盐酸雷莫司琼的合成工艺

Synthesis of ramosetron hydrochloride

目的研究盐酸雷莫司琼的合成工艺。方法主要是以4,5,6,7-四氢苯并咪唑-5-羧酸甲酯硫酸盐为中间体,经乙酰化、芳香环碳酰化制备1-乙酰基-5-[(1-甲基吲哚-3-基)羰基]-4,5,6,7-四氢苯并咪唑,此化合物再经水解、拆分得到盐酸雷莫司琼。结果本工艺所得盐酸雷莫司琼总收率为21.2%。结论盐酸雷莫司琼的合成工艺稳定,操作简便,适合工业化生产。

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.