:7]>>[CH:1]#[C:2][CH2:3][C:4]([CH3:5])([C:6](=[O:7])[OH:8])[C:9](=[O:10])[OH:11]
C#CCC(C)(C(=O)OCC)C(=O)OCC
C#CCC(C)(C(=O)O)C(=O)O
null
null
O.C(C)O
Deprotection
OtherReaction
6e62db7aac546f574bcfb83067ba8906c30fcbfedfc37aa16b5eaad33833f45a
ed5fed81ba501ef41c88831ec6b9463b899bfdd0815c4145ae51c79addb226d0
null
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-C-C>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[C:4]-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]
null
[]
null
null
2
HOUR
187 g (0.88 mol) of diethyl 2-methyl-2-propargyl-malonate are added to a solution of 101 g (1.8 mol) of potassium hydroxide in a mixture of 560 ml of water/ethanol (1:1) and the mixture is refluxed with stirring for 2 hours. After the reaction has ended (monitored by TLC) the mixture is evaporated to dryness in vacuo a...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Carboxylic acid.Carboxylic acid
null
null
null
Other
O.C(C)O
null
2
C#CCC(C)(C(=O)OCC)C(=O)OCC>O.C(C)O>C#CCC(C)(C(=O)O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-909765aa47fa47b3808e7296f9f062de
C#CCC(C)C(=O)Cl.O=C1Nc2cccnc2Nc2ccccc21>>C#CCC(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
C(CCC)[Li].N1=CC=CC2=C1NC1=C(C(N2)=O)C=CC=C1.CC(C(=O)Cl)CC#C>>O=C(C(CC#C)C)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2
Cl[C:6]([CH:4]([CH2:3][C:2]#[CH:1])[CH3:5])=[O:7].[NH:8]1[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15](=[O:16])[NH:17][c:18]2[cH:19][cH:20][cH:21][n:22][c:23]21>>[CH:1]#[C:2][CH2:3][CH:4]([CH3:5])[C:6](=[O:7])[N:8]1[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15](=[O:16])[NH:17][c:18]2[cH:19][cH:20][cH:21][n:22][c:23]...
C#CCC(C)C(=O)Cl.O=C1Nc2cccnc2Nc2ccccc21
C#CCC(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
null
null
CCCCCC.C(C)(=O)OCC.O1CCCC1
Acylation
N-alkylation of secondary amines with alkyl halides
46c0938aafd554a4057df12dbebe677cf04009fa5bed51927bc1d071fff7b2b6
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C1Nc2cccnc2Nc2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[C:5]-[C:6]#[C;D1;H1:7].[O;D1;H0:8]=[C:9]1-[#7:10]-[c:11]:[c:12](:[#7;a:13]:[c:14])-[NH;D2;+0:15]-[c:16](:[c:17]):[c:18]-1>>[C;D1;H1:7]#[C:6]-[C:5]-[C:3](-[C;D1;H3:4])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:15]1-[c:12](:[#7;a:13]:[c:14]):[c:11]-[#7:10]-[C:9](=[O;D1;...
null
[]
null
null
null
null
At 0° to 10° C., with stirring, 416 ml (0.65 mol) of an n-butyl-lithium solution in n-hexane are added dropwise to a suspension of 63 g (0.3 mol) of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one in 1500 ml of absolute tetrahydrofuran. THe mixture is stirred for a further hour at ambient temperature, then cooled...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
c1ccc2c(c1)CNc1cccnc1N2
c1ccc2c(c1)CNc1cccnc1[NH]2
c1ccc2c(c1)CNc1cccnc1[NH]2
HCl
CCCCCC.C(C)(=O)OCC.O1CCCC1
null
null
C#CCC(C)C(=O)Cl.O=C1Nc2cccnc2Nc2ccccc21>CCCCCC.C(C)(=O)OCC.O1CCCC1>C#CCC(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-301ed65de99248bebe2bd6e6ac674570
C#CCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21.C1CCNCC1.C=O>>O=C1Nc2cccnc2N(C(=O)CCC#CCN2CCCCC2)c2ccccc21
O=C(CCC#C)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2.C=O.N1CCCCC1>>O=C(CCC#CCN1CCCCC1)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2
[O:1]=[C:2]1[NH:3][c:4]2[cH:5][cH:6][cH:7][n:8][c:9]2[N:10]([C:11](=[O:12])[CH2:13][CH2:14][C:15]#[CH:16])[c:24]2[cH:25][cH:26][cH:27][cH:28][c:29]21.[NH:18]1[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]1.O=[CH2:17]>>[O:1]=[C:2]1[NH:3][c:4]2[cH:5][cH:6][cH:7][n:8][c:9]2[N:10]([C:11](=[O:12])[CH2:13][CH2:14][C:15]#[C:16][CH2...
C#CCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21.C1CCNCC1.C=O
O=C1Nc2cccnc2N(C(=O)CCC#CCN2CCCCC2)c2ccccc21
null
[Cu]Cl
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
1c251f14c75b80b0dd3c8a9f2ea21fcdf95b017bc463f94c2b4be04acef3803b
7dc88503da2577b71123fe820b1c2cdad87aca8735340a4da3de40929f65c4dd
O=C1Nc2cccnc2N(C(=O)CCC#CCN2CCCCC2)c2ccccc21
O=[CH2;D1;+0:1].[C:2]-[C:3]#[CH;D1;+0:4].[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:2]-[C:3]#[C;H0;D2;+0:4]-[CH2;D2;+0:1]-[N;H0;D3;+0:7](-[C:6]-[C:5])-[C:8]-[C:9]
null
[]
null
null
null
null
A mixture consisting of 9.6 g (0.03 mol) of 5,11-dihydro-11-[1-oxo-4-pentynyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, 1.08 g (0.036 mol) of paraformaldehyde, 3.06 g (0.036 mol) of piperidine, 0.2 g of copper(I) chloride and 150 ml of dioxan is refluxed for 1 hour. After the reaction has ended the insoluble constitue...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Secondary amine.Alkyne
Tertiary amine.Alkyne
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccc2c(c1)CNc1cccnc1[NH]2
HO-
[Cu]Cl.O1CCOCC1
null
null
C#CCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21.C1CCNCC1.C=O>[Cu]Cl.O1CCOCC1>O=C1Nc2cccnc2N(C(=O)CCC#CCN2CCCCC2)c2ccccc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6577de97230742bfbdfb63b5e64d45dc
C#CCC(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21.C=O.CN1CCNCC1>>CC(CC#CCN1CCN(C)CC1)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
O=C(C(CC#C)C)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2.CN1CCNCC1.C(\C=C/C(=O)O)(=O)O.C=O>>O=C(C(CC#CCN1CCN(CC1)C)C)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2
[CH3:1][CH:2]([CH2:3][C:4]#[CH:5])[C:14](=[O:15])[N:16]1[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[C:23](=[O:24])[NH:25][c:26]2[cH:27][cH:28][cH:29][n:30][c:31]21.O=[CH2:6].[NH:7]1[CH2:8][CH2:9][N:10]([CH3:11])[CH2:12][CH2:13]1>>[CH3:1][CH:2]([CH2:3][C:4]#[C:5][CH2:6][N:7]1[CH2:8][CH2:9][N:10]([CH3:11])[CH2:12][CH2:13]...
C#CCC(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21.C=O.CN1CCNCC1
CC(CC#CCN1CCN(C)CC1)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
null
[Cu]Cl
O.O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
258faf155111cceefd44ed14e274394ce1b8b4d98ee6f574efdd5ed2b5325f2d
7dc88503da2577b71123fe820b1c2cdad87aca8735340a4da3de40929f65c4dd
O=C1Nc2cccnc2N(C(=O)CCC#CCN2CCNCC2)c2ccccc21
O=[CH2;D1;+0:1].[#7:2]1-[C:3]-[C:4]-[NH;D2;+0:5]-[C:6]-[C:7]-1.[C:8]-[C:9]#[CH;D1;+0:10]>>[C:8]-[C:9]#[C;H0;D2;+0:10]-[CH2;D2;+0:1]-[N;H0;D3;+0:5]1-[C:4]-[C:3]-[#7:2]-[C:7]-[C:6]-1
null
[]
null
null
1
HOUR
A reaction mixture consisting of 36.6 g (0.12 mol) of 5,11-dihydro-11-[1-oxo-2-methyl-4-pentynyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, 4 g (0.13 mol) of paraformaldehyde, 13.2 g (0.13 mol) of N-methylpiperazine, 0.2 g of copper(I) chloride and 600 ml of dioxan is refluxed for 2 hours. After the reaction has ended ...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Secondary amine.Alkyne
Tertiary amine.Alkyne
C1CNCC[NH]1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccc2c(c1)CNc1cccnc1[NH]2
HO-
[Cu]Cl.O.O1CCOCC1
null
1
C#CCC(C)C(=O)N1c2ccccc2C(=O)Nc2cccnc21.C=O.CN1CCNCC1>[Cu]Cl.O.O1CCOCC1>CC(CC#CCN1CCN(C)CC1)C(=O)N1c2ccccc2C(=O)Nc2cccnc21
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a11989da57094792a3813bfd266f2693
Cl>>Cl.Cl
O=C(C(CC#CCN1CCN(CC1)C)C)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2.Cl>>Cl.Cl.O=C(C(CC#CCN1CCN(CC1)C)C)N1C2=C(NC(C3=C1C=CC=C3)=O)C=CC=N2
[ClH:32]>>[ClH:32].[ClH:33]
Cl
Cl.Cl
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
28 g (0.067 mol) of 5,11-dihydro-11-[1-oxo-2-methyl-6-(4-methyl-1-piperazinyl)-4-hexynyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one are suspended in 350 ml of absolute ethanol and 45 ml of ethereal hydrochloric acid are added with stirring at boiling temperature. A clear solution is obtained at first, which goes cloudy ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
C(C)O
null
null
Cl>C(C)O>Cl.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-aceb139e08c74474b4660ef26669537f
CC(C)(C)c1cc(CCC(N)=O)cc(C(C)(C)C)c1O.O=C(Cl)SCl>>CC(C)(C)c1cc(CCc2nsc(=O)o2)cc(C(C)(C)C)c1O
OC1=C(C=C(C=C1C(C)(C)C)CCC(=O)N)C(C)(C)C.ClC(=O)SCl>>OC1=C(C=C(C=C1C(C)(C)C)CCC1=NSC(O1)=O)C(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([CH2:8][CH2:9][C:10]([NH2:11])=[O:15])[cH:16][c:17]([C:18]([CH3:19])([CH3:20])[CH3:21])[c:22]1[OH:23].Cl[S:12][C:13](Cl)=[O:14]>>[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([CH2:8][CH2:9][c:10]2[n:11][s:12][c:13](=[O:14])[o:15]2)[cH:16][c:17]([C:18]([CH3:19])([CH3:20]...
