dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
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large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dcc5f15a2f3f46578b2a4b1538a1f0d4
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.S(O)(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]
54
[{"value": 54.0, "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 2 is used except that the 4,4'-difluorodiphenylmethane, water, and sulfuric acid are first mixed, then heated before the MnO2 is added. The yield is 54% 4,4'-difluorobenzophenone that is 95% pure. Conditions: See reaction.notes.procedure_details. Workup: are first mixed; is added
10.6084/m9.figshare.5104873.v1
null
null
Ketone
null
null
c1ccccc1.c1ccccc1
HO-
O=[Mn]=O.O
null
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-96051f14cb3b4b208319a04c297eb60a
COC(O)C(F)(F)F.c1c[nH]c(Cc2ccc[nH]2)c1>>FC(F)(F)C(c1ccc[nH]1)c1ccc[nH]1
C1=CNC(=C1)CC2=CC=CN2.N1C=CC=C1.COC(C(F)(F)F)O.Cl>>N1C(=CC=C1)C(C(F)(F)F)C=1NC=CC1
CO[CH:5](O)[C:2]([F:1])([F:3])[F:4].C([c:6]1[cH:7][cH:8][cH:9][nH:10]1)[c:11]1[cH:12][cH:13][cH:14][nH:15]1>>[F:1][C:2]([F:3])([F:4])[CH:5]([c:6]1[cH:7][cH:8][cH:9][nH:10]1)[c:11]1[cH:12][cH:13][cH:14][nH:15]1
COC(O)C(F)(F)F.c1c[nH]c(Cc2ccc[nH]2)c1
FC(F)(F)C(c1ccc[nH]1)c1ccc[nH]1
null
null
O1CCCC1
C-C Coupling
OtherReaction
26bb76746e821a862b1e2d546d22a30a9fdcdd23dd039944c7d038242961e716
d57bc9a8102fea3a5aa53b38c291195cce6195e07ef2332b8d2a4f85929ab48b
c1c[nH]c(Cc2ccc[nH]2)c1
C(-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[c:5]:1)-[c;H0;D3;+0:6]1:[#7;a:7]:[c:8]:[c:9]:[c:10]:1.C-O-[CH;D3;+0:11](-O)-[C:12](-[F;D1;H0:13])(-[F;D1;H0:14])-[F;D1;H0:15]>>[F;D1;H0:13]-[C:12](-[F;D1;H0:14])(-[F;D1;H0:15])-[CH;D3;+0:11](-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]:[c:5]:1)-[c;H0;D3;+0:6]1:[#7;a:7]:[c:8]:[c:9]:[c:1...
80
[{"value": 80.0, "product": "N1C(=CC=C1)C(C(F)(F)F)C=1NC=CC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Pyrrole (150 mmol) and trifluoroacetaldehyde methyl hemiacetal (75 mmol) in tetrahydrofuran are heated at reflux with catalytic amounts of hydrochloric acid for 2 hours under an inert atmosphere. GC analysis of the reaction mixture indicated the presence of the desired dipyrromethane in greater than 80% yield. Neutrali...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary alcohol
null
c1cc[nH]c1.c1cc[nH]c1
c1cc[nH]c1.c1cc[nH]c1
c1cc[nH]c1.c1cc[nH]c1
HO-
O1CCCC1
null
null
COC(O)C(F)(F)F.c1c[nH]c(Cc2ccc[nH]2)c1>O1CCCC1>FC(F)(F)C(c1ccc[nH]1)c1ccc[nH]1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-68a3f07b1c044ef79787604ed33c105d
C1=Cc2ccccc2C1.Cc1cc(C)c([Si](Cl)(Cl)c2c(C)cc(C)cc2C)c(C)c1.[Li][CH2]CCC>>Cc1cc(C)c([Si](c2c(C)cc(C)cc2C)(C2C=Cc3ccccc32)C2C=Cc3ccccc32)c(C)c1
C1(=C(C(=CC(=C1)C)C)[Si](Cl)(Cl)C1=C(C=C(C=C1C)C)C)C.C1C=CC2=CC=CC=C12.C(CCC)[Li]>>C1(=C(C(=CC(=C1)C)C)[Si](C1C=CC2=CC=CC=C12)(C1C=CC2=CC=CC=C12)C1=C(C=C(C=C1C)C)C)C
[CH2:26]1[CH:27]=[CH:28][c:29]2[cH:30][cH:31][cH:32][cH:33][c:34]21.Cl[Si:7](Cl)([c:6]1[c:4]([CH3:5])[cH:3][c:2]([CH3:1])[cH:37][c:35]1[CH3:36])[c:8]1[c:9]([CH3:10])[cH:11][c:12]([CH3:13])[cH:14][c:15]1[CH3:16].[Li][CH2:19][CH2:18][CH2:17][CH3:25]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[c:6]([Si:7]([c:8]2[c:9]([CH3:10])[cH:...
C1=Cc2ccccc2C1.Cc1cc(C)c([Si](Cl)(Cl)c2c(C)cc(C)cc2C)c(C)c1.[Li][CH2]CCC
Cc1cc(C)c([Si](c2c(C)cc(C)cc2C)(C2C=Cc3ccccc32)C2C=Cc3ccccc32)c(C)c1
null
null
C1CCOC1
Functional Group Addition
OtherReaction
f5ba5559104034d0f598342b2bcfc145616a870a9c5fd32040e01d9d349081e9
56324ad3df7b9487aaee7bd464929a93e4e28f6516884ae0bd489c1176bd68e8
C1=CC([Si](c2ccccc2)(c2ccccc2)C2C=Cc3ccccc32)c2ccccc21
Cl-[Si;H0;D4;+0:1](-Cl)(-[c:2](:[c:3]):[c:4])-[c:5](:[c:6]):[c:7].[CH3;D1;+0:8]-[CH2;D2;+0:9]-[CH2;D2;+0:10]-[CH2;D2;+0:11]-[Li].[c:12]:[c:13]1:[c:14]-[C:15]=[C:16]-[CH2;D2;+0:17]-1>>[c:6]:[c:5](-[Si;H0;D4;+0:1](-[CH;D3;+0:9]1-[CH;D2;+0:10]=[CH;D2;+0:11]-[c:18](:[c:19]):[c;H0;D3;+0:8]-1:[c:20]:[c:21])(-[CH;D3;+0:17]1-[...
null
[]
null
null
null
null
7 g of indene in 50 cm3of THF were reacted with 24 cm3 of butyllithium (2.5-molar in hexane) at 0° C. under inert conditions. The mixture was heated to room temperature, added dropwise to a solution of 10 g of dimesityldichlorosilane in 40 cm3 of THF, and the mixture was refluxed for 4 hours. Decomposition of the batch...
10.6084/m9.figshare.5104873.v1
null
Silyl protective group.Alkyl lithium
Silyl protective group
C1=Cc2ccccc2C1
C1=Cc2ccccc2C1.C1=Cc2ccccc2C1
c1ccccc1.c1ccccc1.C1=Cc2ccccc2C1.C1=Cc2ccccc2C1
HCl.Li
C1CCOC1
null
null
C1=Cc2ccccc2C1.Cc1cc(C)c([Si](Cl)(Cl)c2c(C)cc(C)cc2C)c(C)c1.[Li][CH2]CCC>C1CCOC1>Cc1cc(C)c([Si](c2c(C)cc(C)cc2C)(C2C=Cc3ccccc32)C2C=Cc3ccccc32)c(C)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d4e2b55500174bc5b7869b5b5174c913
C#C[Si](C)(C)C.COc1ccc(C2=CC(=O)CCC2)cc1OC1CCCC1>>COc1ccc(C2(C#C[Si](C)(C)C)CCCC(=O)C2)cc1OC1CCCC1
C(CCC)[Li].C[Si](C)(C)C#C.[Cl-].C[Al+]C.C1(CCCC1)OC=1C=C(C=CC1OC)C1=CC(CCC1)=O.[C-]#[C-].[Al+3].[C-]#[C-].[C-]#[C-].[Al+3].Cl.P(=O)([O-])([O-])[O-].[K+].[K+].[K+].[H-].C(C(C)C)[Al+]CC(C)C>>C1(CCCC1)OC=1C=C(C=CC1OC)C1(CC(CCC1)=O)C#C[Si](C)(C)C
[CH:8]#[C:9][Si:10]([CH3:11])([CH3:12])[CH3:13].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2=[CH:19][C:17](=[O:18])[CH2:16][CH2:15][CH2:14]2)[cH:20][c:21]1[O:22][CH:23]1[CH2:24][CH2:25][CH2:26][CH2:27]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2([C:8]#[C:9][Si:10]([CH3:11])([CH3:12])[CH3:13])[CH2:14][CH2:15][CH2:16][C:1...
C#C[Si](C)(C)C.COc1ccc(C2=CC(=O)CCC2)cc1OC1CCCC1
COc1ccc(C2(C#C[Si](C)(C)C)CCCC(=O)C2)cc1OC1CCCC1
null
C/C(=C/C(=O)C)/[O-].C/C(=C/C(=O)C)/[O-].[Ni+2]
CCOCC
C-C Coupling
OtherReaction
ddd89ebc1749bc44b47a2b082f77fd8d8e29610c5cb4f10c5a05976ac8c3fe51
496ecbb5613a35d3e186da35e0b9e585797614c00ffb214bf902564b30c30743
O=C1CCCC(c2cccc(OC3CCCC3)c2)C1
[C;D1;H3:1]-[#14:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C:5]#[CH;D1;+0:6].[O;D1;H0:7]=[C:8]1-[C:9]-[C:10]-[C:11]-[C;H0;D3;+0:12](-[c:13](:[c:14]):[c:15])=[CH;D2;+0:16]-1>>[C;D1;H3:1]-[#14:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C:5]#[C;H0;D2;+0:6]-[C;H0;D4;+0:12]1(-[c:13](:[c:14]):[c:15])-[C:11]-[C:10]-[C:9]-[C:8](=[O;D1;H0:7])-[CH2;...
null
[]
-10
CELSIUS
1.5
HOUR
n-Butyllithium (2.45M in hexanes, 5.7 mL, 13.96 mmol) was added dropwise over 5 min to a solution of trimethylsilylacetylene (1.97 mL, 13.96 mmol) dissolved in dry ether (30 mL) at -45° C. under an argon atmosphere. After 1.5 h, this solution was cannulated into a solution of dimethylaluminum chloride (1.0M in hexanes,...
10.6084/m9.figshare.5104873.v1
null
Ketone.Alkyne
Ketone.Alkyne
C1=CCCCC1
C1CCCCC1
c1ccccc1.C1CCCCC1.C1CCCC1
null
C/C(=C/C(=O)C)/[O-].C/C(=C/C(=O)C)/[O-].[Ni+2].CCOCC
-10
1.5
C#C[Si](C)(C)C.COc1ccc(C2=CC(=O)CCC2)cc1OC1CCCC1>C/C(=C/C(=O)C)/[O-].C/C(=C/C(=O)C)/[O-].[Ni+2].CCOCC>COc1ccc(C2(C#C[Si](C)(C)C)CCCC(=O)C2)cc1OC1CCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a765bb3f88ef412dab87283ec66e35db
COc1ccc(C2(C#C[Si](C)(C)C)CCCC(=O)C2)cc1OC1CCCC1>>C#CC1(c2ccc(OC)c(OC3CCCC3)c2)CCCC(=O)C1
[F-].[K+].C1(CCCC1)OC=1C=C(C=CC1OC)C1(CC(CCC1)=O)C#C[Si](C)(C)C.O>>C1(CCCC1)OC=1C=C(C=CC1OC)C1(CC(CCC1)=O)C#C
C[Si](C)(C)[C:1]#[C:2][C:3]1([c:4]2[cH:5][cH:6][c:7]([O:8][CH3:9])[c:10]([O:11][CH:12]3[CH2:13][CH2:14][CH2:15][CH2:16]3)[cH:17]2)[CH2:18][CH2:19][CH2:20][C:21](=[O:22])[CH2:23]1>>[CH:1]#[C:2][C:3]1([c:4]2[cH:5][cH:6][c:7]([O:8][CH3:9])[c:10]([O:11][CH:12]3[CH2:13][CH2:14][CH2:15][CH2:16]3)[cH:17]2)[CH2:18][CH2:19][CH2...
COc1ccc(C2(C#C[Si](C)(C)C)CCCC(=O)C2)cc1OC1CCCC1
C#CC1(c2ccc(OC)c(OC3CCCC3)c2)CCCC(=O)C1
null
null
CN(C=O)C
Deprotection
TMS deprotection from alkyne
e85676bb81da384790c9c858d44f182cdd01e3a79f77f7a239fe38487234cb96
56d526d7c9cb1bd7bee4940e216a9b1dd4597fd025a186b8d6e4675d8f4db26b
O=C1CCCC(c2cccc(OC3CCCC3)c2)C1
C-[Si](-C)(-C)-[C;H0;D2;+0:1]#[C:2]-[C:3]>>[C:3]-[C:2]#[CH;D1;+0:1]
null
[]
null
null
18
HOUR
A mixture of potassium fluoride (900 mg, 15.6 mmol) and 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-trimethylsilylethynylcyclohexan-1-one (0.3 g, 0.78 mmol) were stirred in dry N,N-dimethylformamide (3 mL) under an argon atmosphere. After 18 h, the solvent was removed in vacuo, the residue was partitioned between water and ...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Silyl protective group
Alkyne
null
null
c1ccccc1.C1CCCC1.C1CCCCC1
Other
CN(C=O)C
null
18
COc1ccc(C2(C#C[Si](C)(C)C)CCCC(=O)C2)cc1OC1CCCC1>CN(C=O)C>C#CC1(c2ccc(OC)c(OC3CCCC3)c2)CCCC(=O)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-269b34579b6543ad8b25187fc9fff0bb
CC(C)(C)C=NC1CCNC1.O=C(O)c1cn(C2CC2)c2c(F)c(F)c(F)cc2c1=O>>NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)C1
C1(CC1)N1C=C(C(C2=CC(=C(C(=C12)F)F)F)=O)C(=O)O.CC(C=NC1CNCC1)(C)C.Cl>>Cl.NC1CN(CC1)C1=C(C=C2C(C(=CN(C2=C1F)C1CC1)C(=O)O)=O)F
CC(C)(C)C=[N:2][CH:3]1[CH2:4][CH2:5][NH:6][CH2:26]1.F[c:7]1[c:8]([F:9])[cH:10][c:11]2[c:12](=[O:13])[c:14]([C:15](=[O:16])[OH:17])[cH:18][n:19]([CH:20]3[CH2:21][CH2:22]3)[c:23]2[c:24]1[F:25]>>[NH2:2][CH:3]1[CH2:4][CH2:5][N:6]([c:7]2[c:8]([F:9])[cH:10][c:11]3[c:12](=[O:13])[c:14]([C:15](=[O:16])[OH:17])[cH:18][n:19]([CH...
CC(C)(C)C=NC1CCNC1.O=C(O)c1cn(C2CC2)c2c(F)c(F)c(F)cc2c1=O
NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)C1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
710de7c0f65dd5c2121f3b57da0b26f7168348cc6c1e92dfd93051671f74f524
f353eb8fdf386bd5566d538a686db0446740ceebfed68cde5410916b51190f54
O=c1ccn(C2CC2)c2cc(N3CCCC3)ccc12
C-C(-C)(-C)-C=[N;H0;D2;+0:1]-[C:2]1-[C:3]-[NH;D2;+0:4]-[C:5]-[C:6]-1.F-[c;H0;D3;+0:7]1:[c:8](-[F;D1;H0:9]):[c:10](:[c:11]:[c:12]:[c:13]:1-[F;D1;H0:14]):[#7;a:15](-[C:16]):[c:17]>>[C:16]-[#7;a:15](:[c:17]):[c:10]1:[c:11]:[c:12]:[c:13](-[F;D1;H0:14]):[c;H0;D3;+0:7](-[N;H0;D3;+0:4]2-[C:3]-[C:2](-[NH2;D1;+0:1])-[C:6]-[C:5]...
null
[]
null
null
null
null
If, for example, 1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid is reacted with 3-(2,2-dimethylpropylideneamino)-pyrrolidine and the reaction product is treated with hydrochloric acid, 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid hydrochl...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Substituted imine.Secondary amine
Primary amine.Tertiary amine
C1CCNC1.c1ccc2ncccc2c1
C1CC[NH]C1.c1ccc2ncccc2c1
C1CC[NH]C1.c1ccc2ncccc2c1.C1CC1
HF
null
null
null
CC(C)(C)C=NC1CCNC1.O=C(O)c1cn(C2CC2)c2c(F)c(F)c(F)cc2c1=O>>NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2F)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9c49b6d642f487a8b46731f4e1e7af0
N[C@H]1CCNC1.O=C(O)c1cn(C2CC2)c2c(Cl)c(F)c(F)cc2c1=O.O=C(O)c1cn(C2CC2)c2c(Cl)c(N3CC[C@H](N=Cc4cccc([N+](=O)[O-])c4)C3)c(F)cc2c1=O>>Cl.N[C@H]1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1
ClC=1C(=C(C=C2C(C(=CN(C12)C1CC1)C(=O)O)=O)F)N1C[C@H](CC1)N=CC1=CC(=CC=C1)[N+](=O)[O-].[N+](=O)([O-])C=1C=C(C=O)C=CC1.N[C@@H]1CNCC1.ClC=1C(=C(C=C2C(C(=CN(C12)C1CC1)C(=O)O)=O)F)F>>Cl.N[C@@H]1CN(CC1)C1=C(C=C2C(C(=CN(C2=C1Cl)C1CC1)C(=O)O)=O)F
[NH2:2][C@H:3]1[CH2:4][CH2:5][NH:6][CH2:26]1.F[c:7]1[c:8]([F:9])[cH:10][c:11]2[c:12](=[O:13])[c:14]([C:15](=[O:16])[OH:17])[cH:18][n:19]([CH:20]3[CH2:21][CH2:22]3)[c:23]2[c:24]1[Cl:25].O=C(O)c1cn(C2CC2)c2c([Cl:1])c(N3CC[C@H](N=Cc4cccc([N+](=O)[O-])c4)C3)c(F)cc2c1=O>>[ClH:1].[NH2:2][C@H:3]1[CH2:4][CH2:5][N:6]([c:7]2[c:8...
N[C@H]1CCNC1.O=C(O)c1cn(C2CC2)c2c(Cl)c(F)c(F)cc2c1=O.O=C(O)c1cn(C2CC2)c2c(Cl)c(N3CC[C@H](N=Cc4cccc([N+](=O)[O-])c4)C3)c(F)cc2c1=O
Cl.N[C@H]1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1
null
null
null
Functional Group Interconversion
OtherReaction
78881d4233cf847b87824634d66c42a6f7871c5d6d250c7f037843fc9638c5c1
07252a64ae90f2baee4c93a74a5ef061c0a9357a49917c41f677ac91017b1b84
O=c1ccn(C2CC2)c2cc(N3CCCC3)ccc12
F-[c;H0;D3;+0:1]1:[c:2](-[Cl;D1;H0:3]):[c:4](:[c:5]:[c:6]:[c:7]:1-[F;D1;H0:8]):[#7;a:9](-[C:10]):[c:11].F-c1:c:c2:c(=O):c(-C(-O)=O):c:n(-C3-C-C-3):c:2:c(-[Cl;H0;D1;+0:12]):c:1-N1-C-C-[C@H](-N=C-c2:c:c:c:c(-[N+](=O)-[O-]):c:2)-C-1.[C:13]1-[C:14]-[C:15]-[C:16]-[NH;D2;+0:17]-1>>[C:10]-[#7;a:9](:[c:11]):[c:4]1:[c:5]:[c:6]:...
null
[]
null
null
null
null
If, for example, the reaction mixture of 3-nitrobenzaldehyde and (S)-3-aminopyrrolidine is reacted with 8-chloro-1-cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid in a one-pot reaction, the course of the reaction via the intermediately formed 8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-7-[(S)-3-(3...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Carboxylic acid.Substituted imine.Nitro group.Secondary amine.Tertiary amine
Tertiary amine
C1CCNC1.c1ccc2ncccc2c1.C1CC1.c1ccc2ncccc2c1.C1CCNC1.c1ccccc1
C1CC[NH]C1.c1ccc2ncccc2c1
C1CC[NH]C1.c1ccc2ncccc2c1.C1CC1
HF
null
null
null
N[C@H]1CCNC1.O=C(O)c1cn(C2CC2)c2c(Cl)c(F)c(F)cc2c1=O.O=C(O)c1cn(C2CC2)c2c(Cl)c(N3CC[C@H](N=Cc4cccc([N+](=O)[O-])c4)C3)c(F)cc2c1=O>>Cl.N[C@H]1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c0f745d78785401496f0649633321e35
CC(C)(C)C=O.NC1CCNC1>>CC(C)(C)C=NC1CCNC1
NC1CNCC1.C(C(C)(C)C)=O>>CC(C=NC1CNCC1)(C)C
O=[CH:5][C:2]([CH3:1])([CH3:3])[CH3:4].[NH2:6][CH:7]1[CH2:8][CH2:9][NH:10][CH2:11]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[CH:5]=[N:6][CH:7]1[CH2:8][CH2:9][NH:10][CH2:11]1
CC(C)(C)C=O.NC1CCNC1
CC(C)(C)C=NC1CCNC1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Addition of primary amines to aldehydes/thiocarbonyls
d409dfd3247abb6c1b1364aec380d25720f21e374fd2124063f2d2ce54d31c4f
9b341044a5a058244685b0b956d33f593ccdcd7346fa1d8d7b98a302fd35b8a2
C1CCNC1
O=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5].[#7:6]-[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10]>>[#7:6]-[C:7]-[C:8](-[N;H0;D2;+0:9]=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5])-[C:10]
74
[{"value": 74.0, "product": "CC(C=NC1CNCC1)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
34.5 g (0.4 mol) of 3-aminopyrrolidine are initially introduced into 100 ml of toluene, and 34.5 g (0.3 mol) of 75% strength pivalaldehyde (preparation from Riedel-de-Haen) in 100 ml of toluene are added dropwise at 20° C., while cooling in a water bath. The mixture is subsequently stirred at room temperature for 2 hou...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Substituted imine
null
null
C1CCNC1
HO-
C1(=CC=CC=C1)C
null
2
CC(C)(C)C=O.NC1CCNC1>C1(=CC=CC=C1)C>CC(C)(C)C=NC1CCNC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8341607dd237492f8c1a68b89ed51a7c
CC(C)(C)C=O.NC1CCNC1>>CC(C)(C)C=NC1CCNC1
C(C(C)(C)C)=O.NC1CNCC1>>CC(C=NC1CNCC1)(C)C
O=[CH:5][C:2]([CH3:1])([CH3:3])[CH3:4].[NH2:6][CH:7]1[CH2:8][CH2:9][NH:10][CH2:11]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[CH:5]=[N:6][CH:7]1[CH2:8][CH2:9][NH:10][CH2:11]1
CC(C)(C)C=O.NC1CCNC1
CC(C)(C)C=NC1CCNC1
null
null
null
Heteroatom Alkylation and Arylation
Addition of primary amines to aldehydes/thiocarbonyls
d409dfd3247abb6c1b1364aec380d25720f21e374fd2124063f2d2ce54d31c4f
9b341044a5a058244685b0b956d33f593ccdcd7346fa1d8d7b98a302fd35b8a2
C1CCNC1
O=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5].[#7:6]-[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10]>>[#7:6]-[C:7]-[C:8](-[N;H0;D2;+0:9]=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5])-[C:10]
null
[]
null
null
1
HOUR
12.1 g (0.1 mol) of 71% strength pivalaldehyde, initially introduced into the reaction vessel and 8.6 g (0.1 mol) of 3-aminopyrrolidine are added dropwise at 20° C. to 30° C., while cooling in a water bath. The mixture is subsequently stirred at room temperature for 1 hour and is then distilled. Yield: 13.5 g (85% of t...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Substituted imine
null
null
C1CCNC1
HO-
null
null
1
CC(C)(C)C=O.NC1CCNC1>>CC(C)(C)C=NC1CCNC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-260f7eb07f4b4633acca339360195729
C.c1ccc(CNC2CCN(Cc3ccccc3)C2)cc1>>CC(C)(C)C=NC1CCNC1
C(C1=CC=CC=C1)N1CC(CC1)NCC1=CC=CC=C1.C>>CC(C=NC1CNCC1)(C)C
[CH4:1].c1ccc(C[N:10]2[CH2:9][CH2:8][CH:7]([NH:6][CH2:5][c:2]3[cH:3]ccc[cH:4]3)[CH2:11]2)cc1>>[CH3:1][C:2]([CH3:3])([CH3:4])[CH:5]=[N:6][CH:7]1[CH2:8][CH2:9][NH:10][CH2:11]1
C.c1ccc(CNC2CCN(Cc3ccccc3)C2)cc1
CC(C)(C)C=NC1CCNC1
null
[Pd]
CO
C-C Coupling
OtherReaction
008045eaa7bd2f16a9005ebf9e735a9e3e3fc5bf26dd5ea812e145f5407c5bbc
d7a8bf426327cb09b51ad349220aebac5ec6b853324d0e830c43b4d7f3b2056c
C1CCNC1
C(-[N;H0;D3;+0:1]1-[C:2]-[C:3](-[NH;D2;+0:4]-[CH2;D2;+0:5]-[c;H0;D3;+0:6]2:[cH;D2;+0:7]:c:c:c:[cH;D2;+0:8]:2)-[C:9]-[C:10]-1)-c1:c:c:c:c:c:1.[CH4;D0;+0:11]>>[CH3;D1;+0:11]-[C;H0;D4;+0:6](-[CH3;D1;+0:7])(-[CH3;D1;+0:8])-[CH;D2;+0:5]=[N;H0;D2;+0:4]-[C:3]1-[C:2]-[NH;D2;+0:1]-[C:10]-[C:9]-1
58
[{"value": 58.0, "product": "CC(C=NC1CNCC1)(C)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
36.8 g (0.138 mol) of 1-benzyl-3-benzylaminopyrrolidine are hydrogenated in 160 ml of methanol over 5 g of 5% strength palladium on active charcoal at 130° C. under a hydrogen pressure of 100 bar for 10 hours. The catalyst is filtered off and 16.6 g (0.138 mol ) of 71% strength pivalaldehyde are added to the filtrate, ...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Tertiary amine
Substituted imine.Secondary amine
c1ccccc1.C1CC[NH]C1.c1ccccc1
C1CCNC1
C1CCNC1
Other
[Pd].CO
null
null
C.c1ccc(CNC2CCN(Cc3ccccc3)C2)cc1>[Pd].CO>CC(C)(C)C=NC1CCNC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2630f868c1ae4906a64306843a19fa7f
CC(C)(C)C=O.NCC1CCNC1>>CC(C)(C)C=NCC1CCNC1
NCC1CNCC1.C(C(C)(C)C)=O>>CC(C=NCC1CNCC1)(C)C
O=[CH:5][C:2]([CH3:1])([CH3:3])[CH3:4].[NH2:6][CH2:7][CH:8]1[CH2:9][CH2:10][NH:11][CH2:12]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[CH:5]=[N:6][CH2:7][CH:8]1[CH2:9][CH2:10][NH:11][CH2:12]1
CC(C)(C)C=O.NCC1CCNC1
CC(C)(C)C=NCC1CCNC1
null
null
CO
Heteroatom Alkylation and Arylation
Addition of primary amines to aldehydes/thiocarbonyls
d409dfd3247abb6c1b1364aec380d25720f21e374fd2124063f2d2ce54d31c4f
9b341044a5a058244685b0b956d33f593ccdcd7346fa1d8d7b98a302fd35b8a2
C1CCNC1
O=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[N;H0;D2;+0:8]=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5]
null
[]
null
null
1
HOUR
2.0 g (20 mmol) of 3-aminomethyl-pyrrolidine are initially introduced into 10 ml of methanol, and 1.8 g (22 mmol) of 97% strength pivalaldehyde are added dropwise at room temperature, after which the internal temperature rises to 30° C. The mixture is subsequently stirred for 1 hour and then concentrated, and the resid...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Substituted imine
null
null
C1CCNC1
HO-
CO
null
1
CC(C)(C)C=O.NCC1CCNC1>CO>CC(C)(C)C=NCC1CCNC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-13330458b3c94465aa5dc67623f8b399
CS(=O)(=O)Cl.N.O=C(c1ccccc1)N1CC=CC1>>CS[C@@H]1CN(C(=O)c2ccccc2)C[C@H]1N
C([O-])([O-])=O.[Na+].[Na+].C(C1=CC=CC=C1)(=O)N1CC=CC1.CS(=O)(=O)Cl.N>>C(C1=CC=CC=C1)(=O)N1C[C@H]([C@@H](C1)SC)N
O=[S:2](=O)(Cl)[CH3:1].[NH3:16].[CH:3]1=[CH:15][CH2:14][N:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[CH2:4]1>>[CH3:1][S:2][C@@H:3]1[CH2:4][N:5]([C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[CH2:14][C@H:15]1[NH2:16]
CS(=O)(=O)Cl.N.O=C(c1ccccc1)N1CC=CC1
CS[C@@H]1CN(C(=O)c2ccccc2)C[C@H]1N
null
null
C(Cl)Cl.O.O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
628efffe4c4c45177dcbdedc5f5da0b6ed938771e8cd394fe86b6a42018453f5
c76f65538900d68fb447211fd1a77e66f67bd4754b2f351d4c3fdeffd1b6f063
O=C(c1ccccc1)N1CCCC1
Cl-[S;H0;D4;+0:1](=O)(=O)-[C;D1;H3:2].[NH3;D0;+0:3].[O;D1;H0:4]=[C:5]-[#7:6]1-[C:7]-[CH;D2;+0:8]=[CH;D2;+0:9]-[C:10]-1>>[C;D1;H3:2]-[S;H0;D2;+0:1]-[C@@H;D3;+0:9]1-[C:10]-[#7:6](-[C:5]=[O;D1;H0:4])-[C:7]-[C@H;D3;+0:8]-1-[NH2;D1;+0:3]
null
[]
null
null
16
HOUR
41.5 g (0.24 mol) of 1-benzoyl-2,5-dihydropyrrole are initially introduced into 240 ml of methylene chloride, and 24.8 g (0.3 mol) of methanesulphonyl chloride are added dropwise at 0° C. The mixture is subsequently stirred at room temperature for 16 hours, the solvent is then stripped off under 8 mbar and the residue ...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Primary amine.Monosulfide
C1=CC[NH]C1
C1CC[NH]C1
C1CC[NH]C1.c1ccccc1
HCl
C(Cl)Cl.O.O1CCCC1
null
16
CS(=O)(=O)Cl.N.O=C(c1ccccc1)N1CC=CC1>C(Cl)Cl.O.O1CCCC1>CS[C@@H]1CN(C(=O)c2ccccc2)C[C@H]1N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e8dac3a3e84b49d4bd31f050b2729740
CC(C)(C)C=O.CS[C@@H]1CNC[C@H]1N>>CS[C@@H]1CNC[C@H]1N=CC(C)(C)C
N[C@@H]1CNC[C@H]1SC.C(C(C)(C)C)=O>>CC(C=N[C@@H]1CNC[C@H]1SC)(C)C
O=[CH:9][C:10]([CH3:11])([CH3:12])[CH3:13].[CH3:1][S:2][C@@H:3]1[CH2:4][NH:5][CH2:6][C@H:7]1[NH2:8]>>[CH3:1][S:2][C@@H:3]1[CH2:4][NH:5][CH2:6][C@H:7]1[N:8]=[CH:9][C:10]([CH3:11])([CH3:12])[CH3:13]
CC(C)(C)C=O.CS[C@@H]1CNC[C@H]1N
CS[C@@H]1CNC[C@H]1N=CC(C)(C)C
null
null
CO
Heteroatom Alkylation and Arylation
Addition of primary amines to aldehydes/thiocarbonyls
d409dfd3247abb6c1b1364aec380d25720f21e374fd2124063f2d2ce54d31c4f
9b341044a5a058244685b0b956d33f593ccdcd7346fa1d8d7b98a302fd35b8a2
C1CCNC1
O=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5].[#7:6]-[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10]>>[#7:6]-[C:7]-[C:8](-[N;H0;D2;+0:9]=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[C;D1;H3:5])-[C:10]
null
[]
null
null
30
MINUTE
1.32 g (10 mmol) of trans-3-amino-4-methylthio-pyrrolidine are initially introduced into 5 ml of methanol, and 1.23 ml (11 mmol) of 97% strength pivalaldehyde are added dropwise, after which the temperature rises from 25° to 36° C. The mixture is subsequently stirred for a further 30 minutes, without cooling, the batch...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Substituted imine
null
null
C1CCNC1
HO-
CO
null
0.5
CC(C)(C)C=O.CS[C@@H]1CNC[C@H]1N>CO>CS[C@@H]1CNC[C@H]1N=CC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-182cab8e991e46b5ad9d638c603333a5
CC(C)(C)C=O.NC1CCNC1.O=C(O)C1=CN(C2CC2)c2c(cc(F)c(F)c2Cl)C1>>NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1
C(C(C)(C)C)=O.NC1CNCC1.ClC=1C(=C(C=C2CC(=CN(C12)C1CC1)C(=O)O)F)F.N12CCN(CC1)CC2.CC(C=NC1CNCC1)(C)C>>NC1CN(CC1)C1=C(C=C2C(C(=CN(C2=C1Cl)C1CC1)C(=O)O)=O)F
CC(C)(C)C=[O:12].[NH2:1][CH:2]1[CH2:3][CH2:4][NH:5][CH2:25]1.F[c:6]1[c:7]([F:8])[cH:9][c:10]2[c:22]([c:23]1[Cl:24])[N:18]([CH:19]1[CH2:20][CH2:21]1)[CH:17]=[C:13]([C:14](=[O:15])[OH:16])[CH2:11]2>>[NH2:1][CH:2]1[CH2:3][CH2:4][N:5]([c:6]2[c:7]([F:8])[cH:9][c:10]3[c:11](=[O:12])[c:13]([C:14](=[O:15])[OH:16])[cH:17][n:18]...
