有机化学 ›› 2014, Vol. 34 ›› Issue (4): 662-680.DOI: 10.6023/cjoc201310039 上一篇    下一篇

综述与进展

含氟药物研究进展和芳(杂)环氟化及N(n=1,2,3)氟甲基化新方法

张霁, 金传飞, 张英俊   

  1. 广东东阳光集团 药业研究院 东莞 523871
  • 收稿日期:2013-10-29 修回日期:2013-12-09 发布日期:2013-12-19
  • 通讯作者: 张霁 E-mail:zhangji@hecpharm.com
  • 基金资助:

    广东省引进创新科研团队计划资助项目

Recent Advances in Research and Development of Fluorinated Drugs and New Methods for Fluorination, Mono-, Di-and Tri-fluoromethylation

Zhang Ji, Jin Chuanfei, Zhang Yingjun   

  1. HEC Pharm Group, HEC Research and Development Center, Dongguan 523871
  • Received:2013-10-29 Revised:2013-12-09 Published:2013-12-19
  • Supported by:

    Project supported by the Introduction of Innovative R&D Team Program of Guangdong Province.

论述了最近几年含氟药物的最新研究成果和含氟新药的研究概况,从药物化学工作者的角度对芳(杂环)的氟化反应,氟甲基化、二氟甲基化和三氟甲基化反应进展和亮点做了分析归纳和总结,对一些金属催化的氟化新反应的机理进行了简单的阐述. 指出药物结构优化中充分利用氟化学的最新研究成果是一条值得探索的捷径.

关键词: 氟, 含氟药物, 氟化反应, 三氟甲基化, 二氟甲基化, 一氟甲基化, 药物设计

This review outlines the recent advances of fluorinated drugs and latest research overview from the perspective of a medicinal chemist wherein the synthesis and use of trifluoromethylation, difluoromethylation, monofluoromethylation and fluorinated aromatic (heterocyclic) compounds are highlighted. It is pointed out that the full use of the latest progress in fluorine chemistry provides a shortcut to new fluorinated compounds or previously difficult to prepare compounds which is worth exploring for drug discovery.

Key words: fluorine, fluorinated drugs, fluorination, trifluoromethylation, difluoromethylation, monofluoromethylation, drug design