dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0972b428a21c41088cff53aef93eb87c
COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(CN(C)C(=O)OC(C)(C)C)cc1>>CNCc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc2OC)cc1
C(C)(C)(C)OC(=O)N(C)CC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.FC(C(=O)O)(F)F>>FC1=CC=C(C(=O)C2CCN(CC2)CCN(C(C2=CC=C(C=C2)CNC)=O)C2=C(C=CC=C2)OC)C=C1
CC(C)(C)OC(=O)[N:2]([CH3:1])[CH2:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[N:10]([CH2:11][CH2:12][N:13]2[CH2:14][CH2:15][CH:16]([C:17](=[O:18])[c:19]3[cH:20][cH:21][c:22]([F:23])[cH:24][cH:25]3)[CH2:26][CH2:27]2)[c:28]2[cH:29][cH:30][cH:31][cH:32][c:33]2[O:34][CH3:35])[cH:36][cH:37]1>>[CH3:1][NH:2][CH2:3][c:4]1[cH:5][cH:...
COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(CN(C)C(=O)OC(C)(C)C)cc1
CNCc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc2OC)cc1
null
null
C(Cl)Cl
Reduction
Boc amine deprotection
bbda4640db5f48af4538caded12fdadd56eacd6d4e5f7aefe46282d665df167e
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2ccccc2)CC1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1](-[C;D1;H3:2])-[C:3]-[c:4]>>[C;D1;H3:2]-[NH;D2;+0:1]-[C:3]-[c:4]
98.9
[{"value": 98.9, "product": "FC1=CC=C(C(=O)C2CCN(CC2)CCN(C(C2=CC=C(C=C2)CNC)=O)C2=C(C=CC=C2)OC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.9, "product": "FC1=CC=C(C(=O)C2CCN(CC2)CCN(C(C2=CC=C(C=C2)CNC)=O)C2=C(C=CC=C2)OC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
4-(N-tert-Butoxycarbonyl-N-methylamino)methyl-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(2-methoxyphenyl)benzamide (144 mg, 0.239 mmol) was dissolved in methylene chloride (4 ml) to which was subsequently added dropwise trifluoroacetic acid (0.4 ml) while cooling in an ice bath. After 2 hours of stirring at the same...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
2
COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(CN(C)C(=O)OC(C)(C)C)cc1>C(Cl)Cl>CNCc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc2OC)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-13297e7c81bb418aa27b32cfac5bc697
CC(C)(C)N=C=O.COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(N)cc1>>COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(NC(=O)NC(C)(C)C)cc1
NC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(C)(C)(C)N=C=O>>C(C)(C)(C)NC(NC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)=O
[C:34](=[O:35])=[N:36][C:37]([CH3:38])([CH3:39])[CH3:40].[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[N:9]([CH2:10][CH2:11][N:12]1[CH2:13][CH2:14][CH:15]([C:16](=[O:17])[c:18]2[cH:19][cH:20][c:21]([F:22])[cH:23][cH:24]2)[CH2:25][CH2:26]1)[C:27](=[O:28])[c:29]1[cH:30][cH:31][c:32]([NH2:33])[cH:41][cH:42]1>>[CH3:1][O...
CC(C)(C)N=C=O.COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(N)cc1
COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(NC(=O)NC(C)(C)C)cc1
null
null
null
Acylation
Urea synthesis via isocyanate and primary amine
d39cd7dc52a79bb265ff8ef61ef7bf9dc7f7b5fb0150fcb4881bdfb18ab9c380
a5dc801930c765d2a435a0a2973e50163c305ba8e7641d6adbcc1550b7b96de7
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2ccccc2)CC1
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[O;D1;H0:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[C;D1;H3:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[NH;D2;+0:5]-[C;H0;D3;+0:6](=[O;D1;H0:7])-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]
77.6
[{"value": 77.6, "product": "C(C)(C)(C)NC(NC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.3, "product": "C(C)(C)(C)NC(NC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is...
null
null
null
null
Using 4-amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(2-methoxyphenyl)benzamide (77.7 mg, 0.164 mmol) and tertbutyl isocyanate (0.022 ml, 0.196 mmol), the procedure of inventive Example 144 was repeated to obtain 72.9 mg (77.6%) of the title compound in a colorless oily form. Conditions: See reaction.notes.proced...
10.6084/m9.figshare.5104873.v1
null
Isocyanate.Primary amine
Urea
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
null
null
null
null
CC(C)(C)N=C=O.COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(N)cc1>>COc1ccccc1N(CCN1CCC(C(=O)c2ccc(F)cc2)CC1)C(=O)c1ccc(NC(=O)NC(C)(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1cf1796f970a4f61aff232d412aa105f
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.N#C[O-]>>COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(N)=O)cc2)c1
[OH-].[Na+].[O-]C#N.[K+].NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C([O-])(O)=O.[Na+]>>N(C(=O)N)C1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([N:8]([CH2:9][CH2:10][N:11]2[CH2:12][CH2:13][CH:14]([C:15](=[O:16])[c:17]3[cH:18][cH:19][c:20]([F:21])[cH:22][cH:23]3)[CH2:24][CH2:25]2)[C:26](=[O:27])[c:28]2[cH:29][cH:30][c:31]([NH2:32])[cH:36][cH:37]2)[cH:38]1.[C:33](#[N:34])[O-:35]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]...
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.N#C[O-]
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(N)=O)cc2)c1
null
null
C(C)(=O)O.O
Acylation
OtherReaction
f8798d1193af6f9b314ac8855e814716b90ff3758bcfa29778cc632fcaa83b7a
5efe06db19c806d9e9798893351dc14c0cc48f1e8f8c857f54c6171e86c96a1b
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2ccccc2)CC1
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[O-;H0;D1:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[NH2;D1;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
48.4
[{"value": 48.4, "product": "N(C(=O)N)C1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.4, "product": "N(C(=O)N)C1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false...
null
null
null
null
4-Amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide (237.2 mg, 0.50 mmol) was dissolved in acetic acid-water (1:2, 1.8 ml) to which was subsequently added dropwise an aqueous solution (0.5 ml) of potassium cyanate (81.1 mg, 0.90 mmol) After 3 hours of stirring at room temperature, the reacti...
10.6084/m9.figshare.5104873.v1
null
Nitrile.Primary amine
Urea
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
null
C(C)(=O)O.O
null
null
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.N#C[O-]>C(C)(=O)O.O>COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(N)=O)cc2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-325ebeb3b83e42ed8fa3b3afdd734121
CI.COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(C)=O)cc2)cc1>>CCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccc(OC)cc2)cc1
[Cl-].[NH4+].[H-].[Na+].C(C)(=O)NC1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.CI>>CCC(=O)NC1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
I[CH3:1].[CH3:2][C:3](=[O:4])[NH:5][c:6]1[cH:7][cH:8][c:9]([C:10](=[O:11])[N:12]([CH2:13][CH2:14][N:15]2[CH2:16][CH2:17][CH:18]([C:19](=[O:20])[c:21]3[cH:22][cH:23][c:24]([F:25])[cH:26][cH:27]3)[CH2:28][CH2:29]2)[c:30]2[cH:31][cH:32][c:33]([O:34][CH3:35])[cH:36][cH:37]2)[cH:38][cH:39]1>>[CH3:1][CH2:2][C:3](=[O:4])[NH:5...
CI.COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(C)=O)cc2)cc1
CCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccc(OC)cc2)cc1
null
null
C1CCOC1
C-C Coupling
Methylation with MeI_primary
0e09d968095a587418cca2841b1e4f096e8103de8fbb60e833faf1fb3df36a41
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2ccccc2)CC1
I-[CH3;D1;+0:1].[CH3;D1;+0:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[c:6]>>[CH3;D1;+0:1]-[CH2;D2;+0:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[c:6]
80.4
[{"value": 80.4, "product": "CCC(=O)NC1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.3, "product": "CCC(=O)NC1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
4-Acetylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(4-methoxyphenyl)benzamide (155.0 mg, 0.30 mmol) was dissolved in THF (3.0 ml) to which were subsequently added 60% sodium hydride {28.0 mg, 0.70 mmol) and methyl iodide (0.060 ml, 1.00 mmol) at room temperature, followed by 2 hours of stirring. The reaction so...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
HI
C1CCOC1
null
2
CI.COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(C)=O)cc2)cc1>C1CCOC1>CCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccc(OC)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-af152361a976447c83199ce000045ab8
COC1CCC(OC)O1.COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)cc1>>COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(-n3cccc3)cc2)cc1
NC1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.COC1OC(CC1)OC>>N1(C=CC=C1)C1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
CO[CH:32]1O[CH:35](OC)[CH2:34][CH2:33]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([N:7]([CH2:8][CH2:9][N:10]2[CH2:11][CH2:12][CH:13]([C:14](=[O:15])[c:16]3[cH:17][cH:18][c:19]([F:20])[cH:21][cH:22]3)[CH2:23][CH2:24]2)[C:25](=[O:26])[c:27]2[cH:28][cH:29][c:30]([NH2:31])[cH:36][cH:37]2)[cH:38][cH:39]1>>[CH3:1][O:2][c:3]1[cH:4]...
COC1CCC(OC)O1.COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)cc1
COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(-n3cccc3)cc2)cc1
null
null
C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
0e9d22b0723ec2930c6f0b28cb06c2d86835df697b962917265b2a52889a76e9
37da407ba22aeb87f9320448e7710117027e549cd7c89e722598c54789c5481f
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccc(-n3cccc3)cc2)c2ccccc2)CC1
C-O-[CH;D3;+0:1]1-O-[CH;D3;+0:2](-O-C)-[CH2;D2;+0:3]-[CH2;D2;+0:4]-1.[NH2;D1;+0:5]-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[n;H0;D3;+0:5]1:[cH;D2;+0:1]:[cH;D2;+0:4]:[cH;D2;+0:3]:[cH;D2;+0:2]:1):[c:9]:[c:10]
82.6
[{"value": 82.0, "product": "N1(C=CC=C1)C1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.6, "product": "N1(C=CC=C1)C1=CC=C(C(=O)N(C2=CC=C(C=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": f...
null
null
null
null
4-Amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(4-methoxyphenyl)benzamide (237.0 mg, 0.50 mmol) was dissolved in acetic acid (5.0 ml), and the solution was mixed with 2,5-dimethoxytetrahydrofuran (0.065 ml, 0.50 mmol) and heated for 1 hour under reflux. After cooling, acetic acid was distilled off under a reduced...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Primary amine
null
C1CCOC1
c1cc[nH]c1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1cc[nH]c1
HO-
C(C)(=O)O
null
null
COC1CCC(OC)O1.COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)cc1>C(C)(=O)O>COc1ccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(-n3cccc3)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a87ab204e6184d2c93e710080ffacda1
COC1CCC(OC)O1.COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1>>COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(-n3cccc3)cc2)c1
NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.COC1OC(CC1)OC>>N1(C=CC=C1)C1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
CO[CH:33]1O[CH:36](OC)[CH2:35][CH2:34]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([N:8]([CH2:9][CH2:10][N:11]2[CH2:12][CH2:13][CH:14]([C:15](=[O:16])[c:17]3[cH:18][cH:19][c:20]([F:21])[cH:22][cH:23]3)[CH2:24][CH2:25]2)[C:26](=[O:27])[c:28]2[cH:29][cH:30][c:31]([NH2:32])[cH:37][cH:38]2)[cH:39]1>>[CH3:1][O:2][c:3]1[cH:4]...
COC1CCC(OC)O1.COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(-n3cccc3)cc2)c1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
0e9d22b0723ec2930c6f0b28cb06c2d86835df697b962917265b2a52889a76e9
37da407ba22aeb87f9320448e7710117027e549cd7c89e722598c54789c5481f
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccc(-n3cccc3)cc2)c2ccccc2)CC1
C-O-[CH;D3;+0:1]1-O-[CH;D3;+0:2](-O-C)-[CH2;D2;+0:3]-[CH2;D2;+0:4]-1.[NH2;D1;+0:5]-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[n;H0;D3;+0:5]1:[cH;D2;+0:1]:[cH;D2;+0:4]:[cH;D2;+0:3]:[cH;D2;+0:2]:1):[c:9]:[c:10]
78
[{"value": 78.0, "product": "N1(C=CC=C1)C1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.0, "product": "N1(C=CC=C1)C1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": f...
null
null
null
null
Using 4-amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide (238.1 mg, 0.50 mmol) and 2,5-dimethoxytetrahydrofuran (0.066 ml, 0.50 mmol), the procedure of Inventive Example 149 was repeated to obtain 205.0 mg (78.0%) of the title compound in a light brown amorphous form. Conditions: See reacti...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Primary amine
null
C1CCOC1
c1cc[nH]c1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1cc[nH]c1
HO-
null
null
null
COC1CCC(OC)O1.COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1>>COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(-n3cccc3)cc2)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-afe5cbc25fd340cf8536ac9ee64ce538
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(C)=O)cc2)c1>>CC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccc(O)c2)cc1
B(Br)(Br)Br.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C([O-])(O)=O.[Na+]>>C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)O)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
C[O:34][c:33]1[cH:32][cH:31][cH:30][c:29]([N:11]([C:9]([c:8]2[cH:7][cH:6][c:5]([NH:4][C:2]([CH3:1])=[O:3])[cH:37][cH:36]2)=[O:10])[CH2:12][CH2:13][N:14]2[CH2:15][CH2:16][CH:17]([C:18](=[O:19])[c:20]3[cH:21][cH:22][c:23]([F:24])[cH:25][cH:26]3)[CH2:27][CH2:28]2)[cH:35]1>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]...
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(C)=O)cc2)c1
CC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccc(O)c2)cc1
null
null
C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2ccccc2)CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
76.7
[{"value": 76.7, "product": "C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)O)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.1, "product": "C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)O)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
4-Acetylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide (50.0 mg, 0.10 mmol) was dissolved in methylene chloride (3.0 ml) to which was subsequently added a methylene chloride solution (1 ml) of boron tribromide (0.018 ml, 0.19 mmol) at 0° C. After 12 hours of stirring at 0° C. to room temp...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
Other
C(Cl)Cl
null
12
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(NC(C)=O)cc2)c1>C(Cl)Cl>CC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccc(O)c2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-210fb1b1e78248f89d667958215bdb36
O=C(Nc1cccnc1)c1ccc([N+](=O)[O-])cc1.O=C(c1ccccc1)C1CCN(CCCl)CC1>>O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2cccnc2)CC1
[I-].[Na+].[N+](=O)([O-])C1=CC=C(C(=O)NC=2C=NC=CC2)C=C1.[H-].[Na+].[Cl-].[Na+].ClCCN1CCC(CC1)C(C1=CC=CC=C1)=O>>[N+](=O)([O-])C1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1
[NH:15]([C:16](=[O:17])[c:18]1[cH:19][cH:20][c:21]([N+:22](=[O:23])[O-:24])[cH:25][cH:26]1)[c:27]1[cH:28][cH:29][cH:30][n:31][cH:32]1.Cl[CH2:14][CH2:13][N:12]1[CH2:11][CH2:10][CH:9]([C:2](=[O:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][cH:8]2)[CH2:34][CH2:33]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[CH:9]1[CH2:10][CH...
O=C(Nc1cccnc1)c1ccc([N+](=O)[O-])cc1.O=C(c1ccccc1)C1CCN(CCCl)CC1
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2cccnc2)CC1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
db9b1b8804b469c037e0a5ba95031d33e73dcd5fc2a6fa79163c623adf75f2a1
4a6c1e88c9e8bed487b746792f88d478ff36cc235f9a217d4632e6babdebdc9a
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
Cl-[CH2;D2;+0:1]-[C:2]-[#7:3].[O;D1;H0:4]=[C:5](-[c:6])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]:[#7;a:11]:[c:12]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7](-[C:5](=[O;D1;H0:4])-[c:6])-[c:8](:[c:9]):[c:10]:[#7;a:11]:[c:12]
24
[{"value": 24.0, "product": "[N+](=O)([O-])C1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 24.0, "product": "[N+](=O)([O-])C1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
1
HOUR
In an atmosphere of argon, 4-nitro-N-(3-pyridyl)benzamide (973 mg, 4.00 mmol) was dissolved in DMF (10 ml) to which was subsequently added sodium hydride (176 mg, 60%, 4.40 mmol) at room temperature, stirred for 1 hour at 60° C., and added dropwise 1-(2-chloroethyl)-4-benzoylpiperidine (1.38 g, 5.49 mmol) and a catalyt...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amide
Tertiary amide
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
HCl
CN(C)C=O
60
1
O=C(Nc1cccnc1)c1ccc([N+](=O)[O-])cc1.O=C(c1ccccc1)C1CCN(CCCl)CC1>CN(C)C=O>O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2cccnc2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-83156c93ebe44f9b836d2b41d4fbb6ea
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)C(F)(F)F>>O=C(c1ccc(F)cc1)C1CCN(CCN(C(=O)c2ccc(NC(=O)C(F)(F)F)cc2)c2cccnc2)CC1
C([O-])(O)=O.[Na+].N1=CC=CC=C1.NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.FC(C(=O)O)(F)F>>FC(C(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)(F)F
[O:1]=[C:2]([c:3]1[cH:4][cH:5][c:6]([F:7])[cH:8][cH:9]1)[CH:10]1[CH2:11][CH2:12][N:13]([CH2:14][CH2:15][N:16]([C:17](=[O:18])[c:19]2[cH:20][cH:21][c:22]([NH2:23])[cH:30][cH:31]2)[c:32]2[cH:33][cH:34][cH:35][n:36][cH:37]2)[CH2:38][CH2:39]1.O[C:24](=[O:25])[C:26]([F:27])([F:28])[F:29]>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][c:6]...
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)C(F)(F)F
O=C(c1ccc(F)cc1)C1CCN(CCN(C(=O)c2ccc(NC(=O)C(F)(F)F)cc2)c2cccnc2)CC1
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[F;D1;H0:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[F;D1;H0:4]-[C:3](-[F;D1;H0:5])(-[F;D1;H0:6])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]
81.2
[{"value": 81.2, "product": "FC(C(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.2, "product": "FC(C(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": fal...
null
null
3
HOUR
4-Amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-pyridyl)benzamide (229.3 mg, 0.51 mmol) was dissolved in methylene chloride (2.0 ml) to which were subsequently added pyridine (0.05 ml, 0.62 mmol) and anhydrous trifluoroacetic acid (0.09 ml, 0.64 mmol) at 0° C. After 3 hours of stirring at 0° C. to room temperat...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
HO-
C(Cl)Cl
null
3
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)C(F)(F)F>C(Cl)Cl>O=C(c1ccc(F)cc1)C1CCN(CCN(C(=O)c2ccc(NC(=O)C(F)(F)F)cc2)c2cccnc2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-579f2de7dc1447cc98ef05252e3642bd
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(Cl)c1ccccc1>>O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1)c1ccccc1
C([O-])(O)=O.[Na+].N1=CC=CC=C1.NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(C1=CC=CC=C1)(=O)Cl>>C(C1=CC=CC=C1)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
[NH2:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[N:10]([CH2:11][CH2:12][N:13]2[CH2:14][CH2:15][CH:16]([C:17](=[O:18])[c:19]3[cH:20][cH:21][c:22]([F:23])[cH:24][cH:25]3)[CH2:26][CH2:27]2)[c:28]2[cH:29][cH:30][cH:31][n:32][cH:33]2)[cH:34][cH:35]1.Cl[C:2](=[O:1])[c:36]1[cH:37][cH:38][cH:39][cH:40][cH:41]1>>[O:1]=[C:2]([NH:3][...
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(Cl)c1ccccc1
O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1)c1ccccc1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1)c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
71.3
[{"value": 70.6, "product": "C(C1=CC=CC=C1)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.3, "product": "C(C1=CC=CC=C1)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_des...
null
null
14
HOUR
4-Amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-pyridyl)benzamide (225.3 mg, 0.50 mmol) was dissolved in methylene chloride (2.0 ml) to which were subsequently added pyridine (0.05 ml, 0.62 mmol) and benzoyl chloride (0.09 ml, 0.77 mmol). After 14 hours of stirring at room temperature, the reaction solution was...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1
HCl
C(Cl)Cl
null
14
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(Cl)c1ccccc1>C(Cl)Cl>O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1)c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-df4b0db0bdde491cb5906e69e4e16de2
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1.O=C(Cl)c1ccccc1>>O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1)c1ccccc1
NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1.C(C1=CC=CC=C1)(=O)Cl.N1=CC=CC=C1>>C(C1=CC=CC=C1)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1
[NH2:3][c:4]1[cH:5][cH:6][c:7]([C:8](=[O:9])[N:10]([CH2:11][CH2:12][N:13]2[CH2:14][CH2:15][CH:16]([C:17](=[O:18])[c:19]3[cH:20][cH:21][cH:22][cH:23][cH:24]3)[CH2:25][CH2:26]2)[c:27]2[cH:28][cH:29][cH:30][n:31][cH:32]2)[cH:33][cH:34]1.Cl[C:2](=[O:1])[c:35]1[cH:36][cH:37][cH:38][cH:39][cH:40]1>>[O:1]=[C:2]([NH:3][c:4]1[c...
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1.O=C(Cl)c1ccccc1
O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1)c1ccccc1
null
null
null
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1)c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
85.9
[{"value": 85.9, "product": "C(C1=CC=CC=C1)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.9, "product": "C(C1=CC=CC=C1)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired":...
null
null
null
null
Using 4-amino-N-[2-(4-benzoylpiperidino)ethyl]-N-(3-pyridyl)benzamide (210.7 mg, 0.49 mmol), benzoyl chloride (0.07 ml, 0.60 mmol) and pyridine (0.05 ml, 0.62 mmol), the procedure of Inventive Example 165 was repeated to obtain 224.3 mg (85.9%) of the title compound in a colorless powder form. Conditions: See reaction....
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1
HCl
null
null
null
Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1.O=C(Cl)c1ccccc1>>O=C(Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccccc3)CC2)c2cccnc2)cc1)c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e047a94edb4343a0b2070338fbae9a7f
Cl>>Cl
FC1=CC=C(C(=O)C2CCN(CC2)CCN(S(=O)(=O)C2=CCC(C=C2)=NO)C2=C(C=CC=C2)OC)C=C1.Cl.CCOCC>>Cl.FC1=CC=C(C(=O)C2CCN(CC2)CCN(S(=O)(=O)C2=CCC(C=C2)=NO)C2=C(C=CC=C2)OC)C=C1
[ClH:38]>>[ClH:38]
Cl
Cl
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
99.8
[{"value": 99.8, "product": "Cl.FC1=CC=C(C(=O)C2CCN(CC2)CCN(S(=O)(=O)C2=CCC(C=C2)=NO)C2=C(C=CC=C2)OC)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-4-(N-hydroxyimino)-N-(2-methoxyphenyl)benzenesulfonamide (65 mg, 0.12 mmol) was dissolved in methylene chloride (2 ml) to which was subsequently added saturated hydrogen chloride/ether solution (1 ml). After 5 minutes of stirring, the solvent was removed by evaporation, and th...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(Cl)Cl
null
0.083333
Cl>C(Cl)Cl>Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e34cf84fd5b941c6b9c20c5106e6df70
O=C(O)C(=O)O>>O=C(O)C(=O)O
FC1=CC=C(C(=O)C2CCN(CC2)CCN(C(C2=CC(=CC=C2)OC)=O)C2=C(C=CC=C2)OC)C=C1.C(C(=O)O)(=O)O>>C(C(=O)O)(=O)O.FC1=CC=C(C(=O)C2CCN(CC2)CCN(C(C2=CC(=CC=C2)OC)=O)C2=C(C=CC=C2)OC)C=C1
[O:37]=[C:38]([OH:39])[C:40](=[O:41])[OH:42]>>[O:37]=[C:38]([OH:39])[C:40](=[O:41])[OH:42]
O=C(O)C(=O)O
O=C(O)C(=O)O
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
79.2
[{"value": 79.2, "product": "C(C(=O)O)(=O)O.FC1=CC=C(C(=O)C2CCN(CC2)CCN(C(C2=CC(=CC=C2)OC)=O)C2=C(C=CC=C2)OC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.0, "product": "C(C(=O)O)(=O)O.FC1=CC=C(C(=O)C2CCN(CC2)CCN(C(C2=CC(=CC=C2)OC)=O)C2=C(C=CC=C2)OC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is...
null
null
5
MINUTE
N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-3-methoxy-N-(2-methoxyphenyl)benzamide (107 mg, 0.218 mmol) was dissolved in methanol (10 ml) to which was subsequently added oxalic acid (19.7 mg, 0.218 mmol). After 5 minutes of stirring at room temperature, methanol was removed by evaporation, and the resulting residue was ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
CO
null
0.083333
O=C(O)C(=O)O>CO>O=C(O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6520b67c10374e1083985864bd8780e4
O=C(O)C(=O)O>>O=C(O)C(=O)O.O=C(O)C(=O)O
N[C@H](C(=O)NCC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)C.C(C(=O)O)(=O)O>>C(C(=O)O)(=O)O.C(C(=O)O)(=O)O.N[C@H](C(=O)NCC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)C
[O:42]=[C:43]([OH:50])[C:51](=[O:52])[OH:53]>>[O:42]=[C:43]([OH:44])[C:45](=[O:46])[OH:47].[O:48]=[C:49]([OH:50])[C:51](=[O:52])[OH:53]
O=C(O)C(=O)O
O=C(O)C(=O)O.O=C(O)C(=O)O
null
null
CO
Miscellaneous
OtherReaction
d52db42154f846296f410f93ad678e29ddc4afd10ba8f991fe2f0397ee45638b
fe8a5e2dc0843e8c5be2b5940263c4d09e942bd97e1a4358b629c45d65454049
null
[O;D1;H0:1]=[C;H0;D3;+0:2](-[OH;D1;+0:3])-[C;H0;D3;+0:4](=[O;D1;H0:5])-[O;D1;H1:6]>>[O;D1;H0:1]=[C;H0;D3;+0:2](-[O;D1;H1:7])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10].[O;D1;H0:11]=[C:12](-[OH;D1;+0:3])-[C;H0;D3;+0:4](=[O;D1;H0:5])-[O;D1;H1:6]
85.1
[{"value": 85.1, "product": "C(C(=O)O)(=O)O.C(C(=O)O)(=O)O.N[C@H](C(=O)NCC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.2, "product": "C(C(=O)O)(=O)O.C(C(=O)O)(=O)O.N[C@H](C(=O)NCC1=CC=C(C(=O)N(C2=C(C=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C...
null
null
5
MINUTE
4-[(S)-2-Aminopropionyl]aminomethyl-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(2-methoxyphenyl)benzamide (84.7 mg, 0.155 mmol) was dissolved in methanol (5 ml) and mixed with oxalic acid (28 mg, 0.311 mmol). After 5 minutes of stirring at room temperature, methanol was removed by evaporation, and the resulting amorp...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid
Carboxylic acid.Carboxylic acid.Carboxylic acid.Carboxylic acid
null
null
null
Other
CO
null
0.083333
O=C(O)C(=O)O>CO>O=C(O)C(=O)O.O=C(O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-302c0855e821470884d0b4e53dc0fedc
O=C(O)/C=C/C(=O)O>>O=C(O)/C=C/C(=O)O
C(\C=C\C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1>>C(\C=C\C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
[O:39]=[C:40]([OH:41])/[CH:42]=[CH:43]/[C:44](=[O:45])[OH:46]>>[O:39]=[C:40]([OH:41])/[CH:42]=[CH:43]/[C:44](=[O:45])[OH:46]
O=C(O)/C=C/C(=O)O
O=C(O)/C=C/C(=O)O
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
80
[{"value": 80.0, "product": "C(\\C=C\\C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.9, "product": "C(\\C=C\\C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "...
