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-02ee2261663048188cf6d85d2cc96e3f
ord-d0ca2bb5fa8e4a7e9c2ffd5aff410073
CCO.O=C(O)c1cccnc1O.O=P(Cl)(Cl)Cl>>CCOC(=O)c1cccnc1Cl
C(C)O.OC1=C(C(=O)O)C=CC=N1.P(Cl)(Cl)(Cl)(Cl)Cl.P(=O)(Cl)(Cl)Cl>>ClC1=C(C(=O)OCC)C=CC=N1
[CH3:1][CH2:2][OH:3].O[C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][n:10][c:11]1O.O=P(Cl)(Cl)[Cl:12]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][cH:9][n:10][c:11]1[Cl:12]
CCO.O=C(O)c1cccnc1O.O=P(Cl)(Cl)Cl
CCOC(=O)c1cccnc1Cl
null
null
null
Protection
OtherReaction
75789a74555597973d21551267c3e0e83091d9db09905fd888789d98d5f9563f
4df5c87c1bba9487ca0dac6d5d13d25b2b96819110434b9c385838ee1b983c5e
c1ccncc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c;H0;D3;+0:6](-O):[#7;a:7]:[c:8].[C;D1;H3:9]-[C:10]-[OH;D1;+0:11]>>[C;D1;H3:9]-[C:10]-[O;H0;D2;+0:11]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c;H0;D3;+0:6](-[Cl;H0;D1;+0:1]):[#7;a:7]:[c:8]
60
[{"value": 60.0, "product": "ClC1=C(C(=O)OCC)C=CC=N1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a mixture of 2-hydroxynicotinic acid (13.91 g., 0.1 mole) and phosphorus pentachloride (42 g., 0.2 mole) was added phosphorus oxychloride (25 ml., excess) and then stirred at room temperature for 30 minutes. This was then heated at 120° C. for 2 hours. The reaction mixture was then concentrated in vacuo until a red ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol.Aromatic alcohol
Aromatic halide.Ester
c1ccncc1
c1ccncc1
c1ccncc1
HCl
null
null
0.5
CCO.O=C(O)c1cccnc1O.O=P(Cl)(Cl)Cl>>CCOC(=O)c1cccnc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ca3b6b7778984b1dafee3bcd7b9942eb
CN(C)C=O.c1c[nH]c(-c2cnco2)c1>>O=Cc1ccc(-c2cnco2)[nH]1
C(C)(=O)[O-].[Na+].N1C(=CC=C1)C1=CN=CO1.CN(C=O)C.P(=O)(Cl)(Cl)Cl>>C(=O)C1=CC=C(N1)C1=CN=CO1
CN(C)[CH:2]=[O:1].[cH:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][n:9][cH:10][o:11]2)[nH:12]1>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][n:9][cH:10][o:11]2)[nH:12]1
CN(C)C=O.c1c[nH]c(-c2cnco2)c1
O=Cc1ccc(-c2cnco2)[nH]1
null
null
C(Cl)(Cl)Cl.ClCCCl
C-C Coupling
OtherReaction
2b5f756dc741b2c8883ed99aca6ca6cc1773d635791cb1bbe9b51efb615b4170
f0bd75a0630092c31f21f61f4a015c77ae0dff14a0b742b4370d7a38fda490f7
c1c[nH]c(-c2cnco2)c1
C-N(-C)-[CH;D2;+0:1]=[O;D1;H0:2].[#7;a:3]1:[c:4]:[c:5]:[c:6]:[cH;D2;+0:7]:1>>[O;D1;H0:2]=[CH;D2;+0:1]-[c;H0;D3;+0:7]1:[#7;a:3]:[c:4]:[c:5]:[c:6]:1
80
[{"value": 80.0, "product": "C(=O)C1=CC=C(N1)C1=CN=CO1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To an ice cooled 1 mL dimethylformamide was added 0.82 g (5.4 mmol) of phosphorus oxychloride while stirring under a nitrogen atmosphere. The mixture was stirred 20 minutes and then was added a solution of 0.60 g (4.5 mmol) of 5-(pyrrol-2-yl)oxazole in 15 mL of 1,2-dichloroethane while cooling in an ice bath. The react...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Aldehyde
c1cc[nH]c1
c1cc[nH]c1
c1cc[nH]c1.c1cocn1
Other
C(Cl)(Cl)Cl.ClCCCl
null
null
CN(C)C=O.c1c[nH]c(-c2cnco2)c1>C(Cl)(Cl)Cl.ClCCCl>O=Cc1ccc(-c2cnco2)[nH]1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2288569fc3ee4fffb9e3876b2052db84
Nc1ccccc1O.O=C(O)c1ccc[nH]1>>c1c[nH]c(-c2nc3ccccc3o2)c1
N1C(=CC=C1)C(=O)O.NC1=C(C=CC=C1)O.B(O)(O)O>>N1C(=CC=C1)C=1OC2=C(N1)C=CC=C2
[NH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[OH:13].O=[C:5](O)[c:4]1[nH:3][cH:2][cH:1][cH:14]1>>[cH:1]1[cH:2][nH:3][c:4](-[c:5]2[n:6][c:7]3[cH:8][cH:9][cH:10][cH:11][c:12]3[o:13]2)[cH:14]1
Nc1ccccc1O.O=C(O)c1ccc[nH]1
c1c[nH]c(-c2nc3ccccc3o2)c1
null
null
C(C)(=O)OCC.C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
Benzoxazole formation from ester/carboxylic acid
ab90945f453b9d98729e6912eac27527ccc8f6879f9fc67f913646675914d5f8
082415a064525fb5ab1054c8f1a07a8509dc65297c7337b4b21c60d0aec70378
c1c[nH]c(-c2nc3ccccc3o2)c1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[c:5]:[c:6]:1.[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10](-[OH;D1;+0:11]):[c:12]>>[c:12]:[c:10]1:[o;H0;D2;+0:11]:[c;H0;D3;+0:1](-[c;H0;D3;+0:2]2:[#7;a:3]:[c:4]:[c:5]:[c:6]:2):[n;H0;D2;+0:7]:[c:8]:1:[c:9]
52
[{"value": 52.0, "product": "N1C(=CC=C1)C=1OC2=C(N1)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 51.6, "product": "N1C(=CC=C1)C=1OC2=C(N1)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2-(Pyrrol-2-yl)benzoxazole was prepared as follows: A mixture of 5.55 g (0.05 mol) of pyrrole-2-carboxylic acid and 5.46 g (0.05 mol) of o-aminophenol and 3.09 g (0.05 mol) boric acid in 50 mL of xylene was heated under reflux for 3 days while removing water which was generated from reaction using a Dean-Stark trap. Th...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol.Primary amine
null
c1ccccc1
c1ccc2ocnc2c1
c1cc[nH]c1.c1ccc2ocnc2c1
HO-
C(C)(=O)OCC.C=1(C(=CC=CC1)C)C
null
null
Nc1ccccc1O.O=C(O)c1ccc[nH]1>C(C)(=O)OCC.C=1(C(=CC=CC1)C)C>c1c[nH]c(-c2nc3ccccc3o2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-514be903fc7a4ed1b961eb5abfbc5505
Nc1ccccc1S.O=C(O)c1ccc[nH]1>>c1c[nH]c(-c2nc3ccccc3s2)c1
N1C(=CC=C1)C(=O)O.NC1=C(C=CC=C1)S.B(O)(O)O>>N1C(=CC=C1)C=1SC2=C(N1)C=CC=C2
[NH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[SH:13].O=[C:5](O)[c:4]1[nH:3][cH:2][cH:1][cH:14]1>>[cH:1]1[cH:2][nH:3][c:4](-[c:5]2[n:6][c:7]3[cH:8][cH:9][cH:10][cH:11][c:12]3[s:13]2)[cH:14]1
Nc1ccccc1S.O=C(O)c1ccc[nH]1
c1c[nH]c(-c2nc3ccccc3s2)c1
null
null
C(C)(=O)OCC.C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
Benzothiazole formation from ester/carboxylic acid
5c56e3620e73de41a8f6dd28e5dfdee2d821cd47d85c852a5166976e26e39b41
cfddc96fe868437500f756276ee466b3dbb82293a2c1f3605d6b16aab79b3f9d
c1c[nH]c(-c2nc3ccccc3s2)c1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[c:5]:[c:6]:1.[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10](-[SH;D1;+0:11]):[c:12]>>[c:12]:[c:10]1:[s;H0;D2;+0:11]:[c;H0;D3;+0:1](-[c;H0;D3;+0:2]2:[#7;a:3]:[c:4]:[c:5]:[c:6]:2):[n;H0;D2;+0:7]:[c:8]:1:[c:9]
14
[{"value": 14.0, "product": "N1C(=CC=C1)C=1SC2=C(N1)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 14.0, "product": "N1C(=CC=C1)C=1SC2=C(N1)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 5.55 g (50 mmol) of pyrrole-2-carboxylic acid, 6.26 g (50 mmol) of 2-aminothiophenol and 3.09 g (50 mmol) of boric acid in 250 mL of xylene was heated under reflux for 3 days while removing water which was generated from reaction using a Dean-Stark trap. the cooled reaction mixture was diluted with 200 mL ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Aromatic thiol
null
c1ccccc1
c1ccc2scnc2c1
c1cc[nH]c1.c1ccc2scnc2c1
HO-
C(C)(=O)OCC.C=1(C(=CC=CC1)C)C
null
null
Nc1ccccc1S.O=C(O)c1ccc[nH]1>C(C)(=O)OCC.C=1(C(=CC=CC1)C)C>c1c[nH]c(-c2nc3ccccc3s2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f133d8b34fb84de6ae33d093fc5b41e4
Nc1ccccc1N.O=C(O)c1ccc[nH]1>>c1c[nH]c(-c2nc3ccccc3[nH]2)c1
C1(=C(C=CC=C1)N)N.N1C(=CC=C1)C(=O)O>>N1C(=CC=C1)C=1NC2=C(N1)C=CC=C2
[NH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[NH2:13].O=[C:5](O)[c:4]1[nH:3][cH:2][cH:1][cH:14]1>>[cH:1]1[cH:2][nH:3][c:4](-[c:5]2[n:6][c:7]3[cH:8][cH:9][cH:10][cH:11][c:12]3[nH:13]2)[cH:14]1
Nc1ccccc1N.O=C(O)c1ccc[nH]1
c1c[nH]c(-c2nc3ccccc3[nH]2)c1
null
null
C([O-])(O)=O.[Na+]
Aromatic Heterocycle Formation
OtherReaction
8409c8c0d4e4ea3a5ac4d357a90931cd25bdeaf070f3095e8e16fa38a40808ca
7e1f92e04d2c8ce23daa6dd33c69b56cfa9feb423ec9a3444bfeb568a99ef87e
c1c[nH]c(-c2nc3ccccc3[nH]2)c1
O-[C;H0;D3;+0:1](=O)-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[c:5]:[c:6]:1.[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10](-[NH2;D1;+0:11]):[c:12]>>[c:9]:[c:8]1:[nH;D2;+0:7]:[c;H0;D3;+0:1](-[c;H0;D3;+0:2]2:[#7;a:3]:[c:4]:[c:5]:[c:6]:2):[n;H0;D2;+0:11]:[c:10]:1:[c:12]
27.3
[{"value": 25.0, "product": "N1C(=CC=C1)C=1NC2=C(N1)C=CC=C2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 27.3, "product": "N1C(=CC=C1)C=1NC2=C(N1)C=CC=C2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
30
MINUTE
A mixture of 1.08 g (10 mmol) of o-phenylenediamine and 20 g of polyophosphate esters was heated gently at 80° C. and was added portionwise 1.11 g (10 mmol) of pyrrole-2-carboxylic acid. After the mixture was stirred at 100° C. for 30 minutes, it was poured into a saturated solution of sodium bicarbonate (500 mL) and s...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Primary amine
null
c1ccccc1
c1ccc2[nH]cnc2c1
c1cc[nH]c1.c1ccc2[nH]cnc2c1
HO-
C([O-])(O)=O.[Na+]
80
0.5
Nc1ccccc1N.O=C(O)c1ccc[nH]1>C([O-])(O)=O.[Na+]>c1c[nH]c(-c2nc3ccccc3[nH]2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7c1e2ef533ec401fb17ad35bd72360ba
COC1O[C@H]2[C@H](OCc3ccccc3)[C@@H]1NC[C@@H]2OCc1ccccc1.O=C(Cl)OCc1ccccc1>>COC1O[C@H]2[C@H](OCc3ccccc3)[C@@H]1N(C(=O)OCc1ccccc1)C[C@@H]2OCc1ccccc1
C(C1=CC=CC=C1)O[C@@H]1[C@H]2C(OC)O[C@@H]1[C@@H](OCC1=CC=CC=C1)CN2.C([O-])(O)=O.[Na+].C(C1=CC=CC=C1)OC(=O)Cl>>C(C1=CC=CC=C1)OC(=O)N1[C@@H]2C(OC)O[C@@H]([C@@H]2OCC2=CC=CC=C2)[C@@H](OCC2=CC=CC=C2)C1
[CH3:1][O:2][CH:3]1[O:4][C@H:5]2[C@H:6]([O:7][CH2:8][c:9]3[cH:10][cH:11][cH:12][cH:13][cH:14]3)[C@@H:15]1[NH:16][CH2:27][C@@H:28]2[O:29][CH2:30][c:31]1[cH:32][cH:33][cH:34][cH:35][cH:36]1.Cl[C:17](=[O:18])[O:19][CH2:20][c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1>>[CH3:1][O:2][CH:3]1[O:4][C@H:5]2[C@H:6]([O:7][CH2:8][c:9...
COC1O[C@H]2[C@H](OCc3ccccc3)[C@@H]1NC[C@@H]2OCc1ccccc1.O=C(Cl)OCc1ccccc1
COC1O[C@H]2[C@H](OCc3ccccc3)[C@@H]1N(C(=O)OCc1ccccc1)C[C@@H]2OCc1ccccc1
null
null
C(C)OCC
Protection
N-alkylation of secondary amines with alkyl halides
badcf1c4f27013e2481f7ad2e4c9d69ce5bce4dee89060f3a7e5bed4347af601
d86dc1e6d0e089b3444b62ddfcf4c4822bdac4b60e628553036562518c29adcd
O=C(OCc1ccccc1)N1C[C@H](OCc2ccccc2)[C@H]2OC[C@@H]1[C@H]2OCc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#8:5]-[C:6]-[C:7](-[C:8])-[NH;D2;+0:9]-[C:10]-[C:11]>>[#8:5]-[C:6]-[C:7](-[C:8])-[N;H0;D3;+0:9](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-[C:10]-[C:11]
null
[]
null
null
2
HOUR
To the crude amine (15), in a solution of diethyl ether:saturated sodium bicarbonate (3:2, 20 ml), was added benzylchloroformate (0.2 ml, 1.2 mmol). The reaction was then stirred, at such a rate as to make it one phase, for 2 hours. The aqueous phase was then separated and washed with diethyl ether (3×10 ml). The combi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Secondary amine
Carbamic ester
C1C[C@@H]2C[C@@H](CO2)N1
C1C[C@@H]2C[C@@H](CO2)[NH]1
c1ccccc1.c1ccccc1.C1C[C@@H]2C[C@@H](CO2)[NH]1.c1ccccc1
HCl
C(C)OCC
null
2
COC1O[C@H]2[C@H](OCc3ccccc3)[C@@H]1NC[C@@H]2OCc1ccccc1.O=C(Cl)OCc1ccccc1>C(C)OCC>COC1O[C@H]2[C@H](OCc3ccccc3)[C@@H]1N(C(=O)OCc1ccccc1)C[C@@H]2OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b687ad6eeb954cfaa22dfb459d6be666
O=C(OCc1ccccc1)N1C[C@H](OCc2ccccc2)[C@@H](O)[C@H](OCc2ccccc2)[C@H]1CO>>OC[C@H]1NC[C@H](O)[C@@H](O)[C@@H]1O
C(C1=CC=CC=C1)OC(=O)N1C[C@H](OCC2=CC=CC=C2)[C@@H](O)[C@H](OCC2=CC=CC=C2)[C@H]1CO.C(C)OCC>>N1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO
O=C(OCc1ccccc1)[N:4]1[C@H:3]([CH2:2][OH:1])[C@@H:10]([O:11]Cc2ccccc2)[C@H:8]([OH:9])[C@@H:6]([O:7]Cc2ccccc2)[CH2:5]1>>[OH:1][CH2:2][C@H:3]1[NH:4][CH2:5][C@H:6]([OH:7])[C@@H:8]([OH:9])[C@@H:10]1[OH:11]
O=C(OCc1ccccc1)N1C[C@H](OCc2ccccc2)[C@@H](O)[C@H](OCc2ccccc2)[C@H]1CO
OC[C@H]1NC[C@H](O)[C@@H](O)[C@@H]1O
null
[Pd]
C(C)(=O)O
Reduction
OtherReaction
1dcef89f6803aee8587c37ade3c513b4d9b22ca03377d66f5b09b432cbc37040
a63a032ebc37eef5f651c3d6a414fd6089bf1618f6929f2e95beb31d07025d65
C1CCNCC1
O=C(-O-C-c1:c:c:c:c:c:1)-[N;H0;D3;+0:1]1-[C:2]-[C:3](-[O;H0;D2;+0:4]-C-c2:c:c:c:c:c:2)-[C:5]-[C:6](-[O;H0;D2;+0:7]-C-c2:c:c:c:c:c:2)-[C:8]-1-[C:9]>>[C:9]-[C:8]1-[NH;D2;+0:1]-[C:2]-[C:3](-[OH;D1;+0:4])-[C:5]-[C:6]-1-[OH;D1;+0:7]
96
[{"value": 95.0, "product": "N1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.0, "product": "N1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The diol (17) (580 mg, 1.2 mmol) was stirred in glacial acetic acid (30 ml) in the presence of palladium black (100 mg) under hydrogen for 3 days, by which time no starting material (Rf 0.2) remained by t.l.c. (diethyl ether). Filtration and removal of the solvent then gave a gum which was purified by ion exchange chro...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Ether.Ether
Secondary alcohol.Secondary alcohol.Secondary amine
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
C1CCNCC1
C1CCNCC1
HO-
[Pd].C(C)(=O)O
null
null
O=C(OCc1ccccc1)N1C[C@H](OCc2ccccc2)[C@@H](O)[C@H](OCc2ccccc2)[C@H]1CO>[Pd].C(C)(=O)O>OC[C@H]1NC[C@H](O)[C@@H](O)[C@@H]1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8f260ae7aa8349298a8c230f70739320
C=CCBr.COC(=O)CC(=O)c1cccnc1>>C=CCC(C(=O)OC)C(=O)c1cccnc1
C(C=C)Br.C(C1=CN=CC=C1)(=O)CC(=O)OC.[Na].C(C=C)Br>>COC(C(CC=C)C(C1=CN=CC=C1)=O)=O
Br[CH2:3][CH:2]=[CH2:1].[CH2:4]([C:5](=[O:6])[O:7][CH3:8])[C:9](=[O:10])[c:11]1[cH:12][cH:13][cH:14][n:15][cH:16]1>>[CH2:1]=[CH:2][CH2:3][CH:4]([C:5](=[O:6])[O:7][CH3:8])[C:9](=[O:10])[c:11]1[cH:12][cH:13][cH:14][n:15][cH:16]1
C=CCBr.COC(=O)CC(=O)c1cccnc1
C=CCC(C(=O)OC)C(=O)c1cccnc1
null
null
CO
C-C Coupling
OtherReaction
a419f976441b589a3c956c0f129ce3053512f0325f3e460530d895d12d1b751d
c9d64189f02be16d3a7baf78522635b86019231c97f41522f031694d4f90e5ad
c1ccncc1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[#7;a:4]:[c:5]:[c:6]-[C:7](=[O;D1;H0:8])-[CH2;D2;+0:9]-[C:10](=[O;D1;H0:11])-[#8:12]-[C;D1;H3:13]>>[#7;a:4]:[c:5]:[c:6]-[C:7](=[O;D1;H0:8])-[CH;D3;+0:9](-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3])-[C:10](=[O;D1;H0:11])-[#8:12]-[C;D1;H3:13]
null
[]
25
CELSIUS
30
MINUTE
Methyl 2-(nicotinoyl)acetate (17.9 g, prepared by the method of E. Wenkert el al. J. Org. Chem., 1983, 48, 5006) was added under argon to a solution of sodium metal (2.3 g) in methanol (200 ml) and the resulting mixture was stirred at 25° C. for 30 mins. Allyl bromide (12.0 g) was then added and stirring was continued ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone.Ester.Allyl
null
null
c1ccncc1
HBr
CO
25
0.5
C=CCBr.COC(=O)CC(=O)c1cccnc1>CO>C=CCC(C(=O)OC)C(=O)c1cccnc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-db8a01301d8543ea840e78a021d649d8
CCOC(CBr)OCC.Oc1ccccc1>>CCOC(COc1ccccc1)OCC
[H-].[Na+].C1(=CC=CC=C1)O.C(C)OC(CBr)OCC>>C(C)OC(COC1=CC=CC=C1)OCC
Br[CH2:5][CH:4]([O:3][CH2:2][CH3:1])[O:13][CH2:14][CH3:15].[OH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][CH2:2][O:3][CH:4]([CH2:5][O:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[O:13][CH2:14][CH3:15]
CCOC(CBr)OCC.Oc1ccccc1
CCOC(COc1ccccc1)OCC
null
null
CN1CCCN(C1=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2](-[#8:3])-[#8:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[#8:3]-[C:2](-[#8:4])-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
110
CELSIUS
30
MINUTE
Sodium hydride (5.83 g of a 55% dispersion in mineral oil) was added to a solution of phenol (12.56 g) in DMPU (25 ml) at 5° C. and the mixture was stirred for 30 minutes. Bromoacetaldehyde diethyl acetal (10.05 ml) was added and the mixture was heated at 110° C. for 5 hours, then allowed to cool. The mixture was parti...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1
HBr
CN1CCCN(C1=O)C
110
0.5
CCOC(CBr)OCC.Oc1ccccc1>CN1CCCN(C1=O)C>CCOC(COc1ccccc1)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-42782490ce0446c8903b1dfab0a8e409
CCCC[B+]CCCC.O=Cc1cccnc1.O=S(=O)([O-])C(F)(F)F>>C=CCC(CO)C(O)c1cccnc1
N1=CC(=CC=C1)C=O.[O-]S(=O)(=O)C(F)(F)F.C(CCC)[B+]CCCC.C(C)(C)N(CC)C(C)C>>C(C=C)C(C(O)C=1C=NC=CC1)CO
CCCC[B+][CH2:4][CH2:3][CH2:2][CH3:1].[CH:7](=[O:8])[c:9]1[cH:10][cH:11][cH:12][n:13][cH:14]1.O=S([O-])(C(F)(F)F)=[O:6]>>[CH2:1]=[CH:2][CH2:3][CH:4]([CH2:5][OH:6])[CH:7]([OH:8])[c:9]1[cH:10][cH:11][cH:12][n:13][cH:14]1
CCCC[B+]CCCC.O=Cc1cccnc1.O=S(=O)([O-])C(F)(F)F
C=CCC(CO)C(O)c1cccnc1
null
null
ClCCl
Heteroatom Alkylation and Arylation
OtherReaction
e529e8e1b0a2dbb0f2eab56bc1d2a270a57b1a636e658baa7f607f318ac43e7d
fa190e00978154d1e8722264bdac6e8d3f095f9701d0ca8f2dfa2980318c7fc0
c1ccncc1
C-C-C-C-[B+]-[CH2;D2;+0:1]-[C:2]-[CH2;D2;+0:3]-[CH3;D1;+0:4].F-C(-F)(-F)-S(=O)(-[O-])=[O;H0;D1;+0:5].[O;H0;D1;+0:6]=[CH;D2;+0:7]-[c:8](:[c:9]):[c:10]:[#7;a:11]:[c:12]>>[CH2;D1;+0:4]=[CH;D2;+0:3]-[C:2]-[CH;D3;+0:1](-[C:13]-[OH;D1;+0:5])-[CH;D3;+0:7](-[OH;D1;+0:6])-[c:8](:[c:9]):[c:10]:[#7;a:11]:[c:12]
null
[]
5
CELSIUS
30
MINUTE
A 1M solution of dibutylboron triflate in dichloromethane (32.7 ml) was added to a solution of A (6.28 g) in dry dichloromethane (110 ml), cooled to 5° C. under argon, followed by diisopropylethylamine (6.25 ml). The reaction mixture was stirred at 5° C. for 30 minutes and then cooled to -78° C. 3-Pyridinecarboxaldehyd...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Aldehyde.Sulfonic acid
Primary alcohol.Secondary alcohol.Allyl
null
null
c1ccncc1
HF.B
ClCCl
5
0.5
CCCC[B+]CCCC.O=Cc1cccnc1.O=S(=O)([O-])C(F)(F)F>ClCCl>C=CCC(CO)C(O)c1cccnc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9ae2160c95854c49add8e88e86c3dc61
CC(C)(CO)NC(=O)OC(C)(C)C>>CC(C)(C=O)NC(=O)OC(C)(C)C
C(=O)(OC(C)(C)C)NC(CO)(C)C.CC(=O)OI1(C=2C=CC=CC2C(=O)O1)(OC(=O)C)OC(=O)C.[OH-].[Na+]>>C(=O)(OC(C)(C)C)NC(C=O)(C)C
[CH3:1][C:2]([CH3:3])([CH2:4][OH:5])[NH:6][C:7](=[O:8])[O:9][C:10]([CH3:11])([CH3:12])[CH3:13]>>[CH3:1][C:2]([CH3:3])([CH:4]=[O:5])[NH:6][C:7](=[O:8])[O:9][C:10]([CH3:11])([CH3:12])[CH3:13]
CC(C)(CO)NC(=O)OC(C)(C)C
CC(C)(C=O)NC(=O)OC(C)(C)C
null
null
C(Cl)Cl.C(C)OCC
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
41bfa9deea81b465c88ad21fdfb64a2e1ba29490558cf430df132cb98b4a538b
0a03c6724c1862e8f86d4a463afda55b8e067dc6cb42597b472eb7cabc03eda3
null
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[#8:5]-[C:6](=[O;D1;H0:7])-[#7:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[CH2;D2;+0:12]-[OH;D1;+0:13]>>[C;D1;H3:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[#8:5]-[C:6](=[O;D1;H0:7])-[#7:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[CH;D2;+0:12]=[O;H0;D1;+0:13]
87.9
[{"value": 87.9, "product": "C(=O)(OC(C)(C)C)NC(C=O)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
The resulting N-BOC-2-amino-2-methyl-1-propanol (3.69 g, 19.5 mmol) was dissolved in methylene chloride (74 ml) and added to a stirred suspension of Dess-Martin periodinane (10.75 g, 25.35 mmol; Aldrich Chemical Company, Milwaukee, Wis.) in methylene chloride (89 ml). After stirring for 20 minutes under nitrogen, the r...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Aldehyde
null
null
null
null
C(Cl)Cl.C(C)OCC
null
0.333333
CC(C)(CO)NC(=O)OC(C)(C)C>C(Cl)Cl.C(C)OCC>CC(C)(C=O)NC(=O)OC(C)(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-478badbfe80b4ba79d32c3a102b14cc6
CC(=O)Cc1ccccc1.NCCC(=O)O>>CC(Cc1ccccc1)NCCC(=O)O
C1(=CC=CC=C1)CC(C)=O.NCCC(=O)O.C(#N)[BH3-].[Na+]>>C(=O)(O)CCNC(C)CC1=CC=CC=C1
O=[C:2]([CH3:1])[CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1.[NH2:10][CH2:11][CH2:12][C:13](=[O:14])[OH:15]>>[CH3:1][CH:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[NH:10][CH2:11][CH2:12][C:13](=[O:14])[OH:15]
CC(=O)Cc1ccccc1.NCCC(=O)O
CC(Cc1ccccc1)NCCC(=O)O
null
null
CO.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
Reductive amination with ketone
4940e8ed9a0db9bde699fdcdc3aff2cff0409c19478aa0ed1acfd98213338adf
07faf85ffe990e88a1de7fd04a339bf226f78d8bfae9712ea59eebd76bb54b9f
c1ccccc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[c:4].[NH2;D1;+0:5]-[C:6]-[C:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]>>[C;D1;H3:2]-[CH;D3;+0:1](-[C:3]-[c:4])-[NH;D2;+0:5]-[C:6]-[C:7]-[C:8](=[O;D1;H0:9])-[O;D1;H1:10]
60.2
[{"value": 60.2, "product": "C(=O)(O)CCNC(C)CC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
Phenylacetone (100 mg, 0.745 mmol) was dissolved in anhydrous methanol (2.0 ml). Beta-alanine (398 mg, 4.47 mmol) was added, followed by sodium cyanoborohydride (94 mg, 1.49 mmol). After 18 hours of stirring under nitrogen, the reaction mixture was filtered, and the filtrate solvent was removed in vacuo. The resulting ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Secondary amine
null
null
c1ccccc1
Other
CO.C(C)(=O)OCC
null
18
CC(=O)Cc1ccccc1.NCCC(=O)O>CO.C(C)(=O)OCC>CC(Cc1ccccc1)NCCC(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2356c1ff19bd4e029e4fdd495659ed04
CC(=O)Nc1ccc(O)cc1.CC(C)(Oc1ccc(N)cc1)C(=O)O>>CC(=O)Nc1ccc(OC(C)(C)C(=O)O)cc1
NC1=CC=C(OC(C(=O)O)(C)C)C=C1.C(Cl)(Cl)Cl.[OH-].[Na+].N(C(=O)C)C1=CC=C(C=C1)O.CC(=O)C>>N(C(=O)C)C1=CC=C(OC(C(=O)O)(C)C)C=C1
Oc1ccc(N[C:2]([CH3:1])=[O:3])cc1.[NH2:4][c:5]1[cH:6][cH:7][c:8]([O:9][C:10]([CH3:11])([CH3:12])[C:13](=[O:14])[OH:15])[cH:16][cH:17]1>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]([O:9][C:10]([CH3:11])([CH3:12])[C:13](=[O:14])[OH:15])[cH:16][cH:17]1
CC(=O)Nc1ccc(O)cc1.CC(C)(Oc1ccc(N)cc1)C(=O)O
CC(=O)Nc1ccc(OC(C)(C)C(=O)O)cc1
null
null
null
Acylation
OtherReaction
f0587316dec6322bc8536bc1554a2dcfb19ea5ea59546c16f81f49f5f2fb7d70
07fa0d1f4d8418421a4320317c5bccf00c4e081ec51f5368bcd2c8236c65866e
c1ccccc1
O-c1:c:c:c(-N-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]):c:c:1.[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
60
[{"value": 60.0, "product": "N(C(=O)C)C1=CC=C(OC(C(=O)O)(C)C)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
0.5
HOUR
FIG. 2A illustrates a reaction scheme for preparing 2-(4-aminophenoxy)-2-methyl propionic acid, a compound that is useful as a precursor in the preparation of Group I compounds. In accordance with the scheme of FIG. 2A, 8 grams (g) (0.2 mol) of pulverized sodium hydroxide is added to a suspension of 5.28 g (0.035 mol) ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Aromatic alcohol.Primary amine
Secondary amide
c1ccccc1
null
c1ccccc1
HO-
null
null
0.5
CC(=O)Nc1ccc(O)cc1.CC(C)(Oc1ccc(N)cc1)C(=O)O>>CC(=O)Nc1ccc(OC(C)(C)C(=O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-13b9f603fcc84708924f96e5ef9dda01
CC(=O)Nc1ccc(OC(C)(C)C(=O)O)cc1>>CC(C)(Oc1ccc(N)cc1)C(=O)O
N(C(=O)C)C1=CC=C(OC(C(=O)O)(C)C)C=C1.C(C)(=O)O>>NC1=CC=C(OC(C(=O)O)(C)C)C=C1
CC(=O)[NH:9][c:8]1[cH:7][cH:6][c:5]([O:4][C:2]([CH3:1])([CH3:3])[C:12](=[O:13])[OH:14])[cH:11][cH:10]1>>[CH3:1][C:2]([CH3:3])([O:4][c:5]1[cH:6][cH:7][c:8]([NH2:9])[cH:10][cH:11]1)[C:12](=[O:13])[OH:14]
CC(=O)Nc1ccc(OC(C)(C)C(=O)O)cc1
CC(C)(Oc1ccc(N)cc1)C(=O)O
null
null
[OH-].[K+]
Reduction
Hydrogenolysis of amides/imides/carbamates
755df58c254dea764fdda078ffd678ec540bba057c83683be04c253f1270ac7b
025f7cefe51e71668ad5d09fca32df168e9b538347403e4d5c1748073e538adc
c1ccccc1
C-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
62
[{"value": 62.0, "product": "NC1=CC=C(OC(C(=O)O)(C)C)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 61.5, "product": "NC1=CC=C(OC(C(=O)O)(C)C)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.18 g (0.005 mol) of the 2-(4-acetaminophenoxy)-2-methyl propionic acid is boiled in 10% KOH (60 ml) for 1/2 hour. The solution is then cooled and acidified with acetic acid to yield 0.6 g (62% yield) of 2-(4-aminophenoxy)-2-methyl propionic acid as a yellowish white powder, mp 214°-16° C. Conditions: See reaction.not...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
Primary amine
null
null
c1ccccc1
HO-
[OH-].[K+]
null
null
CC(=O)Nc1ccc(OC(C)(C)C(=O)O)cc1>[OH-].[K+]>CC(C)(Oc1ccc(N)cc1)C(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2138dfdaab5f4ec785968d0e14338622
CC(C)(Oc1ccc(N)cc1)C(=O)O.O=C(Cl)Cc1ccccc1>>CC(C)(Oc1ccc(NC(=O)Cc2ccccc2)cc1)C(=O)O
NC1=CC=C(OC(C(=O)O)(C)C)C=C1.C1(=CC=CC=C1)CC(=O)Cl.O.[OH-].[Na+]>>C1(=CC=CC=C1)CC(=O)NC1=CC=C(OC(C(=O)O)(C)C)C=C1
[CH3:1][C:2]([CH3:3])([O:4][c:5]1[cH:6][cH:7][c:8]([NH2:9])[cH:19][cH:20]1)[C:21](=[O:22])[OH:23].Cl[C:10](=[O:11])[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[CH3:1][C:2]([CH3:3])([O:4][c:5]1[cH:6][cH:7][c:8]([NH:9][C:10](=[O:11])[CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][cH:20]1)[C:21](=[O:2...
