dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-716f9534c2df48828b24217a5065dbca
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCC1=CCCc2ccccc21>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCC1=CCCc2ccccc21
C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.Cl.C1(=CCCC2=CC=CC=C12)CCN>>C1(=CCCC2=CC=CC=C12)CCNC(C(C)(CC1=CNC2=CC=CC=C12)NC(OC1C2CC3CC(CC1C3)C2)=O)=O
O[C:27]([C:2]([CH3:1])([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12)[NH:13][C:14](=[O:15])[O:16][CH:17]1[CH:18]2[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23]2)[CH2:24][CH:25]1[CH2:26]3)=[O:28].[NH2:29][CH2:30][CH2:31][C:32]1=[CH:33][CH2:34][CH2:35][c:36]2[cH:37][cH:38][cH:39][cH:40][c:41]21>>[CH3:1][C:2...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCC1=CCCc2ccccc21
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCC1=CCCc2ccccc21
null
null
null
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCC1=CCCc2ccccc21)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]=[C:10]-[C:11]-[C:12]-[NH2;D1;+0:13]>>[C:9]=[C:10]-[C:11]-[C:12]-[NH;D2;+0:13]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8]
null
[]
null
null
null
null
Following the procedure of Example 70, the title compound was prepared from 0.50 g (1.26 mmol) of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan and 0.29 g (1.38 mmol) of 3,4-dihydro-1-naphthalene-ethanamine hydrochloride. The purified product after chromatography was obtained as a white foam, 0.41 g (59%); 1H NMR (CDCl...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.C1=Cc2ccccc2CC1.C1C2CC3CC1CC(C2)C3
HO-
null
null
null
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCC1=CCCc2ccccc21>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCC1=CCCc2ccccc21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-656af9e4f60848a7981ea7b0d9518cf5
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1cccs1>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1cccs1
C(C)N(CC)CC.Cl.S1C(=CC=C1)CCN.C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.ON1N=NC2=C1C=CC=C2.CN(CCCN=C=NCC)C>>N1C=C(C2=CC=CC=C12)CC(C(NCCC=1SC=CC1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O
O[C:27]([C:2]([CH3:1])([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12)[NH:13][C:14](=[O:15])[O:16][CH:17]1[CH:18]2[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23]2)[CH2:24][CH:25]1[CH2:26]3)=[O:28].[NH2:29][CH2:30][CH2:31][c:32]1[cH:33][cH:34][cH:35][s:36]1>>[CH3:1][C:2]([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8]...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1cccs1
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1cccs1
null
null
CN(C=O)C.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1cccs1)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8]
61
[{"value": 61.0, "product": "N1C=C(C2=CC=CC=C12)CC(C(NCCC=1SC=CC1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.7, "product": "N1C=C(C2=CC=CC=C12)CC(C(NCCC=1SC=CC1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan (0,401 g, 1.01 mmol) in dry ethyl acetate (6 mL) and N,N-dimethylformamide (4 mL) under nitrogen atmosphere was added 1-hydroxybenzotriazole (0.138 g, 1.02 mmol) followed by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (0.199 g, 1.04 mmol). this mixture wa...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccsc1.c1ccc2[nH]ccc2c1.C1C2CC3CC1CC(C2)C3
HO-
CN(C=O)C.C(C)(=O)OCC
null
2
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1cccs1>CN(C=O)C.C(C)(=O)OCC>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1cccs1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-61c6d8aabb5a41be87f76a5ca9c7a047
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.Cn1cccc1CCN>>Cn1cccc1CCNC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3
NCCC=1N(C=CC1)C.CN(CCCN=C=NCC)C.C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.ON1N=NC2=C1C=CC=C2>>N1C=C(C2=CC=CC=C12)CC(C(=O)NCCC=1N(C=CC1)C)(C)NC(OC1C2CC3CC(CC1C3)C2)=O
O[C:10](=[O:11])[C:12]([CH3:13])([CH2:14][c:15]1[cH:16][nH:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]12)[NH:24][C:25](=[O:26])[O:27][CH:28]1[CH:29]2[CH2:30][CH:31]3[CH2:32][CH:33]([CH2:34]2)[CH2:35][CH:36]1[CH2:37]3.[CH3:1][n:2]1[cH:3][cH:4][cH:5][c:6]1[CH2:7][CH2:8][NH2:9]>>[CH3:1][n:2]1[cH:3][cH:4][cH:5][c:6]1[CH2:...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.Cn1cccc1CCN
Cn1cccc1CCNC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3
null
null
CN(C=O)C.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccc[nH]1)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:4]-[C:3](-[C;D1;H3:5])(-[#7:6]-[C:7]=[O;D1;H0:8])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:11]-[C:10]-[C:9]
null
[]
null
null
2
HOUR
To a solution of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan (0.401 g, 1.01 mmol) in dry ethyl acetate (4 mL) and N,N-dimethylformamide (4 mL) under nitrogen atmosphere was added 1-hydroxybenzotriazole (0.139 g, 1.03 mmol) followed by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (0.199 g, 1.04 mmol). This mixture wa...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc[nH]1.c1ccc2[nH]ccc2c1.C1C2CC3CC1CC(C2)C3
HO-
CN(C=O)C.C(C)(=O)OCC
null
2
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.Cn1cccc1CCN>CN(C=O)C.C(C)(=O)OCC>Cn1cccc1CCNC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ec175e3168cb4a1d9c1c6ae6b0efcecf
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccccn1>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccn1
NCCC1=NC=CC=C1.Cl.CN(CCCN=C=NCC)C.C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.ON1N=NC2=C1C=CC=C2>>N1C=C(C2=CC=CC=C12)CC(C(NCCC1=NC=CC=C1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O
O[C:27]([C:2]([CH3:1])([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12)[NH:13][C:14](=[O:15])[O:16][CH:17]1[CH:18]2[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23]2)[CH2:24][CH:25]1[CH2:26]3)=[O:28].[NH2:29][CH2:30][CH2:31][c:32]1[cH:33][cH:34][cH:35][cH:36][n:37]1>>[CH3:1][C:2]([CH2:3][c:4]1[cH:5][nH:6][c:7]...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccccn1
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccn1
null
null
CN(C=O)C.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccccn1)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8]
72.2
[{"value": 72.0, "product": "N1C=C(C2=CC=CC=C12)CC(C(NCCC1=NC=CC=C1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.2, "product": "N1C=C(C2=CC=CC=C12)CC(C(NCCC1=NC=CC=C1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan (0.400 g, 1.01 mmol) in ethyl acetate (6 mL) and N,N-dimethylformamide (4 mL) under nitrogen atmosphere was added 1-hydroxybenzotriazole (0.138 g, 1.02 mmol) followed by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (0.198 g, 1.03 mmol). This ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.c1ccncc1.C1C2CC3CC1CC(C2)C3
HO-
CN(C=O)C.C(C)(=O)OCC
null
2
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccccn1>CN(C=O)C.C(C)(=O)OCC>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccn1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7194255956584fd99d5e7200184f0486
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1c[nH]cn1>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1c[nH]cn1
C(C)N(CC)CC.Cl.Cl.NCCC1=CNC=N1.C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.FC1=C(C(=C(C(=C1O)F)F)F)F.CN(CCCN=C=NCC)C>>N1C=NC(=C1)CCNC(C(C)(CC1=CNC2=CC=CC=C12)NC(OC1C2CC3CC(CC1C3)C2)=O)=O
O[C:27]([C:2]([CH3:1])([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12)[NH:13][C:14](=[O:15])[O:16][CH:17]1[CH:18]2[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23]2)[CH2:24][CH:25]1[CH2:26]3)=[O:28].[NH2:29][CH2:30][CH2:31][c:32]1[cH:33][nH:34][cH:35][n:36]1>>[CH3:1][C:2]([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8]...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1c[nH]cn1
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1c[nH]cn1
null
null
CN(C=O)C.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1c[nH]cn1)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8]
47.3
[{"value": 47.0, "product": "N1C=NC(=C1)CCNC(C(C)(CC1=CNC2=CC=CC=C12)NC(OC1C2CC3CC(CC1C3)C2)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 47.3, "product": "N1C=NC(=C1)CCNC(C(C)(CC1=CNC2=CC=CC=C12)NC(OC1C2CC3CC(CC1C3)C2)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan (0.401 g, 1.01 mmol) in dry ethyl acetate (6 mL) and N,N-dimethylformamide (4 mL) under nitrogen atmosphere was added pentafluorophenol (0.189 g, 1.03 mmol) followed by 1-(3-dimethylaminopropyl)-3-ethyl carbodiimide (0.200 g, 1.04 mmol). This mixture was st...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1c[nH]cn1.c1ccc2[nH]ccc2c1.C1C2CC3CC1CC(C2)C3
HO-
CN(C=O)C.C(C)(=O)OCC
null
2
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1c[nH]cn1>CN(C=O)C.C(C)(=O)OCC>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1c[nH]cn1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-becfad45d9734a6d87f686999f99d161
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1cnccn1>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1cnccn1
C(C)N(CC)CC.Cl.N1=C(C=NC=C1)CCN.C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.O.ON1N=NC2=C1C=CC=C2.C1(CCCCC1)N=C=NC1CCCCC1>>N1C=C(C2=CC=CC=C12)CC(C(NCCC1=NC=CN=C1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O
O[C:27]([C:2]([CH3:1])([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12)[NH:13][C:14](=[O:15])[O:16][CH:17]1[CH:18]2[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23]2)[CH2:24][CH:25]1[CH2:26]3)=[O:28].[NH2:29][CH2:30][CH2:31][c:32]1[cH:33][n:34][cH:35][cH:36][n:37]1>>[CH3:1][C:2]([CH2:3][c:4]1[cH:5][nH:6][c:7]2...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1cnccn1
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1cnccn1
null
null
O.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1cnccn1)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8]
63.2
[{"value": 63.0, "product": "N1C=C(C2=CC=CC=C12)CC(C(NCCC1=NC=CN=C1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.2, "product": "N1C=C(C2=CC=CC=C12)CC(C(NCCC1=NC=CN=C1)=O)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.75
HOUR
A room temperature solution of 0.40 g (1.01 mmol) of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan and 0.15 g (1.11 mmol) of 1-hydroxybenzotriazole hydrate in 15 mL of anhydrous ethyl acetate under N2 atmosphere was treated with 0.23 g (1.11 mmol) of 1,3-dicyclohexylcarbodiimide in one portion. The reaction was stirred...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.c1cnccn1.C1C2CC3CC1CC(C2)C3
HO-
O.C(C)(=O)OCC
null
1.75
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1cnccn1>O.C(C)(=O)OCC>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1cnccn1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7786619ae1dc47dd91ffb8bbbb049c69
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccco1>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccco1
C(C)N(CC)CC.Cl.O1C(=CC=C1)CCN.C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.O.ON1N=NC2=C1C=CC=C2.Cl.CN(CCCN=C=NCC)C>>O1C(=CC=C1)CCNC(C(C)(CC1=CNC2=CC=CC=C12)NC(OC1C2CC3CC(CC1C3)C2)=O)=O
O[C:27]([C:2]([CH3:1])([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12)[NH:13][C:14](=[O:15])[O:16][CH:17]1[CH:18]2[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23]2)[CH2:24][CH:25]1[CH2:26]3)=[O:28].[NH2:29][CH2:30][CH2:31][c:32]1[cH:33][cH:34][cH:35][o:36]1>>[CH3:1][C:2]([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8]...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccco1
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccco1
null
null
O.CN(C=O)C.C(C)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccco1)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8]
70
[{"value": 70.0, "product": "O1C(=CC=C1)CCNC(C(C)(CC1=CNC2=CC=CC=C12)NC(OC1C2CC3CC(CC1C3)C2)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.9, "product": "O1C(=CC=C1)CCNC(C(C)(CC1=CNC2=CC=CC=C12)NC(OC1C2CC3CC(CC1C3)C2)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.75
HOUR
A room temperature solution of 0.30 g (0.76 mmol) of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan and 0.11 g (0.81 mmol) of 1-hydroxybenzotriazole hydrate in 10 mL of anhydrous N,N-dimethylformamide under N2 atmosphere was treated with 0.16 g (0.83 mmol 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride in on...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccoc1.c1ccc2[nH]ccc2c1.C1C2CC3CC1CC(C2)C3
HO-
O.CN(C=O)C.C(C)OCC
null
1.75
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccco1>O.CN(C=O)C.C(C)OCC>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccco1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-05e081f90841429c9b821ae03ea8e13a
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccc2ccccc2n1>>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc2ccccc2n1
NCCC1=NC2=CC=CC=C2C=C1.C12C(C3CC(CC(C1)C3)C2)OC(=O)NC(CC2=CNC3=CC=CC=C23)(C(=O)O)C.CN1CCOCC1.ClC(=O)OCC(C)C>>N1C=C(C2=CC=CC=C12)CC(C(=O)NCCC1=NC2=CC=CC=C2C=C1)(C)NC(OC1C2CC3CC(CC1C3)C2)=O
O[C:27]([C:2]([CH3:1])([CH2:3][c:4]1[cH:5][nH:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]12)[NH:13][C:14](=[O:15])[O:16][CH:17]1[CH:18]2[CH2:19][CH:20]3[CH2:21][CH:22]([CH2:23]2)[CH2:24][CH:25]1[CH2:26]3)=[O:28].[NH2:29][CH2:30][CH2:31][c:32]1[cH:33][cH:34][c:35]2[cH:36][cH:37][cH:38][cH:39][c:40]2[n:41]1>>[CH3:1][C:2]([C...
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccc2ccccc2n1
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc2ccccc2n1
null
null
C1CCOC1
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NCCc1ccc2ccccc2n1)OC1C2CC3CC(C2)CC1C3
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8]
17.3
[{"value": 17.0, "product": "N1C=C(C2=CC=CC=C12)CC(C(=O)NCCC1=NC2=CC=CC=C2C=C1)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 17.3, "product": "N1C=C(C2=CC=CC=C12)CC(C(=O)NCCC1=NC2=CC=CC=C2C=C1)(C)NC(OC1C2CC3CC(CC1C3)C2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": f...
-22
CELSIUS
1
HOUR
To a stirred solution of 2-adamantyloxycarbonyl-α-methyl-DL-tryptophan (1.59 g, 4.0 mmole) in dry THF (50 mL) at -22° C. was added N-methylmorpholine (0.644 g, 6.3 mmole) and isobutyl chloroformate (0.632 g, 4.6 mmole). The mixture was stirred at -22° C. for 1 hour and then a solution of 2-(2-aminoethyl)quinoline (0.69...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.c1ccc2ncccc2c1.C1C2CC3CC1CC(C2)C3
HO-
C1CCOC1
-22
1
CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)O.NCCc1ccc2ccccc2n1>C1CCOC1>CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc2ccccc2n1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2045145affa643dba59de3928e171cbb
COC(=O)C(N)Cc1c[nH]c2ccccc12.C[Si](C)(C)CCOCCl>>COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C
C[Si](C)(C)CCOCCl.C1CCOC1.COC(=O)C(CC1=CNC2=CC=CC=C21)N.C(C)(C)[N-]C(C)C.[Li+].C1CCOC1.C1CCOC1>>COC(C(NCOC(C)[Si](C)(C)C)CC1=CNC2=CC=CC=C12)=O
[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][nH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]12)[NH2:16].Cl[CH2:17][O:18][CH2:20][CH2:19][Si:21]([CH3:22])([CH3:23])[CH3:24]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][nH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]12)[NH:16][CH2:17][O:18][CH:19]([CH3:20])[S...
COC(=O)C(N)Cc1c[nH]c2ccccc12.C[Si](C)(C)CCOCCl
COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
b600a81df87bea1685df54aaf8b30bd23674e9b7dd2a3cc8662e71bd3684ebef
d995b0d46e4aacf6b403d700b3e57edde7ae1aa34d450d1418ad3604b33a8a71
c1ccc2[nH]ccc2c1
Cl-[CH2;D2;+0:1]-[O;H0;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[#14:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].[C:9]-[C:10](-[NH2;D1;+0:11])-[C:12](=[O;D1;H0:13])-[#8:14]-[C;D1;H3:15]>>[C:9]-[C:10](-[NH;D2;+0:11]-[CH2;D2;+0:1]-[O;H0;D2;+0:2]-[CH;D3;+0:4](-[CH3;D1;+0:3])-[#14:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8])-[C:...
44
[{"value": 44.0, "product": "COC(C(NCOC(C)[Si](C)(C)C)CC1=CNC2=CC=CC=C12)=O", "details": "PERCENTYIELD", "is_desired": false}]
-10
CELSIUS
45
MINUTE
A solution of DL-tryptophan methyl esterbenzaldimine (4.0 g, 13 mmol) in 30 mL THF was added over 15 minutes to a mixture of 20.2 mL lithiumdiisopropylamide (10% suspension in hexan) and 70 mL dry THF, cooled to -10° C. under nitrogen atmosphere. The stirring was continued for an additional 45 minutes, keeping the temp...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary amine
Ether.Secondary amine
null
null
c1ccc2[nH]ccc2c1
HCl
null
-10
0.75
COC(=O)C(N)Cc1c[nH]c2ccccc12.C[Si](C)(C)CCOCCl>>COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c16042dc65ff40eb8e55e17df4d32ef8
COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C.O=C(Cl)OC1C2CC3CC(C2)CC1C3>>COC(=O)C(Cc1c[nH]c2ccccc12)N(COC(C)[Si](C)(C)C)C(=O)OC1C2CC3CC(C2)CC1C3
COC(C(NCOC(C)[Si](C)(C)C)CC1=CNC2=CC=CC=C12)=O.C(C)(C)N(CC)C(C)C.C12C(C3CC(CC(C1)C3)C2)OC(=O)Cl>>COC(C(N(C(=O)OC1C2CC3CC(CC1C3)C2)COC(C)[Si](C)(C)C)CC2=CNC3=CC=CC=C23)=O
[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][nH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]12)[NH:16][CH2:17][O:18][CH:19]([CH3:20])[Si:21]([CH3:22])([CH3:23])[CH3:24].Cl[C:25](=[O:26])[O:27][CH:28]1[CH:29]2[CH2:30][CH:31]3[CH2:32][CH:33]([CH2:34]2)[CH2:35][CH:36]1[CH2:37]3>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:...
COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C.O=C(Cl)OC1C2CC3CC(C2)CC1C3
COC(=O)C(Cc1c[nH]c2ccccc12)N(COC(C)[Si](C)(C)C)C(=O)OC1C2CC3CC(C2)CC1C3
null
null
O.C1CCOC1
Protection
N-alkylation of secondary amines with alkyl halides
496a200c7c2fc7c000296e03cda40efb8e258ccaeb02fa999285bf74ddc49346
d86dc1e6d0e089b3444b62ddfcf4c4822bdac4b60e628553036562518c29adcd
O=C(NCCc1c[nH]c2ccccc12)OC1C2CC3CC(C2)CC1C3
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#8:5]-[C:6]-[NH;D2;+0:7]-[C:8](-[C:9])-[C:10](=[O;D1;H0:11])-[#8:12]-[C;D1;H3:13]>>[#8:5]-[C:6]-[N;H0;D3;+0:7](-[C:8](-[C:9])-[C:10](=[O;D1;H0:11])-[#8:12]-[C;D1;H3:13])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]
67.8
[{"value": 67.8, "product": "COC(C(N(C(=O)OC1C2CC3CC(CC1C3)C2)COC(C)[Si](C)(C)C)CC2=CNC3=CC=CC=C23)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.8, "product": "COC(C(N(C(=O)OC1C2CC3CC(CC1C3)C2)COC(C)[Si](C)(C)C)CC2=CNC3=CC=CC=C23)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A mixture of α-trimethylsilylethoxymethyl-DL-tryptophan methyl ester (1.0 g, 2.8 mmol), diisopropylethylamine (0.4 g, 3 mmol) and 2-adarnantylchloroformate (0.65 g, 3 mmol) in 20 mL dry THF was stirred at room temperature for 4 hours. The reaction mixture was diluted with distilled water and extracted with ethyl acetat...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Secondary amine
Carbamic ester
null
null
c1ccc2[nH]ccc2c1.C1C2CC3CC1CC(C2)C3
HCl
O.C1CCOC1
null
4
COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C.O=C(Cl)OC1C2CC3CC(C2)CC1C3>O.C1CCOC1>COC(=O)C(Cc1c[nH]c2ccccc12)N(COC(C)[Si](C)(C)C)C(=O)OC1C2CC3CC(C2)CC1C3
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4a62f664045b4f719a06c2ba54a774ab
COC(=O)C(Cc1c[nH]c2ccccc12)N(COC(C)[Si](C)(C)C)C(=O)OC1C2CC3CC(C2)CC1C3>>CC(OCN(C(=O)OC1C2CC3CC(C2)CC1C3)C(Cc1c[nH]c2ccccc12)C(=O)O)[Si](C)(C)C
Cl.COC(C(N(C(=O)OC1C2CC3CC(CC1C3)C2)COC(C)[Si](C)(C)C)CC2=CNC3=CC=CC=C23)=O.[Li+].[OH-].O1CCOCC1>>C12C(C3CC(CC(C1)C3)C2)OC(=O)N(C(CC2=CNC3=CC=CC=C23)C(=O)O)COC(C)[Si](C)(C)C
C[O:32][C:30]([CH:19]([N:5]([CH2:4][O:3][CH:2]([CH3:1])[Si:33]([CH3:34])([CH3:35])[CH3:36])[C:6](=[O:7])[O:8][CH:9]1[CH:10]2[CH2:11][CH:12]3[CH2:13][CH:14]([CH2:15]2)[CH2:16][CH:17]1[CH2:18]3)[CH2:20][c:21]1[cH:22][nH:23][c:24]2[cH:25][cH:26][cH:27][cH:28][c:29]12)=[O:31]>>[CH3:1][CH:2]([O:3][CH2:4][N:5]([C:6](=[O:7])[...
COC(=O)C(Cc1c[nH]c2ccccc12)N(COC(C)[Si](C)(C)C)C(=O)OC1C2CC3CC(C2)CC1C3
CC(OCN(C(=O)OC1C2CC3CC(C2)CC1C3)C(Cc1c[nH]c2ccccc12)C(=O)O)[Si](C)(C)C
null
null
O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(NCCc1c[nH]c2ccccc12)OC1C2CC3CC(C2)CC1C3
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]
91.8
[{"value": 91.7, "product": "C12C(C3CC(CC(C1)C3)C2)OC(=O)N(C(CC2=CNC3=CC=CC=C23)C(=O)O)COC(C)[Si](C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.8, "product": "C12C(C3CC(CC(C1)C3)C2)OC(=O)N(C(CC2=CNC3=CC=CC=C23)C(=O)O)COC(C)[Si](C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
16
HOUR
A mixture of N-[(2-adamantyloxy)carbonyl]-α-trimethylsilylethoxymethyl-DL-tryptophan methyl ester (4.5 g, 8.5 mmol), LiOH (0.22 g, 9.1 mmol), dioxane (90 mL), and water (30 mL) was stirred at 60° C. for 16 hours. After cooling, the reaction mixture was acidified to pH 4 with 1N hydrochloric acid and extracted with ethy...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2[nH]ccc2c1.C1C2CC3CC1CC(C2)C3
Other
O
60
16
COC(=O)C(Cc1c[nH]c2ccccc12)N(COC(C)[Si](C)(C)C)C(=O)OC1C2CC3CC(C2)CC1C3>O>CC(OCN(C(=O)OC1C2CC3CC(C2)CC1C3)C(Cc1c[nH]c2ccccc12)C(=O)O)[Si](C)(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-57f8129fa3464cad91a4662f4e8ab2fb
COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C>>COC(=O)C(N)(CO)Cc1c[nH]c2ccccc12
COC(C(NCOC(C)[Si](C)(C)C)CC1=CNC2=CC=CC=C12)=O.C(C)(=O)OCC>>COC(C(N)(CC1=CNC2=CC=CC=C12)CO)=O
CC([Si](C)(C)C)[O:8][CH2:7][NH:6][CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH2:9][c:10]1[cH:11][nH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12>>[CH3:1][O:2][C:3](=[O:4])[C:5]([NH2:6])([CH2:7][OH:8])[CH2:9][c:10]1[cH:11][nH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12
COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C
COC(=O)C(N)(CO)Cc1c[nH]c2ccccc12
null
null
FC(C(=O)O)(F)F
Miscellaneous
OtherReaction
f4a1a9f21e7e8515dc7a4b1f8faa9b0cbf9a43438874da739540d6f45e6febbd
da56836e50fc8ebc4ed3ba37b3d761a3463c51e4e2154a888c5f4909cc73f12b
c1ccc2[nH]ccc2c1
C-C(-[O;H0;D2;+0:1]-[CH2;D2;+0:2]-[NH;D2;+0:3]-[CH;D3;+0:4](-[C:5]-[c:6]:[c:7]:[#7;a:8])-[C:9](=[O;D1;H0:10])-[#8:11]-[C;D1;H3:12])-[Si](-C)(-C)-C>>[#7;a:8]:[c:7]:[c:6]-[C:5]-[C;H0;D4;+0:4](-[NH2;D1;+0:3])(-[CH2;D2;+0:2]-[OH;D1;+0:1])-[C:9](=[O;D1;H0:10])-[#8:11]-[C;D1;H3:12]
null
[]
null
null
null
null
α-Trimethylsilylethoxymethyl-DL-tryptophan methyl ester (1.0 g, 2.8 mmol) was stirred for 48 hours at room temperature in trifluoroacetic acid (10 mL). After evaporation of the acid in vacuo, the oily residue was treated with aqueous sodium bicarbonate and extracted with ethyl acetate. The organic layer was dried over ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Secondary amine.Silyl protective group
Ester.Primary alcohol.Primary amine
null
null
c1ccc2[nH]ccc2c1
Other
FC(C(=O)O)(F)F
null
null
COC(=O)C(Cc1c[nH]c2ccccc12)NCOC(C)[Si](C)(C)C>FC(C(=O)O)(F)F>COC(=O)C(N)(CO)Cc1c[nH]c2ccccc12
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e43d263a87e646cca91cfc51f8006d76
CCOC(=O)c1cc2ccccc2[nH]1.Cc1ccc(S(=O)(=O)Cl)cc1>>CCOC(=O)c1cc2ccccc2n1S(=O)(=O)c1ccc(C)cc1
[H-].[Na+].C1(=CC=C(C=C1)S(=O)(=O)Cl)C.C(C)OC(=O)C=1NC2=CC=CC=C2C1>>C(C)OC(=O)C=1N(C2=CC=CC=C2C1)S(=O)(=O)C1=CC=C(C=C1)C
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[nH:14]1.Cl[S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][c:21]([CH3:22])[cH:23][cH:24]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[n:14]1[S:15](=[O:16])(=[O:17])[c:18]1[cH:19][cH:20][c:21]([CH3...
