马来酸氟吡汀的合成工艺改进研究  

Improvement of synthesis method for flupirtine maleate

作　　者：董凯[1] 

机构地区：[1]天津红日药业股份有限公司,天津武清301700

出　　处：《现代药物与临床》2017年第9期1605-1608,共4页Drugs & Clinic

基　　金：天津市科技支撑计划资助项目(14ZCZDSY00003)

摘　　要：目的对马来酸氟吡汀的合成工艺进行改进研究。方法以对氟苄胺和2-氨基-3-硝基-6-氯吡啶为起始原料,通过取代反应合成中间体2-氨基-3-硝基-6-对氟苄胺基吡啶,然后再通过一锅法合成马来酸氟吡汀。结果合成了目标化合物马来酸氟吡汀,并利用1H-NMR、MS、IR等确证了结构。本合成工艺的总收率为46.7%,质量分数为99.95%。结论该合成工艺改进后操作性好,条件温和,更适于药品的工业化生产。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.

关 键 词：马来酸氟吡汀 对氟苄胺 2-氨基-3-硝基-6-氯吡啶 工业化生产 

分 类 号：R914[医药卫生—药物化学]