dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d90b8545ce624e38851dac4a9f3f4f7e
C=C(Cl)C#N.CC(=O)N[C@@H]1CCC[C@H]1[Hg][Cl]>>CC(=O)N[C@@H]1CCC[C@H]1CC(Cl)C#N
C(C)(=O)N[C@H]1[C@@H](CCC1)[Hg]Cl.ClC(C#N)=C.[BH4-].[Na+]>>C(C)(=O)N[C@H]1[C@@H](CCC1)CC(C#N)Cl
[CH2:10]=[C:11]([Cl:12])[C:13]#[N:14].[Cl][Hg][C@H:9]1[C@H:5]([NH:4][C:2]([CH3:1])=[O:3])[CH2:6][CH2:7][CH2:8]1>>[CH3:1][C:2](=[O:3])[NH:4][C@@H:5]1[CH2:6][CH2:7][CH2:8][C@H:9]1[CH2:10][CH:11]([Cl:12])[C:13]#[N:14]
C=C(Cl)C#N.CC(=O)N[C@@H]1CCC[C@H]1[Hg][Cl]
CC(=O)N[C@@H]1CCC[C@H]1CC(Cl)C#N
null
null
C(C)O
C-C Coupling
OtherReaction
813c883b37d223e954814d49496c21b60c618eb7559fd40099bdb9a8228830b8
6e201f253d299cba9dce11df416351b338d329a97929620e1451b17f0c1815ea
C1CCCC1
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5]1-[C:6]-[C:7]-[C:8]-[C@H;D3;+0:9]-1-[Hg]-[Cl].[CH2;D1;+0:10]=[C;H0;D3;+0:11](-[Cl;D1;H0:12])-[C:13]#[N;D1;H0:14]>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5]1-[C:6]-[C:7]-[C:8]-[C@H;D3;+0:9]-1-[CH2;D2;+0:10]-[CH;D3;+0:11](-[Cl;D1;H0:12])-[C:13]#[N;D1;H0:14]
null
[]
null
null
1
HOUR
16.1 g of trans-1-acetamido-2-chloromercuriocyclopentane are suspended in 200 ml of ethanol. 10.7 ml of 2-chloroacrylonitrile are added, followed by 1.7 g of sodium borohydride in 40 ml of ethanol as rapidly as possible while cooling in ice. After 1 hour at room temperature, the mixture is filtered with suction through...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Vinyl
Secondary halide
C1CCCC1
C1CCCC1
C1CCCC1
Other
C(C)O
null
1
C=C(Cl)C#N.CC(=O)N[C@@H]1CCC[C@H]1[Hg][Cl]>C(C)O>CC(=O)N[C@@H]1CCC[C@H]1CC(Cl)C#N
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-97229f5d221e4003a7da36fedb95fb89
BrCCCc1ccccc1.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1>>COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCc1ccccc1
C1COCCOCCOCCOCCOCCO1.COC=1NC(=C(C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C.C([O-])([O-])=O.[K+].[K+].C1(=CC=CC=C1)CCCBr>>COC=1N(C(C(=C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C)CCCC1=CC=CC=C1
Br[CH2:25][CH2:26][CH2:27][c:28]1[cH:29][cH:30][cH:31][cH:32][cH:33]1.[CH3:1][O:2][C:3]1=[N:4][CH:5]([c:6]2[cH:7][cH:8][cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14]2)[C:15]([C:16](=[O:17])[O:18][CH:19]([CH3:20])[CH3:21])=[C:22]([CH3:23])[NH:24]1>>[CH3:1][O:2][C:3]1=[N:4][C:5]([c:6]2[cH:7][cH:8][cH:9][c:10]([N+:11](=[O:1...
BrCCCc1ccccc1.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1
COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCc1ccccc1
null
null
CCOCC.CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
69bd184bd50d5f8030cbcd013a55654dd34a76502f9c7e73150d5666f6af2c6d
79f91905cac93931d90e647e5870a720684802114bcbb1f1276120120f789420
C1=NC(c2ccccc2)=CCN1CCCc1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]-[C:5]1=[#7:6]-[CH;D3;+0:7](-[c:8](:[c:9]):[c:10])-[C;H0;D3;+0:11](-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15])=[C;H0;D3;+0:16](-[C;D1;H3:17])-[NH;D2;+0:18]-1>>[#8:4]-[C:5]1=[#7:6]-[C;H0;D3;+0:7](-[c:8](:[c:9]):[c:10])=[C;H0;D3;+0:11](-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15])-[CH;D3;+0:16](-[C...
60.7
[{"value": 60.7, "product": "COC=1N(C(C(=C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C)CCCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
72
HOUR
A solution of 1,4-dihydro-2-methoxy-6-methyl-4-(3-nitrophenyl)-5-pyrimidinecarboxylic acid, 1-methylethyl ester (4.0 g, 12.0 mmol) in dry dimethylformamide (10 ml) under argon was treated with finely ground potassium carbonate (4.97 g, 36.0 mmoles), 3-phenylpropyl bromide (2.19 ml, 14.4 mmoles) and a catalytic amount o...
10.6084/m9.figshare.5104873.v1
null
Enamine.Primary halide.Ester
Ester.Tertiary amine
C1=CNC=NC1
C1=CN=C[NH]C1
C1=CN=C[NH]C1.c1ccccc1.c1ccccc1
HBr
CCOCC.CN(C=O)C
null
72
BrCCCc1ccccc1.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1>CCOCC.CN(C=O)C>COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCc1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-4b02aacf4a8944cd8a856d38eed02d31
COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCc1ccccc1>>CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)N(CCCc2ccccc2)C(=O)N1
COC=1N(C(C(=C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C)CCCC1=CC=CC=C1.Cl>>CC1=C(C(N(C(N1)=O)CCCC1=CC=CC=C1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C
C[O:31][C:30]1=[N:32][C:10]([c:11]2[cH:12][cH:13][cH:14][c:15]([N+:16](=[O:17])[O-:18])[cH:19]2)=[C:3]([C:4](=[O:5])[O:6][CH:7]([CH3:8])[CH3:9])[CH:2]([CH3:1])[N:20]1[CH2:21][CH2:22][CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1>>[CH3:1][C:2]1=[C:3]([C:4](=[O:5])[O:6][CH:7]([CH3:8])[CH3:9])[CH:10]([c:11]2[cH:12][c...
COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCc1ccccc1
CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)N(CCCc2ccccc2)C(=O)N1
null
null
CO
Miscellaneous
OtherReaction
d538af1adbc15be2de60ad1e905730d779fc523cf32febd61d9d4602374832b0
fd1bed75df609a723368d936508c74e6b719ae806e80d6fe44cafd400786f4c4
O=C1NC=CC(c2ccccc2)N1CCCc1ccccc1
C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2]1=[N;H0;D2;+0:3]-[C;H0;D3;+0:4](-[c:5](:[c:6]):[c:7])=[C;H0;D3;+0:8](-[C:9](=[O;D1;H0:10])-[#8:11]-[C:12])-[CH;D3;+0:13](-[C;D1;H3:14])-[N;H0;D3;+0:15]-1-[C:16]-[C:17]>>[C:17]-[C:16]-[N;H0;D3;+0:15]1-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[NH;D2;+0:3]-[C;H0;D3;+0:13](-[C;D1;H3:14])=[C;H0;D3;+0:8...
169.6
[{"value": 169.6, "product": "CC1=C(C(N(C(N1)=O)CCCC1=CC=CC=C1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of 1,6-dihydro-2-methoxy-6-methyl-4-(3-nitrophenyl)-1-(3-phenylpropyl)-5-pyrimidinecarboxylic acid, 1-methylethyl ester (1.96 g. 4.34 mmoles) in methanol (20 ml) was treated with 2.5 N hydrochloric acid (5 ml) and the resulting mixture was allowed to stir at room temperature overnight. A colorless solid prec...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Tertiary amine
Enamine.Ester.Urea
C1=CN=C[NH]C1
C1=CNC[NH]C1
C1=CNC[NH]C1.c1ccccc1.c1ccccc1
Other
CO
null
8
COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCc1ccccc1>CO>CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)N(CCCc2ccccc2)C(=O)N1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-149ebce89605495e8a96c6b0c1e5b343
C=CCBr.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1>>C=CCN1C(OC)=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C1C
COC=1NC(=C(C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C.C([O-])([O-])=O.[K+].[K+].C(C=C)Br>>COC=1N(C(C(=C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C)CC=C
Br[CH2:3][CH:2]=[CH2:1].[NH:4]1[C:5]([O:6][CH3:7])=[N:8][CH:9]([c:10]2[cH:11][cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])[cH:18]2)[C:19]([C:20](=[O:21])[O:22][CH:23]([CH3:24])[CH3:25])=[C:26]1[CH3:27]>>[CH2:1]=[CH:2][CH2:3][N:4]1[C:5]([O:6][CH3:7])=[N:8][C:9]([c:10]2[cH:11][cH:12][cH:13][c:14]([N+:15](=[O:16])[O-:17])...
C=CCBr.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1
C=CCN1C(OC)=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C1C
null
null
CN(C=O)C.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
eead7f143e10bd3d3fa729cd1133dbc68f4a42e9e5f83d11674551b45e00250e
053e47696b6258b5976a7f5c88bd667d518c6a89339edb8d9a46e06a01e12534
C1=NC(c2ccccc2)=CCN1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[#8:4]-[C:5]1=[#7:6]-[CH;D3;+0:7](-[c:8](:[c:9]):[c:10])-[C;H0;D3;+0:11](-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15])=[C;H0;D3;+0:16](-[C;D1;H3:17])-[NH;D2;+0:18]-1>>[#8:4]-[C:5]1=[#7:6]-[C;H0;D3;+0:7](-[c:8](:[c:9]):[c:10])=[C;H0;D3;+0:11](-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15])-[CH;D3;+0:1...
58.9
[{"value": 58.9, "product": "COC=1N(C(C(=C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C)CC=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
HOUR
A solution of 1,4-dihydro-2-methoxy-6-methyl-4-(3-nitrophenyl)-5-pyrimidinecarboxylic acid, 1-methylethyl ester (4.0 g, 12.0 mmol; see Example 1A) in dry dimethylformamide (10 ml) was treated with finely ground potassium carbonate (6.6 g, 48.0 mmoles) and allyl bromide (1.7 ml, 20.0 mmole). The resulting suspension was...
10.6084/m9.figshare.5104873.v1
null
Enamine.Primary halide.Ester.Allyl
Ester.Tertiary amine.Allyl
C1=CNC=NC1
C1=CN=C[NH]C1
C1=CN=C[NH]C1.c1ccccc1
HBr
CN(C=O)C.C(C)(=O)OCC
null
10
C=CCBr.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1>CN(C=O)C.C(C)(=O)OCC>C=CCN1C(OC)=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C1C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-580a557c2ed64af0a505c01de0c132cc
CN(CCCCl)Cc1ccccc1.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1>>COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCN(C)Cc1ccccc1
C1COCCOCCOCCOCCOCCO1.COC=1NC(=C(C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C.C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)N(C)CCCCl>>COC=1N(C(C(=C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C)CCCN(CC1=CC=CC=C1)C
Cl[CH2:25][CH2:26][CH2:27][N:28]([CH3:29])[CH2:30][c:31]1[cH:32][cH:33][cH:34][cH:35][cH:36]1.[CH3:1][O:2][C:3]1=[N:4][CH:5]([c:6]2[cH:7][cH:8][cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14]2)[C:15]([C:16](=[O:17])[O:18][CH:19]([CH3:20])[CH3:21])=[C:22]([CH3:23])[NH:24]1>>[CH3:1][O:2][C:3]1=[N:4][C:5]([c:6]2[cH:7][cH:8][c...
CN(CCCCl)Cc1ccccc1.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1
COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCN(C)Cc1ccccc1
null
null
CCOCC.CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
69bd184bd50d5f8030cbcd013a55654dd34a76502f9c7e73150d5666f6af2c6d
79f91905cac93931d90e647e5870a720684802114bcbb1f1276120120f789420
C1=NC(c2ccccc2)=CCN1CCCNCc1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]-[C:5]1=[#7:6]-[CH;D3;+0:7](-[c:8](:[c:9]):[c:10])-[C;H0;D3;+0:11](-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15])=[C;H0;D3;+0:16](-[C;D1;H3:17])-[NH;D2;+0:18]-1>>[#8:4]-[C:5]1=[#7:6]-[C;H0;D3;+0:7](-[c:8](:[c:9]):[c:10])=[C;H0;D3;+0:11](-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15])-[CH;D3;+0:16](-[C...
50.9
[{"value": 50.9, "product": "COC=1N(C(C(=C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC(C)C)C)CCCN(CC1=CC=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 1,4-dihydro-2-methoxy-6-methyl-4-(3-nitrophenyl)-5-pyrimidinecarboxylic acid, 1-methyethyl ester (2.0 g, 6.0 mmol) in dimethylformamide (7.0 ml) was treated with finely ground potassium carbonate (1.7 g, 12.0 mmoles), N-benzyl-3-chloro-N-methylpropylamine (2.37 g, 12.0 mmol) and a catalytic amount of 18-c...
10.6084/m9.figshare.5104873.v1
null
Enamine.Primary halide.Ester
Ester.Tertiary amine
C1=CNC=NC1
C1=CN=C[NH]C1
C1=CN=C[NH]C1.c1ccccc1.c1ccccc1
HCl
CCOCC.CN(C=O)C
null
null
CN(CCCCl)Cc1ccccc1.COC1=NC(c2cccc([N+](=O)[O-])c2)C(C(=O)OC(C)C)=C(C)N1>CCOCC.CN(C=O)C>COC1=NC(c2cccc([N+](=O)[O-])c2)=C(C(=O)OC(C)C)C(C)N1CCCN(C)Cc1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f2cd4b96968d4d249dc0ff9ac8165438
COc1ccc(CCl)cc1.NC(N)=S>>COc1ccc(CSC(=N)N)cc1.Cl
NC(=S)N.COC1=CC=C(CCl)C=C1>>Cl.COC1=CC=C(CSC(N)=N)C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][Cl:14])[cH:12][cH:13]1.[S:8]=[C:9]([NH2:10])[NH2:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][S:8][C:9](=[NH:10])[NH2:11])[cH:12][cH:13]1.[ClH:14]
COc1ccc(CCl)cc1.NC(N)=S
COc1ccc(CSC(=N)N)cc1.Cl
null
null
O1CCCC1.CCOCC
Protection
OtherReaction
dae623ec10e42086cc0292009bc19d7d58877ce2428714b92cfbbb5102c39de2
f72dba6c0cce6a796ff9aeda8637cc446706f96a34b889e05557c4a922c09746
c1ccccc1
[Cl;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5].[N;D1;H2:6]-[C;H0;D3;+0:7](-[NH2;D1;+0:8])=[S;H0;D1;+0:9]>>[ClH;D0;+0:1].[N;D1;H2:6]-[C;H0;D3;+0:7](=[NH;D1;+0:8])-[S;H0;D2;+0:9]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
93.8
[{"value": 93.8, "product": "Cl.COC1=CC=C(CSC(N)=N)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
2
HOUR
A suspension of thiourea (38 g, 50.0 mmole) in dry tetrahydrofuran (40 ml) was cooled to 0° C. under argon and was treated dropwise with 4-methoxybenzylchloride (8.0 g, 50.0 mmole). After the addition was completed, the cooling bath was removed and the reaction was allowed to stir at room temperature for 2 hours. It wa...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Monosulfide
null
null
c1ccccc1
null
O1CCCC1.CCOCC
0
2
COc1ccc(CCl)cc1.NC(N)=S>O1CCCC1.CCOCC>COc1ccc(CSC(=N)N)cc1.Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d76b34220cb74d5c9ef8c5b1ac5cef9c
C=CCBr.COC(=O)C1=C(C)NC(SCc2ccc(OC)cc2)=NC1c1cccc([N+](=O)[O-])c1>>C=CCN1C(SCc2ccc(OC)cc2)=NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1
[H-].[Na+].COC1=CC=C(C=C1)CSC=1NC(=C(C(N1)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC)C.C(C=C)Br>>COC1=CC=C(C=C1)CSC=1N(C(C(=C(N1)C)C(=O)OC)C1=CC(=CC=C1)[N+](=O)[O-])CC=C
Br[CH2:3][CH:2]=[CH2:1].[N:4]1=[C:5]([S:6][CH2:7][c:8]2[cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14][cH:15]2)[NH:16][C:17]([CH3:18])=[C:19]([C:20](=[O:21])[O:22][CH3:23])[CH:24]1[c:25]1[cH:26][cH:27][cH:28][c:29]([N+:30](=[O:31])[O-:32])[cH:33]1>>[CH2:1]=[CH:2][CH2:3][N:4]1[C:5]([S:6][CH2:7][c:8]2[cH:9][cH:10][c:11]([O:12...
C=CCBr.COC(=O)C1=C(C)NC(SCc2ccc(OC)cc2)=NC1c1cccc([N+](=O)[O-])c1
C=CCN1C(SCc2ccc(OC)cc2)=NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
f03f094e921b267e82057738c56ab464b4b57b7d8df30d00ca3f068584045edc
420901d0309b6d43f9fb54f735a3fdb3c597eba34e73c20212594aadd4810bda
C1=CC(c2ccccc2)NC(SCc2ccccc2)=N1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[#8:4]-[C:5](=[O;D1;H0:6])-[C:7]1=[C:8](-[C;D1;H3:9])-[NH;D2;+0:10]-[C;H0;D3;+0:11](-[#16:12]-[C:13])=[N;H0;D2;+0:14]-[C:15]-1-[c:16]>>[#8:4]-[C:5](=[O;D1;H0:6])-[C:7]1=[C:8](-[C;D1;H3:9])-[N;H0;D2;+0:10]=[C;H0;D3;+0:11](-[#16:12]-[C:13])-[N;H0;D3;+0:14](-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:...
null
[]
null
null
10
MINUTE
A slurry of sodium hydride (168 mg, 4.2 mmole, 60% in mineral oil dispersion) in 5 ml of dry tetrahydrofuran at 0° C. under argon was treated dropwise with 1,4-dihydro-2-[[(4-methoxyphenyl)methyl]thio]-6-methyl-4-(3-nitrophenyl)-5-pyrimidinecarboxylic acid, methyl ester in 15 ml of dry tetrahydrofuran. After an additio...
10.6084/m9.figshare.5104873.v1
null
Enamine.Primary halide.Monosulfide.Allyl
Tertiary amine.Monosulfide.Allyl
C1=CNC=NC1
C1=CN=C[NH]C1
C1=CN=C[NH]C1.c1ccccc1.c1ccccc1
HBr
O1CCCC1
null
0.166667
C=CCBr.COC(=O)C1=C(C)NC(SCc2ccc(OC)cc2)=NC1c1cccc([N+](=O)[O-])c1>O1CCCC1>C=CCN1C(SCc2ccc(OC)cc2)=NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-ebc0f98a75d5489382dc12d3f1ffea4a
C=CCN1C(SCc2ccc(OC)cc2)=NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1>>C=CCN1C(=S)NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1
COC1=CC=C(C=C1)CSC=1N(C(C(=C(N1)C)C(=O)OC)C1=CC(=CC=C1)[N+](=O)[O-])CC=C.FC(C(=O)O)(F)F.C(C)S>>CC1=C(C(N(C(N1)=S)CC=C)C1=CC(=CC=C1)[N+](=O)[O-])C(=O)OC
COc1ccc(C[S:6][C:5]2=[N:7][C:8]([CH3:9])=[C:10]([C:11](=[O:12])[O:13][CH3:14])[CH:15]([c:16]3[cH:17][cH:18][cH:19][c:20]([N+:21](=[O:22])[O-:23])[cH:24]3)[N:4]2[CH2:3][CH:2]=[CH2:1])cc1>>[CH2:1]=[CH:2][CH2:3][N:4]1[C:5](=[S:6])[NH:7][C:8]([CH3:9])=[C:10]([C:11](=[O:12])[O:13][CH3:14])[CH:15]1[c:16]1[cH:17][cH:18][cH:19...
C=CCN1C(SCc2ccc(OC)cc2)=NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1
C=CCN1C(=S)NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1
null
null
ClCCl
Miscellaneous
OtherReaction
1981159823e39300360aee1006beb0d9a9f179e23d79282fd80a02bf8fef051f
4615674a4902b93d1abcb6db311cc613ae24f07687969fb173863070d67c3b66
S=C1NC=CC(c2ccccc2)N1
C-O-c1:c:c:c(-C-[S;H0;D2;+0:1]-[C;H0;D3;+0:2]2=[N;H0;D2;+0:3]-[C:4](-[C;D1;H3:5])=[C:6](-[C:7](-[#8:8])=[O;D1;H0:9])-[C:10]-[#7:11]-2-[C:12]-[C:13]=[C;D1;H2:14]):c:c:1>>[#8:8]-[C:7](=[O;D1;H0:9])-[C:6]1=[C:4](-[C;D1;H3:5])-[NH;D2;+0:3]-[C;H0;D3;+0:2](=[S;H0;D1;+0:1])-[#7:11](-[C:12]-[C:13]=[C;D1;H2:14])-[C:10]-1
null
[]
null
null
2
HOUR
1,6-Dihydro-2-[[(4-methoxyphenyl)methyl]thio]-4-methyl-6-(3-nitrophenyl)-1-(2-propenyl)-5-pyrimidinecarboxylic acid, methyl ester (1.0 g, 2.14 mmol) in 15 ml of dichloromethane under argon at room temperature was treated with trifluoroacetic acid (0.6 ml, 0.85 g, 7.7 mmole) and ethanethiol (0.4 ml, 0.33 g, 5.4 mmole). ...
10.6084/m9.figshare.5104873.v1
null
Ether.Monosulfide
Enamine.Thiourea
c1ccccc1.C1=CN=C[NH]C1
C1=CNC[NH]C1
C1=CNC[NH]C1.c1ccccc1
HO-
ClCCl
null
2
C=CCN1C(SCc2ccc(OC)cc2)=NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1>ClCCl>C=CCN1C(=S)NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f73f852b61ff4be4a5f6a8930b465af7
COC(=O)[C@@H](C)NC(=O)[C@@H]1CCCN1C(=O)C(C)CSC(C)=O>>CC(CS)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O
COC([C@H](NC([C@H]1N(CCC1)C(C(CSC(C)=O)C)=O)=O)C)=O.[OH-].[K+]>>SCC(C(=O)N1[C@H](C(=O)N[C@H](C)C(=O)O)CCC1)C
CC(=O)[S:4][CH2:3][CH:2]([CH3:1])[C:5](=[O:6])[N:7]1[CH2:8][CH2:9][CH2:10][C@H:11]1[C:12](=[O:13])[NH:14][C@H:15]([CH3:16])[C:17](=[O:18])[O:19]C>>[CH3:1][CH:2]([CH2:3][SH:4])[C:5](=[O:6])[N:7]1[CH2:8][CH2:9][CH2:10][C@H:11]1[C:12](=[O:13])[NH:14][C@H:15]([CH3:16])[C:17](=[O:18])[OH:19]
COC(=O)[C@@H](C)NC(=O)[C@@H]1CCCN1C(=O)C(C)CSC(C)=O
CC(CS)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O
null
null
null
Reduction
OtherReaction
1bcd8cbb2f136b4bcba1690e9ba45c4e43c89ba76f0e22de82a7d3fe318c82a9
5654c46fe4cb226f88ec3c899c7f9be1825c357673ea686958f9ef4883ee1db3
C1CCNC1
C-C(=O)-[S;H0;D2;+0:1]-[C:2]-[C:3]-[C:4](-[#7:5])=[O;D1;H0:6].C-[O;H0;D2;+0:7]-[C:8](-[C:9])=[O;D1;H0:10]>>[#7:5]-[C:4](=[O;D1;H0:6])-[C:3]-[C:2]-[SH;D1;+0:1].[C:9]-[C:8](=[O;D1;H0:10])-[OH;D1;+0:7]
62.7
[{"value": 62.7, "product": "SCC(C(=O)N1[C@H](C(=O)N[C@H](C)C(=O)O)CCC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
(S)-[3-(Acetylthio)-2-methyl 1-oxopropyl]-L-prolyl-D-alanine methyl ester (4 g) is taken into potassium hydroxide/aqueous methanol (3 g of potassium hydroxide in 14 ml of water and 70 ml of methanol) and the solution is kept at room temperature for 2 hours. The product (2.1 g) is isolated using the procedure described ...
10.6084/m9.figshare.5104873.v1
null
Ester.Carbo-thioester
Carboxylic acid.Aliphatic thiol
null
null
C1CC[NH]C1
HO-
null
null
2
COC(=O)[C@@H](C)NC(=O)[C@@H]1CCCN1C(=O)C(C)CSC(C)=O>>CC(CS)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-94d50d7044474d4f8c6033ec795dc15c
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CSC2>>Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2
N1=CC(=CC=C1)C1=CC(=C2N1CSC2)C(=O)O.CN(C=O)C.ClCCCl>>Cl.ClC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2
C(C[Cl:4])[Cl:1].O[C:3](=[O:2])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][S:17][CH2:18]2>>[ClH:1].[O:2]=[C:3]([Cl:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][S:17][CH2:18]2
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CSC2
Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2
null
null
C1CCCCC1.S(=O)(Cl)Cl
Functional Group Interconversion
Alcohol to chloride_Other
cf8f2baf4bb848035eb10b6a611e1a1957d0ca765a4605f66fc3dd62ac8bf212
d17829d7867afbdc103a0b2c7f35d7a0a76eb305fe44b655f945b9584718a72c
c1cncc(-c2ccc3n2CSC3)c1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2.[Cl;H0;D1;+0:11]-C-C-[Cl;H0;D1;+0:12]>>[Cl;H0;D1;+0:12]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2.[ClH;D0;+0:11]
null
[]
20
CELSIUS
30
MINUTE
A suspension of 5-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole-7-carboxylic acid (8.8 g) in a mixture of thionyl chloride (6.25 cc), dimethylformamide (0.05 cc) and 1,2dichloroethane (100 cc) is heated under reflux with stirring for 2 hours and 30 minutes. The reaction mixture is cooled to a temperature of about 20° C. and...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Carboxylic acid
Acyl halide
null
null
c1ccncc1.c1cc2n(c1)CSC2
HO-
C1CCCCC1.S(=O)(Cl)Cl
20
0.5
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CSC2>C1CCCCC1.S(=O)(Cl)Cl>Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-47cc5b7ec62c400e8d9aa5bf0052b74e
O=C(Cl)c1cccnc1.O=C(O)C1CSCN1>>O=C(O)C1CSCN1C(=O)c1cccnc1
Cl.C(C1=CN=CC=C1)(=O)Cl.S1CNC(C1)C(=O)O.C(C)N(CC)CC>>C(C1=CN=CC=C1)(=O)N1CSCC1C(=O)O
Cl[C:9](=[O:10])[c:11]1[cH:12][cH:13][cH:14][n:15][cH:16]1.[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][S:6][CH2:7][NH:8]1>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][S:6][CH2:7][N:8]1[C:9](=[O:10])[c:11]1[cH:12][cH:13][cH:14][n:15][cH:16]1
O=C(Cl)c1cccnc1.O=C(O)C1CSCN1
O=C(O)C1CSCN1C(=O)c1cccnc1
null
null
C(Cl)(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
54f36c76161a8ed9c718bf3b5609daa0d109fa9e172dfbee46708dc908b72e36
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1cccnc1)N1CCSC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[#7;a:6]:[c:7].[O;D1;H0:8]=[C:9](-[O;D1;H1:10])-[C:11]1-[C:12]-[#16:13]-[C:14]-[NH;D2;+0:15]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[N;H0;D3;+0:15]1-[C:14]-[#16:13]-[C:12]-[C:11]-1-[C:9](=[O;D1;H0:8])-[O;D1;H1:10])-[c:3](:[c:4]):[c:5]:[#7;a:6]:[c:7]
56.4
[{"value": 56.4, "product": "C(C1=CN=CC=C1)(=O)N1CSCC1C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
64
CELSIUS
16
HOUR
Nicotinoyl chloride hydrochloride (534 g) is added over 1 hour at a temperature of between 30° and 52° C. to a solution of thiazolidine-4-carboxylic acid (400 g) and triethylamine (613 g) in chloroform (4,500 cc). The solution obtained is heated at a temperature of about 64° C. for 4 hours. After stirring at a temperat...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
C1CSCN1
C1CSC[NH]1
C1CSC[NH]1.c1ccncc1
HCl
C(Cl)(Cl)Cl
64
16
O=C(Cl)c1cccnc1.O=C(O)C1CSCN1>C(Cl)(Cl)Cl>O=C(O)C1CSCN1C(=O)c1cccnc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-4a4238247c624393b3e38a48addec651
Nc1ccccc1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2>>O=C(Nc1ccccc1)c1cc(-c2cccnc2)n2c1CSC2
[OH-].[Na+].NC1=CC=CC=C1.Cl.ClC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2.C>>C1(=CC=CC=C1)NC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2
[NH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1.Cl[C:2](=[O:1])[c:10]1[cH:11][c:12](-[c:13]2[cH:14][cH:15][cH:16][n:17][cH:18]2)[n:19]2[c:20]1[CH2:21][S:22][CH2:23]2>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[c:10]1[cH:11][c:12](-[c:13]2[cH:14][cH:15][cH:16][n:17][cH:18]2)[n:19]2[c:20]1[CH2:21][S:22][CH2:23...
