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414 values
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36
36
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large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
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14
3.37k
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1
581
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1
433
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634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
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346 values
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64
64
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large_stringlengths
64
64
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large_stringlengths
5
288
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large_stringlengths
24
2.64k
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float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
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large_stringclasses
3 values
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float64
0
4k
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large_stringclasses
4 values
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large_stringlengths
1
23.6k
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96 values
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large_stringlengths
3
716
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large_stringlengths
3
539
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large_stringlengths
5
293
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large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
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float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-311e46e924e444df924ddcbbce7004ba
COc1cc(C(O)c2ccccc2F)ccc1OCc1ccccc1>>COc1cc(C(=O)c2ccccc2F)ccc1OCc1ccccc1
[Cr](=O)(=O)([O-])Cl.[NH+]1=CC=CC=C1.C(C1=CC=CC=C1)OC1=C(C=C(C(C2=C(C=CC=C2)F)O)C=C1)OC>>C(C1=CC=CC=C1)OC1=C(C=C(C(=O)C2=C(C=CC=C2)F)C=C1)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]([OH:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[F:14])[cH:15][cH:16][c:17]1[O:18][CH2:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[F:14])[cH:15][cH:16][c:17]1[O:18][CH2:19][c:20]1[cH:21][cH:22][cH...
COc1cc(C(O)c2ccccc2F)ccc1OCc1ccccc1
COc1cc(C(=O)c2ccccc2F)ccc1OCc1ccccc1
null
null
null
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
c7c20d2959ac48847b03cc1265962cf99a8ec8a85900c087dabb30077298c66c
767cfd93f5821ebb9e1e72addd9cb404b20b0c821d246ae6b87a5776b74a455b
O=C(c1ccccc1)c1ccc(OCc2ccccc2)cc1
[OH;D1;+0:1]-[CH;D3;+0:2](-[c:3](:[c:4]):[c:5])-[c:6](:[c:7]):[c:8]>>[O;H0;D1;+0:1]=[C;H0;D3;+0:2](-[c:3](:[c:4]):[c:5])-[c:6](:[c:7]):[c:8]
null
[]
null
null
3
HOUR
69.8 g of 4-(benzyloxy)-2'-fluoro-3-methoxybenzhydrol (dissolved in 600 ml of methylene chloride) are treated within 30 minutes at 20° with 45.3 g of pyridinium chlorochromate and stirred at 20° for 3 hours. The precipitate formed is subsequently filtered and washed with methylene chloride. The filtrate is evaporated a...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ketone
null
null
c1ccccc1.c1ccccc1.c1ccccc1
null
null
null
3
COc1cc(C(O)c2ccccc2F)ccc1OCc1ccccc1>>COc1cc(C(=O)c2ccccc2F)ccc1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a0b6669d0ef14f60878fe0cc42ec141a
COc1cc(C(=O)c2ccccc2F)ccc1OCc1ccccc1>>COc1cc(C(=O)c2ccccc2F)ccc1O
Br.C(C1=CC=CC=C1)OC1=C(C=C(C(=O)C2=C(C=CC=C2)F)C=C1)OC>>FC1=C(C=CC=C1)C(C1=CC(=C(C=C1)O)OC)=O
c1ccc(C[O:18][c:17]2[c:3]([O:2][CH3:1])[cH:4][c:5]([C:6](=[O:7])[c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[F:14])[cH:15][cH:16]2)cc1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[F:14])[cH:15][cH:16][c:17]1[OH:18]
COc1cc(C(=O)c2ccccc2F)ccc1OCc1ccccc1
COc1cc(C(=O)c2ccccc2F)ccc1O
null
null
C(C)(=O)O
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(c1ccccc1)c1ccccc1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
null
[]
null
null
1.5
HOUR
170 ml of 33 percent hydrobromic acid in glacial acetic acid are added at 20°-25° within 20 minutes to 42.4 g of 4-(benzyloxy)-2'-fluoro-3-methoxybenzophenone (dissolved in 450 ml of methylene chloride). After stirring at 20° for 1.5 hours, the reaction mixture is poured into 750 ml of ice-water; the methylene chloride...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccccc1.c1ccccc1
Other
C(C)(=O)O
null
1.5
COc1cc(C(=O)c2ccccc2F)ccc1OCc1ccccc1>C(C)(=O)O>COc1cc(C(=O)c2ccccc2F)ccc1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-44336f450f774728b453f11af0e91f07
COc1cc(C(=O)c2ccccc2F)ccc1O.O=[N+]([O-])O>>COc1cc(C(=O)c2ccccc2F)cc([N+](=O)[O-])c1O
[N+](=O)(O)[O-].FC1=C(C=CC=C1)C(C1=CC(=C(C=C1)O)OC)=O>>FC1=C(C=CC=C1)C(C1=CC(=C(C(=C1)[N+](=O)[O-])O)OC)=O
[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[F:14])[cH:15][cH:16][c:20]1[OH:21].O[N+:17](=[O:18])[O-:19]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[F:14])[cH:15][c:16]([N+:17](=[O:18])[O-:19])[c:20]1[OH:21]
COc1cc(C(=O)c2ccccc2F)ccc1O.O=[N+]([O-])O
COc1cc(C(=O)c2ccccc2F)cc([N+](=O)[O-])c1O
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=C(c1ccccc1)c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[O;D1;H0:4]=[C:5]-[c:6]:[c:7]:[cH;D2;+0:8]:[c:9](-[O;D1;H1:10]):[c:11]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;D1;H0:3])-[c;H0;D3;+0:8](:[c:7]:[c:6]-[C:5]=[O;D1;H0:4]):[c:9](-[O;D1;H1:10]):[c:11]
null
[]
null
null
1.5
HOUR
7.8 ml of 65 percent nitric acid are added dropwise at 20° within 20 minutes to 29.4 g of 2'-fluoro-4-hydroxy-3-methoxybenzophenone (dissolved in 450 ml of acetic acid). After stirring for 1.5 hours, the reaction mixture is poured into 2 l of ice-water and the precipitate formed is filtered off, washed with water and d...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
null
null
1.5
COc1cc(C(=O)c2ccccc2F)ccc1O.O=[N+]([O-])O>>COc1cc(C(=O)c2ccccc2F)cc([N+](=O)[O-])c1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-de5a925d6e474d548e5d51dfa8edebcc
NC(=S)NCCc1ccccc1.O=C(CBr)c1cc(O)c(O)c([N+](=O)[O-])c1>>Br.O=[N+]([O-])c1cc(-c2csc(NCCc3ccccc3)n2)cc(O)c1O
BrCC(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])O)O.C(CC1=CC=CC=C1)NC(=S)N>>Br.[N+](=O)([O-])C1=C(C(O)=CC(=C1)C=1N=C(SC1)NCCC1=CC=CC=C1)O
[S:10]=[C:11]([NH:12][CH2:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[NH2:21].O=[C:8]([c:7]1[cH:6][c:5]([N+:3](=[O:2])[O-:4])[c:25]([OH:26])[c:23]([OH:24])[cH:22]1)[CH2:9][Br:1]>>[BrH:1].[O:2]=[N+:3]([O-:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][s:10][c:11]([NH:12][CH2:13][CH2:14][c:15]3[cH:16][cH:17][cH:18][cH:19...
NC(=S)NCCc1ccccc1.O=C(CBr)c1cc(O)c(O)c([N+](=O)[O-])c1
Br.O=[N+]([O-])c1cc(-c2csc(NCCc3ccccc3)n2)cc(O)c1O
null
null
C(CCC)O
Aromatic Heterocycle Formation
OtherReaction
bef473efef1d9ea696235ac9e0e73338149dac4bc5d824d8ecb15263a8e3a4b0
39fbe568f79251ca2d63e869c3b1ee705fef7458c6d99863e8f91d4da02df595
c1ccc(CCNc2nc(-c3ccccc3)cs2)cc1
O=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[Br;H0;D1;+0:3])-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[C:9]-[#7:10]-[C;H0;D3;+0:11](-[NH2;D1;+0:12])=[S;H0;D1;+0:13]>>[BrH;D0;+0:3].[C:9]-[#7:10]-[c;H0;D3;+0:11]1:[n;H0;D2;+0:12]:[c;H0;D3;+0:1](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[cH;D2;+0:2]:[s;H0;D2;+0:13]:1
null
[]
null
null
null
null
A suspension of 13.8 g of 2-bromo-3',4'-dihydroxy-5'-nitroacetophenone is treated with 9.0 g of 1-(phenethyl)-2-thiourea in 150 ml of n-butanol and the mixture is heated to boiling under reflux for 3 hours. After cooling to room temperature, the crystals are filtered under suction and crystallized from n-butanol. There...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Thiourea
null
null
c1cscn1
c1ccccc1.c1cscn1.c1ccccc1
HO-
C(CCC)O
null
null
NC(=S)NCCc1ccccc1.O=C(CBr)c1cc(O)c(O)c([N+](=O)[O-])c1>C(CCC)O>Br.O=[N+]([O-])c1cc(-c2csc(NCCc3ccccc3)n2)cc(O)c1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4d95d8063f6240228a4e9c125dc2970a
NC(=S)NC12CC3CC(CC(C3)C1)C2.O=C(CBr)c1cc(O)c(O)c([N+](=O)[O-])c1>>Br.O=[N+]([O-])c1cc(-c2cnc(NC34CC5CC(CC(C5)C3)C4)s2)cc(O)c1O
BrCC(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])O)O.C12(CC3CC(CC(C1)C3)C2)NC(=S)N>>Br.C12(CC3CC(CC(C1)C3)C2)NC=2SC(=CN2)C2=CC(=C(C(O)=C2)O)[N+](=O)[O-]
[NH2:10][C:11]([NH:12][C:13]12[CH2:14][CH:15]3[CH2:16][CH:17]([CH2:18][CH:19]([CH2:20]3)[CH2:21]1)[CH2:22]2)=[S:23].O=[C:8]([c:7]1[cH:6][c:5]([N+:3](=[O:2])[O-:4])[c:27]([OH:28])[c:25]([OH:26])[cH:24]1)[CH2:9][Br:1]>>[BrH:1].[O:2]=[N+:3]([O-:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][n:10][c:11]([NH:12][C:13]34[CH2:14][CH:15]5...
NC(=S)NC12CC3CC(CC(C3)C1)C2.O=C(CBr)c1cc(O)c(O)c([N+](=O)[O-])c1
Br.O=[N+]([O-])c1cc(-c2cnc(NC34CC5CC(CC(C5)C3)C4)s2)cc(O)c1O
null
null
C(CCC)O
Aromatic Heterocycle Formation
OtherReaction
bef473efef1d9ea696235ac9e0e73338149dac4bc5d824d8ecb15263a8e3a4b0
39fbe568f79251ca2d63e869c3b1ee705fef7458c6d99863e8f91d4da02df595
c1ccc(-c2cnc(NC34CC5CC(CC(C5)C3)C4)s2)cc1
O=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[Br;H0;D1;+0:3])-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[C:9]-[#7:10]-[C;H0;D3;+0:11](-[NH2;D1;+0:12])=[S;H0;D1;+0:13]>>[BrH;D0;+0:3].[C:9]-[#7:10]-[c;H0;D3;+0:11]1:[n;H0;D2;+0:12]:[cH;D2;+0:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]):[s;H0;D2;+0:13]:1
null
[]
null
null
null
null
A suspension of 8.3 g of 2-bromo-3',4'-dihydroxy-5'-nitroacetophenone is treated with 1-(1-adamantyl)-2-thiourea in 90 ml of n-butanol and the mixture is heated to boiling under reflux for 4 hours. After cooling to room temperature, the crystals are filtered under suction and recrystallized from n-butanol. There is obt...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Thiourea
null
null
c1cscn1
c1cscn1.c1ccccc1.C1C2CC3CC1CC(C2)C3
HO-
C(CCC)O
null
null
NC(=S)NC12CC3CC(CC(C3)C1)C2.O=C(CBr)c1cc(O)c(O)c([N+](=O)[O-])c1>C(CCC)O>Br.O=[N+]([O-])c1cc(-c2cnc(NC34CC5CC(CC(C5)C3)C4)s2)cc(O)c1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e4e15c3ce7554449852d2801074d3ecb
CC(=O)OCC(=O)c1cc(O)c(O)c([N+](=O)[O-])c1>>O=C(CO)c1cc(O)c(O)c([N+](=O)[O-])c1
C(C)(=O)OCC(C1=CC(=C(C(=C1)[N+](=O)[O-])O)O)=O>>OCC(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])O)O
CC(=O)[O:4][CH2:3][C:2](=[O:1])[c:5]1[cH:6][c:7]([OH:8])[c:9]([OH:10])[c:11]([N+:12](=[O:13])[O-:14])[cH:15]1>>[O:1]=[C:2]([CH2:3][OH:4])[c:5]1[cH:6][c:7]([OH:8])[c:9]([OH:10])[c:11]([N+:12](=[O:13])[O-:14])[cH:15]1
CC(=O)OCC(=O)c1cc(O)c(O)c([N+](=O)[O-])c1
O=C(CO)c1cc(O)c(O)c([N+](=O)[O-])c1
null
null
Cl.C(C)O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccccc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[c:5]>>[O;D1;H0:4]=[C:3](-[c:5])-[C:2]-[OH;D1;+0:1]
null
[]
null
null
null
null
A suspension of 2.6 g of (3,4-dihydroxy-5-nitrobenzoyl)methyl acetate in 20 ml of ethanol and 20 ml of 1N hydrochloric acid is heated to boiling under reflux for 5 hours. The reaction mixture is then evaporated, the residue is distilled with toluene and then recrystallized from ethanol. There is obtained 2,3',4'-trihyd...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1
HO-
Cl.C(C)O
null
null
CC(=O)OCC(=O)c1cc(O)c(O)c([N+](=O)[O-])c1>Cl.C(C)O>O=C(CO)c1cc(O)c(O)c([N+](=O)[O-])c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ca95057036464fb2a555c89433f5e408
CCCCCCOC(=O)C(=O)c1cc(O)c(O)c([N+](=O)[O-])c1.N#C/C(N)=C(/N)C#N>>N#Cc1nc(O)c(-c2cc(O)c(O)c([N+](=O)[O-])c2)nc1C#N
OC=1C=C(C=C(C1O)[N+](=O)[O-])C(C(=O)OCCCCCC)=O.N/C(=C(/C#N)\N)/C#N>>OC1=C(N=C(C(=N1)C#N)C#N)C1=CC(=C(C(=C1)[N+](=O)[O-])O)O
CCCCCCO[C:5](=[O:6])[C:7](=O)[c:8]1[cH:9][c:10]([OH:11])[c:12]([OH:13])[c:14]([N+:15](=[O:16])[O-:17])[cH:18]1.[N:1]#[C:2]/[C:3]([NH2:4])=[C:20](/[NH2:19])[C:21]#[N:22]>>[N:1]#[C:2][c:3]1[n:4][c:5]([OH:6])[c:7](-[c:8]2[cH:9][c:10]([OH:11])[c:12]([OH:13])[c:14]([N+:15](=[O:16])[O-:17])[cH:18]2)[n:19][c:20]1[C:21]#[N:22]
CCCCCCOC(=O)C(=O)c1cc(O)c(O)c([N+](=O)[O-])c1.N#C/C(N)=C(/N)C#N
N#Cc1nc(O)c(-c2cc(O)c(O)c([N+](=O)[O-])c2)nc1C#N
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
b9cc8aadffc394af5d830908307996f03955b4d8cc7045f4b42af3988f24d3a7
e1dd4674d59a7a9788bb2a36dcd479ddd279bc27e880caff550f05806685f20c
c1ccc(-c2cnccn2)cc1
C-C-C-C-C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C;H0;D3;+0:3](=O)-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[N;D1;H0:9]#[C:10]/[C;H0;D3;+0:11](-[NH2;D1;+0:12])=[C;H0;D3;+0:13](/[NH2;D1;+0:14])-[C:15]#[N;D1;H0:16]>>[N;D1;H0:9]#[C:10]-[c;H0;D3;+0:11]1:[n;H0;D2;+0:12]:[c;H0;D3;+0:1](-[OH;D1;+0:2]):[c;H0;D3;+0:3](-[c;H0;D3;+...
null
[]
null
null
null
null
A solution of 4.0 g of n-hexyl 3,4-dihydroxy-5-nitrophenylglyoxylate and 1.5 g of diaminomaleonitrile in 35 ml of ethanol is heated to boiling under reflux for 24 hours. The alcohol is then distilled, the residue is dissolved in ether, washed with water, dried over sodium sulfate, filtered and evaporated. There is obta...
10.6084/m9.figshare.5104873.v1
null
Enamine.Enamine.Ketone.Ester
Aromatic alcohol
null
c1cnccn1
c1cnccn1.c1ccccc1
HO-
C(C)O
null
null
CCCCCCOC(=O)C(=O)c1cc(O)c(O)c([N+](=O)[O-])c1.N#C/C(N)=C(/N)C#N>C(C)O>N#Cc1nc(O)c(-c2cc(O)c(O)c([N+](=O)[O-])c2)nc1C#N
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fd31337ad3a24725a4de49e2d018ed9f
COc1cc(C(=O)CBr)cc(C#N)c1OC>>N#Cc1cc(C(=O)CBr)cc(O)c1O
BrCC(=O)C=1C=C(C(=C(C#N)C1)OC)OC.B(Br)(Br)Br.C(O)([O-])=O.[Na+].C(C)(=O)O>>BrCC(=O)C=1C=C(C(=C(C#N)C1)O)O
C[O:12][c:11]1[cH:10][c:5]([C:6](=[O:7])[CH2:8][Br:9])[cH:4][c:3]([C:2]#[N:1])[c:13]1[O:14]C>>[N:1]#[C:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[CH2:8][Br:9])[cH:10][c:11]([OH:12])[c:13]1[OH:14]
COc1cc(C(=O)CBr)cc(C#N)c1OC
N#Cc1cc(C(=O)CBr)cc(O)c1O
null
null
C(Cl)Cl
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4](-[O;H0;D2;+0:5]-C):[c:6]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4](-[OH;D1;+0:5]):[c:6]
null
[]
null
null
18
HOUR
4.2 g of 5-(bromoacetyl)-2,3-dimethoxybenzonitrile dissolved in 150 ml of methylene chloride are treated with 8.9 ml of boron tribromide. The reaction mixture is stirred at 20° for 18 hours. It is subsequently poured into 220 ml of saturated sodium hydrogen carbonate solution and 100 g of ice, adjusted to pH 6 with gla...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1
Other
C(Cl)Cl
null
18
COc1cc(C(=O)CBr)cc(C#N)c1OC>C(Cl)Cl>N#Cc1cc(C(=O)CBr)cc(O)c1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-21b99671dadd41de8b36e62c0a1d232f
N#Cc1cc(C(=O)CBr)cc(O)c1O.NC(=S)Nc1ccccc1>>N#Cc1cc(-c2csc(Nc3ccccc3)n2)cc(O)c1O
BrCC(=O)C=1C=C(C(=C(C#N)C1)O)O.C1(=CC=CC=C1)NC(=S)N.Cl>>Cl.N(C1=CC=CC=C1)C=1SC=C(N1)C=1C=C(C(=C(C#N)C1)O)O
O=[C:7]([c:6]1[cH:5][c:4]([C:3]#[N:2])[c:22]([OH:23])[c:20]([OH:21])[cH:19]1)[CH2:8]Br.[S:9]=[C:10]([NH:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1)[NH2:18]>>[N:2]#[C:3][c:4]1[cH:5][c:6](-[c:7]2[cH:8][s:9][c:10]([NH:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)[n:18]2)[cH:19][c:20]([OH:21])[c:22]1[OH:23]
N#Cc1cc(C(=O)CBr)cc(O)c1O.NC(=S)Nc1ccccc1
N#Cc1cc(-c2csc(Nc3ccccc3)n2)cc(O)c1O
null
null
CN(C=O)C
Aromatic Heterocycle Formation
OtherReaction
bef473efef1d9ea696235ac9e0e73338149dac4bc5d824d8ecb15263a8e3a4b0
39fbe568f79251ca2d63e869c3b1ee705fef7458c6d99863e8f91d4da02df595
c1ccc(Nc2nc(-c3ccccc3)cs2)cc1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=O)-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7].[NH2;D1;+0:8]-[C;H0;D3;+0:9](=[S;H0;D1;+0:10])-[#7:11]-[c:12]>>[c:12]-[#7:11]-[c;H0;D3;+0:9]1:[n;H0;D2;+0:8]:[c;H0;D3;+0:2](-[c;H0;D3;+0:3](:[c:4]:[c:5]):[c:6]:[c:7]):[cH;D2;+0:1]:[s;H0;D2;+0:10]:1
null
[]
null
null
5
HOUR
3.8 g of 5-(bromoacetyl)-2,3-dihydroxybenzonitrile dissolved in 25 ml of N,N-dimethylformamide are treated with N-phenylthiourea and stirred at 100° for 5 hours. Thereafter, the solvent is removed by evaporation. The residue is treated with 200 ml of 1N sodium carbonate solution and extracted three times with 100 ml of...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Thiourea
null
null
c1cscn1
c1ccccc1.c1cscn1.c1ccccc1
HBr
CN(C=O)C
null
5
N#Cc1cc(C(=O)CBr)cc(O)c1O.NC(=S)Nc1ccccc1>CN(C=O)C>N#Cc1cc(-c2csc(Nc3ccccc3)n2)cc(O)c1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2fdeb7175db243fd8b1813d6a634da82
COc1cc(Br)ccc1OCc1ccccc1.O=Cc1ccnc2ccccc12>>COc1cc(C(O)c2ccnc3ccccc23)ccc1OCc1ccccc1
O.N1=CC=C(C2=CC=CC=C12)C=O.C(C)(C)(C)[Li].C(C1=CC=CC=C1)OC1=C(C=C(C=C1)Br)OC>>C(C1=CC=CC=C1)OC1=C(C=C(C=C1)C(O)C1=CC=NC2=CC=CC=C12)OC
Br[c:5]1[cH:4][c:3]([O:2][CH3:1])[c:20]([O:21][CH2:22][c:23]2[cH:24][cH:25][cH:26][cH:27][cH:28]2)[cH:19][cH:18]1.[CH:6](=[O:7])[c:8]1[cH:9][cH:10][n:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]([OH:7])[c:8]2[cH:9][cH:10][n:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]23)[cH:18][c...
COc1cc(Br)ccc1OCc1ccccc1.O=Cc1ccnc2ccccc12
COc1cc(C(O)c2ccnc3ccccc23)ccc1OCc1ccccc1
null
null
O1CCCC1.C(C)(=O)O
C-C Coupling
Grignard_alcohol
0c8bc0f755f4d9a2cfce93ae43a9a9a531fa8ad86ff120aed0a18ba03c84e4d7
1c0bd0afc1d5e370e3c8193faf738f03752295e40fa0eb99c756011e9a4be26b
c1ccc(COc2ccc(Cc3ccnc4ccccc34)cc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[O;H0;D1;+0:6]=[CH;D2;+0:7]-[c:8]1:[c:9]:[c:10]:[#7;a:11]:[c:12]:[c:13]:1>>[OH;D1;+0:6]-[CH;D3;+0:7](-[c:8]1:[c:9]:[c:10]:[#7;a:11]:[c:12]:[c:13]:1)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
1
HOUR
25 ml of tert.-butyllithium solution (1.4M in hexane) are added dropwise at -70° within 10 minutes to 10 g of 4-(benzyloxy)-3-methoxy-bromobenzene dissolved in 100 ml of tetrahydrofuran. After stirring at -70° for 1 hour, 5 g of quinoline-4-carbaldehyde dissolved in 50 ml of tetrahydrofuran are added dropwise within 30...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aldehyde
Secondary alcohol
c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1.c1ccccc1
Br-
O1CCCC1.C(C)(=O)O
null
1
COc1cc(Br)ccc1OCc1ccccc1.O=Cc1ccnc2ccccc12>O1CCCC1.C(C)(=O)O>COc1cc(C(O)c2ccnc3ccccc23)ccc1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2391726614f84beea4c6846656d926fa
COc1cc(C(=O)c2ccnc3ccccc23)ccc1OCc1ccccc1>>COc1cc(C(=O)c2ccnc3ccccc23)ccc1O
C([O-])(O)=O.[Na+].Br.N1=CC=C(C2=CC=CC=C12)C(=O)C1=CC(=C(C=C1)OCC1=CC=CC=C1)OC>>N1=CC=C(C2=CC=CC=C12)C(=O)C1=CC(=C(C=C1)O)OC
c1ccc(C[O:21][c:20]2[c:3]([O:2][CH3:1])[cH:4][c:5]([C:6](=[O:7])[c:8]3[cH:9][cH:10][n:11][c:12]4[cH:13][cH:14][cH:15][cH:16][c:17]34)[cH:18][cH:19]2)cc1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][n:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]23)[cH:18][cH:19][c:20]1[OH:21]
COc1cc(C(=O)c2ccnc3ccccc23)ccc1OCc1ccccc1
COc1cc(C(=O)c2ccnc3ccccc23)ccc1O
null
null
C(C)(=O)O.C(Cl)Cl
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(c1ccccc1)c1ccnc2ccccc12
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
null
[]
null
null
4.5
HOUR
15 ml of 33 percent hydrobromic acid in glacial acetic acid are added dropwise within 5 minutes at room temperature to 7.5 g of 4-(benzyloxy)-3-methoxyphenyl 4-quinolyl ketone dissolved in 150 ml of methylene chloride. After stirring at 20° for 4.5 hours, the reaction mixture is poured portionwise into 250 ml of satura...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
c1ccccc1.c1ccc2ncccc2c1
Other
C(C)(=O)O.C(Cl)Cl
null
4.5
COc1cc(C(=O)c2ccnc3ccccc23)ccc1OCc1ccccc1>C(C)(=O)O.C(Cl)Cl>COc1cc(C(=O)c2ccnc3ccccc23)ccc1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-79d72dfbe430467d8bd631340094b4e0
COc1cc(C(=O)c2ccnc3ccccc23)ccc1O.O=[N+]([O-])O>>COc1cc(C(=O)c2ccnc3ccccc23)cc([N+](=O)[O-])c1O
N.[N+](=O)(O)[O-].N1=CC=C(C2=CC=CC=C12)C(=O)C1=CC(=C(C=C1)O)OC>>N1=CC=C(C2=CC=CC=C12)C(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])O)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][n:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]23)[cH:18][cH:19][c:23]1[OH:24].O[N+:20](=[O:21])[O-:22]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][n:11][c:12]3[cH:13][cH:14][cH:15][cH:16][c:17]23)[cH:18][c:19]([N+:20](=[O:21])[O-:22])[c:...
