马来酸氟吡汀的一锅法合成

摘要

目的：改进马来酸氟吡汀的合成工艺。方法以2，6－二氯－3－硝基吡啶为原料，经氨解、缩合、还原、酰化、成盐五步“一锅法”制得马来酸氟吡汀，收率76％。结果与结论目标化合物的结构经1 H－NMR和MS谱确证。改进后的工艺成本低廉，操作简便，有利于工业化生产。%ABSTRACT:OBJECTIVE To improve the synthetic procedure of flupirtine maleate .METHODS Flupirtine maleate,an non-opioid analgesic acting on the central nervous system ,was prepared from 2,6-dichloro-3-nitropyridine by aminolysis, condensation, reduction, acylation and acidification by one-pot process with a yield of 76%.RE-SULTS and CONCLUSION The structure of target compound was confirmed by 1 H-NMR and MS spectra.The improved process is easy for synthesis and suitable for industrial manufacturing owing to its advantages of low cost , convenient operations by one-pot process.