抗癫痫药瑞替加滨的合成工艺改进

Improvement to the Synthesis of Retigabine,an Antiepileptic Drug

抗癫痫原料药瑞替加滨现有的合成工艺进行了分析,以可行的工艺为基础,进行了优化和改进。确定以对硝基苯胺和氯甲酸乙酯为起始原料,经取代、还原、缩合等反应得到目标产物瑞替加滨二盐酸盐,目标化合物的结构经熔点(MP)、核磁共振氢谱(1H-NMR)和质谱(MS)确证。与文献报道相比,本工艺避免了使用高温,高压的反应条件和有危险性的催化剂,以常温、常压和常用试剂代替。所使用的原料易得,反应条件温和,操作安全,可作为工业化生产一个新的选择。

In this article,the current synthesis technique of retigabine that is a prescription anti-epilepsy medication was analyzed. The synthesis route was improved based on the practical processing route. The target product was synthesized from nitroaniline and ethyl chlorocarbonate via substitution,reduction and condensation reaction,et al. the structure of retigabine dihydrochloride was comfired by melting point,1H-NMR and MS. Compared with the reported literature,this method avoides the use of the reaction conditions of high temperature,high pressure and dangerous catalysts,which replaced by normal temperature,atmospheric pressure and common reagents. This synthesis processing has the advantages of easily available raw materials,mild reactive conditions,and operational safety. This method can be used for industrial production as a new choice.