CC(C)(C)c1cc(CCC(N)=O)cc(C(C)(C)C)c1O.O=C(Cl)SCl
CC(C)(C)c1cc(CCc2nsc(=O)o2)cc(C(C)(C)C)c1O
null
null
C1(=CC=CC=C1)C
Aromatic Heterocycle Formation
OtherReaction
cf2b908c510698a7414ecaa776babe4f8bc22e2ce68209bffd1e189a5ff20552
31356cd529b7c8e4ab7bb0b9ea7ddefab415abb5d70069735affc33ac8027277
O=c1oc(CCc2ccccc2)ns1
Cl-[S;H0;D2;+0:1]-[C;H0;D3;+0:2](-Cl)=[O;D1;H0:3].[C:4]-[C:5]-[C;H0;D3;+0:6](-[NH2;D1;+0:7])=[O;H0;D1;+0:8]>>[C:4]-[C:5]-[c;H0;D3;+0:6]1:[n;H0;D2;+0:7]:[s;H0;D2;+0:1]:[c;H0;D3;+0:2](=[O;D1;H0:3]):[o;H0;D2;+0:8]:1
null
[]
60
CELSIUS
null
null
A suspension of 13.45 grams of 3-[4-hydroxy-3,5-di- tert-butylphenyl]propionamide in 150 ml of toluene is admixed with 20.22 grams of chlorocarbonyl sulfenyl chloride added dropwise. After heating the reaction mixture at 60° C. for 20 hours, the solvent is removed under reduced pressure. The residue is recrystallized f...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amide.Monosulfide
null
null
c1nsco1
c1ccccc1.c1nsco1
HCl
C1(=CC=CC=C1)C
60
null
CC(C)(C)c1cc(CCC(N)=O)cc(C(C)(C)C)c1O.O=C(Cl)SCl>C1(=CC=CC=C1)C>CC(C)(C)c1cc(CCc2nsc(=O)o2)cc(C(C)(C)C)c1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4237d7b249d34c2e8737a3ca18720997
CC(C)(C)c1cc(C(N)=O)cc(C(C)(C)C)c1O.O=C(Cl)SCl>>CC(C)(C)c1cc(-c2nsc(=O)o2)cc(C(C)(C)C)c1O
OC1=C(C=C(C(=O)N)C=C1C(C)(C)C)C(C)(C)C.ClC(=O)SCl>>OC1=C(C=C(C=C1C(C)(C)C)C1=NSC(O1)=O)C(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([C:8]([NH2:9])=[O:13])[cH:14][c:15]([C:16]([CH3:17])([CH3:18])[CH3:19])[c:20]1[OH:21].Cl[S:10][C:11](Cl)=[O:12]>>[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7](-[c:8]2[n:9][s:10][c:11](=[O:12])[o:13]2)[cH:14][c:15]([C:16]([CH3:17])([CH3:18])[CH3:19])[c:20]1[OH:21]
CC(C)(C)c1cc(C(N)=O)cc(C(C)(C)C)c1O.O=C(Cl)SCl
CC(C)(C)c1cc(-c2nsc(=O)o2)cc(C(C)(C)C)c1O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
cf2b908c510698a7414ecaa776babe4f8bc22e2ce68209bffd1e189a5ff20552
31356cd529b7c8e4ab7bb0b9ea7ddefab415abb5d70069735affc33ac8027277
O=c1oc(-c2ccccc2)ns1
Cl-[S;H0;D2;+0:1]-[C;H0;D3;+0:2](-Cl)=[O;D1;H0:3].[NH2;D1;+0:4]-[C;H0;D3;+0:5](=[O;H0;D1;+0:6])-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]>>[O;D1;H0:3]=[c;H0;D3;+0:2]1:[o;H0;D2;+0:6]:[c;H0;D3;+0:5](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[n;H0;D2;+0:4]:[s;H0;D2;+0:1]:1
null
[]
null
null
null
null
The procedure of Example 1 is repeated using 3.03 grams of 4-hydroxy-3,5-di-tert-butylbenzamide and 3.18 grams of chlorocarbonylsulfenyl choride. Recrystallization from toluene:heptane (1:1) affords the title compound as a white crystalline solid: mp 155°-157° C. (dec.). Conditions: See reaction.notes.procedure_details...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amide.Monosulfide
null
null
c1nsco1
c1ccccc1.c1nsco1
HCl
null
null
null
CC(C)(C)c1cc(C(N)=O)cc(C(C)(C)C)c1O.O=C(Cl)SCl>>CC(C)(C)c1cc(-c2nsc(=O)o2)cc(C(C)(C)C)c1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e675a8e1c24342e682f05cf2d84ae06b
CN1c2ccccc2C(c2ccccc2F)=NCC1CN.O=C(O)Cc1c[nH]c2ccccc12>>CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1c[nH]c2ccccc12.O
CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CN.N1C=C(C2=CC=CC=C12)CC(=O)O.Cl.C(C)N=C=NCCCN(C)C>>O.CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CNC(=O)CC2=CNC1=CC=CC=C21
[CH3:1][N:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[F:16])=[N:17][CH2:18][CH:19]1[CH2:20][NH2:21].[C:22](=[O:23])([CH2:24][c:25]1[cH:26][nH:27][c:28]2[cH:29][cH:30][cH:31][cH:32][c:33]12)[OH:34]>>[CH3:1][N:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]([c:10]2[cH:11][cH:12][c...
CN1c2ccccc2C(c2ccccc2F)=NCC1CN.O=C(O)Cc1c[nH]c2ccccc12
CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1c[nH]c2ccccc12.O
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Cc1c[nH]c2ccccc12)NCC1CN=C(c2ccccc2)c2ccccc2N1
[#7;a:1]:[c:2]:[c:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[OH;D1;+0:7].[#7:8]-[C:9]-[C:10]-[NH2;D1;+0:11]>>[#7:8]-[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C:4]-[c:3]:[c:2]:[#7;a:1].[OH2;D0;+0:7]
71.9
[{"value": 71.9, "product": "O.CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CNC(=O)CC2=CNC1=CC=CC=C21", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
According to the method of Example 1, 1-methyl-2-aminomethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (250 mg, 0.88 mmole) and indole-3-acetic acid (154 mg, 0.88 mmole) were combined with 4 ml of dry methylene chloride, and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (169 mg, 0.88 mmole) wa...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
C1=NCC[NH]c2ccccc21.c1ccccc1.c1ccc2[nH]ccc2c1
null
C(Cl)Cl
null
8
CN1c2ccccc2C(c2ccccc2F)=NCC1CN.O=C(O)Cc1c[nH]c2ccccc12>C(Cl)Cl>CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1c[nH]c2ccccc12.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0bc03ba9e5e2470fbc42b20b354ea151
CN1c2ccccc2C(c2ccccc2F)=NCC1CCl.Nc1cccc(C(F)(F)F)c1>>CN1c2ccccc2C(c2ccccc2F)=NCC1CNc1cccc(C(F)(F)F)c1
CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CCl.FC(C=1C=C(N)C=CC1)(F)F.C([O-])([O-])=O.[K+].[K+].[I-].[Na+]>>CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CNC2=CC(=CC=C2)C(F)(F)F
Cl[CH2:20][CH:19]1[N:2]([CH3:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[F:16])=[N:17][CH2:18]1.[NH2:21][c:22]1[cH:23][cH:24][cH:25][c:26]([C:27]([F:28])([F:29])[F:30])[cH:31]1>>[CH3:1][N:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[...
CN1c2ccccc2C(c2ccccc2F)=NCC1CCl.Nc1cccc(C(F)(F)F)c1
CN1c2ccccc2C(c2ccccc2F)=NCC1CNc1cccc(C(F)(F)F)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(NCC2CN=C(c3ccccc3)c3ccccc3N2)cc1
Cl-[CH2;D2;+0:1]-[C:2](-[C:3]-[#7:4])-[#7:5](-[C;D1;H3:6])-[c:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#7:4]-[C:3]-[C:2](-[CH2;D2;+0:1]-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11])-[#7:5](-[C;D1;H3:6])-[c:7]
null
[]
null
null
null
null
According to the method of Example 5, 1-methyl-2-chloromethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (200 mg, 0.66 mmole) and m-trifluoromethyl aniline (319 mg, 1.97 mmole) were combined in 2 ml of dry N,N-dimethylformamide, and potassium carbonate (273 mg, 1.97 mmole) and sodium iodide (198 mg, 1.32 mmo...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
C1=NCC[NH]c2ccccc21.c1ccccc1.c1ccccc1
HCl
CN(C=O)C
null
null
CN1c2ccccc2C(c2ccccc2F)=NCC1CCl.Nc1cccc(C(F)(F)F)c1>CN(C=O)C>CN1c2ccccc2C(c2ccccc2F)=NCC1CNc1cccc(C(F)(F)F)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-554210ee51bc42a99644559814429e25
CC(C)COC(=O)Cl.CN1c2ccccc2C(c2ccccc2F)=NCC1CN>>CC(C)COC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C
CN1CCOCC1.CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CN.ClC(=O)OCC(C)C>>CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CNC(=O)OCC(C)C
Cl[C:6]([O:5][CH2:4][CH:2]([CH3:1])[CH3:3])=[O:7].[NH2:8][CH2:9][CH:10]1[CH2:11][N:12]=[C:13]([c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[F:20])[c:21]2[cH:22][cH:23][cH:24][cH:25][c:26]2[N:27]1[CH3:28]>>[CH3:1][CH:2]([CH3:3])[CH2:4][O:5][C:6](=[O:7])[NH:8][CH2:9][CH:10]1[CH2:11][N:12]=[C:13]([c:14]2[cH:15][cH:16][cH:17]...
CC(C)COC(=O)Cl.CN1c2ccccc2C(c2ccccc2F)=NCC1CN
CC(C)COC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C
null
null
C(Cl)Cl
Protection
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
038720aa61a7efa0f2a9ee6f2e0adf63a9ffdc2be4697c11a6215baef34f97b2
205f353513ce9506ab61831799da8fb73ec2ef5cfa927664496d3ce72c438860
c1ccc(C2=NCCNc3ccccc32)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#7:5]-[C:6]-[C:7]-[NH2;D1;+0:8]>>[#7:5]-[C:6]-[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]
68.2
[{"value": 68.2, "product": "CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CNC(=O)OCC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
According to the method of Example 1, 1-methyl-2-aminomethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (250 mg, 0.88 mmole) and isobutyl chloroformate (114 μl, 0.88 mmole) were combined with 4 ml of dry methylene chloride, and 97 μl of N-methylmorpholine (0.88 mmole) at -5° C. was added to the mixture. The ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Carbamic ester
null
null
c1ccccc1.C1=NCC[NH]c2ccccc21
HCl
C(Cl)Cl
null
null
CC(C)COC(=O)Cl.CN1c2ccccc2C(c2ccccc2F)=NCC1CN>C(Cl)Cl>CC(C)COC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-83875325c1ee4a0ea07fd297824b70f1
CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C>>CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12.CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12.Cl.Cl.Cl.O.O.O
CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CNC(C(CC2=CNC1=CC=CC=C21)NC(=O)OC(C)(C)C)=O.Cl>>O.Cl.Cl.CN1C(CN=C(C2=C1C=CC=C2)C2=C(C=CC=C2)F)CNC(C(CC2=CNC1=CC=CC=C21)N)=O.O.O.CN2C(CN=C(C1=C2C=CC=C1)C1=C(C=CC=C1)F)CNC(C(CC1=CNC2=CC=CC=C12)N)=O.Cl.Cl
[CH3:1][N:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[F:16])=[N:17][CH2:18][CH:19]1[CH2:55][NH:56][C:57](=[O:58])[CH:59]([NH:60][C:22](=[O:23])[O:75][C:47]([CH3:20])([CH3:34])[CH3:48])[CH2:61][c:62]1[cH:63][nH:64][c:65]2[cH:66][cH:67][cH:68][cH:69][c:70]12>>[CH3:1][N:2]1[c:3]...
CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C
CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12.CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12.Cl.Cl.Cl.O.O.O
null
null
C(C)(=O)OCC
Aromatic Heterocycle Formation
OtherReaction
8968ac2f70f8636a6f5d0ecf8299382e98a875ff0d4db68f9dee6e025c153c00
196819a33b21068293125ac03c76555aae00bf0dadf1efc47ec526fe42bdb80a
O=C(CCc1c[nH]c2ccccc12)NCC1CN=C(c2ccccc2)c2ccccc2N1.O=C(CCc1c[nH]c2ccccc12)NCC1CN=C(c2ccccc2)c2ccccc2N1
[C:1]-[C:2](-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[C;H0;D4;+0:7](-[CH3;D1;+0:8])(-[CH3;D1;+0:9])-[CH3;D1;+0:10])-[C:11](=[O;D1;H0:12])-[#7:13]-[CH2;D2;+0:14]-[CH;D3;+0:15](-[C:16]-[#7:17]=[C:18])-[#7:19](-[C;D1;H3:20])-[c:21]>>[#7:22]-[C:23](-[CH2;D2;+0:14]-[#7:13]-[C:11](=[O;D1;H0:12])-[C:2](-[C:1]...