COc1cc(C(=O)c2ccnc3ccccc23)ccc1O.O=[N+]([O-])O
COc1cc(C(=O)c2ccnc3ccccc23)cc([N+](=O)[O-])c1O
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=C(c1ccccc1)c1ccnc2ccccc12
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[O;D1;H0:4]=[C:5]-[c:6]:[c:7]:[cH;D2;+0:8]:[c:9](-[O;D1;H1:10]):[c:11]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;D1;H0:3])-[c;H0;D3;+0:8](:[c:7]:[c:6]-[C:5]=[O;D1;H0:4]):[c:9](-[O;D1;H1:10]):[c:11]
null
[]
null
null
3
HOUR
0.37 ml of 65 percent nitric acid is added dropwise at room temperature to 1.3 g of 4-hydroxy-3-methoxyphenyl 4-quinolyl ketone. After stirring for 3 hours the reaction mixture is poured into ice-water, adjusted to pH 6 with conc. ammonia and the precipitate formed is filtered. The thus-obtained residue is heated under...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ncccc2c1
HO-
null
null
3
COc1cc(C(=O)c2ccnc3ccccc23)ccc1O.O=[N+]([O-])O>>COc1cc(C(=O)c2ccnc3ccccc23)cc([N+](=O)[O-])c1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0e0e72cbaa14419480f213f20421c579
COc1cc(C(=O)c2ccnc3ccccc23)cc([N+](=O)[O-])c1O>>O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1ccnc2ccccc12
N1=CC=C(C2=CC=CC=C12)C(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])O)OC.Br>>Br.N1=CC=C(C2=CC=CC=C12)C(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])O)O
C[O:7][c:6]1[cH:5][c:4]([C:3](=[O:2])[c:15]2[cH:16][cH:17][n:18][c:19]3[cH:20][cH:21][cH:22][cH:23][c:24]23)[cH:14][c:10]([N+:11](=[O:12])[O-:13])[c:8]1[OH:9]>>[O:2]=[C:3]([c:4]1[cH:5][c:6]([OH:7])[c:8]([OH:9])[c:10]([N+:11](=[O:12])[O-:13])[cH:14]1)[c:15]1[cH:16][cH:17][n:18][c:19]2[cH:20][cH:21][cH:22][cH:23][c:24]12
COc1cc(C(=O)c2ccnc3ccccc23)cc([N+](=O)[O-])c1O
O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1ccnc2ccccc12
null
null
O
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(c1ccccc1)c1ccnc2ccccc12
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
18
HOUR
1 g of 4-hydroxy-3-methoxy-5-nitrophenyl 4-quinolyl ketone dissolved in 30 ml of 48 percent aqueous hydrobromic acid is stirred at 100° for 18 hours. After cooling to room temperature, the reaction mixture is diluted with 30 ml of water and the precipitate is filtered under suction. There is obtained 3,4-dihydroxy-5-ni...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1ccc2ncccc2c1
Other
O
null
18
COc1cc(C(=O)c2ccnc3ccccc23)cc([N+](=O)[O-])c1O>O>O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1ccnc2ccccc12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ac475188b08e48ee8e91a622daaf4906
COc1cc(C=O)cc([N+](=O)[O-])c1OC.[Li][CH2]CCC>>COc1cc(C(O)c2cccs2)cc([N+](=O)[O-])c1OC
C(CCC)[Li].COC=1C=C(C=O)C=C(C1OC)[N+](=O)[O-].S(O)(O)(=O)=O>>COC=1C=C(C=C(C1OC)[N+](=O)[O-])C(O)C=1SC=CC1
[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]=[O:7])[cH:13][c:14]([N+:15](=[O:16])[O-:17])[c:18]1[O:19][CH3:20].[Li][CH2:10][CH2:11][CH2:9][CH3:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]([OH:7])[c:8]2[cH:9][cH:10][cH:11][s:12]2)[cH:13][c:14]([N+:15](=[O:16])[O-:17])[c:18]1[O:19][CH3:20]
COc1cc(C=O)cc([N+](=O)[O-])c1OC.[Li][CH2]CCC
COc1cc(C(O)c2cccs2)cc([N+](=O)[O-])c1OC
null
null
O1CCCC1
Aromatic Heterocycle Formation
OtherReaction
661e7f8071acc0898ca40b7ca38444f163c7212e8a16f4ad52f40bf89281dbb8
18b29b9c7cb3e5d60d4b6da2d631bced0464176d02310b4899c1610484f5ac30
c1ccc(Cc2cccs2)cc1
[CH3;D1;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[Li].[O;H0;D1;+0:5]=[CH;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[OH;D1;+0:5]-[CH;D3;+0:6](-[c:7](:[c:8]):[c:9])-[c;H0;D3;+0:1]1:[#16;a:10]:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:2]:1
null
[]
null
null
30
MINUTE
18.8 ml of n-butyllithium solution (1.6M in hexane) are added dropwise at -50° within 10 minutes to 4.03 g of thiophone dissolved in 40 ml of tetrahydrofuran. After stirring at -50° for 30 minutes 6.3 g of 3,4-dimethoxy-5-nitrobenzaldehyde dissolved in 100 ml of tetrahydrofuran are added dropwise within 30 minutes. The...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Alkyl lithium
Secondary alcohol
null
c1ccsc1
c1ccccc1.c1ccsc1
null
O1CCCC1
null
0.5
COc1cc(C=O)cc([N+](=O)[O-])c1OC.[Li][CH2]CCC>O1CCCC1>COc1cc(C(O)c2cccs2)cc([N+](=O)[O-])c1OC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c6ffc2b54698401c861526dd4690776e
COc1cc(C(O)c2cccs2)cc([N+](=O)[O-])c1OC>>COc1cc(C(=O)c2cccs2)cc([N+](=O)[O-])c1OC
COC=1C=C(C=C(C1OC)[N+](=O)[O-])C(O)C=1SC=CC1>>S1C(=CC=C1)C(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])OC)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]([OH:7])[c:8]2[cH:9][cH:10][cH:11][s:12]2)[cH:13][c:14]([N+:15](=[O:16])[O-:17])[c:18]1[O:19][CH3:20]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][s:12]2)[cH:13][c:14]([N+:15](=[O:16])[O-:17])[c:18]1[O:19][CH3:20]
COc1cc(C(O)c2cccs2)cc([N+](=O)[O-])c1OC
COc1cc(C(=O)c2cccs2)cc([N+](=O)[O-])c1OC
null
[O-2].[O-2].[Mn+4]
CC(=O)C
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
c7c20d2959ac48847b03cc1265962cf99a8ec8a85900c087dabb30077298c66c
767cfd93f5821ebb9e1e72addd9cb404b20b0c821d246ae6b87a5776b74a455b
O=C(c1ccccc1)c1cccs1
[OH;D1;+0:1]-[CH;D3;+0:2](-[c:3](:[c:4]):[c:5])-[c:6](:[c:7]):[#16;a:8]:[c:9]>>[O;H0;D1;+0:1]=[C;H0;D3;+0:2](-[c:3](:[c:4]):[c:5])-[c:6](:[c:7]):[#16;a:8]:[c:9]
null
[]
null
null
null
null
9.9 g of α-(3,4-dimethoxy-5-nitrophenyl)-2-thiophenemethanol dissolved in 300 ml of acetone are treated with 90 g of manganese dioxide and heated under reflux for 4 hours. The manganese dioxide is removed by suction filtration and the filtrate is evaporated. There is obtained 3,4-dimethoxy-5-nitrophenyl 2-thienyl keton...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ketone
null
null
c1ccccc1.c1ccsc1
null
[O-2].[O-2].[Mn+4].CC(=O)C
null
null
COc1cc(C(O)c2cccs2)cc([N+](=O)[O-])c1OC>[O-2].[O-2].[Mn+4].CC(=O)C>COc1cc(C(=O)c2cccs2)cc([N+](=O)[O-])c1OC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d4e18fa418d445f6af7e22b2933b4461
COc1cc(C(=O)c2cccs2)cc([N+](=O)[O-])c1OC>>O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1cccs1
S1C(=CC=C1)C(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])OC)OC>>S1C(=CC=C1)C(=O)C1=CC(=C(C(=C1)[N+](=O)[O-])O)O
C[O:6][c:5]1[cH:4][c:3]([C:2](=[O:1])[c:14]2[cH:15][cH:16][cH:17][s:18]2)[cH:13][c:9]([N+:10](=[O:11])[O-:12])[c:7]1[O:8]C>>[O:1]=[C:2]([c:3]1[cH:4][c:5]([OH:6])[c:7]([OH:8])[c:9]([N+:10](=[O:11])[O-:12])[cH:13]1)[c:14]1[cH:15][cH:16][cH:17][s:18]1
COc1cc(C(=O)c2cccs2)cc([N+](=O)[O-])c1OC
O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1cccs1
null
null
C(C)(=O)O.Br
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
O=C(c1ccccc1)c1cccs1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4](-[O;H0;D2;+0:5]-C):[c:6]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4](-[OH;D1;+0:5]):[c:6]
null
[]
null
null
null
null
2 g of 3,4-dimethoxy-5-nitrophenyl 2-thienyl ketone are stirred at 100° for 8 hours in a mixture of 20 ml of 30-33 percent hydrobromic acid in glacial acetic acid and 20 ml of 48 percent aqueous hydrobromic acid. The reaction mixture is subsequently evaporated to dryness. The residue is taken up in ethyl acetate, washe...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1.c1ccsc1
Other
C(C)(=O)O.Br
null
null
COc1cc(C(=O)c2cccs2)cc([N+](=O)[O-])c1OC>C(C)(=O)O.Br>O=C(c1cc(O)c(O)c([N+](=O)[O-])c1)c1cccs1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b0b474ca97b1456681b659e1caf77daf
CC(=O)Nc1ccccc1.O=[N+]([O-])O>>CC(=O)Nc1ccc([N+](=O)[O-])cc1
C(C)(=O)NC1=CC=CC=C1.[N+](=O)(O)[O-].S(O)(O)(=O)=O>>CC(=O)NC1=CC=C(C=C1)[N+](=O)[O-]
[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][cH:8][cH:12][cH:13]1.O[N+:9](=[O:10])[O-:11]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1
CC(=O)Nc1ccccc1.O=[N+]([O-])O
CC(=O)Nc1ccc([N+](=O)[O-])cc1
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;D1;H0:3])-[c;H0;D3;+0:6](:[c:5]:[c:4]):[c:7]:[c:8]
null
[]
null
null
null
null
nitrating acetanilide using a mixture of nitric acid and sulfuric acid to produce 4-nitroacetanilide and nitrating further using a mixture of nitric acid and sulfuric acid to produce VI; Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
CC(=O)Nc1ccccc1.O=[N+]([O-])O>>CC(=O)Nc1ccc([N+](=O)[O-])cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3c454c91ecb24bbd82b66c7cb9c203d6
Nc1c([N+](=O)[O-])cc([N+](=O)[O-])cc1[N+](=O)[O-]>>Nc1c([N+](=O)[O-])cc([N+](=O)[O-])c(N)c1[N+](=O)[O-]
Cl.C1=C(C=C(C(=C1[N+](=O)[O-])N)[N+](=O)[O-])[N+](=O)[O-].C(C1=CC=CC=C1)ON.C[O-].[Na+]>>C1=C(C(=C(C(=C1[N+](=O)[O-])N)[N+](=O)[O-])N)[N+](=O)[O-]
[NH2:1][c:2]1[c:3]([N+:4](=[O:5])[O-:6])[cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][c:14]1[N+:15](=[O:16])[O-:17]>>[NH2:1][c:2]1[c:3]([N+:4](=[O:5])[O-:6])[cH:7][c:8]([N+:9](=[O:10])[O-:11])[c:12]([NH2:13])[c:14]1[N+:15](=[O:16])[O-:17]
Nc1c([N+](=O)[O-])cc([N+](=O)[O-])cc1[N+](=O)[O-]
Nc1c([N+](=O)[O-])cc([N+](=O)[O-])c(N)c1[N+](=O)[O-]
null
null
CS(=O)C
Functional Group Addition
OtherReaction
60732f4102305dd78afd0dd3679bbaf7f92e00d937b526eb4d81318ee97c4790
d69ce1fde4173969963123914389bef807fad83b73b8a587195a7122d5cdf1d2
c1ccccc1
[#7;+:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5](-[#7;+:6]):[c:7]>>[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[N;D1;H2:8]):[c:5](-[#7;+:6]):[c:7]
87.4
[{"value": 87.0, "product": "C1=C(C(=C(C(=C1[N+](=O)[O-])N)[N+](=O)[O-])N)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.4, "product": "C1=C(C(=C(C(=C1[N+](=O)[O-])N)[N+](=O)[O-])N)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
HOUR
DMSO (15 ml) is added with rapid stirring to a mixture of picramide (0.477 g, 2.09 mmol), O-benzylhydroxylamine (1.64 g, 10.3 mmol) and sodium methoxide (1.91 g, 35.4 mmol). The brown suspension is stirred at ambient temperature for 15 hr. The reaction mixture is poured into cold 0.12N aqueous HCl (200 ml). The resulti...
10.6084/m9.figshare.5104873.v1
null
null
Primary amine
c1ccccc1
c1ccccc1
c1ccccc1
Other
CS(=O)C
null
15
Nc1c([N+](=O)[O-])cc([N+](=O)[O-])cc1[N+](=O)[O-]>CS(=O)C>Nc1c([N+](=O)[O-])cc([N+](=O)[O-])c(N)c1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7244e5de2c67430a83f92a241e475c14
CC(=O)Nc1ccccc1.O=[N+]([O-])O>>CC(=O)Nc1ccc([N+](=O)[O-])cc1
C(C)(=O)NC1=CC=CC=C1.[N+](=O)(O)[O-].S(O)(O)(=O)=O>>CC(=O)NC1=CC=C(C=C1)[N+](=O)[O-]
[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][cH:8][cH:12][cH:13]1.O[N+:9](=[O:10])[O-:11]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1
CC(=O)Nc1ccccc1.O=[N+]([O-])O
CC(=O)Nc1ccc([N+](=O)[O-])cc1
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;D1;H0:3])-[c;H0;D3;+0:6](:[c:5]:[c:4]):[c:7]:[c:8]
null
[]
null
null
null
null
nitrating acetanilide using a mixture of nitric acid and sulfuric acid to produce 4-nitroacetanilide and nitrating further using a mixture of nitric acid and sulfuric acid to produce compound VI; Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
CC(=O)Nc1ccccc1.O=[N+]([O-])O>>CC(=O)Nc1ccc([N+](=O)[O-])cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d7c519f58a6c4629bc42c97f592c844b
CC(=O)Oc1ccc2c(c1)[C@H](O)C[C@@H]1[C@@H]2CC[C@]2(C)C=CC[C@@H]12>>C[C@@]12C=CC[C@H]1[C@@H]1C[C@@H](O)c3cc(O)ccc3[C@H]1CC2
C(C)(=O)OC1=CC=2[C@@H](C[C@H]3[C@@H]4CC=C[C@@]4(C)CC[C@@H]3C2C=C1)O.C(C)(=O)[O-]>>C[C@@]12C=CC[C@H]1[C@@H]1C[C@H](C=3C=C(C=CC3[C@H]1CC2)O)O
CC(=O)[O:14][c:13]1[cH:12][c:11]2[c:17]([cH:16][cH:15]1)[C@@H:18]1[C@H:7]([C@H:6]3[C@@:2]([CH3:1])([CH:3]=[CH:4][CH2:5]3)[CH2:20][CH2:19]1)[CH2:8][C@H:9]2[OH:10]>>[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][C@@H:9]([OH:10])[c:11]3[cH:12][c:13]([OH:14])[cH:15][cH:16][c:17]3[C@H:18]1[CH2:19][CH2:20]2
CC(=O)Oc1ccc2c(c1)[C@H](O)C[C@@H]1[C@@H]2CC[C@]2(C)C=CC[C@@H]12
C[C@@]12C=CC[C@H]1[C@@H]1C[C@@H](O)c3cc(O)ccc3[C@H]1CC2
null
null
null
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
db7d50f1ad65e3456617ab9bc6ab5b9ede0e069a6dd971d117a653e2a40b05de
efe1c37482b229370967d04d1a68db10ee663983a92b84fa0f009f5bb178597f
C1=CC2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
6β-HYDROXYESTRA-1,3,5(10),16-TETRAEN-3-YL ACETATE (Acetate of E12/N1) Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ester
Aromatic alcohol
null
null
C1=C[C@@H]2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
HO-
null
null
null
CC(=O)Oc1ccc2c(c1)[C@H](O)C[C@@H]1[C@@H]2CC[C@]2(C)C=CC[C@@H]12>>C[C@@]12C=CC[C@H]1[C@@H]1C[C@@H](O)c3cc(O)ccc3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-33907cecb1614b779cc8c7288c4d0f70
CC(=O)Oc1ccc2c3c(ccc2c1)[C@@H]1CC=C[C@@]1(C)CC3>>C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C
C(C)(=O)OC1=CC2=CC=C3[C@@H]4CC=C[C@@]4(C)CCC3=C2C=C1.C(C)(=O)[O-]>>C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)=O
CC(=O)[O:12][c:11]1[cH:10][c:9]2[cH:8][cH:7][c:6]3[c:16]([c:15]2[cH:14][cH:13]1)[CH2:17][CH2:18][C@:19]1([CH3:20])[CH:2]=[CH:3][CH2:4][C@@H:5]31>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][C:9]4=[CH:10][C:11](=[O:12])[CH2:13][CH2:14][C@@H:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]
CC(=O)Oc1ccc2c3c(ccc2c1)[C@@H]1CC=C[C@@]1(C)CC3
C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C
null
null
null
Reduction
OtherReaction
c0f1a18ea822e10b2b924b15b29531f2a9546a4fcb3176721a6e21fd9610a270
042913d2a4053e95d008323463f697351e585aee96acad85f412a98f9122a77f
C=C1CC[C@@H]2C1CC[C@H]1[C@H]2CCC2=CC(=O)CC[C@@H]21
C-C(=O)-[O;H0;D2;+0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[c;H0;D3;+0:4]2:[cH;D2;+0:5]:[cH;D2;+0:6]:[c;H0;D3;+0:7]3:[c;H0;D3;+0:8](:[c;H0;D3;+0:9]:2:[cH;D2;+0:10]:[cH;D2;+0:11]:1)-[C:12]-[C:13]-[C:14]1(-[C;D1;H3:15])-[CH;D2;+0:16]=[CH;D2;+0:17]-[C:18]-[C:19]-3-1>>[C;D1;H2:20]=[C;H0;D3;+0:16]1-[CH2;D2;+0:17]-[C:18]-[C:19]2-[C...
null
[]
null
null
null
null
ESTRA-1,3,5,7,9,16-HEXAEN-3-YL ACETATE (Acetate of E10/N1) Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ester
Ketone.Vinyl
C1=C[C@H]2CCc3c(ccc4ccccc34)[C@@H]2C1
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
Other
null
null
null
CC(=O)Oc1ccc2c3c(ccc2c1)[C@@H]1CC=C[C@@]1(C)CC3>>C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-faefcb6adc014d408ac9431750c1a3af
C[C@@]12C=CC[C@H]1[C@@H]1CC(=O)c3cc(CC(=O)[O-])ccc3[C@H]1CC2>>C[C@@]12C=CC[C@H]1[C@@H]1CC(O)c3cc(O)ccc3[C@H]1CC2
[H-].[Al+3].[Li+].[H-].[H-].[H-].C1CCOC1.C[C@@]12C=CC[C@H]1[C@@H]1CC(C=3C=C(C=CC3[C@H]1CC2)CC(=O)[O-])=O.C1CCOC1.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>C[C@@]12C=CC[C@H]1[C@@H]1CC(C=3C=C(C=CC3[C@H]1CC2)O)O
O=C(C[c:13]1[cH:12][c:11]2[c:17]([cH:16][cH:15]1)[C@@H:18]1[C@H:7]([C@H:6]3[C@@:2]([CH3:1])([CH:3]=[CH:4][CH2:5]3)[CH2:20][CH2:19]1)[CH2:8][C:9]2=[O:10])[O-:14]>>[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH:9]([OH:10])[c:11]3[cH:12][c:13]([OH:14])[cH:15][cH:16][c:17]3[C@H:18]1[CH2:19][CH2:20]2
C[C@@]12C=CC[C@H]1[C@@H]1CC(=O)c3cc(CC(=O)[O-])ccc3[C@H]1CC2
C[C@@]12C=CC[C@H]1[C@@H]1CC(O)c3cc(O)ccc3[C@H]1CC2
null
null
null
Miscellaneous
OtherReaction
cc2f5e8005a287a08c065935489dee192fce1a046b7112c1d4cb35ce45b1c55a
ab1b13ab052e8454aed68379869f83b5f307c8e8172db29eaf75ac46c3da9c09
C1=CC2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
O=C(-[O-;H0;D1:1])-C-[c;H0;D3;+0:2]1:[c:3]:[c:4](:[c:5]:[c:6]:[c:7]:1)-[C;H0;D3;+0:8](=[O;H0;D1;+0:9])-[C:10]-[C:11]>>[C:11]-[C:10]-[CH;D3;+0:8](-[OH;D1;+0:9])-[c:4]1:[c:3]:[c;H0;D3;+0:2](-[OH;D1;+0:1]):[c:7]:[c:6]:[c:5]:1
10
[{"value": 10.0, "product": "C[C@@]12C=CC[C@H]1[C@@H]1CC(C=3C=C(C=CC3[C@H]1CC2)O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of lithium aluminum hydride (LAH, 95%, 46.9 mg, 1.17 mmol) in 5 mL of anhydrous THF was added estra-1,3,5(10),16-tetraen-6-one-3-yl-acetate (6) (422.9 mg, 1.360 mmol) in 5 mL of anhydrous THF dropwise, with stirring. The reaction was stirred 50 min., after which further LAH (46.5 mg, 1.16 mmol) was adde...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol.Aromatic alcohol
C1=C[C@H]2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
C1=C[C@@H]2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
C1=C[C@@H]2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
Other
null
null
null
C[C@@]12C=CC[C@H]1[C@@H]1CC(=O)c3cc(CC(=O)[O-])ccc3[C@H]1CC2>>C[C@@]12C=CC[C@H]1[C@@H]1CC(O)c3cc(O)ccc3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cc1b14e0a7fe4a6e80978c8fa4432adb
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O>>C[C@@]12CCC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2
Cl.NN.[OH-].[K+].C[C@]12CC[C@@H]3C=4C=CC(=CC4CC=C3[C@@H]1CCC2=O)O>>C[C@@]12CCC[C@H]1C1=CCC=3C=C(C=CC3[C@H]1CC2)O
O=[C:3]1[C@:2]2([CH3:1])[C@@H:6]([CH2:5][CH2:4]1)[C:7]1=[CH:8][CH2:9][c:10]3[cH:11][c:12]([OH:13])[cH:14][cH:15][c:16]3[C@H:17]1[CH2:18][CH2:19]2>>[CH3:1][C@@:2]12[CH2:3][CH2:4][CH2:5][C@H:6]1[C:7]1=[CH:8][CH2:9][c:10]3[cH:11][c:12]([OH:13])[cH:14][cH:15][c:16]3[C@H:17]1[CH2:18][CH2:19]2
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O
C[C@@]12CCC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2
null
null
O.C(COCCO)O
Reduction
OtherReaction
11b0f05f13f348a1e22dfedd2b26d07f1878b2edd41602781ca10f6aa8c5cfef
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
C1=C2[C@H](CCC3CCC[C@@H]23)c2ccccc2C1
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4](-[C:5]=[C:6])-[C:7]-1(-[C;D1;H3:8])-[C:9]>>[C:9]-[C:7]1(-[C;D1;H3:8])-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4]-1-[C:5]=[C:6]
14
[{"value": 14.0, "product": "C[C@@]12CCC[C@H]1C1=CCC=3C=C(C=CC3[C@H]1CC2)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 13.9, "product": "C[C@@]12CCC[C@H]1C1=CCC=3C=C(C=CC3[C@H]1CC2)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a suspension of equilin (100.2 mg, 0.3733 mmol) in 2 mL of diethylene glycol were added hydrazine (59 μL, 1.9 mmol) and potassium hydroxide (0.04 g, 0.7 mmol). The mixture was stirred in an oil bath at 200°-214° C. for 2 h, after which the cooled reaction was diluted with 10 mL of water, neutralized with 1N HCl, and...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
C1=C2[C@H](CC[C@@H]3CCC[C@@H]23)c2ccccc2C1
C1=C2[C@H](CC[C@H]3CCC[C@@H]23)c2ccccc2C1
C1=C2[C@H](CC[C@H]3CCC[C@@H]23)c2ccccc2C1
Other
O.C(COCCO)O
null
2
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O>O.C(COCCO)O>C[C@@]12CCC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-13e55dc3a2d64554a99a1dd2a344d976
C[C@]12CC[C@@H]3c4ccc(O)cc4C=C[C@H]3[C@@H]1CCC2=O>>C[C@@]12CCC[C@H]1[C@@H]1C=Cc3cc(O)ccc3[C@H]1CC2
Cl.C[C@@]12C(CC[C@H]1[C@@H]1C=CC=3C=C(C=CC3[C@H]1CC2)O)=O.NN.[OH-].[K+]>>C[C@@]12CCC[C@H]1[C@@H]1C=CC=3C=C(C=CC3[C@H]1CC2)O
O=[C:3]1[C@:2]2([CH3:1])[C@@H:6]([CH2:5][CH2:4]1)[C@@H:7]1[CH:8]=[CH:9][c:10]3[cH:11][c:12]([OH:13])[cH:14][cH:15][c:16]3[C@H:17]1[CH2:18][CH2:19]2>>[CH3:1][C@@:2]12[CH2:3][CH2:4][CH2:5][C@H:6]1[C@@H:7]1[CH:8]=[CH:9][c:10]3[cH:11][c:12]([OH:13])[cH:14][cH:15][c:16]3[C@H:17]1[CH2:18][CH2:19]2
C[C@]12CC[C@@H]3c4ccc(O)cc4C=C[C@H]3[C@@H]1CCC2=O
C[C@@]12CCC[C@H]1[C@@H]1C=Cc3cc(O)ccc3[C@H]1CC2
null
null
O.C(COCCO)O
Reduction
OtherReaction
eecb09633bf6a470053455cdcdf5805617dbff75e27df63d7964b5bd688fd862
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
C1=C[C@@H]2[C@H](CCC3CCC[C@H]32)c2ccccc21
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1(-[C;D1;H3:6])-[C:7]>>[C:7]-[C:5]1(-[C;D1;H3:6])-[C:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-1
null
[]
null
null
null
null
Estra-1,3,5(10),6-tetraen-3-ol-17-one (91.1 mg, 0.339 mmol), hydrazine (54 μL, 1.7 mmol), and potassium hydroxide (0.06 g) in 1.8 mL of diethylene glycol were heated in a 200° C. bath under argon for 2 h. After cooling to RT 10 mL of water were added and the solution was acidified to pH≈2 with 1N HCl. The resulting sus...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
C1=C[C@H]2[C@@H]3CCC[C@H]3CC[C@@H]2c2ccccc21
C1=C[C@H]2[C@@H]3CCC[C@@H]3CC[C@@H]2c2ccccc21
C1=C[C@H]2[C@@H]3CCC[C@@H]3CC[C@@H]2c2ccccc21
Other
O.C(COCCO)O
null
null
C[C@]12CC[C@@H]3c4ccc(O)cc4C=C[C@H]3[C@@H]1CCC2=O>O.C(COCCO)O>C[C@@]12CCC[C@H]1[C@@H]1C=Cc3cc(O)ccc3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-64dc57ddcc04413ba25434526df7bca5
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CC[C@@H]3[C@H]1CC2>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(O)CC[C@@H]3[C@H]1CC2
O.O.O.O.O.O.O.O.O.O.S(=O)(=O)([O-])[O-].[Na+].[Na+].C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)=O.C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)=O.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)O
[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH2:9][C:10]3=[CH:11][C:12](=[O:13])[CH2:14][CH2:15][C@@H:16]3[C@H:17]1[CH2:18][CH2:19]2>>[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH2:9][C:10]3=[CH:11][CH:12]([OH:13])[CH2:14][CH2:15][C@@H:16]3[C@H:17]1[CH2:18][CH2:19]2
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CC[C@@H]3[C@H]1CC2
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(O)CC[C@@H]3[C@H]1CC2
null
null
CCOCC
Reduction
Reduction of ketone to secondary alcohol
dee937cc1d956629e7fc3568753db0f6a443a8832909c31808ca7ad163002c5f
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CC2CC[C@H]3[C@@H](CCC4=CCCC[C@@H]43)[C@@H]2C1
[C:1]-[C:2]1=[C:3]-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[C:6]-[C:7]-[C:8]-1>>[C:1]-[C:2]1=[C:3]-[CH;D3;+0:4](-[OH;D1;+0:5])-[C:6]-[C:7]-[C:8]-1
null
[]
null
null
17
MINUTE
To estra-4,16-dien-3-one, (1) (87.2 mg, 0.340 mmol) in 1.7 mL of anh. ether was added lithium aluminum hydride (15.0 mg, 0.395 mmol) and the suspension was stirred 17 min. Reaction was then agitated 10 min. with 0.50 g of sodium sulfate decahydrate and filtered through Celite. The residue was washed with three 10 mL po...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4=CCCC[C@@H]43)[C@@H]2C1
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4=CCCC[C@@H]43)[C@@H]2C1
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4=CCCC[C@@H]43)[C@@H]2C1
null
CCOCC
null
0.283333
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CC[C@@H]3[C@H]1CC2>CCOCC>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(O)CC[C@@H]3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-03b574ac27ae4dca90e3d4f976fa9ef4
C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CC[C@@H]3[C@H]1CC2
C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=CC(=O)CC[C@H]34.C(C)(=O)[O-].CC(=O)OC(=O)C.N#N.C(C)(=O)[O-]>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)=O
O[C@@H:3]1[C@:2]2([CH3:1])[C@@H:6]([CH2:5][CH2:4]1)[C@@H:7]1[CH2:8][CH2:9][C:10]3=[CH:11][C:12](=[O:13])[CH2:14][CH2:15][C@@H:16]3[C@H:17]1[CH2:18][CH2:19]2>>[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH2:9][C:10]3=[CH:11][C:12](=[O:13])[CH2:14][CH2:15][C@@H:16]3[C@H:17]1[CH2:18][CH2:19]2
C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CC[C@@H]3[C@H]1CC2
null
null
N1=CC=CC=C1.C1(=CC=CC=C1)C.C(Cl)Cl
Functional Group Interconversion
