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抗抑郁药盐酸托莫西汀的合成工艺改进

Improved synthesis of an antidepressant,atomoxetine hydrochloride

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【作者】 奚倬勋吴范宏张俊俞晓东吴艳萍

【Author】 XI Zhuo-xun~1,WU Fan-hong~1,ZHANG Jun~1,YU Xiao-dong~2,WU Yan-ping~2(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)

【机构】 华东理工大学化学与制药学院上海康鸣高科技有限公司上海康鸣高科技有限公司 上海200237上海200237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。

【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.

  • 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2005年05期
  • 【分类号】TQ463;
  • 【被引频次】9
  • 【下载频次】590
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