CC(C)(C)C=O.NC1CCNC1.O=C(O)C1=CN(C2CC2)c2c(cc(F)c(F)c2Cl)C1
NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1
null
null
C(C)#N.CN(C=O)C
Protection
OtherReaction
52e09cc305f93f960459b1e9edab534f38d5b3d20558176aff439762f0537811
92145626fd4a33c3d445ebad61a15684a0400f49184758a2a80d7bdbd8a8df7f
O=c1ccn(C2CC2)c2cc(N3CCCC3)ccc12
C-C(-C)(-C)-C=[O;H0;D1;+0:1].F-[c;H0;D3;+0:2]1:[c:3](-[Cl;D1;H0:4]):[c:5]2:[c:6](:[c:7]:[c:8]:1-[F;D1;H0:9])-[CH2;D2;+0:10]-[C;H0;D3;+0:11](-[C:12](=[O;D1;H0:13])-[O;D1;H1:14])=[CH;D2;+0:15]-[N;H0;D3;+0:16]-2-[C:17]1-[C:18]-[C:19]-1.[C:20]1-[C:21]-[C:22]-[C:23]-[NH;D2;+0:24]-1>>[Cl;D1;H0:4]-[c:3]1:[c:5]2:[c:6](:[c:7]:[...
null
[]
null
null
1
HOUR
0.95 g (11 mmol) of pivalaldehyde are added dropwise to a solution of 0.86 g (10 mmol) of 3-aminopyrrolidine in 10 ml of acetonitrile at room temperature in the course of 5 minutes, during which the temperature rises from 22.5° C. to 27.5° C. The mixture is subsequently stirred for 1 hour and a virtually complete conve...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Aldehyde.Secondary amine
Tertiary amine
C1CCNC1.C1=C[NH]c2ccccc2C1
C1CC[NH]C1.c1ccc2ncccc2c1
C1CC[NH]C1.c1ccc2ncccc2c1.C1CC1
HF
C(C)#N.CN(C=O)C
null
1
CC(C)(C)C=O.NC1CCNC1.O=C(O)C1=CN(C2CC2)c2c(cc(F)c(F)c2Cl)C1>C(C)#N.CN(C=O)C>NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-32bc0b3ba19f4eee8fecd0b31789e6b2
CCOC(=O)CN1Cc2ccccc2C[C@H](N2C(=O)c3ccccc3C2=O)C1=O.O=C(Cl)OCc1ccccc1>>CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O
C(C)N(CC)CC.C(C1=CC=CC=C1)OC(=O)Cl.C1(C=2C(C(N1[C@@H]1C(N(CC3=C(C1)C=CC=C3)CC(=O)OCC)=O)=O)=CC=CC2)=O.C(C)O>>C1(=CC=CC=C1)COC(=O)N[C@@H]1C(N(CC2=C(C1)C=CC=C2)CC(=O)OCC)=O
O=C1c2ccccc2C(=O)[N:17]1[C@H:16]1[CH2:15][c:14]2[c:9]([cH:10][cH:11][cH:12][cH:13]2)[CH2:8][N:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:28]1=[O:29].Cl[C:18](=[O:19])[O:20][CH2:21][c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]1[CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]...
CCOC(=O)CN1Cc2ccccc2C[C@H](N2C(=O)c3ccccc3C2=O)C1=O.O=C(Cl)OCc1ccccc1
CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O
null
null
C1(=CC=CC=C1)C.C(C)(=O)OCC.O.NN
Protection
OtherReaction
fe3102b6b408f3d3825eb2b8e397463241cc48fe0961b1edbc9ae90e981158d6
1040b538a38b728279e7919c87da3a9c1d00e9f692e311a76ca8b5e574dd287d
O=C(N[C@H]1Cc2ccccc2CNC1=O)OCc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].O=C1-[N;H0;D3;+0:5](-[C:6](-[C:7])-[C:8](=[O;D1;H0:9])-[#7:10](-[C:11]-[C:12](-[#8:13])=[O;D1;H0:14])-[C:15])-C(=O)-c2:c:c:c:c:c:2-1>>[#8:13]-[C:12](=[O;D1;H0:14])-[C:11]-[#7:10](-[C:15])-[C:8](=[O;D1;H0:9])-[C:6](-[NH;D2;+0:5]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-[C:7...
null
[]
0
CELSIUS
2
HOUR
A solution of (S)-1,3,4,5-tetrahydro-4-phthalimido-3-oxo-2H-2-benzazepine-2-acetic acid, ethyl ester (1.67 g., 4.26 mmol.) in 1.0M hydrazine hydrate in ethanol (9.0 ml., 9.0 mmol.) was stirred at room temperature under argon for 36 hours. The mixture was diluted with an equal volume of ethyl acetate, filtered and filtr...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Substituted dicarboximide
Carbamic ester
c1ccc2c(c1)C[NH]C2
null
c1ccc2c(c1)CCC[NH]C2.c1ccccc1
HCl
C1(=CC=CC=C1)C.C(C)(=O)OCC.O.NN
0
2
CCOC(=O)CN1Cc2ccccc2C[C@H](N2C(=O)c3ccccc3C2=O)C1=O.O=C(Cl)OCc1ccccc1>C1(=CC=CC=C1)C.C(C)(=O)OCC.O.NN>CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d232c1adede245b1b40453d6829ded7a
CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O>>CCOC(=O)CN1Cc2ccccc2C[C@H](N)C1=O
C(Cl)(Cl)Cl.CO.C1(=CC=CC=C1)COC(=O)N[C@@H]1C(N(CC2=C(C1)C=CC=C2)CC(=O)OCC)=O.C(Cl)Cl>>N[C@@H]1C(N(CC2=C(C1)C=CC=C2)CC(=O)OCC)=O
O=C(OCc1ccccc1)[NH:17][C@H:16]1[CH2:15][c:14]2[c:9]([cH:10][cH:11][cH:12][cH:13]2)[CH2:8][N:7]([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:18]1=[O:19]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]1[CH2:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[CH2:15][C@H:16]([NH2:17])[C:18]1=[O:19]
CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O
CCOC(=O)CN1Cc2ccccc2C[C@H](N)C1=O
null
[OH-].[OH-].[Pd+2]
C(C)O
Reduction
Hydrogenolysis of amides/imides/carbamates
087b6600ba91d3df931fe6979f2445c192cbfd59e04fd2d8a10f7c7573ac669f
4e549866ec1acadec4c84aaf8495992a28ec78d8ea5ef1b9f44dd843b0dcb7d4
O=C1CCc2ccccc2CN1
O=C(-O-C-c1:c:c:c:c:c:1)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#7:6](-[C:7]-[C:8](-[#8:9])=[O;D1;H0:10])-[C:11]>>[#8:9]-[C:8](=[O;D1;H0:10])-[C:7]-[#7:6](-[C:11])-[C:4](=[O;D1;H0:5])-[C:2](-[NH2;D1;+0:1])-[C:3]
null
[]
null
null
2
HOUR
20% Palladium hydroxide/carbon catalyst was added to a solution of (S)-1,3,4,5-tetrahydro-4-[[(phenylmethoxy)carbonyl]amino]-3-oxo-2H-2-benzazepine-2-acetic acid, ethyl ester (1.037 g., 2.62 mmole) in absolute ethanol (20 ml.) and the resulting suspension was stirred under a hydrogen atmosphere (balloon) for 2 hours. T...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether
Primary amine
c1ccccc1
null
c1ccc2c(c1)CCC[NH]C2
HO-
[OH-].[OH-].[Pd+2].C(C)O
null
2
CCOC(=O)CN1Cc2ccccc2C[C@H](NC(=O)OCc2ccccc2)C1=O>[OH-].[OH-].[Pd+2].C(C)O>CCOC(=O)CN1Cc2ccccc2C[C@H](N)C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a5a96d1b986849b2b488b84cd2b4e308
CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)O.CI>>COC(=O)[C@H](CCCCNC(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
CI.C([O-])([O-])=O.[Cs+].[Cs+].N#N.CC(C)(OC(=O)N[C@@H](CCCCNC(=O)OCC1=CC=CC=C1)C(=O)O)C.O.CO>>N#N.CC(C)(OC(=O)N[C@@H](CCCCNC(=O)OCC1=CC=CC=C1)C(=O)OC)C
[OH:2][C:3](=[O:4])[C@H:5]([CH2:6][CH2:7][CH2:8][CH2:9][NH:10][C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[NH:21][C:22](=[O:23])[O:24][C:25]([CH3:26])([CH3:27])[CH3:28].I[CH3:1]>>[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH2:6][CH2:7][CH2:8][CH2:9][NH:10][C:11](=[O:12])[O:13][CH2:14][c:15]1[cH:16][...
CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)O.CI
COC(=O)[C@H](CCCCNC(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
null
null
C(C)(=O)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
9474aa79a2adc7353c0c02444ca598a6f486ecdd7ed5edb9ae0645721ee50389
badd4f82161bb0ee7acffd023ea4caae5d036bce7065c10ab0a06e83a6a6f119
c1ccccc1
I-[CH3;D1;+0:1].[C:2]-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]>>[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH3;D1;+0:1]
null
[]
null
null
5
MINUTE
Cesium carbonate (4.28 g., 13.1 moles) was added to a mixture of N2 -[(1,1-dimethylethoxy)carbonyl]-N6 -[(phenylmethoxy)carbonyl]-L-lysine (10 g., 26.3 moles) and 20% water-methanol (60 ml.). The solution became homogeneous within 5 minutes so the solvent was stripped and the residual water removed azeotropically with ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1ccccc1
HI
C(C)(=O)OCC
null
0.083333
CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)O.CI>C(C)(=O)OCC>COC(=O)[C@H](CCCCNC(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8042b51b648746afafc70ab52ab4a4bc
CC(C)(C)OC(=O)N[C@@H](CO)C(=O)O.O=[N+]([O-])c1ccccc1F>>CC(C)(C)OC(=O)N[C@@H](COc1ccccc1[N+](=O)[O-])C(=O)O
[H-].[Na+].FC1=C(C=CC=C1)[N+](=O)[O-].C(Cl)Cl.CC(C)(OC(=O)N[C@@H](CO)C(=O)O)C>>CC(C)(OC(=O)N[C@@H](COC1=C(C=CC=C1)[N+](=O)[O-])C(=O)O)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C@@H:9]([CH2:10][OH:11])[C:21](=[O:22])[OH:23].F[c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[N+:18](=[O:19])[O-:20]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C@@H:9]([CH2:10][O:11][c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[N+:18](=[O:19])[O-:20])[C:21](...
CC(C)(C)OC(=O)N[C@@H](CO)C(=O)O.O=[N+]([O-])c1ccccc1F
CC(C)(C)OC(=O)N[C@@H](COc1ccccc1[N+](=O)[O-])C(=O)O
null
null
CN(C=O)C.CO.C(C)(=O)O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[O;D1;H0:7]=[C:8](-[O;D1;H1:9])-[C:10]-[C:11]-[OH;D1;+0:12]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[O;H0;D2;+0:12]-[C:11]-[C:10]-[C:8](=[O;D1;H0:7])-[O;D1;H1:9]):[c:2]:[c:3]
null
[]
null
null
null
null
A solution of N-[(1,1-dimethylethoxy)carbonyl]-L-serine (24.3 g., 0.118 mole) in dry dimethylformamide (25 ml.) was added dropwise over a period of 1.0 hour to a cooled (0°, ice-salt bath) suspension of 60% sodium hydride (10.1 g., 0.25 mole) in dry dimethylformamide (200 ml.) and stirring was continued at 0° until the...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1
HF
CN(C=O)C.CO.C(C)(=O)O
null
null
CC(C)(C)OC(=O)N[C@@H](CO)C(=O)O.O=[N+]([O-])c1ccccc1F>CN(C=O)C.CO.C(C)(=O)O>CC(C)(C)OC(=O)N[C@@H](COc1ccccc1[N+](=O)[O-])C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d33b6c72571d4550bdc29dc44648e499
CCOC(=O)CBr.O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1>>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OCc2ccccc2)CSC[C@H]1c1ccccc1
[OH-].[K+].BrCC(=O)OCC.BrCC(=O)OCC.C1(=CC=CC=C1)[C@@H]1CSC[C@@H](C(N1)=O)NC(=O)OCC1=CC=CC=C1>>O=C1N([C@@H](CSC[C@@H]1NC(=O)OCC1=CC=CC=C1)C1=CC=CC=C1)CC(=O)OCC
Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[NH:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O:14][CH2:15][c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[CH2:22][S:23][CH2:24][C@H:25]1[c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O...
CCOC(=O)CBr.O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1
CCOC(=O)CN1C(=O)[C@@H](NC(=O)OCc2ccccc2)CSC[C@H]1c1ccccc1
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
C(C)(=O)OCC.O1CCCC1.S(=O)(=O)([O-])[O-].[Mg+2]
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
448d2a9bdfd31665de19d5d708bf0615b1c0dce8080afe65ff0e19354a21937a
933a6f1013d44497c9c5902b73c24fbdc7813d20b886bdbc4c670d5b43ca2182
O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[#16:6]-[C:7]-[C:8](-[c:9])-[NH;D2;+0:10]-[C:11](=[O;D1;H0:12])-[C:13]>>[#16:6]-[C:7]-[C:8](-[c:9])-[N;H0;D3;+0:10](-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:11](=[O;D1;H0:12])-[C:13]
null
[]
null
null
null
null
A solution of (3R-cis)-tetrahydro-3-phenyl-6-[[(phenylmethoxy)carbonyl]amino]-1,4-thiazepine-5(4H)-one (1.16 g., 3.25 mmol) [prepared as described by Yanagisawa et al., J. Med. Chem., Vol. 30, p. 1984-1991 (1987)] in distilled tetrahydrofuran (30 ml.), under an atmosphere of argon, was cooled to 0° C. and treated with ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Secondary amide
Ester.Tertiary amide
C1CNCCSC1
C1C[NH]CCSC1
C1C[NH]CCSC1.c1ccccc1.c1ccccc1
HBr
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C)(=O)OCC.O1CCCC1.S(=O)(=O)([O-])[O-].[Mg+2]
null
null
CCOC(=O)CBr.O=C(N[C@H]1CSC[C@@H](c2ccccc2)NC1=O)OCc1ccccc1>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C)(=O)OCC.O1CCCC1.S(=O)(=O)([O-])[O-].[Mg+2]>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OCc2ccccc2)CSC[C@H]1c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c5d05c1fc29046a898bb31a5a6831fa6
N[C@@H](Cc1ccccc1)C(=O)O.[Br-]>>O=C(O)[C@@H](Br)Cc1ccccc1
N(=O)[O-].[Na+].C1(=CC=CC=C1)C.N[C@@H](CC1=CC=CC=C1)C(=O)O.[Br-].[K+]>>Br[C@H](C(=O)O)CC1=CC=CC=C1
N[C@H:4]([C:2](=[O:1])[OH:3])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1.[Br-:5]>>[O:1]=[C:2]([OH:3])[C@@H:4]([Br:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1
N[C@@H](Cc1ccccc1)C(=O)O.[Br-]
O=C(O)[C@@H](Br)Cc1ccccc1
null
null
C(C)(=O)O.S(O)(O)(=O)=O
Functional Group Interconversion
OtherReaction
117344ae409beae3589a30d5997369184f62edb887830bd6b795e8dfdf82920d
9544d3c5449a12cdcbad58c02e82937c94837ec7c67e3baf5ab21c8ae3b17e42
c1ccccc1
N-[C@@H;D3;+0:1](-[C:2]-[c:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[Br-;H0;D0:7]>>[Br;H0;D1;+0:7]-[C@@H;D3;+0:1](-[C:2]-[c:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6]
null
[]
null
null
1
HOUR
A solution of L-phenylalanine (30.0 g., 0.175 mole) and potassium bromide (73.5 g., 0.618 mole) in 2.5N sulfuric acid (365 ml.) was cooled down to 0° (ice-salt bath) and treated portionwise with sodium nitrite (19.3 g., 0.28 mole) over a period of 1.0 hour. Stirring was continued for 1.0 hour at 0° and at room temperat...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Secondary halide
null
null
c1ccccc1
Other
C(C)(=O)O.S(O)(O)(=O)=O
null
1
N[C@@H](Cc1ccccc1)C(=O)O.[Br-]>C(C)(=O)O.S(O)(O)(=O)=O>O=C(O)[C@@H](Br)Cc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-71de4245449c4d6b882f5e5c1262b960
C[C@@H](O)[C@H](NC(=O)OC(C)(C)C)C(=O)O.O=[N+]([O-])c1ccccc1F>>C[C@@H](Oc1ccccc1[N+](=O)[O-])[C@H](NC(=O)OC(C)(C)C)C(=O)O
CC(C)(OC(=O)N[C@@H]([C@H](O)C)C(=O)O)C.[H-].[Na+].FC1=C(C=CC=C1)[N+](=O)[O-]>>CC(C)(OC(=O)N[C@@H]([C@H](OC1=C(C=CC=C1)[N+](=O)[O-])C)C(=O)O)C
[CH3:1][C@@H:2]([OH:3])[C@H:13]([NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21])[C:22](=[O:23])[OH:24].F[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[N+:10](=[O:11])[O-:12]>>[CH3:1][C@@H:2]([O:3][c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[N+:10](=[O:11])[O-:12])[C@H:13]([NH:14][C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:...
C[C@@H](O)[C@H](NC(=O)OC(C)(C)C)C(=O)O.O=[N+]([O-])c1ccccc1F
C[C@@H](Oc1ccccc1[N+](=O)[O-])[C@H](NC(=O)OC(C)(C)C)C(=O)O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
fc6e1b465ae75176f3fa192a660d0d622bdf538cea285b0e2b9dc00b273004b2
1f70dbbaebc288b3a5d3f37803812d9d22b151831cd4b8351080508554b19875
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[C;D1;H3:7]-[C:8](-[OH;D1;+0:9])-[C:10]-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[C:8](-[C;D1;H3:7])-[C:10]-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]):[c:2]:[c:3]
null
[]
0
CELSIUS
null
null
A solution of N-[(1,1-dimethylethoxy)carbonyl]-L-threonine (5.02 g., 22.9 mmol.) in dry dimethylformamide (10 ml.) was added dropwise over a period of 30 minutes to a cooled (0° C.) suspension of 60% sodium hydride (1.93 g., 48.25 mmol., 2.11 eq.) in dry dimethylformamide (40 ml.). The reaction was stirred at 0° C. unt...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1
HF
CN(C=O)C
0
null
C[C@@H](O)[C@H](NC(=O)OC(C)(C)C)C(=O)O.O=[N+]([O-])c1ccccc1F>CN(C=O)C>C[C@@H](Oc1ccccc1[N+](=O)[O-])[C@H](NC(=O)OC(C)(C)C)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fa2dad0a7d324e3da4abe3023c156072
CO.N[C@@H](CCCCO)C(=O)O>>COC(=O)[C@@H](N)CCCCO
N[C@H](C(=O)O)CCCCO.Cl.CO>>Cl.N[C@H](C(=O)OC)CCCCO
[CH3:1][OH:2].O[C:3](=[O:4])[C@@H:5]([NH2:6])[CH2:7][CH2:8][CH2:9][CH2:10][OH:11]>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([NH2:6])[CH2:7][CH2:8][CH2:9][CH2:10][OH:11]
CO.N[C@@H](CCCCO)C(=O)O
COC(=O)[C@@H](N)CCCCO
null
null
null
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
null
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[N;D1;H2:5].[C;D1;H3:6]-[OH;D1;+0:7]>>[C:4]-[C:3](-[N;D1;H2:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:7]-[C;D1;H3:6]
null
[]
null
null
2.5
HOUR
A slurry of (S)-2-amino-6-hydroxyhexanoic acid (2.42 g., 16.4 mmole) in dry methanol (60 ml.) was treated with gaseous hydrogen chloride until the mixture began to reflux. The homogeneous solution was then stirred at room temperature for 2.5 hours. The solvent was stripped and the residue azeotroped three times with to...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
null
HO-
null
null
2.5
CO.N[C@@H](CCCCO)C(=O)O>>COC(=O)[C@@H](N)CCCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-32b402f60fe74c78b310c537e44ff646
CCOC(=O)CN.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>>CCCC[C@@H](C(=O)NCC(=O)OCC)N1C(=O)c2ccccc2C1=O
Cl.NCC(=O)OCC.CN1CCOCC1.C1(C=2C(C(N1[C@H](C(=O)O)CCCCO)=O)=CC=CC2)=O.OC1=CC=CC=2NN=NC21>>C1(C=2C(C(N1[C@H](C(=O)NCC(=O)OCC)CCCC)=O)=CC=CC2)=O
[NH2:8][CH2:9][C:10](=[O:11])[O:12][CH2:13][CH3:14].O[CH2:1][CH2:2][CH2:3][CH2:4][C@@H:5]([C:6](O)=[O:7])[N:15]1[C:16](=[O:17])[c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[C:24]1=[O:25]>>[CH3:1][CH2:2][CH2:3][CH2:4][C@@H:5]([C:6](=[O:7])[NH:8][CH2:9][C:10](=[O:11])[O:12][CH2:13][CH3:14])[N:15]1[C:16](=[O:17])[c:18]2[cH:1...
