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盐酸氟西汀的合成 被引量:6

Synthesis of Fluoxetine Hydrochloride
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摘要 苯乙酮与甲胺盐酸盐、多聚甲醛进行M ann ich反应生成3-甲胺基-1-苯基丙酮盐酸盐(1);1在甲醇中用硼氢化钾还原制备3-甲胺基-1-苯基丙醇(2);2经醚化、成盐合成了抗抑郁药———盐酸氟西汀(4),总收率41%。4的结构经1H NMR和MS表征。 Fluoxetine hydrochloride(4) in overall yield of 41.0% was synthesized by a four-step reaction in which acetophenone reacted with methylamine hydrochloride and paraformaldehyde to obtain 3-methylaminopropiophenone hydrochloride (1); then 1 was reduced by potassium borohydride i,n methanol to prepare 3-methylamino-1-phenylpropanol(2) ; finally, 2 reacted with 4-chlorobenzo-trif- luoride and formed salt. The structrue of 4 was characterized by ^1H NMR and MS.
出处 《合成化学》 CAS CSCD 2008年第3期354-355,361,共3页 Chinese Journal of Synthetic Chemistry
基金 国家自然科学基金资助项目(20576094)
关键词 MANNICH反应 氟西汀 抗抑郁药 药物合成 Mannich reaction Fluoxetine antidepressant synthesis
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