瑞替加滨的合成

Synthesis of Retigabine

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 %.