CCOC(=O)CN.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
CCCC[C@@H](C(=O)NCC(=O)OCC)N1C(=O)c2ccccc2C1=O
null
null
CN(C=O)C
Acylation
OtherReaction
0417a24920227ec1bd95566b2c81b0ce9679eff3bca069621b0123bac13830c8
a1b92777bbff0323f68374ba2bb35d2b7447e9327d1247846bdecf2f4bf4b05b
O=C1NC(=O)c2ccccc21
O-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4]-[C:5](-[#7:6](-[C:7]=[O;D1;H0:8])-[C:9]=[O;D1;H0:10])-[C;H0;D3;+0:11](-O)=[O;D1;H0:12].[C:13]-[#8:14]-[C:15](=[O;D1;H0:16])-[C:17]-[NH2;D1;+0:18]>>[C:13]-[#8:14]-[C:15](=[O;D1;H0:16])-[C:17]-[NH;D2;+0:18]-[C;H0;D3;+0:11](=[O;D1;H0:12])-[C:5](-[C:4]-[C:3]-[C:2]-[CH3;D1;+0:1])-[#7:6](-[C...
null
[]
null
null
5
MINUTE
A slurry of glycine, ethyl ester, hydrochloride salt (2.718 g, 19.5 mmol.) in dimethylformamide (36 ml.) was treated with 4-methyl morpholine (2.60 ml., 2.39 g., 23.6 mmol.) and stirred at room temperature for 5 minutes. The mixture was then treated with (S)-2-phthalimido-6-hydroxyhexanoic acid (4.50 g., 16.2 mmol.) an...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol.Primary amine
Secondary amide
null
null
c1ccc2c(c1)C[NH]C2
HO-
CN(C=O)C
null
0.083333
CCOC(=O)CN.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>CN(C=O)C>CCCC[C@@H](C(=O)NCC(=O)OCC)N1C(=O)c2ccccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-75d6830239304b61acc836550d1f3a66
C=CC(=O)OCC.[N-]=[N+]=NC1CCc2ccccc2NC1=O>>CCOC(=O)CCN1C(=O)C(N=[N+]=[N-])CCc2ccccc21
N(=[N+]=[N-])C1C(NC2=C(CC1)C=CC=C2)=O.C(C=C)(=O)OCC.C(C)(C)(C)O.[K]>>N(=[N+]=[N-])C1C(N(C2=C(CC1)C=CC=C2)CCC(=O)OCC)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]=[CH2:7].[NH:8]1[C:9](=[O:10])[CH:11]([N:12]=[N+:13]=[N-:14])[CH2:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][CH2:7][N:8]1[C:9](=[O:10])[CH:11]([N:12]=[N+:13]=[N-:14])[CH2:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]21
C=CC(=O)OCC.[N-]=[N+]=NC1CCc2ccccc2NC1=O
CCOC(=O)CCN1C(=O)C(N=[N+]=[N-])CCc2ccccc21
null
null
O1CCCC1.C(C)(C)(C)O.O1CCCC1
Heteroatom Alkylation and Arylation
aza-Michael addition secondary
ba7c4bd71d9dac9254c12d0209ebbe315a4f74699e256502917bd8de51885203
91e54cd6e65f2c08b5c1a8b4338c7ceefc90d4eb91eb55b2313d1887e8793e60
O=C1CCCc2ccccc2N1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH;D2;+0:5]=[CH2;D1;+0:6].[C:7]-[C:8](=[O;D1;H0:9])-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13]>>[C:7]-[C:8](=[O;D1;H0:9])-[N;H0;D3;+0:10](-[CH2;D2;+0:6]-[CH2;D2;+0:5]-[C:3](=[O;D1;H0:4])-[#8:2]-[C:1])-[c:11](:[c:12]):[c:13]
null
[]
null
null
null
null
A solution of 3-azido-1,3,4,5-tetrahydro-2H-1-benzazepine-2-one [prepared as described by Watthey et al., J. Med. Chem., 28, p. 1511-15156 (1985)] in tetrahydrofuran/tert-butanol was cooled to 0° C. and treated with ethyl acrylate and 1N tert-butanol, potassium salt/tetrahydrofuran according to the procedure of Example...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amide.Vinyl
Ester.Tertiary amide
c1ccc2c(c1)CCCCN2
c1ccc2c(c1)CCCC[NH]2
c1ccc2c(c1)CCCC[NH]2
null
O1CCCC1.C(C)(C)(C)O.O1CCCC1
null
null
C=CC(=O)OCC.[N-]=[N+]=NC1CCc2ccccc2NC1=O>O1CCCC1.C(C)(C)(C)O.O1CCCC1>CCOC(=O)CCN1C(=O)C(N=[N+]=[N-])CCc2ccccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a1ba75f5f74140a4b9b975cdffd4a9e5
CC(C)(C)OC(=O)NN.CCOC(=O)CBr>>CCOC(=O)CNNC(=O)OC(C)(C)C
C(C)N(CC)CC.C(C)N(CC)CC.BrCC(=O)OCC.C(C)N(CC)CC.N(N)C(=O)OC(C)(C)C.BrCC(=O)OCC.BrCC(=O)OCC>>CC(C)(OC(=O)NNCC(=O)OCC)C
[NH2:7][NH:8][C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15].Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH:7][NH:8][C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15]
CC(C)(C)OC(=O)NN.CCOC(=O)CBr
CCOC(=O)CNNC(=O)OC(C)(C)C
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
a10280ad95ed368c75fdf1d65f9c7b02199bd814b62740ab81803f6da82dc483
150ef5d6000fad15b6e5d9a7d488fe3ba905820f4205bfb36d0ee312b4df76ec
null
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C;D1;H3:6]-[C:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[#8:10]-[C:11](=[O;D1;H0:12])-[#7:13]-[NH2;D1;+0:14]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[NH;D2;+0:14]-[#7:13]-[C:11](=[O;D1;H0:12])-[#8:10]-[C:7](-[C;D1;H3:6])(-[C;D1;H3:8])-[C;D1;H3:9]
null
[]
null
null
null
null
Triethylamine (13.94 ml., 0.1 mol.) was added to a solution of hydrazine carboxylic acid, 1,1-dimethylethyl ester (13.216 g., 0.1 mole) in benzene (100 ml.), followed by the addition of ethyl bromoacetate (11.09 ml., 0.1 mol.). The reaction mixture was refluxed (oil bath, 95°-100° C.) for 14 hours, after which triethyl...
10.6084/m9.figshare.5104873.v1
null
Acylhydrazine.Primary halide
Acylhydrazine.Ester
null
null
null
HBr
C1=CC=CC=C1
null
null
CC(C)(C)OC(=O)NN.CCOC(=O)CBr>C1=CC=CC=C1>CCOC(=O)CNNC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8692cdf1384947d9936fad43dc8bd8f6
CCCC[C@@H](N)C(=O)O.[Br-]>>CCCC[C@H](Br)C(=O)O
[Br-].[K+].N[C@H](CCCC)C(=O)O.N(=O)[O-].[Na+]>>Br[C@H](C(=O)O)CCCC
N[C@H:5]([CH2:4][CH2:3][CH2:2][CH3:1])[C:7](=[O:8])[OH:9].[Br-:6]>>[CH3:1][CH2:2][CH2:3][CH2:4][C@H:5]([Br:6])[C:7](=[O:8])[OH:9]
CCCC[C@@H](N)C(=O)O.[Br-]
CCCC[C@H](Br)C(=O)O
null
null
S(O)(O)(=O)=O
Functional Group Interconversion
OtherReaction
117344ae409beae3589a30d5997369184f62edb887830bd6b795e8dfdf82920d
9544d3c5449a12cdcbad58c02e82937c94837ec7c67e3baf5ab21c8ae3b17e42
null
N-[C@H;D3;+0:1](-[C:2]-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[Br-;H0;D0:7]>>[Br;H0;D1;+0:7]-[C@@H;D3;+0:1](-[C:2]-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6]
null
[]
-10
CELSIUS
1
HOUR
Potassium bromide (15.9 g., 133 mmol.) was added to a stirred solution of D-norleucine (5.0 g., 38 mmol.) in 2.5N sulfuric acid (77 ml.) at room temperature. The reaction mixture was cooled to -10° C. and solid sodium nitrite (3.94 g., 57 mmol.) was added portionwise, maintaining the temperature between -10° and -5° C....
10.6084/m9.figshare.5104873.v1
null
Primary amine
Secondary halide
null
null
null
Other
S(O)(O)(=O)=O
-10
1
CCCC[C@@H](N)C(=O)O.[Br-]>S(O)(O)(=O)=O>CCCC[C@H](Br)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8a9fc26c3201445093ccc42bd50dbc2c
CC(C)(C)OC(=O)C1CCNN1.O=C(Cl)OCc1ccccc1>>CC(C)(C)OC(=O)C1CCN(C(=O)OCc2ccccc2)N1
C(C1=CC=CC=C1)OC(=O)Cl.N1=CC=CC=C1.N1NC(CC1)C(=O)OC(C)(C)C>>C1(=CC=CC=C1)COC(=O)N1NC(CC1)C(=O)OC(C)(C)C
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH:8]1[CH2:9][CH2:10][NH:11][NH:22]1.Cl[C:12](=[O:13])[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[CH:8]1[CH2:9][CH2:10][N:11]([C:12](=[O:13])[O:14][CH2:15][c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[NH:22]1
CC(C)(C)OC(=O)C1CCNN1.O=C(Cl)OCc1ccccc1
CC(C)(C)OC(=O)C1CCN(C(=O)OCc2ccccc2)N1
null
null
C(C)#N.C(C)(=O)OCC
Protection
N-alkylation of secondary amines with alkyl halides
73992b21715ecca97b52ecaee4e44c394a77dca0dfe1f68c20d7957ed17ccc9d
5fd6250903fa66c378faf3ffa4e2360187bf8e16b5a0c6900f15dfbc5082c0be
O=C(OCc1ccccc1)N1CCCN1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]1-[#7:9]-[NH;D2;+0:10]-[C:11]-[C:12]-1>>[#8:5]-[C:6](=[O;D1;H0:7])-[C:8]1-[#7:9]-[N;H0;D3;+0:10](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-[C:11]-[C:12]-1
null
[]
0
CELSIUS
3
HOUR
A solution of 3-pyrazolidinecarboxylic acid, 1,1-dimethylethyl ester (10.935 g., 63.5 mmol.) in dry acetonitrile (90 ml.) was cooled to 0° C. (ice-salt bath) and treated with dry pyridine (11.0 ml.) followed by a solution of benzylchloroformate (12.54 g., 10.5 ml., 69.9 mmol.) in dry acetonitrile (25 ml.). The reaction...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Hydrazine
Acylhydrazine
C1CNNC1
C1CN[NH]C1
C1CN[NH]C1.c1ccccc1
HCl
C(C)#N.C(C)(=O)OCC
0
3
CC(C)(C)OC(=O)C1CCNN1.O=C(Cl)OCc1ccccc1>C(C)#N.C(C)(=O)OCC>CC(C)(C)OC(=O)C1CCN(C(=O)OCc2ccccc2)N1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f8e6f6d403494c7b94171529ebac16f6
CC(C)C[C@@H](N)C(=O)O.[Br-]>>CC(C)C[C@H](Br)C(=O)O
[Br-].[K+].N[C@H](CC(C)C)C(=O)O.N(=O)[O-].[Na+]>>Br[C@H](C(=O)O)CC(C)C
N[C@H:5]([CH2:4][CH:2]([CH3:1])[CH3:3])[C:7](=[O:8])[OH:9].[Br-:6]>>[CH3:1][CH:2]([CH3:3])[CH2:4][C@H:5]([Br:6])[C:7](=[O:8])[OH:9]
CC(C)C[C@@H](N)C(=O)O.[Br-]
CC(C)C[C@H](Br)C(=O)O
null
null
S(O)(O)(=O)=O
Functional Group Interconversion
OtherReaction
117344ae409beae3589a30d5997369184f62edb887830bd6b795e8dfdf82920d
9544d3c5449a12cdcbad58c02e82937c94837ec7c67e3baf5ab21c8ae3b17e42
null
N-[C@H;D3;+0:1](-[C:2]-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[Br-;H0;D0:7]>>[Br;H0;D1;+0:7]-[C@@H;D3;+0:1](-[C:2]-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6]
null
[]
-10
CELSIUS
1
HOUR
Potassium bromide (9.5 g., 80 mmol.) was added to a stirred solution of D-leucine (3.0 g., 23 mmol.) in 2.5N sulfuric acid (47 ml.) at room temperature. The reaction mixture was cooled to -10° C. and solid sodium nitrite (2.4 g., 34 mmol.) was added portionwise, maintaining the temperature between -10° and -5° C. After...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Secondary halide
null
null
null
Other
S(O)(O)(=O)=O
-10
1
CC(C)C[C@@H](N)C(=O)O.[Br-]>S(O)(O)(=O)=O>CC(C)C[C@H](Br)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bc6e6e4b092043918a2288ce8fa820b4
CC(=Cc1ccccc1)C(=O)O>>CC(Cc1ccccc1)C(=O)O
CC(C(=O)O)=CC1=CC=CC=C1>>CC(C(=O)O)CC1=CC=CC=C1
[CH3:1][C:2](=[CH:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[OH:12]>>[CH3:1][CH:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[OH:12]
CC(=Cc1ccccc1)C(=O)O
CC(Cc1ccccc1)C(=O)O
null
[Pd]
CO
Reduction
Hydrogenation (double to single)
0bc3968b35f0839c230afb4215314da278abd4e1f10e42ec3012c5512de49ea5
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
c1ccccc1
[C;D1;H3:1]-[C;H0;D3;+0:2](=[CH;D2;+0:3]-[c:4](:[c:5]):[c:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]>>[C;D1;H3:1]-[CH;D3;+0:2](-[CH2;D2;+0:3]-[c:4](:[c:5]):[c:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]
null
[]
null
null
null
null
A solution of α-methyl cinnamic acid (10.0 g., 61.7 mmol.) in dry methanol (250 ml.) was treated with 10% palladium on carbon and hydrogenated (balloon used) at room temperature for 16 hours. The reaction mixture was diluted with methanol (250 ml.), filtered through a Celite pad in a millipore unit, washing the pad wel...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
[Pd].CO
null
null
CC(=Cc1ccccc1)C(=O)O>[Pd].CO>CC(Cc1ccccc1)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bb89d795a1f04c6a9aea5994f10b7016
BrCc1ccccc1.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>>O=C(OCc1ccccc1)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
C([O-])([O-])=O.[Cs+].[Cs+].C1(C=2C(C(N1[C@H](C(=O)O)CCCCO)=O)=CC=CC2)=O.C(C1=CC=CC=C1)Br>>C1(C=2C(C(N1[C@H](C(=O)OCC1=CC=CC=C1)CCCCO)=O)=CC=CC2)=O
Br[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1.[O:1]=[C:2]([OH:3])[C@H:11]([CH2:12][CH2:13][CH2:14][CH2:15][OH:16])[N:17]1[C:18](=[O:19])[c:20]2[cH:21][cH:22][cH:23][cH:24][c:25]2[C:26]1=[O:27]>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C@H:11]([CH2:12][CH2:13][CH2:14][CH2:15][OH:16])[N:17]1[C:18...
BrCc1ccccc1.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
O=C(OCc1ccccc1)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
O=C(CN1C(=O)c2ccccc2C1=O)OCc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]>>[C:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
2
HOUR
A slurry of cesium carbonate (3.819 g, 11.7 mmol.) and (S)-2-phthalimido-6-hydroxyhexanoic acid (6.00 g, 21.6 mmol.) in dimethylformamide (60 ml.) was treated with benzyl bromide (3.30 ml., 4.75 g., 27.7 mmol.). After stirring at room temperature for 2 hours, the mixture was partitioned between ethyl acetate and water....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1ccccc1.c1ccc2c(c1)C[NH]C2
HBr
CN(C=O)C
null
2
BrCc1ccccc1.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>CN(C=O)C>O=C(OCc1ccccc1)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-42ed6fb7dd91419caecfec4b1a99a601
CI.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>>COC(=O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
C1(C=2C(C(N1[C@H](C(=O)O)CCCCO)=O)=CC=CC2)=O.C([O-])([O-])=O.[Cs+].[Cs+].CI>>C1(C=2C(C(N1[C@H](C(=O)OC)CCCCO)=O)=CC=CC2)=O
I[CH3:1].[OH:2][C:3](=[O:4])[C@H:5]([CH2:6][CH2:7][CH2:8][CH2:9][OH:10])[N:11]1[C:12](=[O:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[O:21]>>[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH2:6][CH2:7][CH2:8][CH2:9][OH:10])[N:11]1[C:12](=[O:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[O:21]
CI.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
COC(=O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
null
null
CN(C=O)C.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
9474aa79a2adc7353c0c02444ca598a6f486ecdd7ed5edb9ae0645721ee50389
badd4f82161bb0ee7acffd023ea4caae5d036bce7065c10ab0a06e83a6a6f119
O=C1NC(=O)c2ccccc21
I-[CH3;D1;+0:1].[C:2]-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]>>[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH3;D1;+0:1]
196
[{"value": 196.0, "product": "C1(C=2C(C(N1[C@H](C(=O)OC)CCCCO)=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A slurry of (S)-2-phthalimido-6-hydroxyhexanoic acid (3.752 g., 13.5 mmol.) and cesium carbonate (2.178 g., 6.7 mmol.) in dimethylformamide (44 ml.) was treated with methyl iodide (3.0 ml., 6.84 g., 48.2 mmol.). After stirring at room temperature for 2 hours, the mixture was diluted with ethyl acetate and washed succes...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1ccc2c(c1)C[NH]C2
HI
CN(C=O)C.C(C)(=O)OCC
null
2
CI.O=C(O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O>CN(C=O)C.C(C)(=O)OCC>COC(=O)[C@H](CCCCO)N1C(=O)c2ccccc2C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-610f08ba6e464144a63f27b6b8c29436
CCOC(=O)CBr.C[C@@H]1CCC[C@H](NC(=O)OC(C)(C)C)C(=O)N1>>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)CCC[C@H]1C
CC(C)(OC(=O)N[C@@H]1C(N[C@@H](CCC1)C)=O)C.C[Si](C)(C)[N-][Si](C)(C)C.[Li+].BrCC(=O)OCC>>CC(C)(OC(=O)N[C@@H]1C(N([C@@H](CCC1)C)CC(=O)OCC)=O)C
Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[NH:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O:14][C:15]([CH3:16])([CH3:17])[CH3:18])[CH2:19][CH2:20][CH2:21][C@H:22]1[CH3:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]1[C:8](=[O:9])[C@@H:10]([NH:11][C:12](=[O:13])[O:14][C:15]([CH3:16])([CH3:17])[CH3:18])[CH2:19][CH...
CCOC(=O)CBr.C[C@@H]1CCC[C@H](NC(=O)OC(C)(C)C)C(=O)N1
CCOC(=O)CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)CCC[C@H]1C
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
21efda898581b4e7e1b0a01b07328527522c0c899fbfe8483d7f4fdc1f9e273c
933a6f1013d44497c9c5902b73c24fbdc7813d20b886bdbc4c670d5b43ca2182
O=C1CCCCCN1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C:6]-[C:7](=[O;D1;H0:8])-[NH;D2;+0:9]-[C:10](-[C;D1;H3:11])-[C:12]>>[C:6]-[C:7](=[O;D1;H0:8])-[N;H0;D3;+0:9](-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[C:10](-[C;D1;H3:11])-[C:12]
null
[]
null
null
30
MINUTE
A solution of (3S-cis)-hexahydro-3-[[(1,1-dimethylethoxy)carbonyl]amino]-7-methyl-2H-azepin-2-one [prepared as described in Example 64(f), 500 mg., 2.06 mmol.] in tetrahydrofuran (13 ml.) at room temperature under argon was treated dropwise with 1.0M lithium bis(trimethylsilyl)amide in tetrahydrofuran (2.7 ml., 2.7 mmo...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Secondary amide
Ester.Tertiary amide
C1CCCNCC1
C1CCC[NH]CC1
C1CCC[NH]CC1
HBr
O1CCCC1
null
0.5
CCOC(=O)CBr.C[C@@H]1CCC[C@H](NC(=O)OC(C)(C)C)C(=O)N1>O1CCCC1>CCOC(=O)CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)CCC[C@H]1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9580e3afee14b25a5c17e12c653103b
CC(C)NC(C)C.ClCCCCBr.O=C(O)C1CCCC1>>CC(C)[N-]C(C)C.O=C(O)C1(CCCCCl)CCCC1.[Li+]
BrCCCCCl.C1(CCCC1)C(=O)O.C(C)(C)NC(C)C.C(CCC)[Li]>>C(C)(C)[N-]C(C)C.[Li+].ClCCCCC1(CCCC1)C(=O)O
[CH3:1][CH:2]([CH3:3])[NH:4][CH:5]([CH3:6])[CH3:7].Br[CH2:12][CH2:13][CH2:14][CH2:15][Cl:16].[O:8]=[C:9]([OH:10])[CH:11]1[CH2:17][CH2:18][CH2:19][CH2:20]1>>[CH3:1][CH:2]([CH3:3])[N-:4][CH:5]([CH3:6])[CH3:7].[O:8]=[C:9]([OH:10])[C:11]1([CH2:12][CH2:13][CH2:14][CH2:15][Cl:16])[CH2:17][CH2:18][CH2:19][CH2:20]1.[Li+:21]
CC(C)NC(C)C.ClCCCCBr.O=C(O)C1CCCC1
CC(C)[N-]C(C)C.O=C(O)C1(CCCCCl)CCCC1.[Li+]
null
null
O1CCCC1
C-C Coupling
OtherReaction
77153b7242f8754879e3f0b886657cd5957a50555e81a521ab32e496bf739211
9ba1e0467902f373f7806da8e18ec7a85760b64f74aa649da2579d00e73d9ca4
C1CCCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[C:5](-[C;D1;H3:6])-[NH;D2;+0:7]-[C:8](-[C;D1;H3:9])-[C;D1;H3:10].[O;D1;H0:11]=[C:12](-[O;D1;H1:13])-[CH;D3;+0:14]1-[C:15]-[C:16]-[C:17]-[C:18]-1>>[C;D1;H3:4]-[C:5](-[C;D1;H3:6])-[N-;H0;D2:7]-[C:8](-[C;D1;H3:9])-[C;D1;H3:10].[C:3]-[C:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:14]1(-[C:12](=[O...
null
[]
-74
CELSIUS
15
MINUTE
A solution of lithium diisopropylamide was prepared under nitrogen from diisopropylamine (31.0 ml., 220 mmol.) and n-butyl lithium (1.5M in hexane, 88.0 ml., 220 mmol.) in tetrahydrofuran (80 ml.), maintaining the temperature between -3° C.-1° C. After stirring 15 minutes, cyclopentanecarboxylic acid (11.4 g., 100 mmol...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
null
C1CCCC1
C1CCCC1
C1CCCC1
null
O1CCCC1
-74
0.25
CC(C)NC(C)C.ClCCCCBr.O=C(O)C1CCCC1>O1CCCC1>CC(C)[N-]C(C)C.O=C(O)C1(CCCCCl)CCCC1.[Li+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0d8ba9ae803d40f58c0f4e79b8f5ba5f
CCCCC.CCOCC.CCOCC>>O=C1CCCCCC12CCCC2
C(C)(C)(C)[Li].CCOCC.CCOCC.CCCCC>>C1CCCC12C(CCCCC2)=O
[CH3:8][CH2:12][CH2:11][CH2:10][CH3:9].C([O:1][CH2:2][CH3:3])[CH3:5].CCO[CH2:7][CH3:6]>>[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][C:8]12[CH2:9][CH2:10][CH2:11][CH2:12]2
CCCCC.CCOCC.CCOCC
O=C1CCCCCC12CCCC2
null
null
null
Acylation
OtherReaction
7f9c56080232237cb2af9c91b9ac11dba4e3d417835241b7fb2a95600fe5c061
71cd9ffc2461c2b8f2c58f8e59f7f0e3e5cc0afbee292adb82f64bbd7fde8e75
O=C1CCCCCC12CCCC2
C-C-O-[CH2;D2;+0:1]-[CH3;D1;+0:2].[CH3;D1;+0:3]-[CH2;D2;+0:4]-[O;H0;D2;+0:5]-C-[CH3;D1;+0:6].[CH3;D1;+0:7]-[C:8]-[C:9]-[C:10]-[CH3;D1;+0:11]>>[O;H0;D1;+0:5]=[C;H0;D3;+0:4]1-[CH2;D2;+0:3]-[C:12]-[CH2;D2;+0:6]-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:7]-12-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-2
null
[]
-100
CELSIUS
null
null
t-Butyl lithium (1.7M in pentane, 20.0 ml., 34 mmol.) was slowly added to ether (38 ml.) at -20° C. as the reaction was further cooled to -100° C. in a methanol/dry ice/liquid nitrogen bath. To this -100° C. solution was added the product from part (c) (5.0 g., 16.1 mmol.) in 2:1 ether/pentane (3 ml.) over 35 minutes, ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Ketone
null
C1CCCC2(CC1)CCCC2
C1CCCC2(CC1)CCCC2
HO-
null
-100
null
CCCCC.CCOCC.CCOCC>>O=C1CCCCCC12CCCC2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-91db5ae7637043fcbd8aafa42c743728
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 [prepared 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-445ecc728ecd4029a651f6f2abfe3d94
O=C(Cl)c1ccc([N+](=O)[O-])cc1.O=C1CCCNc2ccccc21>>O=C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
C([O-])(O)=O.[Na+].N1CCCC(C2=C1C=CC=C2)=O.C(C)N(CC)CC.[N+](=O)([O-])C1=CC=C(C(=O)Cl)C=C1>>[N+](=O)([O-])C1=CC=C(C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=C1
Cl[C:7](=[O:8])[c:9]1[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][cH:17]1.[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][NH:6][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]21>>[O:1]=[C:2]1[CH2:3][CH2:4][CH2:5][N:6]([C:7](=[O:8])[c:9]2[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][cH:17]2)[c:18]2[cH:19][cH:20][cH:21][cH:22]...
