【摘要】 目的:合成抗抑郁药米氮平。方法:以N-甲基乙醇胺、氧化苯乙烯和2-氨基烟酸为原料,经亲核开环、氯代、碱化、还原、胺烷基化和环合6步制得了抗抑郁药米氮平。结果:文献报道的相应各步反应条件得以优化,产率由22.6%提高到49.5%,各中间体及产物经红外光谱、核磁共振氢谱确证。结论:本方法简化了操作步骤,优化了反应条件,降低了成本,提高了收率。更多还原

【Abstract】 Objective: To synthesize antidepressant mirtazapine. Methods: Starting from styrene oxide,N-methylethanolamine and 2aminonicotinic acid,the target compound was synthesized via 6 reactive steps involving nucleophilic ring-opening,chlorination,alkalinization,reduction,N-alklation and cyclization.Results: The total yield was 49.5%,compared to the yield of 22.6% reported in the literature.Structures of the target product and key intermediates were verified by IR and 1HNMR.Conclusion: This optimal synthetic procedure with lower cost and higher yield is worthy to have a further pilot manufacture.更多还原