OtherReaction
e0b95ade950374b335849c20f817b6abe1cda9d562afeb4f105c11c5a481b532
f8118e7f3e1d7109575c0c77239dee8da98ec71a2b23460bcda2084274bdf7e7
O=C1C=C2CC[C@@H]3[C@H](CCC4C=CC[C@H]43)[C@H]2CC1
O-[C@H;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[C:5]-1(-[C;D1;H3:6])-[C:7]>>[C:7]-[C:5]1(-[C;D1;H3:6])-[C:4]-[C:3]-[CH;D2;+0:2]=[CH;D2;+0:1]-1
28
[{"value": 28.0, "product": "C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
This synthesis is depicted in FIG. 11. 19-Nor-testosterone (XIX) is commercially available, e.g., from Chemical Dynamics Corp. It provides the starting material for 19-Nor-16-androstene derivatives. 19-Nor-testosterone (XIX) was converted into the acetate (Hartman, J. A. et al., J. Am. Chem. Soc. (1956) 78:5662) with a...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4=CCCC[C@@H]43)[C@@H]2C1
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4=CCCC[C@@H]43)[C@@H]2C1
HO-
N1=CC=CC=C1.C1(=CC=CC=C1)C.C(Cl)Cl
null
null
C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O>N1=CC=CC=C1.C1(=CC=CC=C1)C.C(Cl)Cl>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CC[C@@H]3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8ea679507e1a43dfb8823c5133c2a071
C[C@@]12C=CC[C@H]1[C@@H]1CCC3CC(=O)CC[C@@H]3[C@H]1CC2>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3C[C@H](O)CC[C@@H]3[C@H]1CC2
CCC([BH-](C(CC)C)C(CC)C)C.[Li+].C[C@@]12C=CC[C@H]1[C@@H]1CCC3CC(CC[C@@H]3[C@H]1CC2)=O.[OH-].[Na+].OO>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3C[C@@H](CC[C@@H]3[C@H]1CC2)O
[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH2:9][CH:10]3[CH2:11][C:12](=[O:13])[CH2:14][CH2:15][C@@H:16]3[C@H:17]1[CH2:18][CH2:19]2>>[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH2:9][CH:10]3[CH2:11][C@H:12]([OH:13])[CH2:14][CH2:15][C@@H:16]3[C@H:17]1[CH2:18][CH2:19]2
C[C@@]12C=CC[C@H]1[C@@H]1CCC3CC(=O)CC[C@@H]3[C@H]1CC2
C[C@@]12C=CC[C@H]1[C@@H]1CCC3C[C@H](O)CC[C@@H]3[C@H]1CC2
null
null
O.CCOCC.C1CCOC1
Reduction
Reduction of ketone to secondary alcohol
cb85db3f3980e7ea597896adaf5455a2c05ef13ef2470093bc4791ad567ed2e7
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CC2CC[C@H]3[C@@H](CCC4CCCC[C@@H]43)[C@@H]2C1
[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[C:5]-[C:6]>>[C:1]-[C:2]-[C@H;D3;+0:3](-[OH;D1;+0:4])-[C:5]-[C:6]
87
[{"value": 87.0, "product": "C[C@@]12C=CC[C@H]1[C@@H]1CCC3C[C@@H](CC[C@@H]3[C@H]1CC2)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.7, "product": "C[C@@]12C=CC[C@H]1[C@@H]1CCC3C[C@@H](CC[C@@H]3[C@H]1CC2)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
This synthesis is depicted in FIG. 11. L-Selectride (d, lithium tri(sec-butyl)hydridoborate, 4 ml of a 1M solution in THF, 4 mmol) was added dropwise at 0° to a solution of ketone 10 (800 mg, 3.10 mmol) in dry ether (5 ml). After stirring for 1 h at 0°, water was added (10 ml). The boranes were oxidized by adding 10% a...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4CCCC[C@@H]43)[C@@H]2C1
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4CCCC[C@@H]43)[C@@H]2C1
C1=C[C@@H]2CC[C@H]3[C@@H](CCC4CCCC[C@@H]43)[C@@H]2C1
null
O.CCOCC.C1CCOC1
null
1
C[C@@]12C=CC[C@H]1[C@@H]1CCC3CC(=O)CC[C@@H]3[C@H]1CC2>O.CCOCC.C1CCOC1>C[C@@]12C=CC[C@H]1[C@@H]1CCC3C[C@H](O)CC[C@@H]3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4eb3c756514440079e34b385af51e750
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=C(CCC(=O)C3)[C@H]1CC2>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CCC3=C1CC2
C[C@@]12C=CC[C@H]1[C@@H]1CCC=3CC(CCC3[C@H]1CC2)=O.C[C@@]12C=CC[C@H]1[C@@H]1CCC=3CC(CCC3[C@H]1CC2)=O.N1=CC=CC=C1.C1(=CC=CC=C1)O>>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(CCC3=C1CC2)=O
[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH2:9][C:10]3=[C:16]([CH2:15][CH2:14][C:12](=[O:13])[CH2:11]3)[C@H:17]1[CH2:18][CH2:19]2>>[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH2:9][C:10]3=[CH:11][C:12](=[O:13])[CH2:14][CH2:15][C:16]3=[C:17]1[CH2:18][CH2:19]2
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=C(CCC(=O)C3)[C@H]1CC2
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CCC3=C1CC2
null
null
C(C)(=O)OCC
Miscellaneous
OtherReaction
90fc578482e51c8b1c4837e66a0377326f0e500906b54de91f1021394be28d13
f394080031812a9c0cde55fa330311dfe42bea38dbdf0b4621700859838ffa32
O=C1C=C2CC[C@@H]3C(=C2CC1)CCC1C=CC[C@H]13
[C:1]-[C:2]-[C@H;D3;+0:3]1-[C:4](-[C:5])-[C:6]-[C:7]-[C;H0;D3;+0:8]2=[C;H0;D3;+0:9]-1-[C:10]-[C:11]-[C:12](=[O;D1;H0:13])-[CH2;D2;+0:14]-2>>[C:1]-[C:2]-[C;H0;D3;+0:3]1=[C;H0;D3;+0:9]2-[C:10]-[C:11]-[C:12](=[O;D1;H0:13])-[CH;D2;+0:14]=[C;H0;D3;+0:8]-2-[C:7]-[C:6]-[C:4]-1-[C:5]
31
[{"value": 31.0, "product": "C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(CCC3=C1CC2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
MINUTE
Estra-5(10),16-dien-3-one, 3 (0.38 g, 1.5 mmol), in pyridine (5.0 mL, 62 mmol) was cooled in an ice-salt bath to -13° C. and pyridinium bromide perbromide (1.58 g, 4.94 mmol) was added in small portions so that T<-4° C. After swirling 1 min. phenol (0.25 g, 2.7 mmol) was added and reaction continued 24 h at room temper...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
C1=C[C@@H]2CC[C@@H]3C4=C(CCCC4)CC[C@H]3[C@@H]2C1
C1=C[C@@H]2CCC3=C4CCCC=C4CC[C@H]3[C@@H]2C1
C1=C[C@@H]2CCC3=C4CCCC=C4CC[C@H]3[C@@H]2C1
null
C(C)(=O)OCC
null
0.016667
C[C@@]12C=CC[C@H]1[C@@H]1CCC3=C(CCC(=O)C3)[C@H]1CC2>C(C)(=O)OCC>C[C@@]12C=CC[C@H]1[C@@H]1CCC3=CC(=O)CCC3=C1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-52f5f6e37c8948ff842063e43a31449a
CC(=O)Oc1ccc2c(c1)C(=O)C[C@@H]1[C@@H]2CC[C@]2(C)C=CC[C@@H]12>>C[C@@]12C=CC[C@H]1[C@@H]1CC(O)c3cc(O)ccc3[C@H]1CC2
[H-].[Al+3].[Li+].[H-].[H-].[H-].C(C)(=O)OC1=CC=2C(C[C@H]3[C@@H]4CC=C[C@@]4(C)CC[C@@H]3C2C=C1)=O.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>C[C@@]12C=CC[C@H]1[C@@H]1CC(C=3C=C(C=CC3[C@H]1CC2)O)O
CC(=O)[O:14][c:13]1[cH:12][c:11]2[c:17]([cH:16][cH:15]1)[C@@H:18]1[C@H:7]([C@H:6]3[C@@:2]([CH3:1])([CH:3]=[CH:4][CH2:5]3)[CH2:20][CH2:19]1)[CH2:8][C:9]2=[O:10]>>[CH3:1][C@@:2]12[CH:3]=[CH:4][CH2:5][C@H:6]1[C@@H:7]1[CH2:8][CH:9]([OH:10])[c:11]3[cH:12][c:13]([OH:14])[cH:15][cH:16][c:17]3[C@H:18]1[CH2:19][CH2:20]2
CC(=O)Oc1ccc2c(c1)C(=O)C[C@@H]1[C@@H]2CC[C@]2(C)C=CC[C@@H]12
C[C@@]12C=CC[C@H]1[C@@H]1CC(O)c3cc(O)ccc3[C@H]1CC2
null
null
C1CCOC1
Reduction
OtherReaction
5c3011efb770f5bb284f9eda986003f634d1804b0054957f56865b0f5cfeb83c
0ceccbeb1a171407aae4661a0628d0d4c1bc76338bade38dd330e39814e68322
C1=CC2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]:[c:5](:[c:6])-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[C:9]-[C:10]>>[C:10]-[C:9]-[CH;D3;+0:7](-[OH;D1;+0:8])-[c:5](:[c:6]):[c:4]:[c:2](-[OH;D1;+0:1]):[c:3]
10
[{"value": 10.0, "product": "C[C@@]12C=CC[C@H]1[C@@H]1CC(C=3C=C(C=CC3[C@H]1CC2)O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of lithium aluminum hydride (LAH, 95%, 46.9 mg, 1.17 mmol) in 5 mL of anhydrous THF was added estra-1,3,5(10),16-tetraen-6-one-3-yl acetate, 6 (422.9 mg, 1.360 mmol) in 5 mL of anhydrous THF dropwise, with stirring. See FIG. 13. The reaction was stirred 50 min., after which further LAH (46.5 mg, 1.16 mm...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Secondary alcohol.Aromatic alcohol
C1=C[C@H]2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
C1=C[C@@H]2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
C1=C[C@@H]2CC[C@@H]3c4ccccc4CC[C@H]3[C@@H]2C1
Other
C1CCOC1
null
null
CC(=O)Oc1ccc2c(c1)C(=O)C[C@@H]1[C@@H]2CC[C@]2(C)C=CC[C@@H]12>C1CCOC1>C[C@@]12C=CC[C@H]1[C@@H]1CC(O)c3cc(O)ccc3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b8d6ef4ffcec455e83cfc0cf4e62d64c
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O>>C[C@@]12CCC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2
NN.[OH-].[K+].C[C@]12CC[C@@H]3C=4C=CC(=CC4CC=C3[C@@H]1CCC2=O)O.Cl>>C[C@@]12CCC[C@H]1C1=CCC=3C=C(C=CC3[C@H]1CC2)O
O=[C:3]1[C@:2]2([CH3:1])[C@@H:6]([CH2:5][CH2:4]1)[C:7]1=[CH:8][CH2:9][c:10]3[cH:11][c:12]([OH:13])[cH:14][cH:15][c:16]3[C@H:17]1[CH2:18][CH2:19]2>>[CH3:1][C@@:2]12[CH2:3][CH2:4][CH2:5][C@H:6]1[C:7]1=[CH:8][CH2:9][c:10]3[cH:11][c:12]([OH:13])[cH:14][cH:15][c:16]3[C@H:17]1[CH2:18][CH2:19]2
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O
C[C@@]12CCC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2
null
null
O.C(COCCO)O
Reduction
OtherReaction
11b0f05f13f348a1e22dfedd2b26d07f1878b2edd41602781ca10f6aa8c5cfef
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
C1=C2[C@H](CCC3CCC[C@@H]23)c2ccccc2C1
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4](-[C:5]=[C:6])-[C:7]-1(-[C;D1;H3:8])-[C:9]>>[C:9]-[C:7]1(-[C;D1;H3:8])-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4]-1-[C:5]=[C:6]
14
[{"value": 14.0, "product": "C[C@@]12CCC[C@H]1C1=CCC=3C=C(C=CC3[C@H]1CC2)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 13.9, "product": "C[C@@]12CCC[C@H]1C1=CCC=3C=C(C=CC3[C@H]1CC2)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of equilin (100.2 mg, 0.3733 mmol) in 2 mL of diethylene glycol were added hydrazine (59 μL, 1.9 mmol) and potassium hydroxide (0.04 g, 0.7 mmol). See FIG. 14. The mixture was stirred in an oil bath at 200°-214° C. for 2h, after which the cooled reaction was diluted with 10 mL of water, neutralized with...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
C1=C2[C@H](CC[C@@H]3CCC[C@@H]23)c2ccccc2C1
C1=C2[C@H](CC[C@H]3CCC[C@@H]23)c2ccccc2C1
C1=C2[C@H](CC[C@H]3CCC[C@@H]23)c2ccccc2C1
Other
O.C(COCCO)O
null
null
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O>O.C(COCCO)O>C[C@@]12CCC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-97916d286a614ca395578599dd7642c2
CC(=O)OC(C)=O.C[C@@]12C=CC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2>>CC(=O)Oc1ccc2c(c1)CC=C1[C@@H]2CC[C@]2(C)C=CC[C@@H]12
C[C@@]12C=CC[C@H]1C1=CCC=3C=C(C=CC3[C@H]1CC2)O.N1=CC=CC=C1.C(C)(=O)OC(C)=O>>C(C)(=O)OC1=CC=2CC=C3[C@@H]4CC=C[C@@]4(C)CC[C@@H]3C2C=C1
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[CH2:11][CH:12]=[C:13]1[C@@H:14]2[CH2:15][CH2:16][C@:17]2([CH3:18])[CH:19]=[CH:20][CH2:21][C@@H:22]12>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[CH2:11][CH:12]=[C:13]1[C@@H:14]2[CH2:15][CH2:16][C@:17]2([CH3:18])[CH:19]=[CH:2...
CC(=O)OC(C)=O.C[C@@]12C=CC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2
CC(=O)Oc1ccc2c(c1)CC=C1[C@@H]2CC[C@]2(C)C=CC[C@@H]12
null
null
C(C)(=O)OCC
Acylation
Acetic anhydride and alcohol to ester
55f321cc520ab80a97c517ea4db1ffe6ba0ea312e2db70f74b0966421bec0a44
96218bff9f96200922f4dff3481116557fe6986cba41ef7bff8cc8a0b43bd224
C1=CC2CC[C@H]3C(=CCc4ccccc43)[C@@H]2C1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
35.1
[{"value": 35.0, "product": "C(C)(=O)OC1=CC=2CC=C3[C@@H]4CC=C[C@@]4(C)CC[C@@H]3C2C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 35.1, "product": "C(C)(=O)OC1=CC=2CC=C3[C@@H]4CC=C[C@@]4(C)CC[C@@H]3C2C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of estra-1,3,5(10),7,16-pentaen-3-ol (5, 192.1 mg, 0.7612 mmol) in anh. pyridine (2.6 mL, 32 mmol) and acetic anhydride (0.36 mL, 3.8 mmol) was stirred 6 h, after which 30 mL, of ethyl acetate were added. The mixture was washed with three 10 mL portions of 1M hydrochloric acid+10 mL of saturated sodium bicar...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aromatic alcohol
Ester
null
null
C1=C[C@H]2CC[C@H]3C(=CCc4ccccc43)[C@@H]2C1
HO-
C(C)(=O)OCC
null
null
CC(=O)OC(C)=O.C[C@@]12C=CC[C@H]1C1=CCc3cc(O)ccc3[C@H]1CC2>C(C)(=O)OCC>CC(=O)Oc1ccc2c(c1)CC=C1[C@@H]2CC[C@]2(C)C=CC[C@@H]12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-468cb3245f1d495c916c0c2155cad422
CC(=O)OC(C)=O.C[C@@]12C=CC[C@H]1c1ccc3cc(O)ccc3c1CC2>>CC(=O)Oc1ccc2c3c(ccc2c1)[C@@H]1CC=C[C@@]1(C)CC3
C[C@@]12C=CC[C@H]1C=1C=CC=3C=C(C=CC3C1CC2)O.N1=CC=CC=C1.C(C)(=O)OC(C)=O>>C(C)(=O)OC1=CC=2C=CC=3[C@@H]4CC=C[C@@]4(C)CCC3C2C=C1
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][c:5]1[cH:6][cH:7][c:8]2[c:9]3[c:10]([cH:11][cH:12][c:13]2[cH:14]1)[C@@H:15]1[CH2:16][CH:17]=[CH:18][C@@:19]1([CH3:20])[CH2:21][CH2:22]3>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][cH:7][c:8]2[c:9]3[c:10]([cH:11][cH:12][c:13]2[cH:14]1)[C@@H:15]1[CH2:16][CH:17]=[CH:18][C@@:19]1([CH3:20])[CH2...
CC(=O)OC(C)=O.C[C@@]12C=CC[C@H]1c1ccc3cc(O)ccc3c1CC2
CC(=O)Oc1ccc2c3c(ccc2c1)[C@@H]1CC=C[C@@]1(C)CC3
null
null
C(C)(=O)OCC
Acylation
Acetic anhydride and alcohol to ester
55f321cc520ab80a97c517ea4db1ffe6ba0ea312e2db70f74b0966421bec0a44
96218bff9f96200922f4dff3481116557fe6986cba41ef7bff8cc8a0b43bd224
C1=CC2CCc3c(ccc4ccccc34)[C@@H]2C1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
A solution of estra-1,3,5(10),6,8,16-hexaen-3-ol Q8, 148.8 mg, 0.5944 mmol) in anh. pyridine (2.0 mL, 25 mmol) and acetic anhydride (0.28 mL, 3.0 mmol) was stirred 6 h, after which ethyl acetate (20 mL) was added. See FIG. 16. The mixture was washed with three 10 mL portions of 1N hydrochloric acid+10 mL of saturated s...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aromatic alcohol
Ester
null
null
C1=C[C@H]2CCc3c(ccc4ccccc34)[C@@H]2C1
HO-
C(C)(=O)OCC
null
null
CC(=O)OC(C)=O.C[C@@]12C=CC[C@H]1c1ccc3cc(O)ccc3c1CC2>C(C)(=O)OCC>CC(=O)Oc1ccc2c3c(ccc2c1)[C@@H]1CC=C[C@@]1(C)CC3
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f5acae62e6b3429fbdd22b19dd4f3794
C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O>>C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C
CC(C)([O-])C.[K+].C[C@]12CC[C@@H]3C=4C=CC(=CC4CC[C@H]3[C@@H]1CCC2=O)O>>C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC=3C=C(C=CC3[C@H]1CC2)O
O=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[cH:10][c:11]([OH:12])[cH:13][cH:14][c:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[cH:10][c:11]([OH:12])[cH:13][cH:14][c:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]
C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O
C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
CS(=O)C
Functional Group Interconversion
OtherReaction
2a089c86876da4b63340b50ce6162eb9d8dae1d5c1a6286dd27616876622d717
f395a9efbb80a99833acb686d4944d4880257993d074f4e04e21822999af09fe
C=C1CC[C@@H]2C1CC[C@@H]1c3ccccc3CC[C@H]12
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1(-[C;D1;H3:6])-[C:7]>>[C:7]-[C:5]1(-[C;D1;H3:6])-[C:4]-[C:3]-[C:2]-[C;H0;D3;+0:1]-1=[C;D1;H2:8]
76.3
[{"value": 76.0, "product": "C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC=3C=C(C=CC3[C@H]1CC2)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 76.3, "product": "C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC=3C=C(C=CC3[C@H]1CC2)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A suspension of methyltriphenylphosphonium bromide (100.03 g, 0.28001 mol) and potassium t-butoxide (31.42 g, 0.2800 mol) in anh. dimethylsulfoxide (DMSO, 320 mL) under argon was stirred in an oil bath (68°-81° C.) 1 h, after which estrone (15.14 g, 55.99 mmol) in anh. DMSO (320 mL) was added via syringe. See FIG. 17. ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Vinyl
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.CS(=O)C
null
1
C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CCC2=O>[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.CS(=O)C>C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d81d78f7d3a948e5a0a669fa1bb5c419
C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C.CC(=O)OC(C)=O>>C=C1CC[C@H]2[C@@H]3CCc4cc(OC(C)=O)ccc4[C@H]3CC[C@]12C
C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC=3C=C(C=CC3[C@H]1CC2)O.N1=CC=CC=C1.C(C)(=O)OC(C)=O>>C(C)(=O)OC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1)=C
[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[cH:10][c:11]([OH:12])[cH:16][cH:17][c:18]4[C@H:19]3[CH2:20][CH2:21][C@:22]12[CH3:23].CC(=O)O[C:13]([CH3:14])=[O:15]>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[cH:10][c:11]([O:12][C:13]([CH3:14])=[O:15])[cH:16][cH:17][c:18]4[C@H:19...
C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C.CC(=O)OC(C)=O
C=C1CC[C@H]2[C@@H]3CCc4cc(OC(C)=O)ccc4[C@H]3CC[C@]12C
null
null
C(C)(=O)OCC
Acylation
Acetic anhydride and alcohol to ester
55f321cc520ab80a97c517ea4db1ffe6ba0ea312e2db70f74b0966421bec0a44
96218bff9f96200922f4dff3481116557fe6986cba41ef7bff8cc8a0b43bd224
C=C1CC[C@@H]2C1CC[C@@H]1c3ccccc3CC[C@H]12
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
A solution of 17-methylenestra-1,3,5(10)-trien-3-ol (10, 5.84 g, 21.8 mmol) in anh. pyridine (32 mL, 0.40 mol) and acetic anhydride (9.7 mL, 0.10 mol) was stirred 24, after which ethyl acetate (250 mL) was added. See FIG. 17. The mixture was washed with three 100 mL portions of 1N hydrochloric acid+100 mL of saturated ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aromatic alcohol
Ester
null
null
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
HO-
C(C)(=O)OCC
null
null
C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C.CC(=O)OC(C)=O>C(C)(=O)OCC>C=C1CC[C@H]2[C@@H]3CCc4cc(OC(C)=O)ccc4[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fa3190d1b079451ab839b5c743c6536d
C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C.COS(=O)(=O)OC>>C=C1CC[C@H]2[C@@H]3CCc4cc(OC)ccc4[C@H]3CC[C@]12C
S(=O)(=O)(OC)OC.O.C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC=3C=C(C=CC3[C@H]1CC2)O.C([O-])([O-])=O.[K+].[K+].S(=O)(=O)(OC)OC>>COC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1)=C
[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[cH:10][c:11]([OH:12])[cH:14][cH:15][c:16]4[C@H:17]3[CH2:18][CH2:19][C@:20]12[CH3:21].COS(=O)(=O)O[CH3:13]>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[cH:10][c:11]([O:12][CH3:13])[cH:14][cH:15][c:16]4[C@H:17]3[CH2:18][CH2:19][C@:20]...
C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C.COS(=O)(=O)OC
C=C1CC[C@H]2[C@@H]3CCc4cc(OC)ccc4[C@H]3CC[C@]12C
null
null
C(C)O
Heteroatom Alkylation and Arylation
Methylation of OH with DMS
b8b041187bac58376aae824630608e7deb49a01db3d652291f8b379c10d4e434
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
C=C1CC[C@@H]2C1CC[C@@H]1c3ccccc3CC[C@H]12
C-O-S(=O)(=O)-O-[CH3;D1;+0:1].[OH;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]
69
[{"value": 69.0, "product": "COC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1)=C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 68.5, "product": "COC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1)=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirred suspension of 17-methylenestra-1,3,5(10)-trien-3-ol (5.37 g, 20.0 mmol) and potassium carbonate (50.82 g, 0.3678 mol) at reflux in 90% ethanol (500 mL) was added dimethyl sulfate (5.0 mL, 53 mmol). After 1/2 h reflux additional dimethyl sulfate (36 mL, 0.38 mol, in three 12 mL aliquots) was added over the ...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
HO-
C(C)O
null
null
C=C1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C.COS(=O)(=O)OC>C(C)O>C=C1CC[C@H]2[C@@H]3CCc4cc(OC)ccc4[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fb10217d359f48f58ad443914a1b25a3
C=C1CC[C@H]2[C@@H]3CCc4cc(OC)ccc4[C@H]3CC[C@]12C>>C=C1CC[C@H]2[C@@H]3CCC4=C(CC=C(OC)C4)[C@H]3CC[C@]12C
N.COC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1)=C.C(C)(C)(C)O.[Li]>>COC=1CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2CC1)=C
[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[c:10]([cH:11][cH:12][c:13]([O:14][CH3:15])[cH:16]4)[C@H:17]3[CH2:18][CH2:19][C@:20]12[CH3:21]>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][C:9]4=[C:10]([CH2:11][CH:12]=[C:13]([O:14][CH3:15])[CH2:16]4)[C@H:17]3[CH2:18][CH2:19][C@:20]12[CH3...
C=C1CC[C@H]2[C@@H]3CCc4cc(OC)ccc4[C@H]3CC[C@]12C
C=C1CC[C@H]2[C@@H]3CCC4=C(CC=C(OC)C4)[C@H]3CC[C@]12C
null
null
O.CO.C1CCOC1
Miscellaneous
OtherReaction
cd6b08444c76e87f4ece7264249dc37390bc498e903fcc9da807aa1c49e6b2c3
bced64702950df7cf56df22d8c2487b007734fece951727fd2c8a1c63fbcf6cc
C=C1CC[C@@H]2C1CC[C@@H]1C3=C(CC=CC3)CC[C@H]12
[C:1]-[C:2]1-[C:3]-[C:4]-[C:5]-[c;H0;D3;+0:6]2:[cH;D2;+0:7]:[c;H0;D3;+0:8](-[#8:9]-[C;D1;H3:10]):[cH;D2;+0:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13]:2-1>>[C:1]-[C:2]1-[C:3]-[C:4]-[C:5]-[C;H0;D3;+0:6]2=[C;H0;D3;+0:13]-1-[CH2;D2;+0:12]-[CH;D2;+0:11]=[C;H0;D3;+0:8](-[#8:9]-[C;D1;H3:10])-[CH2;D2;+0:7]-2
72
[{"value": 72.0, "product": "COC=1CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2CC1)=C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.6, "product": "COC=1CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2CC1)=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Approximately 70 mL of anh. ammonia was distilled through a KOH tower into a 250 mL flame-dried 3-neck flask fitted with an inlet adapter, magnetic stirring bar, dry ice/acetone condenser, and ground glass stopper. See FIG. 17. A solution of 17-methylenestra-1,3,5(10)-trien-3-yl methyl ether (14, 1.1297 g, 4.0001 mmol)...
10.6084/m9.figshare.5104873.v1
null
Ether
Ether
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
C1=CCC2=C(C1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
C1=CCC2=C(C1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
null
O.CO.C1CCOC1
null
8
C=C1CC[C@H]2[C@@H]3CCc4cc(OC)ccc4[C@H]3CC[C@]12C>O.CO.C1CCOC1>C=C1CC[C@H]2[C@@H]3CCC4=C(CC=C(OC)C4)[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fe253937794b47dba1a5c9239e4b8e93
C=C1CC[C@H]2[C@@H]3CCC4=C(CC=C(OC)C4)[C@H]3CC[C@]12C>>C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C
Cl.O.COC=1CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2CC1)=C.C([O-])(O)=O.[Na+]>>C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)=O
C[O:12][C:11]1=[CH:13][CH2:14][C:15]2=[C:9]([CH2:8][CH2:7][C@H:6]3[C@@H:5]4[CH2:4][CH2:3][C:2](=[CH2:1])[C@@:19]4([CH3:20])[CH2:18][CH2:17][C@@H:16]32)[CH2:10]1>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][C:9]4=[CH:10][C:11](=[O:12])[CH2:13][CH2:14][C@@H:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]
C=C1CC[C@H]2[C@@H]3CCC4=C(CC=C(OC)C4)[C@H]3CC[C@]12C
C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C
null
null
CC(=O)C.CO
Miscellaneous
OtherReaction
ea3d0afa2d1ffd7144e5caf5674fcf0682e454869e2a8d1788fe76c2c7afe20e
06ee4e636755478860a38bbf5b67d3037b3b941f1ee50aea08d8ea3a7f23e056
C=C1CC[C@@H]2C1CC[C@H]1[C@H]2CCC2=CC(=O)CC[C@@H]21
C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2]1=[CH;D2;+0:3]-[C:4]-[C;H0;D3;+0:5]2=[C;H0;D3;+0:6](-[C:7]-[C:8]-[C:9]-[C:10]-2-[C:11])-[CH2;D2;+0:12]-1>>[C:11]-[C:10]1-[C:9]-[C:8]-[C:7]-[C;H0;D3;+0:6]2=[CH;D2;+0:12]-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[CH2;D2;+0:3]-[C:4]-[C@H;D3;+0:5]-1-2
null
[]
null
null
1
HOUR
Con. hydrochloric acid (6.0 mL) and water (6.0 mL) were added to a solution of 17-methylenestra-2,5(10)-dien-3-yl methyl ether (15, 702.8 mg. 2.471 mmol) in methanol (6 mL) and acetone (20 mL). See Example 17. After stirring 1 h, sodium bicarbonate (7.50 g) was added cautiously. The mixture was concentrated under reduc...
