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-018fd0e1351f4fd09b20fcddd97b4c7a
ord-974d91301ba44ad1ab30f6b6ace60cf9
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC>>COC(=O)CC(C)(C)C=CC(Cl)(Br)C(F)(F)F
BrC(C(C=C(C)C)O)(C(F)(F)F)Cl.C(C)(OC)(OC)OC>>BrC(C=CC(CC(=O)OC)(C)C)(C(F)(F)F)Cl
O[CH:10]([CH:9]=[C:6]([CH3:7])[CH3:8])[C:11]([Cl:12])([Br:13])[C:14]([F:15])([F:16])[F:17].CO[C:3]([O:2][CH3:1])([O:4]C)[CH3:5]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][C:6]([CH3:7])([CH3:8])[CH:9]=[CH:10][C:11]([Cl:12])([Br:13])[C:14]([F:15])([F:16])[F:17]
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC
COC(=O)CC(C)(C)C=CC(Cl)(Br)C(F)(F)F
null
O.[O-2].[O-2].[O-2].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.[Al+3].[Al+3]
null
Acylation
OtherReaction
62d15542be43b94a80da01568db53380356499d771ca28bc7e0ff722d34a5863
98ff49def7e6e395079390a512d545b9d4d6c593686e816bc1a43a7ae419027a
null
C-O-[C;H0;D4;+0:1](-[CH3;D1;+0:2])(-[#8:3]-[C;D1;H3:4])-[O;H0;D2;+0:5]-C.O-[CH;D3;+0:6](-[CH;D2;+0:7]=[C;H0;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10])-[C:11](-[Br;D1;H0:12])(-[Cl;D1;H0:13])-[C:14](-[F;D1;H0:15])(-[F;D1;H0:16])-[F;D1;H0:17]>>[Br;D1;H0:12]-[C:11](-[Cl;D1;H0:13])(-[CH;D2;+0:6]=[CH;D2;+0:7]-[C;H0;D4;+0:8](-[C;D1...
65
[{"value": 59.0, "product": "BrC(C=CC(CC(=O)OC)(C)C)(C(F)(F)F)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.0, "product": "BrC(C=CC(CC(=O)OC)(C)C)(C(F)(F)F)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
111
CELSIUS
1
HOUR
5-Bromo-5-chloro-4-hydroxy-2-methyl-6,6,6-trifluorohex-2-ene (10.0 g), trimethyl orthoacetate (16.0 g) and Montmorillonite KSF (0.5 g) were charged to a round-bottomed flask fitted with: nitrogen inlet/bubbler, thermometer and still-head. The mixture was heated with agitation, and the methanol-trimethyl orthoacetate di...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Secondary alcohol
Ester
null
null
null
HO-
O.[O-2].[O-2].[O-2].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.[Al+3].[Al+3]
111
1
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC>O.[O-2].[O-2].[O-2].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.[Al+3].[Al+3]>COC(=O)CC(C)(C)C=CC(Cl)(Br)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4d77e42f5c494f69b479d484b8ed6d48
CC(C)=CC(O)C(Cl)(Cl)C(F)(F)F.CCOC(C)(OCC)OCC>>CCOC(=O)CC(C)(C)C=CC(Cl)(Cl)C(F)(F)F
C(C)(OCC)(OCC)OCC.ClC(C(C=C(C)C)O)(C(F)(F)F)Cl.C(C(C)C)(=O)O>>ClC(C=CC(CC(=O)OCC)(C)C)(C(F)(F)F)Cl
O[CH:11]([CH:10]=[C:7]([CH3:8])[CH3:9])[C:12]([Cl:13])([Cl:14])[C:15]([F:16])([F:17])[F:18].CCO[C:4]([O:3][CH2:2][CH3:1])([O:5]CC)[CH3:6]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7]([CH3:8])([CH3:9])[CH:10]=[CH:11][C:12]([Cl:13])([Cl:14])[C:15]([F:16])([F:17])[F:18]
CC(C)=CC(O)C(Cl)(Cl)C(F)(F)F.CCOC(C)(OCC)OCC
CCOC(=O)CC(C)(C)C=CC(Cl)(Cl)C(F)(F)F
null
null
null
Acylation
OtherReaction
62d15542be43b94a80da01568db53380356499d771ca28bc7e0ff722d34a5863
98ff49def7e6e395079390a512d545b9d4d6c593686e816bc1a43a7ae419027a
null
C-C-O-[C;H0;D4;+0:1](-[CH3;D1;+0:2])(-[#8:3]-[C:4])-[O;H0;D2;+0:5]-C-C.O-[CH;D3;+0:6](-[CH;D2;+0:7]=[C;H0;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10])-[C:11](-[Cl;D1;H0:12])(-[Cl;D1;H0:13])-[C:14](-[F;D1;H0:15])(-[F;D1;H0:16])-[F;D1;H0:17]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;H0;D1;+0:5])-[CH2;D2;+0:2]-[C;H0;D4;+0:8](-[C;D1;H3:9])...
null
[]
null
null
null
null
A mixture of triethyl orthoacetate (25 ml), 5,5-dichloro-4-hydroxy-2-methyl-6,6,6-trifluorohex-2-ene (3.5 g), and isobutyric acid (0.11 g) was heated at the reflux temperature. The refluxing volatiles were condensed and collected in a Dean & Stark apparatus containing molecular sieves (4A) to collect the by-product eth...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Secondary alcohol
Ester
null
null
null
HO-
null
null
null
CC(C)=CC(O)C(Cl)(Cl)C(F)(F)F.CCOC(C)(OCC)OCC>>CCOC(=O)CC(C)(C)C=CC(Cl)(Cl)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9878f8a1a69f4990b1191065d489c660
N#Cc1ccc(O)cc1.O=C([O-])C(F)(F)Cl>>N#Cc1ccc(OC(F)F)cc1
C(C)(=O)OCC.C(#N)C1=CC=C(C=C1)O.ClC(C(=O)[O-])(F)F.[Na+].[OH-].[Na+]>>FC(OC1=CC=C(C#N)C=C1)F
[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([OH:7])[cH:11][cH:12]1.O=C([O-])[C:8](Cl)([F:9])[F:10]>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH:8]([F:9])[F:10])[cH:11][cH:12]1
N#Cc1ccc(O)cc1.O=C([O-])C(F)(F)Cl
N#Cc1ccc(OC(F)F)cc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
76f211f5353542c9b838eb8e1b527f9863b90e0b018b98c3cf34f50f16bd6596
5bf13e9b56816027718c6488fc8075a60a5c356ea2671f45c1f3f8f299767493
c1ccccc1
Cl-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[F;D1;H0:3])-C(=O)-[O-].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
41
[{"value": 41.0, "product": "FC(OC1=CC=C(C#N)C=C1)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 40.8, "product": "FC(OC1=CC=C(C#N)C=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
4-Cyanophenol (0.50 g, 4.2 mmol, Aldrich), sodium chlorodifluoroacetate (0.77 g, 5 mmol, Alfa Products), and sodium hydroxide (0.20 g, 5 mmol) were combined in dry DMF (2 mL) under an atmosphere of argon. After stirring at 125°-130° C. for 5 h, the mixture was cooled to RT, ethyl acetate (50 mL) was added and the organ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Aromatic alcohol
Secondary halide.Secondary halide.Ether
null
null
c1ccccc1
Other
CN(C)C=O
null
5
N#Cc1ccc(O)cc1.O=C([O-])C(F)(F)Cl>CN(C)C=O>N#Cc1ccc(OC(F)F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b2d252a75b1947e3893ae5090ef4d0e4
O=C([O-])C(F)(F)Cl.O=[N+]([O-])c1ccc(O)cc1>>O=[N+]([O-])c1ccc(OC(F)F)cc1
[N+](=O)([O-])C1=CC=C(C=C1)O.ClC(C(=O)[O-])(F)F.[Na+].[OH-].[Na+]>>FC(OC1=CC=C(C=C1)[N+](=O)[O-])F
O=C([O-])[C:9](Cl)([F:10])[F:11].[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([OH:8])[cH:12][cH:13]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([O:8][CH:9]([F:10])[F:11])[cH:12][cH:13]1
O=C([O-])C(F)(F)Cl.O=[N+]([O-])c1ccc(O)cc1
O=[N+]([O-])c1ccc(OC(F)F)cc1
null
null
CN(C)C=O.O
Heteroatom Alkylation and Arylation
OtherReaction
76f211f5353542c9b838eb8e1b527f9863b90e0b018b98c3cf34f50f16bd6596
5bf13e9b56816027718c6488fc8075a60a5c356ea2671f45c1f3f8f299767493
c1ccccc1
Cl-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[F;D1;H0:3])-C(=O)-[O-].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
73.4
[{"value": 73.0, "product": "FC(OC1=CC=C(C=C1)[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.4, "product": "FC(OC1=CC=C(C=C1)[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
125
CELSIUS
1
HOUR
4-Nitrophenol (0.10 g, 0.72 mmol, Aldrich), sodium chlorodifluoroacetate (0.11 g, 0.72 mmol, Alfa Products) and sodium hydroxide (0.03 g, 0.72 mmol) were combined in dry DMF (1 mL) under an atmosphere of argon. After stirring at 125° C. for 1 h, the mixture was cooled to RT, was diluted with water and was extracted twi...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Aromatic alcohol
Secondary halide.Secondary halide.Ether
null
null
c1ccccc1
Other
CN(C)C=O.O
125
1
O=C([O-])C(F)(F)Cl.O=[N+]([O-])c1ccc(O)cc1>CN(C)C=O.O>O=[N+]([O-])c1ccc(OC(F)F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4972bb959a7b4018a8ed305bf737462c
COC(=O)C(F)(F)Cl.N#Cc1ccc(O)cc1>>N#Cc1ccc(OC(F)F)cc1
C(C)(=O)OCC.C(#N)C1=CC=C(C=C1)O.ClC(C(=O)OC)(F)F.C([O-])([O-])=O.[K+].[K+]>>FC(OC1=CC=C(C#N)C=C1)F
COC(=O)[C:8](Cl)([F:9])[F:10].[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([OH:7])[cH:11][cH:12]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH:8]([F:9])[F:10])[cH:11][cH:12]1
COC(=O)C(F)(F)Cl.N#Cc1ccc(O)cc1
N#Cc1ccc(OC(F)F)cc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
a71f3c9bdb498e0df7854c01d285462745eacb61fcde4051c28043b77fa1bd37
895b1d2fe77d134f12b38f8d837ea80b2e81ef793fb29282c01859f1f67233b7
c1ccccc1
C-O-C(=O)-[C;H0;D4;+0:1](-Cl)(-[F;D1;H0:2])-[F;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
53.2
[{"value": 53.0, "product": "FC(OC1=CC=C(C#N)C=C1)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.2, "product": "FC(OC1=CC=C(C#N)C=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
0.3
HOUR
4-Cyanophenol (0.12 G, 1.0 mmol, Aldrich), methyl chlorodifluoroacetate (0.29 g, 2.0 mmol, Aldrich) and potassium carbonate (0.29 g, 2.1 mmol) were combined in dry DMF (0.5 mL) under an argon atmosphere. After stirring at 75°-80° C. for 0.3 h, the mixture was cooled to RT, ethyl acetate (20 mL) was added and the organi...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Ester.Aromatic alcohol
Secondary halide.Secondary halide.Ether
null
null
c1ccccc1
HCl
CN(C)C=O
null
0.3
COC(=O)C(F)(F)Cl.N#Cc1ccc(O)cc1>CN(C)C=O>N#Cc1ccc(OC(F)F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-78322038f273421dabe49798105b950a
COC(=O)C(F)(F)Cl.O=[N+]([O-])c1ccc(O)cc1>>O=[N+]([O-])c1ccc(OC(F)F)cc1
C(C)(=O)OCC.[N+](=O)([O-])C1=CC=C(C=C1)O.ClC(C(=O)OC)(F)F.C([O-])([O-])=O.[K+].[K+]>>FC(OC1=CC=C(C=C1)[N+](=O)[O-])F
COC(=O)[C:9](Cl)([F:10])[F:11].[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([OH:8])[cH:12][cH:13]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([O:8][CH:9]([F:10])[F:11])[cH:12][cH:13]1
COC(=O)C(F)(F)Cl.O=[N+]([O-])c1ccc(O)cc1
O=[N+]([O-])c1ccc(OC(F)F)cc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
a71f3c9bdb498e0df7854c01d285462745eacb61fcde4051c28043b77fa1bd37
895b1d2fe77d134f12b38f8d837ea80b2e81ef793fb29282c01859f1f67233b7
c1ccccc1
C-O-C(=O)-[C;H0;D4;+0:1](-Cl)(-[F;D1;H0:2])-[F;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
65
[{"value": 65.0, "product": "FC(OC1=CC=C(C=C1)[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.5, "product": "FC(OC1=CC=C(C=C1)[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
0.5
HOUR
4-Nitrophenol (0.14 g, 1.0 mmol, Aldrich), methyl chlorodifluoroacetate (0.29 g, 2.0 mmol, Aldrich) and potassium carbonate (0.29 g, 2.1 mmol) were combined in dry DMF (0.5 mL) under an argon atmosphere. After stirring at 95°-100° C. for 0.5 h, the mixture was cooled to RT, ethyl acetate (20 mL) was added and the organ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Ester.Aromatic alcohol
Secondary halide.Secondary halide.Ether
null
null
c1ccccc1
HCl
CN(C)C=O
null
0.5
COC(=O)C(F)(F)Cl.O=[N+]([O-])c1ccc(O)cc1>CN(C)C=O>O=[N+]([O-])c1ccc(OC(F)F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e57e5ba30ba5446d9ef33fda5e7bc0ab
COC(=O)C(F)(F)Cl.O=Cc1ccc(O)c(O)c1>>O=Cc1ccc(OC(F)F)c(O)c1
OC=1C=C(C=O)C=CC1O.ClC(C(=O)OC)(F)F.C([O-])([O-])=O.[K+].[K+]>>FC(OC1=C(C=C(C=O)C=C1)O)F
COC(=O)[C:8](Cl)([F:9])[F:10].[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([OH:7])[c:11]([OH:12])[cH:13]1>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH:8]([F:9])[F:10])[c:11]([OH:12])[cH:13]1
COC(=O)C(F)(F)Cl.O=Cc1ccc(O)c(O)c1
O=Cc1ccc(OC(F)F)c(O)c1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
a71f3c9bdb498e0df7854c01d285462745eacb61fcde4051c28043b77fa1bd37
895b1d2fe77d134f12b38f8d837ea80b2e81ef793fb29282c01859f1f67233b7
c1ccccc1
C-O-C(=O)-[C;H0;D4;+0:1](-Cl)(-[F;D1;H0:2])-[F;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
38
[{"value": 38.0, "product": "FC(OC1=C(C=C(C=O)C=C1)O)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 29.4, "product": "FC(OC1=C(C=C(C=O)C=C1)O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
3,4-Dihydroxybenzaldehyde (0.50 g, 3.62 mmol, Aldrich), methyl chlorodifluoroacetate (0.52 g, 3.62 mmol, Aldrich) and potassium carbonate (0.50 g, 3.62 mmol) were combined in DMF (5.0 mL) under an argon atmosphere. After stirring at 60°-65° C. for 3 h, DMF was removed in vacuo and the residue was partioned between aque...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Ester.Aromatic alcohol
Secondary halide.Secondary halide.Ether
null
null
c1ccccc1
HCl
CN(C)C=O
null
3
COC(=O)C(F)(F)Cl.O=Cc1ccc(O)c(O)c1>CN(C)C=O>O=Cc1ccc(OC(F)F)c(O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-550474a9556d462983b860f2b003f86a
CC(=O)N1CCc2cc(O)c(Br)cc21.COC(=O)C(F)(F)Cl>>CC(=O)N1CCc2cc(OC(F)F)c(Br)cc21
C(C)(=O)N1CCC2=CC(=C(C=C12)Br)O.ClC(C(=O)OC)(F)F.ClC(C(=O)OC)(F)F.C([O-])([O-])=O.[K+].[K+].C([O-])([O-])=O.[K+].[K+]>>C(C)(=O)N1CCC2=CC(=C(C=C12)Br)OC(F)F
[CH3:1][C:2](=[O:3])[N:4]1[CH2:5][CH2:6][c:7]2[cH:8][c:9]([OH:10])[c:14]([Br:15])[cH:16][c:17]21.COC(=O)[C:11](Cl)([F:12])[F:13]>>[CH3:1][C:2](=[O:3])[N:4]1[CH2:5][CH2:6][c:7]2[cH:8][c:9]([O:10][CH:11]([F:12])[F:13])[c:14]([Br:15])[cH:16][c:17]21
CC(=O)N1CCc2cc(O)c(Br)cc21.COC(=O)C(F)(F)Cl
CC(=O)N1CCc2cc(OC(F)F)c(Br)cc21
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
a71f3c9bdb498e0df7854c01d285462745eacb61fcde4051c28043b77fa1bd37
895b1d2fe77d134f12b38f8d837ea80b2e81ef793fb29282c01859f1f67233b7
c1ccc2c(c1)CCN2
C-O-C(=O)-[C;H0;D4;+0:1](-Cl)(-[F;D1;H0:2])-[F;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
3
HOUR
1-Acetyl-6-bromo-5-hydroxyindoline (2 g, 7.8 mmol), methyl 2-chloro-2,2-difluoroacetate (0.82 ml, 7.8 mmol) and potassium carbonate (1.08 g, 7.8 mmol) were suspended in N,N-dimethylformamide (20 mL) under an argon atmosphere and placed in a 65° C. oil bath. After 3 hr, additional methyl 2-chloro-2,2-difluoroacetate (0....
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Ester.Aromatic alcohol
Secondary halide.Secondary halide.Ether
null
null
c1ccc2c(c1)CC[NH]2
HCl
CN(C=O)C
null
3
CC(=O)N1CCc2cc(O)c(Br)cc21.COC(=O)C(F)(F)Cl>CN(C=O)C>CC(=O)N1CCc2cc(OC(F)F)c(Br)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-065831d99277499b89b8f6f92e86ad30
CCCCCCCCCCCCC.CCOC(=O)CCc1cccc(I)c1.Cc1ccc(N)cc1C.Cc1ccccc1>>CCOC(=O)CCc1cccc(N(c2cccc(CCC(=O)OCC)c2)c2ccc(C)c(C)c2)c1
CCCCCCCCCCCCC.NC1=CC(=C(C=C1)C)C.IC=1C=C(CCC(=O)OCC)C=CC1.C1(=CC=CC=C1)C.C([O-])([O-])=O.[K+].[K+]>>C(C)OC(=O)CCC=1C=C(C=CC1)N(C1=CC(=C(C=C1)C)C)C1=CC(=CC=C1)CCC(=O)OCC
CCCCCC[CH2:6]CCCC[CH2:2][CH3:1].I[c:14]1[cH:15][cH:16][cH:17][c:18]([CH2:19][CH2:20][C:21](=[O:22])[O:23][CH2:24][CH3:25])[cH:26]1.[NH2:13][c:27]1[cH:28][cH:29][c:30]([CH3:31])[c:32]([CH3:33])[cH:34]1.[CH3:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:35]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:...
CCCCCCCCCCCCC.CCOC(=O)CCc1cccc(I)c1.Cc1ccc(N)cc1C.Cc1ccccc1
CCOC(=O)CCc1cccc(N(c2cccc(CCC(=O)OCC)c2)c2ccc(C)c(C)c2)c1
null
O.O.O.O.O.S(=O)(=O)([O-])[O-].[Cu+2]
null
Acylation
OtherReaction
54501e10e8da214bc308903d3daa045a3ef2162f00410d5a0b32f2299aacc8c8
dbb0eb744f989d85895c22aaae807ffdec084fe09a76f7c236614e64944edef6
c1ccc(N(c2ccccc2)c2ccccc2)cc1
C-C-C-C-C-C-[CH2;D2;+0:1]-C-C-C-C-[CH2;D2;+0:2]-[C;D1;H3:3].I-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[CH3;D1;+0:9]-[c:10]1:[c:11]:[cH;D2;+0:12]:[c:13]:[c:14]:[c:15]:1.[NH2;D1;+0:16]-[c:17](:[c:18]):[c:19]>>[C;D1;H3:3]-[CH2;D2;+0:2]-[#8:20]-[C:21](=[O;D1;H0:22])-[CH2;D2;+0:1]-[CH2;D2;+0:9]-[c:10]1:[c:11]:[c;H0;D3;+0:1...
null
[]
230
CELSIUS
null
null
In a 100 ml-volume flask, 6 g of 3,4-xylidine, 34 g of ethyl 3-iododihydrocinnamate, 19 g of potassium carbonate, 5 g of copper sulfate pentahydrate and 20 ml of n-tridecane were placed, and the mixture was reacted under heating at 230° C. for 10 hours in a nitrogen stream. After the reaction, the system was cooled to ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Ester.Tertiary amine
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
HI
O.O.O.O.O.S(=O)(=O)([O-])[O-].[Cu+2]
230
null
CCCCCCCCCCCCC.CCOC(=O)CCc1cccc(I)c1.Cc1ccc(N)cc1C.Cc1ccccc1>O.O.O.O.O.S(=O)(=O)([O-])[O-].[Cu+2]>CCOC(=O)CCc1cccc(N(c2cccc(CCC(=O)OCC)c2)c2ccc(C)c(C)c2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-70576781abfa4a2db8a2ad21736fa5f6
CCCCCCCCCCCCC.CCOC(=O)CCc1cccc(I)c1.Cc1ccccc1.O=C([O-])[O-].c1ccc(Nc2ccc(-c3ccc(Nc4ccccc4)cc3)cc2)cc1>>CCOC(=O)CCc1cccc(N(c2ccccc2)c2ccc(-c3ccc(N(c4ccccc4)c4cccc(CCC(=O)OCC)c4)cc3)cc2)c1
CCCCCCCCCCCCC.C1(=CC=CC=C1)NC1=CC=C(C=C1)C1=CC=C(NC2=CC=CC=C2)C=C1.IC=1C=C(CCC(=O)OCC)C=CC1.C1(=CC=CC=C1)C.C([O-])([O-])=O.[K+].[K+]>>C1(=CC=CC=C1)N(C1=CC=C(C=C1)C1=CC=C(C=C1)N(C1=CC(=CC=C1)CCC(=O)OCC)C1=CC=CC=C1)C1=CC(=CC=C1)CCC(=O)OCC
CCCCCC[CH2:41]CCCC[CH2:45][CH3:46].I[c:12]1[cH:11][cH:10][cH:9][c:8]([CH2:7][CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:52]1.[cH:35]1[cH:36][cH:37][cH:38][c:39]([CH3:40])[cH:47]1.[O-][C:42](=[O:43])[O-:44].[NH:13]([c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[c:20]1[cH:21][cH:22][c:23](-[c:24]2[cH:25][cH:26][c:27]([NH:2...
CCCCCCCCCCCCC.CCOC(=O)CCc1cccc(I)c1.Cc1ccccc1.O=C([O-])[O-].c1ccc(Nc2ccc(-c3ccc(Nc4ccccc4)cc3)cc2)cc1
CCOC(=O)CCc1cccc(N(c2ccccc2)c2ccc(-c3ccc(N(c4ccccc4)c4cccc(CCC(=O)OCC)c4)cc3)cc2)c1
null
O.O.O.O.O.S(=O)(=O)([O-])[O-].[Cu+2]
null
C-C Coupling
OtherReaction
497f9e9d1397a0e31d3ddb287447ba2626934ccb58ababaec9ed702cbd7901d6
44c1f5b065c6391b4ea52e08552a04f6c348986b4cd4a5d798ee2c633f2c2d31
c1ccc(N(c2ccccc2)c2ccc(-c3ccc(N(c4ccccc4)c4ccccc4)cc3)cc2)cc1
C-C-C-C-C-C-[CH2;D2;+0:1]-C-C-C-C-[CH2;D2;+0:2]-[C;D1;H3:3].I-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8].[CH3;D1;+0:9]-[c:10]1:[c:11]:[c:12]:[c:13]:[cH;D2;+0:14]:[c:15]:1.[O-;H0;D1:16]-[C;H0;D3;+0:17](-[O-])=[O;D1;H0:18].[c:19]:[c:20](-[NH;D2;+0:21]-[c:22](:[c:23]):[c:24]):[c:25].[c:26]:[c:27](-[NH;D2;+0:28]-[c:29](:[c:3...
null
[]
230
CELSIUS
null
null
In a 100 ml-volume flask, 10.77 g of N,N'-diphenylbenzidine, 23.0 g of ethyl 3-iododihydrocinnamate, 11.61 g of potassium carbonate, 1.0 g of copper sulfate pentahydrate and 20 ml of n-tridecane were placed, and the mixture was reacted under heating at 230° C. for one hour in a nitrogen stream. After the reaction, the ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine.Secondary amine
Ester.Tertiary amine.Tertiary amine
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HI
O.O.O.O.O.S(=O)(=O)([O-])[O-].[Cu+2]
230
null
CCCCCCCCCCCCC.CCOC(=O)CCc1cccc(I)c1.Cc1ccccc1.O=C([O-])[O-].c1ccc(Nc2ccc(-c3ccc(Nc4ccccc4)cc3)cc2)cc1>O.O.O.O.O.S(=O)(=O)([O-])[O-].[Cu+2]>CCOC(=O)CCc1cccc(N(c2ccccc2)c2ccc(-c3ccc(N(c4ccccc4)c4cccc(CCC(=O)OCC)c4)cc3)cc2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-db854b27d2914399bbe5f288a9a9adb4
BrCCCBr.O=Cc1ccc(O)cc1>>O=Cc1ccc(OCCCOc2ccc(C=O)cc2)cc1
OC1=CC=C(C=O)C=C1.BrCCCBr>>C(=O)C1=CC=C(OCCCOC2=CC=C(C=C2)C=O)C=C1
Br[CH2:2][CH2:9][CH2:19]Br.[OH:1][c:6]1[cH:5][cH:4][c:15]([CH:16]=[O:17])[cH:18][cH:20]1>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]([CH:16]=[O:17])[cH:18][cH:19]2)[cH:20][cH:21]1
BrCCCBr.O=Cc1ccc(O)cc1
O=Cc1ccc(OCCCOc2ccc(C=O)cc2)cc1
null
null
C([O-])([O-])=O.[K+].[K+].CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
9ca249d8c990495c198a5173c824a6a22faf7c6f4c2389fbcc6bed0485ec4ce9
b4c10ccb2388cb913655268bc27e1f9fe5931851a3f009855875eaf96444dbfc
c1ccc(OCCCOc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-Br.[O;D1;H0:4]=[C:5]-[c;H0;D3;+0:6]1:[cH;D2;+0:7]:[cH;D2;+0:8]:[c;H0;D3;+0:9](-[OH;D1;+0:10]):[c:11]:[cH;D2;+0:12]:1>>[O;D1;H0:4]=[C:5]-[c;H0;D3;+0:6]1:[c:13]:[c:14]:[c:15](-[#8:16]-[C:17]-[CH2;D2;+0:2]-[C:18]-[#8:19]-[c;H0;D3;+0:9]2:[c:11]:[cH;D2;+0:12]:[c:20](-[CH;D2;+0:3]...
76
[{"value": 76.0, "product": "C(=O)C1=CC=C(OCCCOC2=CC=C(C=C2)C=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
10.0 g of 4-hydroxybenzaldehyde and 8.3 g of 1,3-dibromopropane were reacted for 24 hours in 6.2 g of potassium carbonate solution in 100 ml of DMF under reflux. The reaction mixture was poured into cold distilled water to obtain a precipitate. After filtration and vacuum drying the precipitate, the resultant was recry...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Aldehyde.Aromatic alcohol
Aldehyde.Aldehyde.Ether.Ether
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Br-
C([O-])([O-])=O.[K+].[K+].CN(C)C=O
null
null
BrCCCBr.O=Cc1ccc(O)cc1>C([O-])([O-])=O.[K+].[K+].CN(C)C=O>O=Cc1ccc(OCCCOc2ccc(C=O)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e22638b8245f48a095b97a9f8f553d18
CCCCOC1=C(SCCCCCC(=O)OC)[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)C1>>CCCCOC1=C(SCCCCCC(=O)O)[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)C1
Cl.COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@H](CCCC)C)O)O)OCCCC)=O.P(=O)([O-])([O-])[O-].S(=O)(=O)([O-])[O-].[NH4+].[NH4+]>>C(CCC)OC1=C(SCCCCCC(=O)O)[C@H]([C@@H](C1)O)\C=C\[C@H](C[C@H](CCCC)C)O
C[O:16][C:14]([CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][S:8][C:7]1=[C:6]([O:5][CH2:4][CH2:3][CH2:2][CH3:1])[CH2:31][C@@H:29]([OH:30])[C@@H:17]1/[CH:18]=[CH:19]/[C@@H:20]([OH:21])[CH2:22][C@@H:23]([CH3:24])[CH2:25][CH2:26][CH2:27][CH3:28])=[O:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][C:6]1=[C:7]([S:8][CH2:9][CH2:10][CH2:11][...