CC(C)(Oc1ccc(N)cc1)C(=O)O.O=C(Cl)Cc1ccccc1
CC(C)(Oc1ccc(NC(=O)Cc2ccccc2)cc1)C(=O)O
null
[OH-].[Na+]
CCOCC.O1CCCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(Cc1ccccc1)Nc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]-[c:4])-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
57.4
[{"value": 56.0, "product": "C1(=CC=CC=C1)CC(=O)NC1=CC=C(OC(C(=O)O)(C)C)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.4, "product": "C1(=CC=CC=C1)CC(=O)NC1=CC=C(OC(C(=O)O)(C)C)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
FIG. 2C illustrates a general reaction scheme for preparing the Group I 2-[4-(arylacetamido)phenoxy]-2-methyl propionic acids. In accordance with the illustrated scheme, 1 g (0.005 mol) of 2-(4-aminophenoxy)-2-methyl propionic acid is dissolved with stirring in 10 ml of water containing 0.41 g (0.1 mol) of NaOH. To thi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HCl
[OH-].[Na+].CCOCC.O1CCCC1
null
1
CC(C)(Oc1ccc(N)cc1)C(=O)O.O=C(Cl)Cc1ccccc1>[OH-].[Na+].CCOCC.O1CCCC1>CC(C)(Oc1ccc(NC(=O)Cc2ccccc2)cc1)C(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-70204c4fc8114c65865ea0d378637a4f
Nc1ccc(Cl)cc1.O=C(O)Cc1ccc(O)cc1>>O=C(Cc1cccc(O)c1)Nc1ccc(Cl)cc1
CC(=O)C.P(Cl)(Cl)(Cl)(Cl)Cl.OC1=CC=C(C=C1)CC(=O)O.ClC1=CC=C(N)C=C1>>ClC1=CC=C(NC(=O)CC=2C=C(C=CC2)O)C=C1
[NH2:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1.O[C:2](=[O:1])[CH2:3][c:4]1[cH:5][cH:10][c:8]([OH:9])[cH:7][cH:6]1>>[O:1]=[C:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([OH:9])[cH:10]1)[NH:11][c:12]1[cH:13][cH:14][c:15]([Cl:16])[cH:17][cH:18]1
Nc1ccc(Cl)cc1.O=C(O)Cc1ccc(O)cc1
O=C(Cc1cccc(O)c1)Nc1ccc(Cl)cc1
null
null
C(C)C(=O)CC.C1(=CC(=CC(=C1)C)C)C
Acylation
OtherReaction
4d66d758b08f9f828e782c8e08171e18b46fe11b590da48a7f0ca692ffa62bad
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Cc1ccccc1)Nc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c;H0;D3;+0:4]1:[cH;D2;+0:5]:[cH;D2;+0:6]:[c:7](-[O;D1;H1:8]):[c:9]:[cH;D2;+0:10]:1.[NH2;D1;+0:11]-[c:12](:[c:13]):[c:14]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C:3]-[c;H0;D3;+0:4]1:[cH;D2;+0:6]:[c:7](-[O;D1;H1:8]):[c:9]:[cH;D2;+0:10]:[cH;D2;+0:5]:1)-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14]
90
[{"value": 90.0, "product": "ClC1=CC=C(NC(=O)CC=2C=C(C=CC2)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
FIG. 6b presents a similar reaction scheme to FIG. 6a, except that 3- rather than 4-hydroxyphenylacetic acid (HPAA) is used as the precursor material so that the final compound has a meta rather than a para substitution. In addition, rather than reacting with acetone (dimethyl ketone) a diethyl ketone is used to positi...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
C(C)C(=O)CC.C1(=CC(=CC(=C1)C)C)C
null
2
Nc1ccc(Cl)cc1.O=C(O)Cc1ccc(O)cc1>C(C)C(=O)CC.C1(=CC(=CC(=C1)C)C)C>O=C(Cc1cccc(O)c1)Nc1ccc(Cl)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c5f43a80403f4b4babc1305c8508f598
CN(C)C1C(=O)C(C(N)=O)=C(O)C2(O)C(=O)C3=C(O)c4c(O)cccc4CC3CC12.O=C1CCC(=O)N1Br>>CN(C)C1C(O)=C(C(N)=O)C(=O)C2(O)C(O)=C3C(=O)c4c(O)ccc(Br)c4CC3CC12
S(O)(O)(=O)=O.CN(C)C1C2CC3CC4=C(C(=CC=C4)O)C(=C3C(=O)C2(C(=C(C1=O)C(=O)N)O)O)O.BrN1C(CCC1=O)=O.C(C)OCC>>S(=O)(=O)(O)O.BrC1=C2CC3CC4C(C(=C(C(C4(C(=C3C(C2=C(C=C1)O)=O)O)O)=O)C(=O)N)O)N(C)C
[CH3:1][N:2]([CH3:3])[CH:4]1[C:5](=[O:6])[C:7]([C:8]([NH2:9])=[O:10])=[C:11]([OH:12])[C:13]2([OH:14])[C:15](=[O:16])[C:17]3=[C:18]([OH:19])[c:20]4[c:21]([OH:22])[cH:23][cH:24][cH:25][c:27]4[CH2:28][CH:29]3[CH2:30][CH:31]12.O=C1CCC(=O)N1[Br:26]>>[CH3:1][N:2]([CH3:3])[CH:4]1[C:5]([OH:6])=[C:7]([C:8]([NH2:9])=[O:10])[C:11...
CN(C)C1C(=O)C(C(N)=O)=C(O)C2(O)C(=O)C3=C(O)c4c(O)cccc4CC3CC12.O=C1CCC(=O)N1Br
CN(C)C1C(O)=C(C(N)=O)C(=O)C2(O)C(O)=C3C(=O)c4c(O)ccc(Br)c4CC3CC12
null
null
null
Acylation
OtherReaction
067f4bf724c6e44fe372eb2fec6145982ef9256ce32da29996886b4531327f93
fe885760af681fc3d379e2235d0034d8359ce2474dcf96974b27a7acba880032
O=C1C2=CC3C(=O)C=CCC3CC2Cc2ccccc21
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[#7:2]-[C:3]1-[C:4]2-[C:5]-[C:6]3-[C:7]-[c:8]4:[cH;D2;+0:9]:[c:10]:[c:11]:[c:12]:[c:13]:4-[C;H0;D3;+0:14](-[OH;D1;+0:15])=[C;H0;D3;+0:16]-3-[C;H0;D3;+0:17](=[O;H0;D1;+0:18])-[C:19]-2(-[O;D1;H1:20])-[C;H0;D3;+0:21](-[OH;D1;+0:22])=[C;H0;D3;+0:23](-[C:24](-[N;D1;H2:25])=[O;D1;H0:26])-[C...
null
[]
0
CELSIUS
45
MINUTE
A solution of 4.14. g of 6-demethyl-6-deoxytetracycline, prepared by the described literature procedure, and 1.99 g of N-bromosuccinimide dissolved in 50 ml of concentrated sulfuric acid is stirred at 0° C. for 45 minutes or until solution occurs. The reaction mixture is added dropwise to 2 L of cold diethyl ether. The...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Tertiary amide.Tertiary amide.Enol.Enol
Aromatic halide.Ketone.Ketone.Enol.Enol
C1=CC2CC3=Cc4ccccc4CC3CC2CC1.C1CCNC1
C1=CCC2CC3Cc4ccccc4CC3=CC2C1
C1=CCC2CC3Cc4ccccc4CC3=CC2C1
HO-
null
0
0.75
CN(C)C1C(=O)C(C(N)=O)=C(O)C2(O)C(=O)C3=C(O)c4c(O)cccc4CC3CC12.O=C1CCC(=O)N1Br>>CN(C)C1C(O)=C(C(N)=O)C(=O)C2(O)C(O)=C3C(=O)c4c(O)ccc(Br)c4CC3CC12
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bbaa095270804d84806076369776a1e2
C1=CCCC1.Cl[SiH](Cl)Cl>>Cl[Si](Cl)(Cl)C1CCCC1
C1=CCCC1.Cl[SiH](Cl)Cl.C(C)(C)O>>C1(CCCC1)[Si](Cl)(Cl)Cl
[CH:5]1=[CH:9][CH2:8][CH2:7][CH2:6]1.[Cl:1][SiH:2]([Cl:3])[Cl:4]>>[Cl:1][Si:2]([Cl:3])([Cl:4])[CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9]1
C1=CCCC1.Cl[SiH](Cl)Cl
Cl[Si](Cl)(Cl)C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
null
Miscellaneous
OtherReaction
973dc51cc8732bf0bda1491fded43c0890bf4aedb1728cf351a967b36f591bfa
ebe950a4f1214ee7787c0782c7e3e1a5d4a0740c23df8283e2cc604317625e61
C1CCCC1
[C:1]1-[C:2]-[C:3]-[CH;D2;+0:4]=[CH;D2;+0:5]-1.[Cl;D1;H0:6]-[SiH;D3;+0:7](-[Cl;D1;H0:8])-[Cl;D1;H0:9]>>[Cl;D1;H0:6]-[Si;H0;D4;+0:7](-[Cl;D1;H0:8])(-[Cl;D1;H0:9])-[CH;D3;+0:5]1-[C:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-1
null
[]
150
CELSIUS
30
MINUTE
In a 100 ml autoclave were charged 16.7 g (0.245 mole) of cyclopentene, 30.1 g (0.222 mole) of trichlorosilane and 25 μl of a 0.077 m mole/ml chloroplatinic acid solution in isopropyl alcohol (platinum content 1.92×10-6 mole), which were then stirred at 150° C. for 30 minutes. Cyclopentyl trichlorosilane was obtained q...
10.6084/m9.figshare.5104873.v1
null
null
Silyl protective group
C1=CCCC1
C1CCCC1
C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
150
0.5
C1=CCCC1.Cl[SiH](Cl)Cl>[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl>Cl[Si](Cl)(Cl)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-10db705dac8b406da8c9efae3471dda0
CCC(C)O.CO[Si](OC)(OC)C1CCCC1>>CCC(C)O[Si](OC)(OC)C1CCCC1
C1(CCCC1)[Si](OC)(OC)OC.C(C)(CC)O.C[Si](Cl)(C)C>>C(C)(CC)O[Si](OC)(OC)C1CCCC1
[CH3:1][CH2:2][CH:3]([CH3:4])[OH:5].CO[Si:6]([O:7][CH3:8])([O:9][CH3:10])[CH:11]1[CH2:12][CH2:13][CH2:14][CH2:15]1>>[CH3:1][CH2:2][CH:3]([CH3:4])[O:5][Si:6]([O:7][CH3:8])([O:9][CH3:10])[CH:11]1[CH2:12][CH2:13][CH2:14][CH2:15]1
CCC(C)O.CO[Si](OC)(OC)C1CCCC1
CCC(C)O[Si](OC)(OC)C1CCCC1
null
C[O-].[Na+]
null
Protection
OtherReaction
ea139b3cb6171a748fbc881d815cc598a14c6b8245b87168b4a15a10e325f24c
1e2a25dd539d267852f3b05b92dd4080ece1d4c7abb9db1b6fd2b64d2b33a864
C1CCCC1
C-O-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8].[C:9]-[C:10](-[C;D1;H3:11])-[OH;D1;+0:12]>>[C:7]-[C:6](-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[O;H0;D2;+0:12]-[C:10](-[C:9])-[C;D1;H3:11])-[C:8]
84.3
[{"value": 84.0, "product": "C(C)(CC)O[Si](OC)(OC)C1CCCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.3, "product": "C(C)(CC)O[Si](OC)(OC)C1CCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In a 100 ml three-neck flask provided with a magnetic stirrer were charged 10.3 g (0.0542 mole) of cyclopentyl trimethoxysilane, 40.3 g (0.543 mole) of sec-butyl alcohol and 33.7 mg (0.625 m mole) of sodium methoxide, which were then reacted with each other at room temperature for 2 hours under stirring. Then, trimethy...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
Silyl protective group
null
null
C1CCCC1
HO-
C[O-].[Na+]
null
null
CCC(C)O.CO[Si](OC)(OC)C1CCCC1>C[O-].[Na+]>CCC(C)O[Si](OC)(OC)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dfdccf328d594417823f1d891b869737
CO[Si](OC)(OC)C1CCCC1.OC1CCCCC1>>CO[Si](OC)(OC1CCCCC1)C1CCCC1
C1(CCCC1)[Si](OC)(OC)OC.C1(CCCCC1)O>>C1(CCCCC1)O[Si](OC)(OC)C1CCCC1
CO[Si:3]([O:2][CH3:1])([O:4][CH3:5])[CH:13]1[CH2:14][CH2:15][CH2:16][CH2:17]1.[OH:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][CH2:12]1>>[CH3:1][O:2][Si:3]([O:4][CH3:5])([O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][CH2:12]1)[CH:13]1[CH2:14][CH2:15][CH2:16][CH2:17]1
CO[Si](OC)(OC)C1CCCC1.OC1CCCCC1
CO[Si](OC)(OC1CCCCC1)C1CCCC1
null
C[O-].[Na+]
null
Protection
OtherReaction
ea139b3cb6171a748fbc881d815cc598a14c6b8245b87168b4a15a10e325f24c
1e2a25dd539d267852f3b05b92dd4080ece1d4c7abb9db1b6fd2b64d2b33a864
C1CCC(O[SiH2]C2CCCC2)CC1
C-O-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8].[C:9]-[C:10](-[OH;D1;+0:11])-[C:12]>>[C:9]-[C:10](-[O;H0;D2;+0:11]-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8])-[C:12]
83.3
[{"value": 83.0, "product": "C1(CCCCC1)O[Si](OC)(OC)C1CCCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 83.3, "product": "C1(CCCCC1)O[Si](OC)(OC)C1CCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedures of Example 2 were repeated with the exception that 10.0 g (0.0526 mole) of cyclopentyl trimethoxysilane, 85.1 mg (1.58 m mole) of sodium methoxide, and 52.7 g (0.526 mole) of cyclohexanol in place of sec-butyl alcohol were used and the reaction time was one and a half hours. Then, 11.3 g (0.0438 mole) of...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
Silyl protective group
null
null
C1CCCCC1.C1CCCC1
HO-
C[O-].[Na+]
null
null
CO[Si](OC)(OC)C1CCCC1.OC1CCCCC1>C[O-].[Na+]>CO[Si](OC)(OC1CCCCC1)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-db48ca45905a4ffa943827bd251f129c
C1=CCCC1.Cl[SiH](Cl)Cl>>Cl[Si](Cl)(Cl)C1CCCC1
C1=CCCC1.Cl[SiH](Cl)Cl.C(C)(C)O>>C1(CCCC1)[Si](Cl)(Cl)Cl
[CH:5]1=[CH:9][CH2:8][CH2:7][CH2:6]1.[Cl:1][SiH:2]([Cl:3])[Cl:4]>>[Cl:1][Si:2]([Cl:3])([Cl:4])[CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9]1
C1=CCCC1.Cl[SiH](Cl)Cl
Cl[Si](Cl)(Cl)C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
null
Miscellaneous
OtherReaction
973dc51cc8732bf0bda1491fded43c0890bf4aedb1728cf351a967b36f591bfa
ebe950a4f1214ee7787c0782c7e3e1a5d4a0740c23df8283e2cc604317625e61
C1CCCC1
[C:1]1-[C:2]-[C:3]-[CH;D2;+0:4]=[CH;D2;+0:5]-1.[Cl;D1;H0:6]-[SiH;D3;+0:7](-[Cl;D1;H0:8])-[Cl;D1;H0:9]>>[Cl;D1;H0:6]-[Si;H0;D4;+0:7](-[Cl;D1;H0:8])(-[Cl;D1;H0:9])-[CH;D3;+0:5]1-[C:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-1
null
[]
150
CELSIUS
30
MINUTE
In a 100 ml autoclave were charged 13.5 g (0.198 mole) of cyclopentene, 24.4 g (0.180 mole) of trichlorosilane and 25 μl of a 0.077 m mole/ml chloroplatinic acid solution in isopropyl alcohol (platinum content 1.92×10-6 mole), which were then stirred at 150° C. for 30 minutes. Cyclopentyl trichlorosilane was obtained q...
10.6084/m9.figshare.5104873.v1
null
null
Silyl protective group
C1=CCCC1
C1CCCC1
C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
150
0.5
C1=CCCC1.Cl[SiH](Cl)Cl>[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl>Cl[Si](Cl)(Cl)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-44523718c32f4f8db78be90afe1a804e
CCC(C)(C)O.CO[Si](OC)(OC)C1CCCC1>>CCC(C)(C)O[Si](OC)(OC)C1CCCC1
C1(CCCC1)[Si](OC)(OC)OC.C(C)(C)(CC)O.C[Si](Cl)(C)C>>C(C)(C)(CC)O[Si](OC)(OC)C1CCCC1
[CH3:1][CH2:2][C:3]([CH3:4])([CH3:5])[OH:6].CO[Si:7]([O:8][CH3:9])([O:10][CH3:11])[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1>>[CH3:1][CH2:2][C:3]([CH3:4])([CH3:5])[O:6][Si:7]([O:8][CH3:9])([O:10][CH3:11])[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1
CCC(C)(C)O.CO[Si](OC)(OC)C1CCCC1
CCC(C)(C)O[Si](OC)(OC)C1CCCC1
null
C[O-].[Na+]
null
Protection
OtherReaction
9769bfd0e2301823e43c8e03cbd04c370095023efd8ba0f40deaf2a30665c67c
d4f7fc2e4845ce90b51777d3c64652d4a3aab88a89713e59aada938381b9c2e3
C1CCCC1
C-O-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8].[C:9]-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[OH;D1;+0:13]>>[C:7]-[C:6](-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[O;H0;D2;+0:13]-[C:10](-[C:9])(-[C;D1;H3:11])-[C;D1;H3:12])-[C:8]
82
[{"value": 82.0, "product": "C(C)(C)(CC)O[Si](OC)(OC)C1CCCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.7, "product": "C(C)(C)(CC)O[Si](OC)(OC)C1CCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In a 100 ml three-neck flask provided with a magnetic stirrer and a reflux condenser were charged 10.1 g (0.0531 mole) of cyclopentyl trimethoxysilane, 30.6 g (0.347 mole) of tert-amyl alcohol and 86.4 mg (1.6 m mole) of sodium methoxide, which were then reacted with each other in an oil bath of 105° C. for 4 hours und...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol.Silyl protective group
Silyl protective group
null
null
C1CCCC1
HO-
C[O-].[Na+]
null
null
CCC(C)(C)O.CO[Si](OC)(OC)C1CCCC1>C[O-].[Na+]>CCC(C)(C)O[Si](OC)(OC)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e4a11d3163094ac6b8aeb21c55a2d94d
C1=CCCC1.Cl[SiH](Cl)Cl>>Cl[Si](Cl)(Cl)C1CCCC1
C1=CCCC1.Cl[SiH](Cl)Cl.C(C)(C)O>>C1(CCCC1)[Si](Cl)(Cl)Cl
[CH:5]1=[CH:9][CH2:8][CH2:7][CH2:6]1.[Cl:1][SiH:2]([Cl:3])[Cl:4]>>[Cl:1][Si:2]([Cl:3])([Cl:4])[CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9]1
C1=CCCC1.Cl[SiH](Cl)Cl
Cl[Si](Cl)(Cl)C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
null
Miscellaneous
OtherReaction
973dc51cc8732bf0bda1491fded43c0890bf4aedb1728cf351a967b36f591bfa
ebe950a4f1214ee7787c0782c7e3e1a5d4a0740c23df8283e2cc604317625e61
C1CCCC1
[C:1]1-[C:2]-[C:3]-[CH;D2;+0:4]=[CH;D2;+0:5]-1.[Cl;D1;H0:6]-[SiH;D3;+0:7](-[Cl;D1;H0:8])-[Cl;D1;H0:9]>>[Cl;D1;H0:6]-[Si;H0;D4;+0:7](-[Cl;D1;H0:8])(-[Cl;D1;H0:9])-[CH;D3;+0:5]1-[C:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-1
null
[]
150
CELSIUS
30
MINUTE
In a 100 ml autoclave were charged 13.9 g (0.204 mole) of cyclopentene, 25.1 g (0.185 mole) of trichlorosilane and 25 μl of a 0.077 m mole/ml chloroplatinic acid solution in isopropyl alcohol (platinum content 1.92×10-6 mole), which were then stirred at 150° C. for 30 minutes. Cyclopentyl trichlorosilane was obtained q...