null
[]
0
CELSIUS
null
null
1-Methyl-2-[2-((1,1-dimethylethoxy)carbonyl)amino-3-(1H-indol-3-yl)propanoyl]aminomethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (50 mg, 0.08 mmole) was dissolved in 2 ml of ethyl acetate, cooled to 0° C. and treated with hydrogen chloride gas for 1 hour. The solvent and excess hydrogen chloride were remo...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Aromatic halide.Substituted imine.Secondary amide.Primary amine.Primary amine.Tertiary amine
C1=NCC[NH]c2ccccc21
C1=NCC[NH]c2ccccc21.c1ccc2[nH]ccc2c1.C1=NCC[NH]c2ccccc21.c1ccccc1
C1=NCC[NH]c2ccccc21.c1ccccc1.c1ccc2[nH]ccc2c1.C1=NCC[NH]c2ccccc21.c1ccccc1.c1ccc2[nH]ccc2c1
Other
C(C)(=O)OCC
0
null
CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C>C(C)(=O)OCC>CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12.CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12.Cl.Cl.Cl.O.O.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7b2385246443417da1587de409a23533
Oc1ccccc1>>Oc1ccccc1
CC(C)=C.C1(=CC=CC=C1)O.C(C)(C)(C)C1=C(C=CC=C1)O.C1(=CC=CC=C1)O.C1(=CC=CC=C1)O>>C(C)(C)(C)C1=C(C=CC=C1)O.C1(=CC=CC=C1)O
[OH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[OH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
Oc1ccccc1
Oc1ccccc1
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccccc1
null
null
[]
null
null
null
null
A mixture of tert-butyl phenol and phenol prepared by alkylating phenol with isobutylene to a C4 /phenol ratio of 0.25 to provide a t-butyl phenol/phenol mixture was flash distilled to remove color. The mixture had an average t-butyl:phenyl ratio of about 0.3 (about 25% phenol:75% t-butyl phenols). 360.7 grams of t-but...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
null
null
null
Oc1ccccc1>>Oc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0eba15b633444881a771df4d2bfbd10e
O=C(Cl)C(=O)Cl.O=C(O)Cc1ccc(Cl)cc1>>O=C(Cl)Cc1ccc(Cl)cc1
ClC1=CC=C(C=C1)CC(=O)O.C(C(=O)Cl)(=O)Cl>>ClC1=CC=C(C=C1)CC(=O)Cl
O=C(Cl)C(=O)[Cl:3].O[C:2](=[O:1])[CH2:4][c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]1>>[O:1]=[C:2]([Cl:3])[CH2:4][c:5]1[cH:6][cH:7][c:8]([Cl:9])[cH:10][cH:11]1
O=C(Cl)C(=O)Cl.O=C(O)Cc1ccc(Cl)cc1
O=C(Cl)Cc1ccc(Cl)cc1
null
CN(C=O)C
C(Cl)Cl
Functional Group Interconversion
Alcohol to chloride_Other
013cec2edeb273a7a148f349d36a52d99ff4e7bcf8eed78085df830088e387ac
aedb1f68dc5b7eb0583043e1125b741382b17974140a2f46554f0110e2ddc884
c1ccccc1
Cl-C(=O)-C(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[c:5]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[c:5]
null
[]
null
null
null
null
4-Chlorophenylacetic acid (1.7 g, 10 mmol) and oxalyl chloride (2 ml, 23 mmol) were stirred in 100 ml methylene chloride with two drops of dimethylformamide for two hours. The solvent and excess oxalyl chloride were removed under vacuum to give p-chlorophenylacetyl chloride. The 4-chlorophenylacetyl chloride and 4,4,6,...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Carboxylic acid
Acyl halide
null
null
c1ccccc1
HCl
CN(C=O)C.C(Cl)Cl
null
null
O=C(Cl)C(=O)Cl.O=C(O)Cc1ccc(Cl)cc1>CN(C=O)C.C(Cl)Cl>O=C(Cl)Cc1ccc(Cl)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c1dd4451b34a40baa98f4c9107295354
CC1(C)C(=O)CC(=O)C(C)(C)C1=O.O=C(Cl)Cc1ccc(Cl)cc1>>CC1(C)C(=O)C(C(=O)Cc2ccc(Cl)cc2)C(=O)C(C)(C)C1=O
ClC1=CC=C(C=C1)CC(=O)Cl.CC1(C(CC(C(C1=O)(C)C)=O)=O)C.C(C)N(CC)CC>>ClC1=CC=C(C=C1)CC(=O)C1C(C(C(C(C1=O)(C)C)=O)(C)C)=O
[CH3:1][C:2]1([CH3:3])[C:4](=[O:5])[CH2:6][C:17](=[O:18])[C:19]([CH3:20])([CH3:21])[C:22]1=[O:23].Cl[C:7](=[O:8])[CH2:9][c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1>>[CH3:1][C:2]1([CH3:3])[C:4](=[O:5])[CH:6]([C:7](=[O:8])[CH2:9][c:10]2[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]2)[C:17](=[O:18])[C:19]([CH3:20])([...
CC1(C)C(=O)CC(=O)C(C)(C)C1=O.O=C(Cl)Cc1ccc(Cl)cc1
CC1(C)C(=O)C(C(=O)Cc2ccc(Cl)cc2)C(=O)C(C)(C)C1=O
null
null
C(Cl)Cl
C-C Coupling
OtherReaction
44b16f3124d9704735b41660f61a79407d933597f005f0d8a27803cc59b3b159
d1ef8d6a572be6944eed6d1e50ba23f9d6e95602669b67dac90442aed5304e90
O=C1CC(=O)C(C(=O)Cc2ccccc2)C(=O)C1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[O;D1;H0:5]=[C:6]1-[C:7]-[C:8](=[O;D1;H0:9])-[C:10]-[C:11](=[O;D1;H0:12])-[CH2;D2;+0:13]-1>>[O;D1;H0:5]=[C:6]1-[C:7]-[C:8](=[O;D1;H0:9])-[C:10]-[C:11](=[O;D1;H0:12])-[CH;D3;+0:13]-1-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
null
[]
null
null
30
MINUTE
4-Chlorophenylacetic acid (1.7 g, 10 mmol) and oxalyl chloride (2 ml, 23 mmol) were stirred in 100 ml methylene chloride with two drops of dimethylformamide for two hours. The solvent and excess oxalyl chloride were removed under vacuum to give p-chlorophenylacetyl chloride. The 4-chlorophenylacetyl chloride and 4,4,6,...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ketone.Ketone
Ketone.Ketone.Ketone
C1CCCCC1
C1CCCCC1
C1CCCCC1.c1ccccc1
HCl
C(Cl)Cl
null
0.5
CC1(C)C(=O)CC(=O)C(C)(C)C1=O.O=C(Cl)Cc1ccc(Cl)cc1>C(Cl)Cl>CC1(C)C(=O)C(C(=O)Cc2ccc(Cl)cc2)C(=O)C(C)(C)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8b39f025038f42bb9c0a692743fbf1b9
C=CCCCC.C[Si](C)(C)N=P(=N[Si](C)(C)C)N([Si](C)(C)C)[Si](C)(C)C>>C=CCCCC.C=CCCCCCCCC
C[Si](C)(C)N([Si](C)(C)C)P(=N[Si](C)(C)C)=N[Si](C)(C)C.CCCCC=C>>CCCCCCCCC=C.CCCCC=C
[CH2:4]([CH2:5][CH3:6])[CH2:9][CH:8]=[CH2:7].C[Si](N(P(=N[Si]([CH3:2])([CH3:3])[CH3:12])=N[Si](C)([CH3:1])[CH3:16])[Si]([CH3:11])([CH3:13])[CH3:14])([CH3:10])[CH3:15]>>[CH2:1]=[CH:2][CH2:3][CH2:4][CH2:5][CH3:6].[CH2:7]=[CH:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH3:16]
C=CCCCC.C[Si](C)(C)N=P(=N[Si](C)(C)C)N([Si](C)(C)C)[Si](C)(C)C
C=CCCCC.C=CCCCCCCCC
null
null
CCCCCCCCC=C
C-C Coupling
OtherReaction
5c97663cc59484df51d4ae713931f41e24635e8d16b23eeb265c5150810ce2ac
7089ff7c4563abebd52a1bee7b98fff1f2ed170af78f0e97f731a31027a60280
null
C-[Si](-[CH3;D1;+0:1])(-[CH3;D1;+0:2])-N=P(=N-[Si](-[CH3;D1;+0:3])(-[CH3;D1;+0:4])-[CH3;D1;+0:5])-N(-[Si](-[CH3;D1;+0:6])(-[CH3;D1;+0:7])-[CH3;D1;+0:8])-[Si](-C)(-[CH3;D1;+0:9])-[CH3;D1;+0:10].[C;D1;H2:11]=[C:12]-[CH2;D2;+0:13]-[CH2;D2;+0:14]-[C:15]-[C;D1;H3:16]>>[C;D1;H2:11]=[C:12]-[CH2;D2;+0:13]-[CH2;D2;+0:9]-[CH2;D2...
null
[]
0
CELSIUS
3
HOUR
In a glass vessel pre-conditioned by heating under vacuum and filled with argon 0.34 g (1.24 mmol) of bis(cyclooctadiene-1,5)nickel and 0.46 g (1.25 mmol) of bis(trimethylsilyl)amino-bis(trimethylsilylimino)phosphorane were dissolved in 20 ml of decene-1, and the solution was stirred at 0° C. for 3 hours. Then to the g...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine.Allyl.Silyl protective group.Silyl protective group.Silyl protective group.Silyl protective group
Allyl.Allyl
null
null
null
Other
CCCCCCCCC=C
0
3
C=CCCCC.C[Si](C)(C)N=P(=N[Si](C)(C)C)N([Si](C)(C)C)[Si](C)(C)C>CCCCCCCCC=C>C=CCCCC.C=CCCCCCCCC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ad0a48963d2543e0863f057522180da5
CC(C)N.ClCCc1cc(Cl)ccc1Sc1ccc(Cl)cc1CCCl>>CC(C)NCCSc1ccc(Cl)cc1.Cl
C(Cl)(Cl)Cl.O.ClCCC1=C(C=CC(=C1)Cl)SC1=C(C=C(C=C1)Cl)CCCl.C(C)(C)N>>Cl.ClC1=CC=C(C=C1)SCCNC(C)C
[CH3:1][CH:2]([CH3:3])[NH2:4].Clc1ccc([S:7][c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][c:14]2[CH2:6][CH2:5]Cl)c(CC[Cl:15])c1>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1.[ClH:15]
CC(C)N.ClCCc1cc(Cl)ccc1Sc1ccc(Cl)cc1CCCl
CC(C)NCCSc1ccc(Cl)cc1.Cl
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1d86d3596d2041492b8d73673891c723ec2c0956e8bb9de7bc8e3a9850977867
4858ea9fab1cc5b44bc5feb39f5a6f848b895d40e8e1919c3de421fd1be8a2c4
c1ccccc1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6](-[S;H0;D2;+0:7]-c1:c:c:c(-Cl):c:c:1-C-C-[Cl;H0;D1;+0:8]):[c:9].[C;D1;H3:10]-[C:11](-[C;D1;H3:12])-[NH2;D1;+0:13]>>[C;D1;H3:10]-[C:11](-[C;D1;H3:12])-[NH;D2;+0:13]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[S;H0;D2;+0:7]-[c:6](:[c:9]):[cH;D2;+0:3]:[c:4]:[c:5].[ClH;D0;+...
null
[]
null
null
null
null
A solution of 24.0 g (0.116 mole) chloroethyl-p-chlorophenyl sulfide in 100 ml of isopropylamine was agitated overnight in a stainless steel bomb at 80° C. The reaction mixture was then stripped to dryness and the residue partitioned between water and chloroform. The chloroform layer was extracted with 1N sulfuric acid...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary halide.Primary halide.Primary amine.Monosulfide
Secondary amine.Monosulfide
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1
HCl
null
null
null
CC(C)N.ClCCc1cc(Cl)ccc1Sc1ccc(Cl)cc1CCCl>>CC(C)NCCSc1ccc(Cl)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1fcdce9b06cf4aeaa6aaa374d1411429
CC(C)NCCSc1ccc(Cl)cc1>>CC(C)NCCS(=O)c1ccc(Cl)cc1
ClC1=CC=C(C=C1)SCCNC(C)C.B(=O)O[O-].[Na+].[OH-].[Na+]>>ClC1=CC=C(C=C1)S(=O)CCNC(C)C
[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7][c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1
CC(C)NCCSc1ccc(Cl)cc1
CC(C)NCCS(=O)c1ccc(Cl)cc1
null
null
S(O)(O)(=O)=O
Oxidation
Sulfanyl to sulfinyl
9edfaf6d72a81452ea8e3a1cdcb10a58409fff36608e97019e7273998b3d5373
f5f6bb6ca76a2267cd589767b4d67e7a17ab1ac383eeb6143dcd5d92e00e1b6a
c1ccccc1
[C:1]-[C:2]-[S;H0;D2;+0:3]-[c:4](:[c:5]):[c:6]>>[C:1]-[C:2]-[S;H0;D3;+0:3](=[O;D1;H0:7])-[c:4](:[c:5]):[c:6]
90.6
[{"value": 90.6, "product": "ClC1=CC=C(C=C1)S(=O)CCNC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 15.05 g (0.066 mole) of N-[2-[(4-chlorophenyl)thio]ethyl]-1-methylethanamine and 12.0 g (0.0779 mole) of sodium perborate in 400 ml of 1M sulfuric acid was stirred at room temperature for about 18 hr. The solution was made basic with 50% sodium hydroxide and the basic solution was extracted with methylene...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Sulfoxide
null
null
c1ccccc1
null
S(O)(O)(=O)=O
null
null
CC(C)NCCSc1ccc(Cl)cc1>S(O)(O)(=O)=O>CC(C)NCCS(=O)c1ccc(Cl)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a8eb42d4c700427bb2f6aedd4d4b659d
O=C1NC(=O)c2ccccc21.O=S(=O)(CCCCl)c1ccc(Cl)cc1>>O=C1c2ccccc2C(=O)N1CCCS(=O)(=O)c1ccc(Cl)cc1
ClCCCS(=O)(=O)C1=CC=C(C=C1)Cl.C1(C=2C(C(N1)=O)=CC=CC2)=O.[K]>>ClC1=CC=C(C=C1)S(=O)(=O)CCCN1C(C2=CC=CC=C2C1=O)=O
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[NH:11]1.Cl[CH2:12][CH2:13][CH2:14][S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][c:21]([Cl:22])[cH:23][cH:24]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][c:21]([...