CCOC(=O)c1cc2ccccc2[nH]1.Cc1ccc(S(=O)(=O)Cl)cc1
CCOC(=O)c1cc2ccccc2n1S(=O)(=O)c1ccc(C)cc1
null
null
C1CCOC1
Acylation
OtherReaction
1f9175819c9c0179267ecae12f340317ed0385d3996f36daaf36cb61a5ef4625
b7cf703ff8ec1befb0c6e5230d29d7904f3e22c3606b15633c7e7a7fc4abca48
O=S(=O)(c1ccccc1)n1ccc2ccccc21
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[c:11]1:[c:12]:[c:13]:[c:14](:[c:15]):[nH;D2;+0:16]:1>>[C:7]-[#8:8]-[C:9](=[O;D1;H0:10])-[c:11]1:[c:12]:[c:13]:[c:14](:[c:15]):[n;H0;D3;+0:16]:1-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
30
CELSIUS
null
null
To a stirred suspension of sodium hydride (3.7 g, 120 mmol, 80% in paraffin oil) in dry THF (75 mL), a solution of indol-2-carboxylic acid ethyl ester (18.9 g, 100 mmol) in dry THF (75 mL) was added in 1 hour with stirring while the inner temperature was maintained under 30° C. The reaction mixture was stirred for 30 m...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Sulfonyl halide
Tosylate
c1ccc2[nH]ccc2c1
c1cc2ccccc2[nH]1
c1cc2ccccc2[nH]1.c1ccccc1
HCl
C1CCOC1
30
null
CCOC(=O)c1cc2ccccc2[nH]1.Cc1ccc(S(=O)(=O)Cl)cc1>C1CCOC1>CCOC(=O)c1cc2ccccc2n1S(=O)(=O)c1ccc(C)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-bd07e98aceef4b509d4e39b6ba9624c9
CC1(C)CCC(C)(C)c2cc(C(=O)CBr)ccc21>>CC1(C)CCC(C)(C)c2ccccc21
BrCC(=O)C=1C=C2C(CCC(C2=CC1)(C)C)(C)C.SCCS(=O)(=O)O.[Na].C([O-])([O-])=O.[K+].[K+]>>[Na].CC1(CCC(C2=CC=CC=C12)(C)C)C
O=C(CBr)[c:11]1[cH:10][c:9]2[c:14]([cH:13][cH:12]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]2([CH3:7])[CH3:8]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]21
CC1(C)CCC(C)(C)c2cc(C(=O)CBr)ccc21
CC1(C)CCC(C)(C)c2ccccc21
null
null
O.CN(C)C=O.C(C)(=O)OCC.C1CCOC1
Reduction
OtherReaction
5ab4144bb99e4b2d73510be0cdfcb7cadb6ac496474c2b2bde8c6a8b2cda5acf
a90507cbf9a8f6b61ec3939c06e1d4feba68ffc1aa9586e1ab836849ec480723
c1ccc2c(c1)CCCC2
Br-C-C(=O)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]>>[c:5]:[c:4]:[cH;D2;+0:1]:[c:2]:[c:3]
null
[]
null
null
30
MINUTE
To a solution of 6-(bromoacetyl)-1,2,3,4-tetrahydro-1,1,4,4-tetramethylnaphthalene (12) (15.5 mg, 0.050 mmol) in DMF (0.13 mL) and THF (0.13 mL) was added a freshly prepared solution of 2-mercapto-1-ethanesulfonic acid, sodium salt (2) (25 mg, 0.15 mmol) and potassium carbonate (21 mg, 0.15 mmol) in water (0.15 mL) at ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
null
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HBr
O.CN(C)C=O.C(C)(=O)OCC.C1CCOC1
null
0.5
CC1(C)CCC(C)(C)c2cc(C(=O)CBr)ccc21>O.CN(C)C=O.C(C)(=O)OCC.C1CCOC1>CC1(C)CCC(C)(C)c2ccccc21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d0e5da991214455380f3f6ed9e4608b4
O=S(=O)([O-])[O-].[Cu]>>O=S(=O)([O-])[O-].[Cu+2]
S(=O)(=O)([O-])[O-].[Cu].C([O-])([O-])=O.[Cl-].[N+](=O)([O-])[O-].[Cu].C(CC(O)(C(=O)O)CC(=O)O)(=O)O.P(=O)([O-])([O-])[O-]>>S(=O)(=O)([O-])[O-].[Cu+2].C(CC(O)(C(=O)O)CC(=O)O)(=O)O
[O:14]=[S:15](=[O:16])([O-:17])[O-:18].[Cu:19]>>[O:14]=[S:15](=[O:16])([O-:17])[O-:18].[Cu+2:19]
O=S(=O)([O-])[O-].[Cu]
O=S(=O)([O-])[O-].[Cu+2]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[Cu;H0;D0;+0:1]>>[Cu+2;H0;D0:1]
null
[]
null
null
null
null
This example presents a synopsis of biocidal solution design calculations for a biocidal solution comprised of citric acid (the ligand, or complexing agent) and copper. One gallon of sewage effluent containing bacteria could be treated with one drop of stock solution prepared as follows. For this example, a biocide sol...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
O=S(=O)([O-])[O-].[Cu]>>O=S(=O)([O-])[O-].[Cu+2]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6cbbb1d8fe334f629a24aeb25dde05cd
O=P1([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])O1.[Na+].[Na+]>>O=C([O-])[O-].OO.OO.[Na+].[Na+]
C([O-])([O-])=O.[Na+].[Na+].OO.[O-]P1(=O)OP(=O)(OP(=O)(OP(=O)(OP(=O)(OP(=O)(O1)[O-])[O-])[O-])[O-])[O-].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]>>C(=O)([O-])[O-].C(=O)([O-])[O-].OO.OO.OO.[Na+].[Na+].[Na+].[Na+]
O=P1([O-])OP(=O)([O-:5])OP(=O)([O-:9])OP([O-:11])(=[O:12])[O:8]P(=O)([O-:7])OP(=O)([O-:10])O1.[Na+:15].[Na+:17]>>[O:5]=[C:6]([O-:7])[O-:8].[OH:9][OH:10].[OH:11][OH:12].[Na+:15].[Na+:17]
O=P1([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])O1.[Na+].[Na+]
O=C([O-])[O-].OO.OO.[Na+].[Na+]
null
null
null
Acylation
OtherReaction
ec059456643c79f498e89d81205a797fefe65415b128fcac155699487a6d8c63
1d95aa8c02f655bb938e918f8b627c35a333785825d3cc1b76b181c1027d234a
null
O=P1(-[O-;H0;D1:1])-O-P(=O)(-[O-])-O-P(=O)(-[O-;H0;D1:2])-O-P(=O)(-[O-;H0;D1:3])-O-P(-[O-;H0;D1:4])(=[O;H0;D1;+0:5])-[O;H0;D2;+0:6]-P(=O)(-[O-;H0;D1:7])-O-1>>[O-;H0;D1:7]-[C:8](-[O-;H0;D1:6])=[O;H0;D1;+0:2].[OH;D1;+0:1]-[OH;D1;+0:3].[OH;D1;+0:4]-[OH;D1;+0:5]
null
[]
null
null
null
null
Wet sodium percarbonate salt was prepared in an operation according to the process described in DE-PS 28 00 760. After reacting sodium carbonate with hydrogen peroxide in a mother liquor containing kitchen salt and sodium hexametaphosphate and crystallising the sodium percarbonate, the latter was separated as far as po...
10.6084/m9.figshare.5104873.v1
null
null
Peroxide.Peroxide
O1POPOPOPOPOP1
null
null
Other
null
null
null
O=P1([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])O1.[Na+].[Na+]>>O=C([O-])[O-].OO.OO.[Na+].[Na+]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b50217a351b14b8aae4981607e137ab9
OO.[Na+]>>O=C([O-])[O-].OO.OO.OO.[Na+].[Na+].[Na+]
C([O-])([O-])=O.[Na+].[Na+].OO>>C(=O)([O-])[O-].C(=O)([O-])[O-].OO.OO.OO.[Na+].[Na+].[Na+].[Na+]
[OH:9][OH:10].[Na+:16]>>[O:5]=[C:6]([O-:7])[O-:8].[OH:9][OH:10].[OH:11][OH:12].[OH:13][OH:14].[Na+:16].[Na+:17].[Na+:18]
OO.[Na+]
O=C([O-])[O-].OO.OO.OO.[Na+].[Na+].[Na+]
null
null
null
Acylation
OtherReaction
0d3f6ecfc31a6f72a96f721a439b5ea2b3b75c89778d8abbdc59cdc1f5118296
1d95aa8c02f655bb938e918f8b627c35a333785825d3cc1b76b181c1027d234a
null
null
null
[]
null
null
null
null
A method for the preparation of stabilized sodium percarbonate comprising forming a sodium percarbonate core by reacting sodium carbonate with hydrogen peroxide in aqueous phase, crystallizing the resulting sodium percarbonate to obtain a wet sodium percarbonate having mother liquor adhering thereto, spraying said wet ...
10.6084/m9.figshare.5104873.v1
null
null
Peroxide.Peroxide
null
null
null
null
null
null
null
OO.[Na+]>>O=C([O-])[O-].OO.OO.OO.[Na+].[Na+].[Na+]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-091fa4e5f2d948a59c39c08379c63ae5
COc1ccc(CSC(C)(C)C(=O)NCCN(CCNC(=O)C(C)(C)SCc2ccc(OC)cc2)Cc2ccc(N)cc2)cc1.S=C(Cl)Cl>>COc1ccc(CSC(C)(C)C(=O)NCCN(CCNC(=O)C(C)(C)SCc2ccc(OC)cc2)Cc2ccc(N=C=S)cc2)cc1
COC1=CC=C(CSC(C(=O)NCCN(CCNC(C(C)(SCC2=CC=C(C=C2)OC)C)=O)CC2=CC=C(C=C2)N)(C)C)C=C1.C(=S)(Cl)Cl>>COC1=CC=C(CSC(C(=O)NCCN(CCNC(C(C)(SCC2=CC=C(C=C2)OC)C)=O)CC2=CC=C(C=C2)N=C=S)(C)C)C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][S:8][C:9]([CH3:10])([CH3:11])[C:12](=[O:13])[NH:14][CH2:15][CH2:16][N:17]([CH2:18][CH2:19][NH:20][C:21](=[O:22])[C:23]([CH3:24])([CH3:25])[S:26][CH2:27][c:28]2[cH:29][cH:30][c:31]([O:32][CH3:33])[cH:34][cH:35]2)[CH2:36][c:37]2[cH:38][cH:39][c:40]([NH2:41])[cH:44][cH:45]2)[cH:...
COc1ccc(CSC(C)(C)C(=O)NCCN(CCNC(=O)C(C)(C)SCc2ccc(OC)cc2)Cc2ccc(N)cc2)cc1.S=C(Cl)Cl
COc1ccc(CSC(C)(C)C(=O)NCCN(CCNC(=O)C(C)(C)SCc2ccc(OC)cc2)Cc2ccc(N=C=S)cc2)cc1
null
null
ClCCl
Heteroatom Alkylation and Arylation
Amine and thiophosgene to isothiocyanate
1226380c52141f79542a4f85564c11e38ca245efc80be1557b635219a638388c
e5752ca9983a57ab07a0b76a5c8a57a6667ab2cd460616b960134623ec0fce31
O=C(CSCc1ccccc1)NCCN(CCNC(=O)CSCc1ccccc1)Cc1ccccc1
Cl-[C;H0;D3;+0:1](-Cl)=[S;D1;H0:2].[NH2;D1;+0:3]-[c:4](:[c:5]):[c:6]>>[S;D1;H0:2]=[C;H0;D2;+0:1]=[N;H0;D2;+0:3]-[c:4](:[c:5]):[c:6]
117.3
[{"value": 116.0, "product": "COC1=CC=C(CSC(C(=O)NCCN(CCNC(C(C)(SCC2=CC=C(C=C2)OC)C)=O)CC2=CC=C(C=C2)N=C=S)(C)C)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 117.3, "product": "COC1=CC=C(CSC(C(=O)NCCN(CCNC(C(C)(SCC2=CC=C(C=C2)OC)C)=O)CC2=CC=C(C=C2)N=C=S)(C)C)C=C1", "details": "CALCULATEDPERCENTYIELD...
null
null
1
HOUR
To a round bottom flask with the aniline 20 (55.7 mg, 0.0853 mmol) and dichloromethane (5 mL) was added 0.2011M solution of thiophosgene (0.42 mL, 0.0845 mmol) in dichloromethane. The heterogeneous reaction mixture was stirred at room temperature for 1 hour and the solvent was removed in vacuo to give the isothiocyanat...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Primary amine
Isothiocyanate
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HCl
ClCCl
null
1
COc1ccc(CSC(C)(C)C(=O)NCCN(CCNC(=O)C(C)(C)SCc2ccc(OC)cc2)Cc2ccc(N)cc2)cc1.S=C(Cl)Cl>ClCCl>COc1ccc(CSC(C)(C)C(=O)NCCN(CCNC(=O)C(C)(C)SCc2ccc(OC)cc2)Cc2ccc(N=C=S)cc2)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7dd6ddcd9fdf4d37b3f1ccc1a56b5f96
CC(N)N1CCN(C)CC(C)(C)SSC(C)(C)CN(C)CC1.NCCN(CCN)CCN>>CN(C)CCN1CCN(C)CC(C)(C)SSC(C)(C)CN(C)CC1
CC1(SSC(CN(CCN(CCN(C1)C)C(C)N)C)(C)C)C.NCCN(CCN)CCN>>CN(C)CCN1CCN(CC(SSC(CN(CC1)C)(C)C)(C)C)C
N[CH:5]([CH3:4])[N:6]1[CH2:7][CH2:8][N:9]([CH3:10])[CH2:11][C:12]([CH3:13])([CH3:14])[S:15][S:16][C:17]([CH3:18])([CH3:19])[CH2:20][N:21]([CH3:22])[CH2:23][CH2:24]1.NCC[N:2]([CH2:1]CN)[CH2:3]CN>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][N:6]1[CH2:7][CH2:8][N:9]([CH3:10])[CH2:11][C:12]([CH3:13])([CH3:14])[S:15][S:16][C:17]([C...
CC(N)N1CCN(C)CC(C)(C)SSC(C)(C)CN(C)CC1.NCCN(CCN)CCN
CN(C)CCN1CCN(C)CC(C)(C)SSC(C)(C)CN(C)CC1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
bdbebd3a501ad46082f4f092582a5b21e7e4cc9025deb1b45c60235941322fdd
a21e2cdfdfe89e200a96df013363dac9801b33cd0e2c9f700170af4f1d6e494c
C1CNCCSSCCNCCN1
N-C-C-[N;H0;D3;+0:1](-[CH2;D2;+0:2]-C-N)-[CH2;D2;+0:3]-C-N.N-[CH;D3;+0:4](-[CH3;D1;+0:5])-[#7:6](-[C:7])-[C:8]>>[C:7]-[#7:6](-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[N;H0;D3;+0:1](-[CH3;D1;+0:2])-[CH3;D1;+0:3])-[C:8]
null
[]
null
null
null
null
1H NMR (300 MHz,in CDCl3): δ2.71 (t,J=6 Hz,4H,-N-CH2 -CH2 -N(CH3)-), 2.64 (s,4H,-N-CH2 -C(CH3)2-S-), 2.62 (t,J=6 Hz,4H,-N-CH2 -CH2 -N(CH3)-), 2.52 (m,2H,-CH2 -CH2 -N(CH3)2), 2.46 (m,2H,-CH2 -CH2 -N(CH3 (2), 2.37 (s,6H,-CH2 -N(CH3)-CH2 -), 2.25 (s,6H,-CH2 -CH2 -N(CH3)2) and 1.28 (s,12H,-S-C(CH3)2 -) ppm. 13C NMR (75 MHz...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine.Primary amine.Primary amine.Tertiary amine
Tertiary amine
null
null
C1C[NH]CCSSCC[NH]CC[NH]1
Other
null
null
null
CC(N)N1CCN(C)CC(C)(C)SSC(C)(C)CN(C)CC1.NCCN(CCN)CCN>>CN(C)CCN1CCN(C)CC(C)(C)SSC(C)(C)CN(C)CC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-2102415670e84ba2a1c07b79e8f9c07d
CC(C)(C)OC(=O)N1CCNCC1.CSCC[C@H](NC(C)=O)C(=O)O>>CSCC[C@H](NC(C)=O)C(=O)N1CCN(C(=O)OC(C)(C)C)CC1
C(C)(C)(C)OC(=O)N1CCNCC1.C1=CC=C2C(=C1)C(=O)C(C2=O)(O)O.II.C1(CCCCC1)N=C=NC1CCCCC1.C(C)(=O)N[C@@H](CCSC)C(=O)O>>C(C)(C)(C)OC(=O)N1CCN(CC1)C([C@@H](NC(C)=O)CCSC)=O
[NH:12]1[CH2:13][CH2:14][N:15]([C:16](=[O:17])[O:18][C:19]([CH3:20])([CH3:21])[CH3:22])[CH2:23][CH2:24]1.O[C:10]([C@H:5]([CH2:4][CH2:3][S:2][CH3:1])[NH:6][C:7]([CH3:8])=[O:9])=[O:11]>>[CH3:1][S:2][CH2:3][CH2:4][C@H:5]([NH:6][C:7]([CH3:8])=[O:9])[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][N:15]([C:16](=[O:17])[O:18][C:19]([C...
CC(C)(C)OC(=O)N1CCNCC1.CSCC[C@H](NC(C)=O)C(=O)O
CSCC[C@H](NC(C)=O)C(=O)N1CCN(C(=O)OC(C)(C)C)CC1
null
C(C)(=O)O
ClCCl.C(C)#N.O1CCCC1
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
ed26ef5eea92a0cc433b3f89a34f4c61724425fa15a9d0ec83a0f7a903eec831
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
C1CNCCN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8].[#7:9]1-[C:10]-[C:11]-[NH;D2;+0:12]-[C:13]-[C:14]-1>>[C:4]-[C:3](-[#7:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:12]1-[C:11]-[C:10]-[#7:9]-[C:14]-[C:13]-1
108.6
[{"value": 108.6, "product": "C(C)(C)(C)OC(=O)N1CCN(CC1)C([C@@H](NC(C)=O)CCSC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of 4.78 g (0.025 mol) of N-acetyl-L-methionine in CH2C12 : acetonitrile (120 ml) was cooled to 0° C. To this solution was added 5.36 g (0.025 mol) of dicyclohexylcarbodiimide (DCC) followed by the rapid addition of 3.90 g (0.021 mol) of N-t-butoxycarbonylpiperazine in 6 ml of dichloromethane. The progress of...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CNCC[NH]1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1
HO-
C(C)(=O)O.ClCCl.C(C)#N.O1CCCC1
null
2
CC(C)(C)OC(=O)N1CCNCC1.CSCC[C@H](NC(C)=O)C(=O)O>C(C)(=O)O.ClCCl.C(C)#N.O1CCCC1>CSCC[C@H](NC(C)=O)C(=O)N1CCN(C(=O)OC(C)(C)C)CC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d54c7161af5a46979c7c7c4306cad827
CSCC[C@H](NC(C)=O)C(=O)N1CCN(C(=O)OC(C)(C)C)CC1>>CSCC[C@H](NC(C)=O)C(=O)N1CCNCC1
C(C)(C)(C)OC(=O)N1CCN(CC1)C([C@@H](NC(C)=O)CCSC)=O.FC(C(=O)O)(F)F>>C(C)(=O)N[C@@H](CCSC)C(=O)N1CCNCC1
CC(C)(C)OC(=O)[N:15]1[CH2:14][CH2:13][N:12]([C:10]([C@H:5]([CH2:4][CH2:3][S:2][CH3:1])[NH:6][C:7]([CH3:8])=[O:9])=[O:11])[CH2:17][CH2:16]1>>[CH3:1][S:2][CH2:3][CH2:4][C@H:5]([NH:6][C:7]([CH3:8])=[O:9])[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][NH:15][CH2:16][CH2:17]1
CSCC[C@H](NC(C)=O)C(=O)N1CCN(C(=O)OC(C)(C)C)CC1
CSCC[C@H](NC(C)=O)C(=O)N1CCNCC1
null
null
ClCCl
Reduction
Boc amine deprotection
2c25e19aee181a3c5131cfdfda27035fd54d4379a11d745dfb75d386bacfd500
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
C1CNCCN1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-[C:6]-1>>[#7:4]1-[C:3]-[C:2]-[NH;D2;+0:1]-[C:6]-[C:5]-1
33.7
[{"value": 33.7, "product": "C(C)(=O)N[C@@H](CCSC)C(=O)N1CCNCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of 8.6 g (0.024 mol) of 1-(t-butoxycarbonyl)-4-(N-acetyl-L-methionyl)piperazine in 60 ml of dichloromethane was added 10 ml of trifluoroacetic acid and the mixture was stirred at room temperature overnight. The solution was extracted with water and the resulting aqueous solution was made basic with sodium...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
C1C[NH]CC[NH]1
C1C[NH]CCN1
C1C[NH]CCN1
HO-
ClCCl
null
8
CSCC[C@H](NC(C)=O)C(=O)N1CCN(C(=O)OC(C)(C)C)CC1>ClCCl>CSCC[C@H](NC(C)=O)C(=O)N1CCNCC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e993cca47d064900bb01c95908565f69
N=C(N)NCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCC(=O)N1)C(=O)Nc1ccc([N+](=O)[O-])cc1>>Nc1ccc([N+](=O)[O-])cc1
N1[C@@H](CCC1=O)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NC1=CC=C([N+](=O)[O-])C=C1>>[N+](=O)([O-])C1=CC=C(N)C=C1
N=C(N)NCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCC(=O)N1)C(=O)[NH:1][c:2]1[cH:3][cH:4][c:5]([N+:6](=[O:7])[O-:8])[cH:9][cH:10]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([N+:6](=[O:7])[O-:8])[cH:9][cH:10]1
N=C(N)NCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCC(=O)N1)C(=O)Nc1ccc([N+](=O)[O-])cc1
Nc1ccc([N+](=O)[O-])cc1
null
null
C(C)(=O)O
Reduction
Hydrogenolysis of amides/imides/carbamates
5182215259cd859a285a29c22302a81e70eb631af3575fcc1696269f183efe3f
18cc77a15f8decf44456aa6785fd69cac51884f3c760a636cccdc428190bc1bc
c1ccccc1
N-C(=N)-N-C-C-C-[C@H](-N-C(=O)-C-N-C(=O)-[C@H]1-C-C-C(=O)-N-1)-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
30
MINUTE
Next, 50 μl of the synthetic peptide substrate (2 mM), pyroGlu-Gly-Arg-p-nitroanilide (S-2444, Kabi, Sweden) were added and the mixture was incubated for 30 minutes at room temperature. The reaction was stopped by the addition of 1 ml of 10% acetic acid. The amount of p-nitroaniline produced was measured by absorbance ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Secondary amide.Secondary amide.Secondary amide.Primary amine.Secondary amine
Primary amine
C1CCNC1
null
c1ccccc1
HO-
C(C)(=O)O
null
0.5
N=C(N)NCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCC(=O)N1)C(=O)Nc1ccc([N+](=O)[O-])cc1>C(C)(=O)O>Nc1ccc([N+](=O)[O-])cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-bd8a36d583c74992ace72789377fc73a
COCCOCCOCCOc1cc([N+](=O)[O-])c([N+](=O)[O-])cc1OCCOCCOCCOC>>COCCOCCOCCOc1ccc(N)c(N)c1OCCOCCOCCOC
O.NN.COCCOCCOCCOC1=C(C=C(C(=C1)[N+](=O)[O-])[N+](=O)[O-])OCCOCCOCCOC.C(Cl)Cl.CO>>NC1=C(C(=C(C=C1)OCCOCCOCCOC)OCCOCCOCCOC)N
O=[N+:16]([O-])[c:15]1[c:14]([N+:18](=O)[O-])[cH:13][c:12]([O:11][CH2:10][CH2:9][O:8][CH2:7][CH2:6][O:5][CH2:4][CH2:3][O:2][CH3:1])[c:19]([O:20][CH2:21][CH2:22][O:23][CH2:24][CH2:25][O:26][CH2:27][CH2:28][O:29][CH3:30])[cH:17]1>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][CH2:7][O:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14...
