dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c1e4715ed61c463392456f127089a013
CCCCC12CCC(=O)C(Br)=C1c1ccc(O)cc1C2.CCCCCC>>C=C1CCC2(CCCC)Cc3cc(O)ccc3C2=C1Br
BrC=1C(CCC2(CC3=CC(=CC=C3C12)O)CCCC)=O.[Li]CCCC.CCCCCC>>BrC=1C(CCC2(CC3=CC(=CC=C3C12)O)CCCC)=C
O=[C:2]1[CH2:3][CH2:4][C:5]2([CH2:6][CH2:7][CH2:8][CH3:9])[CH2:10][c:11]3[cH:12][c:13]([OH:14])[cH:15][cH:16][c:17]3[C:18]2=[C:19]1[Br:20].CCCCC[CH3:1]>>[CH2:1]=[C:2]1[CH2:3][CH2:4][C:5]2([CH2:6][CH2:7][CH2:8][CH3:9])[CH2:10][c:11]3[cH:12][c:13]([OH:14])[cH:15][cH:16][c:17]3[C:18]2=[C:19]1[Br:20]
CCCCC12CCC(=O)C(Br)=C1c1ccc(O)cc1C2.CCCCCC
C=C1CCC2(CCCC)Cc3cc(O)ccc3C2=C1Br
null
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
O1CCCC1
C-C Coupling
OtherReaction
73dd4b4de03e44885902962d344ae12b8d61100cb66e2d30aaa505f073a7553b
93d1d0c14c74e7b67ee3b36f962bbc71783135eee73a676c6ddf9dcb58a45254
C=C1C=C2c3ccccc3CC2CC1
C-C-C-C-C-[CH3;D1;+0:1].O=[C;H0;D3;+0:2]1-[C:3]-[C:4]-[C:5]-[C:6](=[C:7]-1-[Br;D1;H0:8])-[c:9]>>[Br;D1;H0:8]-[C:7]1=[C:6](-[c:9])-[C:5]-[C:4]-[C:3]-[C;H0;D3;+0:2]-1=[CH2;D1;+0:1]
null
[]
0
CELSIUS
10
MINUTE
A suspension of methyltriphenylphosphonium bromide (373 mg, 1.04 mmol) in anhydrous tetrahydrofuran (2 mL) was cooled in an ice bath and stirred under a nitrogen atmosphere while 2.5 N nBuLi in hexane (0.36 mL, 0.90 mmol) was added by syringe. The mixture was stirred at 0° C. for 10 minutes to complete formation of the...
10.6084/m9.figshare.5104873.v1
null
Ketone
Vinyl
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.O1CCCC1
0
0.166667
CCCCC12CCC(=O)C(Br)=C1c1ccc(O)cc1C2.CCCCCC>[Br-].C[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.O1CCCC1>C=C1CCC2(CCCC)Cc3cc(O)ccc3C2=C1Br
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e977cc0a97344407890f175b08eabeec
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)cc1C2
BrC=1C(CCC2(CC3=CC(=CC=C3C12)OC)CCCC)=O.[Cu]C#N>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C#N)OC
Br[C:10]1=[C:13]2[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]1=[O:9])[CH2:22][c:21]1[c:14]2[cH:15][cH:16][c:17]([O:18][CH3:19])[cH:20]1>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]#[N:12])=[C:13]1[c:14]1[cH:15][cH:16][c:17]([O:18][CH3:19])[cH:20][c:21]1[CH2:22]2
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)cc1C2
null
null
CN1C(CCC1)=O
Miscellaneous
OtherReaction
9adadf535edd63596f40811ded4b5d76fe0b83c469549ed7abf606d845021290
8953536f7fe46a44d657de6166386d42d9afab94586603b5dca76fc653fbf47b
O=C1C=C2c3ccccc3CC2CC1
Br-[C;H0;D3;+0:1](=[C:2](-[C:3])-[c:4])-[C:5](=[O;D1;H0:6])-[C:7]>>[C:3]-[C:2](=[C;H0;D3;+0:1](-[C:8]#[N;D1;H0:9])-[C:5](=[O;D1;H0:6])-[C:7])-[c:4]
81
[{"value": 81.0, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C#N)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
160
CELSIUS
null
null
A solution of 4-bromo-9a-butyl-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (50 mg, 0.138 mmol) in anhydrous 1-methyl-2-pyrrolidinone (0.276 mL) was treated with copper(I) cyanide (25 mg, 0.275 mmol). The resulting mixture was stirred under a nitrogen atmosphere and heated in an oil bath at 160° C. for 40 minutes. Th...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide
Ketone.Nitrile
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
Br-
CN1C(CCC1)=O
160
null
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2>CN1C(CCC1)=O>CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-29b5c03d6765413ea7a1f79ffdd37133
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(C#N)=C1c1ccc(O)cc1C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C#N)OC.Cl.N1=CC=CC=C1>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C#N)O
C[O:18][c:17]1[cH:16][cH:15][c:14]2[c:20]([cH:19]1)[CH2:21][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]#[N:12])=[C:13]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]#[N:12])=[C:13]1[c:14]1[cH:15][cH:16][c:17]([OH:18])[cH:19][c:20]1[CH2:21]2
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)cc1C2
CCCCC12CCC(=O)C(C#N)=C1c1ccc(O)cc1C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
192.5
CELSIUS
null
null
A mixture of 9a-butyl-4-cyano-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (17 mg) and pyridine hydrochloride (2 g) was placed under a nitrogen atmosphere and heated in an oil bath at 190-195° C. for 1 hour. After cooling to room temperature, the mixture was partitioned between EtOAc (20 ml) and water (30 mL). The or...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
null
192.5
null
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(C#N)=C1c1ccc(O)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-38f635a0ee364faa8595c22f5d4de8f8
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2.c1ccc([CH2][Sn]23[CH2]CCN(CC[CH2]2)CC[CH2]3)cc1>>CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(OC)cc1C2
BrC=1C(CCC2(CC3=CC(=CC=C3C12)OC)CCCC)=O.C(C1=CC=CC=C1)[Sn]12CCCN(CCC1)CCC2>>C(C1=CC=CC=C1)C=1C(CCC2(CC3=CC(=CC=C3C12)OC)CCCC)=O
Br[C:10]1=[C:18]2[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]1=[O:9])[CH2:27][c:26]1[c:19]2[cH:20][cH:21][c:22]([O:23][CH3:24])[cH:25]1.C1CN2CC[CH2][Sn]([CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)([CH2]1)[CH2]CC2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH2:11][c:12]3[c...
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2.c1ccc([CH2][Sn]23[CH2]CCN(CC[CH2]2)CC[CH2]3)cc1
CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(OC)cc1C2
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
C1(=CC=CC=C1)C
C-C Coupling
Stille reaction_benzyl
3021b6ee7125eedf347f194421a4ef6415260c3f4a43f20fe0cf50f76c5c60f3
9ee104fc2d9c1fefe82f5ea62791da6f9a31f1bd9f50dea4348bdecc37d4a644
O=C1CCC2Cc3ccccc3C2=C1Cc1ccccc1
Br-[C;H0;D3;+0:1](=[C:2](-[C:3])-[c:4])-[C:5](=[O;D1;H0:6])-[C:7].[c:8]:[c:9](-[CH2;D2;+0:10]-[Sn]12-[CH2]-C-C-N(-C-C-[CH2]-1)-C-C-[CH2]-2):[c:11]>>[C:3]-[C:2](=[C;H0;D3;+0:1](-[CH2;D2;+0:10]-[c:9](:[c:8]):[c:11])-[C:5](=[O;D1;H0:6])-[C:7])-[c:4]
95
[{"value": 95.0, "product": "C(C1=CC=CC=C1)C=1C(CCC2(CC3=CC(=CC=C3C12)OC)CCCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A mixture of 4-bromo-9a-butyl-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (29.6 mg, 0.0847 mmol), 5-benzyl-1-aza-5-stanna-bicyclo[3.3.3]undecane (38.5 mg, 85% weight pure, 0.0935 mmol), and Pd(PPh3)4 (9.8 mg, 0.00848 mmol) in anhydrous toluene (1.3 mL) was degassed, placed under a nitrogen atmosphere, stirred, and h...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Ketone.Tertiary amine.Tin
Ketone
C1=C2c3ccccc3CC2CCC1.C1CN2CC[CH2][Sn]([CH2]1)[CH2]CC2
C1=C2c3ccccc3CC2CCC1
c1ccccc1.C1=C2c3ccccc3CC2CCC1
HBr.Sn
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C
100
null
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2.c1ccc([CH2][Sn]23[CH2]CCN(CC[CH2]2)CC[CH2]3)cc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C>CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(OC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-704e1bcd500a470491743a4b68c37bf0
CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(O)cc1C2
C(C1=CC=CC=C1)C=1C(CCC2(CC3=CC(=CC=C3C12)OC)CCCC)=O.B(Br)(Br)Br>>C(C1=CC=CC=C1)C=1C(CCC2(CC3=CC(=CC=C3C12)O)CCCC)=O
C[O:23][c:22]1[cH:21][cH:20][c:19]2[c:25]([cH:24]1)[CH2:26][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)=[C:18]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH2:11][c:12]3[cH:13][cH:14][cH:15][cH:16][cH:17]3)=[C:18]...
CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(OC)cc1C2
CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(O)cc1C2
null
null
C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1CCC2Cc3ccccc3C2=C1Cc1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
3.5
HOUR
A solution of 4-benzyl-9a-butyl-7-methoxy-1,2,9,9a-tetrahydrofluoren-3-one (25.9 mg, 0.718 mmol) in anhydrous CH2Cl2 (1.2 mL) was cooled in a dry ice-acetone bath and stirred under a nitrogen atmosphere while 1M BBr3 in CH2Cl2 (0.215 mL, 0.215 mmol) was added dropwise by syringe. The cooling bath was removed and the mi...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.C1=C2c3ccccc3CC2CCC1
Other
C(Cl)Cl
null
3.5
CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(OC)cc1C2>C(Cl)Cl>CCCCC12CCC(=O)C(Cc3ccccc3)=C1c1ccc(O)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3dd93824a4984141a072324890d98328
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2.CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)[c]1ccc(OCOC)cc1>>CCCCC12CCC(=O)C(c3ccc(OCOC)cc3)=C1c1ccc(OC)cc1C2
BrC=1C(CCC2(CC3=CC(=CC=C3C12)OC)CCCC)=O.C(CCC)[Sn](C1=CC=C(C=C1)OCOC)(CCCC)CCCC>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCOC)OC
Br[C:10]1=[C:21]2[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]1=[O:9])[CH2:30][c:29]1[c:22]2[cH:23][cH:24][c:25]([O:26][CH3:27])[cH:28]1.CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)[c:11]1[cH:12][cH:13][c:14]([O:15][CH2:16][O:17][CH3:18])[cH:19][cH:20]1>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10...
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2.CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)[c]1ccc(OCOC)cc1
CCCCC12CCC(=O)C(c3ccc(OCOC)cc3)=C1c1ccc(OC)cc1C2
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
C1(=CC=CC=C1)C
C-C Coupling
Stille reaction_aryl
034107d4fe65a24d8b46c36ee84093572edbd96657c78798636ee8f3eb50d7b1
0538de7208f7c4515088af2db60bef2f5ed1a90c393cce7cf4a07985b831073d
O=C1CCC2Cc3ccccc3C2=C1c1ccccc1
Br-[C;H0;D3;+0:1](=[C:2](-[C:3])-[c:4])-[C:5](=[O;D1;H0:6])-[C:7].C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-C-C)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12]>>[C:3]-[C:2](=[C;H0;D3;+0:1](-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12])-[C:5](=[O;D1;H0:6])-[C:7])-[c:4]
84.5
[{"value": 84.5, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCOC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
22
HOUR
A mixture of 4-bromo-9a-butyl-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (800 mg, 2.29 mmol), Pd(PPh3)4 (132 mg, 0.114 mmol), and tributyl-(4-methoxymethoxy-phenyl)-stannane (1.174 g, 2.75 mmol) in anhydrous toluene (11.5 mL) was placed under a nitrogen atmosphere and heated with stirring in an oil bath at 100° C. ...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Ketone.Tin
Ketone
C1=C2c3ccccc3CC2CCC1.c1ccccc1
c1ccccc1.C1=C2c3ccccc3CC2CCC1
c1ccccc1.C1=C2c3ccccc3CC2CCC1
HBr.Sn
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C
100
22
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)cc1C2.CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)[c]1ccc(OCOC)cc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.C1(=CC=CC=C1)C>CCCCC12CCC(=O)C(c3ccc(OCOC)cc3)=C1c1ccc(OC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3e877446746d40fd8d3411e8cf355c24
CCCCC12CCC(=O)C(c3ccc(OCOC)cc3)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCOC)OC.Cl>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)O)OC
COC[O:15][c:14]1[cH:13][cH:12][c:11]([C:10]2=[C:18]3[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]2=[O:9])[CH2:27][c:26]2[c:19]3[cH:20][cH:21][c:22]([O:23][CH3:24])[cH:25]2)[cH:17][cH:16]1>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([c:11]3[cH:12][cH:13][c:14]([OH:15])[cH:16][cH:17]3)...
CCCCC12CCC(=O)C(c3ccc(OCOC)cc3)=C1c1ccc(OC)cc1C2
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2
null
null
CO.CCOC(=O)C
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1CCC2Cc3ccccc3C2=C1c1ccccc1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
108.6
[{"value": 92.0, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 108.6, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
A suspension of 9a-butyl-7-methoxy-4-(4-methoxymethoxy-phenyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one (813 mg, 2 mmol) in methanol (12 mL) was warmed in an oil bath at 60° C. and treated with aqueous 2N HCl (4 mL). The resulting mixture was stirred and heated at 60° C. for two hours, then cooled to room temperature and e...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
c1ccccc1.C1=C2c3ccccc3CC2CCC1
HO-
CO.CCOC(=O)C
60
null
CCCCC12CCC(=O)C(c3ccc(OCOC)cc3)=C1c1ccc(OC)cc1C2>CO.CCOC(=O)C>CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1a4333548b494637b07c329108b8dcf4
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2.ClCCN1CCCCC1>>CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(OC)cc1C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)O)OC.C([O-])([O-])=O.[Cs+].[Cs+].Cl.ClCCN1CCCCC1>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCCN1CCCCC1)OC
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([c:11]3[cH:12][cH:13][c:14]([OH:15])[cH:24][cH:25]3)=[C:26]1[c:27]1[cH:28][cH:29][c:30]([O:31][CH3:32])[cH:33][c:34]1[CH2:35]2.Cl[CH2:16][CH2:17][N:18]1[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]1>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=...
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2.ClCCN1CCCCC1
CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(OC)cc1C2
null
null
CCOC(=O)C.CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C1CCC2Cc3ccccc3C2=C1c1ccc(OCCN2CCCCC2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#7:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
96.3
[{"value": 96.0, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCCN1CCCCC1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.3, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCCN1CCCCC1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
A mixture of crude 9a-butyl-4-(4-hydroxyphenyl)-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (787 mg, approx. 2 mmol), cesium carbonate (1.564 g, 4.8 mmol), and 1-(2-chloroethyl)-piperidine monohydrochloride (442 mg, 2.4 mmol) in acetone (5 mL) was stirred and heated in an oil bath at 60° C. for 4 hours. After coolin...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.C1CC[NH]CC1.C1=C2c3ccccc3CC2CCC1
HCl
CCOC(=O)C.CC(=O)C
60
null
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2.ClCCN1CCCCC1>CCOC(=O)C.CC(=O)C>CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(OC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c98b40057f6544e1a3bf91358949001b
CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(O)cc1C2
CCS.[Al+3].[Cl-].[Cl-].[Cl-].Cl.C(=O)(O)[O-].[Na+].C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCCN1CCCCC1)OC>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OCCN1CCCCC1)O
C[O:31][c:30]1[cH:29][cH:28][c:27]2[c:33]([cH:32]1)[CH2:34][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([c:11]3[cH:12][cH:13][c:14]([O:15][CH2:16][CH2:17][N:18]4[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]4)[cH:24][cH:25]3)=[C:26]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:...
CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(OC)cc1C2
CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(O)cc1C2
null
null
CCOC(=O)C.O.O1CCCC1.C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1CCC2Cc3ccccc3C2=C1c1ccc(OCCN2CCCCC2)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
0
CELSIUS
3
MINUTE
An ice-cold solution of 9a-butyl-7-methoxy-4-{4-[2-(1-piperidinyl)-ethoxy]phenyl}-1,2,9,9a-tetrahydro-3H-fluoren-3-one (85 mg, 96% weight pure, 0.172 mmol) in anhydrous CH2Cl2 (1.2 mL) was placed under a nitrogen atmosphere and treated with EtSH (0.055 mL, 0.743 mmol). The resulting solution was added by syringe to AlC...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.C1CC[NH]CC1.C1=C2c3ccccc3CC2CCC1
Other
CCOC(=O)C.O.O1CCCC1.C(Cl)Cl
0
0.05
CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(OC)cc1C2>CCOC(=O)C.O.O1CCCC1.C(Cl)Cl>CCCCC12CCC(=O)C(c3ccc(OCCN4CCCCC4)cc3)=C1c1ccc(O)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-97264f6f2909414bad48b9659123da7c
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(O)cc1C2
CC(C)S.C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)O)OC.[Al+3].[Cl-].[Cl-].[Cl-].Cl>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)O)O
C[O:23][c:22]1[cH:21][cH:20][c:19]2[c:25]([cH:24]1)[CH2:26][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([c:11]3[cH:12][cH:13][c:14]([OH:15])[cH:16][cH:17]3)=[C:18]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([c:11]3[cH:12][cH:13][c:14]([OH:15])[cH:16][cH:17]3)=[C:18]...
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(O)cc1C2
null
null
CCOC(=O)C.C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1CCC2Cc3ccccc3C2=C1c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
0
CELSIUS
null
null
An ice-cold solution of 9a-butyl-4-(4-hydroxy-phenyl)-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (29 mg, 0.08 mmol) in anhydrous CH2Cl2 (1 mL) was added to AlCl3 (96 mg, 0.72 mmol) contained in an ice cooled flask. The mixture was stirred at 0° C. under a nitrogen atmosphere and treated with 2-propanethiol (0.056 m...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.C1=C2c3ccccc3CC2CCC1
Other
CCOC(=O)C.C(Cl)Cl
0
null
CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(OC)cc1C2>CCOC(=O)C.C(Cl)Cl>CCCCC12CCC(=O)C(c3ccc(O)cc3)=C1c1ccc(O)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-adef68c798704d7e9c50dde96c01cffe
CCCCC12CCC(=O)C(c3ccc(OS(=O)(=O)C(F)(F)F)cc3)=C1c1ccc(OC)cc1C2.CCC[CH2][Sn](/[CH]=C/C(=O)OC)([CH2]CCC)[CH2]CCC>>CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)OC)cc3)=C1c1ccc(OC)cc1C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)OS(=O)(=O)C(F)(F)F)OC.C(CCC)[Sn](/C=C/C(=O)OC)(CCCC)CCCC.[Cl-].[Li+]>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)/C=C/C(=O)OC)OC
O=S(=O)(O[c:14]1[cH:13][cH:12][c:11]([C:10]2=[C:23]3[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]2=[O:9])[CH2:32][c:31]2[c:24]3[cH:25][cH:26][c:27]([O:28][CH3:29])[cH:30]2)[cH:22][cH:21]1)C(F)(F)F.CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)/[CH:15]=[CH:16]/[C:17](=[O:18])[O:19][CH3:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]...
CCCCC12CCC(=O)C(c3ccc(OS(=O)(=O)C(F)(F)F)cc3)=C1c1ccc(OC)cc1C2.CCC[CH2][Sn](/[CH]=C/C(=O)OC)([CH2]CCC)[CH2]CCC
CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)OC)cc3)=C1c1ccc(OC)cc1C2
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CN(C=O)C
C-C Coupling
Stille reaction_other OTf
b776466232e20bae8fda61cba5b8d23b6dd6bb33b4d0cbf8dc63285327f4decc
46de4d1253710b3a7d4f46887df51b2ccba46e0a9427959558bd6f96ec8696eb
O=C1CCC2Cc3ccccc3C2=C1c1ccccc1
C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-C-C)/[CH;D2;+0:1]=[C:2]/[C:3](=[O;D1;H0:4])-[#8:5]-[C;D1;H3:6].F-C(-F)(-F)-S(=O)(=O)-O-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]>>[C;D1;H3:6]-[#8:5]-[C:3](=[O;D1;H0:4])/[C:2]=[CH;D2;+0:1]/[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]
96.4
[{"value": 96.4, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)/C=C/C(=O)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
null
null
A mixture of 9a-butyl-7-methoxy-4-[4-(trifluoromethane-sulfonyloxy)-phenyl]-1,2,9,9a-tetrahydro-3H-fluoren-3-one (98.9 mg, 0.2 mmol), methyl (E)-3-tributylstannyl-acrylate (112.5 mg, 0.3 mmol) and lithium chloride (25.4 mg, 0.6 mmol) in anhydrous dimethylformamide (1.0 mL) was purged with nitrogen and treated with bis(...
10.6084/m9.figshare.5104873.v1
null
Triflate.Tin
null
c1ccccc1
c1ccccc1
c1ccccc1.C1=C2c3ccccc3CC2CCC1
TfOH.HO-.Sn
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C=O)C
90
null
CCCCC12CCC(=O)C(c3ccc(OS(=O)(=O)C(F)(F)F)cc3)=C1c1ccc(OC)cc1C2.CCC[CH2][Sn](/[CH]=C/C(=O)OC)([CH2]CCC)[CH2]CCC>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C=O)C>CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)OC)cc3)=C1c1ccc(OC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-80bc9e40f544428a8eacc0993ff83f3d
CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)OC)cc3)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)O)cc3)=C1c1ccc(O)cc1C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)/C=C/C(=O)OC)OC.Cl.N1=CC=CC=C1.Cl.N1=CC=CC=C1>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C1=CC=C(C=C1)/C=C/C(=O)O)O
C[O:19][C:17](/[CH:16]=[CH:15]/[c:14]1[cH:13][cH:12][c:11]([C:10]2=[C:22]3[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]2=[O:9])[CH2:30][c:29]2[c:23]3[cH:24][cH:25][c:26]([O:27]C)[cH:28]2)[cH:21][cH:20]1)=[O:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([c:11]3[cH:12][cH:13][c:14](/...
CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)OC)cc3)=C1c1ccc(OC)cc1C2
CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)O)cc3)=C1c1ccc(O)cc1C2
null
null
null
Deprotection
OtherReaction
4cea9c1cf4071f9c3a5e0d042ee7e87c9888ee05636b0c5b9dfd162b490d7fb6
707aece9d1d6de1fa508344f68d9f46b61d18785c603f5e19232e661c94aa284
O=C1CCC2Cc3ccccc3C2=C1c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])/[C:4]=[C:5]/[c:6].C-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])/[C:4]=[C:5]/[c:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]
null
[]
190
CELSIUS
2
HOUR
A mixture of methyl (2E)-3-[4-(9a-butyl-7-methoxy-3-oxo-2,3,9,9a-tetrahydro-1H-fluoren-4-yl)phenyl]-2-propenoate (60 mg, 92% weight pure, 0.128 mmol) and pyridine hydrochloride (741 mg, 6.41 mmol) was placed under a nitrogen atmosphere, heated in an oil bath at 190° C., and stirred. The reaction flask was periodically ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether
Carboxylic acid.Aromatic alcohol
null
null
c1ccccc1.C1=C2c3ccccc3CC2CCC1
Other
null
190
2
CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)OC)cc3)=C1c1ccc(OC)cc1C2>>CCCCC12CCC(=O)C(c3ccc(/C=C/C(=O)O)cc3)=C1c1ccc(O)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ea29327def8e4fbe9589fa709757dc0d
CCCCC1Cc2cc(OC)ccc2C1=O.NC(=O)CCC(=O)NBr>>CCCCC1Cc2c(ccc(OC)c2Br)C1=O
C(CCC)C1C(C2=CC=C(C=C2C1)OC)=O.BrNC(CCC(=O)N)=O>>BrC1=C2CC(C(C2=CC=C1OC)=O)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]2)[C:16]1=[O:17].NC(=O)CCC(=O)N[Br:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][cH:10][c:11]([O:12][CH3:13])[c:14]2[Br:15])[C:16]1=[O:17]
CCCCC1Cc2cc(OC)ccc2C1=O.NC(=O)CCC(=O)NBr
CCCCC1Cc2c(ccc(OC)c2Br)C1=O
null
null
CCOC(=O)C.CN(C=O)C
Functional Group Interconversion
Bromination
7edae5a3fcd7108ed4ae8780d7a956cfe7b0b617ac7185cf26b15e1960b63e69
f0c47cfd4d5d7957b01579ba4ffee0b3c64b05d7411e52b95a7ea89b926af55c
O=C1CCc2ccccc21
N-C(=O)-C-C-C(=O)-N-[Br;H0;D1;+0:1].[#8:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6](:[c:7]-[C:8]=[O;D1;H0:9])-[C:10]>>[#8:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[Br;H0;D1;+0:1]):[c:6](:[c:7]-[C:8]=[O;D1;H0:9])-[C:10]
3
[{"value": 3.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
14
HOUR
A solution of 2-butyl-5-methoxy-1-indanone (1.869 g, 8.56 mmol) in anhydrous dimethylformamide (8.6 mL) was treated with N-bromosuccinamide (1.676 g, 9.42 mmol). The resulting mixture was stirred under a nitrogen atmosphere and at room temperature for 14 hours, and then heated in an oil bath at 50° C. for 4 hours. Afte...