10.6084/m9.figshare.5104873.v1
null
Ether
Ketone
C1=CCC2=C(C1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
Other
CC(=O)C.CO
null
1
C=C1CC[C@H]2[C@@H]3CCC4=C(CC=C(OC)C4)[C@H]3CC[C@]12C>CC(=O)C.CO>C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-95307c0c52d74de4a0f61e340d47b4aa
C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C>>C=C1CC[C@H]2[C@@H]3CCC4=C[C@@H](O)CC[C@@H]4[C@H]3CC[C@]12C
C(C)(C)(C)O[AlH-](OC(C)(C)C)OC(C)(C)C.[Li+].C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC3=CC(CC[C@@H]3[C@H]1CC2)=O.[O-]S(=O)(=O)[O-].[Na+].[Na+]>>C=C1[C@]2(C)[C@@H](CC1)[C@@H]1CCC3=C[C@H](CC[C@@H]3[C@H]1CC2)O
[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][C:9]4=[CH:10][C:11](=[O:12])[CH2:13][CH2:14][C@@H:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][C:9]4=[CH:10][C@@H:11]([OH:12])[CH2:13][CH2:14][C@@H:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]
C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C
C=C1CC[C@H]2[C@@H]3CCC4=C[C@@H](O)CC[C@@H]4[C@H]3CC[C@]12C
null
null
CCOCC
Reduction
Reduction of ketone to secondary alcohol
390b75d1195a100e50c97c7f859b524c3c3615b11c43a66f31167fa5991c4f1b
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C=C1CC[C@@H]2C1CC[C@H]1[C@H]2CCC2=CCCC[C@@H]21
[C:1]-[C:2]1=[C:3]-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[C:6]-[C:7]-[C:8]-1>>[C:1]-[C:2]1=[C:3]-[C@@H;D3;+0:4](-[OH;D1;+0:5])-[C:6]-[C:7]-[C:8]-1
null
[]
null
null
4
HOUR
Lithium tri-t-butoxyaluminohydride (766.6 mg, 3.015 mmol) was added to a solution of 17-methylenestr-4-en-3-one (16, 203.7 mg, 0.7533 mmol) in 10 mL of anh. ether and the reaction was stirred 4 h. See FIG. 18. Glauber's salt (3.80 g) was added and the suspension was stirred an additional 1/2 h. The mixture was filtered...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
C1=C2CC[C@H]3[C@@H]4CCC[C@H]4CC[C@@H]3[C@H]2CCC1
null
CCOCC
null
4
C=C1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@]12C>CCOCC>C=C1CC[C@H]2[C@@H]3CCC4=C[C@@H](O)CC[C@@H]4[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0e8369bf0a9a4d91adb66baad07b17e0
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O>>C=C1CC[C@H]2C3=CCc4cc(O)ccc4[C@H]3CC[C@]12C
CC(C)([O-])C.[K+].C[C@]12CC[C@@H]3C=4C=CC(=CC4CC=C3[C@@H]1CCC2=O)O>>C=C1[C@]2(C)[C@@H](CC1)C1=CCC=3C=C(C=CC3[C@H]1CC2)O
O=[C:2]1[CH2:3][CH2:4][C@H:5]2[C:6]3=[CH:7][CH2:8][c:9]4[cH:10][c:11]([OH:12])[cH:13][cH:14][c:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C:6]3=[CH:7][CH2:8][c:9]4[cH:10][c:11]([OH:12])[cH:13][cH:14][c:15]4[C@H:16]3[CH2:17][CH2:18][C@:19]12[CH3:20]
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O
C=C1CC[C@H]2C3=CCc4cc(O)ccc4[C@H]3CC[C@]12C
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
CS(=O)C
Functional Group Interconversion
OtherReaction
305fb2af506a862f4985a5f618ab133b7f9e59303be672ddaa067c5a17ed4016
f395a9efbb80a99833acb686d4944d4880257993d074f4e04e21822999af09fe
C=C1CC[C@H]2C3=CCc4ccccc4[C@H]3CCC12
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4](-[C:5]=[C:6])-[C:7]-1(-[C;D1;H3:8])-[C:9]>>[C:9]-[C:7]1(-[C;D1;H3:8])-[C:4](-[C:3]-[C:2]-[C;H0;D3;+0:1]-1=[C;D1;H2:10])-[C:5]=[C:6]
null
[]
null
null
1
HOUR
Methyltriphenylphosphonium bromide (1.9967 g, 5.5892 mmol) and potassium t-butoxide (627.2 mg, 5.589 mmol) suspended in 6.1 mL of anh. DMSO under argon were 1 h in an oil bath (71°-83° C., after which equilin (300.0 mg, 1.118 mmol) in 6.1 μL of anh. DMSO was added via syringe. See FIG. 18. After stirring a further 70 m...
10.6084/m9.figshare.5104873.v1
null
Ketone
Vinyl
C1=C2[C@H](CC[C@@H]3CCC[C@@H]23)c2ccccc2C1
C1=C2[C@H](CC[C@@H]3CCC[C@@H]23)c2ccccc2C1
C1=C2[C@H](CC[C@@H]3CCC[C@@H]23)c2ccccc2C1
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.CS(=O)C
null
1
C[C@]12CC[C@H]3C(=CCc4cc(O)ccc43)[C@@H]1CCC2=O>[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.CS(=O)C>C=C1CC[C@H]2C3=CCc4cc(O)ccc4[C@H]3CC[C@]12C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2e0ece114db9467e960ec8e99788788f
C=CCBr.C=Cc1ccc(OC(C)=O)cc1>>C=CCOc1ccc(C=C)cc1
C(C)(=O)OC1=CC=C(C=C)C=C1.C(C=C)Br>>C(C=C)OC1=CC=C(C=C)C=C1
Br[CH2:3][CH:2]=[CH2:1].CC(=O)[O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[CH2:10])[cH:11][cH:12]1>>[CH2:1]=[CH:2][CH2:3][O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[CH2:10])[cH:11][cH:12]1
C=CCBr.C=Cc1ccc(OC(C)=O)cc1
C=CCOc1ccc(C=C)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
627a64bd2b77f284ffc6fe82ac9807d934aaaf644e904d52b272599944577038
cdd4d9002f407af0bc850abdcb3e8813f27873457591f92bc1a76b4ee9a3be0c
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].C-C(=O)-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H2:3]=[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
82
[{"value": 82.0, "product": "C(C=C)OC1=CC=C(C=C)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The reaction described in Example 1 was repeated on the same scale but with the reaction temperature maintained in the range of 4°-6° C., rather than 10° C., during the addition of 4-acetoxystyrene and allyl bromide. In this case, 4-allyloxystyrene was obtained in 82% yield following vacuum distillation. Residual conce...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ether
null
null
c1ccccc1
HBr
null
null
null
C=CCBr.C=Cc1ccc(OC(C)=O)cc1>>C=CCOc1ccc(C=C)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e7db0fa7d4e34c8d9ea16de03925fd0f
C=CCBr.C=Cc1ccc(OC(C)=O)cc1>>C=CCOc1ccc(C=C)cc1
C(C)(=O)OC1=CC=C(C=C)C=C1.C(C=C)Br>>C(C=C)OC1=CC=C(C=C)C=C1
Br[CH2:3][CH:2]=[CH2:1].CC(=O)[O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[CH2:10])[cH:11][cH:12]1>>[CH2:1]=[CH:2][CH2:3][O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[CH2:10])[cH:11][cH:12]1
C=CCBr.C=Cc1ccc(OC(C)=O)cc1
C=CCOc1ccc(C=C)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
627a64bd2b77f284ffc6fe82ac9807d934aaaf644e904d52b272599944577038
cdd4d9002f407af0bc850abdcb3e8813f27873457591f92bc1a76b4ee9a3be0c
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].C-C(=O)-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H2:3]=[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
66
[{"value": 66.0, "product": "C(C=C)OC1=CC=C(C=C)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The reaction described in Example 1 was repeated on the same scale but with the reaction temperature maintained at ambient (23° C.), rather than 10° C., during the addition of 4-acetoxystyrene and allyl bromide. In this case, 4-allyloxystyrene was obtained in 66 % yield following vacuum distillation. Conditions: See re...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ether
null
null
c1ccccc1
HBr
null
null
null
C=CCBr.C=Cc1ccc(OC(C)=O)cc1>>C=CCOc1ccc(C=C)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-63cf88ed289a47f680735419176263a5
C=CCBr.C=Cc1ccc(OC(C)=O)cc1>>C=CCOc1ccc(C=C)cc1
C(C)(=O)OC1=CC=C(C=C)C=C1.[OH-].[K+].O.C(C=C)Br>>C(C=C)OC1=CC=C(C=C)C=C1
Br[CH2:3][CH:2]=[CH2:1].CC(=O)[O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[CH2:10])[cH:11][cH:12]1>>[CH2:1]=[CH:2][CH2:3][O:4][c:5]1[cH:6][cH:7][c:8]([CH:9]=[CH2:10])[cH:11][cH:12]1
C=CCBr.C=Cc1ccc(OC(C)=O)cc1
C=CCOc1ccc(C=C)cc1
null
null
O1CCOCC1.C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
627a64bd2b77f284ffc6fe82ac9807d934aaaf644e904d52b272599944577038
cdd4d9002f407af0bc850abdcb3e8813f27873457591f92bc1a76b4ee9a3be0c
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].C-C(=O)-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H2:3]=[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
5
CELSIUS
2.5
HOUR
To a 4-necked, nitrogen swept, 2 liter glass reaction vessel equipped with a mechanical stirrer, double-walled condenser, thermocouple and pressure compensating addition funnel is added 1,4-dioxane (600 mls), potassium hydroxide (112.0 g, 2.00 moles) and water (39 g). The mixture is stirred and cooled to 10° C. at whic...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ether
null
null
c1ccccc1
HBr
O1CCOCC1.C1(=CC=CC=C1)C
5
2.5
C=CCBr.C=Cc1ccc(OC(C)=O)cc1>O1CCOCC1.C1(=CC=CC=C1)C>C=CCOc1ccc(C=C)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f24cc0230cab430e999525bce7ab4a89
c1ccc(N=Nc2ccccc2)cc1>>c1ccc(N=Nc2ccc(Nc3ccccc3)cc2)cc1
N(=NC1=CC=CC=C1)C1=CC=CC=C1>>C1=CC=C(C=C1)NC2=CC=C(C=C2)N=NC3=CC=CC=C3
[cH:1]1[cH:3][c:4]([N:5]=[N:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:20][cH:21][cH:7]1>>[cH:1]1[cH:2][cH:3][c:4]([N:5]=[N:6][c:7]2[cH:8][cH:9][c:10]([NH:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)[cH:18][cH:19]2)[cH:20][cH:21]1
c1ccc(N=Nc2ccccc2)cc1
c1ccc(N=Nc2ccc(Nc3ccccc3)cc2)cc1
null
null
NC1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
64b7165b3362727a5e4a6fea8f01ad1f3bfa61b4d1e9957fe4d0366099fdd975
f133b56cb7805e90c3a5a052e39a2b7100d8327860d3b4578b7c2e2fce369e36
c1ccc(N=Nc2ccc(Nc3ccccc3)cc2)cc1
[c:1]:[c:2](-[N;H0;D2;+0:3]=[N;H0;D2;+0:4]-[c:5]1:[c:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:[cH;D2;+0:9]:[cH;D2;+0:10]:1):[c:11]>>[c:1]:[c:2](-[NH;D2;+0:3]-[c:12]1:[c:13]:[c:14]:[c;H0;D3;+0:8](-[#7:15]=[N;H0;D2;+0:4]-[c:5]2:[c:6]:[cH;D2;+0:7]:[cH;D2;+0:9]:[c:16]:[cH;D2;+0:10]:2):[c:17]:[c:18]:1):[c:11]
90
[{"value": 90.0, "product": "C1=CC=C(C=C1)NC2=CC=C(C=C2)N=NC3=CC=CC=C3", "details": "PERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A solution of 25% aqueous tetramethylammonium hydroxide (8 mL) was concentrated under vacuum at 75° C. until solid material formed. Azobenzene (1.8 g) and aniline (10 mL) were added and the solution was stirred under the same conditions for 4 hours and then in the presence of air for 12 hours. Analysis of the reaction ...
10.6084/m9.figshare.5104873.v1
null
Diazene
Diazene.Secondary amine
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
Other
NC1=CC=CC=C1
null
4
c1ccc(N=Nc2ccccc2)cc1>NC1=CC=CC=C1>c1ccc(N=Nc2ccc(Nc3ccccc3)cc2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-44988dfca7bd41258d4d28be93b8e091
C=CC(=C)C>>C=CC(=C)C
C=CC=C.C(C)(=O)O.C(CCC)[Li].C(CCC)[Li].C=CC(C)=C.C=CC(C)=C.C=CC=C.O1CCCC1.C=CC(C)=C>>C=CC(C)=C.C=CC=C.C=CC(C)=C
[CH2:6]=[CH:7][C:8](=[CH2:9])[CH3:10]>>[CH2:6]=[CH:7][C:8](=[CH2:9])[CH3:10]
C=CC(=C)C
C=CC(=C)C
null
null
C1CCCCC1
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
50
CELSIUS
1
HOUR
Three hundred milliliters (mL) of purified, dried cyclohexane was introduced into a six-hundred milliliter stirred glass reactor. Air was removed from the reactor under vacuum and replaced by dry nitrogen. The reactor was equipped with an air driven stirrer, a pressure gauge, thermocouple, top face inlet valve, dip tub...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C1CCCCC1
50
1
C=CC(=C)C>C1CCCCC1>C=CC(=C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0c25e0f6a1bf4fe58b27283b9cf351bd
C=CC=C.C[CH2][Al]([CH2]C)[CH2]C>>C=CC(=C)C.C=CC=C
[H][H].[H][H].[OH-].[NH4+].N.C=CC=C.C=CC(C)=C.[H][H].C(C)[Al](CC)CC.[H][H].[H][H]>>C=CC(C)=C.C=CC=C.C=CC(C)=C
[CH2:11]=[CH:12][CH:13]=[CH2:14].[CH2]([Al]([CH2:2][CH3:1])[CH2:3][CH3:5])[CH3:4]>>[CH2:1]=[CH:2][C:3](=[CH2:4])[CH3:5].[CH2:11]=[CH:12][CH:13]=[CH2:14]
C=CC=C.C[CH2][Al]([CH2]C)[CH2]C
C=CC(=C)C.C=CC=C
null
CCCCCCCC(=O)[O-].CCCCCCCC(=O)[O-].[Ni+2].[Ni]
C1CCCCC1.CO
C-C Coupling
C-methylation
19f47f0a1c39d163ea22e2abf31005b56a6bc0ddcea0a4676c93bcfa8578de99
9295f74b88ae60b5ebc8d79e405026bba0c3f5a8811447b0a4357dab1e3ec179
null
[C;D1;H3:1]-[CH2;D2;+0:2]-[Al](-[CH2;D2;+0:3]-[CH3;D1;+0:4])-[CH2]-[CH3;D1;+0:5]>>[C;D1;H3:1]-[C;H0;D3;+0:2](=[CH2;D1;+0:5])-[CH;D2;+0:3]=[CH2;D1;+0:4]
null
[]
50
CELSIUS
30
MINUTE
A solution of 250 mL of cyclohexane and 23 g of a triblock polymer prepared in a manner similar to that described in Example I was purged of air by evacuation followed by introduction of dry nitrogen. This amount of polymer contained 0.403 moles of polybutadiene unsaturation. To the polymer solution was added 25 mL of ...
10.6084/m9.figshare.5104873.v1
null
null
Vinyl.Vinyl
null
null
null
Other
CCCCCCCC(=O)[O-].CCCCCCCC(=O)[O-].[Ni+2].[Ni].C1CCCCC1.CO
50
0.5
C=CC=C.C[CH2][Al]([CH2]C)[CH2]C>CCCCCCCC(=O)[O-].CCCCCCCC(=O)[O-].[Ni+2].[Ni].C1CCCCC1.CO>C=CC(=C)C.C=CC=C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-595f7592228d409abede8d544a1ed793
C[CH2][Al]([CH2]C)[CH2]C>>C=CC(=C)C
C(C)[Al](CC)CC.[H][H].[H][H].C=CC=C>>C=CC(C)=C.C=CC=C
C[CH2:4][Al]([CH2:1][CH3:2])[CH2:3][CH3:5]>>[CH2:1]=[CH:2][C:3](=[CH2:4])[CH3:5]
C[CH2][Al]([CH2]C)[CH2]C
C=CC(=C)C
null
[Co].[Al].CCCCC(CC)C(=O)[O-].CCCCC(CC)C(=O)[O-].[Co+2]
C1CCCCC1.[Co]
Miscellaneous
OtherReaction
b4e0efc9cc290a9b30be44680637729e6703a0d33ce2c0e94e1cf7262d59b37b
8088804b2f510891cc563e9f665e95c30529f26dee02f10a944fab24cca5ce0b
null
C-[CH2;D2;+0:1]-[Al](-[CH2;D2;+0:2]-[CH3;D1;+0:3])-[CH2;D2;+0:4]-[C;D1;H3:5]>>[C;D1;H3:5]-[C;H0;D3;+0:4](=[CH2;D1;+0:1])-[CH;D2;+0:3]=[CH2;D1;+0:2]
null
[]
null
null
null
null
Part of the polymeric solution (195 g) described in Example V was introduced into a 0.5 L Fischer-Porter reactor. The total amount of polymer added to the reactor was 31.4 g which represents 0.540 moles of butadiene unsaturation. The hydrogenation catalyst was prepared by adding 35.1 mL of a 1.7M triethylaluminum solut...
10.6084/m9.figshare.5104873.v1
null
null
Vinyl.Vinyl
null
null
null
Other
[Co].[Al].CCCCC(CC)C(=O)[O-].CCCCC(CC)C(=O)[O-].[Co+2].C1CCCCC1.[Co]
null
null
C[CH2][Al]([CH2]C)[CH2]C>[Co].[Al].CCCCC(CC)C(=O)[O-].CCCCC(CC)C(=O)[O-].[Co+2].C1CCCCC1.[Co]>C=CC(=C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a3eda3d721a549a6bcd88ad5e8f9a4a3
C=CC=C>>C=CC=C
C(CCC)[Li].C(CCC)[Li].C=CC=C.C=CC(C)=C.[Na]>>C=CC(C)=C.C=CC=C
[CH2:6]=[CH:7][CH:8]=[CH2:9]>>[CH2:6]=[CH:7][CH:8]=[CH2:9]
C=CC=C
C=CC=C
null
null
O1CCCC1.C1CCCCC1.CCCCC
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
4
HOUR
Eleven hundred milliliters of purified pentane was introduced under a nitrogen atmosphere into a two quart glass-bowled pressure reactor. The reactor was equipped with an air driven stirrer, a pressure gauge, a thermometer well, a heat exchange coil, a top surface inlet valve, a dip tube feeder with a valve, a syringe ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
O1CCCC1.C1CCCCC1.CCCCC
null
4
C=CC=C>O1CCCC1.C1CCCCC1.CCCCC>C=CC=C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-25ff45b66b4f4d2196e608014e91c72c
C=Cc1ccc(C)cc1>>C=Cc1ccc(C)cc1
C(CCC)[Li].CC1=CC=C(C=C)C=C1.C=CC=C.C=CC=C.CC1=CC=C(C=C)C=C1.C(CCC)[Li]>>CC1=CC=C(C=C)C=C1.C=CC=C
[CH2:5]=[CH:6][c:7]1[cH:8][cH:9][c:10]([CH3:11])[cH:12][cH:13]1>>[CH2:5]=[CH:6][c:7]1[cH:8][cH:9][c:10]([CH3:11])[cH:12][cH:13]1
C=Cc1ccc(C)cc1
C=Cc1ccc(C)cc1
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccccc1
null
null
[]
35
CELSIUS
3.6
HOUR
One thousand milliliters of purified pentane and 100 mL of tetrahydrofuran distilled over benzophenone ketyl were introduced under a nitrogen atmosphere into a two quart glass bowled stirred pressure reactor. The reactor was equipped with an air driven stirrer, a pressure gauge, a thermometer well, a heat exchange coil...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
null
35
3.6
C=Cc1ccc(C)cc1>>C=Cc1ccc(C)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3592964bb411464a9d252afbb2f06a56
CC(C)(C)OC(=O)N[C@H](CO)C(c1ccccc1)c1ccccc1.FC(F)(F)c1cc(CBr)cc(C(F)(F)F)c1>>CC(C)(C)OC(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1
C(C)(C)(C)OC(=O)N[C@H](CO)C(C1=CC=CC=C1)C1=CC=CC=C1.[H-].[Na+].FC(C=1C=C(CBr)C=C(C1)C(F)(F)F)(F)F>>C(C)(C)(C)OC(=O)N[C@H](COCC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C(C1=CC=CC=C1)C1=CC=CC=C1
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C@H:9]([CH2:10][OH:11])[CH:27]([c:28]1[cH:29][cH:30][cH:31][cH:32][cH:33]1)[c:34]1[cH:35][cH:36][cH:37][cH:38][cH:39]1.Br[CH2:12][c:13]1[cH:14][c:15]([C:16]([F:17])([F:18])[F:19])[cH:20][c:21]([C:22]([F:23])([F:24])[F:25])[cH:26]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:...
CC(C)(C)OC(=O)N[C@H](CO)C(c1ccccc1)c1ccccc1.FC(F)(F)c1cc(CBr)cc(C(F)(F)F)c1
CC(C)(C)OC(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1
null
null
O1CCCC1.CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccc(COCCC(c2ccccc2)c2ccccc2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
16
HOUR
To a cooled solution (0° C.) of (S)-2-t-butoxycarbonylamino-3,3-diphenylpropan-1-ol (2.04 g, 6.2 mmol, Example 1 g) in tetrahydrofuran (50 ml) and dimethylformamide (10 ml) was added sodium hydride (0.187 g, 80% suspension in oil) over 15 minutes. After an additional 10 minutes 3,5-bis(trifluoromethyl)benzyl bromide (1...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HBr
O1CCCC1.CN(C=O)C
null
16
CC(C)(C)OC(=O)N[C@H](CO)C(c1ccccc1)c1ccccc1.FC(F)(F)c1cc(CBr)cc(C(F)(F)F)c1>O1CCCC1.CN(C=O)C>CC(C)(C)OC(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2f9111900eb248048af418ff562d0e49
COC(=O)CBr.N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1>>COC(=O)CN[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1
N[C@H](COCC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C(C1=CC=CC=C1)C1=CC=CC=C1.C(=O)([O-])[O-].[K+].[K+].BrCC(=O)OC>>COC(CN[C@H](COCC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C(C1=CC=CC=C1)C1=CC=CC=C1)=O
Br[CH2:5][C:3]([O:2][CH3:1])=[O:4].[NH2:6][C@H:7]([CH2:8][O:9][CH2:10][c:11]1[cH:12][c:13]([C:14]([F:15])([F:16])[F:17])[cH:18][c:19]([C:20]([F:21])([F:22])[F:23])[cH:24]1)[CH:25]([c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1)[c:32]1[cH:33][cH:34][cH:35][cH:36][cH:37]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][NH:6][C@H:7]([CH2:...
