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
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14
3.37k
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1
581
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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-c3a75813d0b24864aa4f7cd526efd6aa
ord-7d96e6d24ff1482d847701b6c8e3136c
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC>>C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N
CCO[C:16]([CH2:15][CH:14]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]21)=[O:17].[NH2:18][C:19]([NH2:20])=[NH2+:21]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH:14]1[CH2:15][C:16](=[O:17])[NH:18][C:19](=[NH:20])[NH2:21]
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
null
null
null
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
57.3
[{"value": 57.3, "product": "C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
24
HOUR
N-[(2-Isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 5 g of potassium tert-butoxide, 5.2 g of guanidinium chloride and 2.5 g of ethyl (2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol1-yl)acetate. The reaction mixture is stirred at a temperature in the region o...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
null
20
24
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-af40e167416b4c3fa5b7ec94e55ef1e1
CC(C)CN1C(=O)c2ccccc2C1O.CCOCC>>CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C
O.C(C)OCC.[H-].[Na+].OC1N(C(C2=CC=CC=C12)=O)CC(C)C>>C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC
[OH:5][CH:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[N:16]1[CH2:17][CH:18]([CH3:19])[CH3:20].[CH3:1][CH2:2][O:3][CH2:4][CH3:6]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[N:16]1[CH2:17][CH:18]([CH3:19])[CH3:20]
CC(C)CN1C(=O)c2ccccc2C1O.CCOCC
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C
null
null
COCCOC
Heteroatom Alkylation and Arylation
OtherReaction
48a0bd460ac260e177ffa262698d9e6ae802769dd91076aaf638df24b5a534e1
79b1dc52d3be254effebd4b18222e0510623f9682e37c200296c41f37c9f0926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9].[C:10]-[#8:11]-[CH2;D2;+0:12]-[CH3;D1;+0:13]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[CH2;D2;+0:13]-[C;H0;D3;+0:12](=[O;H0;D1;+0:9])-[#8:11]-[C:10]
null
[]
0
CELSIUS
null
null
7.7 cm3 of triethyl phosphonoacetate are added dropwise, while keeping the temperature below 10° C., to a suspension of 1.6 g of 60% sodium hydride in 60 cm3 of 1,2-dimethoxyethane under an inert atmosphere and cooled to 0° C., with stirring. The reaction mixture is allowed to warm to a temperature in the region of 20°...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol
Ester
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
COCCOC
0
null
CC(C)CN1C(=O)c2ccccc2C1O.CCOCC>COCCOC>CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7e460edd1088419d97082403be921997
CC(C)CN1C(=O)c2ccccc2C1=O>>CC(C)CN1C(=O)c2ccccc2C1O
C(C(C)C)N1C(C=2C(C1=O)=CC=CC2)=O.O>>OC1N(C(C2=CC=CC=C12)=O)CC(C)C
[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH:14]1[OH:15]
CC(C)CN1C(=O)c2ccccc2C1=O
CC(C)CN1C(=O)c2ccccc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
88.4
[{"value": 88.4, "product": "OC1N(C(C2=CC=CC=C12)=O)CC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
3-Hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 6.5 g of N-isobutylphthalimide in 60 cm3 of methanol and 1.7 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 20 hours and is then cooled to a temperature in the re...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
20
CC(C)CN1C(=O)c2ccccc2C1=O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2ccccc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-597f172c828f4bd1b22ce94f8d6514bb
CC(C)CN.O=C1OC(=O)c2ccccc21>>CC(C)CN1C(=O)c2ccccc2C1=O
C(C(C)C)N.C1(C=2C(C(=O)O1)=CC=CC2)=O>>C(C(C)C)N1C(C=2C(C1=O)=CC=CC2)=O
[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5].O1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14]1=[O:15]
CC(C)CN.O=C1OC(=O)c2ccccc21
CC(C)CN1C(=O)c2ccccc2C1=O
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
60
CELSIUS
2
HOUR
A solution of 3.2 cm3 of isobutylamine in 3 cm3 of toluene is added to a suspension of 5.2 g of phthalic anhydride in 50 cm3 of toluene, with stirring. The reaction mixture is heated at a temperature in the region of 60° C. for 1 hour, and then at a temperature in the region of 100° C. for 2 hours. Dean-Stark apparatus...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
60
2
CC(C)CN.O=C1OC(=O)c2ccccc21>C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2ccccc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b257c35695494c6886e15c8930a34970
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC>>C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N
CCO[C:16]([CH2:15][CH:14]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]21)=[O:17].[NH2:18][C:19]([NH2:20])=[NH2+:21]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH:14]1[CH2:15][C:16](=[O:17])[NH:18][C:19](=[NH:20])[NH2:21]
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
null
null
null
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
57.3
[{"value": 57.3, "product": "C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
40
HOUR
(−)-N-[(2-Isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-y)acetyl]guanidine is prepared as described in Example 1, starting with 2.6 g of potassium tert-butoxide, 2.6 g of guanidinium chloride and 1.25 g of ethyl (−)-(2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol1-y)acetate. The reaction mixture is stirred at a temperature in the...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
null
20
40
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a066f5e8073d4560a443fc206aa48bfe
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC>>C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N
CCO[C:16]([CH2:15][CH:14]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]21)=[O:17].[NH2:18][C:19]([NH2:20])=[NH2+:21]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH:14]1[CH2:15][C:16](=[O:17])[NH:18][C:19](=[NH:20])[NH2:21]
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
null
null
null
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
53.5
[{"value": 53.5, "product": "C(C(C)C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
40
HOUR
(+)-N-[(2-Isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 2.0 g of potassium tert-butoxide, 2.1 g of guanidinium chloride and 1.0 g of ethyl (+)-(2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol1-y)acetate. The reaction mixture is stirred at a temperature in the...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
null
20
40
CCOC(=O)CC1c2ccccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b2dd0a2274da4fd9a4bbd7aca7dd0685
CCCN1C(=O)c2ccccc2C1CC(=O)OCC.NC(N)=[NH2+]>>CCCN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.O=C1N(C(C2=CC=CC=C12)CC(=O)OCC)CCC>>O=C1N(C(C2=CC=CC=C12)CC(=O)NC(=N)N)CCC
CCO[C:15]([CH2:14][CH:13]1[N:4]([CH2:3][CH2:2][CH3:1])[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]21)=[O:16].[NH2+:17]=[C:18]([NH2:19])[NH2:20]>>[CH3:1][CH2:2][CH2:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[CH:13]1[CH2:14][C:15](=[O:16])[NH:17][C:18](=[NH:19])[NH2:20]
CCCN1C(=O)c2ccccc2C1CC(=O)OCC.NC(N)=[NH2+]
CCCN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
null
null
O
Acylation
OtherReaction
09bfb108fb5b69552e7dcf8792cd0918114fd6e590129b579cec1dd12722db62
e35fd5a84c281db4b9a756e738b7d6904fa44bd3c94329564f747de651850e99
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[N;D1;H2:6]-[C;H0;D3;+0:7](=[NH2+;D1:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[N;D1;H2:6])=[NH;D1;+0:9]
31.8
[{"value": 31.8, "product": "O=C1N(C(C2=CC=CC=C12)CC(=O)NC(=N)N)CCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
1
HOUR
N-[(3-Oxo-2-propyl-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 3.9 g of potassium tert-butoxide, 3.3 g of guanidinium chloride and 1.8 g of ethyl (3-oxo-2-propyl-2,3-dihydro-1H-isoindol1-yl)acetate. The reaction mixture is stirred at a temperature in the region of ...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide
null
null
c1ccc2c(c1)C[NH]C2
HO-
O
20
1
CCCN1C(=O)c2ccccc2C1CC(=O)OCC.NC(N)=[NH2+]>O>CCCN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b899b9d8d8054722b2f738da334d7782
CCCN1C(=O)c2ccccc2C1=O>>CCCN1C(=O)c2ccccc2C1O
C(CC)N1C(C=2C(C1=O)=CC=CC2)=O>>OC1N(C(C2=CC=CC=C12)=O)CCC
[CH3:1][CH2:2][CH2:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14]>>[CH3:1][CH2:2][CH2:3][N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[CH:13]1[OH:14]
CCCN1C(=O)c2ccccc2C1=O
CCCN1C(=O)c2ccccc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
66
[{"value": 66.0, "product": "OC1N(C(C2=CC=CC=C12)=O)CCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
3-Hydroxy-2-propyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 1.5 g of N-propylphthalimide in 25 cm3 of methanol and 0.48 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 20 hours and is then cooled to a temperature in the regio...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
20
CCCN1C(=O)c2ccccc2C1=O>[BH4-].[K+].CO>CCCN1C(=O)c2ccccc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3070f13bd72545d38a8514b0b4057615
CCOC(=O)CC1c2ccccc2C(=O)N1CC.NC(N)=[NH2+]>>CCN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.C(C)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC>>C(C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N
CCO[C:14]([CH2:13][CH:12]1[N:3]([CH2:2][CH3:1])[C:4](=[O:5])[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]21)=[O:15].[NH2:16][C:17]([NH2:18])=[NH2+:19]>>[CH3:1][CH2:2][N:3]1[C:4](=[O:5])[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[CH:12]1[CH2:13][C:14](=[O:15])[NH:16][C:17](=[NH:18])[NH2:19]
CCOC(=O)CC1c2ccccc2C(=O)N1CC.NC(N)=[NH2+]
CCN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
null
null
O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
28
[{"value": 28.0, "product": "C(C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
N-[(2-Ethyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 4.3 g of potassium tert-butoxide, 3.7 g of guanidinium chloride and 1.9 g of ethyl (2-ethyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate. The reaction mixture is stirred at a temperature in the region of 2...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
O
20
20
CCOC(=O)CC1c2ccccc2C(=O)N1CC.NC(N)=[NH2+]>O>CCN1C(=O)c2ccccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a3a35763247f4b86877e29784c87ad69
CCN1C(=O)c2ccccc2C1=O>>CCN1C(=O)c2ccccc2C1O
C(C)N1C(C=2C(C1=O)=CC=CC2)=O>>OC1N(C(C2=CC=CC=C12)=O)CC
[CH3:1][CH2:2][N:3]1[C:4](=[O:5])[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[C:12]1=[O:13]>>[CH3:1][CH2:2][N:3]1[C:4](=[O:5])[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[CH:12]1[OH:13]
CCN1C(=O)c2ccccc2C1=O
CCN1C(=O)c2ccccc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
47
[{"value": 47.0, "product": "OC1N(C(C2=CC=CC=C12)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
3-Hydroxy-2-ethyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 4.0 g of N-ethylphthalimide in 20 cm3 of methanol and 1.2 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 20 hours and is then cooled to a temperature in the region o...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
20
CCN1C(=O)c2ccccc2C1=O>[BH4-].[K+].CO>CCN1C(=O)c2ccccc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fac0dd76dbd746cfa2286832699cea98
CCOC(=O)CC1c2ccccc2C(=O)N1C(C)C.NC(N)=[NH2+]>>CC(C)N1C(=O)c2ccccc2C1CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.C(C)(C)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC>>C(C)(C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N
CCO[C:15]([CH2:14][CH:13]1[N:4]([CH:2]([CH3:1])[CH3:3])[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]21)=[O:16].[NH2:17][C:18]([NH2:19])=[NH2+:20]>>[CH3:1][CH:2]([CH3:3])[N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[CH:13]1[CH2:14][C:15](=[O:16])[NH:17][C:18](=[NH:19])[NH2:20]
CCOC(=O)CC1c2ccccc2C(=O)N1C(C)C.NC(N)=[NH2+]
CC(C)N1C(=O)c2ccccc2C1CC(=O)NC(=N)N
null
null
O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
6.8
[{"value": 6.8, "product": "C(C)(C)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
N-[(2-Isopropyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 1.5 g of potassium tert-butoxide, 1.3 g of guanidinium chloride and 0.7 g of ethyl (2-isopropyl-3-oxo-2,3-dihydro-1H-isoindol1-yl)acetate. The reaction mixture is stirred at a temperature in the regi...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
O
20
20
CCOC(=O)CC1c2ccccc2C(=O)N1C(C)C.NC(N)=[NH2+]>O>CC(C)N1C(=O)c2ccccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2d56f0d53d9b445baa087d3657ed62bc
CC(C)N1C(=O)c2ccccc2C1=O>>CC(C)N1C(=O)c2ccccc2C1O
C(C)(C)N1C(C=2C(C1=O)=CC=CC2)=O>>OC1N(C(C2=CC=CC=C12)=O)C(C)C
[CH3:1][CH:2]([CH3:3])[N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]1=[O:14]>>[CH3:1][CH:2]([CH3:3])[N:4]1[C:5](=[O:6])[c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[CH:13]1[OH:14]
CC(C)N1C(=O)c2ccccc2C1=O
CC(C)N1C(=O)c2ccccc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
150.9
[{"value": 150.9, "product": "OC1N(C(C2=CC=CC=C12)=O)C(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
3-Hydroxy-2-isopropyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 4.0 g of N-isopropylphthalimide in 20 cm3 of methanol and 1.1 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 20 hours and is then cooled to a temperature in the ...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
20
CC(C)N1C(=O)c2ccccc2C1=O>[BH4-].[K+].CO>CC(C)N1C(=O)c2ccccc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ecd23f1631294a80b9563074134158aa
O=C1c2ccccc2C(=O)N1CC1CC1>>O=C1c2ccccc2C(O)N1CC1CC1
C1(CC1)CN1C(C=2C(C1=O)=CC=CC2)=O>>OC1N(C(C2=CC=CC=C12)=O)CC1CC1
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH:13]1[CH2:14][CH2:15]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH:9]([OH:10])[N:11]1[CH2:12][CH:13]1[CH2:14][CH2:15]1
O=C1c2ccccc2C(=O)N1CC1CC1
O=C1c2ccccc2C(O)N1CC1CC1
null
null
ClCCl.[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1c2ccccc2CN1CC1CC1
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
94.4
[{"value": 94.4, "product": "OC1N(C(C2=CC=CC=C12)=O)CC1CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
3-Hydroxy-2-cyclopropylmethyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 4.3 g of N-cyclopropylmethylphthalimide in 40 cm3 of methanol and 1.2 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 20 hours and is then cooled to a tem...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.C1CC1
null
ClCCl.[BH4-].[K+].CO
20
20
O=C1c2ccccc2C(=O)N1CC1CC1>ClCCl.[BH4-].[K+].CO>O=C1c2ccccc2C(O)N1CC1CC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f97ef69472944c5491d3545fbca46f8e
NCC1CC1.O=C1OC(=O)c2ccccc21>>O=C1c2ccccc2C(=O)N1CC1CC1
C1(C=2C(C(=O)O1)=CC=CC2)=O.C1(CC1)CN.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C1(CC1)CN1C(C=2C(C1=O)=CC=CC2)=O
[NH2:11][CH2:12][CH:13]1[CH2:14][CH2:15]1.O1[C:2](=[O:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]1=[O:10]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH:13]1[CH2:14][CH2:15]1
NCC1CC1.O=C1OC(=O)c2ccccc21
O=C1c2ccccc2C(=O)N1CC1CC1
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1c2ccccc2C(=O)N1CC1CC1
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10](:[c:11])-[C;H0;D3;+0:5]-1=[O;D1;H0:4]
null
[]
140
CELSIUS
16
HOUR
N-Cyclopropylmethylphthalimide is prepared as described in Example 2, starting with 4 g of phthalic anhydride, 2.3 cm3 of cyclopropylmethylamine and a catalytic amount of para-toluenesulfonic acid in 40 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for 2 hours and is then cool...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.C1CC1
HO-
C1(=CC=CC=C1)C
140
16
NCC1CC1.O=C1OC(=O)c2ccccc21>C1(=CC=CC=C1)C>O=C1c2ccccc2C(=O)N1CC1CC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d79df0c8d25f43ae84c3534062ef46a2
CCOC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1.NC(N)=[NH2+]>>N=C(N)NC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1
[Na].[Na].C(C1=CC=CC=C1)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC.[Cl-].NC(=[NH2+])N>>C(C1=CC=CC=C1)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N
CCO[C:5](=[O:6])[CH2:7][CH:8]1[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15](=[O:16])[N:17]1[CH2:18][c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1.[NH2:1][C:2]([NH2:3])=[NH2+:4]>>[NH:1]=[C:2]([NH2:3])[NH:4][C:5](=[O:6])[CH2:7][CH:8]1[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15](=[O:16])[N:17]1[CH2:18][c:19]1[cH:20][cH:...
CCOC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1.NC(N)=[NH2+]
N=C(N)NC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1
null
null
C(C)O
Acylation
OtherReaction
09bfb108fb5b69552e7dcf8792cd0918114fd6e590129b579cec1dd12722db62
e35fd5a84c281db4b9a756e738b7d6904fa44bd3c94329564f747de651850e99
O=C1c2ccccc2CN1Cc1ccccc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[N;D1;H2:6]-[C;H0;D3;+0:7](=[NH2+;D1:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[N;D1;H2:6])=[NH;D1;+0:9]
57.6
[{"value": 57.6, "product": "C(C1=CC=CC=C1)N1C(C2=CC=CC=C2C1=O)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
1
HOUR
0.22 g of sodium is added to 20 cm3 of absolute ethanol under an inert atmosphere. After the sodium has totally disappeared, 0.94 g of guanidinium chloride is added. The reaction mixture is stirred under an inert atmosphere at a temperature in the region of 20° C. for 1 hour, followed by addition of a solution of 2 g o...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide
null
null
c1ccc2c(c1)C[NH]C2.c1ccccc1
HO-
C(C)O
20
1
CCOC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1.NC(N)=[NH2+]>C(C)O>N=C(N)NC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-19c73cd70ac34a0cabf6a0b849c0f8e7
CCOC(C)=O.O=C1c2ccccc2C(O)N1Cc1ccccc1>>CCOC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1
C(C)(=O)OCC.[H-].[Na+].OC1N(C(C2=CC=CC=C12)=O)CC1=CC=CC=C1.O>>C(C1=CC=CC=C1)N1C(C2=CC=CC=C2C1=O)CC(=O)OCC
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH3:6].O[CH:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[N:16]1[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH:7]1[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14](=[O:15])[N:16]1[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23...
CCOC(C)=O.O=C1c2ccccc2C(O)N1Cc1ccccc1
CCOC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1
null
null
COCCOC
C-C Coupling
OtherReaction
f15997e17baabc84ad1f24d90439ac1e1bf9c091e3c8b61c6d23db78bb59ba96
ec740fdba0adc3c659d56447beb3ee7a35d222db2ebbeacae7f761e1e85567b3
O=C1c2ccccc2CN1Cc1ccccc1
O-[CH;D3;+0:1]1-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[c:6]:[c:7]-1:[c:8].[C:9]-[#8:10]-[C:11](-[CH3;D1;+0:12])=[O;D1;H0:13]>>[C:3]-[#7:2]1-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](:[c:8])-[CH;D3;+0:1]-1-[CH2;D2;+0:12]-[C:11](=[O;D1;H0:13])-[#8:10]-[C:9]
null
[]
20
CELSIUS
null
null
Ethyl (2-benzyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate is prepared as described in Example 2, starting with 3.2 9 of 60% sodium hydride in 200 cm3 of 1,2-dimethoxyethane, 16.4 cm3 of triethyl phosphonoacetate and 9.5 g of 3-hydroxy-2benzyl-2,3-dihydroisoindol-1-one. The mixture is refluxed for 18 hours and is then ...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol
Ester
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccccc1
HO-
COCCOC
20
null
CCOC(C)=O.O=C1c2ccccc2C(O)N1Cc1ccccc1>COCCOC>CCOC(=O)CC1c2ccccc2C(=O)N1Cc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-54e689850d1440c6b6611a0b94b7c5ed
O=C1c2ccccc2C(=O)N1Cc1ccccc1>>O=C1c2ccccc2C(O)N1Cc1ccccc1
C(C1=CC=CC=C1)N1C(C=2C(C1=O)=CC=CC2)=O.O>>OC1N(C(C2=CC=CC=C12)=O)CC1=CC=CC=C1
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH:9]([OH:10])[N:11]1[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
O=C1c2ccccc2C(=O)N1Cc1ccccc1
O=C1c2ccccc2C(O)N1Cc1ccccc1
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1c2ccccc2CN1Cc1ccccc1
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
92.4
[{"value": 92.4, "product": "OC1N(C(C2=CC=CC=C12)=O)CC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
3-Hydroxy-2-benzyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 10.2 g of N-benzylphthalimide in 100 cm3 of methanol and 2.6 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 20 hours and is then cooled to a temperature in the regi...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccccc1
null
[BH4-].[K+].CO
20
20
O=C1c2ccccc2C(=O)N1Cc1ccccc1>[BH4-].[K+].CO>O=C1c2ccccc2C(O)N1Cc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-660e8600ee76448898112dcc0dde93fb
NCc1ccccc1.O=C1OC(=O)c2ccccc21>>O=C1c2ccccc2C(=O)N1Cc1ccccc1
C1(C=2C(C(=O)O1)=CC=CC2)=O.C(C1=CC=CC=C1)N>>C(C1=CC=CC=C1)N1C(C=2C(C1=O)=CC=CC2)=O
[NH2:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1.O1[C:2](=[O:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]1=[O:10]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
NCc1ccccc1.O=C1OC(=O)c2ccccc21
O=C1c2ccccc2C(=O)N1Cc1ccccc1
null
null
C([O-])(O)=O.[Na+].C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1c2ccccc2C(=O)N1Cc1ccccc1
[NH2;D1;+0:1]-[C:2]-[c:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[O;D1;H0:4]=[C;H0;D3;+0:5]1-[N;H0;D3;+0:1](-[C:2]-[c:3])-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]
null
[]
140
CELSIUS
null
null
N-Benzylphthalimide is prepared as described in Example 2, starting with 10 g of phthalic anhydride, 7.3 cm3 of benzylamine and a catalytic amount of paratoluenesulfonic acid in 100 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for 3 hours and is then cooled to a temperature i...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccccc1
HO-
C([O-])(O)=O.[Na+].C1(=CC=CC=C1)C
140
null
NCc1ccccc1.O=C1OC(=O)c2ccccc21>C([O-])(O)=O.[Na+].C1(=CC=CC=C1)C>O=C1c2ccccc2C(=O)N1Cc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-cfa06a4cd86d493babc00b0e2b633b2d
CCOC(=O)CC1c2cc(C(C)(C)C)ccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1CC(=O)NC(=N)N
[Na].[Cl-].NC(=[NH2+])N.C(C)(C)(C)C1=CC=C2C(N(C(C2=C1)CC(=O)OCC)CC(C)C)=O>>C(C)(C)(C)C1=CC=C2C(N(C(C2=C1)CC(=O)NC(=N)N)CC(C)C)=O
CCO[C:20]([CH2:19][CH:18]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[cH:16][c:17]21)=[O:21].[NH2:22][C:23]([NH2:24])=[NH2+:25]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[cH:16][c:17]2[...
CCOC(=O)CC1c2cc(C(C)(C)C)ccc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1CC(=O)NC(=N)N
null
null
C(C)O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
68.1
[{"value": 68.1, "product": "C(C)(C)(C)C1=CC=C2C(N(C(C2=C1)CC(=O)NC(=N)N)CC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
N-[(6-tert-Butyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 9, starting with 20 cm3 of absolute ethanol, 0.37 g of sodium, 1.56 g of guanidinium chloride and 3.53 g of ethyl (6-tert-butyl-2-isobutyl-3oxo-2,3-dihydro-1H-isoindol-1-yl)acetate in 10 cm3 of absolute e...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
C(C)O
20
16
CCOC(=O)CC1c2cc(C(C)(C)C)ccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>C(C)O>CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-892763597df54b7aa3735c07130c2bb0
CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1O.COCCOC>>CCOC(=O)CC1c2cc(C(C)(C)C)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(C(C)(C)C)cc2C(=O)N1CC(C)C
C(C)(C)(C)C1=CC=C2C(N(C(C2=C1)=O)CC(C)C)O.C(C)(C)(C)C=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O.O.COCCOC.[H-].[Na+]>>C(C)(C)(C)C1=CC=C2C(N(C(C2=C1)CC(=O)OCC)CC(C)C)=O.C(C)(C)(C)C=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O
[CH:7]1([OH:29])[c:17]2[c:8]([cH:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[cH:15][cH:16]2)[C:18](=[O:19])[N:20]1[CH2:21][CH:22]([CH3:23])[CH3:24].[OH:5][CH:31]1[c:41]2[c:32]([cH:33][cH:34][c:35]([C:36]([CH3:37])([CH3:38])[CH3:39])[cH:40]2)[C:42](=[O:43])[N:44]1[CH2:45][CH:46]([CH3:47])[CH3:48].[CH3:1][O:3][CH2:30][C...
CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1O.COCCOC
CCOC(=O)CC1c2cc(C(C)(C)C)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(C(C)(C)C)cc2C(=O)N1CC(C)C
null
null
C(C)(=O)OCC
Acylation
OtherReaction
362a955bcbf55b12a94bfc1a8d73c33ade6a4f218422d9efb2e5766930dcc44e
c862efb9e1d3c5540cbd521d716baf4935af99206f23dafb24139e94d1655cd7
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[#8:5]-[CH3;D1;+0:6].[C:7]-[#7:8]1-[C;H0;D3;+0:9](=[O;D1;H0:10])-[c;H0;D3;+0:11]2:[c:12]:[c:13]:[c:14]:[c:15]:[c;H0;D3;+0:16]:2-[CH;D3;+0:17]-1-[OH;D1;+0:18].[C:19]-[#7:20]1-[C;H0;D3;+0:21](=[O;D1;H0:22])-[c;H0;D3;+0:23]2:[c:24]:[c:25]:[c:26]:[c:27]:[c;H0;D3;+0:2...
null
[]
20
CELSIUS
null
null
Ethyl (5-tert-butyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate and ethyl (6-tert-butyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate are prepared as described in Example 2, starting with 2.9 g of 60% sodium hydride in 200 cm3 of 1,2-dimethoxyethane, 15.2 cm3 of triethyl phosphonoacetate and 9.6 g of ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Tertiary amide.Secondary alcohol.Secondary alcohol
Ester.Ester.Tertiary amide.Tertiary amide
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
C(C)(=O)OCC
20
null
CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1O.COCCOC>C(C)(=O)OCC>CCOC(=O)CC1c2cc(C(C)(C)C)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(C(C)(C)C)cc2C(=O)N1CC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4ae975eb7c3f4dfbbf156b0a5ec3ab12
CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1=O.O>>CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1O
O.C(C)(C)(C)C=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1>>C(C)(C)(C)C=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O.C(C)(C)(C)C1=CC=C2C(N(C(C2=C1)=O)CC(C)C)O
[CH3:1][C:11]([c:10]1[cH:9][c:8]2[c:17]([cH:16][cH:15]1)[C:18](=[O:19])[N:5]([CH2:4][CH:21]([CH3:20])[CH3:22])[C:6]2=[O:7])([CH3:12])[CH3:31].[OH2:26]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[cH:15][cH:16][c:17]2[CH:18]1[OH:19].[CH3:20][CH:21]([CH3:22])[CH2...
CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1=O.O
CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1O
null
null
[BH4-].[K+].CO
Aromatic Heterocycle Formation
OtherReaction
80e81150c5344eb5948e5ffa5d451e70555c1fccb2813d6b936dafb1decbe38f
635345e99333bb5633c1a982d8704d75548f9c7be11489a084be362ff1b669ae
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[C;D1;H3:1]-[C;H0;D4;+0:2](-[CH3;D1;+0:3])(-[CH3;D1;+0:4])-[c:5]1:[c:6]:[c:7]:[c:8]2:[c:9](:[c:10]:1)-[C:11](=[O;D1;H0:12])-[#7:13](-[CH2;D2;+0:14]-[CH;D3;+0:15](-[C;D1;H3:16])-[C;D1;H3:17])-[C;H0;D3;+0:18]-2=[O;H0;D1;+0:19].[OH2;D0;+0:20]>>[C;D1;H3:21]-[C;H0;D4;+0:4](-[C;D1;H3:22])(-[C;D1;H3:23])-[c:24](:[c:25]):[c:26...
null
[]
20
CELSIUS
19
HOUR
5-tert-Butyl-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one and 6-tert-butyl-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one are prepared as described in Example 1, starting with 10.4 g of 4-tert-butyl-N-isobutylphthalimide in 60 cm3 of methanol and 2.3 g of potassium borohydride. The reaction mixture is stirred at a te...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Tertiary amide.Secondary alcohol.Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
[BH4-].[K+].CO
20
19
CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1=O.O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-aa44b9e4c6cb47cdafae0e1281440de9
CC(C)(C)c1ccc2c(c1)C(=O)OC2=O.CC(C)CN>>CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1=O
C(C)(C)(C)C=1C=C2C(C(=O)OC2=O)=CC1.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C(C)(C)(C)C=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1
O1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[cH:16][c:17]2[C:18]1=[O:19].[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[cH:16][c:17]2[C:18]1=[O:19]
CC(C)(C)c1ccc2c(c1)C(=O)OC2=O.CC(C)CN
CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1=O
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
75
CELSIUS
null
null
4-tert-Butyl-N-isobutylphthalimide is prepared as described in Example 2, starting with 10 g of 4-tert-butylphthalic anhydride and 4.9 cm3 of isobutylamine in 100 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 75° C. for 10 minutes, followed by addition of a catalytic amount of para-to...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
75
null
CC(C)(C)c1ccc2c(c1)C(=O)OC2=O.CC(C)CN>C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2ccc(C(C)(C)C)cc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f2c638ea59514f86964a17e8b70d8d03
CCOC(=O)CC1c2ccc(C(C)(C)C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1CC(=O)NC(=N)N
[Na].[Cl-].NC(=[NH2+])N.C(C)(C)(C)C=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O>>C(C)(C)(C)C=1C=C2C(N(C(C2=CC1)CC(=O)NC(=N)N)CC(C)C)=O
CCO[C:20]([CH2:19][CH:18]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[cH:15][cH:16][c:17]21)=[O:21].[NH2:22][C:23]([NH2:24])=[NH2+:25]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]([CH3:12])([CH3:13])[CH3:14])[cH:15][cH:16][c:17]2[...
CCOC(=O)CC1c2ccc(C(C)(C)C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1CC(=O)NC(=N)N
null
null
C(C)O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
58.5
[{"value": 58.5, "product": "C(C)(C)(C)C=1C=C2C(N(C(C2=CC1)CC(=O)NC(=N)N)CC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
18
HOUR
N-[(5-tert-Butyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 9, starting with 10 cm3 of absolute ethanol, 0.19 g of sodium, 0.80 g of guanidinium chloride and 1.81 g of ethyl (5-tert-butyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate in 10 cm3 of absolute ...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
C(C)O
20
18
CCOC(=O)CC1c2ccc(C(C)(C)C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>C(C)O>CC(C)CN1C(=O)c2cc(C(C)(C)C)ccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-59ecbc226b2140e2806ae1c04f1b3579
CCOC(=O)CC1c2ccc(Cl)cc2C(=O)N1CC(C)C.NC(N)=[NH2+].[Cl-]>>CC(C)CN1C(=O)c2cc(Cl)ccc2C1CC(=O)NC(=N)N.CC(C)CN1C(=O)c2ccc(Cl)cc2C1CC(=O)NC(=N)N
[Cl-].NC(=[NH2+])N.ClC=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O.[Na]>>ClC=1C=C2C(N(C(C2=CC1)CC(=O)NC(=N)N)CC(C)C)=O.ClC1=CC=C2C(N(C(C2=C1)CC(=O)NC(=N)N)CC(C)C)=O
[CH3:1][CH:2]([CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([Cl:11])[cH:12][cH:13][c:14]2[CH:15]1[CH2:16][C:17]([O:18][CH2:35][CH3:33])=[O:29])[CH3:24].[NH2:19][C:20](=[NH2+:27])[NH2:43].[Cl-:34]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([Cl:11])[cH:12][cH:13][c:14]2[CH:15]1[CH2:16][C:17](=[O:1...
CCOC(=O)CC1c2ccc(Cl)cc2C(=O)N1CC(C)C.NC(N)=[NH2+].[Cl-]
CC(C)CN1C(=O)c2cc(Cl)ccc2C1CC(=O)NC(=N)N.CC(C)CN1C(=O)c2ccc(Cl)cc2C1CC(=O)NC(=N)N
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
7c82fcc1e74bd5cbdb5491325bc7c3599033fa46b7fea7b0b39f8423f90c3bf1
0bacb8cb440162b22f0fcc771f33b210c66e45c5ea397677a82721c07267effe
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[C;D1;H3:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[C:4]-[#7:5](-[C:6]-[C:7]-[C;H0;D3;+0:8](=[O;H0;D1;+0:9])-[O;H0;D2;+0:10]-[CH2;D2;+0:11]-[CH3;D1;+0:12])-[C:13]=[O;D1;H0:14].[Cl-;H0;D0:15].[NH2+;D1:16]=[C;H0;D3;+0:17](-[NH2;D1;+0:18])-[NH2;D1;+0:19]>>[#7:20]-[C:21](-[N;D1;H2:22])=[NH;D1;+0:19].[C:23]-[C:24]1-[N;H0;D3;+0:16](-[...
null
[]
20
CELSIUS
18
HOUR
N-[(5-Chloro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine and N-[(6chloro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine are prepared as described in Example 9, starting with 20 cm3 of absolute ethanol, 0.35 g of sodium, 1.46 g of guanidinium chloride and 3.1 g of ethyl (5-chloro-2-iso...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Aromatic halide.Secondary amide.Secondary amide.Tertiary amide.Primary amine.Primary amine
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
null
C(C)O
20
18
CCOC(=O)CC1c2ccc(Cl)cc2C(=O)N1CC(C)C.NC(N)=[NH2+].[Cl-]>C(C)O>CC(C)CN1C(=O)c2cc(Cl)ccc2C1CC(=O)NC(=N)N.CC(C)CN1C(=O)c2ccc(Cl)cc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e16c58598d4842e38ce7bee11878f750
CC(C)CN1C(=O)c2cc(Cl)ccc2C1O.CC(C)CN1C(=O)c2ccc(Cl)cc2C1O.COCCOC>>CCOC(=O)CC1c2cc(Cl)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Cl)cc2C(=O)N1CC(C)C
ClC1=CC=C2C(N(C(C2=C1)=O)CC(C)C)O.[H-].[Na+].ClC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O.O.COCCOC>>ClC=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O.ClC1=CC=C2C(N(C(C2=C1)CC(=O)OCC)CC(C)C)=O
[CH:7]1([OH:26])[c:14]2[c:8]([cH:9][c:10]([Cl:11])[cH:12][cH:13]2)[C:15](=[O:16])[N:17]1[CH2:18][CH:19]([CH3:21])[CH3:27].[OH:5][CH:28]1[c:35]2[c:29]([cH:30][cH:31][c:32]([Cl:33])[cH:34]2)[C:36](=[O:37])[N:38]1[CH2:39][CH:40]([CH3:41])[CH3:42].[CH2:1]([O:3][CH3:2])[CH2:25][O:24][CH3:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5]...
CC(C)CN1C(=O)c2cc(Cl)ccc2C1O.CC(C)CN1C(=O)c2ccc(Cl)cc2C1O.COCCOC
CCOC(=O)CC1c2cc(Cl)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Cl)cc2C(=O)N1CC(C)C
null
null
C(C)(=O)OCC
Acylation
OtherReaction
362a955bcbf55b12a94bfc1a8d73c33ade6a4f218422d9efb2e5766930dcc44e
c862efb9e1d3c5540cbd521d716baf4935af99206f23dafb24139e94d1655cd7
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[C;D1;H3:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[C:4]-[#7:5]1-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c;H0;D3;+0:8]2:[c:9]:[c:10]:[c:11]:[c:12]:[c;H0;D3;+0:13]:2-[CH;D3;+0:14]-1-[OH;D1;+0:15].[CH3;D1;+0:16]-[#8:17]-[CH2;D2;+0:18]-[CH2;D2;+0:19]-[O;H0;D2;+0:20]-[CH3;D1;+0:21].[C:22]-[#7:23]1-[C;H0;D3;+0:24](=[O;D1;H0:25])-[c;H0;D3;+0:26...
null
[]
20
CELSIUS
null
null
Ethyl (5-chloro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate and ethyl (6-chloro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate are prepared as described in Example 2, starting with 4 g of 60% sodium hydride in 200 cm3 of 1,2-dimethoxyethane, 20.3 cm3 of triethyl phosphonoacetate and 12 g of 5-chloro-3-...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Tertiary amide.Secondary alcohol.Secondary alcohol
Ester.Ester.Tertiary amide.Tertiary amide
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
C(C)(=O)OCC
20
null
CC(C)CN1C(=O)c2cc(Cl)ccc2C1O.CC(C)CN1C(=O)c2ccc(Cl)cc2C1O.COCCOC>C(C)(=O)OCC>CCOC(=O)CC1c2cc(Cl)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Cl)cc2C(=O)N1CC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3b0e4232745a415f84ee421773f9dc6f
CC(C)CN1C(=O)c2ccc(Cl)cc2C1=O>>CC(C)CN1C(=O)c2ccc(Cl)cc2C1O
ClC=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1.O>>ClC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O
[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][c:14]2[C:15]1=[O:16]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][c:14]2[CH:15]1[OH:16]
CC(C)CN1C(=O)c2ccc(Cl)cc2C1=O
CC(C)CN1C(=O)c2ccc(Cl)cc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
null
[]
20
CELSIUS
20
HOUR
5-Chloro-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one and 6-chloro-3-hydroxy-2isobutyl-2,3-dihydroinsoindol-1-one are prepared as described in Example 1, starting with 12 g of 4-chloro-N-isobutylphthalimide in 100 cm3 of methanol and 3 g of potassium borohydride. The reaction mixture is stirred at a temperature in th...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
20
CC(C)CN1C(=O)c2ccc(Cl)cc2C1=O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2ccc(Cl)cc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e924a00a32eb4943afc624d45db47c6f
CC(C)CN.O=C1OC(=O)c2cc(Cl)ccc21>>CC(C)CN1C(=O)c2ccc(Cl)cc2C1=O
ClC=1C=C2C(C(=O)OC2=O)=CC1.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>ClC=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1
[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5].O1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][c:14]2[C:15]1=[O:16]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][c:14]2[C:15]1=[O:16]
CC(C)CN.O=C1OC(=O)c2cc(Cl)ccc21
CC(C)CN1C(=O)c2ccc(Cl)cc2C1=O
null
null
C([O-])(O)=O.[Na+].C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
140
CELSIUS
null
null
4-Chloro-N-isobutylphthalimide is prepared as described in Example 2, starting with 10 g of 4-chlorophthalic anhydride, 5.4 cm3 of isobutylamine and a catalytic amount of para-toluenesulfonic acid in 100 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for 16 hours and is then co...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C([O-])(O)=O.[Na+].C1(=CC=CC=C1)C
140
null
CC(C)CN.O=C1OC(=O)c2cc(Cl)ccc21>C([O-])(O)=O.[Na+].C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2ccc(Cl)cc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5c5a65e00f3b41589c35f5315322a40f
CCOC(=O)CC1c2cc(Br)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Br)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2cc(Br)ccc2C1CC(=O)NC(=N)N.CC(C)CN1C(=O)c2ccc(Br)cc2C1CC(=O)NC(=N)N
BrC1=CC=C2C(N(C(C2=C1)CC(=O)OCC)CC(C)C)=O.[Cl-].NC(=[NH2+])N.BrC=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O.[Na]>>BrC1=CC=C2C(N(C(C2=C1)CC(=O)NC(=N)N)CC(C)C)=O.BrC=1C=C2C(N(C(C2=CC1)CC(=O)NC(=N)N)CC(C)C)=O
CCO[C:20]([CH2:16][CH:15]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:14]2[c:8]1[cH:9][c:10]([Br:11])[cH:12][cH:13]2)=[O:18].C(O[C:39]([CH2:38][CH:37]1[N:27]([CH2:26][CH:24]([CH3:23])[CH3:25])[C:28](=[O:29])[c:36]2[c:30]1[cH:31][cH:32][c:33]([Br:34])[cH:35]2)=[O:40])[CH3:17].[NH2:19][C:42]([NH2:21])=[NH2+:41]>>...
CCOC(=O)CC1c2cc(Br)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Br)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2cc(Br)ccc2C1CC(=O)NC(=N)N.CC(C)CN1C(=O)c2ccc(Br)cc2C1CC(=O)NC(=N)N
null
null
O.C(C)OCC.C(C)O
Acylation
OtherReaction
58c7bbe22abce425286dc7c77ea04f5fe7262ea222c8df00fb60d9de48138947
c13b7a4604f90d6b297071920a60f6e92464931ecb3ae9d252f9bb3cb252eb66
O=C1NCc2ccccc21.O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[CH2;D2;+0:3]-[CH;D3;+0:4]1-[#7:5](-[C:6])-[C;H0;D3;+0:7](=[O;D1;H0:8])-[c;H0;D3;+0:9]2:[c:10]:[c:11]:[c:12]:[c:13]:[c;H0;D3;+0:14]:2-1.[C:15]-[#7:16]1-[C;H0;D3;+0:17](=[O;D1;H0:18])-[c;H0;D3;+0:19]2:[c:20]:[c:21]:[c:22]:[c:23]:[c;H0;D3;+0:24]:2-[CH;D3;+0:25]-1-[C:26]-[C;H0;D3;+0:2...
null
[]
20
CELSIUS
16
HOUR
N-[(5-Bromo-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine and N-[(6-bromo-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine are prepared as described in Example 9, starting with 30 cm3 of absolute ethanol, 0.36 g of sodium, 1.5 g of guanidinium chloride and 3.7 g of ethyl (5-bromo-2-isobut...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester.Ester.Tertiary amide.Tertiary amide
Secondary amide.Secondary amide.Tertiary amide.Tertiary amide.Primary amine.Primary amine
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
HO-
O.C(C)OCC.C(C)O
20
16
CCOC(=O)CC1c2cc(Br)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Br)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>O.C(C)OCC.C(C)O>CC(C)CN1C(=O)c2cc(Br)ccc2C1CC(=O)NC(=N)N.CC(C)CN1C(=O)c2ccc(Br)cc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3008eb1ac514440086fb77b46c5fc459
CC(C)CN1C(=O)c2cc(Br)ccc2C1O.CC(C)CN1C(=O)c2ccc(Br)cc2C1O.COCCOC>>CCOC(=O)CC1c2cc(Br)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Br)cc2C(=O)N1CC(C)C
BrC1=CC=C2C(N(C(C2=C1)=O)CC(C)C)O.COCCOC.[H-].[Na+].O.BrC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O>>BrC1=CC=C2C(N(C(C2=C1)CC(=O)OCC)CC(C)C)=O.BrC=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O
[CH:7]1([OH:26])[c:14]2[c:8]([cH:9][c:10]([Br:11])[cH:12][cH:13]2)[C:15](=[O:16])[N:17]1[CH2:18][CH:19]([CH3:21])[CH3:27].[OH:5][CH:28]1[c:35]2[c:29]([cH:30][cH:31][c:32]([Br:33])[cH:34]2)[C:36](=[O:37])[N:38]1[CH2:39][CH:40]([CH3:41])[CH3:42].[CH2:1]([O:3][CH3:2])[CH2:25][O:24][CH3:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5]...
CC(C)CN1C(=O)c2cc(Br)ccc2C1O.CC(C)CN1C(=O)c2ccc(Br)cc2C1O.COCCOC
CCOC(=O)CC1c2cc(Br)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Br)cc2C(=O)N1CC(C)C
null
null
null
Acylation
OtherReaction
362a955bcbf55b12a94bfc1a8d73c33ade6a4f218422d9efb2e5766930dcc44e
c862efb9e1d3c5540cbd521d716baf4935af99206f23dafb24139e94d1655cd7
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[C;D1;H3:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[C:4]-[#7:5]1-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c;H0;D3;+0:8]2:[c:9]:[c:10]:[c:11]:[c:12]:[c;H0;D3;+0:13]:2-[CH;D3;+0:14]-1-[OH;D1;+0:15].[CH3;D1;+0:16]-[#8:17]-[CH2;D2;+0:18]-[CH2;D2;+0:19]-[O;H0;D2;+0:20]-[CH3;D1;+0:21].[C:22]-[#7:23]1-[C;H0;D3;+0:24](=[O;D1;H0:25])-[c;H0;D3;+0:26...
null
[]
20
CELSIUS
null
null
Ethyl (5-bromo-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate and ethyl (6-bromo-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate are prepared as described in Example 2, starting with 5.0 g of 60% sodium hydride in 250 cm3 of 1,2-dimethoxyethane, 24.8 cm3 of triethyl phosphonoacetate and 23.7 g of 5-bromo-3...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Tertiary amide.Secondary alcohol.Secondary alcohol
Ester.Ester.Tertiary amide.Tertiary amide
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
null
20
null
CC(C)CN1C(=O)c2cc(Br)ccc2C1O.CC(C)CN1C(=O)c2ccc(Br)cc2C1O.COCCOC>>CCOC(=O)CC1c2cc(Br)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(Br)cc2C(=O)N1CC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-afff836b6a81496ba9bb331b596140e9
CC(C)CN1C(=O)c2ccc(Br)cc2C1=O>>CC(C)CN1C(=O)c2ccc(Br)cc2C1O
BrC=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1.O>>BrC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O
[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Br:12])[cH:13][c:14]2[C:15]1=[O:16]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Br:12])[cH:13][c:14]2[CH:15]1[OH:16]
CC(C)CN1C(=O)c2ccc(Br)cc2C1=O
CC(C)CN1C(=O)c2ccc(Br)cc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
99.7
[{"value": 99.7, "product": "BrC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
5-Bromo-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one and 6-bromo-3-hydroxy-2-isobutyl-2,3-dihydroinsoindol-1-one are prepared as described in Example 1, starting with 23.6 g of 4-bromo-N-isobutylphthalimide in 200 cm3 of methanol and 4.5 g of potassium borohydride. The reaction mixture is stirred at a temperature in ...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
16
CC(C)CN1C(=O)c2ccc(Br)cc2C1=O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2ccc(Br)cc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-db135124f2e94d89be47ea9aaeddff43
CC(C)CN.O=C1OC(=O)c2cc(Br)ccc21>>CC(C)CN1C(=O)c2ccc(Br)cc2C1=O
BrC=1C=C2C(C(=O)OC2=O)=CC1.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>BrC=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1
[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5].O1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Br:12])[cH:13][c:14]2[C:15]1=[O:16]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([Br:12])[cH:13][c:14]2[C:15]1=[O:16]
CC(C)CN.O=C1OC(=O)c2cc(Br)ccc21
CC(C)CN1C(=O)c2ccc(Br)cc2C1=O
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
140
CELSIUS
null
null
4-Bromo-N-isobutylphthalimide is prepared as described in Example 2, starting with 20 g of 4-bromophthalic anhydride, 9.2 cm3 of isobutylamine and a catalytic amount of para-toluenesulfonic acid in 200 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for 6 hours and is then coole...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
140
null
CC(C)CN.O=C1OC(=O)c2cc(Br)ccc21>C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2ccc(Br)cc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a48b7957df4a4c8b9c68670db0bcf645
CCOC(=O)CC1c2ccc(C(F)(F)F)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1CC(=O)NC(=N)N
[Na].[Cl-].NC(=[NH2+])N.FC(C=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O)(F)F>>FC(C=1C=C2C(N(C(C2=CC1)CC(=O)NC(=N)N)CC(C)C)=O)(F)F
CCO[C:20]([CH2:19][CH:18]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15][cH:16][c:17]21)=[O:21].[NH2:22][C:23]([NH2:24])=[NH2+:25]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15][cH:16][c:17]2[CH:18]1[CH2:...
CCOC(=O)CC1c2ccc(C(F)(F)F)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1CC(=O)NC(=N)N
null
null
C(C)OCC.C(C)O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
17.6
[{"value": 17.6, "product": "FC(C=1C=C2C(N(C(C2=CC1)CC(=O)NC(=N)N)CC(C)C)=O)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
N-[2-(2-Isobutyl-3-oxo-5-trifluoromethyl-2,3-dihydro-1H-isoindol-1-yl)-acetyl]-guanidine is prepared as described in Example 9, starting with 10 cm3 of absolute ethanol, 0.19 g of sodium, 0.78 g of guanidinium chloride and 1.86 g of ethyl (5-trifluoromethyl-2-isobutyl-3-oxo-2,3-dihyrdo-1H-isoindol-1-yl)acetate in 10 cm...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
C(C)OCC.C(C)O
20
16
CCOC(=O)CC1c2ccc(C(F)(F)F)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>C(C)OCC.C(C)O>CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-11c04c56488c4ee4b02881805dd5137c
CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1CC(=O)NC(=N)N
[Na].[Cl-].NC(=[NH2+])N.FC(C1=CC=C2C(N(C(C2=C1)CC(=O)OCC)CC(C)C)=O)(F)F>>C(C(C)C)N1C(C2=CC(=CC=C2C1=O)C(F)(F)F)CC(=O)NC(=N)N
CCO[C:20]([CH2:19][CH:18]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([F:13])([F:14])[F:15])[cH:16][c:17]21)=[O:21].[NH2:22][C:23]([NH2:24])=[NH2+:25]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([F:13])([F:14])[F:15])[cH:16][c:17]2[CH:18]1[CH2:...
CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1CC(=O)NC(=N)N
null
null
C(C)OCC.C(C)O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
7.6
[{"value": 7.6, "product": "C(C(C)C)N1C(C2=CC(=CC=C2C1=O)C(F)(F)F)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
N-[2-(2-Isobutyl-3-oxo-6-trifluoromethyl-2,3-dihydro-1H-isoindol-1-yl)-acetyl]-guanidine is prepared as described in Example 9, starting with 10 cm3 of absolute ethanol, 0.13 g of sodium, 0.52 g of guanidinium chloride and 1.25 g of ethyl (6-trifluoromethyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate in 10 cm...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
C(C)OCC.C(C)O
20
16
CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>C(C)OCC.C(C)O>CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b911b6e30eac40c5be3c86438d8fe792
CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1O.COCCOC>>CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(C(F)(F)F)cc2C(=O)N1CC(C)C
FC(C1=CC=C2C(N(C(C2=C1)=O)CC(C)C)O)(F)F.COCCOC.[H-].[Na+].O.FC(C=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O)(F)F>>FC(C1=CC=C2C(N(C(C2=C1)CC(=O)OCC)CC(C)C)=O)(F)F.FC(C=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O)(F)F
[CH:7]1([OH:29])[c:17]2[c:8]([cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15][cH:16]2)[C:18](=[O:19])[N:20]1[CH2:21][CH:22]([CH3:23])[CH3:24].[OH:5][CH:31]1[c:41]2[c:32]([cH:33][cH:34][c:35]([C:36]([F:37])([F:38])[F:39])[cH:40]2)[C:42](=[O:43])[N:44]1[CH2:45][CH:46]([CH3:47])[CH3:48].[CH3:1][O:3][CH2:30][CH2:28][O:27]...
CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1O.COCCOC
CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(C(F)(F)F)cc2C(=O)N1CC(C)C
null
null
null
Acylation
OtherReaction
362a955bcbf55b12a94bfc1a8d73c33ade6a4f218422d9efb2e5766930dcc44e
c862efb9e1d3c5540cbd521d716baf4935af99206f23dafb24139e94d1655cd7
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[#8:5]-[CH3;D1;+0:6].[C:7]-[#7:8]1-[C;H0;D3;+0:9](=[O;D1;H0:10])-[c;H0;D3;+0:11]2:[c:12]:[c:13]:[c:14]:[c:15]:[c;H0;D3;+0:16]:2-[CH;D3;+0:17]-1-[OH;D1;+0:18].[C:19]-[#7:20]1-[C;H0;D3;+0:21](=[O;D1;H0:22])-[c;H0;D3;+0:23]2:[c:24]:[c:25]:[c:26]:[c:27]:[c;H0;D3;+0:2...
null
[]
20
CELSIUS
null
null
Ethyl (5-trifluoromethyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate and ethyl (6-trifluoromethyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate are prepared as described in Example 2, starting with 1.32 g of 60% sodium hydride in 120 cm3 of 1,2-dimethoxyethane, 6.57 cm3 of triethyl phosphonoacetate an...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Tertiary amide.Secondary alcohol.Secondary alcohol
Ester.Ester.Tertiary amide.Tertiary amide
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
null
20
null
CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1O.COCCOC>>CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC(C)C.CCOC(=O)CC1c2ccc(C(F)(F)F)cc2C(=O)N1CC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-80a11acd650b4e7eab47616b569985b3
CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1=O.O>>CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1O
FC(C=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1)(F)F.O>>FC(C1=CC=C2C(N(C(C2=C1)=O)CC(C)C)O)(F)F.FC(C=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O)(F)F
[CH3:1][CH:21]([CH2:4][N:5]1[C:25](=[O:26])[c:27]2[cH:28][cH:29][c:30]([C:31]([F:12])([F:14])[F:34])[cH:35][c:36]2[C:37]1=[O:38])[CH3:11].[OH2:7]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]([F:12])([F:13])[F:14])[cH:15][cH:16][c:17]2[CH:18]1[OH:19].[CH3:20][CH:21]([CH3:22])[CH2:23][N:24]1...
CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1=O.O
CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1O
null
null
[BH4-].[K+].CO
Aromatic Heterocycle Formation
OtherReaction
e4f3ae5275cd862e13f3273d210cd60a39d558600dc1a0f4901b083f858ac0c0
b62fa8b67b6dea62f57ad0bc3864994c950d139694efad0b1d73e172fc7e0cf5
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[CH3;D1;+0:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[CH2;D2;+0:4]-[N;H0;D3;+0:5]1-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8]2:[c:9]:[c:10]:[c:11](-[C;H0;D4;+0:12](-[F;D1;H0:13])(-[F;H0;D1;+0:14])-[F;H0;D1;+0:15]):[c:16]:[c:17]:2-[C;H0;D3;+0:18]-1=[O;H0;D1;+0:19].[OH2;D0;+0:20]>>[C;D1;H3:21]-[CH;D3;+0:2](-[C;D1;H3:22])-[C:23]-[#7:24]1-[...
160.8
[{"value": 160.8, "product": "FC(C=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
5-Trifluoromethyl-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one and 6-trifluoromethyl-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one are prepared as described in Example 1, starting with 14.9 g of 4-trifluoromethyl-N-isobutylphthalimide in 300 cm3 of methanol and 2.96 g of potassium borohydride. The reaction mixture i...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Substituted dicarboximide
Trifluoro group.Trifluoro group.Tertiary amide.Tertiary amide.Secondary alcohol.Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
[BH4-].[K+].CO
20
16
CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1=O.O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2cc(C(F)(F)F)ccc2C1O.CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-bc678ceaffb94426a0467a40e180f547
CC(C)CN.O=C1OC(=O)c2cc(C(F)(F)F)ccc21>>CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1=O
FC(C=1C=C2C(C(=O)OC2=O)=CC1)(F)F.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>FC(C=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1)(F)F
[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5].O1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([F:13])([F:14])[F:15])[cH:16][c:17]2[C:18]1=[O:19]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]([F:13])([F:14])[F:15])[cH:16][c:17]2[C:18]1=[O:19]
CC(C)CN.O=C1OC(=O)c2cc(C(F)(F)F)ccc21
CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1=O
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
140
CELSIUS
null
null
4-Trifluoromethyl-N-isobutylphthalimide is prepared as described in Example 2, starting with 14.8 g of 4-trifluoromethylphthalic anhydride, 7.2 cm3 of isobutylamine and a catalytic amount of para-toluenesulfonic acid in 160 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for 5 h...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
140
null
CC(C)CN.O=C1OC(=O)c2cc(C(F)(F)F)ccc21>C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2ccc(C(F)(F)F)cc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fa2e29fc363c4393b8c8453589380eb7
CCOC(=O)CC1c2ccc(OC(C)C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2cc(OC(C)C)ccc2C1CC(=O)NC(=N)N
[Na].[Cl-].NC(=[NH2+])N.C(C)(C)OC=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O>>C(C(C)C)N1C(C2=CC=C(C=C2C1=O)OC(C)C)CC(=O)NC(=N)N
CCO[C:20]([CH2:19][CH:18]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][c:10]([O:11][CH:12]([CH3:13])[CH3:14])[cH:15][cH:16][c:17]21)=[O:21].[NH2:22][C:23]([NH2:24])=[NH2+:25]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([O:11][CH:12]([CH3:13])[CH3:14])[cH:15][cH:16][c:17]2[CH:18]...
CCOC(=O)CC1c2ccc(OC(C)C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2cc(OC(C)C)ccc2C1CC(=O)NC(=N)N
null
null
C(C)O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
4
[{"value": 4.0, "product": "C(C(C)C)N1C(C2=CC=C(C=C2C1=O)OC(C)C)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
18
HOUR
N-[2-(2-Isobutyl-5-isopropoxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)-acetyl]-guanidine is prepared as described in Example 9, starting with 20 cm3 of absolute ethanol, 0.086 g of sodium, 0.36 g of guanidinium chloride and 0.42 g of ethyl (5-isopropyloxy-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate. The reaction m...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
C(C)O
20
18
CCOC(=O)CC1c2ccc(OC(C)C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>C(C)O>CC(C)CN1C(=O)c2cc(OC(C)C)ccc2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e3f6aa0b566a4969bcee0ee90c3ebf10
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1O.O>>CCOC(=O)CC1c2ccc(OC(C)C)cc2C(=O)N1CC(C)C
[H-].[Na+].C(C)(C)OC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O.O>>C(C)(C)OC=1C=C2C(N(C(C2=CC1)CC(=O)OCC)CC(C)C)=O
[CH3:1][CH:13]([O:12][c:11]1[cH:9][c:8]2[c:17]([cH:16][cH:10]1)[C:18](=[O:19])[N:20]([CH2:21][CH:22]([CH3:23])[CH3:24])[CH:7]2[OH:5])[CH3:15].[OH2:3]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH:7]1[c:8]2[cH:9][cH:10][c:11]([O:12][CH:13]([CH3:14])[CH3:15])[cH:16][c:17]2[C:18](=[O:19])[N:20]1[CH2:21][CH:22]([CH3:23])[CH3...
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1O.O
CCOC(=O)CC1c2ccc(OC(C)C)cc2C(=O)N1CC(C)C
null
null
COCCOC
Acylation
OtherReaction
9431162f4b61d6285783d941b2fe083a1e97fbfe6db09639a37d68fe4088d6a7
f9d6c48cce2371b8da82e921e7975e3937854c11baada232d9ed3e1d8c7bc0db
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]2:[cH;D2;+0:6]:[cH;D2;+0:7]:[c;H0;D3;+0:8](-[#8:9]-[CH;D3;+0:10](-[C;D1;H3:11])-[CH3;D1;+0:12]):[cH;D2;+0:13]:[c:14]:2-[CH;D3;+0:15]-1-[OH;D1;+0:16].[OH2;D0;+0:17]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]2:[cH;D2;+0:6]:[c;H0;D3;+0:8](-[#8:9]-[CH;D3;+0:10](-[C;D1;H3:18])-[C;D1;H3:1...
null
[]
20
CELSIUS
null
null
Ethyl (5-isopropyloxy-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate is prepared as described in Example 2, starting with 0.149 g of 60% sodium hydride in 20 cm3 of 1,2-dimethoxyethane, 1.23 cm3 of triethyl phosphonoacetate and 1.08 g of 5-isopropyloxy-3-hydroxy-2-isobutyl-2,3-dihydro-isoindol-1-one. The mixture...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol
Ester.Ether
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
Other
COCCOC
20
null
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1O.O>COCCOC>CCOC(=O)CC1c2ccc(OC(C)C)cc2C(=O)N1CC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-07df97015a174e91b1461d8c8e727946
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1=O>>CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1O
C(C(C)C)N1C(C=2C(C1=O)=CC(=CC2)OC(C)C)=O.O>>C(C)(C)OC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O
[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([O:12][CH:13]([CH3:14])[CH3:15])[cH:16][c:17]2[C:18]1=[O:19]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([O:12][CH:13]([CH3:14])[CH3:15])[cH:16][c:17]2[CH:18]1[OH:19]
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1=O
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
92.4
[{"value": 92.4, "product": "C(C)(C)OC=1C=C2C(N(C(C2=CC1)=O)CC(C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
17
HOUR
5-Isopropyloxy-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 1.16 g of N-isobutyl-4-isopropyloxyphthalimide in 20 cm3 of methanol and 0.24 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 17 hours and then cool...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
17
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1=O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c5f237b2d7c84b948202dfeb7e36f388
CC(C)Br.CC(C)CN1C(=O)c2ccc(O)cc2C1=O>>CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1=O
OC=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1.BrC(C)C.C([O-])([O-])=O.[K+].[K+]>>C(C(C)C)N1C(C=2C(C1=O)=CC(=CC2)OC(C)C)=O
Br[CH:13]([CH3:14])[CH3:15].[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:16][c:17]2[C:18]1=[O:19]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([O:12][CH:13]([CH3:14])[CH3:15])[cH:16][c:17]2[C:18]1=[O:19]
CC(C)Br.CC(C)CN1C(=O)c2ccc(O)cc2C1=O
CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
bff4876be49b448135c783dd3eeeb68ab3cc5bdc91beadda8a9095106cd5c747
cf768afb66ed5041aefdce1fa6d1e40995a1ab7c4b4a4ca47544fe49ee1e629f
O=C1NC(=O)c2ccccc21
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[C;D1;H3:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[CH;D3;+0:1](-[C;D1;H3:3])-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
60
CELSIUS
17
HOUR
A mixture of 1 g of 4-hydroxy-N-isobutylphthalimide, 0.85 cm3 of 2-bromopropane and 1.38 g of potassium carbonate in 5 cm3 of dimethylformamide is stirred at a temperature in the region of 60° C. for 17 hours. The reaction mixture is then cooled to a temperature in the region of 20° C. and then concentrated to dryness ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)C[NH]C2
HBr
CN(C=O)C
60
17
CC(C)Br.CC(C)CN1C(=O)c2ccc(O)cc2C1=O>CN(C=O)C>CC(C)CN1C(=O)c2ccc(OC(C)C)cc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5e041bb17b184daa98c689fd6550a79d
CC(=O)Oc1ccc2c(c1)C(=O)OC2=O.CC(C)CN>>CC(C)CN1C(=O)c2ccc(O)cc2C1=O
C(C)(=O)OC=1C=C2C(C(=O)OC2=O)=CC1.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>OC=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1
CC(=O)[O:12][c:11]1[cH:10][cH:9][c:8]2[c:14]([cH:13]1)[C:15](=[O:16])O[C:6]2=[O:7].[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([OH:12])[cH:13][c:14]2[C:15]1=[O:16]
CC(=O)Oc1ccc2c(c1)C(=O)OC2=O.CC(C)CN
CC(C)CN1C(=O)c2ccc(O)cc2C1=O
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
4426da7b9ff3850b4860c68f12842b4a9b5cd80f984597b746fbea93119ad9c5
3854c499f8bc211ab83cf60501e3c53dcb79f3dde4ccfc877f4cac8c198a4d9c
O=C1NC(=O)c2ccccc21
C-C(=O)-[O;H0;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[c:5]2:[c:6](:[c:7]:1)-[C;H0;D3;+0:8](=[O;D1;H0:9])-O-[C;H0;D3;+0:10]-2=[O;D1;H0:11].[C:12]-[C:13]-[NH2;D1;+0:14]>>[C:12]-[C:13]-[N;H0;D3;+0:14]1-[C;H0;D3;+0:8](=[O;D1;H0:9])-[c:6]2:[c:7]:[c:2](-[OH;D1;+0:1]):[c:3]:[c:4]:[c:5]:2-[C;H0;D3;+0:10]-1=[O;D1;H0:11]
null
[]
140
CELSIUS
1.5
HOUR
4-Hydroxy-N-isobutylphthalimide is prepared as described in Example 2, starting with 7.26 g of 4-acetoxyphthalic anhydride, 7.35 cm3 of isobutylamine and a catalytic amount of para-toluenesulfonic acid in 75 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for 4 hours and then co...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Ester.Primary amine
Substituted dicarboximide.Aromatic alcohol
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
140
1.5
CC(=O)Oc1ccc2c(c1)C(=O)OC2=O.CC(C)CN>C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2ccc(O)cc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e00eddfb4ac249bf9f014dfcc2aeece2
CCOC(=O)CC1c2c(F)cccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2cccc(F)c2C1CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.FC=1C=CC=C2C(N(C(C12)CC(=O)OCC)CC(C)C)=O>>FC=1C=CC=C2C(N(C(C12)CC(=O)NC(=N)N)CC(C)C)=O
CCO[C:17]([CH2:16][CH:15]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][c:12]([F:13])[c:14]21)=[O:18].[NH2:19][C:20]([NH2:21])=[NH2+:22]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][c:12]([F:13])[c:14]2[CH:15]1[CH2:16][C:17](=[O:18])[NH:19][C:20](=[NH:21])[NH...
CCOC(=O)CC1c2c(F)cccc2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2cccc(F)c2C1CC(=O)NC(=N)N
null
null
null
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
21.4
[{"value": 21.4, "product": "FC=1C=CC=C2C(N(C(C12)CC(=O)NC(=N)N)CC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
N-[(7-Fluoro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 1.29 g of potassium tert-butoxide, 1.32 g of guanidinium chloride and 0.67 g of ethyl (7-fluoro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate. The reaction mixture is stirred at a tem...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
null
20
20
CCOC(=O)CC1c2c(F)cccc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2cccc(F)c2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-eca74393ec4e4c3fb8f3921e68fd6d01
CC(C)CN1C(=O)c2cccc(F)c2C1=O>>CC(C)CN1C(=O)c2cccc(F)c2C1O
FC1=C2C(C(=O)N(C2=O)CC(C)C)=CC=C1>>FC1=C2C(N(C(C2=CC=C1)=O)CC(C)C)O
[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][c:12]([F:13])[c:14]2[C:15]1=[O:16]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][c:12]([F:13])[c:14]2[CH:15]1[OH:16]
CC(C)CN1C(=O)c2cccc(F)c2C1=O
CC(C)CN1C(=O)c2cccc(F)c2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
88.9
[{"value": 88.9, "product": "FC1=C2C(N(C(C2=CC=C1)=O)CC(C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
19
HOUR
4-Fluoro-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1 starting with 3.9 g of 3-fluoro-N-isobutylphthalimide in 20 cm3 of methanol and 0.95 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 19 hours and is then cooled to a tem...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
19
CC(C)CN1C(=O)c2cccc(F)c2C1=O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2cccc(F)c2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-cbdf2c15a68c4c8bbaa462ea6aa0317e
CC(C)CN.O=C1OC(=O)c2c(F)cccc21>>CC(C)CN1C(=O)c2cccc(F)c2C1=O
FC1=C2C(C(=O)OC2=O)=CC=C1.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>FC1=C2C(C(=O)N(C2=O)CC(C)C)=CC=C1
[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5].O1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][c:12]([F:13])[c:14]2[C:15]1=[O:16]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][c:12]([F:13])[c:14]2[C:15]1=[O:16]
CC(C)CN.O=C1OC(=O)c2c(F)cccc21
CC(C)CN1C(=O)c2cccc(F)c2C1=O
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
140
CELSIUS
null
null
3-Fluoro-N-isobutylphthalimide is prepared as described in Example 2, starting with 3.4 g of 3-fluorophthalic anhydride, 2.0 cm3 of isobutylamine and a catalytic amount of para-toluenesulfonic acid in 20 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for 3 hours. After cooling ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
140
null
CC(C)CN.O=C1OC(=O)c2c(F)cccc21>C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2cccc(F)c2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6d16386a67ab42f5b744701a9d4bc6d1
CCOC(=O)CC1c2cc(Cl)c(Cl)cc2C(=O)N1CC(C)C>>CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1CC(=O)O
[Na].[Na].ClC=1C=C2C(N(C(C2=CC1Cl)CC(=O)OCC)CC(C)C)=O.[Cl-].NC(=[NH2+])N>>ClC=1C=C2C(N(C(C2=CC1Cl)CC(=O)O)CC(C)C)=O
CC[O:20][C:18]([CH2:17][CH:16]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[cH:9][c:10]([Cl:11])[c:12]([Cl:13])[cH:14][c:15]21)=[O:19]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([Cl:11])[c:12]([Cl:13])[cH:14][c:15]2[CH:16]1[CH2:17][C:18](=[O:19])[OH:20]
CCOC(=O)CC1c2cc(Cl)c(Cl)cc2C(=O)N1CC(C)C
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1CC(=O)O
null
null
C(C)O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1NCc2ccccc21
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
42.1
[{"value": 42.1, "product": "ClC=1C=C2C(N(C(C2=CC1Cl)CC(=O)O)CC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
1.5
HOUR
0.09 g of sodium is added to 5 cm3 of absolute ethanol under an inert atmosphere. After the sodium has totally disappeared, 0.04 g of guanidinium chloride is added. The reaction mixture is stirred under an inert atmosphere at a temperature in the region of 20° C. for 1.5 hours, followed by addition of a solution of 0.9...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2c(c1)C[NH]C2
Other
C(C)O
20
1.5
CCOC(=O)CC1c2cc(Cl)c(Cl)cc2C(=O)N1CC(C)C>C(C)O>CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1CC(=O)O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9390d1324720489caf2104fa47e0587a
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1O.CCOCC>>CCOC(=O)CC1c2cc(Cl)c(Cl)cc2C(=O)N1CC(C)C
C(C)OCC.[H-].[Na+].ClC=1C=C2C(N(C(C2=CC1Cl)=O)CC(C)C)O.O>>ClC=1C=C2C(N(C(C2=CC1Cl)CC(=O)OCC)CC(C)C)=O
[OH:5][CH:7]1[c:8]2[cH:9][c:10]([Cl:11])[c:12]([Cl:13])[cH:14][c:15]2[C:16](=[O:17])[N:18]1[CH2:19][CH:20]([CH3:21])[CH3:22].[CH3:1][CH2:2][O:3][CH2:4][CH3:6]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH:7]1[c:8]2[cH:9][c:10]([Cl:11])[c:12]([Cl:13])[cH:14][c:15]2[C:16](=[O:17])[N:18]1[CH2:19][CH:20]([CH3:21])[CH3:22]
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1O.CCOCC
CCOC(=O)CC1c2cc(Cl)c(Cl)cc2C(=O)N1CC(C)C
null
null
COCCOC
Heteroatom Alkylation and Arylation
OtherReaction
48a0bd460ac260e177ffa262698d9e6ae802769dd91076aaf638df24b5a534e1
79b1dc52d3be254effebd4b18222e0510623f9682e37c200296c41f37c9f0926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9].[C:10]-[#8:11]-[CH2;D2;+0:12]-[CH3;D1;+0:13]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[CH2;D2;+0:13]-[C;H0;D3;+0:12](=[O;H0;D1;+0:9])-[#8:11]-[C:10]
null
[]
20
CELSIUS
null
null
Ethyl (5,6-dichloro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate is prepared as described in Example 2, starting with 0.75 g of 60% sodium hydride in 45 cm3 of 1,2-dimethoxyethane, 3.71 cm3 of triethyl phosphonoacetate and 3.42 g of 5,6-dichloro-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one. The mixture is re...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol
Ester
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
COCCOC
20
null
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1O.CCOCC>COCCOC>CCOC(=O)CC1c2cc(Cl)c(Cl)cc2C(=O)N1CC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-688d8d59ac9d4758847774241978eef8
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1=O>>CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1O
ClC=1C=C2C(C(=O)N(C2=O)CC(C)C)=CC1Cl>>ClC=1C=C2C(N(C(C2=CC1Cl)=O)CC(C)C)O
[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([Cl:11])[c:12]([Cl:13])[cH:14][c:15]2[C:16]1=[O:17]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][c:10]([Cl:11])[c:12]([Cl:13])[cH:14][c:15]2[CH:16]1[OH:17]
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1=O
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
89.8
[{"value": 89.8, "product": "ClC=1C=C2C(N(C(C2=CC1Cl)=O)CC(C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
16
HOUR
5,6-Dichloro-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 3.78 g of 4,5-dichloro-N-isobutylphthalimide in 75 cm3 of methanol and 0.75 g of potassium borohydride. The reaction mixture is stirred at a temperature in the region of 20° C. for 16 hours and is then coole...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
16
CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1=O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2cc(Cl)c(Cl)cc2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-cc7455381f9940a5aca8ac46fe9bacd5
CCOC(=O)CC1c2c(F)ccc(F)c2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2c(F)ccc(F)c2C1CC(=O)NC(=N)N
FC1=C2C(N(C(C2=C(C=C1)F)CC(=O)OCC)CC(C)C)=O.CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N>>FC1=C2C(N(C(C2=C(C=C1)F)CC(=O)NC(=N)N)CC(C)C)=O
CCO[C:18]([CH2:17][CH:16]1[N:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:6](=[O:7])[c:8]2[c:9]([F:10])[cH:11][cH:12][c:13]([F:14])[c:15]21)=[O:19].[NH2:20][C:21]([NH2:22])=[NH2+:23]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[c:9]([F:10])[cH:11][cH:12][c:13]([F:14])[c:15]2[CH:16]1[CH2:17][C:18](=[O:19])[NH:20][C:21...
