摘要
以1,3-二氟苯为起始原料,依次经傅-克酰基化,1H-三氮唑取代,环氧化,胺解,4H-三氮唑环化,磷酸酯化和钯碳加氢反应等7步反应合成了福司氟康唑的主要杂质——2-(2,4-二氟苯基-1-(1H-1,2,4-三氮唑l-1-基)-3-(4H-1,2,4-三氮唑-4-基)-2-丙基磷酸二氢酯,纯度98%,总收率7.8%,其结构经1H NMR确证。
The main impurity of Fosfluconazole,2-(2,4-difluoro-Phenyl)-1-(1H-1,2,4-triazol-1-yl)-3-(4H-1,2,4-triazol-4-yl) propan-2-yl dihydrogen phosphateoxalate with purity of 98% and total yield of 7. 8%,was synthesized by a seven-step reaction of Friedel- Crafts reaction,nucleophilic substitution,Corey- Chaykovsky reaction,phosphorylation and catalytic hydrogenation,using 1,3-difluorobenzene as starting material. The structure was confirmed by1 H NMR.
出处
《合成化学》
CAS
CSCD
2016年第2期170-173,共4页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金资助项目(21002099)
西南科技大学杰出青年基金资助项目(13zx9104)