O=C(Cl)c1ccc([N+](=O)[O-])cc1.O=C1CCCNc2ccccc21
O=C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
null
null
ClCCl
Acylation
N-alkylation of secondary amines with alkyl halides
64413dd180580e9c8f2736c3a8c0c162d266e6033cf64f74e0aa763b2659218c
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C1CCCN(C(=O)c2ccccc2)c2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[C:7]-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]-[C:12]=[O;D1;H0:13]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5])-[c:9](:[c:10]):[c:11]-[C:12]=[O;D1;H0:13]
null
[]
null
null
null
null
A 3.32 g portion of 2,3,4,5-tetrahydro-1H-1-benzazepin-5-one and 4.31 ml of triethylamine were dissolved in 33 ml of dichloromethane and, with stirring on an ice bath, 4.59 g of p-nitrobenzoyl chloride was added to the resulting solution. The reaction solution was stirred at room temperature for additional 60 minutes. ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
c1ccc2c(c1)CCCCN2
c1ccc2c(c1)CCCC[NH]2
c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HCl
ClCCl
null
null
O=C(Cl)c1ccc([N+](=O)[O-])cc1.O=C1CCCNc2ccccc21>ClCCl>O=C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ef4bb1c6c9b74f7baca312f5b2f73584
O=C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21>>Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
[N+](=O)([O-])C1=CC=C(C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=C1.CN(C=O)C>>NC1=CC=C(C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=C1
O=[N+:1]([O-])[c:2]1[cH:3][cH:4][c:5]([C:6](=[O:7])[N:8]2[CH2:9][CH2:10][CH2:11][C:12](=[O:13])[c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]32)[cH:20][cH:21]1>>[NH2:1][c:2]1[cH:3][cH:4][c:5]([C:6](=[O:7])[N:8]2[CH2:9][CH2:10][CH2:11][C:12](=[O:13])[c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]32)[cH:20][cH:21]1
O=C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21
Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
null
[Ni]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C1CCCN(C(=O)c2ccccc2)c2ccccc21
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A 19.2 g portion of 1-(4-nitrobenzoyl)-2,3,4,5-tetrahydro1H-1-benzazepin-5-one was dissolved in a mixed solvent consisting of 200 ml of dimethylformamide and 100 ml of methyl alcohol, and 3 ml of Raney nickel was added to the resulting solution to carry out hydrogenation at normal pressure. After completion of the hydr...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccc2c(c1)CCCC[NH]2
Other
[Ni].CO
null
null
O=C1CCCN(C(=O)c2ccc([N+](=O)[O-])cc2)c2ccccc21>[Ni].CO>Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2e6e8e890e41483eb3956e85028c6a40
Cc1ccc(-c2ccccc2C(=O)O)cc1.Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1>>Cc1ccc(-c2cc(C(=O)N3CCCC(=O)c4ccccc43)ccc2C(=O)Nc2ccccc2)cc1
CC1=CC=C(C=C1)C1=C(C(=O)O)C=CC=C1.NC1=CC=C(C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=C1>>CC1=CC=C(C=C1)C1=C(C(=O)NC2=CC=CC=C2)C=CC(=C1)C(=O)N1CCCC(C2=C1C=CC=C2)=O
O[C:26]([c:25]1[c:6](-[c:5]2[cH:4][cH:3][c:2]([CH3:1])[cH:36][cH:35]2)[cH:7][cH:8][cH:23][cH:24]1)=[O:27].[C:9](=[O:10])([N:11]1[CH2:12][CH2:13][CH2:14][C:15](=[O:16])[c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]21)[c:32]1[cH:31][cH:30][c:29]([NH2:28])[cH:34][cH:33]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8]([C:9]...
Cc1ccc(-c2ccccc2C(=O)O)cc1.Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
Cc1ccc(-c2cc(C(=O)N3CCCC(=O)c4ccccc43)ccc2C(=O)Nc2ccccc2)cc1
null
null
null
C-C Coupling
OtherReaction
a2bc7e50c766d3f3372491c10a493df5289d5bca86a323cef4d7ecb2538ff9c9
2bdf1de8aca0687dff29f685df308f1db97c12fed21499bf6def3aaf3ba3ab62
O=C(Nc1ccccc1)c1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1-c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]:1.[C:9]-[#7:10](-[C;H0;D3;+0:11](=[O;D1;H0:12])-[c;H0;D3;+0:13]1:[c:14]:[c:15]:[c:16](-[NH2;D1;+0:17]):[c:18]:[c:19]:1)-[c:20]>>[C:9]-[#7:10](-[C;H0;D3;+0:11](=[O;D1;H0:12])-[c;H0;D3;+0:6]1:[c:5]:[c:4]:[c:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;...
null
[]
null
null
null
null
Using o-(4-methylphenyl)benzoic acid and 1-(4-aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one as starting materials, the procedure of Reference Example 3 was repeated to obtain 2-(4-methylphenyl)-4-[(5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide. Conditions: See reaction.notes.procedure_deta...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide.Primary amine
Secondary amide.Tertiary amide
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2.c1ccccc1
HO-
null
null
null
Cc1ccc(-c2ccccc2C(=O)O)cc1.Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1>>Cc1ccc(-c2cc(C(=O)N3CCCC(=O)c4ccccc43)ccc2C(=O)Nc2ccccc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a89ffbbd03274d85a4403eaa7a25775f
NC(=S)Cc1ccccn1.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1>>O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4ccccn4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
C1(=CC=CC=C1)C1=C(C(=O)NC2=CC=C(C=C2)C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=CC=C1.Cl.N1=C(C=CC=C1)CC(=S)N>>N1=C(C=CC=C1)CC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3
[S:14]=[C:15]([CH2:16][c:17]1[cH:18][cH:19][cH:20][cH:21][n:22]1)[NH2:23].O=[C:24]1[CH2:13][CH2:12][CH2:11][N:10]([C:8]([c:7]2[cH:6][cH:5][c:4]([NH:3][C:2](=[O:1])[c:33]3[cH:34][cH:35][cH:36][cH:37][c:38]3-[c:39]3[cH:40][cH:41][cH:42][cH:43][cH:44]3)[cH:32][cH:31]2)=[O:9])[c:30]2[c:25]1[cH:26][cH:27][cH:28][cH:29]2>>[O...
NC(=S)Cc1ccccn1.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1
O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4ccccn4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
90831385c4296843ed9134a5e95a4102cbad965e0d393ec4e6a8a630ca15fc68
16c2ab1613ef9809c999e5005ffb432ea914712ab0b2c1320b2137a583f319ec
O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4ccccn4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[#7:5](-[C:6]=[O;D1;H0:7])-[c:8](:[c:9]):[c;H0;D3;+0:10]-1:[c:11]:[c:12].[#7;a:13]:[c:14]-[C:15]-[C;H0;D3;+0:16](-[NH2;D1;+0:17])=[S;H0;D1;+0:18]>>[#7;a:13]:[c:14]-[C:15]-[c;H0;D3;+0:16]1:[n;H0;D2;+0:17]:[c;H0;D3;+0:1]2:[c;H0;D3;+0:2](:[s;H0;D2;+0:18]:1)-[C:3]-[C:4]-[#7:5](-[...
58.3
[{"value": 58.3, "product": "N1=C(C=CC=C1)CC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using 400 mg of 2-phenyl-4'-[(5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide and 370 mg of 2-pyridylthioacetamide hydrochloride, the procedure of Example 5 was repeated, and the resulting free base was recrystallized from chloroform-diethyl ether to obtain 300 mg of 4'-[[2-(2-pyridylmethyl)-5,6-dihy...
10.6084/m9.figshare.5104873.v1
null
Ketone.Thioamide
null
c1ccc2c(c1)CCCC[NH]2
c1ccc2c(c1)[NH]CCc1scnc12
c1ccccc1.c1ccncc1.c1ccc2c(c1)[NH]CCc1scnc12.c1ccccc1.c1ccccc1
HO-
null
null
null
NC(=S)Cc1ccccn1.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1>>O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4ccccn4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-90050701c8ef48ae805729e1fea02e48
NC(=S)Cc1cccnc1.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1>>O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4cccnc4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
C1(=CC=CC=C1)C1=C(C(=O)NC2=CC=C(C=C2)C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=CC=C1.Cl.N1=CC(=CC=C1)CC(=S)N>>Cl.N1=CC(=CC=C1)CC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3
[S:15]=[C:16]([CH2:17][c:18]1[cH:19][cH:20][cH:21][n:22][cH:23]1)[NH2:24].O=[C:25]1[CH2:14][CH2:13][CH2:12][N:11]([C:9]([c:8]2[cH:7][cH:6][c:5]([NH:4][C:3](=[O:2])[c:34]3[cH:35][cH:36][cH:37][cH:38][c:39]3-[c:40]3[cH:41][cH:42][cH:43][cH:44][cH:45]3)[cH:33][cH:32]2)=[O:10])[c:31]2[c:26]1[cH:27][cH:28][cH:29][cH:30]2>>[...
NC(=S)Cc1cccnc1.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1
O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4cccnc4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
90831385c4296843ed9134a5e95a4102cbad965e0d393ec4e6a8a630ca15fc68
16c2ab1613ef9809c999e5005ffb432ea914712ab0b2c1320b2137a583f319ec
O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4cccnc4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[#7:5](-[C:6]=[O;D1;H0:7])-[c:8](:[c:9]):[c;H0;D3;+0:10]-1:[c:11]:[c:12].[#7;a:13]:[c:14]:[c:15]-[C:16]-[C;H0;D3;+0:17](-[NH2;D1;+0:18])=[S;H0;D1;+0:19]>>[#7;a:13]:[c:14]:[c:15]-[C:16]-[c;H0;D3;+0:17]1:[n;H0;D2;+0:18]:[c;H0;D3;+0:1]2:[c;H0;D3;+0:2](:[s;H0;D2;+0:19]:1)-[C:3]-[...
18.3
[{"value": 18.3, "product": "Cl.N1=CC(=CC=C1)CC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using 400 mg of 2-phenyl-4'-[(5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide and 400 mg of 3-pyridylthioacetamide hydrochloride, the procedure of Example 5 was repeated to obtain 100 mg of 4'-[[2-(3-pyridylmethyl)-5,6-dihydro-4H-thiazolo[5,4-d][1]benzazepin-6-yl)carbonyl]-2-phenylbenzanilide hydroch...
10.6084/m9.figshare.5104873.v1
null
Ketone.Thioamide
null
c1ccc2c(c1)CCCC[NH]2
c1ccc2c(c1)[NH]CCc1scnc12
c1ccccc1.c1ccncc1.c1ccc2c(c1)[NH]CCc1scnc12.c1ccccc1.c1ccccc1
HO-
null
null
null
NC(=S)Cc1cccnc1.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1>>O=C(Nc1ccc(C(=O)N2CCc3sc(Cc4cccnc4)nc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-026832da140844da9cfb5930520fe4e3
CN(C)CCNC(N)=S.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1>>CN(C)CCNc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2
C1(=CC=CC=C1)C1=C(C(=O)NC2=CC=C(C=C2)C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=CC=C1.Cl.CN(C)CCNC(=S)N>>CN(CCNC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3)C
[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][NH:6][C:7]([NH2:8])=[S:11].O=[C:9]1[CH2:10][CH2:12][CH2:13][N:14]([C:15](=[O:16])[c:17]2[cH:18][cH:19][c:20]([NH:21][C:22](=[O:23])[c:24]3[cH:25][cH:26][cH:27][cH:28][c:29]3-[c:30]3[cH:31][cH:32][cH:33][cH:34][cH:35]3)[cH:36][cH:37]2)[c:38]2[cH:39][cH:40][cH:41][cH:42][c:43]21>>[CH3:...
CN(C)CCNC(N)=S.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1
CN(C)CCNc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
46e4505adf07cbe530a0c849599290eef25c051af2c21072fd50c73fa13dc0c2
07a0b9468f27db415286267ce195abab600eca1857ac5ed441aacbc6b5c39b8e
O=C(Nc1ccc(C(=O)N2CCc3scnc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[#7:5](-[C:6]=[O;D1;H0:7])-[c:8](:[c:9]):[c;H0;D3;+0:10]-1:[c:11]:[c:12].[C:13]-[#7:14]-[C;H0;D3;+0:15](-[NH2;D1;+0:16])=[S;H0;D1;+0:17]>>[C:13]-[#7:14]-[c;H0;D3;+0:15]1:[n;H0;D2;+0:16]:[c;H0;D3;+0:1]2:[c;H0;D3;+0:2](:[s;H0;D2;+0:17]:1)-[C:3]-[C:4]-[#7:5](-[C:6]=[O;D1;H0:7])-...
58.8
[{"value": 58.8, "product": "CN(CCNC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Using 400 mg of 2-phenyl-4'-[(5-oxo-2,3,4,5-tetrahydro1H-1-benzazepin-1-yl)carbonyl]benzanilide and 300 mg of dimethylaminoethylthiourea hydrochloride and using ethyl alcohol as the reaction solvent, the procedure of Example 5 was repeated and the resulting residue was recrystallized from ethyl acetate-diethyl ether to...
10.6084/m9.figshare.5104873.v1
null
Ketone.Thiourea
null
c1ccc2c(c1)CCCC[NH]2
c1ccc2c(c1)[NH]CCc1scnc12
c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2c(c1)[NH]CCc1scnc12
HO-
C(C)O
null
null
CN(C)CCNC(N)=S.O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1-c1ccccc1>C(C)O>CN(C)CCNc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-52eeeb285aa44f2a8df38cb2bd9296be
CC(C)(C)OC(=O)NCC(=O)O.CCN=C=NCCCN(C)C.Nc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2>>CC(C)O.NCC(=O)Nc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2
C(C)(C)(C)OC(=O)NCC(=O)O.ON1N=NC2=C1C=CC=C2.CN1CCOCC1.Cl.C(C)N=C=NCCCN(C)C.Br.NC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3>>Cl.CC(C)O.NCC(=O)NC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3
CC(C)(C)OC(=O)[NH:6][CH2:7][C:8]([OH:4])=[O:9].CN(CCCN=C=N[CH2:2][CH3:1])[CH3:3].[NH2:10][c:11]1[n:12][c:13]2[c:14]([s:15]1)[CH2:16][CH2:17][N:18]([C:19](=[O:20])[c:21]1[cH:22][cH:23][c:24]([NH:25][C:26](=[O:27])[c:28]3[cH:29][cH:30][cH:31][cH:32][c:33]3-[c:34]3[cH:35][cH:36][cH:37][cH:38][cH:39]3)[cH:40][cH:41]1)[c:42...
CC(C)(C)OC(=O)NCC(=O)O.CCN=C=NCCCN(C)C.Nc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2
CC(C)O.NCC(=O)Nc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2
null
null
ClCCl.O.C(C)N(CC)CC
Acylation
OtherReaction
47ded26842dab283296de32f5d8298ef874e2d0794235c9ebd8543fdbee99e79
82ca69076342c33c07f6f6551734c390737770207af37de3dbab41142214a909
O=C(Nc1ccc(C(=O)N2CCc3scnc3-c3ccccc32)cc1)c1ccccc1-c1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[OH;D1;+0:5].C-N(-[CH3;D1;+0:6])-C-C-C-N=C=N-[CH2;D2;+0:7]-[C;D1;H3:8].[NH2;D1;+0:9]-[c:10]1:[#16;a:11]:[c:12]:[c:13]:[#7;a:14]:1>>[C;D1;H3:8]-[CH;D3;+0:7](-[CH3;D1;+0:6])-[OH;D1;+0:5].[NH2;D1;+0:1]-[C:2]-[C;H0;D3;+0:3](=[O;D1;H0:4])-[NH;D2;+0:9]-[c:10...
55.7
[{"value": 55.7, "product": "Cl.CC(C)O.NCC(=O)NC=1SC=2CCN(C3=C(C2N1)C=CC=C3)C(=O)C3=CC=C(NC(C1=C(C=CC=C1)C1=CC=CC=C1)=O)C=C3", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
After dissolving 176 mg of t-butoxycarbonylglycine, 205 mg of 1-hydroxybenztriazole and 0.15 ml of N-methylmorpholine in 3.5 ml of dichloromethane, 192 mg of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride was added to the resulting solution with stirring on an ice bath, and the mixture was warmed up to roo...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid.Ether.Primary amine.Tertiary amine.Boc
Secondary amide.Secondary alcohol.Primary amine
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccc2c(c1)[NH]CCc1scnc12
HO-
ClCCl.O.C(C)N(CC)CC
null
8
CC(C)(C)OC(=O)NCC(=O)O.CCN=C=NCCCN(C)C.Nc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2>ClCCl.O.C(C)N(CC)CC>CC(C)O.NCC(=O)Nc1nc2c(s1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1-2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-63cce50ac648477a9245c0dedfc173bd
Cl>>Cl
CC=1NC2=C(CCN(C3=C2C=CC=C3)C(=O)C3=CC=C(NC(C2=C(C=CC=C2)C2=CC=CC=C2)=O)C=C3)N1.Cl.C(C)(=O)OCC>>Cl.CC=1NC2=C(CCN(C3=C2C=CC=C3)C(=O)C3=CC=C(NC(C2=C(C=CC=C2)C2=CC=CC=C2)=O)C=C3)N1
[ClH:39]>>[ClH:39]
Cl
Cl
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
4'-[(2-Methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepin-6-yl)carbonyl]-2-phenylbenzanilide was dissolved in 5 ml of ethyl alcohol, the resulting solution was mixed with 0.19 ml of 4N hydrochloric acid-ethyl acetate and cooled on an ice bath and then the thus precipitated crystals were collected by filtration and wa...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
null
Cl>C(C)O>Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-58cd2e04d7a34df7b31f8a8ce82f18d5
Cl>>Cl
CC1=CC=C(C=C1)C1=C(C(=O)NC2=CC=C(C=C2)C(=O)N2CCC3=C(C4=C2C=CC=C4)NC(=N3)C)C=CC=C1.Cl.C(C)(=O)OCC>>Cl.CC1=CC=C(C=C1)C1=C(C(=O)NC2=CC=C(C=C2)C(=O)N2CCC3=C(C4=C2C=CC=C4)NC(=N3)C)C=CC=C1
[ClH:40]>>[ClH:40]
Cl
Cl
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
2-(4-Methylphenyl)-4'-[(2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepin-6-yl)carbonyl]benzanilide was dissolved in 10 ml of ethyl alcohol, the resulting solution was mixed with 0.37 ml of 4N hydrochloric acid-ethyl acetate and cooled on an ice bath and then the thus precipitated crystals were collected by filtra...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
null
Cl>C(C)O>Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-23a39ece3a4041d69c341d884e898380
Cc1ccccc1C(=O)O.Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1>>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
CC1=C(C(=O)O)C=CC=C1.NC1=CC=C(C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=C1>>CC1=C(C(=O)NC2=CC=C(C=C2)C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=CC=C1
O[C:8]([c:7]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][cH:6]1)=[O:9].[NH2:10][c:11]1[cH:12][cH:13][c:14]([C:15](=[O:16])[N:17]2[CH2:18][CH2:19][CH2:20][C:21](=[O:22])[c:23]3[cH:24][cH:25][cH:26][cH:27][c:28]32)[cH:29][cH:30]1>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][cH:6][c:7]1[C:8](=[O:9])[NH:10][c:11]1[cH:12][cH:13][c:14]([C:15](=[O:...
Cc1ccccc1C(=O)O.Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
null
null
null
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1)c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
Using o-methylbenzoic acid and 1-(4-aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one as starting materials, the procedure of Reference Example 3 was repeated to obtain 2-methyl-4'-[(5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
null
null
null
Cc1ccccc1C(=O)O.Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1>>Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3679fbd88dec487795772a47ae39b783
COc1cc(C(=O)O)ccc1-c1ccccc1.O=C1CCCNc2ccccc21>>COc1ccccc1-c1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
C(C(=O)Cl)(=O)Cl.CN(C=O)C.COC=1C(=CC=C(C1)C(=O)O)C1=CC=CC=C1.O=C1CCCNC2=C1C=CC=C2>>COC1=C(C2=CC=C(C=C2)C(=O)N2CCCC(C3=C2C=CC=C3)=O)C=CC=C1
O[C:13]([c:12]1[cH:4][c:3]([O:2][CH3:1])[c:8](-[c:9]2[cH:10][cH:5][cH:6][cH:27][cH:28]2)[cH:7][cH:11]1)=[O:14].[NH:15]1[CH2:16][CH2:17][CH2:18][C:19](=[O:20])[c:21]2[cH:22][cH:23][cH:24][cH:25][c:26]21>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1-[c:9]1[cH:10][cH:11][c:12]([C:13](=[O:14])[N:15]2[CH2:16][CH2:17][CH...
COc1cc(C(=O)O)ccc1-c1ccccc1.O=C1CCCNc2ccccc21
COc1ccccc1-c1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
null
null
ClCCl.O.C(C)N(CC)CC
Acylation
OtherReaction
2699e622f477dfe56b054072967f9069c986e7f245eb9ffc00114ced8b7936a0
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C1CCCN(C(=O)c2ccc(-c3ccccc3)cc2)c2ccccc21
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[cH;D2;+0:5]:[c:6](-[c:7]2:[c:8]:[cH;D2;+0:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:2):[c:13](-[#8:14]):[cH;D2;+0:15]:1.[C:16]-[C:17]-[NH;D2;+0:18]-[c:19](:[c:20]):[c:21]-[C:22]=[O;D1;H0:23]>>[#8:14]-[c:13]1:[cH;D2;+0:15]:[cH;D2;+0:11]:[cH;D2;+0:10]:[cH;D2...
null
[]
null
null
1
HOUR
A 1.67 g portion of 2-methoxybiphen-4-ylcarboxylic acid was dissolved in 17 ml of dichloromethane, 0.95 ml of oxalyl chloride and a catalytically effective amount of dimethylformamide were added to the resulting solution with cooling on an ice bath and then the resulting mixture was warmed up to room temperature. When ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCCN2
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
c1ccccc1.c1ccccc1.c1ccc2c(c1)CCCC[NH]2
HO-
ClCCl.O.C(C)N(CC)CC
null
1
COc1cc(C(=O)O)ccc1-c1ccccc1.O=C1CCCNc2ccccc21>ClCCl.O.C(C)N(CC)CC>COc1ccccc1-c1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-77372f28b5544f559aa1a847d124d17d
CC(C)c1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1.O>>Cc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3OC(C)C)cc1)CC2
O.[Br-].[Br-].[Br-].C1(=CC=CC=C1)[N+](C)(C)C.C1(=CC=CC=C1)[N+](C)(C)C.C1(=CC=CC=C1)[N+](C)(C)C.O1CCCC1.O=C1CCCN(C2=C1C=CC=C2)C(=O)C2=CC=C(NC(C1=C(C=CC=C1)C(C)C)=O)C=C2>>C(C)(C)OC1=C(C(=O)NC2=CC=C(C=C2)C(=O)N2CCC3=C(C4=C2C=CC=C4)NC(=N3)C)C=CC=C1
O=[C:5]1[CH2:4][CH2:36][CH2:35][N:13]([C:14](=[O:15])[c:16]2[cH:17][cH:18][c:19]([NH:20][C:21](=[O:22])[c:23]3[cH:24][cH:25][cH:26][cH:27][c:28]3[CH:30]([CH3:31])[CH3:32])[cH:33][cH:34]2)[c:12]2[c:7]1[cH:8][cH:9][cH:10][cH:11]2.[OH2:29]>>[CH3:1][c:2]1[n:3][c:4]2[c:5]([nH:6]1)-[c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[N:1...
CC(C)c1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1.O
Cc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3OC(C)C)cc1)CC2
null
null
null
Aromatic Heterocycle Formation
OtherReaction
8da4d93b70782d4182728790bbda24f41f058aac9ebd9ad8cc383fc60ea690aa
5e29fd0fa54248dfa34055e1e50bb98b692fd7998effad13ce7949bd843a9b7e
O=C(Nc1ccc(C(=O)N2CCc3nc[nH]c3-c3ccccc32)cc1)c1ccccc1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[#7:5](-[C:6]=[O;D1;H0:7])-[c:8](:[c:9]):[c;H0;D3;+0:10]-1:[c:11]:[c:12].[C;D1;H3:13]-[CH;D3;+0:14](-[C;D1;H3:15])-[c;H0;D3;+0:16](:[c:17]:[c:18]):[c:19](-[C:20](=[O;D1;H0:21])-[#7:22]-[c:23]):[c:24].[OH2;D0;+0:25]>>[C;D1;H3:13]-[CH;D3;+0:14](-[C;D1;H3:15])-[O;H0;D2;+0:25]-[c...
null
[]
null
null
60
MINUTE
With cooling on an ice bath, a 793 mg portion of phenyltrimethylammonium tribromide was added to 20 ml of tetrahydrofuran solution containing 1.0 g of 4'-[(5-oxo-2,3,4,5-tetrahydro1H-1-benzazepin-1-yl)carbonyl]-2-isopropylbenzanilide, and the mixture was warmed up to room temperature. Filtration was carried out when di...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ether
c1ccccc1.c1ccc2c(c1)CCCC[NH]2
c1ccccc1.c1ccc2c(c1)[NH]CCc1[nH]cnc12
c1ccccc1.c1ccccc1.c1ccc2c(c1)[NH]CCc1[nH]cnc12
null
null
null
1
CC(C)c1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(=O)c3ccccc32)cc1.O>>Cc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3OC(C)C)cc1)CC2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8d43c74a9d90473996cdace2ba79d6f8
Cl>>Cl
COC1=C(C=CC=C1)C1=CC=C(C=C1)C(=O)N1CCC2=C(C3=C1C=CC=C3)NC(=N2)C.Cl.C(C)(=O)OCC>>Cl.COC1=C(C=CC=C1)C1=CC=C(C=C1)C(=O)N1CCC2=C(C3=C1C=CC=C3)NC(=N2)C
[ClH:32]>>[ClH:32]
Cl
Cl
null
null
C(C)O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
6-[(2'-Methoxy-4-biphenylyl)carbonyl]-2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine was dissolved in 4.8 ml of ethyl alcohol, the solution was mixed with 0.44 ml of 4N hydrochloric acid-ethyl acetate and cooled on an ice bath to effect crystal formation, and then the thus formed crystals were collected by fil...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)O
null
null
Cl>C(C)O>Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d699a2fd0bfb49f2b2d9d51a6a3e6ab2
BrCCCCBr.CCOC(C)=O.N#CCc1ccccc1.O>>O=C(O)C1(c2ccccc2)CCCC1
C(C1=CC=CC=C1)C#N.BrCCCCBr.O.C(C)(=O)OCC>>C1(=CC=CC=C1)C1(CCCC1)C(=O)O
Br[CH2:11][CH2:12][CH2:13][CH2:14]Br.CCOC(C)=[O:1].N#[C:2][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1.[OH2:3]>>[O:1]=[C:2]([OH:3])[C:4]1([c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[CH2:11][CH2:12][CH2:13][CH2:14]1
BrCCCCBr.CCOC(C)=O.N#CCc1ccccc1.O
O=C(O)C1(c2ccccc2)CCCC1
null
null
O1CCCC1.[H-].[Na+]
Acylation
OtherReaction
598d21fce22d09c3bae94a7cf2d53009fcc10a866bc3741483fa873ad200cb91
3aba3ab6e23932b358809e97064fffaa9ac61a401ccbbd64df773b827e78c111
c1ccc(C2CCCC2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-Br.C-C-O-C(-C)=[O;H0;D1;+0:5].N#[C;H0;D2;+0:6]-[CH2;D2;+0:7]-[c:8](:[c:9]):[c:10].[OH2;D0;+0:11]>>[O;H0;D1;+0:5]=[C;H0;D3;+0:6](-[OH;D1;+0:11])-[C;H0;D4;+0:7]1(-[c:8](:[c:9]):[c:10])-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-1
null
[]
null
null
1
HOUR
In a stream of argon, 60% sodium hydride was dissolved in 10 ml of tetrahydrofuran, and the solution was mixed with 2.0 g of benzyl cyanide, stirred for 1 hour at room temperature, further mixed with 3.69 g of 1,4-dibromobutane and again stirred for 16 hours at room temperature. The reaction mixture was mixed with wate...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ester.Nitrile
Carboxylic acid
null
C1CCCC1
c1ccccc1.C1CCCC1
HBr
O1CCCC1.[H-].[Na+]
null
1
BrCCCCBr.CCOC(C)=O.N#CCc1ccccc1.O>O1CCCC1.[H-].[Na+]>O=C(O)C1(c2ccccc2)CCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a3bb18217e0f4155870b6f9c59379a87
CI.Cc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc([N+](=O)[O-])cc1)CC2>>Cc1nc2c(n1C)CCN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccc1-2
[H-].[Na+].O.[N+](=O)([O-])C1=CC=C(C(=O)N2CCC3=C(C4=C2C=CC=C4)NC(=N3)C)C=C1.CI>>[N+](=O)([O-])C1=CC=C(C(=O)N2CCC3=C(C4=C2C=CC=C4)N=C(N3C)C)C=C1
I[CH3:7].[CH3:1][c:2]1[n:3][c:4]2[c:5]([nH:6]1)-[c:27]1[c:22]([cH:23][cH:24][cH:25][cH:26]1)[N:10]([C:11](=[O:12])[c:13]1[cH:14][cH:15][c:16]([N+:17](=[O:18])[O-:19])[cH:20][cH:21]1)[CH2:9][CH2:8]2>>[CH3:1][c:2]1[n:3][c:4]2[c:5]([n:6]1[CH3:7])[CH2:8][CH2:9][N:10]([C:11](=[O:12])[c:13]1[cH:14][cH:15][c:16]([N+:17](=[O:1...