CCOC(=O)CC1c2c(F)ccc(F)c2C(=O)N1CC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2c(F)ccc(F)c2C1CC(=O)NC(=N)N
null
null
null
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
null
[]
20
CELSIUS
20
HOUR
N-[(4,7-Difluoro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 2.68 g of potassium tert-butoxide, 2.74 g of guanidinium chloride and 1.49 g of ethyl (4,7-difluoro-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate. The reaction mixture is stirred ...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
null
20
20
CCOC(=O)CC1c2c(F)ccc(F)c2C(=O)N1CC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2c(F)ccc(F)c2C1CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a79682152cf846e7b8e90f252d3d262e
CC(C)CN1C(=O)c2c(F)ccc(F)c2C1=O>>CC(C)CN1C(=O)c2c(F)ccc(F)c2C1O
FC1=C2C(C(=O)N(C2=O)CC(C)C)=C(C=C1)F.O>>FC1=C2C(N(C(C2=C(C=C1)F)=O)CC(C)C)O
[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[c:9]([F:10])[cH:11][cH:12][c:13]([F:14])[c:15]2[C:16]1=[O:17]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[c:9]([F:10])[cH:11][cH:12][c:13]([F:14])[c:15]2[CH:16]1[OH:17]
CC(C)CN1C(=O)c2c(F)ccc(F)c2C1=O
CC(C)CN1C(=O)c2c(F)ccc(F)c2C1O
null
null
[BH4-].[K+].CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
87.9
[{"value": 87.9, "product": "FC1=C2C(N(C(C2=C(C=C1)F)=O)CC(C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
3
HOUR
4,7-Difluoro-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one is prepared as described in Example 1, starting with 6.41 g of 3,6-difluoro-N-isobutylphthalimide in 70 cm3 of methanol and 1.44 g of potassium borohydride. The reaction mixture is: stirred at a temperature in the region of 20° C. for 3 hours and is then coole...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
[BH4-].[K+].CO
20
3
CC(C)CN1C(=O)c2c(F)ccc(F)c2C1=O>[BH4-].[K+].CO>CC(C)CN1C(=O)c2c(F)ccc(F)c2C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f52fc0d1191e4205b49c3b05602ca96c
CC(C)CN.O=C1OC(=O)c2c(F)ccc(F)c21>>CC(C)CN1C(=O)c2c(F)ccc(F)c2C1=O
FC1=C2C(C(=O)OC2=O)=C(C=C1)F.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>FC1=C2C(C(=O)N(C2=O)CC(C)C)=C(C=C1)F
[CH3:1][CH:2]([CH3:3])[CH2:4][NH2:5].O1[C:6](=[O:7])[c:8]2[c:9]([F:10])[cH:11][cH:12][c:13]([F:14])[c:15]2[C:16]1=[O:17]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[c:9]([F:10])[cH:11][cH:12][c:13]([F:14])[c:15]2[C:16]1=[O:17]
CC(C)CN.O=C1OC(=O)c2c(F)ccc(F)c21
CC(C)CN1C(=O)c2c(F)ccc(F)c2C1=O
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
20
CELSIUS
null
null
3,6-Difluoro-N-isobutylphthalimide is prepared as described in Example 2, starting with 5.0 g of 3,6-difluorophthalic anhydride, 2.7 cm3 of isobutylamine and a catalytic amount of para-toluenesulfonic acid in 50 cm3 of toluene. The reaction mixture is refluxed for 3 hours. After cooling to a temperature in the region o...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
20
null
CC(C)CN.O=C1OC(=O)c2c(F)ccc(F)c21>C1(=CC=CC=C1)C>CC(C)CN1C(=O)c2c(F)ccc(F)c2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-61eb84261ad642118fa00b49b9d4e4a9
CCOC(=O)CC1c2cccc(C)c2C(=O)N1CC(C)C.NC(N)=[NH2+]>>Cc1cccc2c1C(=O)N(CC(C)C)C2CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.CC1=C2C(N(C(C2=CC=C1)CC(=O)OCC)CC(C)C)=O>>C(C(C)C)N1C(C2=CC=CC(=C2C1=O)C)CC(=O)NC(=N)N
CCO[C:17]([CH2:16][CH:15]1[c:6]2[cH:5][cH:4][cH:3][c:2]([CH3:1])[c:7]2[C:8](=[O:9])[N:10]1[CH2:11][CH:12]([CH3:13])[CH3:14])=[O:18].[NH2:19][C:20]([NH2:21])=[NH2+:22]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[c:7]1[C:8](=[O:9])[N:10]([CH2:11][CH:12]([CH3:13])[CH3:14])[CH:15]2[CH2:16][C:17](=[O:18])[NH:19][C:20](=[NH:21])[...
CCOC(=O)CC1c2cccc(C)c2C(=O)N1CC(C)C.NC(N)=[NH2+]
Cc1cccc2c1C(=O)N(CC(C)C)C2CC(=O)NC(=N)N
null
null
O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
55.8
[{"value": 55.8, "product": "C(C(C)C)N1C(C2=CC=CC(=C2C1=O)C)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
20
HOUR
N-[2-(2-Isobutyl-4-methyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)-acetyl]-guanidine is prepared as described in Example 1, starting with 0.68 of potassium tert-butoxide, 0.58 g of guanidinium chloride and 0.36 g of ethyl (4-methyl-2-isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate. The reaction mixture is stirred at a t...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
O
20
20
CCOC(=O)CC1c2cccc(C)c2C(=O)N1CC(C)C.NC(N)=[NH2+]>O>Cc1cccc2c1C(=O)N(CC(C)C)C2CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2c8eea89a8d4460bbbfab07745eb889a
Cc1cccc2c1C(=O)N(CC(C)C)C2=O.O>>Cc1cccc2c1C(=O)N(CC(C)C)C2O.Cc1cccc2c1C(O)N(CC(C)C)C2=O
C(C(C)C)N1C(C=2C(C1=O)=C(C=CC2)C)=O.O>>CC=1C=CC=C2C(N(C(C12)=O)CC(C)C)O.CC1=C2C(N(C(C2=CC=C1)=O)CC(C)C)O
[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[c:7]1[C:8](=[O:9])[N:10]([CH2:11][CH:12]([CH3:13])[CH3:18])[C:15]2=[O:32].[OH2:16]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[c:7]1[C:8](=[O:9])[N:10]([CH2:11][CH:12]([CH3:13])[CH3:14])[CH:15]2[OH:16].[CH3:17][c:18]1[cH:19][cH:20][cH:21][c:22]2[c:23]1[CH:24]([OH:25])[N:26]([CH2:27][CH:...
Cc1cccc2c1C(=O)N(CC(C)C)C2=O.O
Cc1cccc2c1C(=O)N(CC(C)C)C2O.Cc1cccc2c1C(O)N(CC(C)C)C2=O
null
null
[BH4-].[K+].CO
Aromatic Heterocycle Formation
OtherReaction
80e81150c5344eb5948e5ffa5d451e70555c1fccb2813d6b936dafb1decbe38f
635345e99333bb5633c1a982d8704d75548f9c7be11489a084be362ff1b669ae
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[C;D1;H3:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[C:4]-[#7:5]1-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](:[c:10])-[C;H0;D3;+0:11]-1=[O;H0;D1;+0:12].[OH2;D0;+0:13]>>[C;D1;H3:1]-[CH;D3;+0:2](-[C;D1;H3:14])-[C:4]-[#7:5]1-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](:[c:10])-[CH;D3;+0:11]-1-[OH;D1;+0:13].[C;D1;H3:15]-[c;H0;D3;+0:3](:[c:16]:[c:17]):[c:18...
null
[]
20
CELSIUS
65
HOUR
4-Methyl-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one and 7-methyl-3-hydroxy-2-isobutyl-2,3-dihydroisoindol-1-one are prepared as described in Example 1, starting with 5.4 g of N-isobutyl-3-methylphthalimide in 20 cm3 of methanol and 1.4 g of potassium borohydride. The reaction mixture is stirred at a temperature in ...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Tertiary amide.Secondary alcohol.Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
[BH4-].[K+].CO
20
65
Cc1cccc2c1C(=O)N(CC(C)C)C2=O.O>[BH4-].[K+].CO>Cc1cccc2c1C(=O)N(CC(C)C)C2O.Cc1cccc2c1C(O)N(CC(C)C)C2=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-820aabc2f56042d9a7389117d47630dc
NCC(F)(F)F.O=C1OC(=O)c2cc(C(F)(F)F)ccc21>>O=C1c2ccc(C(F)(F)F)cc2C(=O)N1CC(F)(F)F
FC(C=1C=C2C(OC(C2=CC1)=O)=O)(F)F.FC(CN)(F)F>>FC(CN1C(C2=CC=C(C=C2C1=O)C(F)(F)F)=O)(F)F
[NH2:15][CH2:16][C:17]([F:18])([F:19])[F:20].O1[C:2](=[O:1])[c:3]2[cH:4][cH:5][c:6]([C:7]([F:8])([F:9])[F:10])[cH:11][c:12]2[C:13]1=[O:14]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][c:6]([C:7]([F:8])([F:9])[F:10])[cH:11][c:12]2[C:13](=[O:14])[N:15]1[CH2:16][C:17]([F:18])([F:19])[F:20]
NCC(F)(F)F.O=C1OC(=O)c2cc(C(F)(F)F)ccc21
O=C1c2ccc(C(F)(F)F)cc2C(=O)N1CC(F)(F)F
null
C1(=CC=C(C=C1)S(=O)(=O)O)C
CC(OCC)=O
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C:5]-[NH2;D1;+0:6].[O;D1;H0:7]=[C;H0;D3;+0:8]1-O-[C;H0;D3;+0:9](=[O;D1;H0:10])-[c:11](:[c:12]):[c:13]-1:[c:14]>>[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C:5]-[N;H0;D3;+0:6]1-[C;H0;D3;+0:8](=[O;D1;H0:7])-[c:13](:[c:14]):[c:11](:[c:12])-[C;H0;D3;+0:9]-1=[O;D1;H0:10]
80
[{"value": 80.0, "product": "FC(CN1C(C2=CC=C(C=C2C1=O)C(F)(F)F)=O)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
5.0 g of 5-trifluoromethyl-isobenzofuran-1,3-dione were dissolved using 50 ml of toluene(anhydrous) and 4.6 g of 2,2,2-trifluoro-ethylamine added. The mixture was left at ambient temperature for 16 h. 50 mg of toluene-4-sulfonic acid were then added and the mixture was refluxed for 5 h. 200 ml of EA were added and the ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=C(C=C1)S(=O)(=O)O)C.CC(OCC)=O
null
16
NCC(F)(F)F.O=C1OC(=O)c2cc(C(F)(F)F)ccc21>C1(=CC=C(C=C1)S(=O)(=O)O)C.CC(OCC)=O>O=C1c2ccc(C(F)(F)F)cc2C(=O)N1CC(F)(F)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-23a394f5306546038bf275f24874feae
O=C(O)c1ccc(C(F)(F)F)cc1C(=O)O>>O=C1OC(=O)c2cc(C(F)(F)F)ccc21
FC(C=1C=C(C(C(=O)O)=CC1)C(=O)O)(F)F.C(C)(=O)OC(C)=O>>FC(C=1C=C2C(OC(C2=CC1)=O)=O)(F)F
O[C:2](=[O:1])[c:15]1[c:6]([C:4]([OH:3])=[O:5])[cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][cH:14]1>>[O:1]=[C:2]1[O:3][C:4](=[O:5])[c:6]2[cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]21
O=C(O)c1ccc(C(F)(F)F)cc1C(=O)O
O=C1OC(=O)c2cc(C(F)(F)F)ccc21
null
null
CC(=O)O
Miscellaneous
OtherReaction
f6c3b96e71f2dd62de4cd2f6ba0ee0d42dced7c72ed20a339ce5512c7fff8e4d
22fb50577915472f1babb105381e408122dc09b3472eabb73e6e4daecfef90f6
O=C1OC(=O)c2ccccc21
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[O;H0;D2;+0:8]-[C:6](=[O;D1;H0:7])-[c:5]:[c:3]-1:[c:4]
null
[]
null
null
null
null
25.0 g of 4-trifluoromethyl-phthalic acid were dissolved in 50 ml of HOAc and 15.1 ml of acetic anhydride added. The mixture was refluxed for 6 h. The solvent was then removed in vacuo. The residue was treated three times with 50 ml of toluene each followed by the removal of the solvent in vacuo. Yield 23.1 g of a colo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid
Anhydride
null
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
HO-
CC(=O)O
null
null
O=C(O)c1ccc(C(F)(F)F)cc1C(=O)O>CC(=O)O>O=C1OC(=O)c2cc(C(F)(F)F)ccc21
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b3fcc1e7440b4a269d9af8201ea07c7b
O=C(O)c1ccc(Cl)cc1C(=O)NCCC(F)(F)F>>O=C1c2ccc(Cl)cc2C(=O)N1CCC(F)(F)F
ClC=1C=C(C(C(=O)O)=CC1)C(=O)NCCC(F)(F)F.C1(=CC=C(C=C1)S(=O)(=O)O)C>>ClC=1C=C2C(C(=O)N(C2=O)CCC(F)(F)F)=CC1
O[C:2](=[O:1])[c:3]1[cH:4][cH:5][c:6]([Cl:7])[cH:8][c:9]1[C:10](=[O:11])[NH:12][CH2:13][CH2:14][C:15]([F:16])([F:17])[F:18]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][c:6]([Cl:7])[cH:8][c:9]2[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][C:15]([F:16])([F:17])[F:18]
O=C(O)c1ccc(Cl)cc1C(=O)NCCC(F)(F)F
O=C1c2ccc(Cl)cc2C(=O)N1CCC(F)(F)F
null
null
C1(=CC=CC=C1)C
Miscellaneous
OtherReaction
d7fbb0259b6b0f12e2c885b7412dd93beb3544caef7818f594854d3230028a3d
48e6b2b999f3f15ec39998545386900040317bcbdbb4347c7e2886995a8c9772
O=C1NC(=O)c2ccccc21
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6](=[O;D1;H0:7])-[NH;D2;+0:8]-[C:9]-[C:10]>>[C:10]-[C:9]-[N;H0;D3;+0:8]1-[C:6](=[O;D1;H0:7])-[c:5]:[c:3](:[c:4])-[C;H0;D3;+0:1]-1=[O;D1;H0:2]
89.5
[{"value": 89.5, "product": "ClC=1C=C2C(C(=O)N(C2=O)CCC(F)(F)F)=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
A mixture of 5.0 g of 4-chloro-N-(3,3,3-trifluoropropyl)phthalamic acid and 30 mg of para-toluenesulfonic acid in 100 cm3 of toluene is refluxed with stirring for 7 hours. The reaction mixture is then concentrated to dryness under reduced pressure. 4.2 g of 4-chloro-N-(3,3,3-trifluoropropyl)phthalimide are thus obtaine...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amide
Substituted dicarboximide
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
null
7
O=C(O)c1ccc(Cl)cc1C(=O)NCCC(F)(F)F>C1(=CC=CC=C1)C>O=C1c2ccc(Cl)cc2C(=O)N1CCC(F)(F)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3fec2dd936f14d04bb58f9128fe4bd66
FC(F)(F)CCI.O=C1NC(=O)c2cc(Cl)ccc21>>O=C(O)c1ccc(Cl)cc1C(=O)NCCC(F)(F)F
Cl.FC(CCI)(F)F.ClC=1C=C2C(C(=O)NC2=O)=CC1.C([O-])([O-])=O.[K+].[K+]>>ClC=1C=C(C(C(=O)O)=CC1)C(=O)NCCC(F)(F)F
I[CH2:14][CH2:15][C:16]([F:17])([F:18])[F:19].[O:1]=[C:2]1[c:4]2[cH:5][cH:6][c:7]([Cl:8])[cH:9][c:10]2[C:11](=[O:12])[NH:13]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([Cl:8])[cH:9][c:10]1[C:11](=[O:12])[NH:13][CH2:14][CH2:15][C:16]([F:17])([F:18])[F:19]
FC(F)(F)CCI.O=C1NC(=O)c2cc(Cl)ccc21
O=C(O)c1ccc(Cl)cc1C(=O)NCCC(F)(F)F
null
null
O.CN(C=O)C
Acylation
OtherReaction
d630c9baaf27a4550b2c2822f6f52caf76cae5da2ce55bafe9665fa3f6a17b02
9891512d75b55e457603aea4ae9bd9289966bb585bb045450013b8407ea1727c
c1ccccc1
I-[CH2;D2;+0:1]-[C:2]-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[F;D1;H0:6].[O;D1;H0:7]=[C:8]1-[NH;D2;+0:9]-[C;H0;D3;+0:10](=[O;D1;H0:11])-[c:12](:[c:13]):[c:14]-1>>[F;D1;H0:4]-[C:3](-[F;D1;H0:5])(-[F;D1;H0:6])-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:9]-[C:8](=[O;D1;H0:7])-[c:14]:[c:12](-[C;H0;D3;+0:10](=[O;D1;H0:11])-[O;D1;H1:15]):[c:1...
105.2
[{"value": 105.2, "product": "ClC=1C=C(C(C(=O)O)=CC1)C(=O)NCCC(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
null
null
3.6 g of 1,1,1-trifluoro-3-iodopropane are added dropwise to a mixture of 7.5 g of 4-chlorophthalimide and 4.6 g of potassium carbonate in 40 cm3 of dimethylformamide at a temperature in the region of 110° C. with stirring. After stirring for 11 hours at a temperature in the region of 120° C., the reaction mixture is c...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Unsubstituted dicarboximide
Carboxylic acid.Secondary amide
c1ccc2c(c1)CNC2
null
c1ccccc1
null
O.CN(C=O)C
20
null
FC(F)(F)CCI.O=C1NC(=O)c2cc(Cl)ccc21>O.CN(C=O)C>O=C(O)c1ccc(Cl)cc1C(=O)NCCC(F)(F)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a119c77f3fcb488fb7c2f4d718a10521
NC=O.O=C1OC(=O)c2cc(Cl)ccc21>>O=C1NC(=O)c2cc(Cl)ccc21
ClC=1C=C2C(C(=O)OC2=O)=CC1.C(=O)N.O>>ClC=1C=C2C(C(=O)NC2=O)=CC1
O=C[NH2:3].O1[C:2](=[O:1])[c:12]2[c:6]([cH:7][c:8]([Cl:9])[cH:10][cH:11]2)[C:4]1=[O:5]>>[O:1]=[C:2]1[NH:3][C:4](=[O:5])[c:6]2[cH:7][c:8]([Cl:9])[cH:10][cH:11][c:12]21
NC=O.O=C1OC(=O)c2cc(Cl)ccc21
O=C1NC(=O)c2cc(Cl)ccc21
null
null
null
Acylation
OtherReaction
1b08e306e982a756f62b8091da5c6965e8ab805fb2f38ac4d4c370ba372f11cb
b1548f80df3f5850960252a7f6b180e1b02eb1ec59e1c45c5494f5aa39e38642
O=C1NC(=O)c2ccccc21
O=C-[NH2;D1;+0:1].[O;D1;H0:2]=[C;H0;D3;+0:3]1-O-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6](:[c:7]):[c:8]-1:[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:3]1-[NH;D2;+0:1]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6](:[c:7]):[c:8]-1:[c:9]
104.6
[{"value": 104.6, "product": "ClC=1C=C2C(C(=O)NC2=O)=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
3
HOUR
A solution of 10.0 g of 4-chlorophthalic anhydride in 24.6 g of formamide is heated at a temperature in the region of 120° C. with stirring for 3 hours and is then cooled to a temperature in the region of 20° C. and poured into 100 cm3 of water. After stirring for 30 minutes, the mixture is filtered and the precipitate...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amide
Unsubstituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)CNC2
c1ccc2c(c1)CNC2
HO-
null
20
3
NC=O.O=C1OC(=O)c2cc(Cl)ccc21>>O=C1NC(=O)c2cc(Cl)ccc21
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-13d23906f9bf4fdab40d38eebd64d16c
CCCN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O>>CCCNC(=O)c1ccccc1C=C(C)C(=O)OCC
C(CC)N.C(C)N(CC)CC.F[B-](F)(F)F.C(#N)C(C(=O)OCC)=NOC(=[N+](C)C)N(C)C.C(C)OC(=O)C(=CC1=C(C(=O)O)C=CC=C1)C.C(C)N(CC)CC>>CC(C(=O)OCC)=CC1=C(C=CC=C1)C(NCCC)=O
[CH3:1][CH2:2][CH2:3][NH2:4].O[C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[CH:13]=[C:14]([CH3:15])[C:16](=[O:17])[O:18][CH2:19][CH3:20]>>[CH3:1][CH2:2][CH2:3][NH:4][C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[CH:13]=[C:14]([CH3:15])[C:16](=[O:17])[O:18][CH2:19][CH3:20]
CCCN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O
CCCNC(=O)c1ccccc1C=C(C)C(=O)OCC
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6]=[C:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:7]=[C:6]-[c:5]:[c:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9]-[C:8]):[c:4]
79.9
[{"value": 79.9, "product": "CC(C(=O)OCC)=CC1=C(C=CC=C1)C(NCCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
A solution of 0.69 cm3 (5.0 mmol) of triethylamine and 1.64 g (5.0 mmol) of O-[(cyano(ethoxycarbonyl)methylene)amino]-1,1,3,3-tetramethyluronium tetrafluoroborate (“TOTU”) in 6 cm3 of dimethylformamide is added at 0° C. to a solution of 1.17 g (5.0 mmol) of 2-(2-ethoxycarbonylpropen-1-yl)benzoic acid in 10 cm3 of dimet...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
CN(C=O)C
0
0.5
CCCN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O>CN(C=O)C>CCCNC(=O)c1ccccc1C=C(C)C(=O)OCC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6b8a37e00587416cad369e3624f6633b
CCOC(=O)C(C)=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccccc1C(=O)O>>CCOC(=O)C(C)=Cc1ccccc1C(=O)O
C(=O)C1=C(C(=O)O)C=CC=C1.C1(=CC=CC=C1)P(=C(C(=O)OCC)C)(C1=CC=CC=C1)C1=CC=CC=C1>>C(C)OC(=O)C(=CC1=C(C(=O)O)C=CC=C1)C
c1ccc(P(c2ccccc2)(c2ccccc2)=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH3:7])cc1.O=[CH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[C:15](=[O:16])[OH:17]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]([CH3:7])=[CH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[C:15](=[O:16])[OH:17]
CCOC(=O)C(C)=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccccc1C(=O)O
CCOC(=O)C(C)=Cc1ccccc1C(=O)O
null
null
CN(C=O)C
C-C Coupling
Wittig reaction with triphenylphosphorane
71bd2654cede51545adee465eb47bf49794d5c57afe21c7fb122478c5a700139
203dd34a20dceaf1737adbf20e01b43c2424e4e4b1722d942d1a796d895396e6
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[O;D1;H1:7].[C:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D3;+0:12](-[C;D1;H3:13])=P(-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:8]-[#8:9]-[C:10](=[O;D1;H0:11])-[C;H0;D3;+0:12](-[C;D1;H3:13])=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]
null
[]
20
CELSIUS
1
HOUR
A mixture of 5.0 g (33.3 mmol) of 2-formylbenzoic acid and 14.5 g (40.0 mmol) of ethyl 2-(triphenylphosphanylidene)propionate in 100 cm3 of dimethylformamide is stirred at a temperature in the region of 20° C. for 1 hour. After removal of the solvent, the residue is dissolved in dichloromethane and then extracted twice...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Ester
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1
HO-
CN(C=O)C
20
1
CCOC(=O)C(C)=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=Cc1ccccc1C(=O)O>CN(C=O)C>CCOC(=O)C(C)=Cc1ccccc1C(=O)O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f35e3b4b3d3c485d9652df08ba3abb70
CCCCNC(=O)c1ccccc1C=C(C)C(=O)OCC.NC(N)=[NH2+]>>CCCCN1C(=O)c2ccccc2C1C(C)C(=O)NC(=N)N
C(CCC)NC(=O)C1=C(C=CC=C1)C=C(C(=O)OCC)C.[Cl-].NC(=[NH2+])N.CC(C)([O-])C.[K+]>>C(CCC)N1C(C2=CC=CC=C2C1=O)C(C(=O)NC(=N)N)C
CCO[C:17]([C:15](=[CH:14][c:13]1[c:8]([C:6]([NH:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:7])[cH:9][cH:10][cH:11][cH:12]1)[CH3:16])=[O:18].[NH2:19][C:20]([NH2:21])=[NH2+:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH:14]1[CH:15]([CH3:16])[C:17](=[O:18])[NH:19][C:20](=[NH:21])[N...
CCCCNC(=O)c1ccccc1C=C(C)C(=O)OCC.NC(N)=[NH2+]
CCCCN1C(=O)c2ccccc2C1C(C)C(=O)NC(=N)N
null
null
CN(C=O)C
Acylation
OtherReaction
dcf49378e6619ff85ba9e749476a6064de1ac232fdca8843859076840b880ae5
bfdf9d8794c4f418c67cbf27cf7a81922d1c4e071347e361c5160485b9471d6e
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-[C;D1;H3:4])=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]-[C:9](=[O;D1;H0:10])-[NH;D2;+0:11]-[C:12]-[C:13].[NH2+;D1:14]=[C;H0;D3;+0:15](-[NH2;D1;+0:16])-[NH2;D1;+0:17]>>[C:13]-[C:12]-[N;H0;D3;+0:11]1-[C:9](=[O;D1;H0:10])-[c:8]:[c:6](:[c:7])-[CH;D3;+0:5]-1-[CH;D3;+0:3](-[C;D1;H3:4]...
