抗抑郁药米氮平的新合成方法  

Synthesis of antidepressant mirtazapine

作　　者：陈升[1] 肖国民[1] 陈绘如[1] 楼佳珍[1] 

机构地区：[1]东南大学化学化工学院,南京210096

出　　处：《中国新药杂志》2007年第2期137-139,共3页Chinese Journal of New Drugs

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。Objective： To synthesize antidepressant mirtazapine. Methods： Starting from styrene oxide, N-methylethanolamine and 2-aminonicotinic 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.

关 键 词：米氮平 抗抑郁药 胺烷基化 药物合成 

分 类 号：R971.43[医药卫生—药品] R914.5[医药卫生—药学]