CCCCOC1=C(SCCCCCC(=O)OC)[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)C1
CCCCOC1=C(SCCCCCC(=O)O)[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)C1
null
null
CC(=O)C
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
C1=CCCC1
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]
14
[{"value": 14.0, "product": "C(CCC)OC1=C(SCCCCCC(=O)O)[C@H]([C@@H](C1)O)\\C=C\\[C@H](C[C@H](CCCC)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 13.9, "product": "C(CCC)OC1=C(SCCCCCC(=O)O)[C@H]([C@@H](C1)O)\\C=C\\[C@H](C[C@H](CCCC)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
Methyl(11R,12S,13E,15S,17S)-9-butyloxy-11,15-dihydroxy-17,20-dimethyl-7-thiaprosta-8,13-dienoate (51 mg, 0.11 mmol) was dissolved in acetone (1 ml). To this solution was added a pH 8 phosphate buffer (10 ml). Further esterase (from porcine liver made by Sigma Co., 114 μl) was added and the mixture was stirred at room t...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1=CCCC1
Other
CC(=O)C
null
5
CCCCOC1=C(SCCCCCC(=O)OC)[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)C1>CC(=O)C>CCCCOC1=C(SCCCCCC(=O)O)[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8f870745fc5f496588a513ddc86e1f2b
CC(C)C(=O)OC(=O)C(C)C.CCCC[C@@H](C)C[C@@H](/C=C/I)O[Si](C)(C)C(C)(C)C.COC(=O)CCCCCSC1=C(O[SiH](C)C)[C@@H](C(C)(C)C)CC1=O>>CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
C(C)(C)(C)[C@@H]1C(=C(C(C1)=O)SCCCCCC(=O)OC)O[SiH](C)C.I\C=C\[C@H](C[C@@H](CCCC)C)O[Si](C)(C)C(C)(C)C.C(C)(C)(C)[Li].C(C(C)C)(=O)OC(C(C)C)=O.C(#CCCCC)[Cu]>>COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@@H](CCCC)C)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C(C)C)=O)=O
CC(C)C(=O)O[C:25](=[O:26])[CH:27]([CH3:28])[CH3:29].I/[CH:10]=[CH:9]/[C@H:8]([CH2:7][C@@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH3:6])[O:40][Si:41]([CH3:42])([CH3:43])[C:44]([CH3:45])([CH3:46])[CH3:47].[C@H:11]1([C:36]([CH3:37])([CH3:38])[CH3:39])[CH2:30][C:23](=[O:24])[C:12]([S:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][...
CC(C)C(=O)OC(=O)C(C)C.CCCC[C@@H](C)C[C@@H](/C=C/I)O[Si](C)(C)C(C)(C)C.COC(=O)CCCCCSC1=C(O[SiH](C)C)[C@@H](C(C)(C)C)CC1=O
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
null
null
CN(P(N(C)C)N(C)C)C
Acylation
OtherReaction
8afc755b548997a6f5fa8fedd78136c9b6506cce35137678927e0ae1199f5198
61a9fef0afe1c5bb4f7915b9a6f9c9607c1132c62df54f96cfacb548bb7b17a5
C1=CCCC1
C-C(-C)-C(=O)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[C;D1;H3:5].I/[CH;D2;+0:6]=[C:7]/[C:8](-[#8:9])-[C:10].[C:11]-[#16:12]-[C;H0;D3;+0:13]1=[C;H0;D3;+0:14](-[#8:15]-[SiH;D3;+0:16](-[C;D1;H3:17])-[C;D1;H3:18])-[C@@H;D3;+0:19](-[C;H0;D4;+0:20](-[C;D1;H3:21])(-[C;D1;H3:22])-[C;D1;H3:23])-[CH2;D2;+0:24]-[C;H0;...
65
[{"value": 65.0, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](C[C@@H](CCCC)C)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C(C)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Using as the materials and reagents (1E,3S,5R)-1-iodo-3-(tert-butyldimethylsiloxy)-5-methyl-1-nonene (476 mg, 1.2 mmol), tert-butyllithium (1.54 mol/l, 1.56 ml, 2.4 mmol), 174 mg of 1-hexynylcopper, hexamethylphosphorous triamide (436 μl), (4R)-tert-butyldimethylsiloxy-2-(5-methoxycarbonylpentylthio)-2-cyclopenten-1-on...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ketone.Monosulfide
Ester.Monosulfide.TMS ether protective group
C1=CCCC1
C1=CCCC1
C1=CCCC1
HI
CN(P(N(C)C)N(C)C)C
null
null
CC(C)C(=O)OC(=O)C(C)C.CCCC[C@@H](C)C[C@@H](/C=C/I)O[Si](C)(C)C(C)(C)C.COC(=O)CCCCCSC1=C(O[SiH](C)C)[C@@H](C(C)(C)C)CC1=O>CN(P(N(C)C)N(C)C)C>CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e25048cd0b1a4d4a97c39af9be62f679
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O
N1=CC=CC=C1.F.COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@@H](CCCC)C)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C(C)C)=O)=O>>COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@@H](CCCC)C)O)O)OC(C(C)C)=O)=O
CC(C)(C)[Si](C)(C)[O:9][C@@H:8]([CH2:7][C@@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH3:6])/[CH:10]=[CH:11]/[C@@H:12]1[C:13]([S:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][C:20](=[O:21])[O:22][CH3:23])=[C:24]([O:25][C:26](=[O:27])[CH:28]([CH3:29])[CH3:30])[CH2:31][C@H:32]1[O:33][Si](C)(C)C(C)(C)C>>[CH3:1][CH2:2][CH2:3][CH2:4...
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CCCC1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
64
[{"value": 64.0, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](C[C@@H](CCCC)C)O)O)OC(C(C)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.6, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](C[C@@H](CCCC)C)O)O)OC(C(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.6 ml) and methyl(11R,12S,13E,15S,17R)-9-isobutyryloxy-11,15-bis(tert-butyldimethylsiloxy)-17,20-dimethyl-7-thiaprosta-8,13-dienoate (466 mg), the same procedure as in Example 2 was performed to obtain methyl(11R,12S,13E,15S,17R)-9-isobutyryloxy-...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1
Other
null
null
null
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)C)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4530e01b498e4c59a4e74ef8002e38f6
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)(C)C)C[C@H]1O
N1=CC=CC=C1.F.COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@@H](CCCC)C)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C(C)(C)C)=O)=O>>COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@@H](CCCC)C)O)O)OC(C(C)(C)C)=O)=O
CC(C)(C)[Si](C)(C)[O:9][C@@H:8]([CH2:7][C@@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH3:6])/[CH:10]=[CH:11]/[C@@H:12]1[C:13]([S:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][C:20](=[O:21])[O:22][CH3:23])=[C:24]([O:25][C:26](=[O:27])[C:28]([CH3:29])([CH3:30])[CH3:31])[CH2:32][C@H:33]1[O:34][Si](C)(C)C(C)(C)C>>[CH3:1][CH2:2][CH2...
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)(C)C)C[C@H]1O
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CCCC1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
55
[{"value": 55.0, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](C[C@@H](CCCC)C)O)O)OC(C(C)(C)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.6, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](C[C@@H](CCCC)C)O)O)OC(C(C)(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": f...
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.7 ml) and methyl(11R,12S,13E,15S,17R)-9-pivaloyloxy-11,15-bis(tert-butyldimethylsiloxy)-17,20-dimethyl-7-thiaprosta-8,13-dienoate (564 mg), the same procedure was performed as in Example 2 was performed to obtain methyl(11R,13E,15S,17R)-9-pivalo...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1
Other
null
null
null
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)(C)C)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)C(C)(C)C)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-947e00ce913b48258528de610493e045
CCCCOC(=O)CCCCCSC1=C(OC(=O)CCC)C[C@@H](O[Si](C)(C)C(C)(C)C)[C@@H]1/C=C/[C@H](C[C@H](C)CCCC)O[Si](C)(C)C(C)(C)C>>CCCCOC(=O)CCCCCSC1=C(OC(=O)CCC)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)C[C@H](C)CCCC
N1=CC=CC=C1.F.C(CCC)(=O)OC1=C(SCCCCCC(=O)OCCCC)[C@H]([C@@H](C1)O[Si](C)(C)C(C)(C)C)\C=C\[C@H](C[C@@H](CCCC)C)O[Si](C)(C)C(C)(C)C>>C(CCC)(=O)OC1=C(SCCCCCC(=O)OCCCC)[C@H]([C@@H](C1)O)\C=C\[C@H](C[C@@H](CCCC)C)O
CC(C)(C)[Si](C)(C)[O:24][C@@H:23]1[CH2:22][C:15]([O:16][C:17](=[O:18])[CH2:19][CH2:20][CH3:21])=[C:14]([S:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][C:6]([O:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:7])[C@H:25]1/[CH:26]=[CH:27]/[C@@H:28]([O:29][Si](C)(C)C(C)(C)C)[CH2:30][C@H:31]([CH3:32])[CH2:33][CH2:34][CH2:35][CH3:36]>>[CH3:...
CCCCOC(=O)CCCCCSC1=C(OC(=O)CCC)C[C@@H](O[Si](C)(C)C(C)(C)C)[C@@H]1/C=C/[C@H](C[C@H](C)CCCC)O[Si](C)(C)C(C)(C)C
CCCCOC(=O)CCCCCSC1=C(OC(=O)CCC)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)C[C@H](C)CCCC
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CCCC1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
72
[{"value": 72.0, "product": "C(CCC)(=O)OC1=C(SCCCCCC(=O)OCCCC)[C@H]([C@@H](C1)O)\\C=C\\[C@H](C[C@@H](CCCC)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.7, "product": "C(CCC)(=O)OC1=C(SCCCCCC(=O)OCCCC)[C@H]([C@@H](C1)O)\\C=C\\[C@H](C[C@@H](CCCC)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired...
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.2 ml) and butyl (11R,12S,13E,15S,17R)-9-butyryloxy-11,15-bis(tert-butyldimethylsiloxy)-17,20-dimethyl-7-thiaprosta-8,13-dienoate (138 mg), the same procedure as in Example 2 was performed to obtain butyl (11R,12S,13E,15S,17R)-9-butyryloxy-11,15-...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1
Other
null
null
null
CCCCOC(=O)CCCCCSC1=C(OC(=O)CCC)C[C@@H](O[Si](C)(C)C(C)(C)C)[C@@H]1/C=C/[C@H](C[C@H](C)CCCC)O[Si](C)(C)C(C)(C)C>>CCCCOC(=O)CCCCCSC1=C(OC(=O)CCC)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)C[C@H](C)CCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-76d32aafd0e142d0832c397f95f52a05
CCCCC[C@@H](/C=C/I)O[Si](C)(C)C(C)(C)C.COC(=O)CCCCCSC1=C(O[SiH](C)C)[C@@H](C(C)(C)C)CC1=O.O=C(OC(=O)c1ccccc1)c1ccccc1.[Li][C](C)(C)C>>CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
C(C)(C)(C)[C@@H]1C(=C(C(C1)=O)SCCCCCC(=O)OC)O[SiH](C)C.I\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C.C(C)(C)(C)[Li].C(C1=CC=CC=C1)(=O)OC(C1=CC=CC=C1)=O.C(#CCCCC)[Cu]>>COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C1=CC=CC=C1)=O)=O
I/[CH:8]=[CH:7]/[C@H:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[O:41][Si:42]([CH3:43])([CH3:44])[C:45]([CH3:46])([CH3:47])[CH3:48].CC(C)(C)[C@H:9]1[CH2:31][C:21](=[O:22])[C:10]([S:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][C:17](=[O:18])[O:19][CH3:20])=[C:32]1[O:33][SiH:34]([CH3:35])[CH3:36].O=C(O[C:23](=[O:24])[c:25]1[c...
CCCCC[C@@H](/C=C/I)O[Si](C)(C)C(C)(C)C.COC(=O)CCCCCSC1=C(O[SiH](C)C)[C@@H](C(C)(C)C)CC1=O.O=C(OC(=O)c1ccccc1)c1ccccc1.[Li][C](C)(C)C
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
null
null
CN(P(N(C)C)N(C)C)C
Acylation
OtherReaction
46d07187e3b0a5bf5c5a95a7583a8697ecd0d97270c703f53c62a843cfbdb1b4
070d9d49bcafdcb794bdb6b71278660ee33eb316daa377ce48b8a62e46ad473d
O=C(OC1=CCCC1)c1ccccc1
C-C(-C)(-C)-[C@H;D3;+0:1]1-[CH2;D2;+0:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[C;H0;D3;+0:5](-[#16:6]-[C:7])=[C;H0;D3;+0:8]-1-[#8:9]-[SiH;D3;+0:10](-[C;D1;H3:11])-[C;D1;H3:12].I/[CH;D2;+0:13]=[C:14]/[C:15](-[#8:16])-[C:17].O=C(-O-[C;H0;D3;+0:18](=[O;D1;H0:19])-[c:20](:[c:21]):[c:22])-c1:c:c:c:c:c:1.[C;D1;H3:23]-[C;H0;D4;+0:...
55.4
[{"value": 33.0, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C1=CC=CC=C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 55.4, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C1=CC=CC=C1)...
null
null
null
null
Using as the materials and reagents (1E,3S)-1-iodo-3-(tert-butyldimethylsiloxy)-1-octene (442 mg, 1.2 mmol), tert-butyllithium (1.54 mol/l, 1.56 ml, 2.4 mmol), 1-hexynylcopper (174 mg), hexamethylphosphorous triamide (436 μl), (4R)-tert-butyldimethylsiloxy-2-(5-methoxycarbonyl-pentylthio)-2-cyclopenten-1-one (373 mg, 1...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ketone.Ester.Ester.Monosulfide.Alkyl lithium
Ester.Monosulfide.TMS ether protective group
C1=CCCC1.c1ccccc1
C1=CCCC1
C1=CCCC1.c1ccccc1
HI.Li
CN(P(N(C)C)N(C)C)C
null
null
CCCCC[C@@H](/C=C/I)O[Si](C)(C)C(C)(C)C.COC(=O)CCCCCSC1=C(O[SiH](C)C)[C@@H](C(C)(C)C)CC1=O.O=C(OC(=O)c1ccccc1)c1ccccc1.[Li][C](C)(C)C>CN(P(N(C)C)N(C)C)C>CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a8c4e36b9c5748c2bdb42724db547b96
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O
N1=CC=CC=C1.F.COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C1=CC=CC=C1)=O)=O>>C(C1=CC=CC=C1)(=O)OC1=C(SCCCCCC(=O)OC)[C@H]([C@@H](C1)O)\C=C\[C@H](CCCCC)O
CC(C)(C)[Si](C)(C)[O:7][C@@H:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])/[CH:8]=[CH:9]/[C@@H:10]1[C:11]([S:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[O:20][CH3:21])=[C:22]([O:23][C:24](=[O:25])[c:26]2[cH:27][cH:28][cH:29][cH:30][cH:31]2)[CH2:32][C@H:33]1[O:34][Si](C)(C)C(C)(C)C>>[CH3:1][CH2:2][CH2:3][CH2:4]...
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
O=C(OC1=CCCC1)c1ccccc1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
88.3
[{"value": 86.0, "product": "C(C1=CC=CC=C1)(=O)OC1=C(SCCCCCC(=O)OC)[C@H]([C@@H](C1)O)\\C=C\\[C@H](CCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.3, "product": "C(C1=CC=CC=C1)(=O)OC1=C(SCCCCCC(=O)OC)[C@H]([C@@H](C1)O)\\C=C\\[C@H](CCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false...
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.3 ml) and methyl(11R,12S,13E,15S)-9-benzoyloxy-11,15-bis(tert-butyldimethylsiloxy)-7-thiaprosta-8,13-dienoate (239 mg), the same procedure as in Example 2 was performed to obtain methyl(11R,13E,15S)-9-benzoyloxy-11,15-dihydroxy-7-thiaprosta-8,13...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1.c1ccccc1
Other
null
null
null
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-76f66933b8914bb1a7437f5254a0de57
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCCCSC1=C(OC(=O)CCC)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCCCC
C(CCC)(=O)OC1=C(SCCCCCC(=O)O)[C@H]([C@@H](C1)O[Si](C)(C)C(C)(C)C)\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C.C(O)([O-])=O.[Na+].N1=CC=CC=C1.F.C(C)#N>>C(CCC)(=O)OC1=C(SCCCCCC)[C@H]([C@@H](C1)O)\C=C\[C@H](CCCCC)O
CC(C)(C)[Si](C)(C)[O:18][C@@H:17]1[CH2:16][C:9]([O:10][C:11](=[O:12])[CH2:13][CH2:14][CH3:15])=[C:8]([S:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][C:1](=O)O)[C@H:19]1/[CH:20]=[CH:21]/[C@@H:22]([O:23][Si](C)(C)C(C)(C)C)[CH2:24][CH2:25][CH2:26][CH2:27][CH3:28]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][S:7][C:8]1=[C:9]([O:10...
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCCCCSC1=C(OC(=O)CCC)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCCCC
null
null
N1=CC=CC=C1.C(C)(=O)OCC
Reduction
OtherReaction
a0e91d17d81c0bb7f1829e6b5b45de64d1a532e1ec02fd5dc124819c438453b0
33f60392ace24dc8f1f760d24515776f5bcdb07ae384abcf60bac7667a41c48e
C1=CCCC1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C.O-[C;H0;D3;+0:12](=O)-[C:13]-[C:14]>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1].[C:14]-[C:13]-[CH3;D1;+0:12]
35
[{"value": 33.0, "product": "C(CCC)(=O)OC1=C(SCCCCCC)[C@H]([C@@H](C1)O)\\C=C\\[C@H](CCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 35.0, "product": "C(CCC)(=O)OC1=C(SCCCCCC)[C@H]([C@@H](C1)O)\\C=C\\[C@H](CCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
A hydrogen fluoride-pyridine solution (0.1 ml) was added to a solution of ice-cooled acetonitrile (1 ml) and pyridine (0.1 ml), then a pyridine (0.1 ml) solution of (11R,12S,13E,15S)-9-butyryloxy-11,15-bis(tert-butyldimethylsiloxy)-7-thiaprosta-8,13-dienoic acid (79 mg) was added. The ice bath was detached, then the so...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1
HO-
N1=CC=CC=C1.C(C)(=O)OCC
null
20
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>N1=CC=CC=C1.C(C)(=O)OCC>CCCCCCSC1=C(OC(=O)CCC)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-22a46d06c9484f61abcb3ba9fcd4507b
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O
N1=CC=CC=C1.F.COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@@H](CCCC)C)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(C1=CC=CC=C1)=O)=O>>COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](C[C@@H](CCCC)C)O)O)OC(C1=CC=CC=C1)=O)=O
CC(C)(C)[Si](C)(C)[O:9][C@@H:8]([CH2:7][C@@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH3:6])/[CH:10]=[CH:11]/[C@@H:12]1[C:13]([S:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][C:20](=[O:21])[O:22][CH3:23])=[C:24]([O:25][C:26](=[O:27])[c:28]2[cH:29][cH:30][cH:31][cH:32][cH:33]2)[CH2:34][C@H:35]1[O:36][Si](C)(C)C(C)(C)C>>[CH3:1][C...
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
O=C(OC1=CCCC1)c1ccccc1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
28
[{"value": 28.0, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](C[C@@H](CCCC)C)O)O)OC(C1=CC=CC=C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 27.7, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](C[C@@H](CCCC)C)O)O)OC(C1=CC=CC=C1)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desir...
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.7 ml) and methyl(11R,12S,13E,15S,17R)-9-benzoyloxy-11,15-bis(tert-butyldimethylsiloxy)-17,20-dimethyl-7-thiaprosta-8,13-dienoate (734 mg), the same procedure as in Example 2 was performed to obtain methyl(11R,12S,13E,15S,17R)-9-benzoyloxy-11,15-...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1.c1ccccc1
Other
null
null
null
CCCC[C@@H](C)C[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCC[C@@H](C)C[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)c2ccccc2)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d5c0f98feabe41e293e98aa397fcf97a
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)[C@H](Cc2ccccc2)NC(=O)OCc2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)[C@H](Cc2ccccc2)NC(=O)OCc2ccccc2)C[C@H]1O
N1=CC=CC=C1.F.COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC([C@@H](NC(=O)OCC1=CC=CC=C1)CC1=CC=CC=C1)=O)=O>>COC(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](CCCCC)O)O)OC([C@@H](NC(=O)OCC1=CC=CC=C1)CC1=CC=CC=C1)=O)=O
CC(C)(C)[Si](C)(C)[O:7][C@@H:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])/[CH:8]=[CH:9]/[C@@H:10]1[C:11]([S:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[O:20][CH3:21])=[C:22]([O:23][C:24](=[O:25])[C@H:26]([CH2:27][c:28]2[cH:29][cH:30][cH:31][cH:32][cH:33]2)[NH:34][C:35](=[O:36])[O:37][CH2:38][c:39]2[cH:40][cH:...
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)[C@H](Cc2ccccc2)NC(=O)OCc2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)[C@H](Cc2ccccc2)NC(=O)OCc2ccccc2)C[C@H]1O
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
O=C(N[C@@H](Cc1ccccc1)C(=O)OC1=CCCC1)OCc1ccccc1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
51
[{"value": 51.0, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](CCCCC)O)O)OC([C@@H](NC(=O)OCC1=CC=CC=C1)CC1=CC=CC=C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.8, "product": "COC(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](CCCCC)O)O)OC([C@@H](NC(=O)OCC1=CC=CC=C1)CC1=CC=CC=C1)=O)=O", "details...
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.3 ml) and methyl(11R,12S,13E,15S)-9-(N-benzyloxycarbonylphenylalanyloxy)-11,15-bis(tert-butyldimethylsiloxy)-7-thiaprosta-8,13-dienoate (140 mg), methyl(11R,12S,13E,15S)-9-(N-benzyloxycarbonylphenylalanyloxy)-11,15-dihydroxy-7-thiaprosta-8,13-di...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1.c1ccccc1.c1ccccc1
Other
null
null
null
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)[C@H](Cc2ccccc2)NC(=O)OCc2ccccc2)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)[C@H](Cc2ccccc2)NC(=O)OCc2ccccc2)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e387f53034b342bebeac204bcb29c54a
CCCCCC(C)(C)C(O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C>>CCCCCC(C)(C)C(O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)CCC)C[C@H]1O
N1=CC=CC=C1.F.C(CCC)(=O)OC1=C(SCCCCCC(=O)OC)[C@H]([C@@H](C1)O[Si](C)(C)C(C)(C)C)\C=C\C(C(CCCCC)(C)C)O>>C(CCC)(=O)OC1=C(SCCCCCC(=O)OC)[C@H]([C@@H](C1)O)\C=C\C(C(CCCCC)(C)C)O
CC(C)(C)[Si](C)(C)[O:34][C@H:33]1[C@H:13](/[CH:12]=[CH:11]/[CH:9]([C:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])([CH3:7])[CH3:8])[OH:10])[C:14]([S:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][C:21](=[O:22])[O:23][CH3:24])=[C:25]([O:26][C:27](=[O:28])[CH2:29][CH2:30][CH3:31])[CH2:32]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6...
CCCCCC(C)(C)C(O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C
CCCCCC(C)(C)C(O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)CCC)C[C@H]1O
null
null
null
Deprotection
Alcohol deprotection from silyl ethers
050b4fb4e1e9936189860d27dded10ae70a294a642c52f800eb9d5aaef7955cc
88623e19d23cdfe8e1a4c167fd6cfc51d774a1c784b87a7bb2df8153ee93e67a
C1=CCCC1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]>>[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
null
[]
null
null
null
null
Using as the materials a hydrogen fluoride-pyridine solution (0.25 ml) and methyl(11R,12S,13E)-9-butyryloxy-11-tert-butyldimethylsiloxy-15-hydroxy-16,16,20-trimethyl-7-thiaprosta-8,13-dienoate (100 mg), the same procedure as in Example 2 was performed to separately obtain two stereoisomers of methyl(11R,12S,13E)-9-buty...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group
Secondary alcohol
null
null
C1=CCCC1
Other
null
null
null
CCCCCC(C)(C)C(O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C>>CCCCCC(C)(C)C(O)/C=C/[C@@H]1C(SCCCCCC(=O)OC)=C(OC(=O)CCC)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3a3271a594c4451684be2191aa815526
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C.[NH4+]>>CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
Cl.C(CCC)(=O)OC1=C(SCCCCCC(=O)O)[C@H]([C@@H](C1)O[Si](C)(C)C(C)(C)C)\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C.ClC(=O)OCC(C)C.[OH-].[NH4+]>>C(CCC)(=O)OC1=C(SCCCCCC(=O)N)[C@H]([C@@H](C1)O[Si](C)(C)C(C)(C)C)\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C
O[C:17]([CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][S:11][C:10]1=[C:20]([O:21][C:22](=[O:23])[CH2:24][CH2:25][CH3:26])[CH2:27][C@@H:28]([O:29][Si:30]([CH3:31])([CH3:32])[C:33]([CH3:34])([CH3:35])[CH3:36])[C@@H:9]1/[CH:8]=[CH:7]/[C@H:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[O:37][Si:38]([CH3:39])([CH3:40])[C:41]([CH3:42])([...
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C.[NH4+]
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
null
null
C(Cl)Cl.C(C)(=O)OCC.C(C)N(CC)CC
Acylation
Carboxylic acid to amide conversion
1283aef55d7ee699f097a8e5267689198c76ba671644401547f902657820236d
cb0a71c3fb37a76e96fbd81aae6f95a28398a03d1ad2c8e877085e735efb98f1
C1=CCCC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[NH4+;D0:5]>>[C:4]-[C:3]-[C;H0;D3;+0:1](-[NH2;D1;+0:5])=[O;D1;H0:2]
84
[{"value": 84.0, "product": "C(CCC)(=O)OC1=C(SCCCCCC(=O)N)[C@H]([C@@H](C1)O[Si](C)(C)C(C)(C)C)\\C=C\\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A methylene chloride (3 ml) solution of (11R,12S,13E,15S)-9-butyryloxy-11,15-bis(tert-butyldimethylsiloxy)-7-thiaprosta-8,13-dienoic acid (201 mg) was cooled to -40° C., then isobutyl chloroformate (47 μl) and triethylamine (63 μl) were added to the solution which was then stirred as is at -40° C. for 30 minutes. Furth...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary amide
null
null
C1=CCCC1
HO-
C(Cl)Cl.C(C)(=O)OCC.C(C)N(CC)CC
null
0.5
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C.[NH4+]>C(Cl)Cl.C(C)(=O)OCC.C(C)N(CC)CC>CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e7a5f5fa47d44c41aa8f5e9d244fb7f5
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O
N1=CC=CC=C1.F.C(CCC)(=O)OC1=C(SCCCCCC(=O)N)[C@H]([C@@H](C1)O[Si](C)(C)C(C)(C)C)\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C>>C(CCC)(=O)OC1=C(SCCCCCC(=O)N)[C@H]([C@@H](C1)O)\C=C\[C@H](CCCCC)O
CC(C)(C)[Si](C)(C)[O:7][C@@H:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])/[CH:8]=[CH:9]/[C@@H:10]1[C:11]([S:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18]([NH2:19])=[O:20])=[C:21]([O:22][C:23](=[O:24])[CH2:25][CH2:26][CH3:27])[CH2:28][C@H:29]1[O:30][Si](C)(C)C(C)(C)C>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C@H:6]([OH:7])/[C...
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CCCC1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
91
[{"value": 91.0, "product": "C(CCC)(=O)OC1=C(SCCCCCC(=O)N)[C@H]([C@@H](C1)O)\\C=C\\[C@H](CCCCC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.7, "product": "C(CCC)(=O)OC1=C(SCCCCCC(=O)N)[C@H]([C@@H](C1)O)\\C=C\\[C@H](CCCCC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.2 ml) and (11R,12S,13E,15S)-9-butyryloxy-11,15-bis(tert-butyldimethylsiloxy)-7-thiaprosta-8,13-dienamide (169 mg), the same procedure was followed as in Example 2 to obtain (11R,12S,13E,15S)-9-butyryloxy-11,15-dihydroxy-7-thiaprosta-8,13-dienami...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1
Other
null
null
null
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(N)=O)=C(OC(=O)CCC)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-77b94b1df1cb49efa2184366a550397e
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)N(CC)CC)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)N(CC)CC)=C(OC(=O)CCC)C[C@H]1O
N1=CC=CC=C1.F.C(C)N(C(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](CCCCC)O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C)OC(CCC)=O)=O)CC>>C(C)N(C(CCCCCSC1=C(C[C@H]([C@@H]1\C=C\[C@H](CCCCC)O)O)OC(CCC)=O)=O)CC
CC(C)(C)[Si](C)(C)[O:7][C@@H:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])/[CH:8]=[CH:9]/[C@@H:10]1[C:11]([S:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[N:20]([CH2:21][CH3:22])[CH2:23][CH3:24])=[C:25]([O:26][C:27](=[O:28])[CH2:29][CH2:30][CH3:31])[CH2:32][C@H:33]1[O:34][Si](C)(C)C(C)(C)C>>[CH3:1][CH2:2][CH2:3]...
