盐酸去甲乌药碱的合成  

Synthesis of Higenamine Hydrocloride

作　　者：徐成 关东 

机构地区：[1]珠海润都制药股份有限公司,广东珠海519090

出　　处：《精细化工中间体》2015年第6期18-20,共3页Fine Chemical Intermediates

基　　金：原创国家1.1类新药盐酸去甲乌药碱的III期临床研究及产业化准备(项目编号:2011A080501012)

摘　　要：以4-甲氧基苯基乙酸和3,4-二甲氧基苯乙胺为起始原料经酰化、环合、还原、脱甲基4步反应得盐酸去甲乌药碱粗品,再通过精制、干燥得到去甲乌药碱精品,纯度达99%以上,质量达到药用标准。总收率为28.1%,其化学结构经~1H NMR、MS确证。该工艺操作简便,收率高,具有广泛的应用前景,适合工业化生产。Using 4-methoxy-phenyl acetic acid and 3,4-dimethoxy-phenylethylamine as the starting materials, the target compound was obtained via four steps including amidation, cyclization, reduction and demethylation with a yield of 28.1%. The structure of the final product was confirmed using ~1H NMR,^（13）C NMR, and MS. The process was simple with higher yield and a broad range of applications, and was suitable for industrial production.

关 键 词：4-甲氧基苯乙酸 3 4-二甲氧基苯乙胺 盐酸去甲乌药碱 

分 类 号：R914.5[医药卫生—药物化学]