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large_stringlengths
36
36
reaction_smiles
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4
873
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19
1.07k
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14
3.37k
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1
581
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1
433
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634 values
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large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
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11 values
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346 values
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64
64
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64
64
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5
288
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large_stringlengths
24
2.64k
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float64
-0.8
90,205,160,000B
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large_stringlengths
2
864
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float64
-230
30.1k
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large_stringclasses
3 values
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float64
0
4k
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large_stringclasses
4 values
procedure_details
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1
23.6k
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96 values
doi
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functional_groups_reactants
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3
716
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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-bf981b58918d46a4bf6543e26edf77e6
CC1(C)CCC[C@H](N2C(=O)c3ccccc3C2=O)C(=O)N1.ClC(c1ccccc1)(c1ccccc1)c1ccccc1>>CC1(C)CCC[C@H](NC(c2ccccc2)(c2ccccc2)c2ccccc2)C(=O)N1
C1(=CC=CC=C1)C(Cl)(C1=CC=CC=C1)C1=CC=CC=C1.O.NN.C1(C=2C(C(N1[C@H]1CCCC(NC1=O)(C)C)=O)=CC=CC2)=O.C1(=CC=CC=C1)C(Cl)(C1=CC=CC=C1)C1=CC=CC=C1.C(C)N(CC)CC>>C1(=CC=CC=C1)C(C1=CC=CC=C1)(C1=CC=CC=C1)N[C@H]1CCCC(NC1=O)(C)C
O=C1c2ccccc2C(=O)[N:8]1[C@H:7]1[CH2:6][CH2:5][CH2:4][C:2]([CH3:1])([CH3:3])[NH:30][C:28]1=[O:29].Cl[C:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH2:6][C@H:7]([NH:8][C:9]([c:10]2[cH:11][cH:...
CC1(C)CCC[C@H](N2C(=O)c3ccccc3C2=O)C(=O)N1.ClC(c1ccccc1)(c1ccccc1)c1ccccc1
CC1(C)CCC[C@H](NC(c2ccccc2)(c2ccccc2)c2ccccc2)C(=O)N1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
a12cf7af8efc46e68d61b624fd0d279b6a62dfdd51fa9a2ebdb998fdcdd29be7
28b72e46db2638ded4e9272b0bcac45fdcf86b73ced593a7dbbac98cf9ed0efd
O=C1NCCCC[C@@H]1NC(c1ccccc1)(c1ccccc1)c1ccccc1
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=C1-[N;H0;D3;+0:11](-[C:12](-[C:13])-[C:14](=[O;D1;H0:15])-[#7:16]-[C:17])-C(=O)-c2:c:c:c:c:c:2-1>>[C:17]-[#7:16]-[C:14](=[O;D1;H0:15])-[C:12](-[NH;D2;+0:11]-[C;H0;D4;+0:1](-[c:2](:[c:3]):[c:4])(-[c:5](:[c:6]):[c:7])-[c:8](:[c:9]):[c:10...
null
[]
null
null
72
HOUR
Hydrazine monohydrate (4.59 ml., 94.6 mmol.) was added to a solution of (S)-hexahydro-6-phthalimido-2,2-dimethyl-2H-azepine-7-one [preparred as described in Example 66(e), 19.98 g., 68.76 mmol.] in methanol (250 ml.) at room temperature under argon. The resulting mixture was stirred for 72 hours then filtered to remove...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Substituted dicarboximide
Secondary amine
c1ccc2c(c1)C[NH]C2
null
C1CCCNCC1.c1ccccc1.c1ccccc1.c1ccccc1
HCl
CO
null
72
CC1(C)CCC[C@H](N2C(=O)c3ccccc3C2=O)C(=O)N1.ClC(c1ccccc1)(c1ccccc1)c1ccccc1>CO>CC1(C)CCC[C@H](NC(c2ccccc2)(c2ccccc2)c2ccccc2)C(=O)N1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fa67e58f427c410f88c862b2ce6dc73e
ClP(Cl)Cl.Oc1ccccc1-c1ccccc1O>>Clp1oc2ccccc2c2ccccc2o1
C=1(C(=CC=CC1)C=1C(=CC=CC1)O)O.P(Cl)(Cl)Cl>>P1(OC2=C(C=CC=C2)C2=C(C=CC=C2)O1)Cl
Cl[P:2](Cl)[Cl:1].[OH:3][c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1-[c:10]1[cH:11][cH:12][cH:13][cH:14][c:15]1[OH:16]>>[Cl:1][p:2]1[o:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[o:16]1
ClP(Cl)Cl.Oc1ccccc1-c1ccccc1O
Clp1oc2ccccc2c2ccccc2o1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
1388d467c73a45f8728568ec2382b0e62344af6950e7aad2f3a259e6a6f7af96
8a2ce476a1d993ef0eccc79c0116619b23ccd96544c672b2781b24ef0818f555
c1ccc2c(c1)o[pH]oc1ccccc12
Cl-[P;H0;D3;+0:1](-Cl)-[Cl;D1;H0:2].[OH;D1;+0:3]-[c:4](:[c:5]):[c;H0;D3;+0:6](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10](-[OH;D1;+0:11]):[c:12]):[c:13]:[c:14]>>[Cl;D1;H0:2]-[p;H0;D3;+0:1]1:[o;H0;D2;+0:3]:[c:4](:[c:5]):[c;H0;D3;+0:6](:[c:13]:[c:14]):[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10](:[c:12]):[o;H0;D2;+0:11]:1
81
[{"value": 81.0, "product": "P1(OC2=C(C=CC=C2)C2=C(C=CC=C2)O1)Cl", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2,2'-biphenol (28.1 g, 0.151 mol) in 49 mL phosphorus trichloride was heated at reflux for 2 hr. The excess PC13 was removed by distillation. The residue was purified by vacuum distillation (140°-143° C. at 0.5 mm Hg) to give 30.70 g (81% yield) 1,1'-biphenyl-2,2'-diyl phosphorochloridite (as a clear visc...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Aromatic alcohol
null
c1ccccc1.c1ccccc1
c1ccc2c(c1)opoc1ccccc12
c1ccc2c(c1)opoc1ccccc12
HCl
null
null
null
ClP(Cl)Cl.Oc1ccccc1-c1ccccc1O>>Clp1oc2ccccc2c2ccccc2o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-440b49e065434692a260e63870f36ce7
Fc1cc(Br)ccc1CBr.OCc1ccccc1>>O=C(NCc1ccc(Br)cc1F)OCc1ccccc1
C(C1=CC=CC=C1)O.O([K])C#N.BrC1=CC(=C(CBr)C=C1)F>>BrC1=CC(=C(CNC(OCC2=CC=CC=C2)=O)C=C1)F
Br[CH2:4][c:5]1[cH:6][cH:7][c:8]([Br:9])[cH:10][c:11]1[F:12].[OH:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[O:1]=[C:2]([NH:3][CH2:4][c:5]1[cH:6][cH:7][c:8]([Br:9])[cH:10][c:11]1[F:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
Fc1cc(Br)ccc1CBr.OCc1ccccc1
O=C(NCc1ccc(Br)cc1F)OCc1ccccc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
1c5f0b45e080118803b9e15ddb72c3da01ea2f14018cf1d8ca981d3ed00fe7f9
5e1dd53cff58b3c5481a3ca8392554a4f9cbbc0fad5e63854b46344482c9bd4c
O=C(NCc1ccccc1)OCc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[C:6]-[c:7]>>[O;D1;H0:8]=[C:9](-[#7:10]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[O;H0;D2;+0:5]-[C:6]-[c:7]
null
[]
110
CELSIUS
null
null
Anhydrous and amine-free DMF (180 ml) and benzyl alcohol (28 ml) and KOCN (0.247 mol, 20 g) are charged into a 500 ml 2-neck round bottom flask having a reflux condenser and drying tube. A solution of 4-bromo-2-fluorobenzyl bromide (0.075 mol, 20 g) in DMF (20 ml) is added rapidly (in the course of 1 min) at room tempe...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Carbamic ester.Ether
null
null
c1ccccc1.c1ccccc1
Br-
CN(C)C=O
110
null
Fc1cc(Br)ccc1CBr.OCc1ccccc1>CN(C)C=O>O=C(NCc1ccc(Br)cc1F)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-50401cea459a444786f5e8507d29997b
CCOC(=O)Cc1cccc(Br)c1>>O=CCc1cccc(Br)c1
[H-].C(C(C)C)[Al+]CC(C)C.[H][H].BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC=1C=C(C=CC1)CC(=O)OCC.BrC=1C=C(C=CC1)CC(=O)OCC>>BrC=1C=C(C=CC1)CC=O
CCO[C:2](=[O:1])[CH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([Br:9])[cH:10]1>>[O:1]=[CH:2][CH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([Br:9])[cH:10]1
CCOC(=O)Cc1cccc(Br)c1
O=CCc1cccc(Br)c1
null
null
null
Reduction
OtherReaction
ec1c6c64dd9be73981e5a6c952ab740869d298b20e87e097e88e1179cc5bc6dc
33ddc7b9457742ba0a376f08a972e4f33779267f6f1fe15e3be786427ae9f4ec
c1ccccc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]>>[O;D1;H0:2]=[CH;D2;+0:1]-[C:3]-[c:4]
null
[]
null
null
null
null
In the preferred compounds of the invention the two R1 substituents are methyl, and the R2 and R3 substituents are hydrogen. Reaction Scheme 4 illustrates a synthetic process for preparing 7-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1-one (Compound G) which serves as a starting material for the synthesis of several pref...
10.6084/m9.figshare.5104873.v1
null
Ester
Aldehyde
null
null
c1ccccc1
HO-
null
null
null
CCOC(=O)Cc1cccc(Br)c1>>O=CCc1cccc(Br)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-81448799139447a985ca454877c95d87
CCOC(=O)C=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=CCc1cccc(Br)c1>>CCOC(=O)CCCc1cccc(Br)c1
BrC=1C=C(C=CC1)CC=O.C(=O)(OCC)C=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>BrC=1C=C(C=CC1)CCCC(=O)OCC
c1ccc(P(c2ccccc2)(c2ccccc2)=[CH:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])cc1.O=[CH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]([Br:14])[cH:15]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]([Br:14])[cH:15]1
CCOC(=O)C=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=CCc1cccc(Br)c1
CCOC(=O)CCCc1cccc(Br)c1
null
null
null
C-C Coupling
OtherReaction
71bd2654cede51545adee465eb47bf49794d5c57afe21c7fb122478c5a700139
203dd34a20dceaf1737adbf20e01b43c2424e4e4b1722d942d1a796d895396e6
c1ccccc1
O=[CH;D2;+0:1]-[C:2]-[c:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH;D2;+0:8]=P(-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[CH2;D2;+0:1]-[C:2]-[c:3]
null
[]
null
null
null
null
In the preferred compounds of the invention the two R1 substituents are methyl, and the R2 and R3 substituents are hydrogen. Reaction Scheme 4 illustrates a synthetic process for preparing 7-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1-one (Compound G) which serves as a starting material for the synthesis of several pref...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Ester
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1
HO-
null
null
null
CCOC(=O)C=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=CCc1cccc(Br)c1>>CCOC(=O)CCCc1cccc(Br)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3c9f9ed9d7a3470fad54d7ea759b23b8
CCO.O=C(O)Cc1ccc(Br)cc1>>CCOC(=O)Cc1ccc(Br)cc1
BrC1=CC=C(C=C1)CC(=O)O.OS(=O)(=O)O.C(C)O.C(=O)([O-])[O-].[K+].[K+]>>BrC1=CC=C(C=C1)CC(=O)OCC
[CH3:1][CH2:2][OH:3].O[C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][c:10]([Br:11])[cH:12][cH:13]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][c:10]([Br:11])[cH:12][cH:13]1
CCO.O=C(O)Cc1ccc(Br)cc1
CCOC(=O)Cc1ccc(Br)cc1
null
null
null
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4].[C;D1;H3:5]-[C:6]-[OH;D1;+0:7]>>[C;D1;H3:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]
null
[]
null
null
null
null
A solution of 43 g (200 mmol) of 4-bromophenylacetic acid and 0.2 g of conc. H2SO4 in 470 ml of ethanol was refluxed for 16 hours. The reaction mixture was cooled to ambient temperature, stirred with 6 g of solid K2CO3 for 30 minutes and then filtered. The filtrate was concentrated in vacuo, diluted with Et2O (200 ml),...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccccc1
HO-
null
null
null
CCO.O=C(O)Cc1ccc(Br)cc1>>CCOC(=O)Cc1ccc(Br)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e43ff72352bb417281bdb41c9d85b8ca
CCOC(=O)Cc1ccc(Br)cc1.O=C(O)Cc1cccc(Br)c1>>CCOC(=O)Cc1cccc(Br)c1
BrC1=CC=C(C=C1)CC(=O)OCC.BrC1=CC=C(C=C1)CC(=O)OCC.BrC=1C=C(C=CC1)CC(=O)O>>BrC=1C=C(C=CC1)CC(=O)OCC
O=C(Cc1ccc(Br)cc1)O[CH2:2][CH3:1].[OH:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Br:12])[cH:13]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][c:11]([Br:12])[cH:13]1
CCOC(=O)Cc1ccc(Br)cc1.O=C(O)Cc1cccc(Br)c1
CCOC(=O)Cc1cccc(Br)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
042509afb850b7ae8d1b416db2a7d99308189364e9a5fcf96184b5eead3a8ee2
b4a89122cda2e12df412f0af60b7839f49d2933dbee64ad6cf28e3443255e82d
c1ccccc1
Br-c1:c:c:c(-C-C(=O)-O-[CH2;D2;+0:1]-[C;D1;H3:2]):c:c:1.[C:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6]>>[C:3]-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C;D1;H3:2]
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of ethyl (4-bromophenyl)acetate (Compound A), 100 g (463 mmol) of 3-bromophenylacetic acid was converted into the title compound (yellow oil) using 2 g of conc. H2SO4 and 500 ml of ethanol. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carboxylic acid.Ester
Ester
c1ccccc1
null
c1ccccc1
HBr
null
null
null
CCOC(=O)Cc1ccc(Br)cc1.O=C(O)Cc1cccc(Br)c1>>CCOC(=O)Cc1cccc(Br)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-33aa1937ff844517b2312155507524cc
CCOC(=O)Cc1ccc(Br)cc1>>O=CCc1ccc(Br)cc1
[H-].C(C(C)C)[Al+]CC(C)C.BrC1=CC=C(C=C1)CC(=O)OCC.BrC1=CC=C(C=C1)CC(=O)OCC.[H-].C(C(C)C)[Al+]CC(C)C>>BrC1=CC=C(C=C1)CC=O
CCO[C:2](=[O:1])[CH2:3][c:4]1[cH:5][cH:6][c:7]([Br:8])[cH:9][cH:10]1>>[O:1]=[CH:2][CH2:3][c:4]1[cH:5][cH:6][c:7]([Br:8])[cH:9][cH:10]1
CCOC(=O)Cc1ccc(Br)cc1
O=CCc1ccc(Br)cc1
null
null
C(Cl)Cl
Reduction
OtherReaction
ec1c6c64dd9be73981e5a6c952ab740869d298b20e87e097e88e1179cc5bc6dc
33ddc7b9457742ba0a376f08a972e4f33779267f6f1fe15e3be786427ae9f4ec
c1ccccc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[c:4]>>[O;D1;H0:2]=[CH;D2;+0:1]-[C:3]-[c:4]
null
[]
-78
CELSIUS
null
null
To a cold solution (-78° C.) of 15 g (62 mmol) of ethyl (4-bromophenyl)acetate (Compound A) in 150 ml of CH2Cl2 was added dropwise (over a span of 1 hour) 65 ml (65 mmol) of diisobutyl aluminum hydride (DIBAL-H, 1M solution in hexane). After the DIBAL-H addition was complete, the reaction was stirred at -78° C. for an ...
10.6084/m9.figshare.5104873.v1
null
Ester
Aldehyde
null
null
c1ccccc1
HO-
C(Cl)Cl
-78
null
CCOC(=O)Cc1ccc(Br)cc1>C(Cl)Cl>O=CCc1ccc(Br)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-da2fa25d7948417ea3bceca3d031dfb8
CCOC(=O)C=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=CCc1ccc(Br)cc1>>CCOC(=O)C=CCc1ccc(Br)cc1
BrC1=CC=C(C=C1)CC=O.ClCl.C(=O)(OCC)C=P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>BrC1=CC=C(C=C1)CC=CC(=O)OCC
c1ccc(P(c2ccccc2)(c2ccccc2)=[CH:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])cc1.O=[CH:7][CH2:8][c:9]1[cH:10][cH:11][c:12]([Br:13])[cH:14][cH:15]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]=[CH:7][CH2:8][c:9]1[cH:10][cH:11][c:12]([Br:13])[cH:14][cH:15]1
CCOC(=O)C=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=CCc1ccc(Br)cc1
CCOC(=O)C=CCc1ccc(Br)cc1
null
null
C(Cl)Cl
C-C Coupling
Wittig reaction with triphenylphosphorane
71bd2654cede51545adee465eb47bf49794d5c57afe21c7fb122478c5a700139
203dd34a20dceaf1737adbf20e01b43c2424e4e4b1722d942d1a796d895396e6
c1ccccc1
O=[CH;D2;+0:1]-[C:2]-[c:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH;D2;+0:8]=P(-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH;D2;+0:8]=[CH;D2;+0:1]-[C:2]-[c:3]
null
[]
null
null
16
HOUR
To a cold solution (-78° C.) of 15 g (62 mmol) of ethyl (4-bromophenyl)acetate (Compound A) in 150 ml of CH2Cl2 was added dropwise (over a span of 1 hour) 65 ml (65 mmol) of diisobutyl aluminum hydride (DIBAL-H, 1M solution in hexane). After the DIBAL-H addition was complete, the reaction was stirred at -78° C. for an ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Ester
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1
HO-
C(Cl)Cl
null
16
CCOC(=O)C=P(c1ccccc1)(c1ccccc1)c1ccccc1.O=CCc1ccc(Br)cc1>C(Cl)Cl>CCOC(=O)C=CCc1ccc(Br)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bbd2b45e8f9b4d7dbebe53c304885efe
CCOC(=O)CCCc1ccc(Br)cc1.CCOC(=O)Cc1cccc(Br)c1>>CCOC(=O)CCCc1cccc(Br)c1
BrC1=CC=C(C=C1)CCCC(=O)OCC.BrC1=CC=C(C=C1)CCCC(=O)OCC.BrC=1C=C(C=CC1)CC(=O)OCC.BrC=1C=C(C=CC1)CC(=O)OCC>>BrC=1C=C(C=CC1)CCCC(=O)OCC
Br[c:12]1[cH:11][cH:10][c:9]([CH2:8][CH2:7][CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:15][cH:13]1.CCOC(=O)Cc1cccc([Br:14])c1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][c:13]([Br:14])[cH:15]1
CCOC(=O)CCCc1ccc(Br)cc1.CCOC(=O)Cc1cccc(Br)c1
CCOC(=O)CCCc1cccc(Br)c1
null
null
null
Functional Group Interconversion
OtherReaction
434198cbd735c3e210a63326c76eb747349a83f3c9f01bbe2eff06a955199ae4
d0508361c24262840b1fde4be03be16061d0fd8ada9f40d1b6c5100911d70222
c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]:[cH;D2;+0:6]:1.C-C-O-C(=O)-C-c1:c:c:c:c(-[Br;H0;D1;+0:7]):c:1>>[Br;H0;D1;+0:7]-[c;H0;D3;+0:6]1:[c:5]:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:1
null
[]
null
null
null
null
Employing the same general multistep preparation as for ethyl 4-(4-bromophenyl)butanoate (Compound C), 60 g (246 mmol) of ethyl (3-bromophenyl)acetate (Compound B) was converted into the title compound (oil) using 255 ml (255 mmol) of diisobutyl aluminum hydride (DIBAL-H, 1M in hexane), 85.8 g (250 mmol) of (carbethoxy...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Ester
Aromatic halide
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1
HBr
null
null
null
CCOC(=O)CCCc1ccc(Br)cc1.CCOC(=O)Cc1cccc(Br)c1>>CCOC(=O)CCCc1cccc(Br)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a7d11788629c4e828999fce2494a1099
CC(C)(O)CCCc1cccc(Br)c1>>CC1(C)CCCc2cc(Br)ccc21
BrC=1C=C(C=CC1)CCCC(C)(O)C.BrC=1C=C(C=CC1)CCCC(C)(O)C.OS(=O)(=O)O>>BrC=1C=C2CCCC(C2=CC1)(C)C
O[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][CH2:6][c:7]1[cH:8][c:9]([Br:10])[cH:11][cH:12][cH:13]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH2:6][c:7]2[cH:8][c:9]([Br:10])[cH:11][cH:12][c:13]21
CC(C)(O)CCCc1cccc(Br)c1
CC1(C)CCCc2cc(Br)ccc21
null
null
O
Functional Group Interconversion
OtherReaction
9c1fb3695518f6dccadbe5ee73c6321afbfb380fa2ad5c0f3b619c242d912134
63e4ba80024292782b5f87f96975225484dff39f49e96eea21874ac0cd9091a0
c1ccc2c(c1)CCCC2
O-[C;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4]-[C:5]-[C:6]-[c:7](:[c:8]):[cH;D2;+0:9]:[c:10]:[c:11]>>[C;D1;H3:2]-[C;H0;D4;+0:1]1(-[C;D1;H3:3])-[C:4]-[C:5]-[C:6]-[c:7](:[c:8]):[c;H0;D3;+0:9]-1:[c:10]:[c:11]
null
[]
null
null
2.5
HOUR
15.0 g (58.3 mmol) of 5-(3-bromophenyl)-2-methyl-pentan-2-ol (Compound E) was cooled to 0° C. and then 2.8 ml of conc. H2SO4 was added. The mixture was stirred for 2.5 hours, diluted with water (20 ml) and extracted with Et2O (3×40 ml). The combined organic layers were washed with water, sat. aqueous NaHCO3 and brine, ...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
null
c1ccccc1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
O
null
2.5
CC(C)(O)CCCc1cccc(Br)c1>O>CC1(C)CCCc2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0f2e1f01e7ab4687bdbd97f9472f7215
CC(=O)O.CC1(C)CCCc2cc(Br)ccc21>>CC1(C)CCC(=O)c2cc(Br)ccc21
C(C)(=O)OC(C)=O.C(C)(=O)O.BrC=1C=C2CCCC(C2=CC1)(C)C.BrC=1C=C2CCCC(C2=CC1)(C)C>>BrC1=CC=C2C(CCC(C2=C1)=O)(C)C
CC(O)=[O:7].[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH2:6][c:8]2[cH:9][c:10]([Br:11])[cH:12][cH:13][c:14]21>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][c:10]([Br:11])[cH:12][cH:13][c:14]21
CC(=O)O.CC1(C)CCCc2cc(Br)ccc21
CC1(C)CCC(=O)c2cc(Br)ccc21
null
[O-2].[O-2].[O-2].[Cr+6]
C1=CC=CC=C1
Miscellaneous
OtherReaction
06b75b2d4fdd308e9ae14eb39d86aacd806c7aa02919897cbe294a3bc24409c8
bd34f155ea119239d8395e98fadac5c7a5507ae7ce37531b09373c8830fc562b
O=C1CCCc2ccccc21
C-C(-O)=[O;H0;D1;+0:1].[C:2]-[C:3]-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[C:2]-[C:3]-[C;H0;D3;+0:4](=[O;H0;D1;+0:1])-[c:5](:[c:6]):[c:7]
null
[]
null
null
1
HOUR
To a cold mixture (0° C.) of 209 g (200 mmol) of chromium trioxide, 100 ml (1.06 mol) of acetic anhydride and 200 ml (3.5 mol) of acetic acid was added a solution of 10 g (41.8 mmol) of 6-bromo-1,2,3,4-tet-rahydro-1,1-dimethylnaphthalene (Compound F) in 125 ml of benzene. The reaction mixture was stirred for 1 hour, qu...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ketone
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
[O-2].[O-2].[O-2].[Cr+6].C1=CC=CC=C1
null
1
CC(=O)O.CC1(C)CCCc2cc(Br)ccc21>[O-2].[O-2].[O-2].[Cr+6].C1=CC=CC=C1>CC1(C)CCC(=O)c2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d35af9b12f1b47e88a643494fdc123b8
CC1(C)CCCc2cc(Br)ccc21.O=C1CCC(=O)N1Br>>CC1(C)CCC(Br)c2cc(Br)ccc21
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.BrC=1C=C2CCCC(C2=CC1)(C)C.BrC=1C=C2CCCC(C2=CC1)(C)C.BrN1C(CCC1=O)=O>>BrC1CCC(C2=CC=C(C=C12)Br)(C)C
[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH2:6][c:8]2[cH:9][c:10]([Br:11])[cH:12][cH:13][c:14]21.O=C1CCC(=O)N1[Br:7]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH:6]([Br:7])[c:8]2[cH:9][c:10]([Br:11])[cH:12][cH:13][c:14]21
CC1(C)CCCc2cc(Br)ccc21.O=C1CCC(=O)N1Br
CC1(C)CCC(Br)c2cc(Br)ccc21
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl secondary
17739125d8cd5498d2767e5d914bf11a628d3cd4978506b1472183bfc6cb0caf
d425bc7fa712969b9477dfeabb5ca2470f442214b30503c51715e13a06c60154
c1ccc2c(c1)CCCC2
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[C:2]-[C:3]-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[Br;H0;D1;+0:1]-[CH;D3;+0:4](-[C:3]-[C:2])-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
To a solution of 1.2 g (5.0 mmol) of 6-bromo-1,2,3,4-tetrahydro-1,1-dimethylnaphthalene (Compound F) in 20 ml of CCl4 was added 0.97 g (5.5 mmol) of N-bromosuccinimide followed by 20 mg (0.08 mmol ) of benzoylperoxide. The mixture was refluxed for 3 hours, filtered and the filtrate washed with water (5 ml). The organic...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Secondary halide
c1ccc2c(c1)CCCC2.C1CCNC1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
C(Cl)(Cl)(Cl)Cl
null
null
CC1(C)CCCc2cc(Br)ccc21.O=C1CCC(=O)N1Br>C(Cl)(Cl)(Cl)Cl>CC1(C)CCC(Br)c2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d9d51c679b094d58b2ae53013e4113f3
CC1(C)CCC(Br)c2cc(Br)ccc21.OC1CCCCC1>>CC1(C)CCC(OC2CCCCC2)c2cc(Br)ccc21
BrC1CCC(C2=CC=C(C=C12)Br)(C)C.BrC1CCC(C2=CC=C(C=C12)Br)(C)C.C1(CCCCC1)O.[Na].[Na].C1(CCCCC1)O>>BrC=1C=C2C(CCC(C2=CC1)(C)C)OC1CCCCC1
Br[CH:6]1[CH2:5][CH2:4][C:2]([CH3:1])([CH3:3])[c:20]2[c:14]1[cH:15][c:16]([Br:17])[cH:18][cH:19]2.[OH:7][CH:8]1[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH:6]([O:7][CH:8]2[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]2)[c:14]2[cH:15][c:16]([Br:17])[cH:18][cH:19][c:20]21
CC1(C)CCC(Br)c2cc(Br)ccc21.OC1CCCCC1
CC1(C)CCC(OC2CCCCC2)c2cc(Br)ccc21
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
34d15a16c487cc76959b4148d45a121e70900b63e696306f158d56c902806bae
ea93f50d7d0ba6e1a92e059c8905ace57b0b1cde9cb71b1ee64fbecaa8f468bb
c1ccc2c(c1)CCCC2OC1CCCCC1
Br-[CH;D3;+0:1](-[C:2]-[C:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8](-[OH;D1;+0:9])-[C:10]>>[C:7]-[C:8](-[O;H0;D2;+0:9]-[CH;D3;+0:1](-[C:2]-[C:3])-[c:4](:[c:5]):[c:6])-[C:10]
null
[]
70
CELSIUS
12
HOUR
To 9 g (89.9 mmol) of cyclohexanol was added 160 mg (7.0 mmol) of sodium metal and the mixture was stirred at 70° C. for 12 hours. After all of the sodium dissolved the reaction mixture was cooled to ambient temperature and then a solution of 1 g (3.2 mmol) of 4,6-dibromo-1,1-dimethyl-1,2,3,4-tetrahydronaphthalene (Com...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary alcohol
Ether
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
C1CCCCC1.c1ccc2c(c1)CCCC2
HBr
null
70
12
CC1(C)CCC(Br)c2cc(Br)ccc21.OC1CCCCC1>>CC1(C)CCC(OC2CCCCC2)c2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5100f97ff6524472837ccd21fd6bb444
CC1(C)CCC(=O)c2ccc(Br)cc21>>C#Cc1ccc2c(c1)C(C)(C)CCC2=O
C[Si](C)(C)C#C.BrC=1C=C2C(CCC(C2=CC1)=O)(C)C.BrC=1C=C2C(CCC(C2=CC1)=O)(C)C.C(=O)([O-])[O-].[K+].[K+]>>C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C
Br[c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[C:9]([CH3:10])([CH3:11])[CH2:12][CH2:13][C:14]2=[O:15]>>[CH:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[C:9]([CH3:10])([CH3:11])[CH2:12][CH2:13][C:14]2=[O:15]
CC1(C)CCC(=O)c2ccc(Br)cc21
C#Cc1ccc2c(c1)C(C)(C)CCC2=O
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CO.C(C)N(CC)CC
Functional Group Interconversion
OtherReaction
9818ebb8d5fc33ce3a31bcb4fdc7e5e2df1ec512dcedf969889ca1e8c4b90a40
3328c8f87c438567981cd74666102f3c9878dcf86df57abda9cd69bae6cfdc49
O=C1CCCc2ccccc21
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]>>[C;D1;H1:6]#[C:7]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
24
HOUR
To a solution (flushed for 15 minutes with a stream of argon) of 13.55 g (53.8 mmol) of 6-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound H) in 280 ml of triethylamine was added 1.87 g (2.66 mmol) of bis(triphenylphosphine)palladium(II) chloride and 0.53 g (2.66 mmol) of cuprous iodide. The solution mixtur...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Alkyne
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
Br-
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO.C(C)N(CC)CC
null
24
CC1(C)CCC(=O)c2ccc(Br)cc21>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CO.C(C)N(CC)CC>C#Cc1ccc2c(c1)C(C)(C)CCC2=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-37e5f74403034441b8cb09beed7ae702
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CC1(C)CCC(=O)c2cc(Br)ccc21>>C#Cc1ccc2c(c1)C(=O)CCC2(C)C
C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C>>C(#C)C1=CC=C2C(CCC(C2=C1)=O)(C)C
C#Cc1ccc2c(c1)C(C)([CH3:15])CCC2=O.C[C:9]1(C)[c:7]2[c:6]([cH:5][cH:4][c:3]([C:2]#[CH:1])[cH:8]2)[C:13](=O)[CH2:12][CH2:11]1.CC1([CH3:14])CCC(=[O:10])c2cc(Br)ccc21>>[CH:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[C:9](=[O:10])[CH2:11][CH2:12][C:13]2([CH3:14])[CH3:15]
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CC1(C)CCC(=O)c2cc(Br)ccc21
C#Cc1ccc2c(c1)C(=O)CCC2(C)C
null
null
null
C-C Coupling
OtherReaction
1365b500a0241976737dfb6a369761907f8fb54b4f9ffb3c30402e49bd252bc2
92eb20c58f7702e061d6464afba78c5922cec9ff6753b5109e17ff517e1560ff
O=C1CCCc2ccccc21
Br-c1:c:c:c2:c(:c:1)-C(=[O;H0;D1;+0:1])-C-C-C-2(-C)-[CH3;D1;+0:2].C-C1(-[CH3;D1;+0:3])-C-C-C(=O)-c2:c:c:c(-C#C):c:c:2-1.C-[C;H0;D4;+0:4]1(-C)-[C:5]-[C:6]-[C;H0;D3;+0:7](=O)-[c:8](:[c:9]):[c:10]-1:[c:11]>>[CH3;D1;+0:2]-[C;H0;D4;+0:7]1(-[CH3;D1;+0:3])-[C:6]-[C:5]-[C;H0;D3;+0:4](=[O;H0;D1;+0:1])-[c:10](:[c:11]):[c:8]-1:[c...
