帕洛诺司琼的合成

Synthesis of palonosetron

目的:合成新型5-HT3受体阻滞剂帕洛诺司琼。方法:以1萘-甲酸和4哌-啶甲酸乙酯为原料经胺化、成环、水解、胺化、脱水、关环、还原等反应合成目标物。结果:合成了帕洛诺司琼,总收率7.6%。结论:本方法合成帕洛诺司琼,操作简便,且提高了收率。

Objective： To synthesize palonosetron a novel 5-HT3 receptar antegonist. Methods： Palonosetron was prepared from 1-naphthalenecarboxylic acid and 4-carbethoxypiperidine via a series of steps such as amination, cyclization, hydrolysis, dehydration, reduction, etc. Results： The total yield of palonosetron was 7.6%. Conclusion ： The modifications of a few steps in the synthesis can simplify the procedure and increase the yields.