反応式
[CH:1]1([N:4]2[CH2:13][C:12]([CH3:15])([CH3:14])[C:11]3[C:6](=[CH:7][CH:8]=[C:9](OS(C(F)(F)F)(=O)=O)[CH:10]=3)[CH2:5]2)[CH2:3][CH2:2]1.C1(P(C2C=CC=CC=2)CCCP(C2C=CC=CC=2)C2C=CC=CC=2)C=CC=CC=1.CS(C)=O.[C]=O.[C:59]([O:62][CH2:63][CH3:64])(=[O:61])C>CCCCCC.C([O-])(=O)C.[Pd+2].C([O-])(=O)C.C(O)C.C(N(CC)CC)C.ClCCCl>[CH2:63]([O:62][C:59]([C:9]1[CH:10]=[C:11]2[C:6](=[CH:7][CH:8]=1)[CH2:5][N:4]([CH:1]1[CH2:3][CH2:2]1)[CH2:13][C:12]2([CH3:15])[CH3:14])=[O:61])[CH3:64]参加物
11
反応物 5
生成物 1
試薬・触媒・溶媒 5
実験手順
Following general procedure K and using 2-cyclopropyl-4,4-dimethyl-6-trifluoromethylsulfonyloxy-1,2,3,4-tetrahydro-isoquinoline (Intermediate 22, 1.6 g, 4.6 mmol), palladium acetate (0.127 g, 0.56 mmol), 1,3-bis(diphenylphosphino)propane (0.160 g, 0.39 mmol), dimethylsulfoxide (2 mL), 1,2-dichloroethane (5 mL), triethyl amine (2 mL) , ethanol (5 mL) and an atmosphere of carbon monoxide followed by flash column chromatography over silica gel (230-400 mesh) using 10% ethyl acetate in hexane as the eluent the title compound was obtained as an oil (1 g, 79%).
出典と根拠
- ORDレコード
- ord-09aab86587864538ab7b81d6ac8fa64f
- 出典データセット
- uspto-grants-2005_02
- 特許番号
- US06855512B2
関連ノート
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