盐酸度洛西汀的合成

Synthesis of duloxetine hydrochloride

目的:合成盐酸度洛西汀。方法:以2-乙酰噻吩、盐酸二甲胺和多聚甲醛为起始厚料,经Mannich反应、还原、拆分、成醚、成盐、两次重结晶等6步反应得到盐酸度洛西汀。结果:目标物经质谱、核磁共振氢谱及元素分析等确证其化学结构,总收率为7%。结论:本路线可简化实验操作,降低成本,适合工业化生产。

Objective: To synthesize duloxetine hydrochloride. Methods: Starting from 2-acetyhhiofuran plus dimethylamine hydrochloride and paraformaldehyde, duloxetine hydrochloride was obtained via a six-step chain reaction including Mannich reaction, reduction, separation, etherification, salt formation and dual crystallizations. Results: The structure of duloxetine was elucidated by MS, ~1H-NMR and element analysis. The total yield of duloxetine hydrochloride was 7%. Conclusion:A simple, easily controlled and low cost process for the synthesis of duloxetine is attained.