盐酸去甲乌药碱的合成

Synthesis of Higenamine Hydrocloride

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.