N-[3-nitro-4-({[(1r,4r)-4-hydroxy-4-methylcyclohexyl]methyl}amino)benzenesulfonyl]-4-{2-oxo-7-azaspiro[3.5]nonan-7-yl}-2-[(3R,8S)-15-{[2- (trimethylsilyl)ethoxy]methyl}-2,5-dioxa-9,15,17-triazatetracyclo[8.7.0.0
Λ{3,8}.0
Λ{12,16}]heptadeca-1(10),11,13,16-tetraen-9-yl]benzamide 、
(2R)-2-(2-methylphenyl)piperidine 在
sodium cyanoborohydride 、 zinc(II) chloride 作用下,
以
甲醇 为溶剂,
以84.7 %的产率得到4-{2-[(2R)-2-(2-methylphenyl)piperidin-1-yl]-7-azaspiro[3.5]nonan-7-yl}-N-[3-nitro-4-({[(1r,4r)-4-hydroxy-4-methylcyclohexyl]methyl}amino)benzenesulfonyl]-2-[(3R,8S)-15-{[2-(trimethylsilyl)ethoxy]methyl}-2,5-dioxa-9,15,17-triazatetracyclo[8.7.0.0
Λ{3,8}.0
Λ{12,16}]heptadeca-1(10),11,13,16-tetraen-9-yl]benzamide