可乐定合成的新方法

A new Synthetic Method of Clonidine

摘要: 报道了以邻氯硝基苯为原料合成可乐定(1)的新方法。邻氯硝基苯先经锌粉、氯化铵还原和甲酸、乙酐甲酰化得N-(2-氯苯基)-N-羟基甲酰胺(3),再经氯化亚砜、五氯化磷氯化,然后与己二胺环合得(1).此法操作简便,成本较低,总收率21.8%。

Abstract: A new synthetic method of clonidine (I) is reported from o-chloronitrobenzeneas the starting material .N-(2-chloro-phenyl)-N-hydroxyformamide is prepared from o-chl-oronitrobenzene as reduction with formic acid/acetic anhydride . is converted to clonidine