COCCOCCOCCOc1cc([N+](=O)[O-])c([N+](=O)[O-])cc1OCCOCCOCCOC
COCCOCCOCCOc1ccc(N)c(N)c1OCCOCCOCCOC
null
[Pd]
CCO.C(C)O
Functional Group Interconversion
OtherReaction
a81380ceeffc56cd7fa244efd2d9a24abc1b81a5a82add2f012ceea085558fc9
86e032c8ebc9cbcd13a880d0d66c541ff63611af16d12657aad958d17abf4587
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2]1:[cH;D2;+0:3]:[c:4](-[#8:5]):[c:6]:[c:7]:[c;H0;D3;+0:8]:1-[N+;H0;D3:9](=O)-[O-]>>[#8:5]-[c:4]1:[c:6]:[c:7]:[cH;D2;+0:8]:[c:2](-[NH2;D1;+0:1]):[c;H0;D3;+0:3]:1-[NH2;D1;+0:9]
89
[{"value": 89.0, "product": "NC1=C(C(=C(C=C1)OCCOCCOCCOC)OCCOCCOCCOC)N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
In an oven dried 500 mL round bottom flask, equipped with a Claisen adapter, pressure equalizing dropping funnel, and reflux condenser, 1,2-bis[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]-4,5-dinitrobenzene 1E (20 g, 0.04 mol) was dissolved in absolute ethanol (200 mL). To this clear solution, 10% palladium on carbon (4 g) wa...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Nitro group
Primary amine.Primary amine
c1ccccc1
c1ccccc1
c1ccccc1
Other
[Pd].CCO.C(C)O
null
null
COCCOCCOCCOc1cc([N+](=O)[O-])c([N+](=O)[O-])cc1OCCOCCOCCOC>[Pd].CCO.C(C)O>COCCOCCOCCOc1ccc(N)c(N)c1OCCOCCOCCOC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-fd3f04ce3b4747f998e88ec1d767b13c
OC[C@@H](O)[C@H](O)[C@@H](O)CO>>OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO
C([O-])([O-])=O.[Ca+2].C([C@H](O)[C@@H](O)[C@H](O)CO)O>>OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
[OH:1][CH2:2][C@@H:3]([OH:4])[C@H:5]([OH:6])[C@@H:7]([OH:8])[CH2:9][OH:10]>>[OH:1][CH2:2][C@@H:3]([OH:4])[C@@H:5]([OH:6])[C@H:7]([OH:8])[C@@H:9]([OH:10])[CH2:11][OH:12]
OC[C@@H](O)[C@H](O)[C@@H](O)CO
OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO
null
null
null
Miscellaneous
OtherReaction
bbfa5a4efa40e7a8b5f5a373cb0ead4374bdc2bf34671b8117c68650dca00b27
c3591f637168801020e6236a976ea21b49baafe37273b6eafe44e2276bb61dcb
null
[C:1]-[C:2](-[O;D1;H1:3])-[CH2;D2;+0:4]-[O;D1;H1:5]>>[C:1]-[C:2](-[O;D1;H1:3])-[C@@H;D3;+0:4](-[O;D1;H1:5])-[C:6]-[O;D1;H1:7]
22
[{"value": 22.0, "product": "OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A stabilized, substantially non-volatile mixture of 15 grams of a medium chain triglyceride and 22.5 grams of menthol crystals was formed. To this mixture was added 0.45 grams of F, D and C Blue No. 1 H.T. Lake. A second mixture comprising 22.5 grams of polyethylene glycol (8,000 carbowax) with 12 grams of hydrogenated...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Primary alcohol.Secondary alcohol
null
null
null
Other
null
null
null
OC[C@@H](O)[C@H](O)[C@@H](O)CO>>OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9001260bcc10489c8c8b22567801e0cf
CC(C)(C)CO.COC(=O)OC>>COC(=O)OCC(C)(C)C
C(C(C)(C)C)O.C(OC)(OC)=O>>C(OC)(OCC(C)(C)C)=O
[OH:5][CH2:6][C:7]([CH3:8])([CH3:9])[CH3:10].CO[C:3]([O:2][CH3:1])=[O:4]>>[CH3:1][O:2][C:3](=[O:4])[O:5][CH2:6][C:7]([CH3:8])([CH3:9])[CH3:10]
CC(C)(C)CO.COC(=O)OC
COC(=O)OCC(C)(C)C
null
C[O-].[Na+].CO
null
Acylation
OtherReaction
1c06f9a8caae6ebc766646ab74a70a6fc416a5e8df2dc72b023befe5d14528a9
772f77da20903ad7c3075e3d8d0f3971a777d13631841b0b2f5034c11a7e5159
null
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4]
55
[{"value": 55.0, "product": "C(OC)(OCC(C)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.0, "product": "C(OC)(OCC(C)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
To a mixed solution of neopentyl alcohol (500 ml, 5.7 mol) and dimethyl carbonate (2070 g, 23.0 mol), a 28% sodium methoxide/methanol solution (11 g) was added and the mixture was heated to 100° C. to remove the methanol by evaporation for 6 hours. After allowing the mixture to cool to room temperature, an aqueous solu...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Primary alcohol
Carbonic Ester
null
null
null
HO-
C[O-].[Na+].CO
100
null
CC(C)(C)CO.COC(=O)OC>C[O-].[Na+].CO>COC(=O)OCC(C)(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-c04ca43d5701435492ee6ef93800bddf
COC(=O)OC.OCC(F)(F)F>>COC(=O)OCC(F)(F)F
FC(CO)(F)F.C(OC)(OC)=O>>C(OC)(OCC(F)(F)F)=O
CO[C:3]([O:2][CH3:1])=[O:4].[OH:5][CH2:6][C:7]([F:8])([F:9])[F:10]>>[CH3:1][O:2][C:3](=[O:4])[O:5][CH2:6][C:7]([F:8])([F:9])[F:10]
COC(=O)OC.OCC(F)(F)F
COC(=O)OCC(F)(F)F
null
C[O-].[Na+].CO
null
Acylation
OtherReaction
1c06f9a8caae6ebc766646ab74a70a6fc416a5e8df2dc72b023befe5d14528a9
772f77da20903ad7c3075e3d8d0f3971a777d13631841b0b2f5034c11a7e5159
null
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[F;D1;H0:5]-[C:6](-[F;D1;H0:7])(-[F;D1;H0:8])-[C:9]-[OH;D1;+0:10]>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:10]-[C:9]-[C:6](-[F;D1;H0:5])(-[F;D1;H0:7])-[F;D1;H0:8]
33
[{"value": 33.0, "product": "C(OC)(OCC(F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 32.8, "product": "C(OC)(OCC(F)(F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
In a flask (3-liter volume) equipped with 10 distillation columns, 2,2,2-trifluoroethanol (790 g, 7.9 ml), dimethyl carbonate (2140 g, 23.7 mol) and a 28% sodium methoxide/methanol solution (15.3 g) were charged. The flask was heated to 100° C. to allow the starting materials to react for 30 hours while removing the me...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Primary alcohol
Carbonic Ester
null
null
null
HO-
C[O-].[Na+].CO
100
null
COC(=O)OC.OCC(F)(F)F>C[O-].[Na+].CO>COC(=O)OCC(F)(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9eb09862d3164d5ba6ac2ced82dc1dbc
CCOC(=O)Cl.OCC(F)(F)F>>CCOC(=O)OCC(F)(F)F
FC(CO)(F)F.C(OCC)(=O)Cl.[OH-].[K+]>>C(OCC)(OCC(F)(F)F)=O
Cl[C:4]([O:3][CH2:2][CH3:1])=[O:5].[OH:6][CH2:7][C:8]([F:9])([F:10])[F:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[O:6][CH2:7][C:8]([F:9])([F:10])[F:11]
CCOC(=O)Cl.OCC(F)(F)F
CCOC(=O)OCC(F)(F)F
null
null
C(C)OCC
Acylation
Schotten-Baumann to ester
ab2604cac7a0887c37303ad0fec59fb6a84cf40820c840730a9f7f5636dcc83e
7ed0ec8c4c25c8af523f531911c9dd0a60119de4cab841f882ce9a65c39be54c
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[F;D1;H0:5]-[C:6](-[F;D1;H0:7])(-[F;D1;H0:8])-[C:9]-[OH;D1;+0:10]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:10]-[C:9]-[C:6](-[F;D1;H0:5])(-[F;D1;H0:7])-[F;D1;H0:8]
70
[{"value": 70.0, "product": "C(OCC)(OCC(F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.7, "product": "C(OCC)(OCC(F)(F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
In a flask (5-liter volume), 2,2,2-trifluoroethanol (800 g, 8.0 mol). ethyl chlorocarbonate (867 g, 8.0 mol) and diethyl ether (1000 ml) were charged. While the flask was cooled so that the reaction was carried out at -5° C. to 0° C., a 29.5% by weight aqueous solution of potassium hydroxide (1500 g) was added dropwise...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary alcohol
Carbonic Ester
null
null
null
HCl
C(C)OCC
null
12
CCOC(=O)Cl.OCC(F)(F)F>C(C)OCC>CCOC(=O)OCC(F)(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b1fd55473c5449a3ab3e758cd1fe68cf
COC(=O)OC.OCC(F)(F)C(F)(F)F>>COC(=O)OCC(F)(F)C(F)(F)F
FC(CO)(C(F)(F)F)F.C(OC)(OC)=O>>C(OC)(OCC(C(F)(F)F)(F)F)=O
CO[C:3]([O:2][CH3:1])=[O:4].[OH:5][CH2:6][C:7]([F:8])([F:9])[C:10]([F:11])([F:12])[F:13]>>[CH3:1][O:2][C:3](=[O:4])[O:5][CH2:6][C:7]([F:8])([F:9])[C:10]([F:11])([F:12])[F:13]
COC(=O)OC.OCC(F)(F)C(F)(F)F
COC(=O)OCC(F)(F)C(F)(F)F
null
C[O-].[Na+].CO
null
Acylation
OtherReaction
1c06f9a8caae6ebc766646ab74a70a6fc416a5e8df2dc72b023befe5d14528a9
772f77da20903ad7c3075e3d8d0f3971a777d13631841b0b2f5034c11a7e5159
null
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4]
51
[{"value": 51.0, "product": "C(OC)(OCC(C(F)(F)F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 50.9, "product": "C(OC)(OCC(C(F)(F)F)(F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
null
null
In a flask (500-ml volume) equipped with 10 distillation columns, 2,2,3,3,3-pentafluoropropanol (100 g, 0.67 mol), dimethyl carbonate (180 g, 2.0 mol) and a 28% sodium methoxide/methanol solution (1.3 g) were charged. The flask was heated to 120° C. to allow the starting materials to react for 10 hours while removing t...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Primary alcohol
Carbonic Ester
null
null
null
HO-
C[O-].[Na+].CO
120
null
COC(=O)OC.OCC(F)(F)C(F)(F)F>C[O-].[Na+].CO>COC(=O)OCC(F)(F)C(F)(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ba2015bcd1b046308257976504d7a0ba
COC(=O)OC.OCC(F)(F)C(F)F>>COC(=O)OCC(F)(F)C(F)F
FC(CO)(C(F)F)F.C(OC)(OC)=O>>C(OC)(OCC(C(F)F)(F)F)=O
CO[C:3]([O:2][CH3:1])=[O:4].[OH:5][CH2:6][C:7]([F:8])([F:9])[CH:10]([F:11])[F:12]>>[CH3:1][O:2][C:3](=[O:4])[O:5][CH2:6][C:7]([F:8])([F:9])[CH:10]([F:11])[F:12]
COC(=O)OC.OCC(F)(F)C(F)F
COC(=O)OCC(F)(F)C(F)F
null
C[O-].[Na+].CO
null
Acylation
OtherReaction
1c06f9a8caae6ebc766646ab74a70a6fc416a5e8df2dc72b023befe5d14528a9
772f77da20903ad7c3075e3d8d0f3971a777d13631841b0b2f5034c11a7e5159
null
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4]
49
[{"value": 49.0, "product": "C(OC)(OCC(C(F)F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.5, "product": "C(OC)(OCC(C(F)F)(F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
null
null
In a flask (500-ml volume) equipped with 10 distillation columns, 2,2,3,3-tetrafluoropropanol (100 g, 0.76 mol), dimethyl carbonate (205 g, 2.3 mol) and a 28% sodium methoxide/methanol solution (1.4 g) were charged. The flask was heated to 120° C. to allow the starting materials to react for 10 hours while removing the...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Primary alcohol
Carbonic Ester
null
null
null
HO-
C[O-].[Na+].CO
120
null
COC(=O)OC.OCC(F)(F)C(F)F>C[O-].[Na+].CO>COC(=O)OCC(F)(F)C(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e37be7e79d144758bf50b3682434fb81
COC(=O)OC.OCC(F)(F)C(F)(F)F>>COC(=O)OCC(F)(F)C(F)(F)F
C(OC)(OC)=O.C(=O)([O-])[O-].[K+].[K+].C[O-].[Na+].CO.FC(CO)(C(F)(F)F)F>>C(OC)(OCC(C(F)(F)F)(F)F)=O
CO[C:3]([O:2][CH3:1])=[O:4].[OH:5][CH2:6][C:7]([F:8])([F:9])[C:10]([F:11])([F:12])[F:13]>>[CH3:1][O:2][C:3](=[O:4])[O:5][CH2:6][C:7]([F:8])([F:9])[C:10]([F:11])([F:12])[F:13]
COC(=O)OC.OCC(F)(F)C(F)(F)F
COC(=O)OCC(F)(F)C(F)(F)F
null
null
null
Acylation
OtherReaction
1c06f9a8caae6ebc766646ab74a70a6fc416a5e8df2dc72b023befe5d14528a9
772f77da20903ad7c3075e3d8d0f3971a777d13631841b0b2f5034c11a7e5159
null
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4]
55
[{"value": 55.0, "product": "C(OC)(OCC(C(F)(F)F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Methyl 2,2,3,3,3-Pentafluoropropyl carbonate was prepared by the same manner as the example 4 except that K2CO3 (0.046 g) was used as a catalyst in stead of a 28% sodium methoxide/methanol solution (1.3 g). After 2,2,3,3,3-pentafluoropropanol and dimethyl carbonate were allowed to react, the mixture thereof was passed ...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Primary alcohol
Carbonic Ester
null
null
null
HO-
null
null
null
COC(=O)OC.OCC(F)(F)C(F)(F)F>>COC(=O)OCC(F)(F)C(F)(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-bce3bb869e764396bc23e7298aa8e4ba
BrBr.Cc1ccc(N)c([N+](=O)[O-])c1>>Cc1cc(Br)c(N)c([N+](=O)[O-])c1
BrBr.CC1=CC(=C(N)C=C1)[N+](=O)[O-]>>BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])N
Br[Br:5].[CH3:1][c:2]1[cH:3][cH:4][c:6]([NH2:7])[c:8]([N+:9](=[O:10])[O-:11])[cH:12]1>>[CH3:1][c:2]1[cH:3][c:4]([Br:5])[c:6]([NH2:7])[c:8]([N+:9](=[O:10])[O-:11])[cH:12]1
BrBr.Cc1ccc(N)c([N+](=O)[O-])c1
Cc1cc(Br)c(N)c([N+](=O)[O-])c1
null
null
C(C)(=O)O
Functional Group Interconversion
Bromination
f6effe61353895b318215d8bd9b6bb1105cafbf7be8c217d748df587260b32c3
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccccc1
Br-[Br;H0;D1;+0:1].[N;D1;H2:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6]:[c:7]>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:3](-[N;D1;H2:2]):[c:4]
98.5
[{"value": 98.0, "product": "BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.5, "product": "BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of bromine (23.24 mL, 453.5 mmol) in glacial acetic acid (50 mL) was added dropwise over 2 h to a mechanically-stirred suspension of 4-methyl-2-nitroaniline (60.00 g, 394.3 mmol) in glacial acetic acid (200 mL) at room temperature under a nitrogen atmosphere. The mixture was stirred at room temperature 1 h, ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccccc1
c1ccccc1
c1ccccc1
HBr
C(C)(=O)O
null
1
BrBr.Cc1ccc(N)c([N+](=O)[O-])c1>C(C)(=O)O>Cc1cc(Br)c(N)c([N+](=O)[O-])c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8b376187240b4ed782555b182275be4f
C=C1CC(=O)O1.Cc1cc(Br)c(N)c([N+](=O)[O-])c1>>CC(=O)CC(=O)Nc1c(Br)cc(C)cc1[N+](=O)[O-]
O.O.[Cl-].[Na+].C=C1CC(=O)O1.BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])N>>BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])NC(CC(C)=O)=O
[CH2:1]=[C:2]1[O:3][C:5](=[O:6])[CH2:4]1.[NH2:7][c:8]1[c:9]([Br:10])[cH:11][c:12]([CH3:13])[cH:14][c:15]1[N+:16](=[O:17])[O-:18]>>[CH3:1][C:2](=[O:3])[CH2:4][C:5](=[O:6])[NH:7][c:8]1[c:9]([Br:10])[cH:11][c:12]([CH3:13])[cH:14][c:15]1[N+:16](=[O:17])[O-:18]
C=C1CC(=O)O1.Cc1cc(Br)c(N)c([N+](=O)[O-])c1
CC(=O)CC(=O)Nc1c(Br)cc(C)cc1[N+](=O)[O-]
null
CN(C1=CC=NC=C1)C
O1CCCC1.ClCCCC
Acylation
OtherReaction
5b7e5290792b5fd05931d61f1ab4fac4b9a12474dc4c1d1fe9f74041167c288b
61e32e3b264beb4549f229750ce3ceb3c4831b980f4210ceb397f2f215863ce1
c1ccccc1
[CH2;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-1.[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[CH3;D1;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:6])-[C:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]
46
[{"value": 46.0, "product": "BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])NC(CC(C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 46.0, "product": "BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])NC(CC(C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of diketene (57.71 mL, 748.2 mmol) was added dropwise over 2 h to a stirred solution of title compound of Step A (34.57 g, 149.6 mmol) and 4-dimethylaminopyridine (914 mg, 7.48 mmol) in dry tetrahydrofuran (450 mL) at room temperature under a nitrogen atmosphere. The reaction was allowed to stir at room temp...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine.Vinyl
Ketone.Secondary amide
C1COC1
null
c1ccccc1
null
CN(C1=CC=NC=C1)C.O1CCCC1.ClCCCC
null
8
C=C1CC(=O)O1.Cc1cc(Br)c(N)c([N+](=O)[O-])c1>CN(C1=CC=NC=C1)C.O1CCCC1.ClCCCC>CC(=O)CC(=O)Nc1c(Br)cc(C)cc1[N+](=O)[O-]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-961ef8e0d2254aeeb0222653c66e30f3
CC(=O)CC(=O)Nc1c(Br)cc(C)cc1[N+](=O)[O-]>>Cc1cc(Br)c2nc(O)c[n+]([O-])c2c1
Cl.Cl.BrC1=C(C(=CC(=C1)C)[N+](=O)[O-])NC(CC(C)=O)=O.[OH-].[Na+]>>BrC=1C=C(C=C2[N+](=CC(=NC12)O)[O-])C
CC(=O)[CH2:10][C:8]([NH:7][c:6]1[c:4]([Br:5])[cH:3][c:2]([CH3:1])[cH:14][c:13]1[N+:11](=O)[O-:12])=[O:9]>>[CH3:1][c:2]1[cH:3][c:4]([Br:5])[c:6]2[n:7][c:8]([OH:9])[cH:10][n+:11]([O-:12])[c:13]2[cH:14]1
CC(=O)CC(=O)Nc1c(Br)cc(C)cc1[N+](=O)[O-]
Cc1cc(Br)c2nc(O)c[n+]([O-])c2c1
null
null
O.C(C)(C)O
Aromatic Heterocycle Formation
OtherReaction
dbeaf95e8c60f8a2239be1828f0c77c3d9697c30429f1dca540d88c35e86b191
b2f32db516037f047521b1073c23b36649646661bfde4f7b72846a5f05afa84a
c1ccc2[nH+]ccnc2c1
C-C(=O)-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7](-[N+;H0;D3:8](=O)-[O;-;D1;H0:9]):[c:10]>>[O;-;D1;H0:9]-[n+;H0;D3:8]1:[cH;D2;+0:1]:[c;H0;D3;+0:2](-[OH;D1;+0:3]):[n;H0;D2;+0:4]:[c:5](:[c:6]):[c:7]:1:[c:10]
91.2
[{"value": 91.0, "product": "BrC=1C=C(C=C2[N+](=CC(=NC12)O)[O-])C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.2, "product": "BrC=1C=C(C=C2[N+](=CC(=NC12)O)[O-])C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
The title compound of Step B (11.75 g, 37.29 mmol) was suspended in a mixture of isopropanol (120 mL) and water (120 mL) at room temperature under a nitrogen atmosphere. A solution of sodium hydroxide (14.91 g of a 50% aqueous solution, 186.4 mmol) diluted with water (10 mL) was added dropwise to the mixture over 30 mi...
10.6084/m9.figshare.5104873.v1
null
Ketone.Nitro group.Secondary amide
Aromatic alcohol
c1ccccc1
C1=Nc2ccccc2[NH+]=C1
C1=Nc2ccccc2[NH+]=C1
HO-
O.C(C)(C)O
null
8
CC(=O)CC(=O)Nc1c(Br)cc(C)cc1[N+](=O)[O-]>O.C(C)(C)O>Cc1cc(Br)c2nc(O)c[n+]([O-])c2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ac830d54b7724a8b93da7678034827fa
Cc1cc(Br)c2nc(O)c[n+]([O-])c2c1>>Cc1cc(Br)c2nc(O)cnc2c1
BrC=1C=C(C=C2[N+](=CC(=NC12)O)[O-])C.S(=O)([O-])S(=O)[O-].[Na+].[Na+]>>BrC=1C=C(C=C2N=CC(=NC12)O)C
[O-][n+:11]1[cH:10][c:8]([OH:9])[n:7][c:6]2[c:4]([Br:5])[cH:3][c:2]([CH3:1])[cH:13][c:12]21>>[CH3:1][c:2]1[cH:3][c:4]([Br:5])[c:6]2[n:7][c:8]([OH:9])[cH:10][n:11][c:12]2[cH:13]1
Cc1cc(Br)c2nc(O)c[n+]([O-])c2c1
Cc1cc(Br)c2nc(O)cnc2c1
null
null
O.C(C)O
Functional Group Interconversion
OtherReaction
cba54b73cc7260c4f6c8071e80144f2309a3f0e13da5d87e78a7e26446efb16e
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
c1ccc2nccnc2c1
[O-]-[n+;H0;D3:1]1:[c:2]:[c:3](-[O;D1;H1:4]):[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[O;D1;H1:4]-[c:3]1:[#7;a:5]:[c:6](:[c:7]):[c:8](:[c:9]):[n;H0;D2;+0:1]:[c:2]:1
65.3
[{"value": 65.0, "product": "BrC=1C=C(C=C2N=CC(=NC12)O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.3, "product": "BrC=1C=C(C=C2N=CC(=NC12)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
The title compound of Step C (25 g, 98 mmol) and sodium dithionite (38 g, 220 mmol) were suspended in a mixture of ethanol (1000 mL) and water (200 mL) at room temperature. After 1 h, most of the solvent was removed under reduced pressure. The residue was diluted with water and acidified with hydrochloric acid. Insolub...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=Nc2ccccc2[NH+]=C1
c1ccc2nccnc2c1
c1ccc2nccnc2c1
Other
O.C(C)O
null
1
Cc1cc(Br)c2nc(O)c[n+]([O-])c2c1>O.C(C)O>Cc1cc(Br)c2nc(O)cnc2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-aa24d111c02e4dc5a5481afc71f24fef
Cc1cc(Br)c2nc(O)cnc2c1.FC(F)Cl>>Cc1cc(Br)c2nc(OC(F)F)cnc2c1
ClC(F)F.O.[OH-].[Na+].BrC=1C=C(C=C2N=CC(=NC12)O)C>>BrC=1C=C(C=C2N=CC(=NC12)OC(F)F)C
[CH3:1][c:2]1[cH:3][c:4]([Br:5])[c:6]2[n:7][c:8]([OH:9])[cH:13][n:14][c:15]2[cH:16]1.Cl[CH:10]([F:11])[F:12]>>[CH3:1][c:2]1[cH:3][c:4]([Br:5])[c:6]2[n:7][c:8]([O:9][CH:10]([F:11])[F:12])[cH:13][n:14][c:15]2[cH:16]1
Cc1cc(Br)c2nc(O)cnc2c1.FC(F)Cl
Cc1cc(Br)c2nc(OC(F)F)cnc2c1
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
O1CCOCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
f71746b437f06cff8a64ae80ec4989a9ba690dfb75f233569f959f7c1c70ee3d
d674a4e29cb9c6ff02aced7b3a1a65ea0cc2cf9c3c85791f3e260cc78f258f15
c1ccc2nccnc2c1
Cl-[CH;D3;+0:1](-[F;D1;H0:2])-[F;D1;H0:3].[OH;D1;+0:4]-[c:5]1:[#7;a:6]:[c:7]:[c:8]:[#7;a:9]:[c:10]:1>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:4]-[c:5]1:[#7;a:6]:[c:7]:[c:8]:[#7;a:9]:[c:10]:1
52
[{"value": 52.0, "product": "BrC=1C=C(C=C2N=CC(=NC12)OC(F)F)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Tetrabutylammonium bromide (689 mg, 2.14 mmol) and sodium hydroxide (17.1 g of a 50% aqueous solution, 214 mmol) were added to a solution of the title compound of Step D (5.11 g, 21.4 mmol) in dioxane (250 mL) at room temperature. Chlorodifluoromethane was condensed with a cold finger trap and added to the reaction mix...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Secondary halide.Aromatic alcohol
Secondary halide.Secondary halide.Ether
null
null
c1ccc2nccnc2c1
HCl
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.O1CCOCC1
null
8
Cc1cc(Br)c2nc(O)cnc2c1.FC(F)Cl>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.O1CCOCC1>Cc1cc(Br)c2nc(OC(F)F)cnc2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f47ceb4b2cb54da08b01b4015880bd80
FC1(F)Oc2ccccc2O1>>OB(O)c1cccc2c1OC(F)(F)O2
Cl.Cl.COB(OC)OC.FC1(OC2=C(O1)C=CC=C2)F.[Cl-].[Na+].C(CCC)[Li]>>FC1(OC2=C(O1)C=CC=C2B(O)O)F
[cH:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[O:10][C:11]([F:12])([F:13])[O:14]2>>[OH:1][B:2]([OH:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[O:10][C:11]([F:12])([F:13])[O:14]2
FC1(F)Oc2ccccc2O1
OB(O)c1cccc2c1OC(F)(F)O2
null
null
O1CCCC1.O
Functional Group Interconversion
OtherReaction
1949fa8ee88afd1f046f27213d5ee74604a3b3aae43c31b9bf334761fbde0e7a
d6d312d46f766d2774f96de1fd96fd8f98a20e51a20ef3280f850cd6a3c77869
c1ccc2c(c1)OCO2
[c:1]:[c:2]:[cH;D2;+0:3]:[c:4]1:[c:5]-[#8:6]-[C:7]-[#8:8]-1>>[O;D1;H1:9]-[#5:10](-[O;D1;H1:11])-[c;H0;D3;+0:3](:[c:2]:[c:1]):[c:4]1:[c:5]-[#8:6]-[C:7]-[#8:8]-1
50
[{"value": 50.0, "product": "FC1(OC2=C(O1)C=CC=C2B(O)O)F", "details": "PERCENTYIELD", "is_desired": false}]
-15
CELSIUS
0.5
HOUR
A solution of n-butyllithium (5.57 mL of a 2.5M solution in hexanes, 13.9 mmol) was added to dry tetrahydrofuran (75 mL) at room temperature under a nitrogen atmosphere. The resulting solution was cooled to -15° C. and N,N,N',N'-tetramethylenediamine (2.10 mL, 13.9 mmol) was added dropwise. The reaction was stirred at ...
10.6084/m9.figshare.5104873.v1
null
null
Boronic acid
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
null
O1CCCC1.O
-15
0.5
FC1(F)Oc2ccccc2O1>O1CCCC1.O>OB(O)c1cccc2c1OC(F)(F)O2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6bdd1d1e091c4828a49bbd517c400336
Cc1cc(Br)c2nc(OC(F)F)cnc2c1.OB(O)c1cccc2c1OC(F)(F)O2>>Cc1cc(-c2cccc3c2OC(F)(F)O3)c2nc(OC(F)F)cnc2c1
C([O-])([O-])=O.[Na+].[Na+].C(C)(=O)OCC.CCCCCC.BrC=1C=C(C=C2N=CC(=NC12)OC(F)F)C.FC1(OC2=C(O1)C=CC=C2B(O)O)F>>FC1(OC2=C(O1)C=CC=C2C=2C=C(C=C1N=CC(=NC21)OC(F)F)C)F
Br[c:4]1[cH:3][c:2]([CH3:1])[cH:26][c:25]2[c:16]1[n:17][c:18]([O:19][CH:20]([F:21])[F:22])[cH:23][n:24]2.OB(O)[c:5]1[cH:6][cH:7][cH:8][c:9]2[c:10]1[O:11][C:12]([F:13])([F:14])[O:15]2>>[CH3:1][c:2]1[cH:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][c:9]3[c:10]2[O:11][C:12]([F:13])([F:14])[O:15]3)[c:16]2[n:17][c:18]([O:19][CH:20]([F:...
Cc1cc(Br)c2nc(OC(F)F)cnc2c1.OB(O)c1cccc2c1OC(F)(F)O2
Cc1cc(-c2cccc3c2OC(F)(F)O3)c2nc(OC(F)F)cnc2c1
null
[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
O.COCCOC
C-C Coupling
Suzuki coupling with boronic acids
ed9bad7efec3b51d5869944ec4ccf9d532559fc12336e44e56b42cc9b75a0d80
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1cc2c(c(-c3cccc4nccnc34)c1)OCO2
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[c:8]:[#7;a:9]:[c:10]:2:1.O-B(-O)-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]1:[c:15]-[#8:16]-[C:17]-[#8:18]-1>>[c:13]:[c:12]:[c;H0;D3;+0:11](-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]2:[#7;a:6]:[c:7]:[c:8]:[#7;a:9]:[c:10]:2:1):[c:14]1:[c:15]-[#8:16]-[C:17]-[#8:18]-1
null
[]
null
null
null
null
To a solution of the title compound of Step E (1.65 g, 5.73 mmol) in ethylene glycol dimethyl ether (25 mL) was added the title compound of Step F (1.73 g, 8.59 mmol), a solution of sodium carbonate (1.82 g, 17.2 mmol) in water (15 mL) and bis(triphenylphosphine) palladium (II) chloride (201 mg, 0.286 mmol). The mixtur...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccc2nccnc2c1.c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2.c1ccc2nccnc2c1
c1ccc2c(c1)OCO2.c1ccc2nccnc2c1
HBr.B
[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.COCCOC
null
null
Cc1cc(Br)c2nc(OC(F)F)cnc2c1.OB(O)c1cccc2c1OC(F)(F)O2>[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.COCCOC>Cc1cc(-c2cccc3c2OC(F)(F)O3)c2nc(OC(F)F)cnc2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-938589f386a14a4bbc484da563c53622
BrBr.FC1(F)Oc2ccccc2O1>>FC1(F)Oc2ccc(Br)cc2O1
BrBr.FC1(OC2=C(O1)C=CC=C2)F>>BrC1=CC2=C(OC(O2)(F)F)C=C1
Br[Br:9].[F:1][C:2]1([F:3])[O:4][c:5]2[cH:6][cH:7][cH:8][cH:10][c:11]2[O:12]1>>[F:1][C:2]1([F:3])[O:4][c:5]2[cH:6][cH:7][c:8]([Br:9])[cH:10][c:11]2[O:12]1
BrBr.FC1(F)Oc2ccccc2O1
FC1(F)Oc2ccc(Br)cc2O1
null
[Fe]
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Bromination
684aaea30ea96ac3399be761a03275b73ad5093abe190412ef63066807650194
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2c(c1)OCO2
Br-[Br;H0;D1;+0:1].[#8:2]-[c:3]:[c:4]:[cH;D2;+0:5]:[c:6]:[c:7]>>[#8:2]-[c:3]:[c:4]:[c;H0;D3;+0:5](-[Br;H0;D1;+0:1]):[c:6]:[c:7]
64.1
[{"value": 64.0, "product": "BrC1=CC2=C(OC(O2)(F)F)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.1, "product": "BrC1=CC2=C(OC(O2)(F)F)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Iron powder (2.8 g, 50 mmol) was added to a solution of 2,2-difluoro-1,3-benzodioxole (15.8 g, 100 mmol) in carbon tetrachloride (200 mL) at 0° C. under a nitrogen atmosphere. Bromine (5.2 mL, 100 mmol) was then added to the mixture dropwise over 15 min. The reaction was heated to reflux for 1 h and then stirred at roo...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
HBr
[Fe].C(Cl)(Cl)(Cl)Cl
null
8
BrBr.FC1(F)Oc2ccccc2O1>[Fe].C(Cl)(Cl)(Cl)Cl>FC1(F)Oc2ccc(Br)cc2O1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-01e142ca746b4a8f92e589c35be32a22
CC(C)OB(OC(C)C)OC(C)C.FC1(F)Oc2ccc(Br)cc2O1>>OB(O)c1ccc2c(c1)OC(F)(F)O2
C(C)(C)OB(OC(C)C)OC(C)C.C(CCC)[Li].BrC1=CC2=C(OC(O2)(F)F)C=C1>>FC1(OC2=C(O1)C=CC(=C2)B(O)O)F
CC(C)O[B:2]([O:1]C(C)C)[O:3]C(C)C.Br[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[O:10][C:11]([F:12])([F:13])[O:14]2>>[OH:1][B:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[O:10][C:11]([F:12])([F:13])[O:14]2
CC(C)OB(OC(C)C)OC(C)C.FC1(F)Oc2ccc(Br)cc2O1
OB(O)c1ccc2c(c1)OC(F)(F)O2
null
null
O1CCCC1
Miscellaneous
Preparation of boronic acids
4c1114821e211241e128738212de27d454c1817efbb83c07fd28c2b2f3081857
dafd25fbe01879c365f8c874026e570f49824f4bb82016b29d0c5d21aeb58ca3
c1ccc2c(c1)OCO2
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]-[#8:6].C-C(-C)-O-[B;H0;D3;+0:7](-[O;H0;D2;+0:8]-C(-C)-C)-[O;H0;D2;+0:9]-C(-C)-C>>[#8:6]-[c:5]:[c:4]:[c;H0;D3;+0:1](-[B;H0;D3;+0:7](-[OH;D1;+0:8])-[OH;D1;+0:9]):[c:2]:[c:3]
117.9
[{"value": 117.9, "product": "FC1(OC2=C(O1)C=CC(=C2)B(O)O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
A solution of the title compound of Step A (15 g, 63 mmol) in tetrahydrofuran (approximately 200 mL) was cooled to -78° C. under a nitrogen atmosphere. A solution of n-butyllithium (40 mL of a 1.6M solution in hexanes) was added dropwise while maintaining the reaction temperature below -55° C. The reaction mixture was ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Boronic acid
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
c1ccc2c(c1)OCO2
HBr
O1CCCC1
null
5
CC(C)OB(OC(C)C)OC(C)C.FC1(F)Oc2ccc(Br)cc2O1>O1CCCC1>OB(O)c1ccc2c(c1)OC(F)(F)O2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-3059335a2ed14734ab0b8b6bd679db34
CC(=O)Nc1ccc(C)cc1Br.OB(O)c1ccc2c(c1)OC(F)(F)O2>>CC(=O)Nc1ccc(C)cc1-c1ccc2c(c1)OC(F)(F)O2
FC1(OC2=C(O1)C=CC(=C2)B(O)O)F.C([O-])([O-])=O.[Na+].[Na+].CC1=CC(=C(C=C1)NC(=O)C)Br.FC1(OC2=C(O1)C=CC(=C2)B(O)O)F.C([O-])([O-])=O.[Na+].[Na+]>>FC1(OC2=C(O1)C=CC(=C2)C2=C(C=CC(=C2)C)NC(C)=O)F
Br[c:11]1[c:5]([NH:4][C:2]([CH3:1])=[O:3])[cH:6][cH:7][c:8]([CH3:9])[cH:10]1.OB(O)[c:12]1[cH:13][cH:14][c:15]2[c:16]([cH:17]1)[O:18][C:19]([F:20])([F:21])[O:22]2>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]([CH3:9])[cH:10][c:11]1-[c:12]1[cH:13][cH:14][c:15]2[c:16]([cH:17]1)[O:18][C:19]([F:20])([F:21])[O:22]2
CC(=O)Nc1ccc(C)cc1Br.OB(O)c1ccc2c(c1)OC(F)(F)O2
CC(=O)Nc1ccc(C)cc1-c1ccc2c(c1)OC(F)(F)O2
null
[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
O.COCCOC
C-C Coupling
Suzuki coupling with boronic acids
4eaac3524feef0fac9270283493ac343cfbd88f66b23f78df9bf06d23e299fd5
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccc3c(c2)OCO3)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8]):[c:9].O-B(-O)-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]-[#8:15]>>[#8:15]-[c:14]:[c:13]:[c;H0;D3;+0:10](-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8]):[c:9]):[c:11]:[c:12]
null
[]
null
null
null
null
To a mixture of 2-bromo-4-methylacetanilide (1.5 g, 6.6 mmol) and the title compound of Step B (2.0 g, 9.9 mmol) in ethylene glycol dimethyl ether (20 mL) were added a solution of sodium carbonate (2.1 g, 20 mmol) in water (20 mL) and bis(triphenylphosphine) palladium (II) chloride (230 mg, 0.33 mmol). The mixture was ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccc2c(c1)OCO2
c1ccccc1.c1ccc2c(c1)OCO2
c1ccccc1.c1ccc2c(c1)OCO2
HBr.B
[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.COCCOC
null
null
CC(=O)Nc1ccc(C)cc1Br.OB(O)c1ccc2c(c1)OC(F)(F)O2>[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.COCCOC>CC(=O)Nc1ccc(C)cc1-c1ccc2c(c1)OC(F)(F)O2
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d18919271ba346f0943598126ca972e9
Cc1ccc(NC(=O)C(C)(C)C)c(B(O)O)c1.FC1(F)Oc2cccc(Br)c2O1>>Cc1ccc(NC(=O)C(C)(C)C)c(-c2cccc3c2OC(F)(F)O3)c1
C(C)(=O)OCC.CCCCCC.B(O)(O)C1=C(C=CC(=C1)C)NC(C(C)(C)C)=O.C([O-])([O-])=O.[Na+].[Na+].BrC1=CC=CC=2OC(OC21)(F)F>>FC1(OC2=C(O1)C=CC=C2C2=C(C=CC(=C2)C)NC(C(C)(C)C)=O)F
OB(O)[c:13]1[c:5]([NH:6][C:7](=[O:8])[C:9]([CH3:10])([CH3:11])[CH3:12])[cH:4][cH:3][c:2]([CH3:1])[cH:25]1.Br[c:14]1[cH:15][cH:16][cH:17][c:18]2[c:19]1[O:20][C:21]([F:22])([F:23])[O:24]2>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([NH:6][C:7](=[O:8])[C:9]([CH3:10])([CH3:11])[CH3:12])[c:13](-[c:14]2[cH:15][cH:16][cH:17][c:18]3[c:19]...