Nc1ccccc1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2
O=C(Nc1ccccc1)c1cc(-c2cccnc2)n2c1CSC2
null
null
C(C)#N.C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(Nc1ccccc1)c1cc(-c2cccnc2)n2c1CSC2
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2.[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2
57.8
[{"value": 57.8, "product": "C1(=CC=CC=C1)NC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
A solution of aniline (11.2 g) in methylene chloride (50 cc) is added over 15 minutes at a temperature of about 24° C. and 29° C. to a suspension of 7-chloroformyl-5-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole hydrochloride (12 g) in methylene chloride (200 cc). The suspension obtained is stirred at a temperature of about...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccncc1.c1cc2n(c1)CSC2
HCl
C(C)#N.C(Cl)Cl
20
16
Nc1ccccc1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2>C(C)#N.C(Cl)Cl>O=C(Nc1ccccc1)c1cc(-c2cccnc2)n2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2dfe2c76b5b841aea8d11b048080f5c7
N#Cc1cc(-c2cccnc2)n2c1CSC2.[OH-]>>NC(=O)c1cc(-c2cccnc2)n2c1CSC2
C(C)O.C.N1=CC(=CC=C1)C1=CC(=C2N1CSC2)C#N.[OH-].[K+]>>N1=CC(=CC=C1)C1=CC(=C2N1CSC2)C(=O)N
[N:1]#[C:2][c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11][cH:12]2)[n:13]2[c:14]1[CH2:15][S:16][CH2:17]2.[OH-:3]>>[NH2:1][C:2](=[O:3])[c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11][cH:12]2)[n:13]2[c:14]1[CH2:15][S:16][CH2:17]2
N#Cc1cc(-c2cccnc2)n2c1CSC2.[OH-]
NC(=O)c1cc(-c2cccnc2)n2c1CSC2
null
null
C(C)(C)(C)O
Heteroatom Alkylation and Arylation
OtherReaction
1d1793919e847ed86dcb16487e62464531560dbf4782f9a5875bfe7e0477a3ec
d6f9d146e8ef95e62f1a3ab55a7e3b4ceec8856a5f71b6dccd4ad850f945b658
c1cncc(-c2ccc3n2CSC3)c1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2.[OH-;D0:11]>>[NH2;D1;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:11])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2
null
[]
20
CELSIUS
16
HOUR
A suspension of 5-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole-7-carbonitrile (11.35 g) and of potassium hydroxide powder (14 g) in tert-butyl alcohol (100 cc) is heated at 85° C. for 1 hour. After 16 hours' stirring at a temperature of about 20° C., the reaction mixture is poured into distilled water (2 liters). The suspe...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amide
null
null
c1ccncc1.c1cc2n(c1)CSC2
null
C(C)(C)(C)O
20
16
N#Cc1cc(-c2cccnc2)n2c1CSC2.[OH-]>C(C)(C)(C)O>NC(=O)c1cc(-c2cccnc2)n2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b36442ef1e0e427da9188dd8ef7623f7
CN.O=C(Cl)c1cc(-c2cccnc2)n2c1CCC2>>CNC(=O)c1cc(-c2cccnc2)n2c1CCC2
C.CN.Cl.ClC(=O)C=1C=C(N2CCCC12)C=1C=NC=CC1.C(C)#N>>CNC(=O)C=1C=C(N2CCCC12)C=1C=NC=CC1
[CH3:1][NH2:2].Cl[C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][CH2:17][CH2:18]2>>[CH3:1][NH:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][CH2:17][CH2:18]2
CN.O=C(Cl)c1cc(-c2cccnc2)n2c1CCC2
CNC(=O)c1cc(-c2cccnc2)n2c1CCC2
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1cncc(-c2ccc3n2CCC3)c1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6](:[c:7]:1-[C:8])-[C:9].[C;D1;H3:10]-[NH2;D1;+0:11]>>[C:8]-[c:7]1:[#7;a:6](:[c:5]:[c:4]:[c:3]:1-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:11]-[C;D1;H3:10])-[C:9]
null
[]
20
CELSIUS
7
HOUR
A suspension of 7-chloroformyl-5-(3-pyridyl)-2,3-dihydro-1H-pyrrolizine hydrochloride (14.1 g) in methylene chloride (250 cc) is saturated with a stream of anhydrous methylamine, while the temperature of the reaction mixture is kept at about 25° C. for 7 hours. The solution obtained is stirred at a temperature of about...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1.c1cc2n(c1)CCC2
HCl
C(Cl)Cl
20
7
CN.O=C(Cl)c1cc(-c2cccnc2)n2c1CCC2>C(Cl)Cl>CNC(=O)c1cc(-c2cccnc2)n2c1CCC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a0e2495416b24776b0ff2e14038ce5c9
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CCC2>>Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CCC2
N1=CC(=CC=C1)C=1N2CCCC2=C(C1)C(=O)O.CN(C=O)C.ClCCCl>>Cl.ClC(=O)C=1C=C(N2CCCC12)C=1C=NC=CC1
C(C[Cl:4])[Cl:1].O[C:3](=[O:2])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][CH2:17][CH2:18]2>>[ClH:1].[O:2]=[C:3]([Cl:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][CH2:17][CH2:18]2
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CCC2
Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CCC2
null
null
C1CCCCC1.S(=O)(Cl)Cl
Functional Group Interconversion
Alcohol to chloride_Other
cf8f2baf4bb848035eb10b6a611e1a1957d0ca765a4605f66fc3dd62ac8bf212
d17829d7867afbdc103a0b2c7f35d7a0a76eb305fe44b655f945b9584718a72c
c1cncc(-c2ccc3n2CCC3)c1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6](:[c:7]:1-[C:8])-[C:9].[Cl;H0;D1;+0:10]-C-C-[Cl;H0;D1;+0:11]>>[C:8]-[c:7]1:[#7;a:6](:[c:5]:[c:4]:[c:3]:1-[C;H0;D3;+0:1](-[Cl;H0;D1;+0:11])=[O;D1;H0:2])-[C:9].[ClH;D0;+0:10]
null
[]
80
CELSIUS
null
null
A suspension of 5-(3-pyridyl)-2,3-dihydro-1H-pyrrolizine-7-carboxylic acid (11.4 g) in a mixture of thionyl chloride (17.4 cc), dimethylformamide (0.05 cc) and 1,2-dichloroethane (150 cc) is heated at a temperature of about 80° C. for 3 hours. The reaction mixture is cooled to a temperature of about 20° C. and concentr...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Carboxylic acid
Acyl halide
null
null
c1ccncc1.c1cc2n(c1)CCC2
HO-
C1CCCCC1.S(=O)(Cl)Cl
80
null
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CCC2>C1CCCCC1.S(=O)(Cl)Cl>Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CCC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-98c4e0936fd54c8bbb7ca27429d6edc9
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CCCC2>>Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CCCC2
N1=CC(=CC=C1)C1=CC(=C2CCCCN12)C(=O)O.CN(C=O)C.ClCCCl>>Cl.ClC(=O)C=1C=C(N2CCCCC12)C=1C=NC=CC1
C(C[Cl:4])[Cl:1].O[C:3](=[O:2])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][CH2:17][CH2:18][CH2:19]2>>[ClH:1].[O:2]=[C:3]([Cl:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][n:12][cH:13]2)[n:14]2[c:15]1[CH2:16][CH2:17][CH2:18][CH2:19]2
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CCCC2
Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CCCC2
null
null
S(=O)(Cl)Cl
Functional Group Interconversion
Alcohol to chloride_Other
cf8f2baf4bb848035eb10b6a611e1a1957d0ca765a4605f66fc3dd62ac8bf212
d17829d7867afbdc103a0b2c7f35d7a0a76eb305fe44b655f945b9584718a72c
c1cncc(-c2ccc3n2CCCC3)c1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6](:[c:7]:1-[C:8])-[C:9].[Cl;H0;D1;+0:10]-C-C-[Cl;H0;D1;+0:11]>>[C:8]-[c:7]1:[#7;a:6](:[c:5]:[c:4]:[c:3]:1-[C;H0;D3;+0:1](-[Cl;H0;D1;+0:11])=[O;D1;H0:2])-[C:9].[ClH;D0;+0:10]
null
[]
70
CELSIUS
3
HOUR
A solution of 3-(3-pyridyl)-5,6,7,8-tetrahydroindolizine-1-carboxylic acid (13.3 g) in a mixture of thionyl chloride (19.2 cc), dimethylformamide (0.05 cc) and 1,2-dichloroethane (160 cc) is heated to a temperature of about 70° C. The suspension obtained is kept at a temperature of about 70° C. for 3 hours. The reactio...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Carboxylic acid
Acyl halide
null
null
c1ccncc1.c1cc2n(c1)CCCC2
HO-
S(=O)(Cl)Cl
70
3
ClCCCl.O=C(O)c1cc(-c2cccnc2)n2c1CCCC2>S(=O)(Cl)Cl>Cl.O=C(Cl)c1cc(-c2cccnc2)n2c1CCCC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f11982bfa30746859d2d86d97b005c43
N#Cc1cc(-c2cccnc2)n2c1CCCC2.OCCO.[OH-]>>O=C(O)c1cc(-c2cccnc2)n2c1CCCC2
N1=CC(=CC=C1)C1=CC(=C2CCCCN12)C#N.[OH-].[K+].C(CO)O.C>>N1=CC(=CC=C1)C1=CC(=C2CCCCN12)C(=O)O
N#[C:2][c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11][cH:12]2)[n:13]2[c:14]1[CH2:15][CH2:16][CH2:17][CH2:18]2.OCC[OH:1].[OH-:3]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11][cH:12]2)[n:13]2[c:14]1[CH2:15][CH2:16][CH2:17][CH2:18]2
N#Cc1cc(-c2cccnc2)n2c1CCCC2.OCCO.[OH-]
O=C(O)c1cc(-c2cccnc2)n2c1CCCC2
null
null
O
Acylation
OtherReaction
5e76f9eb1645dffa65f7e1b9c084dfced9f3cb65f8b76df935c174c7208ba236
3746af5ef2d46561e999a498fd7e2fe230c1b687b933f9146ccf2b5206980b7a
c1cncc(-c2ccc3n2CCCC3)c1
N#[C;H0;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5](:[c:6]:1-[C:7])-[C:8].O-C-C-[OH;D1;+0:9].[OH-;D0:10]>>[C:7]-[c:6]1:[#7;a:5](:[c:4]:[c:3]:[c:2]:1-[C;H0;D3;+0:1](=[O;H0;D1;+0:9])-[OH;D1;+0:10])-[C:8]
null
[]
20
CELSIUS
16
HOUR
A solution of 3-(3-pyridyl)-5,6,7,8-tetrahydroindolizine-1-carbonitrile (15.6 g) and of potassium hydroxide powder (15.8 g) in ethylene glycol (150 cc) is heated at a temperature of about 156° C. for 11 hours and 30 minutes. After 16 hours' stirring at a temperature of about 20° C., the solvent is evaporated off under ...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary alcohol.Primary alcohol
Carboxylic acid
null
null
c1ccncc1.c1cc2n(c1)CCCC2
HO-
O
20
16
N#Cc1cc(-c2cccnc2)n2c1CCCC2.OCCO.[OH-]>O>O=C(O)c1cc(-c2cccnc2)n2c1CCCC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-be1d7015fa194ec1aee8172435d3fa3c
NCc1cccnc1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2>>O=C(NCc1cccnc1)c1cc(-c2cccnc2)n2c1CSC2
C.NCC=1C=NC=CC1.C(C)N(CC)CC.Cl.ClC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2>>N1=CC(=CC=C1)CNC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2
[NH2:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][n:9][cH:10]1.Cl[C:2](=[O:1])[c:11]1[cH:12][c:13](-[c:14]2[cH:15][cH:16][cH:17][n:18][cH:19]2)[n:20]2[c:21]1[CH2:22][S:23][CH2:24]2>>[O:1]=[C:2]([NH:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][n:9][cH:10]1)[c:11]1[cH:12][c:13](-[c:14]2[cH:15][cH:16][cH:17][n:18][cH:19]2)[n:20]2[c:21]1[CH2:22...
NCc1cccnc1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2
O=C(NCc1cccnc1)c1cc(-c2cccnc2)n2c1CSC2
null
null
C(CCC)O.C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCc1cccnc1)c1cc(-c2cccnc2)n2c1CSC2
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2.[#7;a:11]:[c:12]:[c:13]-[C:14]-[NH2;D1;+0:15]>>[#7;a:11]:[c:12]:[c:13]-[C:14]-[NH;D2;+0:15]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2
59.1
[{"value": 59.1, "product": "N1=CC(=CC=C1)CNC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
A solution of 3-aminomethylpyridine (5.5 g) and of triethylamine (10.1 g) in methylene chloride (100 cc) is added over 15 minutes at a temperature between 20° and 30° C. to a suspension of 7-chloroformyl-5-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole hydrochloride (15 g) in methylene chloride (250 cc). The solution obtaine...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1.c1ccncc1.c1cc2n(c1)CSC2
HCl
C(CCC)O.C(Cl)Cl
20
16
NCc1cccnc1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2>C(CCC)O.C(Cl)Cl>O=C(NCc1cccnc1)c1cc(-c2cccnc2)n2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-e9a3504efdb64c92b1aeea28125c9957
O=Cc1cc(-c2cccnc2)n2c1CSC2.[C-]#[N+]CS(=O)(=O)c1ccc(C)cc1>>N#CCc1cc(-c2cccnc2)n2c1CSC2
CO.S(=O)(=O)(C1=CC=C(C)C=C1)C[N+]#[C-].CC(C)(C)[O-].[K+].N1=CC(=CC=C1)C1=CC(=C2N1CSC2)C=O>>N1=CC(=CC=C1)C1=CC(=C2N1CSC2)CC#N
O=[CH:3][c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11][cH:12]2)[n:13]2[c:14]1[CH2:15][S:16][CH2:17]2.Cc1ccc(S(=O)(=O)C[N+:1]#[C-:2])cc1>>[N:1]#[C:2][CH2:3][c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][n:11][cH:12]2)[n:13]2[c:14]1[CH2:15][S:16][CH2:17]2
O=Cc1cc(-c2cccnc2)n2c1CSC2.[C-]#[N+]CS(=O)(=O)c1ccc(C)cc1
N#CCc1cc(-c2cccnc2)n2c1CSC2
null
null
COCCOC
C-C Coupling
OtherReaction
10f9d324cff21cc4d37a63bdf9fbfabb9ad49e9f3f28051ff2b53b0cda5d1082
df3040bf3b8362a80f3d2edcc476b7684492c85dbd12b1ba9c2d3dbd94a9c0d7
c1cncc(-c2ccc3n2CSC3)c1
C-c1:c:c:c(-S(=O)(=O)-C-[N+;H0;D2:1]#[C-;H0;D1:2]):c:c:1.O=[CH;D2;+0:3]-[c:4]1:[c:5]:[c:6]:[#7;a:7]2:[c:8]:1-[C:9]-[#16:10]-[C:11]-2>>[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[CH2;D2;+0:3]-[c:4]1:[c:5]:[c:6]:[#7;a:7]2:[c:8]:1-[C:9]-[#16:10]-[C:11]-2
71.6
[{"value": 71.6, "product": "N1=CC(=CC=C1)C1=CC(=C2N1CSC2)CC#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-30
CELSIUS
1
HOUR
A solution of tosylmethyl isocyanide (7.5 g) in 1,2-dimethoxyethane (50 cc) is added over 20 minutes at a temperature of about -30° C. to a solution of potassium tert-butylate (8.7 g) in 1,2-dimethoxyethane (140 cc) cooled to a temperature of about -30° C. The solution obtained is cooled to a temperature of about -60° ...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Aldehyde.Isocyanide
Nitrile
c1ccccc1
null
c1ccncc1.c1cc2n(c1)CSC2
TsOH.HO-
COCCOC
-30
1
O=Cc1cc(-c2cccnc2)n2c1CSC2.[C-]#[N+]CS(=O)(=O)c1ccc(C)cc1>COCCOC>N#CCc1cc(-c2cccnc2)n2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-824e7f9651f240e689a69529a68f3509
C=C(Cl)C#N.O=C(O)[C@@H]1CC(O)CN1C(=O)c1cccnc1>>N#Cc1cc(-c2cccnc2)n2c1CC(O)C2
[OH-].[Na+].ClC(C#N)=C.C(C1=CN=CC=C1)(=O)N1[C@H](C(=O)O)CC(C1)O.C(C)(=O)OC(C)=O.C(C)(C)O>>OC1CC2=C(C=C(N2C1)C=1C=NC=CC1)C#N
Cl[C:3]([C:2]#[N:1])=[CH2:4].O=C(O)[C@H:13]1[N:12]([C:5](=O)[c:6]2[cH:7][cH:8][cH:9][n:10][cH:11]2)[CH2:17][CH:15]([OH:16])[CH2:14]1>>[N:1]#[C:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][n:10][cH:11]2)[n:12]2[c:13]1[CH2:14][CH:15]([OH:16])[CH2:17]2
C=C(Cl)C#N.O=C(O)[C@@H]1CC(O)CN1C(=O)c1cccnc1
N#Cc1cc(-c2cccnc2)n2c1CC(O)C2
null
null
null
Aromatic Heterocycle Formation
OtherReaction
c95710789d1cdd89ba5f2ce9fde849f30b2083335c55d8155beab7505bfdcd26
8e1448c3647c7e9b55ba5077ceb62ca9e7c8e39a2901fbdd3aad031a0a841681
c1cncc(-c2ccc3n2CCC3)c1
Cl-[C;H0;D3;+0:1](=[CH2;D1;+0:2])-[C:3]#[N;D1;H0:4].O-C(=O)-[C@@H;D3;+0:5]1-[C:6]-[C:7]-[C:8]-[N;H0;D3;+0:9]-1-[C;H0;D3;+0:10](=O)-[c;H0;D3;+0:11]1:[c:12]:[#7;a:13]:[c:14]:[c:15]:[c:16]:1>>[N;D1;H0:4]#[C:3]-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[c;H0;D3;+0:10](-[c;H0;D3;+0:11]2:[c:12]:[#7;a:13]:[c:14]:[c:15]:[c:16]:2):[n;H0;D3;...
null
[]
20
CELSIUS
null
null
A suspension of N-nicotinoyl-4-hydroxyproline (34 g) in a mixture of 2-chloroacrylonitrile (115 cc) and of acetic anhydride (150 cc) is heated at a temperature of about 90° C. for 3 hours and 40 minutes. The solution obtained is concentrated to dryness under reduced pressure (20 mm Hg; 2.7 kPa) at a temperature of abou...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Carboxylic acid.Tertiary amide.Vinyl
null
C1CC[NH]C1
c1cc2n(c1)CCC2
c1ccncc1.c1cc2n(c1)CCC2
HCl
null
20
null
C=C(Cl)C#N.O=C(O)[C@@H]1CC(O)CN1C(=O)c1cccnc1>>N#Cc1cc(-c2cccnc2)n2c1CC(O)C2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a74cdf5f7cf24cd5b1c5653175416195
COc1cccc(N)c1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2>>COc1cccc(NC(=O)c2cc(-c3cccnc3)n3c2CSC3)c1
C.COC=1C=C(N)C=CC1.C(C)N(CC)CC.Cl.ClC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2>>COC=1C=C(C=CC1)NC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[cH:25]1.Cl[C:9](=[O:10])[c:11]1[cH:12][c:13](-[c:14]2[cH:15][cH:16][cH:17][n:18][cH:19]2)[n:20]2[c:21]1[CH2:22][S:23][CH2:24]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH:8][C:9](=[O:10])[c:11]2[cH:12][c:13](-[c:14]3[cH:15][cH:16][cH:17][n:18][cH:19]3)[n:20]3[c:21]2...
COc1cccc(N)c1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2
COc1cccc(NC(=O)c2cc(-c3cccnc3)n3c2CSC3)c1
null
null
C(CCC)O.C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(Nc1ccccc1)c1cc(-c2cccnc2)n2c1CSC2
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2.[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[c:3]1:[c:4]:[c:5]:[#7;a:6]2:[c:7]:1-[C:8]-[#16:9]-[C:10]-2
44.6
[{"value": 44.6, "product": "COC=1C=C(C=CC1)NC(=O)C=1C=C(N2CSCC21)C=2C=NC=CC2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
A solution of 3-methoxyaniline (3.1 g) and of triethylamine (5.1 g) in methylene chloride (50 cc) is added over 15 minutes at a temperature of between 21° and 28° C. to a suspension of 7-chloroformyl-5-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole hydrochloride (7.5 g) in methylene chloride (125 cc). The solution obtained i...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccncc1.c1cc2n(c1)CSC2
HCl
C(CCC)O.C(Cl)Cl
20
16
COc1cccc(N)c1.O=C(Cl)c1cc(-c2cccnc2)n2c1CSC2>C(CCC)O.C(Cl)Cl>COc1cccc(NC(=O)c2cc(-c3cccnc3)n3c2CSC3)c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-145a27aebfd74767a69e19e03a8c59f6
CCCCC(CC)CCl.COC(=O)c1ccc(O)cc1>>CCCCC(CC)COc1ccc(C(=O)OC)cc1
COC(C1=CC=C(C=C1)O)=O.C(C)C(CCl)CCCC.C[O-].[Na+]>>COC(C1=CC=C(C=C1)OCC(CCCC)CC)=O
Cl[CH2:8][CH:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH3:7].[OH:9][c:10]1[cH:11][cH:12][c:13]([C:14](=[O:15])[O:16][CH3:17])[cH:18][cH:19]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([CH2:6][CH3:7])[CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]([C:14](=[O:15])[O:16][CH3:17])[cH:18][cH:19]1
CCCCC(CC)CCl.COC(=O)c1ccc(O)cc1
CCCCC(CC)COc1ccc(C(=O)OC)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2](-[C:3])-[C:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C:3]-[C:2](-[C:4])-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
null
null
null
null
A mixture of 51.7 g (0.34 mol) of 4-hydroxybenzoic acid methylester, 500 ml of dimethyl formamide, 60 g (0.40 mol) of 2-ethylhexylchloride and 21.8 g (0.40 mol) of sodium methylate was heated for 7 hours to boiling temperature and, after cooling and removal of the sodium chloride by filtration, was evaporated to drynes...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1
HCl
CN(C=O)C
null
null
CCCCC(CC)CCl.COC(=O)c1ccc(O)cc1>CN(C=O)C>CCCCC(CC)COc1ccc(C(=O)OC)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b51e3c45dce24bd2a8edaa79ca6d4094
CCCCCCCCCCCCOCCCl.COC(=O)c1ccc(O)cc1>>CCCCCCCCCCCCOCCOc1ccc(C(=O)OC)cc1
COC(C1=CC=C(C=C1)O)=O.C(CCCCCCCCCCC)OCCCl.C[O-].[Na+]>>COC(C1=CC=C(C=C1)OCCOCCCCCCCCCCCC)=O
Cl[CH2:15][CH2:14][O:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[OH:16][c:17]1[cH:18][cH:19][c:20]([C:21](=[O:22])[O:23][CH3:24])[cH:25][cH:26]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][CH2:14][CH2:15][O:16][c:17]1[cH:...
CCCCCCCCCCCCOCCCl.COC(=O)c1ccc(O)cc1
CCCCCCCCCCCCOCCOc1ccc(C(=O)OC)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
A mixture of 20.4 g (0.134 mol) of 4-hydroxybenzoic acid methylester, 200 ml of dimethyl formamide, 40 g (0.160 mol) of 2-dodecyloxy ethylchloride (from 2-dodecyloxy ethanol and thionyl chloride) and 8.6 g (0.160 mol) of sodium methylate was heated for 7 hours to boiling temperature and, after cooling and removal of th...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1
HCl
CN(C=O)C
null
null
CCCCCCCCCCCCOCCCl.COC(=O)c1ccc(O)cc1>CN(C=O)C>CCCCCCCCCCCCOCCOc1ccc(C(=O)OC)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-042c2ac25241438a9cc4967aa8083194
CC(C)CCCCCCCCCCCl>>CC(C)CCCCCCCCCCO
COC(C1=CC=C(C=C1)O)=O.C(CCCCCCCCCC(C)C)Cl>>C(CCCCCCCCCC(C)C)O
Cl[CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH:2]([CH3:1])[CH3:3]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][OH:14]
CC(C)CCCCCCCCCCCl
CC(C)CCCCCCCCCCO
null
null
null
Functional Group Interconversion
Primary alkyl halide to alcohol
4c480ae19804ad5cf02c2cb44a1909d952eb2f0debe381a021a63e61ede789dc
05def2467bf3ab45f9f8ab94784b02043dfccd675fa03a71edc68bf348b4f536
null
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;D1;H1:4]
null
[]
null
null
null
null
This compound was prepared from 4-hydroxybenzoic acid methylester and isotridecylchloride, initially obtained from isotridecanol (an oxalcohol prepared from tetrapropylene) using known techniques. The product recovered exhibited a refractive index of Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide
Primary alcohol
null
null
null
null
null
null
null
CC(C)CCCCCCCCCCCl>>CC(C)CCCCCCCCCCO
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-9ae755645b74495cba90521e9eaebb2c
O=P([O-])([O-])O>>O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].[Ca+2].[Ca+2]
[N+](=O)([O-])[O-].[Ca+2].[N+](=O)([O-])[O-].P(=O)(O)([O-])[O-].[NH4+].[NH4+].N>>P(=O)([O-])([O-])[O-].[Ca+2].[Ca+2].[Ca+2].P(=O)([O-])([O-])[O-]
[O:1]=[P:2]([O-:3])([O-:4])[OH:5]>>[O:1]=[P:2]([O-:3])([O-:4])[O-:5].[O:6]=[P:7]([O-:8])([O-:9])[O-:10].[Ca+2:12].[Ca+2:13]
O=P([O-])([O-])O
O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].[Ca+2].[Ca+2]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[O;-;D1;H0:1]-[#15:2](-[O;-;D1;H0:3])(=[O;D1;H0:4])-[OH;D1;+0:5]>>[O-;H0;D1:5]-[#15:2](-[O;-;D1;H0:1])(-[O;-;D1;H0:3])=[O;D1;H0:4]
null
[]
null
null
null
null
The reaction of 3 l of 0.5 mol/l aqueous solution of calcium nitrate [Ca(NO3)2 ] with 2 l of 0.5 mol/l aqueous solution of ammonium hydrogen phosphate [(NH4)2HPO4 ] was carried out by mixing them under nitrogen gas stream at a temperature equal to or less than 5° C., while adjusting pH to 11 by the addition of aqueous ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
null
null
null
O=P([O-])([O-])O>>O=P([O-])([O-])[O-].O=P([O-])([O-])[O-].[Ca+2].[Ca+2]
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-80585d3d1f174a07a8ac26c8d81210d5
CCO.O=C(O)Cc1sc(F)c(N2C(=O)C3=C(CCCC3)C2=O)c1Cl>>CCOC(=O)Cc1sc(F)c(N2C(=O)C3=C(CCCC3)C2=O)c1Cl
O.ClC=1C(=C(SC1CC(=O)O)F)N1C(C=2CCCCC2C1=O)=O.C(C)O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>ClC=1C(=C(SC1CC(=O)OCC)F)N1C(C=2CCCCC2C1=O)=O
[CH3:1][CH2:2][OH:3].O[C:4](=[O:5])[CH2:6][c:7]1[s:8][c:9]([F:10])[c:11]([N:12]2[C:13](=[O:14])[C:15]3=[C:16]([CH2:17][CH2:18][CH2:19][CH2:20]3)[C:21]2=[O:22])[c:23]1[Cl:24]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][c:7]1[s:8][c:9]([F:10])[c:11]([N:12]2[C:13](=[O:14])[C:15]3=[C:16]([CH2:17][CH2:18][CH2:19][CH2:20]3)[C:2...