null
null
null
null
4-Acetylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide (282.4 mg, 0.55 mmol) was dissolved in methanol (1.5 ml) and mixed with a methanol solution (3.0 ml) of fumaric acid (63.8 mg, 0.55 mmol) at 0° C. Thereafter, the thus precipitated crystals were collected by filtration and washed with...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
CO
null
null
O=C(O)/C=C/C(=O)O>CO>O=C(O)/C=C/C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f8098aa2891d4fcea8abf7e7fa4e55c8
O=C(O)C(O)C(O)C(=O)O>>O=C(O)C(O)C(O)C(=O)O
C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(C(O)C(O)C(=O)O)(=O)O>>C(C(O)C(O)C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
[O:39]=[C:40]([OH:41])[CH:42]([OH:43])[CH:44]([OH:45])[C:46](=[O:47])[OH:48]>>[O:39]=[C:40]([OH:41])[CH:42]([OH:43])[CH:44]([OH:45])[C:46](=[O:47])[OH:48]
O=C(O)C(O)C(O)C(=O)O
O=C(O)C(O)C(O)C(=O)O
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
75.3
[{"value": 75.3, "product": "C(C(O)C(O)C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.4, "product": "C(C(O)C(O)C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details":...
null
null
null
null
Using 4-acetylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide (155.0 mg, 0.30 mmol) and tartaric acid (35.0 mg, 0.30 mmol), the procedure of Inventive Example 211 was repeated to obtain 143.0 mg (75.3%) of the title compound in a colorless powder form. Conditions: See reaction.notes.proced...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
O=C(O)C(O)C(O)C(=O)O>>O=C(O)C(O)C(O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a5a1347378234e5ea5c192cce8e4d5a5
O=C(O)/C=C\C(=O)O>>O=C(O)/C=C\C(=O)O
C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(\C=C/C(=O)O)(=O)O>>C(\C=C/C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1
[O:39]=[C:40]([OH:41])/[CH:42]=[CH:43]\[C:44](=[O:45])[OH:46]>>[O:39]=[C:40]([OH:41])/[CH:42]=[CH:43]\[C:44](=[O:45])[OH:46]
O=C(O)/C=C\C(=O)O
O=C(O)/C=C\C(=O)O
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
86.3
[{"value": 82.0, "product": "C(\\C=C/C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.3, "product": "C(\\C=C/C(=O)O)(=O)O.C(C)(=O)NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1", "details": "CA...
null
null
null
null
Using 4-acetylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide (155.0 mg, 0.30 mmol) and maleic acid (45.0 mg, 0.30 mmol), the procedure of Inventive Example 211 was repeated to obtain 164.0 mg (82.0%) of the title compound in a colorless powder form. Conditions: See reaction.notes.procedur...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
null
null
null
O=C(O)/C=C\C(=O)O>>O=C(O)/C=C\C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5dbd58a197604caab9440bf88042ff6e
O=C(O)/C=C\C(=O)O>>O=C(O)/C=C\C(=O)O
C(\C=C/C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1>>C(\C=C/C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1
[O:33]=[C:34]([OH:35])/[CH:36]=[CH:37]\[C:38](=[O:39])[OH:40]>>[O:33]=[C:34]([OH:35])/[CH:36]=[CH:37]\[C:38](=[O:39])[OH:40]
O=C(O)/C=C\C(=O)O
O=C(O)/C=C\C(=O)O
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
65
[{"value": 65.0, "product": "C(\\C=C/C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.9, "product": "C(\\C=C/C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=CC=C2)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_des...
null
null
null
null
4-Amino-N-[2-(4-benzoylpiperidino)ethyl]-N-(3-pyridyl)benzamide (3.00 g, 7.00 mmol) was dissolved in ethanol (10.0 ml) to which was subsequently added a ethanol solution (20.0 ml) of maleic acid (812.0 mg, 7.00 mmol) at room temperature, and then stirred. After the solvent was removed by evaporation, the thus precipita...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
null
O=C(O)/C=C\C(=O)O>C(C)O>O=C(O)/C=C\C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a962f676bde548c9a208b5b8ceb746c5
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.O=C(O)/C=C/C(=O)O>>COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.O=C(O)/C=C/C(=O)O
C(\C=C\C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1>>C(\C=C\C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C2=CC(=CC=C2)OC)C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([N:8]([CH2:9][CH2:10][N:11]2[CH2:12][CH2:13][CH:14]([C:15](=[O:16])[c:17]3[cH:18][cH:19][c:20]([F:21])[cH:22][cH:23]3)[CH2:24][CH2:25]2)[C:26](=[O:27])[c:28]2[cH:34][cH:65][c:66]([NH2:67])[cH:68][cH:69]2)[cH:35]1.[CH:29](\[C:61](=[O:37])[OH:73])=[CH:75]/[C:76](=[O:77])[OH:78]>>...
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.O=C(O)/C=C/C(=O)O
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.O=C(O)/C=C/C(=O)O
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
d99497f14d4f4bc92f42b4b0346079b94e44e7f2193cc22aed8edda8f26f9827
7d7ef14e29161ac6606a818938036c070d59cc351f9ef3544d96d28ae95e8fcd
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2ccccc2)CC1.O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2ccccc2)CC1
[C:1]-[#7:2](-[c:3])-[C:4](=[O;D1;H0:5])-[c;H0;D3;+0:6]1:[cH;D2;+0:7]:[cH;D2;+0:8]:[c:9](-[N;D1;H2:10]):[c:11]:[cH;D2;+0:12]:1.[O;D1;H0:13]=[C:14](-[O;D1;H1:15])/[CH;D2;+0:16]=[CH;D2;+0:17]/[C;H0;D3;+0:18](=[O;H0;D1;+0:19])-[OH;D1;+0:20]>>[C:1]-[#7:2](-[c:3])-[C:4](=[O;D1;H0:5])-[c;H0;D3;+0:6]1:[cH;D2;+0:17]:[c:21]:[c:...
90.1
[{"value": 90.0, "product": "C(\\C=C\\C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C2=CC(=CC=C2)OC)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C2=CC(=CC=C2)OC)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.1, "product": "C(\\C=C\\C(=O)O)(=O)O.NC1=CC=C(C(=O)N(C2=CC(=CC=C2)O...
null
null
null
null
4-Amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide (475.0 mg, 1.00 mmol) was dissolved in methanol (4.0 ml) and mixed with a methanol solution (3.0 ml) of fumaric acid (58.0 mg, 0.50 mmol) at 0° C. Thereafter, the thus precipitated crystals were collected by filtration and recrystallized fr...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Aromatic halide.Carboxylic acid.Ketone.Ether.Tertiary amide.Primary amine.Tertiary amine
c1ccccc1
c1ccccc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccccc1
Other
CO
null
null
COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.O=C(O)/C=C/C(=O)O>CO>COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.COc1cccc(N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)C(=O)c2ccc(N)cc2)c1.O=C(O)/C=C/C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1d509de57fab4ad7907e706bebccd055
O=C(O)/C=C/C(=O)O.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1>>O=C(O)/C=C/C(=O)O.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1
C(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.C(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1
[O:1]=[C:16]([OH:3])/[CH:4]=[CH:5]/[C:6](=[O:7])[OH:8].[cH:2]1[c:27]([C:25]([CH:24]2[CH2:23][CH2:22][N:21]([CH2:55][CH2:54][N:53]([C:51]([c:50]3[cH:49][cH:13][c:12]([NH:11][CH:10]=[O:9])[cH:78][cH:77]3)=[O:52])[c:71]3[cH:72][cH:73][cH:74][n:75][cH:76]3)[CH2:35][CH2:34]2)=[O:26])[cH:33][cH:32][c:30]([F:31])[cH:29]1>>[O:...
O=C(O)/C=C/C(=O)O.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1
O=C(O)/C=C/C(=O)O.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
e0dd5bcaad88b046af8e17e6365574936f8c260d3d40d3e396f8a17ad590e6b4
b3be6655e88bf7057db2af69af8f15e012e15c8526e235ce83853278f54d5884
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1.O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
[#7;a:1]:[c:2]:[c:3]-[#7:4](-[C:5]-[CH2;D2;+0:6]-[N;H0;D3;+0:7]1-[C:8]-[C:9]-[C:10](-[C:11](=[O;D1;H0:12])-[c;H0;D3;+0:13]2:[c:14]:[c:15]:[c:16](-[F;D1;H0:17]):[cH;D2;+0:18]:[cH;D2;+0:19]:2)-[C:20]-[C:21]-1)-[C:22](=[O;D1;H0:23])-[c:24]1:[c:25]:[cH;D2;+0:26]:[c;H0;D3;+0:27](-[#7:28]-[C:29]=[O;D1;H0:30]):[cH;D2;+0:31]:[...
52.1
[{"value": 52.1, "product": "C(\\C=C\\C(=O)O)(=O)O.C(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.1, "product": "C(\\C=C\\C(=O)O)(=O)O.C(=O)NC1=CC=C(C(=O)N(C=2C=NC...
null
null
null
null
Using 4-formylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-pyridyl)benzamide (208.8 mg, 0.44 mmol) and fumaric acid (25.8 mg, 0.22 mmol), the procedure of Inventive Example 271 was repeated to obtain 122.2 mg (52.1%) of the title compound in a colorless powder form. Conditions: See reaction.notes.procedure_det...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ketone.Tertiary amine
Aromatic halide.Carboxylic acid.Ketone.Ketone.Secondary amide.Tertiary amide.Tertiary amine.Tertiary amine
c1ccccc1.C1CC[NH]CC1.c1ccccc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
Other
null
null
null
O=C(O)/C=C/C(=O)O.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1>>O=C(O)/C=C/C(=O)O.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7ace0fd1bbf443febb2d3c42fd67234e
CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
C(CCCC)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.C(CCCC)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(CCCC)(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][C:5](=[O:6])[NH:7][c:8]1[cH:39][cH:49][c:50]([C:51](=[O:52])[N:53]([CH2:54][CH2:15][N:14]2[CH2:18][CH2:19][CH:20]([C:21](=[O:22])[c:23]3[cH:24][cH:25][c:26]([F:27])[cH:28][cH:29]3)[CH2:30][CH2:31]2)[c:71]2[cH:72][cH:73][cH:74][n:75][cH:76]2)[cH:77][cH:78]1.[CH:9](=[CH:11]/[C:12](=[O:13])[OH...
CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
77a6e278dd1899fb2b2794161dc642076da2e1e94a9c21a82946154653e6ba6d
8f534bc4e0c26fc38c60205abe754e433ff59df7fb20cdb9be5e34183702ecfd
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1.O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
[#7;a:1]:[c:2]:[c:3]-[#7:4](-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[N;H0;D3;+0:7]1-[CH2;D2;+0:8]-[C:9]-[C:10](-[C:11]=[O;D1;H0:12])-[C:13]-[CH2;D2;+0:14]-1)-[C:15](=[O;D1;H0:16])-[c:17]1:[c:18]:[cH;D2;+0:19]:[c;H0;D3;+0:20](-[#7:21]-[C:22](-[C:23])=[O;D1;H0:24]):[cH;D2;+0:25]:[cH;D2;+0:26]:1.[O;D1;H0:27]=[C;H0;D3;+0:28](-[OH;D1;...
84
[{"value": 84.0, "product": "C(\\C=C\\C(=O)O)(=O)O.C(CCCC)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(CCCC)(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.0, "product": "C(\\C=C\\C(=O)O)(=O)O.C(CCCC)(=O)NC1=C...
null
null
null
null
Using 4-valerylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]-ethyl}-N-(3-pyridyl)benzamide (139.4 mg, 0.26 mmol) and fumaric acid (15.4 mg, 0.13 mmol), the procedure of inventive Example 271 was repeated to obtain 128.5 mg (84.0%) of the title compound in a light brown amorphous powder form. Conditions: See reaction.notes...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Tertiary amine
Aromatic halide.Carboxylic acid.Carboxylic acid.Ketone.Secondary amide.Tertiary amide.Tertiary amine.Tertiary amine
c1ccccc1.C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
Other
null
null
null
CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CCCCC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b0202fb642d54f90b89cb29bdb39c9eb
CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
CNC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.CNC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.CNC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1
[CH3:1][NH:2][c:3]1[cH:4][cH:5][c:40]([C:41](=[O:42])[N:43]([CH2:44][CH2:45][N:46]2[CH2:26][CH2:25][CH:15]([C:16](=[O:17])[c:18]3[cH:19][cH:20][c:21]([F:22])[cH:23][cH:24]3)[CH2:14][CH2:47]2)[c:61]2[cH:62][cH:63][cH:64][n:65][cH:66]2)[cH:67][cH:68]1.[CH:6](\[C:7](=[O:8])[OH:71])=[CH:73]/[C:74](=[O:75])[OH:76]>>[CH3:1][...
CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
1ea08c88515e18492fc92ff8d1ebda2338cf66e7185546e193e7efa43313715a
136cf14da7a3e2c40cd9243eaea88d757bbca88fc839111ff5e0267ced2fe70f
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1.O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
[#7;a:1]:[c:2]:[c:3]-[#7:4](-[C:5]-[C:6]-[N;H0;D3;+0:7]1-[CH2;D2;+0:8]-[C:9]-[C:10](-[C:11](=[O;D1;H0:12])-[c:13])-[CH2;D2;+0:14]-[CH2;D2;+0:15]-1)-[C:16](=[O;D1;H0:17])-[c;H0;D3;+0:18]1:[c:19]:[cH;D2;+0:20]:[c;H0;D3;+0:21](-[#7:22]-[C;D1;H3:23]):[c:24]:[cH;D2;+0:25]:1.[O;D1;H0:26]=[C:27](-[O;D1;H1:28])/[CH;D2;+0:29]=[...
79.2
[{"value": 79.2, "product": "C(\\C=C\\C(=O)O)(=O)O.CNC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.CNC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.2, "product": "C(\\C=C\\C(=O)O)(=O)O.CNC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC...
null
null
null
null
Using 4-methylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-pyridyl)benzamide (209.5 mg, 0.45 mmol) and fumaric acid (26.7 mg, 0.23 mmol), the procedure of Inventive Example 271 was repeated to obtain 184.9 mg (79.2%) of the title compound in a light brown powder form. Conditions: See reaction.notes.procedure_d...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amine
Aromatic halide.Carboxylic acid.Ketone.Tertiary amide.Secondary amine.Tertiary amine.Tertiary amine
c1ccccc1.C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
Other
null
null
null
CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CNc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-77277727d2c54daf907c8832e8787aea
CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
CS(=O)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.CS(=O)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.CS(=O)(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1
[CH3:1][S:2](=[O:3])([NH:5][c:6]1[cH:7][cH:8][c:9]([C:10](=[O:11])[N:12]([CH2:13][CH2:14][N:15]2[CH2:16][CH2:17][CH:18]([C:19](=[O:20])[c:21]3[cH:22][cH:23][c:24]([F:25])[cH:26][cH:27]3)[CH2:28][CH2:29]2)[c:30]2[cH:31][cH:32][cH:33][n:34][cH:35]2)[cH:36][cH:37]1)=[O:48].[CH:38](=[CH:46]/[C:47](=[O:57])[OH:77])\[C:80](=...
CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
0cc1932952fb7ddce4943e7c0fc955dc2cef39e8498759d96225f32b90a1a247
a1d0154ed7de4e2cdea2e4f9329a9a5cbd5fa165b1d2696743349d8850c6f002
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1.O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
[C;D1;H3:1]-[S;H0;D4;+0:2](=[O;D1;H0:3])(=[O;H0;D1;+0:4])-[#7:5]-[c:6].[O;D1;H0:7]=[C;H0;D3;+0:8](-[O;D1;H1:9])/[CH;D2;+0:10]=[CH;D2;+0:11]/[C;H0;D3;+0:12](=[O;H0;D1;+0:13])-[OH;D1;+0:14]>>[#7:15]-[#16:16](-[CH3;D1;+0:10])(=[O;D1;H0:17])=[O;D1;H0:18].[C:19]-[#7:20](-[c:21])-[C;H0;D3;+0:12](=[O;H0;D1;+0:4])-[c;H0;D3;+0:...
43.3
[{"value": 43.3, "product": "C(\\C=C\\C(=O)O)(=O)O.CS(=O)(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.CS(=O)(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 43.3, "product": "C(\\C=C\\C(=O)O)(=O)O.CS(=O)(=O)NC1=CC=C...
null
null
null
null
Using 4-methanesulfonylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-pyridyl)benzamide (216.8 mg, 0.41 mmol) and fumaric acid (24.3 mg, 0.21 mmol), the procedure of Inventive Example 271 was repeated to obtain 103.4 mg (43.3%) of the title compound in a light brown powder form. Conditions: See reaction.notes.pr...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Carboxylic acid.Carboxylic acid
Sulfonamide.Sulfonamide.Aromatic halide.Carboxylic acid.Carboxylic acid.Ketone.Tertiary amide.Tertiary amine
null
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
Other
null
null
null
CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CS(=O)(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-034be36ecab9479fa366c758723e800c
CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
C(C)OC(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.C(C)OC(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(C)OC(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1
[C:4](=[O:5])([NH:6][c:7]1[cH:38][cH:47][c:48]([C:49](=[O:50])[N:51]([CH2:52][CH2:53][N:54]2[CH2:30][CH2:29][CH:19]([C:20](=[O:21])[c:22]3[cH:23][cH:24][c:25]([F:26])[cH:27][cH:28]3)[CH2:18][CH2:55]2)[c:69]2[cH:70][cH:71][cH:72][n:73][cH:74]2)[cH:75][cH:76]1)[O:41][CH2:40][CH3:39].[CH:1](=[CH:10]/[C:11]([OH:3])=[O:12])...
CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
d8074e10f13e8c947e4401144c88430dacf96ad4b076ac58e69be8208df1e890
ce6ebc241c0180bc5b7e4aa5c52e1db4bf6065e3c24c593e4e764aae52ad3fd1
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1.O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
[#7;a:1]:[c:2]:[c:3]-[#7:4](-[C:5]-[C:6]-[N;H0;D3;+0:7]1-[CH2;D2;+0:8]-[C:9]-[C:10](-[C:11](=[O;D1;H0:12])-[c:13])-[CH2;D2;+0:14]-[CH2;D2;+0:15]-1)-[C:16](=[O;D1;H0:17])-[c:18]1:[c:19]:[cH;D2;+0:20]:[c;H0;D3;+0:21](-[#7:22]-[C;H0;D3;+0:23](=[O;D1;H0:24])-[O;H0;D2;+0:25]-[C:26]-[C;D1;H3:27]):[cH;D2;+0:28]:[cH;D2;+0:29]:...
75
[{"value": 75.0, "product": "C(\\C=C\\C(=O)O)(=O)O.C(C)OC(=O)NC1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(C)OC(=O)NC1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.0, "product": "C(\\C=C\\C(=O)O)(=O)O.C(C)OC(=O)NC1=CC=C...
null
null
null
null
Using 4-ethoxycarbonylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-pyridyl)benzamide (121.9 mg, 0.24 mmol) and fumaric acid (14.0 mg, 0.12 mmol), the procedure of Inventive Example 271 was repeated to obtain 103.8 mg (75.0%) of the title compound in a light yellow amorphous powder form. Conditions: See reactio...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid.Carboxylic acid.Ether.Tertiary amine
Aromatic halide.Carbamic ester.Carbamic ester.Carboxylic acid.Carboxylic acid.Ketone.Ether.Ether.Tertiary amide.Tertiary amine.Tertiary amine
c1ccccc1.C1CC[NH]CC1
c1ccccc1.C1CC[NH]CC1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
Other
null
null
null
CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.CCOC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-13e89f18360245ff8b311352b34982c9
NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
N(C(=O)N)C1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.C(\C=C\C(=O)O)(=O)O>>C(\C=C\C(=O)O)(=O)O.N(C(=O)N)C1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.N(C(=O)N)C1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1
[NH2:1][C:2](=[O:3])[NH:4][c:5]1[cH:42][cH:43][c:44]([C:45](=[O:46])[N:47]([CH2:12][CH2:13][N:14]2[CH2:15][CH2:16][CH:17]([C:18](=[O:19])[c:20]3[cH:6][cH:22][c:23]([F:24])[cH:25][cH:26]3)[CH2:27][CH2:28]2)[c:65]2[cH:66][cH:67][cH:68][n:69][cH:70]2)[cH:71][cH:72]1.[C:9](=[O:10])([OH:75])/[CH:76]=[CH:77]/[C:78](=[O:79])[...
NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
56fb88dc2a8ec61671fa24ae794a358eda9ef9d167b2c536313e037c1a77c0a9
325c796fb6a1dde76d7100a8e360c70bcf9a979d17e7bce1f300a284d4404e43
O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1.O=C(c1ccccc1)C1CCN(CCN(C(=O)c2ccccc2)c2cccnc2)CC1
[#7:1]-[C:2]-[CH2;D2;+0:3]-[N;H0;D3;+0:4](-[C:5](=[O;D1;H0:6])-[c:7]1:[c:8]:[cH;D2;+0:9]:[c;H0;D3;+0:10](-[#7:11]-[C:12](-[N;D1;H2:13])=[O;D1;H0:14]):[cH;D2;+0:15]:[c:16]:1)-[c:17](:[c:18]):[c:19]:[#7;a:20]:[c:21].[C:22]-[C:23](=[O;D1;H0:24])-[c;H0;D3;+0:25]1:[c:26]:[c:27]:[c:28](-[F;D1;H0:29]):[cH;D2;+0:30]:[cH;D2;+0:...
56.5
[{"value": 56.3, "product": "C(\\C=C\\C(=O)O)(=O)O.N(C(=O)N)C1=CC=C(C(=O)N(C=2C=NC=CC2)CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=C1.N(C(=O)N)C1=CC=C(C(=O)N(CCN2CCC(CC2)C(C2=CC=C(C=C2)F)=O)C=2C=NC=CC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.5, "product": "C(\\C=C\\C(=O)O)(=O)O.N(C(=O)N)C1=CC=C(C(=O)...
null
null
null
null
Using 4-ureido-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-pyridyl)benzamide (174.1 mg, 0.36 mmol) and fumaric acid (20.8 mg, 0.18 mmol), the procedure of Inventive Example 271 was repeated to obtain 111.3 mg (56.3%) of the title compound in a colorless powder form. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ketone.Tertiary amide
Aromatic halide.Carboxylic acid.Ketone.Ketone.Urea.Tertiary amide.Tertiary amide.Tertiary amine
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1
c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1.c1ccccc1.C1CC[NH]CC1.c1ccccc1.c1ccncc1
Other
null
null
null
NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O>>NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.NC(=O)Nc1ccc(C(=O)N(CCN2CCC(C(=O)c3ccc(F)cc3)CC2)c2cccnc2)cc1.O=C(O)/C=C/C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-306a34f7cedd44f8814563b5b59e069e
ClCC1CO1>>O
C(Cl)C1CO1.CN(C)C=1C=CC(=CC1)C(=C2C=CC(=[N+](C)C)C=C2)C=3C=CC(=CC3)N(C)C.[Cl-].CCCCOCCOCCOCCO.ClCCCCCCCC.C(Cl)C1CO1>>CCCCOCCOCCOCCO.O
ClCC1C[O:15]1>>[OH2:15]
ClCC1CO1
O
null
[Br-].C(C)[N+](CC)(CC)CC
C(C)(=O)O.C1(=CC=CC=C1)C.O
Deprotection
OtherReaction
a619f2e0552ef75ef9030e73f4b1ba8ca084840857fdafad4b59fd097c293d2d
0c91e0607effca920df6a9d3a12c737d83516506f3670708be3ed1e59dc9b90b
null
Cl-C-C1-C-[O;H0;D2;+0:1]-1>>[OH2;D0;+0:1]
null
[]
55
CELSIUS
null
null
To a first 250 ml round bottom flask equipped with a stirrer, nitrogen inlet tube, and a distillation head were added 1 part of NP-(EO)150 -OH (surfactant) and 2 parts of toluene. To a second 250 ml round bottom flask equipped with a stirrer, nitrogen inlet tube, and a distillation head were added 1 part of NP-(EO)50 -...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
null
C1CO1
null
null
HCl
[Br-].C(C)[N+](CC)(CC)CC.C(C)(=O)O.C1(=CC=CC=C1)C.O
55
null
ClCC1CO1>[Br-].C(C)[N+](CC)(CC)CC.C(C)(=O)O.C1(=CC=CC=C1)C.O>O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-aa1345f1ddf34fbca738e90d0801abc6
C1CO1.CC(=O)O.CC(=O)O.CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1.ClCC1CO1.ClCC1CO1>>CCCCOCCOCCOCCO.O
OC1=CC=C(C=C1)C(C)(C)C1=CC=C(C=C1)O.C(Cl)C1CO1.C1CO1.C(Cl)C1CO1.C(C)(=O)O.C(C)(=O)O.CN(C)C=1C=CC(=CC1)C(=C2C=CC(=[N+](C)C)C=C2)C=3C=CC(=CC3)N(C)C.[Cl-]>>CCCCOCCOCCOCCO.O
[CH2:2]1[CH2:3][O:11]1.C[C:6](=O)[OH:5].CC(=O)[OH:15].CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)[CH3:1])cc2)cc1.Cl[CH2:10][CH:9]1[CH2:7][O:8]1.Cl[CH2:12][CH:13]1[CH2:4][O:14]1>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][CH2:6][CH2:7][O:8][CH2:9][CH2:10][O:11][CH2:12][CH2:13][OH:14].[OH2:15]
C1CO1.CC(=O)O.CC(=O)O.CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1.ClCC1CO1.ClCC1CO1
CCCCOCCOCCOCCO.O
null
[Br-].C(C)[N+](CC)(CC)CC
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
e5ce9d35bb099894796d2d2252d3dbc197d128e21deb0a1c8abbe13527bff6a4
c8581f7c1d3afdaf3f59e3a015db52ccf6715724aa72f51cf92bb224b8af1304
null
C-C(=O)-[OH;D1;+0:1].C-N(-C)-c1:c:c:c(-C(=C2-C=C-C(=[N+](-C)-C)-C=C-2)-c2:c:c:c(-N(-C)-[CH3;D1;+0:2]):c:c:2):c:c:1.C-[C;H0;D3;+0:3](=O)-[OH;D1;+0:4].Cl-[CH2;D2;+0:5]-[CH;D3;+0:6]1-[#8:7]-[CH2;D2;+0:8]-1.Cl-[CH2;D2;+0:9]-[CH;D3;+0:10]1-[CH2;D2;+0:11]-[O;H0;D2;+0:12]-1.[CH2;D2;+0:13]1-[CH2;D2;+0:14]-[O;H0;D2;+0:15]-1>>[C...
