(±)-盐酸阿朴吗啡的合成

Synthesis of (±)-Apomorphine Hydrochloride

异喹啉在氰化钾作用下和苯甲酰氯经Reissert反应、偶联反应和消除反应、与碘化钾反应成季铵盐、还原成四氢异喹啉、硝基还原、重氮化后经Pschorr环化反应制得(±)-阿朴吗啡二甲醚,再经氢溴酸脱甲基及与盐酸成盐得到(±)-盐酸阿朴吗啡,总收率31%。

（±）-Apomorphine hydrochloride was synthesized from isoquinoline by Reissert reaction, coupling reaction, elimination, reaction with CH3I, reduction, diazotization and Pschorr reaction, respectively to give （±） -10,11- dimethoxyaponorphine, which was subjected to demethylation and then HCl salt formation with an overall yield of 31%.