【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。更多还原

【Abstract】 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 in methanol to prepare 3-methylamino-1-phenylpropanol(2);finally,2 reacted with 4-chlorobenzo-trifluoride and formed salt.The structrue of 4 was characterized by 1H NMR and MS.更多还原