[CH3:1][O:2][C:3]([C:5]1([NH2:17])[CH2:10][CH2:9][N:8]([C:11]2[CH:16]=[CH:15][N:14]=[CH:13][CH:12]=2)[CH2:7][CH2:6]1)=[O:4].Cl[S:19]([C:22]1[CH:31]=[C:30]2[C:25]([CH2:26][CH2:27][N:28]([C:32](=[O:37])[C:33]([F:36])([F:35])[F:34])[CH2:29]2)=[CH:24][CH:23]=1)(=[O:21])=[O:20].N1C=CC=CC=1.O>C(Cl)(Cl)Cl>[CH3:1][O:2][C:3]([C:5]1([NH:17][S:19]([C:22]2[CH:31]=[C:30]3[C:25]([CH2:26][CH2:27][N:28]([C:32](=[O:37])[C:33]([F:36])([F:34])[F:35])[CH2:29]3)=[CH:24][CH:23]=2)(=[O:20])=[O:21])[CH2:10][CH2:9][N:8]([C:11]2[CH:16]=[CH:15][N:14]=[CH:13][CH:12]=2)[CH2:7][CH2:6]1)=[O:4]To a solution of 4-amino-1-(pyridin-4-yl)piperidine-4-carboxylic acid methyl ester (330 mg) in chloroform (5 ml) were added 7-chlorosulfonyl-2-trifluoroacetyl-1,2,3,4-tetrahydroisoquinoline (Journal of Medicinal Chemistry, vol. 23, No.8, p. 837 (1980)) (500 mg) and pyridine (0.23 ml), and the mixture was stirred at room temperature for 12 hours. After completion of the reaction, water was added, and the mixture was extracted with chloroform and washed successively with water and saturated brine. The organic layer was dried over anhydrous sodium sulfate, and the solvent was evaporated. The residue was dried under reduced pressure to give the title compound (627 mg).
読み込み中…