10.6084/m9.figshare.5104873.v1
null
null
Silyl protective group
C1=CCCC1
C1CCCC1
C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
150
0.5
C1=CCCC1.Cl[SiH](Cl)Cl>[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl>Cl[Si](Cl)(Cl)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-26d59802162f454b919e6a3c67915737
CO[Si](OC)(OC)C1CCCC1.OC1CCCC1>>CO[Si](OC)(OC1CCCC1)C1CCCC1
C1(CCCC1)[Si](OC)(OC)OC.C1(CCCC1)O.C[Si](Cl)(C)C>>C1(CCCC1)O[Si](OC)(OC)C1CCCC1
CO[Si:3]([O:2][CH3:1])([O:4][CH3:5])[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1.[OH:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11]1>>[CH3:1][O:2][Si:3]([O:4][CH3:5])([O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11]1)[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1
CO[Si](OC)(OC)C1CCCC1.OC1CCCC1
CO[Si](OC)(OC1CCCC1)C1CCCC1
null
C[O-].[Na+]
null
Protection
OtherReaction
ea139b3cb6171a748fbc881d815cc598a14c6b8245b87168b4a15a10e325f24c
1e2a25dd539d267852f3b05b92dd4080ece1d4c7abb9db1b6fd2b64d2b33a864
C1CCC(O[SiH2]C2CCCC2)C1
C-O-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8].[C:9]-[C:10](-[OH;D1;+0:11])-[C:12]>>[C:9]-[C:10](-[O;H0;D2;+0:11]-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8])-[C:12]
85.1
[{"value": 85.0, "product": "C1(CCCC1)O[Si](OC)(OC)C1CCCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.1, "product": "C1(CCCC1)O[Si](OC)(OC)C1CCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In a 50 ml three-neck flask provided with a magnetic stirrer and a reflux condenser were charged 5.0 g (0.0262 mole) of cyclopentyl trimethoxysilane, 22.5 g (0.262 mole) of cyclopentyl alcohol and 18.6 mg (0.34 m mole) of sodium methoxide, which were then reacted with each other at room temperature for 2 hours under st...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
Silyl protective group
null
null
C1CCCC1.C1CCCC1
HO-
C[O-].[Na+]
null
null
CO[Si](OC)(OC)C1CCCC1.OC1CCCC1>C[O-].[Na+]>CO[Si](OC)(OC1CCCC1)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9bcc3d835c564b278f0acc655903f697
C1=CCCC1.Cl[SiH](Cl)Cl>>Cl[Si](Cl)(Cl)C1CCCC1
C1=CCCC1.Cl[SiH](Cl)Cl.C(C)(C)O>>C1(CCCC1)[Si](Cl)(Cl)Cl
[CH:5]1=[CH:9][CH2:8][CH2:7][CH2:6]1.[Cl:1][SiH:2]([Cl:3])[Cl:4]>>[Cl:1][Si:2]([Cl:3])([Cl:4])[CH:5]1[CH2:6][CH2:7][CH2:8][CH2:9]1
C1=CCCC1.Cl[SiH](Cl)Cl
Cl[Si](Cl)(Cl)C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
null
Miscellaneous
OtherReaction
973dc51cc8732bf0bda1491fded43c0890bf4aedb1728cf351a967b36f591bfa
ebe950a4f1214ee7787c0782c7e3e1a5d4a0740c23df8283e2cc604317625e61
C1CCCC1
[C:1]1-[C:2]-[C:3]-[CH;D2;+0:4]=[CH;D2;+0:5]-1.[Cl;D1;H0:6]-[SiH;D3;+0:7](-[Cl;D1;H0:8])-[Cl;D1;H0:9]>>[Cl;D1;H0:6]-[Si;H0;D4;+0:7](-[Cl;D1;H0:8])(-[Cl;D1;H0:9])-[CH;D3;+0:5]1-[C:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-1
null
[]
150
CELSIUS
30
MINUTE
In a 100 ml autoclave were charged 13.7 g (0.201 mole) of cyclopentene, 24.8 g (0.183 mole) of trichlorosilane and 25 μl of a 0.077 m mole/ml chloroplatinic acid solution in isopropyl alcohol (platinum content 1.92×10-6 mole), which were then stirred at 150° C. for 30 minutes. Cyclopentyl trichlorosilane was obtained q...
10.6084/m9.figshare.5104873.v1
null
null
Silyl protective group
C1=CCCC1
C1CCCC1
C1CCCC1
null
[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl
150
0.5
C1=CCCC1.Cl[SiH](Cl)Cl>[H+].[H+].Cl[Pt-2](Cl)(Cl)(Cl)(Cl)Cl>Cl[Si](Cl)(Cl)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4f67e89866a749378b2de7b9b7e24fbf
CO[Si](OC)(OC)C1CCCC1.OC1CCOC1>>CO[Si](OC)(OC1CCOC1)C1CCCC1
C1(CCCC1)[Si](OC)(OC)OC.OC1COCC1.C[Si](Cl)(C)C>>C1(CCCC1)[Si](OC1COCC1)(OC)OC
CO[Si:3]([O:2][CH3:1])([O:4][CH3:5])[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1.[OH:6][CH:7]1[CH2:8][CH2:9][O:10][CH2:11]1>>[CH3:1][O:2][Si:3]([O:4][CH3:5])([O:6][CH:7]1[CH2:8][CH2:9][O:10][CH2:11]1)[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16]1
CO[Si](OC)(OC)C1CCCC1.OC1CCOC1
CO[Si](OC)(OC1CCOC1)C1CCCC1
null
C[O-].[Na+]
null
Protection
OtherReaction
ea139b3cb6171a748fbc881d815cc598a14c6b8245b87168b4a15a10e325f24c
1e2a25dd539d267852f3b05b92dd4080ece1d4c7abb9db1b6fd2b64d2b33a864
C1CCC([SiH2]OC2CCOC2)C1
C-O-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8].[#8:9]-[C:10]-[C:11](-[OH;D1;+0:12])-[C:13]>>[#8:9]-[C:10]-[C:11](-[O;H0;D2;+0:12]-[Si;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6](-[C:7])-[C:8])-[C:13]
54
[{"value": 54.0, "product": "C1(CCCC1)[Si](OC1COCC1)(OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.0, "product": "C1(CCCC1)[Si](OC1COCC1)(OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In a 100 ml three-neck flask provided with a magnetic stirrer and a reflux condenser were charged 7.7 g (0.0404 mole) of cyclopentyl trimethoxysilane, 35.7 g (0.405 mole) of 3-hydroxy tetrahydrofurane and 53.0 mg (0.98 m mole) of sodium methoxide, which were then reacted with each other in an oil bath of 80° C. for 2 h...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
Silyl protective group
null
null
C1CCOC1.C1CCCC1
HO-
C[O-].[Na+]
null
null
CO[Si](OC)(OC)C1CCCC1.OC1CCOC1>C[O-].[Na+]>CO[Si](OC)(OC1CCOC1)C1CCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a09f60cece474e8a9b8d9edbc056d2df
O=C(Cl)Cl.O=C(c1ccccc1)c1ccc(O)cc1>>O=C(Cl)c1ccc(C(=O)c2ccccc2)cc1
C(=O)(Cl)Cl.C(=O)(Cl)Cl.C(=O)(Cl)Cl.OC1=CC=C(C(=O)C2=CC=CC=C2)C=C1>>ClC(=O)C1=CC=C(C(=O)C2=CC=CC=C2)C=C1
Cl[C:2](=[O:1])[Cl:3].O[c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[cH:16][cH:17]1>>[O:1]=[C:2]([Cl:3])[c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[cH:16][cH:17]1
O=C(Cl)Cl.O=C(c1ccccc1)c1ccc(O)cc1
O=C(Cl)c1ccc(C(=O)c2ccccc2)cc1
null
[Cl-].C(C1=CC=CC=C1)[N+](C)(C)C
CC=1C=CC=CC1C
C-C Coupling
OtherReaction
1a9a73072b79f12d8d265f2cb995c58c1597c5e5abba004b3080381ef79885e5
ef72d272f34893178d8f33792eb77b63ee817d1a04f49561ae829111b8207762
O=C(c1ccccc1)c1ccccc1
Cl-[C;H0;D3;+0:1](-[Cl;D1;H0:2])=[O;D1;H0:3].O-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]>>[Cl;D1;H0:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[c;H0;D3;+0:4](:[c:5]:[c:6]):[c:7]:[c:8]
99.2
[{"value": 93.0, "product": "ClC(=O)C1=CC=C(C(=O)C2=CC=CC=C2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.2, "product": "ClC(=O)C1=CC=C(C(=O)C2=CC=CC=C2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A total of 3.4 kg of phosgene were passed in the course of 5 hours into a solution of 4 kg of 4-hydroxybenzophenone and 190 g of benzyltrimethylammonium chloride in 11.4 kg of o-xylene. During this time, the internal temperature was increased from 95° to 1200° C. After the end of the introduction of phosgene, stirring ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Aromatic alcohol
Acyl halide
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HCl
[Cl-].C(C1=CC=CC=C1)[N+](C)(C)C.CC=1C=CC=CC1C
null
0.5
O=C(Cl)Cl.O=C(c1ccccc1)c1ccc(O)cc1>[Cl-].C(C1=CC=CC=C1)[N+](C)(C)C.CC=1C=CC=CC1C>O=C(Cl)c1ccc(C(=O)c2ccccc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-acde304896214d548673d4710d7c0098
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Br)cc1>>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Br)cc2)OC(C)(C)O1
O.BrC1=CC=C(C=C1)S(=O)(=O)Cl.OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.C(C)N(CC)CC>>BrC1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][OH:13])[O:24][C:25]([CH3:26])([CH3:27])[O:28]1.Cl[S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][c:20]([Br:21])[cH:22][cH:23]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][O:13][S:14](=[...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Br)cc1
CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Br)cc2)OC(C)(C)O1
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
76a2f1ce13fb019af608455a0d79fe83b29c455d623b278b739d67e5b567ea89
e7708aa65b3d8696add9aec26cae169160bb027d6d2772db2030dd9c0b07b540
O=S(=O)(OC[C@@H]1CCOCO1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#8:7]-[C:8]-[C:9]-[OH;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[O;H0;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
144.4
[{"value": 144.4, "product": "BrC1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
To a stirring, 20°-25° C. solution of the (4R-cis)-1,1-dimethylethyl 6-hydroxymethyl-2,2 dimethyl-1,3- dioxane-4-acetate (European Patent Application 0319,847) (10 g, 38 mmol) in methylene chloride) (250 mL) containing triethylamine (10 mL, 72 mmol) is added 4-bromobenzenesulfonyl chloride (15 g, 57.5 mmol). Stirring i...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Sulfonate
null
null
C1COCOC1.c1ccccc1
HCl
C(Cl)Cl
null
20
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Br)cc1>C(Cl)Cl>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Br)cc2)OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2023d8b66fd14bfc92a109f8fab6f737
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Cl)cc1>>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Cl)cc2)OC(C)(C)O1
O.ClC1=CC=C(C=C1)S(=O)(=O)Cl.OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.C(C)N(CC)CC>>ClC1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][OH:13])[O:24][C:25]([CH3:26])([CH3:27])[O:28]1.Cl[S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][c:20]([Cl:21])[cH:22][cH:23]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][O:13][S:14](=[...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Cl)cc1
CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Cl)cc2)OC(C)(C)O1
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
76a2f1ce13fb019af608455a0d79fe83b29c455d623b278b739d67e5b567ea89
e7708aa65b3d8696add9aec26cae169160bb027d6d2772db2030dd9c0b07b540
O=S(=O)(OC[C@@H]1CCOCO1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#8:7]-[C:8]-[C:9]-[OH;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[O;H0;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
130.1
[{"value": 130.1, "product": "ClC1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2.5
HOUR
To a stirring, 0°-5° C. solution of the (4R-cis)-1,1-dimethylethyl 6-hydroxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate (European Patent Application 0319,847) (10 g, 38 mmol) in methylene chloride (250 mL) containing triethylamine (10 mL, 72 mmol) is added 4-chlorobenzenesulfonyl chloride (12.7 g, 60 mmol). Stirring is c...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Sulfonate
null
null
C1COCOC1.c1ccccc1
HCl
C(Cl)Cl
null
2.5
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Cl)cc1>C(Cl)Cl>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Cl)cc2)OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1a1f349b82e5444490349d675368ebff
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1cc(Cl)ccc1Cl>>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2cc(Cl)ccc2Cl)OC(C)(C)O1
O.ClC1=C(C=C(C=C1)Cl)S(=O)(=O)Cl.OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.C(C)N(CC)CC>>ClC1=C(C=C(C=C1)Cl)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][OH:13])[O:25][C:26]([CH3:27])([CH3:28])[O:29]1.Cl[S:14](=[O:15])(=[O:16])[c:17]1[cH:18][c:19]([Cl:20])[cH:21][cH:22][c:23]1[Cl:24]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][O:13][S:...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1cc(Cl)ccc1Cl
CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2cc(Cl)ccc2Cl)OC(C)(C)O1
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
76a2f1ce13fb019af608455a0d79fe83b29c455d623b278b739d67e5b567ea89
e7708aa65b3d8696add9aec26cae169160bb027d6d2772db2030dd9c0b07b540
O=S(=O)(OC[C@@H]1CCOCO1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#8:7]-[C:8]-[C:9]-[OH;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[O;H0;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
137.9
[{"value": 137.9, "product": "ClC1=C(C=C(C=C1)Cl)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3.5
HOUR
To a stirring 0°-5° C. solution of the (4R-cis)-1,1-dimethylethyl 6-hydroxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate (European Patent Application 0319,847) (10 g, 38 mmol) in methylene chloride (250 mL) containing triethylamine (10 mL, 72 mmol) is added 2,5-dichlorobenzenesulfonyl chloride (14.7 g, 57.5 mmol). Stirring...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Sulfonate
null
null
C1COCOC1.c1ccccc1
HCl
C(Cl)Cl
null
3.5
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1cc(Cl)ccc1Cl>C(Cl)Cl>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2cc(Cl)ccc2Cl)OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f0db01e0d32e4cd2b57589e37275a000
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=[N+]([O-])c1ccccc1S(=O)(=O)Cl>>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccccc2[N+](=O)[O-])OC(C)(C)O1
[N+](=O)([O-])C1=C(C=CC=C1)S(=O)(=O)Cl.OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.C(C)N(CC)CC.O.[N+](=O)([O-])C1=C(C=CC=C1)S(=O)(=O)Cl>>[N+](=O)([O-])C1=C(C=CC=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][OH:13])[O:26][C:27]([CH3:28])([CH3:29])[O:30]1.Cl[S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[N+:23](=[O:24])[O-:25]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=[N+]([O-])c1ccccc1S(=O)(=O)Cl
CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccccc2[N+](=O)[O-])OC(C)(C)O1
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
76a2f1ce13fb019af608455a0d79fe83b29c455d623b278b739d67e5b567ea89
e7708aa65b3d8696add9aec26cae169160bb027d6d2772db2030dd9c0b07b540
O=S(=O)(OC[C@@H]1CCOCO1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#8:7]-[C:8]-[C:9]-[OH;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[O;H0;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
122.9
[{"value": 122.9, "product": "[N+](=O)([O-])C1=C(C=CC=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a stirring 20°-25° C. solution of the (4R cis)-1,1-dimethylethyl 6-hydroxymethyl-2,2-dimethyl -1,3-dioxane-4-acetate (European Patent Application 0319,847) (10 g, 0.038 mol) in methylene chloride (250 mL) containing triethylamine (7 mL, 0.05 mol) is added 2-nitrobenzenesulfonyl chloride (9.8 g, 0.043 mol). Stirring ...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Sulfonate
null
null
C1COCOC1.c1ccccc1
HCl
C(Cl)Cl
null
24
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=[N+]([O-])c1ccccc1S(=O)(=O)Cl>C(Cl)Cl>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccccc2[N+](=O)[O-])OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a12e310df1644252937b6e4ef4818172
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=[N+]([O-])c1ccc(S(=O)(=O)Cl)cc1>>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc([N+](=O)[O-])cc2)OC(C)(C)O1
O.[N+](=O)([O-])C1=CC=C(C=C1)S(=O)(=O)Cl.OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.C(C)N(CC)CC>>[N+](=O)([O-])C1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][OH:13])[O:26][C:27]([CH3:28])([CH3:29])[O:30]1.Cl[S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][c:20]([N+:21](=[O:22])[O-:23])[cH:24][cH:25]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=[N+]([O-])c1ccc(S(=O)(=O)Cl)cc1
CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc([N+](=O)[O-])cc2)OC(C)(C)O1
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
76a2f1ce13fb019af608455a0d79fe83b29c455d623b278b739d67e5b567ea89
e7708aa65b3d8696add9aec26cae169160bb027d6d2772db2030dd9c0b07b540
O=S(=O)(OC[C@@H]1CCOCO1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#8:7]-[C:8]-[C:9]-[OH;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[O;H0;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
110.5
[{"value": 110.5, "product": "[N+](=O)([O-])C1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
22
HOUR
To a stirring 20°-25° C. solution of the (4R-cis)-1,1-dimethylethyl 6-hydroxymethyl-2,2-dimethyl-1,3- dioxane-4-acetate (European Patent Application 0319,847) (10 g, 0.038 mol) in methylene chloride (250 mL) containing triethylamine (7 mL, 0.05 mol) is added 4-nitrobenzenesulfonyl chloride (10.5 g, 43 mmol). Stirring i...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Sulfonate
null
null
C1COCOC1.c1ccccc1
HCl
C(Cl)Cl
null
22
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=[N+]([O-])c1ccc(S(=O)(=O)Cl)cc1>C(Cl)Cl>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc([N+](=O)[O-])cc2)OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-25c2d201df154c4a8596ac428de335f8
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Cl)cc1>>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Cl)cc2)OC(C)(C)O1
O.ClC1=CC=C(C=C1)S(=O)(=O)Cl.OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.C(C)N(CC)CC>>ClC1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][OH:13])[O:24][C:25]([CH3:26])([CH3:27])[O:28]1.Cl[S:14](=[O:15])(=[O:16])[c:17]1[cH:18][cH:19][c:20]([Cl:21])[cH:22][cH:23]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][O:13][S:14](=[...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Cl)cc1
CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Cl)cc2)OC(C)(C)O1
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
76a2f1ce13fb019af608455a0d79fe83b29c455d623b278b739d67e5b567ea89
e7708aa65b3d8696add9aec26cae169160bb027d6d2772db2030dd9c0b07b540
O=S(=O)(OC[C@@H]1CCOCO1)c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[#8:7]-[C:8]-[C:9]-[OH;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[O;H0;D2;+0:10]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
130.1
[{"value": 130.1, "product": "ClC1=CC=C(C=C1)S(=O)(=O)OC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2.5
HOUR
To a stirring, 0°-5° C. solution of the (4R-cis)-1,1-dimethylethyl 6-hydroxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate (European Patent Application 0319,847) (10 g, 38 mmol) in methylene chloride (250 mL) containing triethylamine (10 mL, 72 mmol) is added 4-chlorobenzenesulfonyl chloride (12.7 g, 60 mmol). Stirring is c...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Sulfonate
null
null
C1COCOC1.c1ccccc1
HCl
C(Cl)Cl
null
2.5
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CO)OC(C)(C)O1.O=S(=O)(Cl)c1ccc(Cl)cc1>C(Cl)Cl>CC(C)(C)OC(=O)C[C@H]1C[C@@H](COS(=O)(=O)c2ccc(Cl)cc2)OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4431975f4b2f4be985331eb77f3e56b1
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CC#N)OC(C)(C)O1>>CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1
C(#N)C[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.N.[H][H]>>NCC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][C:13]#[N:14])[O:15][C:16]([CH3:17])([CH3:18])[O:19]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH2:8][C@H:9]1[CH2:10][C@@H:11]([CH2:12][CH2:13][NH2:14])[O:15][C:16]([CH3:17])([CH3:18])[O:19]1
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CC#N)OC(C)(C)O1
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1
null
[Ni]
CO
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
C1COCOC1
[#8:1]-[C:2]-[C:3]-[C;H0;D2;+0:4]#[N;H0;D1;+0:5]>>[#8:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[NH2;D1;+0:5]
null
[]
null
null
16
HOUR
A solution of (4R-cis)-1,1-dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate, (Example 1) 5.63 g (0.048 mol), in 100 mL of methanol saturated with gaseous ammonia is treated with 0.5 g of Raney nickel #30 and hydrogen gas in a shaker at 50 pounds per square inch (psi) and 40° C. After 16 hours, thin layer ...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
C1COCOC1
null
[Ni].CO
null
16
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CC#N)OC(C)(C)O1>[Ni].CO>CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-274e1321147e44d895be1b035e36de0f
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1.CC(C)C(=O)C(C(=O)Nc1ccccc1)C(C(=O)c1ccc(F)cc1)c1ccccc1>>CC(C)c1c(C(=O)Nc2ccccc2)c(-c2ccccc2)c(-c2ccc(F)cc2)n1CC[C@@H]1C[C@H](CC(=O)OC(C)(C)C)OC(C)(C)O1
NCC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.FC1=CC=C(C=C1)C(C(C(C(=O)NC1=CC=CC=C1)C(C(C)C)=O)C1=CC=CC=C1)=O.CC(C)O>>FC1=CC=C(C=C1)C=1N(C(=C(C1C1=CC=CC=C1)C(=O)NC1=CC=CC=C1)C(C)C)CC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C
[NH2:30][CH2:31][CH2:32][C@@H:33]1[CH2:34][C@H:35]([CH2:36][C:37](=[O:38])[O:39][C:40]([CH3:41])([CH3:42])[CH3:43])[O:44][C:45]([CH3:46])([CH3:47])[O:48]1.O=[C:4]([CH:2]([CH3:1])[CH3:3])[CH:5]([C:6](=[O:7])[NH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[CH:15]([c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[C:22](=O)[c:...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1.CC(C)C(=O)C(C(=O)Nc1ccccc1)C(C(=O)c1ccc(F)cc1)c1ccccc1
CC(C)c1c(C(=O)Nc2ccccc2)c(-c2ccccc2)c(-c2ccc(F)cc2)n1CC[C@@H]1C[C@H](CC(=O)OC(C)(C)C)OC(C)(C)O1
null
null
CCCCCCC.C1(=CC=CC=C1)C
Aromatic Heterocycle Formation
Paal-Knorr pyrrole synthesis
0cb7b72300a2af7a2e4398a0e1226bb84c0d31edad76ec86c7b51828dc8686b6
e8142154ce82c2e242e52c937b939f3fefdc51b29f1e30581e6f69472c9bf693
O=C(Nc1ccccc1)c1cn(CC[C@@H]2CCOCO2)c(-c2ccccc2)c1-c1ccccc1
O=[C;H0;D3;+0:1](-[CH;D3;+0:2](-[CH;D3;+0:3](-[C:4](=[O;D1;H0:5])-[#7:6]-[c:7])-[C;H0;D3;+0:8](=O)-[C:9](-[C;D1;H3:10])-[C;D1;H3:11])-[c;H0;D3;+0:12](:[c:13]:[c:14]):[c:15]:[c:16])-[c;H0;D3;+0:17](:[c:18]:[c:19]):[c:20]:[c:21].[C:22]-[C:23]-[NH2;D1;+0:24]>>[C:22]-[C:23]-[n;H0;D3;+0:24]1:[c;H0;D3;+0:1](-[c;H0;D3;+0:17](...
null
[]
25
CELSIUS
null
null
A solution of (4R-cis)-1,1-dimethylethyl 6-(2-aminoethyl) -2,2-dimethyl-1,3-dioxane-4-acetate, (Example 2) 1.36 g (4.97 mmol), and (±)-4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N,β-diphenylbenzenebutaneamide mixture of [R-(R*,R*)], [R-(R*,S*)], [S-(R*,R*)], and [S-R*,S*)] isomers, (Example 3) 1.60 g (3.83 mmol), in 50 mL...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Primary amine
null
null
c1cc[nH]c1
c1cc[nH]c1.c1ccccc1.c1ccccc1.c1ccccc1.C1COCOC1
HO-
CCCCCCC.C1(=CC=CC=C1)C
25
null
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1.CC(C)C(=O)C(C(=O)Nc1ccccc1)C(C(=O)c1ccc(F)cc1)c1ccccc1>CCCCCCC.C1(=CC=CC=C1)C>CC(C)c1c(C(=O)Nc2ccccc2)c(-c2ccccc2)c(-c2ccc(F)cc2)n1CC[C@@H]1C[C@H](CC(=O)OC(C)(C)C)OC(C)(C)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-abee60ee9b184c41888df66883fa9eae
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1.CC(C)C(=O)C(C(=O)Nc1ccccc1)C(C(=O)c1ccc(F)cc1)c1ccccc1>>CC(C)c1c(C(=O)Nc2ccccc2)c(-c2ccccc2)c(-c2ccc(F)cc2)n1CC[C@@H]1C[C@@H](O)CC(=O)O1
NCC[C@@H]1C[C@@H](OC(O1)(C)C)CC(=O)OC(C)(C)C.FC1=CC=C(C=C1)C(C(C(C(=O)NC1=CC=CC=C1)C(C(C)C)=O)C1=CC=CC=C1)=O.O1CCCC1.[Cl-].[NH4+]>>FC1=CC=C(C=C1)C1=C(C(=C(N1CC[C@H]1OC(C[C@@H](C1)O)=O)C(C)C)C(=O)NC1=CC=CC=C1)C1=CC=CC=C1
CC(C)(C)O[C:38]([CH2:37][C@H:35]1[CH2:34][C@@H:33]([CH2:32][CH2:31][NH2:30])[O:40]C(C)(C)[O:36]1)=[O:39].O=[C:4]([CH:2]([CH3:1])[CH3:3])[CH:5]([C:6](=[O:7])[NH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[CH:15]([c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[C:22](=O)[c:23]1[cH:24][cH:25][c:26]([F:27])[cH:28][cH:29]1>>[...