93.1
[{"value": 93.1, "product": "C(CCC)N1C(C2=CC=CC=C2C1=O)C(C(=O)NC(=N)N)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
45
MINUTE
N-[2-(2-Butyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)propionyl]guanidine is prepared as described in Example 30, starting with 3.63 g (38.0 mmol) of guanidinium chloride in 20 cm3 of dimethylformamide and 3.84 g (34.2 mmol) of potassium tert-butoxide. The mixture is stirred for 45 minutes at a temperature in the region of ...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester.Secondary amide
Secondary amide.Tertiary amide.Primary amine
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
CN(C=O)C
20
0.75
CCCCNC(=O)c1ccccc1C=C(C)C(=O)OCC.NC(N)=[NH2+]>CN(C=O)C>CCCCN1C(=O)c2ccccc2C1C(C)C(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a9829b5a2b6d4b1e89b997d8209c3e25
CCCCN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O>>CCCCNC(=O)c1ccccc1C=C(C)C(=O)OCC
C(C)OC(=O)C(=CC1=C(C(=O)O)C=CC=C1)C.C(C)N(CC)CC.F[B-](F)(F)F.C(#N)C(C(=O)OCC)=NOC(=[N+](C)C)N(C)C.C(CCC)N.C(C)N(CC)CC>>C(CCC)NC(=O)C1=C(C=CC=C1)C=C(C(=O)OCC)C
[CH3:1][CH2:2][CH2:3][CH2:4][NH2:5].O[C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[CH:14]=[C:15]([CH3:16])[C:17](=[O:18])[O:19][CH2:20][CH3:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[CH:14]=[C:15]([CH3:16])[C:17](=[O:18])[O:19][CH2:20][CH3:21]
CCCCN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O
CCCCNC(=O)c1ccccc1C=C(C)C(=O)OCC
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6]=[C:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:7]=[C:6]-[c:5]:[c:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9]-[C:8]):[c:4]
78.1
[{"value": 78.1, "product": "C(CCC)NC(=O)C1=C(C=CC=C1)C=C(C(=O)OCC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Ethyl 3-(2-butylcarbamoylphenyl)-2-methylacrylate is prepared as described in Example 30, starting with 1.17 g (5.0 mmol) of 2-(2-ethoxycarbonylpropen-1-yl)benzoic acid in 10 cm3 of dimethylformamide, a solution of 0.69 cm3 (5.0 mmol) of triethylamine, 1.64 g (5.0 mmol) of O-[(cyano(ethoxycarbonyl)methylene)amino]-1,1,...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
CN(C=O)C
null
null
CCCCN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O>CN(C=O)C>CCCCNC(=O)c1ccccc1C=C(C)C(=O)OCC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e9998e321b44409ca8f8cc9686415b43
CCOC(=O)C(C)=Cc1ccccc1C(=O)NCC(C)C.NC(N)=[NH2+]>>CC(C)CN1C(=O)c2ccccc2C1C(C)C(=O)NC(=N)N
C(C(C)C)NC(=O)C1=C(C=CC=C1)C=C(C(=O)OCC)C.[Cl-].NC(=[NH2+])N.CC(C)([O-])C.[K+]>>C(C(C)C)N1C(C2=CC=CC=C2C1=O)C(C(=O)NC(=N)N)C
CCO[C:17]([C:15](=[CH:14][c:13]1[c:8]([C:6]([NH:5][CH2:4][CH:2]([CH3:1])[CH3:3])=[O:7])[cH:9][cH:10][cH:11][cH:12]1)[CH3:16])=[O:18].[NH2:19][C:20]([NH2:21])=[NH2+:22]>>[CH3:1][CH:2]([CH3:3])[CH2:4][N:5]1[C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[CH:14]1[CH:15]([CH3:16])[C:17](=[O:18])[NH:19][C:20](=[NH:21])...
CCOC(=O)C(C)=Cc1ccccc1C(=O)NCC(C)C.NC(N)=[NH2+]
CC(C)CN1C(=O)c2ccccc2C1C(C)C(=O)NC(=N)N
null
null
CN(C=O)C
Acylation
OtherReaction
dcf49378e6619ff85ba9e749476a6064de1ac232fdca8843859076840b880ae5
bfdf9d8794c4f418c67cbf27cf7a81922d1c4e071347e361c5160485b9471d6e
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D3;+0:3](-[C;D1;H3:4])=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]-[C:9](=[O;D1;H0:10])-[NH;D2;+0:11]-[C:12]-[C:13].[NH2+;D1:14]=[C;H0;D3;+0:15](-[NH2;D1;+0:16])-[NH2;D1;+0:17]>>[C:13]-[C:12]-[N;H0;D3;+0:11]1-[C:9](=[O;D1;H0:10])-[c:8]:[c:6](:[c:7])-[CH;D3;+0:5]-1-[CH;D3;+0:3](-[C;D1;H3:4]...
73.1
[{"value": 73.1, "product": "C(C(C)C)N1C(C2=CC=CC=C2C1=O)C(C(=O)NC(=N)N)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
45
MINUTE
N-[2-(2-Isobutyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)propionyl]guanidine is prepared as described in Example 30, starting with 3.73 g (39.0 mmol) of guanidinium chloride in 20 cm3 of dimethylformamide and 3.94 g (35.1 mmol) of potassium tert-butoxide. The mixture is stirred for 45 minutes at a temperature in the region ...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester.Secondary amide
Secondary amide.Tertiary amide.Primary amine
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
CN(C=O)C
20
0.75
CCOC(=O)C(C)=Cc1ccccc1C(=O)NCC(C)C.NC(N)=[NH2+]>CN(C=O)C>CC(C)CN1C(=O)c2ccccc2C1C(C)C(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4367c72295bc4b1ba1276fa164677eda
CC(C)CN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O>>CCOC(=O)C(C)=Cc1ccccc1C(=O)NCC(C)C
C(C)OC(=O)C(=CC1=C(C(=O)O)C=CC=C1)C.C(C)N(CC)CC.F[B-](F)(F)F.C(#N)C(C(=O)OCC)=NOC(=[N+](C)C)N(C)C.C(C(C)C)N.C(C)N(CC)CC>>C(C(C)C)NC(=O)C1=C(C=CC=C1)C=C(C(=O)OCC)C
[NH2:17][CH2:18][CH:19]([CH3:20])[CH3:21].O[C:15]([c:14]1[c:9]([CH:8]=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH3:7])[cH:10][cH:11][cH:12][cH:13]1)=[O:16]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]([CH3:7])=[CH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[C:15](=[O:16])[NH:17][CH2:18][CH:19]([CH3:20])[CH3:21]
CC(C)CN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O
CCOC(=O)C(C)=Cc1ccccc1C(=O)NCC(C)C
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6]=[C:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6]=[C:7]
79.5
[{"value": 79.5, "product": "C(C(C)C)NC(=O)C1=C(C=CC=C1)C=C(C(=O)OCC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Ethyl 3-(2-isobutylcarbamoylphenyl)-2-methylacrylate is prepared as described in Example 30, starting with 1.17 g (5.0 mmol) of 2-(2-ethoxycarbonylpropen-1-yl)benzoic acid in 10 cm3 of dimethylformamide, a solution of 0.69 cm3 (5.0 mmol) of triethylamine, 1.64 g (5.0 mmol) of O-[(cyano(ethoxycarbonyl)methylene)amino]-1...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
CN(C=O)C
null
null
CC(C)CN.CCOC(=O)C(C)=Cc1ccccc1C(=O)O>CN(C=O)C>CCOC(=O)C(C)=Cc1ccccc1C(=O)NCC(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a4fe38235e304d6b9283db789fffcca0
CCOC(=O)C(C)=Cc1ccccc1C(=O)O.NCCO>>CCOC(=O)C(C)=Cc1ccccc1C(=O)NCCO
C(O)CN.C(C)N(CC)CC.F[B-](F)(F)F.C(#N)C(C(=O)OCC)=NOC(=[N+](C)C)N(C)C.C(C)N(CC)CC.C(C)OC(=O)C(=CC1=C(C(=O)O)C=CC=C1)C>>OCCNC(=O)C1=C(C=CC=C1)C=C(C(=O)OCC)C
O[C:15]([c:14]1[c:9]([CH:8]=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH3:7])[cH:10][cH:11][cH:12][cH:13]1)=[O:16].[NH2:17][CH2:18][CH2:19][OH:20]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]([CH3:7])=[CH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[C:15](=[O:16])[NH:17][CH2:18][CH2:19][OH:20]
CCOC(=O)C(C)=Cc1ccccc1C(=O)O.NCCO
CCOC(=O)C(C)=Cc1ccccc1C(=O)NCCO
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6]=[C:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]-[C:6]=[C:7]
null
[]
null
null
null
null
Ethyl 3-[2-(2-hydroxyethylcarbamoyl)phenyl]-2-methylacrylate is prepared as described in Example 30, starting with 1.17 g (5.0 mmol) of 2-(2-ethoxycarbonylpropen-1-yl)benzoic acid in 10 cm3 of dimethylformamide, a solution of 0.69 cm3 (5.0 mmol) of triethylamine and 1.64 g (5.0 mmol) of O-[(cyano(ethoxycarbonyl)methyle...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
CN(C=O)C
null
null
CCOC(=O)C(C)=Cc1ccccc1C(=O)O.NCCO>CN(C=O)C>CCOC(=O)C(C)=Cc1ccccc1C(=O)NCCO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b94f6d23a63143b8aab50c54215d1082
CCOC(=O)CC1c2ccc(C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>>Cc1ccc2c(c1)C(=O)N(CC(C)C)C2CC(=O)NC(=N)N
CC(C)([O-])C.[K+].[Cl-].NC(=[NH2+])N.C(C(C)C)N1C(C2=CC=C(C=C2C1=O)C)CC(=O)OCC>>C(C(C)C)N1C(C2=CC=C(C=C2C1=O)C)CC(=O)NC(=N)N
CCO[C:17]([CH2:16][CH:15]1[c:5]2[cH:4][cH:3][c:2]([CH3:1])[cH:7][c:6]2[C:8](=[O:9])[N:10]1[CH2:11][CH:12]([CH3:13])[CH3:14])=[O:18].[NH2:19][C:20]([NH2:21])=[NH2+:22]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7]1)[C:8](=[O:9])[N:10]([CH2:11][CH:12]([CH3:13])[CH3:14])[CH:15]2[CH2:16][C:17](=[O:18])[NH:19][C:20](=[NH:21]...
CCOC(=O)CC1c2ccc(C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]
Cc1ccc2c(c1)C(=O)N(CC(C)C)C2CC(=O)NC(=N)N
null
null
O
Acylation
OtherReaction
2a0d0bb811d7d0d78ab0e0e0dd422aa0d95347cc6185304b02293baab0b54666
bd0631f52f11765fc496c7945dc73cbc70f74ea4cf87d492a8fafb124a54fd13
O=C1NCc2ccccc21
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#7:5].[NH2+;D1:6]=[C;H0;D3;+0:7](-[NH2;D1;+0:8])-[NH2;D1;+0:9]>>[#7:5]-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C;H0;D3;+0:7](-[NH2;D1;+0:6])=[NH;D1;+0:9]
70.2
[{"value": 70.2, "product": "C(C(C)C)N1C(C2=CC=C(C=C2C1=O)C)CC(=O)NC(=N)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
40
HOUR
N-[(2-Isobutyl-5-methyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetyl]guanidine is prepared as described in Example 1, starting with 1.75 g of potassium tert-butoxide, 1.78 g of guanidinium chloride and 0.9 g of ethyl (2-isobutyl-5-methyl-3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetate. The reaction mixture is stirred at a temp...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Amidinium.Ester
Secondary amide.Primary amine
null
null
c1ccc2c(c1)C[NH]C2
HO-
O
20
40
CCOC(=O)CC1c2ccc(C)cc2C(=O)N1CC(C)C.NC(N)=[NH2+]>O>Cc1ccc2c(c1)C(=O)N(CC(C)C)C2CC(=O)NC(=N)N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7818423844994ab0963b37067607d149
Cc1ccc2c(c1)C(=O)N(CC(C)C)C2=O.O>>Cc1ccc2c(c1)C(=O)N(CC(C)C)C2O.Cc1ccc2c(c1)C(O)N(CC(C)C)C2=O
O.C(C(C)C)N1C(C=2C(C1=O)=CC(=CC2)C)=O>>OC1N(C(C2=CC=C(C=C12)C)=O)CC(C)C.OC1N(C(C2=CC(=CC=C12)C)=O)CC(C)C
[CH3:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7]1)[C:8](=[O:9])[N:10]([CH2:11][CH:12]([CH3:13])[CH3:18])[C:15]2=[O:16].[OH2:25]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7]1)[C:8](=[O:9])[N:10]([CH2:11][CH:12]([CH3:13])[CH3:14])[CH:15]2[OH:16].[CH3:17][c:18]1[cH:19][cH:20][c:21]2[c:22]([cH:23]1)[CH:24]([OH:25])[N:26]([CH2:2...
Cc1ccc2c(c1)C(=O)N(CC(C)C)C2=O.O
Cc1ccc2c(c1)C(=O)N(CC(C)C)C2O.Cc1ccc2c(c1)C(O)N(CC(C)C)C2=O
null
null
[BH4-].[K+].CO
Aromatic Heterocycle Formation
OtherReaction
80e81150c5344eb5948e5ffa5d451e70555c1fccb2813d6b936dafb1decbe38f
635345e99333bb5633c1a982d8704d75548f9c7be11489a084be362ff1b669ae
O=C1NCc2ccccc21.O=C1NCc2ccccc21
[C;D1;H3:1]-[CH;D3;+0:2](-[CH3;D1;+0:3])-[C:4]-[#7:5]1-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](:[c:10])-[C;H0;D3;+0:11]-1=[O;H0;D1;+0:12].[OH2;D0;+0:13]>>[#7:14]-[C:15](-[OH;D1;+0:13])-[c:16]:[c:17]:[c;H0;D3;+0:3](-[C;D1;H3:18]):[c:19]:[c:20].[C;D1;H3:1]-[CH;D3;+0:2](-[C;D1;H3:21])-[C:4]-[#7:5]1-[C:6](=[O;D1;H0:7])-[c:8]:[c:9]...
null
[]
20
CELSIUS
16
HOUR
3-Hydroxy-2-isobutyl-5-methyl-2,3-dihydroisoindol-1-one and 3-hydroxy-2-isobutyl-6-methyl-2,3-dihydroisoindol-1-one are prepared as described in Example 1, starting with 6.7 g of N-isobutyl-4-methylphthalimide in 65 cm3 of methanol and 1.7 g of potassium borohydride. The reaction mixture is stirred at a temperature in ...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Tertiary amide.Secondary alcohol.Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccc2c(c1)C[NH]C2
Other
[BH4-].[K+].CO
20
16
Cc1ccc2c(c1)C(=O)N(CC(C)C)C2=O.O>[BH4-].[K+].CO>Cc1ccc2c(c1)C(=O)N(CC(C)C)C2O.Cc1ccc2c(c1)C(O)N(CC(C)C)C2=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8d0acc1108a0435e9315b9e987106bc9
CC(C)CN.Cc1ccc2c(c1)C(=O)OC2=O>>Cc1ccc2c(c1)C(=O)N(CC(C)C)C2=O
CC=1C=C2C(C(=O)OC2=O)=CC1.C(C(C)C)N.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C(C(C)C)N1C(C=2C(C1=O)=CC(=CC2)C)=O
[NH2:10][CH2:11][CH:12]([CH3:13])[CH3:14].O1[C:8](=[O:9])[c:6]2[c:5]([cH:4][cH:3][c:2]([CH3:1])[cH:7]2)[C:15]1=[O:16]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[c:6]([cH:7]1)[C:8](=[O:9])[N:10]([CH2:11][CH:12]([CH3:13])[CH3:14])[C:15]2=[O:16]
CC(C)CN.Cc1ccc2c(c1)C(=O)OC2=O
Cc1ccc2c(c1)C(=O)N(CC(C)C)C2=O
null
null
C1(=CC=CC=C1)C
Acylation
Phthalic anhydride to phthalimide
c3c986d6e09320348d40a4a59ca107882ce771f249842049dc55e55f334c675b
2bbbf7b24648445e31d33a2a26f8618c2067bd23957587cc459f3c45a03ed48a
O=C1NC(=O)c2ccccc21
[C:1]-[C:2]-[NH2;D1;+0:3].[O;D1;H0:4]=[C;H0;D3;+0:5]1-O-[C;H0;D3;+0:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C;H0;D3;+0:5](=[O;D1;H0:4])-[c:10](:[c:11]):[c:8](:[c:9])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
140
CELSIUS
null
null
N-Isobutyl-4-methylphthalimide is prepared as described in Example 2, starting with 6.0 g of 4-methylphthalic anhydride, 3.7 cm3 of isobutylamine and a catalytic amount of para-toluenesulphonic acid in 60 cm3 of toluene. The reaction mixture is heated at a temperature in the region of 140° C. for three hours and is the...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Ester.Ester.Primary amine
Substituted dicarboximide
c1ccc2c(c1)COC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
C1(=CC=CC=C1)C
140
null
CC(C)CN.Cc1ccc2c(c1)C(=O)OC2=O>C1(=CC=CC=C1)C>Cc1ccc2c(c1)C(=O)N(CC(C)C)C2=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a67c2ef8ada640688782f3602f512067
CCOC(=O)CP(=O)(OCC)OCC.CS(=O)(=O)c1ccc2c(c1)C(O)N(CC(F)(F)F)C2=O>>CCOC(=O)CC1c2cc(S(C)(=O)=O)ccc2C(=O)N1CC(F)(F)F
[H-].[Na+].OC1N(C(C2=CC=C(C=C12)S(=O)(=O)C)=O)CC(F)(F)F.CC(OCC)=O.C(C)OC(CP(=O)(OCC)OCC)=O>>C(C)OC(CC1N(C(C2=CC=C(C=C12)S(=O)(=O)C)=O)CC(F)(F)F)=O
CCOP(=O)(OCC)[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].O[CH:7]1[c:8]2[cH:9][c:10]([S:11]([CH3:12])(=[O:13])=[O:14])[cH:15][cH:16][c:17]2[C:18](=[O:19])[N:20]1[CH2:21][C:22]([F:23])([F:24])[F:25]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH:7]1[c:8]2[cH:9][c:10]([S:11]([CH3:12])(=[O:13])=[O:14])[cH:15][cH:16][c:17]2[C:18](...
CCOC(=O)CP(=O)(OCC)OCC.CS(=O)(=O)c1ccc2c(c1)C(O)N(CC(F)(F)F)C2=O
CCOC(=O)CC1c2cc(S(C)(=O)=O)ccc2C(=O)N1CC(F)(F)F
null
null
COCCOC
C-C Coupling
OtherReaction
f15997e17baabc84ad1f24d90439ac1e1bf9c091e3c8b61c6d23db78bb59ba96
ec740fdba0adc3c659d56447beb3ee7a35d222db2ebbeacae7f761e1e85567b3
O=C1NCc2ccccc21
C-C-O-P(=O)(-O-C-C)-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].O-[CH;D3;+0:6]1-[#7:7](-[C:8])-[C:9](=[O;D1;H0:10])-[c:11]:[c:12]-1:[c:13]>>[C:8]-[#7:7]1-[C:9](=[O;D1;H0:10])-[c:11]:[c:12](:[c:13])-[CH;D3;+0:6]-1-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5]
null
[]
null
null
1
HOUR
0.56 g of a 60% suspension of NaH in mineral oil were suspended in 20 ml of DME. Afterwards, 2.8 ml of (diethoxy-phosphoryl)-acetic acid ethyl ester were added dropwise at ambient temperature and the mixture stirred for 1 h at that temperature. A solution prepared of 3-hydroxy-5-methanesulfonyl-2-(2,2,2-trifluoro-ethyl...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol
Ester
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
HO-
COCCOC
null
1
CCOC(=O)CP(=O)(OCC)OCC.CS(=O)(=O)c1ccc2c(c1)C(O)N(CC(F)(F)F)C2=O>COCCOC>CCOC(=O)CC1c2cc(S(C)(=O)=O)ccc2C(=O)N1CC(F)(F)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5390950b57c245ada9df498f35e40b07
CS(=O)(=O)c1ccc2c(c1)C(=O)N(CC(F)(F)F)C2=O>>CS(=O)(=O)c1ccc2c(c1)C(O)N(CC(F)(F)F)C2=O
CS(=O)(=O)C=1C=C2C(N(C(C2=CC1)=O)CC(F)(F)F)=O.CO>>OC1N(C(C2=CC=C(C=C12)S(=O)(=O)C)=O)CC(F)(F)F
[CH3:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[C:11](=[O:12])[N:13]([CH2:14][C:15]([F:16])([F:17])[F:18])[C:19]2=[O:20]>>[CH3:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[CH:11]([OH:12])[N:13]([CH2:14][C:15]([F:16])([F:17])[F:18])[C:19]2=[O:20]
CS(=O)(=O)c1ccc2c(c1)C(=O)N(CC(F)(F)F)C2=O
CS(=O)(=O)c1ccc2c(c1)C(O)N(CC(F)(F)F)C2=O
null
null
O
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1NCc2ccccc21
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
40.9
[{"value": 40.9, "product": "OC1N(C(C2=CC=C(C=C12)S(=O)(=O)C)=O)CC(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
3.4 g of 5-methanesulfonyl-2-(2,2,2-trifluoro-ethyl)-isoindole-1,3-dione were dissolved using 240 ml of MeOH. 0.63 g of KBH4 were then added in small portions at ambient temperature. The reaction mixture was stirred for 20 h at ambient temperature and subsequently poured into 1 l of water at 0° C. The aqueous layer was...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
null
O
null
20
CS(=O)(=O)c1ccc2c(c1)C(=O)N(CC(F)(F)F)C2=O>O>CS(=O)(=O)c1ccc2c(c1)C(O)N(CC(F)(F)F)C2=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b1499d818a0a41168cce09489ab320a9
CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC1CC1>>O=C(O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC1CC1
C(C)OC(CC1N(C(C2=CC=C(C=C12)C(F)(F)F)=O)CC1CC1)=O.[OH-].[Na+]>>C1(CC1)CN1C(C2=CC(=CC=C2C1=O)C(F)(F)F)CC(=O)O
CC[O:3][C:2](=[O:1])[CH2:4][CH:5]1[c:6]2[cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]2[C:16](=[O:17])[N:18]1[CH2:19][CH:20]1[CH2:21][CH2:22]1>>[O:1]=[C:2]([OH:3])[CH2:4][CH:5]1[c:6]2[cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][cH:14][c:15]2[C:16](=[O:17])[N:18]1[CH2:19][CH:20]1[CH2:21][CH2:22]1
CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC1CC1
O=C(O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC1CC1
null
null
C(C)O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1c2ccccc2CN1CC1CC1
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
38.1
[{"value": 38.1, "product": "C1(CC1)CN1C(C2=CC(=CC=C2C1=O)C(F)(F)F)CC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
1.0 g of (2-cyclopropylmethyl-3-oxo-6-trifluoromethyl-2,3-dihydro-1H-isoindol-1-yl)acetic acid ethyl ester were dissolved using 10 ml of ethanol and 3.5 ml of a 1 N aqueous solution of NaOH added. The mixture was stirred for 3 h at ambient temperature and then the solvent removed in vacuo. Afterwards, 30 ml of water we...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2c(c1)C[NH]C2.C1CC1
Other
C(C)O
null
3
CCOC(=O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC1CC1>C(C)O>O=C(O)CC1c2cc(C(F)(F)F)ccc2C(=O)N1CC1CC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-49d1b00280dc4566a34df497dbc0ccdf
COc1cc(C=CC(=O)c2cc(OC)c(OC)c(OC)c2)cc(Br)c1OC.OB(O)c1cccs1>>COc1cc(C(=O)C=Cc2cc(OC)c(OC)c(-c3cccs3)c2)cc(OC)c1OC
O.S1C(=CC=C1)B(O)O.C([O-])([O-])=O.[Na+].[Na+].BrC=1C=C(C=C(C1OC)OC)C=CC(=O)C1=CC(=C(C(=C1)OC)OC)OC>>COC=1C=C(C=C(C1OC)C=1SC=CC1)C=CC(=O)C1=CC(=C(C(=C1)OC)OC)OC
Br[c:26]1[cH:25][c:5]([CH:6]=[CH:8][C:9](=[O:7])[c:10]2[cH:11][c:12]([O:13][CH3:14])[c:15]([O:16][CH3:17])[c:18]([O:27][CH3:28])[cH:24]2)[cH:4][c:3]([O:2][CH3:1])[c:29]1[O:30][CH3:31].OB(O)[c:19]1[cH:20][cH:21][cH:22][s:23]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[CH:8]=[CH:9][c:10]2[cH:11][c:12]([O:13][CH3:14])[c...
COc1cc(C=CC(=O)c2cc(OC)c(OC)c(OC)c2)cc(Br)c1OC.OB(O)c1cccs1
COc1cc(C(=O)C=Cc2cc(OC)c(OC)c(-c3cccs3)c2)cc(OC)c1OC
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
COCCOC
C-C Coupling
Suzuki coupling with boronic acids
b91b99e20230b8ee23ff9c0be751d7e6e9088c9bf2e3c3634cb219f57c76935c
3574f5ee80f247e8e9144c7409a97dc71fd4c3d1727016fd405b163a1bb17c74
O=C(C=Cc1cccc(-c2cccs2)c1)c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3](-[CH;D2;+0:4]=[CH;D2;+0:5]-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-[c:8]2:[c:9]:[c:10]:[c:11](-[#8:12]):[c;H0;D3;+0:13](-[O;H0;D2;+0:14]-[C;D1;H3:15]):[c:16]:2):[c:17]:[c:18]:[c:19]:1-[#8:20].O-B(-O)-[c;H0;D3;+0:21]1:[#16;a:22]:[c:23]:[c:24]:[c:25]:1>>[#8:12]-[c:11]1:[c:10]:[c:9]:[c:8](-[CH;D2;+0...
