| 盐酸阿洛司琼合成工艺改进 |
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| 引用本文： | 朱凤英,陈国广,陈华明,韦萍,欧阳平凯. 盐酸阿洛司琼合成工艺改进[J]. 药学与临床研究, 2002, 10(4): 14-15 |
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| 作者姓名： | 朱凤英 陈国广 陈华明 韦萍 欧阳平凯 |
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| 作者单位： | 南京工业大学制药与生命科学学院（南京２１０００９） |
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| 摘 要： | 目的：改进盐酸阿洛司琼的合成工艺，以利于工业生产。方法：以２，４—哌啶二酮－３—羧酸甲酯与Ｎ—甲基苯肼缩合后在硫酸和醋酸存在下环合得制２，３，４，５—四氢—５—甲基—１Ｈ—吡淀并［４、３—ｂ］吲哚—１—酮，然后甲基化，再与４—羟甲基—５—甲基咪唑在对甲苯磺酸催化下缩合。结果：制得合格的盐酸阿洛司琼，总收率３８％。结论：经改进的工艺操作简便，比原工艺更易于工业化生产。
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| 关 键 词： | 盐酸阿洛司琼 合成工艺 改进 工业生产 |
| 收稿时间： | 2002-04-05 |
Improving the Synthesis of Alosetron Hydrochloride |
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| Zhu Fengying,Chen Guoguang,Chen Huaming,Wei Ping and Ouyang Pingkai. Improving the Synthesis of Alosetron Hydrochloride[J]. Pharmacertical and Clinical Research, 2002, 10(4): 14-15 |
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| Authors: | Zhu Fengying Chen Guoguang Chen Huaming Wei Ping Ouyang Pingkai |
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| Affiliation: | College of Life and Pharmacy Science, Nanjing University of Technology, Nanjing 210009,College of Life and Pharmacy Science, Nanjing University of Technology, Nanjing 210009,College of Life and Pharmacy Science, Nanjing University of Technology, Nanjing 210009,College of Life and Pharmacy Science, Nanjing University of Technology, Nanjing 210009,College of Life and Pharmacy Science, Nanjing University of Technology, Nanjing 210009 |
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| Abstract: | AIMS to improve the preparation process of alosetron hydrochloride on a large scale production; METHODS Alosetron Hydrochloride was preparated by condensation methyl 2,4-piperidindione-3-carboxylate and N-methyl phenyl hydrazine, then cyclization in sulfuric acid-acetic acid,and condensation with 4-hydroxyl-5-methyimidazole. RESULTS the total yield is 38%. CONCLUSIONS the improved process is more convenient on a large-scale production. |
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| Keywords: | Alosetron hydrochloride Synthesis Improvement |
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