Cc1ccc(NC(=O)C(C)(C)C)c(B(O)O)c1.FC1(F)Oc2cccc(Br)c2O1
Cc1ccc(NC(=O)C(C)(C)C)c(-c2cccc3c2OC(F)(F)O3)c1
null
[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
O.COCCOC
C-C Coupling
Suzuki coupling with boronic acids
4eaac3524feef0fac9270283493ac343cfbd88f66b23f78df9bf06d23e299fd5
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2cccc3c2OCO3)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]1:[c:5]-[#8:6]-[C:7]-[#8:8]-1.O-B(-O)-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12](-[#7:13]-[C:14]=[O;D1;H0:15]):[c:16]>>[O;D1;H0:15]=[C:14]-[#7:13]-[c:12](:[c:16]):[c;H0;D3;+0:9](-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]1:[c:5]-[#8:6]-[C:7]-[#8:8]-1):[c:10]:[c:11]
null
[]
null
null
null
null
To a mixture of the title compound of Step B (10.0 g, 42.2 mmol) and the title compound of Step A (4.96 g, 21.1 mmol) in ethylene glycol dimethyl ether (100 mL) were added a solution of sodium carbonate (4.47 g, 42.2 mmol) in water (25 mL) and bis(triphenylphosphine) palladium (II) chloride (740 mg, 1.05 mmol) at room ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccc2c(c1)OCO2
c1ccccc1.c1ccc2c(c1)OCO2
c1ccccc1.c1ccc2c(c1)OCO2
HBr.B
[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.COCCOC
null
null
Cc1ccc(NC(=O)C(C)(C)C)c(B(O)O)c1.FC1(F)Oc2cccc(Br)c2O1>[Pd](Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.O.COCCOC>Cc1ccc(NC(=O)C(C)(C)C)c(-c2cccc3c2OC(F)(F)O3)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9130d3fad57549ea933b423cbc358a19
FC(F)(Br)C(F)(F)Br.FC1(F)Oc2ccccc2OC1(F)F>>FC1(F)Oc2cccc(Br)c2OC1(F)F
BrC(C(Br)(F)F)(F)F.C(CCC)[Li].FC1(C(OC2=C(O1)C=CC=C2)(F)F)F.[Cl-].[Na+]>>BrC1=CC=CC=2OC(C(OC21)(F)F)(F)F
FC(F)(Br)C(F)(F)[Br:10].[F:1][C:2]1([F:3])[O:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:11]2[O:12][C:13]1([F:14])[F:15]>>[F:1][C:2]1([F:3])[O:4][c:5]2[cH:6][cH:7][cH:8][c:9]([Br:10])[c:11]2[O:12][C:13]1([F:14])[F:15]
FC(F)(Br)C(F)(F)Br.FC1(F)Oc2ccccc2OC1(F)F
FC1(F)Oc2cccc(Br)c2OC1(F)F
null
null
O1CCCC1.O
Functional Group Interconversion
Bromination
f73ec388e165bd36cf56b9c8d1e55695fba64178a8b7c568fb122a53aa700f5d
019ad5fd0dfe62cfb4244afde83961e2345586820445df7561489ed4a5d090fa
c1ccc2c(c1)OCCO2
Br-C(-F)(-F)-C(-F)(-F)-[Br;H0;D1;+0:1].[#8:2]-[c:3]:[c:4](:[cH;D2;+0:5]:[c:6]:[c:7])-[#8:8]-[C:9]>>[#8:2]-[c:3]:[c:4](:[c;H0;D3;+0:5](-[Br;H0;D1;+0:1]):[c:6]:[c:7])-[#8:8]-[C:9]
null
[]
-78
CELSIUS
30
MINUTE
A solution of 2,2,3,3-tetrafluoro-2,3-dihydro-1,4-benzodioxin (5.00 g, 24.0 mmol) in dry tetrahydrofuran (150 mL) is cooled to -78° C. under a nitrogen atmosphere. A solution of n-butyllithium (10.6 mL, 26.4 mmol of a 2.5M solution in hexanes) is added dropwise while maintaining the reaction temperature below -65° C. T...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide
Aromatic halide
c1ccc2c(c1)OCCO2
c1ccc2c(c1)OCCO2
c1ccc2c(c1)OCCO2
HF.Br-
O1CCCC1.O
-78
0.5
FC(F)(Br)C(F)(F)Br.FC1(F)Oc2ccccc2OC1(F)F>O1CCCC1.O>FC1(F)Oc2cccc(Br)c2OC1(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-afe96e785cfc4f1c9f88cafef09f3c63
NS(=O)(=O)c1cc(C(=O)O)c(NCc2ccco2)cc1Cl>>NS(=O)(=O)c1cc(C(=O)O)c(NCc2ccco2)cc1Cl
C=1C=C(OC1)CNC2=CC(=C(C=C2C(=O)O)S(=O)(=O)N)Cl.CC=1C=CC=CC1N2C(NC=3C=C(C(=CC3C2=O)S(=O)(=O)N)Cl)C>>CC=1C=CC=CC1N2C(NC=3C=C(C(=CC3C2=O)S(=O)(=O)N)Cl)C.C=1C=C(OC1)CNC2=CC(=C(C=C2C(=O)O)S(=O)(=O)N)Cl
[NH2:25][S:26](=[O:27])(=[O:28])[c:29]1[cH:30][c:31]([C:32](=[O:33])[OH:34])[c:35]([NH:36][CH2:37][c:38]2[cH:39][cH:40][cH:41][o:42]2)[cH:43][c:44]1[Cl:45]>>[NH2:25][S:26](=[O:27])(=[O:28])[c:29]1[cH:30][c:31]([C:32](=[O:33])[OH:34])[c:35]([NH:36][CH2:37][c:38]2[cH:39][cH:40][cH:41][o:42]2)[cH:43][c:44]1[Cl:45]
NS(=O)(=O)c1cc(C(=O)O)c(NCc2ccco2)cc1Cl
NS(=O)(=O)c1cc(C(=O)O)c(NCc2ccco2)cc1Cl
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccc(NCc2ccco2)cc1
null
null
[]
null
null
null
null
Rats (450 g previously untreated) were intraperitoneally administered 0.5 ml of 4 mg/ml lasix solution (4 mg/kg dose) and 0.5 ml of 2 mg/ml metolazone/tris buffer solution, pH 11.5, (2 mg/kg dose). The results are shown in Table V below. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccoc1
null
null
null
null
NS(=O)(=O)c1cc(C(=O)O)c(NCc2ccco2)cc1Cl>>NS(=O)(=O)c1cc(C(=O)O)c(NCc2ccco2)cc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d607fa842ea549ee904a444b8bfe6cd1
CC(C)C1C=C2CCC3C(C)(C(=O)O)CCCC3(C)C2CC1.CCCCCCCCCCCCCC(=O)OC(C)C.O=C(OCc1ccccc1)c1ccccc1>>CCOc1cc(C=O)ccc1O
C(CCCCCCCCCCCCC)(=O)OC(C)C.CC(C)C1CCC2C(=C1)CCC3C2(CCCC3(C)C(=O)O)C.C(C1=CC=CC=C1)(=O)OCC1=CC=CC=C1>>O=CC1=CC(OCC)=C(O)C=C1
CC(C)C1C=C2CCC3C(C)(C(=O)O)CCCC3(C)C2[CH2:10][CH2:9]1.CC(C)OC(CCCCCCCCCCC[CH2:2][CH3:1])=[O:8].c1cc[c:11]([CH2:4][O:3][C:7]([c:6]2cccc[cH:5]2)=[O:12])cc1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][c:6]([CH:7]=[O:8])[cH:9][cH:10][c:11]1[OH:12]
CC(C)C1C=C2CCC3C(C)(C(=O)O)CCCC3(C)C2CC1.CCCCCCCCCCCCCC(=O)OC(C)C.O=C(OCc1ccccc1)c1ccccc1
CCOc1cc(C=O)ccc1O
null
null
null
Protection
OtherReaction
7f2e052feafcd1f221f75489f5cc196697d550bae96a58b5df6b502aa5f03d51
eca569886a5152743c479a4f3ff4d0ecbc5fe85e41f4704bc74405d908761208
c1ccccc1
C-C(-C)-C1-C=C2-C-C-C3-C(-C)(-C-C-C-C-3(-C)-C(-O)=O)-C-2-[CH2;D2;+0:1]-[CH2;D2;+0:2]-1.C-C(-C)-O-C(=[O;H0;D1;+0:3])-C-C-C-C-C-C-C-C-C-C-C-[CH2;D2;+0:4]-[C;D1;H3:5].[O;H0;D1;+0:6]=[C;H0;D3;+0:7](-[O;H0;D2;+0:8]-[CH2;D2;+0:9]-[c;H0;D3;+0:10]1:c:c:c:c:c:1)-[c;H0;D3;+0:11]1:[cH;D2;+0:12]:c:c:c:c:1>>[C;D1;H3:5]-[CH2;D2;+0:4...
null
[]
null
null
null
null
The foregoing formula may require a solubilizing agent, e.g., the methyl ester of dihydroabietic acid (commerical name: HERCOLYN D®), benzyl benzoate, isopropyl myristate and/or C12 -C14 isoparaffin hydrocarbons. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ester.Ester
Aldehyde.Ether.Aromatic alcohol
C1=C2CCC3CCCCC3C2CCC1.c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
CC(C)C1C=C2CCC3C(C)(C(=O)O)CCCC3(C)C2CC1.CCCCCCCCCCCCCC(=O)OC(C)C.O=C(OCc1ccccc1)c1ccccc1>>CCOc1cc(C=O)ccc1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b975ca7d4b05413b8d2fd1f80e50bdb6
CC(=O)O.CCC(CC)COC(C(=O)N(C)CC[NH+](C)C)(c1ccccc1)c1ccccc1.NC(CO)(CO)CO>>CN[C@H](CC(=O)O)C(=O)O
S1C(=CC=C1)C1(CCCCC1)N1CCCCC1.CCC(CC)COC(C1=CC=CC=C1)(C2=CC=CC=C2)C(=O)N(C)CC[NH+](C)C.[Cl-].CC(=O)O.C(C(CO)(CO)N)O>>CN[C@H](CC(=O)O)C(=O)O
[CH3:4][C:5](=[O:6])[OH:7].CCC(CC)COC(c1ccccc1)(c1ccccc1)[C:8]([N:2]([CH3:1])[CH2:3]C[NH+](C)C)=[O:9].NC(CO)(CO)C[OH:10]>>[CH3:1][NH:2][C@H:3]([CH2:4][C:5](=[O:6])[OH:7])[C:8](=[O:9])[OH:10]
CC(=O)O.CCC(CC)COC(C(=O)N(C)CC[NH+](C)C)(c1ccccc1)c1ccccc1.NC(CO)(CO)CO
CN[C@H](CC(=O)O)C(=O)O
null
null
null
Acylation
OtherReaction
888c5838c32bb127332a8288c9576da10f501397ec317cf611e1cbb0cbe611f7
9e3a2fda2223094e7dd934741af3937c724d328b4cefc6d48b1c51affb2653fc
null
C-C-C(-C-C)-C-O-C(-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:3](-[C;D1;H3:4])-[CH2;D2;+0:5]-C-[NH+](-C)-C)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1.N-C(-C-O)(-C-O)-C-[OH;D1;+0:6].[CH3;D1;+0:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]>>[C;D1;H3:4]-[NH;D2;+0:3]-[C@H;D3;+0:5](-[CH2;D2;+0:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10])-[C;H0;D3;+0:1](...
null
[]
null
null
30
MINUTE
The effect on the TCP (1-[1-(2-thienyl)-cyclohexyl]piperidine) binding was measured in rat brain synaptic membranes (SPM) prepared as previously described [J. B. Monahan & J. Michel; J. Neurochem. 48:1699-1708 (1987)]. Prior to their use in the binding assay, frozen SPM were thawed, diluted twenty fold with 50 mM Tris/...
10.6084/m9.figshare.5104873.v1
null
Ether.Tertiary amide.Primary alcohol.Primary alcohol.Primary alcohol.Primary amine
Carboxylic acid.Secondary amine
c1ccccc1.c1ccccc1
null
null
HO-
null
null
0.5
CC(=O)O.CCC(CC)COC(C(=O)N(C)CC[NH+](C)C)(c1ccccc1)c1ccccc1.NC(CO)(CO)CO>>CN[C@H](CC(=O)O)C(=O)O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f82ffc1d185d4762a9b078e4e9fabb07
CCCn1c(=O)c(NC(=O)OC(C)(C)C)nc2ccccc21>>CCCn1c(=O)c(N)nc2ccccc21
C(CC)N1C(C(=NC2=CC=CC=C12)NC(=O)OC(C)(C)C)=O.[OH-].[Na+]>>C(CC)N1C(C(=NC2=CC=CC=C12)N)=O
CC(C)(C)OC(=O)[NH:8][c:7]1[c:5](=[O:6])[n:4]([CH2:3][CH2:2][CH3:1])[c:15]2[c:10]([n:9]1)[cH:11][cH:12][cH:13][cH:14]2>>[CH3:1][CH2:2][CH2:3][n:4]1[c:5](=[O:6])[c:7]([NH2:8])[n:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]12
CCCn1c(=O)c(NC(=O)OC(C)(C)C)nc2ccccc21
CCCn1c(=O)c(N)nc2ccccc21
null
null
Cl.CO
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=c1cnc2ccccc2[nH]1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[c:5]:[#7;a:6](-[C:7]):[c:8]:1=[O;D1;H0:9]>>[C:7]-[#7;a:6]1:[c:5]:[c:4]:[#7;a:3]:[c:2](-[NH2;D1;+0:1]):[c:8]:1=[O;D1;H0:9]
95.7
[{"value": 95.0, "product": "C(CC)N1C(C(=NC2=CC=CC=C12)N)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.7, "product": "C(CC)N1C(C(=NC2=CC=CC=C12)N)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 7.12 grams (0.0234 mol) of carbamate 3 in 50 ml of methanol and 35 ml of 6N hydrochloric acid is stirred at room temperature for 4 hours. The solution is neutralized, with cooling, by addition of 6N sodium hydroxide. The crystals formed are filtered off, washed with water and dried at 50° C. 4.55 g (yield...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccc2nccnc2c1
HO-
Cl.CO
null
null
CCCn1c(=O)c(NC(=O)OC(C)(C)C)nc2ccccc21>Cl.CO>CCCn1c(=O)c(N)nc2ccccc21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-55ff37946a134630811817199fc061c1
Cl>>Cl
C(CC)N1C(C(=NC2=CC=CC=C12)N)=O.Cl.Cl>>Cl.C(CC)N1C(C(=NC2=CC=CC=C12)N)=O
[ClH:16]>>[ClH:16]
Cl
Cl
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
80
[{"value": 80.0, "product": "Cl.C(CC)N1C(C(=NC2=CC=CC=C12)N)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The crystals of compound 4 obtained above are suspended in ethanol. An ethanolic solution of hydrogen chloride gas is then added: the base dissolves and the hydrochloride then begins to precipitate out. After cooling and dilution with ethyl ether, the crystals are filtered off and then washed with a 50/50 ethanol/ethyl...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
null
Cl>C(C)O>Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9cc6bb4134da49a8b23b96d1e3d313cd
CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)O.CC(C)N1C(=O)C(N)N=C(c2ccccc2)c2ccccc21>>CC(C)N1C(=O)C(NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21
NC1C(N(C2=C(C(=N1)C1=CC=CC=C1)C=CC=C2)C(C)C)=O.C(CCl)Cl.C=1C=CC2=C(C1)N=NN2O.C(=O)(OC(C)(C)C)N[C@H](CC1=CC=CC=C1)C(=O)O>>N[C@@H](C(=O)NC1N=C(C2=C(N(C1=O)C(C)C)C=CC=C2)C2=CC=CC=C2)CC2=CC=CC=C2
CC(C)(C)OC(=O)[NH:12][C@@H:11]([C:9](O)=[O:10])[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[CH3:1][CH:2]([CH3:3])[N:4]1[C:5](=[O:6])[CH:7]([NH2:8])[N:20]=[C:21]([c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)[c:28]2[cH:29][cH:30][cH:31][cH:32][c:33]21>>[CH3:1][CH:2]([CH3:3])[N:4]1[C:5](=[O:6])[CH:7]([NH:8][C:9](=[...
CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)O.CC(C)N1C(=O)C(N)N=C(c2ccccc2)c2ccccc21
CC(C)N1C(=O)C(NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21
null
null
C(O)([O-])=O.[Na+].CN(C=O)C.C(C)(=O)OCC
Acylation
OtherReaction
b4c20342f55b434660078663f02be082076e2ff9b9068db91acc0b381022a32e
e525bb030a9f5f4a2fc47bce923bf921a3769ce3300b3fa2600575194671a3f3
O=C(CCc1ccccc1)NC1N=C(c2ccccc2)c2ccccc2NC1=O
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C;H0;D3;+0:4](-O)=[O;D1;H0:5].[C:6]=[#7:7]-[C:8](-[NH2;D1;+0:9])-[C:10](=[O;D1;H0:11])-[#7:12](-[C:13])-[c:14]>>[C:3]-[C:2](-[NH2;D1;+0:1])-[C;H0;D3;+0:4](=[O;D1;H0:5])-[NH;D2;+0:9]-[C:8](-[#7:7]=[C:6])-[C:10](=[O;D1;H0:11])-[#7:12](-[C:13])-[c:14]
null
[]
null
null
2
HOUR
To a stirring solution of (+)-3-amino-2,3-dihydro-1-(2-propyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepine (40.8 g, 139 mmol) in dimethylformamide (140 mL) was added EDC (32.0 g, 167 mmol), HOBT (22.6 g, 167 mmol) and N-BOC-D-phenylalanine (44.3 g, 167 mmol). This was stirred at ambient temperature for 2 h. The reaction was d...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid.Ether.Primary amine.Boc
Secondary amide.Primary amine
null
null
c1ccccc1.c1ccccc1.C1=NCC[NH]c2ccccc21
HO-
C(O)([O-])=O.[Na+].CN(C=O)C.C(C)(=O)OCC
null
2
CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)O.CC(C)N1C(=O)C(N)N=C(c2ccccc2)c2ccccc21>C(O)([O-])=O.[Na+].CN(C=O)C.C(C)(=O)OCC>CC(C)N1C(=O)C(NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6d72a2c9c9c844b7b0c5df8ca422b9cd
CC(=O)O.N#Cc1ccc(C(F)(F)F)cc1C(F)(F)F>>O=C(O)Cc1ccc(C(F)(F)F)cc1C(F)(F)F
C(C)(=O)O.FC(C1=C(C#N)C=CC(=C1)C(F)(F)F)(F)F.OS(=O)(=O)O.O>>FC(C1=C(C=CC(=C1)C(F)(F)F)CC(=O)O)(F)F
C[C:2](=[O:1])[OH:3].N#[C:4][c:5]1[cH:6][cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][c:14]1[C:15]([F:16])([F:17])[F:18]>>[O:1]=[C:2]([OH:3])[CH2:4][c:5]1[cH:6][cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][c:14]1[C:15]([F:16])([F:17])[F:18]
CC(=O)O.N#Cc1ccc(C(F)(F)F)cc1C(F)(F)F
O=C(O)Cc1ccc(C(F)(F)F)cc1C(F)(F)F
null
null
null
C-C Coupling
OtherReaction
90c8dd70249cb7803d1965cca696cfb953e179261cd72d5897d4b9c3ff6c7e49
bf98e437e9d62c3799b8d22cef6764447a2afd089c21ab8eda0c8ca67dbff6fd
c1ccccc1
C-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;D1;H1:3].N#[C;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[O;D1;H1:3])-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
120
CELSIUS
null
null
2,4-Bis(trifluoromethyl)benzonitrile (41.5 mmol, 10.51 g) was taken up in 100 mL acetic acid, 50 mL conc. H2SO4, and 20 mL water. This was heated to 120° C. for 3 h. The reaction was then diluted with 1 L ice water, and extracted with 2×300 mL ethyl acetate. The combined organics were washed with 2×200 mL water, dried ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Nitrile
Carboxylic acid
null
null
c1ccccc1
Other
null
120
null
CC(=O)O.N#Cc1ccc(C(F)(F)F)cc1C(F)(F)F>>O=C(O)Cc1ccc(C(F)(F)F)cc1C(F)(F)F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-11519b9cfafb4d618293384b8bd77b54
CCOC(=O)C1(C(=O)OCC)CC(=O)N1Cc1ccc(OC)cc1OC>>CCOC(=O)C1(C(=O)OCC)CC(=O)N1
COC1=C(CN2C(CC2(C(=O)OCC)C(=O)OCC)=O)C=CC(=C1)OC.S(=O)(=O)([O-])OOS(=O)(=O)[O-].[K+].[K+].P(=O)([O-])([O-])[O-].[K+].[K+].[K+]>>O=C1NC(C1)(C(=O)OCC)C(=O)OCC
COc1ccc(C[N:15]2[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])([C:7](=[O:8])[O:9][CH2:10][CH3:11])[CH2:12][C:13]2=[O:14])c(OC)c1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9][CH2:10][CH3:11])[CH2:12][C:13](=[O:14])[NH:15]1
CCOC(=O)C1(C(=O)OCC)CC(=O)N1Cc1ccc(OC)cc1OC
CCOC(=O)C1(C(=O)OCC)CC(=O)N1
null
null
C(C)#N.O
Reduction
Hydrogenolysis of tertiary amines
8c791012540cd00dd8767581876a3a29b74a76f305dd0f134cf7763b6abd9738
3efc6c7204ad36a2aa7236338bd7163bfb62d1e33efaad6b000b17910587541b
O=C1CCN1
C-O-c1:c:c:c(-C-[N;H0;D3;+0:1]2-[C:2](=[O;D1;H0:3])-[C:4]-[C:5]-2(-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9])-[C:10](=[O;D1;H0:11])-[#8:12]-[C:13]):c(-O-C):c:1>>[C:13]-[#8:12]-[C:10](=[O;D1;H0:11])-[C:5]1(-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9])-[C:4]-[C:2](=[O;D1;H0:3])-[NH;D2;+0:1]-1
null
[]
65
CELSIUS
1
HOUR
1(b) 17.4 g of diethyl 1-(2,4-dimethoxybenzyl)-2-oxoazetidine-4,4-dicarboxylate (prepared as described above) were dissolved in a mixture of 350 ml of acetonitrile and 350 ml of water. 11.2 g of potassium persulfate and 37.4 g of dibasic potassium phosphate were then added to the resulting solution, and the mixture was...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide
Secondary amide
c1ccccc1.C1C[NH]C1
C1CNC1
C1CNC1
HO-
C(C)#N.O
65
1
CCOC(=O)C1(C(=O)OCC)CC(=O)N1Cc1ccc(OC)cc1OC>C(C)#N.O>CCOC(=O)C1(C(=O)OCC)CC(=O)N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-70e6a23c877648c4afd2e249917b361d
CCOC(=O)C1(C(=O)OCC)CC(=O)N1>>O=C1CC(C(=O)[O-])(C(=O)[O-])N1.[Na+]
O=C1NC(C1)(C(=O)OCC)C(=O)OCC.[OH-].[Na+]>>O=C1NC(C1)(C(=O)[O-])C(=O)[O-].[Na+].[Na+]
CC[O:7][C:5]([C:4]1([C:8](=[O:9])[O:10]CC)[CH2:3][C:2](=[O:1])[NH:11]1)=[O:6]>>[O:1]=[C:2]1[CH2:3][C:4]([C:5](=[O:6])[O-:7])([C:8](=[O:9])[O-:10])[NH:11]1.[Na+:13]
CCOC(=O)C1(C(=O)OCC)CC(=O)N1
O=C1CC(C(=O)[O-])(C(=O)[O-])N1.[Na+]
null
null
CO
Functional Group Interconversion
OtherReaction
3d0c4a15f37850238014ea9cf5b9e777f9dd70f2d2ae5ebb7adda479f489012b
a87e633d4c15ade1dd31860f7c44fc378e0d7a7b518b924ae010ea4c26986bb4
O=C1CCN1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4](-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-C-C)-[#7:8]>>[#7:8]-[C:4](-[C:5](-[O-;H0;D1:7])=[O;D1;H0:6])-[C:2](-[O-;H0;D1:1])=[O;D1;H0:3]
null
[]
null
null
1
DAY
1(c) 5.72 g of diethyl 2-oxoazetidine-4,4-dicarboxylate (prepared as described above) were dissolved in 25 ml of methanol. 53.2 ml of a 1N aqueous solution of sodium hydroxide were added to the resulting solution, and the mixture was stirred at room temperature for 1 day. At the end of this time, the reaction mixture w...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
null
null
null
C1CNC1
Other
CO
null
24
CCOC(=O)C1(C(=O)OCC)CC(=O)N1>CO>O=C1CC(C(=O)[O-])(C(=O)[O-])N1.[Na+]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-26423f372bc140e0bcc0d8076fab50a1
CCOC(=O)C(N)C(=O)OCC.O=C(Cl)CCBr>>CCOC(=O)C(NC(=O)CCBr)C(=O)OCC
BrCCC(=O)Cl.C(C)N(CC)CC.Cl.NC(C(=O)OCC)C(=O)OCC.O>>BrCCC(=O)NC(C(=O)OCC)C(=O)OCC
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([NH2:7])[C:13](=[O:14])[O:15][CH2:16][CH3:17].Cl[C:8](=[O:9])[CH2:10][CH2:11][Br:12]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([NH:7][C:8](=[O:9])[CH2:10][CH2:11][Br:12])[C:13](=[O:14])[O:15][CH2:16][CH3:17]
CCOC(=O)C(N)C(=O)OCC.O=C(Cl)CCBr
CCOC(=O)C(NC(=O)CCBr)C(=O)OCC
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9](-[NH2;D1;+0:10])-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:10]-[C:9](-[C:7](=[O;D1;H0:8])-[#8:6]-[C:5])-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]
80.9
[{"value": 80.9, "product": "BrCCC(=O)NC(C(=O)OCC)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
2(a) 2.8 ml of triethylamine were added to a suspension of 2.11 g of diethyl 2-aminomalonate hydrochloride in 50 ml of methylene chloride. 1.71 g of 3-bromopropionyl chloride were then added to the mixture, whilst ice-cooling, and then the mixture was stirred for 30 minutes. At the end of this time, the reaction mixtur...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
null
HCl
C(Cl)Cl
null
0.5
CCOC(=O)C(N)C(=O)OCC.O=C(Cl)CCBr>C(Cl)Cl>CCOC(=O)C(NC(=O)CCBr)C(=O)OCC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-18dc032fadb74d58b47edbd36e5bffb9
CCOC(=O)C(NC(=O)CCBr)C(=O)OCC>>CCOC(=O)C1(C(=O)OCC)CCC(=O)N1
CCCCCCC=CCCC.BrCCC(=O)NC(C(=O)OCC)C(=O)OCC>>O=C1NC(CC1)(C(=O)OCC)C(=O)OCC
Br[CH2:12][CH2:13][C:14](=[O:15])[NH:16][CH:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:7](=[O:8])[O:9][CH2:10][CH3:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1([C:7](=[O:8])[O:9][CH2:10][CH3:11])[CH2:12][CH2:13][C:14](=[O:15])[NH:16]1
CCOC(=O)C(NC(=O)CCBr)C(=O)OCC
CCOC(=O)C1(C(=O)OCC)CCC(=O)N1
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
2ec746c87117cf125fab2602e6958ce66a61fbb749cf3674123a8cc74714adcc
098246e03ca5d64cc349e355265e564e498af79e5bd90f15ba92540c1f7ceed4
O=C1CCCN1
Br-[CH2;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[CH;D3;+0:6](-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10])-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]>>[C:14]-[#8:13]-[C:11](=[O;D1;H0:12])-[C;H0;D4;+0:6]1(-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10])-[#7:5]-[C:3](=[O;D1;H0:4])-[C:2]-[CH2;D2;+0:1]-1
37.3
[{"value": 37.3, "product": "O=C1NC(CC1)(C(=O)OCC)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
2(b) 314 μl of 1,8-diaza[5.4.0]-7-undecene were added to a solution of 620 mg of diethyl 2-(3-bromopropionamido)malonate (prepared as described above) dissolved in methylene chloride, and the mixture was stirred at room temperature for 3 hours. At the end of this time, the reaction mixture was concentrated by evaporati...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ester
Ester.Ester
null
C1CCNC1
C1CCNC1
HBr
C(Cl)Cl
null
3
CCOC(=O)C(NC(=O)CCBr)C(=O)OCC>C(Cl)Cl>CCOC(=O)C1(C(=O)OCC)CCC(=O)N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6b01a25f8be14edba4c5faad2b8765a1
CCOC(=O)C1(C(=O)OCC)CCC(=O)N1>>O=C1CCC(C(=O)[O-])(C(=O)[O-])N1.[Na+]
[OH-].[Na+].O=C1NC(CC1)(C(=O)OCC)C(=O)OCC>>O=C1NC(CC1)(C(=O)[O-])C(=O)[O-].[Na+].[Na+]
CC[O:8][C:6]([C:5]1([C:9](=[O:10])[O:11]CC)[CH2:4][CH2:3][C:2](=[O:1])[NH:12]1)=[O:7]>>[O:1]=[C:2]1[CH2:3][CH2:4][C:5]([C:6](=[O:7])[O-:8])([C:9](=[O:10])[O-:11])[NH:12]1.[Na+:14]
CCOC(=O)C1(C(=O)OCC)CCC(=O)N1
O=C1CCC(C(=O)[O-])(C(=O)[O-])N1.[Na+]
null
null
C(C)O
Functional Group Interconversion
OtherReaction
3d0c4a15f37850238014ea9cf5b9e777f9dd70f2d2ae5ebb7adda479f489012b
a87e633d4c15ade1dd31860f7c44fc378e0d7a7b518b924ae010ea4c26986bb4
O=C1CCCN1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4](-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-C-C)-[#7:8]>>[#7:8]-[C:4](-[C:5](-[O-;H0;D1:7])=[O;D1;H0:6])-[C:2](-[O-;H0;D1:1])=[O;D1;H0:3]
null
[]
null
null
3
DAY
2(c) 8.74 ml of a 1N aqueous solution of sodium hydroxide were added to a solution of 1.0 g of diethyl 2-oxopyrrolidine-5,5-dicarboxylate (prepared as described above) in 10 ml of ethanol, and the mixture was stirred at room temperature for 3 days. At the end of this time, the solvent was removed by distillation under ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
null
null
null
C1CCNC1
Other
C(C)O
null
72
CCOC(=O)C1(C(=O)OCC)CCC(=O)N1>C(C)O>O=C1CCC(C(=O)[O-])(C(=O)[O-])N1.[Na+]
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-8665e4e9ba584e848afe9d8abb3d246a
COc1ccc(CN2C(=O)C([C@@H](C)O)C2C(=O)OCc2ccccc2)c(OC)c1>>C[C@@H](O)C1C(=O)NC1C(=O)OCc1ccccc1
COC1=C(CN2C(C(C2C(=O)OCC2=CC=CC=C2)[C@@H](C)O)=O)C=CC(=C1)OC.S(=O)(=O)([O-])OOS(=O)(=O)[O-].[K+].[K+].P(=O)([O-])([O-])[O-].[K+].[K+].[K+]>>O[C@H](C)C1C(NC1C(=O)OCC1=CC=CC=C1)=O
COc1ccc(C[N:7]2[C:5](=[O:6])[CH:4]([C@@H:2]([CH3:1])[OH:3])[CH:8]2[C:9](=[O:10])[O:11][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)c(OC)c1>>[CH3:1][C@@H:2]([OH:3])[CH:4]1[C:5](=[O:6])[NH:7][CH:8]1[C:9](=[O:10])[O:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
COc1ccc(CN2C(=O)C([C@@H](C)O)C2C(=O)OCc2ccccc2)c(OC)c1
C[C@@H](O)C1C(=O)NC1C(=O)OCc1ccccc1
null
null
C(C)#N.O
Reduction
Hydrogenolysis of tertiary amines
8c791012540cd00dd8767581876a3a29b74a76f305dd0f134cf7763b6abd9738
3efc6c7204ad36a2aa7236338bd7163bfb62d1e33efaad6b000b17910587541b
O=C1CC(C(=O)OCc2ccccc2)N1
C-O-c1:c:c:c(-C-[N;H0;D3;+0:1]2-[C:2](=[O;D1;H0:3])-[C:4]-[C:5]-2-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9]):c(-O-C):c:1>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:5]1-[C:4]-[C:2](=[O;D1;H0:3])-[NH;D2;+0:1]-1
null
[]
70
CELSIUS
60
MINUTE
3(a) 14 g of benzyl 1-(2,4-dimethoxybenzyl)-3-[(R)-1-hydroxyethyl]-2-oxoazetidine-4-carboxylate [which had been synthesized according to a procedure similar to that described in Tetrahedron 46, 1795 (1984)] were dissolved in a mixture of 420 ml of acetonitrile and 420 ml of water. 66.1 g of potassium persulfate and 23....