90
[{"value": 90.0, "product": "COC=1C=C(C=C(C1OC)C=1SC=CC1)C=CC(=O)C1=CC(=C(C(=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.7, "product": "COC=1C=C(C=C(C1OC)C=1SC=CC1)C=CC(=O)C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
3-(3-Bromo-4,5-dimethoxyphenyl)-1-(3,4,5-trimethoxyphenyl)-2-propen-1-one (0.105 g, 0.2 mmol) from Ex-1A was dissolved in ethylene glycol dimethyl ether (20 mL). Tetrakis(triphenylphosphine)palladium(0) (0.116 g, 0.1 mmol) was added, and the mixture was stirred at room temperature under nitrogen for 5 min. 2-Thiopheneb...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Ether.Boronic acid
Ketone.Ether
c1ccccc1.c1ccccc1.c1ccsc1
c1ccccc1.c1ccccc1.c1ccsc1
c1ccccc1.c1ccccc1.c1ccsc1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC
null
0.083333
COc1cc(C=CC(=O)c2cc(OC)c(OC)c(OC)c2)cc(Br)c1OC.OB(O)c1cccs1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC>COc1cc(C(=O)C=Cc2cc(OC)c(OC)c(-c3cccs3)c2)cc(OC)c1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-099c434db9f545c5b23d9e1b226a3eb0
COc1cc(OC)c(C=O)cc1Br.OB(O)c1cc2ccccc2s1>>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O
O.S1C2=C(C=C1B(O)O)C=CC=C2.C([O-])([O-])=O.[Na+].[Na+].BrC=1C(=CC(=C(C=O)C1)OC)OC>>S1C2=C(C=C1C=1C(=CC(=C(C=O)C1)OC)OC)C=CC=C2
Br[c:8]1[c:5]([O:6][CH3:7])[cH:4][c:3]([O:2][CH3:1])[c:19]([CH:20]=[O:21])[cH:18]1.OB(O)[c:9]1[cH:10][c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[s:17]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[c:8](-[c:9]2[cH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[s:17]2)[cH:18][c:19]1[CH:20]=[O:21]
COc1cc(OC)c(C=O)cc1Br.OB(O)c1cc2ccccc2s1
COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
COCCOC
C-C Coupling
Suzuki coupling with boronic acids
a1259a94b31ac9f1988cb839e0910c5b2437b7522341904299ff46277eacea87
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2cc3ccccc3s2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]-[C:4]=[O;D1;H0:5]):[c:6](-[#8:7]):[c:8].O-B(-O)-[c;H0;D3;+0:9]1:[#16;a:10]:[c:11]:[c:12]:[c:13]:1>>[#8:7]-[c:6](:[c:8]):[c;H0;D3;+0:1](-[c;H0;D3;+0:9]1:[#16;a:10]:[c:11]:[c:12]:[c:13]:1):[c:2]:[c:3]-[C:4]=[O;D1;H0:5]
83
[{"value": 83.0, "product": "S1C2=C(C=C1C=1C(=CC(=C(C=O)C1)OC)OC)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.6, "product": "S1C2=C(C=C1C=1C(=CC(=C(C=O)C1)OC)OC)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
Ex-6A: 5-Bromo-2,4-dimethoxybenzaldehyde (4.9 g, 20.0 mmol) was dissolved in ethylene glycol dimethyl ether (50 mL). Tetrakis(triphenylphosphine)palladium(0) (2.32 g, 2 mmol) was added, and the mixture was stirred at room temperature under nitrogen for 5 min. Benzo[b]thiophene-2-boronic acid (4.27 g, 24 mmol) and sodiu...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccc2sccc2c1
c1ccccc1.c1ccc2sccc2c1
c1ccccc1.c1ccc2sccc2c1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC
null
0.083333
COc1cc(OC)c(C=O)cc1Br.OB(O)c1cc2ccccc2s1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-98b804334ce24a75927b047571b456ff
COc1cc(C(C)=O)cc(OC)c1OC.COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O>>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(OC)c(OC)c1
COC=1C=C(C=C(C1OC)OC)C(C)=O.[OH-].[Na+].S1C2=C(C=C1C=1C(=CC(=C(C=O)C1)OC)OC)C=CC=C2>>S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1=CC(=C(C(=C1)OC)OC)OC)OC)OC)C=CC=C2
[CH3:21][C:22](=[O:23])[c:24]1[cH:25][c:26]([O:27][CH3:28])[c:29]([O:30][CH3:31])[c:32]([O:33][CH3:34])[cH:35]1.O=[CH:20][c:19]1[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH3:7])[c:8](-[c:9]2[cH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[s:17]2)[cH:18]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[c:8](-[c:9]2[cH:10][c:11...
COc1cc(C(C)=O)cc(OC)c1OC.COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O
COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(OC)c(OC)c1
null
null
C(C)O
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
O=C(C=Cc1cccc(-c2cc3ccccc3s2)c1)c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[O;D1;H0:7]=[C:6](-[c:8])-[CH;D2;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
92
[{"value": 92.0, "product": "S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1=CC(=C(C(=C1)OC)OC)OC)OC)OC)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.0, "product": "S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1=CC(=C(C(=C1)OC)OC)OC)OC)OC)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
3′,4′,5′-Trimethoxyacetophenone (1.62 g, 7.7 mmol) was dissolved in ethanol (50 mL). Sodium hydroxide solution (50%, 4 mL) was added and the mixture was stirred at room temperature for 30 minutes. 5-(Benzo[b]thien-2-yl)-2,4-dimethoxybenzaldehyde (2.2 g, 7.7 mmol) from Ex-6A was added, and the mixture was stirred at roo...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1.c1ccc2sccc2c1.c1ccccc1
HO-
C(C)O
null
0.5
COc1cc(C(C)=O)cc(OC)c1OC.COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O>C(C)O>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(OC)c(OC)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-754c7a9dc18444ce999681af4bf22fa9
COc1cc(I)ccc1C(C)=O.OB(O)c1cccs1>>COc1cc(-c2cccs2)ccc1C(C)=O
O.S1C(=CC=C1)B(O)O.C([O-])([O-])=O.[Na+].[Na+].IC1=CC(=C(C=C1)C(C)=O)OC>>COC1=C(C=CC(=C1)C=1SC=CC1)C(C)=O
I[c:5]1[cH:4][c:3]([O:2][CH3:1])[c:13]([C:14]([CH3:15])=[O:16])[cH:12][cH:11]1.OB(O)[c:6]1[cH:7][cH:8][cH:9][s:10]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][s:10]2)[cH:11][cH:12][c:13]1[C:14]([CH3:15])=[O:16]
COc1cc(I)ccc1C(C)=O.OB(O)c1cccs1
COc1cc(-c2cccs2)ccc1C(C)=O
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
COCCOC
C-C Coupling
Suzuki coupling with boronic acids
a9e750b5cb26673fc488a731642519fa5963d6a2e4d2eeb976470c7f17606def
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2cccs2)cc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].O-B(-O)-[c;H0;D3;+0:6]1:[#16;a:7]:[c:8]:[c:9]:[c:10]:1>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6]1:[#16;a:7]:[c:8]:[c:9]:[c:10]:1):[c:4]:[c:5]
98
[{"value": 98.0, "product": "COC1=C(C=CC(=C1)C=1SC=CC1)C(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.1, "product": "COC1=C(C=CC(=C1)C=1SC=CC1)C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Ex-57a: 4′-iodo-2′-methoxyacetophenone (1.08 g, 3.9 mmol) in ethylene glycol dimethyl ether (50 ml) was degassed for 15 minutes. Tetrakis(triphenylphosphine)palladium(0) (0.456 g, 0.39 mmol), thiophene-2-boronic acid (0.75 g, 5.9 mmol), and sodium carbonate solution (2 m, 4 ml, 8 mmol) were added. The mixture was stirr...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccsc1
c1ccccc1.c1ccsc1
c1ccccc1.c1ccsc1
HI.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC
null
null
COc1cc(I)ccc1C(C)=O.OB(O)c1cccs1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.COCCOC>COc1cc(-c2cccs2)ccc1C(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-080b4e4ea4564d1bb6cac95e8adafada
COc1cc(-c2cccs2)ccc1C(C)=O.O=Cc1ccc(F)c(F)c1>>COc1cc(-c2cccs2)ccc1C(=O)C=Cc1ccc(F)c(F)c1
COC1=C(C=CC(=C1)C=1SC=CC1)C(C)=O.FC=1C=C(C=O)C=CC1F.C([O-])([O-])=O.[Cs+].[Cs+]>>FC=1C=C(C=CC1F)C=CC(=O)C1=C(C=C(C=C1)C=1SC=CC1)OC
[CH3:1][O:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][s:10]2)[cH:11][cH:12][c:13]1[C:14](=[O:15])[CH3:16].O=[CH:17][c:18]1[cH:19][cH:20][c:21]([F:22])[c:23]([F:24])[cH:25]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][s:10]2)[cH:11][cH:12][c:13]1[C:14](=[O:15])[CH:16]=[CH:17][c:18]1[cH:19][cH:20][c:21]([F...
COc1cc(-c2cccs2)ccc1C(C)=O.O=Cc1ccc(F)c(F)c1
COc1cc(-c2cccs2)ccc1C(=O)C=Cc1ccc(F)c(F)c1
null
null
O1CCCC1
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
O=C(C=Cc1ccccc1)c1ccc(-c2cccs2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[O;D1;H0:7]=[C:6](-[c:8])-[CH;D2;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
69.1
[{"value": 69.0, "product": "FC=1C=C(C=CC1F)C=CC(=O)C1=C(C=C(C=C1)C=1SC=CC1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.1, "product": "FC=1C=C(C=CC1F)C=CC(=O)C1=C(C=C(C=C1)C=1SC=CC1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The 2′-methoxy-4′-(thien-2-yl)acetophenone (0.30 g, 1.3 mmol) from Ex-57A and 3,4-difluorobenzaldehyde 0.19 g, 1.3 mmol) were mixed in tetrahydrofuran (THF, 10 mL). Cesium carbonate (1.2 g, 3.9 mmol) was added, and the mixture was stirred at reflux overnight. Upon cooling to room temperature, the mixture was filtered, ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1.c1ccsc1.c1ccccc1
HO-
O1CCCC1
null
null
COc1cc(-c2cccs2)ccc1C(C)=O.O=Cc1ccc(F)c(F)c1>O1CCCC1>COc1cc(-c2cccs2)ccc1C(=O)C=Cc1ccc(F)c(F)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2095895f6d47499b941b0e13f624eeae
CC(C)(C)[Si](C)(C)Cl.COc1cc(C(C)=O)cc(OC)c1O>>COc1cc(C(C)=O)cc(OC)c1O[Si](C)(C)C(C)(C)C
OC1=C(C=C(C=C1OC)C(C)=O)OC.[Si](C)(C)(C(C)(C)C)Cl.N1C=NC=C1>>COC=1C=C(C=C(C1O[Si](C)(C)C(C)(C)C)OC)C(C)=O
Cl[Si:15]([CH3:16])([CH3:17])[C:18]([CH3:19])([CH3:20])[CH3:21].[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([CH3:7])=[O:8])[cH:9][c:10]([O:11][CH3:12])[c:13]1[OH:14]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([CH3:7])=[O:8])[cH:9][c:10]([O:11][CH3:12])[c:13]1[O:14][Si:15]([CH3:16])([CH3:17])[C:18]([CH3:19])([CH3:20])[CH3:21]
CC(C)(C)[Si](C)(C)Cl.COc1cc(C(C)=O)cc(OC)c1O
COc1cc(C(C)=O)cc(OC)c1O[Si](C)(C)C(C)(C)C
null
null
CN(C=O)C
Protection
Alcohol protection with silyl ethers
91043baed1393f1ecd2302d7d0b31c01cf171d3977dd7c70afa1da52fa298c73
4a917c959d011f885a1269fa3c1f022ee5e09144996246d24e42e65634a451ac
c1ccccc1
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7].[OH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[C;D1;H3:2]-[Si;H0;D4;+0:1](-[C;D1;H3:3])(-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7]
81
[{"value": 81.0, "product": "COC=1C=C(C=C(C1O[Si](C)(C)C(C)(C)C)OC)C(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.8, "product": "COC=1C=C(C=C(C1O[Si](C)(C)C(C)(C)C)OC)C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Ex-59A: To a solution of 4′-hydroxy-3′,5′-dimethoxyacetophenone (1 g, 5.1 mmol) in N,N-dimethylformamide were added tert-butyldimethylsilyl chloride (1,15 g, 7.6 mmol) and imidazole (0.69 g, 10.2 mmol). The mixture was stirred at room temperature overnight. Upon quenching with 1 M sulfuric acid solution, the mixture wa...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Silyl protective group
TMS ether protective group
null
null
c1ccccc1
HCl
CN(C=O)C
null
8
CC(C)(C)[Si](C)(C)Cl.COc1cc(C(C)=O)cc(OC)c1O>CN(C=O)C>COc1cc(C(C)=O)cc(OC)c1O[Si](C)(C)C(C)(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7211d0c745c549738a94877ba304ff6d
COc1cc(C(C)=O)cc(OC)c1O[Si](C)(C)C(C)(C)C.COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O>>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(O[Si](C)(C)C(C)(C)C)c(OC)c1
C(C)(C)[N-]C(C)C.[Li+].S1C2=C(C=C1C=1C(=CC(=C(C=O)C1)OC)OC)C=CC=C2.COC=1C=C(C=C(C1O[Si](C)(C)C(C)(C)C)OC)C(C)=O>>S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1=CC(=C(C(=C1)OC)O[Si](C)(C)C(C)(C)C)OC)OC)OC)C=CC=C2
[CH3:21][C:22](=[O:23])[c:24]1[cH:25][c:26]([O:27][CH3:28])[c:29]([O:30][Si:31]([CH3:32])([CH3:33])[C:34]([CH3:35])([CH3:36])[CH3:37])[c:38]([O:39][CH3:40])[cH:41]1.O=[CH:20][c:19]1[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH3:7])[c:8](-[c:9]2[cH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[s:17]2)[cH:18]1>>[CH3:1][O:2][c:...
COc1cc(C(C)=O)cc(OC)c1O[Si](C)(C)C(C)(C)C.COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O
COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(O[Si](C)(C)C(C)(C)C)c(OC)c1
null
null
O1CCCC1
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
O=C(C=Cc1cccc(-c2cc3ccccc3s2)c1)c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[O;D1;H0:7]=[C:6](-[c:8])-[CH;D2;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
20
[{"value": 20.0, "product": "S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1=CC(=C(C(=C1)OC)O[Si](C)(C)C(C)(C)C)OC)OC)OC)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
Ex-59B: To a solution of 3′,5′-dimethoxy-4′-(tert-butyldimethylsiloxy)acetophenone, from Ex-59A (0.5 g, 1.6 mmol) in tetrahydrofuran (10 mL) chilled with ice/water was added lithium diisopropylamide (2 M, 0.8 mL, 1.6 mmol). The mixture was stirred for 20 minutes while chilled. Then 5-(benzo[b]thien-2-yl)-2,4-dimethoxyb...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccccc1.c1ccc2sccc2c1.c1ccccc1
HO-
O1CCCC1
null
0.333333
COc1cc(C(C)=O)cc(OC)c1O[Si](C)(C)C(C)(C)C.COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=O>O1CCCC1>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(O[Si](C)(C)C(C)(C)C)c(OC)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4c4e46db8cf141edbd9902f9bd36d633
COC1=C(O[SiH3])C(C(=O)C=Cc2cc(-c3cc4ccccc4s3)c(OC)cc2OC)C(C)(C)C(OC)=C1C(C)(C)C>>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(O)c(OC)c1
S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1C(=C(C(=C(C1(C)C)OC)C(C)(C)C)OC)O[SiH3])OC)OC)C=CC=C2.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC.O1CCCC1>>S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1=CC(=C(C(=C1)OC)O)OC)OC)OC)C=CC=C2
CC(C)(C)[C:25]1=[C:26]([O:27][CH3:28])[C:34](C)(C)[CH:24]([C:22]([CH:21]=[CH:20][c:19]2[c:3]([O:2][CH3:1])[cH:4][c:5]([O:6][CH3:7])[c:8](-[c:9]3[cH:10][c:11]4[cH:12][cH:13][cH:14][cH:15][c:16]4[s:17]3)[cH:18]2)=[O:23])[C:31]([O:32][SiH3])=[C:29]1[O:30][CH3:33]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[c:8](-[c:9]2[c...
COC1=C(O[SiH3])C(C(=O)C=Cc2cc(-c3cc4ccccc4s3)c(OC)cc2OC)C(C)(C)C(OC)=C1C(C)(C)C
COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(O)c(OC)c1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
29ddbc8423b0fa3458daa9ba69e19baa703f62fadf1e6e8f61328f5a7c67b877
049fcc0c22defb2af711e7312f2f90383f80c333f7d8cf0e6c6e9942cae1c523
O=C(C=Cc1cccc(-c2cc3ccccc3s2)c1)c1ccccc1
C-C(-C)(-C)-[C;H0;D3;+0:1]1=[C;H0;D3;+0:2](-[#8:3]-[C;D1;H3:4])-[C;H0;D4;+0:5](-C)(-C)-[CH;D3;+0:6](-[C:7](=[O;D1;H0:8])-[C:9]=[C:10]-[c:11])-[C;H0;D3;+0:12](-[O;H0;D2;+0:13]-[SiH3])=[C;H0;D3;+0:14]-1-[O;H0;D2;+0:15]-[CH3;D1;+0:16]>>[C;D1;H3:4]-[#8:3]-[c;H0;D3;+0:2]1:[cH;D2;+0:1]:[c;H0;D3;+0:6](-[C:7](=[O;D1;H0:8])-[C:...
46
[{"value": 46.0, "product": "S1C2=C(C=C1C=1C(=CC(=C(C1)C=CC(=O)C1=CC(=C(C(=C1)OC)O)OC)OC)OC)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 3-[5-(benzo[b]thien-2-yl)2,4-dimethoxyphenyl]-1-(4-tert-butyldimethyl-siloxy-3,5-dimethoxyphenyl)-2-propen-1-one, from Ex-59B, (0.135 g, 0.228 mmol) in tetrahydrofuran (2 mL) was added tetrabutylammonium fluoride (0.061 g. 0.228 mmol), and the mixture was stirred at room temperature for two hours. Upon...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether.Ether
Ketone.Ether.Ether.Aromatic alcohol
C1=CCCC=C1
c1ccccc1
c1ccccc1.c1ccc2sccc2c1.c1ccccc1
Other
null
null
2
COC1=C(O[SiH3])C(C(=O)C=Cc2cc(-c3cc4ccccc4s3)c(OC)cc2OC)C(C)(C)C(OC)=C1C(C)(C)C>>COc1cc(OC)c(-c2cc3ccccc3s2)cc1C=CC(=O)c1cc(OC)c(O)c(OC)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1a6cab735b784644a4361ba81a9aa295
CCOC(=O)CO.COc1cc(C(C)=O)cc(OC)c1O>>CCOC(=O)c1c(OC)cc(C(=O)COC)cc1OC
COC=1C=C(C=C(C1O)OC)C(C)=O.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(CO)(=O)OCC.CCOC(=O)/N=N/C(=O)OCC>>C(C)OC(=O)C1=C(C=C(C=C1OC)C(COC)=O)OC
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:16][OH:15].O[c:6]1[c:7]([O:8][CH3:9])[cH:10][c:11]([C:12](=[O:13])[CH3:14])[cH:17][c:18]1[O:19][CH3:20]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[c:7]([O:8][CH3:9])[cH:10][c:11]([C:12](=[O:13])[CH2:14][O:15][CH3:16])[cH:17][c:18]1[O:19][CH3:20]
CCOC(=O)CO.COc1cc(C(C)=O)cc(OC)c1O
CCOC(=O)c1c(OC)cc(C(=O)COC)cc1OC
null
null
O1CCCC1
C-C Coupling
OtherReaction
4646b155988172b242d5137347c3b0b0feb8517577e33604b4123e53cd998f06
64fc23516941529f5dd54811af89d2b2e13a2dfe6a8d6790d171b8db884686ba
c1ccccc1
O-[c;H0;D3;+0:1]1:[c:2](-[#8:3]):[c:4]:[c:5](-[C:6](-[CH3;D1;+0:7])=[O;D1;H0:8]):[c:9]:[c:10]:1-[#8:11].[C:12]-[#8:13]-[C;H0;D3;+0:14](=[O;D1;H0:15])-[CH2;D2;+0:16]-[OH;D1;+0:17]>>[#8:3]-[c:2]1:[c:4]:[c:5](-[C:6](=[O;D1;H0:8])-[CH2;D2;+0:7]-[O;H0;D2;+0:17]-[CH3;D1;+0:16]):[c:9]:[c:10](-[#8:11]):[c;H0;D3;+0:1]:1-[C;H0;D...