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of 6-ethynyl-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound K), 7 g (27.6 mmol) of 7-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound G) was converted into the title compound using 39 ml (36.6 mmol) of trimethylsilyl acetylene, 0.97 g (1.3 ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Ketone.Ketone.Alkyne
Ketone
c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HBr
null
null
null
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CC1(C)CCC(=O)c2cc(Br)ccc21>>C#Cc1ccc2c(c1)C(=O)CCC2(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-084c85907fd245078e2f7acbc10ccaab
C#Cc1ccc2c(c1)C(C)(C)CCC2=O>>C#Cc1ccc2c(c1)C(C)(C)CCC2
C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.BrC1=CC=C2CCCC(C2=C1)(C)C>>C(#C)C1=CC=C2CCCC(C2=C1)(C)C
O=[C:14]1[c:6]2[cH:5][cH:4][c:3]([C:2]#[CH:1])[cH:8][c:7]2[C:9]([CH3:10])([CH3:11])[CH2:12][CH2:13]1>>[CH:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[C:9]([CH3:10])([CH3:11])[CH2:12][CH2:13][CH2:14]2
C#Cc1ccc2c(c1)C(C)(C)CCC2=O
C#Cc1ccc2c(c1)C(C)(C)CCC2
null
null
null
Reduction
OtherReaction
468c83eaa3986920e31d657ce80fb6963b17b14c1dd69f3228a474d350fb1bc7
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccc2c(c1)CCCC2
O=[C;H0;D3;+0:1](-[C:2]-[C:3])-[c:4](:[c:5]):[c:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of 6-ethynyl-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound K), 2.1 g (8.8 mmol) of 7-bromo-1,1-dimethyl-1,2,3,4-tetrahydronaphthalene was converted into the title compound using 10 ml (93.9 mmol) of trimethylsilyl acetylene, 1.25 g (1.8 mmol) of bis(t...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
Other
null
null
null
C#Cc1ccc2c(c1)C(C)(C)CCC2=O>>C#Cc1ccc2c(c1)C(C)(C)CCC2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0079b2bf1e1f4513a61d1b8da92b8460
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CC1(C)CCC(OC2CCCCC2)c2cc(Br)ccc21>>C#Cc1ccc2c(c1)C(OC1CCCCC1)CCC2(C)C
C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.BrC=1C=C2C(CCC(C2=CC1)(C)C)OC1CCCCC1.BrC=1C=C2C(CCC(C2=CC1)(C)C)OC1CCCCC1>>C1(CCCCC1)OC1CCC(C2=CC=C(C=C12)C#C)(C)C
CC1(C)CCC(=O)c2ccc([C:2]#[CH:1])cc21.Br[c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH:9]([O:10][CH:11]1[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]1)[CH2:17][CH2:18][C:19]2([CH3:20])[CH3:21]>>[CH:1]#[C:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH:9]([O:10][CH:11]1[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]1)[CH2:17][CH2:18][C:19]2(...
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CC1(C)CCC(OC2CCCCC2)c2cc(Br)ccc21
C#Cc1ccc2c(c1)C(OC1CCCCC1)CCC2(C)C
null
null
null
C-C Coupling
OtherReaction
31a3474e92ab2e8b85367011ff722b53d568044350671cd066f20ddbecb87843
a0646be30f9e286d895567733705df3a31f14d5a6362370a8a4aee5300c33666
c1ccc2c(c1)CCCC2OC1CCCCC1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].C-C1(-C)-C-C-C(=O)-c2:c:c:c(-[C;H0;D2;+0:6]#[C;D1;H1:7]):c:c:2-1>>[C;D1;H1:7]#[C;H0;D2;+0:6]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of 6-ethynyl-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound K), 2.1 g (8.8 mmol) of 6-bromo-4-cyclohexyloxy-1,1-dimethyl-1,2,3,4-tetrahydronaphthalene (Compound J) was converted into the title compound using 1 g (10.2 mmol) of trimethylsilyl acetylene,...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone.Alkyne
Alkyne
c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
C1CCCCC1.c1ccc2c(c1)CCCC2
HBr
null
null
null
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CC1(C)CCC(OC2CCCCC2)c2cc(Br)ccc21>>C#Cc1ccc2c(c1)C(OC1CCCCC1)CCC2(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0a6411cd1b2143cf95c4b57b2c8fb6d3
CC1(C)CCCc2cc(Br)ccc21.O=C1CCC(=O)N1Br>>CC1(C)CCC(Br)c2cc(Br)ccc21
C1=CC=CC2=CC=CC=C12.BrC=1C=C2CCCC(C2=CC1)(C)C.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C1=CC=CC2=CC=CC=C12.BrC=1C=C2CCCC(C2=CC1)(C)C.C1=CC=CC2=CC=CC=C12.BrC=1C=C2CCCC(C2=CC1)(C)C.BrN1C(CCC1=O)=O.BrC1=C(C2=CC=CC=C2C=C1)Br>>BrC1CCC(C2=CC=C(C=C12)Br)(C)C
[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH2:6][c:8]2[cH:9][c:10]([Br:11])[cH:12][cH:13][c:14]21.O=C1CCC(=O)N1[Br:7]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH:6]([Br:7])[c:8]2[cH:9][c:10]([Br:11])[cH:12][cH:13][c:14]21
CC1(C)CCCc2cc(Br)ccc21.O=C1CCC(=O)N1Br
CC1(C)CCC(Br)c2cc(Br)ccc21
null
null
null
Functional Group Interconversion
Wohl-Ziegler bromination benzyl secondary
17739125d8cd5498d2767e5d914bf11a628d3cd4978506b1472183bfc6cb0caf
d425bc7fa712969b9477dfeabb5ca2470f442214b30503c51715e13a06c60154
c1ccc2c(c1)CCCC2
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[C:2]-[C:3]-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[Br;H0;D1;+0:1]-[CH;D3;+0:4](-[C:3]-[C:2])-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
Employing the above-described procedure for the conversion of 6-bromo-1,2,3,4-tetrahydro-1,1-dimethylnaphthalene naphthalene (Compound F) to the dibromonaphthalene derivative (Compond I), 3.5 g (14.6 mmol) of (Compound F), 2.86 g (16.1 mmol) of N-bromosuccinimide and 150 mg (0.62 mmol ) of benzoylperoxide gave crude 4,...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Secondary halide
c1ccc2c(c1)CCCC2.C1CCNC1
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
null
null
null
CC1(C)CCCc2cc(Br)ccc21.O=C1CCC(=O)N1Br>>CC1(C)CCC(Br)c2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8ad41e85bae94573960b3d36e878b3e1
CC1(C)CCC(Br)c2cc(Br)ccc21>>CC(=S)C1CCC(C)(C)c2ccc(Br)cc21
BrC1CCC(C2=CC=C(C=C12)Br)(C)C.BrC1CCC(C2=CC=C(C=C12)Br)(C)C.C(C)(=S)[O-].[K+]>>BrC=1C=C2C(CCC(C2=CC1)(C)C)C(C)=S
Br[CH:4]1[CH2:5][CH2:6][C:7]([CH3:8])([CH3:9])[c:10]2[cH:11][cH:12][c:13]([Br:14])[cH:15][c:16]21>>[CH3:1][C:2](=[S:3])[CH:4]1[CH2:5][CH2:6][C:7]([CH3:8])([CH3:9])[c:10]2[cH:11][cH:12][c:13]([Br:14])[cH:15][c:16]21
CC1(C)CCC(Br)c2cc(Br)ccc21
CC(=S)C1CCC(C)(C)c2ccc(Br)cc21
null
null
C1CCOC1
Miscellaneous
OtherReaction
9454b75fa71245ad89b40fe3c2db4bb90e1d43bd9cae8b3499d53736938dead0
9559467ca5e8c56c867a7f0b1d7590b92ee0338e4bcca9d01df5ba4df2a7cb1f
c1ccc2c(c1)CCCC2
Br-[CH;D3;+0:1](-[C:2]-[C:3])-[c:4](:[c:5]):[c:6]>>[C:3]-[C:2]-[CH;D3;+0:1](-[C:7](-[C;D1;H3:8])=[S;D1;H0:9])-[c:4](:[c:5]):[c:6]
null
[]
null
null
null
null
Employing the above-described procedure for the conversion of 6-bromo-1,2,3,4-tetrahydro-1,1-dimethylnaphthalene naphthalene (Compound F) to the dibromonaphthalene derivative (Compond I), 3.5 g (14.6 mmol) of (Compound F), 2.86 g (16.1 mmol) of N-bromosuccinimide and 150 mg (0.62 mmol ) of benzoylperoxide gave crude 4,...
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null
Secondary halide
Thiocarbonyl
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
Br-
C1CCOC1
null
null
CC1(C)CCC(Br)c2cc(Br)ccc21>C1CCOC1>CC(=S)C1CCC(C)(C)c2ccc(Br)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6724f220dc7c4e89ac64b79ac6a33d74
CCO.O=C(O)c1ccc(I)cc1>>CCOC(=O)c1ccc(I)cc1
IC1=CC=C(C(=O)O)C=C1.C(C)O.S(=O)(Cl)Cl>>C(C)OC(C1=CC=C(C=C1)I)=O
[CH3:1][CH2:2][OH:3].O[C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([I:10])[cH:11][cH:12]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([I:10])[cH:11][cH:12]1
CCO.O=C(O)c1ccc(I)cc1
CCOC(=O)c1ccc(I)cc1
null
null
null
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[C:7]-[OH;D1;+0:8]>>[C;D1;H3:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
To a suspension of 10 g (40.32 mmol) of 4-iodobenzoic acid in 100 ml absolute ethanol was added 2 ml thionyl chloride and the mixture was then heated at reflux for 3 hours. Solvent was removed in vacuo and the residue was dissolved in 100 ml ether. The ether solution was washed with saturated NaHCO3 and saturated NaCl ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccccc1
HO-
null
null
null
CCO.O=C(O)c1ccc(I)cc1>>CCOC(=O)c1ccc(I)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-314d43ab585348f7bd5e6d904c0e5adc
CCO.O=C(O)c1ccc(Cl)nc1>>CCOC(=O)c1ccc(Cl)nc1
ClC1=NC=C(C(=O)O)C=C1.C(C)O.C1(CCCCC1)N=C=NC1CCCCC1.CN(C)C1=NC=CC=C1>>ClC1=NC=C(C(=O)OCC)C=C1
[CH3:1][CH2:2][OH:3].O[C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([Cl:10])[n:11][cH:12]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([Cl:10])[n:11][cH:12]1
CCO.O=C(O)c1ccc(Cl)nc1
CCOC(=O)c1ccc(Cl)nc1
null
null
C(Cl)Cl
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
c1ccncc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[#7;a:6]:[c:7].[C;D1;H3:8]-[C:9]-[OH;D1;+0:10]>>[C;D1;H3:8]-[C:9]-[O;H0;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[#7;a:6]:[c:7]
null
[]
null
null
null
null
A mixture of 15.75 g (0.1 mol) 6-chloronicotinic acid, 6.9 g (0.15 mol) ethanol, 22.7 g (0.11 mol) dicyclohexylcarbodiimide and 3.7 g dimethylaminopyridine in 200 ml methylene chloride was heated at reflux for 2 hours. The mixture was allowed to cool, solvent removed in vacuo and the residue subjected to flash chromato...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccncc1
HO-
C(Cl)Cl
null
null
CCO.O=C(O)c1ccc(Cl)nc1>C(Cl)Cl>CCOC(=O)c1ccc(Cl)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9bd2bc35b4cb41778d4b4e86c4962f24
I.O=C(O)c1ccc(Cl)nc1>>O=C(O)c1ccc(I)nc1
[I-].[Na+].I.ClC1=NC=C(C(=O)O)C=C1>>IC1=NC=C(C(=O)O)C=C1
[IH:8].Cl[c:7]1[cH:6][cH:5][c:4]([C:2](=[O:1])[OH:3])[cH:10][n:9]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([I:8])[n:9][cH:10]1
I.O=C(O)c1ccc(Cl)nc1
O=C(O)c1ccc(I)nc1
null
null
CC(=O)C
Miscellaneous
OtherReaction
b82d7209d2f0845b6d508d9b5d94221ef0c6a7295c1411bdc2d44fbaafae04d9
50b3263108b11afcbe25d1a908d5d62fc9b7a01756ee297f5e635ade1a0cdefb
c1ccncc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5].[IH;D0;+0:6]>>[I;H0;D1;+0:6]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
5
MINUTE
To 27.97 g (186.6 mmol) of sodium iodide cooled to -78° C. was added 121.77 g (71.6 ml, 952.0 mmol) of hydriodic acid (57 wt %). The reaction mixture was allowed to warm slightly with stirring for 5 minutes, and then 30.00 g (190.4 mmol) of 6-chloronicotinic acid was added. The resulting mixture was allowed to warm to ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Aromatic halide
c1ccncc1
c1ccncc1
c1ccncc1
HCl
CC(=O)C
null
0.083333
I.O=C(O)c1ccc(Cl)nc1>CC(=O)C>O=C(O)c1ccc(I)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2fe08cc9e6c748808fe5a8679bdd3bfb
CCO.O=C(O)c1ccc(I)nc1>>CCOC(=O)c1ccc(I)nc1
IC1=NC=C(C(=O)O)C=C1.C(C)O.Cl.CN(CCCN=C=NCC)C>>IC1=NC=C(C(=O)OCC)C=C1
O[CH2:2][CH3:1].[OH:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([I:10])[n:11][cH:12]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([I:10])[n:11][cH:12]1
CCO.O=C(O)c1ccc(I)nc1
CCOC(=O)c1ccc(I)nc1
null
CN(C1=CC=NC=C1)C
ClCCl
Heteroatom Alkylation and Arylation
Esterification of Carboxylic Acids
3f9a9ace480b666da05fcfe5450d12b5c1ea5b0d435c195e1dd4bd20281604bb
dcbf04ec563ed0e9dfc79070490a028958024079a671c385858bb18cc8ec995a
c1ccncc1
O-[CH2;D2;+0:1]-[C;D1;H3:2].[#7;a:3]:[c:4]:[c:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[#7;a:3]:[c:4]:[c:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[C;D1;H3:2]
null
[]
50
CELSIUS
null
null
To a suspension of 23.38 g (94.2 mmol) of 6-iodonicotinic acid in 100 ml of dichloromethane was added a solution of 19.86 g (103.6 mmol) of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride in 250 ml of dichloromethane. To this suspension was added 12.40 g (15.8 ml, 269.3 mmol) of ethanol (95%) and 1.15 g (9....
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccncc1
HO-
CN(C1=CC=NC=C1)C.ClCCl
50
null
CCO.O=C(O)c1ccc(I)nc1>CN(C1=CC=NC=C1)C.ClCCl>CCOC(=O)c1ccc(I)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-445de8cff1a04382843fe36a0a03ecd1
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CCOC(=O)c1ccc(I)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.C(#C)C=1C=C2C(CCC(C2=CC1)=O)(C)C.IC1=CC=C(C(=O)OCC)C=C1>>CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C
[CH:10]#[C:11][c:12]1[cH:13][cH:14][c:15]2[c:16]([cH:17]1)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][C:23]2=[O:24].I[c:9]1[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:26][cH:25]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:18]([CH3:19])(...
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CCOC(=O)c1ccc(I)cc1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
C(C)N(CC)CC
C-C Coupling
Sonogashira alkyne_aryl halide
15c08902746c61a960c314898ce6bb5fcc5e189f9e057388c59dba9ec9d0c81c
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
O=C1CCCc2cc(C#Cc3ccccc3)ccc21
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[CH;D1;+0:6]#[C:7]-[c:8]>>[c:8]-[C:7]#[C;H0;D2;+0:6]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
null
null
18
HOUR
To a solution of 8.8 g (47.8 mmol) of 6-ethynyl-1,2,3,4-tetrahydro-4,4-dimethylnaphthalen-1-one (Compound K) flushed for 15 minutes with a stream of argon, and 13.2 g (47.8 mmol) of ethyl 4-iodobenzoate in 200 ml of triethylamine was added 1.1 g (1.6 mmol) of bis(triphenylphosphine)palladium(II) chloride and 0.30 g (1....
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2c(c1)CCCC2
HI
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C(C)N(CC)CC
null
18
C#Cc1ccc2c(c1)C(C)(C)CCC2=O.CCOC(=O)c1ccc(I)cc1>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C(C)N(CC)CC>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e299c501d96048db89b08fd31ee6b9bf
C#Cc1ccc2c(c1)C(=O)CCC2(C)C.C#Cc1ccc2c(c1)C(=O)CCC2(C)C.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)cc1
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.C(#C)C1=CC=C2C(CCC(C2=C1)=O)(C)C.C(#C)C1=CC=C2C(CCC(C2=C1)=O)(C)C>>CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C
C#Cc1ccc2c(c1)C(=[O:19])CCC2(C)C.C#Cc1ccc2c(c1)C(=O)CCC2([CH3:23])[CH3:24].C[C:18]1(C)[c:16]2[c:15]([cH:14][cH:13][c:12]([C:11]#[C:10][c:9]3[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:26][cH:25]3)[cH:17]2)[C:22](=O)[CH2:21][CH2:20]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]...
C#Cc1ccc2c(c1)C(=O)CCC2(C)C.C#Cc1ccc2c(c1)C(=O)CCC2(C)C.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)cc1
null
null
null
C-C Coupling
OtherReaction
dc33cab0b77d3fb96b3667c72300820592501c9c2e822167612a009d145b0c83
885371fb4e33873f638094be96087519d7dde6b81c0705bbbf7b5f832f94f13e
O=C1CCCc2ccc(C#Cc3ccccc3)cc21
C#C-c1:c:c:c2:c(:c:1)-C(=O)-C-C-C-2(-[CH3;D1;+0:1])-[CH3;D1;+0:2].C-C1(-C)-C-C-C(=[O;H0;D1;+0:3])-c2:c:c(-C#C):c:c:c:2-1.C-[C;H0;D4;+0:4]1(-C)-[C:5]-[C:6]-[C;H0;D3;+0:7](=O)-[c:8](:[c:9]):[c:10]-1:[c:11]>>[CH3;D1;+0:1]-[C;H0;D4;+0:7]1(-[CH3;D1;+0:2])-[C:6]-[C:5]-[C;H0;D3;+0:4](=[O;H0;D1;+0:3])-[c:10](:[c:11]):[c:8]-1:[...
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl)ethynyl]benzoate (Compound 1), 4 g (21.7 mmol) of 7-ethynyl-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound L) was converted into the title compound using 6 g (21.7 mmol) of ethyl 4-iodobenzo...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Ketone.Alkyne.Alkyne
Ketone
c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
HO-
null
null
null
C#Cc1ccc2c(c1)C(=O)CCC2(C)C.C#Cc1ccc2c(c1)C(=O)CCC2(C)C.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ccf8d7ba858a4a1d98efae7e84bea37c
C#Cc1ccc2c(c1)C(OC1CCCCC1)CCC2(C)C.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(OC2CCCCC2)CCC3(C)C)cc1
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.C1(CCCCC1)OC1CCC(C2=CC=C(C=C12)C#C)(C)C.C1(CCCCC1)OC1CCC(C2=CC=C(C=C12)C#C)(C)C>>C1(CCCCC1)OC1C=2C=C(C=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1
C#Cc1ccc2c(c1)[CH:18]([O:19][CH:20]1[CH2:21][CH2:22][CH2:23][CH2:24][CH2:25]1)[CH2:26][CH2:27][C:28]2([CH3:29])[CH3:30].CC1(C)CCC(=O)[c:15]2[cH:14][cH:13][c:12]([C:11]#[C:10][c:9]3[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:32][cH:31]3)[cH:17][c:16]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](...
C#Cc1ccc2c(c1)C(OC1CCCCC1)CCC2(C)C.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(OC2CCCCC2)CCC3(C)C)cc1
null
null
null
C-C Coupling
OtherReaction
2b8579d1dea69c0d1f699de464a260c5b1c7d6aa0ee7dc7df5152b5133779971
94a676fe3e982ab149a6f97d161c48e0feb67671b52e80ae2dc697687e7b886e
C(#Cc1ccc2c(c1)C(OC1CCCCC1)CCC2)c1ccccc1
C#C-c1:c:c:c2:c(:c:1)-[CH;D3;+0:1](-[#8:2]-[C:3])-[C:4]-[C:5]-[C;H0;D4;+0:6]-2(-[C;D1;H3:7])-[C;D1;H3:8].C-C1(-C)-C-C-C(=O)-[c;H0;D3;+0:9]2:[c:10]:[c:11]:[c:12](-[C:13]#[C:14]):[c:15]:[c;H0;D3;+0:16]:2-1>>[C:14]#[C:13]-[c:12]1:[c:11]:[c:10]:[c;H0;D3;+0:9]2:[c;H0;D3;+0:16](:[c:15]:1)-[CH;D3;+0:1](-[#8:2]-[C:3])-[C:4]-[C...
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl)ethynyl]benzoate (Compound 1), 90 mg (0.3 mmol) of 4-cyclohexyloxy-6-ethynyl-1,2,3,4-tetrahydro-1,1-dimethylnaphthalene (Compound N) was converted into the title compound using 88 mg (0.32 mmol) of ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether.Alkyne
Ether
c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccccc1.C1CCCCC1.c1ccc2c(c1)CCCC2
HO-
null
null
null
C#Cc1ccc2c(c1)C(OC1CCCCC1)CCC2(C)C.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(OC2CCCCC2)CCC3(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a7c746e75636433f9e27f8624b0dcadb
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>>CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.[Li+].[OH-]>>CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C
CC[O:20][C:18]([c:17]1[cH:16][cH:15][c:14]([C:13]#[C:12][c:11]2[cH:10][cH:9][c:8]3[c:24]([cH:23]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]3=[O:7])[cH:22][cH:21]1)=[O:19]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]#[C:13][c:14]3[cH:15][cH:16][c:17]([C:18](=[O:19])[OH:20])[cH:21][...