CCO.O=C(O)Cc1sc(F)c(N2C(=O)C3=C(CCCC3)C2=O)c1Cl
CCOC(=O)Cc1sc(F)c(N2C(=O)C3=C(CCCC3)C2=O)c1Cl
null
null
C1(=CC=CC=C1)C
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
O=C1C2=C(CCCC2)C(=O)N1c1ccsc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]:[#16;a:5].[C;D1;H3:6]-[C:7]-[OH;D1;+0:8]>>[#16;a:5]:[c:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:8]-[C:7]-[C;D1;H3:6]
null
[]
null
null
null
null
To a solution of 2-(4-chloro-2-fluoro-5-carboxymethylthiophenyl)-4,5,6,7-tetrahydro-2H-isoindole-1,3-dione (1.2 g) and ethanol (1.0 g) in toluene (20 ml), there was added a small amount of p-toluenesulfonic acid, and the mixture was refluxed for 3 hours. Water was added to the reaction mixture. The toluene layer was se...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccsc1.C1CCC2=C(C1)C[NH]C2
HO-
C1(=CC=CC=C1)C
null
null
CCO.O=C(O)Cc1sc(F)c(N2C(=O)C3=C(CCCC3)C2=O)c1Cl>C1(=CC=CC=C1)C>CCOC(=O)Cc1sc(F)c(N2C(=O)C3=C(CCCC3)C2=O)c1Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-66918d79d0a84c83a3cb9be01a6051a0
CC(=O)Nc1cc(CC(O)=S)c(Cl)cc1F>>Nc1cc(CC(O)=S)c(Cl)cc1F
C(C)(=O)NC=1C(=CC(=C(C1)CC(=S)O)Cl)F.Cl.[OH-].[Na+]>>NC=1C(=CC(=C(C1)CC(=S)O)Cl)F
CC(=O)[NH:1][c:2]1[cH:3][c:4]([CH2:5][C:6]([OH:7])=[S:8])[c:9]([Cl:10])[cH:11][c:12]1[F:13]>>[NH2:1][c:2]1[cH:3][c:4]([CH2:5][C:6]([OH:7])=[S:8])[c:9]([Cl:10])[cH:11][c:12]1[F:13]
CC(=O)Nc1cc(CC(O)=S)c(Cl)cc1F
Nc1cc(CC(O)=S)c(Cl)cc1F
null
null
null
Reduction
Hydrogenolysis of amides/imides/carbamates
755df58c254dea764fdda078ffd678ec540bba057c83683be04c253f1270ac7b
025f7cefe51e71668ad5d09fca32df168e9b538347403e4d5c1748073e538adc
c1ccccc1
C-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
73
[{"value": 73.0, "product": "NC=1C(=CC(=C(C1)CC(=S)O)Cl)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 5-(N-acetylamino)-2-chloro-4-fluorophenylthioacetic acid (89.8 g) in a 10% aqueous hydrochloric acid solution was refluxed for 2 hours under heating. After being allowed to cool, an aqueous solution of sodium hydroxide was added to make the suspension at pH 4. After ice-cooling, the precipitated crystal...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
Primary amine
null
null
c1ccccc1
HO-
null
null
null
CC(=O)Nc1cc(CC(O)=S)c(Cl)cc1F>>Nc1cc(CC(O)=S)c(Cl)cc1F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-314841d8e7144a3383cf73952ae86a5e
CC(=O)Nc1ccc(Cl)cc1F.O=[N+]([O-])O>>CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
[N+](=O)(O)[O-].S(O)(O)(=O)=O.C(C)(=O)NC1=C(C=C(C=C1)Cl)F>>C(C)(=O)NC1=CC(=C(C=C1F)Cl)[N+](=O)[O-]
[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:11]([Cl:12])[cH:13][c:14]1[F:15].O[N+:8](=[O:9])[O-:10]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]([N+:8](=[O:9])[O-:10])[c:11]([Cl:12])[cH:13][c:14]1[F:15]
CC(=O)Nc1ccc(Cl)cc1F.O=[N+]([O-])O
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[Cl;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[Cl;D1;H0:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
99.5
[{"value": 99.5, "product": "C(C)(=O)NC1=CC(=C(C=C1F)Cl)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a 20% ice-cooled fuming sulfuric acid (50 g), 4-(N-acetylamino)-1-chloro-3-fluorobenzene (9.4 g) was dissolved, followed by gradual addition of fuming nitric acid (3.5 g) while keeping the temperature at 0° to 5° C. The resultant mixture was stirred at the same temperature for 1 hour and poured into ice (50 g). The ...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
CC(=O)Nc1ccc(Cl)cc1F.O=[N+]([O-])O>>CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-c23a4513b82d45e09e99a39aac139faa
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F>>CC(=O)Nc1cc(N)c(Cl)cc1F
C(C)(=O)NC1=CC(=C(C=C1F)Cl)[N+](=O)[O-]>>C(C)(=O)NC1=CC(=C(C=C1F)Cl)N
O=[N+:8]([O-])[c:7]1[cH:6][c:5]([NH:4][C:2]([CH3:1])=[O:3])[c:12]([F:13])[cH:11][c:9]1[Cl:10]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]([NH2:8])[c:9]([Cl:10])[cH:11][c:12]1[F:13]
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F
CC(=O)Nc1cc(N)c(Cl)cc1F
null
[Fe]
C(C)(=O)O.C(C)(=O)OCC
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
60.4
[{"value": 60.4, "product": "C(C)(=O)NC1=CC(=C(C=C1F)Cl)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
null
null
Iron powder (31.9 g) were suspended in a 5% acetic acid solution (60 ml), and the suspension was heated to 90° C. A solution of 4-(N-acetylamino)-1-chloro-5-fluoro-2-nitrobenzene (13.3 g) in acetic acid (100 l ml) and ethyl acetate (70 ml) was dropwise added thereto, and the resultant mixture was refluxed at 80° C. for...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Fe].C(C)(=O)O.C(C)(=O)OCC
90
null
CC(=O)Nc1cc([N+](=O)[O-])c(Cl)cc1F>[Fe].C(C)(=O)O.C(C)(=O)OCC>CC(=O)Nc1cc(N)c(Cl)cc1F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d8cc237945574052a6d5fb822976a17c
CC(=O)Nc1cc(N)c(Cl)cc1F.O=C(O)CS>>CC(=O)Nc1cc(CC(O)=S)c(Cl)cc1F
C(C(=O)O)S.N(=O)[O-].[Na+].C(C)(=O)NC1=CC(=C(C=C1F)Cl)N.Cl.[OH-].[Na+].S(N)(O)(=O)=O>>C(C)(=O)NC=1C(=CC(=C(C1)CC(=S)O)Cl)F
N[c:7]1[cH:6][c:5]([NH:4][C:2]([CH3:1])=[O:3])[c:15]([F:16])[cH:14][c:12]1[Cl:13].O=[C:9]([CH2:8][SH:11])[OH:10]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]([CH2:8][C:9]([OH:10])=[S:11])[c:12]([Cl:13])[cH:14][c:15]1[F:16]
CC(=O)Nc1cc(N)c(Cl)cc1F.O=C(O)CS
CC(=O)Nc1cc(CC(O)=S)c(Cl)cc1F
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
883928d542c9648afb18ee171e788bfedb6971fec38eb060208ce14a90f845ea
0a479965227def53da1b53ebee7774bac4e68ae016c7e895a59ff807fed83dd3
c1ccccc1
N-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[Cl;D1;H0:5]):[c:6].O=[C;H0;D3;+0:7](-[O;D1;H1:8])-[CH2;D2;+0:9]-[SH;D1;+0:10]>>[Cl;D1;H0:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[CH2;D2;+0:9]-[C;H0;D3;+0:7](-[O;D1;H1:8])=[S;H0;D1;+0:10]):[c:2]:[c:3]
null
[]
null
null
1
HOUR
4-(N-Acetylamino)-2-amino-1-chloro-5-fluorobenzene (7.0 g) was suspended in a mixture of conc. hydrochloric acid (9 ml), water (40 ml) and ice (60 g), and the suspension was kept at -5° to 10° C., preferably at 0° C. A solution of sodium nitrite (2.5 g) in water (8 ml) was dropwise added to the suspension, which was th...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Aliphatic thiol
Thiocarbonyl
c1ccccc1
c1ccccc1
c1ccccc1
HO-
O
null
1
CC(=O)Nc1cc(N)c(Cl)cc1F.O=C(O)CS>O>CC(=O)Nc1cc(CC(O)=S)c(Cl)cc1F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-24917a9021f944739cf6948b30a8a80d
CC(=O)Nc1ccc(Br)cc1F.O=S(=O)(O)O>>CC(=O)Nc1cc(S(=O)(=O)O)c(Br)cc1F
S(O)(O)(=O)=O.BrC1=CC(=C(C=C1)NC(C)=O)F.S(O)(O)(=O)=O>>C(C)(=O)NC=1C(=CC(=C(C1)S(=O)(=O)O)Br)F
[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:12]([Br:13])[cH:14][c:15]1[F:16].O[S:8](=[O:9])(=[O:10])[OH:11]>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][c:7]([S:8](=[O:9])(=[O:10])[OH:11])[c:12]([Br:13])[cH:14][c:15]1[F:16]
CC(=O)Nc1ccc(Br)cc1F.O=S(=O)(O)O
CC(=O)Nc1cc(S(=O)(=O)O)c(Br)cc1F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4de7a411ca4a8e56f858115b27e6157e074d8465bf6f118cb7ff1cf307084c04
a824d87b0e6c732faabe155a548de29df954da8631ad9b191cacb2d591bbcaa7
c1ccccc1
O-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[O;D1;H1:4].[Br;D1;H0:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[Br;D1;H0:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[O;D1;H1:4]):[c:9]:[c:10]
null
[]
20
CELSIUS
2
HOUR
N-(4-Bromo-2-fluorophenyl)acetamide (173.2 g) was suspended in conc. sulfuric acid (80 ml), and 60% fuming sulfuric acid (340 ml) was dropwise added thereto at 10° to 20° C., followed by stirring at 20° C., for 2 hours. The reaction mixture was dropwise added to ice water (500 g) at 10° to 20° C., and the precipitated ...
10.6084/m9.figshare.5104873.v1
null
null
Sulfonic acid
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
20
2
CC(=O)Nc1ccc(Br)cc1F.O=S(=O)(O)O>>CC(=O)Nc1cc(S(=O)(=O)O)c(Br)cc1F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-14408afd0ea04118a6b2aec746408141
Cc1ccc(O)c(-c2cccc3[nH]nnc23)c1.Cc1ccc(O)c(-c2cccc3[nH]nnc23)c1>>Cc1cc(Cc2cc(C)cc(-c3cccc4[nH]nnc34)c2O)c(O)c(-c2cccc3[nH]nnc23)c1
CC1=CC=C(C(=C1)C1=CC=CC=2NN=NC21)O.CC1=CC=C(C(=C1)C1=CC=CC=2NN=NC21)O.C[O-].[Na+]>>C(C1=C(C(=CC(=C1)C)C1=CC=CC=2NN=NC21)O)C2=C(C(=CC(=C2)C)C2=CC=CC=1NN=NC12)O
[CH3:1][c:2]1[cH:3][cH:4][c:23]([OH:24])[c:25](-[c:26]2[cH:27][cH:28][cH:29][c:30]3[nH:31][n:32][n:33][c:34]23)[cH:35]1.[cH:6]1[cH:7][c:8]([CH3:9])[cH:10][c:11](-[c:12]2[cH:13][cH:14][cH:15][c:16]3[nH:17][n:18][n:19][c:20]23)[c:21]1[OH:22]>>[CH3:1][c:2]1[cH:3][c:4]([CH2:5][c:6]2[cH:7][c:8]([CH3:9])[cH:10][c:11](-[c:12]...
Cc1ccc(O)c(-c2cccc3[nH]nnc23)c1.Cc1ccc(O)c(-c2cccc3[nH]nnc23)c1
Cc1cc(Cc2cc(C)cc(-c3cccc4[nH]nnc34)c2O)c(O)c(-c2cccc3[nH]nnc23)c1
null
null
C=1(C(=CC=CC1)C)C
C-C Coupling
OtherReaction
eb2908ed4d02b1e0b8609625a74eaabea2a238c68aadec547cb47821958dd9a8
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
c1cc(Cc2cccc(-c3cccc4[nH]nnc34)c2)cc(-c2cccc3[nH]nnc23)c1
[O;D1;H1:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6].[O;D1;H1:7]-[c:8](:[c:9]):[cH;D2;+0:10]:[c:11]:[c:12]>>[O;D1;H1:7]-[c:8](:[c:9]):[c;H0;D3;+0:10](-[C:13]-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:2](-[O;D1;H1:1]):[c:3]):[c:11]:[c:12]
95
[{"value": 95.0, "product": "C(C1=C(C(=CC(=C1)C)C1=CC=CC=2NN=NC21)O)C2=C(C(=CC(=C2)C)C2=CC=CC=1NN=NC12)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
6.2 g of the Mannich base obtained in Example 1 and 4-methyl-6benzotriazolyl-phenol 4.5 g were dissolved in 200 ml of xylene, and sodium methylate (28% methanol solution) 0.2 g was added. The solution was heated with stirring under reflux at 140°-150° C. for 10 hours with a stream of nitrogen. After distilling of the s...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2[nH]nnc2c1.c1ccc2[nH]nnc2c1
Other
C=1(C(=CC=CC1)C)C
null
null
Cc1ccc(O)c(-c2cccc3[nH]nnc23)c1.Cc1ccc(O)c(-c2cccc3[nH]nnc23)c1>C=1(C(=CC=CC1)C)C>Cc1cc(Cc2cc(C)cc(-c3cccc4[nH]nnc34)c2O)c(O)c(-c2cccc3[nH]nnc23)c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d903185401c6425592f4f674eacdfc7e
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O.[N-]=[N+]=C(c1ccccc1)c1ccccc1>>C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)O)=C.C1(=CC=CC=C1)C(=[N+]=[N-])C1=CC=CC=C1.C1(=CC=CC=C1)C(=[N+]=[N-])C1=CC=CC=C1.C(C)(=O)O.C1(=CC=CC=C1)C(=[N+]=[N-])C1=CC=CC=C1>>O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)=C
[CH2:1]=[C:2]([O:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14])[C:15](=[O:16])[OH:17].[N-]=[N+]=[C:18]([c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1)[c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1>>[CH2:1]=[C:2]([O:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14])[C:15](...
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O.[N-]=[N+]=C(c1ccccc1)c1ccccc1
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
O-alkylation of carboxylic acids with diazo compounds
8531b6eb3abfd6846ce0cb8d79abac610072134e0cc0be40cc269196cd4eea5b
d6eab3abd961fdb019332f17e55277b8a7c7f7a1f79c71be7a6248f0a0e6a15e
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
[#8:1]-[C:2](=[C;D1;H2:3])-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6].[N-]=[N+]=[C;H0;D3;+0:7](-[c:8](:[c:9]):[c:10])-[c:11](:[c:12]):[c:13]>>[#8:1]-[C:2](=[C;D1;H2:3])-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[CH;D3;+0:7](-[c:8](:[c:9]):[c:10])-[c:11](:[c:12]):[c:13]
99.1
[{"value": 99.1, "product": "O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2-[(1,3-Dioxo-2H-isoindol-2-yl)oxy]-2-propenoic acid (1.54 g, 4.8 mmole) was dissolved in 25 ml of acetonitrile and a solution of diphenyldiazomethane (1.17 g, 5.94 mmole/50 ml acetonitrile) was added dropwise. After approximately 1.1 equivalents of diphenyldiazomethane had been added, tlc showed no starting material r...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Diazo
Ester
null
null
c1ccc2c(c1)C[NH]C2.c1ccccc1.c1ccccc1
Other
C(C)#N
null
null
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O.[N-]=[N+]=C(c1ccccc1)c1ccccc1>C(C)#N>C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-326a1ef3e0824d60a1db186de1402dca
CC(C)(C)OC(=O)NC1C(=O)N(OCc2ccccc2)C1(C)C>>CC(C)(C)OC(=O)NC1C(=O)N(O)C1(C)C
C(C)(C)(C)OC(=O)NC1C(N(C1(C)C)OCC1=CC=CC=C1)=O>>C(C)(C)(C)OC(=O)NC1C(N(C1(C)C)O)=O
c1ccc(C[O:13][N:12]2[C:10](=[O:11])[CH:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[C:14]2([CH3:15])[CH3:16])cc1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH:9]1[C:10](=[O:11])[N:12]([OH:13])[C:14]1([CH3:15])[CH3:16]
CC(C)(C)OC(=O)NC1C(=O)N(OCc2ccccc2)C1(C)C
CC(C)(C)OC(=O)NC1C(=O)N(O)C1(C)C
null
[Pd]
CO
Deprotection
OtherReaction
94fa5e5ed4a5b32c4aba0dd3c8151bfdd08491d1bc6453e9fd01d7dc3e51cd0f
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=C1CCN1
[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[#7:5]-1-[O;H0;D2;+0:6]-C-c1:c:c:c:c:c:1>>[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[#7:5]-1-[OH;D1;+0:6]
100.4
[{"value": 100.4, "product": "C(C)(C)(C)OC(=O)NC1C(N(C1(C)C)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
(±)-3-[(t-Butyloxycarbonyl)amino]-4,4-dimethyl-1-(phenylmethoxy)-2-azetidinone (8.07 g, 25 mmol) was hydrogenated at atmospheric pressure and ambient temperature in 40 ml of methanol with 0.6 g of 10% palladium on charcoal as catalyst for 2 hours. The reaction mixture was filtered through a pad of Celite and the filtra...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1
null
C1C[NH]C1
Other
[Pd].CO
null
null
CC(C)(C)OC(=O)NC1C(=O)N(OCc2ccccc2)C1(C)C>[Pd].CO>CC(C)(C)OC(=O)NC1C(=O)N(O)C1(C)C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-372b48998a944947acdc316bd1e13103
CC(C)(C)OC(=O)NC1C(=O)N(O)C1(C)C.O=S(=O)(O)Cl.c1ccncc1>>CC(C)(C)OC(=O)NC1C(=O)N(OS(=O)(=O)[O-])C1(C)C.CCCC[N+](CCCC)(CCCC)CCCC
O.C(C)(C)(C)OC(=O)NC1C(N(C1(C)C)O)=O.ClS(=O)(=O)O.N1=CC=CC=C1>>C(CCC)[N+](CCCC)(CCCC)CCCC.S(=O)(=O)(ON1C(C(C1(C)C)NC(=O)OC(C)(C)C)=O)[O-]
[CH3:1][C:2]([O:5][C:6](=[O:7])[NH:8][CH:9]1[C:10](=[O:11])[N:12]([OH:13])[C:18]1([CH3:19])[CH3:20])([CH3:35])[CH3:36].Cl[S:14](=[O:15])(=[O:16])[OH:17].[cH:22]1[cH:23][cH:24][n:25][cH:30][cH:31]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH:9]1[C:10](=[O:11])[N:12]([O:13][S:14](=[O:15])(=[O:16])[O-:17])[...
CC(C)(C)OC(=O)NC1C(=O)N(O)C1(C)C.O=S(=O)(O)Cl.c1ccncc1
CC(C)(C)OC(=O)NC1C(=O)N(OS(=O)(=O)[O-])C1(C)C.CCCC[N+](CCCC)(CCCC)CCCC
null
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
ClCCl
Acylation
OtherReaction
ce7d354dca39d756db2846188614927bd4293b709a269ae75ac42d8d12a93b22
03c431cf9c388e566f0e58c89e54434d4ef9b7340e6b9a612b938fb432b9d26a
O=C1CCN1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[OH;D1;+0:4].[C;D1;H3:5]-[C;H0;D4;+0:6](-[CH3;D1;+0:7])(-[CH3;D1;+0:8])-[#8:9]-[C:10](=[O;D1;H0:11])-[#7:12]-[C:13]1-[C:14]-[#7:15](-[OH;D1;+0:16])-[C:17]-1=[O;D1;H0:18].[cH;D2;+0:19]1:[cH;D2;+0:20]:[cH;D2;+0:21]:[n;H0;D2;+0:22]:[cH;D2;+0:23]:[cH;D2;+0:24]:1>>[C;D1;H3:5]-[C...
null
[]
25
CELSIUS
10
MINUTE
A solution of chlorosulfonic acid (12.27 g, 0.105 mole) in 210 ml of dichloromethane at -40° C. under argon was treated with 20.5 g (0.26 mole) of pyridine dropwise over 10 minutes. The mixture is stirred for 10 more minutes at 0° C. and 10 minutes at 25° C. A slurry of (±)-3-[(t-butyloxycarbonyl)amino]-1-hydroxy-4,4-d...
10.6084/m9.figshare.5104873.v1
null
Ether.Boc
Ether.Boc
c1ccncc1
null
C1C[NH]C1
null
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.ClCCl
25
0.166667
CC(C)(C)OC(=O)NC1C(=O)N(O)C1(C)C.O=S(=O)(O)Cl.c1ccncc1>S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.ClCCl>CC(C)(C)OC(=O)NC1C(=O)N(OS(=O)(=O)[O-])C1(C)C.CCCC[N+](CCCC)(CCCC)CCCC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-8c0e7bba371b45db9636a661c316681f
C=C(O/N=C(\C(=O)NC1C(=O)N(OS(=O)(=O)O)C1(C)C)c1csc(N)n1)C(=O)OC(c1ccccc1)c1ccccc1>>C=C(O/N=C(\C(=O)NC1C(=O)N(OS(=O)(=O)O)C1(C)C)c1csc(N)n1)C(=O)O
FC(C(=O)O)(F)F.NC=1SC=C(N1)/C(/C(=O)NC1C(N(C1(C)C)OS(=O)(=O)O)=O)=N/OC(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)=C.C(Cl)Cl.C1(=CC=CC=C1)OC>>NC=1SC=C(N1)/C(/C(=O)NC1C(N(C1(C)C)OS(=O)(=O)O)=O)=N/OC(C(=O)O)=C
c1ccc(C(c2ccccc2)[O:29][C:27]([C:2](=[CH2:1])[O:3]/[N:4]=[C:5](\[C:6](=[O:7])[NH:8][CH:9]2[C:10](=[O:11])[N:12]([O:13][S:14](=[O:15])(=[O:16])[OH:17])[C:18]2([CH3:19])[CH3:20])[c:21]2[cH:22][s:23][c:24]([NH2:25])[n:26]2)=[O:28])cc1>>[CH2:1]=[C:2]([O:3]/[N:4]=[C:5](\[C:6](=[O:7])[NH:8][CH:9]1[C:10](=[O:11])[N:12]([O:13]...
C=C(O/N=C(\C(=O)NC1C(=O)N(OS(=O)(=O)O)C1(C)C)c1csc(N)n1)C(=O)OC(c1ccccc1)c1ccccc1
C=C(O/N=C(\C(=O)NC1C(=O)N(OS(=O)(=O)O)C1(C)C)c1csc(N)n1)C(=O)O
null
null
C1(=CC=CC=C1)C
Deprotection
Ester saponification (alkyl deprotection)
6c6fe281a466ba3015c862d0079f398ca54d13fe39ff38458258f53accd43d52
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
N=C(C(=O)NC1CNC1=O)c1cscn1
[#8:1]-[C:2](=[C;D1;H2:3])-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-C(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[#8:1]-[C:2](=[C;D1;H2:3])-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6]
null
[]
-5
CELSIUS
45
MINUTE
To the flask containing (±)-(Z)-2-[[[1-(2-amino-4-thiazolyl)-2-[[4,4-dimethyl-2-oxo-1-(sulfooxy)-3-azetidinyl]amino]-2-oxoethylidene]amino]oxy]-2-propenoic acid, diphenylmethyl ester was added methylene chloride (10 ml) and anisole (10 ml). After cooling to -5° C., trifluoroacetic acid (8 ml) was added and the reaction...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1.c1ccccc1
null
C1C[NH]C1.c1cscn1
Other
C1(=CC=CC=C1)C
-5
0.75
C=C(O/N=C(\C(=O)NC1C(=O)N(OS(=O)(=O)O)C1(C)C)c1csc(N)n1)C(=O)OC(c1ccccc1)c1ccccc1>C1(=CC=CC=C1)C>C=C(O/N=C(\C(=O)NC1C(=O)N(OS(=O)(=O)O)C1(C)C)c1csc(N)n1)C(=O)O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-c3f14a8fcf3b4b7497e5d9c212404b51
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(C)(C)C>>C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O
O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)OC(C)(C)C)=C.FC(C(=O)O)(F)F.C1(=CC=CC=C1)C>>O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)O)=C
CC(C)(C)[O:17][C:15]([C:2](=[CH2:1])[O:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14])=[O:16]>>[CH2:1]=[C:2]([O:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14])[C:15](=[O:16])[OH:17]
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(C)(C)C
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O
null
null
C1(=CC=CC=C1)OC.C(Cl)Cl
Deprotection
Deprotection of carboxylic acid
152e5537e48c95b4a3e767536b0f9f68d1308e5f484070828ab5ed951805157a
7f019d4cfe9b3036d0a2d3a3209aa0e1fcb05418ebee15a4be5e125d315d5f01
O=C1NC(=O)c2ccccc21
C-C(-C)(-C)-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4](-[#8:5])=[C;D1;H2:6]>>[#8:5]-[C:4](=[C;D1;H2:6])-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
98.2
[{"value": 98.2, "product": "O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)O)=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of 2-[(1,3-dioxo-2H-isoindol-2-yl)-oxy]-2-propenoic acid, t-butyl ester (49.9 g, 0.173 mole) in methylene chloride (300 ml) and anisole (150 ml) was treated with trifluoroacetic acid (300 ml). After stirring overnight at room temperature, 800 ml of dry toluene was added and the reaction mixture was concentra...
10.6084/m9.figshare.5104873.v1
null
Ester.Boc
Carboxylic acid
null
null
c1ccc2c(c1)C[NH]C2
Other
C1(=CC=CC=C1)OC.C(Cl)Cl
null
8
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(C)(C)C>C1(=CC=CC=C1)OC.C(Cl)Cl>C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-62540daf740f4ebdb0f0fb22e0de0d65
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O.[N-]=[N+]=C(c1ccccc1)c1ccccc1>>C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)O)=C.C1(=CC=CC=C1)C(=[N+]=[N-])C1=CC=CC=C1>>O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)=C
[CH2:1]=[C:2]([O:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14])[C:15](=[O:16])[OH:17].[N-]=[N+]=[C:18]([c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1)[c:25]1[cH:26][cH:27][cH:28][cH:29][cH:30]1>>[CH2:1]=[C:2]([O:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14])[C:15](...