35.9
[{"value": 35.9, "product": "C(C)OC(=O)C1=C(C=C(C=C1OC)C(COC)=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Ex-61A: 3′,5′-Dimethoxy-4′-hydroxyacetophenone (6.03 g, 31 mmol) and triphenylphosphine (8.05 g, 31 mmol) were stirred in 124 mL of tetrahydrofuran (THF). The mixture was treated with ethyl glycolate (3.2 g, 31 mmol) and diethylazodicarboxylate (4.83 mL, 31 mmol). The reaction mixture was stirred under reflux for about...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Primary alcohol.Aromatic alcohol
Ketone.Ester.Ether
c1ccccc1
c1ccccc1
c1ccccc1
HO-
O1CCCC1
null
null
CCOC(=O)CO.COc1cc(C(C)=O)cc(OC)c1O>O1CCCC1>CCOC(=O)c1c(OC)cc(C(=O)COC)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-772d75e44f814447a810e085fd5bd9f5
BrBr.COc1ccc(C=O)c(O)c1>>COc1cc(O)c(C=O)cc1Br
OC1=C(C=O)C=CC(=C1)OC.BrBr>>BrC=1C(=CC(=C(C=O)C1)O)OC
Br[Br:12].[CH3:1][O:2][c:3]1[cH:4][c:5]([OH:6])[c:7]([CH:8]=[O:9])[cH:10][cH:11]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([OH:6])[c:7]([CH:8]=[O:9])[cH:10][c:11]1[Br:12]
BrBr.COc1ccc(C=O)c(O)c1
COc1cc(O)c(C=O)cc1Br
null
null
ClCCl.CCOC(=O)C
Functional Group Interconversion
Bromination
f6effe61353895b318215d8bd9b6bb1105cafbf7be8c217d748df587260b32c3
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccccc1
Br-[Br;H0;D1;+0:1].[#8:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6]:[c:7]-[C:8]=[O;D1;H0:9]>>[#8:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[Br;H0;D1;+0:1]):[c:6]:[c:7]-[C:8]=[O;D1;H0:9]
84.4
[{"value": 84.4, "product": "BrC=1C(=CC(=C(C=O)C1)O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
1.5
HOUR
Ex-62A: A solution of 2-hydroxy-4-methoxybenzaldehyde (3.03 g, 20 mmol) in 25 mL of dichloromethane was cooled to 0° C. and treated dropwise with a solution of bromine (3.41 g, 21 mmol) in 10 mL of dichloromethane. The reaction mixture was stirred at 0° C. for 1.5 hours. The solvent was removed by rotary evaporation to...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
HBr
ClCCl.CCOC(=O)C
0
1.5
BrBr.COc1ccc(C=O)c(O)c1>ClCCl.CCOC(=O)C>COc1cc(O)c(C=O)cc1Br
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3fdfa8d9995e4854b76f9b05e10b3ae5
COc1cc(O)c(C=O)cc1Br.OB(O)c1cccs1>>COc1cc(O)c(C=O)cc1-c1cc2ccccc2s1
N#N.BrC=1C(=CC(=C(C=O)C1)O)OC.S1C(=CC=C1)B(O)O.C(=O)([O-])[O-].[Na+].[Na+]>>S1C2=C(C=C1C=1C(=CC(=C(C=O)C1)O)OC)C=CC=C2
Br[c:11]1[c:3]([O:2][CH3:1])[cH:4][c:5]([OH:6])[c:7]([CH:8]=[O:9])[cH:10]1.OB(O)[c:19]1[cH:18][cH:17][cH:12][s:20]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([OH:6])[c:7]([CH:8]=[O:9])[cH:10][c:11]1-[c:12]1[cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[s:20]1
COc1cc(O)c(C=O)cc1Br.OB(O)c1cccs1
COc1cc(O)c(C=O)cc1-c1cc2ccccc2s1
null
null
COCCOC
C-C Coupling
OtherReaction
379ca588d522115c6f78ef009bec73b75a2690147aebc41a5faed8ff07b4966b
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2cc3ccccc3s2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]-[C:4]=[O;D1;H0:5]):[c:6](-[#8:7]):[c:8].O-B(-O)-[c;H0;D3;+0:9]1:[#16;a:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[c:13]:1>>[#8:7]-[c:6](:[c:8]):[c;H0;D3;+0:1](-[c;H0;D3;+0:11]1:[#16;a:10]:[c;H0;D3;+0:9]2:[c:13]:[cH;D2;+0:12]:[c:14]:[c:15]:[c:16]:2:[c:17]:1):[c:2]:[c:3]-[C:4]=[O;D1;H0:5]
170.1
[{"value": 170.1, "product": "S1C2=C(C=C1C=1C(=CC(=C(C=O)C1)O)OC)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Ex-62B: A stream of N2 was bubbled through a solution of 5-bromo-2-hydroxy-4-methoxybenzaldehyde (1 g, 4.3 mmol) from Ex-62A in 30 mL of ethylene glycol dimethyl ether for 15 min. Tetrakis-triphenylphosphine palladium (0) (0.5 g, 0.4 mmol) was added along with thiophene-2-boronic acid (1.2 g, 6.5 mmol) and 10 mL of Na2...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccsc1
c1ccccc1.c1ccc2sccc2c1
c1ccccc1.c1ccc2sccc2c1
null
COCCOC
null
null
COc1cc(O)c(C=O)cc1Br.OB(O)c1cccs1>COCCOC>COc1cc(O)c(C=O)cc1-c1cc2ccccc2s1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-53ea9cf14a8744f78909ae696f4bfac7
C=COC(C)=O.CCCCOC(=O)c1ccccc1C(=O)OCCCC>>C=CCOC(=O)c1ccccc1C(=O)OCC=C
C(C=1C(C(=O)OCCCC)=CC=CC1)(=O)OCCCC.S(=O)(=O)([O-])OOS(=O)(=O)[O-].[NH4+].[NH4+].C(C)(=O)OC=C.C(C=1C(C(=O)OCCCC)=CC=CC1)(=O)OCCCC>>C(C=1C(C(=O)OCC=C)=CC=CC1)(=O)OCC=C
CC(=O)O[CH:2]=[CH2:1].CCC[CH2:3][O:4][C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[C:13](=[O:14])[O:15][CH2:16][CH2:17][CH2:18]C>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[C:13](=[O:14])[O:15][CH2:16][CH:17]=[CH2:18]
C=COC(C)=O.CCCCOC(=O)c1ccccc1C(=O)OCCCC
C=CCOC(=O)c1ccccc1C(=O)OCC=C
null
null
O
C-C Coupling
OtherReaction
5704e0572b2792055ea7ace0ab9d5c08e91a5bd5208446dc90bb3e4d4b22231a
e1ec59b264f7681b281d160d0ca665e90513d6835010c1042b2b30c575374e30
c1ccccc1
C-C(=O)-O-[CH;D2;+0:1]=[C;D1;H2:2].C-C-C-[CH2;D2;+0:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c:7].C-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[C:10]-[#8:11]-[C:12]=[O;D1;H0:13]>>[C;D1;H2:2]=[CH;D2;+0:1]-[CH2;D2;+0:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[c:7].[CH2;D1;+0:8]=[CH;D2;+0:9]-[C:10]-[#8:11]-[C:12]=[O;D1;H0:13]
null
[]
80
CELSIUS
5
MINUTE
0.2 g of defoamer and 12 g of Fixapret COC were added to and mixed with a solution of 47 g of polyvinyl alcohol in 600 g of water. The mixture was heated to about 80° C. About 90% of a catalyst solution of 1.3 g of ammonium persulfate in 6 g of water were then added and the mixture was homogenized for about 5 minutes. ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Vinyl
Ester.Allyl.Allyl
null
null
c1ccccc1
HO-
O
80
0.083333
C=COC(C)=O.CCCCOC(=O)c1ccccc1C(=O)OCCCC>O>C=CCOC(=O)c1ccccc1C(=O)OCC=C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-15ed3afbed324fc5a0787f9298282063
CC(C)(C)c1cc(CCN)cc(C(C)(C)C)c1O.CCCCOc1cc(C=CC(=O)O)cc(OCCCC)c1O>>CCCCOc1cc(C=CC(=O)NCCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OCCCC)c1O
C1CCC(CC1)N=C=NC2CCCCC2.C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)O.NCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C.C=1C=CC2=C(C1)N=NN2O>>C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)NCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C
[NH2:13][CH2:14][CH2:15][c:16]1[cH:17][c:18]([C:19]([CH3:20])([CH3:21])[CH3:22])[c:23]([OH:24])[c:25]([C:26]([CH3:27])([CH3:28])[CH3:29])[cH:30]1.O[C:11]([CH:10]=[CH:9][c:8]1[cH:7][c:6]([O:5][CH2:4][CH2:3][CH2:2][CH3:1])[c:38]([OH:39])[c:32]([O:33][CH2:34][CH2:35][CH2:36][CH3:37])[cH:31]1)=[O:12]>>[CH3:1][CH2:2][CH2:3]...
CC(C)(C)c1cc(CCN)cc(C(C)(C)C)c1O.CCCCOc1cc(C=CC(=O)O)cc(OCCCC)c1O
CCCCOc1cc(C=CC(=O)NCCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OCCCC)c1O
null
null
CC#N
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(C=Cc1ccccc1)NCCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5]
91.5
[{"value": 91.0, "product": "C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)NCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.5, "product": "C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)NCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
To the solution of 3-(3,5-dibutoxy-4-hydroxyphenyl)acrylic acid (130 mg, 0.421 mmol), 4-(2-aminoethyl)-2,6-di-t-butylphenol (110 mg, 0.441 mmol) and HOBT (70 mg, 0.51 mmol) in MeCN 10 ml were DCC at 0° C. After 5 minutes, the solution was stirred for 2 hours at room temperature. And then the precipitate was removed by ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
CC#N
null
0.083333
CC(C)(C)c1cc(CCN)cc(C(C)(C)C)c1O.CCCCOc1cc(C=CC(=O)O)cc(OCCCC)c1O>CC#N>CCCCOc1cc(C=CC(=O)NCCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OCCCC)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9510d77d582b450d883ef78c542b5bab
CC(C)(C)c1cc(CCN)cc(C(C)(C)C)c1O.CCCCOc1cc(C=CC(=O)O)cc(OCCCC)c1O.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C>>CCCCOc1cc(C=CC(=O)NCCCCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OCCCC)c1O
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)O.NCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C>>C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)NCCCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C
[NH2:13][CH2:14][CH2:17][c:18]1[cH:19][c:20]([C:21]([CH3:22])([CH3:23])[CH3:24])[c:25]([OH:26])[c:27]([C:28]([CH3:29])([CH3:30])[CH3:31])[cH:32]1.O[C:11]([CH:10]=[CH:9][c:8]1[cH:7][c:6]([O:5][CH2:4][CH2:3][CH2:2][CH3:1])[c:40]([OH:41])[c:34]([O:35][CH2:36][CH2:37][CH2:38][CH3:39])[cH:33]1)=[O:12].CN(C)[P+](On1nnc2cc[cH...
CC(C)(C)c1cc(CCN)cc(C(C)(C)C)c1O.CCCCOc1cc(C=CC(=O)O)cc(OCCCC)c1O.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C
CCCCOc1cc(C=CC(=O)NCCCCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OCCCC)c1O
null
null
CCN(CC)CC.CN(C)C=O.C(Cl)Cl
Acylation
OtherReaction
a24117a319ae7f7ed0e2138d9be038d04bd20f7709e3d139967549efb1cd97fb
6f35efba33558ef5fc3cd84a18d45a4f1577b28d410f08768b27ebd3b689ecd0
O=C(C=Cc1ccccc1)NCCCCc1ccccc1
C-N(-C)-[P+](-O-n1:n:n:c2:c:c:[cH;D2;+0:1]:[cH;D2;+0:2]:c:2:1)(-N(-C)-C)-N(-C)-C.O-[C;H0;D3;+0:3](=[O;D1;H0:4])-[C:5]=[C:6]-[c:7].[NH2;D1;+0:8]-[CH2;D2;+0:9]-[CH2;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[O;D1;H0:4]=[C;H0;D3;+0:3](-[C:5]=[C:6]-[c:7])-[NH;D2;+0:8]-[CH2;D2;+0:9]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:10]-[c:11]...
91
[{"value": 91.0, "product": "C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)NCCCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.8, "product": "C(CCC)OC=1C=C(C=C(C1O)OCCCC)C=CC(=O)NCCCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
To the solution of 3-(3,5-dibutoxy-4-hydroxyphenyl) acrylic acid (53 mg, 0.17 mmol) in DMF (0.76 ml) and Et3N (39 μl), was added 4-(2-aminoethyl)-2,6-di-t-butylphenol (50 mg, 0.19 mmol) at 0° C. The obtained solution was added with the solution of benzotriazol-1-yloxytris (dimethylamino) phosphonium hexafluorophosphate...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Tertiary amine.Tertiary amine.Tertiary amine
Secondary amide
c1ccc2[nH]nnc2c1
null
c1ccccc1.c1ccccc1
HO-
CCN(CC)CC.CN(C)C=O.C(Cl)Cl
0
0.5
CC(C)(C)c1cc(CCN)cc(C(C)(C)C)c1O.CCCCOc1cc(C=CC(=O)O)cc(OCCCC)c1O.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C>CCN(CC)CC.CN(C)C=O.C(Cl)Cl>CCCCOc1cc(C=CC(=O)NCCCCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OCCCC)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7feb93247a2c4c19a4a523417a2e1545
CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O.Cc1ccc(CCCN)cc1C>>CCC(CC)Oc1cc(C=CC(=O)NCCCc2ccc(C)c(C)c2)cc(OC(CC)CC)c1O
C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)O.CC=1C=C(C=CC1C)CCCN.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C>>C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)NCCCC1=CC(=C(C=C1)C)C
O[C:12]([CH:11]=[CH:10][c:9]1[cH:8][c:7]([O:6][CH:3]([CH2:2][CH3:1])[CH2:4][CH3:5])[c:34]([OH:35])[c:27]([O:28][CH:29]([CH2:30][CH3:31])[CH2:32][CH3:33])[cH:26]1)=[O:13].[NH2:14][CH2:15][CH2:16][CH2:17][c:18]1[cH:19][cH:20][c:21]([CH3:22])[c:23]([CH3:24])[cH:25]1>>[CH3:1][CH2:2][CH:3]([CH2:4][CH3:5])[O:6][c:7]1[cH:8][c...
CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O.Cc1ccc(CCCN)cc1C
CCC(CC)Oc1cc(C=CC(=O)NCCCc2ccc(C)c(C)c2)cc(OC(CC)CC)c1O
null
null
CCN(CC)CC.C(Cl)Cl.CN(C)C=O
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(C=Cc1ccccc1)NCCCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5]
90
[{"value": 90.0, "product": "C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)NCCCC1=CC(=C(C=C1)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.0, "product": "C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)NCCCC1=CC(=C(C=C1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
To the solution of 3-[3,5-bis-(1-ethylpropoxy)-4-hydroxyphenyl]acrylic acid (20 mg, 0.06 mmol) in DMF (0.2 ml) and Et3N (10 μl), was added 3(3,4-dimethylphenyl)propylamine (11 mg, 0.07 mmol) at 0° C. and was added the solution of BOP (29 mg, 0.07 mmol) in CH2Cl2 (0.2 ml). The solution was stirred for 30 minutes at 0° C...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
CCN(CC)CC.C(Cl)Cl.CN(C)C=O
0
0.5
CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O.Cc1ccc(CCCN)cc1C>CCN(CC)CC.C(Cl)Cl.CN(C)C=O>CCC(CC)Oc1cc(C=CC(=O)NCCCc2ccc(C)c(C)c2)cc(OC(CC)CC)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7ef39f94167d459b9c350cc232bd33b7
CC(C)(C)c1cc(CN)cc(C(C)(C)C)c1O.CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O>>CCC(CC)Oc1cc(C=CC(=O)NCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OC(CC)CC)c1O
C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)O.NCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C>>C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)NCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C
[NH2:14][CH2:15][c:16]1[cH:17][c:18]([C:19]([CH3:20])([CH3:21])[CH3:22])[c:23]([OH:24])[c:25]([C:26]([CH3:27])([CH3:28])[CH3:29])[cH:30]1.O[C:12]([CH:11]=[CH:10][c:9]1[cH:8][c:7]([O:6][CH:3]([CH2:2][CH3:1])[CH2:4][CH3:5])[c:39]([OH:40])[c:32]([O:33][CH:34]([CH2:35][CH3:36])[CH2:37][CH3:38])[cH:31]1)=[O:13]>>[CH3:1][CH2...
CC(C)(C)c1cc(CN)cc(C(C)(C)C)c1O.CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O
CCC(CC)Oc1cc(C=CC(=O)NCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OC(CC)CC)c1O
null
null
CCN(CC)CC.C(Cl)Cl.CN(C)C=O
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(C=Cc1ccccc1)NCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5].[NH2;D1;+0:6]-[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]=[C:4]-[c:5])-[NH;D2;+0:6]-[C:7]-[c:8]
50.2
[{"value": 50.0, "product": "C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)NCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.2, "product": "C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)NCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": f...
0
CELSIUS
30
MINUTE
To the solution of 3-[3,5-bis-(1-ethylpropoxy)-4-hydroxyphenyl]acrylic acid (30 mg, 0.09 mmol) in DMF (0.2 ml) and Et3N (10 μl), was added 4-aminomethyl-2,6-di-t-butylphenol (23 mg, 0.10 mmol) at 0° C. and was added the solution of BOP (44 mg, 0.10 mmol) in CH2Cl2 (0.6 ml). The solution was stirred for 30 minutes at 0°...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
CCN(CC)CC.C(Cl)Cl.CN(C)C=O
0
0.5
CC(C)(C)c1cc(CN)cc(C(C)(C)C)c1O.CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O>CCN(CC)CC.C(Cl)Cl.CN(C)C=O>CCC(CC)Oc1cc(C=CC(=O)NCc2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)cc(OC(CC)CC)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b8d388da673d433cbe34ec1ef9a357e2
CC(C)(C)c1ccc(CCCCN)c(C(C)(C)C)c1O.CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O>>C=C(C(=O)NCCCCc1cc(C(C)(C)C)c(O)c(C(C)(C)C)c1)c1cc(OC(CC)CC)c(O)c(OC(CC)CC)c1
C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C=CC(=O)O.NCCCCC=1C(=C(C(=CC1)C(C)(C)C)O)C(C)(C)C.CN(C)C=O.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C>>C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C(C(=O)NCCCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C)=C
[NH2:5][CH2:6][CH2:7][CH2:8][CH2:9][c:10]1[cH:11][cH:12][c:17]([C:13]([CH3:14])([CH3:15])[CH3:16])[c:19]([OH:18])[c:24]1[C:20]([CH3:21])([CH3:22])[CH3:23].O[C:3]([CH:2]=[CH:1][c:25]1[cH:26][c:27]([O:28][CH:29]([CH2:30][CH3:31])[CH2:32][CH3:33])[c:34]([OH:35])[c:36]([O:37][CH:38]([CH2:39][CH3:40])[CH2:41][CH3:42])[cH:43...
CC(C)(C)c1ccc(CCCCN)c(C(C)(C)C)c1O.CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O
C=C(C(=O)NCCCCc1cc(C(C)(C)C)c(O)c(C(C)(C)C)c1)c1cc(OC(CC)CC)c(O)c(OC(CC)CC)c1
null
null
CCN(CC)CC.C(Cl)Cl
Acylation
OtherReaction
add518fe46c2080b2e0073b1d5e90b43f22106f49c1c4ba985fd805ec54d04e4
f73dd9323138d95383e7f39d832ec654c389295c6cf7ce02912884ce088ed6f6
C=C(C(=O)NCCCCc1ccccc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D2;+0:3]=[CH;D2;+0:4]-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9].[C:10]-[C:11]-[NH2;D1;+0:12].[C:13]-[c:14]1:[c:15]:[cH;D2;+0:16]:[c;H0;D3;+0:17](-[C;H0;D4;+0:18](-[C;D1;H3:19])(-[C;D1;H3:20])-[C;D1;H3:21]):[c;H0;D3;+0:22](-[OH;D1;+0:23]):[c;H0;D3;+0:24]:1-[C;H0;D4;+0:25](-[C;D1;H3:26])...
90
[{"value": 90.0, "product": "C(C)C(CC)OC=1C=C(C=C(C1O)OC(CC)CC)C(C(=O)NCCCCC1=CC(=C(C(=C1)C(C)(C)C)O)C(C)(C)C)=C", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
To the solution of 3-[3,5-bis-(1-ethylpropoxy)-4-hydroxyphenyl]acrylic acid (30 mg, 0.09 mmol) in DMF (0.6 ml) and Et3N (13 μl) was added 4-(4-aminobutyl-2,6-di-t-butylphenol (28 mg, 0.10 mmol) at 0° C. and was added the solution of BOP (44 mg, 0.10 mmol) in CH2Cl2 (0.6 ml). The solution was stirred for 30 minutes at 0...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol.Primary amine
Secondary amide.Aromatic alcohol.Vinyl
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
HO-
CCN(CC)CC.C(Cl)Cl
0
0.5
CC(C)(C)c1ccc(CCCCN)c(C(C)(C)C)c1O.CCC(CC)Oc1cc(C=CC(=O)O)cc(OC(CC)CC)c1O>CCN(CC)CC.C(Cl)Cl>C=C(C(=O)NCCCCc1cc(C(C)(C)C)c(O)c(C(C)(C)C)c1)c1cc(OC(CC)CC)c(O)c(OC(CC)CC)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ea81dd70bcd34b8da3a095b9c3d2d22e
CCCCCCOc1cc(C=CC(=O)O)cc(OCCCCCC)c1O.Nc1ccccc1O>>CCCCCCOc1cc(C=CC(=O)Nc2ccccc2O)cc(OCCCCCC)c1O
C(CCCCC)OC=1C=C(C=C(C1O)OCCCCCC)C=CC(=O)O.NC1=C(C=CC=C1)O.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C>>C(CCCCC)OC=1C=C(C=C(C1O)OCCCCCC)C=CC(=O)NC1=C(C=CC=C1)O
O[C:13]([CH:12]=[CH:11][c:10]1[cH:9][c:8]([O:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[c:32]([OH:33])[c:24]([O:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH3:31])[cH:23]1)=[O:14].[NH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][c:21]1[OH:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][O:7][c:8]1[cH:9][c:10]([CH:11]=[CH...
CCCCCCOc1cc(C=CC(=O)O)cc(OCCCCCC)c1O.Nc1ccccc1O
CCCCCCOc1cc(C=CC(=O)Nc2ccccc2O)cc(OCCCCCC)c1O
null
null
CCN(CC)CC.C(Cl)Cl.CN(C)C=O
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(C=Cc1ccccc1)Nc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C:4]-[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]=[C:4]-[c:5])-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]
34
[{"value": 34.0, "product": "C(CCCCC)OC=1C=C(C=C(C1O)OCCCCCC)C=CC(=O)NC1=C(C=CC=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 33.9, "product": "C(CCCCC)OC=1C=C(C=C(C1O)OCCCCCC)C=CC(=O)NC1=C(C=CC=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
To the solution of 3-(3,5-bishexyloxy-4-hydroxyphenyl) acrylic acid (40 mg, 0.11 mmol) in DMF (1 ml) and Et3N (17 μl), was added 2-aminophenol (13 mg, 0.12 mmol) at 0° C. and was added the solution of BOP (53 mg, 0.12 mmol) in CH2Cl2 (0.6 ml). The solution was stirred for 30 minutes at 0° C. and then was stirred for 1....
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
CCN(CC)CC.C(Cl)Cl.CN(C)C=O
0
0.5
CCCCCCOc1cc(C=CC(=O)O)cc(OCCCCCC)c1O.Nc1ccccc1O>CCN(CC)CC.C(Cl)Cl.CN(C)C=O>CCCCCCOc1cc(C=CC(=O)Nc2ccccc2O)cc(OCCCCCC)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-775e1765b7fa43c09871eef7ae04f3c2
CCCCCOc1cc(CO)cc(OCCCCC)c1O.O=C(CN1CCNCC1)c1ccc(F)cc1>>CCCCCOc1cc(CN2CCN(CC(=O)c3ccc(F)cc3)CC2)cc(OCCCCC)c1O
N(=NC(=O)OCC)C(=O)OCC.OCC1=CC(=C(C(=C1)OCCCCC)O)OCCCCC.FC1=CC=C(C=C1)C(CN1CCNCC1)=O.C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3>>FC1=CC=C(C=C1)C(CN1CCN(CC1)CC1=CC(=C(C(=C1)OCCCCC)O)OCCCCC)=O
O[CH2:10][c:9]1[cH:8][c:7]([O:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[c:35]([OH:36])[c:28]([O:29][CH2:30][CH2:31][CH2:32][CH2:33][CH3:34])[cH:27]1.[NH:11]1[CH2:12][CH2:13][N:14]([CH2:15][C:16](=[O:17])[c:18]2[cH:19][cH:20][c:21]([F:22])[cH:23][cH:24]2)[CH2:25][CH2:26]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][O:6][c:7]1[cH:...
CCCCCOc1cc(CO)cc(OCCCCC)c1O.O=C(CN1CCNCC1)c1ccc(F)cc1
CCCCCOc1cc(CN2CCN(CC(=O)c3ccc(F)cc3)CC2)cc(OCCCCC)c1O
null
null
O.C1CCOC1
Heteroatom Alkylation and Arylation
OtherReaction
9885b3f1c049b08208f7467939360b5e493f0f916b8555f394ab4272f7b37bd7
87693a475e46c41583976158ec46dcaf8be8cc05c5635654a6a68033770f8d5c
O=C(CN1CCN(Cc2ccccc2)CC1)c1ccccc1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1):[c:4]
15.9
[{"value": 15.0, "product": "FC1=CC=C(C=C1)C(CN1CCN(CC1)CC1=CC(=C(C(=C1)OCCCCC)O)OCCCCC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 15.9, "product": "FC1=CC=C(C=C1)C(CN1CCN(CC1)CC1=CC(=C(C(=C1)OCCCCC)O)OCCCCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
To the solution of 4-hydroxymethyl-2,6-bis-pentyloxyphenol (525 mg, 1.62 mmol), 1-(4-fluorophenyl)-2-piperazine-1-yl-ethanone (432 mg, 1.94 mmol) and PPh3 (509 mg, 1.94 mmol) in drying THF (10 ml) was dropped diethyl azodicarboxylate (0.38 ml, 2.43 mmol) at 0° C. and then was stirred 15 minutes at room temperature. The...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
HO-
O.C1CCOC1
null
0.25
CCCCCOc1cc(CO)cc(OCCCCC)c1O.O=C(CN1CCNCC1)c1ccc(F)cc1>O.C1CCOC1>CCCCCOc1cc(CN2CCN(CC(=O)c3ccc(F)cc3)CC2)cc(OCCCCC)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-87cdbd6209e34c60b3fe63b0dfcb5ba8
CCCCCCCCCOc1cc(C(=O)O)cc(OCCCCCCCCC)c1O.O=C(CN1CCNCC1)c1ccc(Cl)cc1>>CCCCCOc1cc(C(=O)N2CCN(CC(=O)c3ccc(Cl)cc3)CC2)cc(OCCCCC)c1O
OC1=C(C=C(C(=O)O)C=C1OCCCCCCCCC)OCCCCCCCCC.ClC1=CC=C(C=C1)C(CN1CCNCC1)=O.CCN=C=NCCCN(C)C.C=1C=CC2=C(C1)N=NN2O.C(=O)(O)[O-].[Na+]>>ClC1=CC=C(C=C1)C(CN1CCN(CC1)C(C1=CC(=C(C(=C1)OCCCCC)O)OCCCCC)=O)=O
CCCC[CH2:35][CH2:34][CH2:33][CH2:32][CH2:31][O:30][c:29]1[cH:28][c:9]([C:10](O)=[O:11])[cH:8][c:7]([O:6][CH2:5][CH2:4][CH2:3]CCCC[CH2:2][CH3:1])[c:36]1[OH:37].[NH:12]1[CH2:13][CH2:14][N:15]([CH2:16][C:17](=[O:18])[c:19]2[cH:20][cH:21][c:22]([Cl:23])[cH:24][cH:25]2)[CH2:26][CH2:27]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][...
CCCCCCCCCOc1cc(C(=O)O)cc(OCCCCCCCCC)c1O.O=C(CN1CCNCC1)c1ccc(Cl)cc1
CCCCCOc1cc(C(=O)N2CCN(CC(=O)c3ccc(Cl)cc3)CC2)cc(OCCCCC)c1O
null
null
CC#N
Acylation
OtherReaction
ed26ef5eea92a0cc433b3f89a34f4c61724425fa15a9d0ec83a0f7a903eec831
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(CN1CCN(C(=O)c2ccccc2)CC1)c1ccccc1
C-C-C-C-[CH2;D2;+0:1]-[C:2]-[C:3].O-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6](:[c:7]):[c:8].[C:9]-[C:10]-[CH2;D2;+0:11]-C-C-C-C-[CH2;D2;+0:12]-[C;D1;H3:13].[#7:14]1-[C:15]-[C:16]-[NH;D2;+0:17]-[C:18]-[C:19]-1>>[C:9]-[C:10]-[CH2;D2;+0:11]-[CH2;D2;+0:12]-[C;D1;H3:13].[C:3]-[C:2]-[CH3;D1;+0:1].[O;D1;H0:5]=[C;H0;D3;+0:4](-[N;H0;D...