CI.Cc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc([N+](=O)[O-])cc1)CC2
Cc1nc2c(n1C)CCN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccc1-2
null
null
CN(C=O)C.C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
6567d10a77e90bdf51acf993b92a04165f271a5ae281eb951627268c7a6c60f6
7a358c636daddc97c1fb4c29f378044d7eac3f01815d9966e599841f642d631a
O=C(c1ccccc1)N1CCc2[nH]cnc2-c2ccccc21
I-[CH3;D1;+0:1].[C;D1;H3:2]-[c:3]1:[#7;a:4]:[c;H0;D3;+0:5]2:[c;H0;D3;+0:6](:[nH;D2;+0:7]:1)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](:[c:12])-[#7:13](-[C:14]=[O;D1;H0:15])-[C:16]-[CH2;D2;+0:17]-2>>[C;D1;H3:2]-[c:3]1:[#7;a:4]:[c;H0;D3;+0:5]2:[c;H0;D3;+0:6](:[n;H0;D3;+0:7]:1-[CH3;D1;+0:1])-[CH2;D2;+0:17]-[C:16]-[#7:13](-[C:1...
null
[]
null
null
1
HOUR
In a stream of argon, 144 mg of 60% sodium hydride was suspended in a small volume of N,N-dimethylformamide to which, with cooling on an ice bath, was then added dropwise a solution prepared by dissolving 500 mg of 6-(4-nitrobenzoyl)-2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine in 20 ml of N,N-dimethylformam...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccc2c(c1)[NH]CCc1[nH]cnc12
c1nc2c([nH]1)c1ccccc1NCC2
c1ccccc1.c1nc2c([nH]1)c1ccccc1NCC2
HI
CN(C=O)C.C(Cl)(Cl)Cl
null
1
CI.Cc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc([N+](=O)[O-])cc1)CC2>CN(C=O)C.C(Cl)(Cl)Cl>Cc1nc2c(n1C)CCN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccc1-2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b911c15a1a684981b9d7562f530a2f04
Cc1nc2c(n1C)CCN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccc1-2>>Cc1nc2c(n1C)CCN(C(=O)c1ccc(N)cc1)c1ccccc1-2
[N+](=O)([O-])C1=CC=C(C(=O)N2CCC3=C(C4=C2C=CC=C4)N=C(N3C)C)C=C1>>NC1=CC=C(C(=O)N2CCC3=C(C4=C2C=CC=C4)N=C(N3C)C)C=C1
O=[N+:17]([O-])[c:16]1[cH:15][cH:14][c:13]([C:11]([N:10]2[CH2:9][CH2:8][c:5]3[c:4]([n:3][c:2]([CH3:1])[n:6]3[CH3:7])-[c:25]3[c:20]2[cH:21][cH:22][cH:23][cH:24]3)=[O:12])[cH:19][cH:18]1>>[CH3:1][c:2]1[n:3][c:4]2[c:5]([n:6]1[CH3:7])[CH2:8][CH2:9][N:10]([C:11](=[O:12])[c:13]1[cH:14][cH:15][c:16]([NH2:17])[cH:18][cH:19]1)[...
Cc1nc2c(n1C)CCN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccc1-2
Cc1nc2c(n1C)CCN(C(=O)c1ccc(N)cc1)c1ccccc1-2
null
[C].[Pd]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C(c1ccccc1)N1CCc2[nH]cnc2-c2ccccc21
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A 1.421 g portion of 6-(4-nitrobenzoyl)-2,3-dimethyl-3,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine was dissolved in 50 ml of methyl alcohol, and the solution was mixed with 300 mg of palladium-carbon and subjected to hydrogenation under normal pressure. After completion of the hydrogen absorption, the reaction mixture...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1nc2c([nH]1)c1ccccc1NCC2
Other
[C].[Pd].CO
null
null
Cc1nc2c(n1C)CCN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccc1-2>[C].[Pd].CO>Cc1nc2c(n1C)CCN(C(=O)c1ccc(N)cc1)c1ccccc1-2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a12f514f3a754a2d8e08fdd22d30526b
CCOC(=O)Cc1cccc(Br)c1>>O=CCc1cccc(Br)c1
[H-].C(C(C)C)[Al+]CC(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
Compound G can be obtained as described in J. Med. Chem. 1995, 38, 4764-4767, and as shown in Reaction Scheme 1. Thus, referring now specifically to Reaction Scheme 1, ethyl 3-bromophenylacetate (Compound B, made by esterification of 3-bromophenylacetic acid) is reduced with diisobutylaluminum hydride (DIBAL H) to yiel...
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-b3dbd0407beb47cbade768f03604d785
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
Compound G can be obtained as described in J. Med. Chem. 1995, 38, 4764-4767, and as shown in Reaction Scheme 1. Thus, referring now specifically to Reaction Scheme 1, ethyl 3-bromophenylacetate (Compound B, made by esterification of 3-bromophenylacetic acid) is reduced with diisobutylaluminum hydride (DIBAL H) to yiel...
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-72b51fbb7ecd44859f1e2ed402ee2144
CC1(C)CCC(=O)c2cc(Br)ccc21.Sc1ccccc1>>CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21
C1(CCCC2CC=CC=C12)=O.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.C1(=CC=CC=C1)S.C1CC=CC2=CC=CC=C12>>CC1(CC=C(C2=CC(=CC=C12)Br)SC1=CC=CC=C1)C
O=[C: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.[SH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([S:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[c:14]2[cH:15][c:16]([Br:17])[cH:18][cH:19][c:20]21
CC1(C)CCC(=O)c2cc(Br)ccc21.Sc1ccccc1
CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21
null
[Ti](Cl)(Cl)(Cl)Cl
O1CCCC1.C(C)N(CC)CC
Heteroatom Alkylation and Arylation
OtherReaction
0ada3ae671ad3b060b96add65fbcfec1b731cae0a6c858eea87374516a4ac73a
f936d6b76ed560a8fec322bcfbbde18f0a579df08bd9baf16a1cafcec3158898
C1=C(Sc2ccccc2)c2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[SH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[c:10]:[c:9](-[S;H0;D2;+0:8]-[C;H0;D3;+0:1]1=[CH;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7]):[c:11]
null
[]
null
null
null
null
Reaction Scheme 3 provides further examples for the synthesis of compounds within the scope of Formula 5 where the linking group between the dihydronaphthalene moiety and the Y group is --CH=CH--. In the sequence of reactions described here the oxo function of a starting tetrahydronaphthalene-one moiety is modified bef...
10.6084/m9.figshare.5104873.v1
null
Ketone.Aromatic thiol
Monosulfide
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
c1ccccc1.C1=Cc2ccccc2CC1
HO-
[Ti](Cl)(Cl)(Cl)Cl.O1CCCC1.C(C)N(CC)CC
null
null
CC1(C)CCC(=O)c2cc(Br)ccc21.Sc1ccccc1>[Ti](Cl)(Cl)(Cl)Cl.O1CCCC1.C(C)N(CC)CC>CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-254a6649ca41404ba268a53b6dace89f
CCOC(=O)CBr.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1>>CCOC(=O)CC1(O)CCC(C)(C)c2ccc(/C=C/c3ccc(C(=O)OCC)cc3)cc21
C1CCCC2=CC=CC=C12.CC1(C=2C=CC(=CC2C(CC1)=O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.CC1(C=2C=CC(=CC2C(CC1)=O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.BrCC(=O)OCC.C1C(CCC2CC=CC=C12)=O>>CC1(C=2C=CC(=CC2C(CC1)(CC(=O)OCC)O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C
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][cH:16][c:17](/[CH:18]=[CH:19]/[c:20]3[cH:21][cH:22][c:23]([C:24](=[O:25])[O:26][CH2:27][CH3:28])[cH:29][cH:30]3)[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...
CCOC(=O)CBr.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1
CCOC(=O)CC1(O)CCC(C)(C)c2ccc(/C=C/c3ccc(C(=O)OCC)cc3)cc21
null
[Zn]
null
C-C Coupling
Grignard_alcohol
ae6802bc43630c235b581c1f69ee3f400dd59564bb5948df811879329723b99c
86d8e63c1eeb9e82c583fd2409352b28a569a3f780f9f297e86b8d2f688ca9d6
C(=C/c1ccc2c(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
Reaction Scheme 5 discloses another example for the preparation of compounds within the scope of Formula 3. In this example the substituent is introduced to replace the oxo function of tetrahydronaphthalene-2-one after the Z--Y(R2)--A--B group has already been coupled to the tetrahydronaphthalene nucleus. Thus, ethyl(E...
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]
null
null
CCOC(=O)CBr.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1>[Zn]>CCOC(=O)CC1(O)CCC(C)(C)c2ccc(/C=C/c3ccc(C(=O)OCC)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-35d47ce82ae748faaaaa6e03a0967fb0
CC(C)(C)[Si](C)(C)Cl.CC1(C)CCC(O)c2cc(Br)ccc21>>CC1(C)CCC(O[Si](C)(C)C(C)(C)C)c2cc(Br)ccc21
BrC=1C=C2C(CCC(C2=CC1)(C)C)O.[Si](C)(C)(C(C)(C)C)Cl>>BrC=1C=C2C(CCC(C2=CC1)(C)C)O[Si](C)(C)C(C)(C)C
Cl[Si:8]([CH3:9])([CH3:10])[C:11]([CH3:12])([CH3:13])[CH3:14].[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH:6]([OH:7])[c:15]2[cH:16][c:17]([Br:18])[cH:19][cH:20][c:21]21>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH:6]([O:7][Si:8]([CH3:9])([CH3:10])[C:11]([CH3:12])([CH3:13])[CH3:14])[c:15]2[cH:16][c:17]([Br:18])[cH:19][cH:20][c:2...
CC(C)(C)[Si](C)(C)Cl.CC1(C)CCC(O)c2cc(Br)ccc21
CC1(C)CCC(O[Si](C)(C)C(C)(C)C)c2cc(Br)ccc21
null
null
null
Protection
Alcohol protection with silyl ethers
e19079a85b3e2f818dbb25a774b915f0e7349126f5b76d72c22f1c90edfa8480
16de9d9d08d1cc67ec96e76fc213a6b49c0af7979ac901a377ee705ba5071899
c1ccc2c(c1)CCCC2
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7].[C:8]-[C:9](-[OH;D1;+0:10])-[c:11]>>[C:8]-[C:9](-[O;H0;D2;+0:10]-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;D1;H3:7])-[c:11]
null
[]
null
null
null
null
Continuing on with the description of Reaction Scheme 6, 6-bromo-1,2,3,4-tetrahydro-1,1-dimethyl-4-hydroxynaphthalene is reacted in the presence of base with t-butyldimethylsilyl chloride to provide 6-bromo-1,2,3,4-tetrahydro-1,1-dimethyl-4-(t-butyldimethylsilyloxy)naphthalene (Compound B15). The starting 6-bromo-1,2,3...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Silyl protective group
TMS ether protective group
null
null
c1ccc2c(c1)CCCC2
HCl
null
null
null
CC(C)(C)[Si](C)(C)Cl.CC1(C)CCC(O)c2cc(Br)ccc21>>CC1(C)CCC(O[Si](C)(C)C(C)(C)C)c2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d320d86af6964f16a5a4454d35f645dc
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O[Si](C)(C)C(C)(C)C)CCC4(C)C)ccc2c1>>CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1
CC1(C=2C=CC(=CC2C(CC1)O[Si](C)(C)C(C)(C)C)C=1C=C2C=CC(=CC2=CC1)C(=O)OCC)C.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>CC1(C=2C=CC(=CC2C(CC1)O)C=1C=C2C=CC(=CC2=CC1)C(=O)OCC)C
CC(C)(C)[Si](C)(C)[O:19][CH:18]1[c:16]2[c:15]([cH:14][cH:13][c:12](-[c:11]3[cH:10][c:9]4[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:28][c:27]4[cH:26][cH:25]3)[cH:17]2)[C:22]([CH3:23])([CH3:24])[CH2:21][CH2:20]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]2[cH:10][c:11](-[c:12]3[cH:13][cH:14][c:15...
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O[Si](C)(C)C(C)(C)C)CCC4(C)C)ccc2c1
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1
null
null
null
Deprotection
Alcohol deprotection from silyl ethers
050b4fb4e1e9936189860d27dded10ae70a294a642c52f800eb9d5aaef7955cc
88623e19d23cdfe8e1a4c167fd6cfc51d774a1c784b87a7bb2df8153ee93e67a
c1ccc2cc(-c3ccc4c(c3)CCCC4)ccc2c1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2](-[C:3])-[c:4]>>[C:3]-[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
null
null
Continuing on with the description of Reaction Scheme 6, 6-bromo-1,2,3,4-tetrahydro-1,1-dimethyl-4-hydroxynaphthalene is reacted in the presence of base with t-butyldimethylsilyl chloride to provide 6-bromo-1,2,3,4-tetrahydro-1,1-dimethyl-4-(t-butyldimethylsilyloxy)naphthalene (Compound B15). The starting 6-bromo-1,2,3...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group
Secondary alcohol
null
null
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
Other
null
null
null
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O[Si](C)(C)C(C)(C)C)CCC4(C)C)ccc2c1>>CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-36cb55ed95f3473c9784f61cd4f7575f
CC1(C)CCC(=O)c2cc(Br)ccc21.C[C](C)(C)[Mg][Cl]>>CC(C)(C)C1=CCC(C)(C)c2ccc(Br)cc21
C1(=CC=C(C=C1)S(=O)(=O)O)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.C(C)(C)(C)[Mg]Cl>>BrC1=CC=C2C(CC=C(C2=C1)C(C)(C)C)(C)C
O=[C:5]1[CH2:6][CH2:7][C:8]([CH3:9])([CH3:10])[c:11]2[cH:12][cH:13][c:14]([Br:15])[cH:16][c:17]21.[Cl][Mg][C:2]([CH3:1])([CH3:3])[CH3:4]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]1=[CH:6][CH2:7][C:8]([CH3:9])([CH3:10])[c:11]2[cH:12][cH:13][c:14]([Br:15])[cH:16][c:17]21
CC1(C)CCC(=O)c2cc(Br)ccc21.C[C](C)(C)[Mg][Cl]
CC(C)(C)C1=CCC(C)(C)c2ccc(Br)cc21
null
null
O1CCCC1
C-C Coupling
OtherReaction
cad3ebb460626e0b3c0c5e79b5d003dc2c6720d4441d1a3b1dd15d07bbe3c73a
6765e06b4fce5c2cc632b64cfcd2cebf695ba9495ab888b1531784cd07e6e026
C1=Cc2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[C;D1;H3:8]-[C;H0;D4;+0:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[Mg]-[Cl]>>[C;D1;H3:8]-[C;H0;D4;+0:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;H0;D3;+0:1]1=[CH;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7]
null
[]
null
null
null
null
Reaction Scheme 9 discloses the preferred method of synthesis of a starting material from which certain examples for compounds of the invention within the scope of Formula 6 are preferably made. In accordance with this scheme 7-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound G) is reacted with t-butylmagne...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Ketone
null
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HCl.Mg
O1CCCC1
null
null
CC1(C)CCC(=O)c2cc(Br)ccc21.C[C](C)(C)[Mg][Cl]>O1CCCC1>CC(C)(C)C1=CCC(C)(C)c2ccc(Br)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-40f1c896966e44febe91ff5b043dfe79
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+]>>C(C)OC(CC1=CC=C(C=C1)Br)=O
[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-f9d9123ba1f04c7494e0e6ceb5f56621
CCOC(=O)Cc1ccc(Br)cc1.O=C(O)Cc1cccc(Br)c1>>CCOC(=O)Cc1cccc(Br)c1
C(C)OC(CC1=CC=C(C=C1)Br)=O.C(C)OC(CC1=CC=C(C=C1)Br)=O.BrC=1C=C(C=CC1)CC(=O)O>>C(C)OC(CC1=CC(=CC=C1)Br)=O
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. PMR (CDCl3): δ 1.26 (3H, t, J=7.0 Hz), 3.56 (2H, s), 4.16 (2H, q, J=7.0...
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-2d92d9e8c6e2432b8ddf16f2363dcbf0
CCOC(=O)Cc1ccc(Br)cc1>>O=CCc1ccc(Br)cc1
[H-].C(C(C)C)[Al+]CC(C)C.C(C)OC(CC1=CC=C(C=C1)Br)=O.C(C)OC(CC1=CC=C(C=C1)Br)=O.[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 diisobutylaluminum hydride (DIBAL-H, 1M solution in hexane). After the DIBAL-H addition was complete, the reaction was stirred at -78° C. for an ad...
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-dfb925c910634ae6a49615162b2da243
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 diisobutylaluminum hydride (DIBAL-H, 1M solution in hexane). After the DIBAL-H addition was complete, the reaction was stirred at -78° C. for an ad...
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-fd88e66de55049f7ad9914c5bfbadd5a
CCOC(=O)CCCc1ccc(Br)cc1.CCOC(=O)Cc1cccc(Br)c1>>CCOC(=O)CCCc1cccc(Br)c1
C(C)OC(CCCC1=CC=C(C=C1)Br)=O.C(C)OC(CCCC1=CC=C(C=C1)Br)=O.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 ethyl4-(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 diisobutylaluminum hydride (DIBAL-H, 1M in hexane), 85.8 g (250 mmol) of (carbethoxyme...
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-cfa73652b7a144b88fc260b76438c1a1
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-tetrahydro-1,1-dimethylnaphthalene (Compound F) in 125 ml of benzene. The reaction mixture was stirred for 1 hour, que...
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-6185c04dffd4470aa6c626e04baee724
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1cscn1>>CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(c2nccs2)=CCC3(C)C)cc1
S1C=NC=C1.C(CCC)[Li].[NH4+].[Cl-].CC1(C=2C=CC(=CC2C(=CC1)OS(=O)(=O)C(F)(F)F)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.CC1(C=2C=CC(=CC2C(=CC1)OS(=O)(=O)C(F)(F)F)/C=C/C1=CC=C(C(=O)OCC)C=C1)C>>CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CN1)/C=C/C1=CC=C(C(=O)OCC)C=C1)C
O=S(=O)(O[C:18]1=[CH:24][CH2:25][C:26]([CH3:27])([CH3:28])[c:15]2[cH:14][cH:13][c:12](/[CH:11]=[CH:10]/[c:9]3[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:30][cH:29]3)[cH:17][c:16]21)C(F)(F)F.[cH:19]1[n:20][cH:21][cH:22][s:23]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](/[CH:10]=[CH:11]/[c:12]2[c...
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1cscn1
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(c2nccs2)=CCC3(C)C)cc1
null
[Cl-].[Zn+2].[Cl-].C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
C1CCOC1.O1CCCC1
C-C Coupling
OtherReaction
eaab030020d56665bc4d9779272e990b86f74e43fc7c76c6cb4d4209c9406879
253c3b9fccee9bf420e0fb1f267e37bad5aa0c206427cb57447e420babcc09c8
C1=C(c2nccs2)c2cc(/C=C/c3ccccc3)ccc2CC1
F-C(-F)(-F)-S(=O)(=O)-O-[C;H0;D3;+0:1](=[C:2]-[C:3])-[c:4](:[c:5]):[c:6].[#16;a:7]1:[c:8]:[c:9]:[#7;a:10]:[cH;D2;+0:11]:1>>[C:3]-[C:2]=[C;H0;D3;+0:1](-[c;H0;D3;+0:11]1:[#16;a:7]:[c:8]:[c:9]:[#7;a:10]:1)-[c:4](:[c:5]):[c:6]
null
[]
null
null
30
MINUTE
To a cold (-78° C.) solution of thiazole (0.38 g (0.10 mL, 1.4 mmol) in THF (2.0 mL) was added n-butyl lithium (1.6M solution in hexanes, 0.5 mL, 0.8 mmol) and stirred for 30 min. To this solution was added 0.176 g (1.3 mmol) of zinc chloride in 3.0 mL of tetrahydrofuran and stirred for 45 min. The resulting turbid sol...
10.6084/m9.figshare.5104873.v1
null
Triflate
null
C1=Cc2ccccc2CC1.c1cscn1
c1cscn1.C1=Cc2ccccc2CC1
c1ccccc1.c1cscn1.C1=Cc2ccccc2CC1
TfOH.HO-
[Cl-].[Zn+2].[Cl-].C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1CCOC1.O1CCCC1
null
0.5
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1cscn1>[Cl-].[Zn+2].[Cl-].C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1CCOC1.O1CCCC1>CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(c2nccs2)=...
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-833ae973b3214608bac2a8fbd227ff25
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1ccsc1>>CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(c2cccs2)=CCC3(C)C)cc1.[Li][c]1cccs1
CC1(C=2C=CC(=CC2C(=CC1)OS(=O)(=O)C(F)(F)F)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.CC1(C=2C=CC(=CC2C(=CC1)OS(=O)(=O)C(F)(F)F)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.S1C=CC=C1.C(CCC)[Li]>>[Li]C=1SC=CC1.CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)/C=C/C1=CC=C(C(=O)OCC)C=C1)C
O=[S:23](=O)(O[C:18]1=[CH:24][CH2:25][C:26]([CH3:27])([CH3:28])[c:15]2[cH:14][cH:13][c:12](/[CH:11]=[CH:10]/[c:9]3[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:30][cH:29]3)[cH:17][c:16]21)[C:19](F)(F)F.CC1(C)CC=C(OS(=O)(=O)C(F)(F)F)c2cc(/C=C/c3ccc(C(=O)O[CH2:22][CH3:21])c[cH:20]3)ccc21.[cH:32]1[cH:33][cH:34][c...
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1ccsc1
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(c2cccs2)=CCC3(C)C)cc1.[Li][c]1cccs1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.[Cl-].[Zn+2].[Cl-]
O1CCCC1
C-C Coupling
OtherReaction
3ab4abadd4882aae99f9c2cd26eb7fcdba47688026b16b611ccf1d84a12340e9
94f8d63ba54e5b4480bbb52ffd8b132aaa72b3e60c8cdc4274bdef82a5ac73e2
C1=C(c2cccs2)c2cc(/C=C/c3ccccc3)ccc2CC1.c1ccsc1
C-C1(-C)-C-C=C(-O-S(=O)(=O)-C(-F)(-F)-F)-c2:c:c(/C=C/c3:[cH;D2;+0:1]:c:c(-C(=O)-O-[CH2;D2;+0:2]-[CH3;D1;+0:3]):c:c:3):c:c:c:2-1.F-[C;H0;D4;+0:4](-F)(-F)-[S;H0;D4;+0:5](=O)(=O)-O-[C;H0;D3;+0:6](=[C:7]-[C:8])-[c:9](:[c:10]):[c:11].[#16;a:12]1:[c:13]:[c:14]:[c:15]:[cH;D2;+0:16]:1>>[C:8]-[C:7]=[C;H0;D3;+0:6](-[c;H0;D3;+0:4...
null
[]
-78
CELSIUS
35
MINUTE
A solution of lithiothiophene was prepared by the addition of 0.10 g (0.095 mL, 1.2 mmol) of thiophene to a cold solution (-78° C.) of 0.61 g (0.90 mL, 1.4 mmol, 1.6M in hexanes) of n-butyl lithium in 2.0 mL of tetrahydrofuran. The solution was stirred at -78° C. for 35 min and then a solution of 0.158 g (1.2 mmol) of ...
10.6084/m9.figshare.5104873.v1
null
Triflate.Triflate.Ester
Aryl lithium
C1=Cc2ccccc2CC1.C1=Cc2ccccc2CC1.c1ccccc1.c1ccsc1
c1ccsc1.C1=Cc2ccccc2CC1.c1ccsc1
c1ccccc1.c1ccsc1.C1=Cc2ccccc2CC1.c1ccsc1
TfOH.HO-
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.[Cl-].[Zn+2].[Cl-].O1CCCC1
-78
0.583333
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1ccsc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.[Cl-].[Zn+2...
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6359f090cbac49c6a126e41999e4f8b9
C=Cc1ccc(C(=O)OCC)cc1.CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21>>CCOC(=O)c1ccc(/C=C/c2cccc3c2C(Sc2ccccc2)=CCC3(C)C)cc1
BrC1=CC=2C(=CCC(C2C=C1)(C)C)SC1=CC=CC=C1.C(=C)C1=CC=C(C(=O)OCC)C=C1.C1(=C(C=CC=C1)P(C1=C(C=CC=C1)C)C1=C(C=CC=C1)C)C>>CC1(C=2C=CC=C(C2C(=CC1)SC1=CC=CC=C1)/C=C/C1=CC=C(C(=O)OCC)C=C1)C
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([CH:10]=[CH2:11])[cH:31][cH:32]1.Br[c:13]1[cH:12][c:17]2[c:16]([cH:15][cH:14]1)[C:28]([CH3:29])([CH3:30])[CH2:27][CH:26]=[C:18]2[S:19][c:20]1[cH:21][cH:22][cH:23][cH:24][cH:25]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](/[CH:10]=[CH:11]/[c:12]2[cH:1...
C=Cc1ccc(C(=O)OCC)cc1.CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21
CCOC(=O)c1ccc(/C=C/c2cccc3c2C(Sc2ccccc2)=CCC3(C)C)cc1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
C(C)N(CC)CC
C-C Coupling
OtherReaction
d6db5010b59f0381092da76cd6769358edce2251432e88a0ee3eec12ec5f513f
4b186811a4930853b446d93d9faa39b267bddb9ce0b8021bda5c5a3b2bc69f0b
C1=C(Sc2ccccc2)c2c(/C=C/c3ccccc3)cccc2CC1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5](:[cH;D2;+0:6]:1)-[C:7](-[#16:8])=[C:9]-[C:10].[CH2;D1;+0:11]=[C:12]-[c:13]>>[#16:8]-[C:7](=[C:9]-[C:10])-[c:5]1:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:[c;H0;D3;+0:6]:1/[CH;D2;+0:11]=[C:12]/[c:13]
null
[]
90
CELSIUS
null
null
To a degassed solution of 0.35 g (1.0 mmol) of 2-bromo-5,6-dihydro-5,5-dimethyl-8-(phenylthio)-naphthalene (Compound A35) and 0.34 g (1.9 mmol) of ethyl 4-vinylbenzoate in 4.0 mL of triethylamine, was added 0.066 g (0.2 mmol) of tri-o-tolylphosphine and then 0.025 g (0.1 mmol) of palladium(II) acetate. The reaction was...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Vinyl
null
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
c1ccccc1.c1ccccc1.C1=Cc2ccccc2CC1
HBr
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(C)N(CC)CC
90
null
C=Cc1ccc(C(=O)OCC)cc1.CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(C)N(CC)CC>CCOC(=O)c1ccc(/C=C/c2cccc3c2C(Sc2ccccc2)=CCC3(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b1bd58830652436484aeb0d21b29efe6
C=Cc1ccc(C(=O)OCC)cc1.CCSC1=CCC(C)(C)c2ccc(Br)cc21>>CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(SCC)=CCC3(C)C)cc1
BrC1=CC=2C(=CCC(C2C=C1)(C)C)SCC.C(=C)C1=CC=C(C(=O)OCC)C=C1.C1(=C(C=CC=C1)P(C1=C(C=CC=C1)C)C1=C(C=CC=C1)C)C>>CC1(C=2C=CC(=CC2C(=CC1)SCC)/C=C/C1=CC=C(C(=O)OCC)C=C1)C
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([CH:10]=[CH2:11])[cH:27][cH:28]1.Br[c:12]1[cH:13][cH:14][c:15]2[c:16]([cH:17]1)[C:18]([S:19][CH2:20][CH3:21])=[CH:22][CH2:23][C:24]2([CH3:25])[CH3:26]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9](/[CH:10]=[CH:11]/[c:12]2[cH:13][cH:14][c:15]3[c:16]([cH:...