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1.CC(C)C(=O)C(C(=O)Nc1ccccc1)C(C(=O)c1ccc(F)cc1)c1ccccc1
CC(C)c1c(C(=O)Nc2ccccc2)c(-c2ccccc2)c(-c2ccc(F)cc2)n1CC[C@@H]1C[C@@H](O)CC(=O)O1
null
null
O.CCCCCCC.C1(=CC=CC=C1)C
Aromatic Heterocycle Formation
OtherReaction
8e30b51508dc6a589cdd4f06c85afddd9a01bb1823227fed405ef8a23d32c02e
c5a8056bd33aab4597438c284a5d6d5fc73a7560d573a9ac4f0b77bcc8496ccc
O=C1CCC[C@@H](CCn2cc(C(=O)Nc3ccccc3)c(-c3ccccc3)c2-c2ccccc2)O1
C-C(-C)(-C)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]1-[C:5]-[C:6](-[C:7]-[C:8]-[NH2;D1;+0:9])-[O;H0;D2;+0:10]-C(-C)(-C)-[O;H0;D2;+0:11]-1.O=[C;H0;D3;+0:12](-[CH;D3;+0:13](-[CH;D3;+0:14](-[C:15](=[O;D1;H0:16])-[#7:17]-[c:18])-[C;H0;D3;+0:19](=O)-[C:20](-[C;D1;H3:21])-[C;D1;H3:22])-[c;H0;D3;+0:23](:[c:24]:[c:25]):[c:26...
null
[]
null
null
15
HOUR
A solution of (4R-cis)-1,1-dimethylethyl 6-(2-aminoethyl) -2,2-dimethyl-1,3-dioxane-4-acetate, (Example 2) 2.56 g (9.36 mmol), and (±)-4-fluoroα-[2-methyl-1-oxopropyl]-γ-oxo-N,β-diphenylbenzenebutaneamide mixture of [R-(R*,R*)], [R-(R*,S*)], [S-(R*,R*)], and [S (R*,S*)] isomers (Example 3), 3.00 g (7.20 mmol), in 60 mL...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Ester.Ether.Ether.Primary amine.Boc
Ester.Secondary alcohol
C1COCOC1
c1cc[nH]c1.C1CCOCC1
c1cc[nH]c1.c1ccccc1.c1ccccc1.c1ccccc1.C1CCOCC1
HO-
O.CCCCCCC.C1(=CC=CC=C1)C
null
15
CC(C)(C)OC(=O)C[C@H]1C[C@@H](CCN)OC(C)(C)O1.CC(C)C(=O)C(C(=O)Nc1ccccc1)C(C(=O)c1ccc(F)cc1)c1ccccc1>O.CCCCCCC.C1(=CC=CC=C1)C>CC(C)c1c(C(=O)Nc2ccccc2)c(-c2ccccc2)c(-c2ccc(F)cc2)n1CC[C@@H]1C[C@@H](O)CC(=O)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-da4df0e2a9804ff7a23ad117f2bc5cf7
COC(=O)CC(=O)C(C)C.Nc1ccccc1>>CC(C)C(=O)CC(=O)Nc1ccccc1
NC1=CC=CC=C1.C1(=CC=CC=C1)C.CC(C(CC(=O)OC)=O)C.C(CN)N>>CC(C(CC(=O)NC1=CC=CC=C1)=O)C
CO[C:7]([CH2:6][C:4]([CH:2]([CH3:1])[CH3:3])=[O:5])=[O:8].[NH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1>>[CH3:1][CH:2]([CH3:3])[C:4](=[O:5])[CH2:6][C:7](=[O:8])[NH:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1
COC(=O)CC(=O)C(C)C.Nc1ccccc1
CC(C)C(=O)CC(=O)Nc1ccccc1
null
null
O
Acylation
Aminolysis of esters
04c54ce22aa9bc0cea0de3d900446bcab51cf02bebeb606fa788a47dcd0e37ff
4335147c9ad02004b7c12428d7eac0b2e7e0e2017adc471d01c387239de8017d
c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[C:5])=[O;D1;H0:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[C:5]-[C:4](=[O;D1;H0:6])-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]
157.4
[{"value": 157.4, "product": "CC(C(CC(=O)NC1=CC=CC=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
16
HOUR
A three-necked, 12-L round-bottom flask equipped with a mechanical stirrer, a thermometer, and set up for distillation is charged with 2.6 L of toluene, 1.73 kg (12 mol) of methyl 4-methyl-3-oxopentanoate and 72 g (1.18 mol) of ethylenediamine. The mixture is heated to 80° C. and charged with 0.49 kg of aniline. The mi...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
O
80
16
COC(=O)CC(=O)C(C)C.Nc1ccccc1>O>CC(C)C(=O)CC(=O)Nc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bac2e5d16cf345c093dab45174ba84b2
O=CC(=O)O.Oc1ccccc1>>O=C(O)C(O)c1ccccc1O
C1(=CC=CC=C1)O.C(C=O)(=O)O>>OC1=C(C(C(=O)O)O)C=CC=C1
[O:1]=[C:2]([OH:3])[CH:4]=[O:5].[cH:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[OH:12]>>[O:1]=[C:2]([OH:3])[CH:4]([OH:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[OH:12]
O=CC(=O)O.Oc1ccccc1
O=C(O)C(O)c1ccccc1O
null
null
null
C-C Coupling
OtherReaction
236dc10d6be2d7527fb96a5b91492b698c2d2e32974acf29ee0457d6cf74bb4a
a7cae52d902b2812376f5459a7a8b7ead54e8ef31fd78982d2e99bec532613ba
c1ccccc1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D2;+0:4]=[O;H0;D1;+0:5].[O;D1;H1:6]-[c:7](:[c:8]):[cH;D2;+0:9]:[c:10]:[c:11]>>[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D3;+0:4](-[OH;D1;+0:5])-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:7](-[O;D1;H1:6]):[c:8]
null
[]
null
null
null
null
reacting glyoxylic acid with a boric acid ester of a phenol of the formula: ##STR9## under acid conditions to form a boric acid ester of a 2-hydroxymandelic acid; Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol
c1ccccc1
c1ccccc1
c1ccccc1
null
null
null
null
O=CC(=O)O.Oc1ccccc1>>O=C(O)C(O)c1ccccc1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4d1ae81964184c9cac35555f802dc7dc
CC1(C)C(=O)N(Br)C(=O)N1Br.COc1cc(C(=O)O)cc(OC)c1OC>>COc1cc(C(=O)O)c(Br)c(OC)c1OC
COC=1C=C(C(=O)O)C=C(C1OC)OC.CC1(C(=O)N(C(=O)N1Br)Br)C>>BrC1=C(C(=O)O)C=C(C(=C1OC)OC)OC
CC1(C)C(=O)N(Br)C(=O)N1[Br:10].[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[OH:8])[cH:9][c:11]([O:12][CH3:13])[c:14]1[O:15][CH3:16]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[OH:8])[c:9]([Br:10])[c:11]([O:12][CH3:13])[c:14]1[O:15][CH3:16]
CC1(C)C(=O)N(Br)C(=O)N1Br.COc1cc(C(=O)O)cc(OC)c1OC
COc1cc(C(=O)O)c(Br)c(OC)c1OC
null
null
null
Functional Group Interconversion
Bromination
e7196acac6d3571a6f057a0662dc983b0dda8f4f322e529a27cdf589fdea1d97
704bb5e37b3db6e189ba45e819fbdaa9822cc38202dae736860ec5273d025324
c1ccccc1
Br-N1-C(=O)-N(-[Br;H0;D1;+0:1])-C(-C)(-C)-C-1=O.[#8:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6](-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]):[c:10]>>[#8:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[Br;H0;D1;+0:1]):[c:6](-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]):[c:10]
null
[]
null
null
25
HOUR
Using the procedure described herein above in Example 1, Method E, 3,4,5-trimethoxybenzoic acid was brominated with DBDMH to provide the following results (assay yields) after reacting for 25 hours at 20°-25° C.: Conditions: See reaction.notes.procedure_details. Workup: to provide the; following results; (assay yields)
10.6084/m9.figshare.5104873.v1
null
Urea.Tertiary amide
Aromatic halide
C1CNCN1.c1ccccc1
c1ccccc1
c1ccccc1
HBr
null
null
25
CC1(C)C(=O)N(Br)C(=O)N1Br.COc1cc(C(=O)O)cc(OC)c1OC>>COc1cc(C(=O)O)c(Br)c(OC)c1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4583e7f0d868404ea0bdbff4012d8e64
CC1(C)C(=O)N(Br)C(=O)N1Br.COc1cccc(C(=O)O)c1OC>>COc1ccc(Br)c(C(=O)O)c1OC
COC1=C(C(=O)O)C=CC=C1OC.CC1(C(=O)N(C(=O)N1Br)Br)C>>BrC1=CC=C(C(=C1C(=O)O)OC)OC
CC1(C)C(=O)N(Br)C(=O)N1[Br:7].[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:8]([C:9](=[O:10])[OH:11])[c:12]1[O:13][CH3:14]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([Br:7])[c:8]([C:9](=[O:10])[OH:11])[c:12]1[O:13][CH3:14]
CC1(C)C(=O)N(Br)C(=O)N1Br.COc1cccc(C(=O)O)c1OC
COc1ccc(Br)c(C(=O)O)c1OC
null
null
null
Functional Group Interconversion
Bromination
e7196acac6d3571a6f057a0662dc983b0dda8f4f322e529a27cdf589fdea1d97
704bb5e37b3db6e189ba45e819fbdaa9822cc38202dae736860ec5273d025324
c1ccccc1
Br-N1-C(=O)-N(-[Br;H0;D1;+0:1])-C(-C)(-C)-C-1=O.[O;D1;H0:2]=[C:3](-[O;D1;H1:4])-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:5](-[C:3](=[O;D1;H0:2])-[O;D1;H1:4]):[c:6]
null
[]
null
null
22
HOUR
Using the procedure described herein above in Example 1, Method E, 2,3-dimethoxybenzoic acid was brominated with DBDMH to provide the following results (assay yields) after reacting for 22 hours at 20°-25° C: Conditions: See reaction.notes.procedure_details. Workup: to provide the; following results; (assay yields)
10.6084/m9.figshare.5104873.v1
null
Urea.Tertiary amide
Aromatic halide
C1CNCN1.c1ccccc1
c1ccccc1
c1ccccc1
HBr
null
null
22
CC1(C)C(=O)N(Br)C(=O)N1Br.COc1cccc(C(=O)O)c1OC>>COc1ccc(Br)c(C(=O)O)c1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e9daf0d13fb242e8a2f100e9a0e8682e
CC(=O)Nc1cc(S)c(Cl)cc1F>>Nc1cc(S)c(Cl)cc1F
N(C(=O)C)C=1C(=CC(=C(C1)S)Cl)F.[OH-].[Na+].Cl>>NC=1C(=CC(=C(C1)S)Cl)F
CC(=O)[NH:1][c:2]1[cH:3][c:4]([SH:5])[c:6]([Cl:7])[cH:8][c:9]1[F:10]>>[NH2:1][c:2]1[cH:3][c:4]([SH:5])[c:6]([Cl:7])[cH:8][c:9]1[F:10]
CC(=O)Nc1cc(S)c(Cl)cc1F
Nc1cc(S)c(Cl)cc1F
null
null
O
Reduction
Hydrogenolysis of amides/imides/carbamates
755df58c254dea764fdda078ffd678ec540bba057c83683be04c253f1270ac7b
025f7cefe51e71668ad5d09fca32df168e9b538347403e4d5c1748073e538adc
c1ccccc1
C-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
97.9
[{"value": 97.9, "product": "NC=1C(=CC(=C(C1)S)Cl)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.2, "product": "NC=1C(=CC(=C(C1)S)Cl)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Into a 100 ml reaction flask, 4.8 g (0.022 mol) of 5-acetamino-2-chloro-4-fluoro-thiophenol, 2.55 g (0.064 mol) of sodium hydroxide and 25.5 cc of water were added and stirred under reflux for 4 hours to obtain a uniform solution. The solution was cooled to room temperature and neutralized with 10% hydrochloric acid. T...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
Primary amine
null
null
c1ccccc1
HO-
O
null
null
CC(=O)Nc1cc(S)c(Cl)cc1F>O>Nc1cc(S)c(Cl)cc1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7f55e0a2549a42539e09fd9289ec2f3a
CC(=O)CCCC(=O)OCc1ccccc1.FC(F)(Br)Br>>CC(CCCC(=O)OCc1ccccc1)=C(F)F
CN(C)P(N(C)C)N(C)C.BrC(F)(F)Br.O=C(CCCC(=O)OCC1=CC=CC=C1)C>>FC(=C(CCCC(=O)OCC1=CC=CC=C1)C)F
O=[C:2]([CH3:1])[CH2:3][CH2:4][CH2:5][C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.Br[C:16](Br)([F:17])[F:18]>>[CH3:1][C:2]([CH2:3][CH2:4][CH2:5][C:6](=[O:7])[O:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)=[C:16]([F:17])[F:18]
CC(=O)CCCC(=O)OCc1ccccc1.FC(F)(Br)Br
CC(CCCC(=O)OCc1ccccc1)=C(F)F
null
null
COCCOCCOC
C-C Coupling
OtherReaction
063e2488dc04a2778c8d9e640fba2ecd94fd30d914823aeb4af5739622133a94
d6a105150c2ffb7f6f5aff908de6bf6312362b4e5f748d12674ad40b306aec9d
c1ccccc1
Br-[C;H0;D4;+0:1](-Br)(-[F;D1;H0:2])-[F;D1;H0:3].O=[C;H0;D3;+0:4](-[C;D1;H3:5])-[C:6]-[C:7]>>[C:7]-[C:6]-[C;H0;D3;+0:4](-[C;D1;H3:5])=[C;H0;D3;+0:1](-[F;D1;H0:2])-[F;D1;H0:3]
null
[]
null
null
3
HOUR
27.85 g Tris(dimethylamino)phosphine was added dropwise to a solution of 17.90 g dibromodifluoromethane in 130 ml diglyme, maintained under a nitrogen atmosphere and ice bath cooling. After stirring for one hour on the ice bath, 8.82 g benzyl 5-oxohexanoate in 70 ml diglyme was added slowly, dropwise. The ice bath was ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide.Ketone
Alkenyl halide.Alkenyl halide
null
null
c1ccccc1
Br-
COCCOCCOC
null
3
CC(=O)CCCC(=O)OCc1ccccc1.FC(F)(Br)Br>COCCOCCOC>CC(CCCC(=O)OCc1ccccc1)=C(F)F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d30cf53005b044ea9db9fca6b67dce41
O=C(O)CCCC=C(F)F.O=S(Cl)Cl>>O=C(Cl)CCCC=C(F)F
S(=O)(Cl)Cl.FC(=CCCCC(=O)O)F>>FC(=CCCCC(=O)Cl)F
O[C:2](=[O:1])[CH2:4][CH2:5][CH2:6][CH:7]=[C:8]([F:9])[F:10].O=S(Cl)[Cl:3]>>[O:1]=[C:2]([Cl:3])[CH2:4][CH2:5][CH2:6][CH:7]=[C:8]([F:9])[F:10]
O=C(O)CCCC=C(F)F.O=S(Cl)Cl
O=C(Cl)CCCC=C(F)F
null
null
CN(C=O)C
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
null
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
null
null
10.23 ml (140.68 mmol) Thionyl chloride was added dropwise to 8.0 g (52.29 mmol) of the product of Example 9 at room temperature. A drop of dimethylformamide was added and the mixture heated under reflux for 6 hours. It was then distilled under reduced pressure. Conditions: See reaction.notes.procedure_details. Workup:...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
null
HCl
CN(C=O)C
null
null
O=C(O)CCCC=C(F)F.O=S(Cl)Cl>CN(C=O)C>O=C(Cl)CCCC=C(F)F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-10fea42bec564443a9bc5ae1ea51daad
O=C(OCc1ccccc1)C(CCC(F)=C(F)F)C(=O)OCc1ccccc1>>O=C(O)C(CCC(F)=C(F)F)C(=O)O
[OH-].[K+].C(C)O.FC(CCC(C(=O)OCC1=CC=CC=C1)C(=O)OCC1=CC=CC=C1)=C(F)F>>FC(CCC(C(=O)O)C(=O)O)=C(F)F
c1ccc(C[O:3][C:2](=[O:1])[CH:4]([CH2:5][CH2:6][C:7]([F:8])=[C:9]([F:10])[F:11])[C:12](=[O:13])[O:14]Cc2ccccc2)cc1>>[O:1]=[C:2]([OH:3])[CH:4]([CH2:5][CH2:6][C:7]([F:8])=[C:9]([F:10])[F:11])[C:12](=[O:13])[OH:14]
O=C(OCc1ccccc1)C(CCC(F)=C(F)F)C(=O)OCc1ccccc1
O=C(O)C(CCC(F)=C(F)F)C(=O)O
null
null
O
Deprotection
OtherReaction
c3cedf6fcf01bee6478da3bdaea2e9c7140af795b9e8421ed6d8cc9c9f58df51
ed5fed81ba501ef41c88831ec6b9463b899bfdd0815c4145ae51c79addb226d0
null
[O;D1;H0:1]=[C:2](-[C:3]-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-C-c1:c:c:c:c:c:1)-[O;H0;D2;+0:7]-C-c1:c:c:c:c:c:1>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:7])-[C:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6]
null
[]
null
null
null
null
5.56 g (99 mmol) KOH flakes were dissolved in 6.82 ml water and 13.65 ml ethanol and then treated with 11.12 g (28.34 mmol) of dibenzyl 2-(3,4,4-trifluoro-3-butenyl)-malonate. After heating under reflux for 4 hours, the reaction mixture was poured into 30 ml water and washed with ether. The aqueous phase was acidified ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Carboxylic acid.Carboxylic acid
c1ccccc1.c1ccccc1
null
null
Other
O
null
null
O=C(OCc1ccccc1)C(CCC(F)=C(F)F)C(=O)OCc1ccccc1>O>O=C(O)C(CCC(F)=C(F)F)C(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-790e2a778f77438c9b5e15011df151a3
CC(C)(C)[SiH2]OCCCCC(=C(F)F)C(F)(F)F>>OCCCCC(=C(F)F)C(F)(F)F
FC(=C(CCCCO[SiH2]C(C)(C)C)C(F)(F)F)F>>FC(=C(CCCCO)C(F)(F)F)F
CC(C)(C)[SiH2][O:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6](=[C:7]([F:8])[F:9])[C:10]([F:11])([F:12])[F:13]>>[OH:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6](=[C:7]([F:8])[F:9])[C:10]([F:11])([F:12])[F:13]
CC(C)(C)[SiH2]OCCCCC(=C(F)F)C(F)(F)F
OCCCCC(=C(F)F)C(F)(F)F
null
null
CO
Deprotection
OtherReaction
d7487e9652d81f9226fa8fb90bf02725deb1441d4abc97ee4fdbe439e00122e0
ff9889ffd40f59bd281424811967f384d29acb01a2d54e10590c5a677f81d17a
null
C-C(-C)(-C)-[SiH2]-[O;H0;D2;+0:1]-[C:2]-[C:3]>>[C:3]-[C:2]-[OH;D1;+0:1]
null
[]
null
null
3
HOUR
A solution of 3.59 g (11.28 mmol) 6,6-difluoro-5-trifluoromethyl-1-tert-butylsilyloxy-5-hexene in 50 ml methanol was treated with a teaspoon full of ion exchange resin and the mixture stirred for 3 hours at room temperature. The ion exchange resin was then filtered off and washed with methanol. The filtrate was careful...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol
null
null
null
Other
CO
null
3
CC(C)(C)[SiH2]OCCCCC(=C(F)F)C(F)(F)F>CO>OCCCCC(=C(F)F)C(F)(F)F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6a9f947d18fd4b718325c2f1fee21eab
CC(=O)CCCCCC(=O)OCc1ccccc1.FC(F)(Br)Br>>CC(CCCCCC(=O)OCc1ccccc1)=C(F)F
CN(C)P(N(C)C)N(C)C.BrC(F)(F)Br.O=C(CCCCCC(=O)OCC1=CC=CC=C1)C>>FC(=C(CCCCCC(=O)OCC1=CC=CC=C1)C)F
O=[C:2]([CH3:1])[CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][C:8](=[O:9])[O:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.Br[C:18](Br)([F:19])[F:20]>>[CH3:1][C:2]([CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][C:8](=[O:9])[O:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1)=[C:18]([F:19])[F:20]
CC(=O)CCCCCC(=O)OCc1ccccc1.FC(F)(Br)Br
CC(CCCCCC(=O)OCc1ccccc1)=C(F)F
null
null
COCCOCCOC
C-C Coupling
OtherReaction
063e2488dc04a2778c8d9e640fba2ecd94fd30d914823aeb4af5739622133a94
d6a105150c2ffb7f6f5aff908de6bf6312362b4e5f748d12674ad40b306aec9d
c1ccccc1
Br-[C;H0;D4;+0:1](-Br)(-[F;D1;H0:2])-[F;D1;H0:3].O=[C;H0;D3;+0:4](-[C;D1;H3:5])-[C:6]-[C:7]>>[C:7]-[C:6]-[C;H0;D3;+0:4](-[C;D1;H3:5])=[C;H0;D3;+0:1](-[F;D1;H0:2])-[F;D1;H0:3]
null
[]
null
null
1
HOUR
123 ml (0.68 mol) Tris(dimethylamino)phosphine in 100 ml diglyme was added slowly dropwise to a solution of 26.3 ml (0.34 mol) dibromodifluoromethane in 800 ml diglyme. After stirring for one hour on an ice bath, 43 g (0.17 mol}benzyl 7-oxooctanoate in 100 ml diglyme was slowly added dropwise. The ice bath was removed ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide.Ketone
Alkenyl halide.Alkenyl halide
null
null
c1ccccc1
Br-
COCCOCCOC
null
1
CC(=O)CCCCCC(=O)OCc1ccccc1.FC(F)(Br)Br>COCCOCCOC>CC(CCCCCC(=O)OCc1ccccc1)=C(F)F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c4bb80abbe704cb6b9de76dd9722654e
BrCc1ccccc1.CC(=O)CCCCCC(=O)O>>CC(=O)CCCCCC(=O)OCc1ccccc1
O=C(CCCCCC(=O)O)C.C(C1=CC=CC=C1)Br.C([O-])([O-])=O.[K+].[K+]>>O=C(CCCCCC(=O)OCC1=CC=CC=C1)C
Br[CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1.[CH3:1][C:2](=[O:3])[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][C:9](=[O:10])[OH:11]>>[CH3:1][C:2](=[O:3])[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][C:9](=[O:10])[O:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
BrCc1ccccc1.CC(=O)CCCCCC(=O)O
CC(=O)CCCCCC(=O)OCc1ccccc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
c1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[C:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
Benzyl 7-oxooctanoate was prepared by benzylation of 7-oxooctanoic acid with benzyl bromide and potassium carbonate in dimethyl formamide. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1ccccc1
HBr
CN(C=O)C
null
null
BrCc1ccccc1.CC(=O)CCCCCC(=O)O>CN(C=O)C>CC(=O)CCCCCC(=O)OCc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e1b1a95009504cf9bff9d61402140b73
CC(=O)C1CCCCC1=O.[OH-]>>CC(=O)CCCCCC(=O)O
C(C)(=O)C1C(CCCC1)=O.[OH-].[K+]>>O=C(CCCCCC(=O)O)C
[CH3:1][C:2](=[O:3])[CH:4]1[CH2:5][CH2:6][CH2:7][CH2:8][C:9]1=[O:10].[OH-:11]>>[CH3:1][C:2](=[O:3])[CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][C:9](=[O:10])[OH:11]
CC(=O)C1CCCCC1=O.[OH-]
CC(=O)CCCCCC(=O)O
null
null
null
Acylation
OtherReaction
d6e01e4bce9376c221bbc59d2280a136e5c257de567a453a205d7a0c9331cfc1
553e3366df9577c6f76b744a1617173162a370f5ca95b87c9cc38060deb2e92e
null
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[CH;D3;+0:4]1-[C:5]-[C:6]-[C:7]-[C:8]-[C;H0;D3;+0:9]-1=[O;D1;H0:10].[OH-;D0:11]>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[C:5]-[C:6]-[C:7]-[C:8]-[C;H0;D3;+0:9](=[O;D1;H0:10])-[OH;D1;+0:11]
null
[]
null
null
null
null
7-Oxooctanoic acid was prepared by treatment of 2-acetyl cyclohexanone with aqueous potassium hydroxide (S. Hunig et al; Chem Ber 91, 129-133 (1958)). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Carboxylic acid.Ketone
C1CCCCC1
null
null
null
null
null
null
CC(=O)C1CCCCC1=O.[OH-]>>CC(=O)CCCCCC(=O)O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-de601d7504a04544afaf93084d42b5be
ClCCOCCCl.Oc1ccc(I)cc1.[OH-]>>Ic1ccc(OCCOCCOc2ccc(I)cc2)cc1
ClCCOCCCl.[OH-].[Na+].IC1=CC=C(C=C1)O>>IC1=CC=C(OCCOCCOC2=CC=C(C=C2)I)C=C1
Cl[CH2:3][CH2:5][O:9][CH2:8][CH2:7]Cl.[I:1][c:2]1[cH:15][cH:14][c:13]([OH:12])[cH:19][cH:18]1.[OH-:6]>>[I:1][c:2]1[cH:3][cH:4][c:5]([O:6][CH2:7][CH2:8][O:9][CH2:10][CH2:11][O:12][c:13]2[cH:14][cH:15][c:16]([I:17])[cH:18][cH:19]2)[cH:20][cH:21]1
ClCCOCCCl.Oc1ccc(I)cc1.[OH-]
Ic1ccc(OCCOCCOc2ccc(I)cc2)cc1
null
null
C(CCC)O
Aromatic Heterocycle Formation
OtherReaction
e7f830160b182d96fee8d6f0fdedd44f07771178446e1b5ed644fdfd9fa19d6a
0c5376f97e025bc1b8def6abd84e300900d8c12e37bed566d9fb7dca2bf71d25
c1ccc(OCCOCCOc2ccccc2)cc1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[O;H0;D2;+0:3]-[C:4]-[CH2;D2;+0:5]-Cl.[I;D1;H0:6]-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[c:9]:[c:10](-[OH;D1;+0:11]):[c:12]:[cH;D2;+0:13]:1.[OH-;D0:14]>>[I;D1;H0:15]-[c:16]1:[cH;D2;+0:8]:[c:9]:[c:10](-[O;H0;D2;+0:11]-[C:17]-[C:18]-[O;H0;D2;+0:3]-[C:4]-[CH2;D2;+0:5]-[O;H0;D2;+0:14]-[c;H0;D3;+0:2]2:...
null
[]
null
null
null
null
A mixture prepared by adding 3.08 g of sodium hydroxide and 40 ml of n-butanol to 15.4 g of 4-iodophenol was refluxed. 2 ml of n-butanol solution of 5.01 g of 1,5-dichloro-3-oxapentane was added dropwise to the above prepared mixture over a period of 5 minutes. Conditions: See reaction.notes.procedure_details. Workup: ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary halide.Primary halide.Ether.Aromatic alcohol
Aromatic halide.Aromatic halide.Ether.Ether.Ether
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
null
C(CCC)O
null
null
ClCCOCCCl.Oc1ccc(I)cc1.[OH-]>C(CCC)O>Ic1ccc(OCCOCCOc2ccc(I)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f4cc62040f7c42ea8b1be3806e91e5ff
CC(C)(C)OC(=O)NCC(=O)O.C[C@@H](N)C(=O)OCc1ccccc1.ClCCl>>C[C@@H](NC(=O)CN)C(=O)OCc1ccccc1.Cl
C1(CCCCC1)N=C=NC1CCCCC1.C(C)(C)(C)OC(=O)NCC(=O)O.C1(=CC=C(C=C1)S(=O)(=O)O)C.C(C1=CC=CC=C1)OC([C@H](N)C)=O.C(Cl)Cl.C(C)N(CC)CC>>Cl.C(C1=CC=CC=C1)OC([C@H](NC(CN)=O)C)=O
CC(C)(C)OC(=O)[NH:7][CH2:6][C:4](O)=[O:5].[CH3:1][C@@H:2]([NH2:3])[C:8](=[O:9])[O:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.ClC[Cl:18]>>[CH3:1][C@@H:2]([NH:3][C:4](=[O:5])[CH2:6][NH2:7])[C:8](=[O:9])[O:10][CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[ClH:18]
CC(C)(C)OC(=O)NCC(=O)O.C[C@@H](N)C(=O)OCc1ccccc1.ClCCl
C[C@@H](NC(=O)CN)C(=O)OCc1ccccc1.Cl
null
null
null
Acylation
OtherReaction
c4b6ff1c5a86405f86fe4a3d689987915e1ddb8ecb5b8ab8c4aa3d729fe0ceef
c73530b43160ba59e35b2ca368dd7f9e092fe1309aabd3f94299d7158bc36c97
c1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2]-[C;H0;D3;+0:3](-O)=[O;D1;H0:4].Cl-C-[Cl;H0;D1;+0:5].[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[C:10](-[C;D1;H3:11])-[NH2;D1;+0:12]>>[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[C:10](-[C;D1;H3:11])-[NH;D2;+0:12]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[C:2]-[NH2;D1;+0:1].[ClH;D0;+0:5]
70
[{"value": 70.0, "product": "Cl.C(C1=CC=CC=C1)OC([C@H](NC(CN)=O)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a cold (0° C.) solution of 100 ml. methylene chloride containing 10 g. (57 mmol) of N-t-butyloxycarbonylglycine, 20 g. (57 mmol) of D-alanine benzyl ester p-toluene sulfonic acid salt and 5.77 g. (57 mmol) of triethylamine was added 12.3 g. (60 mmol) of dicyclohexylcarbodiimide and the resulting action mixture allow...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Carbamic ester.Carboxylic acid.Ether.Primary amine.Boc
Secondary amide.Primary amine
null
null
c1ccccc1
HCl
null
null
0.5
CC(C)(C)OC(=O)NCC(=O)O.C[C@@H](N)C(=O)OCc1ccccc1.ClCCl>>C[C@@H](NC(=O)CN)C(=O)OCc1ccccc1.Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e18ec41772ca4d5fa1f5d0902ef672de
CCCCc1ncc(C=N[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl.CI>>CCCCc1ncc(C=N[C@@](C)(Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
C(C)(C)NC(C)C.C(CCC)[Li].COC([C@@H](N=CC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O.CI>>COC([C@@](N=CC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)(CC1=CC=CC=C1)C)=O
[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH:9]=[N:10][C@@H:11]([CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[C:20](=[O:21])[O:22][CH3:23])[n:24]1[CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][c:31]1[Cl:32].I[CH3:12]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH:9]=[N:10][C@@:11]([CH3:12])([CH2:...