null
[]
60
CELSIUS
8
HOUR
To a first 250 ml round bottom flask equipped with a stirrer, nitrogen inlet tube, and a distillation head were added 1 part of DNP-(EO)6 -OH and 2 parts of toluene. To a second 250 ml round bottom flask equipped with a stirrer, nitrogen inlet tube, and a distillation head were added 1 part of bis-phenol A ethoxylated ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Carboxylic acid.Carboxylic acid.Ether.Ether.Ether.Tertiary amine.Tertiary amine
Ether.Ether.Ether.Primary alcohol
C1CO1.c1ccccc1.C1=CCC=CC1.c1ccccc1.C1CO1.C1CO1
null
null
HCl
[Br-].C(C)[N+](CC)(CC)CC.C1(=CC=CC=C1)C
60
8
C1CO1.CC(=O)O.CC(=O)O.CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1.ClCC1CO1.ClCC1CO1>[Br-].C(C)[N+](CC)(CC)CC.C1(=CC=CC=C1)C>CCCCOCCOCCOCCO.O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e7b93282e05f4addbe5f6faab80d2b9a
ClC(Cl)(Cl)CC(Cl)(Cl)Cl.FC(F)(F)CC(F)(F)F>>FC(F)(F)CC(F)(F)Cl
C(F)(F)(F)CC(F)(F)F.C(Cl)(Cl)(Cl)CC(Cl)(Cl)Cl.[OH-].[K+]>>C(F)(F)(F)CC(F)(F)Cl
ClC(Cl)(Cl)CC(Cl)(Cl)[Cl:9].F[C:6]([CH2:5][C:2]([F:1])([F:3])[F:4])([F:7])[F:8]>>[F:1][C:2]([F:3])([F:4])[CH2:5][C:6]([F:7])([F:8])[Cl:9]
ClC(Cl)(Cl)CC(Cl)(Cl)Cl.FC(F)(F)CC(F)(F)F
FC(F)(F)CC(F)(F)Cl
null
Cl[Ti](Cl)(Cl)Cl
null
Functional Group Interconversion
OtherReaction
5c1cc0a421428092036357338c2a9e28d4ea48f9a9bb3b8a410f65d0db5b5151
e96241dee8c87f77fef64eedceb32664ca29c817802fd0a7f1f1f0888f1617b4
null
Cl-C(-Cl)(-Cl)-C-C(-Cl)(-Cl)-[Cl;H0;D1;+0:1].F-[C;H0;D4;+0:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C:5]-[C:6](-[F;D1;H0:7])(-[F;D1;H0:8])-[F;D1;H0:9]>>[Cl;H0;D1;+0:1]-[C;H0;D4;+0:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[C:5]-[C:6](-[F;D1;H0:7])(-[F;D1;H0:8])-[F;D1;H0:9]
null
[]
-10
CELSIUS
null
null
A 600 mL, magnetically stirred, model autoclave fitted with a condenser (maintained at -10° C.), was evacuated, cooled to about -40° C., and charged with 0.6.9 g (0.036 mol) TiCl4 followed by 64 g (0.255 mol) CCl3CH2CCl3, and 102.5 g (5 mol) HF. The temperature was increased to 120° C. and maintained at that temperatur...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Trichloro group.Trichloro group
Tertiary halide.Tertiary halide.Tertiary halide
null
null
null
HF
Cl[Ti](Cl)(Cl)Cl
-10
null
ClC(Cl)(Cl)CC(Cl)(Cl)Cl.FC(F)(F)CC(F)(F)F>Cl[Ti](Cl)(Cl)Cl>FC(F)(F)CC(F)(F)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-784b63b848274e07b64f901c8865b018
CC(C)(C)[Si](C)(C)Cl.O=C1C=CC(O)C1>>CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
OC1C=CC(C1)=O.C(C)N(CC)CC.[Si](C)(C)(C(C)(C)C)Cl>>O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O
Cl[Si:5]([C:2]([CH3:1])([CH3:3])[CH3:4])([CH3:6])[CH3:7].[OH:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1
CC(C)(C)[Si](C)(C)Cl.O=C1C=CC(O)C1
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
null
CN(C1=CC=NC=C1)C
O1CCCC1
Protection
Alcohol protection with silyl ethers
e19079a85b3e2f818dbb25a774b915f0e7349126f5b76d72c22f1c90edfa8480
16de9d9d08d1cc67ec96e76fc213a6b49c0af7979ac901a377ee705ba5071899
O=C1C=CCC1
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7].[O;D1;H0:8]=[C:9]1-[C:10]=[C:11]-[C:12](-[OH;D1;+0:13])-[C:14]-1>>[C;D1;H3:5]-[C:4](-[C;D1;H3:6])(-[C;D1;H3:7])-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[O;H0;D2;+0:13]-[C:12]1-[C:11]=[C:10]-[C:9](=[O;D1;H0:8])-[C:14]-1
83.2
[{"value": 83.2, "product": "O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
8
HOUR
A solution of 4-hydroxy-2-cyclopentenone (191 g, 1.95 mol, prepared in example 1) and triethylamine (430 mL, 3.09 mol) in anhydrous tetrahydrofuran (1L) is treated with 4-dimethylaminopyridine (4.90 g, 40.0 mmol). The solution is cooled to 0° C. and treated portionwise, over 10 minutes, with tert-butyldimethylsilyl chl...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
TMS ether protective group
null
null
C1=CCCC1
HCl
CN(C1=CC=NC=C1)C.O1CCCC1
0
8
CC(C)(C)[Si](C)(C)Cl.O=C1C=CC(O)C1>CN(C1=CC=NC=C1)C.O1CCCC1>CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a6ecf5a0a0dd4c20a3f46740fd5078c7
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
COC(C)(C)C.[H-].[Al+3].[Li+].[H-].[H-].[H-].O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O.[I-].[Li+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
CCCCCCC
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1>>[OH;D1;+0:1]-[C@@H;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1
74
[{"value": 74.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.9, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-20
CELSIUS
5
MINUTE
A mechanically stirred solution of 4-tert-butyldimethylsiloxy-2-cyclopentenone (50.2 g, 236 mmol) in anhydrous toluene (1L) under an atmosphere of argon is treated with lithium iodide (160 g, 1.20 mol). The mixture is cooled to -20° C. and treated with lithium aluminum hydride (9.0 g, 237 mmol) in one portion. The reac...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1
null
CCCCCCC
-20
0.083333
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>CCCCCCC>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-555b3522584c4bcfba8254bfe842b079
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
COC(C)(C)C.[H-].[Al+3].[Li+].[H-].[H-].[H-].O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O.[I-].[Li+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
C1(=CC=CC=C1)C
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1>>[OH;D1;+0:1]-[C@@H;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1
68
[{"value": 68.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.9, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-20
CELSIUS
5
MINUTE
A mechanically stirred solution of 4-tert-butyldimethylsiloxy-2-cyclopentenone (175 g, 824 mmol) in anhydrous toluene (1.5L) under an atmosphere of argon is treated with lithium iodide (240 g, 1.79 mol). The mixture is cooled to -20° C. and treated with lithium aluminum hydride (13.5 g, 356 mmol) in one portion. The re...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1
null
C1(=CC=CC=C1)C
-20
0.083333
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>C1(=CC=CC=C1)C>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3ce9d725cf794ddb8c67a20faaad2014
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
[H-].[Al+3].[Li+].[H-].[H-].[H-].O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O.[I-].[Li+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
C(C)OCC
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1>>[OH;D1;+0:1]-[C@@H;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1
80
[{"value": 80.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}]
-78
CELSIUS
90
MINUTE
A mechanically stirred solution of 4-tert-butyldimethylsiloxy-2-cyclopentenone (1.01 g, 4.76 mmol) in anhydrous ethyl ether (20 mL) under an atmosphere of argon is treated with lithium iodide (3.20 g, 23.9 mmol). The mixture is cooled to -78° C. and treated with lithium aluminum hydride (184 mg, 4.85 mmol) in one porti...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1
null
C(C)OCC
-78
1.5
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>C(C)OCC>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-72213fef623a4ce0b58fb21b87067c20
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
COC(C)(C)C.O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O.[Br-].[Li+].[H-].[Al+3].[Li+].[H-].[H-].[H-]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
C1(=CC=CC=C1)C
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1>>[OH;D1;+0:1]-[C@@H;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1
69.2
[{"value": 69.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.2, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-20
CELSIUS
2
HOUR
A mechanically stirred solution of 4-tert-butyldimethylsiloxy-2-cyclopentenone (501 mg, 2.36 mmol) in anhydrous toluene (10 mL) under an atmosphere of argon is treated with lithium bromide (1.06 g, 12.2 mmol). The mixture is cooled to -20° C. with an ice/salt bath and treated with lithium aluminum hydride (92.0 mg, 2.4...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1
null
C1(=CC=CC=C1)C
-20
2
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>C1(=CC=CC=C1)C>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-763abd07f6784692a9ffa1edeb4f4481
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
[H-].[Al+3].[Li+].[H-].[H-].[H-].O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O.[OH-].[Na+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
null
[Cl-].[Cl-].[Zn+2]
null
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1>>[OH;D1;+0:1]-[C@@H;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1
64.4
[{"value": 64.4, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-20
CELSIUS
2
HOUR
A stirred solution of ZnCl2 (19 mL, 19 mmol, 1M in ether) is treated with 4-tert-butyldimethylsiloxy-2-cyclopentenone (2.0 g, 9.42 mmol) under an atmosphere of argon. The solution is cooled to -20° C. and treated dropwise with lithium aluminum hydride (9.0 mL, 9.0 mmol, 1M in ether) at such a rate as to keep the reacti...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1
null
[Cl-].[Cl-].[Zn+2]
-20
2
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>[Cl-].[Cl-].[Zn+2]>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4213d05daadd4cc1a427b80287607a1d
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
COC(C)(C)C.O([Si](C)(C)C(C)(C)C)C1C=CC(C1)=O.[Mg+2].[Br-].[Br-].[H-].[Al+3].[Li+].[H-].[H-].[H-].[H-].[Al+3].[Li+].[H-].[H-].[H-]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][CH:9]1[CH:10]=[CH:11][C:12](=[O:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
C1(=CC=CC=C1)C
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1>>[OH;D1;+0:1]-[C@@H;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1
64.4
[{"value": 64.4, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-25
CELSIUS
2
HOUR
A stirred solution of 4-tert-butyldimethylsiloxy-2-cyclopentenone (2.0 g, 9.42 mmol) in anhydrous toluene (15 mL) under an atmosphere of argon is treated with MgBr2 (3.5 g, 19.0 mol). The mixture is cooled to -25° C. and treated with lithium aluminum hydride (178 mg, 4.69 mmol) in one portion, followed by addition of a...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1
null
C1(=CC=CC=C1)C
-25
2
CC(C)(C)[Si](C)(C)OC1C=CC(=O)C1>C1(=CC=CC=C1)C>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-023d1f3b80054964a96469c5b88a1cdd
C1=COCCC1.O=C1C=CC(O)C1>>O=C1C=CC(OC2CCCCO2)C1
OC1C=CC(C1)=O.O1CCCC=C1.C1(=CC=C(C=C1)S(=O)(=O)[O-])C.[NH+]1=CC=CC=C1>>O1C(CCCC1)OC1C=CC(C1)=O
[CH:7]1=[CH:8][CH2:9][CH2:10][CH2:11][O:12]1.[O:1]=[C:2]1[CH:3]=[CH:4][CH:5]([OH:6])[CH2:13]1>>[O:1]=[C:2]1[CH:3]=[CH:4][CH:5]([O:6][CH:7]2[CH2:8][CH2:9][CH2:10][CH2:11][O:12]2)[CH2:13]1
C1=COCCC1.O=C1C=CC(O)C1
O=C1C=CC(OC2CCCCO2)C1
null
null
C(C)(=O)OCC.O1CCCC1
Heteroatom Alkylation and Arylation
oxa-Michael addition
7dbeed209463058f59d43728a589e5f7e9550a2179664f08902eb30ad7ba383b
2683964549e7d2a3e8c7989efc3c7275468eaa2a5d254179937977d9931444d1
O=C1C=CC(OC2CCCCO2)C1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[O;D1;H0:7]=[C:8]1-[C:9]-[C:10](-[OH;D1;+0:11])-[C:12]=[C:13]-1>>[O;D1;H0:7]=[C:8]1-[C:9]-[C:10](-[O;H0;D2;+0:11]-[CH;D3;+0:6]2-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-2)-[C:12]=[C:13]-1
76
[{"value": 76.0, "product": "O1C(CCCC1)OC1C=CC(C1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
A solution of 4-hydroxy-2-cyclopentenone (1.41 g, 14.4 mmol) in tetrahydrofuran (24 mL) is treated with 3,4-dihydro-2H-pyran (2 mL) and pyridinium p-toluenesulfonate (500 mg, PPTS). The reaction is stirred at room temperature for 18 hours. The reaction mixture is then diluted with ethyl acetate (25 mL) and washed with ...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
C1=CCCC1.C1CCOCC1
null
C(C)(=O)OCC.O1CCCC1
null
18
C1=COCCC1.O=C1C=CC(O)C1>C(C)(=O)OCC.O1CCCC1>O=C1C=CC(OC2CCCCO2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fcb0d5dcdda04901928d4fd9c09849c7
O=C1C=CC(OC2CCCCO2)C1>>O[C@@H]1C=C[C@H](OC2CCCCO2)C1
[OH-].[Na+].[H-].[Al+3].[Li+].[H-].[H-].[H-].[I-].[Li+].O1C(CCCC1)OC1C=CC(C1)=O>>O1C(CCCC1)O[C@H]1C=C[C@H](C1)O
[O:1]=[C:2]1[CH:3]=[CH:4][CH:5]([O:6][CH:7]2[CH2:8][CH2:9][CH2:10][CH2:11][O:12]2)[CH2:13]1>>[OH:1][C@@H:2]1[CH:3]=[CH:4][C@H:5]([O:6][CH:7]2[CH2:8][CH2:9][CH2:10][CH2:11][O:12]2)[CH2:13]1
O=C1C=CC(OC2CCCCO2)C1
O[C@@H]1C=C[C@H](OC2CCCCO2)C1
null
null
C1(=CC=CC=C1)C.COC(C)(C)C
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=C[C@H](OC2CCCCO2)CC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1>>[OH;D1;+0:1]-[C@H;D3;+0:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1
73.5
[{"value": 73.0, "product": "O1C(CCCC1)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.5, "product": "O1C(CCCC1)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A slurry of lithium aluminum hydride (222 mg, 5.8 mmol), lithium iodide (3.2 g, 24 mmol), tert-butyl methyl ether (6 mL) and toluene (16 mL) is cooled to -15° C. A solution of 4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enone (2.179 g, 11.97 mmol, prepared in example 5) in tert-butyl methyl ether (2 mL) and toluene (2 mL)...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1.C1CCOCC1
null
C1(=CC=CC=C1)C.COC(C)(C)C
null
0.5
O=C1C=CC(OC2CCCCO2)C1>C1(=CC=CC=C1)C.COC(C)(C)C>O[C@@H]1C=C[C@H](OC2CCCCO2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-46441d6502ac4bf9a6e8aa14f7c747f1
CC(C)(C)OC(=N)C(Cl)(Cl)Cl.O=C1C=CC(O)C1>>CC(C)(C)OC1C=CC(=O)C1
C([O-])(O)=O.[Na+].ClC(C(OC(C)(C)C)=N)(Cl)Cl.B(F)(F)F.CCOCC.OC1C=CC(C1)=O>>C(C)(C)(C)OC1C=CC(C1)=O
N=C(O[C:2]([CH3:1])([CH3:3])[CH3:4])C(Cl)(Cl)Cl.[OH:5][CH:6]1[CH:7]=[CH:8][C:9](=[O:10])[CH2:11]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][CH:6]1[CH:7]=[CH:8][C:9](=[O:10])[CH2:11]1
CC(C)(C)OC(=N)C(Cl)(Cl)Cl.O=C1C=CC(O)C1
CC(C)(C)OC1C=CC(=O)C1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
e1602c7639e9590c57e1f519302834b854314fa06b50f2e00792e7923548c28a
9939e71487b269001d097fe9b7393354dcb141bf54208fca597f111e50af4454
O=C1C=CCC1
Cl-C(-Cl)(-Cl)-C(=N)-O-[C;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4].[O;D1;H0:5]=[C:6]1-[C:7]-[C:8](-[OH;D1;+0:9])-[C:10]=[C:11]-1>>[C;D1;H3:2]-[C;H0;D4;+0:1](-[C;D1;H3:3])(-[C;D1;H3:4])-[O;H0;D2;+0:9]-[C:8]1-[C:7]-[C:6](=[O;D1;H0:5])-[C:11]=[C:10]-1
40
[{"value": 40.0, "product": "C(C)(C)(C)OC1C=CC(C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 19.7, "product": "C(C)(C)(C)OC1C=CC(C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
6.5
CELSIUS
2
HOUR
A solution of 4-hydroxy-2-cyclopentenone (1.15 g, 11.7 mmol) in methylene chloride is cooled to 3° C. and treated sequentially with tert-butyl trichloroacetimidate (4.2 mL, 23.7 mmol) and boron trifluoride diethyl etherate (0.15 mL). The reaction mixture is stirred at 3-10° C. for 2 hours and then allowed to warm to ro...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Ether.Secondary alcohol
Ether
null
null
C1=CCCC1
HCl
C(Cl)Cl
6.5
2
CC(C)(C)OC(=N)C(Cl)(Cl)Cl.O=C1C=CC(O)C1>C(Cl)Cl>CC(C)(C)OC1C=CC(=O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e0e346db372f42efa4e13b85899186f1
CC(C)(C)OC1C=CC(=O)C1>>CC(C)(C)O[C@H]1C=C[C@@H](O)C1
[OH-].[Na+].[H-].[Al+3].[Li+].[H-].[H-].[H-].[I-].[Li+].C(C)(C)(C)OC1C=CC(C1)=O>>C(C)(C)(C)O[C@H]1C=C[C@H](C1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][CH:6]1[CH:7]=[CH:8][C:9](=[O:10])[CH2:11]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C@H:6]1[CH:7]=[CH:8][C@@H:9]([OH:10])[CH2:11]1
CC(C)(C)OC1C=CC(=O)C1
CC(C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
C1(=CC=CC=C1)C.COC(C)(C)C
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1>>[OH;D1;+0:1]-[C@H;D3;+0:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1
42
[{"value": 42.0, "product": "C(C)(C)(C)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 42.0, "product": "C(C)(C)(C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A slurry of lithium aluminum hydride (55 mg, 1.44 mmol), lithium iodide (1.65 g, 5.76 mmol), tert-butyl methyl ether (2 mL) and toluene (3 mL) is cooled to -15° C. The slurry is treated dropwise with 4-tert-butoxy-cyclopent-2-enone(430 mg, 2.79 mmol, dissolved in 1 mL of toluene) over 5 minutes. The reaction mixture is...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1
null
C1(=CC=CC=C1)C.COC(C)(C)C
null
2
CC(C)(C)OC1C=CC(=O)C1>C1(=CC=CC=C1)C.COC(C)(C)C>CC(C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4080122b276c4fa69f2e3e82eeb5a920
C=COC(C)=O.CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>>CC(=O)OC1C=CC(O[Si](C)(C)C(C)(C)C)C1
C(Cl)(Cl)Cl.[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O.C(Cl)(Cl)Cl.C(C)N(CC)CC.C(C)(=O)OC=C.[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O>>[Si](C)(C)(C(C)(C)C)OC1C=CC(C1)OC(C)=O
[CH3:1][C:2](=[O:3])[O:4][CH:5]=[CH2:6].O[C@@H]1C=[CH:7][C@H:8]([O:9][Si:10]([CH3:11])([CH3:12])[C:13]([CH3:14])([CH3:15])[CH3:16])[CH2:17]1>>[CH3:1][C:2](=[O:3])[O:4][CH:5]1[CH:6]=[CH:7][CH:8]([O:9][Si:10]([CH3:11])([CH3:12])[C:13]([CH3:14])([CH3:15])[CH3:16])[CH2:17]1
C=COC(C)=O.CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
CC(=O)OC1C=CC(O[Si](C)(C)C(C)(C)C)C1
null
null
COC(C)(C)C
C-C Coupling
Transesterification
92af04861d06eaca931c3f45788ceb88c1b9d7e6fcee8f51a3677fb2464fa656
09fd45f837e2e59063089c7c3532ccf9271bc2124817e628316fb7f09c7d1378
C1=CCCC1
null
51.1
[{"value": 51.0, "product": "[Si](C)(C)(C(C)(C)C)OC1C=CC(C1)OC(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 51.1, "product": "[Si](C)(C)(C(C)(C)C)OC1C=CC(C1)OC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
Cis-4-tert-butyldimethylsilyloxy-2-cyclopentenol (10.0 g, 46.6 mmol, prepared in example 3a) is dissolved in tert-butyl methyl ether (60 mL, anhydrous). To the solution is added triethylamine (4.5 mL, 32.3 mmol), pancreatin (30 g, available from Sigma Chemical Company), and vinyl acetate (22 mL, 239 mmol). The reaction...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol.Vinyl
Ester
C1=CCCC1
C1=CCCC1
C1=CCCC1
HO-
COC(C)(C)C
null
7
C=COC(C)=O.CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>COC(C)(C)C>CC(=O)OC1C=CC(O[Si](C)(C)C(C)(C)C)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-23a5242235f843fa9d331c47debf3305
C=COC(C)=O.O[C@@H]1C=C[C@H](OC2CCCCO2)C1>>CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
C(Cl)(Cl)Cl.O1C(CCCC1)O[C@H]1C=C[C@H](C1)O.C(Cl)(Cl)Cl.C(C)N(CC)CC.C(C)(=O)OC=C.O1C(CCCC1)O[C@H]1C=C[C@H](C1)O>>O1C(CCCC1)O[C@H]1C=C[C@H](C1)OC(C)=O
C=CO[C:2]([CH3:1])=[O:3].[OH:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][CH:10]2[CH2:11][CH2:12][CH2:13][CH2:14][O:15]2)[CH2:16]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][CH:10]2[CH2:11][CH2:12][CH2:13][CH2:14][O:15]2)[CH2:16]1
C=COC(C)=O.O[C@@H]1C=C[C@H](OC2CCCCO2)C1
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
null
null
COC(C)(C)C
Acylation
Transesterification
892ec5198c524815f90afb1f95f6ea3087d4dce6703007366f357ec486f2b695
67dea10bb93a5d805949b0584770f4ae4a5967d92b967e6003c59314fe37aee1
C1=C[C@H](OC2CCCCO2)CC1
C=C-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[OH;D1;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1
45
[{"value": 45.0, "product": "O1C(CCCC1)O[C@H]1C=C[C@H](C1)OC(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 44.9, "product": "O1C(CCCC1)O[C@H]1C=C[C@H](C1)OC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
Cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enol (1.091 g, 5.92 mmol, prepared in example 6) is dissolved in tert-butyl methyl ether (8.6 mL, anhydrous). To the solution is added triethylamine (0.59 mL, 4.2 mmol), pancreatin (3.2 g, available from Sigma Chemical Company), and vinyl acetate (2.7 mL, 29 mmol). The react...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol.Vinyl
Ester
null
null
C1=CCCC1.C1CCOCC1
HO-
COC(C)(C)C
null
7
C=COC(C)=O.O[C@@H]1C=C[C@H](OC2CCCCO2)C1>COC(C)(C)C>CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b7d46a26dfbe492a852ae078a89b028a
CC(=O)OC1C=CC(O[Si](C)(C)C(C)(C)C)C1>>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
[Si](C)(C)(C(C)(C)C)OC1C=CC(C1)OC(C)=O.O.[OH-].[Li+].O>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O
CC(=O)[O:13][CH:12]1[CH:11]=[CH:10][CH:9]([O:8][Si:5]([C:2]([CH3:1])([CH3:3])[CH3:4])([CH3:6])[CH3:7])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1
CC(=O)OC1C=CC(O[Si](C)(C)C(C)(C)C)C1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
C1CCOC1.CO.O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
C1=CCCC1
C-C(=O)-[O;H0;D2;+0:1]-[CH;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1>>[OH;D1;+0:1]-[C@@H;D3;+0:2]1-[C:3]=[C:4]-[C:5]-[C:6]-1
92
[{"value": 92.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 91.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
Dissolve (-)-acetic acid 4-tert-butyldimethylsilyloxy-cyclopent-2-enyl ester (2.3 mmol, prepared in example 10) in THF/methanol/water (2.7/0.9/0.9 mL). Add lithium hydroxide monohydrate (2.5 mmol) with stirring. After stirring for about 3 hours at room temperature, dilute the reaction with water (10 mL) and extract wit...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
C1=CCCC1
HO-
C1CCOC1.CO.O
null
3
CC(=O)OC1C=CC(O[Si](C)(C)C(C)(C)C)C1>C1CCOC1.CO.O>CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-73c1b39d43c34bba9c7f0a1fb0614d7e
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1>>O[C@@H]1C=C[C@H](OC2CCCCO2)C1
O.[OH-].[Li+].O1C(CCCC1)O[C@H]1C=C[C@H](C1)OC(C)=O.COC(C)(C)C.O>>O1C(CCCC1)O[C@H]1C=C[C@H](C1)O
CC(=O)[O:1][C@@H:2]1[CH:3]=[CH:4][C@H:5]([O:6][CH:7]2[CH2:8][CH2:9][CH2:10][CH2:11][O:12]2)[CH2:13]1>>[OH:1][C@@H:2]1[CH:3]=[CH:4][C@H:5]([O:6][CH:7]2[CH2:8][CH2:9][CH2:10][CH2:11][O:12]2)[CH2:13]1
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
O[C@@H]1C=C[C@H](OC2CCCCO2)C1
null
null
C(Cl)(Cl)Cl.C1CCOC1.CO.O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
C1=C[C@H](OC2CCCCO2)CC1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1>>[OH;D1;+0:1]-[C:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1
93
[{"value": 93.0, "product": "O1C(CCCC1)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.4, "product": "O1C(CCCC1)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
Dissolve (-)-acetic acid cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enyl ester (106 mg, 0.47 mmol, prepared in example 11) in THF/methanol/water (1.5/0.5/0.5 mL). Add lithium hydroxide monohydrate (0.57 mmol) with stirring. After stirring for about 3 hours at room temperature, dilute the reaction with tert-butyl meth...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
C1=CCCC1.C1CCOCC1
HO-
C(Cl)(Cl)Cl.C1CCOC1.CO.O
null
3
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1>C(Cl)(Cl)Cl.C1CCOC1.CO.O>O[C@@H]1C=C[C@H](OC2CCCCO2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1ac771ea14f8470d9583f912bd68a7b3
C=COC(C)=O.CC(C)(C)O[C@H]1C=C[C@@H](O)C1>>CC(=O)O[C@@H]1C=C[C@H](OC(C)(C)C)C1
C(C)N(CC)CC.C(C)(=O)OC=C.C(Cl)(Cl)Cl.C(C)(C)(C)O[C@H]1C=C[C@H](C1)O>>C(C)(C)(C)O[C@H]1C=C[C@H](C1)OC(C)=O
C=CO[C:2]([CH3:1])=[O:3].[OH:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][C:10]([CH3:11])([CH3:12])[CH3:13])[CH2:14]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][C:10]([CH3:11])([CH3:12])[CH3:13])[CH2:14]1
C=COC(C)=O.CC(C)(C)O[C@H]1C=C[C@@H](O)C1
CC(=O)O[C@@H]1C=C[C@H](OC(C)(C)C)C1
null
null
COC(C)(C)C
Acylation
Transesterification
892ec5198c524815f90afb1f95f6ea3087d4dce6703007366f357ec486f2b695
67dea10bb93a5d805949b0584770f4ae4a5967d92b967e6003c59314fe37aee1
C1=CCCC1
C=C-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[OH;D1;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1
50
[{"value": 50.0, "product": "C(C)(C)(C)O[C@H]1C=C[C@H](C1)OC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
17
HOUR
Cis-4-tert-butyloxy-cyclopent-2-enol (485 mg, 3.1 mmol, prepared in example 9) is dissolved in tert-butyl methyl ether (8.6 mL, anhydrous). To the solution is added triethylamine (0.7 eq), pancreatin (3 wt eq, available from Sigma Chemical Company), and vinyl acetate (5 eq). The reaction is allowed to stir for 17 hours...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol.Vinyl
Ester
null
null
C1=CCCC1
HO-
COC(C)(C)C
null
17
C=COC(C)=O.CC(C)(C)O[C@H]1C=C[C@@H](O)C1>COC(C)(C)C>CC(=O)O[C@@H]1C=C[C@H](OC(C)(C)C)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-722e940fd7a54e458d6fcaedb1602d00
CC(=O)O[C@@H]1C=C[C@H](OC(C)(C)C)C1>>CC(C)(C)O[C@H]1C=C[C@@H](O)C1
O.[OH-].[Li+].C(Cl)(Cl)Cl.C(C)(C)(C)O[C@H]1C=C[C@H](C1)OC(C)=O.O>>C(C)(C)(C)O[C@H]1C=C[C@H](C1)O
CC(=O)[O:10][C@@H:9]1[CH:8]=[CH:7][C@H:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])[CH2:11]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C@H:6]1[CH:7]=[CH:8][C@@H:9]([OH:10])[CH2:11]1
CC(=O)O[C@@H]1C=C[C@H](OC(C)(C)C)C1
CC(C)(C)O[C@H]1C=C[C@@H](O)C1
null
null
C1CCOC1.CO.O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
C1=CCCC1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1>>[OH;D1;+0:1]-[C:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1
101
[{"value": 101.0, "product": "C(C)(C)(C)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
Dissolve (-)-acetic acid cis-4-tert-butyloxy-cyclopent-2-enyl ester (90 mg, 0.45 mmol, prepared in example 14) in THF/methanol/water (1.5/0.5/0.5 mL). Add lithium hydroxide monohydrate (23.7 mg) with stirring. After stirring for about 2 hours at room temperature, dilute the reaction with water (10 mL) and extract with ...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
C1=CCCC1
HO-
C1CCOC1.CO.O
null
2
CC(=O)O[C@@H]1C=C[C@H](OC(C)(C)C)C1>C1CCOC1.CO.O>CC(C)(C)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-443e36063c0a47edae71957a9c2af350
C=COC(C)=O.CCN(CC)CC.O[C@@H]1C=C[C@H](OCc2ccccc2)C1>>CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1.O[C@@H]1C=C[C@H](OCc2ccccc2)C1
C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O.C(C)N(CC)CC.C(C)(=O)OC=C.C(Cl)(Cl)Cl.C(Cl)(Cl)Cl>>C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O.C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)OC(C)=O
[CH3:1][C:2](=[O:3])[O:18][CH:19]=[CH2:20].N([CH2:29][CH3:28])([CH2:30][CH3:25])[CH2:31][CH3:24].[C@@H:5]1([OH:23])[CH:6]=[CH:7][C@H:8]([O:9][CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[CH2:17]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][CH2:10][c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[CH2...
