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5-HT3受体拮抗剂盐酸阿扎司琼的合成
引用本文:5-HT3受体拮抗剂盐酸阿扎司琼的合成[J]. 中国药科大学学报, 2003, (3): 20-21.
作者姓名:罗小川  陈国华  徐昌盛
作者单位:中国药科大学药化教研室,南京,210009
摘    要:目的:改进5-HT3受体拮抗剂盐酸阿扎司琼的合成工艺。方法:以5-氯-2-羟基苯甲酸甲酯为原料,经硝化、还原等九步反应合成。结果:合成了目标化合物,总收率为40%,其结构经IR,^1HNMR和MS确证。结论:合成路线及工艺较适合于工业化生产。

关 键 词:5-HT3受体拮抗剂  盐酸阿扎司琼  合成
文章编号:1000-5048(2003)03-0214-02
修稿时间:2002-08-21

Synthesis of the 5-HT3 Receptor Antagonist Azasetron Hydrochloride
Synthesis of the 5-HT3 Receptor Antagonist Azasetron Hydrochloride[J]. Journal of China Pharmaceutical University, 2003, (3): 20-21.
Authors:LUO Xiao-Chuan  CHEN Guo-Hu  XU Chang-Sheng
Affiliation:LUO Xiao-Chuan,CHEN Guo-Hua,XU Chang-Sheng Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,China
Abstract:AIM:The purpose is to develop the general process for the synthesis of 5-HT 3 receptor antagonist Azasetron Hydrochloride. METHOD: It was synthesized from methyl 5-chloro-2-hydroxyl benzoic acid via nine-step reaction with nitration,reduction,etc. RESULT: The title compound was obtained with 40% overall yield. The structure was confirmed by IR, 1 HNMR and MS. CONCLUSION:Some improvements for the synthesis of Azasetron Hydrochloride were made.
Keywords:5-HT 3 receptor antagonist  Azasetron hydrochloride  Synthesis
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