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
null
null
C(C)O.C1CCOC1
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1CCCc2cc(C#Cc3ccccc3)ccc21
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
4
HOUR
To a suspension of 0.30 g (0.87 mmol) of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl)ethynyl]benzoate (Compound 1) in 4 ml of THF and 2 ml of ethanol was added 2 ml (2 mmol) of LiOH (1N aqueous solution). The reaction mixture was stirred at room temperature for 4 hours, concentrated in vacuo to near dryn...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
Other
C(C)O.C1CCOC1
null
4
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>C(C)O.C1CCOC1>CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9e18f2a2e4df4babb93886c7acc67a7c
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21.CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21>>CC1(C)CCC(=O)c2cc(C#Cc3ccc(C(=O)O)cc3)ccc21
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C.CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C>>CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C
CC1(C)CCC(=O)[c:24]2[c:8]1[cH:9][c:10]([C:11]#[C:12][c:13]1[cH:14][cH:15][c:16]([C:17](=[O:18])[OH:19])[cH:20][cH:21]1)[cH:22][cH:23]2.O=C(O)c1ccc(C#Cc2ccc3c(c2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]3=[O:7])cc1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]#[C:12][c:13]3[cH:14][cH:15][c...
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21.CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
CC1(C)CCC(=O)c2cc(C#Cc3ccc(C(=O)O)cc3)ccc21
null
null
null
C-C Coupling
OtherReaction
d3f6d1903ff582380fc39e7e066afb4d2aef58322140d130a8213d57d545b6c1
d308d6d88bdc2680ebd4a0ac133a9fce7c59d78c57c9b8a8e267f80ef25c594e
O=C1CCCc2ccc(C#Cc3ccccc3)cc21
C-C1(-C)-C-C-C(=O)-[c;H0;D3;+0:1]2:[c:2]:[c:3]:[c:4](-[C:5]#[C:6]):[c:7]:[c;H0;D3;+0:8]:2-1.O-C(=O)-c1:c:c:c(-C#C-c2:c:c:c3:c(:c:2)-[C;H0;D4;+0:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C:12]-[C:13]-[C;H0;D3;+0:14]-3=[O;D1;H0:15]):c:c:1>>[C:6]#[C:5]-[c:4]1:[c:3]:[c:2]:[c;H0;D3;+0:1]2:[c;H0;D3;+0:8](:[c:7]:1)-[C;H0;D3;+0:14](=[...
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl) ethynyl]benzoic acid (Compound 7), 500 mg (1.45 mmol) of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-3-yl)ethynyl]benzoate (Compound 2) was converted into the title compound using 4 ml (4 mmol)...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ketone.Ketone.Alkyne
Ketone
c1ccc2c(c1)CCCC2.c1ccccc1.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2.c1ccccc1
HO-
null
null
null
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21.CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21>>CC1(C)CCC(=O)c2cc(C#Cc3ccc(C(=O)O)cc3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bb6edbcef5bb4a6484ddbb61dc2f5b2b
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.[BH4-].[Na+]>>OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][C:23]3=[O:24])[cH:25][cH:26]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:18]([CH3:19])([CH...
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1
null
null
C(C)O.C1CCOC1.O
Reduction
Reduction of ketone to secondary alcohol
3712a1f2cb52729543ec421b1a5b2fd3f779bad4223604244414834ade516040
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5](:[c:6]):[c:7]>>[C:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5](:[c:6]):[c:7]
null
[]
null
null
6
HOUR
To a cold solution (0° C.) of 980 mg (2.8 mmol) of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl)ethynyl]benzoate (Compound 1) in 5 ml of THF and 10 ml of ethanol was added 78 mg (2 mmol) of sodium borohydride. The mixture was stirred for 6 hours, diluted with water (10 ml) and extracted with Et2O (4×40 ml...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
null
C(C)O.C1CCOC1.O
null
6
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>C(C)O.C1CCOC1.O>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-29ccf8ac4f5a4867bec6dfaabe5da5da
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(O)CCC3(C)C)cc1
OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1.OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1.CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C>>OC1C=2C=C(C=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3([CH3:23])[CH3:24])cc1.C[C:18]1(C)[c:16]2[c:15]([cH:14][cH:13][c:12]([C:11]#[C:10][c:9]3[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:26][cH:25]3)[cH:17]2)[CH:22]([OH:19])[CH2:21][CH2:20]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][...
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(O)CCC3(C)C)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
c5e6bbc7a9a06463d1cfdc9e7f078d26c8f4b38b4024a0aa1c7dfced71cf66c1
022be287155c79a6d0a8de717f678014006ca37ac9cbb0d100f44924121a0883
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
C-C-O-C(=O)-c1:c:c:c(-C#C-c2:c:c:c3:c(:c:2)-C(=O)-C-C-C-3(-[CH3;D1;+0:1])-[CH3;D1;+0:2]):c:c:1.C-[C;H0;D4;+0:3]1(-C)-[C:4]-[C:5]-[CH;D3;+0:6](-[OH;D1;+0:7])-[c:8](:[c:9]):[c:10]-1:[c:11]>>[CH3;D1;+0:1]-[C;H0;D4;+0:6]1(-[CH3;D1;+0:2])-[C:5]-[C:4]-[CH;D3;+0:3](-[OH;D1;+0:7])-[c:10](:[c:11]):[c:8]-1:[c:9]
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of ethyl 4-[(5,6,7,8-tetrahydro-5-hydroxy-8,8-dimethylnaphth-2-yl)ethynyl]benzoate (Compound 9), 1 g (2.88 mmol) of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-3-yl)ethynyl]benzoate (Compound 2) (was converted into the title compound using 60 mg (1.6...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Secondary alcohol.Alkyne
Secondary alcohol
c1ccccc1.c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
HO-
null
null
null
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(O)CCC3(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a309b213ee744acf9636717f3498282d
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)nc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(O)CCC3(C)C)nc1
OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1.OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1.CC1(CCC(C=2C=C(C=CC12)C#CC1=NC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=C(C=CC12)C#CC1=NC=C(C(=O)OCC)C=C1)=O)C>>OC1C=2C=C(C=CC2C(CC1)(C)C)C#CC1=NC=C(C(=O)OCC)C=C1
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:18](=[O:19])[CH2:20][CH2:21][C:22]3([CH3:23])[CH3:24])[n:25][cH:26]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[CH:18]([OH:19])[CH2:...
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)nc1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(O)CCC3(C)C)nc1
null
null
null
Reduction
Reduction of ketone to secondary alcohol
3712a1f2cb52729543ec421b1a5b2fd3f779bad4223604244414834ade516040
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C(#Cc1ccccn1)c1ccc2c(c1)CCCC2
[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5](:[c:6]):[c:7]>>[C:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of ethyl 4-[(5,6,7,8-tetrahydro-5-hydroxy-8,8-dimethylnaphth-2-yl)ethynyl]benzoate (Compound 9), 700 mg (2 mmol) of ethyl 6-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-3-yl)ethynyl]nicotinate (Compound 4) was converted into the title compound using 60 mg (1....
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccncc1.c1ccc2c(c1)CCCC2
null
null
null
null
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)nc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(O)CCC3(C)C)nc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4b29fc3fad974c179356548ebb415dfd
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)nc1>>CC1(C)CCC(=O)c2cc(C#Cc3ccc(C(=O)O)cn3)ccc21
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C.CC1(CCC(C=2C=C(C=CC12)C#CC1=NC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=C(C=CC12)C#CC1=NC=C(C(=O)OCC)C=C1)=O)C>>CC1(CCC(C=2C=C(C=CC12)C#CC1=NC=C(C(=O)O)C=C1)=O)C
CC[O:19][C:17]([c:16]1[cH:15][cH:14][c:13]([C:12]#[C:11][c:10]2[cH:9][c:8]3[c:24]([cH:23][cH:22]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]3=[O:7])[n:21][cH:20]1)=[O:18]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11]#[C:12][c:13]3[cH:14][cH:15][c:16]([C:17](=[O:18])[OH:19])[cH:20][n:21]3)[...
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)nc1
CC1(C)CCC(=O)c2cc(C#Cc3ccc(C(=O)O)cn3)ccc21
null
null
null
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1CCCc2ccc(C#Cc3ccccn3)cc21
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of 4-[[5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl]ethynyl]benzoic acid (Compound 7), 300 mg (0.86 mmol) of ethyl 6-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-3-yl)ethynyl]nicotinate (Compound 3) was converted into the title compound (pale yellow solid...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2c(c1)CCCC2.c1ccncc1
Other
null
null
null
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(=O)CCC3(C)C)nc1>>CC1(C)CCC(=O)c2cc(C#Cc3ccc(C(=O)O)cn3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-312409619c75422fbcb4db7823828526
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1.C[Si](C)(C)Cl>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O[Si](C)(C)C)cc1
Cl[Si](C)(C)C.OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1.OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1.C(C)N(CC)CC>>CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)O[Si](C)(C)C)C
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][CH:23]3[OH:24])[cH:29][cH:30]1.Cl[Si:25]([CH3:26])([CH3:27])[CH3:28]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:1...
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1.C[Si](C)(C)Cl
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O[Si](C)(C)C)cc1
null
null
C(Cl)Cl
Protection
Alcohol protection with silyl ethers
ea139b3cb6171a748fbc881d815cc598a14c6b8245b87168b4a15a10e325f24c
1e2a25dd539d267852f3b05b92dd4080ece1d4c7abb9db1b6fd2b64d2b33a864
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4].[C:5]-[C:6](-[OH;D1;+0:7])-[c:8]>>[C:5]-[C:6](-[O;H0;D2;+0:7]-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4])-[c:8]
null
[]
null
null
null
null
To a solution of 0.23 g (0.54 mmol) of ethyl 4-[(5,6,7,8-tetrahydro-5-hydroxy-8,8-dimethylnaphth-2-yl)ethynyl]benzoate (Compound 9) in 4 ml of dry CH2Cl2 was added 0.06 ml of triethylamine (0.81 mmol). The solution was flushed with nitrogen and then 0.12 g (0.81 mmol) of chlorotrimethylsilane was slowly added by syring...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
Silyl protective group
null
null
c1ccccc1.c1ccc2c(c1)CCCC2
HCl
C(Cl)Cl
null
null
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O)cc1.C[Si](C)(C)Cl>C(Cl)Cl>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O[Si](C)(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f42f93a338f24d7caa512d7d1159c4df
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O[Si](C)(C)C)cc1>>CC1(C)CCC(O[Si](C)(C)C)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)O[Si](C)(C)C)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)O[Si](C)(C)C)C.OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)O)C=C1.OC1C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)O)C=C1>>CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)O[Si](C)(C)C)C
CC[O:24][C:22]([c:21]1[cH:20][cH:19][c:18]([C:17]#[C:16][c:15]2[cH:14][cH:13][c:12]3[c:28]([cH:27]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][CH:6]3[O:7][Si:8]([CH3:9])([CH3:10])[CH3:11])[cH:26][cH:25]1)=[O:23]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH:6]([O:7][Si:8]([CH3:9])([CH3:10])[CH3:11])[c:12]2[cH:13][cH:14][c:15]([C...
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O[Si](C)(C)C)cc1
CC1(C)CCC(O[Si](C)(C)C)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
null
null
null
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
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
null
null
Employing the same general procedure as for the preparation of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-trimethylsiloxynaphth-2-yl)ethynyl]benzoate (Compound 111), 83 mg (0.26 mmol) of 4-[(5,6,7,8-tetrahydro-5-hydroxy-8,8-dimethylnaphth-2-yl)ethynyl]benzoic acid (Compound 42) was converted into the title compound (w...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
Other
null
null
null
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3O[Si](C)(C)C)cc1>>CC1(C)CCC(O[Si](C)(C)C)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3bc3da49cb6b461196d4eaac084da60d
CCOC(=O)CBr.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>>CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21
BrCC(=O)OCC.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C>>OC1(C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1)CC(=O)OCC
Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[C:7]1(=[O:8])[CH2:9][CH2:10][C:11]([CH3:12])([CH3:13])[c:14]2[cH:15][c:16]([C:17]#[C:18][c:19]3[cH:20][cH:21][c:22]([C:23](=[O:24])[O:25][CH2:26][CH3:27])[cH:28][cH:29]3)[cH:30][cH:31][c:32]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7]1([OH:8])[CH2:9][CH2:10][C:11]([CH3:12]...
CCOC(=O)CBr.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21
null
[Zn]
C1=CC=CC=C1
C-C Coupling
Grignard_alcohol
ae6802bc43630c235b581c1f69ee3f400dd59564bb5948df811879329723b99c
86d8e63c1eeb9e82c583fd2409352b28a569a3f780f9f297e86b8d2f688ca9d6
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C:6]-[C:7]-[C;H0;D3;+0:8](=[O;H0;D1;+0:9])-[c:10](:[c:11]):[c:12]>>[C:6]-[C:7]-[C;H0;D4;+0:8](-[OH;D1;+0:9])(-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[c:10](:[c:11]):[c:12]
null
[]
null
null
null
null
To a refluxing solution of 1.00 g (15.30 mmol) of 20 mesh, granular zinc (activated prior to use by washing with 2% HCl, water, 95% ethanol, acetone, anhydrous Et2O and then dried in vacuum for several hours) in 20 ml of dry benzene was slowly added a mixture of 0.23 ml (1.62 mmol) of ethyl bromoacetate, 0.28 g (0.81 m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ester.Tertiary alcohol
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2.c1ccccc1
Br-
[Zn].C1=CC=CC=C1
null
null
CCOC(=O)CBr.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3=O)cc1>[Zn].C1=CC=CC=C1>CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-558960f60108438697a2928369019551
CC(O)[Si](C)(C)C.CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21>>CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)cc21
CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)O)C=C1)=O)C.CN(C)C1=NC=CC=C1.C[Si](C)(C)C(C)O.Cl.CN(CCCN=C=NCC)C>>CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)=O)C
O[CH:22]([CH3:21])[Si:23]([CH3:24])([CH3:25])[CH3:26].[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]#[C:13][c:14]3[cH:15][cH:16][c:17]([C:18](=[O:19])[OH:20])[cH:27][cH:28]3)[cH:29][c:30]21>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([C:12]#[C:13][c:14]...
CC(O)[Si](C)(C)C.CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)cc21
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
55fde8dca0a408407bb776c4e1e9a22d6eeb5c734b0d7975d23baba4292968d2
505f7b4da8def84a80ac616845cb7b0566b14f3232b5b9d3480d84d3e0d284a0
O=C1CCCc2cc(C#Cc3ccccc3)ccc21
O-[CH;D3;+0:1](-[CH3;D1;+0:2])-[#14:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[C;D1;H3:6].[O;D1;H0:7]=[C:8](-[OH;D1;+0:9])-[c:10]>>[C;D1;H3:4]-[#14:3](-[C;D1;H3:5])(-[C;D1;H3:6])-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[O;H0;D2;+0:9]-[C:8](=[O;D1;H0:7])-[c:10]
null
[]
25
CELSIUS
5
HOUR
To a solution of 0.24 g (0.73 mmol) of 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl)ethynyl]benzoic acid (Compound 7) in 10 ml of dry CH2Cl2 was added 0.09 g (0.74 mmol) of dimethylaminopyridine, 0.115 ml (0.80 mmol) of trimethylsilylethanol and 0.17 g (0.88 mmol) of 1-(3-dimethylaminopropyl)-3-ethyl carbodiimi...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary alcohol
Ester
null
null
c1ccc2c(c1)CCCC2.c1ccccc1
HO-
C(Cl)Cl
25
5
CC(O)[Si](C)(C)C.CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)O)cc3)cc21>C(Cl)Cl>CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c1a4e1e535804129a0f31d37c5904ccb
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)cc21.CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21>>CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21
OC1(C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1)CC(=O)OCC.OC1(C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1)CC(=O)OCC.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)=O)C.CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)=O)C>>OC1(C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)CC(=O)...
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)[O:25][CH2:26][CH2:27][Si:28]([CH3:29])([CH3:30])[CH3:31])cc3)cc21.CCO[C:23]([c:22]1[cH:21][cH:20][c:19]([C:18]#[C:17][c:16]2[cH:15][c:14]3[c:36]([cH:35][cH:34]2)[C:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])([OH:8])[CH2:9][CH2:10][C:11]3([CH3:12])[CH3:13])[cH:33][cH:32]1)=[O:24]>>[CH3:...
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)cc21.CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21
null
null
null
Acylation
OtherReaction
5649976c68db781128c5e8fe1133b554cbbb509205645293d888ba70e249ea5b
9d3a8d45a08916f563b73b1fec78d20ccc19f70a36752aa400881ecf9d6765b1
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].C-C1(-C)-C-C-C(=O)-c2:c:c:c(-C#C-c3:c:c:c(-C(=O)-[O;H0;D2;+0:6]-[C:7]-[C:8]):c:c:3):c:c:2-1>>[C:8]-[C:7]-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of ethyl 4-[(5,6,7,8-tetrahydro-5-hydroxy-8,8-dimethyl-5-carboethoxymethylnaphth-2-yl)ethynyl]benzoate (Compound 113), 0.38 g (0.89 mmol) of trimethylsilylethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-2-yl)ethynyl]benzoate (Compound 116), was converted...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Ester.Alkyne
Ester
c1ccc2c(c1)CCCC2.c1ccccc1
null
c1ccc2c(c1)CCCC2.c1ccccc1
HO-
null
null
null
CC1(C)CCC(=O)c2ccc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)cc21.CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21>>CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-78663f7332f8419998daa1598e9a7019
CCOC(=O)C1(O)CCC(C)(C)c2c1ccc(C#Cc1ccc(C(=O)OCC[Si](C)(C)C)cc1)c2C.CCOC(=O)C1(O)CCC(C)(C)c2c1ccc(C#Cc1ccc(C(=O)OCC[Si](C)(C)C)cc1)c2C>>CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)O)cc3)ccc21
OC1(C=2C=CC(=C(C2C(CC1)(C)C)C)C#CC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)C(=O)OCC.OC1(C=2C=CC(=C(C2C(CC1)(C)C)C)C#CC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)C(=O)OCC.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>OC1(C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)O)C=C1)CC(=O)OCC
CCOC(=O)[C:7]1([OH:8])CCC(C)(C)c2c1ccc(C#Cc1ccc(C(=O)OCC[Si](C)(C)C)cc1)c2C.C[Si](C)(C)CC[O:25][C:23]([c:22]1[cH:21][cH:20][c:19]([C:18]#[C:17][c:16]2[c:15](C)[c:14]3[c:30]([cH:29][cH:28]2)[C:6](O)([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:9][CH2:10][C:11]3([CH3:12])[CH3:13])[cH:27][cH:26]1)=[O:24]>>[CH3:1][CH2:2][O:3][C:4...
CCOC(=O)C1(O)CCC(C)(C)c2c1ccc(C#Cc1ccc(C(=O)OCC[Si](C)(C)C)cc1)c2C.CCOC(=O)C1(O)CCC(C)(C)c2c1ccc(C#Cc1ccc(C(=O)OCC[Si](C)(C)C)cc1)c2C
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)O)cc3)ccc21
null
null
C1CCOC1
C-C Coupling
OtherReaction
5e6086f67bb351dc4b0e6d73161fa1416f05d08374ce8c5066c53fbd31042a7a
44b4ae204a13468e8ec96b5abf6014d1bfbaaea3ec420cf0ca0799433fb2a4cb
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
C-C-O-C(=O)-[C;H0;D4;+0:1]1(-[O;D1;H1:2])-C-C-C(-C)(-C)-c2:c-1:c:c:c(-C#C-c1:c:c:c(-C(=O)-O-C-C-[Si](-C)(-C)-C):c:c:1):c:2-C.C-[Si](-C)(-C)-C-C-[O;H0;D2;+0:3]-[C:4](=[O;D1;H0:5])-[c:6].C-[c;H0;D3;+0:7]1:[c:8]2:[c;H0;D3;+0:9](:[c:10]:[c:11]:[c:12]:1-[C:13]#[C:14]-[c:15])-[C;H0;D4;+0:16](-O)(-[C:17](=[O;D1;H0:18])-[#8:19...
null
[]
null
null
12
HOUR
To a solution of 0.25 g (0.49 mmol) of trimethylsilylethyl 4-[(5,6,7,8-tetrahydro-5-hydroxy-8,8-dimethyl-5-carboethoxy-methylnaphth-2-yl)ethynyl]benzoate (Compound 117) in 5 ml of dry THF (flushed with argon) was added 1.48 ml (1.5 mmol) of tetrabutyl ammonium fluoride (1M solution in THF). The reaction mixture was sti...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester.Tertiary alcohol.Tertiary alcohol.Alkyne.Silyl protective group.Silyl protective group
Carboxylic acid.Ester.Tertiary alcohol
c1ccc2c(c1)CCCC2.c1ccccc1.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2.c1ccccc1
HO-
C1CCOC1
null
12
CCOC(=O)C1(O)CCC(C)(C)c2c1ccc(C#Cc1ccc(C(=O)OCC[Si](C)(C)C)cc1)c2C.CCOC(=O)C1(O)CCC(C)(C)c2c1ccc(C#Cc1ccc(C(=O)OCC[Si](C)(C)C)cc1)c2C>C1CCOC1>CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)O)cc3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c6dac85cc0d34ff6820bdd2f7d903d31
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21.CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21>>CCOC(=O)CC1(O)CCC(C)(C)c2ccc(C#Cc3ccc(C(=O)OCC)cc3)cc21
OC1(C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1)CC(=O)OCC.OC1(C=2C=CC(=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1)CC(=O)OCC.CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C.CC1(CCC(C=2C=C(C=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)=O)C>>OC1(C=2C=C(C=CC2C(CC1)(C)C)C#CC1=CC=C(C(=O)OCC)C=C1)CC(=O)OCC
CCOC(=O)c1ccc(C#Cc2cc[c:32]3[c:14](c2)[C:11]([CH3:12])([CH3:13])[CH2:10][CH2:9][C:7]3([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[OH:8])cc1.CCOC(=O)CC1(O)CCC(C)(C)c2c1[cH:15][cH:16][c:17]([C:18]#[C:19][c:20]1[cH:21][cH:22][c:23]([C:24](=[O:25])[O:26][CH2:27][CH3:28])[cH:29][cH:30]1)[cH:31]2>>[CH3:1][CH2:2][O:3][C:4](=[O:5...
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21.CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21
CCOC(=O)CC1(O)CCC(C)(C)c2ccc(C#Cc3ccc(C(=O)OCC)cc3)cc21
null
null
null
Miscellaneous
OtherReaction
c2e278b01ce4d9711febfb131346be5a90905ed19322581b1150e5fa51455d26
0af981d09dd6a64dfd59aae9124418845f9a67f7be038caa795d2225b5703624
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
C-C-O-C(=O)-C-C1(-O)-C-C-C(-C)(-C)-c2:[cH;D2;+0:1]:[c:2](-[C:3]#[C:4]-[c:5]):[c:6]:[cH;D2;+0:7]:c:2-1.C-C-O-C(=O)-c1:c:c:c(-C#C-c2:c:c:[c;H0;D3;+0:8]3:[c;H0;D3;+0:9](:c:2)-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[C:13]-[C:14]-[C:15]-3(-[O;D1;H1:16])-[C:17]-[C:18](-[#8:19])=[O;D1;H0:20]):c:c:1>>[#8:19]-[C:18](=[O;D1;H0:20]...
null
[]
null
null
null
null
Employing the same general procedure as for the preparation of ethyl 4-[(7,8-dihydro-5-hydroxy-8,8-dimethyl-5-carboethoxymethylnaphth-2-yl)ethynyl]benzoate (Compound 113), 1.00 g (2.88 mmol) of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethyl-5-oxonaphth-3-yl)ethynyl]benzoate (Compound 2) was converted into the title compound...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Tertiary alcohol.Alkyne
null
c1ccccc1.c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2.c1ccccc1
HO-
null
null
null
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21.CCOC(=O)CC1(O)CCC(C)(C)c2cc(C#Cc3ccc(C(=O)OCC)cc3)ccc21>>CCOC(=O)CC1(O)CCC(C)(C)c2ccc(C#Cc3ccc(C(=O)OCC)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a56f7e2293dc4862a8c854ae1b1ae4b3
CC([O-])=S.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3)cc1>>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3C(C)=S)cc1
CC1(CCCC=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)C.CC1(CCCC=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)C.BrN1C(CCC1=O)=O.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C(C)(=S)[O-].[K+]>>CC1(CCC(C=2C=CC(=CC12)C#CC1=CC=C(C(=O)OCC)C=C1)C(C)=S)C
[O-][C:24]([CH3:25])=[S:26].[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17]2)[C:18]([CH3:19])([CH3:20])[CH2:21][CH2:22][CH2:23]3)[cH:27][cH:28]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([C:10]#[C:11][c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:17...
CC([O-])=S.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3)cc1
CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3C(C)=S)cc1
null
null
C(Cl)(Cl)(Cl)Cl
C-C Coupling
OtherReaction
21fe3870b4af9b152fbe9a5de671668cd64bbcc171946f688076c59d13f4f553
55d778e3faa8ee35a0df7132afa41f23510972a70b1f5f04051088f634cdee47
C(#Cc1ccc2c(c1)CCCC2)c1ccccc1
[C;D1;H3:1]-[C;H0;D3;+0:2](-[O-])=[S;D1;H0:3].[C:4]-[C:5]-[CH2;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:4]-[C:5]-[CH;D3;+0:6](-[C;H0;D3;+0:2](-[C;D1;H3:1])=[S;D1;H0:3])-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
To a solution of 543 mg (1.64 mmol) of ethyl 4-[(5,6,7,8-tetrahydro-8,8-dimethylnaphth-2-yl)ethynyl]benzoate (obtainable from Compound M by coupling with ethyl-4-iodobenzoate) in 20 ml of CCl4 was added 320 mg (1.81 mmol) of N-bromosuccinimide and 26 mg (0.11 mmol) of benzoyl peroxide. The mixture was refluxed for 3 ho...
