抗抑郁药盐酸度洛西汀的合成工艺改进

目的：改进盐酸度洛西汀合成工艺。方法：以乙酰噻吩、盐酸二甲胺和多聚甲醛为起始原料，经Mannich反应、还原、拆分、成醚、去甲基、重结晶等6步，改进文献报道的工艺过程，更换部分反应试剂，合成盐酸度洛西汀。结果：所得目标化合物的结构经元素分析、质谱、核磁共振氢谱以及红外光谱确证，总收率由文献报道的7％提高到19．4％。结论：该工艺可降低成本，操作简化，收率高，适合工业化生产。

An Improved Synthesis Method of Anti-depression Drug Duloxetine Hydrochloride

Objective:To improve the method for the synthesis of duloxetine hydrochloride.Methods:Starting with 2-acetylthiofuran plus dimethylamine hydrochloride and paraformaldehyde, deloxetine hydrochloride was synthesized in a facile way via a 6-step chain reaction including Mannich reaction,reduction,separation,etherification,demethylation and recrystalization,where some operations and reagents reported in literature were changed.Results:The structure of target compound was elucidated by element analysis,MS,(()~(1)HNMR) and IR.The total yield was 19.4%,higher than that reported in literature(7%).Conclution: The method is of low cost and of high yield,facile and suitable for industry.