瑞替加滨的合成工艺改进  

Improvement for Synthesis of Retigabine

作　　者：曹云峰[1] 王辉[1] 王俊臣[1] 

机构地区：[1]河南天方药业股份有限公司,河南驻马店463000

出　　处：《广州化工》2015年第6期95-97,共3页GuangZhou Chemical Industry

摘　　要：对抗癫痫原料药瑞替加滨的合成工艺进行了改进,以4-氯-1,2-二硝基苯代替2-硝基-5-氟苯胺为起始原料,经缩合、还原、酰化三步反应得到目标产物瑞替加滨,化学结构经1H NMR、HRMS及元素分析确证。与文献报道相比,本工艺操作过程简单,步骤短,收率高,没有用到昂贵试剂,适于工业化生产。改进后的工艺总收率为67.1%,产品纯度在99%以上(HPLC),符合瑞替加滨原料药的药用要求。The improved process for the synthesis of retigabine as an anti-epileptic agent was introduced.The target compound was synthesized from 4-chloro-1, 2-dinitrobenzene instead of 2-nitro-5-fluoro aniline via condensation, reduction and aceylation.The structure of retigabine was confirmed by 1 H NMR, HRMS and elemental analysis.Compared with reported literature, this process was simple with short steps, high yield, and without using expensive reagents.It is suitable for industrial production.The overall yield of the improved process was 67.1%.The purity of retigabine was above 99%（ HPLC） and met standards required for pharmaceutical use.

关 键 词：瑞替加滨 合成 抗癫痫药 

分 类 号：TQ460.6[化学工程—制药化工]