O=C1NC(=O)c2ccccc21.O=S(=O)(CCCCl)c1ccc(Cl)cc1
O=C1c2ccccc2C(=O)N1CCCS(=O)(=O)c1ccc(Cl)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2022cc53c1563230994721760c16c873bbdd2982bbfbeeef5b40885f32de1173
ed5b40ca5c14bda1cdc43d7e7526ae39e9e787b52b58ca2afd56239c19d62539
O=C1c2ccccc2C(=O)N1CCCS(=O)(=O)c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[O;D1;H0:4]=[C:5]1-[NH;D2;+0:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6]1-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-[C:5]-1=[O;D1;H0:4]
null
[]
null
null
8
HOUR
A solution of 17.8 g (0.07 mole) of 1-chloro-3-(p-chlorophenylsulfonyl)propane and 15.2 g (0.082 mole) of potassium phthalimide in 300 ml of dimethylformamide was stirred at 90°-110° C. for 2 hr and then quenched in water. The mixture was extracted with methylene chloride and the methylene chloride layer dried over mag...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Unsubstituted dicarboximide
Substituted dicarboximide
c1ccc2c(c1)CNC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccccc1
HCl
CN(C=O)C
null
8
O=C1NC(=O)c2ccccc21.O=S(=O)(CCCCl)c1ccc(Cl)cc1>CN(C=O)C>O=C1c2ccccc2C(=O)N1CCCS(=O)(=O)c1ccc(Cl)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c0e824ff2ea84ee0a559f8efc8f63b92
CC(C)NCCSc1cccc2ccccc12.[O-]B1OO1>>CC(C)NCCS(=O)c1cccc2ccccc12
Cl.CC(C)NCCSC1=CC=CC2=CC=CC=C12.B1(OO1)[O-].O.O.O.O.[Na+].[OH-].[Na+]>>Cl.CC(C)NCCS(=O)C1=CC=CC2=CC=CC=C12
[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7][c:9]1[cH:10][cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12.O1OB1[O-:8]>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12
CC(C)NCCSc1cccc2ccccc12.[O-]B1OO1
CC(C)NCCS(=O)c1cccc2ccccc12
null
null
S(O)(O)(=O)=O
Oxidation
OtherReaction
bebc0a9c46895b64479ca506248015f6e3b2f5ce39f30517ca71f796faa475a6
099322fb111e24ec324e6fad75d493a762ca0cd5af0df8c6f3bfd25c910b45a8
c1ccc2ccccc2c1
[C:1]-[C:2]-[S;H0;D2;+0:3]-[c:4](:[c:5]):[c:6].[O-;H0;D1:7]-B1-O-O-1>>[C:1]-[C:2]-[S;H0;D3;+0:3](=[O;H0;D1;+0:7])-[c:4](:[c:5]):[c:6]
9.1
[{"value": 9.1, "product": "Cl.CC(C)NCCS(=O)C1=CC=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 8.6, "product": "Cl.CC(C)NCCS(=O)C1=CC=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 12.0 g (0.043 mole) of 1-methyl-N-[2-(1-naphthalenylthio)ethyl]ethanamine hydrochloride and 19.7 g (0.028 mole) of sodium perborate tetrahydrate in 500 ml of 2N sulfuric acid was stirred overnight at room temperature. The solution was poured over ice and the mixture was made alkaline with 50% sodium hydro...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Monosulfide
Sulfoxide
B1OO1
null
c1ccc2ccccc2c1
B
S(O)(O)(=O)=O
null
null
CC(C)NCCSc1cccc2ccccc12.[O-]B1OO1>S(O)(O)(=O)=O>CC(C)NCCS(=O)c1cccc2ccccc12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cc9151e5ad6b4f33b85396bdbeeebe64
CS(=O)(=O)Cl.OCCSc1ccc(Cl)c(Cl)c1>>CS(=O)(=O)OCCSc1ccc(Cl)c(Cl)c1
ClC=1C=C(C=CC1Cl)SCCO.C(C)N(CC)CC.CS(=O)(=O)Cl>>ClC=1C=C(C=CC1Cl)SCCOS(=O)(=O)C
Cl[S:2]([CH3:1])(=[O:3])=[O:4].[OH:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[c:14]([Cl:15])[cH:16]1>>[CH3:1][S:2](=[O:3])(=[O:4])[O:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[c:14]([Cl:15])[cH:16]1
CS(=O)(=O)Cl.OCCSc1ccc(Cl)c(Cl)c1
CS(=O)(=O)OCCSc1ccc(Cl)c(Cl)c1
null
null
C1=CC=CC=C1
Acylation
Formation of Sulfonic Esters
2fa969eb2c954bb96793348a1b2335ec63fbd290dadec6e3e02295e1768e64cf
cb77b899e4adf980b1def97230ef2861660fd7f9602260ec64747d9afd3a795a
c1ccccc1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]
null
[]
null
null
8
HOUR
To a solution of 117.97 g (0.53 mole) of 2-[(3,4-dichlorophenyl)thio]ethanol (prepared by reacting 3,4-dichlorothiophenol and 2-chloroethanol) and 53.5 g (0.53 mole) of triethylamine in 500 ml of benzene was added dropwise a benzene solution of 60.9 g (0.53 mole) of methanesulfonyl chloride over a one hour period with ...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Mesylate
null
null
c1ccccc1
HCl
C1=CC=CC=C1
null
8
CS(=O)(=O)Cl.OCCSc1ccc(Cl)c(Cl)c1>C1=CC=CC=C1>CS(=O)(=O)OCCSc1ccc(Cl)c(Cl)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e9ac2303bc5d496eaac98b7e1bc15dcc
CC(C)N.CS(=O)(=O)OCCSc1ccc(Cl)c(Cl)c1>>CC(C)NCCSc1ccc(Cl)c(Cl)c1.Cl
ClC=1C=C(C=CC1Cl)SCCOS(=O)(=O)C.C(C)(C)N>>Cl.ClC=1C=C(C=CC1Cl)SCCNC(C)C
[CH3:1][CH:2]([CH3:3])[NH2:4].CS(=O)(=O)O[CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[c:13]([Cl:14])[cH:15]1>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[c:13]([Cl:14])[cH:15]1.[ClH:16]
CC(C)N.CS(=O)(=O)OCCSc1ccc(Cl)c(Cl)c1
CC(C)NCCSc1ccc(Cl)c(Cl)c1.Cl
null
null
null
Heteroatom Alkylation and Arylation
Alkylation of amines
8445343b2fb2fd8a9bc06f8532794f2ba6b99565a6e05a3bb9a4344ce2671186
7e6303acde8be57b43b4c6a673e1c7537b1efde90f08932e09e153dbba53a700
c1ccccc1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]-[#16:3].[C;D1;H3:4]-[C:5](-[C;D1;H3:6])-[NH2;D1;+0:7]>>[#16:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:7]-[C:5](-[C;D1;H3:4])-[C;D1;H3:6]
null
[]
null
null
null
null
A solution of 151.46 g (0.548 mole) of methanesulfonic acid[2-[(3,4-dichlorophenyl)thio]ethyl]ester in 100 ml of isopropylamine was heated overnight in a bomb at 100° C. The isopropylamine was removed in a rotary evaporator and the residue partitioned between chloroform and 5% sodium hydroxide. The chloroform was remov...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Primary amine
Secondary amine
null
null
c1ccccc1
HO-
null
null
null
CC(C)N.CS(=O)(=O)OCCSc1ccc(Cl)c(Cl)c1>>CC(C)NCCSc1ccc(Cl)c(Cl)c1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ce8e45175ab64e68b2f9eff595f3864a
ClCCCSc1ccccc1.O=C1NC(=O)c2ccccc21>>O=C1c2ccccc2C(=O)N1CCCSc1ccccc1
ClCCCSC1=CC=CC=C1.C1(C=2C(C(N1)=O)=CC=CC2)=O.[K]>>C1(=CC=CC=C1)SCCCN1C(C2=CC=CC=C2C1=O)=O
Cl[CH2:12][CH2:13][CH2:14][S:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1.[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[NH:11]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][S:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
ClCCCSc1ccccc1.O=C1NC(=O)c2ccccc21
O=C1c2ccccc2C(=O)N1CCCSc1ccccc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2022cc53c1563230994721760c16c873bbdd2982bbfbeeef5b40885f32de1173
ed5b40ca5c14bda1cdc43d7e7526ae39e9e787b52b58ca2afd56239c19d62539
O=C1c2ccccc2C(=O)N1CCCSc1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[O;D1;H0:4]=[C:5]1-[NH;D2;+0:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6]1-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-[C:5]-1=[O;D1;H0:4]
63.8
[{"value": 63.8, "product": "C1(=CC=CC=C1)SCCCN1C(C2=CC=CC=C2C1=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.8, "product": "C1(=CC=CC=C1)SCCCN1C(C2=CC=CC=C2C1=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 32.86 g (0.177 mole) of 1-chloro-3-(phenylthio)propane and 33.7 g (0.182 mole) of potassium phthalimide in 500 ml of dimethylformamide was stirred at 80° C. for 19 hr. The dimethylformamide was removed in vacuo. The residue was dissolved in methylene chloride and the resulting solution extracted with seve...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Unsubstituted dicarboximide
Substituted dicarboximide
c1ccc2c(c1)CNC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccccc1
HCl
CN(C=O)C
null
null
ClCCCSc1ccccc1.O=C1NC(=O)c2ccccc21>CN(C=O)C>O=C1c2ccccc2C(=O)N1CCCSc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3899e2d65d6d4b47ba44772811d58aca
CC(C)N.O=S(=O)(CCCCl)c1ccccc1>>CC(C)NCCCS(=O)(=O)c1ccccc1.Cl
ClCCCS(=O)(=O)C1=CC=CC=C1.C(C)(C)N>>Cl.CC(C)NCCCS(=O)(=O)C1=CC=CC=C1
[CH3:1][CH:2]([CH3:3])[NH2:4].[CH2:5]([CH2:6][CH2:7][S:8](=[O:9])(=[O:10])[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[Cl:17]>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][CH2:7][S:8](=[O:9])(=[O:10])[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1.[ClH:17]
CC(C)N.O=S(=O)(CCCCl)c1ccccc1
CC(C)NCCCS(=O)(=O)c1ccccc1.Cl
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccccc1
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])-[NH2;D1;+0:4].[C:5]-[C:6]-[CH2;D2;+0:7]-[Cl;H0;D1;+0:8]>>[C:5]-[C:6]-[CH2;D2;+0:7]-[NH;D2;+0:4]-[C:2](-[C;D1;H3:1])-[C;D1;H3:3].[ClH;D0;+0:8]
null
[]
null
null
null
null
A solution of 66.55 g (0.3052 mole) of 3-chloropropylphenyl sulfone (prepared by reacting m-chloroperoxybenzoic acid and 3-chloropropyl phenylsulfide in methylene chloride) in 200 ml of isopropylamine was heated at 100° C. overnight in a bomb. The isopropylamine was removed by rotary evaporation and the residue partiti...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1
null
null
null
null
CC(C)N.O=S(=O)(CCCCl)c1ccccc1>>CC(C)NCCCS(=O)(=O)c1ccccc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ac7bb16995024c46a7800aead047370a
CC(C)N(CCS(=O)(=O)c1ccc(Cl)c(Cl)c1)C(=O)Oc1ccccc1>>CC(C)NCCS(=O)(=O)c1ccc(Cl)c(Cl)c1
C1(=CC=CC=C1)OC(N(C(C)C)CCS(=O)(=O)C1=CC(=C(C=C1)Cl)Cl)=O>>ClC=1C=C(C=CC1Cl)S(=O)(=O)CCNC(C)C
O=C(Oc1ccccc1)[N:4]([CH:2]([CH3:1])[CH3:3])[CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][c:13]([Cl:14])[c:15]([Cl:16])[cH:17]1>>[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][c:13]([Cl:14])[c:15]([Cl:16])[cH:17]1
CC(C)N(CCS(=O)(=O)c1ccc(Cl)c(Cl)c1)C(=O)Oc1ccccc1
CC(C)NCCS(=O)(=O)c1ccc(Cl)c(Cl)c1
null
null
Br
Reduction
Hydrogenolysis of tertiary amines
709a03512f2b36af470a6c002bf594696c9a8d9f4ff0ae82dddda03c8a91a358
20c36f41eeb07c3ba4437b51ba72e8ff3c22d0b27e7197b0e9af3127f331149f
c1ccccc1
O=C(-O-c1:c:c:c:c:c:1)-[N;H0;D3;+0:1](-[C:2]-[C:3])-[C:4](-[C;D1;H3:5])-[C;D1;H3:6]>>[C:3]-[C:2]-[NH;D2;+0:1]-[C:4](-[C;D1;H3:5])-[C;D1;H3:6]
32.4
[{"value": 32.4, "product": "ClC=1C=C(C=CC1Cl)S(=O)(=O)CCNC(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 44.27 g (0.107 mole of N-[2-[(3,4-dichlorophenyl)sulfonyl]ethyl]-N-(1-methylethyl)carbamic acid phenyl ester in 300 ml of 48% HBr was heated at reflux for 12 hr. The reaction mixture was cooled to room temperature, made alkaline with 50% sodium hydroxide-ice and extracted with chloroform. The chloroform l...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether
Secondary amine
c1ccccc1
null
c1ccccc1
HO-
Br
null
null
CC(C)N(CCS(=O)(=O)c1ccc(Cl)c(Cl)c1)C(=O)Oc1ccccc1>Br>CC(C)NCCS(=O)(=O)c1ccc(Cl)c(Cl)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5d2d6d1bd4bb4895b8b561dcce002bb1
CC(C)(N)CCSc1ccc(F)cc1.O=C(Cl)Oc1ccccc1>>CC(C)N(CCSc1ccc(F)cc1)C(=O)Oc1ccccc1
ClC(=O)OC1=CC=CC=C1.C(Cl)Cl.FC1=CC=C(C=C1)SCCC(C)(N)C.C(C)N(CC)CC.C(Cl)Cl>>C1(=CC=CC=C1)OC(N(C(C)C)CCSC1=CC=C(C=C1)F)=O
[CH3:1][C:2]([CH3:3])([NH2:4])[CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][c:11]([F:12])[cH:13][cH:14]1.Cl[C:15](=[O:16])[O:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][CH:2]([CH3:3])[N:4]([CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][c:11]([F:12])[cH:13][cH:14]1)[C:15](=[O:16])[O:17][c:18]1[cH:19][cH:20][cH:21][cH:22][c...
