抗抑郁药米氮平的合成
Synthesis of Antidepressant-Mirtazapine
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摘要: 以环氧苯乙烯和N-甲基乙醇胺为起始原料,经亲核开环、氯代和环合反应得到中间体1-甲基-3-苯基哌嗪。1-甲基-3-苯基哌嗪与2-氯-3-氰基吡啶亲核取代,再经水解、还原和环合等反应得到米氮平,总收率为22.6%,结构经1H-NMR和M S(质谱)确认,HPLC含量为99.79%。Abstract: Mirtazapine was prepared by a seven-step reaction,namely nucleophilic ring-opening reaction,chlorination,cyclization,uncleophilic substitution,hydrolysis,reduction and cyclization from styrene oxide and N-methylethanolamine as the starting materials,with overall yield of 22.6%.The structure of mirtazpine was confirmed by()~1H-NMR(H~1-nuclear magnetic resonance) and MS(mass spectrum),and the purity was 99.79% by HPLC.