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide
Secondary amide
c1ccccc1.C1C[NH]C1
C1CNC1
C1CNC1.c1ccccc1
HO-
C(C)#N.O
70
1
COc1ccc(CN2C(=O)C([C@@H](C)O)C2C(=O)OCc2ccccc2)c(OC)c1>C(C)#N.O>C[C@@H](O)C1C(=O)NC1C(=O)OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-889bb27b57964e04bf32c3b369fdcdbb
C[C@@H](O)C1C(=O)NC1C(=O)OCc1ccccc1>>C[C@@H](O)C1C(=O)NC1C(=O)O
O[C@H](C)C1C(NC1C(=O)OCC1=CC=CC=C1)=O>>O[C@H](C)C1C(NC1C(=O)O)=O
c1ccc(C[O:11][C:9]([CH:8]2[CH:4]([C@@H:2]([CH3:1])[OH:3])[C:5](=[O:6])[NH:7]2)=[O:10])cc1>>[CH3:1][C@@H:2]([OH:3])[CH:4]1[C:5](=[O:6])[NH:7][CH:8]1[C:9](=[O:10])[OH:11]
C[C@@H](O)C1C(=O)NC1C(=O)OCc1ccccc1
C[C@@H](O)C1C(=O)NC1C(=O)O
null
[Pd]
CO
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1CCN1
[#7:1]-[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-C-c1:c:c:c:c:c:1>>[#7:1]-[C:2]-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]
null
[]
null
null
null
null
3(b) 500 mg of the benzyl 3-[(R)-1-hydroxyethyl]-2-oxoazetidine-4-carboxylate (prepared as described in above) were dissolved in 5 ml of methanol, and the mixture was hydrogenated in the presence of 100 mg of a 10% w/w palladium-on-carbon catalyst at room temperature for 2 hours. At the end of this time, the catalyst w...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
C1CNC1
Other
[Pd].CO
null
null
C[C@@H](O)C1C(=O)NC1C(=O)OCc1ccccc1>[Pd].CO>C[C@@H](O)C1C(=O)NC1C(=O)O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-7adcf7d8bf834507a9a5cff0f9c64b36
COC(=O)CCCCCCCCO[C@H]1O[C@H](CO)[C@@H](O)[C@H](OC(C)=O)[C@H]1O[C@H]1O[C@H](COC(C)=O)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1.CS(=O)(=O)[O-]>>COC(=O)CCCCCCCCO[C@H]1O[C@H](COS(C)(=O)=O)[C@@H](O)[C@H](OC(C)=O)[C@H]1O[C@H]1O[C@H](COC(C)=O)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1
C(C)(=O)O[C@@H]1[C@H]([C@@H](OCCCCCCCCC(=O)OC)O[C@@H]([C@H]1O)CO)O[C@@H]1[C@H](OCC2=CC=CC=C2)[C@@H](OCC2=CC=CC=C2)[C@H](OCC2=CC=CC=C2)[C@H](O1)COC(C)=O.S(C)(=O)(=O)[O-]>>C(C)(=O)O[C@@H]1[C@H]([C@@H](OCCCCCCCCC(=O)OC)O[C@@H]([C@H]1O)COS(=O)(=O)C)O[C@@H]1[C@H](OCC2=CC=CC=C2)[C@@H](OCC2=CC=CC=C2)[C@H](OCC2=CC=CC=C2)[C@H](...
[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][C@H:14]1[O:15][C@H:16]([CH2:17][OH:18])[C@@H:23]([OH:24])[C@H:25]([O:26][C:27]([CH3:28])=[O:29])[C@H:30]1[O:31][C@H:32]1[O:33][C@H:34]([CH2:35][O:36][C:37]([CH3:38])=[O:39])[C@@H:40]([O:41][CH2:42][c:43]2[cH:44][cH:45][cH:46][cH:...
COC(=O)CCCCCCCCO[C@H]1O[C@H](CO)[C@@H](O)[C@H](OC(C)=O)[C@H]1O[C@H]1O[C@H](COC(C)=O)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1.CS(=O)(=O)[O-]
COC(=O)CCCCCCCCO[C@H]1O[C@H](COS(C)(=O)=O)[C@@H](O)[C@H](OC(C)=O)[C@H]1O[C@H]1O[C@H](COC(C)=O)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1
null
null
null
Miscellaneous
OtherReaction
9b60953d4bd7396689a9f1dc793198144ad18c5d1bb07ec2a5c21f6f4e815117
6781433991701ad30841681becf17666e4fcc081fce02f6b9b131a47f9893572
c1ccc(CO[C@@H]2[C@@H](OCc3ccccc3)[C@@H](O[C@@H]3CCCOC3)OC[C@H]2OCc2ccccc2)cc1
[#8:1]-[C:2]-[C:3]-[OH;D1;+0:4].[C;D1;H3:5]-[S;H0;D4;+0:6](-[O-])(=[O;D1;H0:7])=[O;D1;H0:8]>>[#8:1]-[C:2]-[C:3]-[O;H0;D2;+0:4]-[S;H0;D4;+0:6](-[C;D1;H3:5])(=[O;D1;H0:7])=[O;D1;H0:8]
85.3
[{"value": 85.3, "product": "C(C)(=O)O[C@@H]1[C@H]([C@@H](OCCCCCCCCC(=O)OC)O[C@@H]([C@H]1O)COS(=O)(=O)C)O[C@@H]1[C@H](OCC2=CC=CC=C2)[C@@H](OCC2=CC=CC=C2)[C@H](OCC2=CC=CC=C2)[C@H](O1)COC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Compound 24 (570 mg, 0.66 mmol) was converted into its methane sulfonyl derivative exactly as described for the preparation of 10 to give 25 (530 mg, 85.3%) as a syrup after chromatography on silica gel using (hexane:ethyl acetate; 3:2) as eluant; [α]D +76.6° (c 0.57, chloroform). 1H-n.m.r. (CDCl3): δ5.19(t, 1H, J2,3 =...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonic acid
Mesylate
null
null
C1CCOCC1.C1CCOCC1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
null
null
null
COC(=O)CCCCCCCCO[C@H]1O[C@H](CO)[C@@H](O)[C@H](OC(C)=O)[C@H]1O[C@H]1O[C@H](COC(C)=O)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1.CS(=O)(=O)[O-]>>COC(=O)CCCCCCCCO[C@H]1O[C@H](COS(C)(=O)=O)[C@@H](O)[C@H](OC(C)=O)[C@H]1O[C@H]1O[C@H](COC(C)=O)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-32ce6edd6bef4c65ac649d1e55c8191a
CC(=O)OC(=S)[C@H]1OC(OC(C)=O)[C@H](OC(C)=O)[C@@H](Oc2ccccc2)[C@@H]1OC(C)=O>>CC(=O)OC[C@H]1OC(O)[C@H](OC(C)=O)C[C@@H]1OC(C)=O
C(C)(=O)OC1[C@H](OC(C)=O)[C@@H](OC2=CC=CC=C2)[C@H](OC(C)=O)[C@H](O1)C(OC(C)=O)=S.C(CCC)[SnH](CCCC)CCCC>>C(C)(=O)O[C@H]1C(O)O[C@@H]([C@H](C1)OC(C)=O)COC(C)=O
CC(=O)[O:9][CH:8]1[O:7][C@H:6]([C:5](=S)[O:4][C:2]([CH3:1])=[O:3])[C@@H:16]([O:17][C:18]([CH3:19])=[O:20])[C@H:15](Oc2ccccc2)[C@H:10]1[O:11][C:12]([CH3:13])=[O:14]>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][C@H:6]1[O:7][CH:8]([OH:9])[C@H:10]([O:11][C:12]([CH3:13])=[O:14])[CH2:15][C@@H:16]1[O:17][C:18]([CH3:19])=[O:20]
CC(=O)OC(=S)[C@H]1OC(OC(C)=O)[C@H](OC(C)=O)[C@@H](Oc2ccccc2)[C@@H]1OC(C)=O
CC(=O)OC[C@H]1OC(O)[C@H](OC(C)=O)C[C@@H]1OC(C)=O
null
null
C1(=CC=CC=C1)C
Reduction
OtherReaction
e4c14ae768ba989e274e1a52463331917b5a935962ecdffbab8769677a602a4d
e38ee42d3bef3956d2e46682a5b1af084766167f26179fd053e6bb57e8e6ca46
C1CCOCC1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]1-[#8:3]-[C:4](-[C;H0;D3;+0:5](=S)-[#8:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9])-[C:10](-[#8:11]-[C:12](-[C;D1;H3:13])=[O;D1;H0:14])-[C@H;D3;+0:15](-O-c2:c:c:c:c:c:2)-[C:16]-1-[#8:17]-[C:18](-[C;D1;H3:19])=[O;D1;H0:20]>>[C;D1;H3:19]-[C:18](=[O;D1;H0:20])-[#8:17]-[C:16]1-[CH2;D2;+0:15]-[C:10](-[#8:...
135.5
[{"value": 135.5, "product": "C(C)(=O)O[C@H]1C(O)O[C@@H]([C@H](C1)OC(C)=O)COC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
1,2,4,6-tetra-O-acetyl-3-O-phenylthiono-glucopyranose (5.2 g) was dissolved in toluene (50 mL) and added to tributyl tin hydride (6.7 mL) and azobisisobutryonitrile (2.8 g). The reaction mixture was heated for 1 to 3 hours at 80° C. to provide for 3-deoxy-2,4,6-tri-O-acetyl-glucopyranose (4.5 g). Conditions: See reacti...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ether.Thiocarbonyl
Ester.Secondary alcohol
C1CCOCC1.c1ccccc1
C1CCOCC1
C1CCOCC1
Other
C1(=CC=CC=C1)C
80
null
CC(=O)OC(=S)[C@H]1OC(OC(C)=O)[C@H](OC(C)=O)[C@@H](Oc2ccccc2)[C@@H]1OC(C)=O>C1(=CC=CC=C1)C>CC(=O)OC[C@H]1OC(O)[C@H](OC(C)=O)C[C@@H]1OC(C)=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-cd7c12114e984514b8d82b35efd01ccd
O=C(Br)C(=O)Br.OC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)C[C@H]1OCc1ccccc1>>BrC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)C[C@H]1OCc1ccccc1
C(C1=CC=CC=C1)O[C@H]1C(O)O[C@@H]([C@H](C1)OCC1=CC=CC=C1)COCC1=CC=CC=C1.CN(C)C=O.C(C(=O)Br)(=O)Br>>C(C1=CC=CC=C1)O[C@H]1C(O[C@@H]([C@H](C1)OCC1=CC=CC=C1)COCC1=CC=CC=C1)Br
O=C(Br)C(=O)[Br:1].O[CH:2]1[O:3][C@H:4]([CH2:5][O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[C@@H:14]([O:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[CH2:23][C@H:24]1[O:25][CH2:26][c:27]1[cH:28][cH:29][cH:30][cH:31][cH:32]1>>[Br:1][CH:2]1[O:3][C@H:4]([CH2:5][O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:...
O=C(Br)C(=O)Br.OC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)C[C@H]1OCc1ccccc1
BrC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)C[C@H]1OCc1ccccc1
null
null
ClCCl
Functional Group Interconversion
OtherReaction
edbe343abcae191e59a8b7c8d1ed8c10f6e52652fcab71eb134001accb9f05b8
b09ce277dcd602b68e9920bcb9affbc52d538599ca7a759ab36af492014f302b
c1ccc(COC[C@H]2OC[C@H](OCc3ccccc3)C[C@@H]2OCc2ccccc2)cc1
Br-C(=O)-C(=O)-[Br;H0;D1;+0:1].O-[CH;D3;+0:2](-[#8:3]-[C:4])-[C:5](-[#8:6])-[C:7]>>[#8:6]-[C:5](-[C:7])-[CH;D3;+0:2](-[Br;H0;D1;+0:1])-[#8:3]-[C:4]
null
[]
0
CELSIUS
1
HOUR
3-Deoxy-2,4,6-tri-O-benzyl-glucopyranose (2.2 g) was dissolved in dichloromethane (20 mL) and dry DMF (880 μL) was added. The reaction solution was cooled at 0° C. and oxalyl bromide (500 μL) was added and the resulting solution stirred at 0° to 5° C. for 1 hour. The solution was then diluted with dichloromethane (100 ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Ether.Secondary alcohol
Secondary halide
C1CCOCC1
C1CCOCC1
C1CCOCC1.c1ccccc1.c1ccccc1.c1ccccc1
HBr
ClCCl
0
1
O=C(Br)C(=O)Br.OC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)C[C@H]1OCc1ccccc1>ClCCl>BrC1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)C[C@H]1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0dea9024bb7d4473a312fe7ad7811c1f
CCN(CC)CC.CO[C@H]1[C@H](O)[C@@H](CO)OC(O)[C@@H]1O>>C=CCC1(O)O[C@H](CO)[C@@H](O)[C@H](OC)[C@H]1O
C(C)N(CC)CC.CO[C@@H]1[C@H](C(O)O[C@@H]([C@H]1O)CO)O.FC(S(=O)(=O)O)(F)F>>C(C=C)C1(O)[C@H](O)[C@@H](OC)[C@H](O)[C@H](O1)CO
CCN([CH2:1]C)[CH2:3][CH3:2].[CH:4]1([OH:5])[O:6][C@H:7]([CH2:8][OH:9])[C@@H:10]([OH:11])[C@H:12]([O:13][CH3:14])[C@H:15]1[OH:16]>>[CH2:1]=[CH:2][CH2:3][C:4]1([OH:5])[O:6][C@H:7]([CH2:8][OH:9])[C@@H:10]([OH:11])[C@H:12]([O:13][CH3:14])[C@H:15]1[OH:16]
CCN(CC)CC.CO[C@H]1[C@H](O)[C@@H](CO)OC(O)[C@@H]1O
C=CCC1(O)O[C@H](CO)[C@@H](O)[C@H](OC)[C@H]1O
null
null
C(C=C)O.FC(C(=O)O)(F)F
C-C Coupling
OtherReaction
6411d57862789c812f7a1e2785e0e32bdd5bdb9657491692cae890b673e328d5
da4b0d2a54a1e8bc31f063d4fb50b426f270269b4ed22f20855284531e33528e
C1CCOCC1
C-C-N(-[CH2;D2;+0:1]-C)-[CH2;D2;+0:2]-[CH3;D1;+0:3].[C:4]-[C:5](-[O;D1;H1:6])-[CH;D3;+0:7](-[O;D1;H1:8])-[#8:9]-[C:10]>>[C:4]-[C:5](-[O;D1;H1:6])-[C;H0;D4;+0:7](-[O;D1;H1:8])(-[CH2;D2;+0:2]-[CH;D2;+0:3]=[CH2;D1;+0:1])-[#8:9]-[C:10]
50.8
[{"value": 50.8, "product": "C(C=C)C1(O)[C@H](O)[C@@H](OC)[C@H](O)[C@H](O1)CO", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
3-O-methyl-1,2:5,6-di-O-isopropylidine-glucopyranose (10.2 g) was dissolved in 90% aqueous trifluoroacetic acid (30 mL) and stirred for 1 hour at room temperature. The reaction mixture was evaporated and then coevaporated with toluene followed by ethanol coevaporation to provide the product which was directly used for ...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol.Tertiary amine
Ether.Tertiary alcohol.Allyl
C1CCOCC1
C1CCOCC1
C1CCOCC1
Other
C(C=C)O.FC(C(=O)O)(F)F
null
1
CCN(CC)CC.CO[C@H]1[C@H](O)[C@@H](CO)OC(O)[C@@H]1O>C(C=C)O.FC(C(=O)O)(F)F>C=CCC1(O)O[C@H](CO)[C@@H](O)[C@H](OC)[C@H]1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a11503481bb24752a1c157037dda3427
BrCc1ccccc1.C=CCC1(O)O[C@H](CO)[C@@H](O)[C@H](OC)[C@H]1O>>C=CCC1(O)O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H](OC)[C@H]1OCc1ccccc1
C(C=C)C1(O)[C@H](O)[C@@H](OC)[C@H](O)[C@H](O1)CO.[H-].[Na+].C(C1=CC=CC=C1)Br>>C(C=C)C1(O)[C@H](OCC2=CC=CC=C2)[C@@H](OC)[C@H](OCC2=CC=CC=C2)[C@H](O1)COCC1=CC=CC=C1
Br[CH2:31][c:32]1[cH:33][cH:34][cH:35][cH:10][cH:37]1.[CH2:1]=[CH:2][CH2:3][C:4]1([OH:5])[O:6][C@H:7]([CH2:8][OH:9])[C@@H:17]([OH:18])[C@H:26]([O:27][CH3:28])[C@H:29]1[OH:30]>>[CH2:1]=[CH:2][CH2:3][C:4]1([OH:5])[O:6][C@H:7]([CH2:8][O:9][CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[C@@H:17]([O:18][CH2:19][c:20]2[...
BrCc1ccccc1.C=CCC1(O)O[C@H](CO)[C@@H](O)[C@H](OC)[C@H]1O
C=CCC1(O)O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H](OC)[C@H]1OCc1ccccc1
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
77fc7189ae8b9a1747b71995b4422540da77d8a96ff834be19fa984e1ea2fe27
b8301bbfbb4611baf6a091c5acabb0fbec33741ec27caf76ebcaa8bffeedfb2b
c1ccc(COC[C@H]2OC[C@H](OCc3ccccc3)C[C@@H]2OCc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:1.[OH;D1;+0:8]-[C:9]1-[C:10]-[C:11](-[OH;D1;+0:12])-[C:13]-[#8:14]-[C:15]-1-[C:16]-[OH;D1;+0:17]>>[c:18]:[c:19](-[CH2;D2;+0:6]-[O;H0;D2;+0:17]-[C:16]-[C:15]1-[#8:14]-[C:13]-[C:11](-[O;H0;D2;+0:12]-[CH2;D2;+0:1]-[c:2]2:[c:3]:[c:4]:[cH;D2;+0:5]:[c...
null
[]
0
CELSIUS
0.5
HOUR
Allyl-3-O-methyl-glucopyranose (4.5 g) was dissolved in anhydrous DMF (120 mL) and sodium hydride (1.84 g, 50% dispersion in oil) was added thereto. The resulting solution was stirred for 0.5 hours at 0° C. Benzyl bromide (6.8 mL) was added dropwise at 0° to 5° C. and the reaction mixture was then stirred for 4 hours a...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol.Secondary alcohol.Secondary alcohol
Ether.Ether.Ether
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
C1CCOCC1.c1ccccc1.c1ccccc1.c1ccccc1
Br-
CN(C)C=O
0
0.5
BrCc1ccccc1.C=CCC1(O)O[C@H](CO)[C@@H](O)[C@H](OC)[C@H]1O>CN(C)C=O>C=CCC1(O)O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H](OC)[C@H]1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-df8ad700d0524d5dbe0290d4c136f968
CCN(CC)CC.OC1OC[C@@H](O)[C@H](O)[C@H]1O>>C=CCC1(O)OC[C@@H](O)[C@H](O)[C@H]1O
OC1[C@H](O)[C@@H](O)[C@H](O)CO1.FC(S(=O)(=O)O)(F)F.C(C)N(CC)CC>>C(C=C)C1(O)[C@H](O)[C@@H](O)[C@H](O)CO1
CCN([CH2:1]C)[CH2:3][CH3:2].[CH:4]1([OH:5])[O:6][CH2:7][C@@H:8]([OH:9])[C@H:10]([OH:11])[C@H:12]1[OH:13]>>[CH2:1]=[CH:2][CH2:3][C:4]1([OH:5])[O:6][CH2:7][C@@H:8]([OH:9])[C@H:10]([OH:11])[C@H:12]1[OH:13]
CCN(CC)CC.OC1OC[C@@H](O)[C@H](O)[C@H]1O
C=CCC1(O)OC[C@@H](O)[C@H](O)[C@H]1O
null
null
C(C=C)O
C-C Coupling
OtherReaction
6411d57862789c812f7a1e2785e0e32bdd5bdb9657491692cae890b673e328d5
da4b0d2a54a1e8bc31f063d4fb50b426f270269b4ed22f20855284531e33528e
C1CCOCC1
C-C-N(-[CH2;D2;+0:1]-C)-[CH2;D2;+0:2]-[CH3;D1;+0:3].[C:4]-[C:5](-[O;D1;H1:6])-[CH;D3;+0:7](-[O;D1;H1:8])-[#8:9]-[C:10]>>[C:4]-[C:5](-[O;D1;H1:6])-[C;H0;D4;+0:7](-[O;D1;H1:8])(-[CH2;D2;+0:2]-[CH;D2;+0:3]=[CH2;D1;+0:1])-[#8:9]-[C:10]
null
[]
0
CELSIUS
15
MINUTE
Xylopyranose (15.0 g) was dissolved in allyl alcohol (150 mL) and trifluoromethane sulfonic acid (235 μL) was dropwise added 0° C. The reaction was stirred at 0° C. for 15 minutes and then heated at 80° C. for 4 hours. The reaction solution was then neutralized with triethylamine and evaporated to dryness. Chromatograp...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol.Tertiary amine
Ether.Tertiary alcohol.Allyl
C1CCOCC1
C1CCOCC1
C1CCOCC1
Other
C(C=C)O
0
0.25
CCN(CC)CC.OC1OC[C@@H](O)[C@H](O)[C@H]1O>C(C=C)O>C=CCC1(O)OC[C@@H](O)[C@H](O)[C@H]1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-86fe5203ed9f4fbdb2fe14c9d318ed68
OBr.OC1OC[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1>>BrC1OC[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1
C(C1=CC=CC=C1)O[C@H]1C(O)OC[C@H]([C@@H]1OCC1=CC=CC=C1)OCC1=CC=CC=C1.CN(C)C=O.OBr>>C(C1=CC=CC=C1)O[C@H]1C(OC[C@H]([C@@H]1OCC1=CC=CC=C1)OCC1=CC=CC=C1)Br
O[Br:1].O[CH:2]1[O:3][CH2:4][C@@H:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[C@H:14]([O:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[C@H:23]1[O:24][CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1>>[Br:1][CH:2]1[O:3][CH2:4][C@@H:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[C@H:1...