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)N(CC)CC)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C
CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)N(CC)CC)=C(OC(=O)CCC)C[C@H]1O
null
null
null
Deprotection
OtherReaction
3c4d3a3b788b4022df80488c890c930a0eff3addc93b825229adfe1b23285620
c96f1dab6a2ddd7b236398a198654bbc85e92a2fc2f6e88d092d4f9a3211cc52
C1=CCCC1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]=[C:5]-[C:6]-1/[C:7]=[C:8]/[C:9](-[C:10])-[O;H0;D2;+0:11]-[Si](-C)(-C)-C(-C)(-C)-C>>[C:10]-[C:9](-[OH;D1;+0:11])/[C:8]=[C:7]/[C:6]1-[C:5]=[C:4]-[C:3]-[C:2]-1-[OH;D1;+0:1]
87.2
[{"value": 78.0, "product": "C(C)N(C(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](CCCCC)O)O)OC(CCC)=O)=O)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.2, "product": "C(C)N(C(CCCCCSC1=C(C[C@H]([C@@H]1\\C=C\\[C@H](CCCCC)O)O)OC(CCC)=O)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using as the material and reagent a hydrogen fluoride-pyridine solution (0.2 ml) and N,N-diethyl(11R,12S,13E,15S)-9-butyryloxy-11,15-bis(tert-butyldimethylsiloxy)-7-thiaprosta-8,13-dienamide (169 mg), the same procedure as in Example 2 was performed to obtain N,N-diethyl(11R,12S,13E,15S)-9-butyryloxy-11,15-dihydroxy-7-...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group
Secondary alcohol.Secondary alcohol
null
null
C1=CCCC1
Other
null
null
null
CCCCC[C@@H](/C=C/[C@@H]1C(SCCCCCC(=O)N(CC)CC)=C(OC(=O)CCC)C[C@H]1O[Si](C)(C)C(C)(C)C)O[Si](C)(C)C(C)(C)C>>CCCCC[C@H](O)/C=C/[C@@H]1C(SCCCCCC(=O)N(CC)CC)=C(OC(=O)CCC)C[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-db7374af57ba4dcaba7944b782005f33
CC(C)(C)C(=C(c1ccc([N+](=O)[O-])cc1)C(C)(C)C)c1ccc([N+](=O)[O-])cc1>>CC(C)(C)C(=C(c1ccc([N+](=O)[O-])cc1)C(C)(C)C)c1ccc(N)cc1
CC(C)(C(=C(C(C)(C)C)C1=CC=C(C=C1)[N+](=O)[O-])C1=CC=C(C=C1)[N+](=O)[O-])C.C1=CCCCC1>>CC(C)(C(=C(C(C)(C)C)C1=CC=C(C=C1)N)C1=CC=C(C=C1)[N+](=O)[O-])C
O=[N+:24]([O-])[c:23]1[cH:22][cH:21][c:20]([C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[C:6]([c:7]2[cH:8][cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14][cH:15]2)[C:16]([CH3:17])([CH3:18])[CH3:19])[cH:26][cH:25]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[C:6]([c:7]1[cH:8][cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14][cH:15]1)[C:16]([...
CC(C)(C)C(=C(c1ccc([N+](=O)[O-])cc1)C(C)(C)C)c1ccc([N+](=O)[O-])cc1
CC(C)(C)C(=C(c1ccc([N+](=O)[O-])cc1)C(C)(C)C)c1ccc(N)cc1
null
[Pd]
C1CCOC1
Functional Group Interconversion
Reduction of nitro groups to amines
5c1ea979989295c14f1f65f49e58974d5c524451abca65fc2e6cec44e3d0784f
10b8579fd1662beac4350d758bc16e1f45ee6ea295ff9572db62110c9e2a77db
C(=Cc1ccccc1)c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
50
[{"value": 50.0, "product": "CC(C)(C(=C(C(C)(C)C)C1=CC=C(C=C1)N)C1=CC=C(C=C1)[N+](=O)[O-])C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.9, "product": "CC(C)(C(=C(C(C)(C)C)C1=CC=C(C=C1)N)C1=CC=C(C=C1)[N+](=O)[O-])C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 0.62 g 2,2,5,5-tetramethyl-3,4-di(4-nitrophenyl)hex-3-ene,2.6 g cyclohexene and 1.4 g 10% Pd/C in THF was refluxed for 2 hrs. The Pd/C was removed by filtration and the residue after evaporation of the solvent was purified by chromatography on silica gel (25% CH2Cl2 -hexane) to give 0.285 g (50%) 2,2,5,5-...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
[Pd].C1CCOC1
null
null
CC(C)(C)C(=C(c1ccc([N+](=O)[O-])cc1)C(C)(C)C)c1ccc([N+](=O)[O-])cc1>[Pd].C1CCOC1>CC(C)(C)C(=C(c1ccc([N+](=O)[O-])cc1)C(C)(C)C)c1ccc(N)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7e4da2f6c23d4c1a8affe98a75ef0117
CC(=O)NC1(c2ccccc2)CCN(CCC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1>>CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1
C(C)(=O)O.C(C)(=O)NC1(CCN(CC1)CCC(CN)C1=CC(=C(C=C1)Cl)Cl)C1=CC=CC=C1.FC(C=1C=C(C=O)C=C(C1)C(F)(F)F)(F)F.C(#N)[BH3-].[Na+]>>C(C)(=O)NC1(CCN(CC1)C(CC(CN)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1
[CH3:1][C:2](=[O:3])[NH:4][C:5]1([c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[CH2:12][CH2:13][N:14]([CH2:15][CH2:31][CH:32]([CH2:33][NH2:34])[c:35]2[cH:36][cH:37][c:38]([Cl:39])[c:40]([Cl:41])[cH:42]2)[CH2:43][CH2:44]1.O=[CH:16][c:17]1[cH:18][c:19]([C:20]([F:21])([F:22])[F:23])[cH:24][c:25]([C:26]([F:27])([F:28])[F:29])[cH...
CC(=O)NC1(c2ccccc2)CCN(CCC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1
null
null
ClCCl.Cl.CO.O
C-C Coupling
OtherReaction
43d4e2f03e758941ee99f59641d5d56e6475fe935434d251d75d5cdebbe19869
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
c1ccc(CCC(Cc2ccccc2)N2CCC(c3ccccc3)CC2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[#7:6](-[CH2;D2;+0:7]-[C:8]-[C:9])-[C:10]>>[C:5]-[#7:6](-[CH;D3;+0:7](-[C:8]-[C:9])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:10]
null
[]
0
CELSIUS
null
null
To a solution of 4-(4-acetamido-4-phenylpiperidino)-2-(3,4-dichlorophenyl)butylamine (0.30 g) in methanol (3 mL) was added 3,5-bis(trifluoromethyl)benzaldehyde (0.088 mL) and the mixture cooled to 0° C. To this stirred mixture was sequentially added acetic acid (0.046 mL) and a solution of sodium cyanoborohydride (0.50...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
Other
ClCCl.Cl.CO.O
0
null
CC(=O)NC1(c2ccccc2)CCN(CCC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1>ClCCl.Cl.CO.O>CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-615b2ecff1214a958b8e4deec4b08fcd
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=Cc1ccccc1>>CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CNCc2ccccc2)c2ccc(Cl)c(Cl)c2)CC1
C(C)(=O)NC1(CCN(CC1)C(CC(CN)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1.C(C1=CC=CC=C1)=O.ClC=1C=C(C=CC1Cl)CCCCN.FC(C=1C=C(C=O)C=C(C1)C(F)(F)F)(F)F>>C(C)(=O)NC1(CCN(CC1)C(CC(CNCC1=CC=CC=C1)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1
[CH3:1][C:2](=[O:3])[NH:4][C:5]1([c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[CH2:12][CH2:13][N:14]([CH:15]([CH2:16][c:17]2[cH:18][c:19]([C:20]([F:21])([F:22])[F:23])[cH:24][c:25]([C:26]([F:27])([F:28])[F:29])[cH:30]2)[CH2:31][CH:32]([CH2:33][NH2:34])[c:42]2[cH:43][cH:44][c:45]([Cl:46])[c:47]([Cl:48])[cH:49]2)[CH2:50][CH2:...
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=Cc1ccccc1
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CNCc2ccccc2)c2ccc(Cl)c(Cl)c2)CC1
null
null
null
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
c1ccc(CNCC(CC(Cc2ccccc2)N2CCC(c3ccccc3)CC2)c2ccccc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
Using a procedure similar to that described in Example 1, except replacing the (3,4-dichlorophenyl)butylamine and the 3,5-bis-(trifluoromethyl)benzaldehyde used therein with 4-(4-acetamido-4-phenylpiperidino)-2-(3,4-dichlorophenyl)-N-[3,5-bis(trifluoromethyl)benzyl]butylamine and benzaldehyde, respectively, the title c...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1ccccc1
Other
null
null
null
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=Cc1ccccc1>>CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CNCc2ccccc2)c2ccc(Cl)c(Cl)c2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a37d4b3af3174cb3b9d2b4d6eb76f09a
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.CC(=O)OC(C)=O>>CC(=O)NCC(CC(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N1CCC(NC(C)=O)(c2ccccc2)CC1)c1ccc(Cl)c(Cl)c1
C(C)(=O)OC(C)=O.C(C)(=O)NC1(CCN(CC1)C(CC(CN)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1.C(C)(=O)OC(C)=O.C(C)(C)N(CC)C(C)C>>C(C)(=O)NC1(CCN(CC1)C(CC(CNC(C)=O)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1
[NH2:4][CH2:5][CH:6]([CH2:7][CH:8]([CH2:9][c:10]1[cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17][c:18]([C:19]([F:20])([F:21])[F:22])[cH:23]1)[N:24]1[CH2:25][CH2:26][C:27]([NH:28][C:29]([CH3:30])=[O:31])([c:32]2[cH:33][cH:34][cH:35][cH:36][cH:37]2)[CH2:38][CH2:39]1)[c:40]1[cH:41][cH:42][c:43]([Cl:44])[c:45]([Cl:46])[...
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.CC(=O)OC(C)=O
CC(=O)NCC(CC(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N1CCC(NC(C)=O)(c2ccccc2)CC1)c1ccc(Cl)c(Cl)c1
null
CN(C1=CC=NC=C1)C
ClCCl.Cl.O.O1CCCC1
Acylation
Aminolysis of esters
87d35e51b477fc9a658a6f307eb56d84c8879182772c9dd3a42ec0d584fd2684
627cbc0550c9f51ad0105d9fcf46677e8c93bed87ee95bfe69292a82550c95b7
c1ccc(CCC(Cc2ccccc2)N2CCC(c3ccccc3)CC2)cc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
8
HOUR
To a stirred solution of 4-(4-acetamido-4-phenylpiperidino)-2-(3,4-dichlorophenyl)-N-[3,5-bis(trifluoromethyl)benzyl]butylamine (0.4 g) in tetrahydrofuran (4 mL) was added acetic anhydride (0.085 mL) and diisopropylethylamine (0.32 mL). After 2 hours at room temperature 4-dimethylaminopyridine (7 mg) was added and the ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Secondary amide
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
HO-
CN(C1=CC=NC=C1)C.ClCCl.Cl.O.O1CCCC1
null
8
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.CC(=O)OC(C)=O>CN(C1=CC=NC=C1)C.ClCCl.Cl.O.O1CCCC1>CC(=O)NCC(CC(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N1CCC(NC(C)=O)(c2ccccc2)CC1)c1ccc(Cl)c(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-be2035c7c1d141fb862b1d083535d3de
C=O.CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1>>CNCC(CC(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N1CCC(NC(C)=O)(c2ccccc2)CC1)c1ccc(Cl)c(Cl)c1
C(C)(=O)O.C(C)(=O)NC1(CCN(CC1)C(CC(CN)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1.C=O.C(#N)[BH3-].[Na+]>>C(C)(=O)NC1(CCN(CC1)C(CC(CNC)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1
O=[CH2:1].[NH2:2][CH2:3][CH:4]([CH2:5][CH:6]([CH2:7][c:8]1[cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15][c:16]([C:17]([F:18])([F:19])[F:20])[cH:21]1)[N:22]1[CH2:23][CH2:24][C:25]([NH:26][C:27]([CH3:28])=[O:29])([c:30]2[cH:31][cH:32][cH:33][cH:34][cH:35]2)[CH2:36][CH2:37]1)[c:38]1[cH:39][cH:40][c:41]([Cl:42])[c:43]([...
C=O.CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1
CNCC(CC(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N1CCC(NC(C)=O)(c2ccccc2)CC1)c1ccc(Cl)c(Cl)c1
null
null
ClCCl.CO.O.C([O-])(O)=O.[Na+]
Heteroatom Alkylation and Arylation
Reductive methylation of primary amine with formaldehyde
51d235def9103cd7a524cbedb590276839772d481304df37a121e64cb81721f4
cf32f1267c674fd84d46b8a676a46bd4e3a018dea282d34ea9ab93d79b66d0ee
c1ccc(CCC(Cc2ccccc2)N2CCC(c3ccccc3)CC2)cc1
O=[CH2;D1;+0:1].[C:2]-[C:3]-[NH2;D1;+0:4]>>[C:2]-[C:3]-[NH;D2;+0:4]-[CH3;D1;+0:1]
null
[]
0
CELSIUS
null
null
To a stirred solution of 4-(4-acetamido-4-phenylpiperidino)-2-(3,4-dichlorophenyl)-N-[3,5-bis(trifluoromethyl)benzyl]butylamine (0.30 g) in methanol (4 mL) was added aqueous formaldehyde (37% w/w, 0.027 mL). The mixture was cooled to 0° C. and acetic acid (0.038 mL) was added followed by a solution of sodium cyanoboroh...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Primary amine
Secondary amine
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
Other
ClCCl.CO.O.C([O-])(O)=O.[Na+]
0
null
C=O.CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1>ClCCl.CO.O.C([O-])(O)=O.[Na+]>CNCC(CC(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N1CCC(NC(C)=O)(c2ccccc2)CC1)c1ccc(Cl)c(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0f557f1000674f4b902d975b3b805985
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=CO>>CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CNC=O)c2ccc(Cl)c(Cl)c2)CC1
C(=O)O.Cl.CN(CCCN=C=NCC)C.C(C)(=O)NC1(CCN(CC1)C(CC(CN)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1.CN1CCOCC1>>C(C)(=O)NC1(CCN(CC1)C(CC(CNC=O)C1=CC(=C(C=C1)Cl)Cl)CC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C1=CC=CC=C1
[CH3:1][C:2](=[O:3])[NH:4][C:5]1([c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[CH2:12][CH2:13][N:14]([CH:15]([CH2:16][c:17]2[cH:18][c:19]([C:20]([F:21])([F:22])[F:23])[cH:24][c:25]([C:26]([F:27])([F:28])[F:29])[cH:30]2)[CH2:31][CH:32]([CH2:33][NH2:34])[c:37]2[cH:38][cH:39][c:40]([Cl:41])[c:42]([Cl:43])[cH:44]2)[CH2:45][CH2:...
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=CO
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CNC=O)c2ccc(Cl)c(Cl)c2)CC1
null
null
ClCCl.Cl.O
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccc(CCC(Cc2ccccc2)N2CCC(c3ccccc3)CC2)cc1
O-[CH;D2;+0:1]=[O;D1;H0:2].[C:3]-[C:4]-[NH2;D1;+0:5]>>[C:3]-[C:4]-[NH;D2;+0:5]-[CH;D2;+0:1]=[O;D1;H0:2]
null
[]
null
null
15
MINUTE
To a 0° C. solution of formic acid (0.09 mL) in dichloromethane (3 mL) was added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (0.23 g) and the mixture stirred for 15 minutes. To this mixture was added a solution of 4-(4-acetamido-4-phenylpiperidino)-2-(3,4-dichlorophenyl)-N-[3,5-bis(trifluoromethyl)benzy...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
HO-
ClCCl.Cl.O
null
0.25
CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CN)c2ccc(Cl)c(Cl)c2)CC1.O=CO>ClCCl.Cl.O>CC(=O)NC1(c2ccccc2)CCN(C(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC(CNC=O)c2ccc(Cl)c(Cl)c2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4d14267579d347aaab5da8765031fa8d
CC1(N)N=C(O)C=C(O)N1>>Cc1nc(O)cc(O)n1
OC1=NC(NC(=C1)O)(N)C.[O-]CC.[Na+].[Na].Cl.C(C)(=N)N.C(CC(=O)OCC)(=O)OCC>>OC1=NC(=NC(=C1)O)C
N[C:2]1([CH3:1])[N:3]=[C:4]([OH:5])[CH:6]=[C:7]([OH:8])[NH:9]1>>[CH3:1][c:2]1[n:3][c:4]([OH:5])[cH:6][c:7]([OH:8])[n:9]1
CC1(N)N=C(O)C=C(O)N1
Cc1nc(O)cc(O)n1
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
0874d0075314f074b492eff8e0326b779822212aa8c43b93b315cb0c67e901a6
8c3f0b9f773c08a752e3c77dd2b55653809cd7c609bf5f8f068eedde25a3e577
c1cncnc1
N-[C;H0;D4;+0:1]1(-[C;D1;H3:2])-[N;H0;D2;+0:3]=[C;H0;D3;+0:4](-[O;D1;H1:5])-[CH;D2;+0:6]=[C;H0;D3;+0:7](-[O;D1;H1:8])-[NH;D2;+0:9]-1>>[C;D1;H3:2]-[c;H0;D3;+0:1]1:[n;H0;D2;+0:3]:[c;H0;D3;+0:4](-[O;D1;H1:5]):[cH;D2;+0:6]:[c;H0;D3;+0:7](-[O;D1;H1:8]):[n;H0;D2;+0:9]:1
null
[]
null
null
3.5
HOUR
The first intermediate, 4,6-dihydroxy-2-methylpyrimidinamine, is synthesized by preparing sodium ethoxide in situ from sodium and an hydrous ethanol under a nitrogen blanket. Acetamidine hydrochloride and diethyl malonate are added and the reaction mixture heated to boiling for 2 to 5 hours to afford 4,6-dihydroxy-2-me...
10.6084/m9.figshare.5104873.v1
null
Enamine.Enol.Primary amine
Aromatic alcohol.Aromatic alcohol
C1=CNCN=C1
c1cncnc1
c1cncnc1
Other
C(C)O
null
3.5
CC1(N)N=C(O)C=C(O)N1>C(C)O>Cc1nc(O)cc(O)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fc482eaeb84f48f6beade7036825e8ec
Cc1nc(Cl)c([N+](=O)[O-])c(Cl)n1>>Cc1nc(Cl)c(N)c(Cl)n1
ClC1=NC(=NC(=C1[N+](=O)[O-])Cl)C>>ClC1=NC(=NC(=C1N)Cl)C
O=[N+:7]([O-])[c:6]1[c:4]([Cl:5])[n:3][c:2]([CH3:1])[n:10][c:8]1[Cl:9]>>[CH3:1][c:2]1[n:3][c:4]([Cl:5])[c:6]([NH2:7])[c:8]([Cl:9])[n:10]1
Cc1nc(Cl)c([N+](=O)[O-])c(Cl)n1
Cc1nc(Cl)c(N)c(Cl)n1
null
[Ni]
C1(=CC=CC=C1)C
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1cncnc1
O=[N+;H0;D3:1](-[O-])-[c:2]1:[c:3](-[Cl;D1;H0:4]):[#7;a:5]:[c:6]:[#7;a:7]:[c:8]:1-[Cl;D1;H0:9]>>[Cl;D1;H0:4]-[c:3]1:[#7;a:5]:[c:6]:[#7;a:7]:[c:8](-[Cl;D1;H0:9]):[c:2]:1-[NH2;D1;+0:1]
null
[]
null
null
null
null
The third intermediate, 4,6-dichloro-2-methyl-5-nitropyrimidine is hydrogenated over Raney-Ni as a 10% to 30% solution in toluene to afford the corresponding compound, 4,6-dichloro-2-methyl-5-aminopyrimidine, as a fourth intermediate. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1cncnc1
Other
[Ni].C1(=CC=CC=C1)C
null
null
Cc1nc(Cl)c([N+](=O)[O-])c(Cl)n1>[Ni].C1(=CC=CC=C1)C>Cc1nc(Cl)c(N)c(Cl)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-034dc9437bee48c3847af5a6f9237cbd
CC(=O)N1CCNC1=Nc1c(Cl)nc(C)nc1Cl.C[O-]>>COc1nc(C)nc(Cl)c1N=C1NCCN1
C(C)(=O)N1C(NCC1)=NC=1C(=NC(=NC1Cl)C)Cl.C[O-].[Na+].[Na].C[O-].[Na+]>>ClC1=NC(=NC(=C1N=C1NCCN1)OC)C
CC(=O)[N:16]1[C:12](=[N:11][c:10]2[c:3](Cl)[n:4][c:5]([CH3:6])[n:7][c:8]2[Cl:9])[NH:13][CH2:14][CH2:15]1.[CH3:1][O-:2]>>[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([Cl:9])[c:10]1[N:11]=[C:12]1[NH:13][CH2:14][CH2:15][NH:16]1
CC(=O)N1CCNC1=Nc1c(Cl)nc(C)nc1Cl.C[O-]
COc1nc(C)nc(Cl)c1N=C1NCCN1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
261cb092c646fb8b95a4c4b3353ba2904f492f41dd6b7d7795ebd05c8fac5a3d
365bcfafcdf9c10eed012708b51c1f4254f563747f5b31fee043d8c008793122
c1ncc(N=C2NCCN2)cn1
C-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-1=[#7:6]-[c:7]1:[c:8](-[Cl;D1;H0:9]):[#7;a:10]:[c:11]:[#7;a:12]:[c;H0;D3;+0:13]:1-Cl.[C;D1;H3:14]-[O-;H0;D1:15]>>[C;D1;H3:14]-[O;H0;D2;+0:15]-[c;H0;D3;+0:13]1:[#7;a:12]:[c:11]:[#7;a:10]:[c:8](-[Cl;D1;H0:9]):[c:7]:1-[#7:6]=[C:5]1-[#7:4]-[C:3]-[C:2]-[NH;D2;+0:1]-1
null
[]
null
null
null
null
The final product, 4-chloro-N-(imidazolin-2-ylidene)-6-methoxy-2-methyl-5-pyrimidinamine is synthesized by first preparing sodium methoxide in situ from anhydrous methanol and sodium. The fifth intermediate, N-(1-acetylimidazolin-2-ylidene)-4,6-dichloro-2-methyl-5-pyrimidinamine, is added and the reaction mixture broug...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Tertiary amide
Ether.Secondary amine
C1C[NH]CN1.c1cncnc1
c1cncnc1.C1CNCN1
c1cncnc1.C1CNCN1
HCl
CO
null
null
CC(=O)N1CCNC1=Nc1c(Cl)nc(C)nc1Cl.C[O-]>CO>COc1nc(C)nc(Cl)c1N=C1NCCN1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0f828e1e7cdc4b0fbb57ab56bd4b3b86
O=S(=O)(O)O.Oc1ccccc1>>O=S(=O)(O)c1ccc(O)cc1
OS(=O)(=O)O.O=S(=O)=O.C1(=CC=CC=C1)O>>C1=CC(=CC=C1O)S(=O)(=O)O
O[S:2](=[O:1])(=[O:3])[OH:4].[cH:5]1[cH:6][cH:7][c:8]([OH:9])[cH:10][cH:11]1>>[O:1]=[S:2](=[O:3])([OH:4])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:10][cH:11]1
O=S(=O)(O)O.Oc1ccccc1
O=S(=O)(O)c1ccc(O)cc1
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].[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[O;D1;H0:2]=[S;H0;D4;+0:1](=[O;D1;H0:3])(-[O;D1;H1:4])-[c;H0;D3;+0:7](:[c:6]:[c:5]):[c:8]:[c:9]
null
[]
null
null
1
HOUR
440 parts of 66% oleum are added slowly at from 60° to 70° C. to 500 parts of melted phenol, and the mixture is subsequently sulfonated at 100° C. for 1 hour. The phenolsulfonic acid formed is then slowly heated at from 160° to 165° C. in a vacuum of from about 11 to 13 mm, so that only a little phenol distils off, and...
10.6084/m9.figshare.5104873.v1
null
null
Sulfonic acid
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
1
O=S(=O)(O)O.Oc1ccccc1>>O=S(=O)(O)c1ccc(O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-86496e40601a420c9b4fe32d008df94f
O=S(=O)(O)O.Oc1ccccc1>>O=S(=O)(O)c1ccc(O)cc1
OS(=O)(=O)O.O=S(=O)=O.C1(=CC=CC=C1)O>>C1=CC(=CC=C1O)S(=O)(=O)O
O[S:2](=[O:1])(=[O:3])[OH:4].[cH:5]1[cH:6][cH:7][c:8]([OH:9])[cH:10][cH:11]1>>[O:1]=[S:2](=[O:3])([OH:4])[c:5]1[cH:6][cH:7][c:8]([OH:9])[cH:10][cH:11]1
O=S(=O)(O)O.Oc1ccccc1
O=S(=O)(O)c1ccc(O)cc1
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].[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[O;D1;H0:2]=[S;H0;D4;+0:1](=[O;D1;H0:3])(-[O;D1;H1:4])-[c;H0;D3;+0:7](:[c:6]:[c:5]):[c:8]:[c:9]
null
[]
null
null
1
HOUR
478 parts of 20% oleum are added with stirring to 500 parts of melted phenol, with cooling to ensure that the temperature does not exceed 70° C. The mixture is then sulfonated at 105° C. for 1 hour. The phenolsulfonic acid formed is heated slowly at from 150° to 155° C. under reduced pressure of 11 to 13 torr, and this...
10.6084/m9.figshare.5104873.v1
null
null
Sulfonic acid
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
1
O=S(=O)(O)O.Oc1ccccc1>>O=S(=O)(O)c1ccc(O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-99680520cbc245bc8e09a95648450d19
C=CC(=O)OC.O=C(O)CNCC(=O)O>>COC(=O)CCN(CC(=O)O)CC(=O)O
C(C=C)(=O)OC.Cl.[OH-].[Na+].C(C=C)(=O)OC.N(CC(=O)O)CC(=O)O>>C(=O)(O)CN(CCC(=O)OC)CC(=O)O
[CH3:1][O:2][C:3](=[O:4])[CH:5]=[CH2:6].[NH:7]([CH2:8][C:9](=[O:10])[OH:11])[CH2:12][C:13](=[O:14])[OH:15]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][N:7]([CH2:8][C:9](=[O:10])[OH:11])[CH2:12][C:13](=[O:14])[OH:15]
C=CC(=O)OC.O=C(O)CNCC(=O)O
COC(=O)CCN(CC(=O)O)CC(=O)O
null
null
O
Heteroatom Alkylation and Arylation
aza-Michael addition secondary
281338207899411a693d475f5874e69a953d9793da7289fa7cfd38421de9c393
e6898c28c2a6b7f7f5b5322689c9c6b3b6ad3dd52268b1e45ad4c4843df05f7d
null
[C;D1;H3:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH;D2;+0:5]=[CH2;D1;+0:6].[O;D1;H0:7]=[C:8](-[O;D1;H1:9])-[C:10]-[NH;D2;+0:11]-[C:12]-[C:13](=[O;D1;H0:14])-[O;D1;H1:15]>>[C;D1;H3:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[N;H0;D3;+0:11](-[C:12]-[C:13](=[O;D1;H0:14])-[O;D1;H1:15])-[C:10]-[C:8](=[O;D1;H0:7])-[O;D...
96
[{"value": 96.0, "product": "C(=O)(O)CN(CCC(=O)OC)CC(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
6
HOUR
133 g (1.00 mol) of iminodiacetic acid were dissolved in 530 ml of water, and the solution was adjusted to pH 7.0 with 40.5 g (1.00 mol) of solid NaOH. 86.0 g (1.00 mol) of methyl acrylate were added dropwise to this solution at 20° C., and the mixture was then stirred for 6 h. The methyl acrylate content after this ti...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine.Vinyl
Ester.Tertiary amine
null
null
null
null
O
null
6
C=CC(=O)OC.O=C(O)CNCC(=O)O>O>COC(=O)CCN(CC(=O)O)CC(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a90868bcdfa84bafb88a66b6d780809a
O=S(=O)(O)O>>O=S(=O)(O)O
[OH-].[Na+].S(O)(O)(=O)=O.NC(=O)N>>S(O)(O)(=O)=O.NC(=O)N
[O:5]=[S:6](=[O:7])([OH:8])[OH:9]>>[O:5]=[S:6](=[O:7])([OH:8])[OH:9]
O=S(=O)(O)O
O=S(=O)(O)O
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
Prilled urea (17.5 grams, 0.29 moles) was dissolved in 53.5 grams water. To this solution was slowly added sulfuric acid (29.0 grams, 0.26 moles, 89.3%) at 66° C. The temperature was maintained below 50° C. in a cooling bath during the addition. The final solution on titration with 0.5N NaOH (phenolphthalein indicator)...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
O
null
null
O=S(=O)(O)O>O>O=S(=O)(O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-889d3fb76dc4464094f72ea8e4bc1474
C=CC(N)=O.CC(C)(N=NC(C)(C)C1=NCCN1)C1=NCCN1.Cl>>C=CC(N)=O.CCl
C(C=C)(=O)N.[Cl-].C(C=C)(=O)OCC.C(CN(CC(=O)O)CC(=O)O)N(CC(=O)O)CC(=O)O.Cl.Cl.N(=NC(C)(C)C=1NCCN1)C(C)(C)C=1NCCN1>>C(C=C)(=O)N.CCl.C(C=C)(=O)OCC
[CH2:8]=[CH:9][C:10]([NH2:11])=[O:12].CC(C)(N=NC(C)(C1=NCCN1)[CH3:13])C1=NCCN1.[ClH:14]>>[CH2:8]=[CH:9][C:10]([NH2:11])=[O:12].[CH3:13][Cl:14]
C=CC(N)=O.CC(C)(N=NC(C)(C)C1=NCCN1)C1=NCCN1.Cl
C=CC(N)=O.CCl
null
null
O
Miscellaneous
OtherReaction
785bce4c0acb75870b3148764a843e343dc0cf0c38ae2dfc11375d60a1898def
f031920ffd7a64c0e3bc8da8b6bdfc5c52af5440f2051d430a793359451db646
null
C-C(-C)(-N=N-C(-C)(-[CH3;D1;+0:1])-C1=N-C-C-N-1)-C1=N-C-C-N-1.[ClH;D0;+0:2]>>[CH3;D1;+0:1]-[Cl;H0;D1;+0:2]
10
[{"value": 10.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A 10% solution of poly(AMD/DMAEA.MeCl/EA) was prepared as follows: 13.87 parts of 53.58% aqueous acrylamide (AMD), 25.31 parts of a 80% aqueous solution of ethacryloxyethyltrimethylammonium chloride (DMAEA.MeCl), 2.33 parts of ethyl acrylate (EA), 0.3 part EDTA, 258.16 parts of deionized water and 0.030 parts of VA-044...