CCCCc1ncc(C=N[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl.CI
CCCCc1ncc(C=N[C@@](C)(Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
null
null
O1CCCC1
C-C Coupling
Methylation with MeI_tertiary
0570231f487a8ed6f750cd320473f7dbaf49269e0dc5684a4c7ab99270540147
14e59a0462685ab029a3f096b6ab1b088ab82a473dbad968017fbb67b5b8465e
C(=NCCc1ccccc1)c1cncn1Cc1ccccc1
I-[CH3;D1;+0:1].[#7;a:2]:[c:3](-[C:4]=[#7:5]-[C@@H;D3;+0:6](-[C:7]-[c:8])-[C:9](=[O;D1;H0:10])-[#8:11]-[C;D1;H3:12]):[c:13]:[#7;a:14]>>[#7;a:2]:[c:3](-[C:4]=[#7:5]-[C@@;H0;D4;+0:6](-[CH3;D1;+0:1])(-[C:7]-[c:8])-[C:9](=[O;D1;H0:10])-[#8:11]-[C;D1;H3:12]):[c:13]:[#7;a:14]
null
[]
0
CELSIUS
15
MINUTE
To a solution of diisopropylamine (1.27 g, 12.6 mmol) in tetrahydrofuran (50 ml) was added n-butyl lithium (5 ml of 2.5M in hexane, 12.6 mmol) at 0° C. After being stirred at 0° C. for 15 minutes, the solution was cooled to -78° C. and a solution of the imine, N [{1-[(2-chlorophenyl)methyl]-2-n-butyl-1H-imidazol-5-yl}m...
10.6084/m9.figshare.5104873.v1
null
Ester.Substituted imine
Ester.Substituted imine
null
null
c1c[nH]cn1.c1ccccc1.c1ccccc1
HI
O1CCCC1
0
0.25
CCCCc1ncc(C=N[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl.CI>O1CCCC1>CCCCc1ncc(C=N[C@@](C)(Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7b25920dfe6144a1a723eec9437b7937
CCCCc1ncc(C=O)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1cccs1>>CCCCc1ncc(C=N[C@@H](Cc2cccs2)C(=O)OC)n1Cc1ccccc1Cl
C(CCC)C=1N(C(=CN1)C=O)CC1=C(C=CC=C1)Cl.COC([C@@H](N)CC=1SC=CC1)=O.C1(=CC=CC=C1)C>>COC([C@@H](N=CC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC=1SC=CC1)=O
O=[CH:9][c:8]1[cH:7][n:6][c:5]([CH2:4][CH2:3][CH2:2][CH3:1])[n:22]1[CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][c:29]1[Cl:30].[NH2:10][C@@H:11]([CH2:12][c:13]1[cH:14][cH:15][cH:16][s:17]1)[C:18](=[O:19])[O:20][CH3:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH:9]=[N:10][C@@H:11]([CH2:12][c:13]2[cH:14][cH:15...
CCCCc1ncc(C=O)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1cccs1
CCCCc1ncc(C=N[C@@H](Cc2cccs2)C(=O)OC)n1Cc1ccccc1Cl
null
null
O
Heteroatom Alkylation and Arylation
Addition of primary amines to aldehydes/thiocarbonyls
d409dfd3247abb6c1b1364aec380d25720f21e374fd2124063f2d2ce54d31c4f
9b341044a5a058244685b0b956d33f593ccdcd7346fa1d8d7b98a302fd35b8a2
C(=NCCc1cccs1)c1cncn1Cc1ccccc1
O=[CH;D2;+0:1]-[c:2]1:[c:3]:[#7;a:4]:[c:5]:[#7;a:6]:1-[C:7].[C:8]-[C:9](-[NH2;D1;+0:10])-[C:11](=[O;D1;H0:12])-[#8:13]-[C;D1;H3:14]>>[C:8]-[C:9](-[N;H0;D2;+0:10]=[CH;D2;+0:1]-[c:2]1:[c:3]:[#7;a:4]:[c:5]:[#7;a:6]:1-[C:7])-[C:11](=[O;D1;H0:12])-[#8:13]-[C;D1;H3:14]
null
[]
null
null
8
HOUR
A solution of 2-n-butyl-1-[(2-chlorophenyl)methyl]-1H-imidazol-5-carboxaldehyde (0.6 g, 2.12 mmol), β-(2-thienyl)alanine methyl ester (0.4 g, 2.16 mmol) and toluene (25 ml) was refluxed under argon with a Dean-Stark water separator for 8 hours. The solvent was evaporated to an orange-red oil (1.1 g) of the title imine ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Substituted imine
null
null
c1c[nH]cn1.c1ccsc1.c1ccccc1
HO-
O
null
8
CCCCc1ncc(C=O)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1cccs1>O>CCCCc1ncc(C=N[C@@H](Cc2cccs2)C(=O)OC)n1Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-50dfb916fc1b4933aac44bd6fca31f18
CCCCc1ncc(CCO)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1ccccc1>>CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
COC([C@@H](N)CC1=CC=CC=C1)=O.FC(S(=O)(=O)OS(=O)(=O)C(F)(F)F)(F)F.C(CCC)C=1N(C(=CN1)CCO)CC1=C(C=CC=C1)Cl.C(C)(C)N(CC)C(C)C>>COC([C@@H](NCCC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O
O[CH2:10][CH2:9][c:8]1[cH:7][n:6][c:5]([CH2:4][CH2:3][CH2:2][CH3:1])[n:24]1[CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][c:31]1[Cl:32].[NH2:11][C@@H:12]([CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[C:20](=[O:21])[O:22][CH3:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH2:9][CH2:10][NH:11][C@@H:12]([CH...
CCCCc1ncc(CCO)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1ccccc1
CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
Reductive amination with alcohol
80c5fffb5a6cd9bcf0b3d20ee51fe5f6574f02d4cb5ea6a4d33b4a9098b0e672
405fc0d288d595940df82750271ed5f4125713ca8b676b8ed83063765fec7c50
c1ccc(CCNCCc2cncn2Cc2ccccc2)cc1
O-[CH2;D2;+0:1]-[C:2]-[c:3](:[#7;a:4]):[c:5]:[#7;a:6].[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10](=[O;D1;H0:11])-[#8:12]-[C;D1;H3:13]>>[#7;a:4]:[c:3](-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:9]-[C:8](-[C:7])-[C:10](=[O;D1;H0:11])-[#8:12]-[C;D1;H3:13]):[c:5]:[#7;a:6]
65
[{"value": 65.0, "product": "COC([C@@H](NCCC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.6, "product": "COC([C@@H](NCCC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
15
MINUTE
A solution of trifluoromethanesulfonic anhydride (0.954 g, 3.38 mmol) in methylene chloride (5 ml) was cooled to -78° C. under nitrogen, and a solution of 2-n-butyl-1-(2-chlorophenyl)methyl-5-(2-hydroxyethyl)-1H-imidazole (0.9 g, 3.07 mmol), diisopropylethylamine (0.44 g. 3.38 mmol) and methylene chloride (10 ml) was a...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary amine
Secondary amine
null
null
c1c[nH]cn1.c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
-78
0.25
CCCCc1ncc(CCO)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1ccccc1>C(Cl)Cl>CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0938af2f3f7e40ac8becd6f17afdc7e9
CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl>>CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)O)n1Cc1ccccc1Cl
O.COC([C@@H](NCCC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O.COC([C@@H](NCCC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O.C(C)O.[OH-].[K+]>>ClC1=C(C=CC=C1)CN1C(=NC=C1CCN[C@@H](CC1=CC=CC=C1)C(=O)O)CCCC
C[O:22][C:20]([C@@H:12]([NH:11][CH2:10][CH2:9][c:8]1[cH:7][n:6][c:5]([CH2:4][CH2:3][CH2:2][CH3:1])[n:23]1[CH2:24][c:25]1[cH:26][cH:27][cH:28][cH:29][c:30]1[Cl:31])[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)=[O:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH2:9][CH2:10][NH:11][C@@H:12]([CH2:13][c:14...
CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)O)n1Cc1ccccc1Cl
null
null
CCOCC
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc(CCNCCc2cncn2Cc2ccccc2)cc1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
null
null
null
null
The procedure of Example 2 (ii) was followed using 0.9 g (1.99 mmol) of N-[2-{1-[(2-chlorophenyl)methyl]-2-n-butyl-1H-imidazol -5-yl}ethyl]phenylalanine methyl ester, 0.33 g of potassium hydroxide, 15 ml of water and 25 ml of ethanol to afford after workup 0.54 q of product. Trituration with ether provided the title co...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1c[nH]cn1.c1ccccc1.c1ccccc1
Other
CCOCC
null
null
CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl>CCOCC>CCCCc1ncc(CCN[C@@H](Cc2ccccc2)C(=O)O)n1Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2ee5331ec52c4b96954c2cbc8e4bbd96
CCCCc1ncc(CO)n1Cc1ccccc1Cl.O=C1CCC(=O)N1Cl>>CCCCc1nc(Cl)c(CO)n1Cc1ccccc1Cl
ClN1C(CCC1=O)=O.C(CCC)C=1N(C(=CN1)CO)CC1=C(C=CC=C1)Cl.ClN1C(CCC1=O)=O>>C(CCC)C=1N(C(=C(N1)Cl)CO)CC1=C(C=CC=C1)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:9]([CH2:10][OH:11])[n:12]1[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[Cl:20].O=C1CCC(=O)N1[Cl:8]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][c:7]([Cl:8])[c:9]([CH2:10][OH:11])[n:12]1[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[Cl:20]
CCCCc1ncc(CO)n1Cc1ccccc1Cl.O=C1CCC(=O)N1Cl
CCCCc1nc(Cl)c(CO)n1Cc1ccccc1Cl
null
null
O1CCCC1
Functional Group Interconversion
Chlorination
339179e6c50945dd3ac07a96a57059a7154e475073d7636ad2fc68e36469c54f
0e444576b73669992a4073cc3f7b10ed52cb9df09f9f8e4042e39e6a602aa390
c1ccc(Cn2ccnc2)cc1
O=C1-C-C-C(=O)-N-1-[Cl;H0;D1;+0:1].[C:2]-[c:3]1:[cH;D2;+0:4]:[#7;a:5]:[c:6]:[#7;a:7]:1-[C:8]>>[C:2]-[c:3]1:[#7;a:7](-[C:8]):[c:6]:[#7;a:5]:[c;H0;D3;+0:4]:1-[Cl;H0;D1;+0:1]
44.2
[{"value": 44.0, "product": "C(CCC)C=1N(C(=C(N1)Cl)CO)CC1=C(C=CC=C1)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.2, "product": "C(CCC)C=1N(C(=C(N1)Cl)CO)CC1=C(C=CC=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
45
CELSIUS
3
HOUR
A solution of 2-n-butyl-1-(2-chlorophenyl)methyl-5-hydroxymethyl-1H-imidazole (Example 3(i) Method A) (10.2 g. 0.0368 mol) in tetrahydrofuran (100 ml) was treated portionwise with N-chlorosuccinimide (NCS) (4.92 g, 0.0368 mol) and stirred at 45° C. for a total of 3 hours after the addition of the NCS. The tetrahydrofur...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Aromatic halide
c1c[nH]cn1.C1CCNC1
c1c[nH]cn1
c1c[nH]cn1.c1ccccc1
HO-
O1CCCC1
45
3
CCCCc1ncc(CO)n1Cc1ccccc1Cl.O=C1CCC(=O)N1Cl>O1CCCC1>CCCCc1nc(Cl)c(CO)n1Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bc86844699a84905a340fdf779a0e7ca
CCCCc1ncc[nH]1.Fc1cccc(Cl)c1CCl>>CCCCc1nccn1Cc1c(F)cccc1Cl
C(CCC)C=1NC=CN1.[H-].[Na+].ClC1=C(CCl)C(=CC=C1)F>>C(CCC)C=1N(C=CN1)CC1=C(C=CC=C1F)Cl
[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][cH:8][nH:9]1.Cl[CH2:10][c:11]1[c:12]([F:13])[cH:14][cH:15][cH:16][c:17]1[Cl:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][cH:8][n:9]1[CH2:10][c:11]1[c:12]([F:13])[cH:14][cH:15][cH:16][c:17]1[Cl:18]
CCCCc1ncc[nH]1.Fc1cccc(Cl)c1CCl
CCCCc1nccn1Cc1c(F)cccc1Cl
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
5118ce9eea46859cccf16d01cf8151757afd816de0c93fe6fcb74a0ee15c5a67
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cn2ccnc2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[c:6]1:[#7;a:7]:[c:8]:[c:9]:[nH;D2;+0:10]:1>>[C:5]-[c:6]1:[#7;a:7]:[c:8]:[c:9]:[n;H0;D3;+0:10]:1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
95.3
[{"value": 94.0, "product": "C(CCC)C=1N(C=CN1)CC1=C(C=CC=C1F)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.3, "product": "C(CCC)C=1N(C=CN1)CC1=C(C=CC=C1F)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 2 n-butylimidazole (3.75 g, 0.03 mol) in dry dimethylformamide (4 ml) was added to sodium hydride (0.95 g) in dimethylformamide (18 ml). After the gas evolution subsided, the mixture was stirred one hour under argon and 2-chloro-6-fluorobenzylchloride (5.5 q, 0.031 mol) in dimethylformamide (7 ml) was add...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1c[nH]cn1
c1ncc[nH]1
c1ncc[nH]1.c1ccccc1
HCl
CN(C=O)C
null
1
CCCCc1ncc[nH]1.Fc1cccc(Cl)c1CCl>CN(C=O)C>CCCCc1nccn1Cc1c(F)cccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d2c9533997c74d79a948283e529ded3f
CCCCc1ncc(CO)n1Cc1c(F)cccc1Cl>>CCCCc1nccn1Cc1c(F)cccc1Cl
C(CCC)C=1N(C(=CN1)CO)CC1=C(C=CC=C1F)Cl.ClC1=C(C=CC=C1)CN1C(=NC=C1CCN[C@@H](CC1=CC=CC=C1)C(=O)O)CCCC>>C(CCC)C=1N(C=CN1)CC1=C(C=CC=C1F)Cl
OC[c:8]1[cH:7][n:6][c:5]([CH2:4][CH2:3][CH2:2][CH3:1])[n:9]1[CH2:10][c:11]1[c:12]([F:13])[cH:14][cH:15][cH:16][c:17]1[Cl:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][cH:8][n:9]1[CH2:10][c:11]1[c:12]([F:13])[cH:14][cH:15][cH:16][c:17]1[Cl:18]
CCCCc1ncc(CO)n1Cc1c(F)cccc1Cl
CCCCc1nccn1Cc1c(F)cccc1Cl
null
null
null
Reduction
OtherReaction
0bfcf9be29de871a8a1dc7820346d1be2cd5fe407ee81265651f772633ca02be
0a2c8330040d049ae67653e1474aff520bf8a2d8c908ffd7076f536576936945
c1ccc(Cn2ccnc2)cc1
O-C-[c;H0;D3;+0:1]1:[c:2]:[#7;a:3]:[c:4](-[C:5]):[#7;a:6]:1-[C:7]>>[C:7]-[#7;a:6]1:[cH;D2;+0:1]:[c:2]:[#7;a:3]:[c:4]:1-[C:5]
null
[]
null
null
null
null
The procedures of Example 1(ii iii) were used. From 7.63 g of crude 2-n-butyl-1-(2-chloro-6-fluorophenyl)methyl-1H-imidazole was obtained 2.8 q of 2-n-butyl-1-(2-chloro-6-fluorophenyl)methyl-5-hydroxymethyl-1H-imidazo le; mp 106°-108° C. (from ethyl acetate). This material was oxidized with manganese dioxide and worked...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
null
c1c[nH]cn1
c1ncc[nH]1
c1ncc[nH]1.c1ccccc1
HO-
null
null
null
CCCCc1ncc(CO)n1Cc1c(F)cccc1Cl>>CCCCc1nccn1Cc1c(F)cccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-36b3c2ed1dbc482aa4b7a196ab5747d7
CCCCc1nc(Cl)c(CO)n1Cc1ccccc1Cl.CC[C@](N)(Cc1ccccc1)C(=O)OC>>CCCCc1ncc(CN[C@@](CC)(Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
C(CCC)C=1N(C(=C(N1)Cl)CO)CC1=C(C=CC=C1)Cl.COC([C@@](N)(CC1=CC=CC=C1)CC)=O>>COC([C@@](NCC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)(CC1=CC=CC=C1)CC)=O
O[CH2:9][c:8]1[c:7](Cl)[n:6][c:5]([CH2:4][CH2:3][CH2:2][CH3:1])[n:25]1[CH2:26][c:27]1[cH:28][cH:29][cH:30][cH:31][c:32]1[Cl:33].[NH2:10][C@@:11]([CH2:12][CH3:13])([CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[C:21](=[O:22])[O:23][CH3:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH2:9][NH:10][C@@:11](...
CCCCc1nc(Cl)c(CO)n1Cc1ccccc1Cl.CC[C@](N)(Cc1ccccc1)C(=O)OC
CCCCc1ncc(CN[C@@](CC)(Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
381acdd477743c8db4aee37f977438acfb7d2e431e8c4efe7996dd0ebaf534d9
ef8b457f33bb2e8764dcedaad5d616341ac6cab05b3d6d88254b664261093078
c1ccc(CCNCc2cncn2Cc2ccccc2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4](-[C:5]):[c:6]:1-[CH2;D2;+0:7]-O.[C:8]-[C:9](-[C:10])(-[NH2;D1;+0:11])-[C:12](=[O;D1;H0:13])-[#8:14]-[C;D1;H3:15]>>[C:8]-[C:9](-[C:10])(-[NH;D2;+0:11]-[CH2;D2;+0:7]-[c:6]1:[cH;D2;+0:1]:[#7;a:2]:[c:3]:[#7;a:4]:1-[C:5])-[C:12](=[O;D1;H0:13])-[#8:14]-[C;D1;H3:15]
null
[]
null
null
null
null
The procedure of Example 4 (i), Method A, was followed using a-ethylphenylalanine methyl ester in place of α-methyl-phenylalanine methyl ester to give N-[{1-(2-chlorophenyl)methyl-2-n butyl-1H-imidazol-5-yl}methyl-α-ethylphenylalanine methyl ester. Hydrolysis of the ester using the procedure of Example 2 (ii), followed...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol.Primary amine
Secondary amine
c1c[nH]cn1
c1c[nH]cn1
c1c[nH]cn1.c1ccccc1.c1ccccc1
HCl
null
null
null
CCCCc1nc(Cl)c(CO)n1Cc1ccccc1Cl.CC[C@](N)(Cc1ccccc1)C(=O)OC>>CCCCc1ncc(CN[C@@](CC)(Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-88e25dc0a82b4570b0c9e6e0b265c717
C=O.CCCCc1ncc(CN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl>>CCCCc1ncc(CN(C)[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
Cl.COC([C@@H](NCC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O.C=O>>COC([C@@H](N(C)CC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O
O=[CH2:11].[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH2:9][NH:10][C@@H:12]([CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[C:20](=[O:21])[O:22][CH3:23])[n:24]1[CH2:25][c:26]1[cH:27][cH:28][cH:29][cH:30][c:31]1[Cl:32]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH2:9][N:10]([CH3:11])[C@@H:12]([C...
C=O.CCCCc1ncc(CN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
CCCCc1ncc(CN(C)[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
null
null
C(=O)O
Heteroatom Alkylation and Arylation
Eschweiler-Clarke Secondary Amine Methylation
deb0f39510ff32c3bd75ceaf7ece4070b1f686ff120d798ccd640765025dab3c
e1fdef8fde1c506d7c9deb8fd5e6f322eceea2abce3167abcf412a1fa4fd5443
c1ccc(CCNCc2cncn2Cc2ccccc2)cc1
O=[CH2;D1;+0:1].[#7;a:2]:[c:3](-[C:4]-[NH;D2;+0:5]-[C:6](-[C:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C;D1;H3:11]):[c:12]:[#7;a:13]>>[#7;a:2]:[c:3](-[C:4]-[N;H0;D3;+0:5](-[CH3;D1;+0:1])-[C:6](-[C:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C;D1;H3:11]):[c:12]:[#7;a:13]
70.4
[{"value": 70.0, "product": "COC([C@@H](N(C)CC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.4, "product": "COC([C@@H](N(C)CC1=CN=C(N1CC1=C(C=CC=C1)Cl)CCCC)CC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
N-[{1-[(2-Chlorophenyl)methyl]-2-n-butyl-1H-imidazol-5-yl}methyl]phenylalanine methyl ester (prepared in Example 3(i) method B) (o.52 g, 1.18 mmol), 88% formic acid (0.31 g), and 37% aqueous formaldehyde (o.44 g) were heated over a steam bath for 18 hours. The reaction mixture was poured into 10% hydrochloric acid solu...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Secondary amine
Tertiary amine
null
null
c1c[nH]cn1.c1ccccc1.c1ccccc1
Other
C(=O)O
null
null
C=O.CCCCc1ncc(CN[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl>C(=O)O>CCCCc1ncc(CN(C)[C@@H](Cc2ccccc2)C(=O)OC)n1Cc1ccccc1Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4abdcb5f4ce64f6f9dc993a5b72d5eb7
CCCCc1ncc(COC(C)=O)n1C(C)=O.OCCC12CC3CC(CC(C3)C1)C2>>CCCCc1ncc(COC(C)=O)n1CCC12CC3CC(CC(C3)C1)C2
C12(CC3CC(CC(C1)C3)C2)CCO.C(C)(C)N(CC)C(C)C.C(C)(=O)N1C(=NC=C1COC(C)=O)CCCC.S(=O)(=O)(C(F)(F)F)OS(=O)(=O)C(F)(F)F>>C(C)(=O)OCC1=CN=C(N1CCC12CC3CC(CC(C1)C3)C2)CCCC
CC(=O)[n:14]1[c:5]([CH2:4][CH2:3][CH2:2][CH3:1])[n:6][cH:7][c:8]1[CH2:9][O:10][C:11]([CH3:12])=[O:13].O[CH2:15][CH2:16][C:17]12[CH2:18][CH:19]3[CH2:20][CH:21]([CH2:22][CH:23]([CH2:24]3)[CH2:25]1)[CH2:26]2>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([CH2:9][O:10][C:11]([CH3:12])=[O:13])[n:14]1[CH2:15][CH2:16][C:...
CCCCc1ncc(COC(C)=O)n1C(C)=O.OCCC12CC3CC(CC(C3)C1)C2
CCCCc1ncc(COC(C)=O)n1CCC12CC3CC(CC(C3)C1)C2
null
null
C(Cl)Cl.CO.C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
c9c7310a5bc60da55b1f395ba76d921b3153fead201d0dda950cbe942da07ef7
2ab4024aa17b6e89368e6fe8ee731d32c7611cb9b23de403e301e8362fea90b1
c1cn(CCC23CC4CC(CC(C4)C2)C3)cn1
C-C(=O)-[n;H0;D3;+0:1]1:[c:2](-[C:3]):[#7;a:4]:[c:5]:[c:6]:1-[C:7].O-[CH2;D2;+0:8]-[C:9]-[C:10]>>[C:10]-[C:9]-[CH2;D2;+0:8]-[n;H0;D3;+0:1]1:[c:2](-[C:3]):[#7;a:4]:[c:5]:[c:6]:1-[C:7]
null
[]
null
null
4
DAY
A mixture of 2-(1-adamantyl)ethanol (10.7 g) and diisopropylethylamine (11 ml) in methylene chloride (70 ml) was added to triflic anhydride (16.75 g) in 70 ml of methylene chloride at -78° C. for 45 minutes, 1-acetyl-2-n-butyl 5-acetoxymethyl imidazole in 50 ml of methylene chloride was added and the mixture was allowe...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
null
c1cnc[nH]1
c1c[nH]cn1
c1c[nH]cn1.C1C2CC3CC1CC(C2)C3
HO-
C(Cl)Cl.CO.C(Cl)(Cl)Cl
null
96
CCCCc1ncc(COC(C)=O)n1C(C)=O.OCCC12CC3CC(CC(C3)C1)C2>C(Cl)Cl.CO.C(Cl)(Cl)Cl>CCCCc1ncc(COC(C)=O)n1CCC12CC3CC(CC(C3)C1)C2
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7b615b850a714ed28667ec5cac687e9c
CCCCc1nc(Cl)c(CN[C@@H](Cc2ccccc2)C(=O)O)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1cccs1.COC(=O)c1ccc(CBr)cc1>>CCCCc1ncc(CN[C@@H](Cc2cccs2)C(=O)O)n1Cc1ccc(C(=O)O)cc1
C(CCC)C=1N(C(=C(N1)Cl)CO)CC1=C(C=CC=C1)Cl.COC([C@@H](N)CC=1SC=CC1)=O.C(=O)(OC)C1=CC=C(CBr)C=C1.COC([C@@H](N)CC1=CC=CC=C1)=O.C(#N)[BH3-].[Na+].[BH4-].[Na+].ClC1=C(C=CC=C1)CN1C(=NC(=C1CN[C@@H](CC1=CC=CC=C1)C(=O)O)Cl)CCCC>>C(=O)(O)C1=CC=C(C=C1)CN1C(=NC=C1CN[C@@H](CC=1SC=CC1)C(=O)O)CCCC
O=C(O)[C@H](Cc1ccccc1)N[CH2:9][c:8]1[c:7](Cl)[n:6][c:5]([CH2:4][CH2:3][CH2:2][CH3:1])[n:21]1Cc1ccccc1Cl.C[O:20][C:18]([C@@H:11]([NH2:10])[CH2:12][c:13]1[cH:14][cH:15][cH:16][s:17]1)=[O:19].C[O:29][C:27]([c:26]1[cH:25][cH:24][c:23]([CH2:22]Br)[cH:31][cH:30]1)=[O:28]>>[CH3:1][CH2:2][CH2:3][CH2:4][c:5]1[n:6][cH:7][c:8]([C...
CCCCc1nc(Cl)c(CN[C@@H](Cc2ccccc2)C(=O)O)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1cccs1.COC(=O)c1ccc(CBr)cc1
CCCCc1ncc(CN[C@@H](Cc2cccs2)C(=O)O)n1Cc1ccc(C(=O)O)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
abbcf6d4fbda0f95f8d47a1eea51d1d5ab4b6319e2f4833399a3a30ee465bd65
7bbdf5a711431b9eda0cebdcd4441ee7870943efe7023c11bfcc3df4436fe9ae
c1ccc(Cn2cncc2CNCCc2cccs2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].C-[O;H0;D2;+0:5]-[C:6](=[O;D1;H0:7])-[c:8].C-[O;H0;D2;+0:9]-[C:10](=[O;D1;H0:11])-[C:12](-[C:13])-[NH2;D1;+0:14].Cl-[c;H0;D3;+0:15]1:[#7;a:16]:[c:17](-[C:18]):[n;H0;D3;+0:19](-C-c2:c:c:c:c:c:2-Cl):[c:20]:1-[CH2;D2;+0:21]-N-[C@H](-C-c1:c:c:c:c:c:1)-C(-O)=O>>[C:13]-[C:12](-[NH;D2;+0:1...
null
[]
null
null
null
null
The title compound was prepared following the procedure of Example 3 [(i) method B and (ii)] replacing 2-chlorobenzyl bromide with 4-carbomethoxybenzyl bromide, phenylalanine methyl ester with β-(2-thienyl)alanine methyl ester and sodium cyanoborohydride with sodium borohydride; mp 151°-152° C. Conditions: See reaction...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Primary halide.Carboxylic acid.Ester.Ester.Primary amine.Secondary amine
Carboxylic acid.Carboxylic acid.Secondary amine
c1ccccc1.c1c[nH]cn1.c1ccccc1
c1c[nH]cn1
c1c[nH]cn1.c1ccsc1.c1ccccc1
HCl.Br-
null
null
null
CCCCc1nc(Cl)c(CN[C@@H](Cc2ccccc2)C(=O)O)n1Cc1ccccc1Cl.COC(=O)[C@@H](N)Cc1cccs1.COC(=O)c1ccc(CBr)cc1>>CCCCc1ncc(CN[C@@H](Cc2cccs2)C(=O)O)n1Cc1ccc(C(=O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d099e8b2015d49a88b10fcd0cbfb9273
C#Cc1cccc(OCc2ccc(OC)cc2)c1.CON(C)C(=O)c1ccccc1>>COc1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
CON(C(C1=CC=CC=C1)=O)C.C[Si](N[Si](C)(C)C)(C)C.[Li].COC1=CC=C(COC=2C=C(C=CC2)C#C)C=C1>>C1(=CC=CC=C1)C(C#CC1=CC(=CC=C1)OCC1=CC=C(C=C1)OC)=O
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][O:8][c:9]2[cH:10][cH:11][cH:12][c:13]([C:14]#[CH:15])[cH:24]2)[cH:25][cH:26]1.CON(C)[C:16](=[O:17])[c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][O:8][c:9]2[cH:10][cH:11][cH:12][c:13]([C:14]#[C:15][C:16](=[O:17])[c:18]3[cH:19][cH:20][...