OBr.OC1OC[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1
BrC1OC[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1
null
null
ClCCl
Functional Group Interconversion
OtherReaction
ca81d1ab25975c317067435fa62d56552402561ea09dc3fad1fcd10a49b516de
4a24ab9366ad1597555eebbe459af51e23a50a6f7a19fd3b20b61e39b88af65c
c1ccc(CO[C@@H]2[C@@H](OCc3ccccc3)COC[C@H]2OCc2ccccc2)cc1
O-[Br;H0;D1;+0:1].O-[CH;D3;+0:2](-[#8:3]-[C:4])-[C:5](-[#8:6])-[C:7]>>[#8:6]-[C:5](-[C:7])-[CH;D3;+0:2](-[Br;H0;D1;+0:1])-[#8:3]-[C:4]
null
[]
0
CELSIUS
1
HOUR
2,3,4-tri-O-benzyl-xylopyranose was dissolved in dry dichloromethane (50 mL) and dry DMF (3.0 mL) was added. The reaction mixture was cooled at 0° C. and added dropwise oxayl bromide (1.4 mL). The reaction mixture was stirred for 1 hour at 0° to 5° C. and then diluted with dichloromethane (250 mL), washed with water (2...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol
Secondary halide
C1CCOCC1
C1CCOCC1
C1CCOCC1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
ClCCl
0
1
OBr.OC1OC[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1>ClCCl>BrC1OC[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b359345567474302818835351c759593
CO.O=C(O)Cc1ccccc1O>>COC(=O)Cc1ccccc1O
OC1=C(C=CC=C1)CC(=O)O.Cl.CO>>OC1=C(C=CC=C1)CC(=O)OC
[CH3:1][OH:2].O[C:3](=[O:4])[CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[OH:12]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[OH:12]
CO.O=C(O)Cc1ccccc1O
COC(=O)Cc1ccccc1O
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C;D1;H3:5]-[OH;D1;+0:6]>>[C;D1;H3:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
92
[{"value": 92.0, "product": "OC1=C(C=CC=C1)CC(=O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
2-(Hydroxyphenyl)acetic acid (50 g) was added to a solution of hydrogen chloride in methanol [prepared from acetyl chloride (25 ml) and methanol (250 ml)]. The solution was stirred at room temperature for three hours and then allowed to stand overnight (fifteen hours). The resulting mixture was concentrated under reduc...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
null
null
3
CO.O=C(O)Cc1ccccc1O>>COC(=O)Cc1ccccc1O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ff8ee1b2e9464ba793997011769a0de5
BrCc1ccccc1.COC(=O)Cc1ccccc1O>>COC(=O)Cc1ccccc1OCc1ccccc1
O.C([O-])([O-])=O.[K+].[K+].OC1=C(C=CC=C1)CC(=O)OC.C(C1=CC=CC=C1)Br>>C(C1=CC=CC=C1)OC1=C(C=CC=C1)CC(=O)OC
Br[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[CH3:1][O:2][C:3](=[O:4])[CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[OH:12]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
BrCc1ccccc1.COC(=O)Cc1ccccc1O
COC(=O)Cc1ccccc1OCc1ccccc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:7]:[c:6](-[O;H0;D2;+0:5]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:8]
83
[{"value": 83.0, "product": "C(C1=CC=CC=C1)OC1=C(C=CC=C1)CC(=O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Methyl (2-hydroxyphenyl)acetate (21.0 g) was dissolved in DMF (200 ml), and potassium carbonate (19.35 g) was added in one portion. Benzyl bromide (23.94 g) in DMF (50 ml) was added dropwise to this mixture, with stirring, at room temperature. After eighteen hours the mixture was poured into water (500 ml) and extracte...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HBr
CN(C)C=O
null
null
BrCc1ccccc1.COC(=O)Cc1ccccc1O>CN(C)C=O>COC(=O)Cc1ccccc1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-34185b3344f149daad0d7bc149c9dc48
COC(=O)Cc1ccccc1OCc1ccccc1.COC=O>>COC(=O)C(=CO)c1ccccc1OCc1ccccc1
O.C(C1=CC=CC=C1)OC1=C(C=CC=C1)CC(=O)OC.C(=O)OC.[H-].[Na+]>>C(C1=CC=CC=C1)OC1=C(C=CC=C1)C(C(=O)OC)=CO
[CH3:1][O:2][C:3](=[O:4])[CH2:5][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1.CO[CH:6]=[O:7]>>[CH3:1][O:2][C:3](=[O:4])[C:5](=[CH:6][OH:7])[c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
COC(=O)Cc1ccccc1OCc1ccccc1.COC=O
COC(=O)C(=CO)c1ccccc1OCc1ccccc1
null
null
CN(C)C=O
C-C Coupling
OtherReaction
96625d77e84283c0b3d12da7aa89224d3f1463a0c9daded8a4664af279e46c47
8580ed94a2dd8e44b9acc2872ac5603f42e85017f3ed552f3d73a2ad78c46917
c1ccc(COc2ccccc2)cc1
C-O-[CH;D2;+0:1]=[O;H0;D1;+0:2].[C;D1;H3:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[CH2;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[C;D1;H3:3]-[#8:4]-[C:5](=[O;D1;H0:6])-[C;H0;D3;+0:7](=[CH;D2;+0:1]-[OH;D1;+0:2])-[c:8](:[c:9]):[c:10]
null
[]
0
CELSIUS
2
HOUR
A mixture of methyl 2-benzyloxyphenylacetate (26.99 g) and methyl formate (126.62 g) in dry DMF (300 ml) was added dropwise to a stirred suspension of sodium hydride (50% disp. in oil, 10.13 g) in DMF (300 ml) at 0° C. After stirring at 0° C. for two hours the mixture was poured into water (1000 ml) and washed with eth...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether
Ester.Enol
null
null
c1ccccc1.c1ccccc1
HO-
CN(C)C=O
0
2
COC(=O)Cc1ccccc1OCc1ccccc1.COC=O>CN(C)C=O>COC(=O)C(=CO)c1ccccc1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-b04a46ce4c88420bb722e57bd623063c
COC(=O)C(=CO)c1ccccc1OCc1ccccc1.COS(=O)(=O)OC.O.O=C([O-])[O-]>>CO/C=C(/C(=O)OC)c1ccccc1OCc1ccccc1.COC(=O)Cc1ccccc1OCc1ccccc1
O.S(=O)(=O)(OC)OC.C(C1=CC=CC=C1)OC1=C(C=CC=C1)C(C(=O)OC)=CO.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)OC1=C(C=CC=C1)/C(/C(=O)OC)=C\OC.C(C1=CC=CC=C1)OC1=C(C=CC=C1)CC(=O)OC
[OH:2][CH:3]=[C:4]([C:5](=[O:6])[O:7][CH3:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[O:15][CH2:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1.O=S(=O)(O[CH3:1])O[CH3:29].[OH2:34].[O-][C:25]([O-:24])=[O:26]>>[CH3:1][O:2]/[CH:3]=[C:4](/[C:5](=[O:6])[O:7][CH3:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[O:15][CH2:16][c:1...
COC(=O)C(=CO)c1ccccc1OCc1ccccc1.COS(=O)(=O)OC.O.O=C([O-])[O-]
CO/C=C(/C(=O)OC)c1ccccc1OCc1ccccc1.COC(=O)Cc1ccccc1OCc1ccccc1
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
a58d1a35f0d0559f750e4ccf181d02e2200e90dc49e5336181bf59be37e44301
dd4efefcda3ca4680010d4c32943365ea0e60014859128aab77d945ddc5cd5de
c1ccc(COc2ccccc2)cc1.c1ccc(COc2ccccc2)cc1
O=S(=O)(-O-[CH3;D1;+0:1])-O-[CH3;D1;+0:2].[#8:3]-[C:4](=[O;D1;H0:5])-[C:6](-[c:7])=[C:8]-[OH;D1;+0:9].[O-;H0;D1:10]-[C;H0;D3;+0:11](-[O-])=[O;D1;H0:12].[OH2;D0;+0:13]>>[#8:3]-[C:4](=[O;D1;H0:5])/[C:6](-[c:7])=[C:8]/[O;H0;D2;+0:9]-[CH3;D1;+0:1].[C;D1;H3:14]-[O;H0;D2;+0:10]-[C;H0;D3;+0:11](=[O;D1;H0:12])-[C:15]-[c:16]1:[...
null
[]
null
null
null
null
The crude methyl 2-(2'-benzyloxyphenyl)-3-hydroxyacrylate was dissolved in dry DMF (100 ml) and potassium carbonate (29.0 g) was added in one portion. Dimethyl sulphate (16.00 g) in dry DMF (10 ml) was then added dropwise with stirring. After ninety minutes, water (300 ml) was added and the solution was extracted with ...
10.6084/m9.figshare.5104873.v1
null
Enol
Ester.Ether.Ether
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
CN(C)C=O
null
null
COC(=O)C(=CO)c1ccccc1OCc1ccccc1.COS(=O)(=O)OC.O.O=C([O-])[O-]>CN(C)C=O>CO/C=C(/C(=O)OC)c1ccccc1OCc1ccccc1.COC(=O)Cc1ccccc1OCc1ccccc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-abcb076a0ce4404db4518ad1d1b0ccf4
CCCCC#CCCO>>C#CCCCCCCO
NCCCN.C(CC#CCCCC)O>>C(CCCCCC#C)O
[C:1]([CH2:2][CH2:3][CH2:4][CH3:5])#[C:6][CH2:7][CH2:8][OH:9]>>[CH:1]#[C:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][OH:9]
CCCCC#CCCO
C#CCCCCCCO
null
null
CCCCCC
Functional Group Interconversion
OtherReaction
717941f395a910361dbd079f0406c8739db3d600df9659ab84f995c3dd1e77a5
f5163dfbf670ee9f38d1be788eef0e0a983df5868f48fe01d48741d6a3f98157
null
[C:1]-[C:2]-[C;H0;D2;+0:3]#[C;H0;D2;+0:4]-[CH2;D2;+0:5]-[C:6]-[C:7]-[CH3;D1;+0:8]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[CH2;D2;+0:8]-[C:7]-[C:6]-[C;H0;D2;+0:5]#[CH;D1;+0:4]
null
[]
null
null
null
null
35% KH in mineral oil (27 g, 240 mmol) under an argon atmosphere was washed with hexane and treated dropwise with 1,3-diaminopropane. The mixture was stirred at room temperature until it became homogeneous. The flask was cooled to 0∞C. and 3-octyn-1-ol (10 g, 79 mmol, Lancaster Synthesis) was slowly added. The reaction...
10.6084/m9.figshare.5104873.v1
null
Alkyne
Alkyne
null
null
null
null
CCCCCC
null
null
CCCCC#CCCO>CCCCCC>C#CCCCCCCO
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-012466477a7d413f8af56362a0621f75
CCCCC#CCCO>>C#CCCCCCCO
C(CC#CCCCC)O.[H-].[K+].NCCCN>>C(CCCCCC#C)O
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]#[C:6][CH2:7][CH2:8][OH:9]>>[CH:1]#[C:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][OH:9]
CCCCC#CCCO
C#CCCCCCCO
null
null
CCCCCC
Miscellaneous
OtherReaction
1dc82b94ad0bb9c37129929afef1fa70f760dcdf2017a728c72d09b3d0dbf429
7b33466a2cc81bfe95f125510ec1a59cf92dd3caaf14f1a960631fc63bb0a68b
null
[C:1]-[C:2]-[C;H0;D2;+0:3]#[C;H0;D2;+0:4]-[C:5]-[C:6]-[CH2;D2;+0:7]-[CH3;D1;+0:8]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[C:5]-[C:6]-[C;H0;D2;+0:7]#[CH;D1;+0:8]
null
[]
null
null
null
null
Potassium hydride, (35%) in mineral oil (27 g, 240 mmol) under an argon atmosphere was washed with hexane and treated dropwise with 1,3-diaminopropane. The mixture was stirred at room temperature until it became homogeneous. The flask was cooled to 0° C. and 3-octyn-1-ol (10 g, 79 mmol, Lancaster Synthesis) was slowly ...
10.6084/m9.figshare.5104873.v1
null
Alkyne
Alkyne
null
null
null
null
CCCCCC
null
null
CCCCC#CCCO>CCCCCC>C#CCCCCCCO
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e5a9b22eb8bd40e6869c9b589c0e99c1
COc1ccc(CCCCCCCCO)cc1.II>>COc1ccc(CCCCCCCCI)cc1
N1C=NC=C1.COC1=CC=C(C=C1)CCCCCCCCO.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.N1C=NC=C1.II>>ICCCCCCCCC1=CC=C(C=C1)OC
O[CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:17][cH:16]1.I[I:15]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][I:15])[cH:16][cH:17]1
COc1ccc(CCCCCCCCO)cc1.II
COc1ccc(CCCCCCCCI)cc1
null
null
C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
bb752b9027dc4488ba075e5955118a819f80cabd751a7497b67c2eeb1db6b071
cbf41c7cf9fe6b47a243b1674d74ed5bf46a151f7f3a71d206e23176e158facf
c1ccccc1
I-[I;H0;D1;+0:1].O-[CH2;D2;+0:2]-[C:3]-[C:4]>>[C:4]-[C:3]-[CH2;D2;+0:2]-[I;H0;D1;+0:1]
null
[]
65
CELSIUS
null
null
To a stirred solution of 8-(4-methoxyphenyl)octan-1-ol (12.3 g, 52 mmol) in dry toluene (200 mL) under an argon atmosphere was added triphenylphosphine (17.8 g, 67.6 mmol) and imidazole (10.6 g, 156 mmol). After the imidazole had dissolved, I2 (17.1 g, 67.6 mmol) was added. The reaction was then heated at 65° C. for 30...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Primary halide
null
null
c1ccccc1
HI
C1(=CC=CC=C1)C
65
null
COc1ccc(CCCCCCCCO)cc1.II>C1(=CC=CC=C1)C>COc1ccc(CCCCCCCCI)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-bb0e1e7df8314c9ba14cdb118f699551
CCCCCCCCCCCCOc1ccc(C)nc1/C=C/CC(=O)O.O=C(OO)c1cccc(Cl)c1>>CCCCCCCCCCCCOc1ccc(C)[n+]([O-])c1/C=C/CC(=O)O
C(=O)(O)C/C=C/C1=NC(=CC=C1OCCCCCCCCCCCC)C.ClC=1C=C(C(=O)OO)C=CC1.C(=O)(O)[O-].[Na+]>>C(=O)(O)C/C=C/C1=[N+](C(=CC=C1OCCCCCCCCCCCC)C)[O-]
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:15][cH:16][c:17]([CH3:18])[n:19][c:21]1/[CH:22]=[CH:23]/[CH2:24][C:25](=[O:26])[OH:27].O=C(O[OH:20])c1cccc(Cl)c1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][c:14]1[c...
CCCCCCCCCCCCOc1ccc(C)nc1/C=C/CC(=O)O.O=C(OO)c1cccc(Cl)c1
CCCCCCCCCCCCOc1ccc(C)[n+]([O-])c1/C=C/CC(=O)O
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
5b2b5a1eb88c9671c4a604b6f76054cc01cd86a1985fc147f7e56f19c4844d35
98b338a9d01476c0929fd5672e7509121bfe69600fd72e4d1cc6f1782e2d05d9
c1cc[nH+]cc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C;D1;H3:2]-[c:3](:[c:4]):[n;H0;D2;+0:5]:[c:6](/[C:7]=[C:8]/[C:9]-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]):[c:13]>>[C;D1;H3:2]-[c:3](:[c:4]):[n+;H0;D3:5](-[O-;H0;D1:1]):[c:6](/[C:7]=[C:8]/[C:9]-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]):[c:13]
null
[]
null
null
30
MINUTE
2-(E-2-Carboxymethylethenyl)-3-dodecyloxy-6-methylpyridine (2.15 g, 5.95 mmol) was dissolved in dry CH2Cl2 (20 mL) and cooled to 0∞C.; 85% m-chloroperoxybenzoic acid (1.45 g, 7.14 mmol) was added and the reaction was stirred at 0∞C. for 30 minutes and at room temperature for 16 hours. The reaction solution was poured i...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide
null
c1ccncc1.c1ccccc1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
HCl
C(Cl)Cl
null
0.5
CCCCCCCCCCCCOc1ccc(C)nc1/C=C/CC(=O)O.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>CCCCCCCCCCCCOc1ccc(C)[n+]([O-])c1/C=C/CC(=O)O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-56b9447d44f64098b2f16a6ad9eaa5d8
CCCCCCCCCCCCOc1ccc(CO)nc1/C=C/CC(=O)O.O=S(Cl)Cl>>CCCCCCCCCCCCOc1ccc(CCl)nc1/C=C/CC(=O)O.Cl
C(=O)(O)C/C=C/C1=NC(=CC=C1OCCCCCCCCCCCC)CO.S(=O)(Cl)Cl>>Cl.C(=O)(O)C/C=C/C1=NC(=CC=C1OCCCCCCCCCCCC)CCl
O[CH2:18][c:17]1[cH:16][cH:15][c:14]([O:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[c:21](/[CH:22]=[CH:23]/[CH2:24][C:25](=[O:26])[OH:27])[n:20]1.O=S([Cl:19])[Cl:28]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:1...
CCCCCCCCCCCCOc1ccc(CO)nc1/C=C/CC(=O)O.O=S(Cl)Cl
CCCCCCCCCCCCOc1ccc(CCl)nc1/C=C/CC(=O)O.Cl
null
null
C1(=CC=CC=C1)C
Functional Group Interconversion
Alcohol to chloride_SOCl2
bb752b9027dc4488ba075e5955118a819f80cabd751a7497b67c2eeb1db6b071
cbf41c7cf9fe6b47a243b1674d74ed5bf46a151f7f3a71d206e23176e158facf
c1ccncc1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5]/[C:6]=[C:7].O=S(-[Cl;H0;D1;+0:8])-[Cl;H0;D1;+0:9]>>[C:7]=[C:6]/[c:5]:[#7;a:4]:[c:2](-[CH2;D2;+0:1]-[Cl;H0;D1;+0:8]):[c:3].[ClH;D0;+0:9]
null
[]
null
null
1
HOUR
2-(E-2-Carboxymethylethenyl)-3-dodecyloxy-6-(hydroxymethyl)pyridine (250 mg, 0.662 mmol) was dissolved in dry toluene (10 mL) under an argon atmosphere and cooled to 0∞C. Thionyl chloride (0.50 mL, 6.85 mmol) was slowly added and the solution was stirred at 0∞C. for 30 minutes followed by 1 h at room temperature. The s...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Primary halide
null
null
c1ccncc1
Other
C1(=CC=CC=C1)C
null
1
CCCCCCCCCCCCOc1ccc(CO)nc1/C=C/CC(=O)O.O=S(Cl)Cl>C1(=CC=CC=C1)C>CCCCCCCCCCCCOc1ccc(CCl)nc1/C=C/CC(=O)O.Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6d5c70c0bd0043a78a39a3c35601adba
CCCCC#CCCO>>C#CCCCCCCO
NCCCN.C(CC#CCCCC)O>>C(CCCCCC#C)O
[C:1]([CH2:2][CH2:3][CH2:4][CH3:5])#[C:6][CH2:7][CH2:8][OH:9]>>[CH:1]#[C:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][OH:9]
CCCCC#CCCO
C#CCCCCCCO
null
null
CCCCCC
Functional Group Interconversion
OtherReaction
717941f395a910361dbd079f0406c8739db3d600df9659ab84f995c3dd1e77a5
f5163dfbf670ee9f38d1be788eef0e0a983df5868f48fe01d48741d6a3f98157
null
[C:1]-[C:2]-[C;H0;D2;+0:3]#[C;H0;D2;+0:4]-[CH2;D2;+0:5]-[C:6]-[C:7]-[CH3;D1;+0:8]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[CH2;D2;+0:8]-[C:7]-[C:6]-[C;H0;D2;+0:5]#[CH;D1;+0:4]
null
[]
null
null
null
null
35% KH in mineral oil (27 g, 240 mmol) under an argon atmosphere was washed with hexane and treated dropwise with 1,3-diaminopropane. The mixture was stirred at room temperature until it became homogeneous. The flask was cooled to 0° C. and 3-octyn-1-ol (10 g, 79 mmol, Lancaster Synthesis) was slowly added. The reactio...
10.6084/m9.figshare.5104873.v1
null
Alkyne
Alkyne
null
null
null
null
CCCCCC
null
null
CCCCC#CCCO>CCCCCC>C#CCCCCCCO
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5247f69c87d84750ba3f98831c15b7fa
COc1ccc(CCCCCCCCOc2ccc(C)nc2/C=C/CC(=O)O)cc1.O=C(OO)c1cccc(Cl)c1>>COc1ccc(CCCCCCCCOc2ccc(C)[n+]([O-])c2/C=C/CC(=O)O)cc1
C(=O)(O)C/C=C/C1=NC(=CC=C1OCCCCCCCCC1=CC=C(C=C1)OC)C.C1=CC(=CC(=C1)Cl)C(=O)OO>>C(=O)(O)C/C=C/C1=[N+](C(=CC=C1OCCCCCCCCC1=CC=C(C=C1)OC)C)[O-]
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][c:16]2[cH:17][cH:18][c:19]([CH3:20])[n:21][c:23]2/[CH:24]=[CH:25]/[CH2:26][C:27](=[O:28])[OH:29])[cH:30][cH:31]1.O=C(O[OH:22])c1cccc(Cl)c1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH...
COc1ccc(CCCCCCCCOc2ccc(C)nc2/C=C/CC(=O)O)cc1.O=C(OO)c1cccc(Cl)c1
COc1ccc(CCCCCCCCOc2ccc(C)[n+]([O-])c2/C=C/CC(=O)O)cc1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
5b2b5a1eb88c9671c4a604b6f76054cc01cd86a1985fc147f7e56f19c4844d35
98b338a9d01476c0929fd5672e7509121bfe69600fd72e4d1cc6f1782e2d05d9
c1ccc(CCCCCCCCOc2ccc[nH+]c2)cc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C;D1;H3:2]-[c:3](:[c:4]):[n;H0;D2;+0:5]:[c:6](/[C:7]=[C:8]/[C:9]-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]):[c:13]>>[C;D1;H3:2]-[c:3](:[c:4]):[n+;H0;D3:5](-[O-;H0;D1:1]):[c:6](/[C:7]=[C:8]/[C:9]-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]):[c:13]
null
[]
0
CELSIUS
15
HOUR
2-(E-2-Carboxymethylethenyl)-3-[8-(4-methoxyphenyl)octyloxy]-6-methylpyridine (17.1 g, 41.5 mmol) was dissolved in dry CH2Cl2 (105 mL) and cooled to 0° C.; 50% mCPBA (15.8 g, 45.8 mmol) was added in three portions over 10 minutes. The cooling bath was removed and the reaction was stirred for 15 hours at room temperatur...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide
null
c1ccncc1.c1ccccc1
C1=CC=[NH+]C=C1
c1ccccc1.C1=CC=[NH+]C=C1
HCl
C(Cl)Cl
0
15
COc1ccc(CCCCCCCCOc2ccc(C)nc2/C=C/CC(=O)O)cc1.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>COc1ccc(CCCCCCCCOc2ccc(C)[n+]([O-])c2/C=C/CC(=O)O)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-88aa2d2c0607465cb96b3991fe722e52
COc1ccc(CCCCCCCCOc2ccc(C)nc2/C=C/CC(=O)O)cc1.O=C(OO)c1cccc(Cl)c1>>COc1ccc(CCCCCCCCOc2ccc(C)[n+]([O-])c2/C=C/CC(=O)O)cc1
C(=O)(O)C/C=C/C1=NC(=CC=C1OCCCCCCCCC1=CC=C(C=C1)OC)C.ClC1=CC(=CC=C1)C(=O)OO>>C(=O)(O)C/C=C/C1=[N+](C(=CC=C1OCCCCCCCCC1=CC=C(C=C1)OC)C)[O-]
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][O:15][c:16]2[cH:17][cH:18][c:19]([CH3:20])[n:21][c:23]2/[CH:24]=[CH:25]/[CH2:26][C:27](=[O:28])[OH:29])[cH:30][cH:31]1.O=C(O[OH:22])c1cccc(Cl)c1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH...
COc1ccc(CCCCCCCCOc2ccc(C)nc2/C=C/CC(=O)O)cc1.O=C(OO)c1cccc(Cl)c1
COc1ccc(CCCCCCCCOc2ccc(C)[n+]([O-])c2/C=C/CC(=O)O)cc1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
5b2b5a1eb88c9671c4a604b6f76054cc01cd86a1985fc147f7e56f19c4844d35
98b338a9d01476c0929fd5672e7509121bfe69600fd72e4d1cc6f1782e2d05d9
c1ccc(CCCCCCCCOc2ccc[nH+]c2)cc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C;D1;H3:2]-[c:3](:[c:4]):[n;H0;D2;+0:5]:[c:6](/[C:7]=[C:8]/[C:9]-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]):[c:13]>>[C;D1;H3:2]-[c:3](:[c:4]):[n+;H0;D3:5](-[O-;H0;D1:1]):[c:6](/[C:7]=[C:8]/[C:9]-[C:10](=[O;D1;H0:11])-[O;D1;H1:12]):[c:13]
null
[]
0
CELSIUS
15
HOUR
2-(E-2-Carboxymethyl-ethenyl)-3-[8-(4-methoxyphenyl)octyloxy]-6-methylpyridine (17.1 g, 41.5 mmol) was dissolved in dry CH2Cl2 (105 mL) and cooled to 0° C.; 50% m-chlorperbenzoic acid (15.8 g, 45.8 mmol) was added in three portions over 10 minutes. The cooling bath was removed and the reaction was stirred for 15 hours ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide
null
c1ccncc1.c1ccccc1
C1=CC=[NH+]C=C1
c1ccccc1.C1=CC=[NH+]C=C1
HCl
C(Cl)Cl
0
15
COc1ccc(CCCCCCCCOc2ccc(C)nc2/C=C/CC(=O)O)cc1.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>COc1ccc(CCCCCCCCOc2ccc(C)[n+]([O-])c2/C=C/CC(=O)O)cc1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-32928277e9554e8f846f58e8123833be
COC(=O)c1cccc(CBr)c1.NC(N)=S>>COC(=O)c1cccc(CS)c1
BrCC=1C=C(C(=O)OC)C=CC1.NC(=S)N>>SCC=1C=C(C(=O)OC)C=CC1
Br[CH2:10][c:9]1[cH:8][cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:12]1.NC(N)=[S:11]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([CH2:10][SH:11])[cH:12]1
COC(=O)c1cccc(CBr)c1.NC(N)=S
COC(=O)c1cccc(CS)c1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
874b82c2d4f05e98f462796ed8d7ef1e13fce4a8a588b04aa02ed1f40755b5a0
c5ac5fd8ad86e4dc1842d4270aab48696f24c3999504096b608528878069554b
c1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].N-C(-N)=[S;H0;D1;+0:5]>>[SH;D1;+0:5]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
2
DAY
To a solution of methyl 3-bromomethylbenzoate (6.9 g, 30 mmol; Lancaster) in dry acetone (10 mL) was added via dropwise addition a solution of thiourea (2.28 g, 30 mmol) in dry acetone (40 mL) at room temperature. After 15 minutes the precipitated thiouronium salt was collected by filtration; the solids were washed wit...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiourea
Aliphatic thiol
null
null
c1ccccc1
HBr
CC(=O)C
null
48
COC(=O)c1cccc(CBr)c1.NC(N)=S>CC(=O)C>COC(=O)c1cccc(CS)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-378418b0f968496da9d02d2ceabcfed2
BrC1CCCC1.COc1ccc(C=O)cc1O>>COc1ccc(C=O)cc1OC1CCCC1
C([O-])([O-])=O.[Cs+].[Cs+].OC=1C=C(C=O)C=CC1OC.C1(CCCC1)Br.C1(CCCC1)Br.C([O-])([O-])=O.[Cs+].[Cs+]>>C1(CCCC1)OC=1C=C(C=O)C=CC1OC
Br[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[cH:9][c:10]1[OH:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[cH:9][c:10]1[O:11][CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1
BrC1CCCC1.COc1ccc(C=O)cc1O
COc1ccc(C=O)cc1OC1CCCC1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
b21417a59456fdb6c9e74dab1ba6f82edc34a079e35c8c3647ac7fef47b6d270
cf768afb66ed5041aefdce1fa6d1e40995a1ab7c4b4a4ca47544fe49ee1e629f
c1ccc(OC2CCCC2)cc1
Br-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1.[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[c:8]:[c:7](-[O;H0;D2;+0:6]-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1):[c:9]
89.4
[{"value": 89.4, "product": "C1(CCCC1)OC=1C=C(C=O)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
Caesium carbonate (214 g, 0.66 mol) was added to a mixture of 3-hydroxy-4-methoxybenzaldehyde (100 g, 0.66 mol) and cyclopentyl bromide (98 g, 0.66 mol) in anhydrous DMF (50 ml). The reaction mixture was stirred at RT for 16 h then treated with a further portion of cyclopentyl bromide (98 g, 0.66 mol) and caesium carbo...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol
Ether
C1CCCC1
C1CCCC1
c1ccccc1.C1CCCC1
HBr
CN(C)C=O
null
16
BrC1CCCC1.COc1ccc(C=O)cc1O>CN(C)C=O>COc1ccc(C=O)cc1OC1CCCC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-89cc579f3b55493b927b4858bac1ec2f
BrOC1CCCC1.COc1ccc(CO)cc1O>>COc1ccc(CO)cc1OC1CCCC1
C([O-])([O-])=O.[Cs+].[Cs+].OC=1C=C(CO)C=CC1OC.[I-].[Na+].C1(CCCC1)OBr>>C1(CCCC1)OC=1C=C(CO)C=CC1OC
BrO[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][OH:8])[cH:9][c:10]1[OH:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][OH:8])[cH:9][c:10]1[O:11][CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1
BrOC1CCCC1.COc1ccc(CO)cc1O
COc1ccc(CO)cc1OC1CCCC1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1b0b141bf6b317fb3f4853d99c0e21f208620be70a498da9a42860eb95c70530
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
c1ccc(OC2CCCC2)cc1
Br-O-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1.[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[c:8]:[c:7](-[O;H0;D2;+0:6]-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1):[c:9]
35.8
[{"value": 35.8, "product": "C1(CCCC1)OC=1C=C(CO)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
From 3-hydroxy-4-methoxybenzyl alcohol (50 g, 0.324 mol), cyclopentyloxybromide (70 ml, 0.648 mol), caesium carbonate (72.83 g, 0.222 mol) and sodium iodide (5.63 g, 0.037 mol). Chromatography (SiO2 ; EtOAc-C6H14. 1:3) to yield the title compound (25.782 g). (Found C, 69.92; H, 8.18. C13H18O3 requires C, 70.25; H, 8.16...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
C1CCCC1
C1CCCC1
c1ccccc1.C1CCCC1
HBr
null
null
null
BrOC1CCCC1.COc1ccc(CO)cc1O>>COc1ccc(CO)cc1OC1CCCC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-0c5e70e577c94e38b27d7cec9a37378c
CI.Clc1cncc(Cl)c1>>Cc1c(Cl)cncc1Cl
ClC=1C=NC=C(C1)Cl.[Li+].CC(C)[N-]C(C)C.C(O)([O-])=O.[Na+].IC>>ClC=1C=NC=C(C1C)Cl
I[CH3:1].[cH:2]1[c:3]([Cl:4])[cH:5][n:6][cH:7][c:8]1[Cl:9]>>[CH3:1][c:2]1[c:3]([Cl:4])[cH:5][n:6][cH:7][c:8]1[Cl:9]
CI.Clc1cncc(Cl)c1
Cc1c(Cl)cncc1Cl
null
null
ClCCl.C1CCOC1
C-C Coupling
Methylation with MeI_aryl
d4dc1d398fcb789be26f861c3ffb23cfce3504c400401ddf0ee0bd40e14a762b
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
c1ccncc1
I-[CH3;D1;+0:1].[Cl;D1;H0:2]-[c:3]1:[c:4]:[#7;a:5]:[c:6]:[c:7](-[Cl;D1;H0:8]):[cH;D2;+0:9]:1>>[CH3;D1;+0:1]-[c;H0;D3;+0:9]1:[c:3](-[Cl;D1;H0:2]):[c:4]:[#7;a:5]:[c:6]:[c:7]:1-[Cl;D1;H0:8]
53
[{"value": 53.0, "product": "ClC=1C=NC=C(C1C)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
3,5-Dichloropyridine (2.04 g, 13.5 mmol) in THF (5 ml) was added dropwise to a solution of LDA [prepared from diisopropylamine (1.9 ml, 13.5 mmol) and n-butyllithium (1.6M, 8.4 ml, 13.5 mmol)] in THF (25 ml) at -70° C. After stirring at this temperature for 5 min, iodomethane (0.85 ml, 13.5 mmol) was added and the reac...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccncc1
c1ccncc1
c1ccncc1
HI
ClCCl.C1CCOC1
null
0.083333
CI.Clc1cncc(Cl)c1>ClCCl.C1CCOC1>Cc1c(Cl)cncc1Cl
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-4c51ec94fbde4e1a8f48e64a30ce3af0
CCCCCC.CCOC(C)=O.CCOC(C)=O.CO.Cc1ccncc1.[Li][CH2]CCC>>COc1ccc(C(O)Cc2ccncc2)cc1OC1CCCC1
CCOC(=O)C.CCCCCC.CCOC(=O)C.CO.CC1=CC=NC=C1.C(CCC)[Li]>>C1(CCCC1)OC=1C=C(C=CC1OC)C(CC1=CC=NC=C1)O
CCC[CH2:5]C[CH3:20].CC(=O)O[CH2:16][CH3:17].[CH2:3]([CH3:4])[O:18][C:7]([CH3:6])=[O:8].[CH3:1][OH:2].[CH3:9][c:10]1[cH:11][cH:12][n:13][cH:14][cH:15]1.[Li][CH2:21][CH2:22][CH2:23][CH3:19]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([OH:8])[CH2:9][c:10]2[cH:11][cH:12][n:13][cH:14][cH:15]2)[cH:16][c:17]1[O:18][CH:19]1[CH...
