| 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-吡啶并 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 |
| 修稿时间： | 2002年4月5日 |
Improving the Synthesis of Alosetron Hydrochloride |
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| Zhu Fengying,Chen Guoguang,Chen Huaming,Wei Ping,Ouyang Pingkai College of Life and Pharmacy Science,Nanjing University of Technology,Nanjing.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 College of Life and Pharmacy Science Nanjing University of Technology Nanjing |
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| Institution: | Zhu Fengying,Chen Guoguang,Chen Huaming,Wei Ping,Ouyang Pingkai 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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