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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
【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.
【关键词】 药物化学;
工艺改进;
化学合成;
抗抑郁药;
托莫西汀;
【Key words】 medicinal chemistry; process improvement; chemical synthesis; antidepressant; atomoxetine;
【Key words】 medicinal chemistry; process improvement; chemical synthesis; antidepressant; atomoxetine;
- 【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