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Primary amide.Secondary amide
Aromatic halide
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
CCOC(=O)C.CN(C=O)C
null
14
CCCCC1Cc2cc(OC)ccc2C1=O.NC(=O)CCC(=O)NBr>CCOC(=O)C.CN(C=O)C>CCCCC1Cc2c(ccc(OC)c2Br)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-16948c22a2304cf0b6f9a96bed7293bb
CCCCC1Cc2c(ccc(OC)c2Br)C1=O.[CH3][Sn]([CH3])([CH3])[CH3]>>CCCCC1Cc2c(ccc(OC)c2C)C1=O
BrC1=C2CC(C(C2=CC=C1OC)=O)CCCC.[Li+].[Cl-].C1=CC=C(C=C1)P(C2=CC=CC=C2)C3=CC=CC=C3.[Sn](C)(C)(C)C>>C(CCC)C1C(C2=CC=C(C(=C2C1)C)OC)=O
Br[c:14]1[c:7]2[c:8]([cH:9][cH:10][c:11]1[O:12][CH3:13])[C:16](=[O:17])[CH:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2.[CH3][Sn]([CH3])([CH3])[CH3:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][cH:10][c:11]([O:12][CH3:13])[c:14]2[CH3:15])[C:16]1=[O:17]
CCCCC1Cc2c(ccc(OC)c2Br)C1=O.[CH3][Sn]([CH3])([CH3])[CH3]
CCCCC1Cc2c(ccc(OC)c2C)C1=O
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
O.CN(C=O)C
C-C Coupling
Stille reaction_other
5f823a1f140c9788378795502c3f73833375dcf595f9e9d5f6b25610b5e941bf
db27eeefac0475c6d74fa10b3167e95a61caaae74e8bbafd45892452c0c3d4d6
O=C1CCc2ccccc21
Br-[c;H0;D3;+0:1](:[c:2](-[#8:3]):[c:4]):[c:5](:[c:6]-[C:7]=[O;D1;H0:8])-[C:9].[CH3;D1;+0:10]-[Sn](-[CH3])(-[CH3])-[CH3]>>[#8:3]-[c:2](:[c:4]):[c;H0;D3;+0:1](-[CH3;D1;+0:10]):[c:5](:[c:6]-[C:7]=[O;D1;H0:8])-[C:9]
496.7
[{"value": 496.7, "product": "C(CCC)C1C(C2=CC=C(C(=C2C1)C)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A solution of 4-bromo-2-butyl-5-methoxy-1-indanone (1.159 g, 3.90 mmol) in anhydrous dimethylformamide (39 mL) was treated with LiCl (455 mg, 10.73 mmol), PPh3 (205 mg, 0.78 mmol), PdCl2(PPh3)2 (205 mg, 0.292 mmol) and Me4Sn (1.08 mL, 7.80 mmol). The mixture was placed under a nitrogen atmosphere, then stirred and heat...
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Aromatic halide.Tin
null
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HBr.Sn
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.O.CN(C=O)C
100
null
CCCCC1Cc2c(ccc(OC)c2Br)C1=O.[CH3][Sn]([CH3])([CH3])[CH3]>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.O.CN(C=O)C>CCCCC1Cc2c(ccc(OC)c2C)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2a4993889ca6480cb0bfdfaca22cc970
C=CC(C)=O.CCCCC1Cc2c(ccc(OC)c2C)C1=O>>CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2C)C1=O
C(=C)C(=O)C.N12CCCCCC2=NCCC1.C(CCC)C1C(C2=CC=C(C(=C2C1)C)OC)=O>>C(CCC)C1(C(C2=CC=C(C(=C2C1)C)OC)=O)CCC(C)=O
[CH2:6]=[CH:7][C:8]([CH3:9])=[O:10].[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:11][c:12]2[c:13]([cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]2[CH3:20])[C:21]1=[O:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]1([CH2:6][CH2:7][C:8]([CH3:9])=[O:10])[CH2:11][c:12]2[c:13]([cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]2[CH3:20])[C:21]1=[O:22]
C=CC(C)=O.CCCCC1Cc2c(ccc(OC)c2C)C1=O
CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2C)C1=O
null
null
O1CCCC1.CCOCC
C-C Coupling
OtherReaction
c504c0d32586144b6874498db3cc99d4d5bb675e1b2e725385a0386d3f14ac05
68a0b2d4768a64505cf15a6dd6bbd75216aef3c50fb86aff9b39341b3e49f06d
O=C1CCc2ccccc21
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[CH2;D1;+0:5].[C:6]-[C:7]-[CH;D3;+0:8]1-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]>>[C:6]-[C:7]-[C;H0;D4;+0:8]1(-[CH2;D2;+0:5]-[CH2;D2;+0:4]-[C:2](-[C;D1;H3:1])=[O;D1;H0:3])-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]
81.4
[{"value": 81.4, "product": "C(CCC)C1(C(C2=CC=C(C(=C2C1)C)OC)=O)CCC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
HOUR
Methyl vinyl ketone (MVK, 0.49 mL, 5.9 mmol) and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU, 0.12 mL, 0.8 mmol) were added to a solution of impure 2-butyl-5-methoxy-4-methyl-1-indanone (0.90 g, 3.9 mmol) in anhydrous tetrahydrofuran (THF, 3.9 mL). The resulting solution was stirred at room temperature for 30 hours, then d...
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Ketone.Ketone.Vinyl
Ketone.Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
null
O1CCCC1.CCOCC
null
30
C=CC(C)=O.CCCCC1Cc2c(ccc(OC)c2C)C1=O>O1CCCC1.CCOCC>CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2C)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c4d098d6e0c64655809c3a2af90167be
CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2C)C1=O>>CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2
C(CCC)C1(C(C2=CC=C(C(=C2C1)C)OC)=O)CCC(C)=O.C(C)(=O)O.N1CCCC1>>C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)OC)C
O=[C:11]1[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8](=[O:9])[CH3:10])[CH2:21][c:20]2[c:12]1[cH:13][cH:14][c:15]([O:16][CH3:17])[c:18]2[CH3:19]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[CH:10]=[C:11]1[c:12]1[cH:13][cH:14][c:15]([O:16][CH3:17])[c:18]([CH3:19])[c:20]1[CH2:21]2
CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2C)C1=O
CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2
null
null
CCOCC.C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
85ff0aa8be631f96366b93c0f2ba199404913ad074e95e1352514ec4827258a9
b7bc018679e3f4c5a72b49c90c858cc3bcb4db12dedb0216b468af50ef8a00a3
O=C1C=C2c3ccccc3CC2CC1
O=[C;H0;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[C:5]-[C:6]-1(-[C:7])-[C:8]-[C:9]-[C:10](-[CH3;D1;+0:11])=[O;D1;H0:12]>>[C:7]-[C:6]12-[C:5]-[c:4]:[c:2](:[c:3])-[C;H0;D3;+0:1]-1=[CH;D2;+0:11]-[C:10](=[O;D1;H0:12])-[C:9]-[C:8]-2
55.5
[{"value": 55.5, "product": "C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)OC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A solution of impure 2-butyl-5-methoxy-4-methyl-2-(3-oxo-butyl)-1-indanone (0.96 g, 3.17 mmol), acetic acid (0.182 mL, 3.18 mmol) and pyrrolidine (0.265 mL, 3.18 mmol) in anhydrous toluene (15.9 mL) was stirred and heated in an oil bath at 80° C. for 16 hours. After cooling, the reaction mixture was diluted with Et2O (...
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Ketone.Ketone
Ketone
c1ccc2c(c1)CCC2
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
CCOCC.C1(=CC=CC=C1)C
80
null
CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2C)C1=O>CCOCC.C1(=CC=CC=C1)C>CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a3003665ff944b9aba117505583cfbac
CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2>>CCCCC12CCC(=O)C=C1c1ccc(O)c(C)c1C2
C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)OC)C.B(Br)(Br)Br>>C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)O)C
C[O:16][c:15]1[cH:14][cH:13][c:12]2[c:19]([c:17]1[CH3:18])[CH2:20][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[CH:10]=[C:11]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[CH:10]=[C:11]1[c:12]1[cH:13][cH:14][c:15]([OH:16])[c:17]([CH3:18])[c:19]1[CH2:20]2
CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2
CCCCC12CCC(=O)C=C1c1ccc(O)c(C)c1C2
null
null
C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
99.1
[{"value": 99.1, "product": "C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A solution of 9a-butyl-7-methoxy-8-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (28.4 mg, 0.1 mmol) in anhydrous CH2Cl2 (1.7 mL) was stirred under a nitrogen atmosphere and cooled in a dry ice-acetone bath while 1M BBr3 in CH2Cl2 (0.30 mL, 0.3 mmol) was added dropwise by syringe. The cooling bath was removed and the rea...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
C(Cl)Cl
null
4
CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2>C(Cl)Cl>CCCCC12CCC(=O)C=C1c1ccc(O)c(C)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f46b74a624d44e92b683ec8f7cb4db6a
BrBr.CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2>>CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(C)c1C2
BrBr.C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)OC)C.C(Cl)(Cl)(Cl)Cl.C(=O)(O)[O-].[Na+]>>BrC=1C(CCC2(CC3=C(C(=CC=C3C12)OC)C)CCCC)=O
Br[Br:11].[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[CH:10]=[C:12]1[c:13]1[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([CH3:20])[c:21]1[CH2:22]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([Br:11])=[C:12]1[c:13]1[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([CH3:20])[c:21]1[CH2:...
BrBr.CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(C)c1C2
null
null
O.C(Cl)Cl
Functional Group Interconversion
Bromination
73ca391a48874f0a81f3694c6623ffb0a512c874931d8f551485082fa4a0d563
c7222534d68e666d405fc6d911092ac63e3791780d01400eb414eff6e46c2a54
O=C1C=C2c3ccccc3CC2CC1
Br-[Br;H0;D1;+0:1].[C:2]-[C:3](=[CH;D2;+0:4]-[C:5](=[O;D1;H0:6])-[C:7])-[c:8]>>[Br;H0;D1;+0:1]-[C;H0;D3;+0:4](=[C:3](-[C:2])-[c:8])-[C:5](=[O;D1;H0:6])-[C:7]
89
[{"value": 89.0, "product": "BrC=1C(CCC2(CC3=C(C(=CC=C3C12)OC)C)CCCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
A mixture of 9a-butyl-7-methoxy-8-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (133 mg, 0.468 mmol), CCl4 (0.94 mL), and NaHCO3 (196 mg, 2.333 mmol) was cooled in an ice bath and stirred. Bromine (0.024 mL, 0.467 mmol) was added while stirring and swirling the reaction mixture by hand. A gummy, red precipitate formed du...
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Ketone
Alkenyl halide
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HBr
O.C(Cl)Cl
null
0.083333
BrBr.CCCCC12CCC(=O)C=C1c1ccc(OC)c(C)c1C2>O.C(Cl)Cl>CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(C)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ab9cbb76965644d483935f81bfcf3531
C=CC(=O)CC.CCCCC1Cc2c(ccc(OC)c2C)C1=O>>CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2C)C1=O
C(CCC)C1C(C2=CC=C(C(=C2C1)C)OC)=O.C(=C)C(=O)CC.N12CCCCCC2=NCCC1.C(=C)C(=O)CC.N12CCCCCC2=NCCC1>>C(CCC)C1(C(C2=CC=C(C(=C2C1)C)OC)=O)CCC(CC)=O
[CH2:6]=[CH:7][C:8](=[O:9])[CH2:10][CH3:11].[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:12][c:13]2[c:14]([cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]2[CH3:21])[C:22]1=[O:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]1([CH2:6][CH2:7][C:8](=[O:9])[CH2:10][CH3:11])[CH2:12][c:13]2[c:14]([cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]2[CH3:21...
C=CC(=O)CC.CCCCC1Cc2c(ccc(OC)c2C)C1=O
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2C)C1=O
null
null
CCOC(=O)C.O1CCCC1
C-C Coupling
OtherReaction
c504c0d32586144b6874498db3cc99d4d5bb675e1b2e725385a0386d3f14ac05
68a0b2d4768a64505cf15a6dd6bbd75216aef3c50fb86aff9b39341b3e49f06d
O=C1CCc2ccccc21
[C:1]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[CH2;D1;+0:5].[C:6]-[C:7]-[CH;D3;+0:8]1-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]>>[C:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[C;H0;D4;+0:8]1(-[C:7]-[C:6])-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]
null
[]
60
CELSIUS
24
HOUR
A solution of 2-butyl-5-methoxy-4-methyl-1-indanone (100 mg, 0.43 mmol) in tetrahydrofuran (0.43 mL) was treated with ethyl vinyl ketone (EVK, 0.064 mL, 0.646 mmol) and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU, 0.013 mL, 0.086 mmol). The resulting solution was stirred under a nitrogen atmosphere and heated in an oil bat...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Vinyl
Ketone.Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
null
CCOC(=O)C.O1CCCC1
60
24
C=CC(=O)CC.CCCCC1Cc2c(ccc(OC)c2C)C1=O>CCOC(=O)C.O1CCCC1>CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2C)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-619e723c7b9e4e91bac3e3dc222ad9ee
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2C)C1=O>>CCCCC1CC(=O)C(C)=C2c3ccc(OC)c(C)c3CC21
C(CCC)C1(C(C2=CC=C(C(=C2C1)C)OC)=O)CCC(CC)=O>>C(CCC)C1CC(C(=C2C3=CC=C(C(=C3CC12)C)OC)C)=O
O=[C:11]1[c:12]2[cH:13][cH:14][c:15]([O:16][CH3:17])[c:18]([CH3:19])[c:20]2[CH2:21][C:22]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:5][CH2:6][C:7](=[O:8])[CH2:9][CH3:10]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][C:7](=[O:8])[C:9]([CH3:10])=[C:11]2[c:12]3[cH:13][cH:14][c:15]([O:16][CH3:17])[c:18]([CH3:19])[c:20]3[CH2:21][CH:...
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2C)C1=O
CCCCC1CC(=O)C(C)=C2c3ccc(OC)c(C)c3CC21
null
null
CCOC(=O)C.C(C)(=O)O.Cl
C-C Coupling
OtherReaction
c888d527cd34f70db2bbf846edb013cbea97961406b00a885b9ff6fb89e2805c
6724ccabc3992a670343bf52a7363504b61386c3d76e13c5adf76934d5aec2b7
O=C1C=C2c3ccccc3CC2CC1
O=[C;H0;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[C:5]-[C;H0;D4;+0:6]-1(-[CH2;D2;+0:7]-[C:8]-[C:9])-[CH2;D2;+0:10]-[C:11]-[C:12](=[O;D1;H0:13])-[CH2;D2;+0:14]-[C;D1;H3:15]>>[C:9]-[C:8]-[CH2;D2;+0:7]-[CH;D3;+0:10]1-[C:11]-[C:12](=[O;D1;H0:13])-[C;H0;D3;+0:14](-[C;D1;H3:15])=[C;H0;D3;+0:1]2-[CH;D3;+0:6]-1-[C:5]-[c:4]:[c:2]-2:[c:3]
null
[]
100
CELSIUS
null
null
A solution of the crude diketone from step 1 in acetic acid (1 mL) and 6N HCl (1 mL) was stirred and heated in an oil bath at 100° C. for 5 hours. After cooling, the reaction mixture was diluted with EtOAc (20 mL), washed with water (10 mL) and brine (10 mL), dried over MgSO4, filtered, and the solvent evaporated under...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Ketone
c1ccc2c(c1)CCC2
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
CCOC(=O)C.C(C)(=O)O.Cl
100
null
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2C)C1=O>CCOC(=O)C.C(C)(=O)O.Cl>CCCCC1CC(=O)C(C)=C2c3ccc(OC)c(C)c3CC21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-5cbf2f7b75774d3da256736ac277ee13
CCCCC1CC(=O)C(C)=C2c3ccc(OC)c(C)c3CC21>>CCCCC1CC(=O)C(C)=C2c3ccc(O)c(C)c3CC21
B(Br)(Br)Br.C(CCC)C1CC(C(=C2C3=CC=C(C(=C3CC12)C)OC)C)=O>>C(CCC)C1CC(C(=C2C3=CC=C(C(=C3CC12)C)O)C)=O
C[O:16][c:15]1[cH:14][cH:13][c:12]2[c:19]([c:17]1[CH3:18])[CH2:20][CH:21]1[CH:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][C:7](=[O:8])[C:9]([CH3:10])=[C:11]21>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][C:7](=[O:8])[C:9]([CH3:10])=[C:11]2[c:12]3[cH:13][cH:14][c:15]([OH:16])[c:17]([CH3:18])[c:19]3[CH2:20][CH:21]12
CCCCC1CC(=O)C(C)=C2c3ccc(OC)c(C)c3CC21
CCCCC1CC(=O)C(C)=C2c3ccc(O)c(C)c3CC21
null
null
C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
4
HOUR
A solution of 9a butyl-4,8-dimethyl-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (84 mg, 0.28 mmol) in anhydrous CH2Cl2 (3 mL) was placed under a nitrogen atmosphere, cooled in an acetone-dry ice bath, and treated with 1M BBr3 in CH2Cl2 (1.11 mL, 1.11 mmol). The cooling bath was removed and the reaction mixture was s...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
C(Cl)Cl
null
4
CCCCC1CC(=O)C(C)=C2c3ccc(OC)c(C)c3CC21>C(Cl)Cl>CCCCC1CC(=O)C(C)=C2c3ccc(O)c(C)c3CC21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-4ea1ea522fe849c09b6b48ecf0c1b923
CCCCC1Cc2cc(OC)ccc2C1=O.O=C1CCC(=O)N1Cl>>CCCCC1Cc2c(ccc(OC)c2Cl)C1=O
ClN1C(CCC1=O)=O.C(CCC)C1C(C2=CC=C(C=C2C1)OC)=O>>C(CCC)C1C(C2=CC=C(C(=C2C1)Cl)OC)=O
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]2)[C:16]1=[O:17].O=C1CCC(=O)N1[Cl:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][cH:10][c:11]([O:12][CH3:13])[c:14]2[Cl:15])[C:16]1=[O:17]
CCCCC1Cc2cc(OC)ccc2C1=O.O=C1CCC(=O)N1Cl
CCCCC1Cc2c(ccc(OC)c2Cl)C1=O
null
null
CCOC(=O)C.CN(C=O)C
Functional Group Interconversion
Chlorination
810b77391b192e36eecbf89fbd0937a488e789bac7683cb9fabaa7cbc9c32e40
0e444576b73669992a4073cc3f7b10ed52cb9df09f9f8e4042e39e6a602aa390
O=C1CCc2ccccc21
O=C1-C-C-C(=O)-N-1-[Cl;H0;D1;+0:1].[#8:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6](:[c:7]-[C:8]=[O;D1;H0:9])-[C:10]>>[#8:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[Cl;H0;D1;+0:1]):[c:6](:[c:7]-[C:8]=[O;D1;H0:9])-[C:10]
15.4
[{"value": 15.4, "product": "C(CCC)C1C(C2=CC=C(C(=C2C1)Cl)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
N-Chlorosuccinimide (505 mg, 3.8 mmol) was added to a solution of 2-butyl-5-methoxy-1-indanone (825 mg, 3.8 mmol) in anhydrous dimethylformamide (3.8 mL) and the resulting solution was stirred under nitrogen and at room temperature overnight. The reaction mixture was diluted with EtOAc (50 mL), washed with 5% aqueous N...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Aromatic halide
c1ccc2c(c1)CCC2.C1CCNC1
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
CCOC(=O)C.CN(C=O)C
null
8
CCCCC1Cc2cc(OC)ccc2C1=O.O=C1CCC(=O)N1Cl>CCOC(=O)C.CN(C=O)C>CCCCC1Cc2c(ccc(OC)c2Cl)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d1cb4b3435da4997860140228da64a57
C=CC(=O)CC.CCCCC1Cc2c(ccc(OC)c2Cl)C1=O>>CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2Cl)C1=O
C(CCC)C1C(C2=CC=C(C(=C2C1)Cl)OC)=O.C(=C)C(=O)CC.N12CCCCCC2=NCCC1>>C(CCC)C1(C(C2=CC=C(C(=C2C1)Cl)OC)=O)CCC(CC)=O
[CH2:6]=[CH:7][C:8](=[O:9])[CH2:10][CH3:11].[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:12][c:13]2[c:14]([cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]2[Cl:21])[C:22]1=[O:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]1([CH2:6][CH2:7][C:8](=[O:9])[CH2:10][CH3:11])[CH2:12][c:13]2[c:14]([cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]2[Cl:21])...
C=CC(=O)CC.CCCCC1Cc2c(ccc(OC)c2Cl)C1=O
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2Cl)C1=O
null
null
CCOC(=O)C.O1CCCC1
C-C Coupling
OtherReaction
c504c0d32586144b6874498db3cc99d4d5bb675e1b2e725385a0386d3f14ac05
68a0b2d4768a64505cf15a6dd6bbd75216aef3c50fb86aff9b39341b3e49f06d
O=C1CCc2ccccc21
[C:1]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[CH2;D1;+0:5].[C:6]-[C:7]-[CH;D3;+0:8]1-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]>>[C:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[C;H0;D4;+0:8]1(-[C:7]-[C:6])-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]
93.9
[{"value": 93.9, "product": "C(CCC)C1(C(C2=CC=C(C(=C2C1)Cl)OC)=O)CCC(CC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
A solution of 2-butyl-4-chloro-5-methoxy-1-indanone (200 mg, 0.79 mmol) in anhydrous tetrahydrofuran (0.8 mL) was placed under a nitrogen atmosphere and treated with ethyl vinyl ketone (0.118 mL, 1.19 mmol) followed by 1,8-diazabicyclo[5.4.0]undec-7-ene (0.024 mL, 0.158 mmol). The resulting solution was stirred and hea...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Vinyl
Ketone.Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
null
CCOC(=O)C.O1CCCC1
60
null
C=CC(=O)CC.CCCCC1Cc2c(ccc(OC)c2Cl)C1=O>CCOC(=O)C.O1CCCC1>CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2Cl)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6121252028114c99b582eb81c90945f8
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2Cl)C1=O>>CCCCC12CCC(=O)C(C)=C1c1ccc(OC)c(Cl)c1C2
C(CCC)C1(C(C2=CC=C(C(=C2C1)Cl)OC)=O)CCC(CC)=O>>C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C)OC)Cl
O=[C:12]1[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8](=[O:9])[CH2:10][CH3:11])[CH2:22][c:21]2[c:13]1[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]2[Cl:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH3:11])=[C:12]1[c:13]1[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([Cl:20])[c:21]1[CH2:2...
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2Cl)C1=O
CCCCC12CCC(=O)C(C)=C1c1ccc(OC)c(Cl)c1C2
null
null
CCOC(=O)C.C(C)(=O)O.Cl
Functional Group Interconversion
OtherReaction
85ff0aa8be631f96366b93c0f2ba199404913ad074e95e1352514ec4827258a9
b7bc018679e3f4c5a72b49c90c858cc3bcb4db12dedb0216b468af50ef8a00a3
O=C1C=C2c3ccccc3CC2CC1
O=[C;H0;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[C:5]-[C:6]-1(-[C:7])-[C:8]-[C:9]-[C:10](=[O;D1;H0:11])-[CH2;D2;+0:12]-[C;D1;H3:13]>>[C:7]-[C:6]12-[C:5]-[c:4]:[c:2](:[c:3])-[C;H0;D3;+0:1]-1=[C;H0;D3;+0:12](-[C;D1;H3:13])-[C:10](=[O;D1;H0:11])-[C:9]-[C:8]-2
60.6
[{"value": 60.6, "product": "C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C)OC)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
2
DAY
A solution of 2-butyl-4-chloro-5-methoxy-2-(3-oxo-pentyl)-1-indanone (250 mg, 0.74 mmol) in acetic acid (2 mL) was diluted with 6N aqueous HCl (2 mL). The resulting mixture was stirred and heated in an oil bath at 90° C. for 18 hours, then kept at room temperature for 2 days. The mixture was diluted with EtOAc (20 mL),...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Ketone
c1ccc2c(c1)CCC2
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
CCOC(=O)C.C(C)(=O)O.Cl
90
48
CCCCC1(CCC(=O)CC)Cc2c(ccc(OC)c2Cl)C1=O>CCOC(=O)C.C(C)(=O)O.Cl>CCCCC12CCC(=O)C(C)=C1c1ccc(OC)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e71cb2ebf2654d4ba5d844ad5a953bf8
CCCCC12CCC(=O)C(C)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C)=C1c1ccc(O)c(Cl)c1C2
C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C)OC)Cl.Cl.N1=CC=CC=C1>>C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C)O)Cl
C[O:17][c:16]1[cH:15][cH:14][c:13]2[c:20]([c:18]1[Cl:19])[CH2:21][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH3:11])=[C:12]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH3:11])=[C:12]1[c:13]1[cH:14][cH:15][c:16]([OH:17])[c:18]([Cl:19])[c:20]1[CH2:21]2
CCCCC12CCC(=O)C(C)=C1c1ccc(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(C)=C1c1ccc(O)c(Cl)c1C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
195
CELSIUS
null
null
A mixture of 9a-butyl-8-chloro-7-methoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (36.6 mg) and pyridine hydrochloride (2.66) was stirred and heated in an oil bath at 190-200° C. for 80 minutes. After cooling to room temperature, the mixture was partitioned between EtOAc (20 mL) and water (30 mL). The organic phas...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
null
195
null
CCCCC12CCC(=O)C(C)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C)=C1c1ccc(O)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3748d7f80bee42f6a817e582c782f3ac
CCCCC12CCC(=O)C(C)=C1c1ccc(O)cc1C2.COCCl>>CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2
C(C)(C)N(C(C)C)CC.COCCl.C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)O.C(C)(C)N(C(C)C)CC.COCCl>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OCOC
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH3:11])=[C:12]1[c:13]1[cH:14][cH:15][c:16]([OH:17])[cH:21][c:22]1[CH2:23]2.Cl[CH2:18][O:19][CH3:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH3:11])=[C:12]1[c:13]1[cH:14][cH:15][c:16]([O:17][CH2:18][O:19][CH3:20])[cH:2...