10.6084/m9.figshare.5104873.v1
null
Diazene.Secondary amine.Secondary amine
null
C1=NCCN1.C1=NCCN1
null
null
Other
O
null
1
C=CC(N)=O.CC(C)(N=NC(C)(C)C1=NCCN1)C1=NCCN1.Cl>O>C=CC(N)=O.CCl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-174ccccc38a64a6887d340e17eeb43b4
O=[N+]([O-])c1ccc(F)cc1.OCC(F)(F)F>>O=[N+]([O-])c1ccc(OCC(F)(F)F)cc1
O.[Na].FC1=CC=C(C=C1)[N+](=O)[O-].FC(CO)(F)F>>FC(COC1=CC=C(C=C1)[N+](=O)[O-])(F)F
F[c:7]1[cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:15][cH:14]1.[OH:8][CH2:9][C:10]([F:11])([F:12])[F:13]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([O:8][CH2:9][C:10]([F:11])([F:12])[F:13])[cH:14][cH:15]1
O=[N+]([O-])c1ccc(F)cc1.OCC(F)(F)F
O=[N+]([O-])c1ccc(OCC(F)(F)F)cc1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[F;D1;H0:6]-[C:7](-[F;D1;H0:8])(-[F;D1;H0:9])-[C:10]-[OH;D1;+0:11]>>[F;D1;H0:6]-[C:7](-[F;D1;H0:8])(-[F;D1;H0:9])-[C:10]-[O;H0;D2;+0:11]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
62
[{"value": 62.0, "product": "FC(COC1=CC=C(C=C1)[N+](=O)[O-])(F)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Under a nitrogen atmosphere, 10.1 g (0.44 mol) of sodium was dissolved in 200 ml of 2,2,2-trifluoro ethanol in 300 ml of a three-necked flask, to which 40 ml (0.38 mol) of p-fluoronitro benzene was dropped and refluxed for 4 hours. After cooling to a room temperature, water was poured (about 1 liter), and precipitated ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1
HF
null
null
null
O=[N+]([O-])c1ccc(F)cc1.OCC(F)(F)F>>O=[N+]([O-])c1ccc(OCC(F)(F)F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-785e0a0408f94a47b06e9ceee5b1cfa9
O=[N+]([O-])c1ccc(OCC(F)(F)F)cc1>>Nc1ccc(OCC(F)(F)F)cc1
FC(COC1=CC=C(C=C1)[N+](=O)[O-])(F)F.C(C)O.Cl>>FC(COC1=CC=C(N)C=C1)(F)F
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]([O:6][CH2:7][C:8]([F:9])([F:10])[F:11])[cH:12][cH:13]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([O:6][CH2:7][C:8]([F:9])([F:10])[F:11])[cH:12][cH:13]1
O=[N+]([O-])c1ccc(OCC(F)(F)F)cc1
Nc1ccc(OCC(F)(F)F)cc1
null
null
O
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]
94
[{"value": 94.0, "product": "FC(COC1=CC=C(N)C=C1)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.9, "product": "FC(COC1=CC=C(N)C=C1)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In a nitrogen atmosphere, 30.1 g (0.14 mol) of p-(2,2,2-trifluroethoxy) nitrobenzene, 82.1 g (1.47 mol) of reduced iron, 120 ml of ethanol and 40 ml of water were placed in a three-necked flask, to which 1.4 ml of concentrated hydrochloric acid was dropped under stirring and then refluxed for one hour. After cooling to...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
O
null
null
O=[N+]([O-])c1ccc(OCC(F)(F)F)cc1>O>Nc1ccc(OCC(F)(F)F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9102e88c394640fc8efd773b9c3e0835
O=P(O)(O)O.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3>>O=P([O-])([O-])OP(=O)([O-])[O-]
[O-2].[O-2].[Ti+4].[O-2].[O-2].[Ti+4].O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3.[O-2].[O-2].[Ti+4].P(O)(O)(O)=O.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3>>[O-]P([O-])(=O)OP(=O)([O-])[O-].[Ti+4]
[O:1]=[P:2]([OH:3])([OH:4])[OH:5].O=P12OP3(=O)OP(=O)(O1)[O:9][P:6](=[O:7])(O2)[O:8]3>>[O:1]=[P:2]([O-:3])([O-:4])[O:5][P:6](=[O:7])([O-:8])[O-:9]
O=P(O)(O)O.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3
O=P([O-])([O-])OP(=O)([O-])[O-]
null
null
null
Functional Group Interconversion
OtherReaction
984d7e95798f9d2c581130f421f542f9bc9ee9e6dd52cb07273abd9cc125b05b
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
null
O=P12-O-P3(=O)-O-P(=O)(-O-1)-[O;H0;D2;+0:1]-[P;H0;D4;+0:2](=[O;D1;H0:3])(-O-2)-[O;H0;D2;+0:4]-3.[O;D1;H0:5]=[#15:6](-[OH;D1;+0:7])(-[OH;D1;+0:8])-[OH;D1;+0:9]>>[O-;H0;D1:7]-[#15:6](-[O-;H0;D1:8])(=[O;D1;H0:5])-[O;H0;D2;+0:9]-[P;H0;D4;+0:2](-[O-;H0;D1:4])(-[O-;H0;D1:1])=[O;D1;H0:3]
null
[]
null
null
null
null
The method of the present invention generally involves the mixture of titanium dioxide and hot concentrated phosphoric acid in a reaction vessel. The reaction mixture has a phosphorus pentoxide to titanium dioxide mole ratio greater than one. Preferably, the phosphorus pentoxide to titanium dioxide mole ratio is about ...
10.6084/m9.figshare.5104873.v1
null
null
null
O1P2OP3OP1OP(O2)O3
null
null
HO-
null
null
null
O=P(O)(O)O.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3>>O=P([O-])([O-])OP(=O)([O-])[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-36aa7f1e188145b59bcac8eea2adfe61
O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3>>O=P([O-])([O-])OP(=O)([O-])[O-]
[O-2].[O-2].[Ti+4].[O-2].[O-2].[Ti+4].P(O)(O)(O)=O.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3>>[O-]P([O-])(=O)OP(=O)([O-])[O-].[Ti+4]
O=P12OP3(=O)[O:3][P:2](=[O:1])([O:4]1)[O:5][P:6](=[O:7])([O:8]2)[O:9]3>>[O:1]=[P:2]([O-:3])([O-:4])[O:5][P:6](=[O:7])([O-:8])[O-:9]
O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3
O=P([O-])([O-])OP(=O)([O-])[O-]
null
null
null
Functional Group Interconversion
OtherReaction
984d7e95798f9d2c581130f421f542f9bc9ee9e6dd52cb07273abd9cc125b05b
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
null
O=P12-O-P3(=O)-[O;H0;D2;+0:1]-[#15:2](=[O;D1;H0:3])(-[#8:4]-[#15:5](=[O;D1;H0:6])(-[O;H0;D2;+0:7]-1)-[O;H0;D2;+0:8]-3)-[O;H0;D2;+0:9]-2>>[O-;H0;D1:1]-[#15:2](-[O-;H0;D1:9])(=[O;D1;H0:3])-[#8:4]-[#15:5](-[O-;H0;D1:7])(-[O-;H0;D1:8])=[O;D1;H0:6]
90
[{"value": 90.0, "product": "[O-]P([O-])(=O)OP(=O)([O-])[O-].[Ti+4]", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
thermally reacting titanium dioxide and phosphoric acid at a temperature of about 400° C. to about 500° C. in a reaction mixture having a phosphorus pentoxide to titanium dioxide mole ratio of about 1.20 to about 1.25 to form a fine titanium pyrophosphate powder with greater than 90% of said fine titanium pyrophosphate...
10.6084/m9.figshare.5104873.v1
null
null
null
O1P2OP3OP1OP(O2)O3
null
null
Other
null
null
null
O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3>>O=P([O-])([O-])OP(=O)([O-])[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dba6f3dde0664944932faac3af102356
CI.COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OCc1ccccc1>>COC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)OCc1ccccc1
IC.COC([C@@H](NC(=O)OCC1=CC=CC=C1)CC1=CC=C(C=C1)O)=O.C([O-])([O-])=O.[K+].[K+]>>COC([C@@H](NC(=O)OCC1=CC=CC=C1)CC1=CC=C(C=C1)OC)=O
I[CH3:12].[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([OH:11])[cH:13][cH:14]1)[NH:15][C:16](=[O:17])[O:18][CH2:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1>>[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13][cH:14]1)[NH:15][C:16](=[O:17])[O:18][CH2:19][c:20]1[...
CI.COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OCc1ccccc1
COC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)OCc1ccccc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
b8b041187bac58376aae824630608e7deb49a01db3d652291f8b379c10d4e434
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
O=C(NCCc1ccccc1)OCc1ccccc1
I-[CH3;D1;+0:1].[OH;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
8
HOUR
32.94 g (100 mmol) of N-benzyloxycarbonyl-tyrosine methyl ester is mixed in 200 ml of DMF with 27.64 g (200 mmol) of ground potassium carbonate. 15.6 g (110 mmol) of iodomethane is instilled in this suspension and stirred overnight at room temperature. The solution is concentrated by evaporation, dispersed between ethy...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HI
CN(C)C=O
null
8
CI.COC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OCc1ccccc1>CN(C)C=O>COC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2219c1d1d75847559c21756e148ff10b
CC(=O)c1ccc2c(c1)CC(C)O2.OBr>>CC1Cc2cc(C(=O)O)ccc2O1
Cl.BrBr.[OH-].[Na+].C(C)(=O)C=1C=C2CC(OC2=CC1)C.BrO>>C(=O)(O)C=1C=C2CC(OC2=CC1)C
C[C:7]([c:6]1[cH:5][c:4]2[c:12]([cH:11][cH:10]1)[O:13][CH:2]([CH3:1])[CH2:3]2)=[O:8].Br[OH:9]>>[CH3:1][CH:2]1[CH2:3][c:4]2[cH:5][c:6]([C:7](=[O:8])[OH:9])[cH:10][cH:11][c:12]2[O:13]1
CC(=O)c1ccc2c(c1)CC(C)O2.OBr
CC1Cc2cc(C(=O)O)ccc2O1
null
null
O.O1CCOCC1
Acylation
OtherReaction
e1d216f9ec5d1e0ab04cbd7e284acaaebe679828044d718ad57104584ff5302e
7b5bc8122b5027b4d965c982eed9443b26b90bd801407eec9b2b367c037fc8de
c1ccc2c(c1)CCO2
Br-[OH;D1;+0:1].C-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]>>[O;D1;H0:3]=[C;H0;D3;+0:2](-[OH;D1;+0:1])-[c:4](:[c:5]):[c:6]
57.4
[{"value": 57.4, "product": "C(=O)(O)C=1C=C2CC(OC2=CC1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.4, "product": "C(=O)(O)C=1C=C2CC(OC2=CC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
On an ice-common salt bath, 6.25 ml of bromine was added dropwise to a solution of 15.1 g of sodium hydroxide in 100 ml of water under stirring and cooling. To a solution of 6.50 g of 5-acetyl-2-methyl coumaran (Ml) in 100 ml of dioxane, the above mixture (i.e., hypobromous acid solution) was added dropwise at 3°-8° C....
10.6084/m9.figshare.5104873.v1
null
Ketone
Carboxylic acid
null
null
c1ccc2c(c1)CCO2
HBr
O.O1CCOCC1
null
null
CC(=O)c1ccc2c(c1)CC(C)O2.OBr>O.O1CCOCC1>CC1Cc2cc(C(=O)O)ccc2O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-74043014bdd746ff9751b62ff8d91839
CC1Cc2cc(C(=N)N)ccc2O1.CC1Cc2cc(C(=O)O)ccc2O1>>CCCCCCCCc1ccc(-c2cnc(-c3ccc4c(c3)CC(C)O4)nc2)cc1
C[O-].[Na+].Cl.C(N)(=N)C=1C=C2CC(OC2=CC1)C.C(=O)(O)C=1C=C2CC(OC2=CC1)C>>CC1OC2=CC=C(C=C2C1)C1=NC=C(C=N1)C1=CC=C(C=C1)CCCCCCCC
[NH2:15][C:16]([c:17]1[cH:18][cH:19][c:20]2[c:21]([cH:22]1)[CH2:23][CH:24]([CH3:25])[O:26]2)=[NH:27].O=[C:13](O)[c:12]1[cH:5][c:4]2[c:9]([cH:30][cH:29]1)O[CH:2]([CH3:1])[CH2:3]2>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][c:9]1[cH:10][cH:11][c:12](-[c:13]2[cH:14][n:15][c:16](-[c:17]3[cH:18][cH:19][c:20]4[...
CC1Cc2cc(C(=N)N)ccc2O1.CC1Cc2cc(C(=O)O)ccc2O1
CCCCCCCCc1ccc(-c2cnc(-c3ccc4c(c3)CC(C)O4)nc2)cc1
null
null
CO
C-C Coupling
OtherReaction
32ea512a0b0c0a08f0b1a65f4ed6194340dc244897306482934e9b45d932f117
8c413d7c50ade1af88c69e9a2a3bf780b58b3c8c53f942b06480db8d8f10a730
c1ccc(-c2cnc(-c3ccc4c(c3)CCO4)nc2)cc1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[c;H0;D3;+0:5]2:[c;H0;D3;+0:6](:[cH;D2;+0:7]:1)-[C:8]-[CH;D3;+0:9](-[C;D1;H3:10])-O-2.[NH2;D1;+0:11]-[C;H0;D3;+0:12](=[NH;D1;+0:13])-[c;H0;D3;+0:14](:[c:15]:[c:16]):[c:17]:[c:18]>>[C;D1;H3:10]-[CH2;D2;+0:9]-[C:8]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[C:19]-[C:20]-[C:21]-[c;H0;D3;...
58.4
[{"value": 58.4, "product": "CC1OC2=CC=C(C=C2C1)C1=NC=C(C=N1)C1=CC=C(C=C1)CCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
0.40 g (1.88 mM) of 5-amidino-2-methylcoumaran hydrochloride (M5) as an intermediate product prepared in Example 1, 0.79 g (1.90 mM) of 3-dimethylamino-2-(4-octylphenyl)-N,N-dimethylpropene-(2)-ammonium perchlorate 0.41 g (7.59 mM) of sodium methylate and 15 ml of methanol were placed in a 50 ml-round bottomed flask an...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether.Primary amine
null
c1ccc2c(c1)CCO2
c1ccccc1.c1cncnc1
c1ccccc1.c1cncnc1.c1ccc2c(c1)CCO2
null
CO
null
null
CC1Cc2cc(C(=N)N)ccc2O1.CC1Cc2cc(C(=O)O)ccc2O1>CO>CCCCCCCCc1ccc(-c2cnc(-c3ccc4c(c3)CC(C)O4)nc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7cfb9a4aa79d4897a5745b991d796205
CCCCCCCCC(=O)OC(=O)CCCCCCCC.Oc1ccccc1C[P+](c1ccccc1)(c1ccccc1)c1ccccc1>>CCCCCCCCc1cc2ccccc2o1
C(C)N(CC)CC.[Br-].OC1=C(C[P+](C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2)C=CC=C1.C(CCCCCCCC)(=O)OC(CCCCCCCC)=O>>C(CCCCCCC)C=1OC2=C(C1)C=CC=C2
CCCCCCCCC(=O)O[C:9](=O)[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].c1ccc([P+](c2ccccc2)(c2ccccc2)[CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[OH:17])cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][c:9]1[cH:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[o:17]1
CCCCCCCCC(=O)OC(=O)CCCCCCCC.Oc1ccccc1C[P+](c1ccccc1)(c1ccccc1)c1ccccc1
CCCCCCCCc1cc2ccccc2o1
null
null
C1(=CC=CC=C1)C
Miscellaneous
OtherReaction
06e94a6dcd746736c6cf6cc292284b9776b898eaa1042b8cc777d98ad50eab2b
6720b0fe7909c5c14b6890f35a7242cac504e521ec14a785321a1fee7a7aa3da
c1ccc2occc2c1
C-C-C-C-C-C-C-C-C(=O)-O-[C;H0;D3;+0:1](=O)-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7](-[CH2;D2;+0:8]-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1):[c:9]>>[C:3]-[C:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:8]:[c:7](:[c:9]):[c:5](:[c:6]):[o;H0;D2;+0:4]:1
76.6
[{"value": 76.6, "product": "C(CCCCCCC)C=1OC2=C(C1)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
112 g (249 mM) of (2-hydroxybenzyl)triphenylphosphonium bromide, 83 g (278 mM) of nonanoic anhydride, 104 g (1.03 mM) of triethylamine and 800 ml of toluene were placed in a 3 1-three-necked flask, followed by refluxing for 4.5 hours under stirring. After the reaction, the reaction mixture was left standing at room tem...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Aromatic alcohol
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccc2occc2c1
c1ccc2occc2c1
HO-
C1(=CC=CC=C1)C
null
null
CCCCCCCCC(=O)OC(=O)CCCCCCCC.Oc1ccccc1C[P+](c1ccccc1)(c1ccccc1)c1ccccc1>C1(=CC=CC=C1)C>CCCCCCCCc1cc2ccccc2o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f28ffd070d2241e988f52b5c36d20b5d
CCCCCCCCc1cc2ccccc2o1>>CCCCCCCCC1Cc2ccccc2O1
C(CCCCCCC)C=1OC2=C(C1)C=CC=C2>>C(CCCCCCC)C1OC2=CC=CC=C2C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][c:9]1[cH:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[o:17]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH:9]1[CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[O:17]1
CCCCCCCCc1cc2ccccc2o1
CCCCCCCCC1Cc2ccccc2O1
null
[C].[Pd]
C(C)O
Reduction
OtherReaction
b86bd3f15ad056b18f24f98e80df6dc8108bba5322ef4250b69a51408c14b3cb
7ece147c6909fe307632f67c21e1517a1747c8ff389dff4b19e644c711d1d84d
c1ccc2c(c1)CCO2
[C:1]-[C:2]-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[c:5](:[c:6]):[c:7](:[c:8]):[o;H0;D2;+0:9]:1>>[C:1]-[C:2]-[CH;D3;+0:3]1-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7](:[c:8])-[O;H0;D2;+0:9]-1
94.6
[{"value": 94.6, "product": "C(CCCCCCC)C1OC2=CC=CC=C2C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Then, 44 g of 2-octylbenzofuran was dissolved in 440 ml of ethanol. To the solution 35 g of 10%-palladium-carbon was added to effect catalytic reduction for 3 hours sunder normal pressure. After the reaction, the catalyst was removed by filtration and the filtrate was concentrated under reduced pressure to obtain a res...
10.6084/m9.figshare.5104873.v1
null
null
Ether
c1ccc2occc2c1
c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2
null
[C].[Pd].C(C)O
null
null
CCCCCCCCc1cc2ccccc2o1>[C].[Pd].C(C)O>CCCCCCCCC1Cc2ccccc2O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0e0dacda86084c48b46139c9f6c1c731
BrBr.CCCCCCCCC1Cc2ccccc2O1>>CCCCCCCCC1Cc2cc(Br)ccc2O1
C(CCCCCCC)C1OC2=CC=CC=C2C1.BrBr.C(=O)(O)[O-].[Na+].O>>BrC=1C=C2CC(OC2=CC1)CCCCCCCC
Br[Br:14].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH:9]1[CH2:10][c:11]2[cH:12][cH:13][cH:15][cH:16][c:17]2[O:18]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH:9]1[CH2:10][c:11]2[cH:12][c:13]([Br:14])[cH:15][cH:16][c:17]2[O:18]1
BrBr.CCCCCCCCC1Cc2ccccc2O1
CCCCCCCCC1Cc2cc(Br)ccc2O1
null
null
ClCCl
Functional Group Interconversion
Bromination
8a5899f39c577ae2f5dbb7e89484f9814910050aa00e810b5c8bafb1acd06dbc
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2c(c1)CCO2
Br-[Br;H0;D1;+0:1].[c:2]:[c:3]:[cH;D2;+0:4]:[c:5]:[c:6]>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:4](:[c:3]:[c:2]):[c:5]:[c:6]
96.3
[{"value": 96.3, "product": "BrC=1C=C2CC(OC2=CC1)CCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
In a 50 ml-three-necked flask, 2.00 g (8.61 mM) of 2-octylcoumaran and 3.2 ml of dichloremethane were placed and mixed to obtain a solution. To the solution, 0.73 (8.69 mM) of NaHCO3 and 3.2 ml of water were added. To the mixture, a solution of 0.44 ml (0.54 mM) of bromine in 1 ml of dichloromethane were added dropwise...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2
HBr
ClCCl
null
null
BrBr.CCCCCCCCC1Cc2ccccc2O1>ClCCl>CCCCCCCCC1Cc2cc(Br)ccc2O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bcf47efb084b407da3df0c21bd581e1b
CC(C)OB(OC(C)C)OC(C)C.CCCCCCC(Br)CC1Cc2ccccc2O1>>CCCCCCCCC1Cc2cc(B(O)O)ccc2O1
O.C(C)(C)OB(OC(C)C)OC(C)C.BrC(CC1OC2=CC=CC=C2C1)CCCCCC.C(CCC)[Li]>>C(CCCCCCC)C1OC2=CC=C(C=C2C1)B(O)O
CC(C)O[B:14]([O:15]C(C)C)[O:16]C(C)C.Br[CH:7]([CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[CH2:8][CH:9]1[CH2:10][c:11]2[cH:12][cH:13][cH:17][cH:18][c:19]2[O:20]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH:9]1[CH2:10][c:11]2[cH:12][c:13]([B:14]([OH:15])[OH:16])[cH:17][cH:18][c:19]2[O:20]1
CC(C)OB(OC(C)C)OC(C)C.CCCCCCC(Br)CC1Cc2ccccc2O1
CCCCCCCCC1Cc2cc(B(O)O)ccc2O1
null
null
C1CCOC1.CCCCCC
Miscellaneous
OtherReaction
04f258477ada574ec7deb70066f24e9226c81b4144647bddc16f35f3ab7f443f
439f75838a365ac96edb92157a4b914b608bcaa4f1e95debd26b1d95d818cefc
c1ccc2c(c1)CCO2
Br-[CH;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C:5]-[#8:6].[c:7]:[c:8]:[cH;D2;+0:9]:[c:10]:[c:11].C-C(-C)-O-[B;H0;D3;+0:12](-[O;H0;D2;+0:13]-C(-C)-C)-[O;H0;D2;+0:14]-C(-C)-C>>[#8:6]-[C:5]-[C:4]-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:13]-[B;H0;D3;+0:12](-[OH;D1;+0:14])-[c;H0;D3;+0:9](:[c:8]:[c:7]):[c:10]:[c:11]
67.1
[{"value": 67.1, "product": "C(CCCCCCC)C1OC2=CC=C(C=C2C1)B(O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Then, 2.00 g (6.43 mM) of b-bromo-2-octylcoumaran and 28 ml of dry THF were placed in a 100 ml-three-necked flask. To the mixture, 4.5 ml (7.20 mM) of a 1.6M solution of butyllithium in hexane was added dropwise under stirring and nitrogen atmosphere on a dry ice-acetone bath at an inner temperature of -70° to -68° C.,...
10.6084/m9.figshare.5104873.v1
null
Secondary halide
Boronic acid
c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2
c1ccc2c(c1)CCO2
HBr
C1CCOC1.CCCCCC
null
null
CC(C)OB(OC(C)C)OC(C)C.CCCCCCC(Br)CC1Cc2ccccc2O1>C1CCOC1.CCCCCC>CCCCCCCCC1Cc2cc(B(O)O)ccc2O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-03e5f7ccfb154de09af0ec7af5397bc8
CCCCCCCCC1Cc2cc(B(O)O)ccc2O1.CCCCCCCCCCc1cnc(Cl)nc1>>CCCCCCCCCCc1cnc(-c2ccc3c(c2)CC(CCCCCCCC)O3)nc1
C([O-])([O-])=O.[Na+].[Na+].C(CCCCCCC)C1OC2=CC=C(C=C2C1)B(O)O.ClC1=NC=C(C=N1)CCCCCCCCCC.C1=CC=CC=C1>>C(CCCCCCCCC)C=1C=NC(=NC1)C=1C=C2CC(OC2=CC1)CCCCCCCC
OB(O)[c:15]1[cH:16][cH:17][c:18]2[c:19]([cH:20]1)[CH2:21][CH:22]([CH2:23][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH3:30])[O:31]2.Cl[c:14]1[n:13][cH:12][c:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:33][n:32]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][C...
CCCCCCCCC1Cc2cc(B(O)O)ccc2O1.CCCCCCCCCCc1cnc(Cl)nc1
CCCCCCCCCCc1cnc(-c2ccc3c(c2)CC(CCCCCCCC)O3)nc1
null
[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
O
C-C Coupling
Suzuki coupling with boronic acids
651f57f47af816cdb773c531ed2942d02c6e268aa0360db28cee44bddd1a0cfe
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1cnc(-c2ccc3c(c2)CCO3)nc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5].O-B(-O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[#7;a:4]:[c:5]
23.9
[{"value": 22.5, "product": "C(CCCCCCCCC)C=1C=NC(=NC1)C=1C=C2CC(OC2=CC1)CCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 23.9, "product": "C(CCCCCCCCC)C=1C=NC(=NC1)C=1C=C2CC(OC2=CC1)CCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Under nitrogen atmosphere, 0.30 g (1.09 mM) of 2-octylcoumaran-5-boronic acid, 0.26 g (1.02 mM) of 2-chloro-5-decylpyrimidine and 1.5 ml of benzene were placed in a 20 ml-round-bottomed flask. Under stirring, 0.06 g of tetrakis(triphenylphosphine) palladium (0) and 1.5 ml of a 2M-sodium carbonate aqueous solution were ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccc2c(c1)CCO2.c1cncnc1
c1cncnc1.c1ccc2c(c1)CCO2
c1cncnc1.c1ccc2c(c1)CCO2
HCl.B
[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O
null
null
CCCCCCCCC1Cc2cc(B(O)O)ccc2O1.CCCCCCCCCCc1cnc(Cl)nc1>[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O>CCCCCCCCCCc1cnc(-c2ccc3c(c2)CC(CCCCCCCC)O3)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-37d8555154644a60ab7cecfd4db2ff16
CCCCCCCCC1Cc2cc(B(O)O)ccc2O1.CCCCCCCCCCc1cnc(-c2cccc(Br)c2)nc1>>CCCCCCCCCCc1cnc(-c2ccc(-c3ccc4c(c3)CC(CCCCCCCC)O4)cc2)nc1
C([O-])([O-])=O.[Na+].[Na+].C(CCCCCCC)C1OC2=CC=C(C=C2C1)B(O)O.C(C)O.BrC=1C=C(C=CC1)C1=NC=C(C=N1)CCCCCCCCCC>>C(CCCCCCCCC)C=1C=NC(=NC1)C1=CC=C(C=C1)C=1C=C2CC(OC2=CC1)CCCCCCCC
OB(O)[c:19]1[cH:20][cH:21][c:22]2[c:23]([cH:24]1)[CH2:25][CH:26]([CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][CH3:34])[O:35]2.Br[c:36]1[cH:18][cH:17][cH:16][c:15](-[c:14]2[n:13][cH:12][c:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:39][n:38]2)[cH:37]1>>[CH3:1][CH2:2][CH2:3...