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O.[N-]=[N+]=C(c1ccccc1)c1ccccc1
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
O-alkylation of carboxylic acids with diazo compounds
8531b6eb3abfd6846ce0cb8d79abac610072134e0cc0be40cc269196cd4eea5b
d6eab3abd961fdb019332f17e55277b8a7c7f7a1f79c71be7a6248f0a0e6a15e
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
[#8:1]-[C:2](=[C;D1;H2:3])-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6].[N-]=[N+]=[C;H0;D3;+0:7](-[c:8](:[c:9]):[c:10])-[c:11](:[c:12]):[c:13]>>[#8:1]-[C:2](=[C;D1;H2:3])-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[CH;D3;+0:7](-[c:8](:[c:9]):[c:10])-[c:11](:[c:12]):[c:13]
70.3
[{"value": 70.3, "product": "O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2-[(1,3-Dioxo-2H-isoindol-2-yl)oxy]-2-propenoic acid (39.6 g, 0.17 mole) was dissolved in 800 ml of acetonitrile and a solution of diphenyldiazomethane (43.4 g, 0.224 mole/1000 ml acetonitrile) was added dropwise over 3 hours at 0° C. The reaction solution was evaporated to a solid which was triturated with hexane. The...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Diazo
Ester
null
null
c1ccc2c(c1)C[NH]C2.c1ccccc1.c1ccccc1
Other
C(C)#N
null
null
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)O.[N-]=[N+]=C(c1ccccc1)c1ccccc1>C(C)#N>C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-81a98eb62d3a4e8db0a1240526ed7b45
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1>>C=C(ON)C(=O)OC(c1ccccc1)c1ccccc1
O=C1N(C(C2=CC=CC=C12)=O)OC(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)=C.O.NN>>NOC(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)=C
O=C1c2ccccc2C(=O)[N:4]1[O:3][C:2](=[CH2:1])[C:5](=[O:6])[O:7][CH:8]([c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH2:1]=[C:2]([O:3][NH2:4])[C:5](=[O:6])[O:7][CH:8]([c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1
C=C(ON)C(=O)OC(c1ccccc1)c1ccccc1
null
null
C(Cl)Cl.C(C)O
Reduction
Phthalimide deprotection
8c6c904eae7a7d528fa3eeedb7e9706448ab9f7df249a16fa865a9210a6adc85
892f9aeb7d80035b81a0f5a363c9ed6a90780ba9faa3f0708093fa283b8c9a24
c1ccc(Cc2ccccc2)cc1
O=C1-[N;H0;D3;+0:1](-[#8:2]-[C:3](=[C;D1;H2:4])-[C:5](-[#8:6])=[O;D1;H0:7])-C(=O)-c2:c:c:c:c:c:2-1>>[#8:6]-[C:5](=[O;D1;H0:7])-[C:3](=[C;D1;H2:4])-[#8:2]-[NH2;D1;+0:1]
null
[]
null
null
1
HOUR
To a solution of 2-[(1,3-dioxo-2H-isoindol-2-yl)oxy]-2-propenoic acid, diphenylmethyl ester (6.07 g, 15.2 mmole) in 375 ml of methylene chloride under argon at 0° C. was added hydrazine hydrate (0.76 g, 15.2 mmole) in 4 ml absolute ethanol. After one hour at 0° C., the mixture was evaporated to dryness at +10° C. and t...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary amine
c1ccc2c(c1)C[NH]C2
null
c1ccccc1.c1ccccc1
HO-
C(Cl)Cl.C(C)O
null
1
C=C(ON1C(=O)c2ccccc2C1=O)C(=O)OC(c1ccccc1)c1ccccc1>C(Cl)Cl.C(C)O>C=C(ON)C(=O)OC(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b8abfc5399164ec0b2d27d6533f14659
CC(C)(C)OC(=O)N[C@@H]1C(=O)N(OCc2ccccc2)C1(C)C>>CC(C)(C)OC(=O)N[C@@H]1C(=O)N(O)C1(C)C
C(C)(C)(C)OC(=O)N[C@@H]1C(N(C1(C)C)OCC1=CC=CC=C1)=O>>C(C)(C)(C)OC(=O)N[C@@H]1C(N(C1(C)C)O)=O
c1ccc(C[O:13][N:12]2[C:10](=[O:11])[C@@H:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[C:14]2([CH3:15])[CH3:16])cc1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C@@H:9]1[C:10](=[O:11])[N:12]([OH:13])[C:14]1([CH3:15])[CH3:16]
CC(C)(C)OC(=O)N[C@@H]1C(=O)N(OCc2ccccc2)C1(C)C
CC(C)(C)OC(=O)N[C@@H]1C(=O)N(O)C1(C)C
null
[Pd]
C(C)(=O)OCC.C(C)O
Deprotection
OtherReaction
94fa5e5ed4a5b32c4aba0dd3c8151bfdd08491d1bc6453e9fd01d7dc3e51cd0f
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=C1CCN1
[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[#7:5]-1-[O;H0;D2;+0:6]-C-c1:c:c:c:c:c:1>>[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[#7:5]-1-[OH;D1;+0:6]
83.1
[{"value": 83.1, "product": "C(C)(C)(C)OC(=O)N[C@@H]1C(N(C1(C)C)O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 14.77 g (0.0461 mole) of (3S)-3-[(t-butyloxycarbonyl)amino]-4,4-dimethyl-1-(phenylmethoxy)-2-azetidinone in 15 ml of ethanol and 85 ml of ethyl acetate was hydrogenated over 0.75 g of 5% palladium-on-carbon catalyst for 1.5 hours at 1 atmosphere. The reaction mixture was filtered and concentrated to give ...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1
null
C1C[NH]C1
Other
[Pd].C(C)(=O)OCC.C(C)O
null
null
CC(C)(C)OC(=O)N[C@@H]1C(=O)N(OCc2ccccc2)C1(C)C>[Pd].C(C)(=O)OCC.C(C)O>CC(C)(C)OC(=O)N[C@@H]1C(=O)N(O)C1(C)C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-065deac20e75456784ee84a24854b3d8
CC(C)(C)OC(=O)NC1C(=O)N(OS(=O)(=O)O)C12CCC2>>NC1C(=O)N(OS(=O)(=O)O)C12CCC2
C(C)(C)(C)OC(=O)NC1C(N(C12CCC2)OS(=O)(=O)O)=O.[Na].C1(=CC=CC=C1)OC.FC(C(=O)O)(F)F>>NC1C(N(C12CCC2)OS(=O)(=O)O)=O
CC(C)(C)OC(=O)[NH:1][CH:2]1[C:3](=[O:4])[N:5]([O:6][S:7](=[O:8])(=[O:9])[OH:10])[C:11]12[CH2:12][CH2:13][CH2:14]2>>[NH2:1][CH:2]1[C:3](=[O:4])[N:5]([O:6][S:7](=[O:8])(=[O:9])[OH:10])[C:11]12[CH2:12][CH2:13][CH2:14]2
CC(C)(C)OC(=O)NC1C(=O)N(OS(=O)(=O)O)C12CCC2
NC1C(=O)N(OS(=O)(=O)O)C12CCC2
null
null
ClCCl.C1(=CC=CC=C1)C
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=C1CC2(CCC2)N1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2]1-[C:3]-[#7:4](-[#8:5]-[#16:6]-[O;D1;H1:7])-[C:8]-1=[O;D1;H0:9]>>[NH2;D1;+0:1]-[C:2]1-[C:3]-[#7:4](-[#8:5]-[#16:6]-[O;D1;H1:7])-[C:8]-1=[O;D1;H0:9]
null
[]
null
null
0.5
HOUR
3-[(t-Butoxycarbonyl)amino]-2-oxo-1-(sulfooxy)-1-azaspiro[3.3]heptane, monosodium salt (0.3 g, 0.87 mmole) was slurried in 2.5 ml of dry dichloromethane and 1.0 ml of anisole at -10° C. under argon, and then treated with 4.0 ml of trifluoroacetic acid. After 0.5 hour, a solid had formed. After 1.5 hours, 4 ml of dry to...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
C1CC2(C1)CC[NH]2
HO-
ClCCl.C1(=CC=CC=C1)C
null
0.5
CC(C)(C)OC(=O)NC1C(=O)N(OS(=O)(=O)O)C12CCC2>ClCCl.C1(=CC=CC=C1)C>NC1C(=O)N(OS(=O)(=O)O)C12CCC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-14cd47dd92304a94895a0eed6473f454
BrBr.O=c1cc(O)c2cccnc2n1-c1ccccc1>>O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1
OC1=CC(N(C2=NC=CC=C12)C1=CC=CC=C1)=O.BrBr>>BrC=1C(N(C2=NC=CC=C2C1O)C1=CC=CC=C1)=O
Br[Br:4].[O:1]=[c:2]1[cH:3][c:5]([OH:6])[c:7]2[cH:8][cH:9][cH:10][n:11][c:12]2[n:13]1-[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1>>[O:1]=[c:2]1[c:3]([Br:4])[c:5]([OH:6])[c:7]2[cH:8][cH:9][cH:10][n:11][c:12]2[n:13]1-[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
BrBr.O=c1cc(O)c2cccnc2n1-c1ccccc1
O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1
null
null
C(Cl)Cl
Functional Group Interconversion
Bromination
931b303f1bd4c9a087dc1eb2dc5143889aed01c01237ad614920721faf93f5b4
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
O=c1ccc2cccnc2n1-c1ccccc1
Br-[Br;H0;D1;+0:1].[#7;a:2]:[c:3]1:[c:4]:[c:5](-[O;D1;H1:6]):[cH;D2;+0:7]:[c:8](=[O;D1;H0:9]):[#7;a:10]:1-[c:11]>>[#7;a:2]:[c:3]1:[c:4]:[c:5](-[O;D1;H1:6]):[c;H0;D3;+0:7](-[Br;H0;D1;+0:1]):[c:8](=[O;D1;H0:9]):[#7;a:10]:1-[c:11]
65.4
[{"value": 65.4, "product": "BrC=1C(N(C2=NC=CC=C2C1O)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 4-hydroxy-1-phenyl-1,8-naphthyridin-2(1H)-one (1 g) in CH2Cl2 (20 mL) was added, dropwise and with stirring, a solution of bromine (0.7 g) in CH2Cl2 (5 mL). The mixture was stirred at room temperature overnight, after which time the product was filtered off, dried in air and recrystallized from aceto...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1cnc2ncccc2c1
c1cnc2ncccc2c1
c1cnc2ncccc2c1.c1ccccc1
HBr
C(Cl)Cl
null
null
BrBr.O=c1cc(O)c2cccnc2n1-c1ccccc1>C(Cl)Cl>O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-8cc4dd16c7654ef9a2223720cf302a31
CN1CCCC1.O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1>>C[N+]1(c2c(O)c3cccnc3n(-c3ccccc3)c2=O)CCCC1.[OH-]
BrC=1C(N(C2=NC=CC=C2C1O)C1=CC=CC=C1)=O.CN1CCCC1>>[OH-].OC1=C(C(N(C2=NC=CC=C12)C1=CC=CC=C1)=O)[N+]1(CCCC1)C
[CH3:1][N:2]1[CH2:21][CH2:22][CH2:23][CH2:24]1.Br[c:3]1[c:4]([OH:5])[c:6]2[cH:7][cH:8][cH:9][n:10][c:11]2[n:12](-[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[c:19]1=[O:20]>>[CH3:1][N+:2]1([c:3]2[c:4]([OH:5])[c:6]3[cH:7][cH:8][cH:9][n:10][c:11]3[n:12](-[c:13]3[cH:14][cH:15][cH:16][cH:17][cH:18]3)[c:19]2=[O:20])[CH2:21][...
CN1CCCC1.O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1
C[N+]1(c2c(O)c3cccnc3n(-c3ccccc3)c2=O)CCCC1.[OH-]
null
null
N1=CC=CC=C1
Functional Group Interconversion
OtherReaction
e088ee06debd1768d6a7b49fef1c393c335ddbf966a3c2930c1cbe2912e5a136
4e785b123c30fe1e471eaa628309cb7fdb2dcbe05b4ffc27bd0436c6801b9115
O=c1c([NH+]2CCCC2)cc2cccnc2n1-c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2](=[O;D1;H0:3]):[#7;a:4](-[c:5]):[c:6](:[#7;a:7]):[c:8]:[c:9]:1-[O;D1;H1:10].[C;D1;H3:11]-[N;H0;D3;+0:12]1-[C:13]-[C:14]-[C:15]-[C:16]-1>>[#7;a:7]:[c:6]1:[c:8]:[c:9](-[O;D1;H1:10]):[c;H0;D3;+0:1](-[N+;H0;D4:12]2(-[C;D1;H3:11])-[C:13]-[C:14]-[C:15]-[C:16]-2):[c:2](=[O;D1;H0:3]):[#7;a:4]:1-[c:5]
null
[]
null
null
33
HOUR
In dry pyridine (30 mL), 3-bromo-4-hydroxy-1-phenyl-1,8-naphthyridin-2(1H)-one (10 g) was suspended. N-methyl pyrrolidine (20 mL) was added to the suspension. The mixture was heated to 95°-100° C. with stirring, and was kept there for about 33 hours. The product was evaporated under high vacuum to provide a dark oil. T...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Tertiary amine
null
C1CC[NH]C1.c1cnc2ncccc2c1
c1cnc2ncccc2c1.C1CC[NH+]C1
c1cnc2ncccc2c1.c1ccccc1.C1CC[NH+]C1
null
N1=CC=CC=C1
null
33
CN1CCCC1.O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1>N1=CC=CC=C1>C[N+]1(c2c(O)c3cccnc3n(-c3ccccc3)c2=O)CCCC1.[OH-]
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-1a63051189a64827a0e1e208f850bb1d
C1CCNC1.O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1>>O=c1c([NH+]2CCCC2)c(O)c2cccnc2n1-c1ccccc1.[OH-]
BrC=1C(N(C2=NC=CC=C2C1O)C1=CC=CC=C1)=O.N1CCCC1>>[OH-].OC1=C(C(N(C2=NC=CC=C12)C1=CC=CC=C1)=O)[NH+]1CCCC1
[NH:4]1[CH2:5][CH2:6][CH2:7][CH2:8]1.Br[c:3]1[c:2](=[O:1])[n:17](-[c:18]2[cH:19][cH:20][cH:21][cH:22][cH:23]2)[c:16]2[c:11]([c:9]1[OH:10])[cH:12][cH:13][cH:14][n:15]2>>[O:1]=[c:2]1[c:3]([NH+:4]2[CH2:5][CH2:6][CH2:7][CH2:8]2)[c:9]([OH:10])[c:11]2[cH:12][cH:13][cH:14][n:15][c:16]2[n:17]1-[c:18]1[cH:19][cH:20][cH:21][cH:2...
C1CCNC1.O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1
O=c1c([NH+]2CCCC2)c(O)c2cccnc2n1-c1ccccc1.[OH-]
null
null
CN(C)C=O.C(Cl)Cl
Functional Group Interconversion
OtherReaction
0de7eb20484a3f91e640898ecef4af7974e8385696e6cd2373f8565ddad78a13
629eabbde8e9e7fb44d82efe8f99784bd824d43dc9f8e1860cea90fe5325d9b5
O=c1c([NH+]2CCCC2)cc2cccnc2n1-c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2](=[O;D1;H0:3]):[#7;a:4](-[c:5]):[c:6](:[#7;a:7]):[c:8]:[c:9]:1-[O;D1;H1:10].[C:11]1-[C:12]-[C:13]-[C:14]-[NH;D2;+0:15]-1>>[#7;a:7]:[c:6]1:[c:8]:[c:9](-[O;D1;H1:10]):[c;H0;D3;+0:1](-[NH+;D3:15]2-[C:11]-[C:12]-[C:13]-[C:14]-2):[c:2](=[O;D1;H0:3]):[#7;a:4]:1-[c:5]
null
[]
100
CELSIUS
null
null
A solution of 3-bromo-4-hydroxy-1-phenyl-1,8-naphthyridin-2(1H)-one (2 g) in a mixture of pyrrolidine (10 mL) and DMF (5 mL) was stirred and heated at 100° C. for 2 days. The resulting mixture was then cooled, diluted with CH2Cl2 (100 mL) and filtered. The solid was triturated with hot CHCl3, filtered, and dried to yie...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
null
C1CCNC1.c1cnc2ncccc2c1
C1CC[NH+]C1.c1cnc2ncccc2c1
C1CC[NH+]C1.c1cnc2ncccc2c1.c1ccccc1
null
CN(C)C=O.C(Cl)Cl
100
null
C1CCNC1.O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1>CN(C)C=O.C(Cl)Cl>O=c1c([NH+]2CCCC2)c(O)c2cccnc2n1-c1ccccc1.[OH-]
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-3f7c40f113fd4fd48511e36981e2c6a7
O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1>>O=c1c([NH+]2CCC(O)CC2)c(O)c2cccnc2n1-c1ccccc1.[OH-]
BrC=1C(N(C2=NC=CC=C2C1O)C1=CC=CC=C1)=O>>[OH-].OC1=C(C(N(C2=NC=CC=C12)C1=CC=CC=C1)=O)[NH+]1CCC(CC1)O
Br[c:3]1[c:2](=[O:1])[n:4](-[c:20]2[cH:5][cH:24][cH:23][cH:22][cH:21]2)[c:18]2[c:13]([c:11]1[OH:12])[cH:14][cH:15][cH:16][n:17]2>>[O:1]=[c:2]1[c:3]([NH+:4]2[CH2:5][CH2:6][CH:7]([OH:8])[CH2:9][CH2:10]2)[c:11]([OH:12])[c:13]2[cH:14][cH:15][cH:16][n:17][c:18]2[n:19]1-[c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1.[OH-:26]
O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1
O=c1c([NH+]2CCC(O)CC2)c(O)c2cccnc2n1-c1ccccc1.[OH-]
null
null
N1=C(C=CC=C1C)C.OC1CCNCC1
Aromatic Heterocycle Formation
OtherReaction
c0857e3387d83aa1e3e8272b2f93c681ee7f22de4670677c0e8791fe379a529a
9f963a7ceedcacba8bff3744c93bc22895e3751f804d727222d55e99a5bb086d
O=c1c([NH+]2CCCCC2)cc2cccnc2n1-c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2](-[O;D1;H1:3]):[c:4](:[c:5]):[c;H0;D3;+0:6](:[#7;a:7]:[c:8]):[n;H0;D3;+0:9](-[c;H0;D3;+0:10]2:[c:11]:[c:12]:[c:13]:[cH;D2;+0:14]:[cH;D2;+0:15]:2):[c;H0;D3;+0:16]:1=[O;D1;H0:17]>>[O;D1;H0:17]=[c;H0;D3;+0:16]1:[#7;a:18](-[c;H0;D3;+0:10]2:[c:11]:[c:12]:[c:13]:[cH;D2;+0:14]:[c:19]:2):[c;H0;D3;+0:6](...
null
[]
100
CELSIUS
null
null
A solution of 3-bromo-4-hydroxy-1-phenyl-1,8-naphthyridin-2(1H)-one (1 g) in a mixture of 2,6-lutidine (5 mL) and 4-hydroxy-piperidine (3.12 g) was heated at 100° C. for 32 hours. The lutidine was removed by evaporation under high vacuum. The residue was dissolved in CH3CN(20): H2O(80): CH3CO2H(1) and separated by reve...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Secondary alcohol
c1ccccc1.c1cnc2ncccc2c1
C1CC[NH+]CC1.c1cnc2ncccc2c1.c1ccccc1
C1CC[NH+]CC1.c1cnc2ncccc2c1.c1ccccc1
Br-
N1=C(C=CC=C1C)C.OC1CCNCC1
100
null
O=c1c(Br)c(O)c2cccnc2n1-c1ccccc1>N1=C(C=CC=C1C)C.OC1CCNCC1>O=c1c([NH+]2CCC(O)CC2)c(O)c2cccnc2n1-c1ccccc1.[OH-]
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2a9efe2e38d441bdb33e0120ea48ea1f
CCOc1cc2c(c(OCC)c1OCC)COC2=O.O=[N+]([O-])O>>CCOc1c2c(c([N+](=O)[O-])c(OCC)c1OCC)C(=O)OC2
C(C)(=O)O.C(C)OC1=C2COC(=O)C2=CC(=C1OCC)OCC.[N+](=O)(O)[O-]>>C(C)OC1=C2COC(=O)C2=C(C(=C1OCC)OCC)[N+](=O)[O-]
[CH3:1][CH2:2][O:3][c:4]1[c:5]2[c:6]([cH:7][c:11]([O:12][CH2:13][CH3:14])[c:15]1[O:16][CH2:17][CH3:18])[C:19](=[O:20])[O:21][CH2:22]2.O[N+:8](=[O:9])[O-:10]>>[CH3:1][CH2:2][O:3][c:4]1[c:5]2[c:6]([c:7]([N+:8](=[O:9])[O-:10])[c:11]([O:12][CH2:13][CH3:14])[c:15]1[O:16][CH2:17][CH3:18])[C:19](=[O:20])[O:21][CH2:22]2
CCOc1cc2c(c(OCC)c1OCC)COC2=O.O=[N+]([O-])O
CCOc1c2c(c([N+](=O)[O-])c(OCC)c1OCC)C(=O)OC2
null
null
O
Functional Group Addition
Aromatic nitration with HNO3
ee3ad82349d0ec639a2d273ef62f31226e87972cc0517103400f7bde30591a6c
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=C1OCc2ccccc21
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[#8:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]1:[c:9]-[C:10]-[#8:11]-[C:12]-1=[O;D1;H0:13]>>[#8:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]1:[c:9]-[C:10]-[#8:11]-[C:12]-1=[O;D1;H0:13]
35
[{"value": 35.0, "product": "C(C)OC1=C2COC(=O)C2=C(C(=C1OCC)OCC)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Glacial acetic acid (14 ml) was added to 5.32 g (0.02 mole) of 4,5,6-triethoxyphthalide. Into the reaction mixture on a water bath at 30-35° C., 14 ml of fuming nitric acid, d=1.52, was gradually added dropwise over a time period of 9 hours. After completion of the addition, the reaction mixture was allowed to stand ov...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
HO-
O
null
8
CCOc1cc2c(c(OCC)c1OCC)COC2=O.O=[N+]([O-])O>O>CCOc1c2c(c([N+](=O)[O-])c(OCC)c1OCC)C(=O)OC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-39e3a70ecded4f8ea6d40804995deae2
CO.O=C1OC([N+](=O)[O-])c2ccccc21>>O=C1OCc2ccccc21.c1ccc2cnccc2c1
[N+](=O)([O-])C1OC(=O)C2=CC=CC=C12.CO>>C1=NC=CC2=CC=CC=C12.C1(=O)OCC2=CC=CC=C12
O[CH3:4].O=[N+:16]([O-])[CH:17]1[O:3][C:2](=[O:1])[c:10]2[c:5]1[cH:6][cH:7][cH:8][cH:9]2>>[O:1]=[C:2]1[O:3][CH2:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]21.[cH:11]1[cH:12][cH:13][c:14]2[cH:15][n:16][cH:17][cH:18][c:19]2[cH:20]1
CO.O=C1OC([N+](=O)[O-])c2ccccc21
O=C1OCc2ccccc21.c1ccc2cnccc2c1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
f9a5a1d5d598abfebf99033f479fa9fc5ec64164c0038edd6c13b7a0160aecd8
dae788f4a1f4377f83595fb07b32c0e1335ba5803d0ca58b98d832eeef4ad9ce
O=C1OCc2ccccc21.c1ccc2cnccc2c1
O-[CH3;D1;+0:1].O=[N+;H0;D3:2](-[O-])-[CH;D3;+0:3]1-[O;H0;D2;+0:4]-[C:5](=[O;D1;H0:6])-[c:7](:[c:8]):[c;H0;D3;+0:9]-1:[c:10]:[c:11]>>[O;D1;H0:6]=[C:5]1-[O;H0;D2;+0:4]-[CH2;D2;+0:1]-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:7]-1:[c:8].[c:12]1:[c:13]:[n;H0;D2;+0:2]:[cH;D2;+0:3]:[c:14]:[c:15]:1
null
[]
null
null
null
null
wherein R4 to R7 are as defined above, in methanol in an amount of 1.5 to 10 times by volume of nitrophthalide and a reaction temperature of 50° to 80° C. for a reaction period of 8 to 36 hours to produce a phthalide isoquinoline represented by the general formula (III): ##STR11## Conditions: See reaction.notes.procedu...
10.6084/m9.figshare.5104873.v1
null
Ester.Nitro group.Methanol
Ester
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2.c1ccc2cnccc2c1
c1ccc2c(c1)COC2.c1ccc2cnccc2c1
null
null
null
null
CO.O=C1OC([N+](=O)[O-])c2ccccc21>>O=C1OCc2ccccc21.c1ccc2cnccc2c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-ae4597ad267b47eb9940dcaad6564230
COc1nc(C)nc(N)n1.O=C([O-])N(c1ccccc1)S(=O)(=O)c1ccc(Cl)nn1>>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccc(Cl)nn2)n1
ClC=1N=NC(=CC1)S(=O)(=O)N(C([O-])=O)C1=CC=CC=C1.NC1=NC(=NC(=N1)OC)C>>ClC=1N=NC(=CC1)S(=O)(=O)NC(=O)NC1=NC(=NC(=N1)OC)C
[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH2:9])[n:23]1.[O-][C:10](=[O:11])[N:12](c1ccccc1)[S:13](=[O:14])(=[O:15])[c:16]1[cH:17][cH:18][c:19]([Cl:20])[n:21][n:22]1>>[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][S:13](=[O:14])(=[O:15])[c:16]2[cH:17][cH:18][c:19]([Cl:20])[n:21][n:2...
COc1nc(C)nc(N)n1.O=C([O-])N(c1ccccc1)S(=O)(=O)c1ccc(Cl)nn1
COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccc(Cl)nn2)n1
null
null
O1CCOCC1
Acylation
OtherReaction
c711cd1efb286da599cb4f6d31ebc08e3e00fafe8cc5f1f83ddfd8a6db9b39ec
d376f5b2bb9d4421ae0e8d656f00ea10021a6d76153a24b5fa5e6591c71665a7
O=C(Nc1ncncn1)NS(=O)(=O)c1cccnn1
[#7;a:1]:[#7;a:2]:[c:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[N;H0;D3;+0:7](-[C;H0;D3;+0:8](-[O-])=[O;D1;H0:9])-c1:c:c:c:c:c:1.[NH2;D1;+0:10]-[c:11]1:[#7;a:12]:[c:13]:[#7;a:14]:[c:15]:[#7;a:16]:1>>[#7;a:1]:[#7;a:2]:[c:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[NH;D2;+0:7]-[C;H0;D3;+0:8](=[O;D1;H0:9])-[NH;D2;+0:10]-[c:11]1:...
43.3
[{"value": 43.3, "product": "ClC=1N=NC(=CC1)S(=O)(=O)NC(=O)NC1=NC(=NC(=N1)OC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 14.2 g of N-(3-chloropyridazine-6-sulfonyl)phenylcarbamate and 6.3 g of 2-amino-4-methoxy-6-methyl-1,3,5-triazine are refluxed for 1 hour in 120 ml of absolute dioxan. When the reaction is complete, the mixture is concentrated in vacuo and the residue is taken up in a saturated aqueous solution of sodium b...
10.6084/m9.figshare.5104873.v1
null
Carbamic acid.Primary amine
Sulfonamide.Urea
c1ccccc1
null
c1ncncn1.c1ccnnc1
HO-
O1CCOCC1
null
null
COc1nc(C)nc(N)n1.O=C([O-])N(c1ccccc1)S(=O)(=O)c1ccc(Cl)nn1>O1CCOCC1>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccc(Cl)nn2)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a8d6626d43bf43faa9840510eb71c657
N#CC1NC(=O)[C@H]1N.O=C(Cl)Cc1ccccc1>>N#C[C@H]1NC(=O)[C@H]1NC(=O)Cc1ccccc1
C1(=CC=CC=C1)CC(=O)Cl.CC=1C=CC(=CC1)S(=O)(=O)O.N[C@@H]1C(NC1C#N)=O.N1=CC=CC=C1>>C(#N)[C@@H]1[C@@H](C(N1)=O)NC(CC1=CC=CC=C1)=O
[N:1]#[C:2][CH:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH2:8].Cl[C:9](=[O:10])[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[N:1]#[C:2][C@H:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH:8][C:9](=[O:10])[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
N#CC1NC(=O)[C@H]1N.O=C(Cl)Cc1ccccc1
N#C[C@H]1NC(=O)[C@H]1NC(=O)Cc1ccccc1
null
null
O.C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(Cc1ccccc1)N[C@H]1CNC1=O
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[NH2;D1;+0:5]-[C:6]1-[C:7]-[#7:8]-[C:9]-1=[O;D1;H0:10]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]-[c:4])-[NH;D2;+0:5]-[C:6]1-[C:7]-[#7:8]-[C:9]-1=[O;D1;H0:10]
null
[]
25
CELSIUS
null
null
In 100 ml of methylene chloride were dissolved under ice-cooling 5 g of p-toluenesulfonate of (3S, 4RS)-3-amino-4-cyano-2-azetidinone and 4.2 g of pyridine. To the solution was added 3 g of phenylacetyl chloride. The mixture was stirred at room temperature (about 25° C.) for ten minutes, which was shaken with water. Th...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
C1CNC1.c1ccccc1
HCl
O.C(Cl)Cl
25
null
N#CC1NC(=O)[C@H]1N.O=C(Cl)Cc1ccccc1>O.C(Cl)Cl>N#C[C@H]1NC(=O)[C@H]1NC(=O)Cc1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-188d82f13f314cc0b26d94522c8c649d
CC(C)(ON=C(C(=O)Cl)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1.N#C[C@H]1NC(=O)[C@H]1N>>CC(C)(ON=C(C(=O)N[C@@H]1C(=O)N[C@@H]1C#N)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1
C(C)N(CC)CC.C1(=CC=C(C=C1)S(=O)(=O)O)C.N[C@@H]1C(N[C@@H]1C#N)=O.Cl.ClCC(=O)NC=1SC=C(N1)C(C(=O)Cl)=NOC(C)(C)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-]>>ClCC(=O)NC=1SC=C(N1)C(C(=O)N[C@@H]1C(N[C@@H]1C#N)=O)=NOC(C)(C)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-]
Cl[C:7]([C:6](=[N:5][O:4][C:2]([CH3:1])([CH3:3])[C:27](=[O:28])[O:29][CH2:30][c:31]1[cH:32][cH:33][c:34]([N+:35](=[O:36])[O-:37])[cH:38][cH:39]1)[c:17]1[cH:18][s:19][c:20]([NH:21][C:22](=[O:23])[CH2:24][Cl:25])[n:26]1)=[O:8].[NH2:9][C@@H:10]1[C:11](=[O:12])[NH:13][C@@H:14]1[C:15]#[N:16]>>[CH3:1][C:2]([CH3:3])([O:4][N:5...