10.6084/m9.figshare.5104873.v1
null
Thiocarbonyl
Thiocarbonyl
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
HO-
C(Cl)(Cl)(Cl)Cl
null
null
CC([O-])=S.CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3)cc1>C(Cl)(Cl)(Cl)Cl>CCOC(=O)c1ccc(C#Cc2ccc3c(c2)C(C)(C)CCC3C(C)=S)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cfae32b2602f43d987a2a67d53a3bee8
CC(C)C=C=O.FC(F)(F)C(Cl)Br>>CC(C)=CC(O)C(Cl)(Br)C(F)(F)F
CC(C)([O-])C.[Na+].BrC(C(F)(F)F)Cl.CC(C=C=O)C.O1CCCC1>>BrC(C(C=C(C)C)O)(C(F)(F)F)Cl
[CH3:1][CH:2]([CH3:3])[CH:4]=[C:5]=[O:6].[CH:7]([Cl:8])([Br:9])[C:10]([F:11])([F:12])[F:13]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH:5]([OH:6])[C:7]([Cl:8])([Br:9])[C:10]([F:11])([F:12])[F:13]
CC(C)C=C=O.FC(F)(F)C(Cl)Br
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F
null
null
CN(C=O)C
C-C Coupling
OtherReaction
a555a0218c8ffda0a8d9ad72f436a897605d75c2ecc35d1571cb0a895708f2b6
c0aafa762e8e97773a571cd9698e9eec9342bb07704960a5a3263af845ada306
null
[Br;D1;H0:1]-[CH;D3;+0:2](-[Cl;D1;H0:3])-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[F;D1;H0:7].[C;D1;H3:8]-[CH;D3;+0:9](-[C;D1;H3:10])-[CH;D2;+0:11]=[C;H0;D2;+0:12]=[O;H0;D1;+0:13]>>[Br;D1;H0:1]-[C;H0;D4;+0:2](-[Cl;D1;H0:3])(-[CH;D3;+0:12](-[OH;D1;+0:13])-[CH;D2;+0:11]=[C;H0;D3;+0:9](-[C;D1;H3:8])-[C;D1;H3:10])-[C:4](-[F;D1;H0...
null
[]
-78
CELSIUS
40
MINUTE
Sodium t-butoxide (1.39 g of a 42% solution in dry dimethyl formamide was added dropwise over a period of 5 minutes to a stirred mixture of 1-bromo-1-chloro-2,2,2-trifluoroethane (0.535 ml), 3-methylbut-1-en-1-al (0.538 ml) and dry tetrahydrofuran (10 ml) maintained at a temperature of -78° C. by external cooling under...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide
Tertiary halide.Tertiary halide.Secondary alcohol
null
null
null
null
CN(C=O)C
-78
0.666667
CC(C)C=C=O.FC(F)(F)C(Cl)Br>CN(C=O)C>CC(C)=CC(O)C(Cl)(Br)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-56961baabfe2420f864e8e6d0f4d6728
CC(C)=CC=O.FC(F)(F)C(Cl)Br>>CC(C)=CC(O)C(Cl)(Br)C(F)(F)F
BrC(C(F)(F)F)Cl.C(C=C(C)C)=O.CC(C)([O-])C.[Na+]>>BrC(C(C=C(C)C)O)(C(F)(F)F)Cl
[CH3:1][C:2]([CH3:3])=[CH:4][CH:5]=[O:6].[CH:7]([Cl:8])([Br:9])[C:10]([F:11])([F:12])[F:13]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH:5]([OH:6])[C:7]([Cl:8])([Br:9])[C:10]([F:11])([F:12])[F:13]
CC(C)=CC=O.FC(F)(F)C(Cl)Br
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F
null
null
O1CCCC1
C-C Coupling
OtherReaction
5435d0ec6b37aa9738fb0b43202d46adad1fb62e47985a626acc8e0a0b0a1203
cb00fcdc041dbd2da5d224bc1b019b9ae570e5bc5d8f0a5146770346817407c6
null
[Br;D1;H0:1]-[CH;D3;+0:2](-[Cl;D1;H0:3])-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[F;D1;H0:7].[C;D1;H3:8]-[C:9](-[C;D1;H3:10])=[C:11]-[CH;D2;+0:12]=[O;H0;D1;+0:13]>>[Br;D1;H0:1]-[C;H0;D4;+0:2](-[Cl;D1;H0:3])(-[CH;D3;+0:12](-[OH;D1;+0:13])-[C:11]=[C:9](-[C;D1;H3:8])-[C;D1;H3:10])-[C:4](-[F;D1;H0:5])(-[F;D1;H0:6])-[F;D1;H0:7]
73.8
[{"value": 70.0, "product": "BrC(C(C=C(C)C)O)(C(F)(F)F)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.8, "product": "BrC(C(C=C(C)C)O)(C(F)(F)F)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-60
CELSIUS
null
null
Tetrahydrofuran (230 ml) and sodium t-butoxide (57.6 g; 40% w/v solution in dimethylformamide) was charged to a split-neck reaction flask, and cooled to -60° C. with stirring. 1-Bromo-1-chloro-2,2,2-trifluorethane (47.6 g) and senecialdehyde (20.9 g) were charged simultaneously over 25 minutes, then the mixture was sti...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Aldehyde
Tertiary halide.Tertiary halide.Secondary alcohol
null
null
null
null
O1CCCC1
-60
null
CC(C)=CC=O.FC(F)(F)C(Cl)Br>O1CCCC1>CC(C)=CC(O)C(Cl)(Br)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-08430d7f4e5041b2a041747d195c0a59
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC>>COC(C)(OC)OC(C=C(C)C)C(Cl)(Br)C(F)(F)F
BrC(C(C=C(C)C)O)(C(F)(F)F)Cl.C(C)(OC)(OC)OC.C(C(C)C)(=O)O>>BrC(C(C=C(C)C)OC(C)(OC)OC)(C(F)(F)F)Cl
[OH:7][CH:8]([CH:9]=[C:10]([CH3:11])[CH3:12])[C:13]([Cl:14])([Br:15])[C:16]([F:17])([F:18])[F:19].CO[C:3]([O:2][CH3:1])([CH3:4])[O:5][CH3:6]>>[CH3:1][O:2][C:3]([CH3:4])([O:5][CH3:6])[O:7][CH:8]([CH:9]=[C:10]([CH3:11])[CH3:12])[C:13]([Cl:14])([Br:15])[C:16]([F:17])([F:18])[F:19]
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC
COC(C)(OC)OC(C=C(C)C)C(Cl)(Br)C(F)(F)F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
da59a6e496e58629453a78c5e1487b31b25688d768592f6d7000493943d39c02
9cde3f0ce3308e8c18bafc8301e5ba0177f0ef4f63237b39a252a2d6edcd92fd
null
C-O-[C;H0;D4;+0:1](-[C;D1;H3:2])(-[#8:3]-[C;D1;H3:4])-[#8:5]-[C;D1;H3:6].[C:7]-[C:8](-[OH;D1;+0:9])-[C:10]=[C:11](-[C;D1;H3:12])-[C;D1;H3:13]>>[C:7]-[C:8](-[C:10]=[C:11](-[C;D1;H3:12])-[C;D1;H3:13])-[O;H0;D2;+0:9]-[C;H0;D4;+0:1](-[C;D1;H3:2])(-[#8:3]-[C;D1;H3:4])-[#8:5]-[C;D1;H3:6]
null
[]
111
CELSIUS
null
null
5-Bromo-5-chloro-4-hydroxy-2-methyl-6,6,6-trifluorohex-2-ene (10.0 g), trimethyl orthoacetate (48.0 g) and isobutyric acid (0.29 g) were charged to a round-bottomed flask fitted with: nitrogen inlet/bubbler, thermometer and Dean and Stark received packed with 5A molecular seives. The mixture was heated with agitation t...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Secondary alcohol
Ether.Ether.Ether
null
null
null
HO-
null
111
null
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC>>COC(C)(OC)OC(C=C(C)C)C(Cl)(Br)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d60f1ea20aa0467e8d0f2bb79c4451e3
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC>>COC(=O)CC(C)(C)C=CC(Cl)(Br)C(F)(F)F
BrC(C(C=C(C)C)O)(C(F)(F)F)Cl.C(C)(OC)(OC)OC>>BrC(C=CC(CC(=O)OC)(C)C)(C(F)(F)F)Cl
O[CH:10]([CH:9]=[C:6]([CH3:7])[CH3:8])[C:11]([Cl:12])([Br:13])[C:14]([F:15])([F:16])[F:17].CO[C:3]([O:2][CH3:1])([O:4]C)[CH3:5]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][C:6]([CH3:7])([CH3:8])[CH:9]=[CH:10][C:11]([Cl:12])([Br:13])[C:14]([F:15])([F:16])[F:17]
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC
COC(=O)CC(C)(C)C=CC(Cl)(Br)C(F)(F)F
null
O.[O-2].[O-2].[O-2].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.[Al+3].[Al+3]
null
Acylation
OtherReaction
62d15542be43b94a80da01568db53380356499d771ca28bc7e0ff722d34a5863
98ff49def7e6e395079390a512d545b9d4d6c593686e816bc1a43a7ae419027a
null
C-O-[C;H0;D4;+0:1](-[CH3;D1;+0:2])(-[#8:3]-[C;D1;H3:4])-[O;H0;D2;+0:5]-C.O-[CH;D3;+0:6](-[CH;D2;+0:7]=[C;H0;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10])-[C:11](-[Br;D1;H0:12])(-[Cl;D1;H0:13])-[C:14](-[F;D1;H0:15])(-[F;D1;H0:16])-[F;D1;H0:17]>>[Br;D1;H0:12]-[C:11](-[Cl;D1;H0:13])(-[CH;D2;+0:6]=[CH;D2;+0:7]-[C;H0;D4;+0:8](-[C;D1...
65
[{"value": 59.0, "product": "BrC(C=CC(CC(=O)OC)(C)C)(C(F)(F)F)Cl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.0, "product": "BrC(C=CC(CC(=O)OC)(C)C)(C(F)(F)F)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
111
CELSIUS
1
HOUR
5-Bromo-5-chloro-4-hydroxy-2-methyl-6,6,6-trifluorohex-2-ene (10.0 g), trimethyl orthoacetate (16.0 g) and Montmorillonite KSF (0.5 g) were charged to a round-bottomed flask fitted with: nitrogen inlet/bubbler, thermometer and still-head. The mixture was heated with agitation, and the methanol-trimethyl orthoacetate di...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Secondary alcohol
Ester
null
null
null
HO-
O.[O-2].[O-2].[O-2].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.[Al+3].[Al+3]
111
1
CC(C)=CC(O)C(Cl)(Br)C(F)(F)F.COC(C)(OC)OC>O.[O-2].[O-2].[O-2].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.[Al+3].[Al+3]>COC(=O)CC(C)(C)C=CC(Cl)(Br)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d42202fb4a7943b3bbc1a6d0fce478fe
CC(C)=CC(O)C(Cl)(Cl)C(F)(F)F.CCOC(C)(OCC)OCC>>CCOC(=O)CC(C)(C)C=CC(Cl)(Cl)C(F)(F)F
C(C)(OCC)(OCC)OCC.ClC(C(C=C(C)C)O)(C(F)(F)F)Cl.C(C(C)C)(=O)O>>ClC(C=CC(CC(=O)OCC)(C)C)(C(F)(F)F)Cl
O[CH:11]([CH:10]=[C:7]([CH3:8])[CH3:9])[C:12]([Cl:13])([Cl:14])[C:15]([F:16])([F:17])[F:18].CCO[C:4]([O:3][CH2:2][CH3:1])([O:5]CC)[CH3:6]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7]([CH3:8])([CH3:9])[CH:10]=[CH:11][C:12]([Cl:13])([Cl:14])[C:15]([F:16])([F:17])[F:18]
CC(C)=CC(O)C(Cl)(Cl)C(F)(F)F.CCOC(C)(OCC)OCC
CCOC(=O)CC(C)(C)C=CC(Cl)(Cl)C(F)(F)F
null
null
null
Acylation
OtherReaction
62d15542be43b94a80da01568db53380356499d771ca28bc7e0ff722d34a5863
98ff49def7e6e395079390a512d545b9d4d6c593686e816bc1a43a7ae419027a
null
C-C-O-[C;H0;D4;+0:1](-[CH3;D1;+0:2])(-[#8:3]-[C:4])-[O;H0;D2;+0:5]-C-C.O-[CH;D3;+0:6](-[CH;D2;+0:7]=[C;H0;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10])-[C:11](-[Cl;D1;H0:12])(-[Cl;D1;H0:13])-[C:14](-[F;D1;H0:15])(-[F;D1;H0:16])-[F;D1;H0:17]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;H0;D1;+0:5])-[CH2;D2;+0:2]-[C;H0;D4;+0:8](-[C;D1;H3:9])...
null
[]
null
null
null
null
A mixture of triethyl orthoacetate (25 ml), 5,5-dichloro-4-hydroxy-2-methyl-6,6,6-trifluorohex-2-ene (3.5 g), and isobutyric acid (0.11 g) was heated at the reflux temperature. The refluxing volatiles were condensed and collected in a Dean & Stark apparatus containing molecular sieves (4A) to collect the by-product eth...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Secondary alcohol
Ester
null
null
null
HO-
null
null
null
CC(C)=CC(O)C(Cl)(Cl)C(F)(F)F.CCOC(C)(OCC)OCC>>CCOC(=O)CC(C)(C)C=CC(Cl)(Cl)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-70ae7882edfe4b59882bded66d4f531c
CC1(C)OC(CO)C(CO)O1.CCOC(=O)CC(=O)CCl>>CCOC(=O)CC(=O)COCC1OC(C)(C)OC1COCC(=O)CC(=O)OCC
[H-].[Na+].ClCC(CC(=O)OCC)=O.CC1(OC(C(O1)CO)CO)C>>C(C)OC(CC(COCC1OC(OC1COCC(CC(=O)OCC)=O)(C)C)=O)=O
[CH3:1][C:14]1([CH3:16])[O:13][CH:12]([CH2:2][OH:3])[CH:18]([CH2:19][OH:20])[O:17]1.Cl[CH2:21][C:22](=[O:23])[CH2:24][C:25](=[O:26])[O:27][CH2:28][CH3:29]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7](=[O:8])[CH2:9][O:10][CH2:11][CH:12]1[O:13][C:14]([CH3:15])([CH3:16])[O:17][CH:18]1[CH2:19][O:20][CH2:21][C:22](=[O:23])...
CC1(C)OC(CO)C(CO)O1.CCOC(=O)CC(=O)CCl
CCOC(=O)CC(=O)COCC1OC(C)(C)OC1COCC(=O)CC(=O)OCC
null
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
0344072df22acf89147411ca83c03c260456897ced6262baad4d664f99cc7453
6718608c291f284d92dbc0a9a9fe817322a6ccdd03478eb057cf50201a353fab
C1COCO1
Cl-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7].[C;D1;H3:8]-[C;H0;D4;+0:9]1(-[CH3;D1;+0:10])-[#8:11]-[CH;D3;+0:12](-[CH2;D2;+0:13]-[OH;D1;+0:14])-[C:15](-[C:16]-[OH;D1;+0:17])-[#8:18]-1>>[#8:19]-[C:20]-[CH;D3;+0:12]1-[#8:11]-[C;H0;D4;+0:9](-[C;D1;H3:21])(-[C;D1;H3:8])-[#8:18]-[C:15]-1-[C:16]-[O;H0...
43.7
[{"value": 43.7, "product": "C(C)OC(CC(COCC1OC(OC1COCC(CC(=O)OCC)=O)(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of sodium hydride (4.0 g, 60% dispersion in oil) in tetrahydrofuran (150 mL) under a nitrogen atmosphere was added a solution of 2,2-dimethyl-[1,3]dioxolane-4,5-dimethanol (VII, 4.05 g) in tetrahydrofuran (25 mL) over 2 min at room temperature, followed by solid tetrabutylammonium hydrogen sulfate (0.4 ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Ether.Ether.Primary alcohol.Primary alcohol
Ketone.Ketone.Ester.Ether.Ether.Ether.Ether
C1COCO1
C1COCO1
C1COCO1
null
S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.O1CCCC1
null
null
CC1(C)OC(CO)C(CO)O1.CCOC(=O)CC(=O)CCl>S(=O)(=O)(O)[O-].C(CCC)[N+](CCCC)(CCCC)CCCC.O1CCCC1>CCOC(=O)CC(=O)COCC1OC(C)(C)OC1COCC(=O)CC(=O)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bcfe7e4ce5914fd798eabd94aed3d84f
CC1(C)OCC(CO)O1.CCOC(=O)CC(=O)CCl>>CCOC(=O)CC(=O)COCC1COC(C)(C)O1
ClCC(CC(=O)OCC)=O.CC1(OCC(O1)CO)C.[H-].[Na+]>>C(C)OC(CC(COCC1OC(OC1)(C)C)=O)=O
[OH:10][CH2:11][CH:12]1[CH2:13][O:14][C:15]([CH3:16])([CH3:17])[O:18]1.Cl[CH2:9][C:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])=[O:8]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7](=[O:8])[CH2:9][O:10][CH2:11][CH:12]1[CH2:13][O:14][C:15]([CH3:16])([CH3:17])[O:18]1
CC1(C)OCC(CO)O1.CCOC(=O)CC(=O)CCl
CCOC(=O)CC(=O)COCC1COC(C)(C)O1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
fbcfc5578f28d9d8930a708c71944acf35323dc567d3a35141adc89c3fb4ae9e
7d4d679c705f72095ba1d241e831385ef35d8aef34f3127d947d089fa3227973
C1COCO1
Cl-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7].[#8:8]-[C:9]-[C:10]-[OH;D1;+0:11]>>[#8:8]-[C:9]-[C:10]-[O;H0;D2;+0:11]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[C:5](-[#8:6])=[O;D1;H0:7]
50.1
[{"value": 50.1, "product": "C(C)OC(CC(COCC1OC(OC1)(C)C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
HOUR
To a suspension of sodium hydride (55 g, 60% dispersion in oil) in tetrahydrofuran (1L) under a nitrogen atmosphere was added a solution of 2,2-dimethyl-[1,3]dioxolane-4-methanol (XV, 102.4 g) in tetrahydrofuran (250 mL) over 15 min at room temperature. The resulting mixture was cooled in an ice bath and a solution of ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Primary alcohol
Ketone.Ether
null
null
C1COCO1
HCl
O1CCCC1
null
20
CC1(C)OCC(CO)O1.CCOC(=O)CC(=O)CCl>O1CCCC1>CCOC(=O)CC(=O)COCC1COC(C)(C)O1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-df519091f55147ec9c9c3a495aefb74e
CCOC(=O)C1=C(COCC(O)CO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl>>CCOC(=O)C1=C(COCC=O)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
[Cl-].[NH4+].COC(=O)C=1C(C(=C(NC1C)COCC(CO)O)C(=O)OCC)C1=C(C=CC=C1)Cl.I(=O)(=O)(=O)[O-].[Na+]>>COC(=O)C1=C(NC(=C(C1C1=C(C=CC=C1)Cl)C(=O)OCC)COCC=O)C
OC[CH:11]([CH2:10][O:9][CH2:8][C:7]1=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH:21]([c:22]2[cH:23][cH:24][cH:25][cH:26][c:27]2[Cl:28])[C:16]([C:17](=[O:18])[O:19][CH3:20])=[C:14]([CH3:15])[NH:13]1)[OH:12]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([CH2:8][O:9][CH2:10][CH:11]=[O:12])[NH:13][C:14]([CH3:15])=[C:16]([C:...
CCOC(=O)C1=C(COCC(O)CO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
CCOC(=O)C1=C(COCC=O)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
null
null
CO.O
Miscellaneous
OtherReaction
6b26fe5aae922ff894047a49926c0aceb5638cd263aa19950a2aab435845c036
1f7d0f705fc2b6dec522235bbfa5fd9d570e6409417a0c4e8313976c2a5c011a
C1=CC(c2ccccc2)C=CN1
O-C-[CH;D3;+0:1](-[OH;D1;+0:2])-[C:3]-[#8:4]>>[#8:4]-[C:3]-[CH;D2;+0:1]=[O;H0;D1;+0:2]
97.9
[{"value": 97.9, "product": "COC(=O)C1=C(NC(=C(C1C1=C(C=CC=C1)Cl)C(=O)OCC)COCC=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To an ice-cooled solution of 4-(2-chlorophenyl)-2-(2,3-dihydroxypropoxymethyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester (IC, 13.0 g) in methanol (150 mL) was added a solution of sodium periodate (7.6 g) dissolved in water (100 mL) dropwise over 15 min. After stirring for 10 min, a satur...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Secondary alcohol
Aldehyde
null
null
C1=CNC=CC1.c1ccccc1
HO-
CO.O
null
0.166667
CCOC(=O)C1=C(COCC(O)CO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl>CO.O>CCOC(=O)C1=C(COCC=O)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4264e1627523496cb0a0bc9ac274b94e
CCOC(=O)C1=C(COCC=O)NC(C)=C(C(=O)OC)C1c1ccccc1Cl.[NH3+]O>>CCOC(=O)C1=C(COCC=NO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
COC(=O)C1=C(NC(=C(C1C1=C(C=CC=C1)Cl)C(=O)OCC)COCC=O)C.Cl.O[NH3+].C(C)N(CC)CC>>COC(=O)C=1C(C(=C(NC1C)COCC=NO)C(=O)OCC)C1=C(C=CC=C1)Cl
O=[CH:11][CH2:10][O:9][CH2:8][C:7]1=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH:22]([c:23]2[cH:24][cH:25][cH:26][cH:27][c:28]2[Cl:29])[C:17]([C:18](=[O:19])[O:20][CH3:21])=[C:15]([CH3:16])[NH:14]1.[NH3+:12][OH:13]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([CH2:8][O:9][CH2:10][CH:11]=[N:12][OH:13])[NH:14][C:15]([CH3:...
CCOC(=O)C1=C(COCC=O)NC(C)=C(C(=O)OC)C1c1ccccc1Cl.[NH3+]O
CCOC(=O)C1=C(COCC=NO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
null
null
CO
Functional Group Interconversion
OtherReaction
9575b3f7e9975c02abe24e99b2681a2813f6f73af9b27467491bf10c6c26ae48
5ddad3e703fe819c706f37fb03eddf29d0a60c973b030a231bcdc1b66cd51b53
C1=CC(c2ccccc2)C=CN1
O=[CH;D2;+0:1]-[C:2]-[#8:3].[NH3+;D1:4]-[O;D1;H1:5]>>[#8:3]-[C:2]-[CH;D2;+0:1]=[N;H0;D2;+0:4]-[O;D1;H1:5]
null
[]
null
null
6
HOUR
A mixture of 4-(2-chlorophenyl)-2-methyl-6-(2-oxo-ethoxymethyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid 5-ethyl 3-methyl ester (ID, 6.2 g), hydroxylammonium hydrochloride (1.27 g) and triethylamine (1.85 g) in methanol (100 mL) was stirred at room temperature for 6 h. Methanol was removed under reduced pressure and t...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Oxime
null
null
C1=CNC=CC1.c1ccccc1
HO-
CO
null
6
CCOC(=O)C1=C(COCC=O)NC(C)=C(C(=O)OC)C1c1ccccc1Cl.[NH3+]O>CO>CCOC(=O)C1=C(COCC=NO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-db51435d97f64dfb86f4de59e3efb185
CCOC(=O)C1=C(COCC=NO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl>>CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
COC(=O)C=1C(C(=C(NC1C)COCC=NO)C(=O)OCC)C1=C(C=CC=C1)Cl.C(=O)[O-].[NH4+]>>COC(=O)C=1C(C(=C(NC1C)COCCN)C(=O)OCC)C1=C(C=CC=C1)Cl
O[N:12]=[CH:11][CH2:10][O:9][CH2:8][C:7]1=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH:21]([c:22]2[cH:23][cH:24][cH:25][cH:26][c:27]2[Cl:28])[C:16]([C:17](=[O:18])[O:19][CH3:20])=[C:14]([CH3:15])[NH:13]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([CH2:8][O:9][CH2:10][CH2:11][NH2:12])[NH:13][C:14]([CH3:15])=[C:16]([C:1...
CCOC(=O)C1=C(COCC=NO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
null
[OH-].[OH-].[Pd+2]
CO
Reduction
OtherReaction
2911de7676f9c054838849cab652dcb324de4944866edb887235c5bf7854a715
4a7bf747f64425b21ceaa04fbc4c046ccf522c774aa5649ec92eba03e46bfee5
C1=CC(c2ccccc2)C=CN1
O-[N;H0;D2;+0:1]=[CH;D2;+0:2]-[C:3]-[#8:4]>>[#8:4]-[C:3]-[CH2;D2;+0:2]-[NH2;D1;+0:1]
60.7
[{"value": 60.7, "product": "COC(=O)C=1C(C(=C(NC1C)COCCN)C(=O)OCC)C1=C(C=CC=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4-(2-chlorophenyl)-2-(2-hydroxyimino-ethoxymethyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester (IBa, 150 mg), palladium hydroxide on carbon (10 mg) and ammonium formate (224 mg) in methanol (10 mL) was refluxed for 5 h under a nitrogen atmosphere. On cooling to room temperatur...
10.6084/m9.figshare.5104873.v1
null
Oxime
Primary amine
null
null
C1=CNC=CC1.c1ccccc1
Other
[OH-].[OH-].[Pd+2].CO
null
null
CCOC(=O)C1=C(COCC=NO)NC(C)=C(C(=O)OC)C1c1ccccc1Cl>[OH-].[OH-].[Pd+2].CO>CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1b853575abe94e7c8c35c82d1e1ed7b0
CCOC(=O)C1=C(COCC(OC)OC)NC(C)=C(C(=O)OC)C1c1ccccc1Cl>>CCOC(=O)C1=C2COC=CN2C(C)=C(C(=O)OC)C1c1ccccc1Cl
COC(=O)C=1C(C(=C(NC1C)COCC(OC)OC)C(=O)OCC)C1=C(C=CC=C1)Cl.Cl>>COC(=O)C=1C(C(=C2COC=CN2C1C)C(=O)OCC)C1=C(C=CC=C1)Cl
CO[CH:11](OC)[CH2:10][O:9][CH2:8][C:7]1=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH:20]([c:21]2[cH:22][cH:23][cH:24][cH:25][c:26]2[Cl:27])[C:15]([C:16](=[O:17])[O:18][CH3:19])=[C:13]([CH3:14])[NH:12]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]2[CH2:8][O:9][CH:10]=[CH:11][N:12]2[C:13]([CH3:14])=[C:15]([C:16](=[O:17])[...
CCOC(=O)C1=C(COCC(OC)OC)NC(C)=C(C(=O)OC)C1c1ccccc1Cl
CCOC(=O)C1=C2COC=CN2C(C)=C(C(=O)OC)C1c1ccccc1Cl
null
null
O1CCCC1
Functional Group Interconversion
OtherReaction
ff6e2150b37df9c6c7faec8b31e0ff9a35bb825185a402a3b3e4ef2fea8d8338
de73217b601b2798317d9de7c02a4c2a49bf20113d826b0123ad95bf25a4855f
C1=CN2C=CC(c3ccccc3)C=C2CO1
C-O-[CH;D3;+0:1](-O-C)-[CH2;D2;+0:2]-[#8:3]-[C:4]-[C:5]1=[C:6](-[C:7](-[#8:8])=[O;D1;H0:9])-[C:10]-[C:11](-[C:12](-[#8:13])=[O;D1;H0:14])=[C:15](-[C;D1;H3:16])-[NH;D2;+0:17]-1>>[#8:13]-[C:12](=[O;D1;H0:14])-[C:11]1=[C:15](-[C;D1;H3:16])-[N;H0;D3;+0:17]2-[CH;D2;+0:1]=[CH;D2;+0:2]-[#8:3]-[C:4]-[C:5]-2=[C:6](-[C:7](-[#8:8...
65.8
[{"value": 65.8, "product": "COC(=O)C=1C(C(=C2COC=CN2C1C)C(=O)OCC)C1=C(C=CC=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 4-(2-chlorophenyl)-2-(2,2-dimethoxy-ethoxymethyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester (XX, 9.2 g) in tetrahydrofuran (200 mL) was added 3N hydrochloric acid (40 mL). The mixture was then refluxed for 4 h. On cooling to room temperature, tetrahydrofuran was removed ...
10.6084/m9.figshare.5104873.v1
null
Enamine.Enamine.Ether.Ether.Ether
Enamine.Enamine.Enamine
C1=CNC=CC1
C1=CN2C=COCC2=CC1
C1=CN2C=COCC2=CC1.c1ccccc1
HO-
O1CCCC1
null
null
CCOC(=O)C1=C(COCC(OC)OC)NC(C)=C(C(=O)OC)C1c1ccccc1Cl>O1CCCC1>CCOC(=O)C1=C2COC=CN2C(C)=C(C(=O)OC)C1c1ccccc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d1e2912f9b2444eeb1e5ad64e18d1404
CCOC(=O)CC(=O)CCl.COC(=O)C=C(C)NCCO.O=Cc1ccccc1Cl>>CCOC(=O)C1=C(CCl)N2CCOC2(C)C(C(=O)OC)C1c1ccccc1Cl
ClC1=C(C=O)C=CC=C1.ClCC(CC(=O)OCC)=O.COC(C=C(C)NCCO)=O>>COC(=O)C1C2(N(C(=C(C1C1=C(C=CC=C1)Cl)C(=O)OCC)CCl)CCO2)C
O=[C:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:8][Cl:9].[NH:10]([CH2:11][CH2:12][OH:13])[C:14]([CH3:15])=[CH:16][C:17](=[O:18])[O:19][CH3:20].O=[CH:21][c:22]1[cH:23][cH:24][cH:25][cH:26][c:27]1[Cl:28]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([CH2:8][Cl:9])[N:10]2[CH2:11][CH2:12][O:13][C:14]2([CH3:15])[CH:16]...
