The synthesis process of retigabine as an antiepileptic drug was improved. The target product was synthesized from nitroaniline and ethyl chlorocarbonate via substitution, reduction and condensation reactions. The structure of retigabine dihydrochloride was confirmed by melting point, 1H NMR and MS. Compared with the reported literature, this method avoided the reaction condition of high temperature, high pressure and dangerous catalysts, which was replaced by normal temperature, atmospheric pressure and common reagents. This synthesis process has many advantages, such as easily available raw materials, mild reactive conditions and good operational safety. This method can be used in the industrial production of retigabine.%对抗癫痫原料药瑞替加滨的合成工艺进行了改进,对硝基苯胺和氯甲酸乙酯为起始原料,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.
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