瑞替加滨的合成  

Synthesis of Retigabine

作　　者：祁金龙[1] 张超[1] 吴茵[2] 刘保霞[1] 张海林[1] 

机构地区：[1]河北医科大学药理学教研室,河北石家庄050017 [2]河北省人民医院药学部,河北石家庄050051

出　　处：《中国医药工业杂志》2013年第3期223-225,共3页Chinese Journal of Pharmaceuticals

基　　金：国家"973"计划(2007CB512102);国家自然科学基金重点项目(30730031)

摘　　要：对硝基苯胺经酰化、硝基还原、氨基保护、硝化、氨基脱保护,与对氟苯甲醛缩合得到N-[2-硝基-4-(4-氟苯亚甲胺基)苯基]氨基甲酸乙酯,再用Pd/C催化氢化同时还原硝基和亚胺得到抗癫痫药瑞替加滨,总收率约44%。Retigabine, an anti-epileptic agent, was synthesized from 4-nitroaniline by acylation, reduction of nitro group, protection of amino group, nitration, deprotection of amino group, and then condensation with 4-fluorobenzaldehyde to give ethyl N- E4- E （4-fluorobenzylidene） amino] -2-nitrophenyl] carbamate, followed by Pd/C- catalyzed reduction of both nitro group and Schiffs base simultaneously with an overall yield about 44 %.

关 键 词：瑞替加滨 抗癫痫药 合成 

分 类 号：R971.6[医药卫生—药品]