CC(C)(ON=C(C(=O)Cl)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1.N#C[C@H]1NC(=O)[C@H]1N
CC(C)(ON=C(C(=O)N[C@@H]1C(=O)N[C@@H]1C#N)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1
null
null
O1CCCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(CON=C(C(=O)N[C@H]1CNC1=O)c1cscn1)OCc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[#7:4]-[#8:5])-[c:6](:[#7;a:7]):[c:8]:[#16;a:9].[NH2;D1;+0:10]-[C:11]1-[C:12]-[#7:13]-[C:14]-1=[O;D1;H0:15]>>[#16;a:9]:[c:8]:[c:6](-[C:3](=[#7:4]-[#8:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:11]1-[C:12]-[#7:13]-[C:14]-1=[O;D1;H0:15]):[#7;a:7]
44.1
[{"value": 44.1, "product": "ClCC(=O)NC=1SC=C(N1)C(C(=O)N[C@@H]1C(N[C@@H]1C#N)=O)=NOC(C)(C)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
40
MINUTE
In 12 ml of tetrahydrofuran was dissolved 0.30 g of (3S, 4S)-3-amino-4-cyano-2-azetidinone p-toluenesulfonate. To the solution were added, under ice-cooling, 0.12 g of triethylamine and, subsequently 0.60 g of 2-(2-chloroacetamidothiazol-4-yl)-2-(1-p-nitrobenzyloxycarbonyl-1-methylethoxyimino)acetyl chloride hydrochlor...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
C1CNC1.c1cscn1.c1ccccc1
HCl
O1CCCC1
null
0.666667
CC(C)(ON=C(C(=O)Cl)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1.N#C[C@H]1NC(=O)[C@H]1N>O1CCCC1>CC(C)(ON=C(C(=O)N[C@@H]1C(=O)N[C@@H]1C#N)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-9b042347b36c4a3287150473876816b6
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N>>N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
CS(=O)(=O)[C@@H]1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.[C-]#N.[K+].C(C)(=O)OCC.C(C)(=O)OCC>>C(#N)C1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
CS(=O)(=O)[C@H:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH:8][C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1.[N:1]#[C-:2]>>[N:1]#[C:2][CH:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH:8][C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17]...
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N
N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
null
null
O.CN(C)C=O
C-C Coupling
OtherReaction
4e2b6fe3999f8013b5d72b11baedbb086b0bf3517953db3002e7a90160212e1f
afc317b75dc27dd96f8b185a6d88494042f714247ebd3d6ce3b0e647608c4473
O=C1NC[C@@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
C-S(=O)(=O)-[C@H;D3;+0:1]1-[#7:2]-[C:3](=[O;D1;H0:4])-[C:5]-1-[#7:6].[C-;H0;D1:7]#[N;D1;H0:8]>>[#7:6]-[C:5]1-[C:3](=[O;D1;H0:4])-[#7:2]-[CH;D3;+0:1]-1-[C;H0;D2;+0:7]#[N;D1;H0:8]
77.2
[{"value": 77.2, "product": "C(#N)C1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
25
CELSIUS
30
MINUTE
To a solution of 12.3 g of (3R, 4R)-4-methylsulfonyl-3-tritylamino-2-azetidinone in 150 ml of DMF is added a solution of 1.6 g of potassium cyanide in 24 ml of water under ice-cooling and the mixture is stirred at room temperature (approx. 25° C.) for 30 minutes. To the reaction mixture are added ice water and ethyl ac...
10.6084/m9.figshare.5104873.v1
null
Sulfone
Nitrile
C1CNC1
C1CNC1
C1CNC1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
O.CN(C)C=O
25
0.5
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N>O.CN(C)C=O>N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-1554984ff1894fc28fe6a21cbc9b7c15
CC(C)(C)[Si](C)(C)Cl.N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1>>CC(C)(C)[Si](C)(C)N1C(=O)[C@@H](NC(c2ccccc2)(c2ccccc2)c2ccccc2)C1C#N
C(#N)C1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.C(C)N(CC)CC.[Si](C)(C)(C(C)(C)C)Cl>>[Si](C)(C)(C(C)(C)C)N1C([C@H](C1C#N)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=O
Cl[Si:5]([C:2]([CH3:1])([CH3:3])[CH3:4])([CH3:6])[CH3:7].[NH:8]1[C:9](=[O:10])[C@@H:11]([NH:12][C:13]([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)([c:20]2[cH:21][cH:22][cH:23][cH:24][cH:25]2)[c:26]2[cH:27][cH:28][cH:29][cH:30][cH:31]2)[CH:32]1[C:33]#[N:34]>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[N:8]1[C...
CC(C)(C)[Si](C)(C)Cl.N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
CC(C)(C)[Si](C)(C)N1C(=O)[C@@H](NC(c2ccccc2)(c2ccccc2)c2ccccc2)C1C#N
null
null
C(Cl)Cl
Protection
OtherReaction
571205ba0a22d3d60d9a45b3b137645dbca02e496a419b6be1f95f33017d0b79
f67e5eeebc56cd2b347c1c8f322829d7af5cd2d5682d82dce87a0ff304294500
O=C1NC[C@@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7].[N;D1;H0:8]#[C:9]-[C:10]1-[C:11]-[C:12](=[O;D1;H0:13])-[NH;D2;+0:14]-1>>[C;D1;H3:5]-[C:4](-[C;D1;H3:6])(-[C;D1;H3:7])-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[N;H0;D3;+0:14]1-[C:10](-[C:9]#[N;D1;H0:8])-[C:11]-[C:12]-1=[O;D1...
44
[{"value": 44.0, "product": "[Si](C)(C)(C(C)(C)C)N1C([C@H](C1C#N)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 1.10 g of (3s, 4RS)-4-cyano-3-tritylamino-2-azetidinone, 0.50 g of triethylamine and 20 ml of methylene chloride is added 0.56 g of tert-butyldimethylsilyl chloride under ice-cooling and stirring. The mixture is stirred at room temperature (approx. 25° C.) for 30 minutes and the reaction mixture is conc...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Silyl protective group
Tertiary amide.Silyl protective group
C1CNC1
C1C[NH]C1
C1C[NH]C1.c1ccccc1.c1ccccc1.c1ccccc1
HCl
C(Cl)Cl
null
null
CC(C)(C)[Si](C)(C)Cl.N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1>C(Cl)Cl>CC(C)(C)[Si](C)(C)N1C(=O)[C@@H](NC(c2ccccc2)(c2ccccc2)c2ccccc2)C1C#N
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f9d3196cf5bc4df3bc21273101cc2edd
CC(C)(ON=C(C(=O)NC1C(=O)NC1C#N)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1.OO>>CC(C)(ON=C(C(=O)N[C@@H]1C(=O)N[C@@H]1C(N)=O)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1
OO.[OH-].[Na+].ClCC(=O)NC=1SC=C(N1)C(C(=O)NC1C(NC1C#N)=O)=NOC(C)(C)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-]>>C(N)(=O)[C@@H]1[C@@H](C(N1)=O)NC(C(=NOC(C)(C)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])C=1N=C(SC1)NC(CCl)=O)=O
[CH3:1][C:2]([CH3:3])([O:4][N:5]=[C:6]([C:7](=[O:8])[NH:9][CH:10]1[C:11](=[O:12])[NH:13][CH:14]1[C:15]#[N:16])[c:18]1[cH:19][s:20][c:21]([NH:22][C:23](=[O:24])[CH2:25][Cl:26])[n:27]1)[C:28](=[O:29])[O:30][CH2:31][c:32]1[cH:33][cH:34][c:35]([N+:36](=[O:37])[O-:38])[cH:39][cH:40]1.O[OH:17]>>[CH3:1][C:2]([CH3:3])([O:4][N:...
CC(C)(ON=C(C(=O)NC1C(=O)NC1C#N)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1.OO
CC(C)(ON=C(C(=O)N[C@@H]1C(=O)N[C@@H]1C(N)=O)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Nitrile and hydrogen peroxide to amide
b438c1a5a5f49012c6adf1e24ab44bc669089beaf4e5b0289cbfa931d3ceafda
37ed9176b981633816a0414a3f5b39ee33c11d757fe87a2cac8fe30b523bffdf
O=C(CON=C(C(=O)N[C@H]1CNC1=O)c1cscn1)OCc1ccccc1
O-[OH;D1;+0:1].[N;H0;D1;+0:2]#[C;H0;D2;+0:3]-[CH;D3;+0:4]1-[#7:5]-[C:6](=[O;D1;H0:7])-[C:8]-1-[#7:9]-[C:10]=[O;D1;H0:11]>>[NH2;D1;+0:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:1])-[C@H;D3;+0:4]1-[#7:5]-[C:6](=[O;D1;H0:7])-[C:8]-1-[#7:9]-[C:10]=[O;D1;H0:11]
null
[]
25
CELSIUS
30
MINUTE
In 2 ml of dimethyl sulfoxide is dissolved 0.38 g of (3S,4S)-b 3-[2-(2-chloroacetamidothiazol-4-yl)-2-(1-p-nitrobenzyloxycarbonyl-1-methylethoxyimino)acetamido]-4-cyano-2-azetidinone and, following addition of 0.1 ml of 30% aqueous hydrogen peroxide and 0.1 ml of 1N sodium hydroxide, the mixture is stirred at approx. 2...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Peroxide
Primary amide
null
null
C1CNC1.c1cscn1.c1ccccc1
Other
CS(=O)C
25
0.5
CC(C)(ON=C(C(=O)NC1C(=O)NC1C#N)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1.OO>CS(=O)C>CC(C)(ON=C(C(=O)N[C@@H]1C(=O)N[C@@H]1C(N)=O)c1csc(NC(=O)CCl)n1)C(=O)OCc1ccc([N+](=O)[O-])cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-ef45cd8e19f346a2939b798513a0897d
N#C[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.OO>>NC(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
C(#N)[C@@H]1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.Cl.OO.[OH-].[Na+]>>C(N)(=O)[C@@H]1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
[N:1]#[C:2][C@H:4]1[NH:5][C:6](=[O:7])[C@H:8]1[NH:9][C:10]([c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)([c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1)[c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1.O[OH:3]>>[NH2:1][C:2](=[O:3])[C@H:4]1[NH:5][C:6](=[O:7])[C@H:8]1[NH:9][C:10]([c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)([c:17]...
N#C[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.OO
NC(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
null
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
ClCCl
Heteroatom Alkylation and Arylation
Nitrile and hydrogen peroxide to amide
b438c1a5a5f49012c6adf1e24ab44bc669089beaf4e5b0289cbfa931d3ceafda
37ed9176b981633816a0414a3f5b39ee33c11d757fe87a2cac8fe30b523bffdf
O=C1NC[C@@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
O-[OH;D1;+0:1].[N;H0;D1;+0:2]#[C;H0;D2;+0:3]-[C:4]1-[#7:5]-[C:6](=[O;D1;H0:7])-[C:8]-1>>[NH2;D1;+0:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:1])-[C:4]1-[#7:5]-[C:6](=[O;D1;H0:7])-[C:8]-1
null
[]
null
null
null
null
In 2 ml of dichloromethane is dissolved 160 mg of (3S,4S)-4-cyano-3-triphenylmethylamino-2-azetidinone and, following addition of 154 mg of tetra-n-butylammonium hydrogen sulfate, 0.103 ml of 30% aqueous hydrogen peroxide and 0.68 ml of 1N sodium hydroxide are added under ice-cooling and stirring. The mixture is stirre...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Peroxide
Primary amide
null
null
C1CNC1.c1ccccc1.c1ccccc1.c1ccccc1
Other
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.ClCCl
null
null
N#C[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.OO>S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.ClCCl>NC(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-98f46b24b7374845b869dde97ca1bcc2
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N>>N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
[C-]#N.[K+].CS(=O)(=O)[C@@H]1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>C(#N)C1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
CS(=O)(=O)[C@H:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH:8][C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1.[N:1]#[C-:2]>>[N:1]#[C:2][CH:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH:8][C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17]...
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N
N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
null
[Cl-].C(CCCCCCC)[N+](C)(CCCCCCCC)CCCCCCCC
O.C(Cl)(Cl)(Cl)Cl
C-C Coupling
OtherReaction
4e2b6fe3999f8013b5d72b11baedbb086b0bf3517953db3002e7a90160212e1f
afc317b75dc27dd96f8b185a6d88494042f714247ebd3d6ce3b0e647608c4473
O=C1NC[C@@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
C-S(=O)(=O)-[C@H;D3;+0:1]1-[#7:2]-[C:3](=[O;D1;H0:4])-[C:5]-1-[#7:6].[C-;H0;D1:7]#[N;D1;H0:8]>>[#7:6]-[C:5]1-[C:3](=[O;D1;H0:4])-[#7:2]-[CH;D3;+0:1]-1-[C;H0;D2;+0:7]#[N;D1;H0:8]
72.2
[{"value": 72.2, "product": "C(#N)C1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In 120 ml of carbon tetrachloride are dissolved 12.2 g of (3R,4R)-4-methylsulfonyl-3-tritylamino-2-azetidinone and 2.44 g of tri-n-octylmethylammonium chloride and, under stirring, a solution of 2.15 g of potassium cyanide in 30 ml of water is added. The mixture is stirred vigorously at the same temperature for 15 minu...
10.6084/m9.figshare.5104873.v1
null
Sulfone
Nitrile
C1CNC1
C1CNC1
C1CNC1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
[Cl-].C(CCCCCCC)[N+](C)(CCCCCCCC)CCCCCCCC.O.C(Cl)(Cl)(Cl)Cl
null
null
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N>[Cl-].C(CCCCCCC)[N+](C)(CCCCCCCC)CCCCCCCC.O.C(Cl)(Cl)(Cl)Cl>N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f19b343e797049888b9b1649d2bc69eb
N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.OO>>NC(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
OO.[OH-].[Na+].C(#N)C1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>C(N)(=O)[C@@H]1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
[N:1]#[C:2][CH:4]1[NH:5][C:6](=[O:7])[C@H:8]1[NH:9][C:10]([c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)([c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1)[c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1.O[OH:3]>>[NH2:1][C:2](=[O:3])[C@H:4]1[NH:5][C:6](=[O:7])[C@H:8]1[NH:9][C:10]([c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)([c:17]1...
N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.OO
NC(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
null
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
Nitrile and hydrogen peroxide to amide
b438c1a5a5f49012c6adf1e24ab44bc669089beaf4e5b0289cbfa931d3ceafda
37ed9176b981633816a0414a3f5b39ee33c11d757fe87a2cac8fe30b523bffdf
O=C1NC[C@@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
O-[OH;D1;+0:1].[#7:2]-[C:3]1-[C:4](=[O;D1;H0:5])-[#7:6]-[CH;D3;+0:7]-1-[C;H0;D2;+0:8]#[N;H0;D1;+0:9]>>[#7:2]-[C:3]1-[C:4](=[O;D1;H0:5])-[#7:6]-[C@@H;D3;+0:7]-1-[C;H0;D3;+0:8](-[NH2;D1;+0:9])=[O;H0;D1;+0:1]
20.4
[{"value": 20.4, "product": "C(N)(=O)[C@@H]1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In 40 ml of chloroform is dissolved 3.54 g of (3S,4RS)-4-cyano-3-tritylamino-2-azetidinone as obtained in Example 20 and, following addition of 3.4 g of tetra-n-butylammonium hydrogen sulfate, 2.3 g of 30% hydrogen peroxide and 15 ml of 1N sodium hydroxide are added under ice-cooling and stirring. The mixture is stirre...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Peroxide
Primary amide
null
null
C1CNC1.c1ccccc1.c1ccccc1.c1ccccc1
Other
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(Cl)(Cl)Cl
null
null
N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.OO>S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(Cl)(Cl)Cl>NC(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-ae461d73bcff45228281b4f8a3db474f
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N>>N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
[C-]#N.[K+].CS(=O)(=O)[C@@H]1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>C(#N)C1[C@@H](C(N1)=O)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
CS(=O)(=O)[C@H:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH:8][C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1.[N:1]#[C-:2]>>[N:1]#[C:2][CH:3]1[NH:4][C:5](=[O:6])[C@H:7]1[NH:8][C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17]...
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N
N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
null
CCCCC[N+](CCCCC)(CCCCC)CCCCC.[Br-]
C1=CC=CC=C1.O
C-C Coupling
OtherReaction
4e2b6fe3999f8013b5d72b11baedbb086b0bf3517953db3002e7a90160212e1f
afc317b75dc27dd96f8b185a6d88494042f714247ebd3d6ce3b0e647608c4473
O=C1NC[C@@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
C-S(=O)(=O)-[C@H;D3;+0:1]1-[#7:2]-[C:3](=[O;D1;H0:4])-[C:5]-1-[#7:6].[C-;H0;D1:7]#[N;D1;H0:8]>>[#7:6]-[C:5]1-[C:3](=[O;D1;H0:4])-[#7:2]-[CH;D3;+0:1]-1-[C;H0;D2;+0:7]#[N;D1;H0:8]
null
[]
null
null
15
MINUTE
In 2 ml of benzene are dissolved 0.5 mmol of (3R,4R)-4-methylsulfonyl-3-tritylamino-2-azetidinone and 0.1 mmol of tetra-n-amylammonium bromide, and a solution of 0.55 mmol of potassium cyanide in 0.55 ml of water is added at 15° C. The mixture is stirred vigorously for 15 minutes and treated in the same manner as Examp...
10.6084/m9.figshare.5104873.v1
null
Sulfone
Nitrile
C1CNC1
C1CNC1
C1CNC1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
CCCCC[N+](CCCCC)(CCCCC)CCCCC.[Br-].C1=CC=CC=C1.O
null
0.25
CS(=O)(=O)[C@H]1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1.[C-]#N>CCCCC[N+](CCCCC)(CCCCC)CCCCC.[Br-].C1=CC=CC=C1.O>N#CC1NC(=O)[C@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2a80223beefe44d9b08f195aabbc7f3b
O=S(=O)(OCC(F)(F)F)C(F)(F)F.Oc1ccc(O)cc1>>FC(F)(F)COc1ccc(OCC(F)(F)F)cc1
C1(O)=CC=C(O)C=C1.C([O-])([O-])=O.[K+].[K+].FC(S(=O)(=O)OCC(F)(F)F)(F)F>>FC(COC1=CC=C(C=C1)OCC(F)(F)F)(F)F
O=S(=O)(O[CH2:5][C:2]([F:1])([F:3])[F:4])[C:13]([F:14])([F:15])[F:16].[OH:6][c:7]1[cH:8][cH:9][c:10]([OH:11])[cH:17][cH:18]1>>[F:1][C:2]([F:3])([F:4])[CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([O:11][CH2:12][C:13]([F:14])([F:15])[F:16])[cH:17][cH:18]1
O=S(=O)(OCC(F)(F)F)C(F)(F)F.Oc1ccc(O)cc1
FC(F)(F)COc1ccc(OCC(F)(F)F)cc1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
40e52addd69bfb60edf49cf338a3e101168e05048346fdb8a656fea7da57757c
2966f4b83ace9b36068d1786a601e1728bcf23c7155547a11ed2d75bfe3b84a3
c1ccccc1
O=S(=O)(-O-[CH2;D2;+0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[F;D1;H0:5])-[C;H0;D4;+0:6](-[F;D1;H0:7])(-[F;D1;H0:8])-[F;D1;H0:9].[OH;D1;+0:10]-[c:11]1:[c:12]:[c:13]:[c:14](-[OH;D1;+0:15]):[c:16]:[c:17]:1>>[F;D1;H0:7]-[C;H0;D4;+0:6](-[F;D1;H0:8])(-[F;D1;H0:9])-[C:18]-[O;H0;D2;+0:10]-[c:11]1:[c:12]:[c:13]:[c:14](-[O;H0;D2;...
88
[{"value": 88.0, "product": "FC(COC1=CC=C(C=C1)OCC(F)(F)F)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a mixture of 2.42 moles (334.4 g.) of potassium carbonate, 2.2 moles (510.6 g.) of 2,2,2-trifluoroethyl trifluoromethanesulfonate in 1.02 liter of acetone is added a solution of 1.0 mole (110 g.) of hydroquinone in 1.1 liter of acetone, slowly over a 2 hour period. The reaction is then heated at reflux for 24 hours,...
10.6084/m9.figshare.5104873.v1
null
Triflate.Aromatic alcohol.Aromatic alcohol
Trifluoro group.Ether.Ether
null
null
c1ccccc1
Other
CC(=O)C
null
2
O=S(=O)(OCC(F)(F)F)C(F)(F)F.Oc1ccc(O)cc1>CC(=O)C>FC(F)(F)COc1ccc(OCC(F)(F)F)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-bd78296ee7604ae9bddbd1b3c3be1a26
CC(=O)OC(C)=O.FC(F)(F)COc1ccc(OCC(F)(F)F)cc1>>CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
Cl.[Cl-].[Al+3].[Cl-].[Cl-].FC(COC1=CC=C(C=C1)OCC(F)(F)F)(F)F.C(C)(=O)OC(C)=O>>CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F
CC(=O)O[C:2]([CH3:1])=[O:3].[cH:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]
CC(=O)OC(C)=O.FC(F)(F)COc1ccc(OCC(F)(F)F)cc1
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
null
ClCCl.CCCCCC
C-C Coupling
Friedel-Crafts acylation
d99b77b773ef3c26c74d2c747a21e4608137c0863599d8a950dc561200cf7372
e8c3519869b9d5fd7c4ab2911407db4a86c645fb02749ed598ab3b129e3927f8
c1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#8:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[#8:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]):[c:8]:[c:9]
90
[{"value": 90.0, "product": "CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 2.43 moles (324 g.) of aluminum chloride in 648 ml. of dichloromethane is added a solution 0.88 mole (274 g.) of 1,4-bis(2,2,2-trifluoroethoxy)benzene and 0.97 mole (92 ml.) of acetic anhydride in 880 ml. of dichloromethane over a 3 hour period while maintaining the temperature at above 0° C. The reacti...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HO-
ClCCl.CCCCCC
null
null
CC(=O)OC(C)=O.FC(F)(F)COc1ccc(OCC(F)(F)F)cc1>ClCCl.CCCCCC>CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-335d4ec0845a4042ae6c145b2c618492
CC(=O)OC(C)=O.FC(F)(F)COc1ccc(OCC(F)(F)F)cc1>>CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
FC(COC1=CC=C(C=C1)OCC(F)(F)F)(F)F.C(C)(=O)OC(C)=O.Cl.[Cl-].[Al+3].[Cl-].[Cl-]>>CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F
CC(=O)O[C:2]([CH3:1])=[O:3].[cH:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]
CC(=O)OC(C)=O.FC(F)(F)COc1ccc(OCC(F)(F)F)cc1
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
null
ClCCl
C-C Coupling
Friedel-Crafts acylation
d99b77b773ef3c26c74d2c747a21e4608137c0863599d8a950dc561200cf7372
e8c3519869b9d5fd7c4ab2911407db4a86c645fb02749ed598ab3b129e3927f8
c1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#8:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[#8:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]):[c:8]:[c:9]
82
[{"value": 82.0, "product": "CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.3, "product": "CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a mixture of 4.367 kilograms (32.75 moles) of aluminum chloride and 8.8 liters of dichloromethane at 0° C. is added gradually a solution of 3,267 kilograms of 1,4-bis(2,2,2-trifluoroethoxy)benzene and 1.899 kilograms (13.7 moles) of acetic anhydride in 1.3 liters of dichloromethane. The reaction temperature is maint...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HO-
ClCCl
null
16
CC(=O)OC(C)=O.FC(F)(F)COc1ccc(OCC(F)(F)F)cc1>ClCCl>CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-e8cf184961434382a1570af4c29666d4
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[OH-]>>O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F.[OH-].[Na+].ClCl.[OH-].[Na+]>>FC(COC1=C(C(=O)O)C=C(C=C1)OCC(F)(F)F)(F)F
C[C:2](=[O:1])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21].[OH-:3]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[OH-]
O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
null
O
Acylation
OtherReaction
e1d216f9ec5d1e0ab04cbd7e284acaaebe679828044d718ad57104584ff5302e
7b5bc8122b5027b4d965c982eed9443b26b90bd801407eec9b2b367c037fc8de
c1ccccc1
C-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[OH-;D0:6]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[OH;D1;+0:6])-[c:3](:[c:4]):[c:5]
94.5
[{"value": 94.5, "product": "FC(COC1=C(C(=O)O)C=C(C=C1)OCC(F)(F)F)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
To a solution of 7.3 moles (292 g.) of sodium hydroxide in 600 ml. of water is added ice to make the total volume of 1.75 liters. Chlorine gas is passed into the solution while maintaining the temperature below 10° C. until it is neutral to litmus, and 2.19 moles (87.6 g.) of sodium hydroxide dissolved in 200 ml. of wa...
10.6084/m9.figshare.5104873.v1
null
Ketone
Carboxylic acid
null
null
c1ccccc1
Other
O
50
null
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[OH-]>O>O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-91f05881152f4417803aa3e3b341a28e
O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.O=S(Cl)Cl>>O=C(Cl)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
FC(COC1=C(C(=O)O)C=C(C=C1)OCC(F)(F)F)(F)F.S(=O)(Cl)Cl>>FC(COC1=C(C(=O)Cl)C=C(C=C1)OCC(F)(F)F)(F)F
O[C:2](=[O:1])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21].O=S(Cl)[Cl:3]>>[O:1]=[C:2]([Cl:3])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]
O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.O=S(Cl)Cl
O=C(Cl)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
null
C1=CC=CC=C1
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
c1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
To a solution of 0.688 mole (219 g.) of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid in 657 ml. of benzene is added 1.376M. (100.4 ml.) of thionyl chloride slowly over 1 hour while heating to about 60° C. The mixture is then heated at reflux for about 8 hours, then evaporated to provide the desired product, 2,5-bis(2,2,2...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1
HCl
C1=CC=CC=C1
null
null
O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.O=S(Cl)Cl>C1=CC=CC=C1>O=C(Cl)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-c720cf44b01b4661bc3a257853320079
O=C(NCc1ccccn1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F>>O=C(NCC1CCCCN1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
FC(COC1=C(C(=O)NCC2=NC=CC=C2)C=C(C=C1)OCC(F)(F)F)(F)F.C(C)(=O)O.[H][H]>>C(C)(=O)O.FC(COC1=C(C(=O)NCC2NCCCC2)C=C(C=C1)OCC(F)(F)F)(F)F
[O:5]=[C:6]([NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][n:14]1)[c:15]1[cH:16][c:17]([O:18][CH2:19][C:20]([F:21])([F:22])[F:23])[cH:24][cH:25][c:26]1[O:27][CH2:28][C:29]([F:30])([F:31])[F:32]>>[O:5]=[C:6]([NH:7][CH2:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13][NH:14]1)[c:15]1[cH:16][c:17]([O:18][CH2:19][C:20]([F:21])([...
O=C(NCc1ccccn1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
O=C(NCC1CCCCN1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
[Pt]
CCCCCC
Reduction
OtherReaction
8a6c78a63989dd47e282eb33ae5ce6bfcead5defaa210963e9125c31297ee886
2b7f370a519e29b4dede190aa36b37f30822496e32f2c8bfa9736e631bde52e2
O=C(NCC1CCCCN1)c1ccccc1
[O;D1;H0:1]=[C:2]-[#7:3]-[C:4]-[c;H0;D3;+0:5]1:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:[cH;D2;+0:9]:[n;H0;D2;+0:10]:1>>[O;D1;H0:1]=[C:2]-[#7:3]-[C:4]-[CH;D3;+0:5]1-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[NH;D2;+0:10]-1
71
[{"value": 71.0, "product": "C(C)(=O)O.FC(COC1=C(C(=O)NCC2NCCCC2)C=C(C=C1)OCC(F)(F)F)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
6.5
HOUR
A mixture of 0.33 mole (134.7 g.) 2,5-bis(2,2,2-trifluoroethoxy)-N-(2-pyridylmethyl)benzamide, 1.347 liter of glacial acetic acid and 13.5 g. of 5 percent platinum on carbon is reduced in a Parr apparatus at a pressure of about 10 pounds of hydrogen at room temperature. The reaction is complete in 6-7 hours. The reacti...