C=Cc1ccc(C(=O)OCC)cc1.CCSC1=CCC(C)(C)c2ccc(Br)cc21
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(SCC)=CCC3(C)C)cc1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
C(C)N(CC)CC
C-C Coupling
Heck terminal vinyl
d6db5010b59f0381092da76cd6769358edce2251432e88a0ee3eec12ec5f513f
4b186811a4930853b446d93d9faa39b267bddb9ce0b8021bda5c5a3b2bc69f0b
C1=Cc2cc(/C=C/c3ccccc3)ccc2CC1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]-[C:6]=[C:7].[CH2;D1;+0:8]=[C:9]-[c:10]>>[C:7]=[C:6]-[c:5]:[c:4]:[c;H0;D3;+0:1](/[CH;D2;+0:8]=[C:9]/[c:10]):[c:2]:[c:3]
null
[]
90
CELSIUS
null
null
To a degassed solution of 0.50 g (1.7 mmol) of 2-bromo-5,6-dihydro-5,5-dimethyl-8-(ethylthio)-naphthalene (Compound A36) and 0.45 g (2.5 mmol) of ethyl 4-vinylbenzoate in 4.0 mL of triethylamine, was added 109 mg (0.36 mmol) of tri-o-tolylphosphine and then 35 mg (0.16 mmol) of palladium(II) acetate. The reaction was h...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Vinyl
null
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
c1ccccc1.C1=Cc2ccccc2CC1
HBr
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(C)N(CC)CC
90
null
C=Cc1ccc(C(=O)OCC)cc1.CCSC1=CCC(C)(C)c2ccc(Br)cc21>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(C)N(CC)CC>CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(SCC)=CCC3(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ccd6fb9e203040fbbcdbd667f32b7bf3
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.SCCCS>>CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(C2SCCCS2)CCC3(C)C)cc1
CC1(C=2C=CC(=CC2C(CC1)=O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.CC1(C=2C=CC(=CC2C(CC1)=O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.C(CCS)S.C(Cl)Cl>>CC1(C=2C=CC(=CC2C(CC1)C1SCCCS1)/C=C/C1=CC=C(C(=O)OCC)C=C1)C
O=[C:18]1[c:16]2[c:15]([cH:14][cH:13][c:12](/[CH:11]=[CH:10]/[c:9]3[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:31][cH:30]3)[cH:17]2)[C:27]([CH3:28])([CH3:29])[CH2:26][CH2:25]1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)[C:19](=O)CCC3(C)C)cc1.[SH:20][CH2:21][CH2:22][CH2:23][SH:24]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[c...
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.SCCCS
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(C2SCCCS2)CCC3(C)C)cc1
null
null
C([O-])([O-])=O.[K+].[K+]
Heteroatom Alkylation and Arylation
OtherReaction
64dafd51f6e96d2f44dadf0a6d95a9dbc5cf350f99e7383f9b372b1304b1e932
da72bab5ffc932eb295072267fea429a9d06ee1d767d90827ba9b07cdc2bf904
C(=C/c1ccc2c(c1)C(C1SCCCS1)CCC2)\c1ccccc1
C-C-O-C(=O)-c1:c:c:c(/C=C/c2:c:c:c3:c(:c:2)-[C;H0;D3;+0:1](=O)-C-C-C-3(-C)-C):c:c:1.O=[C;H0;D3;+0:2](-[C:3]-[C:4])-[c:5](:[c:6]):[c:7].[SH;D1;+0:8]-[C:9]-[C:10]-[C:11]-[SH;D1;+0:12]>>[C:4]-[C:3]-[CH;D3;+0:2](-[CH;D3;+0:1]1-[S;H0;D2;+0:8]-[C:9]-[C:10]-[C:11]-[S;H0;D2;+0:12]-1)-[c:5](:[c:6]):[c:7]
null
[]
null
null
4
HOUR
To a cold solution (0° C.) of 140 mg (0.40 mmol) of ethyl(E)-4-[2-(5,5-dimethyl-5,6,-dihydro-naphthalen-8(7H)-one-2-yl)ethenyl]-benzoate (Compound A2), in 6.0 mL of methylene chloride was added dropwise 130 mg (0.12 mL, 1.2 mmol) of 1,3-propanedithiol and 0.17 g (0.15 mL, 102 mmol) of borontrifluoride diethyl etherate....
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Ester.Aliphatic thiol.Aliphatic thiol
Monosulfide.Monosulfide
c1ccc2c(c1)CCCC2.c1ccccc1.c1ccc2c(c1)CCCC2
C1CSCSC1.c1ccc2c(c1)CCCC2
c1ccccc1.C1CSCSC1.c1ccc2c(c1)CCCC2
HO-
C([O-])([O-])=O.[K+].[K+]
null
4
CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.SCCCS>C([O-])([O-])=O.[K+].[K+]>CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(C2SCCCS2)CCC3(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-223a80a8841041078a01144bb56456f4
CCOC(=O)CBr.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1>>CCCOC(=O)C1(O)CCC(C)(C)c2ccc(/C=C/c3ccc(C(=O)OCC)cc3)cc21
CC1(C=2C=CC(=CC2C(CC1)=O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.CC1(C=2C=CC(=CC2C(CC1)=O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C.C1=CC=CC=C1.C1=CC=CC=C1.BrCC(=O)OCC>>CC1(C=2C=CC(=CC2C(CC1)(C(=O)OCCC)O)/C=C/C1=CC=C(C(=O)OCC)C=C1)C
Br[CH2:7][C:5]([O:4][CH2:3][CH3:2])=[O:6].O=C1[CH2:9][CH2:10][C:11]([CH3:12])([CH3:13])[c:14]2[cH:15][cH:16][c:17](/[CH:18]=[CH:19]/[c:20]3[cH:21][cH:22][c:23]([C:24](=[O:25])[O:26][CH2:27][CH3:28])[cH:29][cH:30]3)[cH:31][c:32]21.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=[O:8])CCC3(C)C)cc1>>[CH3:1][CH2:2][CH2:3][O:4][C:5](=[O:6...
CCOC(=O)CBr.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1
CCCOC(=O)C1(O)CCC(C)(C)c2ccc(/C=C/c3ccc(C(=O)OCC)cc3)cc21
null
[Zn]
null
Heteroatom Alkylation and Arylation
OtherReaction
e9daa679284560e3818bb78145ca809068888d6601447cd2e1942192e8d7b935
0d4b3a07af04e7d8299f6f866f25c8b805b051e483ac6e2127853c0cc486c00a
C(=C/c1ccc2c(c1)CCCC2)\c1ccccc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5]-[CH3;D1;+0:6].C-C-O-C(=O)-c1:c:c:c(/C=C/c2:c:c:c3:c(:c:2)-C(=[O;H0;D1;+0:7])-C-C-C-3(-C)-C):c:c:1.O=C1-[CH2;D2;+0:8]-[C:9]-[C:10]-[c:11](:[c:12]):[c;H0;D3;+0:13]-1:[c:14]:[c:15]/[C:16]=[C:17]>>[C:17]=[C:16]/[c:15]:[c:14]:[c;H0;D3;+0:13]1:[c:11](:[c:12])-[C:10]-[C:9]-[CH...
null
[]
null
null
null
null
To a refluxing solution of 0.75 g (11.5 mmol) of granular zinc in 5.0 mL of benzene was added a solution of ethyl(E)-4-[2-(5,5-dimethyl-5,6,-dihydro-naphthalen-8(7H)-one-2-yl)ethenyl]-benzoate (Compound A2) in 5.0 mL of benzene followed by 0.27 g (0.18 mmol) of ethyl bromoacetate. The resulting mixture was refluxed for...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Ketone.Ester.Ester
Ester.Tertiary alcohol
c1ccc2c(c1)CCCC2.c1ccccc1.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2.c1ccccc1
HBr
[Zn]
null
null
CCOC(=O)CBr.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1.CCOC(=O)c1ccc(/C=C/c2ccc3c(c2)C(=O)CCC3(C)C)cc1>[Zn]>CCCOC(=O)C1(O)CCC(C)(C)c2ccc(/C=C/c3ccc(C(=O)OCC)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-becf0ee7c3024fadba4ea32c31403111
CC1(C)CCC(=O)c2cc(Br)ccc21.Sc1ccccc1>>CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21
BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.C1CCOC1.C1(=CC=CC=C1)S.C(C)N(CC)CC.C1CCOC1>>CC1(CC=C(C2=CC(=CC=C12)Br)SC1=CC=CC=C1)C
O=[C: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.[SH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([S:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[c:14]2[cH:15][c:16]([Br:17])[cH:18][cH:19][c:20]21
CC1(C)CCC(=O)c2cc(Br)ccc21.Sc1ccccc1
CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21
null
[Ti](Cl)(Cl)(Cl)Cl
O
Heteroatom Alkylation and Arylation
OtherReaction
0ada3ae671ad3b060b96add65fbcfec1b731cae0a6c858eea87374516a4ac73a
f936d6b76ed560a8fec322bcfbbde18f0a579df08bd9baf16a1cafcec3158898
C1=C(Sc2ccccc2)c2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[SH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[c:10]:[c:9](-[S;H0;D2;+0:8]-[C;H0;D3;+0:1]1=[CH;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7]):[c:11]
null
[]
null
null
5
HOUR
To a stirred solution of 4,4-dimethyl-7-bromo-3,4-dihydronaphthalen-1(2H)one (Compound G, 1.48 g, 5.9 mmol), titanium tetrachloride (1.09 g, 5.7 mmol) and THF (10 mL) was added a mixture of thiophenol (660 mg, 6 mmol), triethylamine (1.16 g, 11.5 mmol) and THF (20 mL) via an addition funnel at ambient temperature. The ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Aromatic thiol
Monosulfide
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
c1ccccc1.C1=Cc2ccccc2CC1
HO-
[Ti](Cl)(Cl)(Cl)Cl.O
null
5
CC1(C)CCC(=O)c2cc(Br)ccc21.Sc1ccccc1>[Ti](Cl)(Cl)(Cl)Cl.O>CC1(C)CC=C(Sc2ccccc2)c2cc(Br)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-afbd95ad9dd44e7e978ad560efb01622
CC1(C)CCC(=O)c2cc(Br)ccc21.CCS>>CCSC1=CCC(C)(C)c2ccc(Br)cc21
BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.C(C)S.C(C)N(CC)CC>>BrC1=CC=2C(=CCC(C2C=C1)(C)C)SCC
O=[C: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][CH2:2][SH:3]>>[CH3:1][CH2:2][S:3][C:4]1=[CH: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(=O)c2cc(Br)ccc21.CCS
CCSC1=CCC(C)(C)c2ccc(Br)cc21
null
[Ti](Cl)(Cl)(Cl)Cl
O.O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
bda6e7a342b4c92698d6328240364017658687b3f6d783caade4c130bf5f7284
643de5ae757bb3e6c9835c2c9ec31b7c88e55e46a044a7a875bb5d5888cf6cf3
C1=Cc2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[C;D1;H3:8]-[C:9]-[SH;D1;+0:10]>>[C;D1;H3:8]-[C:9]-[S;H0;D2;+0:10]-[C;H0;D3;+0:1]1=[CH;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7]
null
[]
null
null
10
MINUTE
To a solution of 1.03 g (4.1 mmol) of 7-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound G) in 30.0 mL of tetrahydrofuran, was added dropwise 0.49 g (0.85 mL, 7.8 mmol) of titaniumtetrachloride and the resulting solution stirred for 10 min. A solution of 35 mg (0.50 mL, 6.7 mmol) of ethanethiol and 0.54 g (...
10.6084/m9.figshare.5104873.v1
null
Ketone.Aliphatic thiol
Monosulfide
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HO-
[Ti](Cl)(Cl)(Cl)Cl.O.O1CCCC1
null
0.166667
CC1(C)CCC(=O)c2cc(Br)ccc21.CCS>[Ti](Cl)(Cl)(Cl)Cl.O.O1CCCC1>CCSC1=CCC(C)(C)c2ccc(Br)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-97b20453788c4bc8828b820164729c18
CC1(C)CCCc2cc(B(O)O)ccc21.CCOC(=O)c1ccc2cc(Br)ccc2c1>>CCOC(=O)c1ccc2cc(C3Cc4ccccc4C(C)(C)C3)ccc2c1
C(C)(=O)OCC.BrC=1C=C2C=CC(=CC2=CC1)C(=O)OCC.C1(=CC=CC=C1)C.CC1(C=2C=CC(=CC2CCC1)B(O)O)C>>C(C)OC(=O)C1=CC2=CC=C(C=C2C=C1)C1CC(C=2C=CC=CC2C1)(C)C
OB(O)[c:16]1[cH:15][c:14]2[c:19]([cH:18][cH:17]1)[C:20]([CH3:21])([CH3:22])[CH2:23][CH2:12][CH2:13]2.Br[c:11]1[cH:10][c:9]2[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:27][c:26]2[cH:25][cH:24]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]2[cH:10][c:11]([CH:12]3[CH2:13][c:14]4[cH:15][cH:16][cH:17][...
CC1(C)CCCc2cc(B(O)O)ccc21.CCOC(=O)c1ccc2cc(Br)ccc2c1
CCOC(=O)c1ccc2cc(C3Cc4ccccc4C(C)(C)C3)ccc2c1
null
null
C([O-])([O-])=O.[Na+].[Na+].CCCCCC.CO.C(=O)([O-])[O-].[Na+].[Na+]
C-C Coupling
OtherReaction
8c1ecf349dc0cac2cc32df7a1092f55021e4e4a0fc1edd7e41af351130e7178a
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc2c(c1)CCC(c1ccc3ccccc3c1)C2
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].O-B(-O)-[c;H0;D3;+0:6](:[c:7]:[c:8]-[C:9]-[CH2;D2;+0:10]-[C:11]-[C:12]):[c:13]:[c:14]>>[C:12]-[C:11]-[CH;D3;+0:10](-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5])-[C:9]-[c:8]:[c:7]:[cH;D2;+0:6]:[c:13]:[c:14]
null
[]
80
CELSIUS
null
null
To a degassed solution of 0.39 g (1.4 mmol) of ethyl 6-bromo-naphthalene-2-carboxylate and 3.0 mL of toluene, was added sequentially 49 mg (0.04 mmol) of tetrakis-triphenylphosphine palladium(0), 2.0 mL (2.0 mmol) of 1M sodium carbonate and then a solution of 0.32 g (1.6 mmol) of (5,6,7,8-tetrahydro-5,5-dimethylnaphth-...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccc2c(c1)CCCC2.c1ccc2ccccc2c1
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
HBr.B
C([O-])([O-])=O.[Na+].[Na+].CCCCCC.CO.C(=O)([O-])[O-].[Na+].[Na+]
80
null
CC1(C)CCCc2cc(B(O)O)ccc21.CCOC(=O)c1ccc2cc(Br)ccc2c1>C([O-])([O-])=O.[Na+].[Na+].CCCCCC.CO.C(=O)([O-])[O-].[Na+].[Na+]>CCOC(=O)c1ccc2cc(C3Cc4ccccc4C(C)(C)C3)ccc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9be964bec0914ee8a55f4080f106b48c
CC1(C)CCC(O[Si](C)(C)C(C)(C)C)c2cc(B(O)O)ccc21.CCOC(=O)c1cccc2cc(Br)ccc12>>CCOC(=O)c1ccc2cc(C3CC(C)(C)c4ccccc4C3O[Si](C)(C)C(C)(C)C)ccc2c1
CC1(C=2C=CC(=CC2C(CC1)O[Si](C)(C)C(C)(C)C)B(O)O)C.BrC=1C=C2C=CC=C(C2=CC1)C(=O)OCC.C([O-])([O-])=O.[Na+].[Na+].C1(=CC=CC=C1)C>>C(C)OC(=O)C1=CC2=CC=C(C=C2C=C1)C1CC(C=2C=CC=CC2C1O[Si](C)(C)C(C)(C)C)(C)C
OB(O)[c:20]1[cH:19][cH:18][c:17]2[c:22]([cH:21]1)[CH:23]([O:24][Si:25]([CH3:26])([CH3:27])[C:28]([CH3:29])([CH3:30])[CH3:31])[CH2:12][CH2:13][C:14]2([CH3:15])[CH3:16].Br[c:11]1[cH:10][c:9]2[c:34]([c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:7][cH:8][cH:35]2)[cH:33][cH:32]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH...
CC1(C)CCC(O[Si](C)(C)C(C)(C)C)c2cc(B(O)O)ccc21.CCOC(=O)c1cccc2cc(Br)ccc12
CCOC(=O)c1ccc2cc(C3CC(C)(C)c4ccccc4C3O[Si](C)(C)C(C)(C)C)ccc2c1
null
null
CO
C-C Coupling
OtherReaction
e7b6f1d120a40f2704f595d417e6c75976f2e148ca7773f9836acb061b27d70f
4180a79a01f5556153dc91b20f033722a6f8d4c6baaa6b570c0ebf5e6298912a
c1ccc2c(c1)CCC(c1ccc3ccccc3c1)C2
Br-[c;H0;D3;+0:1]1:[c:2]:[c;H0;D3;+0:3]2:[cH;D2;+0:4]:[cH;D2;+0:5]:[c:6]:[c;H0;D3;+0:7](-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11]):[c;H0;D3;+0:12]:2:[c:13]:[c:14]:1.O-B(-O)-[c;H0;D3;+0:15](:[c:16]:[c:17]):[c:18]:[c:19]-[C:20](-[#8:21])-[CH2;D2;+0:22]-[C:23]-[C:24]>>[#8:21]-[C:20](-[c:19]:[c:18]:[cH;D2;+0:15]:[c:16]:[c:17])-[...
null
[]
90
CELSIUS
null
null
To a degassed solution of 722 mg (2.6 mmol) of ethyl 6-bromo-naphthalenecarboxylate in 6.0 mL of toluene, was added sequentially 90 mg (0.08 mmol) of tetrakis-triphenylphosphine palladium (O), 5.0 mL (10.0 mmol) of 2M sodium carbonate, and a solution of 1.018 g (3.1 mmol) of (5,6,7,8-tetrahydro-5,5-dimethyl-8-(t-butyld...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ester.Boronic acid
Ester
c1ccc2c(c1)CCCC2.c1ccc2ccccc2c1
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
HBr.B
CO
90
null
CC1(C)CCC(O[Si](C)(C)C(C)(C)C)c2cc(B(O)O)ccc21.CCOC(=O)c1cccc2cc(Br)ccc12>CO>CCOC(=O)c1ccc2cc(C3CC(C)(C)c4ccccc4C3O[Si](C)(C)C(C)(C)C)ccc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-03a49a1bcde34b059ad4b6f47e61b002
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1>>CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(=O)CCC4(C)C)ccc2c1
CC1(C=2C=CC(=CC2C(CC1)O)C=1C=C2C=CC(=CC2=CC1)C(=O)OCC)C.CC1(C=2C=CC(=CC2C(CC1)O)C=1C=C2C=CC(=CC2=CC1)C(=O)OCC)C.C[N+]1(CCOCC1)[O-].C(C)(=O)OCC>>C(C)OC(=O)C1=CC2=CC=C(C=C2C=C1)C1=CC=2C(CCC(C2C=C1)(C)C)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]2[cH:10][c:11](-[c:12]3[cH:13][cH:14][c:15]4[c:16]([cH:17]3)[CH:18]([OH:19])[CH2:20][CH2:21][C:22]4([CH3:23])[CH3:24])[cH:25][cH:26][c:27]2[cH:28]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]2[cH:10][c:11](-[c:12]3[cH:13][cH:14][c:15]4[c:16]([cH:17]3)[...
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(=O)CCC4(C)C)ccc2c1
null
null
C(Cl)Cl.CCCCCC.O
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
b5ed2230f6b74a2addb911914d598ef68d7e447cad6e33e5f6091319c5e0b79b
767cfd93f5821ebb9e1e72addd9cb404b20b0c821d246ae6b87a5776b74a455b
O=C1CCCc2ccc(-c3ccc4ccccc4c3)cc21
[C:1]-[C:2]-[CH;D3;+0:3](-[OH;D1;+0:4])-[c:5](:[c:6]):[c:7]>>[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[c:5](:[c:6]):[c:7]
null
[]
null
null
3
HOUR
To a solution of 101 mg (0.27 mmol) of ethyl-6-[5,6,7,8-tetrahydro-5,5-dimethyl-8-hydroxy-naphth-7-yl]naphth-2-oate (Compound B4) in 1.5 mL of methylene chloride was added 50 mg (0.43 mmol) of N-methylmorpholine N-oxide and 6.0 mg (0.017 mmol) of tetrapropylammonium perruthenate(VII). The reaction was stirred at room t...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ketone
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
null
C(Cl)Cl.CCCCCC.O
null
3
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1>C(Cl)Cl.CCCCCC.O>CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(=O)CCC4(C)C)ccc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-13e57f77780b42eab24c40acb5fbde1d
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1.CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1.COCCl>>CCOC(=O)c1ccc2cc(C3CC(C)(C)c4ccccc4C3OCOC)ccc2c1
COCCl.O.CC1(C=2C=CC(=CC2C(CC1)O)C=1C=C2C=CC(=CC2=CC1)C(=O)OCC)C.CC1(C=2C=CC(=CC2C(CC1)O)C=1C=C2C=CC(=CC2=CC1)C(=O)OCC)C.CCN(C(C)C)C(C)C.[I-].C(C)(C)(C)[NH3+]>>C(C)OC(=O)C1=CC2=CC=C(C=C2C=C1)C1CC(C=2C=CC=CC2C1OCOC)(C)C
CCOC(=O)c1ccc2cc(-[c:20]3[cH:19][cH:18][c:17]4[c:22]([cH:21]3)[CH:23]([OH:24])[CH2:12][CH2:13][C:14]4([CH3:15])[CH3:16])ccc2c1.CC1(C)CCC(O)c2cc(-[c:11]3[cH:10][c:9]4[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:31][c:30]4[cH:29][cH:28]3)ccc21.Cl[CH2:25][O:26][CH3:27]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:...
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1.CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1.COCCl
CCOC(=O)c1ccc2cc(C3CC(C)(C)c4ccccc4C3OCOC)ccc2c1
null
null
C(Cl)Cl.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
d1c73ad34a93da1da54be2006a8803b8c04d84dedebae94dc755c6dc7d59ce1c
49912efb2c127ee8d87392198e88165a6b142ddbbf53b1600b735d645c264d98
c1ccc2c(c1)CCC(c1ccc3ccccc3c1)C2
C-C-O-C(=O)-c1:c:c:c2:c:c(-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]-[C:6](-[OH;D1;+0:7])-[CH2;D2;+0:8]-[C:9]-[C:10]):c:c:c:2:c:1.C-C1(-C)-C-C-C(-O)-c2:c:c(-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[c:15]):c:c:c:2-1.Cl-[CH2;D2;+0:16]-[#8:17]-[C;D1;H3:18]>>[C:10]-[C:9]-[CH;D3;+0:8](-[c;H0;D3;+0:11](:[c:12]:[c:13]):[c:14]:[...
null
[]
null
null
14
HOUR
To a cold (0° C.) solution of 130 mg (0.35 mmol) of ethyl-6-[5,6,7,8-tetrahydro-5,5-dimethyl-8-(hydroxy)-naphth-7-yl]naphth-2-oate (Compound B4) in 2.0 mL of methylene chloride was added 50 mg (0.15 mL, 0.86 mmol) of Hunig's base, followed by 0.21 g (0.20 mL, 2.6 mmol) chloromethyl methyl ether was added and stirred at...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ether.Secondary alcohol.Secondary alcohol
Ether.Ether
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2.c1ccc2c(c1)CCCC2.c1ccc2ccccc2c1
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
c1ccc2ccccc2c1.c1ccc2c(c1)CCCC2
HCl
C(Cl)Cl.C(C)(=O)OCC
null
14
CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1.CCOC(=O)c1ccc2cc(-c3ccc4c(c3)C(O)CCC4(C)C)ccc2c1.COCCl>C(Cl)Cl.C(C)(=O)OCC>CCOC(=O)c1ccc2cc(C3CC(C)(C)c4ccccc4C3OCOC)ccc2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1def6f145a124de08c583f52bfc46d3d
CC(C)OB(OC(C)C)OC(C)C.CC1(C)CCCc2cc(Br)ccc21>>CC1(C)CCCc2cc(B(O)O)ccc21
C(C)(C)OB(OC(C)C)OC(C)C.BrC=1C=C2CCCC(C2=CC1)(C)C.[Li]CCCC>>CC1(C=2C=CC(=CC2CCC1)B(O)O)C
CC(C)O[B:10]([O:11]C(C)C)[O:12]C(C)C.Br[c:9]1[cH:8][c:7]2[c:15]([cH:14][cH:13]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][CH2:6]2>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][CH2:6][c:7]2[cH:8][c:9]([B:10]([OH:11])[OH:12])[cH:13][cH:14][c:15]21
CC(C)OB(OC(C)C)OC(C)C.CC1(C)CCCc2cc(Br)ccc21
CC1(C)CCCc2cc(B(O)O)ccc21
null
null
C1(=CC=CC=C1)C.Cl
Miscellaneous
Preparation of boronic acids
44976aedc627652e57cf654966855ab06a9db6d01924d4ea2bf9f8b5ec0f6db6
dafd25fbe01879c365f8c874026e570f49824f4bb82016b29d0c5d21aeb58ca3
c1ccc2c(c1)CCCC2
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].C-C(-C)-O-[B;H0;D3;+0:6](-[O;H0;D2;+0:7]-C(-C)-C)-[O;H0;D2;+0:8]-C(-C)-C>>[OH;D1;+0:7]-[B;H0;D3;+0:6](-[OH;D1;+0:8])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
-78
CELSIUS
45
MINUTE
To a cold (-78° C.) solution of 2.02 g (8.4 mmol) of 6-bromo-1,2,3,4-tetrahydro-1,1-dimethylnaphthalene in 11.0 mL of toluene, was added 4.6 g (6.8 mL, 10.9 mmol, 1.6M in hexane) of n-BuLi. The resulting solution was stirred at -78° C. for 45 min. and then 2.40 g (3.0 mL, 12.7 mmol) of triisopropylborate was dropwise a...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Boronic acid
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HBr
C1(=CC=CC=C1)C.Cl
-78
0.75
CC(C)OB(OC(C)C)OC(C)C.CC1(C)CCCc2cc(Br)ccc21>C1(=CC=CC=C1)C.Cl>CC1(C)CCCc2cc(B(O)O)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-95296aadd2f34ea7a8a15d80c932bee0
CC1(C)CCC(=O)c2cc(Br)ccc21.C[C](C)(C)[Mg][Cl]>>CC(C)(C)C1=CCC(C)(C)c2ccc(Br)cc21
C(C)(C)(C)[Mg]Cl.CO.C1(=CC=C(C=C1)S(=O)(=O)O)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C>>BrC1=CC=C2C(CC=C(C2=C1)C(C)(C)C)(C)C
O=[C:5]1[CH2:6][CH2:7][C:8]([CH3:9])([CH3:10])[c:11]2[cH:12][cH:13][c:14]([Br:15])[cH:16][c:17]21.[Cl][Mg][C:2]([CH3:1])([CH3:3])[CH3:4]>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5]1=[CH:6][CH2:7][C:8]([CH3:9])([CH3:10])[c:11]2[cH:12][cH:13][c:14]([Br:15])[cH:16][c:17]21
CC1(C)CCC(=O)c2cc(Br)ccc21.C[C](C)(C)[Mg][Cl]
CC(C)(C)C1=CCC(C)(C)c2ccc(Br)cc21
null
null
C1CCOC1
C-C Coupling
OtherReaction
cad3ebb460626e0b3c0c5e79b5d003dc2c6720d4441d1a3b1dd15d07bbe3c73a
6765e06b4fce5c2cc632b64cfcd2cebf695ba9495ab888b1531784cd07e6e026
C1=Cc2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[C;D1;H3:8]-[C;H0;D4;+0:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[Mg]-[Cl]>>[C;D1;H3:8]-[C;H0;D4;+0:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;H0;D3;+0:1]1=[CH;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7]
null
[]
-20
CELSIUS
1
HOUR
In a flame dried round bottom flask 7-bromo-3,4-dihydro-4,4-dimethylnaphthalen-1(2H)-one (Compound G, 2.0 g, 7.93 mmol) was dissolved in anhydrous THF (50 ml) and 3,4,5,6,-tetrahydro-2(H)-pyrimidinone (DMPU) (11.5 ml, 95.16 mmol) was added, under argon atmosphere. The reaction was then cooled to -20° C. and a solution ...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Ketone
null
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HCl.Mg
C1CCOC1
-20
1
CC1(C)CCC(=O)c2cc(Br)ccc21.C[C](C)(C)[Mg][Cl]>C1CCOC1>CC(C)(C)C1=CCC(C)(C)c2ccc(Br)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-763f0c0f3fec45499feba900588ad0eb
CCOC(=O)CC1(O)CCC(C)(C)c2ccc(N=Nc3ccc(C(=O)OCC)cc3)cc21>>CCOC(=O)CC1=CCC(C)(C)c2ccc(N=Nc3ccc(C(=O)OCC)cc3)cc21
CC1(C=2C=CC(=CC2C(CC1)(CC(=O)OCC)O)N=NC1=CC=C(C(=O)OCC)C=C1)C.CC1(C=2C=CC(=CC2C(CC1)(CC(=O)OCC)O)N=NC1=CC=C(C(=O)OCC)C=C1)C.C1CCC(CC1)N=C=NC2CCCCC2>>CC1(C=2C=CC(=CC2C(=CC1)CC(=O)OCC)N=NC1=CC=C(C(=O)OCC)C=C1)C
O[C:7]1([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:8][CH2:9][C:10]([CH3:11])([CH3:12])[c:13]2[cH:14][cH:15][c:16]([N:17]=[N: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][c:31]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7]1=[CH:8][CH2:9][C:10]([CH3:11])([CH3:12])[c:13]2...