CC(C)(N)CCSc1ccc(F)cc1.O=C(Cl)Oc1ccccc1
CC(C)N(CCSc1ccc(F)cc1)C(=O)Oc1ccccc1
null
null
null
Protection
OtherReaction
a42633a79ab98a6c6618a6a985c9ef85d612db2a3108c005e1fc58b635172b16
c7c30c8e119de916171bede109f693a93326df60c194f5e0a34518c63f4ffc24
O=C(NCCSc1ccccc1)Oc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4].[#16:5]-[C:6]-[CH2;D2;+0:7]-[C;H0;D4;+0:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[NH2;D1;+0:11]>>[#16:5]-[C:6]-[CH2;D2;+0:7]-[N;H0;D3;+0:11](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[c:4])-[CH;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10]
null
[]
null
null
8
HOUR
To a solution of 38.5 g (0.15 mole) of N-[2-(4-fluorophenylthio]ethyl-1-methyl-ethanamine and 15.5 g (0.15 mole) of triethylamine in 300 ml of methylene chloride which was cooled in an ice bath was added dropwise with stirring a solution of 23.5 g (0.15 mole) of phenyl chloroformate in 100 ml of methylene chloride over...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary amine
Carbamic ester.Ether
null
null
c1ccccc1.c1ccccc1
HCl
null
null
8
CC(C)(N)CCSc1ccc(F)cc1.O=C(Cl)Oc1ccccc1>>CC(C)N(CCSc1ccc(F)cc1)C(=O)Oc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b9c7f498abcf44048992767b6acc95b5
CC(C)N(CCS(=O)(=O)c1ccc(F)cc1)C(=O)Oc1ccccc1.ClCCl>>CC(C)NCCS(=O)(=O)c1ccc(F)cc1.Cl
C1(=CC=CC=C1)OC(N(C(C)C)CCS(=O)(=O)C1=CC=C(C=C1)F)=O.[OH-].[Na+].C(Cl)Cl>>Cl.FC1=CC=C(C=C1)S(=O)(=O)CCNC(C)C
O=C(Oc1ccccc1)[N:4]([CH:2]([CH3:1])[CH3:3])[CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]1.ClC[Cl:17]>>[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][c:13]([F:14])[cH:15][cH:16]1.[ClH:17]
CC(C)N(CCS(=O)(=O)c1ccc(F)cc1)C(=O)Oc1ccccc1.ClCCl
CC(C)NCCS(=O)(=O)c1ccc(F)cc1.Cl
null
null
CO.Br
Miscellaneous
OtherReaction
1e3af0eec45bbe3bcf3b649e925407a5e4d014627901b089faf032374572d852
3359bcd5552243e6ac1c05029938c325e73803d6c6cb6bada5dcc73b6e54effe
c1ccccc1
Cl-C-[Cl;H0;D1;+0:1].O=C(-O-c1:c:c:c:c:c:1)-[N;H0;D3;+0:2](-[C:3]-[C:4])-[C:5](-[C;D1;H3:6])-[C;D1;H3:7]>>[C:4]-[C:3]-[NH;D2;+0:2]-[C:5](-[C;D1;H3:6])-[C;D1;H3:7].[ClH;D0;+0:1]
null
[]
null
null
null
null
A solution of 60.25 g (0.165 mole) of N-[2-[(4-fluorophenyl)sulfonyl]ethyl]-N-(1-methylethyl)carbamic acid phenyl ester in 400 ml of 48% HBr was heated at reflux for 8 hr. The reaction mixture was cooled with ice and made alkaline with 50% sodium hydroxide. The aqueous phase was extracted with chloroform. The chlorofor...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Carbamic ester.Ether
Secondary amine
c1ccccc1
null
c1ccccc1
HCl
CO.Br
null
null
CC(C)N(CCS(=O)(=O)c1ccc(F)cc1)C(=O)Oc1ccccc1.ClCCl>CO.Br>CC(C)NCCS(=O)(=O)c1ccc(F)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6acd335397af4423ab4dfd5c48ff189b
O=C1NC(=O)c2ccccc21.O=S(=O)(CCCl)c1ccccc1>>O=C1c2ccccc2C(=O)N1CCS(=O)(=O)c1ccccc1
ClCCS(=O)(=O)C1=CC=CC=C1.C1(C=2C(C(N1)=O)=CC=CC2)=O.[K]>>C1(=CC=CC=C1)S(=O)(=O)CCN1C(C2=CC=CC=C2C1=O)=O
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[NH:11]1.Cl[CH2:12][CH2:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1
O=C1NC(=O)c2ccccc21.O=S(=O)(CCCl)c1ccccc1
O=C1c2ccccc2C(=O)N1CCS(=O)(=O)c1ccccc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2022cc53c1563230994721760c16c873bbdd2982bbfbeeef5b40885f32de1173
ed5b40ca5c14bda1cdc43d7e7526ae39e9e787b52b58ca2afd56239c19d62539
O=C1c2ccccc2C(=O)N1CCS(=O)(=O)c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[#16:3].[O;D1;H0:4]=[C:5]1-[NH;D2;+0:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-1>>[#16:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6]1-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-[C:5]-1=[O;D1;H0:4]
35.7
[{"value": 35.7, "product": "C1(=CC=CC=C1)S(=O)(=O)CCN1C(C2=CC=CC=C2C1=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 30.7 g (0.15 mole) of 2-chloroethylphenylsulfone and 69.5 g (0.375 mole) of potassium phthalimide in 600 ml of dimethylformamide was heated overnight at 85° C. The reaction mixture was stripped to dryness and the residue was partitioned between water and chloroform. The chloroform layer was dried and filt...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Unsubstituted dicarboximide
Substituted dicarboximide
c1ccc2c(c1)CNC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccccc1
HCl
CN(C=O)C
null
null
O=C1NC(=O)c2ccccc21.O=S(=O)(CCCl)c1ccccc1>CN(C=O)C>O=C1c2ccccc2C(=O)N1CCS(=O)(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ff66ca3284074b0b8a71d6f999b087a9
O=C1c2ccccc2C(=O)N1CCS(=O)(=O)c1ccccc1>>NCCS(=O)(=O)c1ccccc1
C1(=CC=CC=C1)S(=O)(=O)CCN1C(C2=CC=CC=C2C1=O)=O.O.NN.Cl>>Cl.C1(=CC=CC=C1)S(=O)(=O)CCN
O=C1c2ccccc2C(=O)[N:2]1[CH2:3][CH2:4][S:5](=[O:6])(=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[NH2:2][CH2:3][CH2:4][S:5](=[O:6])(=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
O=C1c2ccccc2C(=O)N1CCS(=O)(=O)c1ccccc1
NCCS(=O)(=O)c1ccccc1
null
null
C(C)O
Reduction
Phthalimide deprotection
d9f63cee80ef758bd939ff2a10772447b3092f1576180488281833a98eb1691a
dbfe4201a9328005dfaec4c3f363ddbb4ef3c9b825f648735dc97b2b57396333
c1ccccc1
O=C1-[N;H0;D3;+0:1](-[C:2]-[C:3])-C(=O)-c2:c:c:c:c:c:2-1>>[C:3]-[C:2]-[NH2;D1;+0:1]
40.5
[{"value": 40.5, "product": "Cl.C1(=CC=CC=C1)S(=O)(=O)CCN", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 32.3 g (0.102 mole) of 2-[2-(phenylsulfonyl)ethyl]-1H-isoindole-1,3-(2H)-dione and 11.8 g (0.2 mole) of 85% hydrazine hydrate in 500 ml of absolute ethanol was refluxed for 6 hr. The reaction mixture was cooled to room temperature, filtered and concentrated. The concentrate was dissolved in chloroform and...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Primary amine
c1ccc2c(c1)C[NH]C2
null
c1ccccc1
HO-
C(C)O
null
null
O=C1c2ccccc2C(=O)N1CCS(=O)(=O)c1ccccc1>C(C)O>NCCS(=O)(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fb82c5ce9e9d4fb38a0048e765370c2d
CC(C)N(CCS(=O)(=O)c1ccc(Cl)c(Cl)c1)C(=O)Oc1ccccc1.CC(C)N(CCS(=O)(=O)c1ccc(Cl)cc1)C(=O)Oc1ccccc1>>CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.Cl
C1(=CC=CC=C1)OC(N(C(C)C)CCS(=O)(=O)C1=CC=C(C=C1)Cl)=O.C1(=CC=CC=C1)OC(N(C(C)C)CCS(=O)(=O)C1=CC(=C(C=C1)Cl)Cl)=O>>Cl.ClC1=CC=C(C=C1)S(=O)(=O)CCNC(C)C
CC(C)N(CCS(=O)(=O)c1ccc(Cl)c([Cl:17])c1)C(=O)Oc1ccccc1.O=C(Oc1ccccc1)[N:4]([CH:2]([CH3:1])[CH3:3])[CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][c:13]([Cl:14])[cH:15][cH:16]1>>[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][c:13]([Cl:14])[cH:15][cH:16]1.[ClH:17]
CC(C)N(CCS(=O)(=O)c1ccc(Cl)c(Cl)c1)C(=O)Oc1ccccc1.CC(C)N(CCS(=O)(=O)c1ccc(Cl)cc1)C(=O)Oc1ccccc1
CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.Cl
null
null
null
Miscellaneous
OtherReaction
39ab2d8b53fe99c862a1c70f1614b8c6491ecef0516bee7b8c04d8bf4b2a1cdf
1880bffaf232174b62dff529914e28dcd990da054d75043261a3bbf09bf32805
c1ccccc1