CCCCC12CCC(=O)C(C)=C1c1ccc(O)cc1C2.COCCl
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2
null
null
CCOC(=O)C.CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
6e90ffbf0683e1a3ee55c5e3ea453aefc5ddd369c0150ed0150f9546d7e47f4f
efd670663709b79afcad1306da9f69b33a0147cfa3639ca4c0b54b35ef4b1852
O=C1C=C2c3ccccc3CC2CC1
Cl-[CH2;D2;+0:1]-[#8:2]-[C;D1;H3:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:3]-[#8:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
75.4
[{"value": 75.4, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OCOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5.5
HOUR
A solution of 9a-butyl-7-hydroxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (5.30 g, 21 mmol) in anhydrous dimethylformamide (50 mL) was cooled in an ice bath, stirred under a nitrogen atmosphere, and treated successively with N,N-diisopropyl-ethylamine (10.5 mL, 60 mmol) and chloromethyl methyl ether (3.45 mL, 41 m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Aromatic alcohol
Ether.Ether
null
null
C1=C2c3ccccc3CC2CCC1
HCl
CCOC(=O)C.CN(C=O)C
null
5.5
CCCCC12CCC(=O)C(C)=C1c1ccc(O)cc1C2.COCCl>CCOC(=O)C.CN(C=O)C>CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-95e98eaea1a94f0591c92261b6aa3074
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.CI>>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2
IC.C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OCOC.[Li+].CC(C)[N-]C(C)C.[NH4+].[Cl-].C(=O)=O.CC(=O)C>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)C)=O)C)OCOC
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19])[C:20](=[O:21])[CH2:22][CH2:24]2.I[CH3:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19])[C:20](=...
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.CI
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2
null
null
C1CCOC1.CCOC(=O)C
C-C Coupling
Methylation with MeI_secondary
5ad82e3a335a3b61932305272f1c5165265cfa3d334bee0a6b6bb8d630fc2131
6c72a64362b644ff7380f8d0c7bdda962edffb1f22535d7f0916fcd367b6b992
O=C1C=C2c3ccccc3CC2CC1
I-[CH3;D1;+0:1].[C;D1;H3:2]-[C:3]1=[C:4](-[c:5])-[C:6]-[C:7]-[CH2;D2;+0:8]-[C:9]-1=[O;D1;H0:10]>>[C;D1;H3:2]-[C:3]1=[C:4](-[c:5])-[C:6]-[C:7]-[CH;D3;+0:8](-[CH3;D1;+0:1])-[C:9]-1=[O;D1;H0:10]
null
[]
0
CELSIUS
30
MINUTE
A solution of 9a-butyl-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (162 mg, 0.52 mmol) in anhydrous THF (2.5 mL) was cooled in an ice bath and stirred under a nitrogen atmosphere while 0.4M LDA in THF (1.55 mL, 0.62 mmol) was added by syringe. After stirring at 0° C. for 30 minutes, the solution was ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HI
C1CCOC1.CCOC(=O)C
0
0.5
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.CI>C1CCOC1.CCOC(=O)C>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-62b89ac0566e47018eebadecdf9ff60c
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2.CCCI>>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(CCC)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)C)=O)C)OCOC.[Li+].CC(C)[N-]C(C)C.ICCC>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)(CCC)C)=O)C)OCOC
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19])[C:20](=[O:21])[CH:22]([CH3:23])[CH2:27]2.I[CH2:24][CH2:25][CH3:26]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1...
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2.CCCI
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(CCC)C2
null
null
C1CCOC1
C-C Coupling
OtherReaction
2d1eeb1a4c757ce03bc2ed50cc7f2b79e982da0747960d20374c2a44a78b6ea2
836e0f77354d9f44b98dde88e343d5cebbf81f14d452aa51d1e50ec699999492
O=C1C=C2c3ccccc3CC2CC1
I-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3].[C;D1;H3:4]-[C:5]1=[C:6](-[c:7])-[C:8]-[C:9]-[CH;D3;+0:10](-[C;D1;H3:11])-[C:12]-1=[O;D1;H0:13]>>[C;D1;H3:4]-[C:5]1=[C:6](-[c:7])-[C:8]-[C:9]-[C;H0;D4;+0:10](-[C;D1;H3:11])(-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3])-[C:12]-1=[O;D1;H0:13]
null
[]
-78
CELSIUS
null
null
A solution of (2SR,9aSR)-9a-butyl-2,4-dimethyl-7-methoxymethoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (110 mg, 0.34 mmol) in anhydrous THF (1.5 mL) was cooled in an ice bath, stirred under a nitrogen atmosphere, and treated with 0.4M LDA in THF (1 mL, 0.4 mmol). After stirring at 0° C. for 30 minutes, the solution was c...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HI
C1CCOC1
-78
null
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2.CCCI>C1CCOC1>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(CCC)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-58e5100c1cca454d952bc1df3a46b49a
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(CCC)C2>>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(C)(CCC)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)(CCC)C)=O)C)OCOC.Cl>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)(CCC)C)=O)C)O
COC[O:10][c:9]1[cH:8][c:7]2[c:13]([cH:12][cH:11]1)[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[C:19]([CH3:20])([CH2:21][CH2:22][CH3:23])[CH2:24][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[C:19](...
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(CCC)C2
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(C)(CCC)C2
null
null
CO
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1C=C2c3ccccc3CC2CC1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
85
CELSIUS
null
null
A solution of (2SR,9aRS)-9a-butyl-2,4-dimethyl-7-methoxymethoxy-2-propyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (40 mg, 0.11 mmol) in methanol (approx. 0.5-1 mL) was placed under a nitrogen atmosphere and treated with 2N aqueous HCl (0.165 mL, 0.37 mmol). The resulting yellow solution was stirred and heated in an oil bat...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
HO-
CO
85
null
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(CCC)C2>CO>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(C)(CCC)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1cea5b97e21b47708df149edb4f91295
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2.CI>>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(C)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)C)=O)C)OCOC.[Li+].CC(C)[N-]C(C)C.IC>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)(C)C)=O)C)OCOC
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19])[C:20](=[O:21])[CH:22]([CH3:23])[CH2:25]2.I[CH3:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19]...
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2.CI
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(C)C2
null
null
C1CCOC1
C-C Coupling
Methylation with MeI_tertiary
5ad82e3a335a3b61932305272f1c5165265cfa3d334bee0a6b6bb8d630fc2131
6c72a64362b644ff7380f8d0c7bdda962edffb1f22535d7f0916fcd367b6b992
O=C1C=C2c3ccccc3CC2CC1
I-[CH3;D1;+0:1].[C;D1;H3:2]-[C:3]1=[C:4](-[c:5])-[C:6]-[C:7]-[CH;D3;+0:8](-[C;D1;H3:9])-[C:10]-1=[O;D1;H0:11]>>[C;D1;H3:2]-[C:3]1=[C:4](-[c:5])-[C:6]-[C:7]-[C;H0;D4;+0:8](-[C;D1;H3:9])(-[CH3;D1;+0:1])-[C:10]-1=[O;D1;H0:11]
null
[]
-78
CELSIUS
null
null
A solution of (2SR,9aSR)-9a-butyl-2,4-dimethyl-7-methoxymethoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (39 mg, 0.12 mmol) in anhydrous THF (1.0 mL) was cooled in an ice bath, stirred under a nitrogen atmosphere, and treated with 0.4M LDA in THF (0.39 mL, 0.16 mmol). After stirring at 0° C. for 30 minutes, the yellow solu...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HI
C1CCOC1
-78
null
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)C2.CI>C1CCOC1>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(C)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b696197867354374bb82affcc3d1f4f4
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(C)C2>>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(C)(C)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)(C)C)=O)C)OCOC.Cl.C(=O)(O)[O-].[Na+]>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)(C)C)=O)C)O
COC[O:10][c:9]1[cH:8][c:7]2[c:13]([cH:12][cH:11]1)[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[C:19]([CH3:20])([CH3:21])[CH2:22][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[C:19]([CH3:20])([CH3:2...
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(C)C2
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(C)(C)C2
null
null
CO.CCOC(=O)C
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1C=C2c3ccccc3CC2CC1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
67.5
CELSIUS
null
null
A solution of 9a-butyl-7-methoxymethoxy-2,2,4-trimethyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (28 mg, 0.08 mmol) in methanol (2 mL) was placed under a nitrogen atmosphere and treated with 2N aqueous HCl (0.12 mL, 0.24 mmol). The resulting yellow solution was stirred and heated in an oil bath at 55-80° C. for 45 minutes....
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
HO-
CO.CCOC(=O)C
67.5
null
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(C)(C)C2>CO.CCOC(=O)C>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(C)(C)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-823a4e2ec3744ad0aa61ce7065b5483c
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.II>>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(I)C2
[Li+].CC(C)[N-]C(C)C.C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OCOC.II>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)I)=O)C)OCOC
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19])[C:20](=[O:21])[CH2:22][CH2:24]2.I[I:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19])[C:20](=[O...
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.II
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(I)C2
null
null
C1CCOC1.CCOC(=O)C
Functional Group Interconversion
OtherReaction
73ce905e1642fa0e07c12cc5678c93e00cb126654e05346b16307491c72f308f
fe149a07f370bdd2ea40b2dff4f3462711fb34a60b8733c443efdeb5ab4d5c53
O=C1C=C2c3ccccc3CC2CC1
I-[I;H0;D1;+0:1].[C;D1;H3:2]-[C:3]1=[C:4](-[c:5])-[C:6]-[C:7]-[CH2;D2;+0:8]-[C:9]-1=[O;D1;H0:10]>>[C;D1;H3:2]-[C:3]1=[C:4](-[c:5])-[C:6]-[C:7]-[CH;D3;+0:8](-[I;H0;D1;+0:1])-[C:9]-1=[O;D1;H0:10]
null
[]
null
null
null
null
A solution of 9a-butyl-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (134 mg, 0.43 mmol) in anhydrous THF (2.5 mL) was cooled in an ice bath, stirred under a nitrogen atmosphere, and treated with 0.4M LDA in THF (1.2 mL, 0.48 mmol). After stirring at 0° C. for 30 minutes, the enolate solution was coole...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary halide
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HI
C1CCOC1.CCOC(=O)C
null
null
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.II>C1CCOC1.CCOC(=O)C>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(I)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d4279359932d424a94d83bc5d764d5a1
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(I)C2>>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(I)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)I)=O)C)OCOC.Cl.C(=O)(O)[O-].[Na+]>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)I)=O)C)O
COC[O:10][c:9]1[cH:8][c:7]2[c:13]([cH:12][cH:11]1)[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([I:20])[CH2:21][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([I:20])[CH2:21]2
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(I)C2
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(I)C2
null
null
CO.CCOC(=O)C
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1C=C2c3ccccc3CC2CC1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
70
CELSIUS
null
null
A suspension of (2SR,9aRS)-9a-butyl-2-iodo-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (50 mg, 0.11 mmol) in methanol (3.5 mL) was placed under a nitrogen atmosphere, heated in an oil bath at 70° C. to affect solution, then treated with 2N aqueous HCl (0.195 mL, 0.39 mmol). The resulting solution was...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
HO-
CO.CCOC(=O)C
70
null
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(I)C2>CO.CCOC(=O)C>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(I)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1359d29ce9324090968a6c78e5d5d25d
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.C[Si](C)(C)Cl>>CCCCC12CC=C(O[Si](C)(C)C)C(C)=C1c1ccc(OCOC)cc1C2
Cl[Si](C)(C)C.C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OCOC.[Li+].CC(C)[N-]C(C)C.C(=O)(O)[O-].[Na+].C(=O)=O.CC(=O)C>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(=CC1)O[Si](C)(C)C)C)OCOC
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:14]([CH3:15])=[C:16]1[c:17]1[cH:18][cH:19][c:20]([O:21][CH2:22][O:23][CH3:24])[cH:25][c:26]1[CH2:27]2.Cl[Si:10]([CH3:11])([CH3:12])[CH3:13]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH:7]=[C:8]([O:9][Si:10]([CH3:11])([CH3:12])[CH3:13])[C:14]([CH3:15])=[...
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.C[Si](C)(C)Cl
CCCCC12CC=C(O[Si](C)(C)C)C(C)=C1c1ccc(OCOC)cc1C2
null
null
C1CCOC1.CCOC(=O)C
Acylation
OtherReaction
588731292d95bafa6ace96d9ff24559ce1957afa3790246098cafd64029214d6
c13dd54c2034fa9746e04e6d624199b4092538f90a428225c0e821f09d4466f2
C1=CCC2Cc3ccccc3C2=C1
Cl-[Si;H0;D4;+0:1](-[C;D1;H3:2])(-[C;D1;H3:3])-[C;D1;H3:4].[C;D1;H3:5]-[C:6]1=[C:7](-[c:8])-[C:9]-[C:10]-[CH2;D2;+0:11]-[C;H0;D3;+0:12]-1=[O;H0;D1;+0:13]>>[C;D1;H3:2]-[Si;H0;D4;+0:1](-[C;D1;H3:3])(-[C;D1;H3:4])-[O;H0;D2;+0:13]-[C;H0;D3;+0:12]1=[CH;D2;+0:11]-[C:10]-[C:9]-[C:7](=[C:6]-1-[C;D1;H3:5])-[c:8]
null
[]
0
CELSIUS
30
MINUTE
A solution of 9a-butyl-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (163 mg, 0.52 mmol) in anhydrous THF (2.5 mL) was cooled in an ice bath and stirred under a nitrogen atmosphere while 0.4M LDA in THF (1.9 mL, 0.78 mmol) was added by syringe. After stirring at 0° C. for 30 minutes, the solution was c...
10.6084/m9.figshare.5104873.v1
null
Ketone.Silyl protective group
Silyl protective group
C1=C2c3ccccc3CC2CCC1
C1=CCC2Cc3ccccc3C2=C1
C1=CCC2Cc3ccccc3C2=C1
HCl
C1CCOC1.CCOC(=O)C
0
0.5
CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2.C[Si](C)(C)Cl>C1CCOC1.CCOC(=O)C>CCCCC12CC=C(O[Si](C)(C)C)C(C)=C1c1ccc(OCOC)cc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-72dc067bf29f4615811dcb079c390574
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(O)C2>>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(O)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)O)=O)C)OCOC.Cl>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)O)=O)C)O
COC[O:10][c:9]1[cH:8][c:7]2[c:13]([cH:12][cH:11]1)[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([OH:20])[CH2:21][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([OH:20])[CH2:21]2
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(O)C2
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(O)C2
null
null
CO.CCOC(=O)C
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1C=C2c3ccccc3CC2CC1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
80
CELSIUS
null
null
A solution of (2SR,9aRS)-9a-butyl-2-hydroxy-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (73 mg, 0.22 mmol) in methanol (5 mL) was placed under a nitrogen atmosphere, treated with 2N aqueous HCl (0.33 mL, 0.66 mmol), and stirred with heating in an oil bath at 80° C. for 30 minutes. After cooling to ro...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
HO-
CO.CCOC(=O)C
80
null
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(O)C2>CO.CCOC(=O)C>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(O)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6135e02ccc8a47dd9175ba392412cef1
C=CCBr.CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2>>C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O
C(C=C)Br.C(CCC)C12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OCOC.[Li+].CC(C)[N-]C(C)C.Cl.C(=O)=O.CC(=O)C>>C(C=C)C1CC2(CC3=CC(=CC=C3C2=C(C1=O)C)OCOC)CCCC
Br[CH2:3][CH:2]=[CH2:1].[CH2:4]1[CH2:5][C:6]2([CH2:7][CH2:8][CH2:9][CH3:10])[CH2:11][c:12]3[cH:13][c:14]([O:15][CH2:16][O:17][CH3:18])[cH:19][cH:20][c:21]3[C:22]2=[C:23]([CH3:24])[C:25]1=[O:26]>>[CH2:1]=[CH:2][CH2:3][CH:4]1[CH2:5][C:6]2([CH2:7][CH2:8][CH2:9][CH3:10])[CH2:11][c:12]3[cH:13][c:14]([O:15][CH2:16][O:17][CH3...
C=CCBr.CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2
C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O
null
null
C1CCOC1.CCOC(=O)C
C-C Coupling
OtherReaction
e2c7d74e8f73814e3527352c2cc5c462d7ae54bf350f989a871b42e01d15041a
f5ccd90096c3201115eb6510107831f398bf8f80381c3ea6084a10b0ebb25a81
O=C1C=C2c3ccccc3CC2CC1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[C;D1;H3:4]-[C:5]1=[C:6](-[c:7])-[C:8]-[C:9]-[CH2;D2;+0:10]-[C:11]-1=[O;D1;H0:12]>>[C;D1;H2:3]=[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:10]1-[C:9]-[C:8]-[C:6](=[C:5](-[C;D1;H3:4])-[C:11]-1=[O;D1;H0:12])-[c:7]
null
[]
null
null
null
null
A solution of 9a-butyl-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (230 mg, 0.73 mmol) in anhydrous THF (3.8 mL) was cooled in an ice bath, stirred under a nitrogen atmosphere, and treated with freshly prepared 0.4M LDA in THF (2.2 mL, 0.88 mmol). The resulting solution was stirred at 0° C. for 30 mi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone.Allyl
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HBr
C1CCOC1.CCOC(=O)C
null
null
C=CCBr.CCCCC12CCC(=O)C(C)=C1c1ccc(OCOC)cc1C2>C1CCOC1.CCOC(=O)C>C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-30c070b61f1b4129a0cb3214237639c6
C1COCCO1.C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O>>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2
C(C=C)C1CC2(CC3=CC(=CC=C3C2=C(C1=O)C)OCOC)CCCC.O1CCOCC1>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CC(CO)=O)=O)C)OCOC
C1C[O:27]CC[O:25]1.[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16]3[C:17]1=[C:18]([CH3:19])[C:20](=[O:21])[CH:22]([CH2:23][CH:24]=[CH2:26])[CH2:28]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([O:10][CH2:11][O:12][CH3:13])[cH:14][cH:15][c:16...
C1COCCO1.C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2
null
null
O
Functional Group Interconversion
OtherReaction
667ca994095416535757cb9f161b113c486928eb5d344a0fe640637a77786136
b5efe610ee05d133e43d6cd5169de83ef9e451cf7c4171956516c2320bb703ea
O=C1C=C2c3ccccc3CC2CC1
C1-C-[O;H0;D2;+0:1]-C-C-[O;H0;D2;+0:2]-1.[CH2;D1;+0:3]=[CH;D2;+0:4]-[C:5]-[C:6]-[C:7]=[O;D1;H0:8]>>[O;D1;H0:8]=[C:7]-[C:6]-[C:5]-[C;H0;D3;+0:4](=[O;H0;D1;+0:2])-[CH2;D2;+0:3]-[OH;D1;+0:1]
null
[]
null
null
15
MINUTE
A solution of (2SR,9aSR)-2-allyl-9a-butyl-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (170 mg, 0.48 mmol) in dioxane (9 mL) was diluted with water (3 mL) and treated with a single crystal of OSO4 followed by NaIO4 (125 mg, 0.58 mmol). The mixture was stirred at room temperature for 15 minutes, treate...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Allyl
Ketone.Primary alcohol
C1COCCO1
null
C1=C2c3ccccc3CC2CCC1
Other
O
null
0.25
C1COCCO1.C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O>O>CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-91f58590443c4623a63d18722cfb6815
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC=O)C2>>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC=O)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CC=O)=O)C)OCOC.Cl>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CC=O)=O)C)O
COC[O:10][c:9]1[cH:8][c:7]2[c:13]([cH:12][cH:11]1)[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([CH2:20][CH:21]=[O:22])[CH2:23][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([CH2:20][C...
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC=O)C2
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC=O)C2
null
null
CO.CCOC(=O)C
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1C=C2c3ccccc3CC2CC1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
67.1
[{"value": 67.1, "product": "C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CC=O)=O)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A solution of (2RS,9aSR)-9a-butyl-7-methoxymethoxy-4-methyl-2-(2-oxoethyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one (85 mg) in methanol (1 mL) was diluted with 2N HCl (0.36 mL, 0.72 mmol). The resulting mixture was stirred at room temperature for 30 minutes followed by heating in an oil bath at 80° C. for 40 minutes. On co...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
HO-
CO.CCOC(=O)C
null
0.5
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC=O)C2>CO.CCOC(=O)C>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC=O)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6d0e5e3c98d34755babed58fc6c14987
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC=O)C2>>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CCO)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CC=O)=O)C)O.[BH4-].[Na+]>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CCO)=O)C)O
[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([CH2:20][CH:21]=[O:22])[CH2:23]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([CH2:20][CH2:2...
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC=O)C2
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CCO)C2
null
null
CC(C)O
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
O=C1C=C2c3ccccc3CC2CC1
[O;D1;H0:1]=[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[O;H0;D1;+0:6]>>[O;D1;H0:1]=[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-[OH;D1;+0:6]
null
[]
null
null
40
MINUTE
A solution of (2RS,9aSR)-9a-butyl-7-hydroxy-4-methyl-2-(2-oxo-ethyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one (17 mg, 0.05 mmol) in 2-propanol (2 mL) was treated with NaBH4 (1.9 mg, 0.05 mmol) and the mixture was stirred at room temperature for 40 minutes. The solvent was evaporated under vacuum. The residue was taken up i...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
C1=C2c3ccccc3CC2CCC1
null
CC(C)O
null
0.666667
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC=O)C2>CC(C)O>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CCO)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-cf2f58d1d9b2468d8835b967eb71e56a
C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O>>C=CCC1CC2(CCCC)Cc3cc(O)ccc3C2=C(C)C1=O
C(C=C)C1CC2(CC3=CC(=CC=C3C2=C(C1=O)C)OCOC)CCCC.Cl>>C(C=C)C1CC2(CC3=CC(=CC=C3C2=C(C1=O)C)O)CCCC
COC[O:15][c:14]1[cH:13][c:12]2[c:18]([cH:17][cH:16]1)[C:19]1=[C:20]([CH3:21])[C:22](=[O:23])[CH:4]([CH2:3][CH:2]=[CH2:1])[CH2:5][C:6]1([CH2:7][CH2:8][CH2:9][CH3:10])[CH2:11]2>>[CH2:1]=[CH:2][CH2:3][CH:4]1[CH2:5][C:6]2([CH2:7][CH2:8][CH2:9][CH3:10])[CH2:11][c:12]3[cH:13][c:14]([OH:15])[cH:16][cH:17][c:18]3[C:19]2=[C:20]...
C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O
C=CCC1CC2(CCCC)Cc3cc(O)ccc3C2=C(C)C1=O
null
null
C1CCOC1.CCOC(=O)C
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1C=C2c3ccccc3CC2CC1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
50
CELSIUS
null
null
A solution of (2SR,9aSR)-2-allyl-9a-butyl-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (5 mg, 0.015 mmol) in THF (0.5 mL) was treated with 6N HCl (0.5 mL) and the resulting solution was heated at 50° C. overnight. The mixture was diluted with EtOAc (30 mL), washed with 5% NaHCO3 and brine, dried over ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
HO-
C1CCOC1.CCOC(=O)C
50
null
C=CCC1CC2(CCCC)Cc3cc(OCOC)ccc3C2=C(C)C1=O>C1CCOC1.CCOC(=O)C>C=CCC1CC2(CCCC)Cc3cc(O)ccc3C2=C(C)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b15b3e94ee9748ad969eea6cc232a478
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2>>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2
C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CC(CO)=O)=O)C)OCOC.Cl>>C(CCC)C12CC3=CC(=CC=C3C2=C(C(C(C1)CC(CO)=O)=O)C)O
COC[O:10][c:9]1[cH:8][c:7]2[c:13]([cH:12][cH:11]1)[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[CH:19]([CH2:20][C:21](=[O:22])[CH2:23][OH:24])[CH2:25][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][c:7]3[cH:8][c:9]([OH:10])[cH:11][cH:12][c:13]3[C:14]1=[C:15]([CH3:16])[C:17](=[O:18])[C...