CCOC(=O)CC1(O)CCC(C)(C)c2ccc(N=Nc3ccc(C(=O)OCC)cc3)cc21
CCOC(=O)CC1=CCC(C)(C)c2ccc(N=Nc3ccc(C(=O)OCC)cc3)cc21
null
Cl[Cu]
C1=CC=CC=C1
Functional Group Interconversion
OtherReaction
55de719a68f8efde968ccdcfe54c921765e82cad5ee57c0bae7adf2d5c6460b3
63e4ba80024292782b5f87f96975225484dff39f49e96eea21874ac0cd9091a0
C1=Cc2cc(N=Nc3ccccc3)ccc2CC1
O-[C;H0;D4;+0:1]1(-[C:2]-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6])-[CH2;D2;+0:7]-[C:8]-[C:9]-[c:10]:[c:11]-1:[c:12]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C:2]-[C;H0;D3;+0:1]1=[CH;D2;+0:7]-[C:8]-[C:9]-[c:10]:[c:11]-1:[c:12]
null
[]
null
null
null
null
A solution of (±)ethyl 4-[(5,5-dimethyl-8-hydroxy-8-carbethoxymethyl-5,6,7,8-tetrahydronaphth-2-yl)azo]benzoate (Compound D1, 108 mg, 0.25 mmol), DCC (55.9 mg, 0.271 mmol) and CuCl (36.6 mg, 0.37 mmol) in 8 ml of dry benzene was heated under reflux for 7 days. After cooling to room temperature, the solids were filtered...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
null
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1.c1ccccc1
HO-
Cl[Cu].C1=CC=CC=C1
null
null
CCOC(=O)CC1(O)CCC(C)(C)c2ccc(N=Nc3ccc(C(=O)OCC)cc3)cc21>Cl[Cu].C1=CC=CC=C1>CCOC(=O)CC1=CCC(C)(C)c2ccc(N=Nc3ccc(C(=O)OCC)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-febdc1c7fac448b78a423b7cf31b3624
CC1(C)CCC(=O)c2ccccc21.O=[N+]([O-])O>>CC1(C)CCC(=O)c2cc([N+](=O)[O-])ccc21
OS(=O)(=O)O.[N+](=O)(O)[O-].OS(=O)(=O)O.CC1(CCC(C2=CC=CC=C12)=O)C>>CC1(CCC(C2=CC(=CC=C12)[N+](=O)[O-])=O)C
[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:14][cH:15][c:16]21.O[N+:11](=[O:12])[O-:13]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14][cH:15][c:16]21
CC1(C)CCC(=O)c2ccccc21.O=[N+]([O-])O
CC1(C)CCC(=O)c2cc([N+](=O)[O-])ccc21
null
null
null
Functional Group Addition
Aromatic nitration with HNO3
5993c528ef8bcdffbf8c0a893a552b598272f75e0f1825b53fb570da12e0cd5d
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
O=C1CCCc2ccccc21
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[O;D1;H0:4]=[C:5]-[c:6]:[c:7]:[cH;D2;+0:8]:[c:9]:[c:10]>>[O;-;D1;H0:2]-[N+;H0;D3:1](=[O;D1;H0:3])-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:7]:[c:6]-[C:5]=[O;D1;H0:4]
null
[]
null
null
20
MINUTE
To 1.7 mL (3.0g, 30.6 mmol, 18M) H2SO4 at 5° C. (ice-NaCl bath) was slowly added 783.0 mg (4.49 mmol) of 3,4-dihydro-4,4-dimethyl-naphthalen-1(2H)-one. A solution of HNO3 (426.7 mg 6.88 mmol, 0.43 mL, 16M), and 1.31 g (0.013 mol, 0.74 mL, 18M) Of H2SO4 were slowly added. After 20 min, ice was added and the resulting mi...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
null
null
0.333333
CC1(C)CCC(=O)c2ccccc21.O=[N+]([O-])O>>CC1(C)CCC(=O)c2cc([N+](=O)[O-])ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c7356141cfe445de9c86a692d1573d44
CC1(C)CCC(=O)c2cc([N+](=O)[O-])ccc21>>CC1(C)CCC(=O)c2cc(N)ccc21
CC1(CCC(C2=CC(=CC=C12)[N+](=O)[O-])=O)C.CC1(CCC(C2=CC(=CC=C12)[N+](=O)[O-])=O)C>>CC1(CCC(C2=CC(=CC=C12)N)=O)C
O=[N+:11]([O-])[c:10]1[cH:9][c:8]2[c:14]([cH:13][cH:12]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]2=[O:7]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][c:10]([NH2:11])[cH:12][cH:13][c:14]21
CC1(C)CCC(=O)c2cc([N+](=O)[O-])ccc21
CC1(C)CCC(=O)c2cc(N)ccc21
null
[Pd]
CCOC(=O)C
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C1CCCc2ccccc21
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A solution of 230.0 mg (1.05 mmol) 3,4-dihydro-4,4-dimethyl-7-nitro-naphthalen-1(2H)-one (Compound D8) in 5.0 mL of EtOAc was stirred at room temperature with a catalytic amount of 10% Pd-C under 1 atm of H2 for 24 h. The catalyst was removed by filtration through a pad of Celite, and the filtrate concentrated under re...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccc2c(c1)CCCC2
Other
[Pd].CCOC(=O)C
null
null
CC1(C)CCC(=O)c2cc([N+](=O)[O-])ccc21>[Pd].CCOC(=O)C>CC1(C)CCC(=O)c2cc(N)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ef3ec04d343b4c5986b9256d5cce3915
CCOC(=O)c1ccc(N=Nc2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1ccsc1>>CCOC(=O)c1ccc(N=Nc2ccc3c(c2)C(c2cccs2)=CCC3(C)C)cc1
CC1(C=2C=CC(=CC2C(=CC1)OS(=O)(=O)C(F)(F)F)N=NC1=CC=C(C(=O)OCC)C=C1)C.S1C=CC=C1.[Li]C(C)(C)C>>CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)N=NC1=CC=C(C(=O)OCC)C=C1)C
O=S(=O)(O[C:18]1=[CH:24][CH2:25][C:26]([CH3:27])([CH3:28])[c:15]2[cH:14][cH:13][c:12]([N:11]=[N:10][c:9]3[cH:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:30][cH:29]3)[cH:17][c:16]21)C(F)(F)F.[cH:19]1[cH:20][cH:21][cH:22][s:23]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([N:10]=[N:11][c:12]2[cH:13][c...
CCOC(=O)c1ccc(N=Nc2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1ccsc1
CCOC(=O)c1ccc(N=Nc2ccc3c(c2)C(c2cccs2)=CCC3(C)C)cc1
null
[Cl-].[Cl-].[Zn+2].C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
C1CCOC1.[NH4+].[Cl-]
C-C Coupling
OtherReaction
1635e33838212f74c180ab5d22f02760affb57410f7f71f8f01e910656be3423
253c3b9fccee9bf420e0fb1f267e37bad5aa0c206427cb57447e420babcc09c8
C1=C(c2cccs2)c2cc(N=Nc3ccccc3)ccc2CC1
F-C(-F)(-F)-S(=O)(=O)-O-[C;H0;D3;+0:1](=[C:2]-[C:3])-[c:4](:[c:5]):[c:6].[#16;a:7]1:[c:8]:[c:9]:[c:10]:[cH;D2;+0:11]:1>>[C:3]-[C:2]=[C;H0;D3;+0:1](-[c;H0;D3;+0:11]1:[#16;a:7]:[c:8]:[c:9]:[c:10]:1)-[c:4](:[c:5]):[c:6]
null
[]
null
null
2
HOUR
To a cold solution (-78° C.) of thiophene (0.07 ml, 0.75 mmol) in 1.5 ml of THF was added t-BuLi (0.457 ml, 0.75 mmol, 1.7M in pentane) and stirred for 2 h. To this solution, ZnCl2 (168 mg, 1.2 mmol) in 1.5 ml of THF was added. The resulting solution was warmed to room temperature, stirred for 1 h and was added (via ca...
10.6084/m9.figshare.5104873.v1
null
Triflate
null
C1=Cc2ccccc2CC1.c1ccsc1
c1ccsc1.C1=Cc2ccccc2CC1
c1ccccc1.c1ccsc1.C1=Cc2ccccc2CC1
TfOH.HO-
[Cl-].[Cl-].[Zn+2].C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1CCOC1.[NH4+].[Cl-]
null
2
CCOC(=O)c1ccc(N=Nc2ccc3c(c2)C(OS(=O)(=O)C(F)(F)F)=CCC3(C)C)cc1.c1ccsc1>[Cl-].[Cl-].[Zn+2].C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1CCOC1.[NH4+].[Cl-]>CCOC(=O)c1ccc(N=Nc2ccc3c(c2)C(c2cccs2)...
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-71d8a412e47743ae868fcc2cf8c525e8
CC(=O)c1ccc2c(c1)C(C)(C)CCC2=O.OCCO>>CC1(C)CCC(=O)c2ccc(C3(C)OCCO3)cc21
C(CO)O.CC1(CCC(C2=CC(=CC=C12)C(C)=O)=O)C.O.C1(=CC=C(C=C1)S(=O)(=O)O)C.CC1(CCC(C2=CC=C(C=C12)C(C)=O)=O)C>>CC1(OCCO1)C=1C=C2C(CCC(C2=CC1)=O)(C)C
O=[C:12]([c:11]1[cH:10][cH:9][c:8]2[c:19]([cH:18]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]2=[O:7])[CH3:13].[OH:14][CH2:15][CH2:16][OH:17]>>[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]3([CH3:13])[O:14][CH2:15][CH2:16][O:17]3)[cH:18][c:19]21
CC(=O)c1ccc2c(c1)C(C)(C)CCC2=O.OCCO
CC1(C)CCC(=O)c2ccc(C3(C)OCCO3)cc21
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
2baa95c632045e217509d8ec12cda8674252268fe3f8cb44eb2e5ebe0f27c30f
f8121a7732f8ef583111433d2b2d82886bf3a134c51dc6363d813c8cbf4e36f5
O=C1CCCc2cc(C3OCCO3)ccc21
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[c:5].[OH;D1;+0:6]-[C:7]-[C:8]-[OH;D1;+0:9]>>[C;D1;H3:2]-[C;H0;D4;+0:1]1(-[c:3](:[c:4]):[c:5])-[O;H0;D2;+0:6]-[C:7]-[C:8]-[O;H0;D2;+0:9]-1
10
[{"value": 10.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 1.80 g (8.34 mmol) of a 1:5 mixture of 3,4-dihydro-4,4-dimethyl-7-acetyl-naphthalen-1(2H)-one (Compound D14a); and 3,4-dihydro-4,4-dimethyl-6-acetyl-naphthalen-1(2H)-one (Compound D14b) in 50 mL benzene was combined with 517.7 mg (8.34 mmol) of ethylene glycol and 20.0 mg (0.11 mmol) of p-toluenesulfonic ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary alcohol.Primary alcohol
Ether.Ether
null
C1COCO1
c1ccc2c(c1)CCCC2.C1COCO1
HO-
C1=CC=CC=C1
null
null
CC(=O)c1ccc2c(c1)C(C)(C)CCC2=O.OCCO>C1=CC=CC=C1>CC1(C)CCC(=O)c2ccc(C3(C)OCCO3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-46f36199a03b442ba91746cd3e3add7b
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C3(C)OCCO3)ccc21>>CCOC(=O)CC1=CCC(C)(C)c2cc(C(C)=O)ccc21
CC1(OCCO1)C=1C=C2C(CCC(C2=CC1)(CC(=O)OCC)O)(C)C.CC=1C=CC(=CC1)S(=O)(=O)O.O>>CC1(CC=C(C2=CC=C(C=C12)C(C)=O)CC(=O)OCC)C
O[C:7]1([CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:8][CH2:9][C:10]([CH3:11])([CH3:12])[c:13]2[cH:14][c:15]([C:16]3([CH3:17])OCC[O:18]3)[cH:19][cH:20][c:21]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7]1=[CH:8][CH2:9][C:10]([CH3:11])([CH3:12])[c:13]2[cH:14][c:15]([C:16]([CH3:17])=[O:18])[cH:19][cH:20][c:21]21
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C3(C)OCCO3)ccc21
CCOC(=O)CC1=CCC(C)(C)c2cc(C(C)=O)ccc21
null
null
C1=CC=CC=C1
Functional Group Interconversion
OtherReaction
9d4ab51434e135588277b1abca09c019ba592a5324ec3ef14e049c0ab80fdb7b
443dac47cd5d45a6cddf21b9d72a18d45ad34952e38f4958ebce8b1ddd0eb30d
C1=Cc2ccccc2CC1
O-[C;H0;D4;+0:1]1(-[C:2]-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6])-[CH2;D2;+0:7]-[C:8]-[C:9]-[c:10]2:[c:11]:[c:12](-[C;H0;D4;+0:13]3(-[C;D1;H3:14])-O-C-C-[O;H0;D2;+0:15]-3):[c:16]:[c:17]:[c:18]:2-1>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[C:2]-[C;H0;D3;+0:1]1=[CH;D2;+0:7]-[C:8]-[C:9]-[c:10]2:[c:11]:[c:12](-[C;H0;D3;+0:13](-[C;D1;H3:...
null
[]
null
null
null
null
A solution of (±)6-(2-methyl-1,3-dioxolan-2-yl)-1,2,3,4-tetrahydro-4,4-dimethyl-1-hydroxy-1-(carboethoxymethyl)-naphthlene ((Compound D16, 321 mg, 0.90 mmol) and catalytic amount of TsOH in 20 ml of benzene was refluxed for 12 h. During the reaction the water generated from the reaction was periodically removed by a De...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary alcohol
Ketone
c1ccc2c(c1)CCCC2.C1COCO1
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HO-
C1=CC=CC=C1
null
null
CCOC(=O)CC1(O)CCC(C)(C)c2cc(C3(C)OCCO3)ccc21>C1=CC=CC=C1>CCOC(=O)CC1=CCC(C)(C)c2cc(C(C)=O)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-130b3a00a9dc43f5a473799157e45ada
CC1(C)CCC(=O)c2ccccc21.CCOCC.[Li][C](C)(C)C>>CC(=O)c1ccc2c(c1)C(C)(C)CC=C2C(C)(C)C
O=S(Cl)Cl.CC1(CCC(C2=CC=CC=C12)=O)C.[Li]C(C)(C)C.CCOCC>>CC1(CC=C(C2=CC=C(C=C12)C(C)=O)C(C)(C)C)C
[O:3]=[C:15]1[c:7]2[cH:6][cH:5][cH:4][cH:9][c:8]2[C:10]([CH3:11])([CH3:12])[CH2:13][CH2:14]1.CCO[CH2:2][CH3:1].[Li][C:16]([CH3:17])([CH3:18])[CH3:19]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[C:10]([CH3:11])([CH3:12])[CH2:13][CH:14]=[C:15]2[C:16]([CH3:17])([CH3:18])[CH3:19]
CC1(C)CCC(=O)c2ccccc21.CCOCC.[Li][C](C)(C)C
CC(=O)c1ccc2c(c1)C(C)(C)CC=C2C(C)(C)C
null
null
null
C-C Coupling
OtherReaction
2ea059215f3fee8060392dd5e073e50c86e682d9ccd36b54923fc97f9447780d
2a55fa5b64016cbe1065d8e162e8394140e0c89b5a40b3ee805cb2dd6c82c75d
C1=Cc2ccccc2CC1
C-C-O-[CH2;D2;+0:1]-[C;D1;H3:2].[C;D1;H3:3]-[C;H0;D4;+0:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[Li].[O;H0;D1;+0:7]=[C;H0;D3;+0:8]1-[CH2;D2;+0:9]-[C:10]-[C:11]-[c:12]2:[c:13]:[cH;D2;+0:14]:[c:15]:[c:16]:[c:17]:2-1>>[C;D1;H3:3]-[C;H0;D4;+0:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[C;H0;D3;+0:8]1=[CH;D2;+0:9]-[C:10]-[C:11]-[c:12]2:[c:13]:[...
null
[]
-78
CELSIUS
30
MINUTE
To a solution of 6-(2-methyl-1,3-dioxolan-2-yl)!-3,4-dihydro-4,4-dimethylnaphthlen-1(2H)-one ((Compound D15, 353 mg, 1.36 mmol) in 3 ml of dry ether at -78° C. was added dropwise t-BuLi (1 ml, 1.7 mmol, 1.7M solution in pentane). This dear light yellow solution was left at -78° C. for 30 min. Then, fleshly distilled SO...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether.Alkyl lithium
Ketone
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1
HO-.Li
null
-78
0.5
CC1(C)CCC(=O)c2ccccc21.CCOCC.[Li][C](C)(C)C>>CC(=O)c1ccc2c(c1)C(C)(C)CC=C2C(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-772b5fad62a14312b842257dffc914b5
CC(=O)c1ccc2c(c1)C(C)(C)CC=C2c1cccs1.O=Cc1ccc(C(=O)O)cc1>>CC1(C)CC=C(c2cccs2)c2ccc(C(=O)C=Cc3ccc(C(=O)O)cc3)cc21
S1C(=CC=C1)C1=CCC(C2=CC(=CC=C12)C(C)=O)(C)C.C(=O)(O)C1=CC=C(C=O)C=C1.[OH-].[Na+]>>O=C(C=CC1=CC=C(C(=O)O)C=C1)C1=CC=2C(CC=C(C2C=C1)C=1SC=CC1)(C)C
[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]2[cH:8][cH:9][cH:10][s:11]2)[c:12]2[cH:13][cH:14][c:15]([C:16](=[O:17])[CH3:18])[cH:29][c:30]21.O=[CH:19][c:20]1[cH:21][cH:22][c:23]([C:24](=[O:25])[OH:26])[cH:27][cH:28]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]2[cH:8][cH:9][cH:10][s:11]2)[c:12]2[cH:13][cH:14][c:1...
CC(=O)c1ccc2c(c1)C(C)(C)CC=C2c1cccs1.O=Cc1ccc(C(=O)O)cc1
CC1(C)CC=C(c2cccs2)c2ccc(C(=O)C=Cc3ccc(C(=O)O)cc3)cc21
null
null
CO
C-C Coupling
Aldehyde and ketone to alpha,beta-unsaturated carbonyl
df1bdbab1a06af9561d74fe6bc94ee8bda1d14faad9db1ada3a214bd64a24cf8
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
O=C(C=Cc1ccccc1)c1ccc2c(c1)CCC=C2c1cccs1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-[C:6](=[O;D1;H0:7])-[c:8]>>[O;D1;H0:7]=[C:6](-[c:8])-[CH;D2;+0:5]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
12
HOUR
To a solution of 62.6 mg (0.222 mmol) 3,4-dihydro-1-(2-thienyl)-4,4-dimethyl-6-acetylnaphthalene (Compound D33) in 4.0 mL of MeOH were added 33.4 mg (0.222 mmol) of 4-carboxy benzaldehyde, and 240.0 mg (6.00 mmol; 2.0 mL of 3M aqueous NaOH). The resulting solution was stirred at room temperature for 12 h, concentrated ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
null
null
c1ccsc1.C1=Cc2ccccc2CC1.c1ccccc1
HO-
CO
null
12
CC(=O)c1ccc2c(c1)C(C)(C)CC=C2c1cccs1.O=Cc1ccc(C(=O)O)cc1>CO>CC1(C)CC=C(c2cccs2)c2ccc(C(=O)C=Cc3ccc(C(=O)O)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5f9f7585dafc4f17ad29c89236ac8a9d
COC(=O)c1ccc2c(c1)C(=O)CCC2(C)C>>CC1(C)CCC(=O)c2ccccc21
CC1(C=2C=CC(=CC2C(CC1)=O)C(=O)OC)C.CC1(C=2C=CC(=CC2C(CC1)=O)C(=O)OC)C.[OH-].[Na+].Cl>>CC1(C=2C=CC=CC2C(CC1)=O)C
COC(=O)[c:10]1[cH:9][c:8]2[c:13]([cH:12][cH:11]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH2:5][C:6]2=[O:7]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]21
COC(=O)c1ccc2c(c1)C(=O)CCC2(C)C
CC1(C)CCC(=O)c2ccccc21
null
null
C(C)O.C1CCOC1
Reduction
Decarboxylation
d6bbb76477b08de1e249c18973b19813a0f61a90fc74922e437d8dcd688d09f7
b8e5da8ea19c403a2e974791a9cf591400749acb6b71151717aaece4f3b22bef
O=C1CCCc2ccccc21
C-O-C(=O)-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]-[C:6]=[O;D1;H0:7]>>[O;D1;H0:7]=[C:6]-[c:5]:[c:4]:[cH;D2;+0:1]:[c:2]:[c:3]
null
[]
null
null
16
HOUR
To a solution of methyl-5,5-dimethyl-5,6-dihydro-naphthalen-8(7H)-one-2-carboxylate (Compound E2, 1.05 g, 4.5 mmol) in 10 mL of ethanol and THF (10 mL) was added sodiumhydroxide 9 mL (1M solution). The solution was stirred for 16 h and thereafter acidified with 10% HCl. The mixture was extracted with ethyl acetate, the...
10.6084/m9.figshare.5104873.v1
null
Ester
null
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
HO-
C(C)O.C1CCOC1
null
16
COC(=O)c1ccc2c(c1)C(=O)CCC2(C)C>C(C)O.C1CCOC1>CC1(C)CCC(=O)c2ccccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d9c61c395e2c4475a549c72777a848f0
COC(=O)c1ccc2c(c1)C(OS(=O)(=O)C(F)(F)F)=CCC2(C)C.c1ccsc1>>COC(=O)c1ccc2c(c1)C(c1cccs1)=CCC2(C)C
CC1(C=2C=CC(=CC2C(=CC1)OS(=O)(=O)C(F)(F)F)C(=O)OC)C.CC1(C=2C=CC(=CC2C(=CC1)OS(=O)(=O)C(F)(F)F)C(=O)OC)C.S1C=CC=C1.C(CCC)[Li]>>CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)OC)C
O=S(=O)(O[C:11]1=[CH:17][CH2:18][C:19]([CH3:20])([CH3:21])[c:8]2[cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:10][c:9]21)C(F)(F)F.[cH:12]1[cH:13][cH:14][cH:15][s:16]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[C:11]([c:12]1[cH:13][cH:14][cH:15][s:16]1)=[CH:17][CH2:18][C:19]2([CH3:20])[CH3:21]
COC(=O)c1ccc2c(c1)C(OS(=O)(=O)C(F)(F)F)=CCC2(C)C.c1ccsc1
COC(=O)c1ccc2c(c1)C(c1cccs1)=CCC2(C)C
null
[Cl-].[Cl-].[Zn+2]
C1CCOC1
C-C Coupling
OtherReaction
1635e33838212f74c180ab5d22f02760affb57410f7f71f8f01e910656be3423
253c3b9fccee9bf420e0fb1f267e37bad5aa0c206427cb57447e420babcc09c8
C1=C(c2cccs2)c2ccccc2CC1
F-C(-F)(-F)-S(=O)(=O)-O-[C;H0;D3;+0:1](=[C:2]-[C:3])-[c:4](:[c:5]):[c:6].[#16;a:7]1:[c:8]:[c:9]:[c:10]:[cH;D2;+0:11]:1>>[C:3]-[C:2]=[C;H0;D3;+0:1](-[c;H0;D3;+0:11]1:[#16;a:7]:[c:8]:[c:9]:[c:10]:1)-[c:4](:[c:5]):[c:6]
5
[{"value": 5.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
3
HOUR
(Compound E5) To a solution of 329.0 mg (3.93 mmol) of thiophene in 2.0 mL THF at 0° C. was added 251.8 mg (3.93 mmol, 1.56 mL of 2.5M solution in hexanes) of n-butyllithium. After stirring for 3 h at 0° C., a solution of 845.0 mg (6.28 mmol) of ZnCl2 in 5.0 mL THF was added and the resulting solution stirred for 30 mi...