C#Cc1cccc(OCc2ccc(OC)cc2)c1.CON(C)C(=O)c1ccccc1
COc1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
null
null
O1CCCC1
C-C Coupling
OtherReaction
70300835c4109ac6dd5d70878496806f120b832b4507de4dfe0bbdc19bbdd827
67d51335ef436619c1a58767ff7244203654d1fbbffcdb7f79bf5d30a9071b21
O=C(C#Cc1cccc(OCc2ccccc2)c1)c1ccccc1
C-O-N(-C)-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8])-[c:3](:[c:4]):[c:5]
null
[]
0
CELSIUS
45
MINUTE
Place lithium hexamethyldisilazane (2 mL of a 1M solution in tetrahydrofuran, 2 mmol) and tetrahydrofuran (8 mL) under an argon atmosphere and cool to 0° C. Add a solution of 3-(4-methoxybenzyloxy)phenylacetylene (0.48 g, 2 mmol) in tetrahydrofuran and stir the brown solution for 45 minutes at 0° C. Add N-methoxy-N-met...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Alkyne
Ketone
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HO-
O1CCCC1
0
0.75
C#Cc1cccc(OCc2ccc(OC)cc2)c1.CON(C)C(=O)c1ccccc1>O1CCCC1>COc1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b6c9f2f23d2345ee9bd3354a56c32325
CNOC.COc1cc(C(=O)Cl)cc(OC)c1OC>>COc1cc(C(=O)N(C)OC)cc(OC)c1OC
COC=1C=C(C(=O)Cl)C=C(C1OC)OC.Cl.CNOC.N1=CC=CC=C1>>CON(C(C1=CC(=C(C(=C1)OC)OC)OC)=O)C
[NH:8]([CH3:9])[O:10][CH3:11].Cl[C:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:16]([O:17][CH3:18])[c:13]([O:14][CH3:15])[cH:12]1)=[O:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[N:8]([CH3:9])[O:10][CH3:11])[cH:12][c:13]([O:14][CH3:15])[c:16]1[O:17][CH3:18]
CNOC.COc1cc(C(=O)Cl)cc(OC)c1OC
COc1cc(C(=O)N(C)OC)cc(OC)c1OC
null
null
C(C)O
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[#8:7]-[NH;D2;+0:8]-[C;D1;H3:9]>>[C;D1;H3:6]-[#8:7]-[N;H0;D3;+0:8](-[C;D1;H3:9])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
97.9
[{"value": 97.9, "product": "CON(C(C1=CC(=C(C(=C1)OC)OC)OC)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
1
HOUR
Dissolve 3,4,5-trimethoxybenzoyl chloride (2.3 g, 10 mmol) and N,O-dimethylhydroxylamine hydrochloride (1.10 g, 11 mmol) in ethanol-free chloroform at room temperature. Cool the solution to 0° C. and add pyridine (1.85 g, 22 mmol). Stir at ambient temperature for 1 hour and evaporate the solvent in vacuo. Partition the...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccccc1
HCl
C(C)O
0
1
CNOC.COc1cc(C(=O)Cl)cc(OC)c1OC>C(C)O>COc1cc(C(=O)N(C)OC)cc(OC)c1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-49f779f24ab24cde9206b27accb4fa10
C#Cc1ccccc1.COc1cc(C(=O)N(C)OC)cc(OC)c1OC>>COc1cc(C(=O)C#Cc2ccccc2)cc(OC)c1OC
CON(C(C1=CC(=C(C(=C1)OC)OC)OC)=O)C.C[Si](N[Si](C)(C)C)(C)C.[Li].C1(=CC=CC=C1)C#C>>COC=1C=C(C=C(C1OC)OC)C(C#CC1=CC=CC=C1)=O
[CH:8]#[C:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.CON(C)[C:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:20]([O:21][CH3:22])[c:17]([O:18][CH3:19])[cH:16]1)=[O:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[C:8]#[C:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[cH:16][c:17]([O:18][CH3:19])[c:20]1[O:21][CH3:22]
C#Cc1ccccc1.COc1cc(C(=O)N(C)OC)cc(OC)c1OC
COc1cc(C(=O)C#Cc2ccccc2)cc(OC)c1OC
null
null
O1CCCC1
C-C Coupling
OtherReaction
70300835c4109ac6dd5d70878496806f120b832b4507de4dfe0bbdc19bbdd827
67d51335ef436619c1a58767ff7244203654d1fbbffcdb7f79bf5d30a9071b21
O=C(C#Cc1ccccc1)c1ccccc1
C-O-N(-C)-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8])-[c:3](:[c:4]):[c:5]
34.9
[{"value": 34.9, "product": "COC=1C=C(C=C(C1OC)OC)C(C#CC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Place lithium hexamethyldisilazane (3 mL of a 1M solution in tetrahydrofuran, 3 mmol) and tetrahydrofuran (10 mL) under an argon atmosphere and cool to 0° C. Add phenylacetylene (0.33 mL, 3 mmol) and stir at 0° C. for 30 minutes. Add N-methoxy-N-methyl-(3,4,5-trimethoxy)benzamide (0.76 g, 3 mmol), remove the cooling ba...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Alkyne
Ketone
null
null
c1ccccc1.c1ccccc1
HO-
O1CCCC1
null
1
C#Cc1ccccc1.COc1cc(C(=O)N(C)OC)cc(OC)c1OC>O1CCCC1>COc1cc(C(=O)C#Cc2ccccc2)cc(OC)c1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2aabad6285ab40aaa1f0ffe29c00c7a8
C#Cc1ccccc1.CON(C)C(=O)c1ccccc1>>O=C(C#Cc1ccccc1)c1ccccc1
C1(=CC=CC=C1)C#C.CON(C(C1=CC=CC=C1)=O)C.C(C)(C)[N-]C(C)C.[Li+].O1CCCC1>>C1(=CC=CC=C1)C(C#CC1=CC=CC=C1)=O
[CH:3]#[C:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1.CON(C)[C:2](=[O:1])[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[O:1]=[C:2]([C:3]#[C:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
C#Cc1ccccc1.CON(C)C(=O)c1ccccc1
O=C(C#Cc1ccccc1)c1ccccc1
null
null
C1CCCCC1
C-C Coupling
OtherReaction
70300835c4109ac6dd5d70878496806f120b832b4507de4dfe0bbdc19bbdd827
67d51335ef436619c1a58767ff7244203654d1fbbffcdb7f79bf5d30a9071b21
O=C(C#Cc1ccccc1)c1ccccc1
C-O-N(-C)-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8])-[c:3](:[c:4]):[c:5]
61.4
[{"value": 61.4, "product": "C1(=CC=CC=C1)C(C#CC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
Place lithium diisopropylamide (10 mL of a 1.5M solution in cyclohexane) and tetrahydrofuran (40 mL) under an argon atmosphere and cool to 0° C. Add, by dropwise addition, phenylacetylene (1.65 mL, 15 mmol). Remove the cooling bath and stir for 30 minutes as room temperature. Cool the yellow solution to 0° C. and add, ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Alkyne
Ketone
null
null
c1ccccc1.c1ccccc1
HO-
C1CCCCC1
null
0.5
C#Cc1ccccc1.CON(C)C(=O)c1ccccc1>C1CCCCC1>O=C(C#Cc1ccccc1)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8b7ba583998740be987368a88e5eb0cd
C#Cc1cccc(OCc2ccccc2)c1.CON(C)C(=O)c1ccccc1>>O=C(C#Cc1cccc(OCc2ccccc2)c1)c1ccccc1
CON(C(C1=CC=CC=C1)=O)C.C[Si](N[Si](C)(C)C)(C)C.[Li].C(C1=CC=CC=C1)OC=1C=C(C=CC1)C#C>>C1(=CC=CC=C1)C(C#CC1=CC(=CC=C1)OCC1=CC=CC=C1)=O
[CH:3]#[C:4][c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18]1.CON(C)[C:2](=[O:1])[c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1>>[O:1]=[C:2]([C:3]#[C:4][c:5]1[cH:6][cH:7][cH:8][c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18]1)[c:19]1[cH:20][cH:21][cH:22...
C#Cc1cccc(OCc2ccccc2)c1.CON(C)C(=O)c1ccccc1
O=C(C#Cc1cccc(OCc2ccccc2)c1)c1ccccc1
null
null
O1CCCC1
C-C Coupling
OtherReaction
70300835c4109ac6dd5d70878496806f120b832b4507de4dfe0bbdc19bbdd827
67d51335ef436619c1a58767ff7244203654d1fbbffcdb7f79bf5d30a9071b21
O=C(C#Cc1cccc(OCc2ccccc2)c1)c1ccccc1
C-O-N(-C)-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8])-[c:3](:[c:4]):[c:5]
57
[{"value": 57.0, "product": "C1(=CC=CC=C1)C(C#CC1=CC(=CC=C1)OCC1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.0, "product": "C1(=CC=CC=C1)C(C#CC1=CC(=CC=C1)OCC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
45
MINUTE
Place lithium hexamethyldisilazane (15 mL of a 1M solution in tetrahydrofuran, 15 mmol) and tetrahydrofuran (75 mL) under an argon atmosphere and cool with an ice-water bath. Add, by dropwise addition, a solution of 3-benzyloxyphenylacetylene (3.13 g, 15 mmol) in tetrahydrofuran. Stir at 0° C. for 45 minutes, then add,...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Alkyne
Ketone
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HO-
O1CCCC1
0
0.75
C#Cc1cccc(OCc2ccccc2)c1.CON(C)C(=O)c1ccccc1>O1CCCC1>O=C(C#Cc1cccc(OCc2ccccc2)c1)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ebb9a025acde4ca7b55929f332170217
CCOc1ccc(C=O)cc1>>CCOc1ccc(CO)cc1
C(C)OC1=CC=C(C=O)C=C1.[BH4-].[Na+].Cl>>C(C)OC1=CC=C(CO)C=C1
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH:8]=[O:9])[cH:10][cH:11]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][OH:9])[cH:10][cH:11]1
CCOc1ccc(C=O)cc1
CCOc1ccc(CO)cc1
null
null
C(C)O
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccccc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
Mix 4-ethoxybenzaldehyde (3.3 g, 22 mmol), sodium borohydride (830 mg, 22 mmol) and absolute ethanol (25 mL). Stir at room temperature until the reaction is complete, pour onto dilute hydrochloric acid and extract into ethyl acetate. Separate the organic phase and extract the aqueous phase with ethyl acetate (2×). Comb...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccccc1
null
C(C)O
null
null
CCOc1ccc(C=O)cc1>C(C)O>CCOc1ccc(CO)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-43a0aaa7336a47c9a189d7a4c5585e94
CCOc1ccc(CO)cc1.O=Cc1cccc(O)c1>>CCOc1ccc(COc2cccc(C=O)c2)cc1
C(C)OC1=CC=C(CO)C=C1.OC=1C=C(C=O)C=CC1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>C(C)OC1=CC=C(COC=2C=C(C=O)C=CC2)C=C1
O[CH2:8][c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[cH:19][cH:18]1.[OH:9][c:10]1[cH:11][cH:12][cH:13][c:14]([CH:15]=[O:16])[cH:17]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][c:14]([CH:15]=[O:16])[cH:17]2)[cH:18][cH:19]1
CCOc1ccc(CO)cc1.O=Cc1cccc(O)c1
CCOc1ccc(COc2cccc(C=O)c2)cc1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Mitsunobu aryl ether
86bfb73617450d22f9456ed5ce4d96a73f1f8fc0c016bebae57fda68e2da86a2
2258bd14c3b5449b92dc09cf9fa522f88d5071b4af20f7e968b60aa1ae6db0cf
c1ccc(COc2ccccc2)cc1
O-[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]
null
[]
null
null
null
null
Mix 4-ethoxybenzyl alcohol (3.35 g. 22 mmol), 3-hydroxybenzaldehyde (2.69 g, 22 mmol), triphenylphosphine (5.8 g, 22 mmol) and diethylazadicarboxylate (3.83 g, 22 mmol) in tetrahydrofuran (25 mL). Stir at room temperature under anhydrous atmosphere until the reaction is done. Concentrate the solution in vacuo and dilut...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HO-
O1CCCC1
null
null
CCOc1ccc(CO)cc1.O=Cc1cccc(O)c1>O1CCCC1>CCOc1ccc(COc2cccc(C=O)c2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6297d7b87210484783ae1ce1e663fd0f
C#Cc1cccc(OCc2ccc(OCC)cc2)c1.CON(C)C(=O)c1ccccc1>>CCOc1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
CON(C(C1=CC=CC=C1)=O)C.C[Si](N[Si](C)(C)C)(C)C.[Li].C(C)OC1=CC=C(COC=2C=C(C=CC2)C#C)C=C1>>C1(=CC=CC=C1)C(C#CC1=CC(=CC=C1)OCC1=CC=C(C=C1)OCC)=O
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][c:14]([C:15]#[CH:16])[cH:25]2)[cH:26][cH:27]1.CON(C)[C:17](=[O:18])[c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][c:14]([C:15]#[C:16][C:17](=[O:18])[c:19]...
C#Cc1cccc(OCc2ccc(OCC)cc2)c1.CON(C)C(=O)c1ccccc1
CCOc1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
null
null
O1CCCC1
C-C Coupling
OtherReaction
70300835c4109ac6dd5d70878496806f120b832b4507de4dfe0bbdc19bbdd827
67d51335ef436619c1a58767ff7244203654d1fbbffcdb7f79bf5d30a9071b21
O=C(C#Cc1cccc(OCc2ccccc2)c1)c1ccccc1
C-O-N(-C)-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8])-[c:3](:[c:4]):[c:5]
null
[]
0
CELSIUS
45
MINUTE
Place lithium hexamethyldisilazane (2 mL of a 1M solution in tetrahydrofuran, 2 mmol) and tetrahydrofuran (8 mL) under an argon atmosphere and cool to 0° C. Add a solution of 3-(4-ethoxybenzyloxy)phenylacetylene (0.51 g, 2 mmol) in tetrahydrofuran and stir the solution for 45 minutes at 0° C. Add N-methoxy-N-methylbenz...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Alkyne
Ketone
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HO-
O1CCCC1
0
0.75
C#Cc1cccc(OCc2ccc(OCC)cc2)c1.CON(C)C(=O)c1ccccc1>O1CCCC1>CCOc1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d66256aab42c4645ba01c94ac4791f03
CN(C)c1ccc(C=O)cc1>>CN(C)c1ccc(CO)cc1
CN(C1=CC=C(C=O)C=C1)C.[BH4-].[Na+].Cl>>CN(C1=CC=C(CO)C=C1)C
[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7]([CH:8]=[O:9])[cH:10][cH:11]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7]([CH2:8][OH:9])[cH:10][cH:11]1
CN(C)c1ccc(C=O)cc1
CN(C)c1ccc(CO)cc1
null
null
C(C)O
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccccc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
Mix 4-dimethylaminobenzaldehyde (3.3 g, 22 mmol), sodium borohydride (830 mg, 22 mmol) and absolute ethanol (25 mL). Stir at room temperature until the reaction is complete, pour onto dilute hydrochloric acid and extract into ethyl acetate. Separate the organic phase and extract the aqueous phase with ethyl acetate (2×...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccccc1
null
C(C)O
null
null
CN(C)c1ccc(C=O)cc1>C(C)O>CN(C)c1ccc(CO)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7100e9edbf604a50bcb345884fc1b480
CN(C)c1ccc(CO)cc1.O=Cc1cccc(O)c1>>CN(C)c1ccc(COc2cccc(C=O)c2)cc1
CN(C1=CC=C(CO)C=C1)C.OC=1C=C(C=O)C=CC1.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>CN(C1=CC=C(COC=2C=C(C=O)C=CC2)C=C1)C
O[CH2:8][c:7]1[cH:6][cH:5][c:4]([N:2]([CH3:1])[CH3:3])[cH:19][cH:18]1.[OH:9][c:10]1[cH:11][cH:12][cH:13][c:14]([CH:15]=[O:16])[cH:17]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7]([CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][c:14]([CH:15]=[O:16])[cH:17]2)[cH:18][cH:19]1
CN(C)c1ccc(CO)cc1.O=Cc1cccc(O)c1
CN(C)c1ccc(COc2cccc(C=O)c2)cc1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Mitsunobu aryl ether
86bfb73617450d22f9456ed5ce4d96a73f1f8fc0c016bebae57fda68e2da86a2
2258bd14c3b5449b92dc09cf9fa522f88d5071b4af20f7e968b60aa1ae6db0cf
c1ccc(COc2ccccc2)cc1
O-[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]
null
[]
null
null
null
null
Mix 4-(dimethylamino)benzyl alcohol (3.35 g. 22 mmol), 3-hydroxybenzaldehyde (2.69 g, 22 mmol), triphenylphosphine (5.8 g, 22 mmol) and diethylazadicarboxylate (3.83 g, 22 mmol) in tetrahydrofuran (25 mL). Stir at room temperature under anhydrous atmosphere until the reaction is done. Concentrate the solution in vacuo ...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HO-
O1CCCC1
null
null
CN(C)c1ccc(CO)cc1.O=Cc1cccc(O)c1>O1CCCC1>CN(C)c1ccc(COc2cccc(C=O)c2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1dcbf41e8a1e4ec0990437ca83de30a4
C#Cc1cccc(OCc2ccc(N(C)C)cc2)c1.CON(C)C(=O)c1ccccc1>>CN(C)c1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
CON(C(C1=CC=CC=C1)=O)C.C[Si](N[Si](C)(C)C)(C)C.[Li].CN(C1=CC=C(COC=2C=C(C=CC2)C#C)C=C1)C>>C1(=CC=CC=C1)C(C#CC1=CC(=CC=C1)OCC1=CC=C(C=C1)N(C)C)=O
[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7]([CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][c:14]([C:15]#[CH:16])[cH:25]2)[cH:26][cH:27]1.CON(C)[C:17](=[O:18])[c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7]([CH2:8][O:9][c:10]2[cH:11][cH:12][cH:13][c:14]([C:15]#[C:16][C:17](=[O:18])[c...
C#Cc1cccc(OCc2ccc(N(C)C)cc2)c1.CON(C)C(=O)c1ccccc1
CN(C)c1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
null
null
O1CCCC1
C-C Coupling
OtherReaction
70300835c4109ac6dd5d70878496806f120b832b4507de4dfe0bbdc19bbdd827
67d51335ef436619c1a58767ff7244203654d1fbbffcdb7f79bf5d30a9071b21
O=C(C#Cc1cccc(OCc2ccccc2)c1)c1ccccc1
C-O-N(-C)-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[C;H0;D2;+0:6]#[C:7]-[c:8])-[c:3](:[c:4]):[c:5]
null
[]
0
CELSIUS
45
MINUTE
Place lithium hexamethyldisilazane (2 mL of a 1M solution in tetrahydrofuran, 2 mmol) and tetrahydrofuran (8 mL) under an argon atmosphere and cool to 0° C. Add a solution of 3-(4-(dimethylamino)benzyloxy)phenylacetylene (0.51 g, 2 mmol) in tetrahydrofuran and stir the solution for 45 minutes at 0° C. Add N-methoxy-N-m...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Alkyne
Ketone
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HO-
O1CCCC1
0
0.75
C#Cc1cccc(OCc2ccc(N(C)C)cc2)c1.CON(C)C(=O)c1ccccc1>O1CCCC1>CN(C)c1ccc(COc2cccc(C#CC(=O)c3ccccc3)c2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c746273d17404f66b6613167aa8be31a
C=CCBr.CCOC(=O)CC(=O)COC1CCCCC1>>C=CCC(C(=O)COC1CCCCC1)C(=O)OCC
[Na].C(C=C)Br.C1(CCCCC1)OCC(CC(=O)OCC)=O>>C1(CCCCC1)OCC(=O)C(C(=O)OCC)CC=C
Br[CH2:3][CH:2]=[CH2:1].[CH2:4]([C:5](=[O:6])[CH2:7][O:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13][CH2:14]1)[C:15](=[O:16])[O:17][CH2:18][CH3:19]>>[CH2:1]=[CH:2][CH2:3][CH:4]([C:5](=[O:6])[CH2:7][O:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13][CH2:14]1)[C:15](=[O:16])[O:17][CH2:18][CH3:19]
C=CCBr.CCOC(=O)CC(=O)COC1CCCCC1
C=CCC(C(=O)COC1CCCCC1)C(=O)OCC
null
null
C(C)O
C-C Coupling
OtherReaction
a419f976441b589a3c956c0f129ce3053512f0325f3e460530d895d12d1b751d
c9d64189f02be16d3a7baf78522635b86019231c97f41522f031694d4f90e5ad
C1CCCCC1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[C:9](-[C:10])=[O;D1;H0:11]>>[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH;D3;+0:8](-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3])-[C:9](-[C:10])=[O;D1;H0:11]
null
[]
50
CELSIUS
2
HOUR
320 g of ethyl 4-cyclohexyloxy-acetoacetate (1.4 mol) are initially introduced into a threenecked flask fitted with a stirrer, dropping funnel, drying tube and reflux condenser, and an Na ethanolate solution prepared from 32 g of sodium (1.4 mol) and 475 g of ethanol is added at 50° C. in the course of 30 minutes. 170 ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone.Ester.Allyl
null
null
C1CCCCC1
HBr
C(C)O
50
2
C=CCBr.CCOC(=O)CC(=O)COC1CCCCC1>C(C)O>C=CCC(C(=O)COC1CCCCC1)C(=O)OCC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-65ad894ecf63452786d85d75967b1990
C=CCC(C(=O)COC1CCCCC1)C(=O)OCC>>C=CCCC(=O)COC1CCCCC1
C1(CCCCC1)OCC(=O)C(C(=O)OCC)CC=C.[OH-].[Na+]>>C1(CCCCC1)OCC(CCC=C)=O
CCOC(=O)[CH:4]([CH2:3][CH:2]=[CH2:1])[C:5](=[O:6])[CH2:7][O:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13][CH2:14]1>>[CH2:1]=[CH:2][CH2:3][CH2:4][C:5](=[O:6])[CH2:7][O:8][CH:9]1[CH2:10][CH2:11][CH2:12][CH2:13][CH2:14]1
C=CCC(C(=O)COC1CCCCC1)C(=O)OCC
C=CCCC(=O)COC1CCCCC1
null
null
CCOCC
Reduction
Decarboxylation
fdc964bea6eaeadfb2309e01318abba99b151c57fdaf3760a2830a6479750a9b
f277909394d9f4e61cc2cdb65fef123102672ca91cfff7f8513cb0baf66138ac
C1CCCCC1
C-C-O-C(=O)-[CH;D3;+0:1](-[C:2]-[C:3]=[C;D1;H2:4])-[C:5](-[C:6])=[O;D1;H0:7]>>[C:6]-[C:5](=[O;D1;H0:7])-[CH2;D2;+0:1]-[C:2]-[C:3]=[C;D1;H2:4]
58.6
[{"value": 58.6, "product": "C1(CCCCC1)OCC(CCC=C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
140 g of ethyl 2-(cyclohexyloxyacetyl)-4-pentenoate are heated under reflux in 650 g of 5% strength aqueous sodium hydroxide solution for 4 hours. 500 ml of ether are added to the reaction mixture. The organic phase is separated off and concentrated and the residue is distilled. About 60 g of 1-cyclohexyloxy-hex-5-en-2...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Ketone
null
null
C1CCCCC1
HO-
CCOCC
null
null
C=CCC(C(=O)COC1CCCCC1)C(=O)OCC>CCOCC>C=CCCC(=O)COC1CCCCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-24c621edc5884c249b64914319a77e74
CCOC(=O)C1(c2ccc(OCC)cc2)CC1(F)F>>CCOc1ccc(C2(CO)CC2(F)F)cc1
[H-].[Al+3].[Li+].[H-].[H-].[H-].C(C)OC(=O)C1(C(C1)(F)F)C1=CC=C(C=C1)OCC.O.[OH-].[Na+].O>>C(C)OC1=CC=C(C=C1)C1(C(C1)(F)F)CO
CCO[C:9]([C:8]1([c:7]2[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[cH:16][cH:15]2)[CH2:11][C:12]1([F:13])[F:14])=[O:10]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8]2([CH2:9][OH:10])[CH2:11][C:12]2([F:13])[F:14])[cH:15][cH:16]1
CCOC(=O)C1(c2ccc(OCC)cc2)CC1(F)F
CCOc1ccc(C2(CO)CC2(F)F)cc1
null
null
CCOCC
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccc(C2CC2)cc1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3]1(-[c:4])-[C:5]-[C:6]-1>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[C:3]1(-[c:4])-[C:5]-[C:6]-1
92
[{"value": 92.0, "product": "C(C)OC1=CC=C(C=C1)C1(C(C1)(F)F)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 1.0 g of lithium aluminium hydride in 120 ml of dry ether, at room temperature is added dropwise 5.4 g (0.02 moles) of ethyl-1-(4-ethoxyphenyl)-2,2-difluorocyclopropane-1-carboxylate in 20 ml of ether. The reaction mixture is stirred for 1 hr after which 1.0 ml of water 1.0 ml of 15% NaOH, followed by 3.0 ml of wate...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1.C1CC1
HO-
CCOCC
null
null
CCOC(=O)C1(c2ccc(OCC)cc2)CC1(F)F>CCOCC>CCOc1ccc(C2(CO)CC2(F)F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4fe44030a62b460f8a5604dcd68ea078
CCOc1ccc(CC#N)cc1>>CCOc1ccc(C2(C#N)CC2)cc1
Cl.C(CCC)[Li].ClCCCl.C(C)OC1=CC=C(C=C1)CC#N>>C(#N)C1(CC1)C1=CC=C(C=C1)OCC
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH2:8][C:9]#[N:10])[cH:13][cH:14]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8]2([C:9]#[N:10])[CH2:11][CH2:12]2)[cH:13][cH:14]1
CCOc1ccc(CC#N)cc1
CCOc1ccc(C2(C#N)CC2)cc1
null
null
CCOCC.CCCCCC.O1CCCC1
C-C Coupling
OtherReaction
ac91075a06a8cce8890c40dac805065f8c8b8f1e346a2fcf9830e69753a8b680
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
c1ccc(C2CC2)cc1
[N;D1;H0:1]#[C:2]-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6]>>[N;D1;H0:1]#[C:2]-[C;H0;D4;+0:3]1(-[c:4](:[c:5]):[c:6])-[C:7]-[C:8]-1
null
[]
null
null
1
HOUR
To 7.5 ml (0.012 mol) of 1.7M n-butyllithium in hexane, at room temperature, under an atmosphere of nitrogen, is added rapidly 10 ml of anhydrous tetrahydrofuran, followed by a solution of 4-ethoxyphenyl acetonitrile (0.8 g 0.005 mol) in 4 ml of tetrahydrofuran, during 5 minutes. The reaction mixture is stirred magneti...