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2
CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2
null
null
CO
Reduction
OtherReaction
92f30feec6876d2f8c7439342f0f488fd5811a8fdb3b3cb63d7289bd57242715
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
O=C1C=C2c3ccccc3CC2CC1
C-O-C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A solution of (2RS,9aSR)-9a-butyl-2-(3-hydroxy-2-oxopropyl)-7-methoxymethoxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (24 mg, 0.06 mmol) in methanol (1 mL) was treated with 2N HCl (0.36 mL, 0.18 mmol) and the resulting solution was heated at reflux for 20 minutes. After cooling, the mixture was concentrated under ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
HO-
CO
null
null
CCCCC12Cc3cc(OCOC)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2>CO>CCCCC12Cc3cc(O)ccc3C1=C(C)C(=O)C(CC(=O)CO)C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d0bd1b0c03f844d7a23d87971c34bc62
CCCI.COc1ccc2c(c1)C=CC2>>CCCC1C=Cc2cc(OC)ccc21
[NH4+].[Cl-].COC=1C=C2C=CCC2=CC1.[Li]C.ICCC>>COC=1C=C2C=CC(C2=CC1)CCC
I[CH2:3][CH2:2][CH3:1].[CH2:4]1[CH:5]=[CH:6][c:7]2[cH:8][c:9]([O:10][CH3:11])[cH:12][cH:13][c:14]21>>[CH3:1][CH2:2][CH2:3][CH:4]1[CH:5]=[CH:6][c:7]2[cH:8][c:9]([O:10][CH3:11])[cH:12][cH:13][c:14]21
CCCI.COc1ccc2c(c1)C=CC2
CCCC1C=Cc2cc(OC)ccc21
null
null
CCOCC
C-C Coupling
OtherReaction
ee93cac7990a00c1dd3a845ddbd566fe7d8a8ffc7df7c031c0125f10973487d9
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
C1=Cc2ccccc2C1
I-[CH2;D2;+0:1]-[C:2]-[C;D1;H3:3].[c:4]:[c:5]1:[c:6]-[C:7]=[C:8]-[CH2;D2;+0:9]-1>>[C;D1;H3:3]-[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:9]1-[C:8]=[C:7]-[c:6]:[c:5]-1:[c:4]
108.3
[{"value": 108.3, "product": "COC=1C=C2C=CC(C2=CC1)CCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of 5-methoxy-1H-indene (0.895 g, 6.12 mmol) in anhydrous Et2O (7.5 mL) was treated with 1.4M MeLi in Et2O (4.7 mL, 6.58 mmol) added dropwise over 10 minutes. The resulting hazy solution was stirred at room temperature an additional 15 minutes, then cooled in an ice bath and treated with iodopropane (1.00 mL,...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
C1=Cc2ccccc2C1
C1=Cc2ccccc2C1
C1=Cc2ccccc2C1
HI
CCOCC
null
0.25
CCCI.COc1ccc2c(c1)C=CC2>CCOCC>CCCC1C=Cc2cc(OC)ccc21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f7b0953821a446b293b603d05a892eeb
CCCC1C=Cc2cc(OC)ccc21>>CCCC1CCc2ccc(OC)cc21
COC=1C=C2C=CC(C2=CC1)CCC.C(C)O>>COC1=CC=C2CCC(C2=C1)CCC
[CH3:1][CH2:2][CH2:3][CH:4]1[CH:5]=[CH:6][c:14]2[c:7]1[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13]2>>[CH3:1][CH2:2][CH2:3][CH:4]1[CH2:5][CH2:6][c:7]2[cH:8][cH:9][c:10]([O:11][CH3:12])[cH:13][c:14]21
CCCC1C=Cc2cc(OC)ccc21
CCCC1CCc2ccc(OC)cc21
null
[Pd]
null
Miscellaneous
OtherReaction
01ad2b60de955da99a059ed8e67687c8e839e9c53d04e18169490b4081371a85
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccc2c(c1)CCC2
[C:1]-[C:2]-[CH;D3;+0:3]1-[CH;D2;+0:4]=[CH;D2;+0:5]-[c;H0;D3;+0:6]2:[c:7]:[c:8]:[c:9]:[c:10]:[c;H0;D3;+0:11]:2-1>>[C:1]-[C:2]-[CH;D3;+0:3]1-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[c;H0;D3;+0:11]2:[c:10]:[c:9]:[c:8]:[c:7]:[c;H0;D3;+0:6]:2-1
null
[]
null
null
60
MINUTE
The mixture of indenes from step 1 (1.24 g, approx. 6.1 mmol) was dissolved in ethanol (40 mL), treated with 10% Pd on carbon (58 mg), and hydrogenated at 40 psi and room temperature for 60 minutes. The catalyst was removed by filtration and the filtrate was evaporated under vacuum to provide a mixture (1.287 g) of 6-m...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=Cc2ccccc2C1
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
null
[Pd]
null
1
CCCC1C=Cc2cc(OC)ccc21>[Pd]>CCCC1CCc2ccc(OC)cc21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3f65a22cc30c4c71b7a3d15e3263d86d
CCCC1CCc2ccc(OC)cc21.[O]=[Mn](=[O])(=[O])[O-]>>CCCC1CC(=O)c2ccc(OC)cc21
COC1=CC=C2CCC(C2=C1)CCC.[O-][Mn](=O)(=O)=O.[K+]>>COC=1C=C2C(CC(C2=CC1)=O)CCC
[CH3:1][CH2:2][CH2:3][CH:4]1[CH2:5][CH2:6][c:8]2[cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14][c:15]21.[O]=[Mn](=[O])([O-])=[O:7]>>[CH3:1][CH2:2][CH2:3][CH:4]1[CH2:5][C:6](=[O:7])[c:8]2[cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14][c:15]21
CCCC1CCc2ccc(OC)cc21.[O]=[Mn](=[O])(=[O])[O-]
CCCC1CC(=O)c2ccc(OC)cc21
null
[O-]S(=O)(=O)[O-].[Cu+2]
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
32ab24ed955b97edb4307c2f3e4046b88d7a3304f9d6f8e3f49a6ef57e022b90
a196f7191876ee39420290ab9d6c2b9eeb3251b37ae345fc435efba1949a85d9
O=C1CCc2ccccc21
[O-]-[Mn](=[O;H0;D1;+0:1])(=[O])=[O].[c:2]:[c:3]1:[c:4]-[C:5]-[C:6]-[CH2;D2;+0:7]-1>>[O;H0;D1;+0:1]=[C;H0;D3;+0:7]1-[C:6]-[C:5]-[c:4]:[c:3]-1:[c:2]
15.1
[{"value": 15.1, "product": "COC=1C=C2C(CC(C2=CC1)=O)CCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The mixture of indans from step 2 (1.287 g, approx. 6.1 mmol) in CH2Cl2 (50 mL) was treated with a finely ground mixture of KMnO4 (7.00 g) and CuSO4.xH2O. The resulting mixture was heated at reflux for 89 hours, then cooled to room temperature and filtered through a celite pad. The filtrate was dried over MgSO4, filter...
10.6084/m9.figshare.5104873.v1
null
null
Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
[O-]S(=O)(=O)[O-].[Cu+2].C(Cl)Cl
null
null
CCCC1CCc2ccc(OC)cc21.[O]=[Mn](=[O])(=[O])[O-]>[O-]S(=O)(=O)[O-].[Cu+2].C(Cl)Cl>CCCC1CC(=O)c2ccc(OC)cc21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-61d811177b4e4cd88b1e29266c8ae876
CCC1(CC=O)OCCO1.CCCC1CC(=O)c2ccc(OC)cc21>>CCCC1c2cc(OC)ccc2C(=O)C1CCC1(CC)OCCO1
Cl.[OH-].[K+].COC=1C=C2C(CC(C2=CC1)=O)CCC.C(C)C1(OCCO1)CC=O>>C(C)C1(OCCO1)CCC1C(C2=CC=C(C=C2C1CCC)OC)=O
O=[CH:16][CH2:17][C:18]1([CH2:19][CH3:20])[O:21][CH2:22][CH2:23][O:24]1.[CH3:1][CH2:2][CH2:3][CH:4]1[c:5]2[cH:6][c:7]([O:8][CH3:9])[cH:10][cH:11][c:12]2[C:13](=[O:14])[CH2:15]1>>[CH3:1][CH2:2][CH2:3][CH:4]1[c:5]2[cH:6][c:7]([O:8][CH3:9])[cH:10][cH:11][c:12]2[C:13](=[O:14])[CH:15]1[CH2:16][CH2:17][C:18]1([CH2:19][CH3:20...
CCC1(CC=O)OCCO1.CCCC1CC(=O)c2ccc(OC)cc21
CCCC1c2cc(OC)ccc2C(=O)C1CCC1(CC)OCCO1
null
[Pd]
C(C)O
C-C Coupling
OtherReaction
68e28f9095e1f150f32da6921211b9a27c818a0dd75d077bb5baa7c9b256c798
c93e93ada40f7f922a54fe24d38f540ecf5ff25d55d497f79f5f400f75d0c7ae
O=C1c2ccccc2CC1CCC1OCCO1
O=[CH;D2;+0:1]-[C:2]-[C:3](-[#8:4])-[#8:5].[C:6]-[C:7]1-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[c:11]:[c:12]-1>>[#8:4]-[C:3](-[C:2]-[CH2;D2;+0:1]-[CH;D3;+0:8]1-[C:9](=[O;D1;H0:10])-[c:11]:[c:12]-[C:7]-1-[C:6])-[#8:5]
29.1
[{"value": 29.1, "product": "C(C)C1(OCCO1)CCC1C(C2=CC=C(C=C2C1CCC)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A mixture of 5-methoxy-3-propyl-1-indanone (184 mg, 0.90 mmol) and (2-ethyl-[1,3]dioxolan-2-yl)acetaldehyde (173 mg, 1.20 mmol) was treated with a solution of KOH (85% wt. pure, 20 mg, 0.30 mmol) in ethanol (1.0 mL). The resulting mixture was stirred at room temperature for 30 minutes, then treated with 10% Pd on carbo...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2.C1COCO1
Other
[Pd].C(C)O
null
0.5
CCC1(CC=O)OCCO1.CCCC1CC(=O)c2ccc(OC)cc21>[Pd].C(C)O>CCCC1c2cc(OC)ccc2C(=O)C1CCC1(CC)OCCO1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-7dd6343aeafb46f08ecf5adfe3390eb6
CCCC1c2cc(OC)ccc2C2=C(C)C(=O)CCC21>>CCCC1c2cc(O)ccc2C2=C(C)C(=O)CCC21
COC1=CC=C2C3=C(C(CCC3C(C2=C1)CCC)=O)C.B(Br)(Br)Br>>OC1=CC=C2C3=C(C(CCC3C(C2=C1)CCC)=O)C
C[O:8][c:7]1[cH:6][c:5]2[c:11]([cH:10][cH:9]1)[C:12]1=[C:13]([CH3:14])[C:15](=[O:16])[CH2:17][CH2:18][CH:19]1[CH:4]2[CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH:4]1[c:5]2[cH:6][c:7]([OH:8])[cH:9][cH:10][c:11]2[C:12]2=[C:13]([CH3:14])[C:15](=[O:16])[CH2:17][CH2:18][CH:19]12
CCCC1c2cc(OC)ccc2C2=C(C)C(=O)CCC21
CCCC1c2cc(O)ccc2C2=C(C)C(=O)CCC21
null
null
C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
2.6
HOUR
A solution of (9SR,9aSR)-7-methoxy-4-methyl-9-propyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (38.3 mg, 0.142 mmol) in anhydrous CH2Cl2 (1.1 mL) was placed under a nitrogen atmosphere, cooled in a dry ice-acetone bath, and stirred while 1M BBr3 in CH2Cl2 (0.354 mL, 0.345 mmol) was added by syringe. The cooling bath was rem...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
C(Cl)Cl
null
2.6
CCCC1c2cc(OC)ccc2C2=C(C)C(=O)CCC21>C(Cl)Cl>CCCC1c2cc(O)ccc2C2=C(C)C(=O)CCC21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-5089406476cf406e8260118814d5a2c0
CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2Cl)C1=O>>CCCCC12CCC(=O)C=C1c1ccc(OC)c(Cl)c1C2
C(CCC)C1C(C2=CC=C(C(=C2C1)Cl)OC)=O.C(=C)C(=O)C.C[O-].[Na+].CO.C(CCC)C1(C(C2=CC=C(C(=C2C1)Cl)OC)=O)CCC(C)=O.N1CCCC1.C(C)(=O)O>>C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)OC)Cl
O=[C:11]1[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8](=[O:9])[CH3:10])[CH2:21][c:20]2[c:12]1[cH:13][cH:14][c:15]([O:16][CH3:17])[c:18]2[Cl:19]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[CH:10]=[C:11]1[c:12]1[cH:13][cH:14][c:15]([O:16][CH3:17])[c:18]([Cl:19])[c:20]1[CH2:21]2
CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2Cl)C1=O
CCCCC12CCC(=O)C=C1c1ccc(OC)c(Cl)c1C2
null
null
O1CCCC1.C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
85ff0aa8be631f96366b93c0f2ba199404913ad074e95e1352514ec4827258a9
b7bc018679e3f4c5a72b49c90c858cc3bcb4db12dedb0216b468af50ef8a00a3
O=C1C=C2c3ccccc3CC2CC1
O=[C;H0;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[C:5]-[C:6]-1(-[C:7])-[C:8]-[C:9]-[C:10](-[CH3;D1;+0:11])=[O;D1;H0:12]>>[C:7]-[C:6]12-[C:5]-[c:4]:[c:2](:[c:3])-[C;H0;D3;+0:1]-1=[CH;D2;+0:11]-[C:10](=[O;D1;H0:12])-[C:9]-[C:8]-2
null
[]
null
null
90
MINUTE
A solution 2-butyl-4-chloro-5-methoxy-1-indanone (550 mg, 2.03 mmol) in tetrahydrofuran (4.06 mL) was treated with methyl vinyl ketone (0.203 mL, 2.44 mmol) and 0.5N sodium methoxide in methanol (0.812 mL, 0.406 mmol). The mixture was stirred at room temperature for 90 minutes to effect conversion to 2-butyl-4-chloro-5...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Ketone
c1ccc2c(c1)CCC2
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
O1CCCC1.C1(=CC=CC=C1)C
null
1.5
CCCCC1(CCC(C)=O)Cc2c(ccc(OC)c2Cl)C1=O>O1CCCC1.C1(=CC=CC=C1)C>CCCCC12CCC(=O)C=C1c1ccc(OC)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9cf6287b0a4c41f28bee99b9776571b1
BrBr.CCCCC12CCC(=O)C=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2
C(CCC)C12CC3=C(C(=CC=C3C2=CC(CC1)=O)OC)Cl.C([O-])(O)=O.[Na+].BrBr>>BrC=1C(CCC2(CC3=C(C(=CC=C3C12)OC)Cl)CCCC)=O
Br[Br:11].[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[CH:10]=[C:12]1[c:13]1[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([Cl:20])[c:21]1[CH2:22]2>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([Br:11])=[C:12]1[c:13]1[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([Cl:20])[c:21]1[CH2:22...
BrBr.CCCCC12CCC(=O)C=C1c1ccc(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2
null
null
ClCCl.C(Cl)Cl
Functional Group Interconversion
Bromination
73ca391a48874f0a81f3694c6623ffb0a512c874931d8f551485082fa4a0d563
c7222534d68e666d405fc6d911092ac63e3791780d01400eb414eff6e46c2a54
O=C1C=C2c3ccccc3CC2CC1
Br-[Br;H0;D1;+0:1].[C:2]-[C:3](=[CH;D2;+0:4]-[C:5](=[O;D1;H0:6])-[C:7])-[c:8]>>[Br;H0;D1;+0:1]-[C;H0;D3;+0:4](=[C:3](-[C:2])-[c:8])-[C:5](=[O;D1;H0:6])-[C:7]
null
[]
null
null
30
MINUTE
A solution of 9a-butyl-8-chloro-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (555 mg, 1.82 mmol) in anhydrous dichloromethane (18.2 mL) was treated with sodium bicarbonate (765 mg, 9.1 mmol) and bromine (0.093 mL, 1.82 mmol). The mixture was stirred at room temperature for 30 minutes and then diluted with CH2Cl2 (50 ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Alkenyl halide
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HBr
ClCCl.C(Cl)Cl
null
0.5
BrBr.CCCCC12CCC(=O)C=C1c1ccc(OC)c(Cl)c1C2>ClCCl.C(Cl)Cl>CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2585e949972544e68ec775b4010b196e
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C(F)(F)F)=C1c1ccc(O)c(Cl)c1C2
B(Br)(Br)Br.C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C(F)(F)F)OC)Cl.B(Br)(Br)Br>>C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C(F)(F)F)O)Cl
C[O:20][c:19]1[cH:18][cH:17][c:16]2[c:23]([c:21]1[Cl:22])[CH2:24][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]([F:12])([F:13])[F:14])=[C:15]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]([F:12])([F:13])[F:14])=[C:15]1[c:16]1[cH:17][cH:18][c:19]([OH:20])[c:...
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1ccc(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1ccc(O)c(Cl)c1C2
null
null
ClCCl.C(Cl)Cl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
95
MINUTE
A solution of 9a-butyl-8-chloro-7-methoxy-4-(trifluoromethyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one (32 mg, 0.086 mmol) in anhydrous dichloromethane (0.86 mL) was cooled in a dry ice-acetone bath (−78° C.) and the solution was treated with 1M boron tribromide in dichloromethane (0.258 mL, 0.258 mmol). The cooling bath w...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
ClCCl.C(Cl)Cl
null
1.583333
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1ccc(OC)c(Cl)c1C2>ClCCl.C(Cl)Cl>CCCCC12CCC(=O)C(C(F)(F)F)=C1c1ccc(O)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6e31e21fba51466aaf8cfe2488e576b3
C=[C](OCC)[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2>>C=C(OCC)C1=C2c3ccc(OC)c(Cl)c3CC2(CCCC)CCC1=O
BrC=1C(CCC2(CC3=C(C(=CC=C3C12)OC)Cl)CCCC)=O.C(CCC)[Sn](C(=C)OCC)(CCCC)CCCC>>C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C(=C)OCC)OC)Cl
CCC[CH2][Sn]([CH2]CCC)([CH2]CCC)[C:2](=[CH2:1])[O:3][CH2:4][CH3:5].Br[C:6]1=[C:7]2[c:8]3[cH:9][cH:10][c:11]([O:12][CH3:13])[c:14]([Cl:15])[c:16]3[CH2:17][C:18]2([CH2:19][CH2:20][CH2:21][CH3:22])[CH2:23][CH2:24][C:25]1=[O:26]>>[CH2:1]=[C:2]([O:3][CH2:4][CH3:5])[C:6]1=[C:7]2[c:8]3[cH:9][cH:10][c:11]([O:12][CH3:13])[c:14]...
C=[C](OCC)[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2
C=C(OCC)C1=C2c3ccc(OC)c(Cl)c3CC2(CCCC)CCC1=O
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
C1(=CC=CC=C1)C
C-C Coupling
Stille reaction_other
9c48440b626589bda452d19ba29733afd2b18391c3ba2e9aaffdf5d6a1aee497
d1092acfedce3fd35bb9bbd3772a9f24078f9c16eee7ceb70d0a0949d0e81c99
O=C1C=C2c3ccccc3CC2CC1
Br-[C;H0;D3;+0:1](=[C:2](-[C:3])-[c:4])-[C:5](=[O;D1;H0:6])-[C:7].C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-C-C)-[C;H0;D3;+0:8](=[C;D1;H2:9])-[#8:10]-[C:11]>>[C:3]-[C:2](=[C;H0;D3;+0:1](-[C;H0;D3;+0:8](=[C;D1;H2:9])-[#8:10]-[C:11])-[C:5](=[O;D1;H0:6])-[C:7])-[c:4]
76
[{"value": 76.0, "product": "C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C(=C)OCC)OC)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A solution of 4-bromo-9a-butyl-8-chloro-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (90 mg, 0.235 mmol) in anhydrous toluene (1.2 mL) was treated with tributyl(1-ethoxyvinyl)stannane (0.111 mL, 0.352 mmol) and bis(triphenylphosphine)palladium(II) chloride (33 mg, 0.047 mmol). The mixture was placed under a nitrogen ...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Ketone.Ether.Vinyl.Tin
Ketone.Ether
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HBr.Sn
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C1(=CC=CC=C1)C
100
null
C=[C](OCC)[Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.C1(=CC=CC=C1)C>C=C(OCC)C1=C2c3ccc(OC)c(Cl)c3CC2(CCCC)CCC1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-194006f950674b50a93e6edc19549752
C=C(OCC)C1=C2c3ccc(OC)c(Cl)c3CC2(CCCC)CCC1=O>>CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(OC)c(Cl)c1C2
C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C(=C)OCC)OC)Cl.Cl>>C(C)(=O)C=1C(CCC2(CC3=C(C(=CC=C3C12)OC)Cl)CCCC)=O
CC[O:13][C:11]([C:10]1=[C:14]2[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]1=[O:9])[CH2:24][c:23]1[c:15]2[cH:16][cH:17][c:18]([O:19][CH3:20])[c:21]1[Cl:22])=[CH2:12]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]([CH3:12])=[O:13])=[C:14]1[c:15]1[cH:16][cH:17][c:18]([O:19][CH3:20]...
C=C(OCC)C1=C2c3ccc(OC)c(Cl)c3CC2(CCCC)CCC1=O
CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(OC)c(Cl)c1C2
null
null
O.C(C)O
Miscellaneous
OtherReaction
3e02cda7ca3208f28d8355e2c059d63c9e4eb2c7eba0cae088d693f3c74db23e
215582e9637166736070a53bb588f4e45b0dfc6c974d1df4c97ac5a98451627c
O=C1C=C2c3ccccc3CC2CC1
C-C-[O;H0;D2;+0:1]-[C;H0;D3;+0:2](=[CH2;D1;+0:3])-[C:4](=[C:5](-[C:6])-[c:7])-[C:8](=[O;D1;H0:9])-[C:10]>>[C:6]-[C:5](=[C:4](-[C;H0;D3;+0:2](-[CH3;D1;+0:3])=[O;H0;D1;+0:1])-[C:8](=[O;D1;H0:9])-[C:10])-[c:7]
null
[]
80
CELSIUS
null
null
The product from step 1 in ethanol (1.0 mL), water (0.2 mL) and aqueous 2N HCl (0.2 mL) was stirred and heated in an oil bath at 80° C. for 40 minutes. After cooling, the mixture was partitioned between EtOAc (20 mL) and water (20 mL). The organic phase was washed with brine (20 mL), dried over MgSO4, filtered, and eva...
10.6084/m9.figshare.5104873.v1
null
Ether.Vinyl
Ketone
null
null
C1=C2c3ccccc3CC2CCC1
Other
O.C(C)O
80
null
C=C(OCC)C1=C2c3ccc(OC)c(Cl)c3CC2(CCCC)CCC1=O>O.C(C)O>CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(OC)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-49e41638e01341c08bfbc41dd6e4affb
CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(O)c(Cl)c1C2
C(C)(=O)C=1C(CCC2(CC3=C(C(=CC=C3C12)OC)Cl)CCCC)=O.Cl.N1=CC=CC=C1>>C(C)(=O)C=1C(CCC2(CC3=C(C(=CC=C3C12)O)Cl)CCCC)=O
C[O:19][c:18]1[cH:17][cH:16][c:15]2[c:22]([c:20]1[Cl:21])[CH2:23][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]([CH3:12])=[O:13])=[C:14]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]([CH3:12])=[O:13])=[C:14]1[c:15]1[cH:16][cH:17][c:18]([OH:19])[c:20]([Cl:21...
CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(O)c(Cl)c1C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
200
CELSIUS
null
null
A mixture of 4-acetyl-9a-butyl-8-chloro-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (54 mg) and pyridine hydrochloride (3.5 g) was heated in an oil bath at 200° C. for one hour. After cooling to room temperature, the mixture was partitioned between EtOAc (50 mL) and water (50 mL). The organic phase was washed with b...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
null
200
null
CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C(C)=O)=C1c1ccc(O)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e993677936f64b12a731aaf297bed3e9
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)c(Cl)c1C2
BrC=1C(CCC2(CC3=C(C(=CC=C3C12)OC)Cl)CCCC)=O.[Cu]C#N>>C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C#N)OC)Cl
Br[C:10]1=[C:13]2[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8]1=[O:9])[CH2:23][c:22]1[c:14]2[cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]1[Cl:21]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]#[N:12])=[C:13]1[c:14]1[cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]([Cl:21])[c:22]1[CH2:23]2
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)c(Cl)c1C2
null
null
CN1C(CCC1)=O
Miscellaneous
OtherReaction
9adadf535edd63596f40811ded4b5d76fe0b83c469549ed7abf606d845021290
8953536f7fe46a44d657de6166386d42d9afab94586603b5dca76fc653fbf47b
O=C1C=C2c3ccccc3CC2CC1
Br-[C;H0;D3;+0:1](=[C:2](-[C:3])-[c:4])-[C:5](=[O;D1;H0:6])-[C:7]>>[C:3]-[C:2](=[C;H0;D3;+0:1](-[C:8]#[N;D1;H0:9])-[C:5](=[O;D1;H0:6])-[C:7])-[c:4]
73.5
[{"value": 73.5, "product": "C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C#N)OC)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
150
CELSIUS
null
null
A solution of 4-bromo-9a-butyl-8-chloro-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (103 mg, 0.268 mmol) in anhydrous 1-methyl-2-pyrrolidinone (0.54 mL) was treated with copper(I) cyanide (24 mg, 0.268 mmol). The mixture was placed under a nitrogen atmosphere, stirred, and heated in an oil bath at 150° C. for 1.5 ho...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide
Ketone.Nitrile
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
Br-
CN1C(CCC1)=O
150
null
CCCCC12CCC(=O)C(Br)=C1c1ccc(OC)c(Cl)c1C2>CN1C(CCC1)=O>CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-4492a1316c2143eaaae289f2e539a4d5
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C#N)=C1c1ccc(O)c(Cl)c1C2
C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C#N)OC)Cl.Cl.N1=CC=CC=C1>>C(CCC)C12CC3=C(C(=CC=C3C2=C(C(CC1)=O)C#N)O)Cl
C[O:18][c:17]1[cH:16][cH:15][c:14]2[c:21]([c:19]1[Cl:20])[CH2:22][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]#[N:12])=[C:13]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]#[N:12])=[C:13]1[c:14]1[cH:15][cH:16][c:17]([OH:18])[c:19]([Cl:20])[c:21]1[CH2:22]2
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(C#N)=C1c1ccc(O)c(Cl)c1C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
200
CELSIUS
null
null
A mixture of 9a-butyl-8-chloro-4-cyano-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (65 mg) and pyridine hydrochloride (4.2 g) was heated in an oil bath at 200° C. for 85 minutes. After cooling to room temperature, the mixture was partitioned between EtOAc (50 mL) and water (50 mL). The organic phase was washed with ...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
null
200
null
CCCCC12CCC(=O)C(C#N)=C1c1ccc(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C#N)=C1c1ccc(O)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-964e1b3c9e4a4ee4925791c3c6f268ce
CCCCCC(=O)Cl.COc1ccccc1F>>CCCCCC(=O)c1ccc(OC)c(F)c1
Cl.[Cl-].[Al+3].[Cl-].[Cl-].FC1=C(C=CC=C1)OC.C(CCCCC)(=O)Cl>>FC=1C=C(C=CC1OC)C(CCCCC)=O
Cl[C:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:7].[cH:8]1[cH:9][cH:10][c:11]([O:12][CH3:13])[c:14]([F:15])[cH:16]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][cH:10][c:11]([O:12][CH3:13])[c:14]([F:15])[cH:16]1
CCCCCC(=O)Cl.COc1ccccc1F
CCCCCC(=O)c1ccc(OC)c(F)c1
null
null
null
C-C Coupling
Friedel-Crafts acylation
55541449ad4f182ef3dc0497085b282b1dcb76e0fb5ed140dc4eab4973eacb28
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:6]:[c:5]
90.4
[{"value": 90.4, "product": "FC=1C=C(C=CC1OC)C(CCCCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
45
MINUTE
Aluminum chloride (6.5 g, 48.8 mmol) was added to a stirred mixture of 1-fluoro-2-methoxybenzene (5.0 mL, 44.4 mmol) and hexanoyl chloride (7.5 mL, 53.3 mmol) at room temperature. The mixture warmed and HCl evolution occurred. The resulting mixture was stirred at room temperature for 45 minutes and then partitioned bet...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HCl
null
null
0.75
CCCCCC(=O)Cl.COc1ccccc1F>>CCCCCC(=O)c1ccc(OC)c(F)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1a97121dbeb748ada83910f7c64b7fb6
CCCCC1Cc2cc(OC)c(F)cc2C1=O>>CCCCC1Cc2cc(O)c(F)cc2C1=O
C(CCC)C1C(C2=CC(=C(C=C2C1)OC)F)=O.Cl.N1=CC=CC=C1>>C(CCC)C1C(C2=CC(=C(C=C2C1)O)F)=O
C[O:10][c:9]1[cH:8][c:7]2[c:14]([cH:13][c:11]1[F:12])[C:15](=[O:16])[CH:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[cH:8][c:9]([OH:10])[c:11]([F:12])[cH:13][c:14]2[C:15]1=[O:16]
CCCCC1Cc2cc(OC)c(F)cc2C1=O
CCCCC1Cc2cc(O)c(F)cc2C1=O
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1CCc2ccccc21
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
95.1
[{"value": 95.1, "product": "C(CCC)C1C(C2=CC(=C(C=C2C1)O)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
200
CELSIUS
null
null
A mixture of 2-butyl-6-fluoro-5-methoxy-1-indanone (2.0 g) and pyridine hydrochloride (15.0 g) was heated in an oil bath at 200° C. for 75 minutes. After cooling to room temperature, the mixture was partitioned between EtOAc (100 mL) and water (75 mL) containing brine (25 mL). The organic phase was washed with brine (5...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccc2c(c1)CCC2
Other
null
200
null
CCCCC1Cc2cc(OC)c(F)cc2C1=O>>CCCCC1Cc2cc(O)c(F)cc2C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-003b390b794440cdb243ce9841e7b453
CCCCC1Cc2cc(O)c(F)cc2C1=O.O=C1CCC(=O)N1Br>>CCCCC1Cc2c(cc(F)c(O)c2Br)C1=O
BrN1C(CCC1=O)=O.C(CCC)C1C(C2=CC(=C(C=C2C1)O)F)=O>>BrC1=C2CC(C(C2=CC(=C1O)F)=O)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][c:10]([F:11])[c:12]([OH:13])[cH:14]2)[C:16]1=[O:17].O=C1CCC(=O)N1[Br:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][c:10]([F:11])[c:12]([OH:13])[c:14]2[Br:15])[C:16]1=[O:17]
CCCCC1Cc2cc(O)c(F)cc2C1=O.O=C1CCC(=O)N1Br
CCCCC1Cc2c(cc(F)c(O)c2Br)C1=O
null
null
CN(C=O)C
Functional Group Interconversion
Bromination
810b77391b192e36eecbf89fbd0937a488e789bac7683cb9fabaa7cbc9c32e40
0e444576b73669992a4073cc3f7b10ed52cb9df09f9f8e4042e39e6a602aa390
O=C1CCc2ccccc21
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[C:2]-[c:3](:[c:4]-[C:5]=[O;D1;H0:6]):[cH;D2;+0:7]:[c:8](-[O;D1;H1:9]):[c:10]>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:7](:[c:8](-[O;D1;H1:9]):[c:10]):[c:3](:[c:4]-[C:5]=[O;D1;H0:6])-[C:2]
90.9
[{"value": 90.9, "product": "BrC1=C2CC(C(C2=CC(=C1O)F)=O)CCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
N-Bromosuccinimide (1.41 g, 7.93 mmol) was added to a solution of 2-butyl-6-fluoro-5-hydroxy-1-indanone (1.76 g, 7.93 mmol) in anhydrous N,N-dimethylformamide (15 mL). The resulting solution was stirred at room temperature for two hours. The solvent was evaporated under vacuum and the residue was partitioned between Et...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Aromatic halide
c1ccc2c(c1)CCC2.C1CCNC1
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
CN(C=O)C
null
2
CCCCC1Cc2cc(O)c(F)cc2C1=O.O=C1CCC(=O)N1Br>CN(C=O)C>CCCCC1Cc2c(cc(F)c(O)c2Br)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-835f01ea929a484fbdde0611e5ce74b3
CCCCC1Cc2c(cc(F)c(O)c2Br)C1=O.CI>>CCCCC1Cc2c(cc(F)c(OC)c2Br)C1=O
BrC1=C2CC(C(C2=CC(=C1O)F)=O)CCCC.CI.C([O-])(O)=O.[Na+]>>BrC1=C2CC(C(C2=CC(=C1OC)F)=O)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][c:10]([F:11])[c:12]([OH:13])[c:15]2[Br:16])[C:17]1=[O:18].I[CH3:14]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][c:10]([F:11])[c:12]([O:13][CH3:14])[c:15]2[Br:16])[C:17]1=[O:18]
CCCCC1Cc2c(cc(F)c(O)c2Br)C1=O.CI
CCCCC1Cc2c(cc(F)c(OC)c2Br)C1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
b8b041187bac58376aae824630608e7deb49a01db3d652291f8b379c10d4e434
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
O=C1CCc2ccccc21
I-[CH3;D1;+0:1].[OH;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]
81.6
[{"value": 81.6, "product": "BrC1=C2CC(C(C2=CC(=C1OC)F)=O)CCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
17
HOUR
A mixture of 4-bromo-2-butyl-6-fluoro-5-hydroxy-1-indanone (2.17 g, 7.23 mmol), N,N-dimethylformamide (14.5 mL), methyl iodide (0.675 mL, 10.84 mmol), and sodium bicarbonate (1.50 g, 18.1 mmol) was stirred at room temperature for 17 hours. The solvent was evaporated under vacuum. The residue in EtOAc (150 mL) was washe...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
null
null
c1ccc2c(c1)CCC2
HI
CN(C=O)C
null
17
CCCCC1Cc2c(cc(F)c(O)c2Br)C1=O.CI>CN(C=O)C>CCCCC1Cc2c(cc(F)c(OC)c2Br)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-270913168eb241f99a23be25455ccdcc
CCCCC1Cc2c(cc(F)c(OC)c2Br)C1=O.[CH3][Sn]([CH3])([CH3])[CH3]>>CCCCC1Cc2c(cc(F)c(OC)c2C)C1=O
BrC1=C2CC(C(C2=CC(=C1OC)F)=O)CCCC.C[Sn](C)(C)C.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.[Cl-].[Li+]>>C(CCC)C1C(C2=CC(=C(C(=C2C1)C)OC)F)=O
Br[c:15]1[c:7]2[c:8]([cH:9][c:10]([F:11])[c:12]1[O:13][CH3:14])[C:17](=[O:18])[CH:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6]2.[CH3][Sn]([CH3])([CH3])[CH3:16]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][c:10]([F:11])[c:12]([O:13][CH3:14])[c:15]2[CH3:16])[C:17]1=[O:18]
CCCCC1Cc2c(cc(F)c(OC)c2Br)C1=O.[CH3][Sn]([CH3])([CH3])[CH3]
CCCCC1Cc2c(cc(F)c(OC)c2C)C1=O
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
CN(C=O)C
C-C Coupling
Stille reaction_other
5f823a1f140c9788378795502c3f73833375dcf595f9e9d5f6b25610b5e941bf
db27eeefac0475c6d74fa10b3167e95a61caaae74e8bbafd45892452c0c3d4d6
O=C1CCc2ccccc21
Br-[c;H0;D3;+0:1](:[c:2](-[#8:3]):[c:4]):[c:5](:[c:6]-[C:7]=[O;D1;H0:8])-[C:9].[CH3;D1;+0:10]-[Sn](-[CH3])(-[CH3])-[CH3]>>[#8:3]-[c:2](:[c:4]):[c;H0;D3;+0:1](-[CH3;D1;+0:10]):[c:5](:[c:6]-[C:7]=[O;D1;H0:8])-[C:9]
24.5
[{"value": 24.5, "product": "C(CCC)C1C(C2=CC(=C(C(=C2C1)C)OC)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A mixture of 4-bromo-2-butyl-6-fluoro-5-methoxy-1-indanone (1.86 g, 5.94 mmol), bis(triphenylphosphine)palladium(II) chloride (208 mg, 0.297 mmol), tetramethyltin (0.989 mL, 7.128 mmol), triphenylphosphine (156 mg, 0.594 mmol), lithium chloride (504 mg, 11.88 mmol), and anhydrous N,N-dimethyl-formamide (11.9 mL) was pl...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Tin
null
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HBr.Sn
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C=O)C
100
null
CCCCC1Cc2c(cc(F)c(OC)c2Br)C1=O.[CH3][Sn]([CH3])([CH3])[CH3]>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.CN(C=O)C>CCCCC1Cc2c(cc(F)c(OC)c2C)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3bfd2b8db18a4c68b99e3c5c20362e76
CCCCC1(CCC(=O)CCC)Cc2c(cc(F)c(OC)c2C)C1=O>>CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(C)c1C2
C(CCC)C1(C(C2=CC(=C(C(=C2C1)C)OC)F)=O)CCC(CCC)=O.C(CCC)C1C(C2=CC(=C(C(=C2C1)C)OC)F)=O.C(=C)C(=O)CCC.N12CCCCCC2=NCCC1.Cl>>C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)CC)F)OC)C
O=[C:13]1[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8](=[O:9])[CH2:10][CH2:11][CH3:12])[CH2:24][c:23]2[c:14]1[cH:15][c:16]([F:17])[c:18]([O:19][CH3:20])[c:21]2[CH3:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH2:11][CH3:12])=[C:13]1[c:14]1[cH:15][c:16]([F:17])[c:18]([O:19][CH3:2...
CCCCC1(CCC(=O)CCC)Cc2c(cc(F)c(OC)c2C)C1=O
CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(C)c1C2
null
null
C(C)(=O)O.O1CCCC1
Functional Group Interconversion
OtherReaction
85ff0aa8be631f96366b93c0f2ba199404913ad074e95e1352514ec4827258a9
b7bc018679e3f4c5a72b49c90c858cc3bcb4db12dedb0216b468af50ef8a00a3
O=C1C=C2c3ccccc3CC2CC1
O=[C;H0;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[C:5]-[C:6]-1(-[C:7])-[C:8]-[C:9]-[C:10](=[O;D1;H0:11])-[CH2;D2;+0:12]-[C:13]-[C;D1;H3:14]>>[C:7]-[C:6]12-[C:5]-[c:4]:[c:2](:[c:3])-[C;H0;D3;+0:1]-1=[C;H0;D3;+0:12](-[C:13]-[C;D1;H3:14])-[C:10](=[O;D1;H0:11])-[C:9]-[C:8]-2
null
[]
50
CELSIUS
64
HOUR
A solution of 2-butyl-6-fluoro-5-methoxy-4-methyl-1-indanone (118 mg, 0.47 mmol) in anhydrous tetrahydrofuran (0.47 mL) was treated with propyl vinyl ketone (0.065 mL, 0.56 mmol) and 1,8-diazabicyclo[5.4.0]undec-7-ene (0.0143 mL, 0.094 mmol). The mixture was stirred and heated in an oil bath at 50° C. for 6 hours and t...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Ketone
c1ccc2c(c1)CCC2
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
C(C)(=O)O.O1CCCC1
50
64
CCCCC1(CCC(=O)CCC)Cc2c(cc(F)c(OC)c2C)C1=O>C(C)(=O)O.O1CCCC1>CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(C)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a350b29a8dfe43538f450062d73c643c
CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(C)c1C2>>CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(O)c(C)c1C2
C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)CC)F)OC)C.B(Br)(Br)Br>>C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)CC)F)O)C
C[O:19][c:18]1[c:16]([F:17])[cH:15][c:14]2[c:22]([c:20]1[CH3:21])[CH2:23][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH2:11][CH3:12])=[C:13]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH2:11][CH3:12])=[C:13]1[c:14]1[cH:15][c:16]([F:17])[c:18]([OH:19])[c:20]([CH3:...
CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(C)c1C2
CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(O)c(C)c1C2
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
90
MINUTE
A solution of 9a-butyl-4-ethyl-6-fluoro-7-methoxy-8-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-one (93 mg, 0.28 mmol) in anhydrous dichloromethane (1.4 mL) was cooled in a dry ice-acetone bath (−78° C.) and the solution treated with 1M boron tribromide in dichloromethane (1.4 mL, 1.4 mmol). The cooling bath was removed an...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
ClCCl
null
1.5
CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(C)c1C2>ClCCl>CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(O)c(C)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ec39dbd4e6074985880755ae6356933c
CCCCCC(=O)Cl.COc1c(F)cccc1Cl>>CCCCCC(=O)c1cc(F)c(OC)c(Cl)c1
Cl.[Cl-].[Al+3].[Cl-].[Cl-].ClC1=C(C(=CC=C1)F)OC.C(CCCCC)(=O)Cl>>ClC=1C=C(C=C(C1OC)F)C(CCCCC)=O
Cl[C:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:7].[cH:8]1[cH:9][c:10]([F:11])[c:12]([O:13][CH3:14])[c:15]([Cl:16])[cH:17]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6](=[O:7])[c:8]1[cH:9][c:10]([F:11])[c:12]([O:13][CH3:14])[c:15]([Cl:16])[cH:17]1
CCCCCC(=O)Cl.COc1c(F)cccc1Cl
CCCCCC(=O)c1cc(F)c(OC)c(Cl)c1
null
null
null
C-C Coupling
Friedel-Crafts acylation
55541449ad4f182ef3dc0497085b282b1dcb76e0fb5ed140dc4eab4973eacb28
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[c:5]:[c:6]:[cH;D2;+0:7]:[c:8]:[c:9]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:6]:[c:5]
null
[]
null
null
67
HOUR
Aluminum chloride (1.16 g, 8.72 mmol) was added to a stirred mixture of 1-chloro-3-fluoro-2-methoxybenzene (1.00 mL, 8.72 mmol) and hexanoyl chloride (1.47 mL, 10.46 mmol) at room temperature. The mixture warmed and HCl evolution occurred. The resulting mixture was stirred at room temperature for 67 hours and then part...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1ccccc1
c1ccccc1
c1ccccc1
HCl
null
null
67
CCCCCC(=O)Cl.COc1c(F)cccc1Cl>>CCCCCC(=O)c1cc(F)c(OC)c(Cl)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-644c4332f59e457193dc2c4b5fdfdc26
C=O.CCCCCC(=O)c1cc(F)c(OC)c(Cl)c1>>CCCCC1Cc2c(cc(F)c(OC)c2Cl)C1=O
ClC=1C=C(C=C(C1OC)F)C(CCCCC)=O.C=O.C([O-])([O-])=O.[K+].[K+]>>C(CCC)C1C(C2=CC(=C(C(=C2C1)Cl)OC)F)=O
O=[CH2:6].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:17]([c:8]1[cH:7][c:15]([Cl:16])[c:12]([O:13][CH3:14])[c:10]([F:11])[cH:9]1)=[O:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]1[CH2:6][c:7]2[c:8]([cH:9][c:10]([F:11])[c:12]([O:13][CH3:14])[c:15]2[Cl:16])[C:17]1=[O:18]
C=O.CCCCCC(=O)c1cc(F)c(OC)c(Cl)c1
CCCCC1Cc2c(cc(F)c(OC)c2Cl)C1=O
null
null
CO
C-C Coupling
OtherReaction
be5065257dca5929b2d78368822674c085beb35c1db50df521ad25c0f1e1d5d4
2250efeff48c31e3815cbf34eea492a4c680e679ee80813f830cfdaaf31b101f
O=C1CCc2ccccc21
O=[CH2;D1;+0:1].[C:2]-[C:3]-[CH2;D2;+0:4]-[C:5](=[O;D1;H0:6])-[c:7](:[c:8]):[cH;D2;+0:9]:[c:10](-[Cl;D1;H0:11]):[c:12]>>[C:2]-[C:3]-[CH;D3;+0:4]1-[CH2;D2;+0:1]-[c;H0;D3;+0:9](:[c:10](-[Cl;D1;H0:11]):[c:12]):[c:7](:[c:8])-[C:5]-1=[O;D1;H0:6]
null
[]
50
CELSIUS
null
null
A mixture of the crude 1-(3-chloro-5-fluoro-4-methoxyphenyl)-1-hexanone from step 1, methanol (8.7 mL), 37% aqueous formaldehyde (0.786 mL, 10.5 mmol), and potassium carbonate (1.2 g, 8.72 mmol) was stirred and heated in an oil bath at 50° C. for 7 hours. The mixture was evaporated under vacuum and the residue partitio...
10.6084/m9.figshare.5104873.v1
null
Formaldehyde.Ketone
Ketone
c1ccccc1
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
HO-
CO
50
null
C=O.CCCCCC(=O)c1cc(F)c(OC)c(Cl)c1>CO>CCCCC1Cc2c(cc(F)c(OC)c2Cl)C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-3ce351c7b8ea4f2facd72afa9105e46c
CCCCC12CCC(=O)C(C)=C1c1cc(F)c(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C)=C1c1cc(F)c(O)c(Cl)c1C2
C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)C)F)OC)Cl.Cl.N1=CC=CC=C1>>C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)C)F)O)Cl
C[O:18][c:17]1[c:15]([F:16])[cH:14][c:13]2[c:21]([c:19]1[Cl:20])[CH2:22][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH3:11])=[C:12]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH3:11])=[C:12]1[c:13]1[cH:14][c:15]([F:16])[c:17]([OH:18])[c:19]([Cl:20])[c:21]1[CH2:22...
CCCCC12CCC(=O)C(C)=C1c1cc(F)c(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(C)=C1c1cc(F)c(O)c(Cl)c1C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
200
CELSIUS
null
null
The product mixture from step 3 and pyridine hydrochloride (5.3 g) were combined and heated in an oil bath at 200° C. for 90 minutes. After cooling, the mixture was partitioned between EtOAc (50 mL) and water (50 ml). The organic phase was washed with brine (50 mL), dried over MgSO4, filtered, and evaporated under vacu...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
null
200
null
CCCCC12CCC(=O)C(C)=C1c1cc(F)c(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C)=C1c1cc(F)c(O)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-325295534468402fb193b69d30d93a94
CCCCC1(CCC(=O)CCC)Cc2c(cc(F)c(OC)c2Cl)C1=O>>CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(Cl)c1C2
C[O-].[Na+].CO.N12CCCCCC2=NCCC1.C(CCC)C1(C(C2=CC(=C(C(=C2C1)Cl)OC)F)=O)CCC(CCC)=O.Cl.C(=C)C(=O)CCC>>C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)CC)F)OC)Cl
O=[C:13]1[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8](=[O:9])[CH2:10][CH2:11][CH3:12])[CH2:24][c:23]2[c:14]1[cH:15][c:16]([F:17])[c:18]([O:19][CH3:20])[c:21]2[Cl:22]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([CH2:11][CH3:12])=[C:13]1[c:14]1[cH:15][c:16]([F:17])[c:18]([O:19][CH3:20...
CCCCC1(CCC(=O)CCC)Cc2c(cc(F)c(OC)c2Cl)C1=O
CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(Cl)c1C2
null
null
C(C)(=O)O.O1CCCC1
Functional Group Interconversion
OtherReaction
85ff0aa8be631f96366b93c0f2ba199404913ad074e95e1352514ec4827258a9
b7bc018679e3f4c5a72b49c90c858cc3bcb4db12dedb0216b468af50ef8a00a3
O=C1C=C2c3ccccc3CC2CC1
O=[C;H0;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[C:5]-[C:6]-1(-[C:7])-[C:8]-[C:9]-[C:10](=[O;D1;H0:11])-[CH2;D2;+0:12]-[C:13]-[C;D1;H3:14]>>[C:7]-[C:6]12-[C:5]-[c:4]:[c:2](:[c:3])-[C;H0;D3;+0:1]-1=[C;H0;D3;+0:12](-[C:13]-[C;D1;H3:14])-[C:10](=[O;D1;H0:11])-[C:9]-[C:8]-2
null
[]
60
CELSIUS
null
null
A sample of the crude product from step 2 in the preceding example (386 mg, 1.36 mmol) in anhydrous tetrahydrofuran (2.7 mL) was treated with propyl vinyl ketone (0.188 mL, 1.63 mmol) and 1,8-diazabicyclo[5.4.0]undec-7-ene (0.041 mL, 0.272 mmol). The mixture was stirred and heated in an oil bath at 60° C. for two hours...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Ketone
c1ccc2c(c1)CCC2
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
C(C)(=O)O.O1CCCC1
60
null
CCCCC1(CCC(=O)CCC)Cc2c(cc(F)c(OC)c2Cl)C1=O>C(C)(=O)O.O1CCCC1>CCCCC12CCC(=O)C(CC)=C1c1cc(F)c(OC)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f4004a05731743db9d750d86b5473e91
CCCCC1(CCC(C)=O)Cc2c(cc(F)c(OC)c2Cl)C1=O>>CCCCC12CCC(=O)C=C1c1cc(F)c(OC)c(Cl)c1C2
N1CCCC1.C(C)(=O)O.C(CCC)C1C(C2=CC(=C(C(=C2C1)Cl)OC)F)=O.C(=C)C(=O)C.C[O-].[Na+].CO.C(CCC)C1(C(C2=CC(=C(C(=C2C1)Cl)OC)F)=O)CCC(C)=O>>C(CCC)C12CC3=C(C(=C(C=C3C2=CC(CC1)=O)F)OC)Cl
O=[C:11]1[C:5]([CH2:4][CH2:3][CH2:2][CH3:1])([CH2:6][CH2:7][C:8](=[O:9])[CH3:10])[CH2:22][c:21]2[c:12]1[cH:13][c:14]([F:15])[c:16]([O:17][CH3:18])[c:19]2[Cl:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[CH:10]=[C:11]1[c:12]1[cH:13][c:14]([F:15])[c:16]([O:17][CH3:18])[c:19]([Cl:20])[c:21]1[CH2:22]2
CCCCC1(CCC(C)=O)Cc2c(cc(F)c(OC)c2Cl)C1=O
CCCCC12CCC(=O)C=C1c1cc(F)c(OC)c(Cl)c1C2
null
null
O1CCCC1.C1(=CC=CC=C1)C
Functional Group Interconversion
OtherReaction
85ff0aa8be631f96366b93c0f2ba199404913ad074e95e1352514ec4827258a9
b7bc018679e3f4c5a72b49c90c858cc3bcb4db12dedb0216b468af50ef8a00a3
O=C1C=C2c3ccccc3CC2CC1
O=[C;H0;D3;+0:1]1-[c:2](:[c:3]):[c:4]-[C:5]-[C:6]-1(-[C:7])-[C:8]-[C:9]-[C:10](-[CH3;D1;+0:11])=[O;D1;H0:12]>>[C:7]-[C:6]12-[C:5]-[c:4]:[c:2](:[c:3])-[C;H0;D3;+0:1]-1=[CH;D2;+0:11]-[C:10](=[O;D1;H0:12])-[C:9]-[C:8]-2
null
[]
null
null
5.5
HOUR
A solution of crude 2-butyl-4-chloro-6-fluoro-5-methoxy-1-indanone (386 mg, 1.4 mmol) in tetrahydrofuran (2.8 mL) was treated with methyl vinyl ketone (0.150 mL, 1.78 mmol) and 0.5N sodium methoxide in methanol (1.1 mL, 0.56 mmol). The mixture was stirred at room temperature for 5.5 hours to effect conversion to 2-buty...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Ketone
c1ccc2c(c1)CCC2
C1=C2c3ccccc3CC2CCC1
C1=C2c3ccccc3CC2CCC1
HO-
O1CCCC1.C1(=CC=CC=C1)C
null
5.5
CCCCC1(CCC(C)=O)Cc2c(cc(F)c(OC)c2Cl)C1=O>O1CCCC1.C1(=CC=CC=C1)C>CCCCC12CCC(=O)C=C1c1cc(F)c(OC)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-72b7c7dabe5b4cf6835bd1c3a2ab8214
CCCCC12CCC(=O)C(Br)=C1c1cc(F)c(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(Br)=C1c1cc(F)c(O)c(Cl)c1C2
BrC=1C(CCC2(CC3=C(C(=C(C=C3C12)F)OC)Cl)CCCC)=O.B(Br)(Br)Br>>BrC=1C(CCC2(CC3=C(C(=C(C=C3C12)F)O)Cl)CCCC)=O
C[O:18][c:17]1[c:15]([F:16])[cH:14][c:13]2[c:21]([c:19]1[Cl:20])[CH2:22][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([Br:11])=[C:12]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([Br:11])=[C:12]1[c:13]1[cH:14][c:15]([F:16])[c:17]([OH:18])[c:19]([Cl:20])[c:21]1[CH2:22]2
CCCCC12CCC(=O)C(Br)=C1c1cc(F)c(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(Br)=C1c1cc(F)c(O)c(Cl)c1C2
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
1
HOUR
A solution of 4-bromo-9a-butyl-8-chloro-6-fluoro-7-methoxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one (31 mg, 0.077 mmol) in anhydrous dichloromethane (0.5 mL) was cooled in a dry ice-acetone bath (−78° C.) and the solution treated with 1M boron tribromide in dichloromethane (0.231 mL, 0.231 mmol). The cooling bath was remov...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
ClCCl
null
1
CCCCC12CCC(=O)C(Br)=C1c1cc(F)c(OC)c(Cl)c1C2>ClCCl>CCCCC12CCC(=O)C(Br)=C1c1cc(F)c(O)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2114ab91aa8947dd91beb80fa17fd697
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1cc(F)c(OC)c(Cl)c1C2>>CCCCC12CCC(=O)C(C(F)(F)F)=C1c1cc(F)c(O)c(Cl)c1C2
C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)C(F)(F)F)F)OC)Cl.B(Br)(Br)Br>>C(CCC)C12CC3=C(C(=C(C=C3C2=C(C(CC1)=O)C(F)(F)F)F)O)Cl
C[O:21][c:20]1[c:18]([F:19])[cH:17][c:16]2[c:24]([c:22]1[Cl:23])[CH2:25][C:5]1([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]([F:12])([F:13])[F:14])=[C:15]12>>[CH3:1][CH2:2][CH2:3][CH2:4][C:5]12[CH2:6][CH2:7][C:8](=[O:9])[C:10]([C:11]([F:12])([F:13])[F:14])=[C:15]1[c:16]1[cH:17][c:18]([F:19])[c:2...
