盐酸去甲乌药碱的新合成法

A novel synthesis of higenamine hydrochloride

目的研究盐酸去甲乌药碱的新合成法。方法以盐酸多巴胺为起始原料,经苄基保护后与4-苄氧基苯乙酰氯反应得酰胺,再在三氯氧磷作用下环合,最后经还原和脱保护得目标化合物。结果与结论选用苄基为羟基的保护基团,利用催化氢化脱保护,该法较文献选用的甲基或者亚甲基保护法更为高效、便捷,总收率达48.4%。

Aim To get higenamine hydrochloride via a new concise synthetic route. Methods The benzylprotected dopamine was converted to the amide of 4-benzyloxyphenylacetic acid. Then the target compound was obtained from this amide via cyclization with POCl3, reduction, and deprotection. Results and conclu- sion Instead of methyl or methylene protection groups reported in literatures, benzyl was employed to protect all the hydroxyl groups in this paper. This novel synthesis is more efficient and convenient in an overall yield of 48.4 %.