COC(=O)CBr.N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1
COC(=O)CN[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1
null
null
CN(C=O)C.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
308780347cfd56717124ea78bf2bc5de380db774d7ce948246e279dfd7d8998b
d2327a8d30a39f085182e5e2f77f5b022ac99c077866b86103acfec639a8f73d
c1ccc(COCCC(c2ccccc2)c2ccccc2)cc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].[C:6]-[C:7](-[C:8])-[NH2;D1;+0:9]>>[C:6]-[C:7](-[C:8])-[NH;D2;+0:9]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5]
null
[]
null
null
0.75
HOUR
To a solution of (S)-2-amino-1-((3,5-bis(trifluoromethyl) phenyl)methyloxy)-3,3-diphenylpropane (8.6 g, Example 1i) and anhydrous K2CO3 (13.0 g)in dimethylformamide (50 ml) was added methyl bromoacetate (4.5 ml). The reaction was stirred at room temperature for 0.75 h then diluted with ethyl acetate (200 ml) and washed...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Primary amine
Ester.Secondary amine
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HBr
CN(C=O)C.C(C)(=O)OCC
null
0.75
COC(=O)CBr.N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1>CN(C=O)C.C(C)(=O)OCC>COC(=O)CN[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(c1ccccc1)c1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2dbe524b12974d9382613c2ccfb3e4d0
CSCc1cc(C(C)(C)C)cc(Cl)c1N>>Cc1cc(C(C)(C)C)cc(Cl)c1N
C(C)(C)(C)C1=CC(=C(N)C(=C1)CSC)Cl>>C(C)(C)(C)C1=CC(=C(N)C(=C1)C)Cl
CS[CH2:1][c:2]1[cH:3][c:4]([C:5]([CH3:6])([CH3:7])[CH3:8])[cH:9][c:10]([Cl:11])[c:12]1[NH2:13]>>[CH3:1][c:2]1[cH:3][c:4]([C:5]([CH3:6])([CH3:7])[CH3:8])[cH:9][c:10]([Cl:11])[c:12]1[NH2:13]
CSCc1cc(C(C)(C)C)cc(Cl)c1N
Cc1cc(C(C)(C)C)cc(Cl)c1N
null
[Ni]
CO
Reduction
OtherReaction
4b57e24218e2409c207dcfe624aba83448b3ad4b3549d9bc7855651565b7e76d
32a5269109432865a866e9a2b5da238f4471b13dee7daf193dc4e8c41b091706
c1ccccc1
C-S-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[CH3;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
4-t-Butyl-2-chloro-6-(methylthiomethyl)aniline (1.3 g) was dissolved in methanol (50 ml) and Raney-nickel (prewashed to pH 7) was added portionwise until t.l.c. indicated all starting material had reacted (ether-hexane, 1:10). The Raney-nickel was removed by filtration through Celite and the filtrate was evaporated. Th...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
null
null
null
c1ccccc1
Other
[Ni].CO
null
null
CSCc1cc(C(C)(C)C)cc(Cl)c1N>[Ni].CO>Cc1cc(C(C)(C)C)cc(Cl)c1N
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4135a6eeef0c445ba7a7b80232208f57
Cc1cc(C(C)(C)C)cc(Cl)c1N>>Cc1cc(Cl)cc(C(C)(C)C)c1
C(C)(C)(C)C1=CC(=C(N)C(=C1)C)Cl.S(O)(O)(=O)=O.N(=O)[O-].[Na+]>>C(C)(C)(C)C=1C=C(C=C(C1)Cl)C
N[c:3]1[c:2]([CH3:1])[cH:12][c:7]([C:8]([CH3:9])([CH3:10])[CH3:11])[cH:6][c:4]1[Cl:5]>>[CH3:1][c:2]1[cH:3][c:4]([Cl:5])[cH:6][c:7]([C:8]([CH3:9])([CH3:10])[CH3:11])[cH:12]1
Cc1cc(C(C)(C)C)cc(Cl)c1N
Cc1cc(Cl)cc(C(C)(C)C)c1
null
null
C(C)O
Reduction
OtherReaction
a069304de6b46c6d557b2e80c544464adc3bb98001f26c098e87c25f29d552f9
a4f16f822d2806606c05d0c4baa1761ad37a11006840dde863a01a253bdff5dd
c1ccccc1
N-[c;H0;D3;+0:1](:[c:2](-[C;D1;H3:3]):[c:4]):[c:5](-[Cl;D1;H0:6]):[c:7]>>[C;D1;H3:3]-[c:2](:[c:4]):[cH;D2;+0:1]:[c:5](-[Cl;D1;H0:6]):[c:7]
null
[]
null
null
null
null
4-t-Butyl-2-chloro-6-methylaniline (1.97 g) was dissolved in ethanol (50 ml), sulphuric acid (1.88 ml, conc.) was added dropwise and the resulting blue solution was heated at reflux. Sodium nitrite (1.72 g) was added portionwise over 30 min. The resulting mixture was heated at reflux for a further 30 rain, then cooled ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccccc1
c1ccccc1
c1ccccc1
Other
C(C)O
null
null
Cc1cc(C(C)(C)C)cc(Cl)c1N>C(C)O>Cc1cc(Cl)cc(C(C)(C)C)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-dac80fb0f36f4b17b2c012191b64c977
Cc1cc(Cl)cc(C(C)(C)C)c1.O=C1CCC(=O)N1Br>>CC(C)(C)c1cc(Cl)cc(CBr)c1
C(C)(C)(C)C=1C=C(C=C(C1)Cl)C.BrN1C(CCC1=O)=O.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O>>C(C)(C)(C)C=1C=C(CBr)C=C(C1)Cl
[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([Cl:8])[cH:9][c:10]([CH3:11])[cH:13]1.O=C1CCC(=O)N1[Br:12]>>[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([Cl:8])[cH:9][c:10]([CH2:11][Br:12])[cH:13]1
Cc1cc(Cl)cc(C(C)(C)C)c1.O=C1CCC(=O)N1Br
CC(C)(C)c1cc(Cl)cc(CBr)c1
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
3-t-Butyl-5-chlorotoluene (5.7 g) was dissolved in carbon tetrachloride (80 ml) and N-bromosuccinimide (5.56 g) was added followed by benzoyl peroxide (750 mg). This mixture was heated at reflux for 6 h. The mixture was cooled, filtered through Celite and the filtrate was concentrated in vacuo. The residue was purified...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
C(Cl)(Cl)(Cl)Cl
null
null
Cc1cc(Cl)cc(C(C)(C)C)c1.O=C1CCC(=O)N1Br>C(Cl)(Cl)(Cl)Cl>CC(C)(C)c1cc(Cl)cc(CBr)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-202a9bbb4dca40d0b986898be9ca314e
COc1cc(C)cc(C)c1.O=C1CCC(=O)N1Br>>COc1cc(C)cc(CBr)c1
CC=1C=C(C=C(C1)C)OC.BrN1C(CCC1=O)=O>>BrCC=1C=C(C=C(C1)C)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([CH3:6])[cH:7][c:8]([CH3:9])[cH:11]1.O=C1CCC(=O)N1[Br:10]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH3:6])[cH:7][c:8]([CH2:9][Br:10])[cH:11]1
COc1cc(C)cc(C)c1.O=C1CCC(=O)N1Br
COc1cc(C)cc(CBr)c1
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A refluxing solution of 3,5-dimethylanisole (13 g), azoisobutyronitrile (1.6 g) and N-bromosuccinimide (17 g) in carbon tetrachloride (100 ml) was irradiated with light for 6 h. The solution was filtered and the solvent removed in vacuo. The residue was purified by chromatography on silica gel (eluting with 0-5% ethyl ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
C(Cl)(Cl)(Cl)Cl
null
null
COc1cc(C)cc(C)c1.O=C1CCC(=O)N1Br>C(Cl)(Cl)(Cl)Cl>COc1cc(C)cc(CBr)c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d84299200b2b4f29be7d2236be2306f3
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21>>O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
C12C(C3C1C(=O)OC3=O)C(=O)OC2=O.C1=CC(=CC(=C1)N)C(=O)N>>C12C(C3C1C(=O)OC3=O)C(=O)OC2=O.C1=CC(=CC(=C1)N)C(=O)N
[O:11]=[C:12]1[O:13][C:14](=[O:15])[CH:16]2[CH:17]1[CH:18]1[C:19](=[O:20])[O:21][C:22](=[O:23])[CH:24]21>>[O:11]=[C:12]1[O:13][C:14](=[O:15])[CH:16]2[CH:17]1[CH:18]1[C:19](=[O:20])[O:21][C:22](=[O:23])[CH:24]21
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
null
null
CN1CCCC1=O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
null
null
[]
null
null
null
null
19.22 g (0.098 mol) of CBDA and 12.22 g (0.1 mol) of 3-ABA were reacted in 283 g of NMP at room temperature for 5 hours to prepare a polyamic acid solution. The polymerization reaction proceeded easily and uniformly, and the molecular weights were measured in the same manner as in Preparation Example 1 and as a result,...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
C1OCC2C1C1COCC21
null
CN1CCCC1=O
null
null
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21>CN1CCCC1=O>O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d185d75b7569442fb2f6092f3d83f5ac
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21>>O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
C12C(C3C1C(=O)OC3=O)C(=O)OC2=O.C1=CC=C2C=C3C=C(C=CC3=CC2=C1)CCCC(=O)O>>C12C(C3C1C(=O)OC3=O)C(=O)OC2=O.C1=CC=C2C=C3C=C(C=CC3=CC2=C1)CCCC(=O)O
[O:21]=[C:22]1[O:23][C:24](=[O:25])[CH:26]2[CH:27]1[CH:28]1[C:29](=[O:30])[O:31][C:32](=[O:33])[CH:34]21>>[O:21]=[C:22]1[O:23][C:24](=[O:25])[CH:26]2[CH:27]1[CH:28]1[C:29](=[O:30])[O:31][C:32](=[O:33])[CH:34]21
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
null
null
CN1CCCC1=O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
null
null
[]
null
null
null
null
19.22 g (0.098 mol) of CBDA, 9.77 g (0.08 mol) of 4-ABA and 5.85 g (0.02 mol) of DADOB were reacted in 197 g of NMP at room temperature for 5 hours to prepare a polyamic acid solution. The polymerization reaction proceeded easily and uniformly, and the molecular weights were measured in the same manner as in Preparatio...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
C1OCC2C1C1COCC21
null
CN1CCCC1=O
null
null
O=C1OC(=O)C2C1C1C(=O)OC(=O)C21>CN1CCCC1=O>O=C1OC(=O)C2C1C1C(=O)OC(=O)C21
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-00c4384d6b5048e79b0f47e3215b50a5
O=c1oc(=O)c2cc3c(=O)oc(=O)c3cc12>>O=c1oc(=O)c2cc3c(=O)oc(=O)c3cc12
C1=C2C(=CC3=C1C(=O)OC3=O)C(=O)OC2=O.C1=CC=C2C=C3C=C(C=CC3=CC2=C1)CCCC(=O)O>>C1=C2C(=CC3=C1C(=O)OC3=O)C(=O)OC2=O.C1=CC=C2C=C3C=C(C=CC3=CC2=C1)CCCC(=O)O
[O:21]=[c:22]1[o:23][c:24](=[O:25])[c:26]2[cH:27][c:28]3[c:29](=[O:30])[o:31][c:32](=[O:33])[c:34]3[cH:35][c:36]12>>[O:21]=[c:22]1[o:23][c:24](=[O:25])[c:26]2[cH:27][c:28]3[c:29](=[O:30])[o:31][c:32](=[O:33])[c:34]3[cH:35][c:36]12
O=c1oc(=O)c2cc3c(=O)oc(=O)c3cc12
O=c1oc(=O)c2cc3c(=O)oc(=O)c3cc12
null
null
CN1CCCC1=O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=c1oc(=O)c2cc3c(=O)oc(=O)c3cc12
null
null
[]
null
null
null
null
20.94 g (0.096 mol) of PMDA, 11.00 g (0.09 mol) of 4-ABA and 3.49 g (0.01 mol) of DAHOB were reacted in 201 g of NMP at room temperature for 5 hours to prepare a polyamic acid solution. The polymerization reaction proceeded easily and uniformly, and the molecular weights were measured in the same manner as in Preparati...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1occ2cc3cocc3cc12
null
CN1CCCC1=O
null
null
O=c1oc(=O)c2cc3c(=O)oc(=O)c3cc12>CN1CCCC1=O>O=c1oc(=O)c2cc3c(=O)oc(=O)c3cc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-817cd11527084050ab0e75f85e5e8e0a
CCCS(=O)(=O)Cl.Cc1ccccc1C(C#N)=C1SC=CC1=NO>>CCCS(=O)(=O)ON=C1C=CSC1=C(C#N)c1ccccc1C
ON=C1C(SC=C1)=C(C#N)C1=C(C=CC=C1)C.C(CC)S(=O)(=O)Cl.O.C(C)N(CC)CC>>C(CC)S(=O)(=O)ON=C1C(SC=C1)=C(C#N)C1=C(C=CC=C1)C
Cl[S:4]([CH2:3][CH2:2][CH3:1])(=[O:5])=[O:6].[OH:7][N:8]=[C:9]1[CH:10]=[CH:11][S:12][C:13]1=[C:14]([C:15]#[N:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[CH3:23]>>[CH3:1][CH2:2][CH2:3][S:4](=[O:5])(=[O:6])[O:7][N:8]=[C:9]1[CH:10]=[CH:11][S:12][C:13]1=[C:14]([C:15]#[N:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[CH3...
CCCS(=O)(=O)Cl.Cc1ccccc1C(C#N)=C1SC=CC1=NO
CCCS(=O)(=O)ON=C1C=CSC1=C(C#N)c1ccccc1C
null
null
O1CCCC1.ClCCl
Acylation
OtherReaction
50146a9530af828763c7589f586cdd6b32faf532de89bafbd92bbb2e801c1a6a
f6092cbe9db0fc6e43032da5237b29b2d78e210f79dcfa1490f3f662cbf1cda2
N=C1C=CSC1=Cc1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[C:4]-[C:5].[C:6]=[C:7]1-[#16:8]-[C:9]=[C:10]-[C:11]-1=[#7:12]-[OH;D1;+0:13]>>[C:6]=[C:7]1-[#16:8]-[C:9]=[C:10]-[C:11]-1=[#7:12]-[O;H0;D2;+0:13]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[C:4]-[C:5]
70
[{"value": 70.0, "product": "C(CC)S(=O)(=O)ON=C1C(SC=C1)=C(C#N)C1=C(C=CC=C1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
In 490 g of tetrahydrofuran were dissolved 45 g (0.19 mol) of (3-(hydroxy)imino-3H-thiophen-2-ylidene)-(2-methylphenyl)-acetonitrile in Synthesis Example 1 and 27.0 g (0.19 mol) of commercially available propanesulfonyl chloride. To the solution cooled, 20.6 g (0.20 mol) of triethylamine was added dropwise such that th...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide.Oxime
Sulfonate
null
null
C1=CSCC1.c1ccccc1
HCl
O1CCCC1.ClCCl
null
1
CCCS(=O)(=O)Cl.Cc1ccccc1C(C#N)=C1SC=CC1=NO>O1CCCC1.ClCCl>CCCS(=O)(=O)ON=C1C=CSC1=C(C#N)c1ccccc1C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-eea2c1ce513848f792f52b7e8a031284
Nc1ccccc1N.O=C(O)C(F)(F)C(F)(F)C(=O)O>>FC(F)(c1nc2ccccc2[nH]1)C(F)(F)c1nc2ccccc2[nH]1
C1(=C(C=CC=C1)N)N.FC(C(C(=O)O)(F)F)(C(=O)O)F>>N1=C(NC2=C1C=CC=C2)C(C(F)(F)C=2NC1=C(N2)C=CC=C1)(F)F
[NH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[NH2:12].O=[C:16](O)[C:2]([F:1])([F:3])[C:18]([F:14])([F:15])[C:23](=O)O>>[F:1][C:2]([F:3])([c:4]1[n:5][c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[nH:12]1)[C:13]([F:14])([F:15])[c:16]1[n:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[nH:24]1
Nc1ccccc1N.O=C(O)C(F)(F)C(F)(F)C(=O)O
FC(F)(c1nc2ccccc2[nH]1)C(F)(F)c1nc2ccccc2[nH]1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
d8bb4423619e5b6e1a1183ec72b61c8c6bd81d8c419173f3499a36a0ba67607d
6affff663b9fd2961056497c561c38101c041d6e07e5e9d7618df47ef448e4e4
c1ccc2[nH]c(CCc3nc4ccccc4[nH]3)nc2c1
O-[C;H0;D3;+0:1](=O)-[C;H0;D4;+0:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C;H0;D4;+0:5](-[F;H0;D1;+0:6])(-[F;H0;D1;+0:7])-[C;H0;D3;+0:8](-O)=O.[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12](-[NH2;D1;+0:13]):[c:14]>>[F;D1;H0:3]-[C;H0;D4;+0:2](-[F;D1;H0:4])(-[c:15]1:[n;H0;D2;+0:13]:[c:12](:[c:14]):[c:10](:[c:11]):[nH;D2;+0:9]:1)-[C:16](-[F...
null
[]
160
CELSIUS
7
HOUR
In a 250 mL 35/25 ball joint flask, 1,2-phenylenediamine (5.92 g, 54.7 mmol) was combined with tetrafluorosuccinic acid (5.2 g, 27.36 mmol). Polyphosphoric acid (83 g) was added directly to the solid mixture. The flask was fitted with an air-driven mechanical stirring shaft and heated to 160° C. under a nitrogen purge ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide.Carboxylic acid.Carboxylic acid.Primary amine.Primary amine
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide
c1ccccc1
c1ccc2[nH]cnc2c1.c1ccc2[nH]cnc2c1
c1ccc2[nH]cnc2c1.c1ccc2[nH]cnc2c1
null
null
160
7
Nc1ccccc1N.O=C(O)C(F)(F)C(F)(F)C(=O)O>>FC(F)(c1nc2ccccc2[nH]1)C(F)(F)c1nc2ccccc2[nH]1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-f4736c1983ad4437920881e9356b17a0
C=CCCCCCCCCC(=O)O.O=C(Cl)C(=O)Cl>>C=CCCCCCCCCC(=O)Cl
C(CCCCCCCCC=C)(=O)O.C(=O)(C(=O)Cl)Cl>>C(CCCCCCCCC=C)(=O)Cl
O[C:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH:2]=[CH2:1])=[O:12].O=C(Cl)C(=O)[Cl:13]>>[CH2:1]=[CH:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][C:11](=[O:12])[Cl:13]
C=CCCCCCCCCC(=O)O.O=C(Cl)C(=O)Cl
C=CCCCCCCCCC(=O)Cl
null
null
C(Cl)Cl
Functional Group Interconversion
Alcohol to chloride_Other
013cec2edeb273a7a148f349d36a52d99ff4e7bcf8eed78085df830088e387ac
aedb1f68dc5b7eb0583043e1125b741382b17974140a2f46554f0110e2ddc884
null
Cl-C(=O)-C(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
100
[{"value": 100.0, "product": "C(CCCCCCCCC=C)(=O)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a stirred solution of 10-undecenoic acid (5.055 mL, 25 mmol) in CH2Cl2 (50 mL) was slowly added (COCl)2 (4.364 mL, 50 mmol). The mixture was stirred at room temperature overnight. The solvent was removed under reduced pressure to give 10-undecenoyl chloride (25 mmol). The product was used for the next reaction witho...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Carboxylic acid
Acyl halide
null
null
null
HCl
C(Cl)Cl
null
8
C=CCCCCCCCCC(=O)O.O=C(Cl)C(=O)Cl>C(Cl)Cl>C=CCCCCCCCCC(=O)Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-9ba0da86e63347cf8a214eba91698af6
C=CCCCCCCCCC(=O)Cl.CCOC(=O)CC(=O)[O-]>>C=CCCCCCCCCC(=O)CC(=O)OCC
C(CC(=O)[O-])(=O)OCC.[Li]CCCC.C(CCCCCCCCC=C)(=O)Cl>>O=C(CC(=O)OCC)CCCCCCCCC=C
Cl[C:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH:2]=[CH2:1])=[O:12].O=C([O-])[CH2:13][C:14](=[O:15])[O:16][CH2:17][CH3:18]>>[CH2:1]=[CH:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][C:11](=[O:12])[CH2:13][C:14](=[O:15])[O:16][CH2:17][CH3:18]
C=CCCCCCCCCC(=O)Cl.CCOC(=O)CC(=O)[O-]
C=CCCCCCCCCC(=O)CC(=O)OCC
null
null
C1CCOC1
C-C Coupling
OtherReaction
9c255438d8e6adeba9ee52582b8e97af5f85bef382cd416953270ac55bd10486
4c7bc8856483317e0c04a17d8cd6aba13cdf5ed9f64b61fe01f230a819039f82
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].O=C(-[O-])-[CH2;D2;+0:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:5]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
98.6
[{"value": 98.6, "product": "O=C(CC(=O)OCC)CCCCCCCCC=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
1
HOUR
A stirred solution of monoethyl malonate (5.3 g, 40 mmol) in anhydrous THF (150 mL) was cooled to −78° C. under an argon atmosphere, and n-BuLi (2.5 M, 32 mL, 80 mmol) was added drop-wise via an air-tight syringe. After the addition, the temperature was raised to 0° C., and the stirring was continued for 1 hour. The re...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ester
Ketone
null
null
null
Other
C1CCOC1
0
1
C=CCCCCCCCCC(=O)Cl.CCOC(=O)CC(=O)[O-]>C1CCOC1>C=CCCCCCCCCC(=O)CC(=O)OCC
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-aee179ab58eb4efda743c97ebbe68cb4
CCCCCCCCCC(=O)Cl.CCOC(=O)CC(=O)[O-]>>CCCCCCCCCC(=O)CC(=O)OCC
C(CC(=O)[O-])(=O)OCC.[Li]CCCC.C(CCCCCCCCC)(=O)Cl>>O=C(CC(=O)OCC)CCCCCCCCC
O=C(Cl)[CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[O-][C:10](=[O:11])[CH2:12][C:13](=[O:14])[O:15][CH2:16][CH3:17]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C:10](=[O:11])[CH2:12][C:13](=[O:14])[O:15][CH2:16][CH3:17]
CCCCCCCCCC(=O)Cl.CCOC(=O)CC(=O)[O-]
CCCCCCCCCC(=O)CC(=O)OCC
null
null
C1CCOC1
C-C Coupling
OtherReaction
e0a45010daec094b0d5e8e4fbe0fbbb99cf9610754539ead723b25846a3ea8fc
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
null
Cl-C(=O)-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]-[C;H0;D3;+0:9](-[O-])=[O;D1;H0:10]>>[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]-[C;H0;D3;+0:9](=[O;D1;H0:10])-[CH2;D2;+0:1]-[C:2]-[C:3]
120.2
[{"value": 120.2, "product": "O=C(CC(=O)OCC)CCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
1
HOUR
A stirred solution of monoethyl malonate (1.26 g, 9.6 mmol) in 25 mL anhydrous THF was cooled to −78° C. under an argon atmosphere, and n-BuLi (2.5 M, 8 mL, 20 mmol) was added drop-wise via an air-tight syringe. After the addition, the temperature was raised to 0° C., and the stirring was continued for 1 hour. The mixt...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
null
null
null
Other
C1CCOC1
0
1
CCCCCCCCCC(=O)Cl.CCOC(=O)CC(=O)[O-]>C1CCOC1>CCCCCCCCCC(=O)CC(=O)OCC
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-bccd1606f68f46538243c62ad1d15035
CCCCCCCCCC(=O)CC(=O)OCC.OCCO>>CCCCCCCCCC1(CC(=O)OCC)OCCO1
O=C(CC(=O)OCC)CCCCCCCCC.C(CO)O.CC=1C=CC(=CC1)S(=O)(=O)O>>C1OC(CC(=O)OCC)(CCCCCCCCC)OC1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C:10]([CH2:11][C:12](=[O:13])[O:14][CH2:15][CH3:16])=[O:17].O[CH2:18][CH2:19][OH:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C:10]1([CH2:11][C:12](=[O:13])[O:14][CH2:15][CH3:16])[O:17][CH2:18][CH2:19][O:20]1
CCCCCCCCCC(=O)CC(=O)OCC.OCCO
CCCCCCCCCC1(CC(=O)OCC)OCCO1
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
2baa95c632045e217509d8ec12cda8674252268fe3f8cb44eb2e5ebe0f27c30f
f8121a7732f8ef583111433d2b2d82886bf3a134c51dc6363d813c8cbf4e36f5
C1COCO1
O-[CH2;D2;+0:1]-[C:2]-[OH;D1;+0:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]-[C;H0;D3;+0:9](=[O;H0;D1;+0:10])-[C:11]-[C:12]>>[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]-[C;H0;D4;+0:9]1(-[C:11]-[C:12])-[O;H0;D2;+0:10]-[CH2;D2;+0:1]-[C:2]-[O;H0;D2;+0:3]-1
79
[{"value": 79.0, "product": "C1OC(CC(=O)OCC)(CCCCCCCCC)OC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The mixture of ethyl 3-oxododecanoate (1.456 g, ca. 5 mmol), ethylene glycol (2.78 mL, 50 mmol) and a catalytic amount of p-TsOH (95 mg, 0.5 mmol) in benzene (50 mL) was heated to 110° C. under an argon atmosphere overnight. The solvent was removed, and the residue was diluted with 50 mL ethyl acetate. The solution was...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary alcohol.Primary alcohol
Ether.Ether
null
C1COCO1
C1COCO1
HO-
C1=CC=CC=C1
null
null
CCCCCCCCCC(=O)CC(=O)OCC.OCCO>C1=CC=CC=C1>CCCCCCCCCC1(CC(=O)OCC)OCCO1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-082ac3331501484a9c124c4ecaa3c4fc
CCCCCCCCCC1(CC(=O)OCC)OCCO1>>CCCCCCCCCC1(CC(=O)O)OCCO1
Cl.C1OC(CC(=O)OCC)(CCCCCCCCC)OC1.O[Li].O.C1CCOC1>>C1OC(CC(=O)O)(CCCCCCCCC)OC1
CC[O:14][C:12]([CH2:11][C:10]1([CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[O:15][CH2:16][CH2:17][O:18]1)=[O:13]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C:10]1([CH2:11][C:12](=[O:13])[OH:14])[O:15][CH2:16][CH2:17][O:18]1
CCCCCCCCCC1(CC(=O)OCC)OCCO1
CCCCCCCCCC1(CC(=O)O)OCCO1
null
null
O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
C1COCO1
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
81
[{"value": 81.0, "product": "C1OC(CC(=O)O)(CCCCCCCCC)OC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.8, "product": "C1OC(CC(=O)O)(CCCCCCCCC)OC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a 25 mL flask were added ethyl 3,3-ethylenedioxydodecanoate (1.131 g, 3.95 mmol), LiOH.H2O (840 mg, 20 mmol), THF (5 mL), and water (5 mL). The mixture was stirred at room temperature overnight. The solution was acidified by the addition of 1 M HCl (50 mL), and extracted with ethyl acetate (3×50 mL). The organic lay...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1COCO1
Other
O
null
8
CCCCCCCCCC1(CC(=O)OCC)OCCO1>O>CCCCCCCCCC1(CC(=O)O)OCCO1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-2a6750458ed94fe5aaffc536dc12f1f2
CCCCCCCCCC1(CC(=O)O)OCCO1.N[C@@H]1CCC[C@H]1O>>CCCCCCCCCC(=O)CC(=O)N[C@@H]1CCC[C@H]1O
C(CCl)Cl.CCN(C(C)C)C(C)C.C1OC(CC(=O)O)(CCCCCCCCC)OC1.Cl.N[C@H]1[C@@H](CCC1)O>>O[C@H]1[C@@H](CCC1)NC(CC(CCCCCCCCC)=O)=O
O[C:13]([CH2:12][C:10]1([CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])OCC[O:11]1)=[O:14].[NH2:15][C@@H:16]1[CH2:17][CH2:18][CH2:19][C@H:20]1[OH:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C:10](=[O:11])[CH2:12][C:13](=[O:14])[NH:15][C@@H:16]1[CH2:17][CH2:18][CH2:19][C@H:20]1[O...
CCCCCCCCCC1(CC(=O)O)OCCO1.N[C@@H]1CCC[C@H]1O
CCCCCCCCCC(=O)CC(=O)N[C@@H]1CCC[C@H]1O
null
CN(C)C=1C=CN=CC1
CN(C)C=O.C(=O)(C(F)(F)F)O
Acylation
OtherReaction
d0c6aecfd4ea74a053ef63024963609c51e883e82bba95129bbece5aa4e2b368
e776385d4a3d7d421c579bc9c2d56b9a8877fa86a206c7577e42d62c95dc339e
C1CCCC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C;H0;D4;+0:4]1(-[C:5]-[C:6])-O-C-C-[O;H0;D2;+0:7]-1.[C:8]-[C:9](-[NH2;D1;+0:10])-[C:11]>>[C:8]-[C:9](-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C;H0;D3;+0:4](=[O;H0;D1;+0:7])-[C:5]-[C:6])-[C:11]
54
[{"value": 54.0, "product": "O[C@H]1[C@@H](CCC1)NC(CC(CCCCCCCCC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a solution of 3,3-ethylenedioxydodecanoic acid (55 mg, 0.213 mmol) (Pearson et al., Proc. Natl Acad. Sci. USA 91:197-201 (1994); Bu et al., Synthetic agonists of a Pseudomonas aeruginosa quorum sensing molecule, submitted for publication, which are hereby incorporated by reference in their entirety) and trans-2-amin...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether.Ether.Primary amine
Ketone.Secondary amide
C1COCO1
null
C1CCCC1
HO-
CN(C)C=1C=CN=CC1.CN(C)C=O.C(=O)(C(F)(F)F)O
null
18
CCCCCCCCCC1(CC(=O)O)OCCO1.N[C@@H]1CCC[C@H]1O>CN(C)C=1C=CN=CC1.CN(C)C=O.C(=O)(C(F)(F)F)O>CCCCCCCCCC(=O)CC(=O)N[C@@H]1CCC[C@H]1O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-04d741497f364ad9b516fc50990e2c22
CCCC(=O)N[C@H]1CCOC1=O>>CCCC(=O)O.N[C@@H]1CCCC[C@H]1O.N[C@@H]1CCC[C@H]1O
C(CCl)Cl.CCCC(=O)N[C@H]1CCOC1=O>>C(CCC)(=O)O.N[C@H]1[C@@H](CCC1)O.N[C@H]1[C@@H](CCCC1)O
[CH3:1][CH2:2][CH2:3][C:4](=[O:5])[NH:7][C@H:8]1[CH2:9][CH2:10][O:6][C:13]1=[O:14]>>[CH3:1][CH2:2][CH2:3][C:4](=[O:5])[OH:6].[NH2:7][C@@H:8]1[CH2:9][CH2:10][CH2:11][CH2:12][C@H:13]1[OH:14].[NH2:15][C@@H:16]1[CH2:17][CH2:18][CH2:19][C@H:20]1[OH:21]
CCCC(=O)N[C@H]1CCOC1=O
CCCC(=O)O.N[C@@H]1CCCC[C@H]1O.N[C@@H]1CCC[C@H]1O
null
null
null
Functional Group Addition
Oxidation of amide to carboxylic acid
542012aeaa708674d041630f8b9df1bea6718662aacc80b9ee6b28e816479fa9
5e2ad6f68252a0c4cc0e9b52bcfe117d063b6982056e6c894db512d3b9f8d6f9
C1CCCC1.C1CCCCC1
[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:5]-[C:6]1-[C:7]-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:10]-1=[O;H0;D1;+0:11]>>[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[OH;D1;+0:9].[NH2;D1;+0:5]-[C:6]1-[C:7]-[CH2;D2;+0:8]-[C:12]-[C:13]-[C@H;D3;+0:10]-1-[OH;D1;+0:11]
null
[]
null
null
null
null
The procedure for the preparation of C4-HSL was used for this series of molecules. The EDC-mediated coupling of butyric acid and trans-2- amino-cyclopentanol or trans-2-amino-cyclohexanol afforded 6 in 66% yield or 8 in 82% yield. 6: IR (KBr) 3284, 2960, 1643, 1567, 1058 cm−1; 1H NMR (500 MHz, CDCl3) δ 0.952 (t, J=7.5 ...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amide
Carboxylic acid.Secondary alcohol.Secondary alcohol.Primary amine.Primary amine
C1CCOC1
C1CCCCC1.C1CCCC1
C1CCCCC1.C1CCCC1
Other
null
null
null
CCCC(=O)N[C@H]1CCOC1=O>>CCCC(=O)O.N[C@@H]1CCCC[C@H]1O.N[C@@H]1CCC[C@H]1O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ca9f5351d49a4a978457ad82bd1fbd60
CCCC[C@@H](NC(=O)[C@H](N)CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)NCC(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O.O=C(O)C(F)(F)F>>CC(C)(C)OC(=O)NCC(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O
C(=O)(C(F)(F)F)O.N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)NCC(=O)N[C@H](CC1=CC=C(C=C1)O)C(=O)N.C1(=CC=CC=C1)O.C1(=CC=CC=C1)C.C(=O)(C(F)(F)F)O>>N(CC(=O)N[C@H](CC1=CC=C(C=C1)O)C(=O)N)C(=O)OC(C)(C)C
CCCC[C@@H](NC(=O)[C@H](N)CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@@H](C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)[C:6](=[O:7])[NH:8][CH2:9][C:10](=[O:11])[NH:12][C@H:13]([CH2:14][c:15]1[cH:16][cH:17][c:18]([OH:19])[cH:20][cH:21]1)[C:22]([NH2:23])=[O:24])[CH2:3]CC[CH3:4].O=[C:2]([C:1](F)(F)F)[...