C-C(-C)-N(-C-C-S(=O)(=O)-c1:c:c:c(-Cl):c(-[Cl;H0;D1;+0:1]):c:1)-C(=O)-O-c1:c:c:c:c:c:1.O=C(-O-c1:c:c:c:c:c:1)-[N;H0;D3;+0:2](-[C:3]-[C:4])-[C:5](-[C;D1;H3:6])-[C;D1;H3:7]>>[C:4]-[C:3]-[NH;D2;+0:2]-[C:5](-[C;D1;H3:6])-[C;D1;H3:7].[ClH;D0;+0:1]
null
[]
null
null
null
null
When in the procedure of Preparation 29, N-[2-[(4-chlorophenyl)sulfonyl]ethyl]-N-(1-methylethyl)carbamic acid phenyl ester is substituted for N-[2-[(3,4-dichlorophenyl)sulfonyl]ethyl]-N-(1-methylethyl)carbamic acid phenyl ester, the title compound is obtained. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Carbamic ester.Carbamic ester.Ether.Ether.Sulfone
Secondary amine
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1
HCl
null
null
null
CC(C)N(CCS(=O)(=O)c1ccc(Cl)c(Cl)c1)C(=O)Oc1ccccc1.CC(C)N(CCS(=O)(=O)c1ccc(Cl)cc1)C(=O)Oc1ccccc1>>CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ae4c77ae86b04fcaa9012d4cce7a5a3a
CN.O=S(=O)(CCCl)c1ccccc1>>CNCCS(=O)(=O)c1ccccc1
ClCCS(=O)(=O)C1=CC=CC=C1.CN>>CNCCS(=O)(=O)C1=CC=CC=C1
[CH3:1][NH2:2].Cl[CH2:3][CH2:4][S:5](=[O:6])(=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][NH:2][CH2:3][CH2:4][S:5](=[O:6])(=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
CN.O=S(=O)(CCCl)c1ccccc1
CNCCS(=O)(=O)c1ccccc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[#16:3].[C;D1;H3:4]-[NH2;D1;+0:5]>>[#16:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:5]-[C;D1;H3:4]
null
[]
null
null
null
null
A solution of 2-chloroethylphenyl sulfone and a large excess of methylamine (40% solution in water) in acetonitrile is stirred at room temperature overnight. The solvent is removed in vacuo and the residue is partitioned between methylene chloride and dilute sodium hydroxide. The methylene chloride solution is extracte...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1
HCl
C(C)#N
null
null
CN.O=S(=O)(CCCl)c1ccccc1>C(C)#N>CNCCS(=O)(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e0ed1f7a66854e2588702449ee9bd2ce
CC(C)N(CCCl)C(C)C.O=C1NC(=O)c2ccccc21>>CC(C)N(CCN1C(=O)c2ccccc2C1=O)C(C)C
Cl.C(C)(C)N(CCCl)C(C)C.C1(C=2C(C(N1)=O)=CC=CC2)=O.[K]>>Cl.CC(C)N(C(C)C)CCN1C(C2=CC=CC=C2C1=O)=O
Cl[CH2:6][CH2:5][N:4]([CH:2]([CH3:1])[CH3:3])[CH:18]([CH3:19])[CH3:20].[NH:7]1[C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[C:16]1=[O:17]>>[CH3:1][CH:2]([CH3:3])[N:4]([CH2:5][CH2:6][N:7]1[C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[C:16]1=[O:17])[CH:18]([CH3:19])[CH3:20]
CC(C)N(CCCl)C(C)C.O=C1NC(=O)c2ccccc21
CC(C)N(CCN1C(=O)c2ccccc2C1=O)C(C)C
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2022cc53c1563230994721760c16c873bbdd2982bbfbeeef5b40885f32de1173
ed5b40ca5c14bda1cdc43d7e7526ae39e9e787b52b58ca2afd56239c19d62539
O=C1NC(=O)c2ccccc21
Cl-[CH2;D2;+0:1]-[C:2]-[#7:3].[O;D1;H0:4]=[C:5]1-[NH;D2;+0:6]-[C:7](=[O;D1;H0:8])-[c:9]:[c:10]-1>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6]1-[C:5](=[O;D1;H0:4])-[c:10]:[c:9]-[C:7]-1=[O;D1;H0:8]
62.3
[{"value": 62.3, "product": "Cl.CC(C)N(C(C)C)CCN1C(C2=CC=CC=C2C1=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 6.7, "product": "Cl.CC(C)N(C(C)C)CCN1C(C2=CC=CC=C2C1=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-diisopropylaminoethyl chloride hydrochloride (40.0 g, 0.2 mole) and potassium phthalimide (74.0 g, 0.4 mole) as stirred overnight at 85° C. in 500 ml of dimethyl formamide. The reaction mixture was stirred to dryness on a rotary evaporator, and the residue was partitioned between chloroform and water. T...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Unsubstituted dicarboximide
Substituted dicarboximide
c1ccc2c(c1)CNC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HCl
CN(C=O)C
null
null
CC(C)N(CCCl)C(C)C.O=C1NC(=O)c2ccccc21>CN(C=O)C>CC(C)N(CCN1C(=O)c2ccccc2C1=O)C(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d69cadb84c1f457aa9645d6fe5e18d9e
CC(C)N(CCN1C(=O)c2ccccc2C1=O)C(C)C.Cl>>CC(C)N(CCN)C(C)C.Cl
C1(=C(C(=C(C(=C1F)F)F)N)F)N.Cl.Cl.CC(C)N(C(C)C)CCN1C(C2=CC=CC=C2C1=O)=O.O.NN>>Cl.Cl.CC(C)N(CCN)C(C)C
O=C1c2ccccc2C(=O)[N:7]1[CH2:6][CH2:5][N:4]([CH:2]([CH3:1])[CH3:3])[CH:8]([CH3:9])[CH3:10].[ClH:12]>>[CH3:1][CH:2]([CH3:3])[N:4]([CH2:5][CH2:6][NH2:7])[CH:8]([CH3:9])[CH3:10].[ClH:12]
CC(C)N(CCN1C(=O)c2ccccc2C1=O)C(C)C.Cl
CC(C)N(CCN)C(C)C.Cl
null
null
C(C)O.CO
Miscellaneous
OtherReaction
cd703f280330e7612c3c3b2e3cc2f8f9332381f29a1fd88b2de2a38281774976
febc1d4b7b44ea3f7762312e158d5ab0fc0ca67ce6d66e23a51e3baafdb353e3
null
O=C1-[N;H0;D3;+0:1](-[C:2]-[C:3])-C(=O)-c2:c:c:c:c:c:2-1>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
8
HOUR
A solution of 40.54 g (0.148 mole) of 2-[2-[[N,N-bis(1-methylethyl)amino]ethyl]-2H-isoindole-1,3-dione and hydrazine hydrate (85%, 11.8 g, 0.2 mole) in 400 ml of 95% ethanol was heated at reflux for 5 hours. The reaction mixture was allowed to cool to room temperature while standing overnight. A white solid formed. The...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Primary amine
c1ccc2c(c1)C[NH]C2
null
null
HO-
C(C)O.CO
null
8
CC(C)N(CCN1C(=O)c2ccccc2C1=O)C(C)C.Cl>C(C)O.CO>CC(C)N(CCN)C(C)C.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5b62d5e0639c4fe99fa536f8aadfd356
CCN(CC)CC.CCOCC.NCCc1ccccc1.O=S(=O)(CCCl)c1ccccc1>>Cl.Cl.O.O=S(=O)(CCNCCc1ccccc1)c1ccccc1.O=S(=O)(CCNCCc1ccccc1)c1ccccc1
CCOCC.ClCCS(=O)(=O)C1=CC=CC=C1.C(CC1=CC=CC=C1)N.C(C)N(CC)CC>>O.Cl.C1(=CC=CC=C1)S(=O)(=O)CCNCCC1=CC=CC=C1.C1(=CC=CC=C1)S(=O)(=O)CCNCCC1=CC=CC=C1.Cl
[CH2:8]([N:9]([CH2:10][CH3:15])[CH2:13][CH3:14])[CH3:16].[O:3]([CH2:12][CH3:11])[CH2:17][CH3:38].[NH2:29][CH2:30][CH2:31][c:32]1[cH:33][cH:34][cH:35][cH:36][cH:37]1.[Cl:1][CH2:28][CH2:7][S:5](=[O:6])([c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)=[O:26]>>[ClH:1].[ClH:2].[OH2:3].[O:4]=[S:5](=[O:6])([CH2:7][CH2:8][NH:9][CH...
CCN(CC)CC.CCOCC.NCCc1ccccc1.O=S(=O)(CCCl)c1ccccc1
Cl.Cl.O.O=S(=O)(CCNCCc1ccccc1)c1ccccc1.O=S(=O)(CCNCCc1ccccc1)c1ccccc1
null
null
C(C)#N.Cl.CO
Aromatic Heterocycle Formation
OtherReaction
72be0d2e1bf20ce2c679b00c1c160ada3ce336114055468e1a99db416052f9c2
ea7f51779ce0ba54a18c0e6e9df94f90cd9f6ea9c35213f225da6192c9409911
O=S(=O)(CCNCCc1ccccc1)c1ccccc1.O=S(=O)(CCNCCc1ccccc1)c1ccccc1
[CH3;D1;+0:1]-[CH2;D2;+0:2]-[N;H0;D3;+0:3](-[CH2;D2;+0:4]-[CH3;D1;+0:5])-[CH2;D2;+0:6]-[CH3;D1;+0:7].[CH3;D1;+0:8]-[CH2;D2;+0:9]-[O;H0;D2;+0:10]-[CH2;D2;+0:11]-[CH3;D1;+0:12].[C:13]-[C:14]-[NH2;D1;+0:15].[Cl;H0;D1;+0:16]-[CH2;D2;+0:17]-[CH2;D2;+0:18]-[S;H0;D4;+0:19](=[O;D1;H0:20])(=[O;H0;D1;+0:21])-[c:22](:[c:23]):[c:2...
89.1
[{"value": 60.0, "product": "O.Cl.C1(=CC=CC=C1)S(=O)(=O)CCNCCC1=CC=CC=C1.C1(=CC=CC=C1)S(=O)(=O)CCNCCC1=CC=CC=C1.Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.1, "product": "O.Cl.C1(=CC=CC=C1)S(=O)(=O)CCNCCC1=CC=CC=C1.C1(=CC=CC=C1)S(=O)(=O)CCNCCC1=CC=CC=C1.Cl", "details": "CALCULATEDPERCENTYIELD", "...