CCCCCCCCC1Cc2cc(B(O)O)ccc2O1.CCCCCCCCCCc1cnc(-c2cccc(Br)c2)nc1
CCCCCCCCCCc1cnc(-c2ccc(-c3ccc4c(c3)CC(CCCCCCCC)O4)cc2)nc1
null
[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
C1=CC=CC=C1
C-C Coupling
OtherReaction
56c93a2f9806908798c499807b17d3f0e66e3ff1161f180dd511ec545b7e9634
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1cnc(-c2ccc(-c3ccc4c(c3)CCO4)cc2)nc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]:[cH;D2;+0:6]:1.O-B(-O)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]>>[c:9]:[c:8]:[c;H0;D3;+0:7](-[c;H0;D3;+0:6]1:[c:5]:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:1):[c:10]:[c:11]
66.5
[{"value": 66.5, "product": "C(CCCCCCCCC)C=1C=NC(=NC1)C1=CC=C(C=C1)C=1C=C2CC(OC2=CC1)CCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.5, "product": "C(CCCCCCCCC)C=1C=NC(=NC1)C1=CC=C(C=C1)C=1C=C2CC(OC2=CC1)CCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Under nitrogen atmosphere, 0.25 g (0.91 mM) of 2-octylcoumaran-5-boronic acid, 0.7 ml of ethanol, 0.30 g (0.80 mM) of 2-(3-bromophenyl)-5-decylpyrimidine and 1.3 ml of benzene were placed in a 20 ml-round-bottomed flask. Under stirring, 0.05 g of tetrakis(triphenylphosphine) palladium (0) and 1.3 ml of a 2M-sodium carb...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccc2c(c1)CCO2.c1ccccc1
c1ccccc1.c1ccc2c(c1)CCO2
c1cncnc1.c1ccccc1.c1ccc2c(c1)CCO2
HBr.B
[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1=CC=CC=C1
null
null
CCCCCCCCC1Cc2cc(B(O)O)ccc2O1.CCCCCCCCCCc1cnc(-c2cccc(Br)c2)nc1>[Pd].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1=CC=CC=C1>CCCCCCCCCCc1cnc(-c2ccc(-c3ccc4c(c3)CC(CCCCCCCC)O4)cc2)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-81a231be09734e50823c3b6abac323f1
C=CC(=O)Cl.OCCOc1ccccc1O>>C=CC(=O)Oc1ccccc1
OCCOC1=C(C=CC=C1)O.C(C)N(CC)CC.O1CCCC1.C(C=C)(=O)Cl>>C(C=C)(=O)OC1=CC=CC=C1
Cl[C:3]([CH:2]=[CH2:1])=[O:4].OCCO[c:11]1[c:6]([OH:5])[cH:7][cH:8][cH:9][cH:10]1>>[CH2:1]=[CH:2][C:3](=[O:4])[O:5][c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1
C=CC(=O)Cl.OCCOc1ccccc1O
C=CC(=O)Oc1ccccc1
null
C1=CC=CC=2SC3=CC=CC=C3NC12
null
Acylation
OtherReaction
a688b942154e6a847b3c1f63e2609740d90a3a21e5c3293f44fc051e2ce89f3e
fb24c4440c0fbc7ace4fff55268919df3e2b4365d542ebdb85cd4b96d977c435
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4].O-C-C-O-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8](-[OH;D1;+0:9]):[c:10]>>[C;D1;H2:4]=[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[c:8](:[c:10]):[cH;D2;+0:5]:[c:6]:[c:7]
62
[{"value": 62.0, "product": "C(C=C)(=O)OC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A 500-ml, two necked flask was equipped with magnetic stirring bar, nitrogen atmosphere and an addition funnel. The flask was charged with 25 g of 2-(2-hydroxyethoxy)phenol (0.16 mol.), 33 g of triethylamine (0.32 mol.), 250 ml of tetrahydrofuran and 1 g of phenothiazine. Next, 30 g of acryloyl chloride (0.18 mol.) was...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary alcohol.Aromatic alcohol
Ester
c1ccccc1
c1ccccc1
c1ccccc1
HCl
C1=CC=CC=2SC3=CC=CC=C3NC12
null
null
C=CC(=O)Cl.OCCOc1ccccc1O>C1=CC=CC=2SC3=CC=CC=C3NC12>C=CC(=O)Oc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0a1e984cbfd144cd8fa2cccd3f2e67f2
NCCOCCO.O=C1OC(=O)C2CCCCC12>>O=C1C2CCCCC2C(=O)N1CCOCCO
NCCOCCO.C1(C2C(C(=O)O1)CCCC2)=O>>OCCOCCN1C(C2C(C1=O)CCCC2)=O
[NH2:11][CH2:12][CH2:13][O:14][CH2:15][CH2:16][OH:17].O1[C:2](=[O:1])[CH:3]2[CH2:4][CH2:5][CH2:6][CH2:7][CH:8]2[C:9]1=[O:10]>>[O:1]=[C:2]1[CH:3]2[CH2:4][CH2:5][CH2:6][CH2:7][CH:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][O:14][CH2:15][CH2:16][OH:17]
NCCOCCO.O=C1OC(=O)C2CCCCC12
O=C1C2CCCCC2C(=O)N1CCOCCO
null
null
C(C)O
Acylation
OtherReaction
fd4ebb9664b8f1fa0723d696f691dbe0d733549ae6e429af7ea144f47ba2e4b4
2a4a20e639c386292668b0b265a8e1b50d707d5f0576437dc5ade3e7fd444d29
O=C1NC(=O)C2CCCCC12
[C:1]-[C:2]-[NH2;D1;+0:3].[C:4]-[C:5]1-[C:6](-[C:7])-[C;H0;D3;+0:8](=[O;D1;H0:9])-O-[C;H0;D3;+0:10]-1=[O;D1;H0:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:10](=[O;D1;H0:11])-[C:5](-[C:4])-[C:6](-[C:7])-[C;H0;D3;+0:8]-1=[O;D1;H0:9]
96
[{"value": 96.0, "product": "OCCOCCN1C(C2C(C1=O)CCCC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.6, "product": "OCCOCCN1C(C2C(C1=O)CCCC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 500-ml, two necked flask was equipped with a magnetic stirring bar, heating mantle and condenser. The flask was charged with 51 g of 2-(aminoethoxy) ethanol (0.49 mol.) and 250 ml of ethanol. Next, 75 g of hexahydrophthalic anhydride (0.49 mol.) was slowly added to the flask. After the addition was complete the react...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Substituted dicarboximide
C1CCC2COCC2C1
C1CCC2C[NH]CC2C1
C1CCC2C[NH]CC2C1
HO-
C(C)O
null
null
NCCOCCO.O=C1OC(=O)C2CCCCC12>C(C)O>O=C1C2CCCCC2C(=O)N1CCOCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-af9dc50fe19f475a8fbd4e36870e7ec5
C=CC(=O)Cl.O=C1C2CCCCC2C(=O)N1CCOCCO>>C=CC(=O)OCCOCCN1C(=O)C2CCCCC2C1=O
OCCOCCN1C(C2C(C1=O)CCCC2)=O.C(C)N(CC)CC.C(C=C)(=O)Cl>>C(C=C)(=O)OCCOCCN1C(C2C(C1=O)CCCC2)=O
Cl[C:3]([CH:2]=[CH2:1])=[O:4].[OH:5][CH2:6][CH2:7][O:8][CH2:9][CH2:10][N:11]1[C:12](=[O:13])[CH:14]2[CH2:15][CH2:16][CH2:17][CH2:18][CH:19]2[C:20]1=[O:21]>>[CH2:1]=[CH:2][C:3](=[O:4])[O:5][CH2:6][CH2:7][O:8][CH2:9][CH2:10][N:11]1[C:12](=[O:13])[CH:14]2[CH2:15][CH2:16][CH2:17][CH2:18][CH:19]2[C:20]1=[O:21]
C=CC(=O)Cl.O=C1C2CCCCC2C(=O)N1CCOCCO
C=CC(=O)OCCOCCN1C(=O)C2CCCCC2C1=O
null
C1=CC=CC=2SC3=CC=CC=C3NC12
CC(=O)C
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
O=C1NC(=O)C2CCCCC12
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4]
59.5
[{"value": 59.0, "product": "C(C=C)(=O)OCCOCCN1C(C2C(C1=O)CCCC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 59.5, "product": "C(C=C)(=O)OCCOCCN1C(C2C(C1=O)CCCC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
A one liter, three necked flask was equipped with overhead stirrer, nitrogen atmosphere and an addition funnel. The flask was charged with 100 g of N-(2-hydroxyethoxyethyl)hexahydrophthalimide (0.41 mol.), 42 g of triethylamine (0.41 mol.), 1 g of phenothiazine and 400 ml of acetone. Next, 38 g of acryloyl chloride (0....
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
C1CCC2C[NH]CC2C1
HCl
C1=CC=CC=2SC3=CC=CC=C3NC12.CC(=O)C
null
12
C=CC(=O)Cl.O=C1C2CCCCC2C(=O)N1CCOCCO>C1=CC=CC=2SC3=CC=CC=C3NC12.CC(=O)C>C=CC(=O)OCCOCCN1C(=O)C2CCCCC2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ebb2fd6722bb446b8b566d5f8733e3f7
NCC(O)CO.O=C1OC(=O)C2CCCCC12>>C=CC(=O)OCC(CN1C(=O)C2CCCCC2C1=O)OC(=O)C=C
NCC(CO)O.C1(C2C(C(=O)O1)CCCC2)=O>>C(C=C)(=O)OC(CN1C(C2C(C1=O)CCCC2)=O)COC(C=C)=O
[OH:5][CH2:6][CH:7]([CH2:8][NH2:9])[OH:20].[CH2:1]1[CH2:13][CH:12]2[C:10](=[O:11])[O:19][C:3](=[O:4])[CH:17]2[CH2:16][CH2:15]1>>[CH2:1]=[CH:2][C:3](=[O:4])[O:5][CH2:6][CH:7]([CH2:8][N:9]1[C:10](=[O:11])[CH:12]2[CH2:13][CH2:14][CH2:15][CH2:16][CH:17]2[C:18]1=[O:19])[O:20][C:21](=[O:22])[CH:23]=[CH2:24]
NCC(O)CO.O=C1OC(=O)C2CCCCC12
C=CC(=O)OCC(CN1C(=O)C2CCCCC2C1=O)OC(=O)C=C
null
null
C(C)O
Acylation
OtherReaction
37aad88ec273d256158b0f4cb1f2443a40d4edb4bca01dc8259cc5a878baf5b6
32b0947c632de63f555f97f544b66ccd6cc5dfd855d370241eba47f794e22b4d
O=C1NC(=O)C2CCCCC12
[NH2;D1;+0:1]-[C:2]-[C:3](-[OH;D1;+0:4])-[C:5]-[OH;D1;+0:6].[O;D1;H0:7]=[C;H0;D3;+0:8]1-[O;H0;D2;+0:9]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[CH;D3;+0:12]2-[C:13]-[CH2;D2;+0:14]-[CH2;D2;+0:15]-[CH2;D2;+0:16]-[C:17]-1-2>>[C:18]-[C:19](=[O;D1;H0:20])-[O;H0;D2;+0:4]-[C:3](-[C:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[C:2...
109.7
[{"value": 81.0, "product": "C(C=C)(=O)OC(CN1C(C2C(C1=O)CCCC2)=O)COC(C=C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 109.7, "product": "C(C=C)(=O)OC(CN1C(C2C(C1=O)CCCC2)=O)COC(C=C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 500-ml, two necked flask was equipped a magnetic stirring bar, heating mantle and condenser. The flask was charged with 46 g of 3-amino-1,2-propanediol (0.50 mol.) and 300 ml of ethanol. Next, 77 g of hexahydrophthalic anhydride (0.50 mol.) was slowly added to the flask after which the reaction was refluxed for 12 ho...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary alcohol.Secondary alcohol.Primary amine
Ester.Ester.Substituted dicarboximide.Vinyl.Vinyl
C1CCC2COCC2C1
C1CCC2C[NH]CC2C1
C1CCC2C[NH]CC2C1
Other
C(C)O
null
null
NCC(O)CO.O=C1OC(=O)C2CCCCC12>C(C)O>C=CC(=O)OCC(CN1C(=O)C2CCCCC2C1=O)OC(=O)C=C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-89e65a3dba8b4753baf97d14535ec204
CNCCO.O=C(Cl)c1ccco1>>CN(CCO)C(=O)c1ccco1
CNCCO.O1C(=CC=C1)C(=O)Cl>>OCCN(C(=O)C=1OC=CC1)C
[CH3:1][NH:2][CH2:3][CH2:4][OH:5].Cl[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][o:12]1>>[CH3:1][N:2]([CH2:3][CH2:4][OH:5])[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][o:12]1
CNCCO.O=C(Cl)c1ccco1
CN(CCO)C(=O)c1ccco1
null
null
ClCCl
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
c1ccoc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#8;a:5]:[c:6].[C:7]-[C:8]-[NH;D2;+0:9]-[C;D1;H3:10]>>[C:7]-[C:8]-[N;H0;D3;+0:9](-[C;D1;H3:10])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#8;a:5]:[c:6]
57.6
[{"value": 44.0, "product": "OCCN(C(=O)C=1OC=CC1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.6, "product": "OCCN(C(=O)C=1OC=CC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A one liter, three necked flask was equipped with overhead stirrer, nitrogen atmosphere and an addition funnel. The flask was charged with 115 g of 2-(methylamino)ethanol (1.53 mol.) and 500 ml of dichloromethane. The reaction flask was cooled with an ice bath. Next, 100 g of furoyl chloride (0.77 mol.) was slowly adde...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccoc1
HCl
ClCCl
null
null
CNCCO.O=C(Cl)c1ccco1>ClCCl>CN(CCO)C(=O)c1ccco1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-77519deec78d44d89cdc131b10b54df8
C=CC(=O)Cl.O=C1NCC(CO)O1>>C=CC(=O)OCC1CNC(=O)O1
C(C=C)(=O)Cl.OCC1CNC(O1)=O.C(C)N(CC)CC.C1=CC=CC=2SC3=CC=CC=C3NC12>>C(C=C)(=O)OCC1CNC(O1)=O
Cl[C:3]([CH:2]=[CH2:1])=[O:4].[OH:5][CH2:6][CH:7]1[CH2:8][NH:9][C:10](=[O:11])[O:12]1>>[CH2:1]=[CH:2][C:3](=[O:4])[O:5][CH2:6][CH:7]1[CH2:8][NH:9][C:10](=[O:11])[O:12]1
C=CC(=O)Cl.O=C1NCC(CO)O1
C=CC(=O)OCC1CNC(=O)O1
null
null
O1CCCC1
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
O=C1NCCO1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4].[#8:5]-[C:6]-[C:7]-[OH;D1;+0:8]>>[#8:5]-[C:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4]
null
[]
null
null
null
null
105 g (0.90 mol.) of 5-hydroxymethyl-oxazolidin-2-one were placed into a one liter, three necked, round bottomed flask equipped with a paddle stirrer and thermometer. This was followed by 500 ml of tetrahydrofuran, 101 g (1.0 mol.) of triethylamine and 0.5 g of phenothiazine. Stirring was started as 90 g (1.0 mol.) of ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
C1COCN1
HCl
O1CCCC1
null
null
C=CC(=O)Cl.O=C1NCC(CO)O1>O1CCCC1>C=CC(=O)OCC1CNC(=O)O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bd858f048833400792f09a0d07c7449f
Brc1ccsc1.Fc1cc(Br)cc(F)c1F>>Fc1cc(-c2ccsc2)cc(F)c1F
BrC1=CSC=C1.[Mg].[Mg].BrC1=CC(=C(C(=C1)F)F)F>>FC=1C=C(C=C(C1F)F)C1=CSC=C1
Br[c:5]1[cH:6][cH:7][s:8][cH:9]1.Br[c:4]1[cH:3][c:2]([F:1])[c:13]([F:14])[c:11]([F:12])[cH:10]1>>[F:1][c:2]1[cH:3][c:4](-[c:5]2[cH:6][cH:7][s:8][cH:9]2)[cH:10][c:11]([F:12])[c:13]1[F:14]
Brc1ccsc1.Fc1cc(Br)cc(F)c1F
Fc1cc(-c2ccsc2)cc(F)c1F
null
[Cl-].[Zn+2].[Cl-].C1=CC=C(C=C1)P([C-]2C=CC=C2)C3=CC=CC=C3.C1=CC=C(C=C1)P([C-]2C=CC=C2)C3=CC=CC=C3.Cl[Pd]Cl.[Fe+2]
null
C-C Coupling
Negishi
465b747680a8e5c8f91311f4e5462c5cd984c0085c515df27dc91db7d0c5b083
a7a4ce9a92e2f8a62d28956a69a5cc384426ab72416e87d68c6a3feb23c22d66
c1ccc(-c2ccsc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].Br-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[#16;a:9]:[c:10]:1>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[c:7]:[c:8]:[#16;a:9]:[c:10]:1):[c:4]:[c:5]
null
[]
40
CELSIUS
null
null
In a first three-necked round-bottom flask (100 ml), metallic magnesium (52 mmol) (product #25411-8, manufactured by Aldrich Chemical) was flame dried in an argon atmosphere for 3 to 4 minutes. Upon cooling under the argon atmosphere, 50 ml of freshly dried tetrahydrofuran (product #T 397-4, manufactured by Fisher Scie...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide
null
c1ccsc1.c1ccccc1
c1ccccc1.c1ccsc1
c1ccccc1.c1ccsc1
Br-
[Cl-].[Zn+2].[Cl-].C1=CC=C(C=C1)P([C-]2C=CC=C2)C3=CC=CC=C3.C1=CC=C(C=C1)P([C-]2C=CC=C2)C3=CC=CC=C3.Cl[Pd]Cl.[Fe+2]
40
null
Brc1ccsc1.Fc1cc(Br)cc(F)c1F>[Cl-].[Zn+2].[Cl-].C1=CC=C(C=C1)P([C-]2C=CC=C2)C3=CC=CC=C3.C1=CC=C(C=C1)P([C-]2C=CC=C2)C3=CC=CC=C3.Cl[Pd]Cl.[Fe+2]>Fc1cc(-c2ccsc2)cc(F)c1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d67d9c65c42044a99182159ada0d0d78
Fc1cc(-c2ccsc2)cc(F)c1F>>Fc1ccc(-c2ccsc2)cc1F
FC=1C=C(C=C(C1F)F)C1=CSC=C1.BrC1=CC(=C(C=C1)F)F.BrC1=CC(=C(C(=C1)F)F)F>>FC=1C=C(C=CC1F)C1=CSC=C1
F[c:3]1[c:2]([F:1])[c:12]([F:13])[cH:11][c:5](-[c:6]2[cH:7][cH:8][s:9][cH:10]2)[cH:4]1>>[F:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][s:9][cH:10]2)[cH:11][c:12]1[F:13]
Fc1cc(-c2ccsc2)cc(F)c1F
Fc1ccc(-c2ccsc2)cc1F
null
null
null
Functional Group Interconversion
Aromatic dehalogenation
b66818d3926a4463fb8e1c3d4a89e94e47b4d46960d4bdb7bcfbeeec427cfd4e
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccc(-c2ccsc2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[F;D1;H0:5]):[c:6]>>[F;D1;H0:5]-[c:4](:[c:6]):[cH;D2;+0:1]:[c:2]:[c:3]
null
[]
null
null
null
null
The same procedures set forth above in Example (1)(a) for synthesizing 3(3,4,5-trifluorophenyl)thiophene were followed, with the exception that 1-bromo-3,4-difluorobenzene was substituted for 1-bromo-3,4,5-trifluorobenzene as the 1-bromo-substituted fluorobenzene. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccccc1
c1ccccc1
c1ccccc1.c1ccsc1
Other
null
null
null
Fc1cc(-c2ccsc2)cc(F)c1F>>Fc1ccc(-c2ccsc2)cc1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1353d03acc334b3781453676e9c404d0
Fc1cc(-c2ccsc2)cc(F)c1F>>Fc1cc(F)cc(-c2ccsc2)c1
FC=1C=C(C=C(C1F)F)C1=CSC=C1.BrC1=CC(=CC(=C1)F)F.BrC1=CC(=C(C(=C1)F)F)F>>FC=1C=C(C=C(C1)F)C1=CSC=C1
F[c:3]1[c:2]([F:1])[cH:13][c:7](-[c:8]2[cH:9][cH:10][s:11][cH:12]2)[cH:6][c:4]1[F:5]>>[F:1][c:2]1[cH:3][c:4]([F:5])[cH:6][c:7](-[c:8]2[cH:9][cH:10][s:11][cH:12]2)[cH:13]1
Fc1cc(-c2ccsc2)cc(F)c1F
Fc1cc(F)cc(-c2ccsc2)c1
null
null
null
Functional Group Interconversion
Aromatic dehalogenation
b66818d3926a4463fb8e1c3d4a89e94e47b4d46960d4bdb7bcfbeeec427cfd4e
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccc(-c2ccsc2)cc1
F-[c;H0;D3;+0:1](:[c:2](-[F;D1;H0:3]):[c:4]):[c:5](-[F;D1;H0:6]):[c:7]>>[F;D1;H0:3]-[c:2](:[c:4]):[cH;D2;+0:1]:[c:5](-[F;D1;H0:6]):[c:7]
null
[]
null
null
null
null
The same procedures set forth above in Example (1)(a) for synthesizing 3(3,4,5-trifluorophenyl)thiophene were followed, with the exception that 1-bromo-3,5-difluorobenzene was substituted for 1-bromo-3,4,5-trifluorobenzene as the 1-bromo-substituted fluorobenzene. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccccc1
c1ccccc1
c1ccccc1.c1ccsc1
Other
null
null
null
Fc1cc(-c2ccsc2)cc(F)c1F>>Fc1cc(F)cc(-c2ccsc2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-84962d33083243bb8070accd1465b529
Fc1cc(-c2ccsc2)cc(F)c1F.Fc1ccc(Br)c(F)c1>>Fc1ccc(-c2ccsc2)c(F)c1
FC=1C=C(C=C(C1F)F)C1=CSC=C1.BrC1=C(C=C(C=C1)F)F.BrC1=CC(=C(C(=C1)F)F)F>>FC1=C(C=CC(=C1)F)C1=CSC=C1
Fc1c[c:5](-[c:6]2[cH:7][cH:8][s:9][cH:10]2)cc(F)c1F.Brc1[cH:4][cH:3][c:2]([F:1])[cH:13][c:11]1[F:12]>>[F:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][s:9][cH:10]2)[c:11]([F:12])[cH:13]1
Fc1cc(-c2ccsc2)cc(F)c1F.Fc1ccc(Br)c(F)c1
Fc1ccc(-c2ccsc2)c(F)c1
null
null
null
Miscellaneous
OtherReaction
8b9e24f975dd591e39ba8138d18457a38e7be5393a85a11a540dd0516aef781f
dbb6583364c59bca8c7508ce4061692996dd4e8a899e1de1dcdf405af3c96d3c
c1ccc(-c2ccsc2)cc1
Br-c1:[cH;D2;+0:1]:[c:2]:[c:3]:[c:4]:[c;H0;D3;+0:5]:1-[F;D1;H0:6].F-c1:c:[c;H0;D3;+0:7](-[c:8]2:[c:9]:[#16;a:10]:[c:11]:[c:12]:2):c:c(-F):c:1-F>>[F;D1;H0:6]-[c;H0;D3;+0:5]1:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:[c;H0;D3;+0:7]:1-[c:8]1:[c:9]:[#16;a:10]:[c:11]:[c:12]:1
97
[{"value": 97.0, "product": "FC1=C(C=CC(=C1)F)C1=CSC=C1", "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
The same procedures set forth above in Example (1)(a) for synthesizing 3(3,4,5-trifluorophenyl)thiophene were followed, with the exception that 1-bromo-2,4-difluorobenzene was substituted for 1-bromo-3,4,5-trifluorobenzene as the 1-bromo-substituted fluorobenzene, and the coupling reaction mixture was heated to reflux ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Aromatic halide.Aromatic halide
Aromatic halide
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccsc1
HF.Br-
null
80
null
Fc1cc(-c2ccsc2)cc(F)c1F.Fc1ccc(Br)c(F)c1>>Fc1ccc(-c2ccsc2)c(F)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-921b325d103d4c73b989008641f1fd3d
C=C(C)C(=O)OCCN=C=O.OCc1ccccc1>>C=C(C)C(=O)OCCNC(=O)OCc1ccccc1
C(C(=C)C)(=O)OCCN=C=O.C(C1=CC=CC=C1)O>>C(C(=C)C)(=O)OCCNC(=O)OCC1=CC=CC=C1
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][N:9]=[C:10]=[O:11].[OH:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][NH:9][C:10](=[O:11])[O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
C=C(C)C(=O)OCCN=C=O.OCc1ccccc1
C=C(C)C(=O)OCCNC(=O)OCc1ccccc1
null
C(CCCCCCCCCCC)(=O)[O-].C(CCCCCCCCCCC)(=O)[O-].C(CCC)[Sn+2]CCCC
O1CCOCC1
Protection
OtherReaction
8d2aa5da7fec498749aba98cc9467e8d82c146f343570568bec74a92b10e0ae2
e505c5de73b3f9ad0414c141c59109424d376f26a728bbd154d3edfd03d2f50a
c1ccccc1
[C:1]-[C:2]-[N;H0;D2;+0:3]=[C;H0;D2;+0:4]=[O;D1;H0:5].[OH;D1;+0:6]-[C:7]-[c:8]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[C:7]-[c:8]
80.6
[{"value": 80.6, "product": "C(C(=C)C)(=O)OCCNC(=O)OCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
77.5 g of methacryloyloxyethyl isocyanate (Karenzu MOI, available from Showa Denko K.K.) and 60 g of benzyl alcohol were dissolved in 260 g of dioxane. To the solution were then added 5 drops of di-n-butyltin dilaurate. The reaction mixture was then allowed to undergo reaction at a temperature of 65° C. for 3 hours. Th...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary alcohol
Carbamic ester
null
null
c1ccccc1
null
C(CCCCCCCCCCC)(=O)[O-].C(CCCCCCCCCCC)(=O)[O-].C(CCC)[Sn+2]CCCC.O1CCOCC1
null
null
C=C(C)C(=O)OCCN=C=O.OCc1ccccc1>C(CCCCCCCCCCC)(=O)[O-].C(CCCCCCCCCCC)(=O)[O-].C(CCC)[Sn+2]CCCC.O1CCOCC1>C=C(C)C(=O)OCCNC(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7f1fb53c79494e0b8520d17b81fa2775
C=C(C)C(=O)Cl.CC(C)COC(=O)Nc1ccc(S(N)(=O)=O)cc1>>C=C(C)C(=O)NS(=O)(=O)c1ccc(NC(=O)OCC(C)C)cc1
C(C(C)C)OC(=O)NC1=CC=C(C=C1)S(=O)(=O)N.C(C)N(CC)CC.CN(C(C)=O)C.C(C(=C)C)(=O)Cl>>C(C(C)C)OC(=O)NC1=CC=C(C=C1)S(=O)(=O)NC(C(=C)C)=O
Cl[C:4]([C:2](=[CH2:1])[CH3:3])=[O:5].[NH2:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][c:13]([NH:14][C:15](=[O:16])[O:17][CH2:18][CH:19]([CH3:20])[CH3:21])[cH:22][cH:23]1>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[NH:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][c:13]([NH:14][C:15](=[O:16])[O:17][CH2:18][CH:19]([CH3:20])[CH3...
C=C(C)C(=O)Cl.CC(C)COC(=O)Nc1ccc(S(N)(=O)=O)cc1
C=C(C)C(=O)NS(=O)(=O)c1ccc(NC(=O)OCC(C)C)cc1
null
null
O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
403eb34e708e50f7077a9da490b1654c837258ce901614ddd1204eb6f2a10a27
37dfa12f19cd8cec29206fb8a18b7504935d92bc326a2084e9ef8a13076d3b87
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[C;D1;H2:4])-[C;D1;H3:5].[NH2;D1;+0:6]-[#16:7](=[O;D1;H0:8])(=[O;D1;H0:9])-[c:10]>>[C;D1;H2:4]=[C:3](-[C;D1;H3:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:6]-[#16:7](=[O;D1;H0:8])(=[O;D1;H0:9])-[c:10]
58.8
[{"value": 58.8, "product": "C(C(C)C)OC(=O)NC1=CC=C(C=C1)S(=O)(=O)NC(C(=C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a mixture of 54.4 g of p-isobutyloxycarbonylaminophenyl sulfonamide, 40 g of triethylamine, 2 g of N,N-dimethylaminopyridine and 150 ml of N,N-dimethylacetamide was then added dropwise 22.8 g of methacrylic chloride under cooling with ice. After the completion of the dropwise addition, the reaction mixture was stirr...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Sulfonamide
Sulfonamide.Secondary amide
null
null
c1ccccc1
HCl
O
null
2
C=C(C)C(=O)Cl.CC(C)COC(=O)Nc1ccc(S(N)(=O)=O)cc1>O>C=C(C)C(=O)NS(=O)(=O)c1ccc(NC(=O)OCC(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2d4f64dd7b0a4a1ab9ebcd6c62f6820c
O=C(O)CCC(=O)c1ccc(C(=O)C2(O)CCCCC2)cc1.O=S(Cl)Cl>>O=C(Cl)CCC(=O)c1ccc(C(=O)C2(O)CCCCC2)cc1
C(=O)(O)CCC(=O)C1=CC=C(C=C1)C(=O)C1(CCCCC1)O.S(=O)(Cl)Cl>>ClC(=O)CCC(=O)C1=CC=C(C=C1)C(=O)C1(CCCCC1)O
O[C:2](=[O:1])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([C:12](=[O:13])[C:14]2([OH:15])[CH2:16][CH2:17][CH2:18][CH2:19][CH2:20]2)[cH:21][cH:22]1.O=S(Cl)[Cl:3]>>[O:1]=[C:2]([Cl:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([C:12](=[O:13])[C:14]2([OH:15])[CH2:16][CH2:17][CH2:18][CH2:19][CH2:20]2)[cH:...