80.2
[{"value": 66.0, "product": "ClC1=CC=C(C=C1)C(CN1CCN(CC1)C(C1=CC(=C(C(=C1)OCCCCC)O)OCCCCC)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.2, "product": "ClC1=CC=C(C=C1)C(CN1CCN(CC1)C(C1=CC(=C(C(=C1)OCCCCC)O)OCCCCC)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To 4-hydroxy-3,5-bis-nonyloxy benzoic acid (98 mg, 0.23 mmol), 1-(4-chlorophenyl)-2-piperazine-1-yl-ethanone (111 mg, 0.46 mmol), EDCI (89 mg, 0.46 mmol) and HOBT (63 mg, 0.46 mmol) was added MeCN (3 ml) and stirred for 1 hour at room temperature. The solution was added with NaHCO3 to finish the reaction. The solution ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
HO-
CC#N
null
1
CCCCCCCCCOc1cc(C(=O)O)cc(OCCCCCCCCC)c1O.O=C(CN1CCNCC1)c1ccc(Cl)cc1>CC#N>CCCCCOc1cc(C(=O)N2CCN(CC(=O)c3ccc(Cl)cc3)CC2)cc(OCCCCC)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-478b6b6e95b94ca99e9f4c125d01b3e1
COC(F)(F)C(F)(OC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F)C(F)(F)F.[Li+].[OH-]>>[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC(F)(C(F)(F)F)C(F)(F)OC
FS(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC(F)(C(F)(F)F)C(F)(F)OC.O.[OH-].[Li+]>>S(=O)(=O)(O[Li])C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC(F)(C(F)(F)F)C(F)(F)OC
F[S:3](=[O:4])(=[O:5])[C:6]([F:7])([F:8])[C:9]([F:10])([F:11])[C:12]([F:13])([F:14])[C:15]([F:16])([F:17])[O:18][C:19]([F:20])([C:21]([F:22])([F:23])[F:24])[C:25]([F:26])([F:27])[O:28][CH3:29].[Li+:1].[OH-:2]>>[Li:1][O:2][S:3](=[O:4])(=[O:5])[C:6]([F:7])([F:8])[C:9]([F:10])([F:11])[C:12]([F:13])([F:14])[C:15]([F:16])([...
COC(F)(F)C(F)(OC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F)C(F)(F)F.[Li+].[OH-]
[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC(F)(C(F)(F)F)C(F)(F)OC
null
null
O
Acylation
OtherReaction
9710abdc9908af230f0611317212db046ddbe9e4efaeaa534f6acc066fddc190
0294dd03ed5eb302c97e32c7940c77344565a5370a2663785e5aa80492855f80
null
F-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[C:4](-[C:5])(-[F;D1;H0:6])-[F;D1;H0:7].[Li+;H0;D0:8].[OH-;D0:9]>>[C:5]-[C:4](-[F;D1;H0:6])(-[F;D1;H0:7])-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[O;H0;D2;+0:9]-[Li;H0;D1;+0:8]
null
[]
75
CELSIUS
null
null
A 250 mL round bottom flask was charged with FSO2(CF2)4OCF(CF3)CF2OCH3 (23.3 g, 0.048 mole) deionized water (150 g) and lithium hydroxide monohydrate (4.08 g, 0.097 mole). The resulting mixture was heated at 75° C. for about 18 hours, filtered and the aqueous solution treated with 48% aqueous HF until slightly acidic t...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonate
null
null
null
HF
O
75
null
COC(F)(F)C(F)(OC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F)C(F)(F)F.[Li+].[OH-]>O>[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC(F)(C(F)(F)F)C(F)(F)OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-635850a0aa144e23a987da541fe10f93
COC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F.[Li+].[OH-]>>[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC
[OH-].[Li+].FS(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC.O.[OH-].[Li+].C(=O)=O>>S(=O)(=O)(O[Li])C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC
F[S:3](=[O:4])(=[O:5])[C:6]([F:7])([F:8])[C:9]([F:10])([F:11])[C:12]([F:13])([F:14])[C:15]([F:16])([F:17])[O:18][CH3:19].[Li+:1].[OH-:2]>>[Li:1][O:2][S:3](=[O:4])(=[O:5])[C:6]([F:7])([F:8])[C:9]([F:10])([F:11])[C:12]([F:13])([F:14])[C:15]([F:16])([F:17])[O:18][CH3:19]
COC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F.[Li+].[OH-]
[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC
null
null
O
Acylation
OtherReaction
9710abdc9908af230f0611317212db046ddbe9e4efaeaa534f6acc066fddc190
0294dd03ed5eb302c97e32c7940c77344565a5370a2663785e5aa80492855f80
null
F-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[C:4](-[C:5])(-[F;D1;H0:6])-[F;D1;H0:7].[Li+;H0;D0:8].[OH-;D0:9]>>[C:5]-[C:4](-[F;D1;H0:6])(-[F;D1;H0:7])-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[O;H0;D2;+0:9]-[Li;H0;D1;+0:8]
null
[]
null
null
null
null
FSO2(CF2)4OCH3 (35.8 g, 0.114 mole) was treated with lithium hydroxide monohydrate (12 g, 0.285 mole) in deionized water (150 g) at 75° C. for six hours. After cooling to room temperature, two small pieces of solid carbon dioxide (Dry Ice) were added to neutralize the excess lithium hydroxide. The water was removed by ...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonate
null
null
null
HF
O
null
null
COC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F.[Li+].[OH-]>O>[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-83430d7bf97247ea87fe5e124cbf925b
CCOS(=O)(=O)OCC.O=C(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F.[F-]>>CCOC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F
FS(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(=O)F.[F-].[K+].S(=O)(=O)(OCC)OCC.O>>FS(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCC
CCOS(=O)(=O)O[CH2:2][CH3:1].[O:3]=[C:4]([F:6])[C:7]([F:8])([F:9])[C:10]([F:11])([F:12])[C:13]([F:14])([F:15])[S:16](=[O:17])(=[O:18])[F:19].[F-:5]>>[CH3:1][CH2:2][O:3][C:4]([F:5])([F:6])[C:7]([F:8])([F:9])[C:10]([F:11])([F:12])[C:13]([F:14])([F:15])[S:16](=[O:17])(=[O:18])[F:19]
CCOS(=O)(=O)OCC.O=C(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F.[F-]
CCOC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F
null
CCCCCCCC[N+](C)(CCCCCCCC)CCCCCCCC.[Cl-]
COCCOCCOC
Heteroatom Alkylation and Arylation
OtherReaction
4722b19e5c0bd8859e112a70b85350ef344086146f7bcb1e59f7dbf48410cff2
e3109f17ac6917ddf8a840cf4f3485d420243744a4438cad70cf693ceb10c490
null
C-C-O-S(=O)(=O)-O-[CH2;D2;+0:1]-[C;D1;H3:2].[C:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C;H0;D3;+0:7](-[F;D1;H0:8])=[O;H0;D1;+0:9].[F-;H0;D0:10]>>[C:3]-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[C;H0;D4;+0:7](-[F;D1;H0:8])(-[F;H0;D1;+0:10])-[O;H0;D2;+0:9]-[CH2;D2;+0:1]-[C;D1;H3:2]
62.5
[{"value": 62.5, "product": "FS(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
2
HOUR
In a procedure similar to that described in Preparation of Precursor 1, FSO2(CF2)3COF (70 g, 0.25 mole), KF (21.8 g, 0.37 mole), diglyme (350 ml), Adogen 464 (10.5 g of a 56% solution in anhydrous diglyme) and diethyl sulfate (48 g, 0.312 mole) were combined and reacted at 52° C. for 16 hours. Deionized water (˜250 g) ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Tertiary halide.Tertiary halide.Ether
null
null
null
HO-
CCCCCCCC[N+](C)(CCCCCCCC)CCCCCCCC.[Cl-].COCCOCCOC
65
2
CCOS(=O)(=O)OCC.O=C(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F.[F-]>CCCCCCCC[N+](C)(CCCCCCCC)CCCCCCCC.[Cl-].COCCOCCOC>CCOC(F)(F)C(F)(F)C(F)(F)C(F)(F)S(=O)(=O)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-dff731d31c68444588826d90699f1aeb
O=C=O.O=S(=O)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCc1ccccc1.[Li+]>>[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCc1ccccc1
C(=O)=O.[OH-].[Li+].FS(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCC1=CC=CC=C1.[OH-].[Li+].[OH-]>>S(=O)(=O)(O[Li])C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCC1=CC=CC=C1
O=C=[O:5].F[S:3](=[O:2])(=[O:4])[C:6]([F:7])([F:8])[C:9]([F:10])([F:11])[C:12]([F:13])([F:14])[C:15]([F:16])([F:17])[O:18][CH2:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1.[Li+:1]>>[Li:1][O:2][S:3](=[O:4])(=[O:5])[C:6]([F:7])([F:8])[C:9]([F:10])([F:11])[C:12]([F:13])([F:14])[C:15]([F:16])([F:17])[O:18][CH2:19][c:20]1...
O=C=O.O=S(=O)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCc1ccccc1.[Li+]
[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCc1ccccc1
null
null
CO
Acylation
OtherReaction
729cd61c01d81e8a6c1ab70187b764caa3de36172ac606c8e518f6b48bf433e9
54c7635ffde4d490c1c5e4e3c5f6d7559a2be37595812791a2f3bf2f290b4267
c1ccccc1
F-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;H0;D1;+0:3])-[C:4](-[C:5])(-[F;D1;H0:6])-[F;D1;H0:7].O=C=[O;H0;D1;+0:8].[Li+;H0;D0:9]>>[C:5]-[C:4](-[F;D1;H0:6])(-[F;D1;H0:7])-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;H0;D1;+0:8])-[O;H0;D2;+0:3]-[Li;H0;D1;+0:9]
null
[]
75
CELSIUS
null
null
FSO2(CF2)4OCH2C6H5 was treated with excess aqueous lithium hydroxide as described in Preparation of Precursor 3 except that the solution was heated at 75° C. for eighteen hours. After neutralization of the excess hydroxide with solid carbon dioxide, it was noted that a lower fluorochemical-containing phase was still pr...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide.Carbon dioxide
Sulfonate
null
null
c1ccccc1
Other
CO
75
null
O=C=O.O=S(=O)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCc1ccccc1.[Li+]>CO>[Li][O]S(=O)(=O)C(F)(F)C(F)(F)C(F)(F)C(F)(F)OCc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8279129301e5482eb7927fbcb8008844
O=C(O)c1cc(C(=O)O)c(C(=O)O)cc1C(=O)O>>O=C(O)C1CC(C(=O)O)C(C(=O)O)CC1C(=O)O
[H][H].[H][H].C(C=1C(C(=O)O)=CC(C(=O)O)=C(C(=O)O)C1)(=O)O.[H][H]>>C1(C(CC(C(C1)C(=O)O)C(=O)O)C(=O)O)C(=O)O
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([C:7](=[O:8])[OH:9])[c:10]([C:11](=[O:12])[OH:13])[cH:14][c:15]1[C:16](=[O:17])[OH:18]>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH:6]([C:7](=[O:8])[OH:9])[CH:10]([C:11](=[O:12])[OH:13])[CH2:14][CH:15]1[C:16](=[O:17])[OH:18]
O=C(O)c1cc(C(=O)O)c(C(=O)O)cc1C(=O)O
O=C(O)C1CC(C(=O)O)C(C(=O)O)CC1C(=O)O
null
null
O
Reduction
Arene hydrogenation
cfd1f3b98f7cd3ca3735c14f302dc0acdc6f0d4501cd6920cbb5c1a3d892ff3a
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
C1CCCCC1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[c;H0;D3;+0:4]1:[cH;D2;+0:5]:[c;H0;D3;+0:6](-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]):[c;H0;D3;+0:10](-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]):[cH;D2;+0:14]:[c;H0;D3;+0:15]:1-[C:16](=[O;D1;H0:17])-[O;D1;H1:18]>>[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D3;+0:4]1-[CH2;D2;+0:5]-[CH;D3;+0:6](-[C:7](=[O;D1;H0...
85.1
[{"value": 85.0, "product": "C1(C(CC(C(C1)C(=O)O)C(=O)O)C(=O)O)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.1, "product": "C1(C(CC(C(C1)C(=O)O)C(=O)O)C(=O)O)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
2
HOUR
A 5-L Hastelloy (HC22) autoclave was charged with 552 g of pyromellitic acid, 200 g of a catalyst of Rh supported on activated carbon (available from N.E. Chemcat Corporation) and 1656 g of water, and then the inner atmosphere was replaced with nitrogen gas while stirring the contents. Then, the inner atmosphere was re...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1
C1CCCCC1
C1CCCCC1
null
O
60
2
O=C(O)c1cc(C(=O)O)c(C(=O)O)cc1C(=O)O>O>O=C(O)C1CC(C(=O)O)C(C(=O)O)CC1C(=O)O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fdaf4ca57249458b81ef5c9679d8ec9e
O=C(O)C1CC(C(=O)O)C(C(=O)O)CC1C(=O)O>>O=C1OC(=O)C2CC3C(=O)OC(=O)C3CC12
C1(C(CC(C(C1)C(=O)O)C(=O)O)C(=O)O)C(=O)O.C(C)(=O)OC(C)=O>>C1C2C(CC3C1C(=O)OC3=O)C(=O)OC2=O
O=[C:12]([OH:13])[CH:14]1[CH:8]([C:9](=[O:10])[OH:11])[CH2:7][CH:6]([C:4]([OH:3])=[O:5])[CH:16]([C:2](O)=[O:1])[CH2:15]1>>[O:1]=[C:2]1[O:3][C:4](=[O:5])[CH:6]2[CH2:7][CH:8]3[C:9](=[O:10])[O:11][C:12](=[O:13])[CH:14]3[CH2:15][CH:16]12
O=C(O)C1CC(C(=O)O)C(C(=O)O)CC1C(=O)O
O=C1OC(=O)C2CC3C(=O)OC(=O)C3CC12
null
null
null
Miscellaneous
OtherReaction
fdb3db752eaeb2c80fd8515b522bc844e84deaef56e7ac5590d174386d5f1fcb
e83a95bc3ef3bbc28a0f9ce60ccfbd3725429b901b391dbfdf0df35bff2f3261
O=C1OC(=O)C2CC3C(=O)OC(=O)C3CC12
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4]-[C:5](-[C;H0;D3;+0:6](=O)-[OH;D1;+0:7])-[C:8]-[C:9](=[O;D1;H0:10])-[OH;D1;+0:11])-[C:12]-[C:13](=[O;D1;H0:14])-[OH;D1;+0:15]>>[O;D1;H0:10]=[C:9]1-[C:8]-[C:5](-[C:4]-[C:3]2-[C:12]-[C:13](=[O;D1;H0:14])-[O;H0;D2;+0:15]-[C;H0;D3;+0:1]-2=[O;D1;H0:2])-[C;H0;D3;+0:6](=[O;H0;D1;+0:7...
96.7
[{"value": 96.6, "product": "C1C2C(CC3C1C(=O)OC3=O)C(=O)OC2=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.7, "product": "C1C2C(CC3C1C(=O)OC3=O)C(=O)OC2=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Into a 5-L separable glass flask equipped with a Dimroth condenser, were charged 450 g of 1,2,4,5-cyclohexanetetracarboxylic acid thus obtained and 4000 g of acetic anhydride, and the inner atmosphere was replaced with nitrogen gas while stirring the contents. The contents were heated to a refluxing temperature of the ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Carboxylic acid.Carboxylic acid
Anhydride.Anhydride
null
C1OCC2CC3COCC3CC12
C1OCC2CC3COCC3CC12
HO-
null
null
null
O=C(O)C1CC(C(=O)O)C(C(=O)O)CC1C(=O)O>>O=C1OC(=O)C2CC3C(=O)OC(=O)C3CC12
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-cf997285b9ea42099c032ff04f577df5
Nc1ccccc1.O=C(O)c1ccccc1>>c1ccc(Nc2ccccc2)cc1
C(C)(C)[N-]C(C)C.[Li+].NC1=CC=CC=C1.C[Si](N[Si](C)(C)C)(C)C.[Li].NC1=CC=CC=C1.C(C1=CC=CC=C1)(=O)O.C(C1=CC=CC=C1)(=O)O.C[Si](N[Si](C)(C)C)(C)C.[Li]>>C1(=CC=CC=C1)NC1=CC=CC=C1
[cH:1]1[cH:2][cH:3][c:4]([NH2:5])[cH:12][cH:13]1.O=C(O)[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1>>[cH:1]1[cH:2][cH:3][c:4]([NH:5][c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[cH:12][cH:13]1
Nc1ccccc1.O=C(O)c1ccccc1
c1ccc(Nc2ccccc2)cc1
null
null
O1CCCC1.C(C)#N.CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
4459fb8c888ad7824c7447b1a12ec31571c303016262bf3b624feaa352de16d1
fa64142892e6dfdb381fdd81c9f6becd1fc9340df98b16c99dcdc1b0c3fb2b30
c1ccc(Nc2ccccc2)cc1
O-C(=O)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]):[c:4]:[c:5]
null
[]
-78
CELSIUS
null
null
In Scheme 1, Step A, a 2-(arylamino)-benzoic acid or diphenylamine (3) is prepared from the coupling of a suitable benzoic acid (1) and a suitable aniline (2) in the presence of a strong base, for example, lithium 1,1,1,3,3,3-hexamethyldisilazane (LiHMDS) or lithium diisopropylamide, in a polar aprotic solvent such as ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
O1CCCC1.C(C)#N.CN(C=O)C
-78
null
Nc1ccccc1.O=C(O)c1ccccc1>O1CCCC1.C(C)#N.CN(C=O)C>c1ccc(Nc2ccccc2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5e94547ceccb45d0af9b3876b217d010
C#C[Si](C)(C)C.Nc1ccc(I)cc1F>>C[Si](C)(C)C#Cc1ccc(N)c(F)c1
FC1=C(N)C=CC(=C1)I.[Si](C)(C)(C)C#C>>FC1=C(N)C=CC(=C1)C#C[Si](C)(C)C
[CH3:1][Si:2]([CH3:3])([CH3:4])[C:5]#[CH:6].I[c:7]1[cH:8][cH:9][c:10]([NH2:11])[c:12]([F:13])[cH:14]1>>[CH3:1][Si:2]([CH3:3])([CH3:4])[C:5]#[C:6][c:7]1[cH:8][cH:9][c:10]([NH2:11])[c:12]([F:13])[cH:14]1
C#C[Si](C)(C)C.Nc1ccc(I)cc1F
C[Si](C)(C)C#Cc1ccc(N)c(F)c1
null
[Cu]I.Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
C(C)OCC
C-C Coupling
Sonogashira alkyne_aryl halide
15c08902746c61a960c314898ce6bb5fcc5e189f9e057388c59dba9ec9d0c81c
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
c1ccccc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C;D1;H3:6]-[#14:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[C:10]#[CH;D1;+0:11]>>[C;D1;H3:6]-[#14:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[C:10]#[C;H0;D2;+0:11]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
15
HOUR
2-Fluoro-4-iodoaniline (5.00 g, 21.1 mmol), CuI (90 mg, 0.42 mmol), and (Ph3P)2PdCl2 (300 mg, 0.42 mmol) were weighed into a flask which was sealed and flushed with N2. A solution of TMS-acetylene (2.28 g, 23.2 mmol) in TEA (20 mL) was added, then the entire mixture stirred 15 hours at room temperature. The reaction mi...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1
HI
[Cu]I.Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C(C)OCC
null
15
C#C[Si](C)(C)C.Nc1ccc(I)cc1F>[Cu]I.Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C(C)OCC>C[Si](C)(C)C#Cc1ccc(N)c(F)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1af78b468b504952ac05aa866c280e95
C[Si](C)(C)C#Cc1ccc(N)c(F)c1.O=C(O)c1ccc(F)c(F)c1F>>C[Si](C)(C)C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1
[Li+].C[Si](C)(C)[N-][Si](C)(C)C.FC1=C(N)C=CC(=C1)C#C[Si](C)(C)C.FC1=C(C(=O)O)C=CC(=C1F)F>>FC=1C(=C(C(=O)O)C=CC1F)NC1=C(C=C(C=C1)C#C[Si](C)(C)C)F
[CH3:1][Si:2]([CH3:3])([CH3:4])[C:5]#[C:6][c:7]1[cH:8][cH:9][c:10]([NH2:11])[c:23]([F:24])[cH:25]1.F[c:12]1[c:13]([C:14](=[O:15])[OH:16])[cH:17][cH:18][c:19]([F:20])[c:21]1[F:22]>>[CH3:1][Si:2]([CH3:3])([CH3:4])[C:5]#[C:6][c:7]1[cH:8][cH:9][c:10]([NH:11][c:12]2[c:13]([C:14](=[O:15])[OH:16])[cH:17][cH:18][c:19]([F:20])[...
C[Si](C)(C)C#Cc1ccc(N)c(F)c1.O=C(O)c1ccc(F)c(F)c1F
C[Si](C)(C)C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(Nc2ccccc2)cc1
F-[c;H0;D3;+0:1](:[c:2](-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]):[c:6]):[c:7](-[F;D1;H0:8]):[c:9].[NH2;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[F;D1;H0:8]-[c:7](:[c:9]):[c;H0;D3;+0:1](-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13]):[c:2](-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]):[c:6]
59
[{"value": 59.0, "product": "FC=1C(=C(C(=O)O)C=CC1F)NC1=C(C=C(C=C1)C#C[Si](C)(C)C)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 59.0, "product": "FC=1C(=C(C(=O)O)C=CC1F)NC1=C(C=C(C=C1)C#C[Si](C)(C)C)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
15
HOUR
A mixture of the product of Step A, 2-fluoro-4-[(trimethylsilyl)ethynyl]aniline (3.85 g, 18.6 mmol) and 2,3,4-trifluorobenzoic acid (3.27 g, 18.6 mmol) was dissolved in dry THF (25 mL). The flask was fitted with a pressure-equalising dropping funnel and the entire apparatus evacuated and flushed with N2. The solution w...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HF
C1CCOC1
-78
15
C[Si](C)(C)C#Cc1ccc(N)c(F)c1.O=C(O)c1ccc(F)c(F)c1F>C1CCOC1>C[Si](C)(C)C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fc919ded7e0b4f518a6fe0d13ab6a378
C[Si](C)(C)C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1>>C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1
FC=1C(=C(C(=O)O)C=CC1F)NC1=C(C=C(C=C1)C#C[Si](C)(C)C)F.C(=O)([O-])[O-].[K+].[K+]>>FC=1C(=C(C(=O)O)C=CC1F)NC1=C(C=C(C=C1)C#C)F
C[Si](C)(C)[C:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH:7][c:8]2[c:9]([C:10](=[O:11])[OH:12])[cH:13][cH:14][c:15]([F:16])[c:17]2[F:18])[c:19]([F:20])[cH:21]1>>[CH:1]#[C:2][c:3]1[cH:4][cH:5][c:6]([NH:7][c:8]2[c:9]([C:10](=[O:11])[OH:12])[cH:13][cH:14][c:15]([F:16])[c:17]2[F:18])[c:19]([F:20])[cH:21]1
C[Si](C)(C)C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1
C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1
null
null
CO
Deprotection
TMS deprotection from alkyne
e85676bb81da384790c9c858d44f182cdd01e3a79f77f7a239fe38487234cb96
56d526d7c9cb1bd7bee4940e216a9b1dd4597fd025a186b8d6e4675d8f4db26b
c1ccc(Nc2ccccc2)cc1
C-[Si](-C)(-C)-[C;H0;D2;+0:1]#[C:2]-[c:3]>>[CH;D1;+0:1]#[C:2]-[c:3]
99
[{"value": 99.0, "product": "FC=1C(=C(C(=O)O)C=CC1F)NC1=C(C=C(C=C1)C#C)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.0, "product": "FC=1C(=C(C(=O)O)C=CC1F)NC1=C(C=C(C=C1)C#C)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
HOUR
The product of Step B, 3,4-difluoro-2-[[2-fluoro-4-(trimethylsilylethynyl)phenyl]amino]benzoic acid (3.99 g, 11.0 mmol), was dissolved in MeOH (200 mL), to which was added K2CO3 (3.03 g, 22.0 mmol). This mixture was stirred at room temperature for 15 hours, then the reaction solvent removed under reduced pressure. The ...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Silyl protective group
Alkyne
null
null
c1ccccc1.c1ccccc1
Other
CO
null
15
C[Si](C)(C)C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1>CO>C#Cc1ccc(Nc2c(C(=O)O)ccc(F)c2F)c(F)c1