C=COC(C)=O.CCN(CC)CC.O[C@@H]1C=C[C@H](OCc2ccccc2)C1
CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1.O[C@@H]1C=C[C@H](OCc2ccccc2)C1
null
null
COC(C)(C)C
Aromatic Heterocycle Formation
OtherReaction
8803c3c25f969d3fead08ac604515af42718a94f1cbf68fec7e7b35748f12230
7dd832249f1f72966346dc7ec4ca1592cb736718d1c1e34c640377989877afdc
C1=C[C@H](OCc2ccccc2)CC1.C1=C[C@H](OCc2ccccc2)CC1
[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[CH;D2;+0:5]=[CH2;D1;+0:6].[CH3;D1;+0:7]-[CH2;D2;+0:8]-N(-[CH2;D2;+0:9]-[CH3;D1;+0:10])-[CH2;D2;+0:11]-[CH3;D1;+0:12].[OH;D1;+0:13]-[C@H;D3;+0:14]1-[C:15]-[C:16]-[C:17]=[C:18]-1>>[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[#8:19]-[C@H;D3;+0:14]1-[C:15]-[C:16]-[C:17]...
70
[{"value": 29.0, "product": "C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.0, "product": "C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)OC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
Cis-4-benzyloxy-cyclopent-2-enol (500 mg, prepared in example 16) is dissolved in tert-butyl methyl ether (8.6 mL, anhydrous). To the solution is added triethylamine (0.7 eq), pancreatin (3 wt eq, available from Sigma Chemical Company), and vinyl acetate (5 eq). The reaction is allowed to stir for 7 hours at room tempe...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol.Tertiary amine.Vinyl
Ester.Ether.Secondary alcohol
C1=CCCC1
C1=CCCC1.C1=CCCC1.c1ccccc1
C1=CCCC1.c1ccccc1.C1=CCCC1.c1ccccc1
null
COC(C)(C)C
null
7
C=COC(C)=O.CCN(CC)CC.O[C@@H]1C=C[C@H](OCc2ccccc2)C1>COC(C)(C)C>CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1.O[C@@H]1C=C[C@H](OCc2ccccc2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-91b9cd4f6514451c9af570b41fa98ef5
CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1>>O[C@@H]1C=C[C@H](OCc2ccccc2)C1
O.[OH-].[Li+].C(Cl)(Cl)Cl.C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)OC(C)=O.O>>C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O
CC(=O)[O:1][C@@H:2]1[CH:3]=[CH:4][C@H:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[CH2:14]1>>[OH:1][C@@H:2]1[CH:3]=[CH:4][C@H:5]([O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[CH2:14]1
CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1
O[C@@H]1C=C[C@H](OCc2ccccc2)C1
null
null
C1CCOC1.CO.O
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
C1=C[C@H](OCc2ccccc2)CC1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1>>[OH;D1;+0:1]-[C:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1
92.8
[{"value": 92.0, "product": "C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.8, "product": "C(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
Dissolve (-)-acetic acid cis-4-benzyloxy-cyclopent-2-enyl ester (158 mg, 0.68 mmol, prepared in example 17) in THF/methanol/water (1.5/0.5/0.5 mL). Add lithium hydroxide monohydrate (0.75 mmol) with stirring. After stirring for about 2 hours at room temperature, dilute the reaction with water (10 mL) and extract with t...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
C1=CCCC1.c1ccccc1
HO-
C1CCOC1.CO.O
null
2
CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1>C1CCOC1.CO.O>O[C@@H]1C=C[C@H](OCc2ccccc2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cd21d400e0ca42969b8c9e946aa2ff9e
CC(=O)OC(C)=O.CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>>CC(=O)O[C@@H]1C=C[C@H](O[Si](C)(C)C(C)(C)C)C1
C(C)(=O)OC(C)=O.C(C)(=O)OCC.CCCCCC.[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O.C(C)OCC>>[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)OC(C)=O
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][Si:10]([CH3:11])([CH3:12])[C:13]([CH3:14])([CH3:15])[CH3:16])[CH2:17]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][Si:10]([CH3:11])([CH3:12])[C:13]([CH3:14])([CH3:15])[CH3:16])[CH2:17]1
CC(=O)OC(C)=O.CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
CC(=O)O[C@@H]1C=C[C@H](O[Si](C)(C)C(C)(C)C)C1
null
null
N1=CC=CC=C1
Acylation
Transesterification
a7ad17dd333d7246e42d4632a0a7042db0b0d3b7f2adb7cdb2c46498a22ac4db
c98fee24664998fb42388f3a4804f79d763c5043c4f5565ea3b46913e3a86a6e
C1=CCCC1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[OH;D1;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1
98
[{"value": 98.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)OC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Dissolve (-)-cis-4-tert-butyldimethylsilyloxy-2-cyclopentenol (1 g, 4.67 mmol, prepared in example 10) in pyridine (20 mL) and treat with acetic anhydride (2 mL). Stir the reaction overnight. Dilute the reaction with diethyl ether (100 mL), wash with 3M hydrochloric acid (3×100 mL), saturated sodium bicarbonate (100 mL...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary alcohol
Ester
null
null
C1=CCCC1
HO-
N1=CC=CC=C1
null
null
CC(=O)OC(C)=O.CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>N1=CC=CC=C1>CC(=O)O[C@@H]1C=C[C@H](O[Si](C)(C)C(C)(C)C)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-00533d2621284180b8d6e372c9496cb7
CC(=O)OC(C)=O.O[C@@H]1C=C[C@H](OC2CCCCO2)C1>>CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
C(C)(=O)OCC.C(C)(=O)OC(C)=O.CN(C)C1=NC=CC=C1.O1C(CCCC1)O[C@H]1C=C[C@H](C1)O>>O1C(CCCC1)O[C@H]1C=C[C@H](C1)OC(C)=O
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][CH:10]2[CH2:11][CH2:12][CH2:13][CH2:14][O:15]2)[CH2:16]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[CH:6]=[CH:7][C@H:8]([O:9][CH:10]2[CH2:11][CH2:12][CH2:13][CH2:14][O:15]2)[CH2:16]1
CC(=O)OC(C)=O.O[C@@H]1C=C[C@H](OC2CCCCO2)C1
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
null
null
N1=CC=CC=C1
Acylation
Transesterification
a7ad17dd333d7246e42d4632a0a7042db0b0d3b7f2adb7cdb2c46498a22ac4db
c98fee24664998fb42388f3a4804f79d763c5043c4f5565ea3b46913e3a86a6e
C1=C[C@H](OC2CCCCO2)CC1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[OH;D1;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[C:5]1-[C:6]-[C:7]-[C:8]=[C:9]-1
81
[{"value": 81.0, "product": "O1C(CCCC1)O[C@H]1C=C[C@H](C1)OC(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Dissolve (-)-cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enol (292 mg, 1.59 mmol, prepared in example 11) in pyridine (2.8 mL) and treat with acetic anhydride (0.39 mL) and dimethylaminopyridine (16 mg). Stir the reaction overnight. Concentrate the reaction under vacuum, dissolve the residue with ethyl acetate (10 mL)...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary alcohol
Ester
null
null
C1=CCCC1.C1CCOCC1
HO-
N1=CC=CC=C1
null
null
CC(=O)OC(C)=O.O[C@@H]1C=C[C@H](OC2CCCCO2)C1>N1=CC=CC=C1>CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4b9e268c96f04af98cb23843c3e81f50
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1>>CC(=O)O[C@H]1C=C[C@@H](O)C1
C([O-])(O)=O.C1(=CC=C(C=C1)S(=O)(=O)O)C.O1C(CCCC1)O[C@H]1C=C[C@H](C1)OC(C)=O.C([O-])([O-])=O>>C(C)(=O)O[C@H]1C=C[C@H](C1)O
C1CCC([O:9][C@H:8]2[CH:7]=[CH:6][C@@H:5]([O:4][C:2]([CH3:1])=[O:3])[CH2:10]2)OC1>>[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[CH:6]=[CH:7][C@@H:8]([OH:9])[CH2:10]1
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
CC(=O)O[C@H]1C=C[C@@H](O)C1
null
null
C(Cl)(Cl)Cl.C(C)O
Reduction
OtherReaction
0b83bf1290e2ee90e436d69e159e123816ec005a202c40da90352984400ae7f0
628b56b3f4fed40b9cc8e2f7565bcae98d5e36a3f75394461dabd987fb619482
C1=CCCC1
C1-C-C-C(-[O;H0;D2;+0:1]-[C:2]2-[C:3]-[C:4]-[C:5]=[C:6]-2)-O-C-1>>[OH;D1;+0:1]-[C:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1
75
[{"value": 75.0, "product": "C(C)(=O)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.5, "product": "C(C)(=O)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Dissolve (-)-acetic acid cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enyl ester (192 mg, 0.85 mmol, prepared in example 11) in ethanol (1.5 mL) and treat with p-toluenesulfonic acid (11.7 mg). Stir the reaction at room temperature for 2 hours. Add carbonate or bicarbonate to neutralize the reaction mixture and concent...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Secondary alcohol
C1CCOCC1
null
C1=CCCC1
HO-
C(Cl)(Cl)Cl.C(C)O
null
null
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1>C(Cl)(Cl)Cl.C(C)O>CC(=O)O[C@H]1C=C[C@@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f043af33bf7d4a64ba8d85518371337b
CC(=O)O[C@H]1C=C[C@@H](O)C1>>CC(=O)O[C@@H]1CC[C@H](O)C1
C(C)(=O)O[C@H]1C=C[C@H](C1)O.C(C)N(CC)CC>>C(C)(=O)O[C@H]1C[C@H](CC1)O
[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[CH:6]=[CH:7][C@@H:8]([OH:9])[CH2:10]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[CH2:6][CH2:7][C@H:8]([OH:9])[CH2:10]1
CC(=O)O[C@H]1C=C[C@@H](O)C1
CC(=O)O[C@@H]1CC[C@H](O)C1
null
[Ni]
C(C)O
Reduction
Hydrogenation (double to single)
fd2b5380b956a588192941128a1966dad6a191947eb2dd12a24d8008fa2ed0c2
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
C1CCCC1
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5]1-[C:6]-[C:7](-[O;D1;H1:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-1>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5]1-[C:6]-[C:7](-[O;D1;H1:8])-[CH2;D2;+0:9]-[CH2;D2;+0:10]-1
87.3
[{"value": 87.0, "product": "C(C)(=O)O[C@H]1C[C@H](CC1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.3, "product": "C(C)(=O)O[C@H]1C[C@H](CC1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
Dissolve (-)-cis-4-acetoxy-cyclopent-2-enol (11.0 g, 77.4 mmol, prepared in example 19) in ethanol (50 mL) and treat with Raney nickel (1.1 g, previously washed with water (2×50 mL) and ethanol (2×50 mL), Ra--Ni). Charge the atmosphere with hydrogen at 50 psi (344.74 kPa) and shake the mixture. After 20 minutes, filter...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=CCCC1
C1CCCC1
C1CCCC1
null
[Ni].C(C)O
null
0.333333
CC(=O)O[C@H]1C=C[C@@H](O)C1>[Ni].C(C)O>CC(=O)O[C@@H]1CC[C@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8055ba3e80dd4839935a05e583536aad
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>>CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1
[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O.[BH4-].[Na+]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@@H:9]1[CH2:10][CH2:11][C@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1
null
[Ni]
C(C)O
Reduction
Hydrogenation (double to single)
fd2b5380b956a588192941128a1966dad6a191947eb2dd12a24d8008fa2ed0c2
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
C1CCCC1
[#8:1]-[C:2]1-[C:3]-[C:4](-[O;D1;H1:5])-[CH;D2;+0:6]=[CH;D2;+0:7]-1>>[#8:1]-[C:2]1-[C:3]-[C:4](-[O;D1;H1:5])-[CH2;D2;+0:6]-[CH2;D2;+0:7]-1
87.3
[{"value": 87.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.3, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
5.25
HOUR
Dissolve (-)-cis-4-tert-butyldimethylsilyloxy-2-cyclopentenol (28.85 g, 135 mmol, prepared in example 10) in ethanol (75 mL) and treated with Raney nickel (1.85 g, 32 mmol, previously washed with water (2×50 mL) and ethanol (2×50 mL)). Charge the atmosphere with hydrogen at 50 psi (344.74 kPa) and shake the mixture. Af...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=CCCC1
C1CCCC1
C1CCCC1
null
[Ni].C(C)O
0
5.25
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>[Ni].C(C)O>CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-61afa5168bfe4df280f2c9386fbd28fe
CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1.CS(=O)(=O)Cl>>CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](OS(C)(=O)=O)C1
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O.CS(=O)(=O)Cl.C(C)N(CC)CC>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)OS(=O)(=O)C
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@@H:9]1[CH2:10][CH2:11][C@H:12]([OH:13])[CH2:18]1.Cl[S:14]([CH3:15])(=[O:16])=[O:17]>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@@H:9]1[CH2:10][CH2:11][C@H:12]([O:13][S:14]([CH3:15])(=[O:16])=[O:17])[CH2:18]1
CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1.CS(=O)(=O)Cl
CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](OS(C)(=O)=O)C1
null
null
COC(C)(C)C
Acylation
Formation of Sulfonic Esters
641955d0081c80f158ce2aacd31873a3f3301c87ca0800cf263e288ba8390217
4f9373df8a11470603daf885a5777cebf95940370e32739263d35df0f171a0dd
C1CCCC1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[C:5]-[C:6](-[OH;D1;+0:7])-[C:8]>>[C:5]-[C:6](-[O;H0;D2;+0:7]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4])-[C:8]
97
[{"value": 97.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)OS(=O)(=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.7, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)OS(=O)(=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-5
CELSIUS
2
HOUR
Dissolve (-)-cis-3-tert-butyldimethylsilyloxy-cyclopentanol (9.20 g, 42.5 mmol) in anhydrous tert-butyl methyl ether (50 mL) and cool to -5° C. Treat the solution with methanesulfonyl chloride (3.6 g, 46.5 mmol, mesyl chloride), followed by triethylamine (7.2 mL, 51.7 mmol), at such a rate as to keep the temperature be...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Sulfonyl halide
Mesylate
null
null
C1CCCC1
HCl
COC(C)(C)C
-5
2
CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1.CS(=O)(=O)Cl>COC(C)(C)C>CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](OS(C)(=O)=O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dc292523a26943b1a8ab4fada76c991b
ClC(c1ccccc1)(c1ccccc1)c1ccccc1.O=C1C=CC(O)C1>>O=C1C=CC(OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)Cl.N12CCCCCC2=NCCC1.OC1C=CC(C1)=O>>C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)OC1C=CC(C1)=O
Cl[C:7]([c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)([c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1.[O:1]=[C:2]1[CH:3]=[CH:4][CH:5]([OH:6])[CH2:26]1>>[O:1]=[C:2]1[CH:3]=[CH:4][CH:5]([O:6][C:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[...
ClC(c1ccccc1)(c1ccccc1)c1ccccc1.O=C1C=CC(O)C1
O=C1C=CC(OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
5ab68839e2c0c36dcda93f3c0a707140e3d24e3e006f5c14702a7b8884a9a81e
26c50c761bd192b9bbaacc80ceb1f72503dc7c2f688b52834534ac0a03b55cce
O=C1C=CC(OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
Cl-[C;H0;D4;+0:1](-[c:2](:[c:3]):[c:4])(-[c:5](:[c:6]):[c:7])-[c:8](:[c:9]):[c:10].[O;D1;H0:11]=[C:12]1-[C:13]-[C:14](-[OH;D1;+0:15])-[C:16]=[C:17]-1>>[O;D1;H0:11]=[C:12]1-[C:13]-[C:14](-[O;H0;D2;+0:15]-[C;H0;D4;+0:1](-[c:2](:[c:3]):[c:4])(-[c:5](:[c:6]):[c:7])-[c:8](:[c:9]):[c:10])-[C:16]=[C:17]-1
37
[{"value": 36.0, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)OC1C=CC(C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 37.0, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)OC1C=CC(C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
DAY
A solution of trityl chloride (3.44 g, 12.3 mmol) in methylene chloride (20 mL) is treated sequentially with 1,8-diazabicyclo[5.4.0]undec-7-ene (2.2 mL, 14.7 mmol, DBU) and 4-hydroxy-2-cyclopentenone (1.01 g, 10.0 mmol, in 5 mL of methylene chloride, prepared in example 1). The reaction is stirred for 3 days at room te...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Secondary alcohol
Ether
null
null
C1=CCCC1.c1ccccc1.c1ccccc1.c1ccccc1
HCl
C(Cl)Cl
null
72
ClC(c1ccccc1)(c1ccccc1)c1ccccc1.O=C1C=CC(O)C1>C(Cl)Cl>O=C1C=CC(OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-802e8dff62b74fa49096ebf9f90abcb7
O=C1C=CC(OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1>>O[C@@H]1C=C[C@H](OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)OC1C=CC(C1)=O.[H-].[Al+3].[Li+].[H-].[H-].[H-].[I-].[Li+].COC(C)(C)C>>C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O
[O:1]=[C:2]1[CH:3]=[CH:4][CH:5]([O:6][C:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[c:20]2[cH:21][cH:22][cH:23][cH:24][cH:25]2)[CH2:26]1>>[OH:1][C@@H:2]1[CH:3]=[CH:4][C@H:5]([O:6][C:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[...