O=C(O)CCC(=O)c1ccc(C(=O)C2(O)CCCCC2)cc1.O=S(Cl)Cl
O=C(Cl)CCC(=O)c1ccc(C(=O)C2(O)CCCCC2)cc1
null
null
C(C)OCC
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
O=C(c1ccccc1)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]=[O;D1;H0:7]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]-[C:6]=[O;D1;H0:7]
94
[{"value": 94.0, "product": "ClC(=O)CCC(=O)C1=CC=C(C=C1)C(=O)C1(CCCCC1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.7, "product": "ClC(=O)CCC(=O)C1=CC=C(C=C1)C(=O)C1(CCCCC1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
30
CELSIUS
30
MINUTE
A 250-ml round-bottomed flask fitted with a condenser was charged with 12.0 g of 1-hydroxycyclohexyl 4-(2-carboxyethyl)carbonylphenyl ketone (0.04 mole), 5.95 g (0.05 mole) of thionyl chloride (Aldrich), and 50 ml of diethyl ether. The resulting reaction mixture was stirred at 30° C. for 30 minutes, after which time th...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1.C1CCCCC1
HCl
C(C)OCC
30
0.5
O=C(O)CCC(=O)c1ccc(C(=O)C2(O)CCCCC2)cc1.O=S(Cl)Cl>C(C)OCC>O=C(Cl)CCC(=O)c1ccc(C(=O)C2(O)CCCCC2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e6001659ddac4b01bf370c708fa8cdd0
CC(=O)O[C@H]1COC[C@H]1O.CC(Cl)C(=O)Cl>>CC(=O)O[C@H]1COC[C@H]1OC(=O)C(C)Cl
O[C@@H]1COC[C@@H]1OC(=O)C.N1=CC=CC=C1.ClCCl.ClC(C(=O)Cl)C>>C(C)(=O)O[C@@H]1[C@@H](COC1)OC(C(C)Cl)=O
[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[CH2:6][O:7][CH2:8][C@H:9]1[OH:10].Cl[C:11](=[O:12])[CH:13]([CH3:14])[Cl:15]>>[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[CH2:6][O:7][CH2:8][C@H:9]1[O:10][C:11](=[O:12])[CH:13]([CH3:14])[Cl:15]
CC(=O)O[C@H]1COC[C@H]1O.CC(Cl)C(=O)Cl
CC(=O)O[C@H]1COC[C@H]1OC(=O)C(C)Cl
null
null
O
Acylation
Schotten-Baumann to ester
27b76e29491fa7db5375755e15223de884a194f57a493147db0b5495ea981908
d47ab90ace9b5dcd818151c10aae400dcf599f5a3476072b8dfedc474e97c335
C1CCOC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[Cl;D1;H0:5].[#8:6]-[C:7]-[C:8](-[OH;D1;+0:9])-[C:10]>>[#8:6]-[C:7]-[C:8](-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[Cl;D1;H0:5])-[C:10]
null
[]
23
CELSIUS
4
HOUR
12.4 g of (±)-2-chloropropionyl chloride were added dropwise at 0°-5° C. to an ice-cooled mixture of 15.0 g of (±)-(3R,4S)-3-hydroxy-4-methylcarbonyloxytetrahydrofuran, 8.1 g of anhydrous pyridine and 200 ml of anhydrous dichloromethane. After addition was complete, the reaction mixture was stirred at 23° C. for a furt...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary alcohol
Ester
null
null
C1CCOC1
HCl
O
23
4
CC(=O)O[C@H]1COC[C@H]1O.CC(Cl)C(=O)Cl>O>CC(=O)O[C@H]1COC[C@H]1OC(=O)C(C)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-854b8b53d833423eaf0208d0354bd8e9
NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O.O=C=Nc1cccc([N+](=O)[O-])c1>>O=C(Nc1cccc([N+](=O)[O-])c1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O
[N+](=O)([O-])C=1C=C(C=CC1)N=C=O.C12(CC3CC(CC(C1)C3)C2)CN2C(C(C(N(C3=C2C=CC=C3)C3=CC=CC=C3)=O)N)=O>>C12(CC3CC(CC(C1)C3)C2)CN2C(C(C(N(C3=C2C=CC=C3)C3=CC=CC=C3)=O)NC(=O)NC3=CC(=CC=C3)[N+](=O)[O-])=O
[NH2:13][CH:14]1[C:15](=[O:16])[N:17]([CH2:18][C:19]23[CH2:20][CH:21]4[CH2:22][CH:23]([CH2:24][CH:25]([CH2:26]4)[CH2:27]2)[CH2:28]3)[c:29]2[cH:30][cH:31][cH:32][cH:33][c:34]2[N:35]([c:36]2[cH:37][cH:38][cH:39][cH:40][cH:41]2)[C:42]1=[O:43].[O:1]=[C:2]=[N:3][c:4]1[cH:5][cH:6][cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12]1>>...
NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O.O=C=Nc1cccc([N+](=O)[O-])c1
O=C(Nc1cccc([N+](=O)[O-])c1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O
null
null
C(C)#N.ClCCl
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O
[C:1]-[#7:2]1-[c:3]:[c:4]-[#7:5](-[c:6])-[C:7](=[O;D1;H0:8])-[C:9](-[NH2;D1;+0:10])-[C:11]-1=[O;D1;H0:12].[O;D1;H0:13]=[C;H0;D2;+0:14]=[N;H0;D2;+0:15]-[c:16](:[c:17]):[c:18]>>[C:1]-[#7:2]1-[c:3]:[c:4]-[#7:5](-[c:6])-[C:7](=[O;D1;H0:8])-[C:9](-[NH;D2;+0:10]-[C;H0;D3;+0:14](=[O;D1;H0:13])-[NH;D2;+0:15]-[c:16](:[c:17]):[c...
82.1
[{"value": 82.1, "product": "C12(CC3CC(CC(C1)C3)C2)CN2C(C(C(N(C3=C2C=CC=C3)C3=CC=CC=C3)=O)NC(=O)NC3=CC(=CC=C3)[N+](=O)[O-])=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of 3-nitrophenyl isocyanate (0.082 g) in dry acetonitrile (8 ml) was added to a solution of the 1-(1-Adamantylmethyl-3-amino-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine (0.2 g) in dry acetonitrile (10 ml) under a nitrogen atmosphere. The mixture was stirred at 23° for 2 h, then diluted with d...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)[NH]CCC[NH]2.C1C2CC3CC1CC(C2)C3
null
C(C)#N.ClCCl
null
2
NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O.O=C=Nc1cccc([N+](=O)[O-])c1>C(C)#N.ClCCl>O=C(Nc1cccc([N+](=O)[O-])c1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-888b842697c24f2abdd0a5f6ef3eaa40
C[C@H](NC(=O)OC(C)(C)C)C(=O)O.NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O>>C[C@H](N)C(=O)NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O
C(C)(C)(C)OC(=O)NCC(=O)O.C1=CC=CC=2C(C3=CC=CC=C3C(C12)=O)=O.NCCCNC1=CC=C(C=2C(C3=CC=CC=C3C(C12)=O)=O)NCCCN.C(C)(C)(C)OC(=O)N[C@@H](C)C(=O)O>>NCCCNC1=CC=C(C=2C(C3=CC=CC=C3C(C12)=O)=O)NCCCNC([C@@H](N)C)=O
CC(C)(C)OC(=O)[NH:3][C@@H:2]([CH3:1])[C:4](O)=[O:5].[NH2:6][CH2:7][CH2:8][CH2:9][NH:10][c:11]1[cH:12][cH:13][c:14]([NH:15][CH2:16][CH2:17][CH2:18][NH2:19])[c:20]2[c:21]1[C:22](=[O:23])[c:24]1[cH:25][cH:26][cH:27][cH:28][c:29]1[C:30]2=[O:31]>>[CH3:1][C@H:2]([NH2:3])[C:4](=[O:5])[NH:6][CH2:7][CH2:8][CH2:9][NH:10][c:11]1[...
C[C@H](NC(=O)OC(C)(C)C)C(=O)O.NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O
C[C@H](N)C(=O)NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O
null
null
null
Acylation
OtherReaction
b4c20342f55b434660078663f02be082076e2ff9b9068db91acc0b381022a32e
e525bb030a9f5f4a2fc47bce923bf921a3769ce3300b3fa2600575194671a3f3
O=C1c2ccccc2C(=O)c2ccccc21
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C;D1;H3:3])-[C;H0;D3;+0:4](-O)=[O;D1;H0:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:2](-[C;D1;H3:3])-[NH2;D1;+0:1]
null
[]
null
null
null
null
Example 28 was prepared by an equivalent procedure to that described for Example 24 except that the starting anthraquinone was 1,4-bis[(3-aminopropyl)amino]-anthracene-9,10-dione and N-tertiarybutoxycarbonyl-L-alanine replaced N-tertiarybutoxycarbonylglycine. Conditions: See reaction.notes.procedure_details. Workup: Ex...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid.Ether.Primary amine.Boc
Secondary amide.Primary amine
null
null
c1ccc2c(c1)Cc1ccccc1C2
HO-
null
null
null
C[C@H](NC(=O)OC(C)(C)C)C(=O)O.NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O>>C[C@H](N)C(=O)NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5825bb94a6c044969c60477a29132a82
CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)O.NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O>>NCCCNc1ccc(NCCCNC(=O)[C@@H](N)Cc2ccccc2)c2c1C(=O)c1ccccc1C2=O
C(C)(C)(C)OC(=O)NCC(=O)O.C1=CC=CC=2C(C3=CC=CC=C3C(C12)=O)=O.NCCCNC1=CC=C(C=2C(C3=CC=CC=C3C(C12)=O)=O)NCCCN.C(C)(C)(C)OC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)O>>NCCCNC1=CC=C(C=2C(C3=CC=CC=C3C(C12)=O)=O)NCCCNC([C@@H](N)CC1=CC=CC=C1)=O
CC(C)(C)OC(=O)[NH:18][C@H:17]([C:15](O)=[O:16])[CH2:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1.[NH2:1][CH2:2][CH2:3][CH2:4][NH:5][c:6]1[cH:7][cH:8][c:9]([NH:10][CH2:11][CH2:12][CH2:13][NH2:14])[c:26]2[c:27]1[C:28](=[O:29])[c:30]1[cH:31][cH:32][cH:33][cH:34][c:35]1[C:36]2=[O:37]>>[NH2:1][CH2:2][CH2:3][CH2:4][NH:5][c...
CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)O.NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O
NCCCNc1ccc(NCCCNC(=O)[C@@H](N)Cc2ccccc2)c2c1C(=O)c1ccccc1C2=O
null
null
null
Acylation
OtherReaction
b4c20342f55b434660078663f02be082076e2ff9b9068db91acc0b381022a32e
e525bb030a9f5f4a2fc47bce923bf921a3769ce3300b3fa2600575194671a3f3
O=C(CCc1ccccc1)NCCCNc1cccc2c1C(=O)c1ccccc1C2=O
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C;H0;D3;+0:4](-O)=[O;D1;H0:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:2](-[C:3])-[NH2;D1;+0:1]
null
[]
null
null
null
null
Example 29 was prepared by an equivalent procedure to that described for Example 24 except that the starting anthraquinone was 1,4-bis[(3-aminopropyl)amino]-anthracene-9,10-dione and N-tertiarybutoxycarbonyl-L-phenylalanine replaced N-tertiarybutoxycarbonylglycine. Conditions: See reaction.notes.procedure_details. Work...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid.Ether.Primary amine.Boc
Secondary amide.Primary amine
null
null
c1ccccc1.c1ccc2c(c1)Cc1ccccc1C2
HO-
null
null
null
CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)O.NCCCNc1ccc(NCCCN)c2c1C(=O)c1ccccc1C2=O>>NCCCNc1ccc(NCCCNC(=O)[C@@H](N)Cc2ccccc2)c2c1C(=O)c1ccccc1C2=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bbab05d627554b729c0070280001d3e6
CCOP(=O)(CCOCn1cnc2c(OC)ncnc21)OCC.N>>CCOP(=O)([O-])CCOCn1cnc2c(N)ncnc21.[NH4+]
COC1=C2N=CN(C2=NC=N1)COCCP(OCC)(OCC)=O.N>>N1=CN=C2N(C=NC2=C1N)COCCP(OCC)([O-])=O.[NH4+]
CC[O:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[CH2:7][CH2:8][O:9][CH2:10][n:11]1[cH:12][n:13][c:14]2[c:15](OC)[n:17][cH:18][n:19][c:20]12.[NH3:16]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([O-:6])[CH2:7][CH2:8][O:9][CH2:10][n:11]1[cH:12][n:13][c:14]2[c:15]([NH2:16])[n:17][cH:18][n:19][c:20]12.[NH4+:21]
CCOP(=O)(CCOCn1cnc2c(OC)ncnc21)OCC.N
CCOP(=O)([O-])CCOCn1cnc2c(N)ncnc21.[NH4+]
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
0cd510195a6b358a413cf3d0ba916c1a77eb59b88b58776aeaefdb0f23cd4d52
4764b8d6a7ad8d9253070fdb827f95d720ac9a4f642f3b03b75fe3f308c3d0a7
c1ncc2nc[nH]c2n1
C-C-[O;H0;D2;+0:1]-[#15:2](-[#8:3])(-[C:4])=[O;D1;H0:5].C-O-[c;H0;D3;+0:6]1:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11](-[C:12]):[c:13]:[#7;a:14]:[c:15]:2:1.[NH3;D0;+0:16]>>[#8:3]-[#15:2](-[C:4])(-[O-;H0;D1:1])=[O;D1;H0:5].[C:12]-[#7;a:11]1:[c:13]:[#7;a:14]:[c:15]2:[c:10]:1:[#7;a:9]:[c:8]:[#7;a:7]:[c;H0;D3;+0:6]:2-[NH2;D...
40
[{"value": 40.0, "product": "N1=CN=C2N(C=NC2=C1N)COCCP(OCC)([O-])=O.[NH4+]", "details": "PERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
To a solution of 11 (3.44 g, 10.0 mmol) in MeOH (40 mL) was added a saturated methanolic NH3 solution (100 mL). The solution was heated in a sealed flask at 100° C. for 30 h. The solvent was evaporated and the residue was crystallized from EtOH to give 12 (1.20 g) in 40% yield: mp 190°-193° C.; TLC Rf 0.37 (AcOEt/MeOH=...
10.6084/m9.figshare.5104873.v1
null
Ether
Primary amine
c1ncnc2[nH]cnc12
c1ncnc2[nH]cnc12
c1ncnc2[nH]cnc12
HO-
CO
100
null
CCOP(=O)(CCOCn1cnc2c(OC)ncnc21)OCC.N>CO>CCOP(=O)([O-])CCOCn1cnc2c(N)ncnc21.[NH4+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-665b5ee29c834289ad987373eaa9f519
CCOP(=O)([O-])CCOCn1cnc2c(N)ncnc21>>Nc1ncnc2c1ncn2COCCP(=O)(O)O
N1=CN=C2N(C=NC2=C1N)COCCP(OCC)([O-])=O.[NH4+].CO.O>>N1=CN=C2N(C=NC2=C1N)COCCP(O)(O)=O
CC[O:18][P:15]([CH2:14][CH2:13][O:12][CH2:11][n:10]1[c:6]2[n:5][cH:4][n:3][c:2]([NH2:1])[c:7]2[n:8][cH:9]1)(=[O:16])[O-:17]>>[NH2:1][c:2]1[n:3][cH:4][n:5][c:6]2[c:7]1[n:8][cH:9][n:10]2[CH2:11][O:12][CH2:13][CH2:14][P:15](=[O:16])([OH:17])[OH:18]
CCOP(=O)([O-])CCOCn1cnc2c(N)ncnc21
Nc1ncnc2c1ncn2COCCP(=O)(O)O
null
null
CN(C)C=O
Deprotection
OtherReaction
eaaf8436ac19e7e26db9ff78e61eed5caf13b9167196c3230a9e1eb66b295f8b
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
c1ncc2nc[nH]c2n1
C-C-[O;H0;D2;+0:1]-[#15:2](-[C:3])(-[O-;H0;D1:4])=[O;D1;H0:5]>>[C:3]-[#15:2](=[O;D1;H0:5])(-[OH;D1;+0:4])-[OH;D1;+0:1]
45
[{"value": 45.0, "product": "N1=CN=C2N(C=NC2=C1N)COCCP(O)(O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 43.9, "product": "N1=CN=C2N(C=NC2=C1N)COCCP(O)(O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
40
CELSIUS
6
HOUR
To a solution of 12 (0.32 g, 1.0 mmol) in DMF (7.0 mL) was added Me3 SiBr (1.07 g, 7.01 mmol). After the solution was stirred at 40° C. for 6 h, a mixture of MeOH and H2O(5:1, 20 mL) was added and the solvents were evaporated. The crude residue was purified by use of column chromatography (resin XAD-4, H2O) to afford 1...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ncnc2nc[nH]c12
Other
CN(C)C=O
40
6
CCOP(=O)([O-])CCOCn1cnc2c(N)ncnc21>CN(C)C=O>Nc1ncnc2c1ncn2COCCP(=O)(O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-04b5894104d743daa3447f348afad5c1
CCC(=O)N[C@@H]1CCc2cc3c(cc2[C@H]1O)SCC3>>CCCN[C@@H]1CCc2cc3c(cc2[C@H]1O)SCC3
O[C@H]1[C@@H](CCC2=CC3=C(SCC3)C=C12)NC(CC)=O.[OH-].[Na+]>>O[C@H]1[C@@H](CCC2=CC3=C(SCC3)C=C12)NCCC
O=[C:3]([CH2:2][CH3:1])[NH:4][C@@H:5]1[CH2:6][CH2:7][c:8]2[cH:9][c:10]3[c:11]([cH:12][c:13]2[C@H:14]1[OH:15])[S:16][CH2:17][CH2:18]3>>[CH3:1][CH2:2][CH2:3][NH:4][C@@H:5]1[CH2:6][CH2:7][c:8]2[cH:9][c:10]3[c:11]([cH:12][c:13]2[C@H:14]1[OH:15])[S:16][CH2:17][CH2:18]3
CCC(=O)N[C@@H]1CCc2cc3c(cc2[C@H]1O)SCC3
CCCN[C@@H]1CCc2cc3c(cc2[C@H]1O)SCC3
null
null
O.O1CCCC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1c2c(cc3c1CCS3)CCCC2
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[C:4]-[C;D1;H3:5]>>[C:3]-[#7:2]-[CH2;D2;+0:1]-[C:4]-[C;D1;H3:5]
97
[{"value": 97.0, "product": "O[C@H]1[C@@H](CCC2=CC3=C(SCC3)C=C12)NCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 21.2, "product": "O[C@H]1[C@@H](CCC2=CC3=C(SCC3)C=C12)NCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
In a 500 ml three-necked flask fitted with a magnetic stirrer and a nitrogen inlet, 2.3 g (61 mmol) of AILiH4 are suspended in 75 ml of dry tetrahydrofuran. 6.2 g (24.5 mmol) of the product obtained in Step 2 dissolved in 97 ml of dry tetrahydrofuran are slowly added at room temperature. After 18 hours' stirring at roo...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1c2c(cc3c1CCS3)CCCC2
Other
O.O1CCCC1
null
18
CCC(=O)N[C@@H]1CCc2cc3c(cc2[C@H]1O)SCC3>O.O1CCCC1>CCCN[C@@H]1CCc2cc3c(cc2[C@H]1O)SCC3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-84edcdeb710843f298afe85eff4bc91e
C=CC#N.CN(C)CCCCN>>CN(C)CCCCNCCC#N
C(C=C)#N.CN(CCCCN)C>>C(#N)CCNCCCCN(C)C
[CH2:9]=[CH:10][C:11]#[N:12].[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][CH2:7][NH2:8]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][CH2:7][NH:8][CH2:9][CH2:10][C:11]#[N:12]
C=CC#N.CN(C)CCCCN
CN(C)CCCCNCCC#N
null
null
CO
Heteroatom Alkylation and Arylation
aza-Michael addition primary
b45dd075b7e75caee6dc0a68cb402266c75e0848f7502f06a5dbd8a34863aae2
2e45960e6468a140db4162555f247a2535630c23e1aa16e082b84ce22691ebbf
null
[CH2;D1;+0:1]=[CH;D2;+0:2]-[C:3]#[N;D1;H0:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:3]#[N;D1;H0:4]
80
[{"value": 80.0, "product": "C(#N)CCNCCCCN(C)C", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
A solution of acrylonitrile (1.17 g, 22.07 mmol) in methanol (1.0 ml) was added dropwise to a solution of N,N-dimethyl-1,4-diaminobutane 322 (2.1 g, 18.42 mmol) in methanol (1.0 ml) at 0° C., and the mixture was stirred at 0° C. for sixteen hours. Evaporation of the solvent in vacuo afforded almost pure N-(2-cyanoethyl...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Vinyl
Secondary amine
null
null
null
null
CO
0
null
C=CC#N.CN(C)CCCCN>CO>CN(C)CCCCNCCC#N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9d5cb107bd0146788c6f94e9866436c0
CN(C)CCCCN(CCC#N)C(=O)OC(C)(C)C>>CN(C)CCCCN(CCCN)C(=O)OC(C)(C)C
[H-].[H-].[H-].[H-].[Li+].[Al+3].C(C)(C)(C)OC(=O)N(CCCCN(C)C)CCC#N>>NCCCN(CCCCN(C)C)C(=O)OC(C)(C)C
[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][CH2:7][N:8]([CH2:9][CH2:10][C:11]#[N:12])[C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][CH2:7][N:8]([CH2:9][CH2:10][CH2:11][NH2:12])[C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19]
CN(C)CCCCN(CCC#N)C(=O)OC(C)(C)C
CN(C)CCCCN(CCCN)C(=O)OC(C)(C)C
null
null
CCOCC
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
null
[C:1]-[C:2]-[C;H0;D2;+0:3]#[N;H0;D1;+0:4]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[NH2;D1;+0:4]
59
[{"value": 59.0, "product": "NCCCN(CCCCN(C)C)C(=O)OC(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.7, "product": "NCCCN(CCCCN(C)C)C(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
To a solution of LAH (0.62 mg, 16.30 mmol) in anhydrous ether (100 ml) was added N-(tert-butoxycarbonyl)--N-(2-cyanoethyl)-N',N'-dimethyl-1,4-diaminobutane 324 (2.22 g, 8.10 mmol) in anhydrous ether (50 ml) at 0° C. The mixture was stirred at 0° C. for thirty minutes. The excess LAH was quenched with 1N NaOH at 0° C., ...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
null
null
CCOCC
0
null
CN(C)CCCCN(CCC#N)C(=O)OC(C)(C)C>CCOCC>CN(C)CCCCN(CCCN)C(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-78b65606c5ee45768c20fb14a7e7de91
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)O)[C@@]4(C)CC[C@@H]32)C1.O=C(Cl)C(=O)Cl>>CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)Cl)[C@@]4(C)CC[C@@H]32)C1
C(C)(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H]([C@@H](CCC(=O)O)C)[C@]4(CC[C@@H]3[C@]2(CC1)C)C.C(C(=O)Cl)(=O)Cl>>C(C)(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H]([C@@H](CCC(=O)Cl)C)[C@]4(CC[C@@H]3[C@]2(CC1)C)C
O[C:22]([CH2:21][CH2:20][C@H:18]([C@H:17]1[CH2:16][CH2:15][C@H:14]2[C@@H:13]3[CH2:12][CH:11]=[C:10]4[C@:8]([CH3:9])([CH2:7][CH2:6][C@H:5]([O:4][C:2]([CH3:1])=[O:3])[CH2:30]4)[C@H:29]3[CH2:28][CH2:27][C@@:25]21[CH3:26])[CH3:19])=[O:23].O=C(Cl)C(=O)[Cl:24]>>[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[CH2:6][CH2:7][C@@:8]2([CH3:9])...
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)O)[C@@]4(C)CC[C@@H]32)C1.O=C(Cl)C(=O)Cl
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)Cl)[C@@]4(C)CC[C@@H]32)C1
null
null
ClCCl
Functional Group Interconversion
Alcohol to chloride_Other
013cec2edeb273a7a148f349d36a52d99ff4e7bcf8eed78085df830088e387ac
aedb1f68dc5b7eb0583043e1125b741382b17974140a2f46554f0110e2ddc884
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3[C@@H]2C1
Cl-C(=O)-C(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
1
HOUR
To a solution of 3β-acetoxy-5-cholenic acid (50.0 g, 118 mmole) in dry dichloromethane (200 ml) was added dropwise oxalyl chloride (30 ml, 448 mmole). The solution was stirred at room temperature for one hour and then concentrated in vacuo to obtain 3β-acetoxy-5-cholenic acid chloride 331. 1H NMR (400 MHz, CDCl3) δ: 0....
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Carboxylic acid
Acyl halide
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
HCl
ClCCl
null
1
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)O)[C@@]4(C)CC[C@@H]32)C1.O=C(Cl)C(=O)Cl>ClCCl>CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)Cl)[C@@]4(C)CC[C@@H]32)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b098fde08ae9480bb834d7a3afe28656
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)Cl)[C@@]4(C)CC[C@@H]32)C1.CC(C)Br>>CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)C(C)C)[C@@]4(C)CC[C@@H]32)C1
C(C)(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H]([C@@H](CCC(=O)Cl)C)[C@]4(CC[C@@H]3[C@]2(CC1)C)C.Cl.BrC(C)C.C(C)(C)[Mg]Br.[Mg]>>C(C)(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H]([C@@H](CCC(C(C)C)=O)C)[C@]4(CC[C@@H]3[C@]2(CC1)C)C
Cl[C:22]([CH2:21][CH2:20][C@H:18]([C@H:17]1[CH2:16][CH2:15][C@H:14]2[C@@H:13]3[CH2:12][CH:11]=[C:10]4[C@:8]([CH3:9])([CH2:7][CH2:6][C@H:5]([O:4][C:2]([CH3:1])=[O:3])[CH2:32]4)[C@H:31]3[CH2:30][CH2:29][C@@:27]21[CH3:28])[CH3:19])=[O:23].Br[CH:24]([CH3:25])[CH3:26]>>[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[CH2:6][CH2:7][C@@:8]2...
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)Cl)[C@@]4(C)CC[C@@H]32)C1.CC(C)Br
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)C(C)C)[C@@]4(C)CC[C@@H]32)C1
null
[Br-].[Cd+2].[Br-]
CCOCC.C1=CC=CC=C1
C-C Coupling
OtherReaction
1a82298ae4aa4f3a471f136807b8bb5808cc2b5f42cb51ba765c73e0855ddfc3
9d8d90537f36b9d149b91de6298c1feb746b621c63a1437522f2775cb55320fe
C1=C2CCCCC2[C@H]2CCC3CCC[C@H]3[C@@H]2C1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C;D1;H3:3].Cl-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[C:7]>>[C:7]-[C:6]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[CH;D3;+0:1](-[C;D1;H3:2])-[C;D1;H3:3]
70
[{"value": 70.0, "product": "C(C)(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H]([C@@H](CCC(C(C)C)=O)C)[C@]4(CC[C@@H]3[C@]2(CC1)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.9, "product": "C(C)(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CC[C@H]([C@@H](CCC(C(C)C)=O)C)[C@]4(CC[C@@H]3[C@]2(CC1)C)C", "details": "CALCULATED...
null
null
null
null
To a mixture of magnesium (24 g, 1.00 mole) in dry ether (500 ml) was added dropwise 2-bromopropane (60 ml, 639 mmole) while stirring. After the addition was completed, the reaction mixture was stirred for thirty minutes. The ethereal solution was transferred to another flask. Then to the resulting isopropyl-magnesium ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary halide
Ketone
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
Br-
[Br-].[Cd+2].[Br-].CCOCC.C1=CC=CC=C1
null
null
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)Cl)[C@@]4(C)CC[C@@H]32)C1.CC(C)Br>[Br-].[Cd+2].[Br-].CCOCC.C1=CC=CC=C1>CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@H]3[C@@H]4CC[C@H]([C@H](C)CCC(=O)C(C)C)[C@@]4(C)CC[C@@H]32)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a9146312177a4f9b96171064a8052dc6
C=CC#N.NCCCCN>>N#CCCNCCCCN
NCCCCN.C(C=C)#N>>C(#N)CCNCCCCN
[N:1]#[C:2][CH:3]=[CH2:4].[NH2:5][CH2:6][CH2:7][CH2:8][CH2:9][NH2:10]>>[N:1]#[C:2][CH2:3][CH2:4][NH:5][CH2:6][CH2:7][CH2:8][CH2:9][NH2:10]
C=CC#N.NCCCCN
N#CCCNCCCCN
null
null
CO
Heteroatom Alkylation and Arylation
aza-Michael addition primary
b45dd075b7e75caee6dc0a68cb402266c75e0848f7502f06a5dbd8a34863aae2
2e45960e6468a140db4162555f247a2535630c23e1aa16e082b84ce22691ebbf
null
[CH2;D1;+0:1]=[CH;D2;+0:2]-[C:3]#[N;D1;H0:4].[C:5]-[C:6]-[NH2;D1;+0:7]>>[C:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:3]#[N;D1;H0:4]
80
[{"value": 80.0, "product": "C(#N)CCNCCCCN", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.8, "product": "C(#N)CCNCCCCN", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1,4-diaminobutane (4.3 g, 48.8 mmole) in methanol (1.5 ml) was added a solution of acrylonitrile (3.1 g, 58.4 mmole) in methanol (1.5 ml) at 0° C., and the mixture was stirred for twelve hours. Evaporation of the solvent in vacuo afforded N-(2'-cyanoethyl)-1,4-diaminobutane as a colorless oil (5.5 g, 8...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Vinyl
Secondary amine
null
null
null
null
CO
null
null
C=CC#N.NCCCCN>CO>N#CCCNCCCCN
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-26714608e58f4c188b984bcbdffd717d
CN(C)C=O.On1nnc2ccccc21>>C(=NC1CCCCC1)=NC1CCCCC1
O.CN(C=O)C.C=1C=CC2=C(C1)N=NN2O>>C1CCC(CC1)N=C=NC2CCCCC2
O=[CH:1][N:2]([CH3:10])[CH3:13].O[n:9]1nn[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]21>>[C:1](=[N:2][CH:3]1[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8]1)=[N:9][CH:10]1[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]1
CN(C)C=O.On1nnc2ccccc21
C(=NC1CCCCC1)=NC1CCCCC1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
114f3155f1ca7cd07407db85b051f50fc4a6d62987a3a4d615a136aa5a7fbbfd
8023798407645490f6e731ea699842ac34c1c05388635bc82dc9a964e1bf68d5
C(=NC1CCCCC1)=NC1CCCCC1
O-[n;H0;D3;+0:1]1:n:n:[c;H0;D3;+0:2]2:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[c;H0;D3;+0:7]:2:1.O=[CH;D2;+0:8]-[N;H0;D3;+0:9](-[CH3;D1;+0:10])-[CH3;D1;+0:11]>>[C:12]1-[C:13]-[CH2;D2;+0:11]-[C:14]-[C:15]-[CH;D3;+0:10]-1-[N;H0;D2;+0:1]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[CH;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[...