10.6084/m9.figshare.5104873.v1
null
null
null
null
C1CC1
c1ccccc1.C1CC1
Other
CCOCC.CCCCCC.O1CCCC1
null
1
CCOc1ccc(CC#N)cc1>CCOCC.CCCCCC.O1CCCC1>CCOc1ccc(C2(C#N)CC2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ab56fa56606c42aa84ddab96051d6371
CO.Oc1ccccc1O>>COc1ccccc1O.Oc1ccccc1O
CO.C=1(O)C(O)=CC=CC1>>C=1(O)C(O)=CC=CC1.C=1(C(O)=CC=CC1)OC
[CH3:1][OH:2].[cH:3]1[cH:13][cH:12][c:11]([OH:9])[c:16]([OH:17])[cH:15]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[OH:9].[OH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[OH:17]
CO.Oc1ccccc1O
COc1ccccc1O.Oc1ccccc1O
null
null
null
Aromatic Heterocycle Formation
Mitsunobu aryl ether
9a57d4c07a5f6d2cf92579430cfc733994c27a45d88e5ebd02a1e499ac5e35ef
67125d0d97ed0786028bd231bca324496f85d82449ddec65b9084d96e2533ec5
c1ccccc1.c1ccccc1
[C;D1;H3:1]-[OH;D1;+0:2].[O;D1;H1:3]-[c:4]1:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[c:8]:[c;H0;D3;+0:9]:1-[OH;D1;+0:10]>>[C;D1;H3:1]-[O;H0;D2;+0:2]-[c;H0;D3;+0:6](:[c:11]:[c:12]):[c:13](-[OH;D1;+0:10]):[c:14].[O;D1;H1:15]-[c;H0;D3;+0:9]1:[c:8]:[cH;D2;+0:7]:[c:16]:[cH;D2;+0:5]:[c:4]:1-[O;D1;H1:3]
null
[]
null
null
14
HOUR
The catalyst stratum was heated and when the temperature of the catalyst stratum reached 280° C., a starting compound mixture gas consisting of catechol and methyl alcohol in a molar mixing ratio of 1:3.44 and evaporated in an evaporator was fed, at a feeding rate of 10.5 g/min, together with nitrogen gas, into the rea...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Methanol
Ether.Aromatic alcohol.Aromatic alcohol
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Other
null
null
14
CO.Oc1ccccc1O>>COc1ccccc1O.Oc1ccccc1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bef22d2b530d42b096e5b7de282c4ca6
CO.Oc1ccccc1O>>COc1ccccc1O.Oc1ccccc1
C=1(O)C(O)=CC=CC1.CO>>C1(=CC=CC=C1)O.C=1(C(O)=CC=CC1)OC
[CH3:1][OH:2].[c:3]1([OH:10])[cH:4][cH:5][cH:6][cH:7][c:8]1[OH:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[OH:9].[OH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
CO.Oc1ccccc1O
COc1ccccc1O.Oc1ccccc1
null
null
null
Aromatic Heterocycle Formation
Mitsunobu aryl ether
1c408c593650ad66b08f11ab8cf58e8474f9926d90b8b8d7d3991fc69c445d7c
18d36c13c0c32581070c190f4159cf9b3c3365b00512bcecf63fdb4006ec2a66
c1ccccc1.c1ccccc1
[C;D1;H3:1]-[OH;D1;+0:2].[O;D1;H1:3]-[c:4](:[c:5]):[c;H0;D3;+0:6](-[OH;D1;+0:7]):[c:8]:[c:9]>>[C;D1;H3:1]-[O;H0;D2;+0:2]-[c;H0;D3;+0:6](:[c:8]:[c:9]):[c:4](-[O;D1;H1:3]):[c:5].[OH;D1;+0:7]-[c:10](:[c:11]):[c:12]
null
[]
null
null
14
HOUR
When the temperature of the catalyst stratum reached 280° C., a starting compound mixture consisting of catechol and methyl alcohol in a molar mixing ratio of 1:3.44 was evaporated in a evaporator, and the resultant starting compound mixture gas was fed in a feeding rate of 10.5 g/min. together with a nitrogen gas into...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Methanol
Ether.Aromatic alcohol
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Other
null
null
14
CO.Oc1ccccc1O>>COc1ccccc1O.Oc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bc1049bbac104ae6857eeaa65fae9134
CO.Oc1ccccc1O>>COc1ccccc1O.Oc1ccccc1
C=1(O)C(O)=CC=CC1.CO>>C1(=CC=CC=C1)O.C=1(C(O)=CC=CC1)OC
[CH3:1][OH:2].[c:3]1([OH:10])[cH:4][cH:5][cH:6][cH:7][c:8]1[OH:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[OH:9].[OH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
CO.Oc1ccccc1O
COc1ccccc1O.Oc1ccccc1
null
null
null
Aromatic Heterocycle Formation
Mitsunobu aryl ether
1c408c593650ad66b08f11ab8cf58e8474f9926d90b8b8d7d3991fc69c445d7c
18d36c13c0c32581070c190f4159cf9b3c3365b00512bcecf63fdb4006ec2a66
c1ccccc1.c1ccccc1
[C;D1;H3:1]-[OH;D1;+0:2].[O;D1;H1:3]-[c:4](:[c:5]):[c;H0;D3;+0:6](-[OH;D1;+0:7]):[c:8]:[c:9]>>[C;D1;H3:1]-[O;H0;D2;+0:2]-[c;H0;D3;+0:6](:[c:8]:[c:9]):[c:4](-[O;D1;H1:3]):[c:5].[OH;D1;+0:7]-[c:10](:[c:11]):[c:12]
null
[]
null
null
14
HOUR
When the temperature of the catalyst stratum reached 260° C. in Example 43 and 300° C. in Example 44, a starting compound mixture consisting of catechol and methyl alcohol in a mixing molar ratio of 1:3.44 was evaporated in an evaporator, and the resultant starting compound mixture gas was fed in a feeding rate of 10.5...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Methanol
Ether.Aromatic alcohol
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Other
null
null
14
CO.Oc1ccccc1O>>COc1ccccc1O.Oc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-37aaff7b9d20449697e2d1307179b739
CC(C)(Cl)CCC(C)(C)Cl.Oc1ccccc1>>CC1(C)CCC(C)(C)c2cc(O)ccc21
[Cl-].[Al+3].[Cl-].[Cl-].C1(=CC=CC=C1)O.ClC(C)(CCC(C)(C)Cl)C>>CC1(C=2C=CC(=CC2C(CC1)(C)C)O)C
Cl[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6](Cl)([CH3:7])[CH3:8].[cH:9]1[cH:10][c:11]([OH:12])[cH:13][cH:14][cH:15]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([OH:12])[cH:13][cH:14][c:15]21
CC(C)(Cl)CCC(C)(C)Cl.Oc1ccccc1
CC1(C)CCC(C)(C)c2cc(O)ccc21
null
null
null
C-C Coupling
OtherReaction
faa48b683da39df7e0e9cf4df3d89478446096416db2d6e2d979384c88ae8eca
950e3556c1b5e86d9a0ad65231c6585f2d3e11c0ea678211dde9bdb559a1f623
c1ccc2c(c1)CCCC2
Cl-[C;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4]-[C:5]-[C;H0;D4;+0:6](-Cl)(-[C;D1;H3:7])-[C;D1;H3:8].[c:9]1:[c:10]:[c:11]:[c:12]:[cH;D2;+0:13]:[cH;D2;+0:14]:1>>[C;D1;H3:2]-[C;H0;D4;+0:1]1(-[C;D1;H3:3])-[C:4]-[C:5]-[C;H0;D4;+0:6](-[C;D1;H3:7])(-[C;D1;H3:8])-[c;H0;D3;+0:14]2:[c:9]:[c:10]:[c:11]:[c:12]:[c;H0;D3;+0:13]:...
32.1
[{"value": 32.1, "product": "CC1(C=2C=CC(=CC2C(CC1)(C)C)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
48
HOUR
27.5 g (0.2 mol) of anhydrous aluminum chloride were added by spatula to 250.0 g (2.65 mol) of phenol plus 414.5 g (2.27 mol) of 2,5-dichloro-2,5-dimethylhexane in 500 ml of petroleum ether at room temperature while stirring. After 48 hours, the reaction mixture was poured into ice-water and extracted with ether, and t...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide
null
c1ccccc1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HCl
null
null
48
CC(C)(Cl)CCC(C)(C)Cl.Oc1ccccc1>>CC1(C)CCC(C)(C)c2cc(O)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4f2ef7e7bc5d48b9b8a54d0213b449e8
CC1(C)CCC(C)(C)c2ccccc21.O=[N+]([O-])O>>CC1(C)CCC(C)(C)c2cc([N+](=O)[O-])ccc21
[N+](=O)(O)[O-].CC1(CCC(C2=CC=CC=C12)(C)C)C>>[N+](=O)([O-])C1=CC=2C(CCC(C2C=C1)(C)C)(C)C
[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:15][cH:16][c:17]21.O[N+:12](=[O:13])[O-:14]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([N+:12](=[O:13])[O-:14])[cH:15][cH:16][c:17]21
CC1(C)CCC(C)(C)c2ccccc21.O=[N+]([O-])O
CC1(C)CCC(C)(C)c2cc([N+](=O)[O-])ccc21
null
null
C(C)(=O)O.C(C)(=O)OC(C)=O
Functional Group Addition
Aromatic nitration with HNO3
5993c528ef8bcdffbf8c0a893a552b598272f75e0f1825b53fb570da12e0cd5d
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccc2c(c1)CCCC2
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;D1;H0:3])-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:5]:[c:4]
null
[]
null
null
8
HOUR
77.2 ml of glacial acetic acid and 20.8 ml of nitric acid (98% strength) were mixed while cooling and then added dropwise within 2 hours to a solution of 65.8 g (0.35 mol) of 1,2,3,4-tetrahydro-1,1,4,4-tetramethylnaphthalene in 154 ml of glacial acetic acid and 257 ml of acetic anhydride in a salt/ice bath. After the a...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
C(C)(=O)O.C(C)(=O)OC(C)=O
null
8
CC1(C)CCC(C)(C)c2ccccc21.O=[N+]([O-])O>C(C)(=O)O.C(C)(=O)OC(C)=O>CC1(C)CCC(C)(C)c2cc([N+](=O)[O-])ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-870f165d08ed449088d95aa4882d0671
CC1(C)CCC(C)(C)c2ccccc21.O=S(=O)(O)Cl>>CC1(C)CCC(C)(C)c2cc(S(=O)(=O)Cl)ccc21
CC1(CCC(C2=CC=CC=C12)(C)C)C.ClS(=O)(=O)O>>CC1(C=2C=CC(=CC2C(CC1)(C)C)S(=O)(=O)Cl)C
[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:16][cH:17][c:18]21.O=[S:12]([OH:13])(=[O:14])[Cl:15]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([S:12](=[O:13])(=[O:14])[Cl:15])[cH:16][cH:17][c:18]21
CC1(C)CCC(C)(C)c2ccccc21.O=S(=O)(O)Cl
CC1(C)CCC(C)(C)c2cc(S(=O)(=O)Cl)ccc21
null
null
null
Protection
Aromatic sulfonyl chlorination
8571fb317e67ad387a94c9ed0cf7dddce67335d5f8173100c517d9514fb0d882
c731d053565135be022f3edbe36cf28a9b4364ca579bdb183b2db9578bab4695
c1ccc2c(c1)CCCC2
O=[S;H0;D4;+0:1](-[Cl;D1;H0:2])(=[O;D1;H0:3])-[OH;D1;+0:4].[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[Cl;D1;H0:2]-[S;H0;D4;+0:1](=[O;D1;H0:3])(=[O;H0;D1;+0:4])-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:6]:[c:5]
null
[]
60
CELSIUS
null
null
94.0 g (0.5 mol) of 1,2,3,4-tetrahydro-1,1,4,4-tetramethylnaphthalene were stirred into 100 ml of chlorosulfonic acid at 20° C. within 30 min. The reaction solution was maintained at 60° C. for 1 hour, cooled to room temperature and then poured into 1.5 l of ice and extracted with ether. The organic phase was washed to...
10.6084/m9.figshare.5104873.v1
null
null
Sulfonyl halide
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
null
60
null
CC1(C)CCC(C)(C)c2ccccc21.O=S(=O)(O)Cl>>CC1(C)CCC(C)(C)c2cc(S(=O)(=O)Cl)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2312dd61119e4794b7fcad57c714dd9a
CC1(C)CCC(C)(C)c2cc(O)ccc21.N#Cc1ccc(CCl)cc1>>CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21
CC1(C=2C=CC(=CC2C(CC1)(C)C)O)C.C(#N)C1=CC=C(CCl)C=C1.C([O-])([O-])=O.[K+].[K+].O>>CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C#N)C
[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([OH:12])[cH:22][cH:23][c:24]21.Cl[CH2:13][c:14]1[cH:15][cH:16][c:17]([C:18]#[N:19])[cH:20][cH:21]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][c:17]([C:18]#[N:19])[cH:20...
CC1(C)CCC(C)(C)c2cc(O)ccc21.N#Cc1ccc(CCl)cc1
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21
null
null
CC(CC)=O.CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2ccc3c(c2)CCCC3)cc1
Cl-[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]
98.6
[{"value": 98.6, "product": "CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C#N)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
40.8 g (0.2 mol) of 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthol, 30.4 g (0.2 mol) of 4-cyanobenzyl chloride and 80 g (1.2 mol) of anhydrous potassium carbonate in 400 ml of butanone and 300 ml of dimethylformamide were refluxed for 9 h. The mixture was cooled and then poured into 1.5 l of water, and the solid was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
HCl
CC(CC)=O.CN(C=O)C
null
null
CC1(C)CCC(C)(C)c2cc(O)ccc21.N#Cc1ccc(CCl)cc1>CC(CC)=O.CN(C=O)C>CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-db4c527265944cbe953069fef82d126e
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21.O.[OH-]>>CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21
Cl.CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C#N)C.[OH-].[Na+].O>>CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C(=O)O)C
N#[C:18][c:17]1[cH:16][cH:15][c:14]([CH2:13][O:12][c:11]2[cH:10][c:9]3[c:25]([cH:24][cH:23]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]3([CH3:7])[CH3:8])[cH:22][cH:21]1.[OH2:20].[OH-:19]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][c:17]([C:18](=[O:...
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21.O.[OH-]
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21
null
null
C(C)O
Acylation
OtherReaction
e05c34ebe51fe654c61f91bb118ee544dcd0a035df9f073c07f2e1b77a1f299a
e722778fc7d66899e0f2f256942c8c213a77617f32bb1410d97747833c62e260
c1ccc(COc2ccc3c(c2)CCCC3)cc1
N#[C;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH-;D0:5].[OH2;D0;+0:6]>>[O;H0;D1;+0:5]=[C;H0;D3;+0:1](-[OH;D1;+0:6])-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
20 g (0.063 mol) of 4-cyanobenzyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl ether were refluxed with 163 ml of 10N sodium hydroxide solution in 245 ml of ethanol for 2 h. The mixture was cooled and then poured into water, which was then acidified with hydrochloric acid, and the precipitate was filtered off with...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Carboxylic acid
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
Other
C(C)O
null
null
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21.O.[OH-]>C(C)O>CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-29b56e7bfb744771ab87ed2781bf6d17
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21>>CC1(C)CCC(C)(C)c2cc(OCc3ccc(C=O)cc3)ccc21
S(=O)(=O)([O-])[O-].[Na+].[Na+].[H-].C(C(C)C)[Al+]CC(C)C.CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C#N)C.C(C(O)C(O)C(=O)O)(=O)O>>CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C=O)C
N#[C:18][c:17]1[cH:16][cH:15][c:14]([CH2:13][O:12][c:11]2[cH:10][c:9]3[c:24]([cH:23][cH:22]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]3([CH3:7])[CH3:8])[cH:21][cH:20]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][c:17]([CH:18]=[O:19])[cH:20][cH:21]...
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C=O)cc3)ccc21
null
null
CCOCC
Functional Group Interconversion
OtherReaction
aa5d6273be01dadb1e5fec75e16ca9b6066d03aa195b40fe3322b26fa6d0b811
9f36587406d4620bb1f6625b2c5b8279180c3bebdc2492867ca9e2e72e879d2d
c1ccc(COc2ccc3c(c2)CCCC3)cc1
N#[C;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[O;D1;H0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
25
CELSIUS
40
MINUTE
15.5 ml (19.7 mmol) of diisobutylaluminum hydride solution (20% in hexane) were added dropwise under nitrogen to a solution of 3 g (9.4 mmol) of 4-cyanobenzyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl ether in 40 ml of dry ether at 25° C. The mixture was stirred at 25° C. for 40 min and then 250 ml of saturated...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Aldehyde
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
null
CCOCC
25
0.666667
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21>CCOCC>CC1(C)CCC(C)(C)c2cc(OCc3ccc(C=O)cc3)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8d935727faf84d70b9ee58a54f250c2e
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21>>CC1(C)CCC(C)(C)c2cc(OCc3ccc(CN)cc3)ccc21
S(=O)(=O)([O-])[O-].[Na+].[Na+].CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C#N)C.[H-].[Al+3].[Li+].[H-].[H-].[H-].O>>CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)CN)C
[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][c:17]([C:18]#[N:19])[cH:20][cH:21]3)[cH:22][cH:23][c:24]21>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][c:17]([CH2:18][NH2:19])[cH:20]...
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21
CC1(C)CCC(C)(C)c2cc(OCc3ccc(CN)cc3)ccc21
null
null
CCOCC
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
c1ccc(COc2ccc3c(c2)CCCC3)cc1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[NH2;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A suspension of 3 g (9.4 mmol) of 4-cyanobenzyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl ether in 60 ml of ether was added dropwise under nitrogen to a suspension of 1 g (26 mmol) of lithium aluminum hydride in 50 ml of dry ether at 25° C. The mixture was then stirred under reflux for 3 h, cooled and hydrolyze...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
null
CCOCC
null
null
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C#N)cc3)ccc21>CCOCC>CC1(C)CCC(C)(C)c2cc(OCc3ccc(CN)cc3)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-55e65ba344a54615b9308935a326faf5
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21>>CC1(C)CCC(C)(C)c2cc(OCc3ccc(CO)cc3)ccc21
ClC(=O)OCC.CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C(=O)O)C.C(C)N(CC)CC.[BH4-].[Na+].Cl>>CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)CO)C
O=[C:18]([c:17]1[cH:16][cH:15][c:14]([CH2:13][O:12][c:11]2[cH:10][c:9]3[c:24]([cH:23][cH:22]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]3([CH3:7])[CH3:8])[cH:21][cH:20]1)[OH:19]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([O:12][CH2:13][c:14]3[cH:15][cH:16][c:17]([CH2:18][OH:19])[cH:...
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21
CC1(C)CCC(C)(C)c2cc(OCc3ccc(CO)cc3)ccc21
null
null
O.O1CCCC1
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
c1ccc(COc2ccc3c(c2)CCCC3)cc1
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[c:3](:[c:4]):[c:5]>>[O;D1;H1:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
37.7
[{"value": 37.7, "product": "CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)CO)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
A solution of 0.97 g (9 mmol) of ethyl chloroformate in 5 ml of tetrahydrofuran was added dropwise to a solution of 3 g (9 mmol) of 4-carboxybenzyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl ether and 0.9 g (9 mmol) of triethylamine in 20 ml of dry tetrahydrofuran at 0° C. The mixture was stirred at 0° C for 30 ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
Other
O.O1CCCC1
0
0.5
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21>O.O1CCCC1>CC1(C)CCC(C)(C)c2cc(OCc3ccc(CO)cc3)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-508e4f8861e640268b8364640bb5ce17
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21.CCI>>CCOC(=O)c1ccc(COc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
O.CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C(=O)O)C.C([O-])([O-])=O.[K+].[K+].ICC>>CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C(=O)OCC)C
[OH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][C:23]3([CH3:24])[CH3:25])[cH:26][cH:27]1.I[CH2:2][CH3:1]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:1...
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21.CCI
CCOC(=O)c1ccc(COc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
null
null
CC(CC)=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
c1ccc(COc2ccc3c(c2)CCCC3)cc1
I-[CH2;D2;+0:1]-[C;D1;H3:2].[O;D1;H0:3]=[C:4](-[OH;D1;+0:5])-[c:6]>>[C;D1;H3:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[C:4](=[O;D1;H0:3])-[c:6]
40.9
[{"value": 40.9, "product": "CC1(C=2C=CC(=CC2C(CC1)(C)C)OCC1=CC=C(C=C1)C(=O)OCC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2 g (6 mmol) of 4-carboxybenzyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl ether, 2.7 g (19.6 mmol) of anhydrous potassium carbonate and 19 g (12.4 mmol) of iodoethane in 18 ml of butanone were refluxed for 7 h. The mixture was then poured into water and extracted with ether, and the organic phase was washed wit...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1ccccc1.c1ccc2c(c1)CCCC2
HI
CC(CC)=O
null
null
CC1(C)CCC(C)(C)c2cc(OCc3ccc(C(=O)O)cc3)ccc21.CCI>CC(CC)=O>CCOC(=O)c1ccc(COc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-46be299854ee4a8dbe1a9893d4f4ca6f
CC1(C)CCC(C)(C)c2cc(CBr)ccc21.CCOC(=O)c1ccc(O)cc1>>CCOC(=O)c1ccc(OCc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
O.BrCC1=CC=2C(CCC(C2C=C1)(C)C)(C)C.OC1=CC=C(C(=O)OCC)C=C1.C([O-])([O-])=O.[K+].[K+]>>CC1(C=2C=CC(=CC2C(CC1)(C)C)COC1=CC=C(C=C1)C(=O)OCC)C
Br[CH2:11][c:12]1[cH:13][cH:14][c:15]2[c:16]([cH:17]1)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][C:23]2([CH3:24])[CH3:25].[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([OH:10])[cH:26][cH:27]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([O:10][CH2:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:...
CC1(C)CCC(C)(C)c2cc(CBr)ccc21.CCOC(=O)c1ccc(O)cc1
CCOC(=O)c1ccc(OCc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(OCc2ccc3c(c2)CCCC3)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:3]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]):[c:4]
50.8
[{"value": 50.8, "product": "CC1(C=2C=CC(=CC2C(CC1)(C)C)COC1=CC=C(C=C1)C(=O)OCC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
10 g (36 mmol) of 2-bromomethyl-5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalene, 6 g (36 mmol) of ethyl 4-hydroxybenzoate and 7.2 g (52 mmol) of anhydrous potassium carbonate in 60 ml of dimethylformamide were refluxed for 5.25 h. The mixture was then poured into water and extracted several times with ether, and the ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccc2c(c1)CCCC2
HBr
CN(C=O)C
null
null
CC1(C)CCC(C)(C)c2cc(CBr)ccc21.CCOC(=O)c1ccc(O)cc1>CN(C=O)C>CCOC(=O)c1ccc(OCc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0a7405fa2b2340d382586106ada0c630
CC(=O)OC(C)=O.COC(=O)c1ccc(CNc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1>>COC(=O)c1ccc(CN(C(C)=O)c2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
O.C(=O)(OC)C1=CC=C(CNC2=CC=3C(CCC(C3C=C2)(C)C)(C)C)C=C1.C(C)(=O)OC(C)=O.C(C)N(CC)CC>>C(C)(=O)N(CC1=CC=C(C=C1)C(=O)OC)C1=CC=2C(CCC(C2C=C1)(C)C)(C)C
CC(=O)O[C:11]([CH3:12])=[O:13].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH2:9][NH:10][c:14]2[cH:15][cH:16][c:17]3[c:18]([cH:19]2)[C:20]([CH3:21])([CH3:22])[CH2:23][CH2:24][C:25]3([CH3:26])[CH3:27])[cH:28][cH:29]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH2:9][N:10]([C:11]([CH3:12])=[O:13])[c:14]2[cH...
CC(=O)OC(C)=O.COC(=O)c1ccc(CNc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
COC(=O)c1ccc(CN(C(C)=O)c2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
null
null
ClCCl
Acylation
Aminolysis of esters
72a6d1966b6b15ac7195d4682af251dc9ffac857f784a4242970ab5c7a529369
6593c6062585994f02076cd3c86920ae7244b86659eab65c21b5a8628c6d4bb8
c1ccc(CNc2ccc3c(c2)CCCC3)cc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[c:4]:[c:5](-[NH;D2;+0:6]-[C:7]-[c:8]):[c:9]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[N;H0;D3;+0:6](-[C:7]-[c:8])-[c:5](:[c:4]):[c:9]
null
[]
null
null
null
null
4.2 g (12 mmol) of N-(4-carbomethoxybenzyl)-5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylamine (from Example 11) and 1.6 ml (16 mmol) of acetic anhydride and 2.3 ml (17 mmol) of triethylamine in 100 ml of dichloromethane were stirred at room temperature. After the reaction was complete, the solution was poured into...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amine
Tertiary amide
null
null
c1ccccc1.c1ccc2c(c1)CCCC2
HO-
ClCCl
null
null
CC(=O)OC(C)=O.COC(=O)c1ccc(CNc2ccc3c(c2)C(C)(C)CCC3(C)C)cc1>ClCCl>COC(=O)c1ccc(CN(C(C)=O)c2ccc3c(c2)C(C)(C)CCC3(C)C)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3975e3cba1d24b4fba5c7e42d9b53709
CC1(C)CCC(C)(C)c2cc(SCc3ccc(C(=O)O)cc3)ccc21.[O-][I+3]([O-])([O-])[O-]>>CC1(C)CCC(C)(C)c2cc(S(=O)Cc3ccc(C(=O)O)cc3)ccc21
I(=O)(=O)(=O)[O-].[Na+].CC1(C=2C=CC(=CC2C(CC1)(C)C)SCC1=CC=C(C=C1)C(=O)O)C.Cl>>CC1(C=2C=CC(=CC2C(CC1)(C)C)S(=O)CC1=CC=C(C=C1)C(=O)O)C
[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([S:12][CH2:14][c:15]3[cH:16][cH:17][c:18]([C:19](=[O:20])[OH:21])[cH:22][cH:23]3)[cH:24][cH:25][c:26]21.[O-][I+3]([O-])([O-])[O-:13]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6]([CH3:7])([CH3:8])[c:9]2[cH:10][c:11]([S:12](=[O:13])[CH2:14][c:15...
