目的 研究鹽酸雷莫司瓊的合成工藝。方法 主要是以4,5,6,7-四氫苯并咪唑-5-羧酸甲酯硫酸鹽為中間體，經(jīng)乙酰化、芳香環(huán)碳?；苽?-乙酰基-5-[(1-甲基吲哚-3-基)羰基]-4,5,6,7-四氫苯并咪唑，此化合物再經(jīng)水解、拆分得到鹽酸雷莫司瓊。結(jié)果 本工藝所得鹽酸雷莫司瓊總收率為21.2%。結(jié)論 鹽酸雷莫司瓊的合成工藝穩(wěn)定，操作簡便，適合工業(yè)化生產(chǎn)。

Objective To study the synthetic process of ramosetron hydrochloride. Methods Ramosetron hydrochloride was synthesized by taking 4,5,6,7-tetrahydrobenzimidazole as intermediates, 1-acetyl-5-[(1-methylindole-3-yl)carbonyl]-4,5,6,7- tetrahydrobenzimidazole was obtained via acetylation, carbon acylation action, and then was hydrolyzed and split to obtain ramosetron hydrochloride finally. Results The total yield of ramosetron hydrochloride was 21.2%. Conclusion The synthesis process of ramosetron hydrochloride has seveal advantages such as stable process, simple operation, and suitable for industrial production.