CCCCCC.CCOC(C)=O.CCOC(C)=O.CO.Cc1ccncc1.[Li][CH2]CCC
COc1ccc(C(O)Cc2ccncc2)cc1OC1CCCC1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
4d5b9d11b173cddc7c9965df48907cd64074ac172a04e8355236d47d1d33a538
eaed0ec2e18ddd7689918b523da6af01c4c12f36db516a28cad5374c79aa54fd
c1cc(CCc2ccncc2)cc(OC2CCCC2)c1
C-C(=O)-O-[CH2;D2;+0:1]-[CH3;D1;+0:2].C-C-C-[CH2;D2;+0:3]-C-[CH3;D1;+0:4].[C;D1;H3:5]-[OH;D1;+0:6].[CH3;D1;+0:7]-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:10](-[CH3;D1;+0:11])=[O;H0;D1;+0:12].[CH3;D1;+0:13]-[C:14]-[C:15]-[CH2;D2;+0:16]-[Li].[CH3;D1;+0:17]-[c:18]1:[c:19]:[c:20]:[#7;a:21]:[c:22]:[c:23]:1>>[C;D1;H3:5]-[O;H...
null
[]
null
null
null
null
From 4-methylpyridine (3.00 g, 32.1 mmol); n-butyllithium (32.1 mmol), and Intermediate 1 (6.82 g, 31.0 mmol). The crude product was subject to chromatography [SiO2 ; EtOAc-hexane, 3:2 (500 ml) to 4:1 (1000 ml) then EtOAc-methanol 9:1 (1500 ml)] to afford the title compound. (9.68 g) as fine white needles m.p. 97°-101°...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Methanol.Alkyl lithium
Ether.Ether.Secondary alcohol
null
c1ccccc1.C1CCCC1
c1ccccc1.c1ccncc1.C1CCCC1
HO-.Li
null
null
null
CCCCCC.CCOC(C)=O.CCOC(C)=O.CO.Cc1ccncc1.[Li][CH2]CCC>>COc1ccc(C(O)Cc2ccncc2)cc1OC1CCCC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-46541465def6464b8e0702bdac2c409a
COc1ccc(-c2ccccc2[P+](C)(c2ccccc2)c2ccccc2)cc1OC1CCCC1.O=Cc1ccncc1>>COc1ccc(/C=C\c2ccncc2)cc1OC1CCCC1
[O-]CC.[Na+].N1=CC=C(C=C1)C=O.[Cl-].C1(CCCC1)OC=1C=C(C=CC1OC)C1=C(C=CC=C1)[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C>>C1(CCCC1)OC=1C=C(C=CC1OC)\C=C/C1=CC=NC=C1
C[P+](c1ccccc1)(c1ccccc1)c1cccc[c:7]1-[c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:16]([O:17][CH:18]2[CH2:19][CH2:20][CH2:21][CH2:22]2)[cH:15]1.O=[CH:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[CH:8]\[c:9]2[cH:10][cH:11][n:12][cH:13][cH:14]2)[cH:15][c:16]1[O:17][CH:18]1[CH2:19][...
COc1ccc(-c2ccccc2[P+](C)(c2ccccc2)c2ccccc2)cc1OC1CCCC1.O=Cc1ccncc1
COc1ccc(/C=C\c2ccncc2)cc1OC1CCCC1
null
null
C(C)O
C-C Coupling
OtherReaction
cb5f277ac55a0e763ef643becc05f1522019cc4161daceb249ed2d634b78153b
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
C(=C\c1cccc(OC2CCCC2)c1)\c1ccncc1
C-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:[c;H0;D3;+0:1]:1-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].O=[CH;D2;+0:7]-[c:8]1:[c:9]:[c:10]:[#7;a:11]:[c:12]:[c:13]:1>>[c:4]:[c:3]:[c;H0;D3;+0:2](/[CH;D2;+0:1]=[CH;D2;+0:7]\[c:8]1:[c:9]:[c:10]:[#7;a:11]:[c:12]:[c:13]:1):[c:5]:[c:6]
11.9
[{"value": 11.9, "product": "C1(CCCC1)OC=1C=C(C=CC1OC)\\C=C/C1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of sodium ethoxide [prepared from sodium (0.10 g, 4.50 mmol)] in ethanol (50 ml) was added over 5 min to a stirred mixture of 4-pyridine carboxaldehyde (0.44 g, 4.10 mmol) and (3-cyclopentyloxy-4-methoxyphenyl)-methyltriphenylphosphonium chloride (2.00 g, 4.08 g) in ethanol (30 ml). After 2 h, the reaction m...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1.c1ccncc1.C1CCCC1
HO-
C(C)O
null
2
COc1ccc(-c2ccccc2[P+](C)(c2ccccc2)c2ccccc2)cc1OC1CCCC1.O=Cc1ccncc1>C(C)O>COc1ccc(/C=C\c2ccncc2)cc1OC1CCCC1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-95ef5c03630f4827baa473fbaab9413f
C=CC#N.CCOC(=O)CN>>CCOC(=O)CNCCC#N
Cl.C(C)OC(CN)=O.[OH-].[K+].C(C=C)#N>>C(C)OC(CNCCC#N)=O
[CH2:8]=[CH:9][C:10]#[N:11].[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH2:7]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH:7][CH2:8][CH2:9][C:10]#[N:11]
C=CC#N.CCOC(=O)CN
CCOC(=O)CNCCC#N
null
null
O
Heteroatom Alkylation and Arylation
aza-Michael addition primary
b45dd075b7e75caee6dc0a68cb402266c75e0848f7502f06a5dbd8a34863aae2
2e45960e6468a140db4162555f247a2535630c23e1aa16e082b84ce22691ebbf
null
[CH2;D1;+0:1]=[CH;D2;+0:2]-[C:3]#[N;D1;H0:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9]-[NH2;D1;+0:10]>>[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9]-[NH;D2;+0:10]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:3]#[N;D1;H0:4]
48
[{"value": 48.0, "product": "C(C)OC(CNCCC#N)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
139.6g (1 mole) of glycine ethyl ester hydrochloride was dissolved in 80 ml of distilled water and to this solution was added 230 ml of an aqueous solution of 67.3 g (1.2 mole eq.) of potassium hydroxide. Then, 106.2 g (2 mole eq.) of acrylonitrile was added to the reaction solution while heating and stirring at 50° to...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Vinyl
Secondary amine
null
null
null
null
O
null
null
C=CC#N.CCOC(=O)CN>O>CCOC(=O)CNCCC#N
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-9e63e16f353541c69b169a8401ad9d31
CC(C)(C)ON=C1CNCC1CN.O=C(O)c1cn(C2CC2)c2c(F)c(F)c(F)cc2c1=O>>CC(C)(C)ON=C1CN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)CC1CN
C1(CC1)N1C=C(C(C2=CC(=C(C(=C12)F)F)F)=O)C(=O)O.Cl.Cl.NCC1CNCC1=NOC(C)(C)C>>NCC1CN(CC1=NOC(C)(C)C)C1=C(C=C2C(C(=CN(C2=C1F)C1CC1)C(=O)O)=O)F
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][N:6]=[C:7]1[CH2:8][NH:9][CH2:29][CH:30]1[CH2:31][NH2:32].F[c:10]1[c:11]([F:12])[cH:13][c:14]2[c:15](=[O:16])[c:17]([C:18](=[O:19])[OH:20])[cH:21][n:22]([CH:23]3[CH2:24][CH2:25]3)[c:26]2[c:27]1[F:28]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][N:6]=[C:7]1[CH2:8][N:9]([c:10]2[c:11]([F:12])[cH...
CC(C)(C)ON=C1CNCC1CN.O=C(O)c1cn(C2CC2)c2c(F)c(F)c(F)cc2c1=O
CC(C)(C)ON=C1CN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)CC1CN
null
null
null
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation secondary amine
89f800d0b5c6eace023ec0f16ed65844f5dd409e156b3b4845e1db5de9a38872
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
N=C1CCN(c2ccc3c(=O)ccn(C4CC4)c3c2)C1
F-[c;H0;D3;+0:1]1:[c:2](-[F;D1;H0:3]):[c:4]:[c:5]:[c:6](:[#7;a:7](-[C:8]):[c:9]):[c:10]:1-[F;D1;H0:11].[#7:12]=[C:13]1-[C:14]-[C:15]-[NH;D2;+0:16]-[C:17]-1>>[#7:12]=[C:13]1-[C:14]-[C:15]-[N;H0;D3;+0:16](-[c;H0;D3;+0:1]2:[c:2](-[F;D1;H0:3]):[c:4]:[c:5]:[c:6](:[#7;a:7](-[C:8]):[c:9]):[c:10]:2-[F;D1;H0:11])-[C:17]-1
67.3
[{"value": 67.0, "product": "NCC1CN(CC1=NOC(C)(C)C)C1=C(C=C2C(C(=CN(C2=C1F)C1CC1)C(=O)O)=O)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.3, "product": "NCC1CN(CC1=NOC(C)(C)C)C1=C(C=C2C(C(=CN(C2=C1F)C1CC1)C(=O)O)=O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
141 mg (0.5 mmole) of 1-cyclopropyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and 143 mg (0.55 mmole) of 3-aminomethyl-4-t-butyloxyiminopyrrolidine dihydrochloride were refluxed for 2.5 hours under heating according to the same manner as Example 89 and cooled down to room temperature. Then, the resul...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
C1CCNC1.c1ccc2ncccc2c1
C1CC[NH]C1.c1ccc2ncccc2c1
C1CC[NH]C1.c1ccc2ncccc2c1.C1CC1
HF
null
null
null
CC(C)(C)ON=C1CNCC1CN.O=C(O)c1cn(C2CC2)c2c(F)c(F)c(F)cc2c1=O>>CC(C)(C)ON=C1CN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)CC1CN
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1eee3fd255824bfab45a5acac194afe1
CC(C)(C)ON=C1CNCC1CN.O=C(O)c1cn(-c2ccc(F)cc2F)c2nc(F)c(F)cc2c1=O>>CC(C)(C)ON=C1CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3-c2ccc(F)cc2F)CC1CN
FC=1C=C2C(C(=CN(C2=NC1F)C1=C(C=C(C=C1)F)F)C(=O)O)=O.Cl.Cl.NCC1CNCC1=NOC(C)(C)C.N12CCCCCC2=NCCC1>>NCC1CN(CC1=NOC(C)(C)C)C1=C(C=C2C(C(=CN(C2=N1)C1=C(C=C(C=C1)F)F)C(=O)O)=O)F
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][N:6]=[C:7]1[CH2:8][NH:9][CH2:33][CH:34]1[CH2:35][NH2:36].F[c:10]1[n:11][c:12]2[c:13]([cH:14][c:15]1[F:16])[c:17](=[O:18])[c:19]([C:20](=[O:21])[OH:22])[cH:23][n:24]2-[c:25]1[cH:26][cH:27][c:28]([F:29])[cH:30][c:31]1[F:32]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][N:6]=[C:7]1[CH2:8][N:9]([...
CC(C)(C)ON=C1CNCC1CN.O=C(O)c1cn(-c2ccc(F)cc2F)c2nc(F)c(F)cc2c1=O
CC(C)(C)ON=C1CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3-c2ccc(F)cc2F)CC1CN
null
null
C(C)#N
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation secondary amine
8e57f376730c9014acd2fa503b42327b9db31ded66ca38cadcf6d11720f7e268
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
N=C1CCN(c2ccc3c(=O)ccn(-c4ccccc4)c3n2)C1
F-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]:[#7;a:4]):[c:5](-[F;D1;H0:6]):[c:7].[#7:8]=[C:9]1-[C:10]-[C:11]-[NH;D2;+0:12]-[C:13]-1>>[#7:8]=[C:9]1-[C:10]-[C:11]-[N;H0;D3;+0:12](-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]:[#7;a:4]):[c:5](-[F;D1;H0:6]):[c:7])-[C:13]-1
81
[{"value": 81.0, "product": "NCC1CN(CC1=NOC(C)(C)C)C1=C(C=C2C(C(=CN(C2=N1)C1=C(C=C(C=C1)F)F)C(=O)O)=O)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.6, "product": "NCC1CN(CC1=NOC(C)(C)C)C1=C(C=C2C(C(=CN(C2=N1)C1=C(C=C(C=C1)F)F)C(=O)O)=O)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
168 mg (0.5 mmole) of 6,7-difluoro-1-(2,4-difluorophenyl)-4-oxo-1,4-dihydro-naphthyridine-3-carboxylic acid and 143 mg (0.55 mmole) of 3-aminomethyl-4-t-butyloxyiminopyrrolidine dihydrochloride were suspended in 3 ml of dry acetonitrile. Then, 230 mg (1.5 mmole) of 1,8-diazabicyclo[5.4.0]undec-7-ene was added thereto, ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
C1CCNC1.c1cnc2ncccc2c1
C1CC[NH]C1.c1cnc2ncccc2c1
C1CC[NH]C1.c1cnc2ncccc2c1.c1ccccc1
HF
C(C)#N
null
0.25
CC(C)(C)ON=C1CNCC1CN.O=C(O)c1cn(-c2ccc(F)cc2F)c2nc(F)c(F)cc2c1=O>C(C)#N>CC(C)(C)ON=C1CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3-c2ccc(F)cc2F)CC1CN
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ab5a462bd8504edf8a49db2e10bfe37a
CC(=O)OC1C=CC(=O)N2CC(OC(C)=O)C(OC(C)=O)C12>>CC(=O)O[C@H]1[C@H]2[C@H](OC(C)=O)CCC(O)N2C[C@H]1OC(C)=O
CC(=O)OC1CN2C(C1OC(=O)C)C(C=CC2=O)OC(=O)C.[H][H]>>CC(=O)O[C@@H]1CCC(N2[C@H]1[C@@H]([C@@H](C2)OC(=O)C)OC(=O)C)O
[CH3:1][C:2](=[O:3])[O:4][CH:5]1[CH:6]2[CH:7]([O:8][C:9]([CH3:10])=[O:11])[CH:12]=[CH:13][C:14](=[O:15])[N:16]2[CH2:17][CH:18]1[O:19][C:20]([CH3:21])=[O:22]>>[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[C@H:6]2[C@H:7]([O:8][C:9]([CH3:10])=[O:11])[CH2:12][CH2:13][CH:14]([OH:15])[N:16]2[CH2:17][C@H:18]1[O:19][C:20]([CH3:21])=[O:22]
CC(=O)OC1C=CC(=O)N2CC(OC(C)=O)C(OC(C)=O)C12
CC(=O)O[C@H]1[C@H]2[C@H](OC(C)=O)CCC(O)N2C[C@H]1OC(C)=O
null
null
C(C)O
Reduction
OtherReaction
fd7d2ac66486e4134b1977aca077072436e99a7c66f4ea7b4894a8b071b7b77a
a482d04f40c78ee77b2bb7ee1ddd81c55502fc86accd776e8e7cf5fc57b56aa1
C1CCN2CCC[C@H]2C1
[C:1]-[#7:2]1-[C:3](-[C:4])-[CH;D3;+0:5](-[#8:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9])-[CH;D2;+0:10]=[CH;D2;+0:11]-[C;H0;D3;+0:12]-1=[O;H0;D1;+0:13]>>[C:1]-[#7:2]1-[C:3](-[C:4])-[C@H;D3;+0:5](-[#8:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9])-[CH2;D2;+0:10]-[CH2;D2;+0:11]-[CH;D3;+0:12]-1-[OH;D1;+0:13]
null
[]
null
null
8
HOUR
(1S,2R,8R,8aR)-1,2,8-triacetoxy-1,2,3,5,8,8a-hexahydro-5-oxyindolizine, 13, 22 g (0.070 mole), was hydrogenated at atmospheric pressure of hydrogen in 400 mL ethanol containing 3 g 10% Pd on carbon. The reaction was allowed to proceed overnight. The catalyst was filtered, and the filtrate was evaporated to dryness. The...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Secondary alcohol
C1=CCN2CCCC2C1
C1CCN2CCC[C@H]2C1
C1CCN2CCC[C@H]2C1
null
C(C)O
null
8
CC(=O)OC1C=CC(=O)N2CC(OC(C)=O)C(OC(C)=O)C12>C(C)O>CC(=O)O[C@H]1[C@H]2[C@H](OC(C)=O)CCC(O)N2C[C@H]1OC(C)=O
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e7bfc3a61b0e49e0b569fa6da8eab9c5
CCOP(=O)(CC(=O)N[C@]1(OCc2ccccc2)O[C@H](C)[C@@H](OC(C)=O)C[C@@H]1OC(C)=O)OCC>>CCOP(=O)(CC(=O)NC1(O)O[C@H](C)[C@@H](OC(C)=O)C[C@@H]1OC(C)=O)OCC
C(C)(=O)O[C@@H]1[C@@](OCC2=CC=CC=C2)(O[C@@H]([C@H](C1)OC(C)=O)C)NC(CP(=O)(OCC)OCC)=O.C(C)O>>C(C)(=O)O[C@@H]1C(O)(O[C@@H]([C@H](C1)OC(C)=O)C)NC(CP(=O)(OCC)OCC)=O
c1ccc(C[O:11][C@@:10]2([NH:9][C:7]([CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:26][CH2:27][CH3:28])=[O:8])[O:12][C@H:13]([CH3:14])[C@@H:15]([O:16][C:17]([CH3:18])=[O:19])[CH2:20][C@@H:21]2[O:22][C:23]([CH3:24])=[O:25])cc1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][C:7](=[O:8])[NH:9][C:10]1([OH:11])[O:12][C@H:13]([CH3:14...
CCOP(=O)(CC(=O)N[C@]1(OCc2ccccc2)O[C@H](C)[C@@H](OC(C)=O)C[C@@H]1OC(C)=O)OCC
CCOP(=O)(CC(=O)NC1(O)O[C@H](C)[C@@H](OC(C)=O)C[C@@H]1OC(C)=O)OCC
null
[Pd]
C(=O)O
Deprotection
Hydroxyl benzyl deprotection
3519c572d4cdc6e4492ddc62371f633ac7f142ee47bb7da6e4a9f9b5cd5ff2d0
3e1943ba4c0a89acd871c6a988bf0e8edc398f81f37331b79618b2411f80cd6d
C1CCOCC1
[C:1]-[#8:2]-[C@;H0;D4;+0:3](-[#7:4]-[C:5](-[C:6])=[O;D1;H0:7])(-[O;H0;D2;+0:8]-C-c1:c:c:c:c:c:1)-[C:9](-[#8:10]-[C:11](-[C;D1;H3:12])=[O;D1;H0:13])-[C:14]>>[C:1]-[#8:2]-[C;H0;D4;+0:3](-[OH;D1;+0:8])(-[#7:4]-[C:5](-[C:6])=[O;D1;H0:7])-[C:9](-[#8:10]-[C:11](-[C;D1;H3:12])=[O;D1;H0:13])-[C:14]
null
[]
null
null
null
null
Crude benzyl 2,4-di-O-acetyl-3,6-dideoxydiethylphosphonoacetamido-alpha-D-mannopyranoside, 21, ethanol (10 ml), 2 88% formic acid and 0.1 g Pd black were heated at reflux overnight under argon with stirring. The reaction mixture was filtered and evaporated to dryness, and the residue was chromatographed on SiO2 (40 g; ...
10.6084/m9.figshare.5104873.v1
null
Ether
Tertiary alcohol
c1ccccc1
null
C1CCOCC1
Other
[Pd].C(=O)O
null
null
CCOP(=O)(CC(=O)N[C@]1(OCc2ccccc2)O[C@H](C)[C@@H](OC(C)=O)C[C@@H]1OC(C)=O)OCC>[Pd].C(=O)O>CCOP(=O)(CC(=O)NC1(O)O[C@H](C)[C@@H](OC(C)=O)C[C@@H]1OC(C)=O)OCC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1c6e0a0c6762481f8f0b8e21fe0e5b9e
COC(=O)CCC[N+](=O)[O-].O=Cc1ccccc1.[NH4+]>>O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1
[N+](=O)([O-])CCCC(=O)OC.C(C1=CC=CC=C1)=O.C(C)(=O)[O-].[NH4+]>>[N+](=O)([O-])[C@H]1[C@@H](NC(CC1)=O)C1=CC=CC=C1
CO[C:2](=[O:1])[CH2:3][CH2:4][CH2:5][N+:6](=[O:7])[O-:8].O=[CH:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[NH4+:16]>>[O:1]=[C:2]1[CH2:3][CH2:4][C@@H:5]([N+:6](=[O:7])[O-:8])[C@H:9]([c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[NH:16]1
COC(=O)CCC[N+](=O)[O-].O=Cc1ccccc1.[NH4+]
O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1
null
null
C(C)O
Acylation
OtherReaction
9402e7d2d4a11355b869c0e5053e69e7a49790dcc5ec49c913047b2193486448
62e08fd83e95abe9caffb690356f76bd7ee08d6cde6d54358808c23fd2777059
O=C1CCC[C@H](c2ccccc2)N1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[CH2;D2;+0:5]-[#7;+:6](-[O;-;D1;H0:7])=[O;D1;H0:8].O=[CH;D2;+0:9]-[c:10](:[c:11]):[c:12].[NH4+;D0:13]>>[O;-;D1;H0:7]-[#7;+:6](=[O;D1;H0:8])-[C@@H;D3;+0:5]1-[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:13]-[C@H;D3;+0:9]-1-[c:10](:[c:11]):[c:12]
85
[{"value": 85.0, "product": "[N+](=O)([O-])[C@H]1[C@@H](NC(CC1)=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.7, "product": "[N+](=O)([O-])[C@H]1[C@@H](NC(CC1)=O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Methyl 4-nitrobutyrate (1) (240 g, 1.63 mol), benzaldehyde (189 g, 1.78 mol), ammonium acetate (164 g, 2.12 mol) and ethanol (1680 ml) were placed in a 3-liter 3-necked flask equipped with a mechanical stirrer, under an atmosphere of nitrogen. The mixture was heated under reflux for four hours to yield an orange soluti...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Nitro group
Nitro group.Secondary amide
null
C1CCNCC1
C1CCNCC1.c1ccccc1
HO-
C(C)O
null
null
COC(=O)CCC[N+](=O)[O-].O=Cc1ccccc1.[NH4+]>C(C)O>O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-00e070c838c440f296400559ff44fce7
O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1>>O=C1CCC(=O)C(c2ccccc2)N1
CSC.[N+](=O)([O-])[C@H]1[C@@H](NC(CC1)=O)C1=CC=CC=C1.ClCCl.CC(C)([O-])C.[K+]>>O=C1NC(C(CC1)=O)C1=CC=CC=C1
[O-][N+]([C@@H:5]1[CH2:4][CH2:3][C:2](=[O:1])[NH:14][C@H:7]1[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)=[O:6]>>[O:1]=[C:2]1[CH2:3][CH2:4][C:5](=[O:6])[CH:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[NH:14]1
O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1
O=C1CCC(=O)C(c2ccccc2)N1
null
null
CO
Functional Group Interconversion
Nef reaction (nitro to ketone)
58f95b2144f0a380427d8f8bfa00aef5a7a50ae0b82878d96b22dc91477827d9
1df445eca91b47d301fc1478044e1cd6fb16a038e33213021748ecbc6ef69082
O=C1CCC(=O)C(c2ccccc2)N1
[O-]-[N+](=[O;H0;D1;+0:1])-[C@@H;D3;+0:2]1-[C:3]-[C:4]-[C:5](=[O;D1;H0:6])-[#7:7]-[C@H;D3;+0:8]-1-[c:9](:[c:10]):[c:11]>>[O;D1;H0:6]=[C:5]1-[#7:7]-[CH;D3;+0:8](-[c:9](:[c:10]):[c:11])-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[C:3]-[C:4]-1
78.4
[{"value": 78.0, "product": "O=C1NC(C(CC1)=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.4, "product": "O=C1NC(C(CC1)=O)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
15
MINUTE
trans-3 -Nitro-6-oxo-2-phenylpiperidine (80 g, 0.364 mol) was suspended in methanol:dichloromethane (Example 1a, 1:1, 500 ml) under nitrogen. The suspension was cooled to 0° C. and potassium t-butoxide (44.8 g, 0.4 mol) was added in portions over 30 mins. The cooling bath was then removed and the solution stirred for a...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Ketone
C1CCNCC1
C1CCNCC1
C1CCNCC1.c1ccccc1
HO-
CO
0
0.25
O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1>CO>O=C1CCC(=O)C(c2ccccc2)N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5f52b1beaf2f4650a80696f1a265442e
O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1>>O=C1CCC(=O)C(c2ccccc2)N1
[N+](=O)([O-])[C@H]1[C@@H](NC(CC1)=O)C1=CC=CC=C1.C[O-].[Na+].C(C)(=O)[O-].[NH4+].Cl>>O=C1NC(C(CC1)=O)C1=CC=CC=C1
[O-][N+]([C@@H:5]1[CH2:4][CH2:3][C:2](=[O:1])[NH:14][C@H:7]1[c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)=[O:6]>>[O:1]=[C:2]1[CH2:3][CH2:4][C:5](=[O:6])[CH:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[NH:14]1
O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1
O=C1CCC(=O)C(c2ccccc2)N1
null
[Cl-].[Cl-].[Cl-].[Ti+3]
O.CO
Functional Group Interconversion
Nef reaction (nitro to ketone)
58f95b2144f0a380427d8f8bfa00aef5a7a50ae0b82878d96b22dc91477827d9
1df445eca91b47d301fc1478044e1cd6fb16a038e33213021748ecbc6ef69082
O=C1CCC(=O)C(c2ccccc2)N1
[O-]-[N+](=[O;H0;D1;+0:1])-[C@@H;D3;+0:2]1-[C:3]-[C:4]-[C:5](=[O;D1;H0:6])-[#7:7]-[C@H;D3;+0:8]-1-[c:9](:[c:10]):[c:11]>>[O;D1;H0:6]=[C:5]1-[#7:7]-[CH;D3;+0:8](-[c:9](:[c:10]):[c:11])-[C;H0;D3;+0:2](=[O;H0;D1;+0:1])-[C:3]-[C:4]-1
75
[{"value": 75.0, "product": "O=C1NC(C(CC1)=O)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
1
HOUR
To a 5L flask containing ammonium acetate (450g) which had been thoroughly purged with nitrogen was added a freshly prepared solution of titanium trichloride (300 g, 1.95 mol) in deoxygenated water (2.1L) with ice-bath cooling. To the resulting green solution was added a solution of trans-3-nitro-6-oxo-2-phenylpiperidi...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Ketone
C1CCNCC1
C1CCNCC1
C1CCNCC1.c1ccccc1
HO-
[Cl-].[Cl-].[Cl-].[Ti+3].O.CO
0
1
O=C1CC[C@@H]([N+](=O)[O-])[C@H](c2ccccc2)N1>[Cl-].[Cl-].[Cl-].[Ti+3].O.CO>O=C1CCC(=O)C(c2ccccc2)N1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-a53056ad25d944aab213571494808620
BrP(Br)Br.CC(O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1>>CC(Br)c1cc(C(F)(F)F)cc(C(F)(F)F)c1
FC(C=1C=C(C=C(C1)C(F)(F)F)C(C)O)(F)F.P(Br)(Br)Br>>FC(C=1C=C(C=C(C1)C(F)(F)F)C(C)Br)(F)F
BrP(Br)[Br:3].O[CH:2]([CH3:1])[c:4]1[cH:5][c:6]([C:7]([F:8])([F:9])[F:10])[cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1>>[CH3:1][CH:2]([Br:3])[c:4]1[cH:5][c:6]([C:7]([F:8])([F:9])[F:10])[cH:11][c:12]([C:13]([F:14])([F:15])[F:16])[cH:17]1
BrP(Br)Br.CC(O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1
CC(Br)c1cc(C(F)(F)F)cc(C(F)(F)F)c1
null
null
O
Functional Group Interconversion
OtherReaction
ed0947fcf0a870fa4568d74e29e264525d0acf781c20c116470537e8cf1d911a
495868b18ac37eabad313a8861412e57f019fb3569a2b2e50afa3ee29413ec02
c1ccccc1
Br-P(-Br)-[Br;H0;D1;+0:1].O-[CH;D3;+0:2](-[C;D1;H3:3])-[c:4](:[c:5]):[c:6]>>[Br;H0;D1;+0:1]-[CH;D3;+0:2](-[C;D1;H3:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
30
MINUTE
To 1-(3,5-bis(trifiuoromethyl)phenyl)-1-hydroxyethane (10 g) was added phosphorous tribromide (3.7 ml) to give a clear solution. After 30 minutes the solution was added to water (300 ml) and the solution stirred for a further 30 minutes. Petroleum ether bp=60°-80° C. was added and the organic solution washed with water...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Secondary halide
null
null
c1ccccc1
HBr
O
null
0.5
BrP(Br)Br.CC(O)c1cc(C(F)(F)F)cc(C(F)(F)F)c1>O>CC(Br)c1cc(C(F)(F)F)cc(C(F)(F)F)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-6c6600010a194ad1a86936c8f6fa6879
CC(C)(C)OC(=O)Cl.CC(C)(C)OC(=O)OC(C)(C)C>>CC(C)(C)OC(=O)OC(=O)OC(C)(C)C
Cl[C].CCOCC.C(C)(C)(C)OC(OC(C)(C)C)=O.C(C)(C)(C)OC(=O)Cl.N1=C(C=CC=C1C)C>>C(C)(C)(C)OC(=O)OC(=O)OC(C)(C)C
Cl[C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7].CC(C)(C)[O:8][C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[O:8][C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15]
CC(C)(C)OC(=O)Cl.CC(C)(C)OC(=O)OC(C)(C)C
CC(C)(C)OC(=O)OC(=O)OC(C)(C)C
null
null
ClCCl.C(C)N(CC)CC.N1=CC=CC=C1
Protection
OtherReaction
0f666e2e9239bc3e2b469a8e6062825157731d14d98b0ae40fe57e890a7f8e37
3d5405115c494df9df63719b7f19d67772b344737e1bdbee4bdc791922d38baa
null
C-C(-C)(-C)-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].Cl-[C;H0;D3;+0:9](=[O;D1;H0:10])-[#8:11]-[C:12](-[C;D1;H3:13])(-[C;D1;H3:14])-[C;D1;H3:15]>>[C;D1;H3:6]-[C:5](-[C;D1;H3:7])(-[C;D1;H3:8])-[#8:4]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:1]-[C;H0;D3;+0:9](=[O;D1;H0:10])-[#8:11]-[C...
