| 盐酸雷莫司琼的合成工艺 |
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| 引用本文： | 魏文涛,李祎亮,王文倩.盐酸雷莫司琼的合成工艺[J].现代药物与临床,2012,27(2):94-96. |
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| 作者姓名： | 魏文涛 李祎亮 王文倩 |
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| 作者单位： | 天津泰普药品科技发展有限公司;天津药物研究院 |
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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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| 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 |
Synthesis of ramosetron hydrochloride |
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| WEI Wen-tao,LI Yi-liang and WANG Wen-qian.Synthesis of ramosetron hydrochloride[J].Drugs & Clinic,2012,27(2):94-96. |
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| Authors: | WEI Wen-tao LI Yi-liang and WANG Wen-qian |
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| Institution: | 1.Tianjin Taipu Pharmaceutical Technology Co.,Ltd.,Tianjin 300193,China 2.Tianjin Institute of Pharmaceutical Research,Tianjin 300193,China |
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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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| Keywords: | ramosetron hydrochloride 5-hydroxytryptamine(5-HT3) receptor antagonists acylation 1-acetyl-5-[(1-methylindole-3-yl) carbonyl]-4 5 6 7-tetrahydrobenzimidazole |
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