盐酸度洛西汀的合成  

Synthesis of duloxetine hydrochloride

作　　者：高丽梅[1] 朱凤昌[1] 宋丹青[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所,北京100050

出　　处：《中国新药杂志》2005年第1期74-76,共3页Chinese Journal of New Drugs

摘　　要：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.

关 键 词：盐酸度洛西汀 药物合成 抑郁症 

分 类 号：R914.5[医药卫生—药物化学] R972.4[医药卫生—药学]