Abstract: Based on the synthetic method of dipivefrin hydrochloride reported in literatures,the existing process was selected and optimized.In this work,the optimized method is a six-step synthetic route,including Friedel-Crafts reaction,esterification,N-alkylation,reduction of carbonyl,hydrogenation and recrystallization with the cheap and commercial available catechol as the starting material.The total yield of the optimized route is 43.4%,significantly improving the yield of the original process(23.6%),and the purity of the final product dipivefrin hydrochloride is 98.98%.Therefore,the optimized reaction method is in accordance with the requirements of industrial production.The structures of the target compound were confirmed by MS,IR,¹H-NMR,and ¹³C-NMR.

Key words: adrenoceptor agonists, dipivefrin hydrochloride, process improvement

摘要： 对盐酸地匹福林合成工艺进行研究，并对其进行纯度检测和结构确证。以邻苯二酚为主要起始原料，与氯乙酰氯发生傅克酰化反应得到3，4-二羟基-2'-氯苯乙酮，经特戊酰氯酯化得到4-（2-氯乙酰基）-1，2-二特戊酸苯酯，与N-甲基苄胺亲核取代得到1-（3，4-二特戊酰氧苯基）-2-（N-苄基甲基氨基）-1-酮，再经羰基还原、氢化脱苄、重结晶制得盐酸地匹福林。改进后的路线总收率为43.4%，显著提高了原工艺收率（23.6%），HPLC纯度达到98.98%，并通过MS、IR、¹H-NMR、¹³C-NMR进行了结构确证。

关键词: 肾上腺素受体激动剂, 盐酸地匹福林, 工艺改进