CC1(C)CCC(C)(C)c2cc(SCc3ccc(C(=O)O)cc3)ccc21.[O-][I+3]([O-])([O-])[O-]
CC1(C)CCC(C)(C)c2cc(S(=O)Cc3ccc(C(=O)O)cc3)ccc21
null
null
CN(C=O)C.C(C)O.O
Oxidation
OtherReaction
9edfaf6d72a81452ea8e3a1cdcb10a58409fff36608e97019e7273998b3d5373
f5f6bb6ca76a2267cd589767b4d67e7a17ab1ac383eeb6143dcd5d92e00e1b6a
O=S(Cc1ccccc1)c1ccc2c(c1)CCCC2
[O-;H0;D1:1]-[I+3](-[O-])(-[O-])-[O-].[c:2]:[c:3](-[S;H0;D2;+0:4]-[C:5]-[c:6]):[c:7]>>[O;H0;D1;+0:1]=[S;H0;D3;+0:4](-[C:5]-[c:6])-[c:3](:[c:2]):[c:7]
39.6
[{"value": 39.6, "product": "CC1(C=2C=CC(=CC2C(CC1)(C)C)S(=O)CC1=CC=C(C=C1)C(=O)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of 3.4 g (16 mmol) of sodium periodate in 30 ml of water was added dropwise to 5.3 g (15 mmol) of the thioether from Example 10 in a mixture of 150 ml of ethanol and 40 ml of dimethylformamide at 0° C., and the mixture was then stirred at the same temperature for 2 hours and at room temperature overnight. Th...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Sulfoxide
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
I-
CN(C=O)C.C(C)O.O
null
8
CC1(C)CCC(C)(C)c2cc(SCc3ccc(C(=O)O)cc3)ccc21.[O-][I+3]([O-])([O-])[O-]>CN(C=O)C.C(C)O.O>CC1(C)CCC(C)(C)c2cc(S(=O)Cc3ccc(C(=O)O)cc3)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6f275656c8da41b3801c8b460fc918fa
Cc1cc(C2=CC(C)(C)CC(C)(C)C2)ccc1F.O=C(OO)c1cccc(Cl)c1>>Cc1cc(C23CC(C)(C)CC(C)(C)C2O3)ccc1F
FC1=C(C=C(C=C1)C1=CC(CC(C1)(C)C)(C)C)C.OP(=O)([O-])[O-].[K+].[K+].ClC1=CC(=CC=C1)C(=O)OO>>FC1=C(C=C(C=C1)C12C(C(CC(C1)(C)C)(C)C)O2)C
[CH3:1][c:2]1[cH:3][c:4]([C:5]2=[CH:14][C:11]([CH3:12])([CH3:13])[CH2:10][C:7]([CH3:8])([CH3:9])[CH2:6]2)[cH:16][cH:17][c:18]1[F:19].O=C(O[OH:15])c1cccc(Cl)c1>>[CH3:1][c:2]1[cH:3][c:4]([C:5]23[CH2:6][C:7]([CH3:8])([CH3:9])[CH2:10][C:11]([CH3:12])([CH3:13])[CH:14]2[O:15]3)[cH:16][cH:17][c:18]1[F:19]
Cc1cc(C2=CC(C)(C)CC(C)(C)C2)ccc1F.O=C(OO)c1cccc(Cl)c1
Cc1cc(C23CC(C)(C)CC(C)(C)C2O3)ccc1F
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
7cee396be0f6ae79b424df065d0e9e65c066fbe8972302e80868a1efcff9512b
c40ffbbc3249442e5ee39aaa69a55be7ac2fa45f48637395e415c565c1288454
c1ccc(C23CCCCC2O3)cc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C;D1;H3:2]-[C:3]1(-[C;D1;H3:4])-[C:5]-[C:6]-[C:7]-[C;H0;D3;+0:8](-[c:9](:[c:10]):[c:11])=[CH;D2;+0:12]-1>>[C;D1;H3:2]-[C:3]1(-[C;D1;H3:4])-[C:5]-[C:6]-[C:7]-[C;H0;D4;+0:8]2(-[c:9](:[c:10]):[c:11])-[O;H0;D2;+0:1]-[CH;D3;+0:12]-1-2
88
[{"value": 88.0, "product": "FC1=C(C=C(C=C1)C12C(C(CC(C1)(C)C)(C)C)O2)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.5, "product": "FC1=C(C=C(C=C1)C12C(C(CC(C1)(C)C)(C)C)O2)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
14
HOUR
A solution of meta-chloroperbenzoic acid (20 g, 90 mmol) in 250 ml of CH2Cl2 is added dropwise to a cooled (0° C.) solution of 1-fluoro-2-methyl-4-(3,3,5,5-tetramethylcyclohex-1-en-1-yl)benzene (15 g, 61 mmol) and K2HPO4 (21 g, 90 mmol) in dry CH2Cl2 (100 ml). The resulting milky solution is stirred at room temperature...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide
Ether
C1=CCCCC1.c1ccccc1
C1CCC2OC2C1
c1ccccc1.C1CCC2OC2C1
HCl
C(Cl)Cl
null
14
Cc1cc(C2=CC(C)(C)CC(C)(C)C2)ccc1F.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>Cc1cc(C23CC(C)(C)CC(C)(C)C2O3)ccc1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4f4f202b0c7649758da42a8dec41db76
Cc1cc(C23CC(C)(C)CC(C)(C)C2O3)ccc1F>>Cc1cc(C2CC(C)(C)CC(C)(C)C2=O)ccc1F
FC1=C(C=C(C=C1)C12C(C(CC(C1)(C)C)(C)C)O2)C>>FC1=C(C=C(C=C1)C1C(C(CC(C1)(C)C)(C)C)=O)C
[CH3:1][c:2]1[cH:3][c:4]([C:5]23[CH2:6][C:7]([CH3:8])([CH3:9])[CH2:10][C:11]([CH3:12])([CH3:13])[CH:14]2[O:15]3)[cH:16][cH:17][c:18]1[F:19]>>[CH3:1][c:2]1[cH:3][c:4]([CH:5]2[CH2:6][C:7]([CH3:8])([CH3:9])[CH2:10][C:11]([CH3:12])([CH3:13])[C:14]2=[O:15])[cH:16][cH:17][c:18]1[F:19]
Cc1cc(C23CC(C)(C)CC(C)(C)C2O3)ccc1F
Cc1cc(C2CC(C)(C)CC(C)(C)C2=O)ccc1F
null
null
CCOCC.C1=CC=CC=C1
Miscellaneous
OtherReaction
8ec7f40fa31a913229f3be27a8e864c7048d16f232c5a7a46a87f0c28e7d1259
06ee4e636755478860a38bbf5b67d3037b3b941f1ee50aea08d8ea3a7f23e056
O=C1CCCCC1c1ccccc1
[C;D1;H3:1]-[C:2]1(-[C;D1;H3:3])-[C:4]-[C:5]-[C:6]-[C;H0;D4;+0:7]2(-[c:8](:[c:9]):[c:10])-[O;H0;D2;+0:11]-[CH;D3;+0:12]-1-2>>[C;D1;H3:1]-[C:2]1(-[C;D1;H3:3])-[C:4]-[C:5]-[C:6]-[CH;D3;+0:7](-[c:8](:[c:9]):[c:10])-[C;H0;D3;+0:12]-1=[O;H0;D1;+0:11]
80
[{"value": 80.0, "product": "FC1=C(C=C(C=C1)C1C(C(CC(C1)(C)C)(C)C)=O)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a cooled solution (0° C.) of the epoxide from Example 1, Step A above (32.7 g, 125 mmol) in benzene (200 ml) is added dropwise 7.6 ml BF3 ·OEt2 (62 mmol). The cooling bath is removed and the reaction mixture warmed to room temperature and stirred for 2 hours. The benzene is removed under reduced pressure and provide...
10.6084/m9.figshare.5104873.v1
null
Ether
Ketone
C1CCC2OC2C1
C1CCCCC1
c1ccccc1.C1CCCCC1
null
CCOCC.C1=CC=CC=C1
null
2
Cc1cc(C23CC(C)(C)CC(C)(C)C2O3)ccc1F>CCOCC.C1=CC=CC=C1>Cc1cc(C2CC(C)(C)CC(C)(C)C2=O)ccc1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5ce452de6da847909012d9a70df1b395
Cc1cc(C2CC(C)(C)CC(C)(C)C2(O)C#C[Si](C)(C)C)ccc1F>>Cc1cc(C2=C(C#C[Si](C)(C)C)C(C)(C)CC(C)(C)C2)ccc1F
C[Si](C)(C)C#CC1(C(CC(CC1(C)C)(C)C)C1=CC(=C(C=C1)F)C)O.CC[N+](CC)(CC)S(=O)(=O)N=C([O-])OC>>C[Si](C)(C)C#CC1=C(CC(CC1(C)C)(C)C)C1=CC(=C(C=C1)F)C
O[C:6]1([C:7]#[C:8][Si:9]([CH3:10])([CH3:11])[CH3:12])[CH:5]([c:4]2[cH:3][c:2]([CH3:1])[c:23]([F:24])[cH:22][cH:21]2)[CH2:20][C:17]([CH3:18])([CH3:19])[CH2:16][C:13]1([CH3:14])[CH3:15]>>[CH3:1][c:2]1[cH:3][c:4]([C:5]2=[C:6]([C:7]#[C:8][Si:9]([CH3:10])([CH3:11])[CH3:12])[C:13]([CH3:14])([CH3:15])[CH2:16][C:17]([CH3:18])...
Cc1cc(C2CC(C)(C)CC(C)(C)C2(O)C#C[Si](C)(C)C)ccc1F
Cc1cc(C2=C(C#C[Si](C)(C)C)C(C)(C)CC(C)(C)C2)ccc1F
null
null
C(C)#N.O
Functional Group Interconversion
OtherReaction
bb751e8d8bac081516d1433e6fec088b316018c4b9e2465f1f9c878bad0b1e7c
63e4ba80024292782b5f87f96975225484dff39f49e96eea21874ac0cd9091a0
C1=C(c2ccccc2)CCCC1
O-[C;H0;D4;+0:1]1(-[C:2]#[C:3]-[#14:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7])-[CH;D3;+0:8](-[c:9](:[c:10]):[c:11])-[C:12]-[C:13]-[C:14]-[C:15]-1(-[C;D1;H3:16])-[C;D1;H3:17]>>[C;D1;H3:5]-[#14:4](-[C;D1;H3:6])(-[C;D1;H3:7])-[C:3]#[C:2]-[C;H0;D3;+0:1]1=[C;H0;D3;+0:8](-[c:9](:[c:10]):[c:11])-[C:12]-[C:13]-[C:14]-[C:15]-1...
67
[{"value": 67.0, "product": "C[Si](C)(C)C#CC1=C(CC(CC1(C)C)(C)C)C1=CC(=C(C=C1)F)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of the hydroxy acetylene from Example 1, Step C above (20 g, 55.5 mmol) in acetonitrile (250 ml) is added 20 g (83 mmol) of Burgess reagent. The reaction mixture is heated at reflux for 14 hours, cooled to room temperature and diluted with H2O (1 L). The aqueous solution is extracted with ether and the co...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
null
C1CCCCC1
C1=CCCCC1
c1ccccc1.C1=CCCCC1
HO-
C(C)#N.O
null
null
Cc1cc(C2CC(C)(C)CC(C)(C)C2(O)C#C[Si](C)(C)C)ccc1F>C(C)#N.O>Cc1cc(C2=C(C#C[Si](C)(C)C)C(C)(C)CC(C)(C)C2)ccc1F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-30b768947e544f58a83c823717346385
Cc1cc(C2=C(C#C[Si](C)(C)C)C(C)(C)CC(C)(C)C2)ccc1F>>C#CC1=C(c2ccc(F)c(C)c2)CC(C)(C)CC1(C)C
C[Si](C)(C)C#CC1=C(CC(CC1(C)C)(C)C)C1=CC(=C(C=C1)F)C.C(C)(=O)O.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>C(#C)C1=C(CC(CC1(C)C)(C)C)C1=CC(=C(C=C1)F)C
C[Si](C)(C)[C:1]#[C:2][C:3]1=[C:4]([c:5]2[cH:6][cH:7][c:8]([F:9])[c:10]([CH3:11])[cH:12]2)[CH2:13][C:14]([CH3:15])([CH3:16])[CH2:17][C:18]1([CH3:19])[CH3:20]>>[CH:1]#[C:2][C:3]1=[C:4]([c:5]2[cH:6][cH:7][c:8]([F:9])[c:10]([CH3:11])[cH:12]2)[CH2:13][C:14]([CH3:15])([CH3:16])[CH2:17][C:18]1([CH3:19])[CH3:20]
Cc1cc(C2=C(C#C[Si](C)(C)C)C(C)(C)CC(C)(C)C2)ccc1F
C#CC1=C(c2ccc(F)c(C)c2)CC(C)(C)CC1(C)C
null
null
C1CCOC1.CCOCC
Deprotection
TMS deprotection from alkyne
e85676bb81da384790c9c858d44f182cdd01e3a79f77f7a239fe38487234cb96
56d526d7c9cb1bd7bee4940e216a9b1dd4597fd025a186b8d6e4675d8f4db26b
C1=C(c2ccccc2)CCCC1
C-[Si](-C)(-C)-[C;H0;D2;+0:1]#[C:2]-[C:3](=[C:4](-[c:5])-[C:6])-[C:7]>>[C:6]-[C:4](-[c:5])=[C:3](-[C:2]#[CH;D1;+0:1])-[C:7]
98
[{"value": 98.0, "product": "C(#C)C1=C(CC(CC1(C)C)(C)C)C1=CC(=C(C=C1)F)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a solution of the product from Example 1, Step D above (5 g, 14.6 mmol), and acetic acid (1.3 ml, 21.9 mmol) in THF (15 ml) at 0° C. is added tetrabutylammonium fluoride in THF (1M, 21.9 ml, 21.9 mmol). The resulting solution is stirred for 12 hours at room temperature, diluted with ether and washed with saturated a...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Silyl protective group
Alkyne
null
null
C1=CCCCC1.c1ccccc1
Other
C1CCOC1.CCOCC
null
12
Cc1cc(C2=C(C#C[Si](C)(C)C)C(C)(C)CC(C)(C)C2)ccc1F>C1CCOC1.CCOCC>C#CC1=C(c2ccc(F)c(C)c2)CC(C)(C)CC1(C)C
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9544b342e8b6458bac2c64b1a2c39d77
CC(C)Cc1ccccc1.COc1ccc2ccccc2c1.c1ccc2c(c1)CCCC2>>CC(C)Cc1ccc(C(C)C(=O)O)cc1
C1=CC=CC2=CC=CC=C12.C1CCCC2=CC=CC=C12.C1(=CC=CC=C1)OC.COC1=CC2=CC=CC=C2C=C1.C(C(C)C)C1=CC=CC=C1>>OC(=O)C(C)C1=CC=C(CC(C)C)C=C1
[CH3:1][CH:2]([CH3:3])[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:14][cH:15]1.c1ccc2c[c:11]([O:12][CH3:10])ccc2c1.c1ccc2c(c1)CCC[CH2:9]2>>[CH3:1][CH:2]([CH3:3])[CH2:4][c:5]1[cH:6][cH:7][c:8]([CH:9]([CH3:10])[C:11](=[O:12])[OH:13])[cH:14][cH:15]1
CC(C)Cc1ccccc1.COc1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
CC(C)Cc1ccc(C(C)C(=O)O)cc1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
43854ac68e6b362cc70ec003ae9c53a0cd7ba5a9412787463058beb669774160
5e8ff715284d2753472609e3a99a03d1debb677f7d7e353b2a8ba368120e8e19
c1ccccc1
C1-C-[CH2;D2;+0:1]-c2:c:c:c:c:c:2-C-1.[CH3;D1;+0:2]-[O;H0;D2;+0:3]-[c;H0;D3;+0:4]1:c:c:c2:c:c:c:c:c:2:c:1.[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[CH3;D1;+0:2]-[CH;D3;+0:1](-[C;H0;D3;+0:4](-[O;D1;H1:10])=[O;H0;D1;+0:3])-[c;H0;D3;+0:7](:[c:6]:[c:5]):[c:8]:[c:9]
null
[]
null
null
null
null
Surprisingly, only a few methods for a stereospecific chemical synthesis for 2-aryl-alkanoic acids, especially 2-aryl-propionic acids, are known. Piccolo et al. (J. Org. Chem. 50, 3945-3946, 1985) describe a stereospecific synthesis by the alkylation of benzene or isobutylbenzene with (S)-methyl-2-(chlorosulfonyl)-oxy ...
10.6084/m9.figshare.5104873.v1
null
Ether
Carboxylic acid
c1ccccc1.c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
c1ccccc1
c1ccccc1
Other
C1(=CC=CC=C1)C
null
null
CC(C)Cc1ccccc1.COc1ccc2ccccc2c1.c1ccc2c(c1)CCCC2>C1(=CC=CC=C1)C>CC(C)Cc1ccc(C(C)C(=O)O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d915f9e724c34bff918fbcf5d34e9611
CC(C)NC(C)C.CCC1=N[C@@H](COC)[C@H](c2ccccc2)O1.CCC1=N[C@@H](COC)[C@H](c2ccccc2)O1>>COCC1N=C(C2(C)C=CC(CC(C)C)=CC2)OC1c1ccccc1
C1CCOC1.C(C)(C)NC(C)C.C[Li].C(C)C=1O[C@H]([C@@H](N1)COC)C1=CC=CC=C1.C1CCOC1.C(C)(C)[N-]C(C)C.[Li+].[Br-].C1CCOC1.[Cl-].[Na+].C(C)C=1O[C@H]([C@@H](N1)COC)C1=CC=CC=C1.C1CCOC1>>CC1(CC=C(C=C1)CC(C)C)C=1OC(C(N1)COC)C1=CC=CC=C1
CC(C)NC(C)[CH3:14].[CH3:1][O:2][CH2:3][C@@H:4]1[N:5]=[C:6]([CH2:7][CH3:8])[O:18][C@H:19]1[c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1.COC[C@@H]1N=[C:12]([CH2:13][CH3:15])O[C@H]1c1c[cH:10][cH:11][cH:16][cH:17]1>>[CH3:1][O:2][CH2:3][CH:4]1[N:5]=[C:6]([C:7]2([CH3:8])[CH:9]=[CH:10][C:11]([CH2:12][CH:13]([CH3:14])[CH3:15])=[...
CC(C)NC(C)C.CCC1=N[C@@H](COC)[C@H](c2ccccc2)O1.CCC1=N[C@@H](COC)[C@H](c2ccccc2)O1
COCC1N=C(C2(C)C=CC(CC(C)C)=CC2)OC1c1ccccc1
null
null
null
C-C Coupling
OtherReaction
b93798b2a4617495f363980bc632712fc4a3efeb15812f14a660d79f68875cd2
65bdc187ccffb20164ee1a46c967e081a6b3e14c29368f87af76f0367fea6139
C1=CCC(C2=NCC(c3ccccc3)O2)C=C1
C-C(-C)-N-C(-C)-[CH3;D1;+0:1].C-O-C-[C@H]1-N=[C;H0;D3;+0:2](-[CH2;D2;+0:3]-[C;D1;H3:4])-O-[C@@H]-1-c1:[cH;D2;+0:5]:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:c:1.[C;D1;H3:9]-[CH2;D2;+0:10]-[C:11]1=[#7:12]-[C:13]-[C:14]-[#8:15]-1>>[C;D1;H3:4]-[CH;D3;+0:3](-[CH3;D1;+0:1])-[CH2;D2;+0:2]-[C;H0;D3;+0:7]1=[CH;D2;+0:6]-[CH2;D2;+0...
90
[{"value": 90.0, "product": "CC1(CC=C(C=C1)CC(C)C)C=1OC(C(N1)COC)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of the compound II (155 g, 0.71 mol) in THF (1.6 L) under nitrogen is cooled to -75° C. in a dry-ice-acetone bath. A solution of 0.8 mol of lithium diisopropylamide, derived from 98 ml of diisopropylamine and 300 ml of 2,3M butylithium (methyllithium) in 750 ml of dry THF is prepared, and added under continu...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Secondary amine
null
C1=NCCO1.c1ccccc1
C1=CCCC=C1
C1=NCCO1.C1=CCCC=C1.c1ccccc1
HO-
null
null
null
CC(C)NC(C)C.CCC1=N[C@@H](COC)[C@H](c2ccccc2)O1.CCC1=N[C@@H](COC)[C@H](c2ccccc2)O1>>COCC1N=C(C2(C)C=CC(CC(C)C)=CC2)OC1c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-35982a95451c4e8385f818981ea12a16
CC(C)(C)C(=O)Cl.Nc1cc2c(O)nc[nH]c-2n1>>CC(C)(C)C(=O)Nc1cc2c(O)nc[nH]c-2n1
OC1=C2C(NC=N1)=NC(=C2)N.C(C(C)(C)C)(=O)Cl>>OC1=C2C(NC=N1)=NC(=C2)NC(C(C)(C)C)=O
Cl[C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[O:6].[NH2:7][c:8]1[cH:9][c:10]2[c:11]([OH:12])[n:13][cH:14][nH:15][c:16]-2[n:17]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[O:6])[NH:7][c:8]1[cH:9][c:10]2[c:11]([OH:12])[n:13][cH:14][nH:15][c:16]-2[n:17]1
CC(C)(C)C(=O)Cl.Nc1cc2c(O)nc[nH]c-2n1
CC(C)(C)C(=O)Nc1cc2c(O)nc[nH]c-2n1
null
null
N1=CC=CC=C1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1cc2cnc[nH]c-2n1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[C;D1;H3:6].[#7;a:7]:[c:8]:[#7;a:9]:[c:10](-[NH2;D1;+0:11]):[c:12]>>[#7;a:7]:[c:8]:[#7;a:9]:[c:10](-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[C;D1;H3:6]):[c:12]
89.6
[{"value": 89.0, "product": "OC1=C2C(NC=N1)=NC(=C2)NC(C(C)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.6, "product": "OC1=C2C(NC=N1)=NC(=C2)NC(C(C)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A mixture of 3.0 g (0.02 mole) of 4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidine and 8.4 g (0.07 mol) of pivaloyl chloride in 40 mL of pyridine is stirred for 30 minutes at from 80° to 90° C., the mixture then evaporated to dryness, and the residue dissolved in 30 mL of methanol. Addition of 10% aqueous ammonia yields 4.2 g...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ncc2cc[nH]c2n1
HCl
N1=CC=CC=C1
null
0.5
CC(C)(C)C(=O)Cl.Nc1cc2c(O)nc[nH]c-2n1>N1=CC=CC=C1>CC(C)(C)C(=O)Nc1cc2c(O)nc[nH]c-2n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-099dba7b08f5439bb4cdf076de3f062d
CC(C)(C)C(=O)Nc1cc2c(O)n(I)c(I)nc-2n1>>CC(C)(C)C(=O)Nc1cc2c(O)n(I)cnc-2n1
IC=1N(C(=C2C(N1)=NC(=C2)NC(C(C)(C)C)=O)O)I>>IN1C=NC=2C(=C1O)C=C(N2)NC(C(C)(C)C)=O
I[c:15]1[n:13]([I:14])[c:11]([OH:12])[c:10]2[cH:9][c:8]([NH:7][C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[O:6])[n:18][c:17]-2[n:16]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[O:6])[NH:7][c:8]1[cH:9][c:10]2[c:11]([OH:12])[n:13]([I:14])[cH:15][n:16][c:17]-2[n:18]1
CC(C)(C)C(=O)Nc1cc2c(O)n(I)c(I)nc-2n1
CC(C)(C)C(=O)Nc1cc2c(O)n(I)cnc-2n1
null
[Zn]
C(C)(=O)O.O
Functional Group Interconversion
Aromatic dehalogenation
26ad15a6cd6065fab54d262c57ea46217b9c0a5d9be9f2a942a86df9b473c507
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1cc2c[nH]cnc-2n1
I-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](:[#7;a:4]:[c:5])-[c:6]:[c:7]:[#7;a:8]:1-[I;D1;H0:9]>>[I;D1;H0:9]-[#7;a:8]1:[c:7]:[c:6]-[c:3](:[#7;a:2]:[cH;D2;+0:1]:1):[#7;a:4]:[c:5]
null
[]
null
null
18
HOUR
To a mixture of 4.86 g of 2,3-diiodo-4-hydroxy-6-pivaloylaminopyrrolo[2,3-d]pyrimidine in 100 mL of glacial acetic acid and 25 mL of water are added 1.3 g (20 mmol) of zinc powder. The mixture is stirred at ambient temperature for 18 hours, diluted with 500 mL of water, and cooled. The solid is collected through filtra...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ncc2cc[nH]c2n1
c1cc2cncnc2[nH]1
c1cc2cncnc2[nH]1
I-
[Zn].C(C)(=O)O.O
null
18
CC(C)(C)C(=O)Nc1cc2c(O)n(I)c(I)nc-2n1>[Zn].C(C)(=O)O.O>CC(C)(C)C(=O)Nc1cc2c(O)n(I)cnc-2n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-08c77ae1ea2d4cbc9b60678aaa348fec
C#Cc1ccc(C(=O)N[C@@H](CCC(=O)OC)C(=O)OC)cc1.CC(C)(C)C(=O)Nc1cc2c(O)n(I)cnc-2n1>>COC(=O)CC[C@H](NC(=O)c1ccc(C#Cn2cnc3nc(NC(=O)C(C)(C)C)cc-3c2O)cc1)C(=O)OC
IN1C=NC=2C(=C1O)C=C(N2)NC(C(C)(C)C)=O.C(#C)C1=CC=C(C(=O)N[C@@H](CCC(=O)OC)C(=O)OC)C=C1.C(C)N(CC)CC.O>>OC1=C2C(N=CN1C#CC1=CC=C(C(=O)N[C@@H](CCC(=O)OC)C(=O)OC)C=C1)=NC(=C2)NC(C(C)(C)C)=O
[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][C@H:7]([NH:8][C:9](=[O:10])[c:11]1[cH:12][cH:13][c:14]([C:15]#[CH:16])[cH:34][cH:35]1)[C:36](=[O:37])[O:38][CH3:39].I[n:17]1[cH:18][n:19][c:20]2[n:21][c:22]([NH:23][C:24](=[O:25])[C:26]([CH3:27])([CH3:28])[CH3:29])[cH:30][c:31]-2[c:32]1[OH:33]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH...
C#Cc1ccc(C(=O)N[C@@H](CCC(=O)OC)C(=O)OC)cc1.CC(C)(C)C(=O)Nc1cc2c(O)n(I)cnc-2n1
COC(=O)CC[C@H](NC(=O)c1ccc(C#Cn2cnc3nc(NC(=O)C(C)(C)C)cc-3c2O)cc1)C(=O)OC
null
[Cu]I
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
2f759f114767b91e2231d010a7bf2c8670481fd3eb71a70def1ce9d9314ff239
0ff14f8ed0439469fe0912bb971ad27399d5e9d291750b4a0bb5781f426b3afa
C(#Cn1cnc2nccc-2c1)c1ccccc1
I-[n;H0;D3;+0:1]1:[c:2]:[#7;a:3]:[c:4](:[#7;a:5])-[c:6]:[c:7]:1-[O;D1;H1:8].[CH;D1;+0:9]#[C:10]-[c:11]>>[#7;a:5]:[c:4]1:[#7;a:3]:[c:2]:[n;H0;D3;+0:1](-[C;H0;D2;+0:9]#[C:10]-[c:11]):[c:7](-[O;D1;H1:8]):[c:6]-1
65.4
[{"value": 65.4, "product": "OC1=C2C(N=CN1C#CC1=CC=C(C(=O)N[C@@H](CCC(=O)OC)C(=O)OC)C=C1)=NC(=C2)NC(C(C)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a mixture of 3.6 g (10 mmol) of well-dried 3-iodo-4-hydroxy-6-pivaloylaminopyrrolo[2,3-d]pyrimidine in 40 mL of dimethylformamide are added 4.0 g (13.19 mmol) of dimethyl N-(4-ethynylbenzoyl)-L-glutamate, 0.38 g of copper (I) iodide, 3 mL of triethylamine, and 1.0 g of tetrakis-(triphenylphosphine)palladium. This mi...
10.6084/m9.figshare.5104873.v1
null
Alkyne
Alkyne
c1cc2cncnc2[nH]1
c1cc2cncnc2[nH]1
c1ccccc1.c1cc2cncnc2[nH]1
HI
[Cu]I.CN(C=O)C
null
2
C#Cc1ccc(C(=O)N[C@@H](CCC(=O)OC)C(=O)OC)cc1.CC(C)(C)C(=O)Nc1cc2c(O)n(I)cnc-2n1>[Cu]I.CN(C=O)C>COC(=O)CC[C@H](NC(=O)c1ccc(C#Cn2cnc3nc(NC(=O)C(C)(C)C)cc-3c2O)cc1)C(=O)OC