德拉沙星中间体2,6-二氨基-3,5-二氟吡啶的合成

Synthesis of 2,6-diamino-3,5-difluoropyridine as an Intermediate of Deoxafloxacin

2,6-二氨基-3,5-二氟吡啶由2,3,5,6-四氟吡啶为起始物料,经二次取代一次脱保护等步骤制得。结果得到了淡黄色的目标化合物,摩尔收率80%以上。结论该工艺操作简便,收率较高,产品纯度较高(99.0%以上)。产物的结构经1HNMR和19 FNMR得到确证。

2,6-Diamino-3,5-difluoropyridine is prepared from 2,3,5,6-tetrafluoropyridine as a starting material by a second substitution and a deprotection step.As a result,a pale yellow target compound was obtained with a molar yield of 80%or more.Conclusion The process is simple and easy to operate,with high yield and high product purity(99.0%or more).The structure of the product was confirmed by 1H NMR and 19 F NMR.