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1cc(F)c(OC)c(Cl)c1C2
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1cc(F)c(O)c(Cl)c1C2
null
null
ClCCl
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C1C=C2c3ccccc3CC2CC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
1
HOUR
A solution of 9a-butyl-8-chloro-6-fluoro-7-methoxy-4-(trifluoromethyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one (39 mg, 0.10 mmol) in anhydrous dichloromethane (1.0 mL) was cooled in a dry ice-acetone bath (−78° C.) and the solution was treated with 1M boron tribromide in dichloromethane (0.3 mL, 0.3 mmol). The cooling bat...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
C1=C2c3ccccc3CC2CCC1
Other
ClCCl
null
1
CCCCC12CCC(=O)C(C(F)(F)F)=C1c1cc(F)c(OC)c(Cl)c1C2>ClCCl>CCCCC12CCC(=O)C(C(F)(F)F)=C1c1cc(F)c(O)c(Cl)c1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-787cbd4a712c4b168df30fdb5fe09b66
C=CC(=O)CC.COc1ccc2c(c1)CC(CCO)C2=O>>CCC(=O)CCC1(CCO)Cc2cc(OC)ccc2C1=O
OCCC1C(C2=CC=C(C=C2C1)OC)=O.C(=C)C(=O)CC.C[O-].[Na+]>>OCCC1(C(C2=CC=C(C=C2C1)OC)=O)CCC(CC)=O
[CH3:1][CH2:2][C:3](=[O:4])[CH:5]=[CH2:6].[CH:7]1([CH2:8][CH2:9][OH:10])[CH2:11][c:12]2[cH:13][c:14]([O:15][CH3:16])[cH:17][cH:18][c:19]2[C:20]1=[O:21]>>[CH3:1][CH2:2][C:3](=[O:4])[CH2:5][CH2:6][C:7]1([CH2:8][CH2:9][OH:10])[CH2:11][c:12]2[cH:13][c:14]([O:15][CH3:16])[cH:17][cH:18][c:19]2[C:20]1=[O:21]
C=CC(=O)CC.COc1ccc2c(c1)CC(CCO)C2=O
CCC(=O)CCC1(CCO)Cc2cc(OC)ccc2C1=O
null
null
CO.CCOC(=O)C
C-C Coupling
OtherReaction
c504c0d32586144b6874498db3cc99d4d5bb675e1b2e725385a0386d3f14ac05
68a0b2d4768a64505cf15a6dd6bbd75216aef3c50fb86aff9b39341b3e49f06d
O=C1CCc2ccccc21
[C:1]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:4]=[CH2;D1;+0:5].[C:6]-[C:7]-[CH;D3;+0:8]1-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]>>[C:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[C;H0;D4;+0:8]1(-[C:7]-[C:6])-[C:9]-[c:10]:[c:11]-[C:12]-1=[O;D1;H0:13]
93
[{"value": 93.0, "product": "OCCC1(C(C2=CC=C(C=C2C1)OC)=O)CCC(CC)=O", "details": "PERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
A solution of 2-(2-hydroxyethyl)-5-methoxy-1-indanone (105 mg, 0.51 mmol) in methanol (2.0 mL) at room temperature was treated with ethyl vinyl ketone (EVK, 0.102 mL) and 0.5M sodium methoxide in methanol (0.204 mL, 0.1 mmol). The mixture was stirred in a capped flask and heated in an oil bath at 60° C. for 8 hours. Af...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Vinyl
Ketone.Ketone
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
c1ccc2c(c1)CCC2
null
CO.CCOC(=O)C
60
null
C=CC(=O)CC.COc1ccc2c(c1)CC(CCO)C2=O>CO.CCOC(=O)C>CCC(=O)CCC1(CCO)Cc2cc(OC)ccc2C1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6ca20c97881a46a7b3a605c4a606073c
COc1ccc2c(c1)CC1(CCOS(C)(=O)=O)CCC(=O)C(C)=C21.[I-]>>COc1ccc2c(c1)CC1(CCI)CCC(=O)C(C)=C21
CS(=O)(=O)OCCC12CCC(C(=C1C=1C=CC(=CC1C2)OC)C)=O.[I-].[Na+]>>ICCC12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OC
CS(=O)(=O)O[CH2:12][CH2:11][C:10]12[CH2:9][c:7]3[c:6]([cH:5][cH:4][c:3]([O:2][CH3:1])[cH:8]3)[C:20]1=[C:18]([CH3:19])[C:16](=[O:17])[CH2:15][CH2:14]2.[I-:13]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][C:10]1([CH2:11][CH2:12][I:13])[CH2:14][CH2:15][C:16](=[O:17])[C:18]([CH3:19])=[C:20]21
COc1ccc2c(c1)CC1(CCOS(C)(=O)=O)CCC(=O)C(C)=C21.[I-]
COc1ccc2c(c1)CC1(CCI)CCC(=O)C(C)=C21
null
null
CC(=O)C
Functional Group Interconversion
OtherReaction
119410ad0456baafba3b2935b12d3e44977c506a6dd8cacdd3e4fe37abe9db9f
ddf832dd4937bef392b42ed4281006ae20524cc7fc61b350edeb12d7b5bf783f
O=C1C=C2c3ccccc3CC2CC1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]-[C:3]-[C:4]=[C:5].[I-;H0;D0:6]>>[C:5]=[C:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[I;H0;D1;+0:6]
64
[{"value": 64.0, "product": "ICCC12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.6, "product": "ICCC12CC3=CC(=CC=C3C2=C(C(CC1)=O)C)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
A solution of 2-(2-methoxy-5-methyl-6-oxo-6,7,8,9-tetrahydro-8aH-fluoren-8a-yl)ethyl methanesulfonate (49.7 mg, 0.142 mmol) in acetone (2.0 mL) was treated with sodium iodide (85 mg, 0.57 mmol) and the resulting mixture was stirred and heated in an oil bath at 60° C. for 16 hours. After cooling, the mixture was diluted...
10.6084/m9.figshare.5104873.v1
null
Mesylate
Primary halide
null
null
C1=C2c3ccccc3CC2CCC1
MsOH.HO-
CC(=O)C
60
null
COc1ccc2c(c1)CC1(CCOS(C)(=O)=O)CCC(=O)C(C)=C21.[I-]>CC(=O)C>COc1ccc2c(c1)CC1(CCI)CCC(=O)C(C)=C21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-bd4a17db7fd44b94ad9c395a089d4e4a
CCC(C)(C)C(=O)C(=O)N1CCC[C@H]1C(=O)O.NNc1ccccn1>>CCC(C)(C)C(=O)C(=O)N1CCCC1C(=O)NNc1ccccn1
O=C(C(C(CC)(C)C)=O)N1[C@@H](CCC1)C(=O)O.CCN(C(C)C)C(C)C.N(N)C1=NC=CC=C1.C1CCN(C1)[P+](N2CCCC2)(N3CCCC3)Br.F[P-](F)(F)(F)(F)F.COC([C@H]1NCCC1)=O>>N1=C(C=CC=C1)NNC(=O)C1N(CCC1)C(C(C(CC)(C)C)=O)=O
O[C:15]([C@H:14]1[N:10]([C:8]([C:6]([C:3]([CH2:2][CH3:1])([CH3:4])[CH3:5])=[O:7])=[O:9])[CH2:11][CH2:12][CH2:13]1)=[O:16].[NH2:17][NH:18][c:19]1[cH:20][cH:21][cH:22][cH:23][n:24]1>>[CH3:1][CH2:2][C:3]([CH3:4])([CH3:5])[C:6](=[O:7])[C:8](=[O:9])[N:10]1[CH2:11][CH2:12][CH2:13][CH:14]1[C:15](=[O:16])[NH:17][NH:18][c:19]1[...
CCC(C)(C)C(=O)C(=O)N1CCC[C@H]1C(=O)O.NNc1ccccn1
CCC(C)(C)C(=O)C(=O)N1CCCC1C(=O)NNc1ccccn1
null
CN(C)C=1C=CN=CC1
C1CCOC1.O.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
87776deec7c8d787307af11af64c4c1226af5b5e46e4fe8124762f384e2eebf3
82203b4f77b2f7d17908f28dcc1ecc7f616d152f963b273ffea1254f61a0fe2d
O=C(NNc1ccccn1)C1CCCN1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C@@H;D3;+0:3]1-[C:4]-[C:5]-[C:6]-[#7:7]-1-[C:8](=[O;D1;H0:9])-[C:10]=[O;D1;H0:11].[#7;a:12]:[c:13]-[#7:14]-[NH2;D1;+0:15]>>[#7;a:12]:[c:13]-[#7:14]-[NH;D2;+0:15]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3]1-[C:4]-[C:5]-[C:6]-[#7:7]-1-[C:8](=[O;D1;H0:9])-[C:10]=[O;D1;H0:11]
null
[]
null
null
24
HOUR
A mixture of (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidine-carboxylic acid (482 mg, 2 mmol), prepared from L-proline methyl ester according to the procedure described in WO 96/40633, 2-hydrazinopyridine (364 mg, 2 mmol), PyBrop (932 mg, 2 mmol), DMAP (4-dimethyaminopyridine, 122 mg) and DIEA (4 mL) in THF (dry, 5...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid
Acylhydrazine
null
null
C1CC[NH]C1.c1ccncc1
HO-
CN(C)C=1C=CN=CC1.C1CCOC1.O.C(C)(=O)OCC
null
24
CCC(C)(C)C(=O)C(=O)N1CCC[C@H]1C(=O)O.NNc1ccccn1>CN(C)C=1C=CN=CC1.C1CCOC1.O.C(C)(=O)OCC>CCC(C)(C)C(=O)C(=O)N1CCCC1C(=O)NNc1ccccn1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-46f3493837464fa1985f3dcce3aef5a5
COC(=O)C1CCCCN1C(=O)C(=O)c1cccs1>>O=C(C(=O)N1CCCCC1C(=O)O)c1cccs1
O=C(C(C=1SC=CC1)=O)N1C(CCCC1)C(=O)OC.[Li+].[OH-].Cl>>O=C(C(C=1SC=CC1)=O)N1C(CCCC1)C(=O)O
C[O:13][C:11]([CH:10]1[N:5]([C:3]([C:2](=[O:1])[c:14]2[cH:15][cH:16][cH:17][s:18]2)=[O:4])[CH2:6][CH2:7][CH2:8][CH2:9]1)=[O:12]>>[O:1]=[C:2]([C:3](=[O:4])[N:5]1[CH2:6][CH2:7][CH2:8][CH2:9][CH:10]1[C:11](=[O:12])[OH:13])[c:14]1[cH:15][cH:16][cH:17][s:18]1
COC(=O)C1CCCCN1C(=O)C(=O)c1cccs1
O=C(C(=O)N1CCCCC1C(=O)O)c1cccs1
null
null
CO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(C(=O)N1CCCCC1)c1cccs1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[#7:5]>>[#7:5]-[C:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
null
[]
null
null
16
HOUR
Intermediate 2 (2.45 g, 8.72 mmol) was dissolved in MeOH (50 mL). LiOH solution (1 N, 13 mL) was added at 0° C., and the mixture was stirred at the same temperature for 2 h and at room temperature for 16 h. The reaction mixture was acidified with 1 N HCl, and extracted with ethyl acetate. The organic phase was washed w...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1CC[NH]CC1.c1ccsc1
Other
CO
null
16
COC(=O)C1CCCCN1C(=O)C(=O)c1cccs1>CO>O=C(C(=O)N1CCCCC1C(=O)O)c1cccs1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-617a12e0035e4410b97f42be63d9aec7
Cc1cc(C(F)(F)F)cc(NN)n1.O=C(C(=O)N1CCCCC1C(=O)O)c1cccs1>>Cc1cc(C(F)(F)F)cc(NNC(=O)C2CCCCN2C(=O)C(=O)c2cccs2)n1
O=C(C(C=1SC=CC1)=O)N1C(CCCC1)C(=O)O.C1CCN(C1)[P+](N2CCCC2)(N3CCCC3)Br.F[P-](F)(F)(F)(F)F.CCN(C(C)C)C(C)C.N(N)C1=NC(=CC(=C1)C(F)(F)F)C>>CC1=CC(=CC(=N1)NNC(=O)C1N(CCCC1)C(C(C=1SC=CC1)=O)=O)C(F)(F)F
[CH3:1][c:2]1[cH:3][c:4]([C:5]([F:6])([F:7])[F:8])[cH:9][c:10]([NH:11][NH2:12])[n:30]1.O[C:13](=[O:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:19][N:20]1[C:21](=[O:22])[C:23](=[O:24])[c:25]1[cH:26][cH:27][cH:28][s:29]1>>[CH3:1][c:2]1[cH:3][c:4]([C:5]([F:6])([F:7])[F:8])[cH:9][c:10]([NH:11][NH:12][C:13](=[O:14])[CH:15]2[CH...
Cc1cc(C(F)(F)F)cc(NN)n1.O=C(C(=O)N1CCCCC1C(=O)O)c1cccs1
Cc1cc(C(F)(F)F)cc(NNC(=O)C2CCCCN2C(=O)C(=O)c2cccs2)n1
null
CN(C)C=1C=CN=CC1
C1CCOC1
Acylation
Carboxylic acid with primary amine to amide
87776deec7c8d787307af11af64c4c1226af5b5e46e4fe8124762f384e2eebf3
82203b4f77b2f7d17908f28dcc1ecc7f616d152f963b273ffea1254f61a0fe2d
O=C(C(=O)N1CCCCC1C(=O)NNc1ccccn1)c1cccs1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[C:8]=[O;D1;H0:9])-[C:10].[#7;a:11]:[c:12]-[#7:13]-[NH2;D1;+0:14]>>[#7;a:11]:[c:12]-[#7:13]-[NH;D2;+0:14]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[C:8]=[O;D1;H0:9])-[C:10]
null
[]
null
null
null
null
From Intermediate 3 (267 mg, 1 mmol), 2-hydrazino-6-methyl-4-trifluoromethylpyridine (191 mg, 1 mmol), PyBrop (466 mg, 1 mmol), DMAP (122 mg) and DIEA (2 mL) in THF (30 mL), using the same procedure for Compound 1, the title compound was obtained as a white solid; 110 mg (25%). MS (m/z) 441 (M+1). Conditions: See react...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Carboxylic acid
Acylhydrazine
null
null
c1ccncc1.C1CC[NH]CC1.c1ccsc1
HO-
CN(C)C=1C=CN=CC1.C1CCOC1
null
null
Cc1cc(C(F)(F)F)cc(NN)n1.O=C(C(=O)N1CCCCC1C(=O)O)c1cccs1>CN(C)C=1C=CN=CC1.C1CCOC1>Cc1cc(C(F)(F)F)cc(NNC(=O)C2CCCCN2C(=O)C(=O)c2cccs2)n1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-7d8656799d6241dcb7cc7ca2a9e1f1af
COC(=O)C1CCN1S(=O)(=O)Cc1ccccc1>>O=C(O)C1CCN1S(=O)(=O)Cc1ccccc1
COC(=O)C1N(CC1)S(=O)(=O)CC1=CC=CC=C1.[OH-].[Li+]>>C1(=CC=CC=C1)CS(=O)(=O)N1C(CC1)C(=O)O
C[O:3][C:2](=[O:1])[CH:4]1[CH2:5][CH2:6][N:7]1[S:8](=[O:9])(=[O:10])[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[O:1]=[C:2]([OH:3])[CH:4]1[CH2:5][CH2:6][N:7]1[S:8](=[O:9])(=[O:10])[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
COC(=O)C1CCN1S(=O)(=O)Cc1ccccc1
O=C(O)C1CCN1S(=O)(=O)Cc1ccccc1
null
null
CO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=S(=O)(Cc1ccccc1)N1CCC1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[C:4]-[#7:5]>>[#7:5]-[C:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
82,829.6
[{"value": 83.0, "product": "C1(=CC=CC=C1)CS(=O)(=O)N1C(CC1)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 82829.6, "product": "C1(=CC=CC=C1)CS(=O)(=O)N1C(CC1)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
1-Phenylmethanesulfonyl-azetidine-2-carboxylic acid methyl ester (1.13 g, 4.19 mmoles) was dissolved in methanol (20 mL) and cooled to 0° C. Treatment of this solution with aqueous lithium hydroxide (7.75 mL, 1 M) was followed by warming to ambient temperature over a 3 hour period. Most of the methanol was removed in v...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1C[NH]C1.c1ccccc1
Other
CO
0
null
COC(=O)C1CCN1S(=O)(=O)Cc1ccccc1>CO>O=C(O)C1CCN1S(=O)(=O)Cc1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-67afd482a98941bbb70354163e05eb94
Cc1ccc(C=O)cc1F>>Cc1ccc(C(C)O)cc1F
FC=1C=C(C=O)C=CC1C.C[Mg]Br.Cl>>OC(C)C1=CC(=C(C=C1)C)F
[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH:6]=[O:8])[cH:9][c:10]1[F:11]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH:6]([CH3:7])[OH:8])[cH:9][c:10]1[F:11]
Cc1ccc(C=O)cc1F
Cc1ccc(C(C)O)cc1F
null
null
C1CCOC1
Miscellaneous
OtherReaction
1ffaf80f172e20da969364a5d2977299bc51b204f2262675c45c8ec58ff36ac0
e005d650d08e61fc67b766830eb53235a9bc084cc3667d2f8a73c2fb8bb34277
c1ccccc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[C;D1;H3:6]-[CH;D3;+0:2](-[OH;D1;+0:1])-[c:3](:[c:4]):[c:5]
100.5
[{"value": 100.5, "product": "OC(C)C1=CC(=C(C=C1)C)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To an ice-cold solution of 3-fluoro-4-methylbenzaldehyde (50 mg, 0.36 mmol) in THF (0.5 mL) was added dropwise a 0.93 M solution (0.47 mL) of methylmagnesium bromide (0.44 mmol) in THF. The temperature of the reaction mixture was allowed to rise back to room temperature, at which the reaction mixture was stirred for 1 ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol
null
null
c1ccccc1
Other
C1CCOC1
null
1
Cc1ccc(C=O)cc1F>C1CCOC1>Cc1ccc(C(C)O)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0498ef0e78694a75a5377ea196575744
Cc1ccc(C(C)O)cc1F>>CC(=O)c1ccc(C)c(F)c1
OC(C)C1=CC(=C(C=C1)C)F.C=1C=C[NH+]=CC1.[O-][Cr](=O)(=O)Cl>>FC=1C=C(C=CC1C)C(C)=O
[CH3:1][CH:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([CH3:8])[c:9]([F:10])[cH:11]1>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([CH3:8])[c:9]([F:10])[cH:11]1
Cc1ccc(C(C)O)cc1F
CC(=O)c1ccc(C)c(F)c1
null
null
C(Cl)Cl
Oxidation
Oxidation or Dehydrogenation of Alcohols to Aldehydes and Ketones
c7c20d2959ac48847b03cc1265962cf99a8ec8a85900c087dabb30077298c66c
767cfd93f5821ebb9e1e72addd9cb404b20b0c821d246ae6b87a5776b74a455b
c1ccccc1
[C;D1;H3:1]-[CH;D3;+0:2](-[OH;D1;+0:3])-[c:4](:[c:5]):[c:6]>>[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[c:6]
86.7
[{"value": 86.0, "product": "FC=1C=C(C=CC1C)C(C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.7, "product": "FC=1C=C(C=CC1C)C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 4-(1-hydroxyethyl)-2-fluorotoluene (55.8 mg, 0.36 mmol) in methylene chloride (1 mL) were added molecular sieve 4A (56.0 mg) and PCC 94.0 mg (0.43 mmol), and the mixture was stirred at room temperature for 1 hour. The reaction mixture was filtered through Celite, and the filtrate was concentrated under...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ketone
null
null
c1ccccc1
null
C(Cl)Cl
null
1
Cc1ccc(C(C)O)cc1F>C(Cl)Cl>CC(=O)c1ccc(C)c(F)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-592233984b9b4dd7b002c45f0958065b
CC(=O)c1ccc(C)c(F)c1.CCOC(=O)C(=O)C(=O)OCC>>CCOC(=O)C(O)(CC(=O)c1ccc(C)c(F)c1)C(=O)OCC
FC=1C=C(C=CC1C)C(C)=O.O=C(C(=O)OCC)C(=O)OCC>>C(C)OC(=O)C(C(=O)OCC)(CC(=O)C1=CC(=C(C=C1)C)F)O
[CH3:8][C:9](=[O:10])[c:11]1[cH:12][cH:13][c:14]([CH3:15])[c:16]([F:17])[cH:18]1.[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[O:7])[C:19](=[O:20])[O:21][CH2:22][CH3:23]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]([OH:7])([CH2:8][C:9](=[O:10])[c:11]1[cH:12][cH:13][c:14]([CH3:15])[c:16]([F:17])[cH:18]1)[C:19](=[O:20])[O:21][CH2:22...
CC(=O)c1ccc(C)c(F)c1.CCOC(=O)C(=O)C(=O)OCC
CCOC(=O)C(O)(CC(=O)c1ccc(C)c(F)c1)C(=O)OCC
null
null
null
C-C Coupling
OtherReaction
e88a4a7d8d6b5dee5ec6739bba985b00a792654307585b505d721a6c4424a1e7
622d9e177646f51219fadf1ea3ee007cb7d9c42cff173da68f5fdf3c13916e74
c1ccccc1
[CH3;D1;+0:1]-[C:2](=[O;D1;H0:3])-[c:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C;H0;D3;+0:9](=[O;H0;D1;+0:10])-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]>>[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C;H0;D4;+0:9](-[OH;D1;+0:10])(-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4])-[C:11](=[O;D1;H0:12])-[#8:13]-[C:14]
79.3
[{"value": 79.3, "product": "C(C)OC(=O)C(C(=O)OCC)(CC(=O)C1=CC(=C(C=C1)C)F)O", "details": "PERCENTYIELD", "is_desired": false}]
120
CELSIUS
48
HOUR
A mixture of 3′-fluoro-4′-methylacetophenone (4.92 g, 32.3 mmol) and diethyl ketomalonate (6.19 g, 35.6 mmol) was stirred at 120° C. for 48 hours. The temperature of the reaction mixture was allowed to drop back to room temperature, and the mixture was purified by column chromatography on silica gel [silica gel 100 g, ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone
Ketone.Ester.Ester.Tertiary alcohol
null
null
c1ccccc1
null
null
120
48
CC(=O)c1ccc(C)c(F)c1.CCOC(=O)C(=O)C(=O)OCC>>CCOC(=O)C(O)(CC(=O)c1ccc(C)c(F)c1)C(=O)OCC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e9eae8e4020a414d90a4fd0e994de72c
CCOC(=O)C(O)(CC(=O)c1ccc(C)c(F)c1)C(=O)OCC.NN>>Cc1ccc(-c2cc(C(=O)O)c(=O)[nH]n2)cc1F
[OH-].[Na+].C(C)OC(=O)C(C(=O)OCC)(CC(=O)C1=CC(=C(C=C1)C)F)O.O.NN.Cl>>C(=O)(O)C=1C(NN=C(C1)C1=CC(=C(C=C1)C)F)=O
CCO[C:12]([C:8](O)([CH2:7][C:6](=O)[c:5]1[cH:4][cH:3][c:2]([CH3:1])[c:17]([F:18])[cH:16]1)[C:9](=[O:10])[O:11]CC)=[O:13].[NH2:14][NH2:15]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8]([C:9](=[O:10])[OH:11])[c:12](=[O:13])[nH:14][n:15]2)[cH:16][c:17]1[F:18]
CCOC(=O)C(O)(CC(=O)c1ccc(C)c(F)c1)C(=O)OCC.NN
Cc1ccc(-c2cc(C(=O)O)c(=O)[nH]n2)cc1F
null
null
C(C)(C)O
Aromatic Heterocycle Formation
OtherReaction
ebc1b4166a3a2c5ebd997173df1a8f4786085ddbe534c5ee805b61ad55c292e1
f0716b7f64b3a238ee9f3d2ce4fc900dee4f01e88461c96dbe61fcf07f5faeb5
O=c1ccc(-c2ccccc2)n[nH]1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C;H0;D4;+0:3](-O)(-[CH2;D2;+0:4]-[C;H0;D3;+0:5](=O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10])-[C:11](=[O;D1;H0:12])-[O;H0;D2;+0:13]-C-C.[NH2;D1;+0:14]-[NH2;D1;+0:15]>>[O;D1;H0:12]=[C:11](-[OH;D1;+0:13])-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:...
87.7
[{"value": 87.7, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
6
HOUR
To a solution of ethyl 2-ethoxycarbonyl-4-(3-fluoro-4-methylphenyl)-2-hydroxy-4-oxobutanoate (8.41 9, 25.8 mmol) in isopropanol (100 mL) was added hydrazine monohydrate (2.84 g, 56.8 mmol), and the mixture was heated under stirring at 100 for 6 hours. Then, 2 mol/L sodium hydroxide was added, and the mixture was stirre...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Ester.Ester.Tertiary alcohol
Carboxylic acid
null
c1cnncc1
c1ccccc1.c1cnncc1
HO-
C(C)(C)O
null
6
CCOC(=O)C(O)(CC(=O)c1ccc(C)c(F)c1)C(=O)OCC.NN>C(C)(C)O>Cc1ccc(-c2cc(C(=O)O)c(=O)[nH]n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-447057a76e4c472e8ee185e270a27f68
CC(C)CBr.COC(=O)c1cc(-c2ccc(C)c(F)c2)n[nH]c1=O>>COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O
C(O)([O-])=O.[Na+].FC=1C=C(C=CC1C)C=1C=C(C(NN1)=O)C(=O)OC.C([O-])([O-])=O.[K+].[K+].C(C(C)C)Br>>FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)C(=O)OC
Br[CH2:18][CH:19]([CH3:20])[CH3:21].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]([CH3:12])[c:13]([F:14])[cH:15]2)[n:16][nH:17][c:22]1=[O:23]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][c:11]([CH3:12])[c:13]([F:14])[cH:15]2)[n:16][n:17]([CH2:18][CH:19]([CH3:20])[CH3:21])[c:2...