CCOC(=O)CC(=O)CCl.COC(=O)C=C(C)NCCO.O=Cc1ccccc1Cl
CCOC(=O)C1=C(CCl)N2CCOC2(C)C(C(=O)OC)C1c1ccccc1Cl
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
45bba53f2703211ee8e72a28add2f98a7e77aabd35fbf31ad11867ca7492972e
1b0a543a218938f814aab8e10edc774aa5e088d2d7ffce8b04acddeef534f28b
C1=CN2CCOC2CC1c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[Cl;D1;H0:3])-[CH2;D2;+0:4]-[C:5](=[O;D1;H0:6])-[#8:7]-[C:8].O=[CH;D2;+0:9]-[c:10](:[c:11]):[c:12].[C;D1;H3:13]-[C;H0;D3;+0:14](=[CH;D2;+0:15]-[C:16](=[O;D1;H0:17])-[#8:18]-[C;D1;H3:19])-[NH;D2;+0:20]-[C:21]-[C:22]-[OH;D1;+0:23]>>[C:8]-[#8:7]-[C:5](=[O;D1;H0:6])-[C;H0;D3;+0:4]1=[C;H0;D3;+0:1](-[...
17.6
[{"value": 17.6, "product": "COC(=O)C1C2(N(C(=C(C1C1=C(C=CC=C1)Cl)C(=O)OCC)CCl)CCO2)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
48
HOUR
A mixture of 2-chlorobenzaldehyde (XI, 57.0 g), ethyl 4-chloroacetoacetate (VIII, 69.3 g) and 3-(2-hydroxyethylamino)-but-2-enoic acid methyl ester (XXIII, 63.2 g) in methanol (800 mL) was stirred at room temperature for 48 h. Methanol was removed under reduced pressure and the residue dissolved in ethyl acetate (400 m...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aldehyde.Ketone.Ester.Ester.Primary alcohol
Enamine.Ester.Ester.Ether
null
C1=CN2CCOC2CC1
C1=CN2CCOC2CC1.c1ccccc1
HO-
CO
null
48
CCOC(=O)CC(=O)CCl.COC(=O)C=C(C)NCCO.O=Cc1ccccc1Cl>CO>CCOC(=O)C1=C(CCl)N2CCOC2(C)C(C(=O)OC)C1c1ccccc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-69d79d7234c34dfc9b1df959b118c003
COC(=O)CC(C)=O.NCCO>>COC(=O)C=C(C)NCCO
C(O)CN.C(CC(=O)C)(=O)OC>>COC(C=C(C)NCCO)=O
O=[C:6]([CH2:5][C:3]([O:2][CH3:1])=[O:4])[CH3:7].[NH2:8][CH2:9][CH2:10][OH:11]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]=[C:6]([CH3:7])[NH:8][CH2:9][CH2:10][OH:11]
COC(=O)CC(C)=O.NCCO
COC(=O)C=C(C)NCCO
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2308c5562a388f5a3972b1c218a1d28a1c29d68e0019b4c583e0642f86effe2c
386abf15293513363decea2e36c34c5591e7bebcecf634963fbfb09ec1e3b1bc
null
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[CH2;D2;+0:3]-[C:4](=[O;D1;H0:5])-[#8:6]-[C;D1;H3:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[CH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[#8:6]-[C;D1;H3:7]
91.2
[{"value": 91.2, "product": "COC(C=C(C)NCCO)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To an ice-cooled sample of ethanolamine (6.1 g) was added methyl acetoacetate (11.6 g) dropwise. Compound (XXIII 14.5 g) was formed within 30 min (U.S. Pat. No. 1102800). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Primary amine
Enamine
null
null
null
HO-
null
null
null
COC(=O)CC(C)=O.NCCO>>COC(=O)C=C(C)NCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-54b03352f0df47deb65aac6e35fc4ae0
CCC(Cc1ccccc1-c1ccccc1)C(=O)O.O=S(Cl)Cl>>CCC(Cc1ccccc1-c1ccccc1)C(=O)Cl
C1(=C(C=CC=C1)CC(C(=O)O)CC)C1=CC=CC=C1.S(=O)(Cl)Cl>>C1(=C(C=CC=C1)CC(C(=O)Cl)CC)C1=CC=CC=C1
O[C:17]([CH:3]([CH2:2][CH3:1])[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1-[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)=[O:18].O=S(Cl)[Cl:19]>>[CH3:1][CH2:2][CH:3]([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1-[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[C:17](=[O:18])[Cl:19]
CCC(Cc1ccccc1-c1ccccc1)C(=O)O.O=S(Cl)Cl
CCC(Cc1ccccc1-c1ccccc1)C(=O)Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
c1ccc(-c2ccccc2)cc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4](-[C:5])-[C:6]>>[C:5]-[C:4](-[C:6])-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
106.3
[{"value": 106.3, "product": "C1(=C(C=CC=C1)CC(C(=O)Cl)CC)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A 100-ml three-necked round flask equipped with a stirring bar, a Dimroth condenser, a thermometer and a NaOH trap was charged with 13.3 g (52.4 mmol) of 3-(2-biphenylyl)-2-ethylpropionic acid and 25.9 ml (355 mmol) of thionyl chloride, and the resulting mixture was stirred under reflux for 2.5 hours under a nitrogen a...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1.c1ccccc1
HCl
null
null
null
CCC(Cc1ccccc1-c1ccccc1)C(=O)O.O=S(Cl)Cl>>CCC(Cc1ccccc1-c1ccccc1)C(=O)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-09d8e89ed27a4556962f79ec5f092948
CCC1Cc2c(cccc2-c2ccccc2)C1=O>>CCC1=Cc2c(-c3ccccc3)cccc2C1O
CC(=O)C.[BH4-].[Na+].C(C)C1C(C2=CC=CC(=C2C1)C1=CC=CC=C1)=O.[BH4-].[Na+]>>C(C)C=1C(C2=CC=CC(=C2C1)C1=CC=CC=C1)O
[CH3:1][CH2:2][CH:3]1[CH2:4][c:5]2[c:6](-[c:7]3[cH:8][cH:9][cH:10][cH:11][cH:12]3)[cH:13][cH:14][cH:15][c:16]2[C:17]1=[O:18]>>[CH3:1][CH2:2][C:3]1=[CH:4][c:5]2[c:6](-[c:7]3[cH:8][cH:9][cH:10][cH:11][cH:12]3)[cH:13][cH:14][cH:15][c:16]2[CH:17]1[OH:18]
CCC1Cc2c(cccc2-c2ccccc2)C1=O
CCC1=Cc2c(-c3ccccc3)cccc2C1O
null
null
C(C)O
Miscellaneous
OtherReaction
1c8237a20e7497d53def9024475d65ea3729a4e2375df0c6e7118649b93b9d03
65c0f1e474134afe581396038c9eec1081d3cf2c66a067b33a419661521d5253
C1=Cc2c(cccc2-c2ccccc2)C1
[C;D1;H3:1]-[C:2]-[CH;D3;+0:3]1-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7](:[c:8])-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]>>[C;D1;H3:1]-[C:2]-[C;H0;D3;+0:3]1=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7](:[c:8])-[CH;D3;+0:9]-1-[OH;D1;+0:10]
100.1
[{"value": 99.0, "product": "C(C)C=1C(C2=CC=CC(=C2C1)C1=CC=CC=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.1, "product": "C(C)C=1C(C2=CC=CC(=C2C1)C1=CC=CC=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3.5
HOUR
A 200-ml three-necked round flask equipped with a stirring bar, a Dimroth condenser, a dropping funnel and a thermometer was charged with 0.85 g (22.6 mmol) of sodium borohydride and 28 ml of ethanol. To the mixture was dropwise added a solution containing 10.6 g (45.1 mmol) of the above-obtained 2-ethyl-4-phenyl-1-ind...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
c1ccc2c(c1)CCC2
C1=Cc2ccccc2C1
c1ccccc1.C1=Cc2ccccc2C1
null
C(C)O
null
3.5
CCC1Cc2c(cccc2-c2ccccc2)C1=O>C(C)O>CCC1=Cc2c(-c3ccccc3)cccc2C1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1a1bc6cce7d6438fb61cdd07c56a6ee6
CCC1Cc2c(-c3ccccc3)cccc2C1O>>CCC1=Cc2c(cccc2-c2ccccc2)C1
C(C)C1C(C2=CC=CC(=C2C1)C1=CC=CC=C1)O.C(C)N(CC)CC.CS(=O)(=O)Cl>>C(C)C=1CC2=CC=CC(=C2C1)C1=CC=CC=C1
O[CH:4]1[CH:3]([CH2:2][CH3:1])[CH2:17][c:6]2[c:5]1[cH:7][cH:8][cH:9][c:10]2-[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH3:1][CH2:2][C:3]1=[CH:4][c:5]2[c:6]([cH:7][cH:8][cH:9][c:10]2-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[CH2:17]1
CCC1Cc2c(-c3ccccc3)cccc2C1O
CCC1=Cc2c(cccc2-c2ccccc2)C1
null
CN(C1=CC=NC=C1)C
C(Cl)Cl
Functional Group Interconversion
OtherReaction
77cbac765057fd7cdc9bab7700bc44fd842074b8261be2244e17dfd2370accb3
f8118e7f3e1d7109575c0c77239dee8da98ec71a2b23460bcda2084274bdf7e7
C1=Cc2c(cccc2-c2ccccc2)C1
O-[CH;D3;+0:1]1-[CH;D3;+0:2](-[C:3]-[C;D1;H3:4])-[C:5]-[c;H0;D3;+0:6]2:[c;H0;D3;+0:7](-[c:8](:[c:9]):[c:10]):[c:11]:[c:12]:[cH;D2;+0:13]:[c;H0;D3;+0:14]:2-1>>[C;D1;H3:4]-[C:3]-[C;H0;D3;+0:2]1=[CH;D2;+0:1]-[c;H0;D3;+0:14]2:[c;H0;D3;+0:7](-[c:8](:[c:9]):[c:10]):[c:11]:[c:12]:[cH;D2;+0:13]:[c;H0;D3;+0:6]:2-[C:5]-1
73
[{"value": 73.0, "product": "C(C)C=1CC2=CC=CC(=C2C1)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.1, "product": "C(C)C=1CC2=CC=CC(=C2C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3.5
HOUR
A 300-ml four-necked round flask equipped with a stirring bar, a dropping funnel and a thermometer was charged with 9.78 g (41.3 mmol) of 2-ethyl-1-hydroxy-4-phenylindane, 17.2 ml (123.8 mmol) of triethylamine, 0.25 g (2.1 mmol) of 4-dimethylaminopyridine and 98 ml of methylene chloride. To the mixture was dropwise add...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
c1ccc2c(c1)CCC2
C1=Cc2ccccc2C1
C1=Cc2ccccc2C1.c1ccccc1
HO-
CN(C1=CC=NC=C1)C.C(Cl)Cl
null
3.5
CCC1Cc2c(-c3ccccc3)cccc2C1O>CN(C1=CC=NC=C1)C.C(Cl)Cl>CCC1=Cc2c(cccc2-c2ccccc2)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6f4401e734f84a7c9ca25250dd8869e3
CCCC(Cc1ccccc1Br)C(=O)O.O=S(Cl)Cl>>CCCC(Cc1ccccc1Br)C(=O)Cl
BrC1=C(C=CC=C1)CC(C(=O)O)CCC.S(=O)(Cl)Cl>>BrC1=C(C=CC=C1)CC(C(=O)Cl)CCC
O[C:13]([CH:4]([CH2:3][CH2:2][CH3:1])[CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[Br:12])=[O:14].O=S(Cl)[Cl:15]>>[CH3:1][CH2:2][CH2:3][CH:4]([CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[Br:12])[C:13](=[O:14])[Cl:15]
CCCC(Cc1ccccc1Br)C(=O)O.O=S(Cl)Cl
CCCC(Cc1ccccc1Br)C(=O)Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_SOCl2
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
c1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4](-[C:5])-[C:6]>>[C:5]-[C:4](-[C:6])-[C;H0;D3;+0:2](-[Cl;H0;D1;+0:1])=[O;D1;H0:3]
null
[]
null
null
null
null
A 500-ml three-necked round flask equipped with a stirring bar, a Dimroth condenser, a thermometer and a NaOH trap was charged with 277 mmol of 3-(2-bromophenyl)-2-propylpropionic acid and 200 ml of thionyl chloride, and the mixture was heated under reflux for 2 hours. Then, the excess thionyl chloride was removed by a...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1
HCl
null
null
null
CCCC(Cc1ccccc1Br)C(=O)O.O=S(Cl)Cl>>CCCC(Cc1ccccc1Br)C(=O)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c816ac4ef7654d68886954c067ebcb25
CCC1Cc2c(-c3cc4ccccc4c4ccccc34)cccc2C1O>>CCC1=Cc2c(cccc2-c2cc3ccccc3c3ccccc23)C1
C(C)C1C(C2=CC=CC(=C2C1)C=1C2=CC=CC=C2C=2C=CC=CC2C1)O.C(C)N(CC)CC.C([O-])(O)=O.[Na+].CS(=O)(=O)Cl>>C(C)C=1CC2=CC=CC(=C2C1)C=1C2=CC=CC=C2C=2C=CC=CC2C1
O[CH:25]1[CH:3]([CH2:2][CH3:1])[CH2:4][c:5]2[c:6]1[cH:7][cH:8][cH:9][c:10]2-[c:11]1[cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[c:19]2[cH:20][cH:21][cH:22][cH:23][c:24]12>>[CH3:1][CH2:2][C:3]1=[CH:4][c:5]2[c:6]([cH:7][cH:8][cH:9][c:10]2-[c:11]2[cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]3[c:19]3[cH:20][cH:21][...
CCC1Cc2c(-c3cc4ccccc4c4ccccc34)cccc2C1O
CCC1=Cc2c(cccc2-c2cc3ccccc3c3ccccc23)C1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
5614d5e5fab02a31ec0e60c576932a05bb07db160a8bb51ea2a91a8018c587db
f944c3c276bd629b2b018acd321b0523075bf7bf55eb7a9350e06e053a9e137b
C1=Cc2c(cccc2-c2cc3ccccc3c3ccccc23)C1
O-[CH;D3;+0:1]1-[CH;D3;+0:2](-[C:3]-[C;D1;H3:4])-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8]-1:[c:9]>>[C;D1;H3:4]-[C:3]-[C;H0;D3;+0:2]1=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8](:[c:9])-[CH2;D2;+0:1]-1
83
[{"value": 83.0, "product": "C(C)C=1CC2=CC=CC(=C2C1)C=1C2=CC=CC=C2C=2C=CC=CC2C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82.6, "product": "C(C)C=1CC2=CC=CC(=C2C1)C=1C2=CC=CC=C2C=2C=CC=CC2C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A 300-ml three-necked round flask equipped with a stirring bar, a Dimroth condenser, a dropping funnel and a thermometer was charged with 12.3 g (36.3 mmol) of 2-ethyl-1-hydroxy-4-(9-phenanthryl)indane, 19.7 ml (142 mmol) of triethylamine and 61.5 ml of methylene chloride. To the mixture was gradually dropwise added a ...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
c1ccc2c(c1)CCC2
C1=Cc2ccccc2C1
C1=Cc2ccccc2C1.c1ccc2c(c1)ccc1ccccc12
HO-
C(Cl)Cl
null
4
CCC1Cc2c(-c3cc4ccccc4c4ccccc34)cccc2C1O>C(Cl)Cl>CCC1=Cc2c(cccc2-c2cc3ccccc3c3ccccc23)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9622eb5e098b43e1961ca5b2635ecda8
CCC(CC)(C(=O)O)C(O)C(=O)O.O=Cc1ccccc1Br>>CCC(CC=Cc1ccccc1Br)(C(=O)O)C(=O)O
BrC1=C(C=O)C=CC=C1.C(C)C(C(C(=O)O)O)(C(=O)O)CC.N1CCCCC1.C(C)(=O)O>>BrC1=C(C=CCC(C(=O)O)(C(=O)O)CC)C=CC=C1
OC([CH:17]([C:3]([CH2:2][CH3:1])([CH2:4][CH3:5])[C:14](=[O:15])[OH:16])[OH:19])=[O:18].O=[CH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[Br:13]>>[CH3:1][CH2:2][C:3]([CH2:4][CH:5]=[CH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[Br:13])([C:14](=[O:15])[OH:16])[C:17](=[O:18])[OH:19]
CCC(CC)(C(=O)O)C(O)C(=O)O.O=Cc1ccccc1Br
CCC(CC=Cc1ccccc1Br)(C(=O)O)C(=O)O
null
null
CCOCC.C1=CC=CC=C1
C-C Coupling
OtherReaction
bc1ed0b41ecf79b9ddc55b089d04a1ea8dac22b572a01624651ce6a04c592e6c
1312feaf05378fecf324ae29885ffdc6b26a5bce74a717a259b939d2a1b7fbb8
c1ccccc1
O-C(=[O;H0;D1;+0:1])-[CH;D3;+0:2](-[O;D1;H1:3])-[C:4](-[C:5])(-[C:6]-[CH3;D1;+0:7])-[C:8](=[O;D1;H0:9])-[O;D1;H1:10].O=[CH;D2;+0:11]-[c:12](:[c:13]):[c:14]>>[C:5]-[C:4](-[C:6]-[CH;D2;+0:7]=[CH;D2;+0:11]-[c:12](:[c:13]):[c:14])(-[C:8](=[O;D1;H0:9])-[O;D1;H1:10])-[C;H0;D3;+0:2](-[O;D1;H1:3])=[O;H0;D1;+0:1]
90
[{"value": 90.0, "product": "BrC1=C(C=CCC(C(=O)O)(C(=O)O)CC)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
A 500-ml three-necked round flask (Dean & Stark) equipped with a stirring bar, a Dimroth condenser and a thermometer was charged with 74.0 g (400 mmol) of 2-bromobenzaldehyde, 70.48 g (440 mmol) of diethylmaloic acid, 1.6 ml of piperidine, 4.8 ml of acetic acid and 80 ml of benzene. The mixture was subjected to azeotor...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Carboxylic acid.Secondary alcohol
Carboxylic acid
null
null
c1ccccc1
HO-
CCOCC.C1=CC=CC=C1
null
7
CCC(CC)(C(=O)O)C(O)C(=O)O.O=Cc1ccccc1Br>CCOCC.C1=CC=CC=C1>CCC(CC=Cc1ccccc1Br)(C(=O)O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-720d56245d524a16b94637dbc351cd6f
CCCCC(Cc1ccccc1Br)C(=O)Cl>>CC(C)CC1Cc2c(Br)cccc2C1=O
C(=S)=S.BrC1=C(C=CC=C1)CC(C(=O)Cl)CCCC.[Cl-].[Al+3].[Cl-].[Cl-].C(=S)=S>>BrC1=C2CC(C(C2=CC=C1)=O)CC(C)C
Cl[C:14]([CH:5]([CH2:4][CH2:2][CH2:3][CH3:1])[CH2:6][c:7]1[c:8]([Br:9])[cH:10][cH:11][cH:12][cH:13]1)=[O:15]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([Br:9])[cH:10][cH:11][cH:12][c:13]2[C:14]1=[O:15]
CCCCC(Cc1ccccc1Br)C(=O)Cl
CC(C)CC1Cc2c(Br)cccc2C1=O
null
null
null
Functional Group Interconversion
OtherReaction
7b9734e58924bc575a74e807adf26a9823112e4889035db5164e883ac041f237
f6f1db2fb6b7641a5cc9b525399565f319b23dea2171a8a2e15ad3fed644bcab
O=C1CCc2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4]-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH3;D1;+0:7])-[C:8]-[c:9](:[c:10]):[cH;D2;+0:11]:[c:12]:[c:13]>>[CH3;D1;+0:7]-[CH;D3;+0:5](-[CH3;D1;+0:6])-[C:4]-[C:3]1-[C:8]-[c:9](:[c:10]):[c;H0;D3;+0:11](:[c:12]:[c:13])-[C;H0;D3;+0:1]-1=[O;D1;H0:2]
null
[]
null
null
1
HOUR
A 500-ml four-necked round flask equipped with a stirrer, a Dimroth condenser, a dropping funnel, a thermometer and a NaOH trap was charged with 20.33 g (152.5 mmol) of anhydrous aluminum chloride and 70 ml of carbon disulfide. To the mixture was added dropwise a solution containing 40.2 g (132.6 mmol) of the above-obt...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1ccccc1
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HCl
null
null
1
CCCCC(Cc1ccccc1Br)C(=O)Cl>>CC(C)CC1Cc2c(Br)cccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4507c8e738e140f981dfa47144c9fc10
CC(C)CC1Cc2c(Br)cccc2C1=O>>CC(C)CC1Cc2c(Br)cccc2C1O
B.[Na].BrC1=C2CC(C(C2=CC=C1)=O)CC(C)C>>BrC1=C2CC(C(C2=CC=C1)O)CC(C)C
[CH3:1][CH:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([Br:9])[cH:10][cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([Br:9])[cH:10][cH:11][cH:12][c:13]2[CH:14]1[OH:15]
CC(C)CC1Cc2c(Br)cccc2C1=O
CC(C)CC1Cc2c(Br)cccc2C1O
null
null
C(C)O
Reduction
Reduction of ketone to secondary alcohol
0a3f398c63bd0c6cfcdf56758ab675b7848fb8b1a73b3840e22b4343df98b04f
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccc2c(c1)CCC2
[C:1]-[C:2]1-[C:3]-[c:4]:[c:5](:[c:6])-[C;H0;D3;+0:7]-1=[O;H0;D1;+0:8]>>[C:1]-[C:2]1-[C:3]-[c:4]:[c:5](:[c:6])-[CH;D3;+0:7]-1-[OH;D1;+0:8]
96.4
[{"value": 96.0, "product": "BrC1=C2CC(C(C2=CC=C1)O)CC(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.4, "product": "BrC1=C2CC(C(C2=CC=C1)O)CC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A 300-ml three-necked round flask equipped with a stirring bar, a Dimroth condenser, a dropping funnel and a thermometer was charged with 2.51 g (66.3 mmol) of sodium boron hydride and 85 ml of ethanol. To the mixture was added dropwise a solution containing 37.0 g (132.6 mmol) of the above-obtained 4-bromo-2-i-butyl-1...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
null
C(C)O
null
16
CC(C)CC1Cc2c(Br)cccc2C1=O>C(C)O>CC(C)CC1Cc2c(Br)cccc2C1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-69eb7f64dea14051acb42ba139e8579c
CC(C)CC1Cc2c(Br)cccc2C1O.C[Si](C)(C)Cl>>CC(C)CC1Cc2c(Br)cccc2C1O[Si](C)(C)C
C([O-])(O)=O.[Na+].BrC1=C2CC(C(C2=CC=C1)O)CC(C)C.C(C)N(CC)CC.C[Si](C)(C)Cl>>BrC1=C2CC(C(C2=CC=C1)O[Si](C)(C)C)CC(C)C
[CH3:1][CH:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([Br:9])[cH:10][cH:11][cH:12][c:13]2[CH:14]1[OH:15].Cl[Si:16]([CH3:17])([CH3:18])[CH3:19]>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([Br:9])[cH:10][cH:11][cH:12][c:13]2[CH:14]1[O:15][Si:16]([CH3:17])([CH3:18])[CH3:19]
CC(C)CC1Cc2c(Br)cccc2C1O.C[Si](C)(C)Cl
CC(C)CC1Cc2c(Br)cccc2C1O[Si](C)(C)C
null
null
C(Cl)Cl
Protection
Alcohol protection with silyl ethers
ea139b3cb6171a748fbc881d815cc598a14c6b8245b87168b4a15a10e325f24c
1e2a25dd539d267852f3b05b92dd4080ece1d4c7abb9db1b6fd2b64d2b33a864
c1ccc2c(c1)CCC2
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4].[C:5]-[C:6](-[OH;D1;+0:7])-[c:8]>>[C:5]-[C:6](-[O;H0;D2;+0:7]-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4])-[c:8]
96
[{"value": 96.0, "product": "BrC1=C2CC(C(C2=CC=C1)O[Si](C)(C)C)CC(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.8, "product": "BrC1=C2CC(C(C2=CC=C1)O[Si](C)(C)C)CC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
A 300-ml three-necked round flask equipped with a stirring bar, a Dimroth condenser, a dropping funnel and a thermometer was charged with 34.4 g (127.8 mmol) of 4-bromo-2-i-butyl-1-hydoxyindane, 23.1 ml (166.2 mmol) of triethylamine and 118 ml of methylene chloride. To the mixture was added dropwise 20 ml of a methylen...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
Silyl protective group
null
null
c1ccc2c(c1)CCC2
HCl
C(Cl)Cl
null
1.5
CC(C)CC1Cc2c(Br)cccc2C1O.C[Si](C)(C)Cl>C(Cl)Cl>CC(C)CC1Cc2c(Br)cccc2C1O[Si](C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fb06eeebdaf54faba40d9313cc436031
CC(C)CC1=Cc2c(-c3cccc4ccccc34)cccc2C1O>>CC(C)CC1=Cc2c(cccc2-c2cccc3ccccc23)C1
O.C(C(C)C)C=1C(C2=CC=CC(=C2C1)C1=CC=CC2=CC=CC=C12)O.C(C)N(CC)CC.CS(=O)(=O)Cl>>C(C(C)C)C=1CC2=CC=CC(=C2C1)C1=CC=CC2=CC=CC=C12
O[CH:23]1[C:5]([CH2:4][CH:2]([CH3:1])[CH3:3])=[CH:6][c:7]2[c:8]1[cH:9][cH:10][cH:11][c:12]2-[c:13]1[cH:14][cH:15][cH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12>>[CH3:1][CH:2]([CH3:3])[CH2:4][C:5]1=[CH:6][c:7]2[c:8]([cH:9][cH:10][cH:11][c:12]2-[c:13]2[cH:14][cH:15][cH:16][c:17]3[cH:18][cH:19][cH:20][cH:21][c:22]23)[...