null
null
18
HOUR
A mixture of 70.23 g (0.344 mole) of 2-chloroethylphenylsulfone, 41.92 g (0.343 mole) of phenethylamine and 60 ml of triethylamine in 800 ml of acetonitrile was stirred at room temperature for 18 hr. The solvent was removed in vacuo, and the residue was partitioned between methylene chloride and dilute sodium hydroxide...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary amine.Tertiary amine.Sulfone
Secondary amine.Secondary amine.Sulfone.Sulfone
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
C(C)#N.Cl.CO
null
18
CCN(CC)CC.CCOCC.NCCc1ccccc1.O=S(=O)(CCCl)c1ccccc1>C(C)#N.Cl.CO>Cl.Cl.O.O=S(=O)(CCNCCc1ccccc1)c1ccccc1.O=S(=O)(CCNCCc1ccccc1)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-95c3f93212c34abcafd8589c1a2860f7
CC(C)N.O=S(=O)(CCCCCl)c1ccccc1>>CC(C)NCCCCS(=O)(=O)c1ccccc1.Cl
ClCCCCS(=O)(=O)C1=CC=CC=C1.C(C)(C)N>>Cl.CC(C)NCCCCS(=O)(=O)C1=CC=CC=C1
[CH3:1][CH:2]([CH3:3])[NH2:4].[CH2:5]([CH2:6][CH2:7][CH2:8][S:9](=[O:10])(=[O:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1)[Cl:18]>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][CH2:7][CH2:8][S:9](=[O:10])(=[O:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[ClH:18]
CC(C)N.O=S(=O)(CCCCCl)c1ccccc1
CC(C)NCCCCS(=O)(=O)c1ccccc1.Cl
null
null
C(Cl)(Cl)Cl.CO
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccccc1
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])-[NH2;D1;+0:4].[C:5]-[C:6]-[CH2;D2;+0:7]-[Cl;H0;D1;+0:8]>>[C:5]-[C:6]-[CH2;D2;+0:7]-[NH;D2;+0:4]-[C:2](-[C;D1;H3:1])-[C;D1;H3:3].[ClH;D0;+0:8]
30
[{"value": 30.0, "product": "Cl.CC(C)NCCCCS(=O)(=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 105.95 g (0.456 mole) [(4-chlorobutyl)sulfonyl]benzene was heated overnight at 75° C. on an autoclave in 200 ml of isopropylamine. The reaction mixture was stripped to dryness. The residue obtained was dissolved in chloroform and the chloroform layer was extracted with water. The chloroform layer was drie...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1
null
C(Cl)(Cl)Cl.CO
null
null
CC(C)N.O=S(=O)(CCCCCl)c1ccccc1>C(Cl)(Cl)Cl.CO>CC(C)NCCCCS(=O)(=O)c1ccccc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7339c7a207114a058f08a02bd2cd46d8
CC(C)N.ClCCSc1ccccc1>>CC(C)NCCSc1ccccc1.Cl
C1(=CC=CC=C1)SCCCl.[I-].[K+].C(C)(C)N>>Cl.C1(=CC=CC=C1)SCCNC(C)C
[CH3:1][CH:2]([CH3:3])[NH2:4].[CH2:5]([CH2:6][S:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[Cl:14]>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.[ClH:14]
CC(C)N.ClCCSc1ccccc1
CC(C)NCCSc1ccccc1.Cl
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccccc1
[#16:1]-[C:2]-[CH2;D2;+0:3]-[Cl;H0;D1;+0:4].[C;D1;H3:5]-[C:6](-[C;D1;H3:7])-[NH2;D1;+0:8]>>[#16:1]-[C:2]-[CH2;D2;+0:3]-[NH;D2;+0:8]-[C:6](-[C;D1;H3:5])-[C;D1;H3:7].[ClH;D0;+0:4]
76.9
[{"value": 76.9, "product": "Cl.C1(=CC=CC=C1)SCCNC(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 25 g (0.145 mole) of 2-chloroethyl phenyl sulfide and 1 g (0.006 mole) of potassium iodide in 500 ml of isopropylamine was heated in a bomb at 120° C. for 24 hr. The solvent was removed in vacuo, and the residue was partitioned between methylene chloride and dilute sodium hydroxide. The methylene chloride...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1
null
null
null
null
CC(C)N.ClCCSc1ccccc1>>CC(C)NCCSc1ccccc1.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-28031cec7bf3401286c156beffb1ffb3
CC(C)N.O=S(=O)(CCCl)Cc1ccccc1>>CC(C)NCCS(=O)(=O)Cc1ccccc1
CCOCC.ClCCS(=O)(=O)CC1=CC=CC=C1.C(C)(C)N.Cl>>Cl.C1(=CC=CC=C1)CS(=O)(=O)CCNC(C)C
[CH3:1][CH:2]([CH3:3])[NH2:4].Cl[CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
CC(C)N.O=S(=O)(CCCl)Cc1ccccc1
CC(C)NCCS(=O)(=O)Cc1ccccc1
null
null
CO
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[#16:3].[C;D1;H3:4]-[C:5](-[C;D1;H3:6])-[NH2;D1;+0:7]>>[#16:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:7]-[C:5](-[C;D1;H3:4])-[C;D1;H3:6]
65.8
[{"value": 65.8, "product": "Cl.C1(=CC=CC=C1)CS(=O)(=O)CCNC(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
72
HOUR
A mixture of 51.49 g (0.236 mole) of benzyl 2-chloroethyl sulfone and 600 ml of isopropylamine was stirred at room temperature for 72 hr. The solvent was removed in vacuo, and the residue was partitioned between ether and dilute sodium hydroxide. The ether solution was dried over magnesium sulfate, and the solvent was ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1
HCl
CO
null
72
CC(C)N.O=S(=O)(CCCl)Cc1ccccc1>CO>CC(C)NCCS(=O)(=O)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-df95688818af431f92f3b925fa45e917
CC(C)NCCSc1ccccc1.O.[O-]B1OO1.[OH-]>>CC(C)NCCS(=O)c1ccccc1.O=C(O)/C=C\C(=O)O
Cl.C1(=CC=CC=C1)SCCNC(C)C.B1(OO1)[O-].O.O.O.O.[Na+].[OH-].[Na+]>>C(\C=C/C(=O)O)(=O)O.C1(=CC=CC=C1)S(=O)CCNC(C)C
[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[OH2:22].B1([O-:15])[O:8][O:21]1.[OH-:17]>>[CH3:1][CH:2]([CH3:3])[NH:4][CH2:5][CH2:6][S:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[O:15]=[C:16]([OH:17])/[CH:18]=[CH:19]\[C:20](=[O:21])[OH:22]
CC(C)NCCSc1ccccc1.O.[O-]B1OO1.[OH-]
CC(C)NCCS(=O)c1ccccc1.O=C(O)/C=C\C(=O)O
null
null
S(O)(O)(=O)=O
Acylation
OtherReaction
920aba2fc218fc2206abcbec54b771387c85c815425bd4e22ef20c34e9dfd0bd
d5c4df79b25970cc5824026731621baec2947b39fd15cf98f6ca9fecd5262aac
c1ccccc1
[C:1]-[C:2]-[S;H0;D2;+0:3]-[c:4](:[c:5]):[c:6].[O-;H0;D1:7]-B1-[O;H0;D2;+0:8]-[O;H0;D2;+0:9]-1.[OH-;D0:10].[OH2;D0;+0:11]>>[C:1]-[C:2]-[S;H0;D3;+0:3](=[O;H0;D1;+0:9])-[c:4](:[c:5]):[c:6].[O;H0;D1;+0:7]=[C:12](-[OH;D1;+0:10])/[C:13]=[C:14]\[C:15](=[O;H0;D1;+0:8])-[OH;D1;+0:11]
177.6
[{"value": 88.3, "product": "C(\\C=C/C(=O)O)(=O)O.C1(=CC=CC=C1)S(=O)CCNC(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 177.6, "product": "C(\\C=C/C(=O)O)(=O)O.C1(=CC=CC=C1)S(=O)CCNC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 15.62 g (0.067 mole) of N-[2-(phenylthio)ethyl]-2-propanamine hydrochloride and 15.62 g (0.101 mole) of sodium perborate tetrahydrate in 300 ml of 2M sulfuric acid was stirred at room temperature for 16 hr. The solution was made basic with 50% sodium hydroxide, and the basic solution was extracted with me...
10.6084/m9.figshare.5104873.v1
null
Peroxide.Monosulfide
Carboxylic acid.Carboxylic acid.Sulfoxide
B1OO1
null
c1ccccc1
B
S(O)(O)(=O)=O
null
null
CC(C)NCCSc1ccccc1.O.[O-]B1OO1.[OH-]>S(O)(O)(=O)=O>CC(C)NCCS(=O)c1ccccc1.O=C(O)/C=C\C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-81ada1811183440c81eed8afb7279bd4
NCc1ccccc1.O=S(=O)(CCCl)c1ccccc1>>Cl.O=S(=O)(CCNCc1ccccc1)c1ccccc1
C1(=CC=CC=C1)S(=O)(=O)CCCl.C(C1=CC=CC=C1)N.C(C)N(CC)CC>>Cl.C1(=CC=CC=C1)S(=O)(=O)CCNCC1=CC=CC=C1
[NH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[Cl:1][CH2:6][CH2:5][S:3](=[O:2])(=[O:4])[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[ClH:1].[O:2]=[S:3](=[O:4])([CH2:5][CH2:6][NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
NCc1ccccc1.O=S(=O)(CCCl)c1ccccc1
Cl.O=S(=O)(CCNCc1ccccc1)c1ccccc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
O=S(=O)(CCNCc1ccccc1)c1ccccc1
[#16:1]-[C:2]-[CH2;D2;+0:3]-[Cl;H0;D1;+0:4].[NH2;D1;+0:5]-[C:6]-[c:7]>>[#16:1]-[C:2]-[CH2;D2;+0:3]-[NH;D2;+0:5]-[C:6]-[c:7].[ClH;D0;+0:4]
null
[]
null
null
64
HOUR
A mixture of 71.90 g (0.352 mole) of 2-chloroethyl phenyl sulfone, 37.45 g (0.350 mole) of benzylamine and 60 ml of triethylamine in 800 ml of acetonitrile was stirred at room temperature for ≈64 hr. The solvent was removed in vacuo and the residue was partitioned between methylene chloride and dilute sodium hydroxide....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccccc1
null
C(C)#N
null
64
NCc1ccccc1.O=S(=O)(CCCl)c1ccccc1>C(C)#N>Cl.O=S(=O)(CCNCc1ccccc1)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9b6bca417c434762bad8de93b51a34db
OCCCCCl.Sc1ccccc1>>OCCCCSc1ccccc1
C1(=CC=CC=C1)S.ClCCCCO.C([O-])([O-])=O.[K+].[K+]>>C1(=CC=CC=C1)SCCCCO
Cl[CH2:5][CH2:4][CH2:3][CH2:2][OH:1].[SH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[OH:1][CH2:2][CH2:3][CH2:4][CH2:5][S:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
OCCCCCl.Sc1ccccc1
OCCCCSc1ccccc1
null
null
C(Cl)(Cl)Cl.C(OC)COC
Heteroatom Alkylation and Arylation
thioether_nucl_sub
26df88c6a3f5f203c89584658be4e126cb42994c98a2e16bc812e1036cdae857
8b2f52296c3a93039174c980b6042ba15754e04d6892a1284c3a32985220b214
c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[SH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
57.8
[{"value": 57.8, "product": "C1(=CC=CC=C1)SCCCCO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 3.1, "product": "C1(=CC=CC=C1)SCCCCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of thiophenol (121.2 g, 1.10 mole), 4-chloro-1-butanol (100.0 g, 0.921 mole), and potassium carbonate (138.2 g, 1.0 mole) was heated overnight at gentle reflux in dimethoxyethane. The reaction mixture was filtered and solvent removed by rotary evaporator. The residue obtained was dissolved in chloroform and e...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic thiol
Monosulfide
null
null
c1ccccc1
HCl
C(Cl)(Cl)Cl.C(OC)COC
null
null
OCCCCCl.Sc1ccccc1>C(Cl)(Cl)Cl.C(OC)COC>OCCCCSc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b9ffe40dfc354894b3753bf7aa940b3d
CCOCCCN.O=S(=O)(CCCl)c1ccccc1>>CCOCCCNCCS(=O)(=O)c1ccccc1
Cl.C1(=CC=CC=C1)S(=O)(=O)CCCl.C(C)OCCCN.C(C)N(CC)CC>>Cl.C(C)OCCCNCCS(=O)(=O)C1=CC=CC=C1
[CH3:1][CH2:2][O:3][CH2:4][CH2:5][CH2:6][NH2:7].Cl[CH2:8][CH2:9][S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[CH3:1][CH2:2][O:3][CH2:4][CH2:5][CH2:6][NH:7][CH2:8][CH2:9][S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
CCOCCCN.O=S(=O)(CCCl)c1ccccc1
CCOCCCNCCS(=O)(=O)c1ccccc1
null
null
C(C)#N.CCOCC.CO
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[#16:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[#16:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
63.2
[{"value": 63.2, "product": "Cl.C(C)OCCCNCCS(=O)(=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.2, "product": "Cl.C(C)OCCCNCCS(=O)(=O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
A mixture of 51.4 g (0.253 mole) of 2-chloroethyl phenyl sulfone, 50.2 g (0.417 mole) of 3-ethoxy-1-propanamine, and 33.0 g (0.327 mole) of triethylamine in 400 ml of acetonitrile was stirred at room temperature for 20 hr. The solvent was removed in vacuo and the residue was partitioned between methylene chloride and d...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1
HCl
C(C)#N.CCOCC.CO
null
20
CCOCCCN.O=S(=O)(CCCl)c1ccccc1>C(C)#N.CCOCC.CO>CCOCCCNCCS(=O)(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-712d15a0026748889ba593fd6b6cb891
CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.CCO>>CCOc1ccc(S(=O)(=O)CCNC(C)C)cc1
C(C)O.[H-].[Na+].CS(=O)C.Cl.ClC1=CC=C(C=C1)S(=O)(=O)CCNC(C)C>>Cl.C(C)OC1=CC=C(C=C1)S(=O)(=O)CCNC(C)C
Cl[c:4]1[cH:5][cH:6][c:7]([S:8](=[O:9])(=[O:10])[CH2:11][CH2:12][NH:13][CH:14]([CH3:15])[CH3:16])[cH:17][cH:18]1.[CH3:1][CH2:2][OH:3]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([S:8](=[O:9])(=[O:10])[CH2:11][CH2:12][NH:13][CH:14]([CH3:15])[CH3:16])[cH:17][cH:18]1
CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.CCO
CCOc1ccc(S(=O)(=O)CCNC(C)C)cc1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccccc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C;D1;H3:6]-[C:7]-[OH;D1;+0:8]>>[C;D1;H3:6]-[C:7]-[O;H0;D2;+0:8]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
0.5
HOUR
To a suspension of 6.6 g of a 60% dispersion of sodium hydride in oil (0.165 mole) in 300 mole of dimethyl sulfoxide was added 7.5 g (0.163 mole) of absolute ethanol. The mixture was stirred at room temperature for 0.5 hr, and 20.8 g (0.080 mole) of N-[2-(4-chlorophenylsulfonyl)ethyl]-2-propanamine hydrochloride was ad...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1
HCl
null
null
0.5
CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.CCO>>CCOc1ccc(S(=O)(=O)CCNC(C)C)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-53878bc16b5f4166be999b2b304deda7
CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.[OH-]>>CC(C)NCCS(=O)(=O)c1ccc(O)cc1
Cl.ClC1=CC=C(C=C1)S(=O)(=O)CCNC(C)C.[OH-].[Na+]>>Cl.OC1=CC=C(C=C1)S(=O)(=O)CCNC(C)C
Cl[c:13]1[cH:12][cH:11][c:10]([S:7]([CH2:6][CH2:5][NH:4][CH:2]([CH3:1])[CH3:3])(=[O:8])=[O:9])[cH:16][cH:15]1.[OH-:14]>>[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][c:13]([OH:14])[cH:15][cH:16]1
CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.[OH-]
CC(C)NCCS(=O)(=O)c1ccc(O)cc1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
6fb010fda794df3314b587858e2590d87f73768e0e1a88e417db2b55286986bb
05ba928edd770174a8e0738270a5c99182284743586e41e52e6183b77c44ac41
c1ccccc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[OH-;D0:6]>>[OH;D1;+0:6]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
null
null
A solution of N-[2-[(4-chlorophenyl)sulfonyl]ethyl]-1-methylethanamine hydrochloride and sodium hydroxide in 500 ml of dimethyl sulfoxide is heated at 95° C. for 2 hrs with stirring. The solvent is removed by rotary evaporation (vacuum pump) and the residue is partitioned between water (pH adjusted to 7 by the addition...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Aromatic alcohol
c1ccccc1
c1ccccc1
c1ccccc1
Other
CS(=O)C
null
null
CC(C)NCCS(=O)(=O)c1ccc(Cl)cc1.[OH-]>CS(=O)C>CC(C)NCCS(=O)(=O)c1ccc(O)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bfa7dcd3f23744c99a5e0a575455a555
CC(C)=O.CC(C)NCCS(=O)(=O)c1ccccc1.CCOC(C)=O.CN(CCN)CCc1ccccc1.O=C(n1ccnc1)n1ccnc1>>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)CCc1ccccc1.CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)CCc1ccccc1.O
CC(=O)C.C(C)(=O)OCC.C(=O)(N1C=NC=C1)N1C=NC=C1.CN(CCN)CCC1=CC=CC=C1.CC(C)NCCS(=O)(=O)C1=CC=CC=C1>>O.CC(C)N(C(=O)NCCN(CCC1=CC=CC=C1)C)CCS(=O)(=O)C1=CC=CC=C1.CC(C)N(C(=O)NCCN(C)CCC1=CC=CC=C1)CCS(=O)(=O)C1=CC=CC=C1
[CH3:3][C:32]([CH3:36])=[O:61].[CH3:1][CH:2]([NH:4][CH2:5][CH2:6][S:7](=[O:8])([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)=[O:39])[CH3:33].[O:9]([C:16](=[O:17])[CH3:40])[CH2:23][CH3:24].[NH2:48][CH2:49][CH2:50][N:51]([CH3:52])[CH2:53][CH2:54][c:55]1[cH:56][cH:57][cH:58][cH:59][cH:60]1.n1[cH:25][cH:26][n:34]([C:46]([n:...