CC(C)CBr.COC(=O)c1cc(-c2ccc(C)c(F)c2)n[nH]c1=O
COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
456217c8bdd4490079dbc0339e1b1eedc560d0b24ec9d54c4ed1fbd8e71fb3dc
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1ccc(-c2ccccc2)n[nH]1
Br-[CH2;D2;+0:1]-[C:2](-[C;D1;H3:3])-[C;D1;H3:4].[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](=[O;D1;H0:10]):[nH;D2;+0:11]:[#7;a:12]:[c:13]>>[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](=[O;D1;H0:10]):[n;H0;D3;+0:11](-[CH2;D2;+0:1]-[C:2](-[C;D1;H3:3])-[C;D1;H3:4]):[#7;a:12]:[c:13]
85
[{"value": 84.9, "product": "FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.0, "product": "FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
1
HOUR
To a solution of 6-(3-fluoro-4-methylphenyl)-4-methoxycarbonyl-2H-pyridazin-3-one (5.28 g, 20.0 mmol) in N,N-dimethylformamide (40 mL) were added potassium carbonate (5.53 g, 40.0 mmol) and isobutyl bromide (3.29 g, 24.0 mmol), and the mixture was stirred at 80° C. for 1 hour. The temperature of the reaction mixture wa...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cnncc1
c1ccnnc1
c1ccnnc1.c1ccccc1
HBr
CN(C=O)C
80
1
CC(C)CBr.COC(=O)c1cc(-c2ccc(C)c(F)c2)n[nH]c1=O>CN(C=O)C>COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ab1294f86fcd4655a65edddcfbdbb4bc
COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O>>Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F
Cl.[OH-].[Na+].FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)C(=O)OC.O>>C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O
C[O:11][C:9]([c:8]1[cH:7][c:6](-[c:5]2[cH:4][cH:3][c:2]([CH3:1])[c:21]([F:22])[cH:20]2)[n:19][n:14]([CH2:15][CH:16]([CH3:17])[CH3:18])[c:12]1=[O:13])=[O:10]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8]([C:9](=[O:10])[OH:11])[c:12](=[O:13])[n:14]([CH2:15][CH:16]([CH3:17])[CH3:18])[n:19]2)[cH:20][c:21]1[F:22]
COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O
Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F
null
null
CO
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1ccc(-c2ccccc2)n[nH]1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[c:5]:[#7;a:6]>>[#7;a:6]:[c:5]:[c:4]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
93.8
[{"value": 93.8, "product": "C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.6, "product": "C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
15
MINUTE
To a suspension of 6-(3-fluoro-4-methylphenyl)-2-isobutyl-4-methoxycarbonyl-2H-pyridazin-3-one (5.27 g, 16.6 mmol) in methanol (50 mL) was added a 2 mol/L aqueous sodium hydroxide (50 mL), and the mixture was stirred at 60° C. for 15 minutes. The temperature of the reaction mixture was allowed to drop back to room temp...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1.c1ccnnc1
Other
CO
60
0.25
COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O>CO>Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d75da831e89b460095cd01caa65390ca
Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F>>Cc1ccc(-c2nn(CC(C)C)c(=O)c(O)c2C)cc1F
C(OCC)(=O)Cl.C1CCOC1.Cl.[BH4-].[Na+].C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O.C(C)N(CC)CC.C1CCOC1>>FC=1C=C(C=CC1C)C=1C(=C(C(N(N1)CC(C)C)=O)O)C
O=[C:18]([c:15]1[c:13](=[O:14])[n:8]([CH2:9][CH:10]([CH3:11])[CH3:12])[n:7][c:6](-[c:5]2[cH:4][cH:3][c:2]([CH3:1])[c:20]([F:21])[cH:19]2)[cH:17]1)[OH:16]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][n:8]([CH2:9][CH:10]([CH3:11])[CH3:12])[c:13](=[O:14])[c:15]([OH:16])[c:17]2[CH3:18])[cH:19][c:20]1[F:21]
Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F
Cc1ccc(-c2nn(CC(C)C)c(=O)c(O)c2C)cc1F
null
null
O
Miscellaneous
OtherReaction
50b37df3879a3cb84a59a03d9c916437bc7d466fe1499b85b20332fbfc13cc6a
9b981ffa1dc2208a196fed475e723ee668e37655a0b8fbe764684c618ae17839
O=c1ccc(-c2ccccc2)n[nH]1
O=[C;H0;D3;+0:1](-[OH;D1;+0:2])-[c;H0;D3;+0:3]1:[cH;D2;+0:4]:[c:5](-[c:6]):[#7;a:7]:[#7;a:8](-[C:9]):[c:10]:1=[O;D1;H0:11]>>[C:9]-[#7;a:8]1:[#7;a:7]:[c:5](-[c:6]):[c;H0;D3;+0:4](-[CH3;D1;+0:1]):[c;H0;D3;+0:3](-[OH;D1;+0:2]):[c:10]:1=[O;D1;H0:11]
25
[{"value": 25.0, "product": "FC=1C=C(C=CC1C)C=1C(=C(C(N(N1)CC(C)C)=O)O)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 4-carboxy-6-(3-fluoro-4-methyl-phenyl)-2-isobutyl-2H-pyridazin-3-one (4.53 g, 14.9 mmol) in THF (40 mL) was added triethylamine (1.66 g, 16.4 mmol). To the ice-cooled mixture was added dropwise a solution of ethyl chlorocarbonate (1.78 g, 16.4 mmol) in THF (5 mL), and the mixture was stirred for 30 min...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Aromatic alcohol
c1ccnnc1
c1ccnnc1
c1ccccc1.c1ccnnc1
Other
O
null
0.5
Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F>O>Cc1ccc(-c2nn(CC(C)C)c(=O)c(O)c2C)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-545ec692753a43dfb8f282d8b901e30d
CS(=O)(=O)Cl.Cc1ccc(-c2cc(CO)c(=O)n(CC(C)C)n2)cc1F>>Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F
FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)CO.C(C)N(CC)CC.CS(=O)(=O)Cl.C(O)([O-])=O.[Na+]>>FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)COS(=O)(=O)C
Cl[S:11]([CH3:12])(=[O:13])=[O:14].[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8]([CH2:9][OH:10])[c:15](=[O:16])[n:17]([CH2:18][CH:19]([CH3:20])[CH3:21])[n:22]2)[cH:23][c:24]1[F:25]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8]([CH2:9][O:10][S:11]([CH3:12])(=[O:13])=[O:14])[c:15](=[O:16])[n:17]([CH2:18][CH:19](...
CS(=O)(=O)Cl.Cc1ccc(-c2cc(CO)c(=O)n(CC(C)C)n2)cc1F
Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F
null
null
C(Cl)Cl
Acylation
Formation of Sulfonic Esters
2fa969eb2c954bb96793348a1b2335ec63fbd290dadec6e3e02295e1768e64cf
cb77b899e4adf980b1def97230ef2861660fd7f9602260ec64747d9afd3a795a
O=c1ccc(-c2ccccc2)n[nH]1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[#7;a:5]:[c:6]:[c:7]-[C:8]-[OH;D1;+0:9]>>[#7;a:5]:[c:6]:[c:7]-[C:8]-[O;H0;D2;+0:9]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]
70.4
[{"value": 70.4, "product": "FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)COS(=O)(=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.1, "product": "FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)COS(=O)(=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To an ice-cold solution of 6-(3-fluoro-4-methyl-phenyl)-4-hydroxymethyl-2-isobutyl-2H-pyridazin-3-one (1.08 g, 3.73 mmol) in methylene chloride (20 mL) were added triethylamine (491 mg, 4.85 mmol) and methanesulfonyl chloride (513 mg, 4.48 mmol), and the mixture was stirred for 1 hour. A saturated aqueous solution of s...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Mesylate
null
null
c1ccccc1.c1ccnnc1
HCl
C(Cl)Cl
null
1
CS(=O)(=O)Cl.Cc1ccc(-c2cc(CO)c(=O)n(CC(C)C)n2)cc1F>C(Cl)Cl>Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-fe9e652ae9ab4faca893097b8edf8b1c
CC(C)(C)OC(=O)N1CCNCC1.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F>>Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F
O.FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)COS(=O)(=O)C.C([O-])([O-])=O.[K+].[K+].N1(CCNCC1)C(=O)OC(C)(C)C>>C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O
[NH:16]1[CH2:17][CH2:18][N:19]([C:20](=[O:21])[O:22][C:23]([CH3:24])([CH3:25])[CH3:26])[CH2:27][CH2:28]1.CS(=O)(=O)O[CH2:30][c:15]1[c:13](=[O:14])[n:8]([CH2:9][CH:10]([CH3:11])[CH3:12])[n:7][c:6](-[c:5]2[cH:4][cH:3][c:2]([CH3:1])[c:32]([F:33])[cH:31]2)[cH:29]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][n:8]([CH2:9][C...
CC(C)(C)OC(=O)N1CCNCC1.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F
Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
20463218c281e2c61bf0173d651b213ee8033fd2ccbdfc94848e31db5e0e51b8
35d789812c3241c3a185d06663a309d930259e30563212f3884ef74718436cbc
O=c1[nH]nc(-c2ccccc2)cc1N1CCNCC1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[c:4](-[c:5]):[#7;a:6]:[#7;a:7](-[C:8]):[c:9]:1=[O;D1;H0:10].[#7:11]1-[C:12]-[C:13]-[NH;D2;+0:14]-[C:15]-[C:16]-1>>[C:8]-[#7;a:7]1:[#7;a:6]:[c:4](-[c:5]):[c;H0;D3;+0:3](-[CH3;D1;+0:1]):[c;H0;D3;+0:2](-[N;H0;D3;+0:14]2-[C:13]-[C:12]-[#7:11]-[C:16]-[C:15]-2):[c:9]:...
92.9
[{"value": 92.4, "product": "C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.9, "product": "C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
2
HOUR
To a solution of 6-(3-fluoro-4-methylphenyl)-2-isobutyl-4-methanesulfonyloxy methyl-2H-pyridazin-3-one (100 mg, 0.27 mmol) in acetonitrile (1 mL) were added potassium carbonate (56.3 mg, 0.41 mmol) and tert-butyl 1-piperazine-carboxylate (60.7 mg, 0.33 mmol), and the mixture was stirred at 80° C. for 2 hours. The tempe...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Secondary amine
Tertiary amine
C1CNCC[NH]1.c1ccnnc1
c1ccnnc1.C1C[NH]CC[NH]1
c1ccccc1.c1ccnnc1.C1C[NH]CC[NH]1
MsOH.HO-
C(C)#N
80
2
CC(C)(C)OC(=O)N1CCNCC1.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F>C(C)#N>Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-255e4d7378f140328c7e6ec5faa61ba2
Cc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC(C)C)n2)cc1F>>Cc1ccc(-c2cc(CN3CCNCC3)c(=O)n(CC(C)C)n2)cc1F.Cl
C(C)OCC.C(C)(C)(C)OC(=O)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O.Cl>>Cl.Cl.FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)CN1CCNCC1
CC(C)(C)OC(=O)[N:13]1[CH2:12][CH2:11][N:10]([CH2:9][c:8]2[cH:7][c:6](-[c:5]3[cH:4][cH:3][c:2]([CH3:1])[c:25]([F:26])[cH:24]3)[n:23][n:18]([CH2:19][CH:20]([CH3:21])[CH3:22])[c:16]2=[O:17])[CH2:15][CH2:14]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8]([CH2:9][N:10]3[CH2:11][CH2:12][NH:13][CH2:14][CH2:15]3)[c:16](=[...
Cc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC(C)C)n2)cc1F
Cc1ccc(-c2cc(CN3CCNCC3)c(=O)n(CC(C)C)n2)cc1F.Cl
null
null
C(C)(=O)OCC
Miscellaneous
Boc amine deprotection
ca9288c3be1743ea424604bf62770990eec893f8f7f07c612f680fef8b15531e
c95e79e18f8ea11cf22745e0eab38cab98566b1b63e7d80ee200f4cb4f94f00c
O=c1[nH]nc(-c2ccccc2)cc1CN1CCNCC1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-[C:6]-1>>[#7:4]1-[C:3]-[C:2]-[NH;D2;+0:1]-[C:6]-[C:5]-1
75
[{"value": 75.0, "product": "Cl.Cl.FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)CN1CCNCC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 4-(4-tert-butoxycarbonyl-1-piperazinyl)methyl-6-(3-fluoro-4-methylphenyl)-2-isobutyl-2H-pyridazin-3-one (115 mg, 0.25 mmol) in ethyl acetate (2 mL) was added a 4 mol/L solution (2 mL) of hydrochloric acid in ethyl acetate, and the mixture was stirred at 50 for 1 hour. The temperature of the reaction mi...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
C1C[NH]CC[NH]1
C1C[NH]CCN1
c1ccccc1.c1ccnnc1.C1C[NH]CCN1
HO-
C(C)(=O)OCC
null
1
Cc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC(C)C)n2)cc1F>C(C)(=O)OCC>Cc1ccc(-c2cc(CN3CCNCC3)c(=O)n(CC(C)C)n2)cc1F.Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-409e1ee3b5d24cd29adbd3d222778aab
Cl>>Cl.Cl
Cl.FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)CN1CCN(CC1)C>>Cl.Cl.FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)CN1CCN(CC1)C
[ClH:28]>>[ClH:28].[ClH:29]
Cl
Cl.Cl
null
null
CO.C(C)(=O)OCC
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
63.7
[{"value": 63.7, "product": "Cl.Cl.FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)CN1CCN(CC1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 6-(3-fluoro-4-methylphenyl)-2-isobutyl-4-(4-methyl-1-piperazinyl)methyl-2H-pyridazin-3-one (94.4 mg, 0.25 mmol) in methanol (1 mL) was added dropwise at room temperature under stirring a 4 mol/L solution (0.15 mL) of hydrochloric acid in ethyl acetate. The solvent was distilled off under reduced pressu...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
CO.C(C)(=O)OCC
null
null
Cl>CO.C(C)(=O)OCC>Cl.Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9f4fc513dafa4ea6aad188ea8bbf6697
CNC.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F>>Cc1ccc(-c2cc(CN(C)C)c(=O)n(CC(C)C)n2)cc1F
FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)COS(=O)(=O)C.CNC>>CN(C)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O
[NH:10]([CH3:11])[CH3:12].CS(=O)(=O)O[CH2:9][c:8]1[cH:7][c:6](-[c:5]2[cH:4][cH:3][c:2]([CH3:1])[c:22]([F:23])[cH:21]2)[n:20][n:15]([CH2:16][CH:17]([CH3:18])[CH3:19])[c:13]1=[O:14]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][c:8]([CH2:9][N:10]([CH3:11])[CH3:12])[c:13](=[O:14])[n:15]([CH2:16][CH:17]([CH3:18])[CH3:19])[...
CNC.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F
Cc1ccc(-c2cc(CN(C)C)c(=O)n(CC(C)C)n2)cc1F
null
null
O
Heteroatom Alkylation and Arylation
Alkylation of amines
ba24696731c43f94422863463da0ee528bfb8ec715fd228fe0a6c2ae67b49c25
35d789812c3241c3a185d06663a309d930259e30563212f3884ef74718436cbc
O=c1ccc(-c2ccccc2)n[nH]1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[#7;a:6](-[C:7]):[c:8]:1=[O;D1;H0:9].[C;D1;H3:10]-[NH;D2;+0:11]-[C;D1;H3:12]>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:11](-[C;D1;H3:10])-[C;D1;H3:12]):[c:8]:1=[O;D1;H0:9]
80.9
[{"value": 80.9, "product": "CN(C)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
2
HOUR
To 6-(3-fluoro-4-methylphenyl)-2-isobutyl-4-methane-sulfonyloxymethyl-2H-pyridazin-3-one (100 mg, 0.27 mmol) was added a 40% aqueous dimethylamine (1 mL), and the mixture was stirred at 80° C. for 2 hours. The temperature of the reaction mixture was allowed to drop back to room temperature, and then, water was added. T...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Secondary amine
Tertiary amine
null
null
c1ccccc1.c1ccnnc1
MsOH.HO-
O
80
2
CNC.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F>O>Cc1ccc(-c2cc(CN(C)C)c(=O)n(CC(C)C)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c710a98177e24ecea9f95a6057b7ad14
COc1ccc(C2=NN(CC3CC3)C(=O)C(OC)C2=C=O)cc1F.Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F>>COc1ccc(-c2cc(C(=O)O)c(=O)n(CC3CC3)n2)cc1F
C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)C)F)CC(C)C)=O.C1(CC1)CN1N=C(C(C(C1=O)OC)=C=O)C1=CC(=C(C=C1)OC)F>>C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O
COC1C(=O)N(C[CH:17]2[CH2:18][CH2:19]2)N=C([c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:22]([F:23])[cH:21]2)C1=C=O.Cc1ccc(-[c:7]2[cH:8][c:9]([C:10](=[O:11])[OH:12])[c:13](=[O:14])[n:15]([CH2:16]C(C)C)[n:20]2)cc1F>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([C:10](=[O:11])[OH:12])[c:13](=[O:14])[n:15]([CH2:16][CH:...
COc1ccc(C2=NN(CC3CC3)C(=O)C(OC)C2=C=O)cc1F.Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F
COc1ccc(-c2cc(C(=O)O)c(=O)n(CC3CC3)n2)cc1F
null
null
null
C-C Coupling
OtherReaction
1baeab77a2d9456e7a32be1a7498dec1a8014ae556d713c79bcb77b4e4e75090
017f711087a5cfc6cbc30665004ce603e128db6c57513baa4a730b058257fb7c
O=c1ccc(-c2ccccc2)nn1CC1CC1
C-C(-C)-[CH2;D2;+0:1]-[#7;a:2]1:[#7;a:3]:[c;H0;D3;+0:4](-c2:c:c:c(-C):c(-F):c:2):[c:5]:[c:6](-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]):[c:10]:1.C-O-C1-C(=O)-N(-C-[CH;D3;+0:11]2-[C:12]-[C:13]-2)-N=C(-[c;H0;D3;+0:14](:[c:15]:[c:16]):[c:17]:[c:18])-C-1=C=O>>[O;D1;H0:8]=[C:7](-[O;D1;H1:9])-[c:6]1:[c:10]:[#7;a:2](-[CH2;D2;+0:1]-[CH...
98.9
[{"value": 98.9, "product": "C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (7), 2-cyclo-propylmethyl-6-(3-fluoro-4-methoxyphenyl)-4-methoxy-carbonyl-2H-pyridazin-3-one was reacted to yield the title compound as yellow crystals (yield: 98.9%). Conditions: See reaction.notes.procedure_details. Workup: was reacted
10.6084/m9.figshare.5104873.v1
null
Hydrazone amide.Aromatic halide.Ether
null
C1=NNCCC1.C1CC1.c1ccccc1.c1ccccc1.c1ccnnc1
c1ccccc1.c1ccnnc1.C1CC1
c1ccccc1.c1ccnnc1.C1CC1
HF
null
null
null
COc1ccc(C2=NN(CC3CC3)C(=O)C(OC)C2=C=O)cc1F.Cc1ccc(-c2cc(C(=O)O)c(=O)n(CC(C)C)n2)cc1F>>COc1ccc(-c2cc(C(=O)O)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-29d215b07747424baa326c57ae8e04df
COc1ccc(-c2cc(C(=O)O)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CO)c(=O)n(CC3CC3)n2)cc1F
FC=1C=C(C=CC1C)C=1C(=C(C(N(N1)CC(C)C)=O)O)C.C(=O)(O)C=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O>>C1(CC1)CN1N=C(C=C(C1=O)CO)C1=CC(=C(C=C1)OC)F
O=[C:10]([c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:21]([F:22])[cH:20]2)[n:19][n:14]([CH2:15][CH:16]2[CH2:17][CH2:18]2)[c:12]1=[O:13])[OH:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH2:10][OH:11])[c:12](=[O:13])[n:14]([CH2:15][CH:16]3[CH2:17][CH2:18]3)[n:19]2)[cH:20][c:21]1[F:22]
COc1ccc(-c2cc(C(=O)O)c(=O)n(CC3CC3)n2)cc1F
COc1ccc(-c2cc(CO)c(=O)n(CC3CC3)n2)cc1F
null
null
null
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
O=c1ccc(-c2ccccc2)nn1CC1CC1
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[c:3]1:[c:4]:[c:5]:[#7;a:6]:[#7;a:7](-[C:8]):[c:9]:1=[O;D1;H0:10]>>[C:8]-[#7;a:7]1:[#7;a:6]:[c:5]:[c:4]:[c:3](-[CH2;D2;+0:1]-[O;D1;H1:2]):[c:9]:1=[O;D1;H0:10]
21.3
[{"value": 21.3, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (8), 4-carboxy-2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl)-2H-pyridazin-3-one was reacted to yield the title compound as slightly yellow fine-needles (yield: 21.3%). Conditions: See reaction.notes.procedure_details. Workup: was reacted
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccccc1.c1ccnnc1.C1CC1
Other
null
null
null
COc1ccc(-c2cc(C(=O)O)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CO)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-24caefb412d641299dc0356bb3b2eb83
COc1ccc(-c2cc(CO)c(=O)n(CC3CC3)n2)cc1F.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F>>COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F
FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)COS(=O)(=O)C.C1(CC1)CN1N=C(C=C(C1=O)CO)C1=CC(=C(C=C1)OC)F>>C1(CC1)CN1N=C(C=C(C1=O)COS(=O)(=O)C)C1=CC(=C(C=C1)OC)F
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH2:10][OH:11])[c:16](=[O:17])[n:18]([CH2:19][CH:20]3[CH2:21][CH2:22]3)[n:23]2)[cH:24][c:25]1[F:26].Cc1ccc(-c2cc(CO[S:12]([CH3:13])(=[O:14])=[O:15])c(=O)n(CC(C)C)n2)cc1F>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH2:10][O:11][S:12]([CH3:13])(=[O:14]...
COc1ccc(-c2cc(CO)c(=O)n(CC3CC3)n2)cc1F.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F
COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F
null
null
null
Functional Group Interconversion
OtherReaction
8b0e3d7bee01c1cd08d5b9300989bcd9434e06e13b2628e4e267ebe847060d81
91ea60d6fa98857424dec1beabf111ed8901abdf48d6e9b2323a22e8ccca105d
O=c1ccc(-c2ccccc2)nn1CC1CC1
C-C(-C)-C-n1:n:c(-c2:c:c:c(-C):c(-F):c:2):c:c(-C-O-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]):c:1=O.[#7;a:5]:[c:6]:[c:7]-[C:8]-[OH;D1;+0:9]>>[#7;a:5]:[c:6]:[c:7]-[C:8]-[O;H0;D2;+0:9]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]
80.4
[{"value": 80.4, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (9), 2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl) -4-hydroxymethyl-2H-pyridazin-3-one was reacted to yield the title compound as slightly yellow needles (yield: 80.4%). Conditions: See reaction.notes.procedure_details. Workup: was reacted
10.6084/m9.figshare.5104873.v1
null
Mesylate.Aromatic halide.Primary alcohol
Mesylate
c1ccccc1.c1ccnnc1
null
c1ccccc1.c1ccnnc1.C1CC1
HF
null
null
null
COc1ccc(-c2cc(CO)c(=O)n(CC3CC3)n2)cc1F.Cc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC(C)C)n2)cc1F>>COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b6888d75665f483bbf89bb734af68f01
CN.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F>>CNCc1cc(-c2ccc(OC)c(F)c2)nn(CC2CC2)c1=O
C1(CC1)CN1N=C(C=C(C1=O)COS(=O)(=O)C)C1=CC(=C(C=C1)OC)F.CN.C(C)O>>C1(CC1)CN1N=C(C=C(C1=O)CNC)C1=CC(=C(C=C1)OC)F
[CH3:1][NH2:2].CS(=O)(=O)O[CH2:3][c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([O:11][CH3:12])[c:13]([F:14])[cH:15]2)[n:16][n:17]([CH2:18][CH:19]2[CH2:20][CH2:21]2)[c:22]1=[O:23]>>[CH3:1][NH:2][CH2:3][c:4]1[cH:5][c:6](-[c:7]2[cH:8][cH:9][c:10]([O:11][CH3:12])[c:13]([F:14])[cH:15]2)[n:16][n:17]([CH2:18][CH:19]2[CH2:20][CH...
CN.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F
CNCc1cc(-c2ccc(OC)c(F)c2)nn(CC2CC2)c1=O
null
null
null
Heteroatom Alkylation and Arylation
Alkylation of amines
8445343b2fb2fd8a9bc06f8532794f2ba6b99565a6e05a3bb9a4344ce2671186
7e6303acde8be57b43b4c6a673e1c7537b1efde90f08932e09e153dbba53a700
O=c1ccc(-c2ccccc2)nn1CC1CC1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[#7;a:6](-[C:7]):[c:8]:1=[O;D1;H0:9].[C;D1;H3:10]-[NH2;D1;+0:11]>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2](-[CH2;D2;+0:1]-[NH;D2;+0:11]-[C;D1;H3:10]):[c:8]:1=[O;D1;H0:9]
65.5
[{"value": 65.5, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl)-4-methanesulfonyloxymethyl-2H-pyridazin-3-one (160 mg, 0.42 mmol) in 30% methylamine/ethanol (5 mL) was stirred at 80° C. for 4 hours in a sealed tube. The solvent was distilled off under reduced pressure, and the residue was purified by preparative thin-la...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Primary amine
Secondary amine
null
null
c1ccnnc1.c1ccccc1.C1CC1
MsOH.HO-
null
null
null
CN.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F>>CNCc1cc(-c2ccc(OC)c(F)c2)nn(CC2CC2)c1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-af59a80c4f7f4dd69a14246df32e874b
CN1CCNCC1.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CN3CCN(C)CC3)c(=O)n(CC3CC3)n2)cc1F
C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O.C1(CC1)CN1N=C(C=C(C1=O)COS(=O)(=O)C)C1=CC(=C(C=C1)OC)F.CN1CCNCC1>>C1(CC1)CN1N=C(C=C(C1=O)CN1CCN(CC1)C)C1=CC(=C(C=C1)OC)F
[NH:11]1[CH2:12][CH2:13][N:14]([CH3:15])[CH2:16][CH2:17]1.CS(=O)(=O)O[CH2:10][c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:27]([F:28])[cH:26]2)[n:25][n:20]([CH2:21][CH:22]2[CH2:23][CH2:24]2)[c:18]1=[O:19]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH2:10][N:11]3[CH2:12][CH2:13][N:14]([CH3:15]...