CCCC[C@@H](NC(=O)[C@H](N)CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)NCC(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O.O=C(O)C(F)(F)F
CC(C)(C)OC(=O)NCC(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O
null
null
C1CCOC1
C-C Coupling
OtherReaction
dd722390e0f931a1e91da0a580dd86bb43d4e6a09fcff7959cb32fed079f3dbf
d5fdf5772f396142214745bda546e0d1591f84ba68c45fef9f87b717d7d7541a
c1ccccc1
C-C-C-C-[C@@H](-N-C(=O)-[C@H](-N)-C-C-C-N-C(-N)=N)-C(=O)-N-[C@H](-C-C-C-C)-C(=O)-N-[C@@H](-[CH2;D2;+0:1]-C-C-[CH3;D1;+0:2])-C(=O)-N-[C@H](-C-C-C-N-C(-N)=N)-C(=O)-N-[C@H](-C-C-C-C)-C(=O)-N-[C@H](-C-C-C-C)-C(=O)-N-[C@H](-C-C-C-C)-[C;H0;D3;+0:3](=[O;D1;H0:4])-[#7:5]-[C:6]-[C:7](-[#7:8])=[O;D1;H0:9].F-[C;H0;D4;+0:10](-F)(-...
null
[]
null
null
null
null
The deprotected peptide SF1257-13 (TFA-(D)Arg-(D)Nle-(D)Nle-(D)Nle-(D)Arg-(D)Nle-(D)Nle-(D)Nle-Gly-(D)Tyr-NH2 (SEQ ID NO:1) is made by slowly adding TFA (A×3 l) to a mixture of SF1257-12 (A kg) and phenol (A×0.1 kg) in toluene and THF while maintaining the temperature at ≦18° C. The reaction mixture is allowed to warm ...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Carboxylic acid.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Secondary amide.Primary amine.Primary amine.Primary amine.Secondary amine.Secondary amine
Carbamic ester.Ether.Boc
null
null
c1ccccc1
HF
C1CCOC1
null
null
CCCC[C@@H](NC(=O)[C@H](N)CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)N[C@H](CCCC)C(=O)NCC(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O.O=C(O)C(F)(F)F>C1CCOC1>CC(C)(C)OC(=O)NCC(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-89f48428d4e84988964422372e55b7e2
CCCC[C@H](O)[C@@H](CC1CC1)C(=O)NC1N=C(c2ccccn2)c2ccccc2N(C)C1=O>>CCCCC[C@@H](CC1CC1)C(=O)NC1N=C(c2ccccn2)c2ccccc2N(C)C1=O
C1(CC1)C[C@@H](C(=O)NC1C(N(C2=C(C(=N1)C1=NC=CC=C1)C=CC=C2)C)=O)[C@H](CCCC)O.NC1C(N(C2=C(C(=N1)C1=NC=CC=C1)C=CC=C2)C)=O>>O=C([C@@H](CCCCC)CC1CC1)NC1C(N(C2=C(C(=N1)C1=NC=CC=C1)C=CC=C2)C)=O
O[C@@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[C@@H:6]([CH2:7][CH:8]1[CH2:9][CH2:10]1)[C:11](=[O:12])[NH:13][CH:14]1[N:15]=[C:16]([c:17]2[cH:18][cH:19][cH:20][cH:21][n:22]2)[c:23]2[cH:24][cH:25][cH:26][cH:27][c:28]2[N:29]([CH3:30])[C:31]1=[O:32]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C@@H:6]([CH2:7][CH:8]1[CH2:9][CH2:10]1)[C:11...
CCCC[C@H](O)[C@@H](CC1CC1)C(=O)NC1N=C(c2ccccn2)c2ccccc2N(C)C1=O
CCCCC[C@@H](CC1CC1)C(=O)NC1N=C(c2ccccn2)c2ccccc2N(C)C1=O
null
null
null
Reduction
OtherReaction
3c5af32aa639db2ebe4d9851942e9468e1838e06ae5b2c1669bca1d5e0922c33
46f8a11b80b06e754a5a34198d843342612a5e7ede950bda52ce3a500cedba0b
O=C(CCC1CC1)NC1N=C(c2ccccn2)c2ccccc2NC1=O
O-[C@@H;D3;+0:1](-[C:2]-[C:3])-[C:4](-[C:5])-[C:6](=[O;D1;H0:7])-[#7:8]-[C:9](-[#7:10])-[C:11](=[O;D1;H0:12])-[#7:13]>>[#7:10]-[C:9](-[#7:8]-[C:6](=[O;D1;H0:7])-[C:4](-[C:5])-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:11](=[O;D1;H0:12])-[#7:13]
null
[]
null
null
null
null
(±)-3-(2-(R)-Cyclopropylmethyl-3-(S)-hydroxyl-1-oxoheptyl)amino-1-methyl-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one was made from 1 and 3-amino-1-methyl-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepine-2-one (G. Semple et al Synth. Commun. 1996, 26, 721) according to step 1 in Example 1. MS (ESI): 449 (M...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
null
null
C1CC1.c1ccncc1.C1=NCC[NH]c2ccccc21
Other
null
null
null
CCCC[C@H](O)[C@@H](CC1CC1)C(=O)NC1N=C(c2ccccn2)c2ccccc2N(C)C1=O>>CCCCC[C@@H](CC1CC1)C(=O)NC1N=C(c2ccccn2)c2ccccc2N(C)C1=O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-65c80db4378345879329b129a789998c
CN(C)CCc1c[nH]c2ccc(N)cc12.Cc1c(S(=O)(=O)Cl)sc2ccc(Cl)cc12>>Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN(C)C)c3c2)sc2ccc(Cl)cc12
NC=1C=C2C(=CNC2=CC1)CCN(C)C.ClC1=CC2=C(SC(=C2C)S(=O)(=O)Cl)C=C1>>CN(CCC1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=C(C2=C(S1)C=CC(=C2)Cl)C)C
[NH2:7][c:8]1[cH:9][cH:10][c:11]2[nH:12][cH:13][c:14]([CH2:15][CH2:16][N:17]([CH3:18])[CH3:19])[c:20]2[cH:21]1.Cl[S:4]([c:3]1[c:2]([CH3:1])[c:29]2[c:23]([s:22]1)[cH:24][cH:25][c:26]([Cl:27])[cH:28]2)(=[O:5])=[O:6]>>[CH3:1][c:2]1[c:3]([S:4](=[O:5])(=[O:6])[NH:7][c:8]2[cH:9][cH:10][c:11]3[nH:12][cH:13][c:14]([CH2:15][CH2...
CN(C)CCc1c[nH]c2ccc(N)cc12.Cc1c(S(=O)(=O)Cl)sc2ccc(Cl)cc12
Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN(C)C)c3c2)sc2ccc(Cl)cc12
null
null
N1=CC=CC=C1
Miscellaneous
Sulfonamide synthesis (Schotten-Baumann) primary amine
a86b0632821e188c0a5dc5a5a2aac298ab3eccaee8a52ba46078c3d5975a290d
50f8fbf3d327483c3eeff8f6cbd4065e4c7600bb501fbe08958a5c79a0926428
O=S(=O)(Nc1ccc2[nH]ccc2c1)c1cc2ccccc2s1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[#16;a:6]:[c:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[O;D1;H0:2]=[S;H0;D4;+0:1](=[O;D1;H0:3])(-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11])-[c:4](:[c:5]):[#16;a:6]:[c:7]
82
[{"value": 82.0, "product": "CN(CCC1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=C(C2=C(S1)C=CC(=C2)Cl)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.8, "product": "CN(CCC1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=C(C2=C(S1)C=CC(=C2)Cl)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
To a solution of 3.05 g (15 mMol) of 5-amino-3-(2-dimethylaminoethyl)-1H-indol in 100 ml of pyridine is added dropwise at ambient temperature a solution of 4.21 g (15 mMol) of 5-chloro-3-methyl-benzo[b]thiophene-2-sulphonyl chloride in 20 ml of pyridine. The reaction mixture is stirred at ambient temperature for 20 hou...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Sulfonyl halide
Sulfonamide
null
null
c1ccc2[nH]ccc2c1.c1ccc2sccc2c1
HCl
N1=CC=CC=C1
null
20
CN(C)CCc1c[nH]c2ccc(N)cc12.Cc1c(S(=O)(=O)Cl)sc2ccc(Cl)cc12>N1=CC=CC=C1>Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN(C)C)c3c2)sc2ccc(Cl)cc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-da28e3f72905445186f85e1905136ebe
CCI.CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12>>CCN(CC)CCc1c[nH]c2ccc(N(CC)S(=O)(=O)c3ccc4ccccc4c3)cc12
O.C(C)N(CCC1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC2=CC=CC=C2C=C1)CC.CC(C)([O-])C.[K+].C(C)I>>C(C)N(CCC1=CNC2=CC=C(C=C12)N(S(=O)(=O)C1=CC2=CC=CC=C2C=C1)CC)CC
I[CH2:16][CH3:17].[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][c:8]1[cH:9][nH:10][c:11]2[cH:12][cH:13][c:14]([NH:15][S:18](=[O:19])(=[O:20])[c:21]3[cH:22][cH:23][c:24]4[cH:25][cH:26][cH:27][cH:28][c:29]4[cH:30]3)[cH:31][c:32]12>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[CH2:6][CH2:7][c:8]1[cH:9][nH:10][c:11]2[cH:12][cH:...
CCI.CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12
CCN(CC)CCc1c[nH]c2ccc(N(CC)S(=O)(=O)c3ccc4ccccc4c3)cc12
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0fe6648877a29ae177a907a0d252f35d8beab440bf428116c5424a67bc0e72cd
0b054affe7e4bb904ceae512aabc19d89c93551cb46dfbc6f220fc85e5eeff75
O=S(=O)(Nc1ccc2[nH]ccc2c1)c1ccc2ccccc2c1
I-[CH2;D2;+0:1]-[C;D1;H3:2].[O;D1;H0:3]=[#16:4](=[O;D1;H0:5])(-[c:6])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H3:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7](-[c:8](:[c:9]):[c:10])-[#16:4](=[O;D1;H0:3])(=[O;D1;H0:5])-[c:6]
null
[]
null
null
30
MINUTE
To a mixture of 285 mg (0.7 mMol) of N-[3-(2-diethylaminoethyl)-1H-indol-5-yl]naphthalene-2-sulphonamide (example 17) and 80 mg (0.7 mMol) of potassium t-butoxide in 3 ml of DMSO are stirred for 30 minutes at ambient temperature. Then are added 105 mg (0.7 mMol) of ethyl iodide and left with stirring for 3 hours. Water...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Primary halide
Tertiary amine
null
null
c1ccc2[nH]ccc2c1.c1ccc2ccccc2c1
HI
CS(=O)C
null
0.5
CCI.CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12>CS(=O)C>CCN(CC)CCc1c[nH]c2ccc(N(CC)S(=O)(=O)c3ccc4ccccc4c3)cc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e2ceadb7003543839098c55a9adcf662
CN1CCC(=O)CC1.O=S(=O)(Nc1ccc2[nH]ccc2c1)c1cccc2ccccc12>>CN1CC=C(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1
CN1CCC(CC1)=O.C[O-].[Na+].N1C=CC2=CC(=CC=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12>>CN1CCC(=CC1)C1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12
O=[C:5]1[CH2:4][CH2:3][N:2]([CH3:1])[CH2:30][CH2:29]1.[cH:6]1[cH:7][nH:8][c:9]2[cH:10][cH:11][c:12]([NH:13][S:14](=[O:15])(=[O:16])[c:17]3[cH:18][cH:19][cH:20][c:21]4[cH:22][cH:23][cH:24][cH:25][c:26]34)[cH:27][c:28]12>>[CH3:1][N:2]1[CH2:3][CH:4]=[C:5]([c:6]2[cH:7][nH:8][c:9]3[cH:10][cH:11][c:12]([NH:13][S:14](=[O:15])...
CN1CCC(=O)CC1.O=S(=O)(Nc1ccc2[nH]ccc2c1)c1cccc2ccccc12
CN1CC=C(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1
null
null
CO
C-C Coupling
piperidine_indole
2c09067bd257df167078887e4090fe0d7bc8a234e11e68ee424f29322f615f2e
06a42e352cf517302d592bf38a2fd11b220014e39071074dc7becb6ee0bee4b2
O=S(=O)(Nc1ccc2[nH]cc(C3=CCNCC3)c2c1)c1cccc2ccccc12
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4](-[C;D1;H3:5])-[C:6]-[CH2;D2;+0:7]-1.[c:8]:[c:9]1:[#7;a:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1:[c:14]>>[C;D1;H3:5]-[#7:4]1-[C:3]-[C:2]-[C;H0;D3;+0:1](-[c;H0;D3;+0:12]2:[c:11]:[#7;a:10]:[c:9](:[c:8]):[c:13]:2:[c:14])=[CH;D2;+0:7]-[C:6]-1
52
[{"value": 52.0, "product": "CN1CCC(=CC1)C1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.0, "product": "CN1CCC(=CC1)C1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 712 mg (13.2 mMol) of sodium methoxide in 100 ml of methanol are added 850 mg (2.64 mMol) of N-[1H-indol-5-yl]naphthalene-1-sulphonamide followed by 596 mg (5.28 mMol) of 1-methyl-4-piperidone and the resulting solution is heated to reflux for 48 hours. The reaction mixture is concentrated at reduced p...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
C1CC[NH]CC1.c1ccc2[nH]ccc2c1
C1=CC[NH]CC1.c1ccc2[nH]ccc2c1
C1=CC[NH]CC1.c1ccc2[nH]ccc2c1.c1ccc2ccccc2c1
HO-
CO
null
null
CN1CCC(=O)CC1.O=S(=O)(Nc1ccc2[nH]ccc2c1)c1cccc2ccccc12>CO>CN1CC=C(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-89760789d5364662a7531ad6c3dacc80
CN1CC=C(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1>>CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1
CN1CCC(=CC1)C1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12.[H][H]>>CN1CCC(CC1)C1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12
[CH3:1][N:2]1[CH2:3][CH:4]=[C:5]([c:6]2[cH:7][nH:8][c:9]3[cH:10][cH:11][c:12]([NH:13][S:14](=[O:15])(=[O:16])[c:17]4[cH:18][cH:19][cH:20][c:21]5[cH:22][cH:23][cH:24][cH:25][c:26]45)[cH:27][c:28]23)[CH2:29][CH2:30]1>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([c:6]2[cH:7][nH:8][c:9]3[cH:10][cH:11][c:12]([NH:13][S:14](=[O:15])(=[...
CN1CC=C(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1
CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1
null
[Pd]
CO.C(C)OCC
Reduction
Hydrogenation (double to single)
641ee5df237f030873b7ef4c8f313c4da4e38b634b6176a5872cc6f99e79a814
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
O=S(=O)(Nc1ccc2[nH]cc(C3CCNCC3)c2c1)c1cccc2ccccc12
[C;D1;H3:1]-[#7:2]1-[C:3]-[C:4]-[C;H0;D3;+0:5](-[c:6]2:[c:7]:[c:8]:[#7;a:9]:[c:10]:2)=[CH;D2;+0:11]-[C:12]-1>>[C;D1;H3:1]-[#7:2]1-[C:3]-[C:4]-[CH;D3;+0:5](-[c:6]2:[c:7]:[c:8]:[#7;a:9]:[c:10]:2)-[CH2;D2;+0:11]-[C:12]-1
65
[{"value": 65.0, "product": "CN1CCC(CC1)C1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.8, "product": "CN1CCC(CC1)C1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 417 mg (1 mMol) of N-[3-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-5-yl]naphthalene-1-sulphonamide in 50 ml of methanol are added 100 mg of 5% palladium on carbon. The mixture is hydrogenated at ambient temperature at an initial hydrogen pressure of 3 atmospheres for 20 hours. The reaction mixt...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=CC[NH]CC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccc2[nH]ccc2c1.c1ccc2ccccc2c1
null
[Pd].CO.C(C)OCC
null
null
CN1CC=C(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1>[Pd].CO.C(C)OCC>CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-bbe38b21f1884409ba46563e39eeffe4
Cl>>Cl
Cl.C(C)N(CCC1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12)CC>>Cl.C(C)N(CCC1=CNC2=CC=C(C=C12)NS(=O)(=O)C1=CC=CC2=CC=CC=C12)CC
[ClH:31]>>[ClH:31]
Cl
Cl
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
1.05 g (2.5 mMol) of N-[3-(2-diethylaminoethyl)-1H-indol-5-yl]naphthalene-1-sulphonamide (example 2) are dissolved in 10 ml of ethanol and 0.6 ml are added of a 4.2 N solution of hydrochloric acid in ethanol. It is allowed to crystallise at ambient temperature. N-[3-(2-diethylaminoethyl)-1H-indol-5-yl]naphthalene-1-sul...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
null
Cl>C(C)O>Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e8283582e54f4892a69fd5f201a4c969
Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1>>Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1
C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)O.Cl>>C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)O.Cl
[NH2:2][c:3]1[cH:4][cH:5][n:6]([C@@H:7]2[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12]([OH:13])[C@@H:14]2[OH:15])[c:16](=[O:17])[n:18]1>>[NH2:2][c:3]1[cH:4][cH:5][n:6]([C@@H:7]2[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12]([OH:13])[C@@H:14]2[OH:15])[c:16](=[O:17])[n:18]1
Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1
Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=c1ncccn1[C@H]1CCCO1
null
96.3
[{"value": 96.0, "product": "C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)O.Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.3, "product": "C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)O.Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
2
CELSIUS
null
null
A 5 L, 3-neck flask equipped with an overhead stirrer and thermocouple was charged with cytarabine (500 g, 2.06 mol) and methanol (2.0 L). The suspension was cooled to 2° C. HCl gas was bubbled in, giving a very thick mixture and an exotherm to 25° C. The suspension was diluted with methanol (0.5 L) to facilitate stirr...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1cncnc1.C1CCOC1
null
CO
2
null
Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1>CO>Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-1a09d052e34b42498da108bf302c1b78
CC(=O)CCC(C)=O.Nc1ccc(Br)cn1>>Cc1ccc(C)n1-c1ccc(Br)cn1
NC1=NC=C(C=C1)Br.CC(CCC(C)=O)=O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>BrC=1C=CC(=NC1)N1C(=CC=C1C)C
O=[C:2]([CH3:1])[CH2:3][CH2:4][C:5](=O)[CH3:6].[NH2:7][c:8]1[cH:9][cH:10][c:11]([Br:12])[cH:13][n:14]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH3:6])[n:7]1-[c:8]1[cH:9][cH:10][c:11]([Br:12])[cH:13][n:14]1
CC(=O)CCC(C)=O.Nc1ccc(Br)cn1
Cc1ccc(C)n1-c1ccc(Br)cn1
null
null
CCCCCCC
Aromatic Heterocycle Formation
Paal-Knorr pyrrole synthesis
0dbcc2550964c10d57651fd35699c19ea2fb10549389c3d3c9cfc6181b9e43ad
e8142154ce82c2e242e52c937b939f3fefdc51b29f1e30581e6f69472c9bf693
c1ccc(-n2cccc2)nc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](=O)-[C;D1;H3:6].[NH2;D1;+0:7]-[c;H0;D3;+0:8](:[#7;a:9]:[c:10]):[c:11]:[c:12]>>[C;D1;H3:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[C;D1;H3:6]):[n;H0;D3;+0:7]:1-[c;H0;D3;+0:8](:[#7;a:9]:[c:10]):[c:11]:[c:12]
80
[{"value": 80.0, "product": "BrC=1C=CC(=NC1)N1C(=CC=C1C)C", "details": "PERCENTYIELD", "is_desired": false}]
20
CELSIUS
2
HOUR
2-Amino-5-bromopyridine (6.0 Kg, 34.7 mol), 2,5-hexanedione (4.35 Kg, 38.2 mol) and p-toluenesulfonic acid (12 g) were dissolved in heptane (36 L) and refluxed under Dean Stark conditions overnight. The equipment was set for distillation and heptane (18 L) was removed by distillation. The mixture was cooled to 20° C. f...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Primary amine
null
null
c1ccc[nH]1
c1ccc[nH]1.c1ccncc1
HO-
CCCCCCC
20
2
CC(=O)CCC(C)=O.Nc1ccc(Br)cn1>CCCCCCC>Cc1ccc(C)n1-c1ccc(Br)cn1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-c3942f2c63344068ae32f7ebd7a47258
CON(C)C(=O)CCl.Cc1ccc(C)n1-c1ccc(Br)cn1>>Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1
Cl.ClCC(=O)N(C)OC.BrC=1C=CC(=NC1)N1C(=CC=C1C)C.C(CCC)[Li]>>ClCC(=O)C=1C=NC(=CC1)N1C(=CC=C1C)C
CON(C)[C:12](=[O:13])[CH2:14][Cl:15].Br[c:11]1[cH:10][cH:9][c:8](-[n:7]2[c:2]([CH3:1])[cH:3][cH:4][c:5]2[CH3:6])[n:17][cH:16]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH3:6])[n:7]1-[c:8]1[cH:9][cH:10][c:11]([C:12](=[O:13])[CH2:14][Cl:15])[cH:16][n:17]1
CON(C)C(=O)CCl.Cc1ccc(C)n1-c1ccc(Br)cn1
Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1
null
null
O.CC(C)(C)OC
C-C Coupling
OtherReaction
aeedefb516da447a7938cf0e8e86abd66c9a6aa8bd6688105f56ff15f4aef307
7d9aa59f8ecc532475d910f9ab122332ecbb7f9444a37371b7c1bac80798d342
c1ccc(-n2cccc2)nc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1.C-O-N(-C)-[C;H0;D3;+0:7](=[O;D1;H0:8])-[C:9]-[Cl;D1;H0:10]>>[Cl;D1;H0:10]-[C:9]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[#7;a:5]:[c:6]:1
78.8
[{"value": 78.8, "product": "ClCC(=O)C=1C=NC(=CC1)N1C(=CC=C1C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of 5-bromo-2-(2,5-dimethylpyrrol-1-yl)pyridine (1.00 Kg 3.98 mol) in TBME (7.5 L) was cooled to −70° C. n-Butyl lithium (2.5N in hexane; 1.73 L, 4.32 mol) was added drop-wise over 1 hour maintaining the temperature between −74° C. and −69° C. The mixture was then stirred at a temperature between −74° C. and ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Tertiary amide
Ketone
c1ccncc1
c1ccncc1
c1ccc[nH]1.c1ccncc1
HBr
O.CC(C)(C)OC
null
0.25
CON(C)C(=O)CCl.Cc1ccc(C)n1-c1ccc(Br)cn1>O.CC(C)(C)OC>Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-e8995507e24b4c86a0deb264fbb402c3
Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1>>Cc1ccc(C)n1-c1ccc(C2CO2)cn1
ClCC(=O)C=1C=NC(=CC1)N1C(=CC=C1C)C.O.[BH4-].[Na+]>>CC=1N(C(=CC1)C)C1=NC=C(C=C1)C1OC1
Cl[CH2:13][C:12]([c:11]1[cH:10][cH:9][c:8](-[n:7]2[c:2]([CH3:1])[cH:3][cH:4][c:5]2[CH3:6])[n:16][cH:15]1)=[O:14]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH3:6])[n:7]1-[c:8]1[cH:9][cH:10][c:11]([CH:12]2[CH2:13][O:14]2)[cH:15][n:16]1
Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1
Cc1ccc(C)n1-c1ccc(C2CO2)cn1
null
null
O1CCCC1.O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
040b28e8687bbf29652da8799a10f1a268145019b9a625d75da3ba77970763f1
98d62a2f88bda9a16db724874a7a21c7201c15ae486e75d3477ada88c887a7ad
c1ccn(-c2ccc(C3CO3)cn2)c1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[c:6]:[#7;a:7]:[c:8]>>[c:5]:[c:4](-[CH;D3;+0:2]1-[CH2;D2;+0:1]-[O;H0;D2;+0:3]-1):[c:6]:[#7;a:7]:[c:8]
98
[{"value": 98.0, "product": "CC=1N(C(=CC1)C)C1=NC=C(C=C1)C1OC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Water (1.08 Kg) was added dropwise to a suspension of sodium borohydride (0.17 Kg, 4.36 mol) in 1,4-dioxane (6.49 L) at 16° C. and the resulting solution stirred at room temperature. A solution of 2-chloro-1-[6-(2,5-dimethylpyrrol-1-yl)pyridin-3-yl]ethanone (1.08 Kg, 4.35 mol) in tetrahydrofuran (2.16 L) was added over...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ether
null
C1CO1
c1ccc[nH]1.c1ccncc1.C1CO1
Other
O1CCCC1.O1CCOCC1
null
8
Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1>O1CCCC1.O1CCOCC1>Cc1ccc(C)n1-c1ccc(C2CO2)cn1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-b710966a6568404d83990214ede4ffd5
CCC=O.C[C@H](N)CO.Cc1ccc(C)n1-c1ccc(C2CO2)cn1>>CCCN(CC(O)c1ccc(-n2c(C)ccc2C)nc1)[C@@H](C)CO
C(CC)=O.CC=1N(C(=CC1)C)C1=NC=C(C=C1)C1OC1.N[C@H](CO)C.C(C)(=O)O.C(C)(=O)O[BH-](OC(C)=O)OC(C)=O.[Na+]>>CC=1N(C(=CC1)C)C1=CC=C(C=N1)C(CN([C@H](CO)C)CCC)O
O=[CH:3][CH2:2][CH3:1].[NH2:4][C@@H:21]([CH3:22])[CH2:23][OH:24].[CH2:5]1[CH:6]([c:8]2[cH:9][cH:10][c:11](-[n:12]3[c:13]([CH3:14])[cH:15][cH:16][c:17]3[CH3:18])[n:19][cH:20]2)[O:7]1>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH:6]([OH:7])[c:8]1[cH:9][cH:10][c:11](-[n:12]2[c:13]([CH3:14])[cH:15][cH:16][c:17]2[CH3:18])[n:19][cH...
CCC=O.C[C@H](N)CO.Cc1ccc(C)n1-c1ccc(C2CO2)cn1
CCCN(CC(O)c1ccc(-n2c(C)ccc2C)nc1)[C@@H](C)CO
null
null
O.C1(=CC=CC=C1)C.C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
a87f24ce5b1e3fe1bd7467517d104e8f030c516efb839848b90fcd8dfb3aea84
7f6cbb1838c3a51c1ccf9cb420b73a7085d2d86eff0ad9e99407ef77638b78c4
c1ccc(-n2cccc2)nc1
O=[CH;D2;+0:1]-[C:2]-[C;D1;H3:3].[#7;a:4]:[c:5]:[c:6]-[C:7]1-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-1.[C:10]-[C:11](-[C;D1;H3:12])-[NH2;D1;+0:13]>>[#7;a:4]:[c:5]:[c:6]-[C:7](-[OH;D1;+0:9])-[CH2;D2;+0:8]-[N;H0;D3;+0:13](-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3])-[C:11](-[C:10])-[C;D1;H3:12]
89
[{"value": 89.0, "product": "CC=1N(C(=CC1)C)C1=CC=C(C=N1)C(CN([C@H](CO)C)CCC)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 2-(2,5-dimethylpyrrol-1-yl)-5-oxiranylpyridine (0.65 Kg, 3.04 mol), (S)-(+)-2-amino-1-propanol (0.30 Kg, 3.95 mol) in toluene (6.50 L) was heated to reflux overnight. The reaction mixture was cooled to room temperature and DCM (6.5 L) and water (1.30 L) were added and the phases allowed to separate. Sodium...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ether.Primary amine
Secondary alcohol.Tertiary amine
C1CO1
null
c1ccncc1.c1ccc[nH]1
Other
O.C1(=CC=CC=C1)C.C(Cl)Cl
null
1
CCC=O.C[C@H](N)CO.Cc1ccc(C)n1-c1ccc(C2CO2)cn1>O.C1(=CC=CC=C1)C.C(Cl)Cl>CCCN(CC(O)c1ccc(-n2c(C)ccc2C)nc1)[C@@H](C)CO
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-805059097d6842fea67f3471bb31e042
C[C@H](N)CO.Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1>>Cc1ccc(C)n1-c1ccc(C(O)CN[C@@H](C)CO)cn1
C(Cl)Cl.[BH4-].[Na+].ClCC(=O)C=1C=NC(=CC1)N1C(=CC=C1C)C.N[C@H](CO)C>>CC=1N(C(=CC1)C)C1=CC=C(C=N1)C(CN[C@H](CO)C)O
[NH2:15][C@@H:16]([CH3:17])[CH2:18][OH:19].Cl[CH2:14][C:12]([c:11]1[cH:10][cH:9][c:8](-[n:7]2[c:2]([CH3:1])[cH:3][cH:4][c:5]2[CH3:6])[n:21][cH:20]1)=[O:13]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH3:6])[n:7]1-[c:8]1[cH:9][cH:10][c:11]([CH:12]([OH:13])[CH2:14][NH:15][C@@H:16]([CH3:17])[CH2:18][OH:19])[cH:20][n:21]1
C[C@H](N)CO.Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1
Cc1ccc(C)n1-c1ccc(C(O)CN[C@@H](C)CO)cn1
null
null
O1CCCC1.O
Heteroatom Alkylation and Arylation
OtherReaction
1c7faa1e6cb9e060b7e89d591b967fa7b694f333cb5a775c79fc9a9f84d0a6be
d0da6e2f6de7d14ed85c2c5a966c155ca30e7a0510b1db3dd27bbc45bfc08d34
c1ccc(-n2cccc2)nc1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[c:6]:[#7;a:7]:[c:8].[C:9]-[C:10](-[C;D1;H3:11])-[NH2;D1;+0:12]>>[C:9]-[C:10](-[C;D1;H3:11])-[NH;D2;+0:12]-[CH2;D2;+0:1]-[CH;D3;+0:2](-[OH;D1;+0:3])-[c:4](:[c:5]):[c:6]:[#7;a:7]:[c:8]
65
[{"value": 65.0, "product": "CC=1N(C(=CC1)C)C1=CC=C(C=N1)C(CN[C@H](CO)C)O", "details": "PERCENTYIELD", "is_desired": false}]
15
CELSIUS
8
HOUR
Water (15.0 L) was added to a suspension of sodium borohydride (4.11 Kg, 109 mol) in tetrahydrofuran (140 L) at 15° C. and the resulting solution stirred at 15° C. A solution of 2-chloro-1-[6-(2,5-dimethylpyrrol-1-yl)pyridin-3-yl]ethanone (30.0 Kg, 120.6 mol) in tetrahydrofuran (100 L) and water (15 L) was added over 4...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Primary amine
Secondary alcohol.Secondary amine
null
null
c1ccc[nH]1.c1ccncc1
Other
O1CCCC1.O
15
8
C[C@H](N)CO.Cc1ccc(C)n1-c1ccc(C(=O)CCl)cn1>O1CCCC1.O>Cc1ccc(C)n1-c1ccc(C(O)CN[C@@H](C)CO)cn1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-930a6bc0fb78413f84726922de9c8a63
CC(=O)O[BH-](OC(C)=O)OC(C)=O.Cc1ccc(C)n1-c1ccc(C(O)CN[C@@H](C)CO)cn1>>CCCN(CC(O)c1ccc(-n2c(C)ccc2C)nc1)[C@@H](C)CO
CC=1N(C(=CC1)C)C1=CC=C(C=N1)C(CN[C@H](CO)C)O.C(Cl)Cl.C(C)(=O)O[BH-](OC(C)=O)OC(C)=O.[Na+].C(Cl)Cl.C(Cl)Cl>>CC=1N(C(=CC1)C)C1=CC=C(C=N1)C(CN([C@H](CO)C)CCC)O
CC(=O)O[BH-](OC(C)=O)OC(=O)[CH3:1].[NH:4]([CH2:5][CH:6]([OH:7])[c:8]1[cH:9][cH:10][c:11](-[n:12]2[c:13]([CH3:14])[cH:15][cH:16][c:17]2[CH3:18])[n:19][cH:20]1)[C@@H:21]([CH3:22])[CH2:23][OH:24]>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH:6]([OH:7])[c:8]1[cH:9][cH:10][c:11](-[n:12]2[c:13]([CH3:14])[cH:15][cH:16][c:17]2[CH3:18...