CC(C)CC1=Cc2c(-c3cccc4ccccc34)cccc2C1O
CC(C)CC1=Cc2c(cccc2-c2cccc3ccccc23)C1
null
CN(C1=CC=NC=C1)C
C(Cl)Cl
Reduction
OtherReaction
e9b6a42e50b8eac49607046617d0205c14a3425da3a513186e1138d5359ba2a3
46f8a11b80b06e754a5a34198d843342612a5e7ede950bda52ce3a500cedba0b
C1=Cc2c(cccc2-c2cccc3ccccc23)C1
O-[CH;D3;+0:1]1-[C:2](-[C:3])=[C:4]-[c:5]:[c:6]-1:[c:7]>>[C:3]-[C:2]1=[C:4]-[c:5]:[c:6](:[c:7])-[CH2;D2;+0:1]-1
93
[{"value": 93.0, "product": "C(C(C)C)C=1CC2=CC=CC(=C2C1)C1=CC=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.6, "product": "C(C(C)C)C=1CC2=CC=CC(=C2C1)C1=CC=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
A 200-ml three-necked round flask equipped with a stirring bar, a Dimroth condenser, a dropping funnel and a thermometer was charged with 4.54 g (14.4 mmol) of 2-i-butyl-1-hydroxy-4-(1-naphthyl)indene, 5.13 g (50.8 mmol) of triethylamine, 0.10 g (0.82 mmol) of 4-dimethylaminopyridine and 57.7 ml of methylene chloride. ...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
C1=Cc2ccccc2C1
C1=Cc2ccccc2C1
C1=Cc2ccccc2C1.c1ccc2ccccc2c1
Other
CN(C1=CC=NC=C1)C.C(Cl)Cl
null
3
CC(C)CC1=Cc2c(-c3cccc4ccccc34)cccc2C1O>CN(C1=CC=NC=C1)C.C(Cl)Cl>CC(C)CC1=Cc2c(cccc2-c2cccc3ccccc23)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f88ac48b7e45476aa2b72c1493bc7762
O=C(O)CN(CC(O)CCl)CC(O)CCl>>O=C(O)CN(CC1CO1)CC1CO1
ClCC(CN(CC(=O)O)CC(CCl)O)O.[Na].[OH-].[Na+]>>O1C(CN(CC(=O)O)CC2CO2)C1
Cl[CH2:8][CH:7]([CH2:6][N:5]([CH2:4][C:2](=[O:1])[OH:3])[CH2:10][CH:11]([CH2:12]Cl)[OH:13])[OH:9]>>[O:1]=[C:2]([OH:3])[CH2:4][N:5]([CH2:6][CH:7]1[CH2:8][O:9]1)[CH2:10][CH:11]1[CH2:12][O:13]1
O=C(O)CN(CC(O)CCl)CC(O)CCl
O=C(O)CN(CC1CO1)CC1CO1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
2ec9e41df1eaed03dcbceb90354f5fc8e8bacbfa8468fa18185c2ec00f0def46
cbf4463e0bad0be7f9ea06a8484ca48c009710e8fe37e8786de0b77d450609b7
C(NCC1CO1)C1CO1
Cl-[CH2;D2;+0:1]-[C:2](-[C:3])-[OH;D1;+0:4].Cl-[CH2;D2;+0:5]-[C:6](-[C:7])-[OH;D1;+0:8]>>[C:3]-[C:2]1-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-1.[C:7]-[C:6]1-[CH2;D2;+0:5]-[O;H0;D2;+0:8]-1
84
[{"value": 84.0, "product": "O1C(CN(CC(=O)O)CC2CO2)C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 83.9, "product": "O1C(CN(CC(=O)O)CC2CO2)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A reactor was charged with 20 g (0.07 mole) of sodium N,N-bis(3-chloro-2-hydroxypropyl)glycine obtained in the same manner as in Referential Example 1 and 100 g of water, and the contents were kept at 50° C., to which 35 ml of a 4N aqueous solution of sodium hydroxide were added. After the mixture was stirred for 30 mi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Secondary alcohol.Secondary alcohol
Ether.Ether
null
C1CO1.C1CO1
C1CO1.C1CO1
HCl
O
null
0.5
O=C(O)CN(CC(O)CCl)CC(O)CCl>O>O=C(O)CN(CC1CO1)CC1CO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fee902400dd24de2890c72bb0aeb17a9
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.O=C1CCC(=O)O1>>CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)CCC(=O)O)C(=O)CCC(=O)O
OC(CNCCCCCCCC)CN(CC(CNCCCCCCCC)O)CCS(=O)(=O)O.C1(CCC(=O)O1)=O>>OC(CN(C(CCC(=O)O)=O)CCCCCCCC)CN(CC(CN(C(CCC(=O)O)=O)CCCCCCCC)O)CCS(=O)(=O)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH:9][CH2:10][CH:11]([OH:12])[CH2:13][N:14]([CH2:15][CH2:16][S:17](=[O:18])(=[O:19])[OH:20])[CH2:21][CH:22]([OH:23])[CH2:24][NH:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH3:33].[CH2:34]1[C:38](=[O:39])[O:40][C:45](=[O:46])[CH2:44]1>>[CH3:1][CH2...
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.O=C1CCC(=O)O1
CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)CCC(=O)O)C(=O)CCC(=O)O
null
null
C=1(C(=CC=CC1)C)C
Functional Group Addition
OtherReaction
3bb26b2855a96a180ebf1f241af912f3509a997494f1dbeb14302538de5c1750
4c4c310a2e25b44b6a153f73ca33f28376363c37984b1851430357fdf169a55b
null
[C:1]-[C:2]-[NH;D2;+0:3]-[C:4]-[C:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10].[O;D1;H0:11]=[C;H0;D3;+0:12]1-[CH2;D2;+0:13]-[CH2;D2;+0:14]-[C;H0;D3;+0:15](=[O;D1;H0:16])-[O;H0;D2;+0:17]-1>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9]-[C:10])-[C;H0;D3;+0:13](=[O;D1;H0:18])-[C:19]-[C:20]-[C;H0;D3;+0:12](=[O;D1;H0:11])-[OH;D1;+0:17].[C:...
80.5
[{"value": 76.0, "product": "OC(CN(C(CCC(=O)O)=O)CCCCCCCC)CN(CC(CN(C(CCC(=O)O)=O)CCCCCCCC)O)CCS(=O)(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.5, "product": "OC(CN(C(CCC(=O)O)=O)CCCCCCCC)CN(CC(CN(C(CCC(=O)O)=O)CCCCCCCC)O)CCS(=O)(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A reactor was charged with 27 g (0.05 mole) of 11,15-dihydroxy-13-sulfoethyl-9,13,17-triazapentacosane and 100 g of xylene, to which 12 g (0.12 mole) of succinic anhydride were then added with stirring to conduct a reaction at 50° C. for 6 hours. After xylene was distilled off under reduced pressure, 300 ml of water we...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amine.Secondary amine
Carboxylic acid.Carboxylic acid.Tertiary amide.Tertiary amide
C1CCOC1
null
null
Other
C=1(C(=CC=CC1)C)C
null
null
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.O=C1CCC(=O)O1>C=1(C(=CC=CC1)C)C>CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)CCC(=O)O)C(=O)CCC(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-edde2bbf24c7456a8918ccba8422abf0
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.O=C1C=CC(=O)O1>>CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)C=CC(=O)O)C(=O)C=CC(=O)O
OC(CNCCCCCCCC)CN(CC(CNCCCCCCCC)O)CCS(=O)(=O)O.C1(\C=C/C(=O)O1)=O>>OC(CN(C(C=CC(=O)O)=O)CCCCCCCC)CN(CC(CN(C(C=CC(=O)O)=O)CCCCCCCC)O)CCS(=O)(=O)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH:9][CH2:10][CH:11]([OH:12])[CH2:13][N:14]([CH2:15][CH2:16][S:17](=[O:18])([OH:20])=[O:46])[CH2:21][CH:22]([OH:23])[CH2:24][NH:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH3:33].[CH:34]1=[CH:44][C:45](=[O:47])[O:40][C:38]1=[O:39]>>[CH3:1][CH2:2]...
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.O=C1C=CC(=O)O1
CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)C=CC(=O)O)C(=O)C=CC(=O)O
null
null
C=1(C(=CC=CC1)C)C
Functional Group Addition
OtherReaction
dc140d5ed9dd6ad3cb833885cee8553db570545e53b2e43473a6d4d501dc3140
259d608df1616a51b4b4055e626ee8b0d431be26ac17083f0a7d17f76ab6069e
null
[C:1]-[C:2]-[NH;D2;+0:3]-[C:4]-[C:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10].[C:11]-[C:12]-[S;H0;D4;+0:13](=[O;D1;H0:14])(-[O;D1;H1:15])=[O;H0;D1;+0:16].[O;D1;H0:17]=[C;H0;D3;+0:18]1-[CH;D2;+0:19]=[CH;D2;+0:20]-[C;H0;D3;+0:21](=[O;H0;D1;+0:22])-[O;H0;D2;+0:23]-1>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9]-[C:10])-[C;H0;D3;+0:19](...
80
[{"value": 80.0, "product": "OC(CN(C(C=CC(=O)O)=O)CCCCCCCC)CN(CC(CN(C(C=CC(=O)O)=O)CCCCCCCC)O)CCS(=O)(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.5, "product": "OC(CN(C(C=CC(=O)O)=O)CCCCCCCC)CN(CC(CN(C(C=CC(=O)O)=O)CCCCCCCC)O)CCS(=O)(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": fal...
null
null
null
null
A reactor was charged with 20 g (0.04 mole) of 11,15-dihydroxy-13-sulfoethyl-9,13,17-triazapentacosane and 100 g of xylene, to which 10 g (0.1 mole) of maleic anhydride were then added with stirring to conduct a reaction at 50° C. for 6 hours. After xylene was distilled off under reduced pressure, 300 ml of water were ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amine.Secondary amine.Sulfonic acid
Carboxylic acid.Carboxylic acid.Tertiary amide.Tertiary amide.Sulfonic acid
C1=CCOC1
null
null
Other
C=1(C(=CC=CC1)C)C
null
null
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.O=C1C=CC(=O)O1>C=1(C(=CC=CC1)C)C>CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)C=CC(=O)O)C(=O)C=CC(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7c6c206c7c6b448dac5969421cf30787
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.CCOC(=O)CO>>CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)CO)C(=O)CO
OC(CNCCCCCCCC)CN(CC(CNCCCCCCCC)O)CCS(=O)(=O)O.C(CO)(=O)OCC>>C(CCCCCCC)N(C(CO)=O)CC(CN(CC(CN(C(CO)=O)CCCCCCCC)O)CCS(=O)(=O)O)O
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH:9][CH2:10][CH:11]([OH:12])[CH2:13][N:14]([CH2:15][CH2:16][S:17](=[O:18])([OH:20])=[O:35])[CH2:21][CH:22]([OH:23])[CH2:24][NH:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH3:33].[CH3:34][CH2:36][O:37][C:38](=[O:39])[CH2:40][OH:41]>>[CH3:1][CH2:2...
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.CCOC(=O)CO
CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)CO)C(=O)CO
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
a734285b9b0266344aeed8bc0a479ce60148c2ec41457be505e12de4ce92c30b
8d2d16edbc74466c428de7493aa2e86ef74b2ac3164ce0df05133be761f835c3
null
[CH3;D1;+0:1]-[C:2]-[O;H0;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-[O;D1;H1:7].[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12].[C:13]-[C:14]-[NH;D2;+0:15]-[C:16]-[C:17].[C:18]-[C:19]-[S;H0;D4;+0:20](=[O;D1;H0:21])(-[O;D1;H1:22])=[O;H0;D1;+0:23]>>[C:8]-[C:9]-[N;H0;D3;+0:10](-[C:11]-[C:12])-[C;H0;D3;+0:4](=[O;D1;H0:5])-[C:6]-...
91
[{"value": 91.0, "product": "C(CCCCCCC)N(C(CO)=O)CC(CN(CC(CN(C(CO)=O)CCCCCCCC)O)CCS(=O)(=O)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.6, "product": "C(CCCCCCC)N(C(CO)=O)CC(CN(CC(CN(C(CO)=O)CCCCCCCC)O)CCS(=O)(=O)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
7.5
HOUR
A reactor was charged with 10 g (0.02 mole) of 11,15-dihydroxy-13-sulfoethyl-9,13,17-triazapentacosane, 50 ml of toluene and 5.1 ml (0.05 mole) of ethyl glycolate, and the contents were heated to 100° C. and continuously stirred for 7.5 hours while purging ethanol formed with a nitrogen stream. After completion of a re...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine.Secondary amine.Sulfonic acid
Tertiary amide.Tertiary amide.Primary alcohol.Sulfonic acid
null
null
null
Other
C1(=CC=CC=C1)C
100
7.5
CCCCCCCCNCC(O)CN(CCS(=O)(=O)O)CC(O)CNCCCCCCCC.CCOC(=O)CO>C1(=CC=CC=C1)C>CCCCCCCCN(CC(O)CN(CCS(=O)(=O)O)CC(O)CN(CCCCCCCC)C(=O)CO)C(=O)CO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dd7b84cd2bdd41c8acecfbb08583d7c0
CSC.Nc1cc(F)c(F)cc1F>>CSCc1c(N)c(F)cc(F)c1F
[OH-].[Na+].FC1=C(N)C=C(C(=C1)F)F.CSC.ClN1C(CCC1=O)=O>>CSCC1=C(N)C(=CC(=C1F)F)F
[CH3:1][S:2][CH3:3].[cH:4]1[c:5]([NH2:6])[c:7]([F:8])[cH:9][c:10]([F:11])[c:12]1[F:13]>>[CH3:1][S:2][CH2:3][c:4]1[c:5]([NH2:6])[c:7]([F:8])[cH:9][c:10]([F:11])[c:12]1[F:13]
CSC.Nc1cc(F)c(F)cc1F
CSCc1c(N)c(F)cc(F)c1F
null
null
ClCCl.C(C)N(CC)CC
C-C Coupling
OtherReaction
85a8db8ffc07fc3b1bc470aedfdb3564a15505e4228e084fe460beeb91f08127
3ec03d96d3f7f1d21fd396735dd73d6cac136a1c01b9b5cbf8cabc89b6a4b631
c1ccccc1
[C;D1;H3:1]-[#16:2]-[CH3;D1;+0:3].[F;D1;H0:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8](-[N;D1;H2:9]):[c:10]>>[C;D1;H3:1]-[#16:2]-[CH2;D2;+0:3]-[c;H0;D3;+0:7](:[c:5](-[F;D1;H0:4]):[c:6]):[c:8](-[N;D1;H2:9]):[c:10]
null
[]
0
CELSIUS
15
MINUTE
To 2,4,5-trifluoroaniline (35.0 g) are added anhydrous dichloromethane (530 ml) and dimethyl sulfide (24.6 ml) and the mixture is cooled to 0° C. Thereto N-chlorosuccinimide (38.2 g) is gradually added below 5° C. After the mixture is stirred at the same temperature for 15 minutes, triethylamine (47.7 ml) is gradually ...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
Monosulfide
c1ccccc1
c1ccccc1
c1ccccc1
null
ClCCl.C(C)N(CC)CC
0
0.25
CSC.Nc1cc(F)c(F)cc1F>ClCCl.C(C)N(CC)CC>CSCc1c(N)c(F)cc(F)c1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6ef792f7c5b74d278abb8630ab09df7e
CSCc1c(N)c(F)cc(F)c1F>>Cc1c(N)c(F)cc(F)c1F
CSCC1=C(N)C(=CC(=C1F)F)F>>CC1=C(N)C(=CC(=C1F)F)F
CS[CH2:1][c:2]1[c:3]([NH2:4])[c:5]([F:6])[cH:7][c:8]([F:9])[c:10]1[F:11]>>[CH3:1][c:2]1[c:3]([NH2:4])[c:5]([F:6])[cH:7][c:8]([F:9])[c:10]1[F:11]
CSCc1c(N)c(F)cc(F)c1F
Cc1c(N)c(F)cc(F)c1F
null
[Ni]
C(C)O
Reduction
OtherReaction
4b57e24218e2409c207dcfe624aba83448b3ad4b3549d9bc7855651565b7e76d
32a5269109432865a866e9a2b5da238f4471b13dee7daf193dc4e8c41b091706
c1ccccc1
C-S-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[CH3;D1;+0:1]-[c:2](:[c:3]):[c:4]
71.3
[{"value": 71.3, "product": "CC1=C(N)C(=CC(=C1F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To 2-methylthiomethyl-3,4,6-trifluoroaniline (22.2 g) are added ethanol (400 ml) and Raney nickel (200 g) and the mixture is stirred at room temperature for 30 minutes. After the catalyst is filtered off, the filtrate is added with water and extracted with dichloromethane. The is dried over magnesium sulfate and concen...
10.6084/m9.figshare.5104873.v1
null
Monosulfide
null
null
null
c1ccccc1
Other
[Ni].C(C)O
null
0.5
CSCc1c(N)c(F)cc(F)c1F>[Ni].C(C)O>Cc1c(N)c(F)cc(F)c1F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1e9ca78c8b7943d3b81ed784f0fbf2a2
Cc1c(N)c(F)cc(F)c1F.[C-]#N>>Cc1c(F)c(F)cc(F)c1C#N
[C-]#N.[K+].[OH-].[NH4+].CC1=C(N)C(=CC(=C1F)F)F.S(O)(O)(=O)=O.N(=O)[O-].[Na+]>>CC1=C(C#N)C(=CC(=C1F)F)F
N[c:10]1[c:2]([CH3:1])[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]1[F:9].[C-:11]#[N:12]>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]([F:9])[c:10]1[C:11]#[N:12]
Cc1c(N)c(F)cc(F)c1F.[C-]#N
Cc1c(F)c(F)cc(F)c1C#N
null
S(=O)(=O)([O-])[O-].[Cu+2]
O
C-C Coupling
OtherReaction
b30bff3fbe81433a7565d8ffcdad0af1ed80d4d9274730f7a6e26aad2e552e05
6febc4a6ed64b39af6e5a12de3ade52adc549644adf3ef1f7265276b39762a0d
c1ccccc1
N-[c;H0;D3;+0:1](:[c:2](-[C;D1;H3:3]):[c:4]):[c:5](-[F;D1;H0:6]):[c:7].[C-;H0;D1:8]#[N;D1;H0:9]>>[C;D1;H3:3]-[c:2](:[c:4]):[c;H0;D3;+0:1](-[C;H0;D2;+0:8]#[N;D1;H0:9]):[c:5](-[F;D1;H0:6]):[c:7]
38.2
[{"value": 38.2, "product": "CC1=C(C#N)C(=CC(=C1F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 2-methyl-3,4,6-trifluoroaniline (10.6 g) is added a mixture of conc. sulfuric acid (13.8 ml) and water (46 ml) and the mixture is cooled. Thereto an aqueous solution (20 ml) of sodium nitrite (5.5 g) is added dropwise at 0°-5° C. The solution is gradually added to a mixture of copper (II) sulfate 5 hydrate (41 g), p...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Nitrile
c1ccccc1
c1ccccc1
c1ccccc1
Other
S(=O)(=O)([O-])[O-].[Cu+2].O
null
null
Cc1c(N)c(F)cc(F)c1F.[C-]#N>S(=O)(=O)([O-])[O-].[Cu+2].O>Cc1c(F)c(F)cc(F)c1C#N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-141b4f862c4146f6950ca566cd749152
Cc1c(F)c(F)cc(F)c1C(=O)O.[Cl-]>>Cc1c(F)c(F)cc(F)c1C(=O)Cl
CC1=C(C(=O)O)C(=CC(=C1F)F)F.[Cl-]>>CC1=C(C(=O)Cl)C(=CC(=C1F)F)F
O[C:11]([c:10]1[c:2]([CH3:1])[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]1[F:9])=[O:12].[Cl-:13]>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]([F:9])[c:10]1[C:11](=[O:12])[Cl:13]
Cc1c(F)c(F)cc(F)c1C(=O)O.[Cl-]
Cc1c(F)c(F)cc(F)c1C(=O)Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_Salt
c301c14a9dcd0670d52e8b77396cbe7fd8edeedd757bc43f4162ade1fc52fc93
787f545db5dc0b29dde55b5fbed7db8625b8055f49327f97ed4d83cc47c3af1d
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[Cl-;H0;D0:6]>>[Cl;H0;D1;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
To 2-methyl-3,4,6-trifluorobenzoic acid (3.2 g) is added thiony chloride (7 ml) and the mixture is refluxed for 1 hour. After concentrating, 2-methyl-3,4,6-trifluorobenzoyl chloride (3.3 g) is obtained. Conditions: See reaction.notes.procedure_details. Workup: the mixture is refluxed for 1 hour; After concentrating
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Acyl halide
null
null
c1ccccc1
HO-
null
null
null
Cc1c(F)c(F)cc(F)c1C(=O)O.[Cl-]>>Cc1c(F)c(F)cc(F)c1C(=O)Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2c7533e52831442a89bfed399496e97e
CCOC(=O)CC(=O)OCC.Cc1c(F)c(F)cc(F)c1C(=O)Cl>>CCOC(=O)C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
CC1=C(C(=O)Cl)C(=CC(=C1F)F)F.S(O)(O)(=O)=O.[Mg].C(CC(=O)OCC)(=O)OCC>>CC1=C(C(=O)C(C(=O)OCC)C(=O)OCC)C(=CC(=C1F)F)F
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7](=[O:8])[O:9][CH2:10][CH3:11].Cl[C:12](=[O:13])[c:14]1[c:15]([F:16])[cH:17][c:18]([F:19])[c:20]([F:21])[c:22]1[CH3:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([C:7](=[O:8])[O:9][CH2:10][CH3:11])[C:12](=[O:13])[c:14]1[c:15]([F:16])[cH:17][c:18]([F:19])[c:20]([F:21])[c:22]1[CH3...
CCOC(=O)CC(=O)OCC.Cc1c(F)c(F)cc(F)c1C(=O)Cl
CCOC(=O)C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
null
C(Cl)(Cl)(Cl)Cl
C(C)O.C1(=CC=CC=C1)C.O
C-C Coupling
OtherReaction
872dd4ea89053916cf9ee557745988425973a0fb6c3fde7e681bde82864a0018
a7050091370b27e4945622bf444949c46249e49bd26e357ae44671cc72030a02
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH2;D2;+0:10]-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]>>[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH;D3;+0:10](-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
60
CELSIUS
1
HOUR
Separately, two drops of carbon tetrachloride are added to a solution of metallic magnesium (0.4 g) in absolute ethanol (0.9 ml). When the reaction starts, a mixture of diethyl malonate (2.6 ml), absolute ethanol (1.6 ml) and anhydrous toluene (6 ml) is added dropwise below 60° C. After stirring at 60° C. for 1 hour, t...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ester.Ester
Ketone
null
null
c1ccccc1
HCl
C(Cl)(Cl)(Cl)Cl.C(C)O.C1(=CC=CC=C1)C.O
60
1
CCOC(=O)CC(=O)OCC.Cc1c(F)c(F)cc(F)c1C(=O)Cl>C(Cl)(Cl)(Cl)Cl.C(C)O.C1(=CC=CC=C1)C.O>CCOC(=O)C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2da68ab0871c4a05aa3d4f9224f8df1c
CCOC(=O)C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C>>CCOC(=O)CC(=O)c1c(F)cc(F)c(F)c1C
CC1=C(C(=O)C(C(=O)OCC)C(=O)OCC)C(=CC(=C1F)F)F.C1(=CC=C(C=C1)S(=O)(=O)O)C>>CC1=C(C(=O)CC(=O)OCC)C(=CC(=C1F)F)F
CCOC(=O)[CH:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:7](=[O:8])[c:9]1[c:10]([F:11])[cH:12][c:13]([F:14])[c:15]([F:16])[c:17]1[CH3:18]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7](=[O:8])[c:9]1[c:10]([F:11])[cH:12][c:13]([F:14])[c:15]([F:16])[c:17]1[CH3:18]
CCOC(=O)C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
CCOC(=O)CC(=O)c1c(F)cc(F)c(F)c1C
null
null
O
Reduction
Decarboxylation
c8cf2024f85522a1f5dc304862ec185b9ba9539171a955fed5fc95020255a5b8
92cfcced8d7e743a323bd1528115ee07546647fe3eca55d712fbb9eefe0c9e22
c1ccccc1
C-C-O-C(=O)-[CH;D3;+0:1](-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:6](=[O;D1;H0:7])-[c:8]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[C:6](=[O;D1;H0:7])-[c:8]
82.6
[{"value": 82.6, "product": "CC1=C(C(=O)CC(=O)OCC)C(=CC(=C1F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To diethyl 2-methyl-3,4,6-trifluorobenzoylmalonate (5.1 g) are added water (20 ml) and p-toluenesulfonic acid (30 mg) and the mixture is refluxed for 2.5 hours. After cooling, the resultant is extracted with diethyl ether, and the extract is dried over magnesium sulfate and concentrated to give ethyl 2-methyl-3,4,6-tri...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Ester
Ketone
null
null
c1ccccc1
HO-
O
null
null
CCOC(=O)C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C>O>CCOC(=O)CC(=O)c1c(F)cc(F)c(F)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1c88fe3c527448899e928f57e94a62f9
CCOC(=O)CC(=O)c1c(F)cc(F)c(F)c1C.CCOC(OCC)OCC>>CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
CC1=C(C(=O)CC(=O)OCC)C(=CC(=C1F)F)F.C(C)(=O)OC(C)=O.C(C)OC(OCC)OCC>>CC1=C(C(=O)C(C(=O)OCC)=COCC)C(=CC(=C1F)F)F
[CH2:5]([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[c:13]1[c:14]([F:15])[cH:16][c:17]([F:18])[c:19]([F:20])[c:21]1[CH3:22].CCO[CH:4](OCC)[O:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][O:3][CH:4]=[C:5]([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[c:13]1[c:14]([F:15])[cH:16][c:17]([F:18])[c:19]([F:20])[c:21]1[CH3:22]
CCOC(=O)CC(=O)c1c(F)cc(F)c(F)c1C.CCOC(OCC)OCC
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
null
null
null
C-C Coupling
OtherReaction
7cfff3053680512afd8f3daf149645dfb2cfa4c9c32bf9b885b72097190aacf2
9164ecc9bc41a60ea056ee2b5a56d6c3899e2ff7c236ad9974338a128257f79c
c1ccccc1
C-C-O-[CH;D3;+0:1](-O-C-C)-[#8:2]-[C:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11]>>[C:3]-[#8:2]-[CH;D2;+0:1]=[C;H0;D3;+0:8](-[C:9](=[O;D1;H0:10])-[c:11])-[C:6](=[O;D1;H0:7])-[#8:5]-[C:4]
90
[{"value": 90.0, "product": "CC1=C(C(=O)C(C(=O)OCC)=COCC)C(=CC(=C1F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To ethyl 2-methyl-3,4,6-trifluorobenzoylacetate (3.2 g) are added acetic anhydride (3.0 g) and triethoxymethane (2.7 g) and the mixture is refluxed for 1 hour. After concentrating, ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-ethoxyacrylate (3.5 g) is obtained. Conditions: See reaction.notes.procedure_details. Workup: t...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Ether.Ether.Ether
Ketone.Ester.Ether
null
null
c1ccccc1
HO-
null
null
null
CCOC(=O)CC(=O)c1c(F)cc(F)c(F)c1C.CCOC(OCC)OCC>>CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a6bc9092d4d54296b6f4a8701204549f
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.NC1CC1>>CCOC(=O)C(=CNC1CC1)C(=O)c1c(F)cc(F)c(F)c1C
CC1=C(C(=O)C(C(=O)OCC)=COCC)C(=CC(=C1F)F)F.C1(CC1)N>>CC1=C(C(=O)C(C(=O)OCC)=CNC2CC2)C(=CC(=C1F)F)F
CCO[CH:7]=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:12](=[O:13])[c:14]1[c:15]([F:16])[cH:17][c:18]([F:19])[c:20]([F:21])[c:22]1[CH3:23].[NH2:8][CH:9]1[CH2:10][CH2:11]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[CH:7][NH:8][CH:9]1[CH2:10][CH2:11]1)[C:12](=[O:13])[c:14]1[c:15]([F:16])[cH:17][c:18]([F:19])[c:20]([F:21])[c:2...
