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[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。
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[Abstract]
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.
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