O=C1C=CC(OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
O[C@@H]1C=C[C@H](OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
null
null
C1(=CC=CC=C1)C
Reduction
Reduction of ketone to secondary alcohol
cdb715078de81de44f7378b33188a9fd6e2a8cc99d338ab2c91bd5935d725bcf
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=C[C@H](OC(c2ccccc2)(c2ccccc2)c2ccccc2)CC1
[O;H0;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1>>[OH;D1;+0:1]-[C@H;D3;+0:2]1-[C:3]-[C:4]-[C:5]=[C:6]-1
95
[{"value": 95.0, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.5, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)O[C@H]1C=C[C@H](C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-20
CELSIUS
1
HOUR
A slurry of 4-trityloxy-2-cyclopentenone (1.03 g, 3.03 mmol, prepared in example 27) in toluene (8 mL) is cooled to -20° C. and treated sequentially with lithium aluminum hydride (76 mg, 2.0 mL), lithium iodide (1.06 g, 7.9 mmol) and dropwise with tert-butyl methyl ether (2 mL, over 5 minutes). The reaction is stirred ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCC1
C1=CCCC1
C1=CCCC1.c1ccccc1.c1ccccc1.c1ccccc1
null
C1(=CC=CC=C1)C
-20
1
O=C1C=CC(OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1>C1(=CC=CC=C1)C>O[C@@H]1C=C[C@H](OC(c2ccccc2)(c2ccccc2)c2ccccc2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3b90e77842a74c70b595bd258a689f2e
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>>CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1
[Si](C)(C)(C(C)(C)C)O[C@H]1C=C[C@H](C1)O.[H][H]>>[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O
[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@H:9]1[CH:10]=[CH:11][C@@H:12]([OH:13])[CH2:14]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[Si:5]([CH3:6])([CH3:7])[O:8][C@@H:9]1[CH2:10][CH2:11][C@H:12]([OH:13])[CH2:14]1
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1
CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1
null
null
CO
Reduction
Hydrogenation (double to single)
fd2b5380b956a588192941128a1966dad6a191947eb2dd12a24d8008fa2ed0c2
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
C1CCCC1
[#8:1]-[C:2]1-[C:3]-[C:4](-[O;D1;H1:5])-[CH;D2;+0:6]=[CH;D2;+0:7]-1>>[#8:1]-[C:2]1-[C:3]-[C:4](-[O;D1;H1:5])-[CH2;D2;+0:6]-[CH2;D2;+0:7]-1
92
[{"value": 92.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.0, "product": "[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18.5
HOUR
Combine (+/-)-cis-4-tert-butyldimethylsilyloxy-2-cyclopentenol (2.50 g, 11.6 mmol, prepared in example 3) and Ni2B (8.5 mL of a 0.14M slurry in methanol, 10 mol %) in methanol (14 mL). Stir the slurry under an atmosphere of hydrogen for 18.5 hours. Then replace the hydrogen atmosphere with nitrogen, filter through diat...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=CCCC1
C1CCCC1
C1CCCC1
null
CO
null
18.5
CC(C)(C)[Si](C)(C)O[C@H]1C=C[C@@H](O)C1>CO>CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b1dad0bf641048d099cfa0228402d3a6
C=COC(C)=O.CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1>>CC(=O)O[C@@H]1CC[C@H](O[Si](C)(C)C(C)(C)C)C1
[Si](C)(C)(C(C)(C)C)O[C@H]1C[C@H](CC1)O.C(C)N(CC)CC.C(C)(=O)OC=C>>C(C)(=O)O[C@H]1C[C@H](CC1)O[Si](C)(C)C(C)(C)C
C=CO[C:2]([CH3:1])=[O:3].[OH:4][C@H:5]1[CH2:6][CH2:7][C@@H:8]([O:9][Si:10]([CH3:11])([CH3:12])[C:13]([CH3:14])([CH3:15])[CH3:16])[CH2:17]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[CH2:6][CH2:7][C@H:8]([O:9][Si:10]([CH3:11])([CH3:12])[C:13]([CH3:14])([CH3:15])[CH3:16])[CH2:17]1
C=COC(C)=O.CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1
CC(=O)O[C@@H]1CC[C@H](O[Si](C)(C)C(C)(C)C)C1
null
null
COC(C)(C)C
Acylation
Transesterification
892ec5198c524815f90afb1f95f6ea3087d4dce6703007366f357ec486f2b695
67dea10bb93a5d805949b0584770f4ae4a5967d92b967e6003c59314fe37aee1
C1CCCC1
C=C-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5](-[OH;D1;+0:6])-[C:7]>>[C:4]-[C:5](-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3])-[C:7]
49
[{"value": 49.0, "product": "C(C)(=O)O[C@H]1C[C@H](CC1)O[Si](C)(C)C(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Combine (+/-)-cis-3-tert-butyldimethylsilyloxycyclopentanol (2.119 g, 9.8 mmol, prepared in example 29), pancreatin (6.2 g, 3 weight equivalents), triethylamine (0.9 mL, 6.5 mmol) and vinyl acetate (4.3 mL) in tert-butyl methyl ether (12 mL) and stir for 27 hours at room temperature. Then filter the reaction through di...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary alcohol.Vinyl
Ester
null
null
C1CCCC1
HO-
COC(C)(C)C
null
null
C=COC(C)=O.CC(C)(C)[Si](C)(C)O[C@@H]1CC[C@H](O)C1>COC(C)(C)C>CC(=O)O[C@@H]1CC[C@H](O[Si](C)(C)C(C)(C)C)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d03242f3367b42868367bf19135dae30
COc1cc(C=O)cc(Br)c1O>>COc1cc(C=O)cc(C#N)c1O
C(C)(=O)OCC.BrC=1C=C(C=O)C=C(C1O)OC.CC(=O)N(C)C>>C(=O)C=1C=C(C#N)C(=C(C1)OC)O
Br[c:9]1[cH:8][c:5]([CH:6]=[O:7])[cH:4][c:3]([O:2][CH3:1])[c:12]1[OH:13]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]=[O:7])[cH:8][c:9]([C:10]#[N:11])[c:12]1[OH:13]
COc1cc(C=O)cc(Br)c1O
COc1cc(C=O)cc(C#N)c1O
null
null
CO
Miscellaneous
OtherReaction
3ae4da8b7f110de99cf8afc091b6f0c8540050148e425770f8030bce1480042c
73a96fe5e833259ca394a42f82d6cc2ee7231bcde92d95030d2893b90c3fef76
c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]-[C:4]=[O;D1;H0:5]):[c:6](-[O;D1;H1:7]):[c:8]>>[N;D1;H0:9]#[C:10]-[c;H0;D3;+0:1](:[c:2]:[c:3]-[C:4]=[O;D1;H0:5]):[c:6](-[O;D1;H1:7]):[c:8]
null
[]
null
null
null
null
A mixture of 23.1 g of 3-bromo-4-hydroxy-5-methoxy benzaldehyde, 9.3 g of cuprous cyanide and 140 ml of dimethyl acetamide (DMA) was refluxed for 2 hours with stirring. After cooling, the mixture was poured over ice and extract&d with an ethyl acetate--methanol mixture (90-10). The organic phase was washed and dried an...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Nitrile
c1ccccc1
c1ccccc1
c1ccccc1
Br-
CO
null
null
COc1cc(C=O)cc(Br)c1O>CO>COc1cc(C=O)cc(C#N)c1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8ff9fcd9cfe74e8dbd93a16959bf292e
COc1cc(C=O)cc(C#N)c1O>>N#Cc1cc(C=O)cc(O)c1O
C(=O)C=1C=C(C#N)C(=C(C1)OC)O.B(Br)(Br)Br>>C(=O)C=1C=C(C#N)C(=C(C1)O)O
C[O:10][c:9]1[cH:8][c:5]([CH:6]=[O:7])[cH:4][c:3]([C:2]#[N:1])[c:11]1[OH:12]>>[N:1]#[C:2][c:3]1[cH:4][c:5]([CH:6]=[O:7])[cH:8][c:9]([OH:10])[c:11]1[OH:12]
COc1cc(C=O)cc(C#N)c1O
N#Cc1cc(C=O)cc(O)c1O
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
72.4
[{"value": 72.4, "product": "C(=O)C=1C=C(C#N)C(=C(C1)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
18 g of the product of Step A and 400 ml of dichloromethane were mixed together under nitrogen and the mixture was cooled to 0° C. 150 ml of a molar solution of boron tribromide in dichloromethane were added and the mixture stood for one night at ambient temperature. It was concentrated, cooled again to 0° C. and 250 m...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1
Other
ClCCl
0
null
COc1cc(C=O)cc(C#N)c1O>ClCCl>N#Cc1cc(C=O)cc(O)c1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-49d72313e0d6412c95d675c45339c241
COc1cc(C=O)cc(Cl)c1O>>O=Cc1cc(O)c(O)c(Cl)c1
ClC=1C(=C(C=C(C=O)C1)OC)O.B(Br)(Br)Br>>ClC=1C=C(C=O)C=C(C1O)O
C[O:6][c:5]1[cH:4][c:3]([CH:2]=[O:1])[cH:11][c:9]([Cl:10])[c:7]1[OH:8]>>[O:1]=[CH:2][c:3]1[cH:4][c:5]([OH:6])[c:7]([OH:8])[c:9]([Cl:10])[cH:11]1
COc1cc(C=O)cc(Cl)c1O
O=Cc1cc(O)c(O)c(Cl)c1
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
77.3
[{"value": 77.3, "product": "ClC=1C=C(C=O)C=C(C1O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
37.2 g of commercial 5-chloro vanillin and 800 ml of dichloromethane were mixed together under nitrogen and cooled to 0° C. 300 ml of a molar solution of boron tribromide in dichloromethane are added and the mixture stood for one night at ambient temperature. It was concentrated, cooled again to 0° C. and acidified. Th...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1
Other
ClCCl
0
null
COc1cc(C=O)cc(Cl)c1O>ClCCl>O=Cc1cc(O)c(O)c(Cl)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9efe6333e98c4733b21ed3413c8658d8
COc1cc(C=O)cc([N+](=O)[O-])c1O>>O=Cc1cc(O)c(O)c([N+](=O)[O-])c1
[N+](=O)([O-])C=1C(=C(C=C(C=O)C1)OC)O.B(Br)(Br)Br>>[N+](=O)([O-])C=1C=C(C=O)C=C(C1O)O
C[O:6][c:5]1[cH:4][c:3]([CH:2]=[O:1])[cH:13][c:9]([N+:10](=[O:11])[O-:12])[c:7]1[OH:8]>>[O:1]=[CH:2][c:3]1[cH:4][c:5]([OH:6])[c:7]([OH:8])[c:9]([N+:10](=[O:11])[O-:12])[cH:13]1
COc1cc(C=O)cc([N+](=O)[O-])c1O
O=Cc1cc(O)c(O)c([N+](=O)[O-])c1
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
55.4
[{"value": 55.4, "product": "[N+](=O)([O-])C=1C=C(C=O)C=C(C1O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
2
DAY
35 g of 5-nitro vanillin (commercial) and 1200 ml of dichloromethane were mixed together under nitrogen and the mixture was cooled to 0° C. 533 ml of a molar solution of boron tribromide in dichloromethane were added and the mixture stood for 2 days at abmient temperature and then was concentrated. The residue was take...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1
Other
ClCCl
0
48
COc1cc(C=O)cc([N+](=O)[O-])c1O>ClCCl>O=Cc1cc(O)c(O)c([N+](=O)[O-])c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-23ad7b54403248708606eeee9fbf6470
COc1cc(C=O)cc(I)c1O>>O=Cc1cc(O)c(O)c(I)c1
IC=1C(=C(C=C(C=O)C1)OC)O.B(Br)(Br)Br>>IC=1C=C(C=O)C=C(C1O)O
C[O:6][c:5]1[cH:4][c:3]([CH:2]=[O:1])[cH:11][c:9]([I:10])[c:7]1[OH:8]>>[O:1]=[CH:2][c:3]1[cH:4][c:5]([OH:6])[c:7]([OH:8])[c:9]([I:10])[cH:11]1
COc1cc(C=O)cc(I)c1O
O=Cc1cc(O)c(O)c(I)c1
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
66.2
[{"value": 66.2, "product": "IC=1C=C(C=O)C=C(C1O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
16
HOUR
37.2 g of 5-iodo vanillin (commercial) and 360 ml of dichloromethane were mixed together under nitrogen and the mixture was cooled to 0° C. 135 ml of a molar solution of boron tribromide in dichloromethane were added and the mixture stood for 16 hours at ambient temperature and was then concentrated, cooled to 0° C. an...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1
Other
ClCCl
0
16
COc1cc(C=O)cc(I)c1O>ClCCl>O=Cc1cc(O)c(O)c(I)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9cad495ca4824beabdad8a4e8de68a2c
O=CC(=O)O.Oc1cccc(F)c1O>>O=C(O)C(O)c1ccc(F)c(O)c1O
Cl.FC1=C(C(O)=CC=C1)O.C(C=O)(=O)O.[OH-].[Na+]>>FC1=C(C(=C(C=C1)C(C(=O)O)O)O)O
[O:1]=[C:2]([OH:3])[CH:4]=[O:5].[cH:6]1[cH:7][cH:8][c:9]([F:10])[c:11]([OH:12])[c:13]1[OH:14]>>[O:1]=[C:2]([OH:3])[CH:4]([OH:5])[c:6]1[cH:7][cH:8][c:9]([F:10])[c:11]([OH:12])[c:13]1[OH:14]
O=CC(=O)O.Oc1cccc(F)c1O
O=C(O)C(O)c1ccc(F)c(O)c1O
null
null
O
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]
59
[{"value": 59.0, "product": "FC1=C(C(=C(C=C1)C(C(=O)O)O)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
51.2 g of 3-fluorocatechol and 36.8 g of glyoxylic acid were dissolved at 20° C. in 160 ml of water and 34.8 g of sodium hydroxide in solution in 400 ml of water were added to this solution cooled to 0° C. The mixture was heated for 4 hours at 46° C., then cooled to 0° C. and the pH was brought to 4.6 by the addition o...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol
c1ccccc1
c1ccccc1
c1ccccc1
null
O
0
null
O=CC(=O)O.Oc1cccc(F)c1O>O>O=C(O)C(O)c1ccc(F)c(O)c1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-30ada60bc0e74527b46c8f5abdf6a8c0
COCCOCOc1ccc(C=O)c(Cl)c1OCOCCOC.[OH-]>>COCCOCOc1ccc(C(O)C(=O)O)c(Cl)c1OCOCCOC
[Cl-].[Li+].[OH-].[K+].ClC1=C(C=O)C=CC(=C1OCOCCOC)OCOCCOC.C(Br)(Br)Br.O1CCOCC1.C(Br)(Br)Br>>ClC1=C(C=CC(=C1OCOCCOC)OCOCCOC)C(C(=O)O)O
[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[cH:9][cH:10][c:11]([CH:12]=[O:13])[c:17]([Cl:18])[c:19]1[O:20][CH2:21][O:22][CH2:23][CH2:24][O:25][CH3:26].[OH-:16]>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[cH:9][cH:10][c:11]([CH:12]([OH:13])[C:14](=[O:15])[OH:16])[c:17]([Cl:18])[c:19]1[O:20][CH2:21][O:22][CH...
COCCOCOc1ccc(C=O)c(Cl)c1OCOCCOC.[OH-]
COCCOCOc1ccc(C(O)C(=O)O)c(Cl)c1OCOCCOC
null
null
O
Acylation
OtherReaction
e4754e3793ba0362af7cd262e2f320471fced6da69cfa59aaf69349f987b0106
7b79ddb9582ae558ef0424125dcd16c236a764b78e4d8d3057436676b03c02cd
c1ccccc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5].[OH-;D0:6]>>[O;D1;H0:7]=[C:8](-[OH;D1;+0:6])-[CH;D3;+0:2](-[OH;D1;+0:1])-[c:3](:[c:4]):[c:5]
null
[]
0
CELSIUS
24
HOUR
2.42 g of lithium chloride and 7.02 g of potassium hydroxide were dissolved in 30 ml of water at 0° C. and a solution of 10 g of 2-chloro-3,4-bis-[(2-methoxy-ethoxy)-methoxy] benzaldehyde (synthesized in Preparation 1), 2.8 ml of bromoform and 38 ml of dioxane were added to this mixture. The mixture was stirred for 24 ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Carboxylic acid.Secondary alcohol
null
null
c1ccccc1
null
O
0
24
COCCOCOc1ccc(C=O)c(Cl)c1OCOCCOC.[OH-]>O>COCCOCOc1ccc(C(O)C(=O)O)c(Cl)c1OCOCCOC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5043e9c099ff4fda98d9234332a5cc3e
COCCOCOc1cc(C(O)C(=O)O)cc(F)c1OCOCCOC.[N-]=[N+]=C(c1ccccc1)c1ccccc1>>COCCOCOc1cc(C(O)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC
O.C1(=CC=CC=C1)C(=[N+]=[N-])C1=CC=CC=C1.FC=1C=C(C=C(C1OCOCCOC)OCOCCOC)C(C(=O)O)O>>FC=1C=C(C=C(C1OCOCCOC)OCOCCOC)C(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)O
[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[cH:9][c:10]([CH:11]([OH:12])[C:13](=[O:14])[OH:15])[cH:29][c:30]([F:31])[c:32]1[O:33][CH2:34][O:35][CH2:36][CH2:37][O:38][CH3:39].[N-]=[N+]=[C:16]([c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1)[c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH...
COCCOCOc1cc(C(O)C(=O)O)cc(F)c1OCOCCOC.[N-]=[N+]=C(c1ccccc1)c1ccccc1
COCCOCOc1cc(C(O)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC
null
null
ClCCl.CCOCC
Heteroatom Alkylation and Arylation
O-alkylation of carboxylic acids with diazo compounds
8531b6eb3abfd6846ce0cb8d79abac610072134e0cc0be40cc269196cd4eea5b
d6eab3abd961fdb019332f17e55277b8a7c7f7a1f79c71be7a6248f0a0e6a15e
O=C(Cc1ccccc1)OC(c1ccccc1)c1ccccc1
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4].[N-]=[N+]=[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])-[c:9](:[c:10]):[c:11]>>[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[CH;D3;+0:5](-[c:6](:[c:7]):[c:8])-[c:9](:[c:10]):[c:11]
null
[]
null
null
16
HOUR
5.3 g of the acid of Step A were dissolved in 66 ml of dichloromethane and then 46 ml of a solution of diphenyl diazomethane at 6.5 g in ether were added at 15° C. The mixture was stirred for 16 hours at ambient temperature and then water was added, followed by decanting and acidifying with acetic acid. Washing with a ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Diazo
Ester
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
ClCCl.CCOCC
null
16
COCCOCOc1cc(C(O)C(=O)O)cc(F)c1OCOCCOC.[N-]=[N+]=C(c1ccccc1)c1ccccc1>ClCCl.CCOCC>COCCOCOc1cc(C(O)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0a483aea8a4b498cbaefafb7e4383a84
COCCOCOc1cc(C(ON)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC.O=C(O)C(=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>COCCOCOc1cc(C(ON=C(C(=O)O)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC
O(N)C(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)C1=CC(=C(C(=C1)OCOCCOC)OCOCCOC)F.O=C(C(=O)O)C=1N=C(SC1)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>FC=1C=C(C=C(C1OCOCCOC)OCOCCOC)C(C(OC(C1=CC=CC=C1)C1=CC=CC=C1)=O)ON=C(C(=O)O)C=1N=C(SC1)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[cH:9][c:10]([CH:11]([O:12][NH2:13])[C:43](=[O:44])[O:45][CH:46]([c:47]2[cH:48][cH:49][cH:50][cH:51][cH:52]2)[c:53]2[cH:54][cH:55][cH:56][cH:57][cH:58]2)[cH:59][c:60]([F:61])[c:62]1[O:63][CH2:64][O:65][CH2:66][CH2:67][O:68][CH3:69].O=[C:14]([C:15](=[O:16])[OH:17])[c:18]1...
COCCOCOc1cc(C(ON)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC.O=C(O)C(=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
COCCOCOc1cc(C(ON=C(C(=O)O)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
3d7a74a3d1c5abb5292963d4a3067f1fb8a89aead752dc9bb1d63522c4c0bd5c
6b0edeaa66853687109d0d530554f76edf36b01a8ec084e7ae9c709f0949a6b9
O=C(OC(c1ccccc1)c1ccccc1)C(ON=Cc1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1)c1ccccc1
O=[C;H0;D3;+0:1](-[C:2](=[O;D1;H0:3])-[O;D1;H1:4])-[c:5]1:[#7;a:6]:[c:7]:[#16;a:8]:[c:9]:1.[#8:10]-[C:11](=[O;D1;H0:12])-[C:13]-[#8:14]-[NH2;D1;+0:15]>>[#8:10]-[C:11](=[O;D1;H0:12])-[C:13]-[#8:14]-[N;H0;D2;+0:15]=[C;H0;D3;+0:1](-[C:2](=[O;D1;H0:3])-[O;D1;H1:4])-[c:5]1:[#7;a:6]:[c:7]:[#16;a:8]:[c:9]:1
56
[{"value": 56.0, "product": "FC=1C=C(C=C(C1OCOCCOC)OCOCCOC)C(C(OC(C1=CC=CC=C1)C1=CC=CC=C1)=O)ON=C(C(=O)O)C=1N=C(SC1)NC(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.640 g of the product of Step D and and 0.474 g of oxo-[2-[(triphenylmethyl)-amino]-thiazol-4-yl]-acetic acid (Belgian Patent Application No. 864,828) were stirred for 4 and a half hours under nitrogen and at ambient temperature in the presence of 20 ml of methanol. Then, the solvent was eliminated, and the residue wa...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
null
null
null
c1ccccc1.c1cscn1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
CO
null
null
COCCOCOc1cc(C(ON)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC.O=C(O)C(=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>CO>COCCOCOc1cc(C(ON=C(C(=O)O)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C(=O)OC(c2ccccc2)c2ccccc2)cc(F)c1OCOCCOC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a2d6a5f5e06e41cb9bec46be781f750a
BrC(Br)Br.COCCOCOc1c(C#N)ccc(C=O)c1OCOCCOC.[OH-]>>COCCOCOc1c(C#N)ccc(C(Br)C(=O)O)c1OCOCCOC
Cl.C(#N)C1=C(C(=C(C=O)C=C1)OCOCCOC)OCOCCOC.O1CCOCC1.C(Br)(Br)Br.[Br-].[Li+].[OH-].[K+]>>C(#N)C1=C(C(=C(C=C1)C(C(=O)O)Br)OCOCCOC)OCOCCOC
Br[CH:17](Br)[Br:16].[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[c:9]([C:10]#[N:11])[cH:12][cH:13][c:14]([CH:15]=[O:18])[c:20]1[O:21][CH2:22][O:23][CH2:24][CH2:25][O:26][CH3:27].[OH-:19]>>[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[c:9]([C:10]#[N:11])[cH:12][cH:13][c:14]([CH:15]([Br:16])[C:17](=[O:18])[OH:1...
BrC(Br)Br.COCCOCOc1c(C#N)ccc(C=O)c1OCOCCOC.[OH-]
COCCOCOc1c(C#N)ccc(C(Br)C(=O)O)c1OCOCCOC
null
null
O.C(C)(=O)OCC
Acylation
OtherReaction
365e7b5786ba406db9acc92273a73ca3606e1fc9beae7164dff36307d584b0e8
94f09b5eead91e2869e1eda1f358c9ebd11ae8f3e4a576f716d34b3e7202c271
c1ccccc1
Br-[CH;D3;+0:1](-Br)-[Br;H0;D1;+0:2].[O;H0;D1;+0:3]=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7].[OH-;D0:8]>>[Br;H0;D1;+0:2]-[CH;D3;+0:4](-[C;H0;D3;+0:1](=[O;H0;D1;+0:3])-[OH;D1;+0:8])-[c:5](:[c:6]):[c:7]
null
[]
null
null
72
HOUR
440 microliters of bromoform were added at -5° C. to a mixture of 4.26 mg of lithium bromide, 598 mg of potassium hydroxide and 5 ml of water and then, a solution of 825 mg of a 4-cyano-2,3-bis-[(2-methoxy-ethoxy)-methoxy]-benzaldehyde (preparation given hereafter) in 5 ml of dioxane was added dropwise. The mixture was...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Secondary halide.Aldehyde
Secondary halide.Carboxylic acid
null
null
c1ccccc1
HBr
O.C(C)(=O)OCC
null
72
BrC(Br)Br.COCCOCOc1c(C#N)ccc(C=O)c1OCOCCOC.[OH-]>O.C(C)(=O)OCC>COCCOCOc1c(C#N)ccc(C(Br)C(=O)O)c1OCOCCOC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9e556f57e168442bbbc24bcb8ff4afba
COCCOCOc1c(C#N)ccc(C(Br)C(=O)O)c1OCOCCOC.[N-]=[N+]=C(c1ccccc1)c1ccccc1>>COCCOCOc1c(C#N)ccc(C(Br)C(=O)OC(c2ccccc2)c2ccccc2)c1OCOCCOC
C(#N)C1=C(C(=C(C=C1)C(C(=O)O)Br)OCOCCOC)OCOCCOC.C1(=CC=CC=C1)C(=[N+]=[N-])C1=CC=CC=C1>>C(#N)C1=C(C(=C(C=C1)C(C(=O)OC(C1=CC=CC=C1)C1=CC=CC=C1)Br)OCOCCOC)OCOCCOC
[CH3:1][O:2][CH2:3][CH2:4][O:5][CH2:6][O:7][c:8]1[c:9]([C:10]#[N:11])[cH:12][cH:13][c:14]([CH:15]([Br:16])[C:17](=[O:18])[OH:19])[c:33]1[O:34][CH2:35][O:36][CH2:37][CH2:38][O:39][CH3:40].[N-]=[N+]=[C:20]([c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1)[c:27]1[cH:28][cH:29][cH:30][cH:31][cH:32]1>>[CH3:1][O:2][CH2:3][CH2:4][...
COCCOCOc1c(C#N)ccc(C(Br)C(=O)O)c1OCOCCOC.[N-]=[N+]=C(c1ccccc1)c1ccccc1
COCCOCOc1c(C#N)ccc(C(Br)C(=O)OC(c2ccccc2)c2ccccc2)c1OCOCCOC
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
O-alkylation of carboxylic acids with diazo compounds
8531b6eb3abfd6846ce0cb8d79abac610072134e0cc0be40cc269196cd4eea5b
d6eab3abd961fdb019332f17e55277b8a7c7f7a1f79c71be7a6248f0a0e6a15e
O=C(Cc1ccccc1)OC(c1ccccc1)c1ccccc1
[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4].[N-]=[N+]=[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])-[c:9](:[c:10]):[c:11]>>[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-[CH;D3;+0:5](-[c:6](:[c:7]):[c:8])-[c:9](:[c:10]):[c:11]
null
[]
null
null
null
null
The product of Step A was dissolved in 10 ml of methylene chloride and 470 mg of diphenyl diazomethane were added. Evaporation was carried out followed by chromatography on silica (eluant: cyclohexane - ethyl acetate (2-1)) to obtain 450 mg of the desired, product. Conditions: See reaction.notes.procedure_details. Work...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Diazo
Ester
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
C(Cl)Cl
null
null
COCCOCOc1c(C#N)ccc(C(Br)C(=O)O)c1OCOCCOC.[N-]=[N+]=C(c1ccccc1)c1ccccc1>C(Cl)Cl>COCCOCOc1c(C#N)ccc(C(Br)C(=O)OC(c2ccccc2)c2ccccc2)c1OCOCCOC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-81159db6893c43669dd5945fbf20ea55
COc1ccc(F)c(F)c1.OO>>COc1ccc(F)c(F)c1O
COB(OC)OC.Cl.OO.FC=1C=C(C=CC1F)OC.[Li+].CCC[CH2-]>>FC1=C(C(=CC=C1F)OC)O
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([F:7])[c:8]([F:9])[cH:10]1.O[OH:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([F:7])[c:8]([F:9])[c:10]1[OH:11]
COc1ccc(F)c(F)c1.OO
COc1ccc(F)c(F)c1O
null
null
CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
ae2c40671d5fdb818f0b6d803c1d8cceca080b6105aceeca1808a097ec52d441
a2fdf414569b219d462bc05c91ebf31e5426b96645f5c78cb091f50cc92fc345
c1ccccc1
O-[OH;D1;+0:1].[#8:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6](-[F;D1;H0:7]):[c:8]>>[#8:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[OH;D1;+0:1]):[c:6](-[F;D1;H0:7]):[c:8]
null
[]
null
null
null
null
Using the procedure of Example 39, 125 g of 3,4-difluoroanisole (commercial) and 500 ml of a 1.6M solution of N-butyllithium in hexane were reacted at -72° C., and then 92.4 ml of trimethylborate, 500 ml of hydrochloric acid and 120 g of intermediate compound were reacted and the product was reacted with 440 ml of 30% ...
10.6084/m9.figshare.5104873.v1
null
Peroxide
Aromatic alcohol
c1ccccc1
c1ccccc1
c1ccccc1
HO-
CCCCCC
null
null
COc1ccc(F)c(F)c1.OO>CCCCCC>COc1ccc(F)c(F)c1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3a2ecc42a142468888fdaba3359f6ee1
COCCOCOc1cc(C=CC(=O)[O-])c(Cl)c(Cl)c1OCOCCOC>>C=Cc1cc(OCOCCOC)c(OCOCCOC)c(Cl)c1Cl
ClC1=C(C=CC(=O)[O-])C=C(C(=C1Cl)OCOCCOC)OCOCCOC.[H-].C(C(C)C)[Al+]CC(C)C>>ClC1=C(C=C)C=C(C(=C1Cl)OCOCCOC)OCOCCOC
O=C([O-])[CH:1]=[CH:2][c:3]1[cH:4][c:5]([O:6][CH2:7][O:8][CH2:9][CH2:10][O:11][CH3:12])[c:13]([O:14][CH2:15][O:16][CH2:17][CH2:18][O:19][CH3:20])[c:21]([Cl:22])[c:23]1[Cl:24]>>[CH2:1]=[CH:2][c:3]1[cH:4][c:5]([O:6][CH2:7][O:8][CH2:9][CH2:10][O:11][CH3:12])[c:13]([O:14][CH2:15][O:16][CH2:17][CH2:18][O:19][CH3:20])[c:21](...
COCCOCOc1cc(C=CC(=O)[O-])c(Cl)c(Cl)c1OCOCCOC
C=Cc1cc(OCOCCOC)c(OCOCCOC)c(Cl)c1Cl
null
null
null
Reduction
OtherReaction
02b7eac01118bfd51c4a58b62814356740b902aea3dbc3f759c729b8b0806524
49d4bca12f98a39ef3d7cf431ba8a8e145ac0803658b55b3a56347c5526e322e
c1ccccc1
O=C(-[O-])-[CH;D2;+0:1]=[C:2]-[c:3]>>[CH2;D1;+0:1]=[C:2]-[c:3]
99.6
[{"value": 99.6, "product": "ClC1=C(C=C)C=C(C(=C1Cl)OCOCCOC)OCOCCOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using the procedure of Stage C of Example 40, 20 g of ester of Step B and 88 ml of diisobutylaluminium hydride were reacted to obtain 17.9 g of the expected product melting at 60° C. Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
null
Vinyl
null
null
c1ccccc1
Other
null
null
null
COCCOCOc1cc(C=CC(=O)[O-])c(Cl)c(Cl)c1OCOCCOC>>C=Cc1cc(OCOCCOC)c(OCOCCOC)c(Cl)c1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3ce42197cace4f5dad3160cf94f08e0c
C=Cc1cc(OCOCCOC)c(OCOCCOC)c(Cl)c1Cl.O=C(OO)c1cccc(Cl)c1>>C=CC12C=C(OCOCCOC)C(OCOCCOC)=C(Cl)C1(Cl)O2
ClC1=C(C=C)C=C(C(=C1Cl)OCOCCOC)OCOCCOC.ClC1=CC(=CC=C1)C(=O)OO>>ClC12C(C=C)(C=C(C(=C1Cl)OCOCCOC)OCOCCOC)O2
[CH2:1]=[CH:2][c:3]1[cH:4][c:5]([O:6][CH2:7][O:8][CH2:9][CH2:10][O:11][CH3:12])[c:13]([O:14][CH2:15][O:16][CH2:17][CH2:18][O:19][CH3:20])[c:21]([Cl:22])[c:23]1[Cl:24].O=C(O[OH:25])c1cccc(Cl)c1>>[CH2:1]=[CH:2][C:3]12[CH:4]=[C:5]([O:6][CH2:7][O:8][CH2:9][CH2:10][O:11][CH3:12])[C:13]([O:14][CH2:15][O:16][CH2:17][CH2:18][O...
C=Cc1cc(OCOCCOC)c(OCOCCOC)c(Cl)c1Cl.O=C(OO)c1cccc(Cl)c1
C=CC12C=C(OCOCCOC)C(OCOCCOC)=C(Cl)C1(Cl)O2
null
null
C1CCCCC1.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
72b2f8ff6740abd6644cb0a780d40368540147b13a2e0e8432a1a20e777dd1fd
a81bf860526a3cc8482c48e2baecd9d5497fdceb000730fed6b6c4f895adc8c2
C1=CC2OC2C=C1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C:2]-[#8:3]-[c;H0;D3;+0:4]1:[c;H0;D3;+0:5](-[Cl;D1;H0:6]):[c;H0;D3;+0:7](-[Cl;D1;H0:8]):[c;H0;D3;+0:9](-[C:10]=[C;D1;H2:11]):[cH;D2;+0:12]:[c;H0;D3;+0:13]:1-[#8:14]-[C:15]>>[C:2]-[#8:3]-[C;H0;D3;+0:4]1=[C;H0;D3;+0:5](-[Cl;D1;H0:6])-[C;H0;D4;+0:7]2(-[Cl;D1;H0:8])-[O;H0;D2;+0:1]-...