null
[]
null
null
null
null
The 3-(N-t-butyloxycarbonyl-1'-N-methylaminoethyl)pyrrolidines (60, 61, 62, 63) were prepared by reacting the amines (8-11) with a t-butyloxycarbonyl transfer agent such as di-t-butylcarbonate or t-butyloxycarbonyl chloride or the like in the presence of an acid scavenger such as a tertiary amine including pyridine, lu...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Carbonic Ester.Ether.Boc.Boc
Anhydride
null
null
null
HCl
ClCCl.C(C)N(CC)CC.N1=CC=CC=C1
null
null
CC(C)(C)OC(=O)Cl.CC(C)(C)OC(=O)OC(C)(C)C>ClCCl.C(C)N(CC)CC.N1=CC=CC=C1>CC(C)(C)OC(=O)OC(=O)OC(C)(C)C
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-27ebac39e364439fa985f8a3d3eef3c5
CCOC(=O)Cc1ccc2ccccc2c1>>OCCNc1ccc2ccccc2c1
C(C)(=O)O.[O-]CC.[Na+].C1=C(C=CC2=CC=CC=C12)CC(=O)OCC.N(=O)OCCCC>>C1=C(C=CC2=CC=CC=C12)NCCO
CCO[C:2](=[O:1])[CH2:3][c:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[cH:14]1>>[OH:1][CH2:2][CH2:3][NH:4][c:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[cH:14]1
CCOC(=O)Cc1ccc2ccccc2c1
OCCNc1ccc2ccccc2c1
null
null
C(C)O
Miscellaneous
OtherReaction
baeafa7edc6df17a9d354abb8db9c29baad492dff3d8ef81d31d4184fc5c2c7e
bac4e04d71d5e57ebfb9a4ae4320481a6b98c6289a76c30e38737cd8f725e5e2
c1ccc2ccccc2c1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[CH2;D2;+0:3]-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[CH2;D2;+0:3]-[#7:9]-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]
null
[]
23
CELSIUS
18
HOUR
Ethyl 2-naphthylacetate (11.6 g) was dissolved in ethanol (100 mL) and treated with solid sodium ethoxide (3.5 g) and then dropwise with n-butyl nitrite (7.6 mL). The reaction was stirred at 23° C. for 18 h and treated with acetic acid (5 mL) and stirred for 1 h. The ethanol was removed under reduced pressure and the r...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol.Secondary amine
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
HO-
C(C)O
23
18
CCOC(=O)Cc1ccc2ccccc2c1>C(C)O>OCCNc1ccc2ccccc2c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-e6135515d659427a98f0b27e43c85d8b
NC(=O)c1c(F)cccc1F.O=CC(=O)O>>O=C(NC(O)C(=O)O)c1c(F)cccc1F
FC1=C(C(=O)N)C(=CC=C1)F.O.C(C=O)(=O)O>>FC1=C(C(=O)NC(C(=O)O)O)C(=CC=C1)F
[O:1]=[C:2]([NH2:3])[c:9]1[c:10]([F:11])[cH:12][cH:13][cH:14][c:15]1[F:16].[CH:4](=[O:5])[C:6](=[O:7])[OH:8]>>[O:1]=[C:2]([NH:3][CH:4]([OH:5])[C:6](=[O:7])[OH:8])[c:9]1[c:10]([F:11])[cH:12][cH:13][cH:14][c:15]1[F:16]
NC(=O)c1c(F)cccc1F.O=CC(=O)O
O=C(NC(O)C(=O)O)c1c(F)cccc1F
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
4a3b52c650544f6bcd441fa95d4d2ff87dd9c739061ff39332928c46df320b3d
b10a3ef220ace1bf1449d6e4f07e4fab45c01f4bc98efc71f34b015ef2e7ec16
c1ccccc1
[NH2;D1;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[O;D1;H0:5]=[C:6](-[O;D1;H1:7])-[CH;D2;+0:8]=[O;H0;D1;+0:9]>>[O;D1;H0:3]=[C:2](-[c:4])-[NH;D2;+0:1]-[CH;D3;+0:8](-[OH;D1;+0:9])-[C:6](=[O;D1;H0:5])-[O;D1;H1:7]
52.5
[{"value": 52.5, "product": "FC1=C(C(=O)NC(C(=O)O)O)C(=CC=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 50 g (0.318 mol) of 2,6-difluorobenzamide, 32 g (0.349 mol) of glyoxylic acid monohydrate and 200 mL of acetone was refluxed for 5 h. The reaction was cooled and solvents evaporated to give a white solid. It was triturated with cold acetone to afford 38.56 g of a white solid: mp 125°-127° C. 1H-NMR (DMSO-d...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amide
Secondary amide.Secondary alcohol
null
null
c1ccccc1
null
CC(=O)C
null
null
NC(=O)c1c(F)cccc1F.O=CC(=O)O>CC(=O)C>O=C(NC(O)C(=O)O)c1c(F)cccc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5979ac0adc0b4a1b9ea3a8531e33ee0d
Brc1cccs1.O=C(NC(O)C(=O)O)c1c(F)cccc1F>>O=C(NC(C(=O)O)c1ccc(Br)s1)c1c(F)cccc1F
FC1=C(C(=O)NC(C(=O)O)O)C(=CC=C1)F.BrC=1SC=CC1>>BrC1=CC=C(S1)C(C(=O)O)NC(C1=C(C=CC=C1F)F)=O
[cH:8]1[cH:9][cH:10][c:11]([Br:12])[s:13]1.O[CH:4]([NH:3][C:2](=[O:1])[c:14]1[c:15]([F:16])[cH:17][cH:18][cH:19][c:20]1[F:21])[C:5](=[O:6])[OH:7]>>[O:1]=[C:2]([NH:3][CH:4]([C:5](=[O:6])[OH:7])[c:8]1[cH:9][cH:10][c:11]([Br:12])[s:13]1)[c:14]1[c:15]([F:16])[cH:17][cH:18][cH:19][c:20]1[F:21]
Brc1cccs1.O=C(NC(O)C(=O)O)c1c(F)cccc1F
O=C(NC(C(=O)O)c1ccc(Br)s1)c1c(F)cccc1F
null
null
CS(=O)(=O)O
C-C Coupling
OtherReaction
ad96d5c2435232f883a245478104e1a9fc7c62cf0caf6a785ca127030f4f3fa0
7ccf8a4ec454d6cc03ce1e3efafa301b3c51d9e9635279e99312f4bc816939b8
O=C(NCc1cccs1)c1ccccc1
O-[CH;D3;+0:1](-[#7:2]-[C:3](=[O;D1;H0:4])-[c:5])-[C:6](=[O;D1;H0:7])-[O;D1;H1:8].[#16;a:9]1:[c:10]:[c:11]:[c:12]:[cH;D2;+0:13]:1>>[O;D1;H0:4]=[C:3](-[c:5])-[#7:2]-[CH;D3;+0:1](-[C:6](=[O;D1;H0:7])-[O;D1;H1:8])-[c;H0;D3;+0:13]1:[#16;a:9]:[c:10]:[c:11]:[c:12]:1
52.3
[{"value": 52.3, "product": "BrC1=CC=C(S1)C(C(=O)O)NC(C1=C(C=CC=C1F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 4.76 g (20.6 mmol) of the product of Step A in 140 mL of methanesulfonic acid was immersed in an ice-water bath (temperature between 5°-10° C.). Then, 4.0 g (24.6 mmol) of 2-bromothiophene was added dropwise. It was stirred at the same temperature until a deep blue-black color formed. It was poured into i...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
c1ccsc1
c1ccsc1
c1ccsc1.c1ccccc1
HO-
CS(=O)(=O)O
null
null
Brc1cccs1.O=C(NC(O)C(=O)O)c1c(F)cccc1F>CS(=O)(=O)O>O=C(NC(C(=O)O)c1ccc(Br)s1)c1c(F)cccc1F
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-5bd00e53bfe843f9897be04b64fe95ed
CO.O=C(NC(C(=O)O)c1ccc(Br)s1)c1c(F)cccc1F>>COC(=O)C(NC(=O)c1c(F)cccc1F)c1ccc(Br)s1
BrC1=CC=C(S1)C(C(=O)O)NC(C1=C(C=CC=C1F)F)=O.CO.S(=O)(Cl)Cl>>BrC1=CC=C(S1)C(C(=O)OC)NC(C1=C(C=CC=C1F)F)=O
[CH3:1][OH:2].O[C:3](=[O:4])[CH:5]([NH:6][C:7](=[O:8])[c:9]1[c:10]([F:11])[cH:12][cH:13][cH:14][c:15]1[F:16])[c:17]1[cH:18][cH:19][c:20]([Br:21])[s:22]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([NH:6][C:7](=[O:8])[c:9]1[c:10]([F:11])[cH:12][cH:13][cH:14][c:15]1[F:16])[c:17]1[cH:18][cH:19][c:20]([Br:21])[s:22]1
CO.O=C(NC(C(=O)O)c1ccc(Br)s1)c1c(F)cccc1F
COC(=O)C(NC(=O)c1c(F)cccc1F)c1ccc(Br)s1
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
O=C(NCc1cccs1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[#7:4]-[C:5]=[O;D1;H0:6])-[c:7]:[#16;a:8].[C;D1;H3:9]-[OH;D1;+0:10]>>[#16;a:8]:[c:7]-[C:3](-[#7:4]-[C:5]=[O;D1;H0:6])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:10]-[C;D1;H3:9]
null
[]
null
null
null
null
An amount of 3.415 g (9 mmol) of the product of Step B was dissolved in 19 mL of methanol. It was cooled in an ice-bath and 1.13 mL of thionyl chloride was added dropwise. The mixture was heated at reflux for 30 min. It was cooled and the methanol removed under reduced pressure. A saturated solution of sodium bicarbona...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1.c1ccsc1
HO-
null
null
null
CO.O=C(NC(C(=O)O)c1ccc(Br)s1)c1c(F)cccc1F>>COC(=O)C(NC(=O)c1c(F)cccc1F)c1ccc(Br)s1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-f7ff2b7c98a8486da666ddbb8f451938
Fc1cccc(F)c1C1=NC(c2ccc(Br)s2)CO1.OB(O)c1ccccc1>>Fc1cccc(F)c1C1=NC(c2ccc(-c3ccccc3)s2)CO1
BrC1=CC=C(S1)C1N=C(OC1)C1=C(C=CC=C1F)F.C([O-])([O-])=O.[Na+].[Na+].C1(=CC=CC=C1)B(O)O>>FC1=C(C(=CC=C1)F)C=1OCC(N1)C=1SC(=CC1)C1=CC=CC=C1
Br[c:15]1[cH:14][cH:13][c:12]([CH:11]2[N:10]=[C:9]([c:8]3[c:2]([F:1])[cH:3][cH:4][cH:5][c:6]3[F:7])[O:24][CH2:23]2)[s:22]1.OB(O)[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[F:1][c:2]1[cH:3][cH:4][cH:5][c:6]([F:7])[c:8]1[C:9]1=[N:10][CH:11]([c:12]2[cH:13][cH:14][c:15](-[c:16]3[cH:17][cH:18][cH:19][cH:20][cH:21]3)[s:22]...
Fc1cccc(F)c1C1=NC(c2ccc(Br)s2)CO1.OB(O)c1ccccc1
Fc1cccc(F)c1C1=NC(c2ccc(-c3ccccc3)s2)CO1
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
C1(=CC=CC=C1)C.CO
C-C Coupling
Suzuki coupling with boronic acids
a9e750b5cb26673fc488a731642519fa5963d6a2e4d2eeb976470c7f17606def
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(C2=NC(c3ccc(-c4ccccc4)s3)CO2)cc1
Br-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[c:5]:1.O-B(-O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[c:5]:1):[c:9]:[c:10]
83
[{"value": 83.0, "product": "FC1=C(C(=CC=C1)F)C=1OCC(N1)C=1SC(=CC1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
2
HOUR
To a solution of 100 mg (0.3 mmol) of the product of Step D of Example 2 in 0.6 mL toluene was added successively 10.4 mg (0.009 mmol) of Pd (PPh3)4, 0.3 mL of 2.0 m sodium carbonate, and 44 mg (0.36 mmol) of phenylboronic acid in 0.15 mL of methanol. The mixture was stirred at 80° C. for 2 h. It was cooled and partiti...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccsc1.c1ccccc1
c1ccsc1.c1ccccc1
c1ccccc1.C1=NCCO1.c1ccsc1.c1ccccc1
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.C1(=CC=CC=C1)C.CO
80
2
Fc1cccc(F)c1C1=NC(c2ccc(Br)s2)CO1.OB(O)c1ccccc1>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.C1(=CC=CC=C1)C.CO>Fc1cccc(F)c1C1=NC(c2ccc(-c3ccccc3)s2)CO1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-29a7c6ca98d34ee2a5aada83fa10f22d
CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccc(=O)cc-3[nH]c2-1>>CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc(O)ccc3nc2-1
C(Cl)(Cl)Cl.CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)NC5=CC(=O)C=CC5=C4)O.CO>>CC[C@@]1(C2=C(COC1=O)C(=O)N3CC=4C=C5C=C(C=CC5=NC4C3=C2)O)O
[CH3:1][CH2:2][C@@:3]1([OH:4])[C:5](=[O:6])[O:7][CH2:8][c:9]2[c:10]1[cH:11][c:12]1[n:13]([c:14]2=[O:15])[CH2:16][c:17]2[cH:18][c:19]3[cH:20][cH:21][c:23](=[O:22])[cH:24][c:25]-3[nH:26][c:27]2-1>>[CH3:1][CH2:2][C@@:3]1([OH:4])[C:5](=[O:6])[O:7][CH2:8][c:9]2[c:10]1[cH:11][c:12]1[n:13]([c:14]2=[O:15])[CH2:16][c:17]2[cH:18...
CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccc(=O)cc-3[nH]c2-1
CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc(O)ccc3nc2-1
null
null
FC(C(=O)O)(F)F
Miscellaneous
OtherReaction
b5548fadc146433e9acdf6d786c997613c4f7901c76ad3212d9b86d0ebc399e3
6dd67d2d062ecf3a4bfbb86c40e45739a873f777b0585faa974e3874e3a0b559
O=C1Cc2cc3n(c(=O)c2CO1)Cc1cc2ccccc2nc1-3
[#7;a:1]:[c:2]-[c:3]1:[c:4]:[c:5]:[c;H0;D3;+0:6]2:[c:7]:[cH;D2;+0:8]:[c;H0;D3;+0:9](=[O;H0;D1;+0:10]):[c:11]:[c;H0;D3;+0:12]-2:[nH;D2;+0:13]:1>>[#7;a:1]:[c:2]-[c:3]1:[c:4]:[c:5]:[c;H0;D3;+0:6]2:[c:7]:[c;H0;D3;+0:8](-[OH;D1;+0:10]):[cH;D2;+0:9]:[c:11]:[c;H0;D3;+0:12]:2:[n;H0;D2;+0:13]:1
null
[]
null
null
null
null
Naturally available mixture of 10 and 11-hydroxy camptothecin (1.0 g) is dissolved in anhydrous trifluoroacetic acid (5 ml) and anhydrous methanol (10 ml) to form a homogeneous solution of the quaternized components of the mixture. The homogeneous solution is then absorbed over enough silica gel (60A; 60-230 mesh) to f...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic alcohol
C1Cc2cc3c4nc5ccccc5cc4Cn3cc2CO1
C1Cc2cc3c4nc5ccccc5cc4Cn3cc2CO1
C1Cc2cc3c4nc5ccccc5cc4Cn3cc2CO1
null
FC(C(=O)O)(F)F
null
null
CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3ccc(=O)cc-3[nH]c2-1>FC(C(=O)O)(F)F>CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc(O)ccc3nc2-1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-ce1330cec512459bbd1a23148a42b7c2
CCC=O.CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc(O)ccc3nc2-1>>CCc1c2c(nc3ccc(O)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC=4C=C5C=C(C=CC5=NC4C3=C2)O)O.S(=O)(=O)([O-])OOS(=O)(=O)[O-].[K+].[K+].C(CC)=O.S(O)(O)(=O)=O.FC(C(=O)O)(F)F>>CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)[C@@]5(CC)O)O
O=C[CH2:2][CH3:1].[cH:3]1[c:4]2[c:5]([n:6][c:7]3[cH:8][cH:9][c:10]([OH:11])[cH:12][c:13]13)-[c:14]1[cH:15][c:16]3[c:17]([c:18](=[O:19])[n:20]1[CH2:21]2)[CH2:22][O:23][C:24](=[O:25])[C@:26]3([OH:27])[CH2:28][CH3:29]>>[CH3:1][CH2:2][c:3]1[c:4]2[c:5]([n:6][c:7]3[cH:8][cH:9][c:10]([OH:11])[cH:12][c:13]13)-[c:14]1[cH:15][c:...
CCC=O.CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc(O)ccc3nc2-1
CCc1c2c(nc3ccc(O)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC
null
O.O.O.O.O.O.O.S(=O)(=O)([O-])[O-].[Fe+2]
O
C-C Coupling
OtherReaction
e086937f9b1b4cd3230ad632fe7c477d59bf1145fa5cb9a64da42851bc68f6ea
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
O=C1Cc2cc3n(c(=O)c2CO1)Cc1cc2ccccc2nc1-3
O=C-[CH2;D2;+0:1]-[C;D1;H3:2].[c:3]:[c:4]1:[cH;D2;+0:5]:[c:6]2:[c:7](:[#7;a:8]:[c:9]:1:[c:10])-[c:11]:[#7;a:12]-[C:13]-2>>[C;D1;H3:2]-[CH2;D2;+0:1]-[c;H0;D3;+0:5]1:[c:4](:[c:3]):[c:9](:[c:10]):[#7;a:8]:[c:7]2:[c:6]:1-[C:13]-[#7;a:12]:[c:11]-2
null
[]
null
null
15
MINUTE
The 10-hydroxy camptothecin (800 mg; 2.2 mmol) is suspended in water (24 ml). Iron (II) sulfate heptahydrate (250 mg, 0.85 millimoles) is added to the suspension and then followed by the addition of propionaldehyde (3 ml). The reaction mixture is then cooled in an ice bath and concentrated sulfuric acid (1 ml) and trif...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
C1Cc2cc3c4nc5ccccc5cc4Cn3cc2CO1
C1Cc2cc3c4nc5ccccc5cc4Cn3cc2CO1
C1Cc2cc3c4nc5ccccc5cc4Cn3cc2CO1
HO-
O.O.O.O.O.O.O.S(=O)(=O)([O-])[O-].[Fe+2].O
null
0.25
CCC=O.CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3cc(O)ccc3nc2-1>O.O.O.O.O.O.O.S(=O)(=O)([O-])[O-].[Fe+2].O>CCc1c2c(nc3ccc(O)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-d58c7e03f08a4b1398a99627fe4be9d6
CC(C)(C)OC(=O)[C@@H]1CSC(C2CCCCC2)N1C(=O)CNC(=O)Nc1cccc(CC(=O)OCc2ccccc2)c1>>CC(C)(C)OC(=O)[C@@H]1CSC(C2CCCCC2)N1C(=O)CNC(=O)Nc1cccc(CC(=O)O)c1
CO.C(C)(C)(C)OC(=O)[C@H]1N(C(SC1)C1CCCCC1)C(CNC(NC=1C=C(C=CC1)CC(=O)OCC1=CC=CC=C1)=O)=O.C(=O)[O-].[NH4+]>>C(C)(C)(C)OC(=O)[C@H]1N(C(SC1)C1CCCCC1)C(CNC(NC=1C=C(C=CC1)CC(=O)O)=O)=O
c1ccc(C[O:34][C:32]([CH2:31][c:30]2[cH:29][cH:28][cH:27][c:26]([NH:25][C:23]([NH:22][CH2:21][C:19]([N:18]3[C@H:8]([C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])[CH2:9][S:10][CH:11]3[CH:12]3[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]3)=[O:20])=[O:24])[cH:35]2)=[O:33])cc1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])...
CC(C)(C)OC(=O)[C@@H]1CSC(C2CCCCC2)N1C(=O)CNC(=O)Nc1cccc(CC(=O)OCc2ccccc2)c1
CC(C)(C)OC(=O)[C@@H]1CSC(C2CCCCC2)N1C(=O)CNC(=O)Nc1cccc(CC(=O)O)c1
null
[Pd]
[OH-].[Na+]
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(NCC(=O)N1CCSC1C1CCCCC1)Nc1ccccc1
[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1>>[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]
58.9
[{"value": 58.9, "product": "C(C)(C)(C)OC(=O)[C@H]1N(C(SC1)C1CCCCC1)C(CNC(NC=1C=C(C=CC1)CC(=O)O)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
25
CELSIUS
null
null
30 cm3 of methanol are added slowly under an inert atmosphere into a round-bottomed flask containing 2.0 g of benzyl (4R) -3-{3- [2- (4-tert-butoxycarbonyl-2-cyclohexyl-3-thiazolidinyl)-2-oxoethyl]-ureido}phenyl-acetate (isomer A), 1.7 g of ammonium formate and 2.0 g of palladium on charcoal (10% Pd). The reaction medi...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
C1CSC[NH]1.C1CCCCC1.c1ccccc1
Other
[Pd].[OH-].[Na+]
25
null
CC(C)(C)OC(=O)[C@@H]1CSC(C2CCCCC2)N1C(=O)CNC(=O)Nc1cccc(CC(=O)OCc2ccccc2)c1>[Pd].[OH-].[Na+]>CC(C)(C)OC(=O)[C@@H]1CSC(C2CCCCC2)N1C(=O)CNC(=O)Nc1cccc(CC(=O)O)c1
ord_dataset-c2ad1656a3ca4d08888ffb6e3f3a2742
ord-1643f581587c4ecfa782be2eff73af28
CC(C)(C)OC(=O)NCC(=O)N1C(Cc2ccccc2)SC[C@H]1C(=O)OC(C)(C)C.CC(C)(C)OC(=O)NCC(=O)O>>CC(C)(C)OC(=O)C(N)C(=O)N1C(Cc2ccccc2)SC[C@H]1C(=O)OC(C)(C)C
C1(CCCCC1)N=C=NC1CCCCC1.C(C)(C)(C)OC(=O)NCC(=O)N1C(SC[C@H]1C(=O)OC(C)(C)C)CC1=CC=CC=C1.C(C1=CC=CC=C1)C1SC[C@H](N1)C(=O)OC(C)(C)C.C(C)(C)(C)OC(=O)NCC(=O)O>>C(C)(C)(C)OC(=O)C(C(=O)N1C(SC[C@H]1C(=O)OC(C)(C)C)CC1=CC=CC=C1)N
O=C(O[C:2]([CH3:1])([CH3:3])[CH3:4])[NH:9][CH2:8][C:10](=[O:11])[N:12]1[CH:13]([CH2:14][c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)[S:21][CH2:22][C@H:23]1[C:24](=[O:25])[O:26][C:27]([CH3:28])([CH3:29])[CH3:30].CC(C)(C)OC(=O)NC[C:6]([OH:5])=[O:7]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH:8]([NH2:9])[C:10](=[O...
CC(C)(C)OC(=O)NCC(=O)N1C(Cc2ccccc2)SC[C@H]1C(=O)OC(C)(C)C.CC(C)(C)OC(=O)NCC(=O)O
CC(C)(C)OC(=O)C(N)C(=O)N1C(Cc2ccccc2)SC[C@H]1C(=O)OC(C)(C)C
null
null
null
C-C Coupling
OtherReaction
452c5a4ab0a68e596ed59dbcfcc8c9f944cf2a36a8b48984f7cf3afa8883abf6
d4a1a313373c0e4ca1d53b8624833769c1dcf8d648c794bf6856bc1390fac38c
c1ccc(CC2NCCS2)cc1
C-C(-C)(-C)-O-C(=O)-N-C-[C;H0;D3;+0:1](=[O;D1;H0:2])-[OH;D1;+0:3].O=C(-O-[C;H0;D4;+0:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7])-[NH;D2;+0:8]-[CH2;D2;+0:9]-[C:10](=[O;D1;H0:11])-[#7:12](-[C:13]-[#16:14])-[C:15]-[C:16](-[#8:17])=[O;D1;H0:18]>>[#16:14]-[C:13]-[#7:12](-[C:10](=[O;D1;H0:11])-[CH;D3;+0:9](-[NH2;D1;+0:8])-[C...
null
[]
null
null
null
null
B tert-Butyl (4R)-3-(2-tert-butoxycarbonylaminoacetyl)-2-benzyl-4-thiazolidinecarboxylate (isomer A) may be prepared in a manner similar to that described in Example 1C, but starting with 25.7 g of tert-butyl (2RS,4R)-2-benzyl-4-thiazolidinecarboxylate, 13.9 g of 2-tert-butoxycarbonylaminoacetic acid and 16.3 g of N,N'...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carbamic ester.Carboxylic acid.Ether.Ether.Boc.Boc
Ester.Primary amine
null
null
C1CSC[NH]1.c1ccccc1
HO-
null
null
null
CC(C)(C)OC(=O)NCC(=O)N1C(Cc2ccccc2)SC[C@H]1C(=O)OC(C)(C)C.CC(C)(C)OC(=O)NCC(=O)O>>CC(C)(C)OC(=O)C(N)C(=O)N1C(Cc2ccccc2)SC[C@H]1C(=O)OC(C)(C)C