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抗抑郁药盐酸托莫西汀的合成工艺改进
引用本文:奚倬勋,吴范宏,张俊,俞晓东,吴艳萍.抗抑郁药盐酸托莫西汀的合成工艺改进[J].中国药物化学杂志,2005,15(5):282-284.
作者姓名:奚倬勋  吴范宏  张俊  俞晓东  吴艳萍
作者单位:1. 华东理工大学,化学与制药学院,上海,200237
2. 上海康鸣高科技有限公司,上海,200237
摘    要:目的研究盐酸托莫西汀的合成工艺.方法以1-苯丙醇为起始原料,经氯代、溴代、醚化、胺化、拆分、氯化氢成盐6步反应合成盐酸托莫西汀.结果与结论合成盐酸托莫西汀的总收率为16.4%,比文献值提高了5.4%.改进了中间体5和6的合成工艺.

关 键 词:药物化学  工艺改进  化学合成  抗抑郁药  托莫西汀
文章编号:1005-0108(2005)05-0282-03
收稿时间:2005-04-26
修稿时间:2005-04-26

Improved synthesis of an antidepressant,atomoxetine hydrochloride
XI Zhuo-xun,WU Fan-hong,ZHANG Jun,YU Xiao-dong,WU Yan-ping.Improved synthesis of an antidepressant,atomoxetine hydrochloride[J].Chinese Journal of Medicinal Chemistry,2005,15(5):282-284.
Authors:XI Zhuo-xun  WU Fan-hong  ZHANG Jun  YU Xiao-dong  WU Yan-ping
Institution:1. College of Chemistry and Pharmaceutics, East China University of Science and Technology, Shanghai 200237, China ;2. Shanghai Coming Hi-Technology Co., Ltd, Shanghai 200237, China
Abstract:Aim To study the synthesis of atomoxetine hydrochloride. Methods Atomoxetine hydrochloride was synthesized using 3-phenylpropanol as the starting material via six steps, such as chlorination, bromination, etherification, substitution, separation of levorotary isomer and acidification by gaseous hydrogen chloride. Results and conclusions The target compound was synthesized from 3-phenylpropanol, and the overall yield was 16.4%, 5.4% higher than the yield reported. The preparation process of the intermediate 5 and 6 was also improved.
Keywords:medicinal chemistry  process improvement  chemical synthesis  antidepressant  atomoxetine
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