99.6
[{"value": 99.6, "product": "ClC12C(C=C)(C=C(C(=C1Cl)OCOCCOC)OCOCCOC)O2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using the procedure of Stage D of Example 40, 13.2 g of thee allylic alcohol of Step C and 10.3 g of m-chloro perbenzoic acid were reacted to obtain 13.7 g of the expected product with a Rf=0.25 (AcOEt-cyclohexane 6-4). Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Ether.Ether.Peroxide
Tertiary halide.Alkenyl halide.Ether.Ether.Ether
c1ccccc1.c1ccccc1
C1=CC2OC2C=C1
C1=CC2OC2C=C1
HCl
C1CCCCC1.C(C)(=O)OCC
null
null
C=Cc1cc(OCOCCOC)c(OCOCCOC)c(Cl)c1Cl.O=C(OO)c1cccc(Cl)c1>C1CCCCC1.C(C)(=O)OCC>C=CC12C=C(OCOCCOC)C(OCOCCOC)=C(Cl)C1(Cl)O2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6e731b1d7e854c2a8e627b73580568d3
CCCCCCCCBr.CCOC(=O)OCC>>CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC
Cl.BrCCCCCCCC.[Mg].C(OCC)(OCC)=O>>C(CCCCCCC)C(O)(CCCCCCCC)CCCCCCCC
Br[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH3:26].O([CH2:2][CH3:1])[C:9](O[CH2:3][CH3:6])=[O:10]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][C:9]([OH:10])([CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH3:18])[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH3:26]
CCCCCCCCBr.CCOC(=O)OCC
CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC
null
null
C(C)OCC
C-C Coupling
OtherReaction
8706ba12a6e3eac34bcc4e6f93267fb45dbd62c681eb88a043e053be354fdd53
66c8a44d5e8977ee5c977d626a3446a6c88153f3dc208477947005725264b4ae
null
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[CH2;D2;+0:5]-O-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-O-[CH2;D2;+0:8]-[CH3;D1;+0:9]>>[C:10]-[C:11]-[C;H0;D4;+0:6](-[OH;D1;+0:7])(-[C:12]-[C:13]-[CH2;D2;+0:9]-[C:14]-[C:15]-[CH2;D2;+0:8]-[CH2;D2;+0:5]-[C;D1;H3:4])-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
30
CELSIUS
1
HOUR
This compound may be prepared in the following manner. Three moles of 1-bromooctane are slowly added to 3 moles of magnesium turnings in 0.6 liters of anhydrous ethyl ether (nitrogen atmosphere). One mole of diethyl carbonate in 0.151 anhydrous ethyl ether is slowly added to the mixture. The mixture is stirred for one ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbonic Ester
Tertiary alcohol
null
null
null
Br-
C(C)OCC
30
1
CCCCCCCCBr.CCOC(=O)OCC>C(C)OCC>CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b0a83914dba048c6a657be3218f2bd5a
CCCCCCCCC(Cl)(CCCCCCCC)CCCCCCCC.CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC>>CCCCCCCCC(C)(CCCCCCCC)CCCCCCCC
C(CCCCCCC)C(CCCCCCCC)(CCCCCCCC)Cl.C(CCCCCCC)C(O)(CCCCCCCC)CCCCCCCC.[Cl-].[Ca+2].[Cl-].C[Al](C)C.Cl>>C(CCCCCCC)C(C)(CCCCCCCC)CCCCCCCC
CCCCCCCCC(Cl)(CCCCCCCC)CCCCCCC[CH3:10].O[C:9]([CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])([CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH3:18])[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH3:26]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][C:9]([CH3:10])([CH2:11][CH2:...
CCCCCCCCC(Cl)(CCCCCCCC)CCCCCCCC.CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC
CCCCCCCCC(C)(CCCCCCCC)CCCCCCCC
null
null
C(Cl)Cl
C-C Coupling
OtherReaction
272b9cd949524b0f15cc42e5bff323005c8996c8af1fcaa2d39cd5f393a7d26f
bd96ef07d60c9b141f8e4bcb3de7c88b60e9a3e72642350d7d8f0d1588ccd78f
null
C-C-C-C-C-C-C-C-C(-Cl)(-C-C-C-C-C-C-C-C)-C-C-C-C-C-C-C-[CH3;D1;+0:1].O-[C;H0;D4;+0:2](-[C:3]-[C:4])(-[C:5]-[C:6])-[C:7]-[C:8]>>[C:4]-[C:3]-[C;H0;D4;+0:2](-[CH3;D1;+0:1])(-[C:5]-[C:6])-[C:7]-[C:8]
null
[]
0
CELSIUS
null
null
This compound may be prepared in the following manner. Three moles of 1-bromooctane are slowly added to 3 moles of magnesium turnings in 0.6 liters of anhydrous ethyl ether (nitrogen atmosphere). One mole of diethyl carbonate in 0.151 anhydrous ethyl ether is slowly added to the mixture. The mixture is stirred for one ...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary alcohol
null
null
null
null
HCl
C(Cl)Cl
0
null
CCCCCCCCC(Cl)(CCCCCCCC)CCCCCCCC.CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC>C(Cl)Cl>CCCCCCCCC(C)(CCCCCCCC)CCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5831ca84c85c45188e821732a2150987
CCCCCCCCCCBr.CCOC(=O)OCC>>CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC
Cl.BrCCCCCCCCCC.[Mg].C(OCC)(OCC)=O>>C(CCCCCCCCC)C(O)(CCCCCCCCCC)CCCCCCCCCC
Br[CH2:23][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH3:32].O([CH2:2][CH3:1])[C:11](O[CH2:14][CH3:15])=[O:12]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][C:11]([OH:12])([CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][CH2:21][CH3:22])[CH2:23][CH2:24][C...
CCCCCCCCCCBr.CCOC(=O)OCC
CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC
null
null
C(C)OCC
C-C Coupling
OtherReaction
8706ba12a6e3eac34bcc4e6f93267fb45dbd62c681eb88a043e053be354fdd53
66c8a44d5e8977ee5c977d626a3446a6c88153f3dc208477947005725264b4ae
null
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[CH2;D2;+0:5]-O-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-O-[CH2;D2;+0:8]-[CH3;D1;+0:9]>>[C:10]-[C:11]-[CH2;D2;+0:5]-[C;D1;H3:4].[C:12]-[C:13]-[CH2;D2;+0:9]-[CH2;D2;+0:8]-[C:14]-[C;H0;D4;+0:6](-[OH;D1;+0:7])(-[C:15]-[C:16])-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
30
CELSIUS
1
HOUR
Three moles of 1-bromodecane was slowly added to 3 moles of magnesium turnings in 0.6 liters of anhydrous ethyl ether (nitrogen atmosphere). One mole of diethyl carbonate in 0.151 anhydrous ethyl ether was slowly added to the mixture. After stirring for one hour at 30° C., the mixture was slowly poured into 1.8 liters ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbonic Ester
Tertiary alcohol
null
null
null
Br-
C(C)OCC
30
1
CCCCCCCCCCBr.CCOC(=O)OCC>C(C)OCC>CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-43db573a1030471e9bdddb88415b043e
CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC.Cl>>CCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC
Cl.C(CCCCCCCCC)C(O)(CCCCCCCCCC)CCCCCCCCCC.[Cl-].[Ca+2].[Cl-]>>C(CCCCCCCCC)C(CCCCCCCCCC)(CCCCCCCCCC)Cl
O[C:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])([CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][CH2:21][CH3:22])[CH2:23][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH3:32].[ClH:12]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2...
CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC.Cl
CCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC
null
null
C(Cl)Cl
Miscellaneous
Alcohol to chloride_HCl
06eab52f623b8fb0d86400eecae376db031ba5e5becb07a748e186ad18f204bc
34c38d962daad1da1e92c0e4cf09f41371ed52dbd062ebc36fca2e0c616df50b
null
O-[C;H0;D4;+0:1](-[C:2]-[C:3])(-[C:4]-[C:5])-[C:6]-[C:7].[ClH;D0;+0:8]>>[C:5]-[C:4]-[C;H0;D4;+0:1](-[Cl;H0;D1;+0:8])(-[C:2]-[C:3])-[C:6]-[C:7]
90
[{"value": 90.0, "product": "C(CCCCCCCCC)C(CCCCCCCCCC)(CCCCCCCCCC)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
One mole of tri-n-decylcarbinol was added to a mixture of 0.2 liters of methylene chloride and 0.32 moles calcium chloride. Approximately 1.5 moles of HCl gas was slowly bubbled through the solution. The product mixture is then washed with 1 liter of a 10% sodium carbonate solution. The organic layer is dried with magn...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Tertiary halide
null
null
null
HO-
C(Cl)Cl
null
null
CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC.Cl>C(Cl)Cl>CCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d5601d68778243e1afd472a048d0d106
CCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC>>CCCCCCCCCCC(C)(CCCCCCCCCC)CCCCCCCCCC
C(CCCCCCCCC)C(CCCCCCCCCC)(CCCCCCCCCC)Cl.C[Al](C)C>>C(CCCCCCCCC)C(C)(CCCCCCCCCC)CCCCCCCCCC
Cl[C:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])([CH2:12][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH3:32])[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][CH2:21][CH3:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][C:1...
CCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC
CCCCCCCCCCC(C)(CCCCCCCCCC)CCCCCCCCCC
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
d06dc960ad45ba0387d757dfc480fdfd624a6cb7f28b4f8a95745d58a488baf5
404c724ad3ca06f39bc871693871aba7ab416f4e80555c466ba262b8bc4d8d51
null
Cl-[C;H0;D4;+0:1](-[C:2]-[C:3])(-[C:4]-[C:5])-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:4]-[C;H0;D4;+0:1](-[CH3;D1;+0:6])(-[C:2]-[C:3])-[C:10]-[CH2;D2;+0:7]-[C:8]-[C:9]
75
[{"value": 75.0, "product": "C(CCCCCCCCC)C(C)(CCCCCCCCCC)CCCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
One mole of tri-n-decylmethylchloride was added to 0.75 liters of methylene chloride and the solution was blanketed with nitrogen and cooled to 0° C. 0.33 moles of trimethylaluminum was then added and the mixture was allowed to warm to room temperature. The mixture was slowly quenched with 50 ml of water followed by wa...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide
null
null
null
null
null
C(Cl)Cl
0
null
CCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC>C(Cl)Cl>CCCCCCCCCCC(C)(CCCCCCCCCC)CCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8a7e187e142942fdb6f461d846f40942
CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC>>CCCCCCCCCCC(C)(CCCCCCCCCC)CCCCCCCCCC
C(CCCCCCCCC)C(O)(CCCCCCCCCC)CCCCCCCCCC.C[Al](C)C>>C(CCCCCCCCC)C(C)(CCCCCCCCCC)CCCCCCCCCC
O[C:11]([CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])([CH2:12][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH3:32])[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][CH2:21][CH3:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][C:11...
CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC
CCCCCCCCCCC(C)(CCCCCCCCCC)CCCCCCCCCC
null
[Ti](Cl)(Cl)(Cl)Cl
C(Cl)Cl
Miscellaneous
OtherReaction
11d17e43de92be7fa6f46d5cbef5874ff365848c27d02336596ae498740a47ba
96b5e5e1e667b20dc45eb811e44eb97b30bb7bfac720a7b7a090312707dfb175
null
O-[C;H0;D4;+0:1](-[C:2]-[C:3])(-[C:4]-[C:5])-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:4]-[C;H0;D4;+0:1](-[CH3;D1;+0:6])(-[C:2]-[C:3])-[C:10]-[CH2;D2;+0:7]-[C:8]-[C:9]
70
[{"value": 70.0, "product": "C(CCCCCCCCC)C(C)(CCCCCCCCCC)CCCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
2.5
HOUR
Alternatively, the 0.1 moles of the synthesized tri-n-decylcarbinol was added to 0.2 liters of methylene chloride. The mixture was covered with a blanket of nitrogen and cooled to 0° C. 0.050 mole titanium tetrachloride was added to the mixture and the solution was stirred 2-3 hours at 0° C. 0.066 mole trimethylaluminu...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
null
null
null
null
null
[Ti](Cl)(Cl)(Cl)Cl.C(Cl)Cl
0
2.5
CCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC>[Ti](Cl)(Cl)(Cl)Cl.C(Cl)Cl>CCCCCCCCCCC(C)(CCCCCCCCCC)CCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-53f58a0bd1b3472b91143912053c2870
CCCCCCCCBr.CCOC(=O)OCC>>CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC
Cl.C(CCCCCCC)Br.[Mg].C(OCC)(OCC)=O>>C(CCCCCCC)C(O)(CCCCCCCC)CCCCCCCC
Br[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH3:26].O([CH2:2][CH3:1])[C:9](O[CH2:3][CH3:6])=[O:10]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][C:9]([OH:10])([CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH3:18])[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH3:26]
CCCCCCCCBr.CCOC(=O)OCC
CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC
null
null
C(C)OCC
C-C Coupling
OtherReaction
8706ba12a6e3eac34bcc4e6f93267fb45dbd62c681eb88a043e053be354fdd53
66c8a44d5e8977ee5c977d626a3446a6c88153f3dc208477947005725264b4ae
null
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[CH2;D2;+0:5]-O-[C;H0;D3;+0:6](=[O;H0;D1;+0:7])-O-[CH2;D2;+0:8]-[CH3;D1;+0:9]>>[C:10]-[C:11]-[C;H0;D4;+0:6](-[OH;D1;+0:7])(-[C:12]-[C:13]-[CH2;D2;+0:9]-[C:14]-[C:15]-[CH2;D2;+0:8]-[CH2;D2;+0:5]-[C;D1;H3:4])-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
30
CELSIUS
1
HOUR
This compound may be prepared in the following manner. Three moles of n-octylbromide are slowly added to 3 moles of magnesium turnings in 0.6 liters of anhydrous ethyl ether (nitrogen atmosphere). One mole of diethyl carbonate in 0.151 anhydrous ethyl ether is slowly added to the mixture. The mixture is stirred for one...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carbonic Ester
Tertiary alcohol
null
null
null
Br-
C(C)OCC
30
1
CCCCCCCCBr.CCOC(=O)OCC>C(C)OCC>CCCCCCCCC(O)(CCCCCCCC)CCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-108d826840d345cdb28e811cd9a5ff6a
CCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCC[CH2][Mg][Br].CCOC(=O)OCC>>CCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC
Cl.C(CCCCCCCCC)[Mg]Br.C(C)OC(OCC)=O.C(CCCCCCCCCCCCC)[Mg]Br>>C(CCCCCCCCC)C(O)(CCCCCCCCCCCCCC)CCCCCCCCCC
[Br][Mg][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[Br][Mg][CH2:17][CH2:18][CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH3:26].O([C:15](O[CH2:35][CH3:27])=[O:16])[CH2:28][CH3:29]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH...
CCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCC[CH2][Mg][Br].CCOC(=O)OCC
CCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC
null
null
C(C)OCC
C-C Coupling
OtherReaction
62964fd1377eac5f0eb7f51aea42b9f3e2d3ca0f07b95736432e18531304a33d
624e8b17a308e03f3e6939ffdcbdcca4c9cec90af9e7aef377156454a167fe61
null
[Br]-[Mg]-[CH2;D2;+0:1]-[C:2]-[C:3].[Br]-[Mg]-[CH2;D2;+0:4]-[C:5]-[C:6].[CH3;D1;+0:7]-[CH2;D2;+0:8]-O-[C;H0;D3;+0:9](=[O;H0;D1;+0:10])-O-[CH2;D2;+0:11]-[CH3;D1;+0:12]>>[C:13]-[C:14]-[CH2;D2;+0:8]-[C;D1;H3:15].[C:3]-[C:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:9](-[OH;D1;+0:10])(-[CH2;D2;+0:4]-[C:5]-[C:6])-[CH2;D2;+0:7]-[CH2;D2;+0:1...
null
[]
30
CELSIUS
1
HOUR
Decylmagnesium bromide (0.66 mole) in ethyl ether is slowly added to 0.33 moles of diethylcarbonate in 100 ml ethyl ether and stirred for one hour at 30° C. (nitrogen atmosphere). Tetradecylmagnesium bromide (0.33 moles) is slowly added to the solution and stirred for one hour at 30° C. The mixture is then slowly poure...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Magnesium halide.Carbonic Ester
Tertiary alcohol
null
null
null
null
C(C)OCC
30
1
CCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCC[CH2][Mg][Br].CCOC(=O)OCC>C(C)OCC>CCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3272ce8059be4591a93fe2fa3200dcab
CCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC.Cl>>CCCCCCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC
Cl.C(CCCCCCCCC)C(O)(CCCCCCCCCCCCCC)CCCCCCCCCC.[Cl-].[Ca+2].[Cl-]>>C(CCCCCCCCC)C(CCCCCCCCCCCCCC)(CCCCCCCCCC)Cl
O[C:15]([CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])([CH2:17][CH2:18][CH2:19][CH2:20][CH2:21][CH2:22][CH2:23][CH2:24][CH2:25][CH3:26])[CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][CH2:34][CH2:35][CH3:36].[ClH:16]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5]...
CCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC.Cl
CCCCCCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC
null
null
C(Cl)Cl
Miscellaneous
Alcohol to chloride_HCl
06eab52f623b8fb0d86400eecae376db031ba5e5becb07a748e186ad18f204bc
34c38d962daad1da1e92c0e4cf09f41371ed52dbd062ebc36fca2e0c616df50b
null
O-[C;H0;D4;+0:1](-[C:2]-[C:3])(-[C:4]-[C:5])-[C:6]-[C:7].[ClH;D0;+0:8]>>[C:3]-[C:2]-[C;H0;D4;+0:1](-[Cl;H0;D1;+0:8])(-[C:4]-[C:5])-[C:6]-[C:7]
null
[]
null
null
null
null
One mole of di-n-decyl-n-tetradecylcarbinol is added to 0.2 liters of methylene chloride and 0.32 moles calcium chloride. Approximately 1.5 moles of HCl gas is slowly bubbled through the solution. The product mixture is then washed with 1 liter of a 10% sodium carbonate solution. The organic layer is dried with magnesi...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Tertiary halide
null
null
null
HO-
C(Cl)Cl
null
null
CCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCC.Cl>C(Cl)Cl>CCCCCCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3a5409deb6a74c57b3451bf511fe1b1f
CCCCCCCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCC[CH2][Mg][Br].CCOC(=O)OCC>>CCCCCCCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCCCCCC
C(CCCCCCCCC)[Mg]Br.C(CCCCCCCCCCCCCCCCCC)[Mg]Br.C(C)OC(OCC)=O.Cl.C(CCCCCCCCCCCCC)[Mg]Br>>C(CCCCCCCCCCCCCCCCCC)C(O)(CCCCCCCCCC)CCCCCCCCCCCCCC
[Br][Mg][CH2:19][CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[Br][Mg][CH2:32][CH2:33][CH2:34][CH2:35][CH2:36][CH2:37][CH2:38][CH2:39][CH2:40][CH2:41][CH2:42][CH2:43][CH2:44][CH3:45].[Br][Mg][CH2:22][CH2:23][CH2:24][CH2:25][CH2:26...
CCCCCCCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCC[CH2][Mg][Br].CCOC(=O)OCC
CCCCCCCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCCCCCC
null
null
C(C)OCC
C-C Coupling
OtherReaction
2ff6284ae5c29aecab9688c38dab5c3f668b289ce7880f1ed4e891928aae5c9e
628a23618f2baf89036e21fa6db53ec245ef0b967c8fb58f9713610e1454506d
null
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-O-C-C.[Br]-[Mg]-[CH2;D2;+0:3]-[C:4]-[C:5].[Br]-[Mg]-[CH2;D2;+0:6]-[C:7]-[C:8].[Br]-[Mg]-[CH2;D2;+0:9]-[C:10]-[C:11]>>[C:5]-[C:4]-[CH2;D2;+0:3]-[C;H0;D4;+0:1](-[OH;D1;+0:2])(-[CH2;D2;+0:9]-[C:10]-[C:11])-[CH2;D2;+0:6]-[C:7]-[C:8]
null
[]
30
CELSIUS
1
HOUR
n-Nonadecylmagnesium bromide (0.33 moles) in ethyl ether is slowly added to 0.33 mole of diethylcarbonate in 100 ml diethyl ether and stirred for one hour at 30° C. (nitrogen atmosphere). n-Tetradecylmagnesium bromide (0.33 mole) is slowly added to the solution and stirred for one hour at 30° C. n-Decylmagnesium bromid...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Magnesium halide.Magnesium halide.Carbonic Ester
Tertiary alcohol
null
null
null
HBr.Mg
C(C)OCC
30
1
CCCCCCCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCCCCCC[CH2][Mg][Br].CCCCCCCCC[CH2][Mg][Br].CCOC(=O)OCC>C(C)OCC>CCCCCCCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5357024e5ff4448eabdc6f4dbebdfb2c
CCCCCCCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCCCCCC.Cl>>CCCCCCCCCCCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCCCCCC
Cl.C(CCCCCCCCCCCCCCCCCC)C(O)(CCCCCCCCCC)CCCCCCCCCCCCCC.[Cl-].[Ca+2].[Cl-]>>C(CCCCCCCCCCCCCCCCCC)C(CCCCCCCCCC)(CCCCCCCCCCCCCC)Cl
O[C:20]([CH2:19][CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])([CH2:22][CH2:23][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH3:31])[CH2:32][CH2:33][CH2:34][CH2:35][CH2:36][CH2:37][CH2:38][CH2:39][CH2:40][CH2:41][CH2:4...
CCCCCCCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCCCCCC.Cl
CCCCCCCCCCCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCCCCCC
null
null
C(Cl)Cl
Miscellaneous
Alcohol to chloride_HCl
06eab52f623b8fb0d86400eecae376db031ba5e5becb07a748e186ad18f204bc
34c38d962daad1da1e92c0e4cf09f41371ed52dbd062ebc36fca2e0c616df50b
null
O-[C;H0;D4;+0:1](-[C:2]-[C:3])(-[C:4]-[C:5])-[C:6]-[C:7].[ClH;D0;+0:8]>>[C:3]-[C:2]-[C;H0;D4;+0:1](-[Cl;H0;D1;+0:8])(-[C:4]-[C:5])-[C:6]-[C:7]
null
[]
null
null
null
null
One mole of n-nonadecyl-n-tetradecyl-n-decylcarbinol is added to 0.2 liters of methylene chloride and 0.32 moles calcium chloride. Approximately 1.5 moles of HCl gas is slowly bubbled through the solution. The product mixture is then washed with 1 liter of a 10% sodium carbonate solution. The organic layer is dried wit...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Tertiary halide
null
null
null
HO-
C(Cl)Cl
null
null
CCCCCCCCCCCCCCCCCCCC(O)(CCCCCCCCCC)CCCCCCCCCCCCCC.Cl>C(Cl)Cl>CCCCCCCCCCCCCCCCCCCC(Cl)(CCCCCCCCCC)CCCCCCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ccded561afe0424fa8a1fedcae175ed7
CC1(C)Oc2cc3c(cc2O1)OC(C)(C)O3.O=C=O>>CC1(C)Oc2cc3c(c(C(=O)O)c2O1)OC(C)(C)O3
[OH-].[Na+].CC1(OC2=C(O1)C=C1C(OC(O1)(C)C)=C2)C.C(CCC)[Li].C(=O)=O>>CC1(OC2=C(O1)C(=C1C(OC(O1)(C)C)=C2)C(=O)O)C
[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[cH:6][c:7]3[c:8]([cH:9][c:13]2[O:14]1)[O:15][C:16]([CH3:17])([CH3:18])[O:19]3.[C:10](=[O:11])=[O:12]>>[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[cH:6][c:7]3[c:8]([c:9]([C:10](=[O:11])[OH:12])[c:13]2[O:14]1)[O:15][C:16]([CH3:17])([CH3:18])[O:19]3
CC1(C)Oc2cc3c(cc2O1)OC(C)(C)O3.O=C=O
CC1(C)Oc2cc3c(c(C(=O)O)c2O1)OC(C)(C)O3
null
null
C1CCOC1.O.CCCCCC
Acylation
OtherReaction
a86cfdbc7f612158eb74004352ed48cb5636d9157f80b8a4084730d2d59c5e2c
f2fa2063dd26da08ea200eb6cbb3037b91013a82352a2b60120e98f9e54cbd88
c1c2c(cc3c1OCO3)OCO2
[#8:1]1-[C:2]-[#8:3]-[c:4]:[c:5]-1:[cH;D2;+0:6]:[c:7]1:[c:8]-[#8:9]-[C:10]-[#8:11]-1.[O;D1;H0:12]=[C;H0;D2;+0:13]=[O;H0;D1;+0:14]>>[O;D1;H0:12]=[C;H0;D3;+0:13](-[OH;D1;+0:14])-[c;H0;D3;+0:6](:[c:5]1:[c:4]-[#8:3]-[C:2]-[#8:1]-1):[c:7]1:[c:8]-[#8:9]-[C:10]-[#8:11]-1
null
[]
-20
CELSIUS
8
HOUR
2,2,6,6-Tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dioxole (10.0 g, 45.0 mmol; prepared according to WO-91/12024) was dissolved in dry THF (200 mL) under an argon atmosphere. The solution was cooled to -20° C. and n-butyllithium (20.0 mL, 50.0 mmol) in hexane was added. After attaining ambient temperature, the reaction mix...
