(3R,4R,5S)-1-{[(3S,4S)-4-(5-chloropyridin-2-yl)pyrrolidin-3-yl]carbonyl}-4-(4-fluorophenyl)-3,5-dimethylpiperidin-4-ol 、
1,6-dichloropyridazine 在
N,N-二异丙基乙胺 作用下,
以
乙腈 为溶剂,
以42%的产率得到(3R,4R,5S)-1-{[(3S,4S)-1-(6-chloropyridazin-3-yl)-4-(5-chloropyridin-2-yl)pyrrolidin-3-yl]carbonyl}-4-(4-fluorophenyl)-3,5-dimethylpiperidin-4-ol