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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 improve the synthesis of flupirtine maleate. Methods Starting from p-fluorobenzylamine and 2-amino-3-nitro-6-chloropyridine, the intermediate 2-amino-3-nitro-6-p-fluorobenzylaminopyridine was synthesized by substitution reaction, Flupirtine maleate was synthesized by one-pot method. Results The target compound, flupirtine maleate, was synthesized and confirmed by 1H-NMR, MS, IR and so on. The total yield of the synthesis process was 46.7% and the mass fraction was 99.95%. Conclusion The synthetic process improved operability, mild conditions, more suitable for industrial production of drugs.