10.6084/m9.figshare.5104873.v1
null
null
Secondary amine
c1ccncc1
C1CCNCC1
C1CCNCC1.c1ccccc1
null
[Pt].CCCCCC
null
6.5
O=C(NCc1ccccn1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F>[Pt].CCCCCC>O=C(NCC1CCCCN1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-dc7bfbb943914b4989841cde9342f1f2
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[O-]Cl>>O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
Cl[O-].C(C)(=O)C1=CC=CC=C1.CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F>>FC(COC1=C(C(=O)O)C=C(C=C1)OCC(F)(F)F)(F)F
C[C:2](=[O:1])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21].Cl[O-:3]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[O-]Cl
O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
null
null
Acylation
OtherReaction
e1d216f9ec5d1e0ab04cbd7e284acaaebe679828044d718ad57104584ff5302e
7b5bc8122b5027b4d965c982eed9443b26b90bd801407eec9b2b367c037fc8de
c1ccccc1
C-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[O-;H0;D1:6]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[OH;D1;+0:6])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
replacing the methyl moiety of the acetophenone function of said 2,5-bis(2,2,2-trifluoroethoxy)acetophenone using hypochlorite to yield 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone
Carboxylic acid
null
null
c1ccccc1
HCl
null
null
null
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[O-]Cl>>O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-472b66ff9eef40b493ae1e06eec8e701
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[O-]Cl>>O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
Cl[O-].C(C)(=O)C1=CC=CC=C1.CC(=O)C1=C(C=CC(=C1)OCC(F)(F)F)OCC(F)(F)F>>FC(COC1=C(C(=O)O)C=C(C=C1)OCC(F)(F)F)(F)F
C[C:2](=[O:1])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21].Cl[O-:3]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([O:7][CH2:8][C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]1[O:16][CH2:17][C:18]([F:19])([F:20])[F:21]
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[O-]Cl
O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
null
null
Acylation
OtherReaction
e1d216f9ec5d1e0ab04cbd7e284acaaebe679828044d718ad57104584ff5302e
7b5bc8122b5027b4d965c982eed9443b26b90bd801407eec9b2b367c037fc8de
c1ccccc1
C-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].Cl-[O-;H0;D1:6]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[OH;D1;+0:6])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
replacing the methyl moiety of the acetophenone function of said 2,5-bis(2,2,2-trifluoroethoxy)acetophenone using hypochlorite to yield 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid; and Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone
Carboxylic acid
null
null
c1ccccc1
HCl
null
null
null
CC(=O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F.[O-]Cl>>O=C(O)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-dce6f4e2248c4163ba66fcf4d334a273
NCc1ccccn1.O=C(Cl)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F>>O=C(NCc1ccccn1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
FC(COC1=C(C(=O)Cl)C=C(C=C1)OCC(F)(F)F)(F)F.NCC1=NC=CC=C1>>FC(COC1=C(C(=O)NCC2=NC=CC=C2)C=C(C=C1)OCC(F)(F)F)(F)F
[NH2:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][n:10]1.Cl[C:2](=[O:1])[c:11]1[cH:12][c:13]([O:14][CH2:15][C:16]([F:17])([F:18])[F:19])[cH:20][cH:21][c:22]1[O:23][CH2:24][C:25]([F:26])([F:27])[F:28]>>[O:1]=[C:2]([NH:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][n:10]1)[c:11]1[cH:12][c:13]([O:14][CH2:15][C:16]([F:17])([F:18])[F:1...
NCc1ccccn1.O=C(Cl)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
O=C(NCc1ccccn1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
null
null
null
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCc1ccccn1)c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[#7;a:6]:[c:7]-[C:8]-[NH2;D1;+0:9]>>[#7;a:6]:[c:7]-[C:8]-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
contacting said 2,5-bis(2,2,2trifluoroethoxy)benzoic acid chloride with 2-aminomethylpyridine to provide 2,5-bis(2,2,2-trifluoroethoxy)-N-(2-pyridylmethyl)benzamide. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1.c1ccccc1
HCl
null
null
null
NCc1ccccn1.O=C(Cl)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F>>O=C(NCc1ccccn1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-6075e750f58d40a38d75ded2154666e1
O=C(c1ccc(C(=O)O)c(C(=O)O)c1)c1ccc(C(=O)O)c(C(=O)O)c1>>O=C(c1ccc2c(c1)C(=O)OC2=O)c1ccc2c(c1)C(=O)OC2=O
C1=CC(=C(C=C1C(=O)C2=CC(=C(C=C2)C(=O)O)C(=O)O)C(=O)O)C(=O)O.C1=CC(=C(C=C1C(=O)C2=CC(=C(C=C2)C(=O)O)C(=O)O)C(=O)O)C(=O)O.C(C1=CC=CC=C1)(=O)C1=CC=CC=C1>>C1=CC2=C(C=C1C(=O)C3=CC4=C(C=C3)C(=O)OC4=O)C(=O)OC2=O
O[C:9]([c:7]1[c:6]([C:12]([OH:11])=[O:13])[cH:5][cH:4][c:3]([C:2](=[O:1])[c:14]2[cH:15][cH:16][c:17]([C:23](O)=[O:24])[c:18]([C:20](=[O:21])[OH:22])[cH:19]2)[cH:8]1)=[O:10]>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[C:9](=[O:10])[O:11][C:12]2=[O:13])[c:14]1[cH:15][cH:16][c:17]2[c:18]([cH:19]1)[C:20](=[O:21])[O...
O=C(c1ccc(C(=O)O)c(C(=O)O)c1)c1ccc(C(=O)O)c(C(=O)O)c1
O=C(c1ccc2c(c1)C(=O)OC2=O)c1ccc2c(c1)C(=O)OC2=O
null
null
null
Miscellaneous
OtherReaction
01fc45a364070fbd541127169777f7bd59cd6fb39434dc4c20a62ecba22d8cdc
e83a95bc3ef3bbc28a0f9ce60ccfbd3725429b901b391dbfdf0df35bff2f3261
O=C(c1ccc2c(c1)C(=O)OC2=O)c1ccc2c(c1)C(=O)OC2=O
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8].O-[C;H0;D3;+0:9](=[O;D1;H0:10])-[c:11](:[c:12]):[c:13]-[C:14](=[O;D1;H0:15])-[OH;D1;+0:16]>>[O;D1;H0:10]=[C;H0;D3;+0:9]1-[O;H0;D2;+0:16]-[C:14](=[O;D1;H0:15])-[c:13]:[c:11]-1:[c:12].[O;D1;H0:7]=[C:6]1-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D...
null
[]
null
null
null
null
A process for producing benzophenone tetracarboxylic dianhydride, which comprises adding benzophenone tetracarboxylic acid to a solvent comprising, as the main constituent, an organic compound having a boiling point of more than 100° C. and being inert to benzophenone tetracarboxylic acid and benzophenone tetracarboxyl...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Carboxylic acid.Carboxylic acid
Anhydride.Anhydride
null
c1ccc2c(c1)COC2.c1ccc2c(c1)COC2
c1ccc2c(c1)COC2.c1ccc2c(c1)COC2
HO-
null
null
null
O=C(c1ccc(C(=O)O)c(C(=O)O)c1)c1ccc(C(=O)O)c(C(=O)O)c1>>O=C(c1ccc2c(c1)C(=O)OC2=O)c1ccc2c(c1)C(=O)OC2=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-db112047c19e43b3a1f1f3e0cc3d9b0d
BrCCCBr.Oc1ccc2c(c1)OCO2>>BrCCCOc1ccc2c(c1)OCO2
C(C)(C)(C)O.[OH-].[K+].C1OC=2C=C(C=CC2O1)O.BrCCCBr>>BrCCCOC1=CC2=C(OCO2)C=C1
Br[CH2:4][CH2:3][CH2:2][Br:1].[OH:5][c:6]1[cH:7][cH:8][c:9]2[c:10]([cH:11]1)[O:12][CH2:13][O:14]2>>[Br:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]2[c:10]([cH:11]1)[O:12][CH2:13][O:14]2
BrCCCBr.Oc1ccc2c(c1)OCO2
BrCCCOc1ccc2c(c1)OCO2
null
null
O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2c(c1)OCO2
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
81.7
[{"value": 81.7, "product": "BrCCCOC1=CC2=C(OCO2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a solution prepared by dissolving 7.3 g of potassium hydroxide in 7 ml of water and then adding 120 ml of t-butanol are added 15 g of 3,4-methylenedioxyphenol and 88 g of 1,3-dibromopropane and the mixture is stirred for 3 hours under heating at reflux. After completion of the reaction, the solvent is distilled off ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)OCO2
HBr
O
null
3
BrCCCBr.Oc1ccc2c(c1)OCO2>O>BrCCCOc1ccc2c(c1)OCO2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-89aa6ffc9f4d4c8db3519910dae0cdda
O=C(CNCC1COc2ccccc2O1)c1ccc2c(c1)OCO2>>OC(CNCC1COc2ccccc2O1)c1ccc2c(c1)OCO2
[OH-].[Na+].Cl.O1C(COC2=C1C=CC=C2)CNCC(=O)C2=CC1=C(OCO1)C=C2.[BH4-].[Na+]>>O1C(COC2=C1C=CC=C2)CNCC(O)C2=CC1=C(OCO1)C=C2
[O:1]=[C:2]([CH2:3][NH:4][CH2:5][CH:6]1[CH2:7][O:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[O:15]1)[c:16]1[cH:17][cH:18][c:19]2[c:20]([cH:21]1)[O:22][CH2:23][O:24]2>>[OH:1][CH:2]([CH2:3][NH:4][CH2:5][CH:6]1[CH2:7][O:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[O:15]1)[c:16]1[cH:17][cH:18][c:19]2[c:20]([cH:21]1)[O:22][C...
O=C(CNCC1COc2ccccc2O1)c1ccc2c(c1)OCO2
OC(CNCC1COc2ccccc2O1)c1ccc2c(c1)OCO2
null
null
CO
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccc2c(c1)OCC(CNCCc1ccc3c(c1)OCO3)O2
[#7:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5](:[c:6]):[c:7]>>[#7:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5](:[c:6]):[c:7]
89
[{"value": 89.0, "product": "O1C(COC2=C1C=CC=C2)CNCC(O)C2=CC1=C(OCO1)C=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.4, "product": "O1C(COC2=C1C=CC=C2)CNCC(O)C2=CC1=C(OCO1)C=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
6
HOUR
In 15 ml of methanol is dissolved 1.0 g of 5-[2-{(1,4-benzodioxan-2-ylmethyl)amino}acetyl]-1,3-benzodioxole hydrochloride prepared according to the procedure described in Example 3 and the solution is neutralized with 2N sodium hydroxide. Thereafter, 100 mg of sodium borohydride is added and the mixture is stirred for ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccc2c(c1)OCCO2.c1ccc2c(c1)OCO2
null
CO
null
6
O=C(CNCC1COc2ccccc2O1)c1ccc2c(c1)OCO2>CO>OC(CNCC1COc2ccccc2O1)c1ccc2c(c1)OCO2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-cb6902f9bbd442ae9d8ee9ad3797bedb
NCC1COc2ccccc2O1.O=C(CCCl)Nc1ccc2c(c1)OCO2>>O=C(CCNCC1COc2ccccc2O1)Nc1ccc2c(c1)OCO2
O.ClCCC(=O)NC1=CC2=C(C=C1)OCO2.O1C(COC2=C1C=CC=C2)CN.C(C)N(CC)CC>>O1C(COC2=C1C=CC=C2)CNCCC(=O)NC2=CC1=C(C=C2)OCO1
[NH2:5][CH2:6][CH:7]1[CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[O:16]1.Cl[CH2:4][CH2:3][C:2](=[O:1])[NH:17][c:18]1[cH:19][cH:20][c:21]2[c:22]([cH:23]1)[O:24][CH2:25][O:26]2>>[O:1]=[C:2]([CH2:3][CH2:4][NH:5][CH2:6][CH:7]1[CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[O:16]1)[NH:17][c:18]1[cH:19][cH:2...
NCC1COc2ccccc2O1.O=C(CCCl)Nc1ccc2c(c1)OCO2
O=C(CCNCC1COc2ccccc2O1)Nc1ccc2c(c1)OCO2
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
O=C(CCNCC1COc2ccccc2O1)Nc1ccc2c(c1)OCO2
Cl-[CH2;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[c:6].[#8:7]-[C:8]-[C:9]-[NH2;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[NH;D2;+0:10]-[CH2;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[c:6]
87.5
[{"value": 77.0, "product": "O1C(COC2=C1C=CC=C2)CNCCC(=O)NC2=CC1=C(C=C2)OCO1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.5, "product": "O1C(COC2=C1C=CC=C2)CNCCC(=O)NC2=CC1=C(C=C2)OCO1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
20
HOUR
To a solution of 10 g of N-(3-chloropropionyl)-3,4-methylenedioxyaniline in 50 ml of dimethylformamide are added 8.7 g of 1,4-benzodioxan-2-ylmethylamine and 8.9 g of triethylamine and the mixture is stirred for 20 hours at 50° C. After completion of the reaction, water is added and the mixture is extracted with ethyl ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2c(c1)OCCO2.c1ccc2c(c1)OCO2
HCl
CN(C=O)C
50
20
NCC1COc2ccccc2O1.O=C(CCCl)Nc1ccc2c(c1)OCO2>CN(C=O)C>O=C(CCNCC1COc2ccccc2O1)Nc1ccc2c(c1)OCO2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-ee7884ce19df458082f8329aee02b602
O=C(CCNCC1COc2ccccc2O1)Nc1ccc2c(c1)OCO2>>c1ccc2c(c1)OCC(CNCCCNc1ccc3c(c1)OCO3)O2
[H-].[Al+3].[Li+].[H-].[H-].[H-].O1C(COC2=C1C=CC=C2)CNCCC(=O)NC2=CC1=C(C=C2)OCO1.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>O1C(COC2=C1C=CC=C2)CNCCCNC2=CC1=C(C=C2)OCO1
O=[C:14]([CH2:13][CH2:12][NH:11][CH2:10][CH:9]1[CH2:8][O:7][c:5]2[c:4]([cH:3][cH:2][cH:1][cH:6]2)[O:25]1)[NH:15][c:16]1[cH:17][cH:18][c:19]2[c:20]([cH:21]1)[O:22][CH2:23][O:24]2>>[cH:1]1[cH:2][cH:3][c:4]2[c:5]([cH:6]1)[O:7][CH2:8][CH:9]([CH2:10][NH:11][CH2:12][CH2:13][CH2:14][NH:15][c:16]1[cH:17][cH:18][c:19]3[c:20]([c...
O=C(CCNCC1COc2ccccc2O1)Nc1ccc2c(c1)OCO2
c1ccc2c(c1)OCC(CNCCCNc1ccc3c(c1)OCO3)O2
null
null
O1CCCC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc2c(c1)OCC(CNCCCNc1ccc3c(c1)OCO3)O2
O=[C;H0;D3;+0:1](-[#7:2]-[c:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[CH2;D2;+0:1]-[#7:2]-[c:3]
97.1
[{"value": 80.0, "product": "O1C(COC2=C1C=CC=C2)CNCCCNC2=CC1=C(C=C2)OCO1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.1, "product": "O1C(COC2=C1C=CC=C2)CNCCCNC2=CC1=C(C=C2)OCO1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
4
HOUR
In 50 ml of tetrahydrofuran is suspended 1.5 g of lithium aluminum hydride and a solution of 6.0 g of N-[3-{(1,4-benzodioxan-2-yl}methyl)amino propionyl]-3,4-methylenedioxyaniline prepared according to the procedure described in Example 6 dissolved in 10 ml of tetrahydrofuran is added dropwise to the suspension. After ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccc2c(c1)OCCO2.c1ccc2c(c1)OCO2
Other
O1CCCC1
50
4
O=C(CCNCC1COc2ccccc2O1)Nc1ccc2c(c1)OCO2>O1CCCC1>c1ccc2c(c1)OCC(CNCCCNc1ccc3c(c1)OCO3)O2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f4b2f6b895ea49ca973111d860418a32
C=CC.CC(C)C=O.CCCC=O>>CCCC(O)C(C=O)CC
C=CC.C(CCC)=O.C(C(C)C)=O>>CCCC(C(CC)C=O)O
C=C[CH3:10].C[CH:6]([CH:7]=[O:8])[CH3:9].[CH3:1][CH2:2][CH2:3][CH:4]=[O:5]>>[CH3:1][CH2:2][CH2:3][CH:4]([OH:5])[CH:6]([CH:7]=[O:8])[CH2:9][CH3:10]
C=CC.CC(C)C=O.CCCC=O
CCCC(O)C(C=O)CC
null
null
null
C-C Coupling
OtherReaction
80e1f0b18ea95959b98505afff5c2aa33a934f4b772e171c0da1076665a6ad5b
c9897ef6c812d57d5114df5e38a5a8945d9f218ddf57db27ecece1bf741ab026
null
C-[CH;D3;+0:1](-[CH3;D1;+0:2])-[C:3]=[O;D1;H0:4].C=C-[CH3;D1;+0:5].[C:6]-[C:7]-[CH;D2;+0:8]=[O;H0;D1;+0:9]>>[C:6]-[C:7]-[CH;D3;+0:8](-[OH;D1;+0:9])-[CH;D3;+0:1](-[C:3]=[O;D1;H0:4])-[CH2;D2;+0:2]-[CH3;D1;+0:5]
null
[]
null
null
null
null
This compound is usually prepared by the hydroformylation of propene yielding a reaction mixture which contains n-butanal, as well as i-butanal and other reaction products. The pure n-butanal is separated from the reaction mixture by distillation and is subsequently subjected to aldolisation to form the corresponding b...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Aldehyde.Vinyl
Aldehyde.Secondary alcohol
null
null
null
Other
null
null
null
C=CC.CC(C)C=O.CCCC=O>>CCCC(O)C(C=O)CC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-5f1172c237c240db90b4e91212b88ef5
Cc1cc(C(=O)O)cc(C)c1[N+](=O)[O-].Cc1ccccc1CN>>Cc1ccccc1CNC(=O)c1cc(C)c([N+](=O)[O-])c(C)c1
CC=1C=C(C(=O)Cl)C=C(C1[N+](=O)[O-])C.CC=1C=C(C(=O)O)C=C(C1[N+](=O)[O-])C.CC1=C(CN)C=CC=C1.C(C)N(CC)CC>>CC=1C=C(C(=O)NCC2=C(C=CC=C2)C)C=C(C1[N+](=O)[O-])C
O[C:10](=[O:11])[c:12]1[cH:13][c:14]([CH3:15])[c:16]([N+:17](=[O:18])[O-:19])[c:20]([CH3:21])[cH:22]1.[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][NH2:9]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[CH2:8][NH:9][C:10](=[O:11])[c:12]1[cH:13][c:14]([CH3:15])[c:16]([N+:17](=[O:18])[O-:19])[c:20]([CH3:21])[cH:22]1
Cc1cc(C(=O)O)cc(C)c1[N+](=O)[O-].Cc1ccccc1CN
Cc1ccccc1CNC(=O)c1cc(C)c([N+](=O)[O-])c(C)c1
null
null
O1CCCC1
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NCc1ccccc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:6]-[C:7]-[c:8])-[c:3](:[c:4]):[c:5]
null
[]
null
null
8
HOUR
A solution of 3,5-dimethyl-4-nitrobenzoyl chloride in tetrahyrofuran, generated from 7.0 g of 3,5-dimethyl-4-nitrobenzoic acid by standard procedures, was added to 4.3 g of 2-methylbenzyl amine and 5.0 ml of triethylamine in tetrahydrofuran. The reaction was stirred at ambient temperature overnight, chilled, and filter...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
O1CCCC1
null
8
Cc1cc(C(=O)O)cc(C)c1[N+](=O)[O-].Cc1ccccc1CN>O1CCCC1>Cc1ccccc1CNC(=O)c1cc(C)c([N+](=O)[O-])c(C)c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a117bc2fbc444d72b33f591291414928
BrBr.Cc1c(O)c(C)c(Br)c(C)c1Br>>CC1=C(Br)C(C)(Br)C(Br)=C(C)C1=O
CC1=C(C(=CC(=C1)C)C)O.BrBr.BrC=1C(=C(C(=C(C1C)Br)C)O)C.BrCC1=C(C(=C(C(=C1Br)C)O)C)Br>>BrC1=C(C(C(=C(C1(C)Br)Br)C)=O)C
Br[Br:7].[CH3:1][c:2]1[c:3]([Br:4])[c:5]([CH3:6])[c:8]([Br:9])[c:10]([CH3:11])[c:12]1[OH:13]>>[CH3:1][C:2]1=[C:3]([Br:4])[C:5]([CH3:6])([Br:7])[C:8]([Br:9])=[C:10]([CH3:11])[C:12]1=[O:13]
BrBr.Cc1c(O)c(C)c(Br)c(C)c1Br
CC1=C(Br)C(C)(Br)C(Br)=C(C)C1=O
null
null
O.C(C)(=O)[O-].[Na+].C(C)(=O)O.C(C)(=O)O
Acylation
OtherReaction
cd7b2d41b2cd4da3c6fbe252952f2a86818177d86729a91505440f6eb12ff42e
30b22b6f50ed5709786636242f968e27ffd86e89894ab3f87a968d3be413a783
O=C1C=CCC=C1
Br-[Br;H0;D1;+0:1].[Br;D1;H0:2]-[c;H0;D3;+0:3]1:[c;H0;D3;+0:4](-[C;D1;H3:5]):[c;H0;D3;+0:6](-[OH;D1;+0:7]):[c;H0;D3;+0:8](-[C;D1;H3:9]):[c;H0;D3;+0:10](-[Br;D1;H0:11]):[c;H0;D3;+0:12]:1-[C;D1;H3:13]>>[Br;D1;H0:2]-[C;H0;D3;+0:3]1=[C;H0;D3;+0:4](-[C;D1;H3:5])-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-[C;H0;D3;+0:8](-[C;D1;H3:9])=[...
null
[]
null
null
null
null
The preparation of a halogenated phenol such as 4-bromomethyl-3, 5-dibromo-2, 6-dimethylphenol (tribromomesitol) can involve the following sequence: bromination of 2, 4, 6-trimethylphenol (mesitol) with 2 moles of bromine in acetic acid to prepare 3, 5-dibromo-2, 4, 6-trimethylphenol (dibromometisol) which is isolated ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic alcohol
Tertiary halide.Alkenyl halide.Alkenyl halide.Ketone
c1ccccc1
C1=CCC=CC1
C1=CCC=CC1
HBr
O.C(C)(=O)[O-].[Na+].C(C)(=O)O.C(C)(=O)O
null
null
BrBr.Cc1c(O)c(C)c(Br)c(C)c1Br>O.C(C)(=O)[O-].[Na+].C(C)(=O)O.C(C)(=O)O>CC1=C(Br)C(C)(Br)C(Br)=C(C)C1=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2a36e49790914d26a529926870d300df
Cc1c(O)c(C)c(Br)c(C)c1Br.Cc1cc(C(Br)(Br)Br)cc(C)c1O>>Cc1c(O)c(C)c(Br)c(CBr)c1Br
BrC(C=1C=C(C(=C(C1)C)O)C)(Br)Br.BrC1=C(C(=C(C(=C1C)O)C)Br)C>>BrCC1=C(C(=C(C(=C1Br)C)O)C)Br
[CH3:1][c:2]1[c:3]([OH:4])[c:5]([CH3:6])[c:7]([Br:8])[c:9]([CH3:10])[c:12]1[Br:13].Cc1cc(C(Br)(Br)[Br:11])cc(C)c1O>>[CH3:1][c:2]1[c:3]([OH:4])[c:5]([CH3:6])[c:7]([Br:8])[c:9]([CH2:10][Br:11])[c:12]1[Br:13]
Cc1c(O)c(C)c(Br)c(C)c1Br.Cc1cc(C(Br)(Br)Br)cc(C)c1O
Cc1c(O)c(C)c(Br)c(CBr)c1Br
null
null
null
Functional Group Interconversion
Bromination
c283c4d3091aa0534b9b612860bbb8e64790c700dbfcc856a7f4baab20059420
ae02e01962cf9daf34585e5708190b4128615578bb6c86f760dd7705559059a3
c1ccccc1
Br-C(-Br)(-[Br;H0;D1;+0:1])-c1:c:c(-C):c(-O):c(-C):c: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
[]
25
CELSIUS
3
HOUR
The temperature is increased to 70° C. -75° C., and a solution is obtained. The solution is held at 70° C. -75° C. for 3 hours. The unreacted bromine is removed by distillation with the aid of 1 liter of carbon tetrachloride. When 1 liter of solvent remains with the product, the solution is cooled to 25° C. The light b...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Aromatic alcohol
Primary halide
c1ccccc1
null
c1ccccc1
HBr
null
25
3
Cc1c(O)c(C)c(Br)c(C)c1Br.Cc1cc(C(Br)(Br)Br)cc(C)c1O>>Cc1c(O)c(C)c(Br)c(CBr)c1Br
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-7974117b850745ce99478a14fbf8fabe
O=C(O)C(O)c1ccc(O)c(O)c1.O=S(=O)(Cl)Cl>>O=C(O)C(O)c1cc(O)c(O)cc1Cl
S(=O)(=O)(Cl)Cl.OC=1C=C(C(C(=O)O)O)C=CC1O.O>>ClC1=C(C(C(=O)O)O)C=C(C(=C1)O)O
[O:1]=[C:2]([OH:3])[CH:4]([OH:5])[c:6]1[cH:7][c:8]([OH:9])[c:10]([OH:11])[cH:12][cH:13]1.O=S(=O)(Cl)[Cl:14]>>[O:1]=[C:2]([OH:3])[CH:4]([OH:5])[c:6]1[cH:7][c:8]([OH:9])[c:10]([OH:11])[cH:12][c:13]1[Cl:14]
O=C(O)C(O)c1ccc(O)c(O)c1.O=S(=O)(Cl)Cl
O=C(O)C(O)c1cc(O)c(O)cc1Cl
null
null
C(C)(=O)O
Functional Group Interconversion
Chlorination
f6effe61353895b318215d8bd9b6bb1105cafbf7be8c217d748df587260b32c3
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccccc1
Cl-S(=O)(=O)-[Cl;H0;D1;+0:1].[O;D1;H0:2]=[C:3](-[O;D1;H1:4])-[C:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:6](-[C:5]-[C:3](=[O;D1;H0:2])-[O;D1;H1:4]):[c:7]
null
[]
null
null
2
HOUR
Sulphuryl chloride (0.8 ml) was added to a solution of 3,4-dihydroxymandelic acid (1.84 g, 10 mmol) in warm acetic acid (20 ml). The mixture was stirred for two hours then poured into water and extracted with ethyl acetate (6×40 ml). The extracts were washed with saturated brine (50 ml), dried and evaporated to a cryst...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
HCl
C(C)(=O)O
null
2
O=C(O)C(O)c1ccc(O)c(O)c1.O=S(=O)(Cl)Cl>C(C)(=O)O>O=C(O)C(O)c1cc(O)c(O)cc1Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-28fadf5ad4b9498fb212d6eaee09c186
N.O=CC(=O)O.Oc1ccc(Cl)cc1O>>O=C(O)CNc1cc(O)c(O)cc1Cl
N.C(C=O)(=O)O.ClC=1C=C(C(O)=CC1)O.N.C>>ClC1=C(C=C(C(=C1)O)O)NCC(=O)O
[NH3:5].O=[CH:4][C:2](=[O:1])[OH:3].[cH:6]1[cH:7][c:8]([OH:9])[c:10]([OH:11])[cH:12][c:13]1[Cl:14]>>[O:1]=[C:2]([OH:3])[CH2:4][NH:5][c:6]1[cH:7][c:8]([OH:9])[c:10]([OH:11])[cH:12][c:13]1[Cl:14]
N.O=CC(=O)O.Oc1ccc(Cl)cc1O
O=C(O)CNc1cc(O)c(O)cc1Cl
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
c11d733b1d378c2ca8935818f43643986c21b09db71b80282f52fa3887fa4a14
8883936783e332626550746e6de6ae2ae8af6a13e88264ea7bb1baff157737c0
c1ccccc1
O=[CH;D2;+0:1]-[C:2](=[O;D1;H0:3])-[O;D1;H1:4].[Cl;D1;H0:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10].[NH3;D0;+0:11]>>[Cl;D1;H0:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[NH;D2;+0:11]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[O;D1;H1:4]):[c:9]:[c:10]
null
[]
null
null
8
HOUR
Aqueous ammonia (Sp.Gr 0.88, 37.5 ml) was added dropwise to an ice bath cooled 50% w/v aqueous glyoxylic acid solution (11.25 ml) at <10°. When the addition was complete the solution was heated at 50° for 15 minutes, 4-chlorocatechol (21.7 g) and more aqueous ammonia (12.5 ml) added, then heated at 60° for 4 hours. The...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
8
N.O=CC(=O)O.Oc1ccc(Cl)cc1O>>O=C(O)CNc1cc(O)c(O)cc1Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-87ff1aaf786d4dafa35d8815afcd33ec
O=C(NC(O)C(=O)O)OCc1ccccc1.Oc1ccc(Cl)cc1O>>O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl
C([O-])([O-])=O.[Na+].[Na+].S(O)(O)(=O)=O.ClC=1C=C(C(O)=CC1)O.C(C1=CC=CC=C1)OC(=O)NC(C(=O)O)O>>C(C1=CC=CC=C1)OC(=O)N(CC(=O)O)C1=C(C=C(C(=C1)O)O)Cl
O[CH:4]([C:2](=[O:1])[OH:3])[NH:5][C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[cH:16]1[cH:17][c:18]([OH:19])[c:20]([OH:21])[cH:22][c:23]1[Cl:24]>>[O:1]=[C:2]([OH:3])[CH2:4][N:5]([C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][c:18]([OH:19])[c:20]([OH:21])[cH:...