100
[{"value": 100.0, "product": "C1CCC(CC1)N=C=NC2CCCCC2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The subtitled compound was prepared substantially in accordance with the procedure detailed in Example 33, using 0.17 g (0.55 mmol) of S-2-N(t-butoxycarbonyl)amino-3-p-fluoro-phenylthio propanoic acid, 0.22 g (0.55 mmol) of the subtitled intermediate of Preparation 3B and 0.07 g (0.55 mmol) of HOBT.H2O, and 0.11 g (0.5...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
null
c1ccc2[nH]nnc2c1
C1CCCCC1.C1CCCCC1
C1CCCCC1.C1CCCCC1
null
O1CCCC1
null
null
CN(C)C=O.On1nnc2ccccc21>O1CCCC1>C(=NC1CCCCC1)=NC1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7eea098e740f49b1bcfabe60ca2ecee0
CN(C)C=O.On1nnc2ccccc21>>C(=NC1CCCCC1)=NC1CCCCC1
C=1C=CC2=C(C1)N=NN2O.O.CN(C=O)C>>C1CCC(CC1)N=C=NC2CCCCC2
O=[CH:1][N:2]([CH3:10])[CH3:13].O[n:9]1nn[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]21>>[C:1](=[N:2][CH:3]1[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8]1)=[N:9][CH:10]1[CH2:11][CH2:12][CH2:13][CH2:14][CH2:15]1
CN(C)C=O.On1nnc2ccccc21
C(=NC1CCCCC1)=NC1CCCCC1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
114f3155f1ca7cd07407db85b051f50fc4a6d62987a3a4d615a136aa5a7fbbfd
8023798407645490f6e731ea699842ac34c1c05388635bc82dc9a964e1bf68d5
C(=NC1CCCCC1)=NC1CCCCC1
O-[n;H0;D3;+0:1]1:n:n:[c;H0;D3;+0:2]2:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[c;H0;D3;+0:7]:2:1.O=[CH;D2;+0:8]-[N;H0;D3;+0:9](-[CH3;D1;+0:10])-[CH3;D1;+0:11]>>[C:12]1-[C:13]-[CH2;D2;+0:11]-[C:14]-[C:15]-[CH;D3;+0:10]-1-[N;H0;D2;+0:1]=[C;H0;D2;+0:8]=[N;H0;D2;+0:9]-[CH;D3;+0:2]1-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[...
null
[]
null
null
null
null
The subtitled compound was prepared substantially in accordance with the procedure detailed in Example 33, using 0.41 g (0.12 mmol) of S-2-N(t-butoxycarbonyl)amino-3-naphth-2-ylthio propanoic acid, 0.47 g (0.12 mmol) of the subtitled intermediate of Preparation 3B and 0.16 g (0.12 mmol) of HOBT.H2O, and 0.24 g (0.12 mm...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
null
c1ccc2[nH]nnc2c1
C1CCCCC1.C1CCCCC1
C1CCCCC1.C1CCCCC1
null
O1CCCC1
null
null
CN(C)C=O.On1nnc2ccccc21>O1CCCC1>C(=NC1CCCCC1)=NC1CCCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-83eb8c4f8a924307bcc393ec98b1dc0e
CCc1c(COC(C)=O)[nH]c(C(=O)OCc2ccccc2)c1C.CCc1c[nH]cc1CC.Cc1ccc(S(=O)(=O)O)cc1>>CCc1c(Cc2[nH]c(Cc3[nH]c(C(=O)OCc4ccccc4)c(C)c3CC)c(CC)c2CC)[nH]c(C(=O)OCc2ccccc2)c1C
C(C)C1=CNC=C1CC.C(C)(=O)OCC1=C(C(=C(N1)C(=O)OCC1=CC=CC=C1)C)CC.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C(C1=CC=CC=C1)OC(=O)C1=C(C(=C(N1)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CC)C)C(=O)OCC1=CC=CC=C1)CC)C
O([CH2:5][c:4]1[c:3]([CH2:2][CH3:1])[c:46]([CH3:47])[c:35]([C:36](=[O:37])[O:38][CH2:39][c:40]2[cH:41][cH:42][cH:43][cH:44][cH:45]2)[nH:34]1)[C:8](=[O:14])[CH3:24].[cH:6]1[nH:7][cH:10][c:25]([CH2:26][CH3:27])[c:31]1[CH2:32][CH3:33].O=S(=O)([OH:15])[c:20]1[cH:19][cH:18][c:17]([CH3:16])[cH:22][cH:21]1>>[CH3:1][CH2:2][c:3...
CCc1c(COC(C)=O)[nH]c(C(=O)OCc2ccccc2)c1C.CCc1c[nH]cc1CC.Cc1ccc(S(=O)(=O)O)cc1
CCc1c(Cc2[nH]c(Cc3[nH]c(C(=O)OCc4ccccc4)c(C)c3CC)c(CC)c2CC)[nH]c(C(=O)OCc2ccccc2)c1C
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
600aaf398f929c1262936e200da881e7793fedc5e27f3fc1a58785791ed628e0
65cad71a238f9f57a0a754682b9dac8d4198c0621de1552964f93c5ea2fe28f4
O=C(OCc1ccccc1)c1ccc(Cc2ccc(Cc3ccc(C(=O)OCc4ccccc4)[nH]3)[nH]2)[nH]1
O=S(=O)(-[OH;D1;+0:1])-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[c:5](-[CH3;D1;+0:6]):[c:7]:[c:8]:1.[#8:9]-[C:10](=[O;D1;H0:11])-[c:12]:[#7;a:13]:[c:14](-[CH2;D2;+0:15]-O-[C;H0;D3;+0:16](-[CH3;D1;+0:17])=[O;H0;D1;+0:18]):[c:19].[C;D1;H3:20]-[C:21]-[c;H0;D3;+0:22]1:[cH;D2;+0:23]:[nH;D2;+0:24]:[cH;D2;+0:25]:[c;H0;D3;+0:26]:1-[C:27]-[...
82
[{"value": 82.0, "product": "C(C1=CC=CC=C1)OC(=O)C1=C(C(=C(N1)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CC)C)C(=O)OCC1=CC=CC=C1)CC)C", "details": "PERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
3,4-Diethylpyrrole (2A, FIG. 2)28 (0.6, 4.9 mmol), benzyl 5-(acetoxymethyl)-3-methyl-4-ethyl-pyrrole-2-carboxylate (2B, FIG. 2)29 (2.5 g, 7.9 mmol), and p-toluenesulfonic acid (0.15 g) were dissolved in 60 mL of absolute ethanol and heated at 60° C. for 8 h under nitrogen. The resulting suspension was reduced in volume...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Ester
Ester
c1cc[nH]c1.c1ccccc1
c1cc[nH]c1.c1cc[nH]c1.c1ccccc1
c1cc[nH]c1.c1cc[nH]c1.c1cc[nH]c1.c1ccccc1.c1ccccc1
null
C(C)O
60
null
CCc1c(COC(C)=O)[nH]c(C(=O)OCc2ccccc2)c1C.CCc1c[nH]cc1CC.Cc1ccc(S(=O)(=O)O)cc1>C(C)O>CCc1c(Cc2[nH]c(Cc3[nH]c(C(=O)OCc4ccccc4)c(C)c3CC)c(CC)c2CC)[nH]c(C(=O)OCc2ccccc2)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-faa1480b90664caba1f4a00882c01709
CCc1c[nH]cc1CC.COC(=O)CCc1c(COC(C)=O)[nH]c(C(=O)OCc2ccccc2)c1C.Cc1ccc(S(=O)(=O)O)cc1>>CCc1c(Cc2[nH]c(C(=O)OCc3ccccc3)c(C)c2CCC(=O)OC)[nH]c(Cc2[nH]c(C(=O)OCc3ccccc3)c(C)c2CCC(=O)OC)c1CC
C(C)C1=CNC=C1CC.C(C)(=O)OCC=1NC(=C(C1CCC(=O)OC)C)C(=O)OCC1=CC=CC=C1.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C(C1=CC=CC=C1)OC(=O)C1=C(C(=C(N1)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CCC(=O)OC)C)C(=O)OCC1=CC=CC=C1)CCC(=O)OC)C
[CH3:1][CH2:2][c:3]1[cH:4][nH:7][cH:29][c:53]1[CH2:54][CH3:55].[O:11]([C:24]([CH3:23])=[O:25])[CH2:30][c:31]1[nH:32][c:33]([C:34](=[O:35])[O:36][CH2:37][c:38]2[cH:39][cH:40][cH:41][cH:42][cH:43]2)[c:44]([CH3:45])[c:46]1[CH2:47][CH2:48][C:49]([O:26][CH3:27])=[O:50].O=S([c:9]1[cH:5][cH:52][c:13]([CH3:12])[cH:14][cH:15]1)...
CCc1c[nH]cc1CC.COC(=O)CCc1c(COC(C)=O)[nH]c(C(=O)OCc2ccccc2)c1C.Cc1ccc(S(=O)(=O)O)cc1
CCc1c(Cc2[nH]c(C(=O)OCc3ccccc3)c(C)c2CCC(=O)OC)[nH]c(Cc2[nH]c(C(=O)OCc3ccccc3)c(C)c2CCC(=O)OC)c1CC
null
null
null
Aromatic Heterocycle Formation
OtherReaction
41c704c9268eecf128b8ec15576492d38d32af8d1b98e647657336d6d17e7795
a62d3e14dc3e686bbba664c7702698a10196425b96dfa226dc079bfa87919be9
O=C(OCc1ccccc1)c1ccc(Cc2ccc(Cc3ccc(C(=O)OCc4ccccc4)[nH]3)[nH]2)[nH]1
O=S(=[O;H0;D1;+0:1])(-[OH;D1;+0:2])-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[c:5]:[c;H0;D3;+0:6](-[CH3;D1;+0:7]):[cH;D2;+0:8]:[cH;D2;+0:9]:1.[#8:10]-[C:11](=[O;D1;H0:12])-[c:13]:[#7;a:14]:[c:15](-[CH2;D2;+0:16]-[O;H0;D2;+0:17]-[C;H0;D3;+0:18](-[CH3;D1;+0:19])=[O;D1;H0:20]):[c:21]-[C:22]-[C:23]-[C;H0;D3;+0:24](=[O;D1;H0:25])-[O;H0...
61
[{"value": 61.0, "product": "C(C1=CC=CC=C1)OC(=O)C1=C(C(=C(N1)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CCC(=O)OC)C)C(=O)OCC1=CC=CC=C1)CCC(=O)OC)C", "details": "PERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
7C, FIG. 7. In a 500 mL round bottom flask was placed 250 mL of ethanol from an unopened bottle and this was then purged with dry nitrogen for ten minutes. 3,4-Diethylpyrrole 7B (1.29 g, 0.01 mol) and 2-acetoxymethyl-5-benzyloxycarbonyl-4-methyl-3-methoxycarbonylethylpyrrole 7A (7.83 g, 0.02 mol) were added and the mix...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Ester.Ester
Ester.Ester.Ester
c1cc[nH]c1.c1ccccc1
c1cc[nH]c1.c1cc[nH]c1.c1ccccc1
c1cc[nH]c1.c1cc[nH]c1.c1ccccc1.c1cc[nH]c1.c1ccccc1
null
null
60
null
CCc1c[nH]cc1CC.COC(=O)CCc1c(COC(C)=O)[nH]c(C(=O)OCc2ccccc2)c1C.Cc1ccc(S(=O)(=O)O)cc1>>CCc1c(Cc2[nH]c(C(=O)OCc3ccccc3)c(C)c2CCC(=O)OC)[nH]c(Cc2[nH]c(C(=O)OCc3ccccc3)c(C)c2CCC(=O)OC)c1CC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-712078ea7b614a19ba70e3fd5bf416de
CCc1c(Cc2[nH]c(C=O)c(C)c2CCCOC(C)=O)[nH]c(Cc2[nH]c(C=O)c(C)c2CCCOC(C)=O)c1CC>>CCc1c(Cc2[nH]c(C=O)c(C)c2CCCO)[nH]c(Cc2[nH]c(C=O)c(C)c2CCCO)c1CC
C(C)(=O)OCCCC1=C(NC(=C1C)C=O)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CCCOC(C)=O)C)C=O.[Li+].[OH-]>>C(=O)C1=C(C(=C(N1)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CCCO)C)C=O)CCCO)C
CC(=O)[O:17][CH2:16][CH2:15][CH2:14][c:13]1[c:6]([CH2:5][c:4]2[c:3]([CH2:2][CH3:1])[c:33]([CH2:34][CH3:35])[c:19]([CH2:20][c:21]3[nH:22][c:23]([CH:24]=[O:25])[c:26]([CH3:27])[c:28]3[CH2:29][CH2:30][CH2:31][O:32]C(C)=O)[nH:18]2)[nH:7][c:8]([CH:9]=[O:10])[c:11]1[CH3:12]>>[CH3:1][CH2:2][c:3]1[c:4]([CH2:5][c:6]2[nH:7][c:8]...
CCc1c(Cc2[nH]c(C=O)c(C)c2CCCOC(C)=O)[nH]c(Cc2[nH]c(C=O)c(C)c2CCCOC(C)=O)c1CC
CCc1c(Cc2[nH]c(C=O)c(C)c2CCCO)[nH]c(Cc2[nH]c(C=O)c(C)c2CCCO)c1CC
null
null
CO
Reduction
OtherReaction
8eb0b0948ba02d6bff2e6dcc47886480a262869f201923801796429d5f921f16
3906c52a610c5241bd14656b0a46d01a4c70864c3b16d9b6e34a49708e61df8d
c1c[nH]c(Cc2ccc(Cc3ccc[nH]3)[nH]2)c1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3].C-C(=O)-[O;H0;D2;+0:4]-[C:5]-[C:6]>>[C:3]-[C:2]-[OH;D1;+0:1].[C:6]-[C:5]-[OH;D1;+0:4]
94
[{"value": 94.0, "product": "C(=O)C1=C(C(=C(N1)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CCCO)C)C=O)CCCO)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.6, "product": "C(=O)C1=C(C(=C(N1)CC=1NC(=C(C1CC)CC)CC=1NC(=C(C1CCCO)C)C=O)CCCO)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
7H, FIG. 7. 2,5-Bis[(3-acetoxypropyl-5-formyl-4-methylpyrrol-2-yl)methyl]-3,4-diethylpyrrole 7G (5.98 g, 0.011 mol) and LiOH (1.76 g, 0.042 mol) were added to 400 mL of 95% methanol, which had been degassed with nitrogen prior to use, add the mixture heated to reflux under a nitrogen atmosphere. The reaction became hom...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Primary alcohol.Primary alcohol
null
null
c1cc[nH]c1.c1cc[nH]c1.c1cc[nH]c1
HO-
CO
null
null
CCc1c(Cc2[nH]c(C=O)c(C)c2CCCOC(C)=O)[nH]c(Cc2[nH]c(C=O)c(C)c2CCCOC(C)=O)c1CC>CO>CCc1c(Cc2[nH]c(C=O)c(C)c2CCCO)[nH]c(Cc2[nH]c(C=O)c(C)c2CCCO)c1CC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-61d7db87905c47f9b370b8d2340da826
COc1cc([N+](=O)[O-])c([N+](=O)[O-])cc1OC>>O=[N+]([O-])c1cc(O)c(O)cc1[N+](=O)[O-]
Br.COC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])OC>>OC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])O
C[O:7][c:6]1[cH:5][c:4]([N+:2](=[O:1])[O-:3])[c:11]([N+:12](=[O:13])[O-:14])[cH:10][c:8]1[O:9]C>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([OH:7])[c:8]([OH:9])[cH:10][c:11]1[N+:12](=[O:13])[O-:14]
COc1cc([N+](=O)[O-])c([N+](=O)[O-])cc1OC
O=[N+]([O-])c1cc(O)c(O)cc1[N+](=O)[O-]
null
null
C(C)(=O)O
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4](-[O;H0;D2;+0:5]-C):[c:6]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4](-[OH;D1;+0:5]):[c:6]
9,869.8
[{"value": 84.0, "product": "OC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 9869.8, "product": "OC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
8B, FIG. 8. In a dry 500 mL round bottom flask, 1,2-dimethoxy-4,5-dinitrobenzene (3.2 g, 0.12 mmol) 8A was stirred vigorously in 40 mL of glacial acetic acid at 30° C. Once a homogeneous solution 200 mL of 48% HBr was added to the flask and the reaction was slowly heated to reflux. The reaction was complete as indicate...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1
Other
C(C)(=O)O
null
4
COc1cc([N+](=O)[O-])c([N+](=O)[O-])cc1OC>C(C)(=O)O>O=[N+]([O-])c1cc(O)c(O)cc1[N+](=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-158b075907054ab39ba581443375f769
O=[N+]([O-])c1cc(O)c(O)cc1[N+](=O)[O-].OCC(O)CCl.[OH-]>>O=[N+]([O-])c1cc(OCC(O)CO)c(OCC(O)CO)cc1[N+](=O)[O-]
OC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])O.ClCC(CO)O.[OH-].[K+]>>OC(COC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])OCC(CO)O)CO
[O-:1][N+:2]([c:4]1[cH:5][c:6]([OH:7])[c:13]([OH:14])[cH:20][c:11]1[N+:22](=[O:23])[O-:24])=[O:12].Cl[CH2:8][CH:9]([OH:10])[CH2:18][OH:19].[OH-:17]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([O:7][CH2:8][CH:9]([OH:10])[CH2:11][OH:12])[c:13]([O:14][CH2:15][CH:16]([OH:17])[CH2:18][OH:19])[cH:20][c:21]1[N+:22](=[O:23])[O-:24]
O=[N+]([O-])c1cc(O)c(O)cc1[N+](=O)[O-].OCC(O)CCl.[OH-]
O=[N+]([O-])c1cc(OCC(O)CO)c(OCC(O)CO)cc1[N+](=O)[O-]
null
null
C(CCC)O
C-C Coupling
OtherReaction
77234debcd7382bb96dee1071914678bc9622b5773ffb5986defbec6cbdb1be6
6231048ecbe0ac7045ba507e078985495fd6b43d9ee9f2401519f1f270735cc4
c1ccccc1
Cl-[CH2;D2;+0:1]-[CH;D3;+0:2](-[O;D1;H1:3])-[CH2;D2;+0:4]-[O;D1;H1:5].[O-;H0;D1:6]-[N+;H0;D3:7](=[O;H0;D1;+0:8])-[c;H0;D3;+0:9]1:[c:10]:[c:11](-[OH;D1;+0:12]):[c:13](-[OH;D1;+0:14]):[cH;D2;+0:15]:[c;H0;D3;+0:16]:1-[N+;H0;D3:17](-[O;-;D1;H0:18])=[O;D1;H0:19].[OH-;D0:20]>>[O;-;D1;H0:18]-[N+;H0;D3:17](=[O;D1;H0:19])-[c:21...
67.9
[{"value": 30.0, "product": "OC(COC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])OCC(CO)O)CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.9, "product": "OC(COC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])OCC(CO)O)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
8C, FIG. 8. 1,2-Dihydroxy-4,5-dinitrobenzene 8B (5.0 g, 22 mmol) and 1-chloro-2,3-dihydroxypropane (12.1 g, 110 mmol) were refluxed for 48 hours in a solution of potassium hydroxide (4.4 g) in 1-butanol (100 mL) under a nitrogen atmosphere. The resulting mixture was concentrated under reduced pressure, and the dark res...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Nitro group.Nitro group.Primary alcohol.Secondary alcohol.Aromatic alcohol.Aromatic alcohol
Ether.Ether.Nitro group.Nitro group.Primary alcohol.Primary alcohol.Secondary alcohol.Secondary alcohol
c1ccccc1
c1ccccc1
c1ccccc1
null
C(CCC)O
null
0.25
O=[N+]([O-])c1cc(O)c(O)cc1[N+](=O)[O-].OCC(O)CCl.[OH-]>C(CCC)O>O=[N+]([O-])c1cc(OCC(O)CO)c(OCC(O)CO)cc1[N+](=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1df0841ea5aa4fe28c1d99da441ccf1a
COC(=O)c1nc2ccccc2c(O)c1C(=O)OC.NN>>O=c1[nH][nH]c(=O)c2c(O)c3ccccc3nc12
OC1=C(C(=NC2=CC=CC=C12)C(=O)OC)C(=O)OC.O.NN>>OC1=C2C(=NC=3C=CC=CC13)C(NNC2=O)=O
CO[C:2](=[O:1])[c:17]1[c:7]([C:5](OC)=[O:6])[c:8]([OH:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[n:16]1.[NH2:3][NH2:4]>>[O:1]=[c:2]1[nH:3][nH:4][c:5](=[O:6])[c:7]2[c:8]([OH:9])[c:10]3[cH:11][cH:12][cH:13][cH:14][c:15]3[n:16][c:17]12
COC(=O)c1nc2ccccc2c(O)c1C(=O)OC.NN
O=c1[nH][nH]c(=O)c2c(O)c3ccccc3nc12
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
ec1917a0188259fb1d502a40ed3d9aad8b3b567f28677d868775be5ee838e719
1775b7eba35fc46eaa0b0ad39cde9e207db465168e4fe5d9832db816e257be74
O=c1[nH][nH]c(=O)c2nc3ccccc3cc12
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[#7;a:4]:[c:5]):[c:6](-[C;H0;D3;+0:7](=[O;D1;H0:8])-O-C):[c:9].[NH2;D1;+0:10]-[NH2;D1;+0:11]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:10]:[nH;D2;+0:11]:[c;H0;D3;+0:7](=[O;D1;H0:8]):[c:6](:[c:9]):[c:3]:1:[#7;a:4]:[c:5]
112.8
[{"value": 112.8, "product": "OC1=C2C(=NC=3C=CC=CC13)C(NNC2=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirred suspension of dimethyl 4-hydroxyquinoline-2,3-dicarboxylate (1.00 g, 3.83 mM, prepared as described by H. Biere and W. Seelen, Liebigs Ann. Chem. 1976, 1972) in ethanol (15 mL) was added hydrazine hydrate (9.64 g, 193 mM) whereupon the solids dissolved. The resulting solution was refluxed for 3 hr during w...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ester.Ester
null
c1ccc2ncccc2c1
C1=c2cc3ccccc3nc2=CNN1
C1=c2cc3ccccc3nc2=CNN1
HO-
C(C)O
null
null
COC(=O)c1nc2ccccc2c(O)c1C(=O)OC.NN>C(C)O>O=c1[nH][nH]c(=O)c2c(O)c3ccccc3nc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d09058163d114c2aaa3e06a2b0426827
COC(=O)C#CC(=O)OC.COC(=O)c1ccc(Cl)cc1N>>COC(=O)c1nc2cc(Cl)ccc2c(O)c1C(=O)OC
CC(C)([O-])C.[K+].NC1=C(C(=O)OC)C=CC(=C1)Cl.C(#CC(=O)OC)C(=O)OC.C(#CC(=O)OC)C(=O)OC>>ClC1=CC=C2C(=C(C(=NC2=C1)C(=O)OC)C(=O)OC)O
[CH3:1][O:2][C:3](=[O:4])[C:5]#[C:16][C:17](=[O:18])[O:19][CH3:20].CO[C:14]([c:13]1[c:7]([NH2:6])[cH:8][c:9]([Cl:10])[cH:11][cH:12]1)=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[n:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][cH:12][c:13]2[c:14]([OH:15])[c:16]1[C:17](=[O:18])[O:19][CH3:20]
COC(=O)C#CC(=O)OC.COC(=O)c1ccc(Cl)cc1N
COC(=O)c1nc2cc(Cl)ccc2c(O)c1C(=O)OC
null
null
C(C)(C)(C)O
Aromatic Heterocycle Formation
OtherReaction
f5368757c96521e83619cf21dfc52b28c31825e0516659832aaa47488ac6716c
bbcf1c85e1dbdba58f5fefc8b60992ba8e370d006abd0aa7780d40fd3f3dc3a2
c1ccc2ncccc2c1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D2;+0:12]#[C;H0;D2;+0:13]-[C:14](=[O;D1;H0:15])-[#8:16]-[C;D1;H3:17]>>[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[c;H0;D3;+0:12]1:[n;H0;D2;+0:6]:[c:5](:[c:7]):[c:3](:[c:4]):[c;H0;D3;+0:1](-[OH;D1;+...
28.9
[{"value": 28.9, "product": "ClC1=CC=C2C(=C(C(=NC2=C1)C(=O)OC)C(=O)OC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 28.9, "product": "ClC1=CC=C2C(=C(C(=NC2=C1)C(=O)OC)C(=O)OC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred mixture of methyl 2-amino-4-chlorobenzoate (2.50 g, 13.5 mM) and dimethyl acetylenedicarboxylate (2.05 g, 14.4 mM) in t-butanol (22 mL) was refluxed for 7 hr under a nitrogen atmosphere. After adding additional dimethyl acetylenedicarboxylate (1.16 g, 8.13 mM) and refluxing another 2.5 hr, the reaction mixtur...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Primary amine
Ester.Ester.Aromatic alcohol
c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HO-
C(C)(C)(C)O
null
null
COC(=O)C#CC(=O)OC.COC(=O)c1ccc(Cl)cc1N>C(C)(C)(C)O>COC(=O)c1nc2cc(Cl)ccc2c(O)c1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-11cb73d43db14970822d1f7987ae94cd
Nc1cccc(Cl)c1C(=O)O.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl>>O=c1[nH]c2cccc(Cl)c2c(=O)o1
NC1=C(C(=O)O)C(=CC=C1)Cl.ClC(Cl)(Cl)OC(OC(Cl)(Cl)Cl)=O>>ClC1=CC=CC2=C1C(OC(N2)=O)=O
[NH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([Cl:9])[c:10]1[C:11](=[O:12])[OH:13].ClC(Cl)(Cl)O[C:2](OC(Cl)(Cl)Cl)=[O:1]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][c:8]([Cl:9])[c:10]2[c:11](=[O:12])[o:13]1
Nc1cccc(Cl)c1C(=O)O.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl
O=c1[nH]c2cccc(Cl)c2c(=O)o1
null
null
O1CCCC1
Aromatic Heterocycle Formation
OtherReaction
28a53b633dce43f36b75fb909640acd87a8c845fa916e16156b098b24210c80e
978aee14c5a6c161c15b14d8af7d43f564770f634ab8a62eec842fdff80e6ac1
O=c1[nH]c2ccccc2c(=O)o1
Cl-C(-Cl)(-Cl)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-O-C(-Cl)(-Cl)-Cl.[NH2;D1;+0:3]-[c:4](:[c:5]):[c:6](-[C;H0;D3;+0:7](=[O;D1;H0:8])-[OH;D1;+0:9]):[c:10]>>[O;D1;H0:8]=[c;H0;D3;+0:7]1:[o;H0;D2;+0:9]:[c;H0;D3;+0:1](=[O;D1;H0:2]):[nH;D2;+0:3]:[c:4](:[c:5]):[c:6]:1:[c:10]
250.3
[{"value": 87.0, "product": "ClC1=CC=CC2=C1C(OC(N2)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 250.3, "product": "ClC1=CC=CC2=C1C(OC(N2)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirred warm (50° C.) solution of 2-amino-6-chlorobenzoic acid (2.00 g, 11.7 mM) in tetrahydrofuran (20 mL) was added bis(trichloromethyl)carbonate (1.20 g, 4.10 mM). A vigorous gas evolution ensued along with the formation of a precipitate. The reaction mixture was allowed to cool to room temperature and the prec...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Trichloro group.Carbonic Ester.Carboxylic acid.Primary amine
null
c1ccccc1
c1nc2ccccc2co1
c1nc2ccccc2co1
HCl
O1CCCC1
null
null
Nc1cccc(Cl)c1C(=O)O.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl>O1CCCC1>O=c1[nH]c2cccc(Cl)c2c(=O)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-36369dc8420f49d692dad33fc33db94f
COC(=O)C#CC(=O)OC.COC(=O)c1c(N)cccc1Cl>>COC(=O)c1nc2cccc(Cl)c2c(O)c1C(=O)OC
NC1=C(C(=O)OC)C(=CC=C1)Cl.C(#CC(=O)OC)C(=O)OC.CC(C)([O-])C.[K+]>>ClC1=C2C(=C(C(=NC2=CC=C1)C(=O)OC)C(=O)OC)O
[CH3:1][O:2][C:3](=[O:4])[C:5]#[C:16][C:17](=[O:18])[O:19][CH3:20].CO[C:14]([c:13]1[c:7]([NH2:6])[cH:8][cH:9][cH:10][c:11]1[Cl:12])=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[n:6][c:7]2[cH:8][cH:9][cH:10][c:11]([Cl:12])[c:13]2[c:14]([OH:15])[c:16]1[C:17](=[O:18])[O:19][CH3:20]
COC(=O)C#CC(=O)OC.COC(=O)c1c(N)cccc1Cl
COC(=O)c1nc2cccc(Cl)c2c(O)c1C(=O)OC
null
null
C(C)(C)(C)O
Aromatic Heterocycle Formation
OtherReaction
f5368757c96521e83619cf21dfc52b28c31825e0516659832aaa47488ac6716c
bbcf1c85e1dbdba58f5fefc8b60992ba8e370d006abd0aa7780d40fd3f3dc3a2
c1ccc2ncccc2c1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D2;+0:12]#[C;H0;D2;+0:13]-[C:14](=[O;D1;H0:15])-[#8:16]-[C;D1;H3:17]>>[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[c;H0;D3;+0:12]1:[n;H0;D2;+0:6]:[c:5](:[c:7]):[c:3](:[c:4]):[c;H0;D3;+0:1](-[OH;D1;+...
