盐酸雷莫司琼的合成工艺  

Synthesis of ramosetron hydrochloride

作　　者：魏文涛[1] 李祎亮[2] 王文倩[2] 

机构地区：[1]天津泰普药品科技发展有限公司,天津300193 [2]天津药物研究院,天津300193

出　　处：《现代药物与临床》2012年第2期94-96,共3页Drugs & Clinic

摘　　要：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.

关 键 词：雷莫司琼 5-HT3受体拮抗剂 酰化 1-乙酰基-5-[(1-甲基吲哚-3-基)羰基]-4 5 6 7-四氢苯并咪唑 

分 类 号：R914.5[医药卫生—药物化学]