O=C(NC(O)C(=O)O)OCc1ccccc1.Oc1ccc(Cl)cc1O
O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl
null
null
C(C)(=O)O.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
82bd85c6da7b44e60eeaaedb2361d3b39244ecd3f218fee1ba2ec03dd1fa5d10
ecf89c6cf8e87d34d1bce0363f2597a3a5f86e83f56c6da8dc45241096b01ba6
O=C(Nc1ccccc1)OCc1ccccc1
O-[CH;D3;+0:1](-[NH;D2;+0:2]-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9].[Cl;D1;H0:10]-[c:11](:[c:12]):[cH;D2;+0:13]:[c:14]:[c:15]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[N;H0;D3;+0:2](-[CH2;D2;+0:1]-[C:7](=[O;D1;H0:8])-[O;D1;H1:9])-[c;H0;D3;+0:13](:[c:14]:[c:15]):[c:11](-[Cl;D1;H0:10]):[c:12]
null
[]
null
null
1
HOUR
Acetic acid (27 ml), concentrated sulphuric acid (3 ml) then 4-chlorocatechol (5.06 g. 35 mmole) were added to N-benzyloxycarbonyl 2-hydroxyglycine (6.75 g, 30 mmole) cooled in an ice bath. The mixture was stirred for one hour then poured onto ice and ethyl acetate and adjusted to pH7 with saturated sodium carbonate so...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Secondary alcohol
Carbamic ester
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
C(C)(=O)O.C(C)(=O)OCC
null
1
O=C(NC(O)C(=O)O)OCc1ccccc1.Oc1ccc(Cl)cc1O>C(C)(=O)O.C(C)(=O)OCC>O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-8be6c565ef5649d1915be6fdfbac7331
O=C(O)CN(C(=O)OCc1ccccc1)c1ccc(O)c(O)c1.O=S(=O)(Cl)Cl>>O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl
C(C1=CC=CC=C1)OC(=O)N(CC(=O)O)C1=CC(=C(C=C1)O)O.S(=O)(=O)(Cl)Cl>>C(C1=CC=CC=C1)OC(=O)N(CC(=O)O)C1=C(C=C(C(=C1)O)O)Cl
[O:1]=[C:2]([OH:3])[CH2:4][N:5]([C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][c:18]([OH:19])[c:20]([OH:21])[cH:22][cH:23]1.O=S(=O)(Cl)[Cl:24]>>[O:1]=[C:2]([OH:3])[CH2:4][N:5]([C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[c:16]1[cH:17][c:18]([OH:19])[c:20]([O...
O=C(O)CN(C(=O)OCc1ccccc1)c1ccc(O)c(O)c1.O=S(=O)(Cl)Cl
O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl
null
null
C(C)(=O)O.C(C)(=O)OCC
Functional Group Interconversion
Chlorination
f6effe61353895b318215d8bd9b6bb1105cafbf7be8c217d748df587260b32c3
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
O=C(Nc1ccccc1)OCc1ccccc1
Cl-S(=O)(=O)-[Cl;H0;D1;+0:1].[O;D1;H0:2]=[C:3]-[#7:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:5](-[#7:4]-[C:3]=[O;D1;H0:2]):[c:6]
null
[]
null
null
2
HOUR
N-Benzyloxycarbonyl 3,4-dihydroxyphenylglycine (0.79 g, 2.5 mmole) in acetic acid (10 ml) was treated with sulphuryl chloride (0.2 ml), stirred at room temperature for two hours then diluted with ethyl acetate (50 ml), washed with water (2×3 ml) and brine (20 ml), dried and evaporated to a gum which was crystallized fr...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HCl
C(C)(=O)O.C(C)(=O)OCC
null
2
O=C(O)CN(C(=O)OCc1ccccc1)c1ccc(O)c(O)c1.O=S(=O)(Cl)Cl>C(C)(=O)O.C(C)(=O)OCC>O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f891e300ccd949b285d97d069a945d6c
CC(=O)OC(C)=O.O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl>>CC(=O)Oc1cc(Cl)c(N(CC(=O)O)C(=O)OCc2ccccc2)cc1OC(C)=O
C1CCOC1.C(C1=CC=CC=C1)OC(=O)N(CC(=O)O)C1=C(C=C(C(=C1)O)O)Cl.C([O-])([O-])=O.[Na+].[Na+].C([O-])([O-])=O.[Na+].[Na+].C(C)(=O)OC(C)=O.C(C)(=O)OC(C)=O>>C(C1=CC=CC=C1)OC(=O)N(CC(=O)O)C1=C(C=C(C(=C1)OC(C)=O)OC(C)=O)Cl
O([C:2]([CH3:1])=[O:3])[C:28]([CH3:29])=[O:30].[OH:4][c:5]1[cH:6][c:7]([Cl:8])[c:9]([N:10]([CH2:11][C:12](=[O:13])[OH:14])[C:15](=[O:16])[O:17][CH2:18][c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[cH:25][c:26]1[OH:27]>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][c:7]([Cl:8])[c:9]([N:10]([CH2:11][C:12](=[O:13])[OH:14])[C:15](=...
CC(=O)OC(C)=O.O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl
CC(=O)Oc1cc(Cl)c(N(CC(=O)O)C(=O)OCc2ccccc2)cc1OC(C)=O
null
null
O
Acylation
OtherReaction
9fe842616fe8c5fa0bf72ff72cbb7e6f269a35f85453c588a379d45816b954fa
23705b28103bfefc76c3f909cff1028dc7a10b9fbc3b8b8a232f6d46c105cee3
O=C(Nc1ccccc1)OCc1ccccc1
[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-O-[C;H0;D3;+0:4](-[C;D1;H3:5])=[O;D1;H0:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10](-[OH;D1;+0:11]):[c:12]>>[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[O;H0;D2;+0:11]-[c:10](:[c:12]):[c:8](-[O;H0;D2;+0:7]-[C;H0;D3;+0:4](-[C;D1;H3:5])=[O;D1;H0:6]):[c:9]
null
[]
null
null
null
null
N-Benzyloxycarbonyl 2-chloro-4,5-dihydroxyphenylglycine (1.76 g, 5 mmole) in water (30 ml) and THF (20 ml) was adjusted to pH 7.5 with saturated sodium carbonate solution. Acetic anhydride (1.2 ml) was added and pH 6.5 maintained with saturated sodium carbonate solution, after 15 minutes and again after a further 15 mi...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aromatic alcohol.Aromatic alcohol
Ester.Ester
null
null
c1ccccc1.c1ccccc1
HO-
O
null
null
CC(=O)OC(C)=O.O=C(O)CN(C(=O)OCc1ccccc1)c1cc(O)c(O)cc1Cl>O>CC(=O)Oc1cc(Cl)c(N(CC(=O)O)C(=O)OCc2ccccc2)cc1OC(C)=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-114a2a5a1d2948c59ca0ec05a0544bd0
CCN1CCN(C(=O)NC(O)C(=O)O)C(=O)C1=O.Oc1ccc(Br)cc1O>>CCN1CCN(C(=O)NC(C(=O)O)c2cc(O)c(O)cc2Br)C(=O)C1=O
O=C1N(CCN(C1=O)CC)C(=O)NC(C(=O)O)O.BrC=1C=C(C(O)=CC1)O.C([O-])([O-])=O.[Na+].[Na+].C(C)(=O)OCC.C([O-])([O-])=O.[Na+].[Na+]>>O=C1N(CCN(C1=O)CC)C(=O)NC(C(=O)O)C1=C(C=C(C(=C1)O)O)Br
O[CH:10]([NH:9][C:7]([N:6]1[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[C:25](=[O:26])[C:23]1=[O:24])=[O:8])[C:11](=[O:12])[OH:13].[cH:14]1[cH:15][c:16]([OH:17])[c:18]([OH:19])[cH:20][c:21]1[Br:22]>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][N:6]([C:7](=[O:8])[NH:9][CH:10]([C:11](=[O:12])[OH:13])[c:14]2[cH:15][c:16]([OH:17])[c:18]([OH:...
CCN1CCN(C(=O)NC(O)C(=O)O)C(=O)C1=O.Oc1ccc(Br)cc1O
CCN1CCN(C(=O)NC(C(=O)O)c2cc(O)c(O)cc2Br)C(=O)C1=O
null
null
C(C)(=O)O.S(O)(O)(=O)=O
C-C Coupling
OtherReaction
353f6f3410bb939815e396d07868f2feb4b967c7c280d70099400ec8589322b5
7ccf8a4ec454d6cc03ce1e3efafa301b3c51d9e9635279e99312f4bc816939b8
O=C1NCCN(C(=O)NCc2ccccc2)C1=O
O-[CH;D3;+0:1](-[#7:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[C:6]=[O;D1;H0:7])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10].[Br;D1;H0:11]-[c:12](:[c:13]):[cH;D2;+0:14]:[c:15]:[c:16]>>[Br;D1;H0:11]-[c:12](:[c:13]):[c;H0;D3;+0:14](-[CH;D3;+0:1](-[#7:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[C:6]=[O;D1;H0:7])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]):[c:15]:[c:1...
null
[]
null
null
18
HOUR
4-Bromocatechol (4.77 g, 25.2 mmole) was added to an ice bath cooled suspension of N-(2,3-dioxo-4-ethylpiperazin-1-yl-carbonyl)-2-hydroxyglycine (2.59 g. 10 mmole) in glacial acetic acid (9 ml) and concentrated sulphuric acid (1 ml). The mixture was stirred for 18 hours then poured onto a mixture of ice, saturated sodi...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
c1ccccc1
c1ccccc1
C1C[NH]CC[NH]1.c1ccccc1
HO-
C(C)(=O)O.S(O)(O)(=O)=O
null
18
CCN1CCN(C(=O)NC(O)C(=O)O)C(=O)C1=O.Oc1ccc(Br)cc1O>C(C)(=O)O.S(O)(O)(=O)=O>CCN1CCN(C(=O)NC(C(=O)O)c2cc(O)c(O)cc2Br)C(=O)C1=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-dea297abfbc740adb41576c657c7bfec
CCN1CCN(C(=O)NC(O)C(=O)O)C(=O)C1=O.Oc1ccc(F)cc1O>>CCN1CCN(C(=O)NC(C(=O)O)c2cc(O)c(O)cc2F)C(=O)C1=O
FC=1C=C(C(O)=CC1)O.O=C1N(CCN(C1=O)CC)C(=O)NC(C(=O)O)O.C([O-])([O-])=O.[Na+].[Na+]>>OC1=CC(=C(C=C1O)C(NC(=O)N1C(C(N(CC1)CC)=O)=O)C(=O)O)F
O[CH:10]([NH:9][C:7]([N:6]1[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[C:25](=[O:26])[C:23]1=[O:24])=[O:8])[C:11](=[O:12])[OH:13].[cH:14]1[cH:15][c:16]([OH:17])[c:18]([OH:19])[cH:20][c:21]1[F:22]>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][N:6]([C:7](=[O:8])[NH:9][CH:10]([C:11](=[O:12])[OH:13])[c:14]2[cH:15][c:16]([OH:17])[c:18]([OH:1...
CCN1CCN(C(=O)NC(O)C(=O)O)C(=O)C1=O.Oc1ccc(F)cc1O
CCN1CCN(C(=O)NC(C(=O)O)c2cc(O)c(O)cc2F)C(=O)C1=O
null
null
O.C(C)(=O)O.S(O)(O)(=O)=O
C-C Coupling
OtherReaction
353f6f3410bb939815e396d07868f2feb4b967c7c280d70099400ec8589322b5
7ccf8a4ec454d6cc03ce1e3efafa301b3c51d9e9635279e99312f4bc816939b8
O=C1NCCN(C(=O)NCc2ccccc2)C1=O
O-[CH;D3;+0:1](-[#7:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[C:6]=[O;D1;H0:7])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10].[F;D1;H0:11]-[c:12](:[c:13]):[cH;D2;+0:14]:[c:15]:[c:16]>>[F;D1;H0:11]-[c:12](:[c:13]):[c;H0;D3;+0:14](-[CH;D3;+0:1](-[#7:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[C:6]=[O;D1;H0:7])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]):[c:15]:[c:16]
null
[]
null
null
8
HOUR
4-Fluorocatechol (3.06 g., 24 mmole) was added to a suspension of N-(2,3-dioxo-4-ethylpiperazin-1-ylcarbonyl)-2-hydroxyglycine (3.89 g, 15 mmole) in glacial acetic acid (13.5 ml) and concentrated sulphuric acid (1.5 ml). The mixture was stirred overnight, diluted with water (50 ml), adjusted to pH6 with saturated sodiu...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
c1ccccc1
c1ccccc1
C1C[NH]CC[NH]1.c1ccccc1
HO-
O.C(C)(=O)O.S(O)(O)(=O)=O
null
8
CCN1CCN(C(=O)NC(O)C(=O)O)C(=O)C1=O.Oc1ccc(F)cc1O>O.C(C)(=O)O.S(O)(O)(=O)=O>CCN1CCN(C(=O)NC(C(=O)O)c2cc(O)c(O)cc2F)C(=O)C1=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a6cb9adcc92d41e3970945481aec0a42
O=C(O)c1ccc(C(=O)O)c2c(C(=O)O)ccc(C(=O)O)c12>>O=C(O)c1ccc(C(=O)O)c2c3ccc(c(=O)oc3=O)c12
C1=CC=C2C=CC3=CC=CC4=CC=C1C2=C34.C1(=CC=C(C=2C(=CC=C(C12)C(=O)O)C(=O)O)C(=O)O)C(=O)O>>C12=CC=C(C=3C(=CC=C(C13)C(=O)O)C(=O)O)C(=O)OC2=O
O[C:16]([c:15]1[cH:14][cH:13][c:12]([C:19]([OH:18])=[O:20])[c:11]2[c:7]([C:8](=[O:9])[OH:10])[cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[c:21]21)=[O:17]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[OH:10])[c:11]2[c:12]3[cH:13][cH:14][c:15]([c:16](=[O:17])[o:18][c:19]3=[O:20])[c:21]12
O=C(O)c1ccc(C(=O)O)c2c(C(=O)O)ccc(C(=O)O)c12
O=C(O)c1ccc(C(=O)O)c2c3ccc(c(=O)oc3=O)c12
null
null
null
Aromatic Heterocycle Formation
OtherReaction
934f8084f78d0d57668b9bdfb8c4a326135833bbaa40eb5b5508d2fbbfa357fe
63a2bae03e4c021ca09a5731c2cc874376b3b6ed89490f90594503c6ca351cff
O=c1oc(=O)c2ccc1c1ccccc21
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[c:6](-[C;H0;D3;+0:7](=[O;D1;H0:8])-[OH;D1;+0:9]):[c:10]:[c:11]:1>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[o;H0;D2;+0:9]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[c:6]2:[c:10]:[c:11]:[c:3]:1:[c:4]:[c:5]:2
null
[]
null
null
null
null
The 1,3,6,8-tetrabromopyrene is obtained in an amount of 564 parts and a purity of about 83%, which corresponds to a yield of about 2% of theory, based on 100% pure pyrene, which on further processing to naphthalene-1,4,5,8-tetracarboxylic acid gives 258 parts of naphthalene-1,4,5,8-tetracarboxylic 1,4-monoanhydride. C...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid
null
c1ccc2ccccc2c1
C1=c2ccc(c3ccccc23)=CO1
C1=c2ccc(c3ccccc23)=CO1
HO-
null
null
null
O=C(O)c1ccc(C(=O)O)c2c(C(=O)O)ccc(C(=O)O)c12>>O=C(O)c1ccc(C(=O)O)c2c3ccc(c(=O)oc3=O)c12
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-dad2eed20186402398cc850a972487d1
C=CCS.CC(=O)OC1CC(=O)N1>>C=CCSC1CC(=O)N1
[OH-].[Na+].C(C=C)S.C(C)(=O)OC1CC(N1)=O>>C(C=C)SC1CC(N1)=O
[CH2:1]=[CH:2][CH2:3][SH:4].CC(=O)O[CH:5]1[CH2:6][C:7](=[O:8])[NH:9]1>>[CH2:1]=[CH:2][CH2:3][S:4][CH:5]1[CH2:6][C:7](=[O:8])[NH:9]1
C=CCS.CC(=O)OC1CC(=O)N1
C=CCSC1CC(=O)N1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
20eec362e306239fc5d47a6d83bf174290e0e0295dfb6eb5816503ddec5d1c06
42b46623e04892eb7ae9d9dbbd3cf095172c8c83bd28d92882cec40cddf86ad3
O=C1CCN1
C-C(=O)-O-[CH;D3;+0:1]1-[#7:2]-[C:3](=[O;D1;H0:4])-[C:5]-1.[C;D1;H2:6]=[C:7]-[C:8]-[SH;D1;+0:9]>>[C;D1;H2:6]=[C:7]-[C:8]-[S;H0;D2;+0:9]-[CH;D3;+0:1]1-[#7:2]-[C:3](=[O;D1;H0:4])-[C:5]-1
null
[]
null
null
30
MINUTE
A solution of 42.9 g of sodium hydroxide in 500 ml of water was made up under nitrogen and cooled to room temperature, 108 ml of allyl mercaptan was added and the mixture stirred under nitrogen for 30 minutes. 138.7 g of 4-acetoxyazetidin-2-one was added to the mixture over 10 minutes under nitrogen and the reaction mi...
10.6084/m9.figshare.5104873.v1
null
Ester.Aliphatic thiol
Monosulfide
C1CNC1
C1CNC1
C1CNC1
HO-
O
null
0.5
C=CCS.CC(=O)OC1CC(=O)N1>O>C=CCSC1CC(=O)N1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2367364d91d348c0b828b1a5a79f548f
C=CCSC1CC(=O)N1.O=C([O-])C(Br)Cc1ccc([N+](=O)[O-])cc1>>C=CCSC1CC(=O)N1CC(=O)OCc1ccc([N+](=O)[O-])cc1
O.CN(C=O)C.C([O-])([O-])=O.[K+].[K+].[N+](=O)([O-])C1=CC=C(CC(C(=O)[O-])Br)C=C1.C(C=C)SC1CC(N1)=O.CN(C=O)C>>C(C=C)SC1CC(N1CC(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])=O
[CH2:1]=[CH:2][CH2:3][S:4][CH:5]1[CH2:6][C:7](=[O:8])[NH:9]1.Br[CH:10]([C:11](=[O:12])[O-:13])[CH2:14][c:15]1[cH:16][cH:17][c:18]([N+:19](=[O:20])[O-:21])[cH:22][cH:23]1>>[CH2:1]=[CH:2][CH2:3][S:4][CH:5]1[CH2:6][C:7](=[O:8])[N:9]1[CH2:10][C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][c:18]([N+:19](=[O:20])[O-:21])[...
C=CCSC1CC(=O)N1.O=C([O-])C(Br)Cc1ccc([N+](=O)[O-])cc1
C=CCSC1CC(=O)N1CC(=O)OCc1ccc([N+](=O)[O-])cc1
null
null
null
Functional Group Addition
OtherReaction
545cf93159254a46658cf2484b35c86399ce672b29d96daabbd4f480b69288e9
8ba69f4a715d9692dba0f9562b4fc4e2d2e9c98051fdd8045bc3496c17eac722
O=C(CN1CCC1=O)OCc1ccccc1
Br-[CH;D3;+0:1](-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5])-[C:6](-[O-;H0;D1:7])=[O;D1;H0:8].[#16:9]-[C:10]1-[C:11]-[C:12](=[O;D1;H0:13])-[NH;D2;+0:14]-1>>[#16:9]-[C:10]1-[C:11]-[C:12](=[O;D1;H0:13])-[N;H0;D3;+0:14]-1-[CH2;D2;+0:1]-[C:6](=[O;D1;H0:8])-[O;H0;D2;+0:7]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
5
MINUTE
11.5 g of 4-nitrobenzylbromoacetate in 30 ml of dimethylformamide was added to 5.0 g of 4-allylthioazetidin-2-one dissolved in 70 ml of dimethylformamide with stirring under argon at room temperature. After 5 mins, 10.61 g of potassium carbonate was added to the solution. During the following 20 mins there was a colour...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary amide
Ester.Tertiary amide
C1CNC1
C1C[NH]C1
C1C[NH]C1.c1ccccc1
Br-
null
null
0.083333
C=CCSC1CC(=O)N1.O=C([O-])C(Br)Cc1ccc([N+](=O)[O-])cc1>>C=CCSC1CC(=O)N1CC(=O)OCc1ccc([N+](=O)[O-])cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2a15c84a63fd4fae939388f85b41aae4
C=CCSC1CC(=O)N1CC(=O)OC>>C=CCSC1CC(=O)N1CC(=O)O
[OH-].[K+].C(C=C)SC1CC(N1CC(=O)OC)=O.Cl>>C(C=C)SC1CC(N1CC(=O)O)=O
C[O:13][C:11]([CH2:10][N:9]1[CH:5]([S:4][CH2:3][CH:2]=[CH2:1])[CH2:6][C:7]1=[O:8])=[O:12]>>[CH2:1]=[CH:2][CH2:3][S:4][CH:5]1[CH2:6][C:7](=[O:8])[N:9]1[CH2:10][C:11](=[O:12])[OH:13]
C=CCSC1CC(=O)N1CC(=O)OC
C=CCSC1CC(=O)N1CC(=O)O
null
null
O.C(C)O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1CCN1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
null
null
null
null
2.34 g of potassium hydroxide dissolved in a mixture of 285 ml of ethanol and 15 ml of water was added to 6.0 g of methyl 2-(4-allylthioazetidin-2-on-1-yl)acetate with stirring at room temperature. The solution was poured into 720 ml 1M hydrochloric acid, extracted into dichloromethane (2×650 ml), the organic layer ext...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1C[NH]C1
Other
O.C(C)O
null
null
C=CCSC1CC(=O)N1CC(=O)OC>O.C(C)O>C=CCSC1CC(=O)N1CC(=O)O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-8d0305e3f8b44de28230f95fd82629e7
Cc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1>>Cc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1
O=C1CC2SC(=C(N12)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])OC1=CC=C(C=C1)C.C([O-])(O)=O.[Na+]>>O=C1CC2SC(=C(N12)C(=O)[O-])OC1=CC=C(C=C1)C.[Na+]
O=[N+]([O-])c1ccc(C[O:11][C:9]([C:8]2=[C:7]([O:6][c:5]3[cH:4][cH:3][c:2]([CH3:1])[cH:19][cH:18]3)[S:17][CH:16]3[N:12]2[C:13](=[O:14])[CH2:15]3)=[O:10])cc1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([O:6][C:7]2=[C:8]([C:9](=[O:10])[O-:11])[N:12]3[C:13](=[O:14])[CH2:15][CH:16]3[S:17]2)[cH:18][cH:19]1
Cc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1
Cc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1
null
[Pd]
O1CCOCC1
Miscellaneous
Ester to carboxylate
44f4ca8fa6db8bf6ed2065c1ada1557da240f35fc0d170173f2ffb8dd19aae75
572c1e76b1abdca43e2a1bb50332b6c1ee49391ecad01eed2f9507f24676fa6d
O=C1CC2SC(Oc3ccccc3)=CN12
O=[N+](-[O-])-c1:c:c:c(-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4](=[C:5](-[#8:6])-[#16:7])-[#7:8]-[C:9]=[O;D1;H0:10]):c:c:1>>[#16:7]-[C:5](-[#8:6])=[C:4](-[C:2](-[O-;H0;D1:1])=[O;D1;H0:3])-[#7:8]-[C:9]=[O;D1;H0:10]
null
[]
null
null
90
MINUTE
To a solution of 53 mg of 4-nitrobenzyl 7-oxo-3-(4-tolyloxy)-4-thia-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylate in dioxan was added an aqueous solution of 10 mg of sodium bicarbonate, and 50 mg of palladium on charcoal (10%). The mixture was hydrogenated with shaking at 50 p.s.i. for 90 minutes. Conditions: See reactio...
10.6084/m9.figshare.5104873.v1
null
Ester.Nitro group
null
c1ccccc1
null
c1ccccc1.C1=CN2CCC2S1
HO-
[Pd].O1CCOCC1
null
1.5
Cc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1>[Pd].O1CCOCC1>Cc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-6d313810f4dd42a88f65f7287dd25216
Cc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1>>Cc1ccc(OC2=C(C(=O)O)N3C(=O)CC3S2)cc1
O=C1CC2SC(=C(N12)C(=O)[O-])OC1=CC=C(C=C1)C.[Na+].Cl>>O=C1CC2SC(=C(N12)C(=O)O)OC1=CC=C(C=C1)C
[CH3:1][c:2]1[cH:3][cH:4][c:5]([O:6][C:7]2=[C:8]([C:9](=[O:10])[O-:11])[N:12]3[C:13](=[O:14])[CH2:15][CH:16]3[S:17]2)[cH:18][cH:19]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([O:6][C:7]2=[C:8]([C:9](=[O:10])[OH:11])[N:12]3[C:13](=[O:14])[CH2:15][CH:16]3[S:17]2)[cH:18][cH:19]1
Cc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1
Cc1ccc(OC2=C(C(=O)O)N3C(=O)CC3S2)cc1
null
null
null
Reduction
Carboxylate to carboxylic acid
65edb34f59b888c9ecb87d6c8e9fd76d082de6afc49403d96c457f834c73148e
222e2311064b3cb906d6bdeba44711f5dada050c096bbbcc7b35038975f228e8
O=C1CC2SC(Oc3ccccc3)=CN12
[#16:1]-[C:2](-[#8:3])=[C:4](-[C:5](-[O-;H0;D1:6])=[O;D1;H0:7])-[#7:8]-[C:9]=[O;D1;H0:10]>>[#16:1]-[C:2](-[#8:3])=[C:4](-[C:5](=[O;D1;H0:7])-[OH;D1;+0:6])-[#7:8]-[C:9]=[O;D1;H0:10]
48.2
[{"value": 48.2, "product": "O=C1CC2SC(=C(N12)C(=O)O)OC1=CC=C(C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
An aqueous solution of 32 mg of sodium 7-oxo-3-(4-tolyloxy)-4-thia-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylate was acidified to pH 2.0 with dilute hydrochloric acid, and was then extracted with ethyl acetate. The organic layer was backwashed with water, and then dried and evaporated in vacuo to afford 14.3 mg of the ab...
10.6084/m9.figshare.5104873.v1
null
null
Carboxylic acid
null
null
c1ccccc1.C1=CN2CCC2S1
null
null
null
null
Cc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1>>Cc1ccc(OC2=C(C(=O)O)N3C(=O)CC3S2)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-ff18f171073b41e1bae56734e71a1c01
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccccc1>>O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
C(C=C)S(=O)C1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])C(=S)OC1=CC=CC=C1)=O.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>O=C1CC2SC(=C(N12)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])OC1=CC=CC=C1
C=CC[S:23](=O)[CH:24]1[CH2:25][C:26](=[O:27])[N:28]1[CH:14]([C:2](=[O:1])[O:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:15](=S)[O:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:14]1=[C:15]([O:16][c:...