CN1CCNCC1.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F
COc1ccc(-c2cc(CN3CCN(C)CC3)c(=O)n(CC3CC3)n2)cc1F
null
null
null
Heteroatom Alkylation and Arylation
Alkylation of amines
bc40e881c80f733cc18ae6a4c32c0d2e3ac9ce7b07d3a2cb609684e869dc6007
35d789812c3241c3a185d06663a309d930259e30563212f3884ef74718436cbc
O=c1c(CN2CCNCC2)cc(-c2ccccc2)nn1CC1CC1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[#7;a:6](-[C:7]):[c:8]:1=[O;D1;H0:9].[#7:10]1-[C:11]-[C:12]-[NH;D2;+0:13]-[C:14]-[C:15]-1>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:13]2-[C:12]-[C:11]-[#7:10]-[C:15]-[C:14]-2):[c:8]:1=[O;D1;H0:9]
73.8
[{"value": 73.8, "product": "C1(CC1)CN1N=C(C=C(C1=O)CN1CCN(CC1)C)C1=CC(=C(C=C1)OC)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (10), 2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl)-4-methanesulfonyloxymethyl-2H-pyridazin-3-one and 1-methylpiperazine were reacted to yield the title compound as a yellow oil (yield: 73.8%). Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Mesylate.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.c1ccnnc1.C1C[NH]CC[NH]1.C1CC1
MsOH.HO-
null
null
null
CN1CCNCC1.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CN3CCN(C)CC3)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-bfd306210c44435dac7c631e7d34723f
COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F.c1ccc(CN2CCNCC2)cc1>>COc1ccc(-c2cc(CN3CCN(Cc4ccccc4)CC3)c(=O)n(CC3CC3)n2)cc1F
C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O.C1(CC1)CN1N=C(C=C(C1=O)COS(=O)(=O)C)C1=CC(=C(C=C1)OC)F.C(C1=CC=CC=C1)N1CCNCC1>>C(C1=CC=CC=C1)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O
CS(=O)(=O)O[CH2:10][c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:33]([F:34])[cH:32]2)[n:31][n:26]([CH2:27][CH:28]2[CH2:29][CH2:30]2)[c:24]1=[O:25].[NH:11]1[CH2:12][CH2:13][N:14]([CH2:15][c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[CH2:22][CH2:23]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH...
COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F.c1ccc(CN2CCNCC2)cc1
COc1ccc(-c2cc(CN3CCN(Cc4ccccc4)CC3)c(=O)n(CC3CC3)n2)cc1F
null
null
null
Heteroatom Alkylation and Arylation
Alkylation of amines
bc40e881c80f733cc18ae6a4c32c0d2e3ac9ce7b07d3a2cb609684e869dc6007
35d789812c3241c3a185d06663a309d930259e30563212f3884ef74718436cbc
O=c1c(CN2CCN(Cc3ccccc3)CC2)cc(-c2ccccc2)nn1CC1CC1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[#7;a:6](-[C:7]):[c:8]:1=[O;D1;H0:9].[#7:10]1-[C:11]-[C:12]-[NH;D2;+0:13]-[C:14]-[C:15]-1>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:13]2-[C:12]-[C:11]-[#7:10]-[C:15]-[C:14]-2):[c:8]:1=[O;D1;H0:9]
97.7
[{"value": 97.7, "product": "C(C1=CC=CC=C1)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (10), 2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl)-4-methane-sulfonyloxymethyl-2H-pyridazin-3-one and 1-benzylpiperazine were reacted to yield the title compound as a yellow oil (yield: 97.7%). Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Mesylate.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.c1ccnnc1.C1C[NH]CC[NH]1.c1ccccc1.C1CC1
MsOH.HO-
null
null
null
COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F.c1ccc(CN2CCNCC2)cc1>>COc1ccc(-c2cc(CN3CCN(Cc4ccccc4)CC3)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1b22b684fe264dafbcb44e4cb70461a5
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC3CC3)n2)cc1F
C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O.C1(CC1)CN1N=C(C=C(C1=O)COS(=O)(=O)C)C1=CC(=C(C=C1)OC)F.N1(CCNCC1)C(=O)OC(C)(C)C>>C(C)(C)(C)OC(=O)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O
[NH:11]1[CH2:12][CH2:13][N:14]([C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21])[CH2:22][CH2:23]1.CS(=O)(=O)O[CH2:10][c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:33]([F:34])[cH:32]2)[n:31][n:26]([CH2:27][CH:28]2[CH2:29][CH2:30]2)[c:24]1=[O:25]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]...
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F
COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC3CC3)n2)cc1F
null
null
null
Heteroatom Alkylation and Arylation
Alkylation of amines
bc40e881c80f733cc18ae6a4c32c0d2e3ac9ce7b07d3a2cb609684e869dc6007
35d789812c3241c3a185d06663a309d930259e30563212f3884ef74718436cbc
O=c1c(CN2CCNCC2)cc(-c2ccccc2)nn1CC1CC1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[#7;a:6](-[C:7]):[c:8]:1=[O;D1;H0:9].[#7:10]1-[C:11]-[C:12]-[NH;D2;+0:13]-[C:14]-[C:15]-1>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:13]2-[C:12]-[C:11]-[#7:10]-[C:15]-[C:14]-2):[c:8]:1=[O;D1;H0:9]
98.9
[{"value": 98.9, "product": "C(C)(C)(C)OC(=O)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (10), 2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl)-4-methane-sulfonyloxymethyl-2H-pyridazin-3-one and tert-butyl 1-piperazinecarboxylate were reacted to yield the title compound as a pale brown oil (yield: 98.9%). Conditions: See reaction.notes.procedure_details. Workup: were re...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.c1ccnnc1.C1C[NH]CC[NH]1.C1CC1
MsOH.HO-
null
null
null
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0cf4acc0e65e454d8e4597bc7e4fb977
COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CN3CCNCC3)c(=O)n(CC3CC3)n2)cc1F
C(C)(C)(C)OC(=O)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O.C([O-])([O-])=O.[K+].[K+]>>C1(CC1)CN1N=C(C=C(C1=O)CN1CCNCC1)C1=CC(=C(C=C1)OC)F
CC(C)(C)OC(=O)[N:14]1[CH2:13][CH2:12][N:11]([CH2:10][c:9]2[cH:8][c:7](-[c:6]3[cH:5][cH:4][c:3]([O:2][CH3:1])[c:26]([F:27])[cH:25]3)[n:24][n:19]([CH2:20][CH:21]3[CH2:22][CH2:23]3)[c:17]2=[O:18])[CH2:16][CH2:15]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH2:10][N:11]3[CH2:12][CH2:13][NH:14][CH2:15][CH2:16...
COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC3CC3)n2)cc1F
COc1ccc(-c2cc(CN3CCNCC3)c(=O)n(CC3CC3)n2)cc1F
null
null
O
Reduction
Boc amine deprotection
2c25e19aee181a3c5131cfdfda27035fd54d4379a11d745dfb75d386bacfd500
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
O=c1c(CN2CCNCC2)cc(-c2ccccc2)nn1CC1CC1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-[C:6]-1>>[#7:4]1-[C:3]-[C:2]-[NH;D2;+0:1]-[C:6]-[C:5]-1
69.2
[{"value": 69.2, "product": "C1(CC1)CN1N=C(C=C(C1=O)CN1CCNCC1)C1=CC(=C(C=C1)OC)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 68.6, "product": "C1(CC1)CN1N=C(C=C(C1=O)CN1CCNCC1)C1=CC(=C(C=C1)OC)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
4-(4-tert-Butoxycarbonyl-1-piperazinyl)methyl-2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl)-2H-pyridazine-3-one (220 mg, 0.47 mmol) was dissolved in ice-cold trifluoroacetic acid (2 mL), and at the same temperature, the mixture was stirred for 15 minutes. Water (10 mL) was added to the reaction mixture. The mixture ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
C1C[NH]CC[NH]1
C1C[NH]CCN1
c1ccccc1.c1ccnnc1.C1C[NH]CCN1.C1CC1
HO-
O
null
0.25
COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC3CC3)n2)cc1F>O>COc1ccc(-c2cc(CN3CCNCC3)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-238e053add69416583ec29575c2096aa
COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F.O=C1NC(=O)c2ccccc21>>COc1ccc(-c2cc(CN3C(=O)c4ccccc4C3=O)c(=O)n(CC3CC3)n2)cc1F
O.C1(CC1)CN1N=C(C=C(C1=O)COS(=O)(=O)C)C1=CC(=C(C=C1)OC)F.C1(C=2C(C(N1)=O)=CC=CC2)=O.[K]>>C1(CC1)CN1N=C(C=C(C1=O)CN1C(C=2C(C1=O)=CC=CC2)=O)C2=CC(=C(C=C2)OC)F
CS(=O)(=O)O[CH2:10][c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:31]([F:32])[cH:30]2)[n:29][n:24]([CH2:25][CH:26]2[CH2:27][CH2:28]2)[c:22]1=[O:23].[NH: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]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH2:10][N:11]3[C:12](=[...
COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F.O=C1NC(=O)c2ccccc21
COc1ccc(-c2cc(CN3C(=O)c4ccccc4C3=O)c(=O)n(CC3CC3)n2)cc1F
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Alkylation of amines
8c55c1be63954a68557ba4cda7025bc5216a4a18e41dee3e27297e05487159d8
3761faea2e60c075e79428329c94e300333bad052ba97daeccc915afb3519a77
O=C1c2ccccc2C(=O)N1Cc1cc(-c2ccccc2)nn(CC2CC2)c1=O
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#7;a:5]:[#7;a:6](-[C:7]):[c:8]:1=[O;D1;H0:9].[O;D1;H0:10]=[C:11]1-[NH;D2;+0:12]-[C:13](=[O;D1;H0:14])-[c:15]:[c:16]-1>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:4]:[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:12]2-[C:11](=[O;D1;H0:10])-[c:16]:[c:15]-[C:13]-2=[O;D1;H0:14]):[c:8]:1=[O;D1;H0:9]
81.8
[{"value": 81.0, "product": "C1(CC1)CN1N=C(C=C(C1=O)CN1C(C=2C(C1=O)=CC=CC2)=O)C2=CC(=C(C=C2)OC)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.8, "product": "C1(CC1)CN1N=C(C=C(C1=O)CN1C(C=2C(C1=O)=CC=CC2)=O)C2=CC(=C(C=C2)OC)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
2
HOUR
To a solution of 2-cyclopropylmethyl-6-(3-fluoro-4-methoxyphenyl)-4-methanesulfonyloxymethyl-2H-pyridazin-3-one (220 mg, 0.57 mmol) in N,N-dimethylformamide (5 mL) was added potassium phthalimide (160 mg, 0.87 mmol), and the mixture was stirred at 80° C. for 2 hours. Water (30 mL) was added to the reaction mixture. Aft...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Unsubstituted dicarboximide
Substituted dicarboximide
c1ccc2c(c1)CNC2
c1ccc2c(c1)C[NH]C2
c1ccccc1.c1ccnnc1.c1ccc2c(c1)C[NH]C2.C1CC1
MsOH.HO-
CN(C=O)C
80
2
COc1ccc(-c2cc(COS(C)(=O)=O)c(=O)n(CC3CC3)n2)cc1F.O=C1NC(=O)c2ccccc21>CN(C=O)C>COc1ccc(-c2cc(CN3C(=O)c4ccccc4C3=O)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-38d2c167043c4980b48ac9206ec0428a
COc1ccc(-c2cc(CN3C(=O)c4ccccc4C3=O)c(=O)n(CC3CC3)n2)cc1F>>COc1ccc(-c2cc(CN)c(=O)n(CC3CC3)n2)cc1F
C1(CC1)CN1N=C(C=C(C1=O)CN1C(C=2C(C1=O)=CC=CC2)=O)C2=CC(=C(C=C2)OC)F.O.NN>>NCC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O
O=C1c2ccccc2C(=O)[N:11]1[CH2:10][c:9]1[cH:8][c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:21]([F:22])[cH:20]2)[n:19][n:14]([CH2:15][CH:16]2[CH2:17][CH2:18]2)[c:12]1=[O:13]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][c:9]([CH2:10][NH2:11])[c:12](=[O:13])[n:14]([CH2:15][CH:16]3[CH2:17][CH2:18]3)[n:19]2)[cH:20][c:...
COc1ccc(-c2cc(CN3C(=O)c4ccccc4C3=O)c(=O)n(CC3CC3)n2)cc1F
COc1ccc(-c2cc(CN)c(=O)n(CC3CC3)n2)cc1F
null
null
CO
Reduction
Phthalimide deprotection
d9f63cee80ef758bd939ff2a10772447b3092f1576180488281833a98eb1691a
dbfe4201a9328005dfaec4c3f363ddbb4ef3c9b825f648735dc97b2b57396333
O=c1ccc(-c2ccccc2)nn1CC1CC1
O=C1-[N;H0;D3;+0:1](-[C:2]-[c:3]:[c:4]:[#7;a:5])-C(=O)-c2:c:c:c:c:c:2-1>>[#7;a:5]:[c:4]:[c:3]-[C:2]-[NH2;D1;+0:1]
99.7
[{"value": 97.8, "product": "NCC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.7, "product": "NCC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC1CC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 2-cyclopropylmethyl-6-(3-fluoro-4-methoxypheyl)-4-phthalimidomethyl-2H-pyridazin-3-one (190 mg, 0.43 mmol) in methanol (5 mL) was added hydrazine monohydrate (110 mg, 2.20 mmol), and the mixture was heated under reflux for 2 hours. Methanol was distilled off, and chloroform (20 mL) was added to the res...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Primary amine
c1ccc2c(c1)C[NH]C2
null
c1ccccc1.c1ccnnc1.C1CC1
HO-
CO
null
null
COc1ccc(-c2cc(CN3C(=O)c4ccccc4C3=O)c(=O)n(CC3CC3)n2)cc1F>CO>COc1ccc(-c2cc(CN)c(=O)n(CC3CC3)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d070f2e59f204245b53f8b942c85a307
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(-c2nn(CC(C)C)c(=O)c(OS(C)(=O)=O)c2C)cc1F.Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F>>COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC(C)C)n2)cc1F
C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O.FC=1C=C(C=CC1OC)C=1C(=C(C(N(N1)CC(C)C)=O)OS(=O)(=O)C)C.N1(CCNCC1)C(=O)OC(C)(C)C>>C(C)(C)(C)OC(=O)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC(C)C)=O
[NH:11]1[CH2:12][CH2:13][N:14]([C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21])[CH2:22][CH2:23]1.CS(=O)(=O)O[c:9]1[c:8](C)[c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:33]([F:34])[cH:32]2)[n:31][n:26]([CH2:27][CH:28]([CH3:29])[CH3:30])[c:24]1=[O:25].Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2[CH3:10...
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(-c2nn(CC(C)C)c(=O)c(OS(C)(=O)=O)c2C)cc1F.Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F
COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC(C)C)n2)cc1F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2a0dbc48e846de8e0c36eabe2ecaa3dda67e2c62a942dd827dcb6cda2589c033
f8979a7dc32618975f84bf1d08d0eb1a0766a30fc7e3bcdfee8ffc6d86d4188b
O=c1[nH]nc(-c2ccccc2)cc1CN1CCNCC1
C-C(-C)-C-n1:n:c(-c2:c:c:c(-C):c(-F):c:2):c(-[CH3;D1;+0:1]):c(-N2-C-C-N(-C(=O)-O-C(-C)(-C)-C)-C-C-2):c:1=O.C-[c;H0;D3;+0:2]1:[c:3](-[c:4]):[#7;a:5]:[#7;a:6](-[C:7]):[c:8](=[O;D1;H0:9]):[c;H0;D3;+0:10]:1-O-S(-C)(=O)=O.[#7:11]1-[C:12]-[C:13]-[NH;D2;+0:14]-[C:15]-[C:16]-1>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:3](-[c:4]):[cH;D2;+0:...
94.3
[{"value": 94.3, "product": "C(C)(C)(C)OC(=O)N1CCN(CC1)CC=1C(N(N=C(C1)C1=CC(=C(C=C1)OC)F)CC(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (10), 6-(3-fluoro-4-methoxyphenyl)-2-isobutyl-4-methane-sulfonyloxy-methyl-2H-pyridazin-3-one and tert-butyl 1-piperazine-carboxylate were reacted to yield the title compound as a yellow oil (yield: 94.3%). Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
null
Mesylate.Aromatic halide.Carbamic ester.Ether.Secondary amine.Tertiary amine.Boc
Tertiary amine
C1CNCC[NH]1.c1ccnnc1.c1ccccc1.c1ccnnc1.C1CNCCN1
c1ccnnc1.C1C[NH]CC[NH]1
c1ccccc1.c1ccnnc1.C1C[NH]CC[NH]1
MsOH.HF
null
null
null
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(-c2nn(CC(C)C)c(=O)c(OS(C)(=O)=O)c2C)cc1F.Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F>>COc1ccc(-c2cc(CN3CCN(C(=O)OC(C)(C)C)CC3)c(=O)n(CC(C)C)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9a890b21ea1b4a5fba0835c8a826d216
CN1CCNCC1.COc1ccc(-c2nn(CC(C)C)c(=O)c(OS(C)(=O)=O)c2C)cc1F.Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F>>COc1ccc(-c2cc(CN3CCN(C)CC3)c(=O)n(CC(C)C)n2)cc1F
C(C)(C)(C)OC(=O)N1CCN(CC1)C=1C(N(N=C(C1C)C1=CC(=C(C=C1)C)F)CC(C)C)=O.FC=1C=C(C=CC1OC)C=1C(=C(C(N(N1)CC(C)C)=O)OS(=O)(=O)C)C.CN1CCNCC1>>FC=1C=C(C=CC1OC)C=1C=C(C(N(N1)CC(C)C)=O)CN1CCN(CC1)C
[NH:11]1[CH2:12][CH2:13][N:14]([CH3:15])[CH2:16][CH2:17]1.CS(=O)(=O)O[c:9]1[c:8](C)[c:7](-[c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:27]([F:28])[cH:26]2)[n:25][n:20]([CH2:21][CH:22]([CH3:23])[CH3:24])[c:18]1=[O:19].Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2[CH3:10])cc1F>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c...
CN1CCNCC1.COc1ccc(-c2nn(CC(C)C)c(=O)c(OS(C)(=O)=O)c2C)cc1F.Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F
COc1ccc(-c2cc(CN3CCN(C)CC3)c(=O)n(CC(C)C)n2)cc1F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2a0dbc48e846de8e0c36eabe2ecaa3dda67e2c62a942dd827dcb6cda2589c033
f8979a7dc32618975f84bf1d08d0eb1a0766a30fc7e3bcdfee8ffc6d86d4188b
O=c1[nH]nc(-c2ccccc2)cc1CN1CCNCC1
C-C(-C)-C-n1:n:c(-c2:c:c:c(-C):c(-F):c:2):c(-[CH3;D1;+0:1]):c(-N2-C-C-N(-C(=O)-O-C(-C)(-C)-C)-C-C-2):c:1=O.C-[c;H0;D3;+0:2]1:[c:3](-[c:4]):[#7;a:5]:[#7;a:6](-[C:7]):[c:8](=[O;D1;H0:9]):[c;H0;D3;+0:10]:1-O-S(-C)(=O)=O.[#7:11]1-[C:12]-[C:13]-[NH;D2;+0:14]-[C:15]-[C:16]-1>>[C:7]-[#7;a:6]1:[#7;a:5]:[c:3](-[c:4]):[cH;D2;+0:...
80.9
[{"value": 80.9, "product": "FC=1C=C(C=CC1OC)C=1C=C(C(N(N1)CC(C)C)=O)CN1CCN(CC1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (10), 6-(3-fluoro-4-methoxyphenyl)-2-isobutyl-4-methanesulfonyloxy-methyl-2H-pyridazin-3-one and 1-methylpiperazine were reacted to yield the title compound as a yellow oil (yield: 80.9%). Conditions: See reaction.notes.procedure_details. Workup: were reacted
10.6084/m9.figshare.5104873.v1
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Mesylate.Aromatic halide.Carbamic ester.Ether.Secondary amine.Tertiary amine.Boc
Tertiary amine
C1CNCC[NH]1.c1ccnnc1.c1ccccc1.c1ccnnc1.C1CNCCN1
c1ccnnc1.C1C[NH]CC[NH]1
c1ccccc1.c1ccnnc1.C1C[NH]CC[NH]1
MsOH.HF
null
null
null
CN1CCNCC1.COc1ccc(-c2nn(CC(C)C)c(=O)c(OS(C)(=O)=O)c2C)cc1F.Cc1ccc(-c2nn(CC(C)C)c(=O)c(N3CCN(C(=O)OC(C)(C)C)CC3)c2C)cc1F>>COc1ccc(-c2cc(CN3CCN(C)CC3)c(=O)n(CC(C)C)n2)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-41ba53391d074cb3803addfbb5300834
COC1C(=O)NN=C(c2ccc(C)c(F)c2)C1=C=O.O=C(O)c1cc(-c2ccccc2)n[nH]c1=O>>COC(=O)c1cc(-c2ccccc2)n[nH]c1=O
FC=1C=C(C=CC1C)C=1C(C(C(NN1)=O)OC)=C=O.C(=O)(O)C=1C(NN=C(C1)C1=CC=CC=C1)=O>>COC(=O)C=1C(NN=C(C1)C1=CC=CC=C1)=O
Cc1ccc(C2=NNC(=O)C(O[CH3:1])C2=C=O)cc1F.[OH:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[n:14][nH:15][c:16]1=[O:17]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[n:14][nH:15][c:16]1=[O:17]
COC1C(=O)NN=C(c2ccc(C)c(F)c2)C1=C=O.O=C(O)c1cc(-c2ccccc2)n[nH]c1=O
COC(=O)c1cc(-c2ccccc2)n[nH]c1=O
null
null
null
Heteroatom Alkylation and Arylation
O-methylation
271dcd3906504ae2d6e121d10bca7a3a0f064ba1774506d60dea989df3d3484a
2f542dc6f0dfac8dbe5372e0f739640c8522541a995d8198c5c7f5141d6123a2
O=c1ccc(-c2ccccc2)n[nH]1
C-c1:c:c:c(-C2=N-N-C(=O)-C(-O-[CH3;D1;+0:1])-C-2=C=O):c:c:1-F.[#7;a:2]:[c:3]:[c:4]-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]>>[#7;a:2]:[c:3]:[c:4]-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-[CH3;D1;+0:1]
98.9
[{"value": 98.9, "product": "COC(=O)C=1C(NN=C(C1)C1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (5), 4-carboxy-6-phenyl-2H-pyridazin-3-one was reacted to yield the title compound as pale yellow crystals (yield: 98.9%). Conditions: See reaction.notes.procedure_details. Workup: was reacted
10.6084/m9.figshare.5104873.v1
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Hydrazone amide.Aromatic halide.Carboxylic acid.Ether
Ester
c1ccccc1.C1=NNCCC1
null
c1cnncc1.c1ccccc1
HF
null
null
null
COC1C(=O)NN=C(c2ccc(C)c(F)c2)C1=C=O.O=C(O)c1cc(-c2ccccc2)n[nH]c1=O>>COC(=O)c1cc(-c2ccccc2)n[nH]c1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0095c865a56e4289b73179372c43aea2
COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O.COC(=O)c1cc(-c2ccccc2)n[nH]c1=O>>COC(=O)c1cc(-c2ccccc2)nn(CC(C)C)c1=O
FC=1C=C(C=CC1C)C=1C=C(C(N(N1)CC(C)C)=O)C(=O)OC.COC(=O)C=1C(NN=C(C1)C1=CC=CC=C1)=O>>C(C(C)C)N1N=C(C=C(C1=O)C(=O)OC)C1=CC=CC=C1
Cc1cc[c:8](-[c:7]2[cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[c:20](=[O:21])[n:15]([CH2:16][CH:17]([CH3:18])[CH3:19])[n:14]2)[cH:13]c1F.COC(=O)c1cc(-c2c[cH:12][cH:11][cH:10][cH:9]2)n[nH]c1=O>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][c:7](-[c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[n:14][n:15]([CH2:16][CH:17]([CH3:18])[CH3:19])...
COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O.COC(=O)c1cc(-c2ccccc2)n[nH]c1=O
COC(=O)c1cc(-c2ccccc2)nn(CC(C)C)c1=O
null
null
null
Miscellaneous
OtherReaction
7b30369b089395f834ea5a700f03ff7779f66f1cdc56a630ae059821527c476e
7494cceafaa45c0a4e5f400921a6429ff2b5672c3e28c3ffe3859e2ee8af3168
O=c1ccc(-c2ccccc2)n[nH]1
C-O-C(=O)-c1:c:c(-c2:[cH;D2;+0:1]:[c:2]:[c:3]:[cH;D2;+0:4]:c:2):n:[nH]:c:1=O.C-c1:c:c:[c;H0;D3;+0:5](-[c:6](:[c:7]):[#7;a:8]:[#7;a:9](-[C:10]):[c:11]):[cH;D2;+0:12]:c:1-F>>[C:10]-[#7;a:9](:[c:11]):[#7;a:8]:[c:6](-[c;H0;D3;+0:5]1:[cH;D2;+0:12]:[cH;D2;+0:4]:[c:3]:[c:2]:[cH;D2;+0:1]:1):[c:7]
94.1
[{"value": 94.1, "product": "C(C(C)C)N1N=C(C=C(C1=O)C(=O)OC)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Following the procedure of Example 1 (6), 4-methoxycarbonyl-6-phenyl-2H-pyridazin-3-one was reacted to yield the title compound as a yellow oil (yield: 94.1%). Conditions: See reaction.notes.procedure_details. Workup: was reacted
10.6084/m9.figshare.5104873.v1
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Aromatic halide.Ester
null
c1ccccc1.c1ccnnc1.c1ccccc1
c1ccccc1
c1ccnnc1.c1ccccc1
HF
null
null
null
COC(=O)c1cc(-c2ccc(C)c(F)c2)nn(CC(C)C)c1=O.COC(=O)c1cc(-c2ccccc2)n[nH]c1=O>>COC(=O)c1cc(-c2ccccc2)nn(CC(C)C)c1=O