目的 對(duì)馬來酸氟吡汀的合成工藝進(jìn)行改進(jìn)研究。方法 以對(duì)氟芐胺和2-氨基-3-硝基-6-氯吡啶為起始原料，通過取代反應(yīng)合成中間體2-氨基-3-硝基-6-對(duì)氟芐胺基吡啶，然后再通過一鍋法合成馬來酸氟吡汀。結(jié)果 合成了目標(biāo)化合物馬來酸氟吡汀，并利用¹H-NMR、MS、IR等確證了結(jié)構(gòu)。本合成工藝的總收率為46.7%，質(zhì)量分?jǐn)?shù)為99.95%。結(jié)論 該合成工藝改進(jìn)后操作性好，條件溫和，更適于藥品的工業(yè)化生產(chǎn)。

Objective To study the improved method for synthesis of flupirtine maleate. Methods 4-Fluorobenzylamine and 2-amino-6-chloro-3-nitropyridine were used as the starting materials to synthesize N₂-(4-fluorophentl)-5-nitropyridine-2,6-diamine by substitution reaction. Flupirtine maleate was synthesized by one pot method. Results The target compound flupirtine maleate was achieved and characterized by ¹H-NMR, MS, and IR. The total yield of this synthetic route was 46.7%, and the purity of target compound was 99.95%. Conclusion The synthetic process has the advantages of simple operation, mild conditions, and suitable for industrial production as drugs.

天津市科技支撐計(jì)劃資助項(xiàng)目（14ZCZDSY00003）