10.6084/m9.figshare.5104873.v1
null
Triflate
null
C1=Cc2ccccc2CC1.c1ccsc1
c1ccsc1.C1=Cc2ccccc2CC1
c1ccsc1.C1=Cc2ccccc2CC1
TfOH.HO-
[Cl-].[Cl-].[Zn+2].C1CCOC1
0
3
COC(=O)c1ccc2c(c1)C(OS(=O)(=O)C(F)(F)F)=CCC2(C)C.c1ccsc1>[Cl-].[Cl-].[Zn+2].C1CCOC1>COC(=O)c1ccc2c(c1)C(c1cccs1)=CCC2(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8760b059f5814b0b8512bcb8b33a9346
COC(=O)c1ccc2c(c1)C(c1cccs1)=CCC2(C)C>>CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21
CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)OC)C.CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)OC)C.[OH-].[Na+]>>CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)O)C
C[O:17][C:15]([c:14]1[cH:13][c:12]2[c:20]([cH:19][cH:18]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH:5]=[C:6]2[c:7]1[cH:8][cH:9][cH:10][s:11]1)=[O:16]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]2[cH:8][cH:9][cH:10][s:11]2)[c:12]2[cH:13][c:14]([C:15](=[O:16])[OH:17])[cH:18][cH:19][c:20]21
COC(=O)c1ccc2c(c1)C(c1cccs1)=CCC2(C)C
CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21
null
null
C1CCOC1.CCO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
C1=C(c2cccs2)c2ccccc2CC1
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
[]
35
CELSIUS
null
null
To a solution of methyl 5,5-dimethyl-5,6-dihydro-8-(2-thienyl)-2-naphthalenecarboxylate (Compound E5, 430.0 mg, 1.44 mmol) in 3.0 mL of EtOH and 3.0 mL THF was added NaOH (240.0 mg, 6.00 mmol; 3.0 mL of a 2N aqueous solution). The resulting solution was warmed to 35° C. for 6 h, cooled to room temperature and quenched ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccsc1.C1=Cc2ccccc2CC1
Other
C1CCOC1.CCO
35
null
COC(=O)c1ccc2c(c1)C(c1cccs1)=CCC2(C)C>C1CCOC1.CCO>CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-efe92404a0254b2b89ad1b766a802326
CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21.CCOC(=O)c1ccc(O)cc1>>CCOC(=O)c1ccc(OC(=O)c2ccc3c(c2)C(c2cccs2)=CCC3(C)C)cc1
CCOC(=O)C.CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)O)C.CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)O)C.OC1=CC=C(C(=O)OCC)C=C1.Cl.CN(CCCN=C=NCC)C>>CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)OC1=CC=C(C(=O)OCC)C=C1)C
O[C:11](=[O:12])[c:13]1[cH:14][cH:15][c:16]2[c:17]([cH:18]1)[C:19]([c:20]1[cH:21][cH:22][cH:23][s:24]1)=[CH:25][CH2:26][C:27]2([CH3:28])[CH3:29].[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([OH:10])[cH:30][cH:31]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([O:10][C:11](=[O:12])[c:13]2[cH:14][cH...
CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21.CCOC(=O)c1ccc(O)cc1
CCOC(=O)c1ccc(OC(=O)c2ccc3c(c2)C(c2cccs2)=CCC3(C)C)cc1
null
null
CN(C)C=O
Acylation
Mitsunobu esterification
f18451ac648b00cb7c6684a3e64bee855b0320c7eb0f62b757b29d5fb6745560
1489fe0065c6531b60fda87a3857d7da1cd21873868856f058c20706f927fa08
O=C(Oc1ccccc1)c1ccc2c(c1)C(c1cccs1)=CCC2
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A solution of 5,5-dimethyl-5,6-dihydro-8-(2-thienyl)-naphthalene-2-carboxylic acid (Compound E6, 50.0 mg, 0.177 mmol), ethyl 4-hydroxybenzoate (38.2 mg, 0.230 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (44.0 mg, 0.230 mmol), and 4-N,N-dimethylaminopyridine (28.0 mg, 0.230 mmol) in 2.0 mL DMF was...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol
Ester
null
null
c1ccccc1.c1ccsc1.C1=Cc2ccccc2CC1
HO-
CN(C)C=O
null
null
CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21.CCOC(=O)c1ccc(O)cc1>CN(C)C=O>CCOC(=O)c1ccc(OC(=O)c2ccc3c(c2)C(c2cccs2)=CCC3(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d50f3e28aedd4932b721cce8a6aefdfd
CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21.C[Si](C)(C)CCOC(=O)c1ccc(O)cc1>>CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21
CCOCC.CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)O)C.CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)O)C.OC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1.Cl.CN(CCCN=C=NCC)C>>CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)OC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)C
O[C:15]([c:14]1[cH:13][c:12]2[c:35]([cH:34][cH:33]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH:5]=[C:6]2[c:7]1[cH:8][cH:9][cH:10][s:11]1)=[O:16].[OH:17][c:18]1[cH:19][cH:20][c:21]([C:22](=[O:23])[O:24][CH2:25][CH2:26][Si:27]([CH3:28])([CH3:29])[CH3:30])[cH:31][cH:32]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]2[cH:8][cH:9...
CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21.C[Si](C)(C)CCOC(=O)c1ccc(O)cc1
CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21
null
null
CN(C)C=O
Acylation
Mitsunobu esterification
f18451ac648b00cb7c6684a3e64bee855b0320c7eb0f62b757b29d5fb6745560
1489fe0065c6531b60fda87a3857d7da1cd21873868856f058c20706f927fa08
O=C(Oc1ccccc1)c1ccc2c(c1)C(c1cccs1)=CCC2
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A solution of 5,5-dimethyl-5,6-dihydro-8-(2-thienyl)-naphthalene-2-carboxylic acid (Compound E6, 79.0 mg, 0.280 mmol), 2-trimethylsilylethyl 4-hydroxybenzoate (73.3 mg, 0.308 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (70.0 mg, 0.364 mmol), and 4-N,N-dimethylaminopyridine (44.5 mg, 0.364 mmol) i...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Aromatic alcohol
Ester
null
null
c1ccsc1.C1=Cc2ccccc2CC1.c1ccccc1
HO-
CN(C)C=O
null
null
CC1(C)CC=C(c2cccs2)c2cc(C(=O)O)ccc21.C[Si](C)(C)CCOC(=O)c1ccc(O)cc1>CN(C)C=O>CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-54921a0488e14a3e81bfab9c9a8565e8
CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21>>CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)O)cc3)ccc21
CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)OC1=CC=C(C(=O)OCC[Si](C)(C)C)C=C1)C.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC>>CC1(C=2C=CC(=CC2C(=CC1)C=1SC=CC1)C(=O)OC1=CC=C(C(=O)O)C=C1)C
C[Si](C)(C)CC[O:24][C:22]([c:21]1[cH:20][cH:19][c:18]([O:17][C:15]([c:14]2[cH:13][c:12]3[c:29]([cH:28][cH:27]2)[C:2]([CH3:1])([CH3:3])[CH2:4][CH:5]=[C:6]3[c:7]2[cH:8][cH:9][cH:10][s:11]2)=[O:16])[cH:26][cH:25]1)=[O:23]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]2[cH:8][cH:9][cH:10][s:11]2)[c:12]2[cH:13][c:14]([C:1...
CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21
CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)O)cc3)ccc21
null
null
C1CCOC1.CCOC(=O)C
Deprotection
Ester saponification (alkyl deprotection)
a3c1e490feb6b7fce3c6323047260c78ad5d894f96ffb52fbe21f86a88668678
5b01c4b72bcb1d31e02ab060e26bc1888b853fee0b286003b9b19e22cf024145
O=C(Oc1ccccc1)c1ccc2c(c1)C(c1cccs1)=CCC2
C-[Si](-C)(-C)-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
8
HOUR
To a solution of 2-trimethylsilylethyl 4-[[(5,5-dimethyl-5,6-dihydro-8-(2-thienyl)-naphthalen-2-yl)carbonyl]oxy]-benzoate (Compound E10, 100.0 mg, 0.198 mmol) in 2.0 mL THF at room temperature was added 155.3 mg of tetrabutylammonium fluoride (0.594 mmol 0.6 mL of a 1M solution in THF). After stirring overnight the rea...
10.6084/m9.figshare.5104873.v1
null
Ester.Silyl protective group
Carboxylic acid
null
null
c1ccsc1.C1=Cc2ccccc2CC1.c1ccccc1
Other
C1CCOC1.CCOC(=O)C
null
8
CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)OCC[Si](C)(C)C)cc3)ccc21>C1CCOC1.CCOC(=O)C>CC1(C)CC=C(c2cccs2)c2cc(C(=O)Oc3ccc(C(=O)O)cc3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-83bf3c1c076c4485b404b1a77f65cfe6
COC(=O)c1ccc2c(c1)C(=O)CCC2(C)C.Sc1ccccc1>>COC(=O)c1ccc2c(c1)C(Sc1ccccc1)=CCC2(C)C
C1(=CC=CC=C1)S.CCN(CC)CC.CC1(C=2C=CC(=CC2C(CC1)=O)C(=O)OC)C.CC1(C=2C=CC(=CC2C(CC1)=O)C(=O)OC)C.O>>COC(=O)C1=CC=2C(=CCC(C2C=C1)(C)C)SC1=CC=CC=C1
O=[C:11]1[c:9]2[c:8]([cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:10]2)[C:21]([CH3:22])([CH3:23])[CH2:20][CH2:19]1.[SH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[C:11]([S:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1)=[CH:19][CH2:20][C:21]2([CH3:...
COC(=O)c1ccc2c(c1)C(=O)CCC2(C)C.Sc1ccccc1
COC(=O)c1ccc2c(c1)C(Sc1ccccc1)=CCC2(C)C
null
Cl[Ti](Cl)(Cl)Cl
C1CCOC1
Heteroatom Alkylation and Arylation
OtherReaction
0ada3ae671ad3b060b96add65fbcfec1b731cae0a6c858eea87374516a4ac73a
f936d6b76ed560a8fec322bcfbbde18f0a579df08bd9baf16a1cafcec3158898
C1=C(Sc2ccccc2)c2ccccc2CC1
O=[C;H0;D3;+0:1]1-[CH2;D2;+0:2]-[C:3]-[C:4]-[c:5]:[c:6]-1:[c:7].[SH;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[c:7]:[c:6]1:[c:5]-[C:4]-[C:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1]-1-[S;H0;D2;+0:8]-[c:9](:[c:10]):[c:11]
null
[]
null
null
null
null
To a solution of methyl-5,5-dimethyl-5,6-dihydro-naphthalen-8(7H)-one-2-carboxylate (Compound E2, 835.0 mg, 3.60 mmol) in 25.0 mL of THF at room temperature was added TiCl4 (670.0 mg, 3.55 mmol). Thereafter a solution of thiophenol (430.0 mg, 3.90 mmol) and Et3N (730.0 mg, 7.20 mmol) in 10 mL THF was added. The resulti...
10.6084/m9.figshare.5104873.v1
null
Ketone.Aromatic thiol
Monosulfide
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
c1ccccc1.C1=Cc2ccccc2CC1
HO-
Cl[Ti](Cl)(Cl)Cl.C1CCOC1
null
null
COC(=O)c1ccc2c(c1)C(=O)CCC2(C)C.Sc1ccccc1>Cl[Ti](Cl)(Cl)Cl.C1CCOC1>COC(=O)c1ccc2c(c1)C(Sc1ccccc1)=CCC2(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e3e7b7ca98e641d6a2d408b95787c8d2
COC(=O)c1ccc2c(c1)C(Sc1ccccc1)=CCC2(C)C>>CC1(C)CC=C(Sc2ccccc2)c2cc(C(=O)O)ccc21
CC1(C=2C=CC(=CC2C(=CC1)SC1=CC=CC=C1)C(=O)OC)C.CC1(C=2C=CC(=CC2C(=CC1)SC1=CC=CC=C1)C(=O)OC)C.[OH-].[Na+]>>CC1(C=2C=CC(=CC2C(=CC1)SC1=CC=CC=C1)C(=O)O)C
C[O:19][C:17]([c:16]1[cH:15][c:14]2[c:22]([cH:21][cH:20]1)[C:2]([CH3:1])([CH3:3])[CH2:4][CH:5]=[C:6]2[S:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)=[O:18]>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH:5]=[C:6]([S:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[c:14]2[cH:15][c:16]([C:17](=[O:18])[OH:19])[cH:20][cH:21][c:22]21
COC(=O)c1ccc2c(c1)C(Sc1ccccc1)=CCC2(C)C
CC1(C)CC=C(Sc2ccccc2)c2cc(C(=O)O)ccc21
null
null
C1CCOC1.CCO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
C1=C(Sc2ccccc2)c2ccccc2CC1
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
8
HOUR
To a solution of methyl 5,5-dimethyl-5,6-dihydro-8-(phenylthio)-naphthalene-2-carboxylate (Compound E18, 300.0 mg, 0.926 mmol) in 4.0 mL of EtOH and 2.0 mL THF was added NaOH (200.0 mg, 5.00 mmol; 5.0 mL of a 1N aqueous solution). After stirring overnight at room temperature the reaction was quenched by the addition of...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.C1=Cc2ccccc2CC1
Other
C1CCOC1.CCO
null
8
COC(=O)c1ccc2c(c1)C(Sc1ccccc1)=CCC2(C)C>C1CCOC1.CCO>CC1(C)CC=C(Sc2ccccc2)c2cc(C(=O)O)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-bf2e44a5bdea4415bef84fd79bdef046
CC1(C)CCC(=O)c2cc(Br)ccc21.CCOC(=O)CBr>>CCOC(=O)CC1(O)CCC(C)(C)c2ccc(Br)cc21
BrCC(=O)OCC.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C.BrC1=CC=C2C(CCC(C2=C1)=O)(C)C>>OC1(CCC(C2=CC=C(C=C12)Br)(C)C)CC(=O)OCC
[C:7]1(=[O:8])[CH2:9][CH2:10][C:11]([CH3:12])([CH3:13])[c:14]2[cH:15][cH:16][c:17]([Br:18])[cH:19][c:20]21.Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[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])([CH3:13])[c:14]2[cH:15][cH:16][c:17]([Br:18])[cH:19][c:20]21
CC1(C)CCC(=O)c2cc(Br)ccc21.CCOC(=O)CBr
CCOC(=O)CC1(O)CCC(C)(C)c2ccc(Br)cc21
null
[Zn]
C1=CC=CC=C1
C-C Coupling
Grignard_alcohol
ae6802bc43630c235b581c1f69ee3f400dd59564bb5948df811879329723b99c
86d8e63c1eeb9e82c583fd2409352b28a569a3f780f9f297e86b8d2f688ca9d6
c1ccc2c(c1)CCCC2
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 suspension of Zn (1.20 g, 18.4 mmol) in 10 mL benzene at 100° C. was slowly added a solution of ethyl 2-bromoacetate (658.0 mg, 3.94 mmol) and 3,4-dihydro-4,4-dimethyl-7-bromo-naphthalen-1(2H)-one (Compound G, 500.0 mg, 1.97 mmol) in 20.0 mL benzene. The resulting mixture was heated for 2 h, cooled to room tempera...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ester.Tertiary alcohol
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
Br-
[Zn].C1=CC=CC=C1
null
null
CC1(C)CCC(=O)c2cc(Br)ccc21.CCOC(=O)CBr>[Zn].C1=CC=CC=C1>CCOC(=O)CC1(O)CCC(C)(C)c2ccc(Br)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1ecb612d8d5a4573ace4ca6045265aad
CC(=O)OC(C)=O.CCOC(=O)CC1(O)CCC(C)(C)c2ccc(Br)cc21>>CCOC(=O)CC1(OC(C)=O)CCC(C)(C)c2ccc(Br)cc21
OC1(CCC(C2=CC=C(C=C12)Br)(C)C)CC(=O)OCC.C(C)(=O)OC(C)=O>>C(C)(=O)OC1(CCC(C2=CC=C(C=C12)Br)(C)C)CC(=O)OCC
CC(=O)O[C:9]([CH3:10])=[O:11].[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7]1([OH:8])[CH2:12][CH2:13][C:14]([CH3:15])([CH3:16])[c:17]2[cH:18][cH:19][c:20]([Br:21])[cH:22][c:23]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:7]1([O:8][C:9]([CH3:10])=[O:11])[CH2:12][CH2:13][C:14]([CH3:15])([CH3:16])[c:17]2[cH:18][cH:19][c:20...
CC(=O)OC(C)=O.CCOC(=O)CC1(O)CCC(C)(C)c2ccc(Br)cc21
CCOC(=O)CC1(OC(C)=O)CCC(C)(C)c2ccc(Br)cc21
null
null
CCOC(=O)C.C(Cl)Cl
Acylation
Transesterification
7845e6caeb9ebcfc4e11ccde0ca862e171727c1b0b0f5c55f250826811ed7095
aad6c0b0b2e56c19696d13bcd56b340e680e45229f4a56b765d97baaf778738e
c1ccc2c(c1)CCCC2
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#8:4]-[C:5](=[O;D1;H0:6])-[C:7]-[C:8](-[OH;D1;+0:9])(-[C:10])-[c:11]>>[#8:4]-[C:5](=[O;D1;H0:6])-[C:7]-[C:8](-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3])(-[C:10])-[c:11]
null
[]
null
null
8
HOUR
To a solution of (±)ethyl 2-(1-hydroxy-1,2,3,4-tetrahydro-4,4-dimethyl-7-bromo-naphthalen-1-yl)acetate (Compound E47, 200.0 mg, 0.586 mmol) and 4-N,N-dimethylaminopyridine (86.0 mg, 0.703 mmol) in 4.0 mL CH2Cl2 at 0° C. was added acetic anhydride (239.3 mg, 2.344 mmol). The resulting solution was warmed to room tempera...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Tertiary alcohol
Ester
null
null
c1ccc2c(c1)CCCC2
HO-
CCOC(=O)C.C(Cl)Cl
null
8
CC(=O)OC(C)=O.CCOC(=O)CC1(O)CCC(C)(C)c2ccc(Br)cc21>CCOC(=O)C.C(Cl)Cl>CCOC(=O)CC1(OC(C)=O)CCC(C)(C)c2ccc(Br)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f22788fdfdc049bab420209786ecbc6d
CCOC(=O)c1ccc(OC(=O)c2ccc3c(c2)C(O)(C(=O)OCC)CCC3(C)C)cc1>>CCOC(=O)C1=CCC(C)(C)c2ccc(C(=O)Oc3ccc(C(=O)OCC)cc3)cc21
CC1(C=2C=CC(=CC2C(CC1)(C(=O)OCC)O)C(=O)OC1=CC=C(C(=O)OCC)C=C1)C.O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>CC1(C=2C=CC(=CC2C(=CC1)C(=O)OCC)C(=O)OC1=CC=C(C(=O)OCC)C=C1)C
O[C:6]1([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]2[cH:13][cH:14][c:15]([C:16](=[O:17])[O: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][c:31]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[CH:7][CH2:8][C:9]([CH3:10])([CH3:11])[c:12]2[cH:13][...
CCOC(=O)c1ccc(OC(=O)c2ccc3c(c2)C(O)(C(=O)OCC)CCC3(C)C)cc1
CCOC(=O)C1=CCC(C)(C)c2ccc(C(=O)Oc3ccc(C(=O)OCC)cc3)cc21
null
null
C1=CC=CC=C1
Functional Group Interconversion
OtherReaction
0d4902b4a0354b39eb06a3aca835d99df3984d26d91039f7ea7b84a4d6ff29ff
694c4e8841d135e88d9ce8d5ff0cd8a883ffff2e7714effccf3da6c8a7d1d0fb
O=C(Oc1ccccc1)c1ccc2c(c1)C=CCC2
O-[C;H0;D4;+0:1]1(-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5])-[CH2;D2;+0:6]-[C:7]-[C:8]-[c:9]:[c:10]-1:[c:11]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[C;H0;D3;+0:1]1=[CH;D2;+0:6]-[C:7]-[C:8]-[c:9]:[c:10]-1:[c:11]
10
[{"value": 10.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of (±)ethyl 4-[[(5,5-dimethyl-8-hydroxy-8-(carbethoxy)-5,6,7,8-tetrahydronaphthalen-2-yl)carbonyl]oxy]benzoate (Compound E54, 35.0 mg, 0.077 mmol) in 10 mL benzene was added a catalytic amount (approximately 2 mg) of p-toluenesulfonic acid monohydrate. The solution was heated to reflux under a Dean-Stark ...
10.6084/m9.figshare.5104873.v1
null
Ester.Tertiary alcohol
Ester
c1ccc2c(c1)CCCC2
C1=Cc2ccccc2CC1
C1=Cc2ccccc2CC1.c1ccccc1
HO-
C1=CC=CC=C1
null
8
CCOC(=O)c1ccc(OC(=O)c2ccc3c(c2)C(O)(C(=O)OCC)CCC3(C)C)cc1>C1=CC=CC=C1>CCOC(=O)C1=CCC(C)(C)c2ccc(C(=O)Oc3ccc(C(=O)OCC)cc3)cc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-453ce30ee5274954b0f4cd3bf04e1207
CC1(C)CCC(=O)c2cc(C(=O)O)ccc21.CC1(C)CCC(=O)c2cc(C(=O)O)ccc21.CCOC(C)=O.CN(C)c1ccccn1>>CC1(C)CCC(=O)c2cc(C(=O)Oc3ccc(C(=O)OCc4ccccc4)cc3)ccc21
CN(C)C1=NC=CC=C1.C(C)(=O)OCC.CC1(C=2C=CC(=CC2C(CC1)=O)C(=O)O)C.CC1(C=2C=CC(=CC2C(CC1)=O)C(=O)O)C>>C(C1=CC=CC=C1)OC(C1=CC=C(C=C1)OC(=O)C1=CC=2C(CCC(C2C=C1)(C)C)=O)=O
CC1(C)CCC(=O)[c:15]2[c:14]1[cH:29][cH:28][c:17]([C:18](=[O:19])[OH:20])[cH:16]2.[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH:9][c:10]([C:11](=[O:12])[OH:13])[cH:30][cH:31][c:32]21.CC(=O)O[CH2:21][CH3:27].CN(C)[c:22]1n[cH:26][cH:25][cH:24][cH:23]1>>[CH3:1][C:2]1([CH3:3])[CH2:4][CH2:5][C:6](=[O:7])[c:8]2[cH...
CC1(C)CCC(=O)c2cc(C(=O)O)ccc21.CC1(C)CCC(=O)c2cc(C(=O)O)ccc21.CCOC(C)=O.CN(C)c1ccccn1
CC1(C)CCC(=O)c2cc(C(=O)Oc3ccc(C(=O)OCc4ccccc4)cc3)ccc21
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
b8e18650f2f7b7caf5929c1531b8dd577696d464ec72569f4ab2648f973f63cd
c97b5103fb5809046a98660f39dac8bdf0ef3933daf7a854242cffd272e2b30b
O=C(OCc1ccccc1)c1ccc(OC(=O)c2ccc3c(c2)C(=O)CCC3)cc1
C-C(=O)-O-[CH2;D2;+0:1]-[CH3;D1;+0:2].C-C1(-C)-C-C-C(=O)-[c;H0;D3;+0:3]2:[c:4]:[c:5](-[C:6](=[O;D1;H0:7])-[OH;D1;+0:8]):[c:9]:[c:10]:[c;H0;D3;+0:11]:2-1.C-N(-C)-[c;H0;D3;+0:12]1:[c:13]:[c:14]:[c:15]:[cH;D2;+0:16]:n:1.[O;D1;H0:17]=[C:18](-[OH;D1;+0:19])-[c:20]>>[O;D1;H0:17]=[C:18](-[c:20])-[O;H0;D2;+0:19]-[c;H0;D3;+0:11...
null
[]
null
null
10
MINUTE
To a solution of 5,5-dimethyl-5,6,7,8-tetrahydro-8-oxo-naphthalen-2-carboxylic acid (Compound E3, 386 mg, 1.77 mmol) in dimethylformamide (4 mL) was added 1-(3-dimethylaminopropyl)-3-ethylcarboimide hydrochloride (440 mg, 2.3 mmol) followed by dimethylamino pyridine (DMAP) (280 mg, 2.3 mmol). The mixture was stirred fo...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Ketone.Ester.Tertiary amine
Ester.Ester
c1ccc2c(c1)CCCC2.c1ccncc1
c1ccccc1.c1ccccc1
c1ccc2c(c1)CCCC2.c1ccccc1.c1ccccc1
HO-
CN(C=O)C
null
0.166667
CC1(C)CCC(=O)c2cc(C(=O)O)ccc21.CC1(C)CCC(=O)c2cc(C(=O)O)ccc21.CCOC(C)=O.CN(C)c1ccccn1>CN(C=O)C>CC1(C)CCC(=O)c2cc(C(=O)Oc3ccc(C(=O)OCc4ccccc4)cc3)ccc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4fb35b7c4bda4aad9a8f5688f126c64d
C=CN1CCCC1=O>>C=CN1CCCC1=O
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C(C(=C)C)(=O)OCCCCCCCCCCCC.C(=C)N1C(CCC1)=O.N(=NC(C#N)(C)C)C(C#N)(C)C.C(=C)N1C(CCC1)=O.C(C(=C)C)(=O)OCCCCCCCCCCCC>>C(C(=C)C)(=O)OCCCCCCCCCCCC.C(=C)N1C(CCC1)=O
[CH2:19]=[CH:20][N:21]1[CH2:22][CH2:23][CH2:24][C:25]1=[O:26]>>[CH2:19]=[CH:20][N:21]1[CH2:22][CH2:23][CH2:24][C:25]1=[O:26]
C=CN1CCCC1=O
C=CN1CCCC1=O
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1CCCN1
null
null
[]
30
CELSIUS
10
MINUTE
A solution of 95 parts by weight of lauryl methacrylate in 200 parts by weight of IP Solvent 1620 (produced by Idemitsu Petrochemical Co., Ltd.) is prepared. Argon gas is blown into the solution for 10 minutes to displace the gas entrained in the entire reaction system with argon gas. Then, benzoyl peroxide is added as...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
C1CC[NH]C1
null
null
30
0.166667
C=CN1CCCC1=O>>C=CN1CCCC1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-62dac6c13c4c4aa59ca7877a94095e3c
CCCCC[Si@@H]1CC[C@@H](CC(O)C#Cc2ccc(F)cc2)CC1>>CCCCC[Si@@H]1CC[C@@H](/C=C/C#Cc2ccc(F)cc2)CC1
FC1=CC=C(C=C1)C#CC(C[C@@H]1CC[Si@H](CC1)CCCCC)O.O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>FC1=CC=C(C=C1)C#C\C=C\[C@@H]1CC[Si@H](CC1)CCCCC
O[CH:11]([CH2:10][C@H:9]1[CH2:8][CH2:7][Si@H:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[CH2:22][CH2:21]1)[C:12]#[C:13][c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][Si@H:6]1[CH2:7][CH2:8][C@H:9](/[CH:10]=[CH:11]/[C:12]#[C:13][c:14]2[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]2)[CH2:2...
CCCCC[Si@@H]1CC[C@@H](CC(O)C#Cc2ccc(F)cc2)CC1
CCCCC[Si@@H]1CC[C@@H](/C=C/C#Cc2ccc(F)cc2)CC1
null
null
C1=CC=CC=C1
Functional Group Interconversion
OtherReaction
24323612d5486e9fd0704523d3a93bd4db9c6e3295677a91ceb1aea86b497d01
f8118e7f3e1d7109575c0c77239dee8da98ec71a2b23460bcda2084274bdf7e7
C(#Cc1ccccc1)/C=C/C1CC[SiH2]CC1
O-[CH;D3;+0:1](-[C:2]#[C:3]-[c:4])-[CH2;D2;+0:5]-[C:6](-[C:7])-[C:8]>>[C:7]-[C:6](/[CH;D2;+0:5]=[CH;D2;+0:1]/[C:2]#[C:3]-[c:4])-[C:8]
15.9
[{"value": 15.9, "product": "FC1=CC=C(C=C1)C#C\\C=C\\[C@@H]1CC[Si@H](CC1)CCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 15.9, "product": "FC1=CC=C(C=C1)C#C\\C=C\\[C@@H]1CC[Si@H](CC1)CCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1-(4-fluorophenyl)-4-(trans-4-pentyl-4-silacyclohexyl)-1-butyne-3-ol 8.0 g (24 mmol), p-toluenesulfonic acid monohydrate 1.6 g, and benzene 200 ml was heated under reflux to remove the water and then subjected to a conventional post-treatment. The reaction mixture thus obtained was not only a mixture of tr...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
null
null
C1CC[SiH]CC1.c1ccccc1
HO-
C1=CC=CC=C1
null
null
CCCCC[Si@@H]1CC[C@@H](CC(O)C#Cc2ccc(F)cc2)CC1>C1=CC=CC=C1>CCCCC[Si@@H]1CC[C@@H](/C=C/C#Cc2ccc(F)cc2)CC1