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.NC1CC1
CCOC(=O)C(=CNC1CC1)C(=O)c1c(F)cc(F)c(F)c1C
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
cd3db327c21c90c24d38808dacb2ed3fbf57044150e5b341d88de9389ff3759d
54aca1a08d403c8dd5c375df3e63fffc5027b15326b2523cf980a4a251290495
O=C(C=CNC1CC1)c1ccccc1
C-C-O-[CH;D2;+0:1]=[C:2](-[C:3](=[O;D1;H0:4])-[c:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[NH2;D1;+0:10]-[C:11]1-[C:12]-[C:13]-1>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:2](=[CH;D2;+0:1]-[NH;D2;+0:10]-[C:11]1-[C:12]-[C:13]-1)-[C:3](=[O;D1;H0:4])-[c:5]
null
[]
null
null
30
MINUTE
Ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-ethoxyacrylate (3.5 g) is dissolved in ethanol (25 ml) and thereto cyclopropylamine (0.84 ml) is added dropwise under ice-cooling. After stirring at room temperature for 30 minutes, the mixture is concentrated and the residue is purified with column chromatography (silica-gel...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Enamine
null
null
C1CC1.c1ccccc1
HO-
C(C)O
null
0.5
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.NC1CC1>C(C)O>CCOC(=O)C(=CNC1CC1)C(=O)c1c(F)cc(F)c(F)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8baad9aabd414b21a6bb786ba650a995
CCOC(=O)C(=CNC1CC1)C(=O)c1c(F)cc(F)c(F)c1C>>CCOC(=O)c1cn(C2CC2)c2cc(F)c(F)c(C)c2c1=O
CC1=C(C(=O)C(C(=O)OCC)=CNC2CC2)C(=CC(=C1F)F)F.[H-].[Na+]>>C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)OCC
F[c:12]1[cH:13][c:14]([F:15])[c:16]([F:17])[c:18]([CH3:19])[c:20]1[C:21]([C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][NH:8][CH:9]1[CH2:10][CH2:11]1)=[O:22]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8]([CH:9]2[CH2:10][CH2:11]2)[c:12]2[cH:13][c:14]([F:15])[c:16]([F:17])[c:18]([CH3:19])[c:20]2[c:21]1=[O:22]
CCOC(=O)C(=CNC1CC1)C(=O)c1c(F)cc(F)c(F)c1C
CCOC(=O)c1cn(C2CC2)c2cc(F)c(F)c(C)c2c1=O
null
null
O1CCOCC1
Aromatic Heterocycle Formation
OtherReaction
f1bb464adea8e64c138d384f2f02c35f1978964fc9c160676d8ef60c68e5e3df
ecabf5a50b4453255d534845e8b1084d96a0aaf957abdb24947c6089ec559e5f
O=c1ccn(C2CC2)c2ccccc12
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C;H0;D3;+0:7](=[CH;D2;+0:8]-[NH;D2;+0:9]-[C:10]1-[C:11]-[C:12]-1)-[C:13](=[O;D1;H0:14])-[#8:15]-[C:16]):[c:17]>>[C:16]-[#8:15]-[C:13](=[O;D1;H0:14])-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[n;H0;D3;+0:9](-[C:10]2-[C:11]-[C:12]-2):[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4...
81.9
[{"value": 81.9, "product": "C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
Ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-cyclopropylaminoacrylate (2.6 g) is dissolved in anhydrous dioxane (26 ml) and thereto 60% sodium hydride (0.38 g) is gradully added under ice-cooling. After stirring at room temperature for 30 minutes, the reaction mixture is poured into ice-water and extracted with dichloro...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Ketone
Ester
c1ccccc1
c1ccc2ncccc2c1
C1CC1.c1ccc2ncccc2c1
HF
O1CCOCC1
null
0.5
CCOC(=O)C(=CNC1CC1)C(=O)c1c(F)cc(F)c(F)c1C>O1CCOCC1>CCOC(=O)c1cn(C2CC2)c2cc(F)c(F)c(C)c2c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b4ccefd875914706b84816f471c88bad
CCOC(=O)c1cn(C2CC2)c2cc(F)c(F)c(C)c2c1=O>>Cc1c(F)c(F)cc2c1c(=O)c(C(=O)O)cn2C1CC1
C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)OCC.Cl>>C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)O
CC[O:15][C:13]([c:12]1[c:10](=[O:11])[c:9]2[c:2]([CH3:1])[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]2[n:17]([CH:18]2[CH2:19][CH2:20]2)[cH:16]1)=[O:14]>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]2[c:9]1[c:10](=[O:11])[c:12]([C:13](=[O:14])[OH:15])[cH:16][n:17]2[CH:18]1[CH2:19][CH2:20]1
CCOC(=O)c1cn(C2CC2)c2cc(F)c(F)c(C)c2c1=O
Cc1c(F)c(F)cc2c1c(=O)c(C(=O)O)cn2C1CC1
null
null
C(C)(=O)O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1ccn(C2CC2)c2ccccc12
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
92.7
[{"value": 92.7, "product": "C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To ethyl 1-cyclopropyl-6,7-difluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylate (1.9 g) are added 90% acetic acid (20 ml) and conc. hydrochloric acid (5 ml) and the mixture is refluxed for 2 hours. After cooling, the precipitated crystals are isolated, washed with water, ethanol, and diethyl ether in this order t...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2ncccc2c1.C1CC1
Other
C(C)(=O)O
null
null
CCOC(=O)c1cn(C2CC2)c2cc(F)c(F)c(C)c2c1=O>C(C)(=O)O>Cc1c(F)c(F)cc2c1c(=O)c(C(=O)O)cn2C1CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ca06de262c0c42b696248fd0b6d115dc
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.Nc1ccc(F)cc1>>CCOC(=O)C(=CNc1ccc(F)cc1)C(=O)c1c(F)cc(F)c(F)c1C
CC1=C(C(=O)C(C(=O)OCC)=COCC)C(=CC(=C1F)F)F.FC1=CC=C(N)C=C1>>CC1=C(C(=O)C(C(=O)OCC)=CNC2=CC=C(C=C2)F)C(=CC(=C1F)F)F
CCO[CH:7]=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:16](=[O:17])[c:18]1[c:19]([F:20])[cH:21][c:22]([F:23])[c:24]([F:25])[c:26]1[CH3:27].[NH2:8][c:9]1[cH:10][cH:11][c:12]([F:13])[cH:14][cH:15]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[CH:7][NH:8][c:9]1[cH:10][cH:11][c:12]([F:13])[cH:14][cH:15]1)[C:16](=[O:17])[c:18]1[c:...
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.Nc1ccc(F)cc1
CCOC(=O)C(=CNc1ccc(F)cc1)C(=O)c1c(F)cc(F)c(F)c1C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
cd3db327c21c90c24d38808dacb2ed3fbf57044150e5b341d88de9389ff3759d
54aca1a08d403c8dd5c375df3e63fffc5027b15326b2523cf980a4a251290495
O=C(C=CNc1ccccc1)c1ccccc1
C-C-O-[CH;D2;+0:1]=[C:2](-[C:3](=[O;D1;H0:4])-[c:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[NH2;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:2](=[CH;D2;+0:1]-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13])-[C:3](=[O;D1;H0:4])-[c:5]
null
[]
null
null
null
null
Employing ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-ethoxyacrylate (1.0 g) and p-fluoroaniline (0.39 g), the procedure of Reference Example 8 is repeated to give ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-(4-fluorophenyl)aminoacrylate, which is then treated with 60% sodium hydride (0.15 g) as in Reference Example 9 ...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Enamine
null
null
c1ccccc1.c1ccccc1
HO-
null
null
null
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.Nc1ccc(F)cc1>>CCOC(=O)C(=CNc1ccc(F)cc1)C(=O)c1c(F)cc(F)c(F)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ae2d2dcbbfdb4f1f9dfb58ab8ece22a4
CCOC(=O)c1cn(-c2ccc(F)cc2)c2cc(F)c(F)c(C)c2c1=O>>Cc1c(F)c(F)cc2c1c(=O)c(C(=O)O)cn2-c1ccc(F)cc1
FC1=CC=C(C=C1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)OCC.Cl>>FC1=CC=C(C=C1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)O
CC[O:15][C:13]([c:12]1[c:10](=[O:11])[c:9]2[c:2]([CH3:1])[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]2[n:17](-[c:18]2[cH:19][cH:20][c:21]([F:22])[cH:23][cH:24]2)[cH:16]1)=[O:14]>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([F:6])[cH:7][c:8]2[c:9]1[c:10](=[O:11])[c:12]([C:13](=[O:14])[OH:15])[cH:16][n:17]2-[c:18]1[cH:19][cH:20][c:21]([F:22])...
CCOC(=O)c1cn(-c2ccc(F)cc2)c2cc(F)c(F)c(C)c2c1=O
Cc1c(F)c(F)cc2c1c(=O)c(C(=O)O)cn2-c1ccc(F)cc1
null
null
C(C)(=O)O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1ccn(-c2ccccc2)c2ccccc12
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
94.9
[{"value": 94.9, "product": "FC1=CC=C(C=C1)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Employing ethyl 1-(4-fluorophenyl)-5-methyl-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylate (0.56 g), conc. hydrochloric acid (1.5 ml), and 90% acetic acid (6 ml), the procedure of Reference Example 10 is repeated to give 1-(4-fluorophenyl)-5-methyl-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.49 ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2ncccc2c1.c1ccccc1
Other
C(C)(=O)O
null
null
CCOC(=O)c1cn(-c2ccc(F)cc2)c2cc(F)c(F)c(C)c2c1=O>C(C)(=O)O>Cc1c(F)c(F)cc2c1c(=O)c(C(=O)O)cn2-c1ccc(F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3ed5758e449440ffbc8cbb4a1a1e12a0
CCN.CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C>>CCNC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
CC1=C(C(=O)C(C(=O)OCC)=COCC)C(=CC(=C1F)F)F.C(C)N>>CC1=C(C(=O)C(C(=O)OCC)=CNCC)C(=CC(=C1F)F)F
[CH3:1][CH2:2][NH2:3].CCO[CH:4]=[C:5]([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[c:13]1[c:14]([F:15])[cH:16][c:17]([F:18])[c:19]([F:20])[c:21]1[CH3:22]>>[CH3:1][CH2:2][NH:3][CH:4]=[C:5]([C:6](=[O:7])[O:8][CH2:9][CH3:10])[C:11](=[O:12])[c:13]1[c:14]([F:15])[cH:16][c:17]([F:18])[c:19]([F:20])[c:21]1[CH3:22]
CCN.CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
CCNC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
cd3db327c21c90c24d38808dacb2ed3fbf57044150e5b341d88de9389ff3759d
54aca1a08d403c8dd5c375df3e63fffc5027b15326b2523cf980a4a251290495
c1ccccc1
C-C-O-[CH;D2;+0:1]=[C:2](-[C:3](=[O;D1;H0:4])-[c:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[C;D1;H3:10]-[C:11]-[NH2;D1;+0:12]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:2](=[CH;D2;+0:1]-[NH;D2;+0:12]-[C:11]-[C;D1;H3:10])-[C:3](=[O;D1;H0:4])-[c:5]
null
[]
null
null
null
null
Employing ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-ethoxyacrylate (1.0 g) and 70% aqueous ethylamine solution (0.24 ml), the procedure of Reference Example 8 is repeated to give ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-ethylaminoacrylate, which is then treated with 60 % sodium hydride (0.15 g) as in Reference Exa...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Enamine
null
null
c1ccccc1
HO-
null
null
null
CCN.CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C>>CCNC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ced401958df14107b84014195a09d50e
CCOC(=O)c1cn(CC)c2cc(F)c(F)c(C)c2c1=O>>CCn1cc(C(=O)O)c(=O)c2c(C)c(F)c(F)cc21
C(C)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)OCC.Cl>>C(C)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)O
CC[O:8][C:6]([c:5]1[cH:4][n:3]([CH2:2][CH3:1])[c:19]2[c:11]([c:9]1=[O:10])[c:12]([CH3:13])[c:14]([F:15])[c:16]([F:17])[cH:18]2)=[O:7]>>[CH3:1][CH2:2][n:3]1[cH:4][c:5]([C:6](=[O:7])[OH:8])[c:9](=[O:10])[c:11]2[c:12]([CH3:13])[c:14]([F:15])[c:16]([F:17])[cH:18][c:19]12
CCOC(=O)c1cn(CC)c2cc(F)c(F)c(C)c2c1=O
CCn1cc(C(=O)O)c(=O)c2c(C)c(F)c(F)cc21
null
null
C(C)(=O)O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1cc[nH]c2ccccc12
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
80.4
[{"value": 80.4, "product": "C(C)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Employing ethyl 1-ethyl-5-methyl-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylate (0.55 g), conc. hydrochloric acid (1.5 ml) and 90% acetic acid (6 ml), the procedure of Reference Example 10 is repeated to give 1-ethyl-5-methyl-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3- carboxylic acid (0.40 g), as white crystals,...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccc2ncccc2c1
Other
C(C)(=O)O
null
null
CCOC(=O)c1cn(CC)c2cc(F)c(F)c(C)c2c1=O>C(C)(=O)O>CCn1cc(C(=O)O)c(=O)c2c(C)c(F)c(F)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c6d1437bef5145cca37826ac5ae090f0
CO.Cc1c(C(=O)O)cccc1[N+](=O)[O-]>>COC(=O)c1cccc([N+](=O)[O-])c1C
CC1=C(C(=O)O)C=CC=C1[N+](=O)[O-].CO.S(=O)(Cl)Cl>>CC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-]
[CH3:1][OH:2].O[C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([N+:10](=[O:11])[O-:12])[c:13]1[CH3:14]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([N+:10](=[O:11])[O-:12])[c:13]1[CH3:14]
CO.Cc1c(C(=O)O)cccc1[N+](=O)[O-]
COC(=O)c1cccc([N+](=O)[O-])c1C
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[OH;D1;+0:7]>>[C;D1;H3:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
To 2-methyl-3-nitrobenzoic acid (10.0 g) is added methanol (100 ml) and thereto thionyl chloride (8 ml) is added dropwise at room temperature. After reflux for 2 hours, the reaction mixture is poured into ice-water and extracted with dichloromethane. The solvent is concentrated to give methyl 2-methyl-3-nitrobenzoate (...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
null
null
null
CO.Cc1c(C(=O)O)cccc1[N+](=O)[O-]>>COC(=O)c1cccc([N+](=O)[O-])c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a382dee7401645edb9da6c1fce7078a0
COC(=O)c1cccc([N+](=O)[O-])c1C>>COC(=O)c1cccc(N)c1C
CC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-]>>CC1=C(C(=O)OC)C=CC=C1N
O=[N+:10]([O-])[c:9]1[cH:8][cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[c:11]1[CH3:12]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([NH2:10])[c:11]1[CH3:12]
COC(=O)c1cccc([N+](=O)[O-])c1C
COC(=O)c1cccc(N)c1C
null
[Pd]
C(C)(=O)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
101.6
[{"value": 101.6, "product": "CC1=C(C(=O)OC)C=CC=C1N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
Methyl 2-methyl-3-nitrobenzoate (10.0 g) is dissolved in acetic acid (50 ml) and thereto 5% Pd-C (1 g) is added to carry out catalytic reduction at room temperature under 1 atm. After 1.5 hours, the catalyst is filtered off. The reaction mixture is concentrated, and thereto is added water, and the mixture is made alkal...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pd].C(C)(=O)O
null
1.5
COC(=O)c1cccc([N+](=O)[O-])c1C>[Pd].C(C)(=O)O>COC(=O)c1cccc(N)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1b1dfc28218048f1b96339ca5954f763
COC(=O)c1c(Br)cc(Br)c(F)c1C>>Cc1c(F)c(Br)cc(Br)c1C(=O)O
CC1=C(C(=O)OC)C(=CC(=C1F)Br)Br.C(C)O.[OH-].[Na+]>>CC1=C(C(=O)O)C(=CC(=C1F)Br)Br
C[O:13][C:11]([c:10]1[c:2]([CH3:1])[c:3]([F:4])[c:5]([Br:6])[cH:7][c:8]1[Br:9])=[O:12]>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([Br:6])[cH:7][c:8]([Br:9])[c:10]1[C:11](=[O:12])[OH:13]
COC(=O)c1c(Br)cc(Br)c(F)c1C
Cc1c(F)c(Br)cc(Br)c1C(=O)O
null
null
O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccccc1
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]
84.4
[{"value": 84.4, "product": "CC1=C(C(=O)O)C(=CC(=C1F)Br)Br", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To methyl 2-methyl-3-fluoro-4,6-dibromobenzoate (75.5 g) are added ethanol (460 ml) and 10% aqueous solution of sodium hydroxide (460 ml) and the mixture is refluxed for 2 hours. After cooling, the reaction mixture is diluted with water and extracted with diethyl ether. The aqueous layer is made acidic with conc. hydro...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1
Other
O
null
null
COC(=O)c1c(Br)cc(Br)c(F)c1C>O>Cc1c(F)c(Br)cc(Br)c1C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-54a17c6717d34e7dab9d9ee4a4d665b8
CCOC(=O)C(=CNC1CC1)C(=O)c1c(Br)cc(Br)c(F)c1C>>CCOC(=O)c1cn(C2CC2)c2cc(Br)c(F)c(C)c2c1=O
BrC1=C(C(=C(C(=O)C(C(=O)OCC)=CNC2CC2)C(=C1)Br)C)F.C([O-])([O-])=O.[K+].[K+]>>C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)Br)F)C)=O)C(=O)OCC
Br[c:12]1[cH:13][c:14]([Br:15])[c:16]([F:17])[c:18]([CH3:19])[c:20]1[C:21]([C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][NH:8][CH:9]1[CH2:10][CH2:11]1)=[O:22]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8]([CH:9]2[CH2:10][CH2:11]2)[c:12]2[cH:13][c:14]([Br:15])[c:16]([F:17])[c:18]([CH3:19])[c:20]2[c:21]1=[O:22]
CCOC(=O)C(=CNC1CC1)C(=O)c1c(Br)cc(Br)c(F)c1C
CCOC(=O)c1cn(C2CC2)c2cc(Br)c(F)c(C)c2c1=O
null
null
CN(C=O)C
Aromatic Heterocycle Formation
OtherReaction
f1bb464adea8e64c138d384f2f02c35f1978964fc9c160676d8ef60c68e5e3df
ecabf5a50b4453255d534845e8b1084d96a0aaf957abdb24947c6089ec559e5f
O=c1ccn(C2CC2)c2ccccc12
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C;H0;D3;+0:7](=[CH;D2;+0:8]-[NH;D2;+0:9]-[C:10]1-[C:11]-[C:12]-1)-[C:13](=[O;D1;H0:14])-[#8:15]-[C:16]):[c:17]>>[C:16]-[#8:15]-[C:13](=[O;D1;H0:14])-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[n;H0;D3;+0:9](-[C:10]2-[C:11]-[C:12]-2):[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:...
91.1
[{"value": 91.1, "product": "C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)Br)F)C)=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture comprising ethyl 2-(4,6-dibromo-3-fluoro-2-methylbenzoyl)-3-cyclopropylaminoacrylate (45.0 g), potassium carbonate (16.7 g) and dimethylformamide (450 ml) is reacted at 140° C. for 30 minutes. After cooling, the reaction mixture is poured into ice-water and the precipitated crystals are filtered, which are re...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Ketone
Ester
c1ccccc1
c1ccc2ncccc2c1
C1CC1.c1ccc2ncccc2c1
HBr
CN(C=O)C
null
null
CCOC(=O)C(=CNC1CC1)C(=O)c1c(Br)cc(Br)c(F)c1C>CN(C=O)C>CCOC(=O)c1cn(C2CC2)c2cc(Br)c(F)c(C)c2c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f9699d46336a408a989760bcba92ed2e
Cc1c(F)c(Br)cc2c1c(=O)c(C(=O)O)cn2C1CC1.O=S(Cl)Cl>>Cc1c(F)c(Cl)cc2c1c(=O)c(C(=O)O)cn2C1CC1
[OH-].[Na+].C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)Br)F)C)=O)C(=O)O.S(=O)(Cl)Cl>>C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)Cl)F)C)=O)C(=O)O
Br[c:5]1[c:3]([F:4])[c:2]([CH3:1])[c:9]2[c:8]([cH:7]1)[n:17]([CH:18]1[CH2:19][CH2:20]1)[cH:16][c:12]([C:13](=[O:14])[OH:15])[c:10]2=[O:11].O=S(Cl)[Cl:6]>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([Cl:6])[cH:7][c:8]2[c:9]1[c:10](=[O:11])[c:12]([C:13](=[O:14])[OH:15])[cH:16][n:17]2[CH:18]1[CH2:19][CH2:20]1
Cc1c(F)c(Br)cc2c1c(=O)c(C(=O)O)cn2C1CC1.O=S(Cl)Cl
Cc1c(F)c(Cl)cc2c1c(=O)c(C(=O)O)cn2C1CC1
null
null
null
Functional Group Interconversion
OtherReaction
e284eb1a1a2e6a7ff4d99faedbf4df50ba8c3875dc22e9335e645ef3c2dbcb0e
4131cd1655d0ec8ecf7e181a36ab37eb3293d734e38ece0acf0e59405d170401
O=c1ccn(C2CC2)c2ccccc12
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3](:[c:4]:[c:5]:[c:6]:1-[F;D1;H0:7]):[#7;a:8](-[C:9]):[c:10].Cl-S(=O)-[Cl;H0;D1;+0:11]>>[C:9]-[#7;a:8](:[c:10]):[c:3]1:[c:2]:[c;H0;D3;+0:1](-[Cl;H0;D1;+0:11]):[c:6](-[F;D1;H0:7]):[c:5]:[c:4]:1
null
[]
null
null
30
MINUTE
To 1-cyclopropyl-6-fluoro-7-bromo-5-methyl-1,4- dihydro-4-oxoquinoline-3-carboxylic acid (0.2 g) is added thionyl chloride (2 ml) and the mixture is refluxed for 1 hour. After cooling, the reaction mixture is poured into ice-water and made alkaline with 10% aqueous sodium hydroxide solution. After stirring for 30 minut...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Aromatic halide
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1.C1CC1
Br-
null
null
0.5
Cc1c(F)c(Br)cc2c1c(=O)c(C(=O)O)cn2C1CC1.O=S(Cl)Cl>>Cc1c(F)c(Cl)cc2c1c(=O)c(C(=O)O)cn2C1CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b88a2a6137fb40db944423fb5f4a79e9
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.Nc1ccc(F)cc1F>>CCOC(=O)C(=CNc1ccc(F)cc1F)C(=O)c1c(F)cc(F)c(F)c1C
CC1=C(C(=O)C(C(=O)OCC)=COCC)C(=CC(=C1F)F)F.FC1=C(N)C=CC(=C1)F>>CC1=C(C(=O)C(C(=O)OCC)=CNC2=C(C=C(C=C2)F)F)C(=CC(=C1F)F)F
CCO[CH:7]=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:17](=[O:18])[c:19]1[c:20]([F:21])[cH:22][c:23]([F:24])[c:25]([F:26])[c:27]1[CH3:28].[NH2:8][c:9]1[cH:10][cH:11][c:12]([F:13])[cH:14][c:15]1[F:16]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[CH:7][NH:8][c:9]1[cH:10][cH:11][c:12]([F:13])[cH:14][c:15]1[F:16])[C:17](=[O:18])...
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.Nc1ccc(F)cc1F
CCOC(=O)C(=CNc1ccc(F)cc1F)C(=O)c1c(F)cc(F)c(F)c1C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
cd3db327c21c90c24d38808dacb2ed3fbf57044150e5b341d88de9389ff3759d
54aca1a08d403c8dd5c375df3e63fffc5027b15326b2523cf980a4a251290495
O=C(C=CNc1ccccc1)c1ccccc1
C-C-O-[CH;D2;+0:1]=[C:2](-[C:3](=[O;D1;H0:4])-[c:5])-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9].[NH2;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:2](=[CH;D2;+0:1]-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13])-[C:3](=[O;D1;H0:4])-[c:5]
87.1
[{"value": 87.1, "product": "CC1=C(C(=O)C(C(=O)OCC)=CNC2=C(C=C(C=C2)F)F)C(=CC(=C1F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Employing ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-ethoxyacrylate (1.0 g) and 2,4-difluoroaniline (0.5 g), the procedure of Reference Example 8 is repeated to give ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-(2,4-difluorophenyl)aminoacrylate (1.1 g). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Enamine
null
null
c1ccccc1.c1ccccc1
HO-
null
null
null
CCOC=C(C(=O)OCC)C(=O)c1c(F)cc(F)c(F)c1C.Nc1ccc(F)cc1F>>CCOC(=O)C(=CNc1ccc(F)cc1F)C(=O)c1c(F)cc(F)c(F)c1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c2cec4d8016440a8aabfc36afde71b94
CCOC(=O)C(=CNc1ccc(F)cc1F)C(=O)c1c(F)cc(F)c(F)c1C>>CCOC(=O)c1cn(-c2ccc(F)cc2F)c2cc(F)c(F)c(C)c2c1=O
CC1=C(C(=O)C(C(=O)OCC)=CNC2=C(C=C(C=C2)F)F)C(=CC(=C1F)F)F.[H-].[Na+]>>FC1=C(C=CC(=C1)F)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)OCC
F[c:17]1[cH:18][c:19]([F:20])[c:21]([F:22])[c:23]([CH3:24])[c:25]1[C:26]([C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][NH:8][c:9]1[cH:10][cH:11][c:12]([F:13])[cH:14][c:15]1[F:16])=[O:27]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8](-[c:9]2[cH:10][cH:11][c:12]([F:13])[cH:14][c:15]2[F:16])[c:17]2[cH:18][c:19]([F:2...
CCOC(=O)C(=CNc1ccc(F)cc1F)C(=O)c1c(F)cc(F)c(F)c1C
CCOC(=O)c1cn(-c2ccc(F)cc2F)c2cc(F)c(F)c(C)c2c1=O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
f1bb464adea8e64c138d384f2f02c35f1978964fc9c160676d8ef60c68e5e3df
ecabf5a50b4453255d534845e8b1084d96a0aaf957abdb24947c6089ec559e5f
O=c1ccn(-c2ccccc2)c2ccccc12
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C;H0;D3;+0:7](=[CH;D2;+0:8]-[NH;D2;+0:9]-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13](-[F;D1;H0:14]):[c:15])-[C:16](=[O;D1;H0:17])-[#8:18]-[C:19]):[c:20]>>[C:19]-[#8:18]-[C:16](=[O;D1;H0:17])-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[n;H0;D3;+0:9](-[c;H0;D3;+0:10](:[c:1...
