马来酸氟吡汀的合成工艺改进研究

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。

Improvement of synthesis method for flupirtine maleate

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.