CC(=O)O[BH-](OC(C)=O)OC(C)=O.Cc1ccc(C)n1-c1ccc(C(O)CN[C@@H](C)CO)cn1
CCCN(CC(O)c1ccc(-n2c(C)ccc2C)nc1)[C@@H](C)CO
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
e1587a52a1bca6a80c6048d43276d8bccf8d3e94e692e6b210e5fd3b22494187
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(-n2cccc2)nc1
C-C(=O)-O-[BH-](-O-C(-C)=O)-O-C(=O)-[CH3;D1;+0:1].[C:2]-[C:3](-[C;D1;H3:4])-[NH;D2;+0:5]-[C:6]-[C:7]>>[C:2]-[C:3](-[C;D1;H3:4])-[N;H0;D3;+0:5](-[C:8]-[C:9]-[CH3;D1;+0:1])-[C:6]-[C:7]
100
[{"value": 100.0, "product": "CC=1N(C(=CC1)C)C1=CC=C(C=N1)C(CN([C@H](CO)C)CCC)O", "details": "PERCENTYIELD", "is_desired": false}]
20
CELSIUS
2
HOUR
Propioanaldehyde (5.02 Kg, 86.4 mol) was added over 10 minutes to a solution of (2S)-2-[{(RS)-2-[6-(2,5-dimethyl-1H-pyrrol-1-yl)pyridin-3-yl]-2-hydroxyethyl} amino]propan-1-ol (22.7 Kg, 78.6 mol) in DCM (123 L) at 20° C. The resulting solution was stirred at 20° C. for 2 hours and then allowed to settle before adding i...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
null
null
c1ccncc1.c1ccc[nH]1
HO-.B
null
20
2
CC(=O)O[BH-](OC(C)=O)OC(C)=O.Cc1ccc(C)n1-c1ccc(C(O)CN[C@@H](C)CO)cn1>>CCCN(CC(O)c1ccc(-n2c(C)ccc2C)nc1)[C@@H](C)CO
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-b3178f60b4774d0b9e3efc65f3fe44ff
COc1cc2c(cc1O)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12>>COc1cc2c(cc1O)CC[C@@H]1[C@@H]2CC[C@]2(C)CCC[C@@H]12
C[C@]12CC[C@@H]3C4=CC(=C(C=C4CC[C@H]3[C@@H]1CCC2=O)O)OC.Cl.O.NN.[OH-].[K+].C[C@]12CC[C@@H]3C4=CC(=C(C=C4CC[C@H]3[C@@H]1CCC2=O)O)OC>>COC=1C(=CC=2CC[C@H]3[C@@H]4CCC[C@@]4(C)CC[C@@H]3C2C1)O
O=[C:18]1[C@@:16]2([CH3:17])[CH2:15][CH2:14][C@@H:13]3[c:5]4[cH:4][c:3]([O:2][CH3:1])[c:8]([OH:9])[cH:7][c:6]4[CH2:10][CH2:11][C@H:12]3[C@@H:21]2[CH2:20][CH2:19]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([cH:7][c:8]1[OH:9])[CH2:10][CH2:11][C@@H:12]1[C@@H:13]2[CH2:14][CH2:15][C@:16]2([CH3:17])[CH2:18][CH2:19][CH2:20][C@@H:2...
COc1cc2c(cc1O)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
COc1cc2c(cc1O)CC[C@@H]1[C@@H]2CC[C@]2(C)CCC[C@@H]12
null
null
C(CCC)O.C(CO)O
Reduction
OtherReaction
fd58e1827afbea1124957b3c36988b8bd802de991df6da1a5316964c3ec7a550
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccc2c(c1)CC[C@@H]1[C@@H]2CCC2CCC[C@H]21
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1(-[C;D1;H3:6])-[C:7]>>[C:7]-[C:5]1(-[C;D1;H3:6])-[C:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-1
72
[{"value": 72.0, "product": "COC=1C(=CC=2CC[C@H]3[C@@H]4CCC[C@@]4(C)CC[C@@H]3C2C1)O", "details": "PERCENTYIELD", "is_desired": false}]
130
CELSIUS
null
null
2-Methoxyestrone (Scheme 1, Compound 4) (450 mg, 1.5 mmol) was suspended in ethylene glycol (10 mL) and n-butanol (2 mL). Hydrazine hydrate (0.145 mL, 3 mmol) was added and the mixture was heated to 130° C. for 1 h. The reaction was cooled to 70° C., KOH (253 mg, 4.5 mmol) was added, then the reaction was heated at 200...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
Other
C(CCC)O.C(CO)O
130
null
COc1cc2c(cc1O)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12>C(CCC)O.C(CO)O>COc1cc2c(cc1O)CC[C@@H]1[C@@H]2CC[C@]2(C)CCC[C@@H]12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-da81b91a196a42238b3e7f89d253e55f
CN(C)C=O.COc1cc2c(cc1OS(=O)(=O)C(F)(F)F)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.C[Si](C)(C)N[Si](C)(C)C>>COc1cc2c(cc1C(N)=O)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
FC(F)(F)S(=O)(=O)OC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1OC)=O.FC(F)(F)S(=O)(=O)OC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1OC)=O.C1(=CC=CC=C1)P(CCCP(C1=CC=CC=C1)C1=CC=CC=C1)C1=CC=CC=C1.C[Si](N[Si](C)(C)C)(C)C.CN(C=O)C>>COC=1C(=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C1)=O)C(=O)N
CN(C)[CH:9]=[O:11].O=S(=O)(O[c:8]1[c:3]([O:2][CH3:1])[cH:4][c:5]2[c:6]([cH:7]1)[CH2:12][CH2:13][C@@H:14]1[C@@H:15]2[CH2:16][CH2:17][C@:18]2([CH3:19])[C:20](=[O:21])[CH2:22][CH2:23][C@@H:24]12)C(F)(F)F.C[Si](C)(C)[NH:10][Si](C)(C)C>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([cH:7][c:8]1[C:9]([NH2:10])=[O:11])[CH2:12][CH2:13][...
CN(C)C=O.COc1cc2c(cc1OS(=O)(=O)C(F)(F)F)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.C[Si](C)(C)N[Si](C)(C)C
COc1cc2c(cc1C(N)=O)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
null
[Pd](Cl)Cl
null
Acylation
OtherReaction
28dfc2095901125ca6aeb494c4f6700f9e5669474dc40f8f7f307fdeb24c9e0f
20828c3ba691e9e648802e3d84cb3d844d05384246e1426a16d21d50c98982f9
O=C1CC[C@@H]2C1CC[C@@H]1c3ccccc3CC[C@H]12
C-N(-C)-[CH;D2;+0:1]=[O;D1;H0:2].C-[Si](-C)(-C)-[NH;D2;+0:3]-[Si](-C)(-C)-C.F-C(-F)(-F)-S(=O)(=O)-O-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7](-[#8:8]):[c:9]>>[#8:8]-[c:7](:[c:9]):[c;H0;D3;+0:4](-[C;H0;D3;+0:1](-[NH2;D1;+0:3])=[O;D1;H0:2]):[c:5]:[c:6]
44
[{"value": 44.0, "product": "COC=1C(=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C1)=O)C(=O)N", "details": "PERCENTYIELD", "is_desired": false}]
110
CELSIUS
5
MINUTE
A 1-L 3 neck round-bottomed flask equipped with an overhead stirrer, reflux condenser, nitrogen inlet and thermocouple, was charged with 2-methoxy-17-oxoestra-1,3,5(10)-triene-3-yl(trifluoromethyl)sulfonate (Scheme 5, Compound 42) (15 g, 34.7 mmol), 1,3-bis(diphenylphosphino)propane (1.54 g, 3.73 mmol), palladium (II) ...
10.6084/m9.figshare.5104873.v1
null
Triflate.Tertiary amide.Secondary amine.Silyl protective group.Silyl protective group
Primary amide
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
TfOH.HO-
[Pd](Cl)Cl
110
0.083333
CN(C)C=O.COc1cc2c(cc1OS(=O)(=O)C(F)(F)F)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.C[Si](C)(C)N[Si](C)(C)C>[Pd](Cl)Cl>COc1cc2c(cc1C(N)=O)CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-409b30f7236646f697e501d779c099f8
C=C1CC[C@H]2[C@@H]3CCc4cc(OS(=O)(=O)C(F)(F)F)c(OC)cc4[C@H]3CC[C@]12C.CN(C)C=O.C[Si](C)(C)N[Si](C)(C)C>>C=C1CC[C@H]2[C@@H]3CCc4cc(C(N)=O)c(OC)cc4[C@H]3CC[C@]12C
FC(F)(F)S(=O)(=O)OC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1OC)=C.FC(F)(F)S(=O)(=O)OC1=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C=C1OC)=C.C1(=CC=CC=C1)P(CCCP(C1=CC=CC=C1)C1=CC=CC=C1)C1=CC=CC=C1.C[Si](N[Si](C)(C)C)(C)C.CN(C=O)C>>COC=1C(=CC=2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3C2C1)=C)C(=O)N
O=S(=O)(O[c:11]1[cH:10][c:9]2[c:19]([cH:18][c:15]1[O:16][CH3:17])[C@@H:20]1[C@H:6]([C@@H:5]3[CH2:4][CH2:3][C:2](=[CH2:1])[C@@:23]3([CH3:24])[CH2:22][CH2:21]1)[CH2:7][CH2:8]2)C(F)(F)F.CN(C)[CH:12]=[O:14].C[Si](C)(C)[NH:13][Si](C)(C)C>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C@H:5]2[C@@H:6]3[CH2:7][CH2:8][c:9]4[cH:10][c:11]([C:12](...
C=C1CC[C@H]2[C@@H]3CCc4cc(OS(=O)(=O)C(F)(F)F)c(OC)cc4[C@H]3CC[C@]12C.CN(C)C=O.C[Si](C)(C)N[Si](C)(C)C
C=C1CC[C@H]2[C@@H]3CCc4cc(C(N)=O)c(OC)cc4[C@H]3CC[C@]12C
null
[Pd](Cl)Cl
null
Acylation
OtherReaction
28dfc2095901125ca6aeb494c4f6700f9e5669474dc40f8f7f307fdeb24c9e0f
20828c3ba691e9e648802e3d84cb3d844d05384246e1426a16d21d50c98982f9
C=C1CC[C@@H]2C1CC[C@@H]1c3ccccc3CC[C@H]12
C-N(-C)-[CH;D2;+0:1]=[O;D1;H0:2].C-[Si](-C)(-C)-[NH;D2;+0:3]-[Si](-C)(-C)-C.F-C(-F)(-F)-S(=O)(=O)-O-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7](-[#8:8]):[c:9]>>[#8:8]-[c:7](:[c:9]):[c;H0;D3;+0:4](-[C;H0;D3;+0:1](-[NH2;D1;+0:3])=[O;D1;H0:2]):[c:5]:[c:6]
null
[]
100
CELSIUS
18
HOUR
A 250 mL three-necked flask equipped with an overhead stirrer, thermocouple, and nitrogen inlet, was charged with 2-Methoxy-17-methyleneestra-1,3,5(110)-trien-3-yl(trifluoromethyl)-sulfonate (Scheme 5, Compound 48) (20.0 g, 46.5 mmol), palladium (II) chloride (0.41 g, 2.3 mmol), 1,3-bis(diphenylphosphino)propane (1.9 g...
10.6084/m9.figshare.5104873.v1
null
Triflate.Tertiary amide.Secondary amine.Silyl protective group.Silyl protective group
Primary amide
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
c1ccc2c(c1)CC[C@H]1[C@@H]3CCC[C@H]3CC[C@H]21
TfOH.HO-
[Pd](Cl)Cl
100
18
C=C1CC[C@H]2[C@@H]3CCc4cc(OS(=O)(=O)C(F)(F)F)c(OC)cc4[C@H]3CC[C@]12C.CN(C)C=O.C[Si](C)(C)N[Si](C)(C)C>[Pd](Cl)Cl>C=C1CC[C@H]2[C@@H]3CCc4cc(C(N)=O)c(OC)cc4[C@H]3CC[C@]12C
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-7607adb8172842e19e814c4670b1e131
CC(=O)OC(C)=O.NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12>>CC(=O)NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12
C(=O)(O)[O-].[Na+].Cl.ClC=1N=C2SC=CN2C1S(=O)(=O)N1C=C(C2=CC=CC=C12)CCN.C(C)N(CC)CC.C(C)(=O)OC(C)=O>>ClC=1N=C2SC=CN2C1S(=O)(=O)N1C=C(C2=CC=CC=C12)CCNC(C)=O
CC(=O)O[C:2]([CH3:1])=[O:3].[NH2:4][CH2:5][CH2:6][c:7]1[cH:8][n:9]([S:10](=[O:11])(=[O:12])[c:13]2[c:14]([Cl:15])[n:16][c:17]3[s:18][cH:19][cH:20][n:21]23)[c:22]2[cH:23][cH:24][cH:25][cH:26][c:27]12>>[CH3:1][C:2](=[O:3])[NH:4][CH2:5][CH2:6][c:7]1[cH:8][n:9]([S:10](=[O:11])(=[O:12])[c:13]2[c:14]([Cl:15])[n:16][c:17]3[s:...
CC(=O)OC(C)=O.NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12
CC(=O)NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12
null
CN(C1=CC=NC=C1)C
ClCCl
Acylation
Aminolysis of esters
87d35e51b477fc9a658a6f307eb56d84c8879182772c9dd3a42ec0d584fd2684
627cbc0550c9f51ad0105d9fcf46677e8c93bed87ee95bfe69292a82550c95b7
O=S(=O)(c1cnc2sccn12)n1ccc2ccccc21
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
92
[{"value": 92.0, "product": "ClC=1N=C2SC=CN2C1S(=O)(=O)N1C=C(C2=CC=CC=C12)CCNC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A stirred mixture of 2-{1-[(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonyl]-1H-indol-3-yl}ethylamine hydrochloride, 417 mg, 1.00 mmol) in dichloromethane and triethylamine (0.40 mL, 3.0 mmol) is treated with catalytic 4-dimethylaminopyridine (DMAP) (˜5 mg) at room temperature under nitrogen. The heterogeneous mixture...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Secondary amide
null
null
c1cn2ccsc2n1.c1c[nH]c2ccccc12
HO-
CN(C1=CC=NC=C1)C.ClCCl
null
16
CC(=O)OC(C)=O.NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12>CN(C1=CC=NC=C1)C.ClCCl>CC(=O)NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-67b6ab2bb49b4b18a905c4f867c281dc
O=C(O)Cc1c[nH]c2ccccc12.O=S(=O)(Cl)c1c(Cl)nc2sccn12>>O=C(O)Cc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12
C(CCC)[Li].N1C=C(C2=CC=CC=C12)CC(=O)O.ClC=1N=C2SC=CN2C1S(=O)(=O)Cl>>ClC=1N=C2SC=CN2C1S(=O)(=O)N1C=C(C2=CC=CC=C12)CC(=O)O
[O:1]=[C:2]([OH:3])[CH2:4][c:5]1[cH:6][nH:7][c:20]2[cH:21][cH:22][cH:23][cH:24][c:25]12.Cl[S:8](=[O:9])(=[O:10])[c:11]1[c:12]([Cl:13])[n:14][c:15]2[s:16][cH:17][cH:18][n:19]12>>[O:1]=[C:2]([OH:3])[CH2:4][c:5]1[cH:6][n:7]([S:8](=[O:9])(=[O:10])[c:11]2[c:12]([Cl:13])[n:14][c:15]3[s:16][cH:17][cH:18][n:19]23)[c:20]2[cH:21...
O=C(O)Cc1c[nH]c2ccccc12.O=S(=O)(Cl)c1c(Cl)nc2sccn12
O=C(O)Cc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12
null
null
C1CCOC1
Acylation
OtherReaction
95ce265d6113e7bac468269631ca11b794a98d7e0e0f7d7a9efc825210a64f28
97f7469015d28c17dd04331dd6d96add6c8052624259a8aad52811d647e364c7
O=S(=O)(c1cnc2sccn12)n1ccc2ccccc21
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4]1:[#7;a:5]2:[c:6]:[c:7]:[#16;a:8]:[c:9]:2:[#7;a:10]:[c:11]:1-[Cl;D1;H0:12].[c:13]:[c:14]1:[c:15]:[c:16]:[c:17]:[nH;D2;+0:18]:1>>[Cl;D1;H0:12]-[c:11]1:[#7;a:10]:[c:9]2:[#16;a:8]:[c:7]:[c:6]:[#7;a:5]:2:[c:4]:1-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[n;H0;D3;+0:18]1:[...
null
[]
null
null
1
HOUR
A stirred solution of 3-indolylacetic acid (175 mg, 1.00 mmol) in THF is cooled to −78° C. under nitrogen and treated portionwise with 2.5 M n-butyllithium in hexanes (0.84 mL, 2.10 mmol) over a 10 min. period. After 1 h at −78° C., the reaction mixture is treated with (6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonyl ...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
null
c1ccc2[nH]ccc2c1
c1c[nH]c2ccccc12
c1cn2ccsc2n1.c1c[nH]c2ccccc12
HCl
C1CCOC1
null
1
O=C(O)Cc1c[nH]c2ccccc12.O=S(=O)(Cl)c1c(Cl)nc2sccn12>C1CCOC1>O=C(O)Cc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-9adc3242043549e2b147b75100f9d183
COC(=O)C1OC(OC(=O)NCCc2cn(S(=O)(=O)c3c(Cl)nc4sccn34)c3ccccc23)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O>>O=C(NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12)O[C@@H]1O[C@H](C(=O)O)[C@@H](O)[C@H](O)[C@H]1O
O[Li].O.COC(=O)C1OC(C(C(C1OC(C)=O)OC(C)=O)OC(C)=O)OC(NCCC1=CN(C2=CC=CC=C12)S(=O)(=O)C1=C(N=C2SC=CN21)Cl)=O.CO>>ClC=1N=C2SC=CN2C1S(=O)(=O)N1C=C(C2=CC=CC=C12)CCNC(=O)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)C(=O)O
CC(=O)[O:35][CH:34]1[CH:30]([C:31](=[O:32])[O:33]C)[O:29][CH:28]([O:27][C:2](=[O:1])[NH:3][CH2:4][CH2:5][c:6]2[cH:7][n:8]([S:9](=[O:10])(=[O:11])[c:12]3[c:13]([Cl:14])[n:15][c:16]4[s:17][cH:18][cH:19][n:20]34)[c:21]3[cH:22][cH:23][cH:24][cH:25][c:26]23)[CH:38]([O:39]C(C)=O)[CH:36]1[O:37]C(C)=O>>[O:1]=[C:2]([NH:3][CH2:4...
COC(=O)C1OC(OC(=O)NCCc2cn(S(=O)(=O)c3c(Cl)nc4sccn34)c3ccccc23)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O
O=C(NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12)O[C@@H]1O[C@H](C(=O)O)[C@@H](O)[C@H](O)[C@H]1O
null
null
O.C1CCOC1
Reduction
OtherReaction
ac21e131e66a6fc26598d42c229af8ee8a14320b82729f3ff0604619f2d5774a
774ba88a5fc25f9cae8664c12e4c35fb030d3c68b1211c590a49c4e8da3b6eaa
O=C(NCCc1cn(S(=O)(=O)c2cnc3sccn23)c2ccccc12)O[C@H]1CCCCO1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[CH;D3;+0:4]1-[#8:5]-[C:6](-[#8:7]-[C:8]=[O;D1;H0:9])-[CH;D3;+0:10](-[O;H0;D2;+0:11]-C(-C)=O)-[CH;D3;+0:12](-[O;H0;D2;+0:13]-C(-C)=O)-[CH;D3;+0:14]-1-[O;H0;D2;+0:15]-C(-C)=O>>[O;D1;H0:9]=[C:8]-[#8:7]-[C:6]1-[#8:5]-[C@H;D3;+0:4](-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1])-[C@@H;D3;+0:14](-[OH...
86
[{"value": 86.0, "product": "ClC=1N=C2SC=CN2C1S(=O)(=O)N1C=C(C2=CC=CC=C12)CCNC(=O)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
2
HOUR
A solution of 3,4,5-triacetoxy-6-(2-{1-[(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonyl]-1H-indol-3-yl}ethycarbamoyloxy)tetrahydropyran-2-carboxylic acid methyl ester (1.0 g, 1.35 mmol) in THF is treated with CH3OH (38.8 mL) and H2O (10 mL), cooled to 0° C. (ice-water bath), treated with a solution of LiOH.H2O (340 m...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester
Carboxylic acid.Secondary alcohol.Secondary alcohol.Secondary alcohol
null
null
c1cn2ccsc2n1.c1c[nH]c2ccccc12.C1CCOCC1
HO-
O.C1CCOC1
0
2
COC(=O)C1OC(OC(=O)NCCc2cn(S(=O)(=O)c3c(Cl)nc4sccn34)c3ccccc23)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O>O.C1CCOC1>O=C(NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12)O[C@@H]1O[C@H](C(=O)O)[C@@H](O)[C@H](O)[C@H]1O
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-47698fe631f744f7bb78fc6f4bd9c905
O=C(Cl)OCc1ccccc1.O=C1CCNCC1>>O=C1CCN(C(=O)OCc2ccccc2)CC1
O.Cl.N1CCC(CC1)=O.C(C1=CC=CC=C1)OC(=O)Cl.Cl>>C(C1=CC=CC=C1)OC(=O)N1CCC(CC1)=O
Cl[C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[O:1]=[C:2]1[CH2:3][CH2:4][NH:5][CH2:16][CH2:17]1>>[O:1]=[C:2]1[CH2:3][CH2:4][N:5]([C:6](=[O:7])[O:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[CH2:16][CH2:17]1
O=C(Cl)OCc1ccccc1.O=C1CCNCC1
O=C1CCN(C(=O)OCc2ccccc2)CC1
null
null
[OH-].[Na+]
Protection
N-alkylation of secondary amines with alkyl halides
c6eb958652ca8104567d61601fc03a9cfee33fb7bb328952993831b03fec41c4
d86dc1e6d0e089b3444b62ddfcf4c4822bdac4b60e628553036562518c29adcd
O=C1CCN(C(=O)OCc2ccccc2)CC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[O;D1;H0:5]=[C:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[C:6](=[O;D1;H0:5])-[C:11]-[C:10]-1
100.3
[{"value": 100.3, "product": "C(C1=CC=CC=C1)OC(=O)N1CCC(CC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A 4-piperidone hydrochloride monohydrate (15.3 g) was dissolved in 2N aqueous solution of sodium hydroxide (100 mL). To the solution was added a benzyloxycarbonyl chloride (20.4 g) at 0° C. The mixture was stirred for 1 hour. The reaction mixture was neutralized with 2N hydrochloric acid, and the aqueous solution was e...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Secondary amine
Carbamic ester
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1
HCl
[OH-].[Na+]
null
1
O=C(Cl)OCc1ccccc1.O=C1CCNCC1>[OH-].[Na+]>O=C1CCN(C(=O)OCc2ccccc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-b14c93ecec2d476e8a8652d824d39716
CCCCN1C(=O)N(CC(C)C)C(=O)C12CCNCC2.OCCCCCCc1ccccc1>>CCCCN1C(=O)N(CC(C)C)C(=O)C12CCN(CCCCCCc1ccccc1)CC2.Cl
C(CCC)N1C(N(C(C12CCNCC2)=O)CC(C)C)=O.C(C)(C)N(C(C)C)CC.[O-]S(=O)Cl.S(=O)(=O)(C1=CC=C(C)C=C1)Cl.C1(=CC=CC=C1)CCCCCCO>>Cl.C(CCC)N1C(N(C(C12CCN(CC2)CCCCCCC2=CC=CC=C2)=O)CC(C)C)=O
[CH3:1][CH2:2][CH2:3][CH2:4][N:5]1[C:6](=[O:7])[N:8]([CH2:9][CH:10]([CH3:11])[CH3:12])[C:13](=[O:14])[C:15]12[CH2:16][CH2:17][NH:18][CH2:31][CH2:32]2.O[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]1[C:6](=[O:7])[N:8]([CH2:9][CH:10]([CH3:11]...
CCCCN1C(=O)N(CC(C)C)C(=O)C12CCNCC2.OCCCCCCc1ccccc1
CCCCN1C(=O)N(CC(C)C)C(=O)C12CCN(CCCCCCc1ccccc1)CC2.Cl
null
null
C(C)#N
Functional Group Interconversion
OtherReaction
f01877d5f4d6b145622352021fe8f9745a4c30591b43e5dec47ccc59181025f7
6e06e85700930d51d4c0cb20c3022615516bd88d7fb3acc5347c37adfe490c2e
O=C1NC(=O)C2(CCN(CCCCCCc3ccccc3)CC2)N1
O-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7]-[C:8]>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:7]-[C:8]
58.9
[{"value": 58.9, "product": "Cl.C(CCC)N1C(N(C(C12CCN(CC2)CCCCCCC2=CC=CC=C2)=O)CC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
18
HOUR
To a solution of the compound prepared in Example 1 (28 mg) and N,N-diisopropylethylamine (155 mg) in acetonitrile (3 mL) were added benzenesulfonylchloride resin (Argonaut, product name PS-TsCl, product number 800276, 1.22 mmol/g, 0.20 mmol) (164 mg) and sulfonyl resin (175 mg) which is prepared from 6-phenylhexanol (...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Secondary amine
Tertiary amine
C1CC2(CCN1)C[NH]C[NH]2
C1CC2(CC[NH]1)C[NH]C[NH]2
C1CC2(CC[NH]1)C[NH]C[NH]2.c1ccccc1
null
C(C)#N
70
18
CCCCN1C(=O)N(CC(C)C)C(=O)C12CCNCC2.OCCCCCCc1ccccc1>C(C)#N>CCCCN1C(=O)N(CC(C)C)C(=O)C12CCN(CCCCCCc1ccccc1)CC2.Cl
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-d47409756b99485191fa800c4bb3463b
CC(C)(C)OC(=O)OC(=O)[O-].CCCCN1C(=O)NC(=O)C12CCNCC2>>CCCCN1C(=O)NC(=O)C12CCN(C(=O)OC(C)(C)C)CC2
Cl.C(CCC)N1C(NC(C12CCNCC2)=O)=O.C([O-])([O-])=O.[K+].[K+].C(=O)(OC(C)(C)C)OC(=O)[O-]>>C(CCC)N1C(NC(C12CCN(CC2)C(=O)OC(C)(C)C)=O)=O
O=C([O-])O[C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21].[CH3:1][CH2:2][CH2:3][CH2:4][N:5]1[C:6](=[O:7])[NH:8][C:9](=[O:10])[C:11]12[CH2:12][CH2:13][NH:14][CH2:22][CH2:23]2>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]1[C:6](=[O:7])[NH:8][C:9](=[O:10])[C:11]12[CH2:12][CH2:13][N:14]([C:15](=[O:16])[O:17][C:18]([CH3:19])([...