80.4
[{"value": 80.2, "product": "ClC1=C2C(=C(C(=NC2=CC=C1)C(=O)OC)C(=O)OC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.4, "product": "ClC1=C2C(=C(C(=NC2=CC=C1)C(=O)OC)C(=O)OC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of methyl 2-amino-6-chlorobenzoate (3.00 g, 16.2 mM) and dimethyl acetylenedicarboxylate (2.64 g, 18.6 mM) in t-butanol (25 mL) was refluxed under a nitrogen atmosphere for 18 hr. The reaction mixture was cooled to room temperature and potassium t-butoxide (2.09 g, 18.6 mM) was added in one portion whereupon...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Primary amine
Ester.Ester.Aromatic alcohol
c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HO-
C(C)(C)(C)O
null
null
COC(=O)C#CC(=O)OC.COC(=O)c1c(N)cccc1Cl>C(C)(C)(C)O>COC(=O)c1nc2cccc(Cl)c2c(O)c1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-62f911c33ec34c2dbe633593e1d5ee82
CC(=O)O.O=C1Nc2cc(Cl)cc(Cl)c2C1=O>>O=c1[nH]c2cc(Cl)cc(Cl)c2c(=O)o1
ClC1=C2C(C(NC2=CC(=C1)Cl)=O)=O.C(C)(=O)O>>ClC1=CC(=CC2=C1C(OC(N2)=O)=O)Cl
CC(=O)[OH:14].[O:1]=[C:2]1[NH:3][c:4]2[cH:5][c:6]([Cl:7])[cH:8][c:9]([Cl:10])[c:11]2[C:12]1=[O:13]>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][c:6]([Cl:7])[cH:8][c:9]([Cl:10])[c:11]2[c:12](=[O:13])[o:14]1
CC(=O)O.O=C1Nc2cc(Cl)cc(Cl)c2C1=O
O=c1[nH]c2cc(Cl)cc(Cl)c2c(=O)o1
null
[O-2].[O-2].[O-2].[Cr+6].[O-2].[O-2].[O-2].[Cr+6]
C(C)(=O)OC(C)=O.O
Miscellaneous
OtherReaction
0f840b75ec018dc5052ca8f2adcc7010a68835c9436e293d8f842301d50cb013
60d059b579be791b3a253c788440e1c71f340c489355625c4d000c8e8143e816
O=c1[nH]c2ccccc2c(=O)o1
C-C(=O)-[OH;D1;+0:1].[O;D1;H0:2]=[C;H0;D3;+0:3]1-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]-1:[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:3]1:[o;H0;D2;+0:1]:[c;H0;D3;+0:4](=[O;D1;H0:5]):[nH;D2;+0:6]:[c:7](:[c:8]):[c:9]:1:[c:10]
72
[{"value": 72.0, "product": "ClC1=CC(=CC2=C1C(OC(N2)=O)=O)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a stirred solution of 4,6-dichloro-1H-indole-2,3-dione (5.00 g, 23.2 mM) in acetic acid (21 mL) and acetic anhydride (21 mL) at 80° C. was added in small portions chromium trioxide (4.12 g, 41.3 mM). The temperature of the reaction mixture was maintained between 80°-90° C. during the addition of the chromium trioxid...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ketone.Secondary amide
null
c1ccc2c(c1)CCN2
c1ccc2cocnc2c1
c1ccc2cocnc2c1
HO-
[O-2].[O-2].[O-2].[Cr+6].[O-2].[O-2].[O-2].[Cr+6].C(C)(=O)OC(C)=O.O
null
null
CC(=O)O.O=C1Nc2cc(Cl)cc(Cl)c2C1=O>[O-2].[O-2].[O-2].[Cr+6].[O-2].[O-2].[O-2].[Cr+6].C(C)(=O)OC(C)=O.O>O=c1[nH]c2cc(Cl)cc(Cl)c2c(=O)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-739ac2ee85f042ce86c3862c763ac88d
O=c1[nH]c2cc(Cl)cc(Cl)c2c(=O)o1>>COC(=O)c1c(N)cc(Cl)cc1Cl
[OH-].[Na+].ClC1=CC(=CC2=C1C(OC(N2)=O)=O)Cl>>NC1=C(C(=O)OC)C(=CC(=C1)Cl)Cl
O=[c:1]1[o:2][c:3](=[O:4])[c:5]2[c:6]([nH:7]1)[cH:8][c:9]([Cl:10])[cH:11][c:12]2[Cl:13]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([NH2:7])[cH:8][c:9]([Cl:10])[cH:11][c:12]1[Cl:13]
O=c1[nH]c2cc(Cl)cc(Cl)c2c(=O)o1
COC(=O)c1c(N)cc(Cl)cc1Cl
null
null
CO
Reduction
OtherReaction
fb3a8999d982d1c42a150fbbeb96fa0db2838a9c48a5140f183de4d3421c8ad6
9f87be38aa9793f80b3cef223629015a04ccba30a9633b313486e0a6edc9c43d
c1ccccc1
O=[c;H0;D3;+0:1]1:[nH;D2;+0:2]:[c:3](:[c:4]):[c:5](:[c:6]):[c;H0;D3;+0:7](=[O;D1;H0:8]):[o;H0;D2;+0:9]:1>>[CH3;D1;+0:1]-[O;H0;D2;+0:9]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c:5](:[c:6]):[c:3](-[NH2;D1;+0:2]):[c:4]
92.2
[{"value": 92.1, "product": "NC1=C(C(=O)OC)C(=CC(=C1)Cl)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.2, "product": "NC1=C(C(=O)OC)C(=CC(=C1)Cl)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
55
CELSIUS
2
HOUR
To a stirred solution of sodium hydroxide (0.070 g, 1.8 mM) in methanol (8.5 mL) was added 5,7-dichloro-2H-3,1-benzoxazine-2,4(1H)-dione (4.13 g, 17.8 mM). The reaction mixture was stirred at 55° C. for 2 hr, allowed to cool to room temperature and concentrated. The residue was diluted with water and the resulting mixt...
10.6084/m9.figshare.5104873.v1
null
null
Ester.Primary amine
c1ccc2cocnc2c1
c1ccccc1
c1ccccc1
Other
CO
55
2
O=c1[nH]c2cc(Cl)cc(Cl)c2c(=O)o1>CO>COC(=O)c1c(N)cc(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-80b7e4ba59954100866003a993d7b735
COC(=O)C#CC(=O)OC.COC(=O)c1c(N)cc(Cl)cc1Cl>>COC(=O)c1nc2cc(Cl)cc(Cl)c2c(O)c1C(=O)OC
NC1=C(C(=O)OC)C(=CC(=C1)Cl)Cl.C(#CC(=O)OC)C(=O)OC.CC(C)([O-])C.[K+]>>ClC1=C2C(=C(C(=NC2=CC(=C1)Cl)C(=O)OC)C(=O)OC)O
[CH3:1][O:2][C:3](=[O:4])[C:5]#[C:17][C:18](=[O:19])[O:20][CH3:21].CO[C:15]([c:14]1[c:7]([NH2:6])[cH:8][c:9]([Cl:10])[cH:11][c:12]1[Cl:13])=[O:16]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[n:6][c:7]2[cH:8][c:9]([Cl:10])[cH:11][c:12]([Cl:13])[c:14]2[c:15]([OH:16])[c:17]1[C:18](=[O:19])[O:20][CH3:21]
COC(=O)C#CC(=O)OC.COC(=O)c1c(N)cc(Cl)cc1Cl
COC(=O)c1nc2cc(Cl)cc(Cl)c2c(O)c1C(=O)OC
null
null
C(C)(C)(C)O
Aromatic Heterocycle Formation
OtherReaction
f5368757c96521e83619cf21dfc52b28c31825e0516659832aaa47488ac6716c
bbcf1c85e1dbdba58f5fefc8b60992ba8e370d006abd0aa7780d40fd3f3dc3a2
c1ccc2ncccc2c1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D2;+0:12]#[C;H0;D2;+0:13]-[C:14](=[O;D1;H0:15])-[#8:16]-[C;D1;H3:17]>>[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[c;H0;D3;+0:12]1:[n;H0;D2;+0:6]:[c:5](:[c:7]):[c:3](:[c:4]):[c;H0;D3;+0:1](-[OH;D1;+...
59
[{"value": 59.0, "product": "ClC1=C2C(=C(C(=NC2=CC(=C1)Cl)C(=O)OC)C(=O)OC)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 59.0, "product": "ClC1=C2C(=C(C(=NC2=CC(=C1)Cl)C(=O)OC)C(=O)OC)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of methyl 2-amino-4,6-dichlorobenzoate (1.30 g, 5.91 mM) and dimethyl acetylenedicarboxylate (0.96 g, 6.78 mM) in t-butanol (14 mL) was refluxed for 18 hr under a nitrogen atmosphere. The reaction mixture was cooled to room temperature and potassium t-butoxide (0.76 g, 6.8 mM) was added to the stirred mixtur...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Primary amine
Ester.Ester.Aromatic alcohol
c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HO-
C(C)(C)(C)O
null
null
COC(=O)C#CC(=O)OC.COC(=O)c1c(N)cc(Cl)cc1Cl>C(C)(C)(C)O>COC(=O)c1nc2cc(Cl)cc(Cl)c2c(O)c1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3dda300c17224ab9a94f5d53c331760a
COC(=O)C#CC(=O)OC.COC(=O)c1c(C)cccc1N>>COC(=O)c1nc2cccc(C)c2c(O)c1C(=O)OC
NC1=C(C(=O)OC)C(=CC=C1)C.C(#CC(=O)OC)C(=O)OC.CC(C)([O-])C.[K+]>>OC1=C(C(=NC2=CC=CC(=C12)C)C(=O)OC)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[C:5]#[C:16][C:17](=[O:18])[O:19][CH3:20].CO[C:14]([c:13]1[c:7]([NH2:6])[cH:8][cH:9][cH:10][c:11]1[CH3:12])=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[n:6][c:7]2[cH:8][cH:9][cH:10][c:11]([CH3:12])[c:13]2[c:14]([OH:15])[c:16]1[C:17](=[O:18])[O:19][CH3:20]
COC(=O)C#CC(=O)OC.COC(=O)c1c(C)cccc1N
COC(=O)c1nc2cccc(C)c2c(O)c1C(=O)OC
null
null
C(C)(C)(C)O
Aromatic Heterocycle Formation
OtherReaction
f5368757c96521e83619cf21dfc52b28c31825e0516659832aaa47488ac6716c
bbcf1c85e1dbdba58f5fefc8b60992ba8e370d006abd0aa7780d40fd3f3dc3a2
c1ccc2ncccc2c1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D2;+0:12]#[C;H0;D2;+0:13]-[C:14](=[O;D1;H0:15])-[#8:16]-[C;D1;H3:17]>>[C;D1;H3:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[c;H0;D3;+0:12]1:[n;H0;D2;+0:6]:[c:5](:[c:7]):[c:3](:[c:4]):[c;H0;D3;+0:1](-[OH;D1;+...
66.4
[{"value": 66.4, "product": "OC1=C(C(=NC2=CC=CC(=C12)C)C(=O)OC)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.4, "product": "OC1=C(C(=NC2=CC=CC(=C12)C)C(=O)OC)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirred mixture of methyl 2-amino-6-methylbenzoate (1.50 g, 9.08 mM) and dimethyl acetylenedicarboxylate (1.40 g, 9.82 mM) in t-butanol (20 mL) was refluxed fpr 18 hr under a nitrogen atmosphere. The reaction mixture was cooled to room temperature and potassium t-butoxide (1.10 g, 9.82 mM) was added in one portion wh...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Primary amine
Ester.Ester.Aromatic alcohol
c1ccccc1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
HO-
C(C)(C)(C)O
null
null
COC(=O)C#CC(=O)OC.COC(=O)c1c(C)cccc1N>C(C)(C)(C)O>COC(=O)c1nc2cccc(C)c2c(O)c1C(=O)OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5139598c1f4b45d2b198d2ebd6c62ba7
Cc1cc(C)cc(N)c1.NO.OC(O)C(Cl)(Cl)Cl>>Cc1cc(C)cc(NC(=O)C=NO)c1
ClC(C(O)O)(Cl)Cl.S(=O)(=O)([O-])[O-].[Na+].[Na+].CC=1C=C(N)C=C(C1)C.Cl.Cl.NO>>CC=1C=C(C=C(C1)C)NC(C=NO)=O
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[cH:6][c:7]([NH2:8])[cH:14]1.[NH2:12][OH:13].O[CH:11]([C:9](Cl)(Cl)Cl)[OH:10]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[cH:6][c:7]([NH:8][C:9](=[O:10])[CH:11]=[N:12][OH:13])[cH:14]1
Cc1cc(C)cc(N)c1.NO.OC(O)C(Cl)(Cl)Cl
Cc1cc(C)cc(NC(=O)C=NO)c1
null
null
O
Acylation
OtherReaction
945b0c41a86c791948d53e53b6060216294cdbc727563e10d955fcd0adda1c96
ed66e3eedfeda41282995a3fcf8794b82675627b3c0201c4e47ec301ec6a89a1
c1ccccc1
Cl-[C;H0;D4;+0:1](-Cl)(-Cl)-[CH;D3;+0:2](-O)-[OH;D1;+0:3].[NH2;D1;+0:4]-[O;D1;H1:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H1:5]-[N;H0;D2;+0:4]=[CH;D2;+0:2]-[C;H0;D3;+0:1](=[O;H0;D1;+0:3])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
95
[{"value": 95.0, "product": "CC=1C=C(C=C(C1)C)NC(C=NO)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To a solution of chloral hydrate (14.1 g, 85.24 mM) and sodium sulfate (88.2g, 7.53 eq.) in 270 mL of water was added a solution of 3,5-dimethylaniline in a solution of concentrated HCl (16 mL) and water (51 mL), whereupon an off-white precipitate formed. The mixture was stirred for 10 min prior to adding an aqueous so...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Secondary alcohol.Secondary alcohol.Primary amine.Primary amine
Secondary amide.Oxime
null
null
c1ccccc1
HCl
O
null
0.166667
Cc1cc(C)cc(N)c1.NO.OC(O)C(Cl)(Cl)Cl>O>Cc1cc(C)cc(NC(=O)C=NO)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d8484403e58847a9996f4809780dd83c
Cc1cc(C)cc(NC(=O)C=NO)c1>>Cc1cc(C)c2c(c1)NC(=O)C2=O
OS(=O)(=O)O.CC=1C=C(C=C(C1)C)NC(C=NO)=O>>CC1=C2C(C(NC2=CC(=C1)C)=O)=O
N(=[CH:12][C:10]([NH:9][c:7]1[cH:6][c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:8]1)=[O:11])[OH:13]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]2[c:7]([cH:8]1)[NH:9][C:10](=[O:11])[C:12]2=[O:13]
Cc1cc(C)cc(NC(=O)C=NO)c1
Cc1cc(C)c2c(c1)NC(=O)C2=O
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
03e26bd863db1451489ee0f1368908e688e08d7fcfd1b579498bc95cc4edfd9e
ab4bf08516e66cf6fd8670ac9e8d4ecd074b35f40b66b51c2d0c9c0d98ab1c51
O=C1Nc2ccccc2C1=O
[C;D1;H3:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5](-[#7:6]-[C:7](=[O;D1;H0:8])-[CH;D2;+0:9]=N-[OH;D1;+0:10]):[c:11]>>[C;D1;H3:1]-[c:2](:[c:3]):[c;H0;D3;+0:4]1:[c:5](:[c:11])-[#7:6]-[C:7](=[O;D1;H0:8])-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]
72.6
[{"value": 72.6, "product": "CC1=C2C(C(NC2=CC(=C1)C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
To a stirred warm (60°-70° C.) solution of concentrated H2SO4 (60 mL) and water (6 mL) was added in small portions N-(3,5-dimethylphenyl)-2-(hydroxyimino)acetamide (15.0 g, 78 mM) so that the temperature of the reaction mixture did not exceed 70° C. After the addition was completed, the reaction mixture was heated at 8...
10.6084/m9.figshare.5104873.v1
null
Oxime
Ketone
c1ccccc1
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
Other
O
80
null
Cc1cc(C)cc(NC(=O)C=NO)c1>O>Cc1cc(C)c2c(c1)NC(=O)C2=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ed246c15161e44ccb5ed8c113f70f2e4
Cc1cc(C)c2c(c1)NC(=O)C2=O.O>>Cc1cc(C)c2c(=O)oc(=O)[nH]c2c1
CC1=C2C(C(NC2=CC(=C1)C)=O)=O.O>>CC1=CC(=CC2=C1C(OC(N2)=O)=O)C
[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]2[c:13]([cH:14]1)[NH:12][C:10](=[O:11])[C:7]2=[O:8].[OH2:9]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]2[c:7](=[O:8])[o:9][c:10](=[O:11])[nH:12][c:13]2[cH:14]1
Cc1cc(C)c2c(c1)NC(=O)C2=O.O
Cc1cc(C)c2c(=O)oc(=O)[nH]c2c1
null
[O-2].[O-2].[O-2].[Cr+6]
C(C)(=O)O
Miscellaneous
OtherReaction
5d9736fd05de108b71c591acfae61cb6af4635bfbe20446a56c7b74a3d5953af
8242b1e5e71ebd9e44538af93284e3a1145dd4183387fabf58d37d4a04b884a5
O=c1[nH]c2ccccc2c(=O)o1
[O;D1;H0:1]=[C;H0;D3;+0:2]1-[NH;D2;+0:3]-[c:4](:[c:5]):[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;D1;H0:9].[OH2;D0;+0:10]>>[O;D1;H0:1]=[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c:4](:[c:5]):[c:6](:[c:7]):[c;H0;D3;+0:8](=[O;D1;H0:9]):[o;H0;D2;+0:10]:1
31
[{"value": 31.0, "product": "CC1=CC(=CC2=C1C(OC(N2)=O)=O)C", "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
To a stirred warm (60° C.) solution of 4,6-dimethyl-1H-indole-2,3-dione (2.0 g, 11.4 mM) in acetic acid (20 mL) was added in small portions chromium trioxide (6.6 g, 66 mM) while maintaining the temperature of the reaction mixture at 65°-70° C. The reaction mixture was then heated at 80° C. for one hour, cooled, poured...
10.6084/m9.figshare.5104873.v1
null
Ketone.Secondary amide
null
c1ccc2c(c1)CCN2
c1ccc2cocnc2c1
c1ccc2cocnc2c1
null
[O-2].[O-2].[O-2].[Cr+6].C(C)(=O)O
80
null
Cc1cc(C)c2c(c1)NC(=O)C2=O.O>[O-2].[O-2].[O-2].[Cr+6].C(C)(=O)O>Cc1cc(C)c2c(=O)oc(=O)[nH]c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1a81f6348ff444b79db47e60e3184959
Cc1cc(C)c2c(=O)oc(=O)[nH]c2c1>>COC(=O)c1c(C)cc(C)cc1N
[OH-].[Na+].CC1=CC(=CC2=C1C(OC(N2)=O)=O)C>>NC1=C(C(=O)OC)C(=CC(=C1)C)C
O=[c:1]1[o:2][c:3](=[O:4])[c:5]2[c:6]([CH3:7])[cH:8][c:9]([CH3:10])[cH:11][c:12]2[nH:13]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([CH3:7])[cH:8][c:9]([CH3:10])[cH:11][c:12]1[NH2:13]
Cc1cc(C)c2c(=O)oc(=O)[nH]c2c1
COC(=O)c1c(C)cc(C)cc1N
null
null
CO
Reduction
OtherReaction
fb3a8999d982d1c42a150fbbeb96fa0db2838a9c48a5140f183de4d3421c8ad6
9f87be38aa9793f80b3cef223629015a04ccba30a9633b313486e0a6edc9c43d
c1ccccc1
O=[c;H0;D3;+0:1]1:[nH;D2;+0:2]:[c:3](:[c:4]):[c:5](:[c:6]):[c;H0;D3;+0:7](=[O;D1;H0:8]):[o;H0;D2;+0:9]:1>>[CH3;D1;+0:1]-[O;H0;D2;+0:9]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c:5](:[c:6]):[c:3](-[NH2;D1;+0:2]):[c:4]
86
[{"value": 86.0, "product": "NC1=C(C(=O)OC)C(=CC(=C1)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.0, "product": "NC1=C(C(=O)OC)C(=CC(=C1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a stirred solution of sodium hydroxide (0.013 g, 0.33 mM) in methanol (1.7 mL) was added 5,7-dimethyl-2H-3,1-benzoxazine-2,4(1H)-dione (0.67 g, 3.5 mM). The mixture was heated to 60° C. and maintained at that temperature for 45 min during which vigorous gas evolution ensued and all solids dissolved completely. The s...
10.6084/m9.figshare.5104873.v1
null
null
Ester.Primary amine
c1ccc2cocnc2c1
c1ccccc1
c1ccccc1
Other
CO
60
null
Cc1cc(C)c2c(=O)oc(=O)[nH]c2c1>CO>COC(=O)c1c(C)cc(C)cc1N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-25ba7dfa0f824982b8c2a5e57de886c1
CC(=O)O.COc1ccc(C#N)c([N+](=O)[O-])c1.O=S(=O)(O)O>>COc1ccc(C(=O)O)c([N+](=O)[O-])c1
[N+](=O)([O-])C1=C(C#N)C=CC(=C1)OC.C(C)(=O)O.S(O)(O)(=O)=O>>[N+](=O)([O-])C1=C(C(=O)O)C=CC(=C1)OC
CC(O)=[O:8].N#[C:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:14][c:10]1[N+:11](=[O:12])[O-:13].O=S(=O)(O)[OH:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[OH:9])[c:10]([N+:11](=[O:12])[O-:13])[cH:14]1
CC(=O)O.COc1ccc(C#N)c([N+](=O)[O-])c1.O=S(=O)(O)O
COc1ccc(C(=O)O)c([N+](=O)[O-])c1
null
null
O
Acylation
OtherReaction
f768caf13c17ba0cc87c566c3e05dbc3f4c74e5e896689cebac8385f7f67f9cd
1db0fabeaac9f8265574309fafb4f2e7a5658521945038cfd32008ac3c3325d4
c1ccccc1
C-C(-O)=[O;H0;D1;+0:1].N#[C;H0;D2;+0:2]-[c:3](:[c:4]):[c:5].O-S(=O)(=O)-[OH;D1;+0:6]>>[O;H0;D1;+0:1]=[C;H0;D3;+0:2](-[OH;D1;+0:6])-[c:3](:[c:4]):[c:5]
91.8
[{"value": 91.8, "product": "[N+](=O)([O-])C1=C(C(=O)O)C=CC(=C1)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-nitro-4-methoxybenzonitrile (14.0 g, 78.6 mM) in a solution of acetic acid (28 mL), sulfuric acid (28 mL) and water (28 mL) was refluxed for 11 hr, allowed to cool and diluted with water (200 mL). The resulting precipitate which formed was collected, washed with water and dried to give the title benzoic ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Nitrile
Carboxylic acid
null
null
c1ccccc1
HO-
O
null
null
CC(=O)O.COc1ccc(C#N)c([N+](=O)[O-])c1.O=S(=O)(O)O>O>COc1ccc(C(=O)O)c([N+](=O)[O-])c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-49d860bfec704ababf3ed788e3799c62
COc1cccc([N+](=O)[O-])c1C(=O)O>>COc1cccc(N)c1C(=O)O
COC1=CC=CC(=C1C(=O)O)[N+](=O)[O-]>>NC1=C(C(=O)O)C(=CC=C1)OC
O=[N+:8]([O-])[c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:9]1[C:10](=[O:11])[OH:12]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[c:9]1[C:10](=[O:11])[OH:12]
COc1cccc([N+](=O)[O-])c1C(=O)O
COc1cccc(N)c1C(=O)O
null
[Pd]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]
100.2
[{"value": 100.0, "product": "NC1=C(C(=O)O)C(=CC=C1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.2, "product": "NC1=C(C(=O)O)C(=CC=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 6-methoxy-2-nitrobenzoic acid (3.25 g, 16.5 mM) in ethanol (180 mL) containing 10% palladium-on-carbon catalyst (0.30g) was hydrogenated using a Parr apparatus. When hydrogen consumption ceased, the resulting mixture was filtered through diatomaceous earth and the filtrate concentrated to provide the titl...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pd].C(C)O
null
null
COc1cccc([N+](=O)[O-])c1C(=O)O>[Pd].C(C)O>COc1cccc(N)c1C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-566fc546dbbd4317ba914612b55bdb28
COc1cccc(N)c1C(=O)O.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl>>COc1cccc2[nH]c(=O)oc(=O)c12
NC1=C(C(=O)O)C(=CC=C1)OC.ClC(Cl)(Cl)OC(OC(Cl)(Cl)Cl)=O>>COC1=CC=CC2=C1C(OC(N2)=O)=O
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[c:14]1[C:12]([OH:11])=[O:13].ClC(Cl)(Cl)O[C:9](OC(Cl)(Cl)Cl)=[O:10]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[nH:8][c:9](=[O:10])[o:11][c:12](=[O:13])[c:14]12
COc1cccc(N)c1C(=O)O.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl
COc1cccc2[nH]c(=O)oc(=O)c12
null
null
O1CCCC1
Aromatic Heterocycle Formation
OtherReaction
28a53b633dce43f36b75fb909640acd87a8c845fa916e16156b098b24210c80e
978aee14c5a6c161c15b14d8af7d43f564770f634ab8a62eec842fdff80e6ac1
O=c1[nH]c2ccccc2c(=O)o1
Cl-C(-Cl)(-Cl)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-O-C(-Cl)(-Cl)-Cl.[NH2;D1;+0:3]-[c:4](:[c:5]):[c:6](-[C;H0;D3;+0:7](=[O;D1;H0:8])-[OH;D1;+0:9]):[c:10]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:3]:[c:4](:[c:5]):[c:6](:[c:10]):[c;H0;D3;+0:7](=[O;D1;H0:8]):[o;H0;D2;+0:9]:1
283.3
[{"value": 94.6, "product": "COC1=CC=CC2=C1C(OC(N2)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 283.3, "product": "COC1=CC=CC2=C1C(OC(N2)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
30
MINUTE
To a stirred warm (50° C.) solution of 2-amino-6-methoxybenzoic acid (2.70 g, 16.2 mM) in tetrahydrofuran (25 mL) under a nitrogen atmosphere was added bis(trichloromethyl)carbonate (1.60 g, 5.38 mM), whereupon a tan precipitate formed. The reaction mixture was maintained at 50° C. for 30 min, cooled, rewarmed to 50° C...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Trichloro group.Carbonic Ester.Carboxylic acid.Primary amine
null
c1ccccc1
c1nc2ccccc2co1
c1nc2ccccc2co1
HCl
O1CCCC1
50
0.5
COc1cccc(N)c1C(=O)O.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl>O1CCCC1>COc1cccc2[nH]c(=O)oc(=O)c12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6710997eb6b640a184d2ce252b03ace7
COc1cccc2[nH]c(=O)oc(=O)c12>>COC(=O)c1c(N)cccc1OC
O.[OH-].[Na+].COC1=CC=CC2=C1C(OC(N2)=O)=O>>NC1=C(C(=O)OC)C(=CC=C1)OC
O=[c:1]1[o:2][c:3](=[O:4])[c:5]2[c:6]([nH:7]1)[cH:8][cH:9][cH:10][c:11]2[O:12][CH3:13]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([NH2:7])[cH:8][cH:9][cH:10][c:11]1[O:12][CH3:13]
COc1cccc2[nH]c(=O)oc(=O)c12
COC(=O)c1c(N)cccc1OC
null
null
CO
Reduction
OtherReaction
4a877ce7f9d8b0e05ec6ae8c859c09c08e7f1fd55a56b7ca38718591b6593140
9f87be38aa9793f80b3cef223629015a04ccba30a9633b313486e0a6edc9c43d
c1ccccc1
O=[c;H0;D3;+0:1]1:[nH;D2;+0:2]:[c:3](:[c:4]):[c:5](:[c:6]):[c;H0;D3;+0:7](=[O;D1;H0:8]):[o;H0;D2;+0:9]:1>>[CH3;D1;+0:1]-[O;H0;D2;+0:9]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c:5](:[c:6]):[c:3](-[NH2;D1;+0:2]):[c:4]
94
[{"value": 94.0, "product": "NC1=C(C(=O)OC)C(=CC=C1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.7, "product": "NC1=C(C(=O)OC)C(=CC=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
14.5
HOUR
To a stirred solution of sodium hydroxide (0.06 g, 1.5 mM) in methanol (7 mL) under a nitrogen atmosphere was added 5-methoxy-2H-3,1-benzoxazine-2,4(1H)-dione (2.90 g, 15.0 mM). The reaction mixture was stirred at 65° C. for 14.5 hr, cooled to room temperature and poured into water. The resulting solution was extracted...
10.6084/m9.figshare.5104873.v1
null
null
Ester.Primary amine
c1nc2ccccc2co1
c1ccccc1
c1ccccc1
Other
CO
65
14.5
COc1cccc2[nH]c(=O)oc(=O)c12>CO>COC(=O)c1c(N)cccc1OC