67
[{"value": 67.0, "product": "FC1=C(C=CC(=C1)F)N1C=C(C(C2=C(C(=C(C=C12)F)F)C)=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Employing ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-(2,4-difluorophenyl)aminoacrylate (1.1 g) and 60% sodium hydride (0.13 g), the procedure of Reference Example 9 is repeated to give ethyl 1-(2,4-difluorophenyl)-5-methyl-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylate (0.7 g). Conditions: See reaction.notes.pr...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Ketone
Ester
c1ccccc1
c1ccc2ncccc2c1
c1ccccc1.c1ccc2ncccc2c1
HF
null
null
null
CCOC(=O)C(=CNc1ccc(F)cc1F)C(=O)c1c(F)cc(F)c(F)c1C>>CCOC(=O)c1cn(-c2ccc(F)cc2F)c2cc(F)c(F)c(C)c2c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4ea23bfddc534be9b03e25cecadbc056
CCOC=C(C(=O)OCC)C(=O)OCC.Cc1c(F)c(N2CCNCC2)cc(NC2CC2)c1[N+](=O)[O-]>>CCOC(=O)C(=CN(c1cc(N2CCNCC2)c(F)c(C)c1[N+](=O)[O-])C1CC1)C(=O)OCC
N1(CCNCC1)C=1C=C(NC2CC2)C(=C(C1F)C)[N+](=O)[O-].C(C)OC=C(C(=O)OCC)C(=O)OCC>>C1(CC1)N(C1=CC(=C(C(=C1[N+](=O)[O-])C)F)N1CCNCC1)C=C(C(=O)OCC)C(=O)OCC
CCO[C:4](=[O:5])[C:6](=[CH:7][O:3][CH2:2][CH3:1])[C:29](=[O:30])[O:31][CH2:32][CH3:33].[NH:8]([c:9]1[cH:10][c:11]([N:12]2[CH2:13][CH2:14][NH:15][CH2:16][CH2:17]2)[c:18]([F:19])[c:20]([CH3:21])[c:22]1[N+:23](=[O:24])[O-:25])[CH:26]1[CH2:27][CH2:28]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[CH:7][N:8]([c:9]1[cH:10][c:11]...
CCOC=C(C(=O)OCC)C(=O)OCC.Cc1c(F)c(N2CCNCC2)cc(NC2CC2)c1[N+](=O)[O-]
CCOC(=O)C(=CN(c1cc(N2CCNCC2)c(F)c(C)c1[N+](=O)[O-])C1CC1)C(=O)OCC
null
null
null
Functional Group Addition
OtherReaction
38cce29c47a06422870d2b994c7fc6572611707b1fe155de9452da80a160e466
575ae94c9a30081d7737dec981506212ab231d10166b2bd9b7134947ffcd0ce1
c1cc(NC2CC2)cc(N2CCNCC2)c1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](=[CH;D2;+0:4]-[O;H0;D2;+0:5]-[C:6]-[C;D1;H3:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11].[c:12]:[c:13](-[NH;D2;+0:14]-[C:15]1-[C:16]-[C:17]-1):[c:18]>>[C:11]-[#8:10]-[C:8](=[O;D1;H0:9])-[C:3](=[CH;D2;+0:4]-[N;H0;D3;+0:14](-[C:15]1-[C:16]-[C:17]-1)-[c:13](:[c:12]):[c:18])-[C;H0;D3;+0:1...
null
[]
150
CELSIUS
null
null
To 3-(1-piperazinyl)-4-fluoro-5-methyl-6-nitro-N-cyclopropylaniline (1.57 g) is added diethyl ethoxymethylenemalonate (1.45 ml) and the mixture is heated at 150° C. for 25 hours. After cooling, the reaction product is purified by silica-gel column-chromatography (dichloromethane:methanol=100:1) to give diethyl [N-cyclo...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Secondary amine
Enamine.Ester
null
null
c1ccccc1.C1C[NH]CCN1.C1CC1
HO-
null
150
null
CCOC=C(C(=O)OCC)C(=O)OCC.Cc1c(F)c(N2CCNCC2)cc(NC2CC2)c1[N+](=O)[O-]>>CCOC(=O)C(=CN(c1cc(N2CCNCC2)c(F)c(C)c1[N+](=O)[O-])C1CC1)C(=O)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cf9ee368bd9548f6bc7d6beba130ae9b
CCOC(=O)c1cn(C2CC2)c2cc(N3CCNCC3)c(F)c(C)c2c1=O>>Cc1c(F)c(N2CCNCC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
N1(CCNCC1)C1=C(C(=C2C(C(=CN(C2=C1)C1CC1)C(=O)OCC)=O)C)F.[OH-].[Na+].C(C)O>>N1(CCNCC1)C1=C(C(=C2C(C(=CN(C2=C1)C1CC1)C(=O)O)=O)C)F
CC[O:20][C:18]([c:17]1[c:15](=[O:16])[c:14]2[c:2]([CH3:1])[c:3]([F:4])[c:5]([N:6]3[CH2:7][CH2:8][NH:9][CH2:10][CH2:11]3)[cH:12][c:13]2[n:22]([CH:23]2[CH2:24][CH2:25]2)[cH:21]1)=[O:19]>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([N:6]2[CH2:7][CH2:8][NH:9][CH2:10][CH2:11]2)[cH:12][c:13]2[c:14]1[c:15](=[O:16])[c:17]([C:18](=[O:19])[O...
CCOC(=O)c1cn(C2CC2)c2cc(N3CCNCC3)c(F)c(C)c2c1=O
Cc1c(F)c(N2CCNCC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
null
null
O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1ccn(C2CC2)c2cc(N3CCNCC3)ccc12
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
56.4
[{"value": 56.4, "product": "N1(CCNCC1)C1=C(C(=C2C(C(=CN(C2=C1)C1CC1)C(=O)O)=O)C)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To ethyl 7-(1-piperazinyl)-1-cyclopropyl-6-fluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylate (23 mg) are added 10% aqueous solution of sodium hydroxide (3 ml) and ethanol (3 ml), and the mixture is refluxed for 1 hour. After cooling, the reaction mixture is diluted with water and washed with dichloromethane. Aft...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1C[NH]CCN1.c1ccc2ncccc2c1.C1CC1
Other
O
null
null
CCOC(=O)c1cn(C2CC2)c2cc(N3CCNCC3)c(F)c(C)c2c1=O>O>Cc1c(F)c(N2CCNCC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2010b52898404086bd489885248322bd
Cc1c(F)c(N2CC(C)C(NC(=O)OC(C)(C)C)C2)cc2c1c(=O)c(C(=O)O)cn2C1CC1>>Cc1c(F)c(N2CC(C)C(N)C2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
C(C)(C)(C)OC(=O)NC1CN(CC1C)C1=C(C(=C2C(C(=CN(C2=C1)C1CC1)C(=O)O)=O)C)F.Cl>>Cl.NC1CN(CC1C)C1=C(C(=C2C(C(=CN(C2=C1)C1CC1)C(=O)O)=O)C)F
CC(C)(C)OC(=O)[NH:11][CH:10]1[CH:8]([CH3:9])[CH2:7][N:6]([c:5]2[c:3]([F:4])[c:2]([CH3:1])[c:15]3[c:14]([cH:13]2)[n:23]([CH:24]2[CH2:25][CH2:26]2)[cH:22][c:18]([C:19](=[O:20])[OH:21])[c:16]3=[O:17])[CH2:12]1>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([N:6]2[CH2:7][CH:8]([CH3:9])[CH:10]([NH2:11])[CH2:12]2)[cH:13][c:14]2[c:15]1[c:16...
Cc1c(F)c(N2CC(C)C(NC(=O)OC(C)(C)C)C2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
Cc1c(F)c(N2CC(C)C(N)C2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
null
null
C(C)O
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=c1ccn(C2CC2)c2cc(N3CCCC3)ccc12
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4]-[#7:5]>>[#7:5]-[C:4]-[C:2](-[NH2;D1;+0:1])-[C:3]
null
[]
null
null
null
null
A mixture comprising 7-(3-t-butoxycarbonylamino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (trans form) (120 mg), ethanol (4 ml) and 10% hydrochloric acid (4 ml) is refluxed for 30 minutes. After concentrating, the obtained residue is recrystallized from methan...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
C1CC[NH]C1.c1ccc2ncccc2c1.C1CC1
HO-
C(C)O
null
null
Cc1c(F)c(N2CC(C)C(NC(=O)OC(C)(C)C)C2)cc2c1c(=O)c(C(=O)O)cn2C1CC1>C(C)O>Cc1c(F)c(N2CC(C)C(N)C2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a4f5c585a2f143a1af864ac4739e3c74
CC(=O)OC(C)=O.Cc1c(F)c(N2CCNCC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1>>CC(=O)N1CCN(c2cc3c(c(C)c2F)c(=O)c(C(=O)O)cn3C2CC2)CC1
Cl.N1(CCNCC1)C1=C(C(=C2C(C(=CN(C2=C1)C1CC1)C(=O)O)=O)C)F.C(C)(=O)OC(C)=O>>C(C)(=O)N1CCN(CC1)C1=C(C(=C2C(C(=CN(C2=C1)C1CC1)C(=O)O)=O)C)F
CC(=O)O[C:2]([CH3:1])=[O:3].[NH:4]1[CH2:5][CH2:6][N:7]([c:8]2[cH:9][c:10]3[c:11]([c:12]([CH3:13])[c:14]2[F:15])[c:16](=[O:17])[c:18]([C:19](=[O:20])[OH:21])[cH:22][n:23]3[CH:24]2[CH2:25][CH2:26]2)[CH2:27][CH2:28]1>>[CH3:1][C:2](=[O:3])[N:4]1[CH2:5][CH2:6][N:7]([c:8]2[cH:9][c:10]3[c:11]([c:12]([CH3:13])[c:14]2[F:15])[c:...
CC(=O)OC(C)=O.Cc1c(F)c(N2CCNCC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
CC(=O)N1CCN(c2cc3c(c(C)c2F)c(=O)c(C(=O)O)cn3C2CC2)CC1
null
null
[OH-].[Na+]
Acylation
Aminolysis of esters
b3be41bbcee62996e53bc3035dc7cc02d97d5bc8a1e1c9b0ca187f26f9fbfafa
6593c6062585994f02076cd3c86920ae7244b86659eab65c21b5a8628c6d4bb8
O=c1ccn(C2CC2)c2cc(N3CCNCC3)ccc12
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#7:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[N;H0;D3;+0:7]1-[C:6]-[C:5]-[#7:4]-[C:9]-[C:8]-1
null
[]
null
null
null
null
To a solution of 7-(1-piperazinyl)-1-cyclopropyl-6-fluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (40 mg) in 5% sodium hydroxide (2 ml) is added acetic anhydride (0.1 ml) at room temperature. After the mixture is made acidic with dilute hydrochloric acid, the resultant is extracted with dichloromethane an...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Secondary amine
Tertiary amide
C1CNCC[NH]1
C1C[NH]CC[NH]1
C1C[NH]CC[NH]1.c1ccc2ncccc2c1.C1CC1
HO-
[OH-].[Na+]
null
null
CC(=O)OC(C)=O.Cc1c(F)c(N2CCNCC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1>[OH-].[Na+]>CC(=O)N1CCN(c2cc3c(c(C)c2F)c(=O)c(C(=O)O)cn3C2CC2)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4dd793d179ff43a5b9d3cc139df171bf
Cc1c(F)c(Br)cc2c1c(=O)c(C(=O)O)cn2C1CC1.O=C1CCNCC1>>Cc1c(F)c(N2CCC(=O)CC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)Br)F)C)=O)C(=O)O.O=C1CCNCC1>>C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)N1CCC(CC1)=O)F)C)=O)C(=O)O
Br[c:5]1[c:3]([F:4])[c:2]([CH3:1])[c:15]2[c:14]([cH:13]1)[n:23]([CH:24]1[CH2:25][CH2:26]1)[cH:22][c:18]([C:19](=[O:20])[OH:21])[c:16]2=[O:17].[NH:6]1[CH2:7][CH2:8][C:9](=[O:10])[CH2:11][CH2:12]1>>[CH3:1][c:2]1[c:3]([F:4])[c:5]([N:6]2[CH2:7][CH2:8][C:9](=[O:10])[CH2:11][CH2:12]2)[cH:13][c:14]2[c:15]1[c:16](=[O:17])[c:18...
Cc1c(F)c(Br)cc2c1c(=O)c(C(=O)O)cn2C1CC1.O=C1CCNCC1
Cc1c(F)c(N2CCC(=O)CC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
null
null
CN1C(CCC1)=O
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
6ca896bdf5cf17e98a9402041cc62e117ebb3e6ff582ec413fbc5219ab9874c5
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
O=C1CCN(c2ccc3c(=O)ccn(C4CC4)c3c2)CC1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3](:[c:4]:[c:5]:[c:6]:1-[F;D1;H0:7]):[#7;a:8](-[C:9]):[c:10].[O;D1;H0:11]=[C:12]1-[C:13]-[C:14]-[NH;D2;+0:15]-[C:16]-[C:17]-1>>[C:9]-[#7;a:8](:[c:10]):[c:3]1:[c:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:15]2-[C:14]-[C:13]-[C:12](=[O;D1;H0:11])-[C:17]-[C:16]-2):[c:6](-[F;D1;H0:7]):[c:5]:[c:4]:1
37.6
[{"value": 37.6, "product": "C1(CC1)N1C=C(C(C2=C(C(=C(C=C12)N1CCC(CC1)=O)F)C)=O)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
null
null
To a solution of 1-cyclopropyl-6-fluoro-7-bromo-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.58 g) in N-methyl-2-pyrrolidone (5 ml) is added 4-oxopiperidine (0.64 g) and the mixture is heated at 90° C. for 20 minutes. The solvent is distilled off under reduced pressure. To the resulting residue is added eth...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccc2ncccc2c1.C1CCNCC1
C1CC[NH]CC1.c1ccc2ncccc2c1
C1CC[NH]CC1.c1ccc2ncccc2c1.C1CC1
HBr
CN1C(CCC1)=O
90
null
Cc1c(F)c(Br)cc2c1c(=O)c(C(=O)O)cn2C1CC1.O=C1CCNCC1>CN1C(CCC1)=O>Cc1c(F)c(N2CCC(=O)CC2)cc2c1c(=O)c(C(=O)O)cn2C1CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-05149c9288364f2583be374274cc2755
CC(C)(C)C(=O)C(=O)[O-].NO>>CC(C)(C)C(=NO)C(=O)O
[Na+].CC(C(C(=O)[O-])=O)(C)C.Cl.NO>>CC(C(C(=O)O)=NO)(C)C
O=[C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])[C:8](=[O:9])[O-:10].[NH2:6][OH:7]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[N:6][OH:7])[C:8](=[O:9])[OH:10]
CC(C)(C)C(=O)C(=O)[O-].NO
CC(C)(C)C(=NO)C(=O)O
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
563f6a8535c43609e054d888343590b2682c219f195349290c332185db5b558f
e64636ca549954a90be725fde08b07bc1a3f451bbed63061829d2618f80d2516
null
O=[C;H0;D3;+0:1](-[C:2](-[O-;H0;D1:3])=[O;D1;H0:4])-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].[NH2;D1;+0:9]-[O;D1;H1:10]>>[C;D1;H3:6]-[C:5](-[C;D1;H3:7])(-[C;D1;H3:8])-[C;H0;D3;+0:1](=[N;H0;D2;+0:9]-[O;D1;H1:10])-[C:2](=[O;D1;H0:4])-[OH;D1;+0:3]
81.2
[{"value": 81.0, "product": "CC(C(C(=O)O)=NO)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.2, "product": "CC(C(C(=O)O)=NO)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
163 g (1 mole) 93.5% trimethylpyruvic acid sodium salt and 69.5 g (1 mole) hydroxylamine hydrochloride were dissolved at 40° C. in 450 ml water. The product crystallized out during slow cooling under agitation. After 1.5 h agitation in an ice bath the crystals were filtered off, washed with 150 ml ice water, dried in a...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Carboxylic acid.Oxime
null
null
null
HO-
O
null
null
CC(C)(C)C(=O)C(=O)[O-].NO>O>CC(C)(C)C(=NO)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dd9603f73e7d4c139f69155d33de1172
CC(C)(C)[C@@H](N)CO.CCOC(=O)Cl>>CC(C)(C)[C@@H]1COC(=O)N1
[OH-].[Na+].N[C@H](C(C)(C)C)CO.O.C(C)OC(=O)Cl>>C(C)(C)(C)[C@H]1NC(OC1)=O
[CH3:1][C:2]([CH3:3])([CH3:4])[C@H:5]([CH2:6][OH:7])[NH2:10].CCO[C:8](Cl)=[O:9]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C@@H:5]1[CH2:6][O:7][C:8](=[O:9])[NH:10]1
CC(C)(C)[C@@H](N)CO.CCOC(=O)Cl
CC(C)(C)[C@@H]1COC(=O)N1
null
null
C1(=CC=CC=C1)C
Protection
OtherReaction
f9d29bd4817ea47fcfe120b170cfc227567f09cb92c6b107b13832ce06e891fc
09b7218caca4bbcd940f7b50cdf774e76319a49137d8b21f1dade5f374345a97
O=C1NCCO1
C-C-O-[C;H0;D3;+0:1](-Cl)=[O;D1;H0:2].[C:3]-[C:4](-[NH2;D1;+0:5])-[C:6]-[OH;D1;+0:7]>>[C:3]-[C:4]1-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-1
80
[{"value": 80.0, "product": "C(C)(C)(C)[C@H]1NC(OC1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.9, "product": "C(C)(C)(C)[C@H]1NC(OC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
null
null
73 g (containing 0.25 mole (R)-tert-leucinol) of the filtrate cited in example 6 was taken up with 27 ml water and 200 ml toluene. 25 ml (0.26 mole) chloroformic acid ethyl ester were then added dropwise at 20°-25° C., during which the pH was maintained at 7-8.5 by the addition of 10 M sodium hydroxide solution. The mi...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary alcohol.Primary amine
Carbamic ester
null
C1COCN1
C1COCN1
HCl
C1(=CC=CC=C1)C
65
null
CC(C)(C)[C@@H](N)CO.CCOC(=O)Cl>C1(=CC=CC=C1)C>CC(C)(C)[C@@H]1COC(=O)N1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-84448ea235a5434095bfa277b099b79d
Cc1ccc(Nc2ccc(C)c(C)c2)cc1C.Ic1ccc(-c2ccccc2)cc1>>Cc1ccc(N(c2ccc(-c3ccccc3)cc2)c2ccc(C)c(C)c2)cc1C
N1=CC=CC2=CC=C3C=CC=NC3=C12.CC=1C=C(C=CC1C)NC1=CC(=C(C=C1)C)C.IC1=CC=C(C=C1)C1=CC=CC=C1.[OH-].[K+]>>CC=1C=C(C=CC1C)N(C1=CC=C(C=C1)C1=CC=CC=C1)C1=CC(=C(C=C1)C)C
[CH3:1][c:2]1[cH:3][cH:4][c:5]([NH:6][c:19]2[cH:20][cH:21][c:22]([CH3:23])[c:24]([CH3:25])[cH:26]2)[cH:27][c:28]1[CH3:29].I[c:7]1[cH:8][cH:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17][cH:18]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([N:6]([c:7]2[cH:8][cH:9][c:10](-[c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[cH...
Cc1ccc(Nc2ccc(C)c(C)c2)cc1C.Ic1ccc(-c2ccccc2)cc1
Cc1ccc(N(c2ccc(-c3ccccc3)cc2)c2ccc(C)c(C)c2)cc1C
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
705933786518ece8447c3a260ed1708cc50b5b37b829540bc5bba9d6bb1dde91
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccc(-c2ccc(N(c3ccccc3)c3ccccc3)cc2)cc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[c:6]:[c:7](-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]):[c:12]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:8](-[c:7](:[c:6]):[c:12])-[c:9](:[c:10]):[c:11]):[c:4]:[c:5]
null
[]
120
CELSIUS
3
HOUR
In a 500 milliliter round bottomed flask equipped with mechanical stirrer and fitted with a Dean-Stark trap under a reflux condenser were placed 12.39 grams (0.055 mole) of bis(3,4-dimethylphenyl)amine, 14 grams (0.050 mole) of 4-iodobiphenyl, 0.25 gram (0.0025 mole) of cuprous chloride, 0.45 gram (0,0025 mole) of 1,10...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HI
C1(=CC=CC=C1)C
120
3
Cc1ccc(Nc2ccc(C)c(C)c2)cc1C.Ic1ccc(-c2ccccc2)cc1>C1(=CC=CC=C1)C>Cc1ccc(N(c2ccc(-c3ccccc3)cc2)c2ccc(C)c(C)c2)cc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c73a1583f23e4b29be1a2f3ab4c01786
Cc1ccc(I)cc1C.Nc1ccc(-c2ccccc2)cc1>>Cc1ccc(N(c2ccc(-c3ccccc3)cc2)c2ccc(C)c(C)c2)cc1C
[OH-].[K+].NC1=CC=C(C=C1)C1=CC=CC=C1.IC=1C=C(C(=CC1)C)C>>CC=1C=C(C=CC1C)N(C1=CC=C(C=C1)C1=CC=CC=C1)C1=CC(=C(C=C1)C)C
I[c:5]1[cH:4][cH:3][c:2]([CH3:1])[c:28]([CH3:29])[cH:27]1.[NH2:6][c:7]1[cH:8][cH:9][c:10](-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17][cH:18]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([N:6]([c:7]2[cH:8][cH:9][c:10](-[c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[cH:17][cH:18]2)[c:19]2[cH:20][cH:21][c:22]([CH3:23])[c:24]([...
Cc1ccc(I)cc1C.Nc1ccc(-c2ccccc2)cc1
Cc1ccc(N(c2ccc(-c3ccccc3)cc2)c2ccc(C)c(C)c2)cc1C
null
N1=CC=CC2=CC=C3C=CC=NC3=C12
C1(=CC=CC=C1)C
Aromatic Heterocycle Formation
OtherReaction
850bf8b88603759e93e21aa4bc6ea75b619f817ec1a4a2b605bfab9b13302179
4798700b8674842eb5bdd2fe41a2eb48ecea3f9c3ee8f644eef6be0214075a26
c1ccc(-c2ccc(N(c3ccccc3)c3ccccc3)cc2)cc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[c:8]:[c:7](-[N;H0;D3;+0:6](-[c:10](:[c:11]):[c:12])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]):[c:9]
70
[{"value": 70.0, "product": "CC=1C=C(C=CC1C)N(C1=CC=C(C=C1)C1=CC=CC=C1)C1=CC(=C(C=C1)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.9, "product": "CC=1C=C(C=CC1C)N(C1=CC=C(C=C1)C1=CC=CC=C1)C1=CC(=C(C=C1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
130
CELSIUS
3
HOUR
In a 250 milliliter round-bottomed flask equipped with mechanical stirrer and fitted with a Dean-Stark trap under a reflux condenser were placed 8.46 grams (0.05 mole) of 4-aminobiphenyl, 25.53 grams (0.11 mole) of 4-iodo-ortho-xylene, 0.25 gram (0.0025 mole) of cuprous chloride, 0.45 gram (0.0025 mole) of 1,10-phenant...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Tertiary amine
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
I-
N1=CC=CC2=CC=C3C=CC=NC3=C12.C1(=CC=CC=C1)C
130
3
Cc1ccc(I)cc1C.Nc1ccc(-c2ccccc2)cc1>N1=CC=CC2=CC=C3C=CC=NC3=C12.C1(=CC=CC=C1)C>Cc1ccc(N(c2ccc(-c3ccccc3)cc2)c2ccc(C)c(C)c2)cc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d880e525dd19411dbb94deface4386f9
Fc1ccc(Cc2ccc(F)cc2)cc1.O=S(=O)(O)O>>O=C(c1ccc(F)cc1)c1ccc(F)cc1
C1=CC(=CC=C1CC2=CC=C(C=C2)F)F.OS(=O)(=O)O.C1(=CC=CC=C1)C.OS(=O)(=O)O>>FC1=CC=C(C(=O)C2=CC=C(C=C2)F)C=C1
[CH2:2]([c:3]1[cH:4][cH:5][c:6]([F:7])[cH:8][cH:9]1)[c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]1.O=S(=O)(O)[OH:1]>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][c:6]([F:7])[cH:8][cH:9]1)[c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]1
Fc1ccc(Cc2ccc(F)cc2)cc1.O=S(=O)(O)O
O=C(c1ccc(F)cc1)c1ccc(F)cc1
null
O=[Mn]=O
O
Heteroatom Alkylation and Arylation
OtherReaction
7a0b8463d98f4c7b922b16e60aaf09698e9f90cf246a26e079db9b5cbdeab585
a196f7191876ee39420290ab9d6c2b9eeb3251b37ae345fc435efba1949a85d9
O=C(c1ccccc1)c1ccccc1
O-S(=O)(=O)-[OH;D1;+0:1].[c:2]:[c:3](-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]):[c:8]>>[O;H0;D1;+0:1]=[C;H0;D3;+0:4](-[c:3](:[c:2]):[c:8])-[c:5](:[c:6]):[c:7]
69.2
[{"value": 68.0, "product": "FC1=CC=C(C(=O)C2=CC=C(C=C2)F)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.2, "product": "FC1=CC=C(C(=O)C2=CC=C(C=C2)F)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
125
CELSIUS
null
null
To a 250 mL round bottomed flask equipped with a heating mantle, overhead agitator, thermometer, condenser, and addition funnel with a tube protruding below the liquid level was added 10.6 g 4,4'-difluorodiphenylmethane (0.051 moles). Agitation was begun and a slurry of 20.5 g MnO2 (0.195 moles) in 30 g water was added...
10.6084/m9.figshare.5104873.v1
null
null
Ketone
null
null
c1ccccc1.c1ccccc1
HO-
O=[Mn]=O.O
125
null
Fc1ccc(Cc2ccc(F)cc2)cc1.O=S(=O)(O)O>O=[Mn]=O.O>O=C(c1ccc(F)cc1)c1ccc(F)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f59502531b224cbdb38244051ab9c738
Fc1ccc(Cc2ccc(F)cc2)cc1.O>>O=C(c1ccc(F)cc1)c1ccc(F)cc1
C1=CC(=CC=C1CC2=CC=C(C=C2)F)F.O>>FC1=CC=C(C(=O)C2=CC=C(C=C2)F)C=C1
[CH2:2]([c:3]1[cH:4][cH:5][c:6]([F:7])[cH:8][cH:9]1)[c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]1.[OH2:1]>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][c:6]([F:7])[cH:8][cH:9]1)[c:10]1[cH:11][cH:12][c:13]([F:14])[cH:15][cH:16]1
Fc1ccc(Cc2ccc(F)cc2)cc1.O
O=C(c1ccc(F)cc1)c1ccc(F)cc1
null
O=[Mn]=O
null
Heteroatom Alkylation and Arylation
OtherReaction
7a0b8463d98f4c7b922b16e60aaf09698e9f90cf246a26e079db9b5cbdeab585
a196f7191876ee39420290ab9d6c2b9eeb3251b37ae345fc435efba1949a85d9
O=C(c1ccccc1)c1ccccc1
[OH2;D0;+0:1].[c:2]:[c:3](-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]):[c:8]>>[O;H0;D1;+0:1]=[C;H0;D3;+0:4](-[c:3](:[c:2]):[c:8])-[c:5](:[c:6]):[c:7]
95
[{"value": 95.0, "product": "FC1=CC=C(C(=O)C2=CC=C(C=C2)F)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
The procedure of Example 1 was used except that 20 g 4,4'-difluorodiphenylmethane, 30 g water, 31 g MnO2 and 50 g H2 SO4 were used. 20 g off-white solids, after toluene removal, afforded 95% pure 4,4'-difluorobenzophenone in a 90% yield. Conditions: See reaction.notes.procedure_details. Workup: 20 g off-white solids, a...
10.6084/m9.figshare.5104873.v1
null
null
Ketone
null
null
c1ccccc1.c1ccccc1
null
O=[Mn]=O
null
null
Fc1ccc(Cc2ccc(F)cc2)cc1.O>O=[Mn]=O>O=C(c1ccc(F)cc1)c1ccc(F)cc1