CC(C)(C)OC(=O)OC(=O)[O-].CCCCN1C(=O)NC(=O)C12CCNCC2
CCCCN1C(=O)NC(=O)C12CCN(C(=O)OC(C)(C)C)CC2
null
null
O
Protection
Boc amine protection of secondary amine
d816530f227781f8e6590c0d5cfe00eacef223384b02c93d14dd45764d658f23
94226cf5c3bba13e4d3d11ce3d1edf3253d2a0a588e2936ded4f0148bd13453e
O=C1NC(=O)C2(CCNCC2)N1
O=C(-[O-])-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7].[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]>>[C:8]-[C:9]-[N;H0;D3;+0:10](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7])-[C:11]-[C:12]
89
[{"value": 89.0, "product": "C(CCC)N1C(NC(C12CCN(CC2)C(=O)OC(C)(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of the compound prepared in Example 5 (326 mg) in water (3 mL) were added potassium carbonate and t-butyl dicarbonate (348 mg) subsequently, and the mixture was stirred for 1 hour at room temperature. The reaction mixture was neutralized with 1N hydrochloric acid. The aqueous layer was extracted three tim...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Carbonic Acid.Carbonic Ester.Secondary amine
Carbamic ester
C1CC2(CCN1)CNC[NH]2
C1CC2(CC[NH]1)CNC[NH]2
C1CC2(CC[NH]1)CNC[NH]2
HO-
O
null
1
CC(C)(C)OC(=O)OC(=O)[O-].CCCCN1C(=O)NC(=O)C12CCNCC2>O>CCCCN1C(=O)NC(=O)C12CCN(C(=O)OC(C)(C)C)CC2
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-976196165fb343849eb72f934f0676e2
CS(C)=O.O=C1CCN(C(=O)OCc2ccccc2)CC1>>C=C1CCN(C(=O)OCc2ccccc2)CC1
CS(=O)C.[H-].[Na+].CS(=O)C.O=C1CCN(CC1)C(=O)OCC1=CC=CC=C1.CS(=O)C.O>>C=C1CCN(CC1)C(=O)OCC1=CC=CC=C1
CS(=O)[CH3:1].O=[C:2]1[CH2:3][CH2:4][N:5]([C:6](=[O:7])[O:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[CH2:16][CH2:17]1>>[CH2:1]=[C:2]1[CH2:3][CH2:4][N:5]([C:6](=[O:7])[O:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[CH2:16][CH2:17]1
CS(C)=O.O=C1CCN(C(=O)OCc2ccccc2)CC1
C=C1CCN(C(=O)OCc2ccccc2)CC1
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
null
C-C Coupling
OtherReaction
593fb794de720cb3f59082c2c95327f5639ea17530f6acb7c816aef56ee603f2
6fc2b071b1f532559c8505df2edcc254183c53cc557dcde7348c30c4ff0e0293
C=C1CCN(C(=O)OCc2ccccc2)CC1
C-S(=O)-[CH3;D1;+0:1].O=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[#7:5]-[C:6]-[C:7]-1>>[CH2;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[#7:5]-[C:6]-[C:7]-1
null
[]
60
CELSIUS
30
MINUTE
A sodium hydride (13.2 g) was added to an anhydrous dimethylsulfoxide (176 mL) and the mixture was heated for 2 hours at 60° C. After cooling, to a suspension of methyltriphenylphosphonium bromide (110.4 g) in dimethylsulfoxide (120 mL) was added the reaction mixture, and the mixture was stirred for 30 minutes at room ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Sulfoxide
Vinyl
C1CC[NH]CC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1
Other
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
60
0.5
CS(C)=O.O=C1CCN(C(=O)OCc2ccccc2)CC1>[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>C=C1CCN(C(=O)OCc2ccccc2)CC1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8edc50dcb802428d8fb2902680b5c810
O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1.O=CCCc1ccccc1>>O=C1c2ccccc2OC2(CCN(CCCc3ccccc3)CC2)CN1Cc1ccccc1
C(C1=CC=CC=C1)N1CC2(CCNCC2)OC2=C(C1=O)C=CC=C2.C1(=CC=CC=C1)CCC=O>>C(C1=CC=CC=C1)N1CC2(CCN(CC2)CCCC2=CC=CC=C2)OC2=C(C1=O)C=CC=C2
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[O:9][C:10]2([CH2:11][CH2:12][NH:13][CH2:23][CH2:24]2)[CH2:25][N:26]1[CH2:27][c:28]1[cH:29][cH:30][cH:31][cH:32][cH:33]1.O=[CH:14][CH2:15][CH2:16][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[O:9][C:10]2([CH2:11][CH2:12][N:1...
O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1.O=CCCc1ccccc1
O=C1c2ccccc2OC2(CCN(CCCc3ccccc3)CC2)CN1Cc1ccccc1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
reductive amination
cab13708e7b292a586907f472f086163341816f4e309b786c5613261810170cd
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
O=C1c2ccccc2OC2(CCN(CCCc3ccccc3)CC2)CN1Cc1ccccc1
O=[CH;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7]-[C:8]>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:7]-[C:8]
null
[]
25
CELSIUS
8
HOUR
To a solution of the compound prepared in Example 30 (0.01 mmol) in tetrahydrofuran (0.4 mL) were added 3-phenylpropanal (0.02 mmol) and MP-BH(OAc)3 (Argonaut, product number 800415, loading; 2.25 mmol/g) (13.3 mg). The mixture was stirred overnight at 25° C. To the reaction mixture were added tetrahydrofuran (0.4 mL) ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1ccc2c(c1)C[NH]CC1(CCNCC1)O2
c1ccc2c(c1)C[NH]CC1(CC[NH]CC1)O2
c1ccc2c(c1)C[NH]CC1(CC[NH]CC1)O2.c1ccccc1.c1ccccc1
Other
O1CCCC1
25
8
O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1.O=CCCc1ccccc1>O1CCCC1>O=C1c2ccccc2OC2(CCN(CCCc3ccccc3)CC2)CN1Cc1ccccc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-36a25b36fc474b1286cb28173d92e0f6
O=C(Cl)C1CCCC1.O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1>>O=C1c2ccccc2OC2(CCN(C(=O)C3CCCC3)CC2)CN1Cc1ccccc1
C(C(CO)(CO)N)O.C(C1=CC=CC=C1)N1CC2(CCNCC2)OC2=C(C1=O)C=CC=C2.C1(CCCC1)C(=O)Cl>>C(C1=CC=CC=C1)N1CC2(CCN(CC2)C(=O)C2CCCC2)OC2=C(C1=O)C=CC=C2
Cl[C:14](=[O:15])[CH:16]1[CH2:17][CH2:18][CH2:19][CH2:20]1.[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[O:9][C:10]2([CH2:11][CH2:12][NH:13][CH2:21][CH2:22]2)[CH2:23][N:24]1[CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[O:9][C:10]2([CH2:11][CH2:12][N:13]([C:14](...
O=C(Cl)C1CCCC1.O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1
O=C1c2ccccc2OC2(CCN(C(=O)C3CCCC3)CC2)CN1Cc1ccccc1
null
null
ClC(C)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
36f1c0bfb99e2f9b2d14ec2c5050fb72b5b1281d5fcbeed0d46117918e5cbf45
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C1c2ccccc2OC2(CCN(C(=O)C3CCCC3)CC2)CN1Cc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[C:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[C:5])-[C:9]-[C:10]
null
[]
25
CELSIUS
8
HOUR
To a solution of the compound prepared in Example 30 (0.010 mmol) in dichloroethane (0.7 mL) were added cyclopentanecarbonylchloride (0.020 mmol) and poly(4-vinylpyridine) (2% cross-linked, Aldrich, CAS#9017-40-7) (5.3 mg). The mixture was stirred overnight at 25° C. To the reaction mixture was added PS-trisamine (Argo...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
c1ccc2c(c1)C[NH]CC1(CCNCC1)O2
c1ccc2c(c1)C[NH]CC1(CC[NH]CC1)O2
c1ccc2c(c1)C[NH]CC1(CC[NH]CC1)O2.C1CCCC1.c1ccccc1
HCl
ClC(C)Cl
25
8
O=C(Cl)C1CCCC1.O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1>ClC(C)Cl>O=C1c2ccccc2OC2(CCN(C(=O)C3CCCC3)CC2)CN1Cc1ccccc1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-ee60cafbad574b10a5cdb22bc2c72c38
O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1.O=C=NC1CCCC1>>O=C(NC1CCCC1)N1CCC2(CC1)CN(Cc1ccccc1)C(=O)c1ccccc1O2
C(C(CO)(CO)N)O.C(C1=CC=CC=C1)N1CC2(CCNCC2)OC2=C(C1=O)C=CC=C2.C1(CCCC1)N=C=O>>C(C1=CC=CC=C1)N1CC2(CCN(CC2)C(=O)NC2CCCC2)OC2=C(C1=O)C=CC=C2
[NH:9]1[CH2:10][CH2:11][C:12]2([CH2:13][CH2:14]1)[CH2:15][N:16]([CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)[C:24](=[O:25])[c:26]1[cH:27][cH:28][cH:29][cH:30][c:31]1[O:32]2.[O:1]=[C:2]=[N:3][CH:4]1[CH2:5][CH2:6][CH2:7][CH2:8]1>>[O:1]=[C:2]([NH:3][CH:4]1[CH2:5][CH2:6][CH2:7][CH2:8]1)[N:9]1[CH2:10][CH2:11][C:12]2...
O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1.O=C=NC1CCCC1
O=C(NC1CCCC1)N1CCC2(CC1)CN(Cc1ccccc1)C(=O)c1ccccc1O2
null
null
ClC(C)Cl
Acylation
Urea synthesis via isocyanate and secondary amine
f4f68aa12a4bf52f03cdb454deba752e653bd798d66151d0bd499d5ce7635a71
5272a383a93723269f1934f97993b0175b43cd993bcdf2f45add1dbb852d1e09
O=C(NC1CCCC1)N1CCC2(CC1)CN(Cc1ccccc1)C(=O)c1ccccc1O2
[C:1]-[C:2](-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5])-[C:6].[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]>>[C:7]-[C:8]-[N;H0;D3;+0:9](-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:3]-[C:2](-[C:1])-[C:6])-[C:10]-[C:11]
null
[]
25
CELSIUS
8
HOUR
To a solution of the compound prepared in Example 30 (0.010 mmol) in dichloroethane (0.7 mL) was added cyclopentylisocyanate (0.020 mmol), the mixture was stirred overnight at 25° C. To the reaction mixture was added PS-trisamine (Argonaut, product number 800229, loading; 4.36 mmol/g) (6.9 mg). After stirring overnight...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Secondary amine
Urea
c1ccc2c(c1)C[NH]CC1(CCNCC1)O2
c1ccc2c(c1)C[NH]CC1(CC[NH]CC1)O2
C1CCCC1.c1ccccc1.c1ccc2c(c1)C[NH]CC1(CC[NH]CC1)O2
null
ClC(C)Cl
25
8
O=C1c2ccccc2OC2(CCNCC2)CN1Cc1ccccc1.O=C=NC1CCCC1>ClC(C)Cl>O=C(NC1CCCC1)N1CCC2(CC1)CN(Cc1ccccc1)C(=O)c1ccccc1O2
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-baafc576f1474e7fb9a12c824e87400d
Oc1ccnc2cccnc12.c1ccc2ncccc2c1>>CCCN.Nc1ccnc2cccnc12
CS(=O)(=O)Cl.FC(S(=O)(=O)OS(=O)(=O)C(F)(F)F)(F)F.N1=CC=CC2=CC=CC=C12.OC1=CC=NC2=CC=CN=C12>>NC1=CC=NC2=CC=CN=C12.C(CC)N
O[c:6]1[cH:7][cH:8][n:9][c:10]2[cH:11][cH:12][cH:13][n:4][c:15]12.c1cc2c[cH:1][cH:2][cH:3]c2[n:5]c1>>[CH3:1][CH2:2][CH2:3][NH2:4].[NH2:5][c:6]1[cH:7][cH:8][n:9][c:10]2[cH:11][cH:12][cH:13][n:14][c:15]12
Oc1ccnc2cccnc12.c1ccc2ncccc2c1
CCCN.Nc1ccnc2cccnc12
null
null
N1=CC=CC=C1.P(=O)(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
b920627501e0b78695d1f74f03b9b5240dde241078ccd0ada39ed7b9c7cd004c
11a0d4fd36384a8e12e77a477d006f39b61f75211efa6ba3ed965004c60c82a4
c1cnc2cccnc2c1
O-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[c:7]:[cH;D2;+0:8]:[n;H0;D2;+0:9]:[c;H0;D3;+0:10]:2:1.[cH;D2;+0:11]1:[cH;D2;+0:12]:[cH;D2;+0:13]:c2:[n;H0;D2;+0:14]:c:c:c:c:2:c:1>>[CH3;D1;+0:11]-[CH2;D2;+0:12]-[CH2;D2;+0:13]-[NH2;D1;+0:9].[NH2;D1;+0:14]-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:[c:7]:[cH;D2;...
null
[]
null
null
null
null
4-Hydroxy-1,5-naphthyridines can be prepared from 3-aminopyridine derivatives by reaction with diethyl ethoxymethylene malonate to produce the 4-hydroxy-3-carboxylic acid ester derivative with subsequent hydrolysis to the acid, followed by thermal decarboxylation in quinoline (as for example described for 4-Hydroxy-[1,...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Primary amine.Primary amine
c1cnc2cccnc2c1.c1ccc2ncccc2c1
c1cnc2cccnc2c1
c1cnc2cccnc2c1
Other
N1=CC=CC=C1.P(=O)(Cl)(Cl)Cl
null
null
Oc1ccnc2cccnc12.c1ccc2ncccc2c1>N1=CC=CC=C1.P(=O)(Cl)(Cl)Cl>CCCN.Nc1ccnc2cccnc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-06b6e82898044d80ac59438df31c00cd
Brc1cccc2ccncc12>>O=c1[nH]ccc2cccc(Br)c12
BrC=1C=CC=C2C=CN=CC12.C(C)OC(C=O)OCC>>BrC=1C=CC=C2C=CNC(C12)=O
[cH:2]1[n:3][cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([Br:11])[c:12]12>>[O:1]=[c:2]1[nH:3][cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([Br:11])[c:12]12
Brc1cccc2ccncc12
O=c1[nH]ccc2cccc(Br)c12
null
null
null
Oxidation
OtherReaction
e9c4006c1d3c140a429b5a663648b08cb79a652ba3eeab8801d7f4317b065849
82a3692de44364afcfd8cc4460435180e0752c31812bf6008d75e02664a32947
O=c1[nH]ccc2ccccc12
[c:1]:[c:2]1:[c:3]:[c:4]:[c:5]:[n;H0;D2;+0:6]:[cH;D2;+0:7]:1>>[O;D1;H0:8]=[c;H0;D3;+0:7]1:[nH;D2;+0:6]:[c:5]:[c:4]:[c:3]:[c:2]:1:[c:1]
null
[]
null
null
null
null
The isoquinolin-8-yl system can be prepared from the appropriately substituted benzylamine by cyclocondensation with diethoxy-acetaldehyde (see, for example, K. Kido and Y. Watanabe, Chemical & Pharmaceutical Bulletin, 35(12), 4964-6; 1987). Alternatively 8-bromo-isoquinoline (prepared by the method of F. T. Tyson, J.A...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2cnccc2c1
c1cccc2ccncc12
c1cccc2ccncc12
Other
null
null
null
Brc1cccc2ccncc12>>O=c1[nH]ccc2cccc(Br)c12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-8d9dc825fe334515b6fc7488d845bd7e
CC1(C)OC(=O)CC(=O)O1.N#Cc1ccc(N)cc1>>CC1(C)OC(=O)C(=CNc2ccc(C#N)cc2)C(=O)O1
NC1=CC=C(C#N)C=C1.CC1(OC(CC(O1)=O)=O)C.COC(OC)OC>>CC1(OC(C(C(O1)=O)=CNC1=CC=C(C#N)C=C1)=O)C
[CH3:1][C:2]1([CH3:3])[O:4][C:5](=[O:6])[CH2:7][C:18](=[O:19])[O:20]1.[NH2:9][c:10]1[cH:11][cH:12][c:13]([C:14]#[N:15])[cH:16][cH:17]1>>[CH3:1][C:2]1([CH3:3])[O:4][C:5](=[O:6])[C:7](=[CH:8][NH:9][c:10]2[cH:11][cH:12][c:13]([C:14]#[N:15])[cH:16][cH:17]2)[C:18](=[O:19])[O:20]1
CC1(C)OC(=O)CC(=O)O1.N#Cc1ccc(N)cc1
CC1(C)OC(=O)C(=CNc2ccc(C#N)cc2)C(=O)O1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
16f6e689ff4988a3075463cf8c372a4929ef73d83eb11dd6443a2ba775713df7
cb45d3f2664ea1c07edca6192a95c91d6c98f4c61196cc5a896d41447e7a94b5
O=C1OCOC(=O)C1=CNc1ccccc1
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[#8:7]-[C:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[CH2;D2;+0:12]-1>>[O;D1;H0:5]=[C:6]1-[#8:7]-[C:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D3;+0:12]-1=[C:13]-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]
97
[{"value": 97.0, "product": "CC1(OC(C(C(O1)=O)=CNC1=CC=C(C#N)C=C1)=O)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4-amino-benzonitrile (12.5 g, 0.106 mol), 2,2-dimethyl-[1,3]dioxane-4,6-dione (18.3 g, 0.127 mol) and trimethylorthoformate (16 ml) in ethanol (100 ml) was refluxed for 3 hours. After cooling the solid was filtered off, washed with ethanol and air dried. The product was obtained as an off-white solid (27.9...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Primary amine
Enamine
C1COCOC1
C1COCOC1
C1COCOC1.c1ccccc1
Other
C(C)O
null
null
CC1(C)OC(=O)CC(=O)O1.N#Cc1ccc(N)cc1>C(C)O>CC1(C)OC(=O)C(=CNc2ccc(C#N)cc2)C(=O)O1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-0e707d5fa7344215a30237ad995c66c0
CC1(C)OC(=O)C(=CNc2ccc(C#N)cc2)C(=O)O1>>N#Cc1ccc2[nH]ccc(=O)c2c1
CC1(OC(C(C(O1)=O)=CNC1=CC=C(C#N)C=C1)=O)C.C1=CC=C(C=C1)C2=CC=CC=C2.C1=CC=C(C=C1)OC2=CC=CC=C2>>O=C1C=CNC2=CC=C(C=C12)C#N
CC1(C)OC(=O)[C:9](=[CH:8][NH:7][c:6]2[cH:5][cH:4][c:3]([C:2]#[N:1])[cH:13][cH:12]2)[C:10](=[O:11])O1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[nH:7][cH:8][cH:9][c:10](=[O:11])[c:12]2[cH:13]1
CC1(C)OC(=O)C(=CNc2ccc(C#N)cc2)C(=O)O1
N#Cc1ccc2[nH]ccc(=O)c2c1
null
null
CCOCC
Reduction
OtherReaction
52b8b44ec33384424e5377fd29a8403152187dc69024d02f388dfabe3faf6d53
be90257307957f9ad8e8667a185148216df19dcbaac80f1b7b16cd45c83e3aa5
O=c1cc[nH]c2ccccc12
C-C1(-C)-O-C(=O)-[C;H0;D3;+0:1](=[CH;D2;+0:2]-[NH;D2;+0:3]-[c:4](:[c:5]):[cH;D2;+0:6]:[c:7]:[c:8])-[C;H0;D3;+0:9](=[O;D1;H0:10])-O-1>>[O;D1;H0:10]=[c;H0;D3;+0:9]1:[cH;D2;+0:1]:[cH;D2;+0:2]:[nH;D2;+0:3]:[c:4](:[c:5]):[c;H0;D3;+0:6]:1:[c:7]:[c:8]
94.3
[{"value": 94.0, "product": "O=C1C=CNC2=CC=C(C=C12)C#N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.3, "product": "O=C1C=CNC2=CC=C(C=C12)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Intermediate (a) (27.5 g, 0.101 mol) was slowly added over five minutes to refluxing Dowtherm A (200 ml). After an additional five minutes at reflux, the mixture was allow to cool to room temperature then ether (200 ml) was added. The product was filtered off, thoroughly washed with ether then air dried to afford the p...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Ester
null
C1COCOC1.c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HO-
CCOCC
null
null
CC1(C)OC(=O)C(=CNc2ccc(C#N)cc2)C(=O)O1>CCOCC>N#Cc1ccc2[nH]ccc(=O)c2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-04563999b3a041a0b74bd013cbe3b613
BrP(Br)Br.N#Cc1ccc2[nH]ccc(=O)c2c1>>N#Cc1ccc2nccc(Br)c2c1
O=C1C=CNC2=CC=C(C=C12)C#N.P(Br)(Br)Br>>BrC1=CC=NC2=CC=C(C=C12)C#N
BrP(Br)[Br:11].O=[c:10]1[cH:9][cH:8][nH:7][c:6]2[cH:5][cH:4][c:3]([C:2]#[N:1])[cH:13][c:12]21>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[n:7][cH:8][cH:9][c:10]([Br:11])[c:12]2[cH:13]1
BrP(Br)Br.N#Cc1ccc2[nH]ccc(=O)c2c1
N#Cc1ccc2nccc(Br)c2c1
null
null
O.CN(C)C=O
Functional Group Interconversion
OtherReaction
438e974ce5f8b1c45ff57c7a7dddacdfe9d2415c193d181f3fd6e6e5ac7f9d1c
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2ncccc2c1
Br-P(-Br)-[Br;H0;D1;+0:1].O=[c;H0;D3;+0:2]1:[c:3]:[c:4]:[nH;D2;+0:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[n;H0;D2;+0:5]:[c:6](:[c:7]):[c:8]:1:[c:9]
87
[{"value": 87.0, "product": "BrC1=CC=NC2=CC=C(C=C12)C#N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.0, "product": "BrC1=CC=NC2=CC=C(C=C12)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of (b) (12 g, 70.5 mmol) in DMF (75 ml) was added dropwise phosphorous tribromide (8 ml, 84.6 mmol) over five minutes (slightly exothermic). The reaction was allowed to cool to room temperature and was then diluted with ice water (100 ml) and stirred 1 hour then diluted with additional water (300 ml). The...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HBr
O.CN(C)C=O
null
1
BrP(Br)Br.N#Cc1ccc2[nH]ccc(=O)c2c1>O.CN(C)C=O>N#Cc1ccc2nccc(Br)c2c1
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-3322c82fa1d54539995fdfa8f5ce8b6b
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.N#Cc1ccc2nccc(Br)c2c1>>C=Cc1ccnc2ccc(C#N)cc12
BrC1=CC=NC2=CC=C(C=C12)C#N.C(=C)[Sn](CCCC)(CCCC)CCCC>>C(=C)C1=CC=NC2=CC=C(C=C12)C#N
CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)[CH:2]=[CH2:1].Br[c:3]1[cH:4][cH:5][n:6][c:7]2[cH:8][cH:9][c:10]([C:11]#[N:12])[cH:13][c:14]12>>[CH2:1]=[CH:2][c:3]1[cH:4][cH:5][n:6][c:7]2[cH:8][cH:9][c:10]([C:11]#[N:12])[cH:13][c:14]12
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.N#Cc1ccc2nccc(Br)c2c1
C=Cc1ccnc2ccc(C#N)cc12
null
[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
C1(=CC=CC=C1)C
C-C Coupling
Stille reaction_vinyl
b76d02284eab1606d02e43e8d6b217f827d8bc76b0b2203ccf942abed5fcc5b2
ec03c739f58696d2a3659a73884744e1a490a20a587da6f115be382b663cf23d
c1ccc2ncccc2c1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5](:[c:6]):[c:7]:1:[c:8].C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-C-C)-[CH;D2;+0:9]=[C;D1;H2:10]>>[C;D1;H2:10]=[CH;D2;+0:9]-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a:4]:[c:5](:[c:6]):[c:7]:1:[c:8]
64.5
[{"value": 64.0, "product": "C(=C)C1=CC=NC2=CC=C(C=C12)C#N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.5, "product": "C(=C)C1=CC=NC2=CC=C(C=C12)C#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of (c) (1 g, 4.3 mmol) and vinyltributyltin (1.5 mL, 5.17 mmol) in degassed toluene (20 ml) was added tetrakis(triphenylphosphine) palladium (0) (245 mg, 5 mol %) and the mixture was refluxed under argon for 2 hours. Evaporation and flash silica chromatography eluting with chloroform afforded the product ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Vinyl.Tin
Vinyl
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HBr.Sn
[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)C
null
null
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.N#Cc1ccc2nccc(Br)c2c1>[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)C>C=Cc1ccnc2ccc(C#N)cc12
ord_dataset-c31cb9b44c404c10ba3aa533aa079e2b
ord-281727cb74e9404f8ec80ef3f0e73d68
C=Cc1ccnc2ccc(C#N)cc12.CC(C)(C)OC(=O)NC1CCNCC1>>CC(C)(C)OC(=O)NC1CCN(CCc2ccnc3ccc(C#N)cc23)CC1
C(=C)C1=CC=NC2=CC=C(C=C12)C#N.C(C)(C)(C)OC(NC1CCNCC1)=O>>C(C)(C)(C)OC(NC1CCN(CC1)CCC1=CC=NC2=CC=C(C=C12)C#N)=O
[CH2:13]=[CH:14][c:15]1[cH:16][cH:17][n:18][c:19]2[cH:20][cH:21][c:22]([C:23]#[N:24])[cH:25][c:26]12.[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH:9]1[CH2:10][CH2:11][NH:12][CH2:27][CH2:28]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH:9]1[CH2:10][CH2:11][N:12]([CH2:13][CH2:14][c:15]2[cH:16][c...
C=Cc1ccnc2ccc(C#N)cc12.CC(C)(C)OC(=O)NC1CCNCC1
CC(C)(C)OC(=O)NC1CCN(CCc2ccnc3ccc(C#N)cc23)CC1
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
aza-Michael addition secondary
d3e8cc768c824777b70742851768dcb27bf5f461c310912ac3f5a7abd08f6975
828fcbb87adfef9f22c9a1e52b43c3df76cb2e49bfe62b57e8b79965772a2bed
c1ccc2c(CCN3CCCCC3)ccnc2c1
[CH2;D1;+0:1]=[CH;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[#7;a:6]:[c:7]:[c:8]:1.[C:9]-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13]>>[C:9]-[C:10]-[N;H0;D3;+0:11](-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[#7;a:6]:[c:7]:[c:8]:1)-[C:12]-[C:13]
99.9
[{"value": 96.0, "product": "C(C)(C)(C)OC(NC1CCN(CC1)CCC1=CC=NC2=CC=C(C=C12)C#N)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.9, "product": "C(C)(C)(C)OC(NC1CCN(CC1)CCC1=CC=NC2=CC=C(C=C12)C#N)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
A mixture of (d) (150 mg, 0.8 mmol), piperidin-4-yl-carbamic acid tert-butyl ester (166 mg, 0.8 mmol) and chloroform (0.5 ml) were heated at 50° C. in a loosely capped vial for 6 hours. The product was purified by flash silica chromatography eluting with a 0-2% methanol in chloroform gradient affording the product as a...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Vinyl
Tertiary amine
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccc2ncccc2c1
null
C(Cl)(Cl)Cl
50
null
C=Cc1ccnc2ccc(C#N)cc12.CC(C)(C)OC(=O)NC1CCNCC1>C(Cl)(Cl)Cl>CC(C)(C)OC(=O)NC1CCN(CCc2ccnc3ccc(C#N)cc23)CC1