CC(C)=O.CC(C)NCCS(=O)(=O)c1ccccc1.CCOC(C)=O.CN(CCN)CCc1ccccc1.O=C(n1ccnc1)n1ccnc1
CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)CCc1ccccc1.CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)CCc1ccccc1.O
null
null
CCOCC.O1CCCC1
Acylation
OtherReaction
38604cddeaa23064e6198c611ade6a1c7d513a6797da9364a1724eac9cfff159
b3ee7c51000750bd4fda626e70d203152f4e00e0aa29f7b6c8649bd8159889fd
O=C(NCCNCCc1ccccc1)NCCS(=O)(=O)c1ccccc1.O=C(NCCNCCc1ccccc1)NCCS(=O)(=O)c1ccccc1
[C;D1;H3:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[NH;D2;+0:4]-[C:5]-[C:6]-[S;H0;D4;+0:7](=[O;D1;H0:8])(=[O;H0;D1;+0:9])-[c:10](:[c:11]):[c:12].[CH3;D1;+0:13]-[C;H0;D3;+0:14](-[CH3;D1;+0:15])=[O;H0;D1;+0:16].[CH3;D1;+0:17]-[CH2;D2;+0:18]-[O;H0;D2;+0:19]-[C;H0;D3;+0:20](-[CH3;D1;+0:21])=[O;D1;H0:22].[C:23]-[C:24]-[NH2;D1;+0:25]....
null
[]
null
null
null
null
A solution of 1,1'-carbonyldiimidazole (8.12 g, 0.05 mole) and N-methyl-N-(2-phenylethyl)-1,2-ethanediamine, 8.0 g (0.0045 mole) in 300 ml of tetrahydrofuran was stirred for 2 hours at room temperature. To the mixture was added 9.37 g (0.0412 mole) of 1-methyl-N-[2-(phenylsulfonyl)ethyl]ethanamine and the reaction was ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Primary amine.Secondary amine.Sulfone
Urea.Urea.Tertiary amine.Sulfone.Sulfone
c1c[nH]cn1.c1c[nH]cn1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
CCOCC.O1CCCC1
null
null
CC(C)=O.CC(C)NCCS(=O)(=O)c1ccccc1.CCOC(C)=O.CN(CCN)CCc1ccccc1.O=C(n1ccnc1)n1ccnc1>CCOCC.O1CCCC1>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)CCc1ccccc1.CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)CCc1ccccc1.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-082c10047ad64187a1aa3f32d4231702
CC(C)NCCS(=O)(=O)c1ccccc1.CN(CCN)Cc1ccccc1.O=C(n1ccnc1)n1ccnc1>>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)Cc1ccccc1
[O-][Si](=O)[O-].[Mg+2].CN(CCN)CC1=CC=CC=C1.C(=O)(N1C=NC=C1)N1C=NC=C1.CC(C)NCCS(=O)(=O)C1=CC=CC=C1>>CC(C)N(C(=O)NCCN(CC1=CC=CC=C1)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][N:21]([CH3:22])[CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]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:...
CC(C)NCCS(=O)(=O)c1ccccc1.CN(CCN)Cc1ccccc1.O=C(n1ccnc1)n1ccnc1
CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)Cc1ccccc1
null
null
C(Cl)(Cl)Cl.O1CCCC1
Acylation
OtherReaction
f4dd0282cbfc717a6a9609eb36d2e65f9c0aac6e585fd933723172d3d62534b8
092fb1988ce3c31a0210cc9ec123f317c79841c29a05a3f2098134944f12c379
O=C(NCCNCc1ccccc1)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]
null
[]
null
null
null
null
A solution of 17.90 g (0.045 mole) of N-methyl-N-(phenylmethyl)-1,2-ethanediamine and 1,1'-carbonyldiimidazole (0.05 mole) in 100 ml of tetrahydrofuran was stirred at room temperature for 1 hour. To the mixture was added 10.52 g, (0.04 mole) of 1-methyl-N-[2-(phenysulfonyl)ethyl]ethanamine and the resulting solution he...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1.c1ccccc1
Other
C(Cl)(Cl)Cl.O1CCCC1
null
null
CC(C)NCCS(=O)(=O)c1ccccc1.CN(CCN)Cc1ccccc1.O=C(n1ccnc1)n1ccnc1>C(Cl)(Cl)Cl.O1CCCC1>CC(C)N(CCS(=O)(=O)c1ccccc1)C(=O)NCCN(C)Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-fefe59a7cdf245f1bf02e5ac9fe770f6
CCNCCN(CC)CC.NCCS(=O)(=O)c1ccccc1.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCN(CC)C(=O)NCCS(=O)(=O)c1ccccc1
C1(=CC=CC=C1)S(=O)(=O)CCN.C(=O)(N1C=NC=C1)N1C=NC=C1.C(CC(O)(C(=O)O)CC(=O)O)(=O)O.C(C)N(CCNCC)CC>>C(CC(O)(C(=O)O)CC(=O)O)(=O)O.C(C)N(CCN(C(=O)NCCS(=O)(=O)C1=CC=CC=C1)CC)CC
[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH:8][CH2:9][CH3:10].[NH2:13][CH2:14][CH2:15][S:16](=[O:17])(=[O:18])[c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1.c1cn([C:11](n2ccnc2)=[O:12])cn1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][N:8]([CH2:9][CH3:10])[C:11](=[O:12])[NH:13][CH2:14][CH2:15][S:16](=[O:17])...
CCNCCN(CC)CC.NCCS(=O)(=O)c1ccccc1.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCN(CC)C(=O)NCCS(=O)(=O)c1ccccc1
null
null
CCOCC.CO.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].[O;D1;H0:9]=[C;H0;D3;+0:10](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:10](=[O;D1;H0:9])-[N;H0;D3;+0:6](-[C:5]-[C:4])-[C:7]-[C;D1;H3:8]
52
[{"value": 52.0, "product": "C(CC(O)(C(=O)O)CC(=O)O)(=O)O.C(C)N(CCN(C(=O)NCCS(=O)(=O)C1=CC=CC=C1)CC)CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 5.55 g (0.030 mole) of 2-(phenylsulfonyl)ethanamine and 5.35 g (0.033 mole) of 1,1'-carbonyldiimidazole in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 4.62 g (0.032 mole) of N,N,N'-triethylethylenediamine in 50 ml of tetrahydrofuran was added, and the mixture was refl...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
CCOCC.CO.O1CCCC1
null
null
CCNCCN(CC)CC.NCCS(=O)(=O)c1ccccc1.O=C(n1ccnc1)n1ccnc1>CCOCC.CO.O1CCCC1>CCN(CC)CCN(CC)C(=O)NCCS(=O)(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d4c4a71d951f42169d6ac22f3b988c3e
CCN(CC)CCN.COc1ccc(S(=O)(=O)CCNC(C)C)cc1.O=C(n1ccnc1)n1ccnc1>>CCN(CC)CCNC(=O)N(CCS(=O)(=O)c1ccc(OC)cc1)C(C)C
COC1=CC=C(C=C1)S(=O)(=O)CCNC(C)C.C(=O)(N1C=NC=C1)N1C=NC=C1.C(C)N(CCN)CC>>C(C)N(CCNC(N(C(C)C)CCS(=O)(=O)C1=CC=C(C=C1)OC)=O)CC
[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][NH2:8].[NH:11]([CH2:12][CH2:13][S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][c:20]([O:21][CH3:22])[cH:23][cH:24]1)[CH:25]([CH3:26])[CH3:27].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]...
CCN(CC)CCN.COc1ccc(S(=O)(=O)CCNC(C)C)cc1.O=C(n1ccnc1)n1ccnc1
CCN(CC)CCNC(=O)N(CCS(=O)(=O)c1ccc(OC)cc1)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]
67.3
[{"value": 67.3, "product": "C(C)N(CCNC(N(C(C)C)CCS(=O)(=O)C1=CC=C(C=C1)OC)=O)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.3, "product": "C(C)N(CCNC(N(C(C)C)CCS(=O)(=O)C1=CC=C(C=C1)OC)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4.54 g (0.28 mole) of 1,1'-carbonyldiimidazole and 2.90 g (0.025 mole) of N,N-diethylethylenediamine in 400 ml of tetrahydrofuran was stirred at room temperature for 1 hr. A solution of 5.89 g (0.0229 mole) of N-[2-[(4-methoxyphenyl)sulfonyl]ethyl]-2-propanamine in 50 ml of tetrahydrofuran was added, and ...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Secondary amine
Urea
c1c[nH]cn1.c1c[nH]cn1
null
c1ccccc1
Other
O1CCCC1
null
null
CCN(CC)CCN.COc1ccc(S(=O)(=O)CCNC(C)C)cc1.O=C(n1ccnc1)n1ccnc1>O1CCCC1>CCN(CC)CCNC(=O)N(CCS(=O)(=O)c1ccc(OC)cc1)C(C)C