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccccc1
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
09567d1fb0e06be53e411508137f88dfa4351f8b0b195081fb14c08fba224024
fdbe926d598ab340f45c824667ff03d3ad5a17b984102931fa7371ce5bc3bef4
O=C(OCc1ccccc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
C=C-C-[S;H0;D3;+0:1](=O)-[C:2]1-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-1-[CH;D3;+0:7](-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11])-[C;H0;D3;+0:12](=S)-[#8:13]-[c:14]>>[C:11]-[#8:10]-[C:8](=[O;D1;H0:9])-[C;H0;D3;+0:7]1=[C;H0;D3;+0:12](-[#8:13]-[c:14])-[S;H0;D2;+0:1]-[C:2]2-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-2-1
18
[{"value": 18.0, "product": "O=C1CC2SC(=C(N12)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])OC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 17.7, "product": "O=C1CC2SC(=C(N12)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])OC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred solution of 97 mg of 4-nitrobenzyl 2-(4-allylsulphinylazetidin-2-on-1-yl)-3-phenoxy-3-thioxopropionate and 52 mg of triphenylphosphine in 2 ml of dry dioxan was heated under an argon atmosphere under reflux for 15 minutes. The mixture was then evaporated in vacuo to dryness; chromatography over silica gel aff...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Thiocarbonyl.Sulfoxide.Allyl
Enamine.Ester.Ether.Monosulfide
null
C1=CN2CCC2S1
c1ccccc1.c1ccccc1.C1=CN2CCC2S1
Other
O1CCOCC1
null
null
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccccc1>O1CCOCC1>O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-5056db55fb364a0293765fbb38651319
O=C([O-])C1=C(Oc2ccccc2)SC2(Cc3ccc([N+](=O)[O-])cc3)CC(=O)N12>>O=C([O-])C1=C(Oc2ccccc2)SC2CC(=O)N12
[N+](=O)([O-])C1=CC=C(CC23SC(=C(N3C(C2)=O)C(=O)[O-])OC2=CC=CC=C2)C=C1.C([O-])(O)=O.[Na+]>>O=C1CC2SC(=C(N12)C(=O)[O-])OC1=CC=CC=C1.[Na+]
O=[N+]([O-])c1ccc(C[C:14]23[S:13][C:5]([O:6][c:7]4[cH:8][cH:9][cH:10][cH:11][cH:12]4)=[C:4]([C:2](=[O:1])[O-:3])[N:18]2[C:16](=[O:17])[CH2:15]3)cc1>>[O:1]=[C:2]([O-:3])[C:4]1=[C:5]([O:6][c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[S:13][CH:14]2[CH2:15][C:16](=[O:17])[N:18]12
O=C([O-])C1=C(Oc2ccccc2)SC2(Cc3ccc([N+](=O)[O-])cc3)CC(=O)N12
O=C([O-])C1=C(Oc2ccccc2)SC2CC(=O)N12
null
[Pd]
O1CCOCC1.O
Reduction
OtherReaction
1e1b471d1d417dd71781146706d5899f32e72e3e0d40425a6f5909f852d481ce
7c6218583be997f699d95dfe65a34b687b1d229c78ffd736b05621faf29962fe
O=C1CC2SC(Oc3ccccc3)=CN12
O=[N+](-[O-])-c1:c:c:c(-C-[C;H0;D4;+0:1]23-[#16:2]-[C:3](-[#8:4])=[C:5](-[C:6](-[O;-;D1;H0:7])=[O;D1;H0:8])-[#7:9]-2-[C:10](=[O;D1;H0:11])-[C:12]-3):c:c:1>>[#8:4]-[C:3]1=[C:5](-[C:6](-[O;-;D1;H0:7])=[O;D1;H0:8])-[#7:9]2-[C:10](=[O;D1;H0:11])-[C:12]-[CH;D3;+0:1]-2-[#16:2]-1
74.6
[{"value": 74.6, "product": "O=C1CC2SC(=C(N12)C(=O)[O-])OC1=CC=CC=C1.[Na+]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of a solution of 56 mg of 4-nitrobenzyl-7-oxo-3-phenoxy-4-thia-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylate in 3 ml of dioxan and 12.5 mg of sodium bicarbonate in 2 ml of water, and 10% palladium/charcoal was hydrogenated at 50 psi at 25° for 90 minutes. The mixture was then filtered through Celite, and lyophi...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Monosulfide
Monosulfide
c1ccccc1.C1=CN2CCC2S1
C1=CN2CCC2S1
c1ccccc1.C1=CN2CCC2S1
HO-
[Pd].O1CCOCC1.O
null
null
O=C([O-])C1=C(Oc2ccccc2)SC2(Cc3ccc([N+](=O)[O-])cc3)CC(=O)N12>[Pd].O1CCOCC1.O>O=C([O-])C1=C(Oc2ccccc2)SC2CC(=O)N12
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-8210441576984f24a7766ee8b616321d
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccccc1>>O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
C(C=C)S(=O)C1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])C(=S)OC1=CC=CC=C1)=O.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>O=C1CC2SC(=C(N12)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])OC1=CC=CC=C1
C=CC[S:23](=O)[CH:24]1[CH2:25][C:26](=[O:27])[N:28]1[CH:14]([C:2](=[O:1])[O:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:15](=S)[O:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:14]1=[C:15]([O:16][c:...
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccccc1
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
09567d1fb0e06be53e411508137f88dfa4351f8b0b195081fb14c08fba224024
fdbe926d598ab340f45c824667ff03d3ad5a17b984102931fa7371ce5bc3bef4
O=C(OCc1ccccc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
C=C-C-[S;H0;D3;+0:1](=O)-[C:2]1-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-1-[CH;D3;+0:7](-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11])-[C;H0;D3;+0:12](=S)-[#8:13]-[c:14]>>[C:11]-[#8:10]-[C:8](=[O;D1;H0:9])-[C;H0;D3;+0:7]1=[C;H0;D3;+0:12](-[#8:13]-[c:14])-[S;H0;D2;+0:1]-[C:2]2-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-2-1
17.3
[{"value": 17.3, "product": "O=C1CC2SC(=C(N12)C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])OC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
110
CELSIUS
null
null
A mixture of 1550 mg of 4-nitrobenzyl 2-(4-allylsulphinylazetidin-2-on-1-yl)-3-phenoxy-3-thioxo-propanate (containing 10% pivalic acid), 808 mg of triphenylphosphine and dioxan was heated under an argon atmosphere at 110° C. for 15 minutes. The mixture was evaporated in vacuo to dryness, and the resulting oil was chrom...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Thiocarbonyl.Sulfoxide.Allyl
Enamine.Ester.Ether.Monosulfide
null
C1=CN2CCC2S1
c1ccccc1.c1ccccc1.C1=CN2CCC2S1
Other
O1CCOCC1
110
null
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccccc1>O1CCOCC1>O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-0bc59737e03a4de3845a019af7b8aba5
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(OC)cc1)C(=O)C(C)(C)C>>C=CCS(=O)C1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(OC)cc1)C(=O)C(C)(C)C
C(C=C)SC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)OC)=O.ClC=1C=C(C(=O)OO)C=CC1>>C(C=C)S(=O)C1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)OC)=O
[CH2:1]=[CH:2][CH2:3][S:4][CH:6]1[CH2:7][C:8](=[O:9])[N:10]1[C:11]([C:12](=[S:13])[O:14][CH2:15][c:16]1[cH:17][cH:18][c:19]([N+:20](=[O:21])[O-:22])[cH:23][cH:24]1)=[C:25]([O:26][c:27]1[cH:28][cH:29][c:30]([O:31][CH3:32])[cH:33][cH:34]1)[C:35](=[O:36])[C:37]([CH3:38])([CH3:39])[CH3:40]>>[CH2:1]=[CH:2][CH2:3][S:4](=[O:5...
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(OC)cc1)C(=O)C(C)(C)C
C=CCS(=O)C1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(OC)cc1)C(=O)C(C)(C)C
null
null
C(C)(=O)OCC
Oxidation
Sulfanyl to sulfinyl
9edfaf6d72a81452ea8e3a1cdcb10a58409fff36608e97019e7273998b3d5373
f5f6bb6ca76a2267cd589767b4d67e7a17ab1ac383eeb6143dcd5d92e00e1b6a
O=C1CCN1C(=COc1ccccc1)C(=S)OCc1ccccc1
[C:1]=[C:2]-[#7:3]1-[C:4](-[S;H0;D2;+0:5]-[C:6]-[C:7]=[C;D1;H2:8])-[C:9]-[C:10]-1=[O;D1;H0:11]>>[C:1]=[C:2]-[#7:3]1-[C:4](-[S;H0;D3;+0:5](=[O;D1;H0:12])-[C:6]-[C:7]=[C;D1;H2:8])-[C:9]-[C:10]-1=[O;D1;H0:11]
62
[{"value": 62.0, "product": "C(C=C)S(=O)C1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 0.35 g of 4-nitrobenzyl 2-(4-allylthioazetidin-2-on-1-yl)-3-(4-methoxyphenoxy)-3-trimethylacetylthio-propenate in ethyl acetate at -78° C. was added a solution of 0.128 g of 80% m-chloroperoxybenzoic acid in ethyl acetate over 10 minutes. The reaction mixture was washed with saturated sodium bicarbonat...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Sulfoxide
null
null
C1C[NH]C1.c1ccccc1.c1ccccc1
null
C(C)(=O)OCC
null
null
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(OC)cc1)C(=O)C(C)(C)C>C(C)(=O)OCC>C=CCS(=O)C1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(OC)cc1)C(=O)C(C)(C)C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-40f7e92ac98a48628919c3bb7ab3d772
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccc(OC)cc1>>COc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1
C(C=C)S(=O)C1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])C(=S)OC1=CC=C(C=C1)OC)=O.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>COC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)OCC2=CC=C(C=C2)[N+](=O)[O-])C=C1
C=CC[S:28](=O)[CH:27]1[N:23]([CH:9]([C:8](=S)[O:7][c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:30][cH:29]2)[C:10](=[O:11])[O:12][CH2:13][c:14]2[cH:15][cH:16][c:17]([N+:18](=[O:19])[O-:20])[cH:21][cH:22]2)[C:24](=[O:25])[CH2:26]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([O:7][C:8]2=[C:9]([C:10](=[O:11])[O:12][CH2:13][c:14]3[cH:...
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccc(OC)cc1
COc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
09567d1fb0e06be53e411508137f88dfa4351f8b0b195081fb14c08fba224024
fdbe926d598ab340f45c824667ff03d3ad5a17b984102931fa7371ce5bc3bef4
O=C(OCc1ccccc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
C=C-C-[S;H0;D3;+0:1](=O)-[C:2]1-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-1-[CH;D3;+0:7](-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11])-[C;H0;D3;+0:12](=S)-[#8:13]-[c:14]>>[C:11]-[#8:10]-[C:8](=[O;D1;H0:9])-[C;H0;D3;+0:7]1=[C;H0;D3;+0:12](-[#8:13]-[c:14])-[S;H0;D2;+0:1]-[C:2]2-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-2-1
17.2
[{"value": 17.2, "product": "COC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)OCC2=CC=C(C=C2)[N+](=O)[O-])C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 422 mg of 4-nitrobenzyl 2-(4-allylsulphinylazetidin-2-on-1-yl)-3-(4-methoxyphenoxy)-3-thioxopropanate, 214 mg of triphenylphosphine, and dioxan was heated under an argon atmosphere at 100° for 15 minutes. Then, the mixture was evaporated in vacuo to dryness, and the resulting oil was chromatographed on sil...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Thiocarbonyl.Sulfoxide.Allyl
Enamine.Ester.Ether.Monosulfide
null
C1=CN2CCC2S1
c1ccccc1.c1ccccc1.C1=CN2CCC2S1
Other
O1CCOCC1
null
null
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccc(OC)cc1>O1CCOCC1>COc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-682a8533f4c743c19b88d6287889b659
COc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1>>COc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1
COC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)OCC2=CC=C(C=C2)[N+](=O)[O-])C=C1.C([O-])(O)=O.[Na+]>>COC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)[O-])C=C1.[Na+]
O=[N+]([O-])c1ccc(C[O:12][C:10]([C:9]2=[C:8]([O:7][c:6]3[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:20][cH:19]3)[S:18][CH:17]3[N:13]2[C:14](=[O:15])[CH2:16]3)=[O:11])cc1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([O:7][C:8]2=[C:9]([C:10](=[O:11])[O-:12])[N:13]3[C:14](=[O:15])[CH2:16][CH:17]3[S:18]2)[cH:19][cH:20]1
COc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1
COc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1
null
[Pd]
O1CCOCC1.O
Miscellaneous
Ester to carboxylate
44f4ca8fa6db8bf6ed2065c1ada1557da240f35fc0d170173f2ffb8dd19aae75
572c1e76b1abdca43e2a1bb50332b6c1ee49391ecad01eed2f9507f24676fa6d
O=C1CC2SC(Oc3ccccc3)=CN12
O=[N+](-[O-])-c1:c:c:c(-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4](=[C:5](-[#8:6])-[#16:7])-[#7:8]-[C:9]=[O;D1;H0:10]):c:c:1>>[#16:7]-[C:5](-[#8:6])=[C:4](-[C:2](-[O-;H0;D1:1])=[O;D1;H0:3])-[#7:8]-[C:9]=[O;D1;H0:10]
null
[]
null
null
null
null
A mixture of a solution of 60 mg of 4-nitrobenzyl 3-(4-methoxyphenoxy)-7-oxo-4-thia-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylate in dioxan and 15 mg of sodium bicarbonate in water, and 10% palladium/charcoal was hydrogenated at 50 psi at 25° for 60 minutes. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ester.Nitro group
null
c1ccccc1
null
c1ccccc1.C1=CN2CCC2S1
HO-
[Pd].O1CCOCC1.O
null
null
COc1ccc(OC2=C(C(=O)OCc3ccc([N+](=O)[O-])cc3)N3C(=O)CC3S2)cc1>[Pd].O1CCOCC1.O>COc1ccc(OC2=C(C(=O)[O-])N3C(=O)CC3S2)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-682bf859e96f4071bbb1d613564a3977
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C>>C=CCS(=O)C1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C
C(C=C)SC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)F)=O.ClC=1C=C(C(=O)OO)C=CC1>>C(C=C)S(=O)C1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)F)=O
[CH2:1]=[CH:2][CH2:3][S:4][CH:6]1[CH2:7][C:8](=[O:9])[N:10]1[C:11]([C:12](=[S:13])[O:14][CH2:15][c:16]1[cH:17][cH:18][c:19]([N+:20](=[O:21])[O-:22])[cH:23][cH:24]1)=[C:25]([O:26][c:27]1[cH:28][cH:29][c:30]([F:31])[cH:32][cH:33]1)[C:34](=[O:35])[C:36]([CH3:37])([CH3:38])[CH3:39]>>[CH2:1]=[CH:2][CH2:3][S:4](=[O:5])[CH:6]...
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C
C=CCS(=O)C1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C
null
null
C(C)(=O)OCC
Oxidation
Sulfanyl to sulfinyl
9edfaf6d72a81452ea8e3a1cdcb10a58409fff36608e97019e7273998b3d5373
f5f6bb6ca76a2267cd589767b4d67e7a17ab1ac383eeb6143dcd5d92e00e1b6a
O=C1CCN1C(=COc1ccccc1)C(=S)OCc1ccccc1
[C:1]=[C:2]-[#7:3]1-[C:4](-[S;H0;D2;+0:5]-[C:6]-[C:7]=[C;D1;H2:8])-[C:9]-[C:10]-1=[O;D1;H0:11]>>[C:1]=[C:2]-[#7:3]1-[C:4](-[S;H0;D3;+0:5](=[O;D1;H0:12])-[C:6]-[C:7]=[C;D1;H2:8])-[C:9]-[C:10]-1=[O;D1;H0:11]
58.3
[{"value": 58.3, "product": "C(C=C)S(=O)C1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 4.0 g of 4-nitrobenzyl 2-(4-allylthioazetidin-2-on-1-yl)-3-(4-fluorophenoxy)-3-trimethylacetylthio-propenate in ethyl acetate at -78° was added a solution of 1.5 g of 80% m-chloroperoxybenzoic acid in ethyl acetate over 10 minutes. The reaction mixture was washed with saturated sodium bicarbonate solut...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Sulfoxide
null
null
C1C[NH]C1.c1ccccc1.c1ccccc1
null
C(C)(=O)OCC
null
null
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C>C(C)(=O)OCC>C=CCS(=O)C1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-6d1cb58153a64ec1b34fdc9b4d50e442
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccc(F)cc1>>O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(F)cc2)SC2CC(=O)N12
C(C=C)S(=O)C1CC(N1C(C(=O)OCC1=CC=C(C=C1)[N+](=O)[O-])C(=S)OC1=CC=C(C=C1)F)=O.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>FC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)OCC2=CC=C(C=C2)[N+](=O)[O-])C=C1
C=CC[S:24](=O)[CH:25]1[CH2:26][C:27](=[O:28])[N:29]1[CH:14]([C:2](=[O:1])[O:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:15](=S)[O:16][c:17]1[cH:18][cH:19][c:20]([F:21])[cH:22][cH:23]1>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][cH:13]1)[C:14]1=[C:15]([O...
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccc(F)cc1
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(F)cc2)SC2CC(=O)N12
null
null
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
09567d1fb0e06be53e411508137f88dfa4351f8b0b195081fb14c08fba224024
fdbe926d598ab340f45c824667ff03d3ad5a17b984102931fa7371ce5bc3bef4
O=C(OCc1ccccc1)C1=C(Oc2ccccc2)SC2CC(=O)N12
C=C-C-[S;H0;D3;+0:1](=O)-[C:2]1-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-1-[CH;D3;+0:7](-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11])-[C;H0;D3;+0:12](=S)-[#8:13]-[c:14]>>[C:11]-[#8:10]-[C:8](=[O;D1;H0:9])-[C;H0;D3;+0:7]1=[C;H0;D3;+0:12](-[#8:13]-[c:14])-[S;H0;D2;+0:1]-[C:2]2-[C:3]-[C:4](=[O;D1;H0:5])-[#7:6]-2-1
12.3
[{"value": 12.3, "product": "FC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)OCC2=CC=C(C=C2)[N+](=O)[O-])C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1.15 g of 4-nitrobenzyl 2-(4-allylsulphinylazetidin-2-on-1-yl)-3-(4-fluorophenoxy)-3-thioxo-propanate, 600 mg of triphenylphosphine, and dioxan was heated under an argon atmosphere at 100° for 15 minutes. Then, the mixture was evaporated in vacuo to dryness, and the resulting oil was chromatographed on sil...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Thiocarbonyl.Sulfoxide.Allyl
Enamine.Ester.Ether.Monosulfide
null
C1=CN2CCC2S1
c1ccccc1.c1ccccc1.C1=CN2CCC2S1
Other
O1CCOCC1
null
null
C=CCS(=O)C1CC(=O)N1C(C(=O)OCc1ccc([N+](=O)[O-])cc1)C(=S)Oc1ccc(F)cc1>O1CCOCC1>O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(F)cc2)SC2CC(=O)N12
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-bbae89eeb1164984848e253d3e573545
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(F)cc2)SC2CCN12>>O=C([O-])C1=C(Oc2ccc(F)cc2)SC2CC(=O)N12
FC1=CC=C(OC2=C(N3CCC3S2)C(=O)OCC2=CC=C(C=C2)[N+](=O)[O-])C=C1.C([O-])(O)=O.[Na+]>>FC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)[O-])C=C1.[Na+]
O=[N+]([O-])c1ccc(C[O:3][C:2](=[O:1])[C:4]2=[C:5]([O:6][c:7]3[cH:8][cH:9][c:10]([F:11])[cH:12][cH:13]3)[S:14][CH:15]3[CH2:16][CH2:17][N:19]23)cc1>>[O:1]=[C:2]([O-:3])[C:4]1=[C:5]([O:6][c:7]2[cH:8][cH:9][c:10]([F:11])[cH:12][cH:13]2)[S:14][CH:15]2[CH2:16][C:17](=[O:18])[N:19]12
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(F)cc2)SC2CCN12
O=C([O-])C1=C(Oc2ccc(F)cc2)SC2CC(=O)N12
null
[Pd]
O1CCOCC1.O
Functional Group Interconversion
OtherReaction
e822a636698cf3ba88c05a1f82fd94d3583383d400ee627bc2b661c38f2052de
4690ed478d743360ccffbea7bd2623366965e371cf2283ac8c3868d9bc115d2f
O=C1CC2SC(Oc3ccccc3)=CN12
O=[N+](-[O-])-c1:c:c:c(-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]2=[C:5](-[#8:6])-[#16:7]-[C:8]3-[C:9]-[CH2;D2;+0:10]-[#7:11]-3-2):c:c:1>>[#8:6]-[C:5]1=[C:4](-[C:2](-[O-;H0;D1:1])=[O;D1;H0:3])-[#7:11]2-[C:8](-[#16:7]-1)-[C:9]-[C;H0;D3;+0:10]-2=[O;D1;H0:12]
95.5
[{"value": 95.5, "product": "FC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)[O-])C=C1.[Na+]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of a solution of 500 mg of 4-nitrobenzyl 3-(4-fluorophenoxy)-4-thia-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylate in dioxan and 101 mg of sodium bicarbonate in water, and 10% palladium/charcoal was hydrogenated at 50 psi at 25° for 60 minutes. Then the reaction mixture was filtered through Celite, and then lyop...
10.6084/m9.figshare.5104873.v1
null
Ester.Nitro group
Tertiary amide
c1ccccc1.C1=CN2CCC2S1
C1=CN2CCC2S1
c1ccccc1.C1=CN2CCC2S1
HO-
[Pd].O1CCOCC1.O
null
null
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(F)cc2)SC2CCN12>[Pd].O1CCOCC1.O>O=C([O-])C1=C(Oc2ccc(F)cc2)SC2CC(=O)N12
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-e9f382e08b304749b5efb94d5aeae9b9
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C.ClCl>>CC(C)(C)C(=O)C(Oc1ccc(F)cc1)=C(C(=S)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
C(C=C)SC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)F)=O.ClCl>>ClC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)F)=O
C=CCS[CH:34]1[N:30]([C:16](=[C:7]([C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[O:6])[O:8][c:9]2[cH:10][cH:11][c:12]([F:13])[cH:14][cH:15]2)[C:17](=[S:18])[O:19][CH2:20][c:21]2[cH:22][cH:23][c:24]([N+:25](=[O:26])[O-:27])[cH:28][cH:29]2)[C:31](=[O:32])[CH2:33]1.Cl[Cl:35]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[O:6])[C:7]([O:8]...
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C.ClCl
CC(C)(C)C(=O)C(Oc1ccc(F)cc1)=C(C(=S)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
null
null
ClCCl.C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
OtherReaction
d4a1f45948ca6338d13758a8eb064414f490d5560b79b989b8f902e12590b6c8
7fecd9068ed121180c7c8f39a016405d4e3d2c3ae4d3dd36c097f13d461df37e
O=C1CCN1C(=COc1ccccc1)C(=S)OCc1ccccc1
C=C-C-S-[CH;D3;+0:1]1-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-1-[C:6](-[C:7](-[#8:8])=[S;D1;H0:9])=[C:10](-[#8:11])-[C:12]=[O;D1;H0:13].Cl-[Cl;H0;D1;+0:14]>>[#8:8]-[C:7](=[S;D1;H0:9])-[C:6](-[#7:5]1-[C:3](=[O;D1;H0:4])-[C:2]-[CH;D3;+0:1]-1-[Cl;H0;D1;+0:14])=[C:10](-[#8:11])-[C:12]=[O;D1;H0:13]
68.5
[{"value": 68.5, "product": "ClC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 7.2 g of 4-nitrobenzyl 2-(4-allylthioazetidin-2-on-1-yl)-3-(4-fluorophenoxy)-3-trimethylacetylthio-propenate (prepared as described in Example 25) in dichloromethane at -20°, was added a solution of 25 mmol of chlorine in carbon tetrachloride. After 30 minutes the mixture was warmed to room temperature...
10.6084/m9.figshare.5104873.v1
null
Monosulfide.Allyl
Secondary halide
C1C[NH]C1
C1C[NH]C1
c1ccccc1.c1ccccc1.C1C[NH]C1
HCl
ClCCl.C(Cl)(Cl)(Cl)Cl
null
null
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(F)cc1)C(=O)C(C)(C)C.ClCl>ClCCl.C(Cl)(Cl)(Cl)Cl>CC(C)(C)C(=O)C(Oc1ccc(F)cc1)=C(C(=S)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-bee91b55d88744178ee3531d3b46f27f
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(Cl)cc1)C(=O)C(C)(C)C.ClCl>>CC(C)(C)C(=O)C(Oc1ccc(Cl)cc1)=C(C(=S)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
C(C=C)SC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)Cl)=O.ClCl>>ClC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)Cl)=O
C=CCS[CH:34]1[N:30]([C:16](=[C:7]([C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[O:6])[O:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]2)[C:17](=[S:18])[O:19][CH2:20][c:21]2[cH:22][cH:23][c:24]([N+:25](=[O:26])[O-:27])[cH:28][cH:29]2)[C:31](=[O:32])[CH2:33]1.Cl[Cl:35]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[O:6])[C:7]([O:8...
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(Cl)cc1)C(=O)C(C)(C)C.ClCl
CC(C)(C)C(=O)C(Oc1ccc(Cl)cc1)=C(C(=S)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
null
null
ClCCl.C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
OtherReaction
d4a1f45948ca6338d13758a8eb064414f490d5560b79b989b8f902e12590b6c8
7fecd9068ed121180c7c8f39a016405d4e3d2c3ae4d3dd36c097f13d461df37e
O=C1CCN1C(=COc1ccccc1)C(=S)OCc1ccccc1
C=C-C-S-[CH;D3;+0:1]1-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-1-[C:6](-[C:7](-[#8:8])=[S;D1;H0:9])=[C:10](-[#8:11])-[C:12]=[O;D1;H0:13].Cl-[Cl;H0;D1;+0:14]>>[#8:8]-[C:7](=[S;D1;H0:9])-[C:6](-[#7:5]1-[C:3](=[O;D1;H0:4])-[C:2]-[CH;D3;+0:1]-1-[Cl;H0;D1;+0:14])=[C:10](-[#8:11])-[C:12]=[O;D1;H0:13]
64.2
[{"value": 64.2, "product": "ClC1CC(N1C(C(=S)OCC1=CC=C(C=C1)[N+](=O)[O-])=C(C(C(C)(C)C)=O)OC1=CC=C(C=C1)Cl)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 0.5 g of 4-nitrobenzyl 2-(4-allylthioazetidin-2-on-1-yl)-3-(4-chlorophenoxy)-3-trimethylacetylthio-propenate in dichloromethane at -20° C. was added a solution of 1.7 mmol chlorine in carbon tetrachloride. After 30 minutes the mixture was warmed to room temperature, evaporated in vacuo, and the residua...
10.6084/m9.figshare.5104873.v1
null
Monosulfide.Allyl
Secondary halide
C1C[NH]C1
C1C[NH]C1
c1ccccc1.c1ccccc1.C1C[NH]C1
HCl
ClCCl.C(Cl)(Cl)(Cl)Cl
null
null
C=CCSC1CC(=O)N1C(C(=S)OCc1ccc([N+](=O)[O-])cc1)=C(Oc1ccc(Cl)cc1)C(=O)C(C)(C)C.ClCl>ClCCl.C(Cl)(Cl)(Cl)Cl>CC(C)(C)C(=O)C(Oc1ccc(Cl)cc1)=C(C(=S)OCc1ccc([N+](=O)[O-])cc1)N1C(=O)CC1Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2acad378d87448b983c09932cd48ed7b
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(Cl)cc2)SC2CCN12>>O=C([O-])C1=C(Oc2ccc(Cl)cc2)SC2CC(=O)N12
ClC1=CC=C(OC2=C(N3CCC3S2)C(=O)OCC2=CC=C(C=C2)[N+](=O)[O-])C=C1.C([O-])(O)=O.[Na+]>>ClC1=CC=C(OC2=C(N3C(CC3S2)=O)C(=O)[O-])C=C1.[Na+]
O=[N+]([O-])c1ccc(C[O:3][C:2](=[O:1])[C:4]2=[C:5]([O:6][c:7]3[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]3)[S:14][CH:15]3[CH2:16][CH2:17][N:19]23)cc1>>[O:1]=[C:2]([O-:3])[C:4]1=[C:5]([O:6][c:7]2[cH:8][cH:9][c:10]([Cl:11])[cH:12][cH:13]2)[S:14][CH:15]2[CH2:16][C:17](=[O:18])[N:19]12
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(Cl)cc2)SC2CCN12
O=C([O-])C1=C(Oc2ccc(Cl)cc2)SC2CC(=O)N12
null
[Pd]
O1CCOCC1.O
Functional Group Interconversion
OtherReaction
e822a636698cf3ba88c05a1f82fd94d3583383d400ee627bc2b661c38f2052de
4690ed478d743360ccffbea7bd2623366965e371cf2283ac8c3868d9bc115d2f
O=C1CC2SC(Oc3ccccc3)=CN12
O=[N+](-[O-])-c1:c:c:c(-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]2=[C:5](-[#8:6])-[#16:7]-[C:8]3-[C:9]-[CH2;D2;+0:10]-[#7:11]-3-2):c:c:1>>[#8:6]-[C:5]1=[C:4](-[C:2](-[O-;H0;D1:1])=[O;D1;H0:3])-[#7:11]2-[C:8](-[#16:7]-1)-[C:9]-[C;H0;D3;+0:10]-2=[O;D1;H0:12]
null
[]
null
null
null
null
A mixture of a solution of 500 mg of 4-nitrobenzyl 3-(4-chlorophenoxy)-4-thia-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylate in dioxan and 97 mg of sodium bicarbonate in water, and 10% palladium/charcoal was hydrogenated at 50 psi at 25° for 60 minutes. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
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Ester.Nitro group
Tertiary amide
c1ccccc1.C1=CN2CCC2S1
C1=CN2CCC2S1
c1ccccc1.C1=CN2CCC2S1
HO-
[Pd].O1CCOCC1.O
null
null
O=C(OCc1ccc([N+](=O)[O-])cc1)C1=C(Oc2ccc(Cl)cc2)SC2CCN12>[Pd].O1CCOCC1.O>O=C([O-])C1=C(Oc2ccc(Cl)cc2)SC2CC(=O)N12