10.6084/m9.figshare.5104873.v1
null
Carbon dioxide
Carboxylic acid
c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1OCO3)OCO2
null
C1CCOC1.O.CCCCCC
-20
8
CC1(C)Oc2cc3c(cc2O1)OC(C)(C)O3.O=C=O>C1CCOC1.O.CCCCCC>CC1(C)Oc2cc3c(c(C(=O)O)c2O1)OC(C)(C)O3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b748cc817d6e4b11bba391ca0648edaa
CC1(C)Oc2cc3c(c(C(=O)O)c2O1)OC(C)(C)O3.CI>>COC(=O)c1c2c(cc3c1OC(C)(C)O3)OC(C)(C)O2
CC1(OC2=C(O1)C(=C1C(OC(O1)(C)C)=C2)C(=O)O)C.C([O-])([O-])=O.[K+].[K+].CI>>COC(=O)C1=C2C(OC(O2)(C)C)=CC2=C1OC(O2)(C)C
[OH:2][C:3](=[O:4])[c:5]1[c:6]2[c:7]([cH:8][c:9]3[c:10]1[O:11][C:12]([CH3:13])([CH3:14])[O:15]3)[O:16][C:17]([CH3:18])([CH3:19])[O:20]2.I[CH3:1]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]2[c:7]([cH:8][c:9]3[c:10]1[O:11][C:12]([CH3:13])([CH3:14])[O:15]3)[O:16][C:17]([CH3:18])([CH3:19])[O:20]2
CC1(C)Oc2cc3c(c(C(=O)O)c2O1)OC(C)(C)O3.CI
COC(=O)c1c2c(cc3c1OC(C)(C)O3)OC(C)(C)O2
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
9474aa79a2adc7353c0c02444ca598a6f486ecdd7ed5edb9ae0645721ee50389
badd4f82161bb0ee7acffd023ea4caae5d036bce7065c10ab0a06e83a6a6f119
c1c2c(cc3c1OCO3)OCO2
I-[CH3;D1;+0:1].[O;D1;H0:2]=[C:3](-[OH;D1;+0:4])-[c:5]>>[CH3;D1;+0:1]-[O;H0;D2;+0:4]-[C:3](=[O;D1;H0:2])-[c:5]
88.3
[{"value": 88.0, "product": "COC(=O)C1=C2C(OC(O2)(C)C)=CC2=C1OC(O2)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.3, "product": "COC(=O)C1=C2C(OC(O2)(C)C)=CC2=C1OC(O2)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
55
CELSIUS
8
HOUR
2,2,6,6-Tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dioxole-4-carboxylic acid (10.0 g, 38.0 mmol) was dissolved in dry DMF (100 mL). Potassium carbonate (15.2 g, 110.0 mmol) was added and the reaction was heated to 55° C. for 30 min. After cooling to ambient temperature, methyl iodide (15.6 g, 110.0 mmol) was added and the ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1c2c(cc3c1OCO3)OCO2
HI
CN(C)C=O
55
8
CC1(C)Oc2cc3c(c(C(=O)O)c2O1)OC(C)(C)O3.CI>CN(C)C=O>COC(=O)c1c2c(cc3c1OC(C)(C)O3)OC(C)(C)O2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6735643c3b9e41779184084c922223ce
CC1(C)Sc2cc3c(cc2S1)SC(C)(C)S3.COC(=O)c1c2c(cc3c1OC(C)(C)O3)OC(C)(C)O2.[Li][CH2]CCC>>CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3
CC1(SC2=C(S1)C=C1C(SC(S1)(C)C)=C2)C.C(CCC)[Li].COC(=O)C1=C2C(OC(O2)(C)C)=CC2=C1OC(O2)(C)C>>CC1(SC2=C(S1)C(=C1C(SC(S1)(C)C)=C2)C(O)(C2=C1C(OC(O1)(C)C)=CC1=C2OC(O1)(C)C)C1=C2C(SC(S2)(C)C)=CC2=C1SC(S2)(C)C)C
[CH3:1][C:19]1([CH3:21])[S:18][c:33]2[cH:28][c:29]3[c:30]([cH:31][c:32]2[S:38]1)[S:39][C:40]([CH3:26])([CH3:41])[S:43]3.O([C:10](=[O:11])[c:12]1[c:13]2[c:14]([cH:15][c:16]3[c:17]1[O:45][C:24]([CH3:3])([CH3:44])[O:4]3)[O:46][C:47]([CH3:48])([CH3:49])[O:50]2)[CH3:20].[Li][CH2:35][CH2:36][CH2:2][CH3:5]>>[CH3:1][C:2]1([CH3...
CC1(C)Sc2cc3c(cc2S1)SC(C)(C)S3.COC(=O)c1c2c(cc3c1OC(C)(C)O3)OC(C)(C)O2.[Li][CH2]CCC
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3
null
null
C1CCOC1
Aromatic Heterocycle Formation
OtherReaction
e452af76f0455ab1d8513150fcc164c0fb93545642074ba0071ff3502d56f9e2
eb8a988e87dd1193fc0c80512a94e5e30ef7d7055d9620e213ba0a6c44aa617d
c1c2c(c(C(c3c4c(cc5c3SCS5)SCS4)c3c4c(cc5c3SCS5)SCS4)c3c1OCO3)OCO2
[C;D1;H3:1]-[C;H0;D4;+0:2]1(-[CH3;D1;+0:3])-[S;H0;D2;+0:4]-[c;H0;D3;+0:5]2:[cH;D2;+0:6]:[c:7]3:[c:8](:[c:9]:[c:10]:2-[S;H0;D2;+0:11]-1)-[#16:12]-[C;H0;D4;+0:13](-[C;D1;H3:14])(-[CH3;D1;+0:15])-[#16:16]-3.[C;D1;H3:17]-[C:18]1(-[C;D1;H3:19])-[O;H0;D2;+0:20]-[c;H0;D3;+0:21]2:[c:22]:[c;H0;D3;+0:23]3:[c;H0;D3;+0:24](:[c:25]...
44
[{"value": 44.0, "product": "CC1(SC2=C(S1)C(=C1C(SC(S1)(C)C)=C2)C(O)(C2=C1C(OC(O1)(C)C)=CC1=C2OC(O1)(C)C)C1=C2C(SC(S2)(C)C)=CC2=C1SC(S2)(C)C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2,2,6,6-Tetramethylbenzo[1,2-d:4,5-d']bis(1,3)dithiole (2.86 g, 10 mmol; prepared according to WO-91/12024) was dissolved in anhydrous THF (75 mL) and cooled to -70° C. n-Butyllithium (4.4 mL, 2.5M in hexane) was added. The reaction mixture was allowed to reach ambient temperature. 4-Methoxycarbonyl-2,2,6,6-tetramethyl...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Ether.Ether.Ether.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Alkyl lithium
Ether.Ether.Ether.Ether.Tertiary alcohol.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
Li
C1CCOC1
null
1
CC1(C)Sc2cc3c(cc2S1)SC(C)(C)S3.COC(=O)c1c2c(cc3c1OC(C)(C)O3)OC(C)(C)O2.[Li][CH2]CCC>C1CCOC1>CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8a322f043809404b8fb31f9aa2d7aec3
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3.CCOC(=O)OCC.CN(C)CCN(C)C.[Li][C](C)(C)C>>CCOC(=O)c1c2c(c(C(O)(c3c4c(c(C(=O)OCC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c4c(c(C(=O)OCC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2
C(C)(C)(C)[Li].CN(C)CCN(C)C.CC1(SC2=C(S1)C(=C1C(SC(S1)(C)C)=C2)C(O)(C2=C1C(OC(O1)(C)C)=CC1=C2OC(O1)(C)C)C1=C2C(SC(S2)(C)C)=CC2=C1SC(S2)(C)C)C.C(OCC)(OCC)=O>>C(C)OC(=O)C1=C2SC(SC2=C(C=2SC(SC21)(C)C)C(O)(C2=C1C(OC(O1)(C)C)=C(C1=C2OC(O1)(C)C)C(=O)OCC)C1=C2C(SC(S2)(C)C)=C(C2=C1SC(S2)(C)C)C(=O)OCC)(C)C
C[C:40]1([CH3:41])[O:5][c:54]2[c:9]([C:10]([OH:11])([c:12]3[c:13]4[c:14]([cH:15][c:21]5[c:22]3[S:23][C:24]([CH3:25])([CH3:26])[S:27]5)[S:28][C:29]([CH3:30])([CH3:31])[S:32]4)[c:33]3[c:34]4[c:35]([cH:36][c:42]5[c:43]3[S:44][C:45]([CH3:46])([CH3:47])[S:48]5)[S:49][C:50]([CH3:51])([CH3:52])[S:53]4)[c:8]3[c:7]([cH:6][c:37]...
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3.CCOC(=O)OCC.CN(C)CCN(C)C.[Li][C](C)(C)C
CCOC(=O)c1c2c(c(C(O)(c3c4c(c(C(=O)OCC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c4c(c(C(=O)OCC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2
null
null
C1=CC=CC=C1
Acylation
OtherReaction
5fcb5e4cfee0f50a20faa57213b39d23f0a1ab10fa059a32f7eaeddb4458f2f7
6a804c132f059daed8d566da6ea8362db9e5aae9e5436ad52cf3e05a9944fcad
c1c2c(c(C(c3c4c(cc5c3SCS5)SCS4)c3c4c(cc5c3SCS5)SCS4)c3c1OCO3)OCO2
C-N(-C)-C-C-N(-C)-[CH3;D1;+0:1].C-[C;H0;D4;+0:2]1(-[C;D1;H3:3])-[#8:4]-[c;H0;D3;+0:5]2:[cH;D2;+0:6]:[c:7]3:[c:8](:[c:9](-[C:10]):[c;H0;D3;+0:11]:2-[O;H0;D2;+0:12]-1)-[#8:13]-[C:14]-[#8:15]-3.[#16:16]1-[C:17]-[#16:18]-[c:19](:[c:20]-1):[cH;D2;+0:21]:[c:22]1:[c:23]-[#16:24]-[C:25]-[#16:26]-1.[#16:27]1-[C:28]-[#16:29]-[c:...
null
[]
null
null
1.5
HOUR
Bis-(2,2,6,6-tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dithiole-4-yl)-mono-(2,2,6,6-tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dioxol-4-yl)methanol (0.50 g, 0.61 mmol) was dissolved in dry benzene (6.0 mL) under an atmosphere of argon. t-Butyllitium (2.44 mL, 1.5M in pentane) and TMEDA (0.545 mL, 3.66 mmol) were added. The re...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester.Ether.Ether.Tertiary amine.Tertiary amine.Alkyl lithium
Ester.Ester.Ester.Ether.Ether
c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
Li
C1=CC=CC=C1
null
1.5
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3.CCOC(=O)OCC.CN(C)CCN(C)C.[Li][C](C)(C)C>C1=CC=CC=C1>CCOC(=O)c1c2c(c(C(O)(c3c4c(c(C(=O)OCC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c4c(c(C(=O)OCC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-20a28c547f764190864154877d314000
CC1(C)Sc2cc3c(cc2S1)SC(C)(C)S3.CI.O=C=O>>COC(=O)c1c2c(cc3c1SC(C)(C)S3)SC(C)(C)S2
C(=O)=O.CI.C([O-])([O-])=O.[K+].[K+].C(CCC)[Li].CC1(SC2=C(S1)C=C1C(SC(S1)(C)C)=C2)C>>COC(=O)C1=C2C(SC(S2)(C)C)=CC2=C1SC(S2)(C)C
[cH:5]1[c:7]2[c:6]([cH:8][c:9]3[c:10]1[S:11][C:12]([CH3:13])([CH3:14])[S:15]3)[S:20][C:17]([CH3:18])([CH3:19])[S:16]2.I[CH3:1].[O:2]=[C:3]=[O:4]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]2[c:7]([cH:8][c:9]3[c:10]1[S:11][C:12]([CH3:13])([CH3:14])[S:15]3)[S:16][C:17]([CH3:18])([CH3:19])[S:20]2
CC1(C)Sc2cc3c(cc2S1)SC(C)(C)S3.CI.O=C=O
COC(=O)c1c2c(cc3c1SC(C)(C)S3)SC(C)(C)S2
null
null
CN(C)C=O.CCOCC
Acylation
OtherReaction
2ac4ae5ad8e7f510ba480690120240df76ffe7841789a7c2d284c6c1b9c4fea5
c0da44b11e2071417522771b259351ca8046db346df1eea32c3b5ee03a22b629
c1c2c(cc3c1SCS3)SCS2
I-[CH3;D1;+0:1].[#16:2]1-[C:3]-[#16:4]-[c:5]2:[cH;D2;+0:6]:[c;H0;D3;+0:7]3:[c;H0;D3;+0:8](:[cH;D2;+0:9]:[c:10]:2-1)-[#16:11]-[C:12]-[#16:13]-3.[O;D1;H0:14]=[C;H0;D2;+0:15]=[O;H0;D1;+0:16]>>[CH3;D1;+0:1]-[O;H0;D2;+0:16]-[C;H0;D3;+0:15](=[O;D1;H0:14])-[c;H0;D3;+0:9]1:[c:10]2:[c:5](:[cH;D2;+0:6]:[c;H0;D3;+0:8]3:[c;H0;D3;+...
null
[]
null
null
30
MINUTE
2,2,6,6-Tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dithiole (2.0 g, 6.98 mmol) was dissolved in dry ether (50.0 mL) in a dry, argon filled reaction flask. n-Butyllithium (3.07 mL, 2.5M in hexane) was added and the reaction mixture was stirred for 30 min. The solution was poured onto solid carbon dioxide and, after stirring...
10.6084/m9.figshare.5104873.v1
null
Monosulfide.Monosulfide.Carbon dioxide
Ester.Monosulfide.Monosulfide
c1c2c(cc3c1SCS3)SCS2
c1c2c(cc3c1SCS3)SCS2
c1c2c(cc3c1SCS3)SCS2
HI
CN(C)C=O.CCOCC
null
0.5
CC1(C)Sc2cc3c(cc2S1)SC(C)(C)S3.CI.O=C=O>CN(C)C=O.CCOCC>COC(=O)c1c2c(cc3c1SC(C)(C)S3)SC(C)(C)S2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-760fc340b5b24bef86b0fc2c43979b8e
CC1(C)Oc2cc3c(cc2O1)OC(C)(C)O3.COC(=O)c1c2c(cc3c1SC(C)(C)S3)SC(C)(C)S2.O.[Li][CH2]CCC>>CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4OC(C)(C)O6)OC(C)(C)O5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3
C(CCC)[Li].CC1(OC2=C(O1)C=C1C(OC(O1)(C)C)=C2)C.O.COC(=O)C1=C2C(SC(S2)(C)C)=CC2=C1SC(S2)(C)C>>CC1(OC2=C(O1)C(=C1C(OC(O1)(C)C)=C2)C(O)(C2=C1C(SC(S1)(C)C)=CC1=C2SC(S1)(C)C)C1=C2C(OC(O2)(C)C)=CC2=C1OC(O2)(C)C)C
[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[cH:6][c:7]3[c:8]([cH:9][c:44]2[O:45]1)[O:23][C:24]([CH3:25])([CH3:26])[O:50]3.[C:10](=[O:11])([c:12]1[c:13]2[c:30]([cH:31][c:32]3[c:33]1[S:34][C:35]([CH3:29])([CH3:36])[S:38]3)[S:39][C:40]([CH3:28])([CH3:41])[S:43]2)[O:18][CH3:19].[OH2:22].[Li][CH2:14][CH2:16][CH2:17][CH3:20]>>[CH3:1][...
CC1(C)Oc2cc3c(cc2O1)OC(C)(C)O3.COC(=O)c1c2c(cc3c1SC(C)(C)S3)SC(C)(C)S2.O.[Li][CH2]CCC
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4OC(C)(C)O6)OC(C)(C)O5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3
null
null
CCOCC
Aromatic Heterocycle Formation
OtherReaction
3c9731cefac7ec6dac7be3711a5cf7750a2196eba6b63fa29411637f97d9f49c
fcf18322b4fb6ad88995c1972b82afb060297e4ba9bf7c0f58733510d9731900
c1c2c(c(C(c3c4c(cc5c3OCO5)OCO4)c3c4c(cc5c3SCS5)SCS4)c3c1OCO3)OCO2
[C;D1;H3:1]-[C;H0;D4;+0:2]1(-[C;D1;H3:3])-[O;H0;D2;+0:4]-[c;H0;D3;+0:5]2:[cH;D2;+0:6]:[c:7]3:[c:8](:[c:9]:[c:10]:2-[O;H0;D2;+0:11]-1)-[#8:12]-[C:13]-[#8:14]-3.[C;D1;H3:15]-[C;H0;D4;+0:16]1(-[CH3;D1;+0:17])-[#16:18]-[c;H0;D3;+0:19]2:[c:20](:[c:21]:[c;H0;D3;+0:22]3:[c;H0;D3;+0:23](:[c;H0;D3;+0:24]:2-[C;H0;D3;+0:25](=[O;H...
null
[]
0
CELSIUS
15
MINUTE
2,2,6,6-Tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dioxole (5.15 g, 23.2 mmol) was dissolved in dry ether (40.0 mL) in a dried, argon filled reaction vessel. The solution was cooled to 0° C. and n-butyllithium (9.29 mL, 2.5M in hexane) was added. After stirring for 15 min at ambient temperature, the mixture was cooled to 0...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Ether.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Alkyl lithium
Ether.Ether.Ether.Ether.Ether.Ether.Tertiary alcohol.Monosulfide.Monosulfide.Monosulfide.Monosulfide
c1c2c(cc3c1OCO3)OCO2.c1c2c(cc3c1SCS3)SCS2
c1c2c(cc3c1OCO3)OCO2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1OCO3)OCO2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
Li
CCOCC
0
0.25
CC1(C)Oc2cc3c(cc2O1)OC(C)(C)O3.COC(=O)c1c2c(cc3c1SC(C)(C)S3)SC(C)(C)S2.O.[Li][CH2]CCC>CCOCC>CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4OC(C)(C)O6)OC(C)(C)O5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c35abaa1aed4412e96a4c1b72c7b8021
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4OC(C)(C)O6)OC(C)(C)O5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3.CN(C)CCN(C)C.O=C=O>>CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)O)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)O)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c(c2C(=O)O)OC(C)(C)O3)O1
C(=O)=O.CN(C)CCN(C)C.C(C)(C)(C)[Li].CC1(OC2=C(O1)C(=C1C(OC(O1)(C)C)=C2)C(O)(C2=C1C(SC(S1)(C)C)=CC1=C2SC(S1)(C)C)C1=C2C(OC(O2)(C)C)=CC2=C1OC(O2)(C)C)C>>C(=O)(O)C1=C2OC(OC2=C(C=2OC(OC21)(C)C)C(O)(C2=C1C(SC(S1)(C)C)=C(C1=C2SC(S1)(C)C)C(=O)O)C1=C2C(OC(O2)(C)C)=C(C2=C1OC(O2)(C)C)C(=O)O)(C)C
[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([c:7]([C:8]([OH:9])([c:10]3[c:11]4[c:12]([cH:13][c:17]5[c:18]3[O:19][C:20]([CH3:21])([CH3:22])[O:23]5)[O:24][C:25]([CH3:26])([CH3:27])[O:28]4)[c:29]3[c:30]4[c:31]([cH:32][c:36]5[c:37]3[S:38][C:39]([CH3:40])([CH3:41])[S:42]5)[S:43][C:44]([CH3:45])([CH3:46])[S:47]4)[c:49]3[c:48]([cH...
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4OC(C)(C)O6)OC(C)(C)O5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3.CN(C)CCN(C)C.O=C=O
CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)O)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)O)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c(c2C(=O)O)OC(C)(C)O3)O1
null
null
CCOCC.C1CCCCC1
Acylation
OtherReaction
e74a997982e87f10791fe4f45689589c2ddca68356fd6979f0c8c39fdbbfedde
cbf0082711680dd33e04480d9b3cd8c3c0149eebf11600a58f74f5586b00ceaa
c1c2c(c(C(c3c4c(cc5c3OCO5)OCO4)c3c4c(cc5c3SCS5)SCS4)c3c1OCO3)OCO2
C-N(-C)-C-C-N(-C)-[CH3;D1;+0:1].[O;D1;H1:2]-[C:3](-[c:4]1:[c:5]2:[c:6](:[cH;D2;+0:7]:[c:8]3:[c:9]:1-[#8:10]-[C:11]-[#8:12]-3)-[#8:13]-[C:14]-[#8:15]-2)(-[c:16]1:[c:17]2:[c:18](:[cH;D2;+0:19]:[c:20]3:[c:21]:1-[#16:22]-[C:23]-[#16:24]-3)-[#16:25]-[C:26]-[#16:27]-2)-[c;H0;D3;+0:28]1:[c:29]2:[c:30](:[cH;D2;+0:31]:[c;H0;D3;...
null
[]
null
null
20
MINUTE
Dry TMEDA (1.21 mL, 8.04 mmol) and t-butyllithium (5.36 mL, 1.5M in pentane) were dissolved in dry cyclohexane (12 mL) at 0° C. Bis-(2,2,6,6-tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dioxol-4-yl)-mono-(2,2,6,6-tetramethyl benzo[1,2-d:4,5-d']-bis(1,3)dithiol-4-yl)methanol (0.608 g, 0.804 mmol) was then added at ambient tem...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amine.Tertiary amine.Carbon dioxide
Carboxylic acid.Carboxylic acid.Carboxylic acid.Ether.Ether
c1c2c(cc3c1OCO3)OCO2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1OCO3)OCO2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
c1c2c(cc3c1OCO3)OCO2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
Other
CCOCC.C1CCCCC1
null
0.333333
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4OC(C)(C)O6)OC(C)(C)O5)c4c5c(cc6c4SC(C)(C)S6)SC(C)(C)S5)c2O1)OC(C)(C)O3.CN(C)CCN(C)C.O=C=O>CCOCC.C1CCCCC1>CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)O)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)O)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c(c2C(=O)O)OC(C)(C)O3)O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-71815a1699b6445f9f96283c7d73efe0
COC(=O)c1c2c(c(C(O)(c3c4c(c(C(=O)OC)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)OC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2>>COC(=O)c1c2c(c(C(c3c4c(c(C(=O)OC)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)OC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2
COC(=O)C1=C2OC(OC2=C(C=2OC(OC21)(C)C)C(O)(C2=C1C(SC(S1)(C)C)=C(C1=C2SC(S1)(C)C)C(=O)OC)C1=C2C(OC(O2)(C)C)=C(C2=C1OC(O2)(C)C)C(=O)OC)(C)C.B(F)(F)F.CCOCC.[Sn](Cl)Cl>>COC(=O)C1=C2OC(OC2=C(C=2OC(OC21)(C)C)C(C2=C1C(SC(S1)(C)C)=C(C1=C2SC(S1)(C)C)C(=O)OC)C1=C2C(OC(O2)(C)C)=C(C2=C1OC(O2)(C)C)C(=O)OC)(C)C
O[C:9]([c:8]1[c:7]2[c:6]([c:5]([C:3]([O:2][CH3:1])=[O:4])[c:51]3[c:50]1[O:56][C:53]([CH3:54])([CH3:55])[O:52]3)[O:61][C:58]([CH3:59])([CH3:60])[O:57]2)([c:10]1[c:11]2[c:12]([c:13]([C:14](=[O:15])[O:16][CH3:17])[c:18]3[c:19]1[O:20][C:21]([CH3:22])([CH3:23])[O:24]3)[O:25][C:26]([CH3:27])([CH3:28])[O:29]2)[c:30]1[c:31]2[c...
COC(=O)c1c2c(c(C(O)(c3c4c(c(C(=O)OC)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)OC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2
COC(=O)c1c2c(c(C(c3c4c(c(C(=O)OC)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)OC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2
null
[Zn]
null
Reduction
OtherReaction
c74e766e62dea6513290ab98d06521c92685074430a200193315f473ed0037ec
dfa71f841ee148297c95b5d95b7150768ab9356304fca8dbfde20c6dadd639d3
c1c2c(c(C(c3c4c(cc5c3OCO5)OCO4)c3c4c(cc5c3SCS5)SCS4)c3c1OCO3)OCO2
O-[C;H0;D4;+0:1](-[c:2](:[c:3]-[#8:4]):[c:5]-[#8:6])(-[c:7](:[c:8]-[#16:9]):[c:10]-[#16:11])-[c:12](:[c:13]-[#8:14]):[c:15]-[#8:16]>>[#16:11]-[c:10]:[c:7](-[CH;D3;+0:1](-[c:2](:[c:3]-[#8:4]):[c:5]-[#8:6])-[c:12](:[c:13]-[#8:14]):[c:15]-[#8:16]):[c:8]-[#16:9]
null
[]
null
null
null
null
Bis-(8-methoxycarbonyl-2,2,6,6-tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dioxol-4-yl)-mono-(8-methoxycarbonyl-2,2,6,6-tetramethylbenzo[1,2-d:4,5-d']-bis(1,3)dithiol-4-yl)methanol (5 mg, 0.005 mmol) was dissolved in dry, degassed acetonitrile under an argon atmosphere. BF3.Et2O (2.0 μL, 0.011 mmol) and tin(II) chloride (3....
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
null
null
null
c1c2c(cc3c1OCO3)OCO2.c1c2c(cc3c1SCS3)SCS2.c1c2c(cc3c1OCO3)OCO2
Other
[Zn]
null
null
COC(=O)c1c2c(c(C(O)(c3c4c(c(C(=O)OC)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)OC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2>[Zn]>COC(=O)c1c2c(c(C(c3c4c(c(C(=O)OC)c5c3OC(C)(C)O5)OC(C)(C)O4)c3c4c(c(C(=O)OC)c5c3SC(C)(C)S5)SC(C)(C)S4)c3c1OC(C)(C)O3)OC(C)(C)O2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8a6d6748b1df4808a57a14672a9c86dc
CC(=O)OCC1(COC(C)=O)Sc2cc3c(cc2S1)SC(COC(C)=O)(COC(C)=O)S3>>OCC1(CO)Sc2cc3c(cc2S1)SC(CO)(CO)S3
C(C)(=O)OCC1(SC2=C(S1)C=C1C(SC(S1)(COC(C)=O)COC(C)=O)=C2)COC(C)=O.C(=O)([O-])[O-].[K+].[K+]>>OCC1(SC2=C(S1)C=C1C(SC(S1)(CO)CO)=C2)CO
CC(=O)[O:1][CH2:2][C:3]1([CH2:4][O:5]C(C)=O)[S:6][c:7]2[cH:8][c:9]3[c:10]([cH:11][c:12]2[S:13]1)[S:14][C:15]([CH2:16][O:17]C(C)=O)([CH2:18][O:19]C(C)=O)[S:20]3>>[OH:1][CH2:2][C:3]1([CH2:4][OH:5])[S:6][c:7]2[cH:8][c:9]3[c:10]([cH:11][c:12]2[S:13]1)[S:14][C:15]([CH2:16][OH:17])([CH2:18][OH:19])[S:20]3
CC(=O)OCC1(COC(C)=O)Sc2cc3c(cc2S1)SC(COC(C)=O)(COC(C)=O)S3
OCC1(CO)Sc2cc3c(cc2S1)SC(CO)(CO)S3
null
null
CO
Reduction
OtherReaction
73cc08f15920db4ea0923c3b24e1a4c6d7380b91c4b3106d69889f1d89e036a6
db6f6d98b99f51adabbd240fbce698bfbe6fd62e873120ade7beae025e5657bb
c1c2c(cc3c1SCS3)SCS2
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3](-[C:4]-[O;H0;D2;+0:5]-C(-C)=O)(-[#16:6])-[#16:7].C-C(=O)-[O;H0;D2;+0:8]-[C:9]-[C:10](-[C:11]-[O;H0;D2;+0:12]-C(-C)=O)(-[#16:13])-[#16:14]>>[#16:13]-[C:10](-[C:9]-[OH;D1;+0:8])(-[C:11]-[OH;D1;+0:12])-[#16:14].[#16:6]-[C:3](-[C:2]-[OH;D1;+0:1])(-[C:4]-[OH;D1;+0:5])-[#16:7]
null
[]
null
null
null
null
2,2,6,6-Tetra(acetoxymethyl)benzo[1,2-d:4,5-d']bis(1,3)dithiole (1.8 g, 3.5 mmol) and K2CO3 (1.9 g) were stirred in methanol (100 mL) for 1 h at ambient temperature. The solvent was evaporated and water (100 mL) was added. The mixture was neutralized (2M HCl) and the precipitate was collected. Conditions: See reaction....
