目的改进促胃动力药西沙比利的合成方法。方法以N-乙氧羰基-4-哌啶酮为起始原料,经羟基化、甲基化、脱保护、还原氨化等8步反应得到目标化合物。结果与结论目标产物西沙比利的结构经MS和1H-NMR确证,反应总收率达24.8%(以N-乙氧羰基-4-哌啶酮计),纯度大于99.5%。与文献报道的工艺相比,该路线操作简便、收率较高、生产成本较低,有利于工业化生产。 Objective To improve the method of synthesizing cisapride, a drug for promoting gastric motility. Methods Starting from N-ethoxycarbonyl-4-piperidone, the target compounds were obtained after 8 steps of hydroxylation, methylation, deprotection and reductive amination. RESULTS AND CONCLUSIONS The target product cisapride was confirmed by MS and 1H-NMR. The overall yield was 24.8% (calculated as N-ethoxycarbonyl-4-piperidinone) and the purity was more than 99.5%. Compared with the reported process, the route is easy to operate, has high yield and low production cost, which is beneficial to industrialized production.