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester
Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol
null
null
c1c2c(cc3c1SCS3)SCS2
HO-
CO
null
null
CC(=O)OCC1(COC(C)=O)Sc2cc3c(cc2S1)SC(COC(C)=O)(COC(C)=O)S3>CO>OCC1(CO)Sc2cc3c(cc2S1)SC(CO)(CO)S3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3fd18c20fe384f209c75449594a77dfc
CC1(C)Oc2cc3c(cc2S1)SC(C)(C)O3.C[Si](C)(C)Cl>>CC1(C)Oc2c(cc3c(c2[Si](C)(C)C)OC(C)(C)S3)S1
CC1(OC=2C(S1)=CC=1SC(OC1C2)(C)C)C.C(CCC)[Li].Cl[Si](C)(C)C>>C[Si](C1=C2C(SC(O2)(C)C)=CC=2SC(OC21)(C)C)(C)C
[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([cH:7][c:8]3[c:9]([cH:10]2)[O:15][C:16]([CH3:17])([CH3:18])[S:19]3)[S:20]1.Cl[Si:11]([CH3:12])([CH3:13])[CH3:14]>>[CH3:1][C:2]1([CH3:3])[O:4][c:5]2[c:6]([cH:7][c:8]3[c:9]([c:10]2[Si:11]([CH3:12])([CH3:13])[CH3:14])[O:15][C:16]([CH3:17])([CH3:18])[S:19]3)[S:20]1
CC1(C)Oc2cc3c(cc2S1)SC(C)(C)O3.C[Si](C)(C)Cl
CC1(C)Oc2c(cc3c(c2[Si](C)(C)C)OC(C)(C)S3)S1
null
null
C1CCOC1
Functional Group Interconversion
OtherReaction
4d920506285c00399efb181b4ec00c0f33dc1bce9f2dbd24ac119a8845500b75
62b25486659a0c3b8981491307676661488416039e4a601c8996c7216be92cf1
c1c2c(cc3c1OCS3)SCO2
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4].[#16:5]1-[C:6]-[#8:7]-[c:8](:[c:9]-1):[cH;D2;+0:10]:[c:11]1:[c:12]-[#16:13]-[C:14]-[#8:15]-1>>[C;D1;H3:2]-[Si;H0;D4;+0:1](-[C;D1;H3:3])(-[C;D1;H3:4])-[c;H0;D3;+0:10](:[c:11]1:[c:12]-[#16:13]-[C:14]-[#8:15]-1):[c:8]1:[c:9]-[#16:5]-[C:6]-[#8:7]-1
null
[]
null
null
15
MINUTE
The reaction was performed under an argon atmosphere using deoxygenated solvents. 2,2,6,6-tetramethylbenzo[1,2-d:5,4-d']-bis(1,3)oxathiole (6.0 g, 23.6 mmol) was dissolved in dry THF (120 mL). The mixture was cooled on an ice-bath and n-butyllithium (10.8 mL, 2.5M in hexane) was added dropwise over 10 min. After 15 min...
10.6084/m9.figshare.5104873.v1
null
Silyl protective group
Silyl protective group
c1c2c(cc3c1OCS3)SCO2
c1c2c(cc3c1OCS3)SCO2
c1c2c(cc3c1OCS3)SCO2
HCl
C1CCOC1
null
0.25
CC1(C)Oc2cc3c(cc2S1)SC(C)(C)O3.C[Si](C)(C)Cl>C1CCOC1>CC1(C)Oc2c(cc3c(c2[Si](C)(C)C)OC(C)(C)S3)S1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3f677304111d45a7802ed37ac3c6141c
CC1(C)Oc2c(c(C(O)(c3c4c(c([Si](C)(C)C)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c([Si](C)(C)C)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2[Si](C)(C)C)OC(C)(C)S3)S1>>CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)O6)OC(C)(C)S5)c4c5c(cc6c4SC(C)(C)O6)OC(C)(C)S5)c2S1)SC(C)(C)O3
C(=O)(O)[O-].[Na+].[I-].[Na+].Cl[Si](C)(C)C.C[Si](C1=C2C(SC(O2)(C)C)=C(C=2SC(OC21)(C)C)C(O)(C2=C1SC(OC1=C(C1=C2SC(O1)(C)C)[Si](C)(C)C)(C)C)C1=C2SC(OC2=C(C2=C1SC(O2)(C)C)[Si](C)(C)C)(C)C)(C)C>>CC1(OC=2C(S1)=C(C=1SC(OC1C2)(C)C)C(O)(C2=C1SC(OC1=CC1=C2SC(O1)(C)C)(C)C)C1=C2SC(OC2=CC2=C1SC(O2)(C)C)(C)C)C
C[Si](C)(C)[c:6]1[c:5]2[c:44]([c:9]([C:10]([OH:11])([c:12]3[c:13]4[c:14]([c:15]([Si](C)(C)C)[c:16]5[c:17]3[S:18][C:19]([CH3:20])([CH3:21])[O:22]5)[O:23][C:24]([CH3:25])([CH3:26])[S:27]4)[c:28]3[c:29]4[c:30]([c:31]([Si](C)(C)C)[c:32]5[c:33]3[S:34][C:35]([CH3:36])([CH3:37])[O:38]5)[O:39][C:40]([CH3:41])([CH3:42])[S:43]4)...
CC1(C)Oc2c(c(C(O)(c3c4c(c([Si](C)(C)C)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c([Si](C)(C)C)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2[Si](C)(C)C)OC(C)(C)S3)S1
CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)O6)OC(C)(C)S5)c4c5c(cc6c4SC(C)(C)O6)OC(C)(C)S5)c2S1)SC(C)(C)O3
null
null
C(C)#N
Miscellaneous
OtherReaction
afe9566dd4aa30908e30516c808e43d3b8eee858237c95b927f53c5eda9e4b43
f3322e71c3e92cdc73f7ed164c490ee5862b18cfe67e54f1ba9ef731a52db4b7
c1c2c(c(C(c3c4c(cc5c3SCO5)OCS4)c3c4c(cc5c3SCO5)OCS4)c3c1OCS3)SCO2
C-[Si](-C)(-C)-[c;H0;D3;+0:1](:[c:2]1:[c:3]-[#16:4]-[C:5]-[#8:6]-1):[c:7]1:[c:8]-[#16:9]-[C:10]-[#8:11]-1.C-[Si](-C)(-C)-[c;H0;D3;+0:12](:[c:13]1:[c:14]-[#16:15]-[C:16]-[#8:17]-1):[c:18]1:[c:19]-[#16:20]-[C:21]-[#8:22]-1.C-[Si](-C)(-C)-[c;H0;D3;+0:23](:[c:24]1:[c:25]-[#16:26]-[C:27]-[#8:28]-1):[c:29]1:[c:30]-[#16:31]-[...
null
[]
null
null
20
MINUTE
Tris-(8-trimethylsilyl-2,2,6,6-tetramethylbenzo[1,2-d:5,4-d']-bis(1,3)oxathiol-4-yl)methanol (0.62 g, 0.62 mmol) was dissolved in acetonitrile (150 mL). Sodium iodide (0.75 g, 6.0 mmol) and chlorotrimethylsilane (0.65 g, 6.0 mmol) was added in one portion. The mixture was stirred for 20 min and then poured onto diethyl...
10.6084/m9.figshare.5104873.v1
null
Silyl protective group.Silyl protective group.Silyl protective group
null
c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2
c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2
c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2
Other
C(C)#N
null
0.333333
CC1(C)Oc2c(c(C(O)(c3c4c(c([Si](C)(C)C)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c([Si](C)(C)C)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2[Si](C)(C)C)OC(C)(C)S3)S1>C(C)#N>CC1(C)Oc2cc3c(c(C(O)(c4c5c(cc6c4SC(C)(C)O6)OC(C)(C)S5)c4c5c(cc6c4SC(C)(C)O6)OC(C)(C)S5)c2S1)SC(C)(C)O3
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9d46f1258cf4095bcf66afa8b7bb539
CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)Cl)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c(C(=O)Cl)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2C(=O)Cl)OC(C)(C)S3)S1.OCCNCCO>>CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)N(CCO)CCO)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c(C(=O)N(CCO)CCO)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2C(=O)N(CCO)CCO)OC(C)(C)S3)S1
ClC(=O)C1=C2C(SC(O2)(C)C)=C(C=2SC(OC21)(C)C)C(O)(C2=C1SC(OC1=C(C1=C2SC(O1)(C)C)C(=O)Cl)(C)C)C1=C2SC(OC2=C(C2=C1SC(O2)(C)C)C(=O)Cl)(C)C.OCCNCCO>>OCCN(C(=O)C1=C2C(SC(O2)(C)C)=C(C=2SC(OC21)(C)C)C(O)(C2=C1SC(OC1=C(C1=C2SC(O1)(C)C)C(=O)N(CCO)CCO)(C)C)C1=C2SC(OC2=C(C2=C1SC(O2)(C)C)C(=O)N(CCO)CCO)(C)C)CCO
Cl[C:14]([c:13]1[c:12]2[c:11]([c:10]([C:8]([c:7]3[c:6]4[c:5]([c:62]([C:63](Cl)=[O:64])[c:61]5[c:60]3[S:76][C:73]([CH3:74])([CH3:75])[O:72]5)[O:4][C:2]([CH3:3])([CH3:42])[S:77]4)([OH:9])[c:35]3[c:36]4[c:37]([c:38]([C:39](Cl)=[O:40])[c:48]5[c:49]3[S:50][C:51]([CH3:1])([CH3:21])[O:54]5)[O:55][C:56]([CH3:57])([CH3:58])[S:5...
CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)Cl)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c(C(=O)Cl)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2C(=O)Cl)OC(C)(C)S3)S1.OCCNCCO
CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)N(CCO)CCO)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c(C(=O)N(CCO)CCO)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2C(=O)N(CCO)CCO)OC(C)(C)S3)S1
null
null
C1=CC=CC=C1.O
Acylation
OtherReaction
d2ac129f39631fe97b426d032dbc96ae91fd7b43567819c49127adcf67e2462c
d83b6db80199c7edcb8f196b1f0ce5b10cd1c761c76ee97e489bb5b2ef866b36
c1c2c(c(C(c3c4c(cc5c3SCO5)OCS4)c3c4c(cc5c3SCO5)OCS4)c3c1OCS3)SCO2
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]-[#8:5]):[c:6]-[#8:7].Cl-[C;H0;D3;+0:8](=[O;D1;H0:9])-[c:10](:[c:11]-[#8:12]):[c:13]1:[c:14]-[#16:15]-[C;H0;D4;+0:16](-[C;D1;H3:17])(-[CH3;D1;+0:18])-[#8:19]-1.Cl-[C;H0;D3;+0:20](=[O;D1;H0:21])-[c:22](:[c:23]-[#8:24]):[c:25]1:[c:26]-[#16:27]-[C;H0;D4;+0:28](-[CH3;D1;+0:29])(-...
63.4
[{"value": 60.0, "product": "OCCN(C(=O)C1=C2C(SC(O2)(C)C)=C(C=2SC(OC21)(C)C)C(O)(C2=C1SC(OC1=C(C1=C2SC(O1)(C)C)C(=O)N(CCO)CCO)(C)C)C1=C2SC(OC2=C(C2=C1SC(O2)(C)C)C(=O)N(CCO)CCO)(C)C)CCO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.4, "product": "OCCN(C(=O)C1=C2C(SC(O2)(C)C)=C(C=2SC(OC21)(C)C)C(O)(C2=C...
null
null
8
HOUR
Tris-(8-chlorocarbonyl-2,2,6,6-tetramethyl-benzo[1,2-d:5,4-d']-bis(1,3)oxathiol-4-yl)methanol (0.80 g, 0.80 mmol) was dissolved in benzene (200 mL). A solution of of bis(2-hydroxyethyl)amine (8.0 g, 48 mmol) in water (200 mL) was added and after vigorous stirring overnight, the mixture was transferred to a separatory f...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Acyl halide.Ether.Ether.Secondary amine.Monosulfide.Monosulfide
Ether.Ether.Tertiary amide.Tertiary amide.Tertiary amide.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Monosulfide.Monosulfide
c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2
c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2
c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2.c1c2c(cc3c1OCS3)SCO2
null
C1=CC=CC=C1.O
null
8
CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)Cl)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c(C(=O)Cl)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2C(=O)Cl)OC(C)(C)S3)S1.OCCNCCO>C1=CC=CC=C1.O>CC1(C)Oc2c(c(C(O)(c3c4c(c(C(=O)N(CCO)CCO)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c4c(c(C(=O)N(CCO)CCO)c5c3SC(C)(C)O5)OC(C)(C)S4)c3c(c2C(=O)N(CCO)CCO)OC(C)(C)S3)S1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-98343e58e325465bbbaa7fdb2b6a1ac0
CC1(C)CCC(=O)c2cc(Br)ccc21.Cc1ccc(Br)cc1>>Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)cc1
BrC1=CC=C(C=C1)C.CC1(CCC(C2=CC(=CC=C12)Br)=O)C.CC1(CCC(C2=CC(=CC=C12)Br)=O)C>>C1(=CC=C(C=C1)C1=CCC(C2=CC=C(C=C12)Br)(C)C)C
O=[C:6]1[CH2:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]2[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]21.Br[c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:20][cH:19]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([C:6]2=[CH:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]3[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]32)[cH:19][cH:20]1
CC1(C)CCC(=O)c2cc(Br)ccc21.Cc1ccc(Br)cc1
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)cc1
null
null
C1CCOC1.C(C)OC(C)=O
C-C Coupling
OtherReaction
2fbbf41647a8c4f0278c25fbcfbace1cdbb174312495bfebc071a73b393e6788
554b1bee1ccf92984990164979ec7aaf354dc2a70796dc88c3036796633e99e1
C1=C(c2ccccc2)c2ccccc2CC1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].O=[C;H0;D3;+0:6]1-[CH2;D2;+0:7]-[C:8]-[C:9]-[c:10]:[c:11]-1:[c:12]>>[c:12]:[c:11]1:[c:10]-[C:9]-[C:8]-[CH;D2;+0:7]=[C;H0;D3;+0:6]-1-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
2
HOUR
To a mixture of Mg metal (650 mg, 27 mmol) in THF (20 mL) was added 4-bromotoluene (5.3 g, 31 mmol) in THF (40 mL). The mixture was stirred for 2 hours at ambient temperature and heated to 70° C. for 30 minutes. After cooling to ambient temperature, 3,4-dihydro-4,4-dimethyl-7-bromo-1(2H)-naphthalenone (Compound A) (2.1...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone
null
c1ccc2c(c1)CCCC2.c1ccccc1
c1ccccc1.C1=Cc2ccccc2CC1
c1ccccc1.C1=Cc2ccccc2CC1
HBr
C1CCOC1.C(C)OC(C)=O
null
2
CC1(C)CCC(=O)c2cc(Br)ccc21.Cc1ccc(Br)cc1>C1CCOC1.C(C)OC(C)=O>Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bf0cea00f0c14b87bedbeafd627d9061
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)cc1.O=C=O>>Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)cc1
C(=O)=O.[Li]C(C)(C)C.CCCCC.C1(=CC=C(C=C1)C1=CCC(C2=CC=C(C=C12)Br)(C)C)C.C1(=CC=C(C=C1)C1=CCC(C2=CC=C(C=C12)Br)(C)C)C.CN(C=O)C>>C1(=CC=C(C=C1)C1=CCC(C2=CC=C(C=C12)C=O)(C)C)C
Br[c:15]1[cH:14][cH:13][c:12]2[c:19]([cH:18]1)[C:6]([c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:21][cH:20]1)=[CH:7][CH2:8][C:9]2([CH3:10])[CH3:11].O=[C:16]=[O:17]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([C:6]2=[CH:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]3[cH:13][cH:14][c:15]([CH:16]=[O:17])[cH:18][c:19]32)[cH:20][cH:21]1
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)cc1.O=C=O
Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)cc1
null
null
C1CCOC1.C(C)OC(C)=O
C-C Coupling
OtherReaction
b4070cec8a084380200c9a64a85dcebfacf7487a23558ab094a57ef7a0675fac
c0100ab7b5bcec44798faf2d53320d9c2adb8a4e38bf9019653825fce736fb17
C1=C(c2ccccc2)c2ccccc2CC1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]-[C:6]=[C:7].O=[C;H0;D2;+0:8]=[O;D1;H0:9]>>[C:7]=[C:6]-[c:5]:[c:4]:[c;H0;D3;+0:1](-[CH;D2;+0:8]=[O;D1;H0:9]):[c:2]:[c:3]
null
[]
null
null
null
null
To a cold (-78° C.), stirred solution of 1-(tol-4-yl)3,4-dihydro-4,4-dimethyl-7-bromo-naphthalene (Compound B 1 g, 3.2 mmol), in THF (17 mL) was added t-BuLi in pentane (1.7M solution, 3 mL, 5.1 mmol). After 10 minutes dry dimethylformamide (DMF) (600 mg, 8 mmol) was added and the dry-ice cooling was replaced with ice-...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carbon dioxide
Aldehyde
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
c1ccccc1.C1=Cc2ccccc2CC1
Br-
C1CCOC1.C(C)OC(C)=O
null
null
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)cc1.O=C=O>C1CCOC1.C(C)OC(C)=O>Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1b0e8d298ae64c8b9df10e43febd3af1
CCOC(=O)c1ccc(CCC(OC)(OC)P(=O)(OCC)OCC)cc1.Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)cc1>>CCOC(=O)c1ccc(/C(=C/c2ccc3c(c2)C(c2ccc(C)cc2)=CCC3(C)C)CC(OC)OC)cc1
C(C)OP(=O)(OCC)C(CCC1=CC=C(C(=O)OCC)C=C1)(OC)OC.[Li]CCCC.CCCCCC.C1(=CC=C(C=C1)C1=CCC(C2=CC=C(C=C12)C=O)(C)C)C.C1(=CC=C(C=C1)C1=CCC(C2=CC=C(C=C12)C=O)(C)C)C>>COC(C/C(=C\C1=CC=C2C(CC=C(C2=C1)C1=CC=C(C=C1)C)(C)C)/C1=CC=C(C(=O)OCC)C=C1)OC
CCOP(=O)(OCC)[C:32]([CH2:31][CH2:10][c:9]1[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:38][cH:37]1)([O:33][CH3:34])[O:35][CH3:36].O=[CH:11][c:12]1[cH:13][cH:14][c:15]2[c:16]([cH:17]1)[C:18]([c:19]1[cH:20][cH:21][c:22]([CH3:23])[cH:24][cH:25]1)=[CH:26][CH2:27][C:28]2([CH3:29])[CH3:30]>>[CH3:1][CH2:2][O:3][C:4]...
CCOC(=O)c1ccc(CCC(OC)(OC)P(=O)(OCC)OCC)cc1.Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)cc1
CCOC(=O)c1ccc(/C(=C/c2ccc3c(c2)C(c2ccc(C)cc2)=CCC3(C)C)CC(OC)OC)cc1
null
null
C1CCOC1
C-C Coupling
OtherReaction
2b2f01a2a3c2f6ea43954e1fcfb38220499a98de93d92d3a033fa1127e06f89d
3598948eace7341b2f4800001ea9b7b5ac95eb54b4840cc8e83ad3a3413fcab8
C1=C(c2ccccc2)c2cc(/C=C/c3ccccc3)ccc2CC1
C-C-O-P(=O)(-O-C-C)-[C;H0;D4;+0:1](-[#8:2]-[C;D1;H3:3])(-[#8:4]-[C;D1;H3:5])-[C:6]-[CH2;D2;+0:7]-[c:8](:[c:9]):[c:10].O=[CH;D2;+0:11]-[c:12](:[c:13]):[c:14]>>[C;D1;H3:3]-[#8:2]-[CH;D3;+0:1](-[#8:4]-[C;D1;H3:5])-[C:6]/[C;H0;D3;+0:7](=[CH;D2;+0:11]\[c:12](:[c:13]):[c:14])-[c:8](:[c:9]):[c:10]
null
[]
null
null
1.5
HOUR
To a cold (-78° C.) solution of ethyl 4-(diethoxyphosphoryl-3,3-dimethoxypropyl)benzoate (Compound D, 350 mg, 0.9 mmol, available in accordance with EPO Application No. 0 210 929 published on Feb. 4, 1987), in THF (9 mL), was added n-BuLi in hexane (1.6M solution, 0.7 mL, 1.1 mmol). The mixture was stirred for 1.5 hour...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ether.Ether
Ether.Ether
null
null
c1ccccc1.c1ccccc1.C1=Cc2ccccc2CC1
HO-
C1CCOC1
null
1.5
CCOC(=O)c1ccc(CCC(OC)(OC)P(=O)(OCC)OCC)cc1.Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)cc1>C1CCOC1>CCOC(=O)c1ccc(/C(=C/c2ccc3c(c2)C(c2ccc(C)cc2)=CCC3(C)C)CC(OC)OC)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-da975157105744468fa3d3bb8edc1433
CCOC(=O)c1ccc(-c2cccc3cc4c(cc23)C(c2ccc(C)cc2)=CCC4(C)C)cc1>>Cc1ccc(C2=CCC(C)(C)c3cc4cccc(-c5ccc(C(=O)O)cc5)c4cc32)cc1
C1(=CC=C(C=C1)C1=CCC(C2=CC3=CC=CC(=C3C=C12)C1=CC=C(C(=O)OCC)C=C1)(C)C)C.C1(=CC=C(C=C1)C1=CCC(C2=CC3=CC=CC(=C3C=C12)C1=CC=C(C(=O)OCC)C=C1)(C)C)C.CO.[Li+].[OH-].Cl>>C1(=CC=C(C=C1)C1=CCC(C2=CC3=CC=CC(=C3C=C12)C1=CC=C(C(=O)O)C=C1)(C)C)C
CC[O:25][C:23]([c:22]1[cH:21][cH:20][c:19](-[c:18]2[cH:17][cH:16][cH:15][c:14]3[cH:13][c:12]4[c:30]([cH:29][c:28]32)[C:6]([c:5]2[cH:4][cH:3][c:2]([CH3:1])[cH:32][cH:31]2)=[CH:7][CH2:8][C:9]4([CH3:10])[CH3:11])[cH:27][cH:26]1)=[O:24]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([C:6]2=[CH:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]3[cH...
CCOC(=O)c1ccc(-c2cccc3cc4c(cc23)C(c2ccc(C)cc2)=CCC4(C)C)cc1
Cc1ccc(C2=CCC(C)(C)c3cc4cccc(-c5ccc(C(=O)O)cc5)c4cc32)cc1
null
null
CCOCC.C1CCOC1
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
C1=C(c2ccccc2)c2cc3c(-c4ccccc4)cccc3cc2CC1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
16
HOUR
To a degassed solution of ethyl 4-[1(tol-4-yl)3,4-dihydro-4,4-dimethyl-anthracen-8-yl]-benzoate (Compound 1, 35 mg, 0.08 mmol), in THF (1.5 mL) and MeOH (1.5 mL) was added LiOH (1M solution in water, 0.3 mL, 0.3 mmol). The mixture was stirred at ambient temperature for 16 hours, diluted with ether (60 mL). The mixture ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.C1=Cc2cc3ccccc3cc2CC1.c1ccccc1
Other
CCOCC.C1CCOC1
null
16
CCOC(=O)c1ccc(-c2cccc3cc4c(cc23)C(c2ccc(C)cc2)=CCC4(C)C)cc1>CCOCC.C1CCOC1>Cc1ccc(C2=CCC(C)(C)c3cc4cccc(-c5ccc(C(=O)O)cc5)c4cc32)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1181981a49704b02b7381620902d58eb
CC1(C)CCC(=O)c2cc(Br)ccc21.Cc1cccs1>>Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)s1
CC1(CCC(C2=CC(=CC=C12)Br)=O)C.CC1(CCC(C2=CC(=CC=C12)Br)=O)C.CC=1SC=CC1.[Li]CCCC>>CC1=CC=C(S1)C1=CCC(C2=CC=C(C=C12)Br)(C)C
O=[C:6]1[CH2:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]2[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]21.[CH3:1][c:2]1[cH:3][cH:4][cH:5][s:19]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([C:6]2=[CH:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]3[cH:13][cH:14][c:15]([Br:16])[cH:17][c:18]32)[s:19]1
CC1(C)CCC(=O)c2cc(Br)ccc21.Cc1cccs1
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)s1
null
null
CCOCC.C(C)OC(C)=O.C1CCOC1
C-C Coupling
OtherReaction
89330b8a34552186e5f49cfb277c70aa6a06cd6639f780a165e8aac713b088a2
06a42e352cf517302d592bf38a2fd11b220014e39071074dc7becb6ee0bee4b2
C1=C(c2cccs2)c2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[#16;a:8]1:[c:9]:[c:10]:[c:11]:[cH;D2;+0:12]:1>>[c:7]:[c:6]1:[c:5]-[C:4]-[C:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1]-1-[c;H0;D3;+0:12]1:[#16;a:8]:[c:9]:[c:10]:[c:11]:1
62.3
[{"value": 62.3, "product": "CC1=CC=C(S1)C1=CCC(C2=CC=C(C=C12)Br)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
1.5
HOUR
To a cold (-78° C.) solution of 2-methylthiophene (800 mg, 8.1 mmol) in THF (10 mL) was added n-BuLi (1.6M solution in hexane, 5 mL). The mixture was stirred for 1.5 hours and transferred to a cold (-78° C.) flask containing 3,4-dihydro-4,4-dimethyl-7-bromo-1(2H)-naphthalenone (Compound A, 1.63 g, 6.5 mmol), in THF (15...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
c1ccc2c(c1)CCCC2.c1ccsc1
c1ccsc1.C1=Cc2ccccc2CC1
c1ccsc1.C1=Cc2ccccc2CC1
HO-
CCOCC.C(C)OC(C)=O.C1CCOC1
0
1.5
CC1(C)CCC(=O)c2cc(Br)ccc21.Cc1cccs1>CCOCC.C(C)OC(C)=O.C1CCOC1>Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)s1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4955e9d4488f4c70a01e631513107eb7
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)s1.O=C=O>>Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)s1
CC1=CC=C(S1)C1=CCC(C2=CC=C(C=C12)Br)(C)C.CC1=CC=C(S1)C1=CCC(C2=CC=C(C=C12)Br)(C)C.[Li]C(C)(C)C.CCCCC.C(=O)=O.CN(C)C=O>>CC1=CC=C(S1)C1=CCC(C2=CC=C(C=C12)C=O)(C)C
Br[c:15]1[cH:14][cH:13][c:12]2[c:19]([cH:18]1)[C:6]([c:5]1[cH:4][cH:3][c:2]([CH3:1])[s:20]1)=[CH:7][CH2:8][C:9]2([CH3:10])[CH3:11].O=[C:16]=[O:17]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([C:6]2=[CH:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]3[cH:13][cH:14][c:15]([CH:16]=[O:17])[cH:18][c:19]32)[s:20]1
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)s1.O=C=O
Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)s1
null
null
C1CCOC1.CCOCC
C-C Coupling
OtherReaction
b4070cec8a084380200c9a64a85dcebfacf7487a23558ab094a57ef7a0675fac
c0100ab7b5bcec44798faf2d53320d9c2adb8a4e38bf9019653825fce736fb17
C1=C(c2cccs2)c2ccccc2CC1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]-[C:6]=[C:7].O=[C;H0;D2;+0:8]=[O;D1;H0:9]>>[C:7]=[C:6]-[c:5]:[c:4]:[c;H0;D3;+0:1](-[CH;D2;+0:8]=[O;D1;H0:9]):[c:2]:[c:3]
null
[]
null
null
15
MINUTE
To a cold (-78° C.) solution of 1-(5-methyl-thien-2-yl)-3,4-dihydro-4,4-dimethyl-7-bromo-naphthalene (Compound F, 1.35 g, 4.1 mmol), in THF (20 mL) was added t-BuLi in pentane (1.7M solution, 3.5 mL, 5.95 mmol). The reaction was stirred for 15 minutes and DMF (600 mg, 5.8 mmol) was added and dry-ice cooling was replace...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carbon dioxide
Aldehyde
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
c1ccsc1.C1=Cc2ccccc2CC1
Br-
C1CCOC1.CCOCC
null
0.25
Cc1ccc(C2=CCC(C)(C)c3ccc(Br)cc32)s1.O=C=O>C1CCOC1.CCOCC>Cc1ccc(C2=CCC(C)(C)c3ccc(C=O)cc32)s1