摘要
在药物分子设计中,含氟基团的引入能够显著改善分子的亲脂性、代谢稳定性以及膜穿透能力.电化学三氟甲基化作为一种绿色高效的合成策略,已成为构建含三氟甲基分子的重要手段.作为最具代表性的三氟甲基化试剂,Langlois试剂凭借其原料易得、反应条件温和、操作简便等优势,在电化学介导的有机小分子三氟甲基化反应中展现出广阔的应用前景.从C—H键的三氟甲基化、O—H三氟甲基化以及S—H三氟甲基化三个方向,系统评述了近5年该试剂在电化学三氟甲基化反应中的应用进展,重点关注反应机理、区域选择性和底物适用性等关键科学问题.
In drug molecule design,the introduction of fluorinated groups can significantly improve the lipophilicity,metabolic stability,and membrane penetration ability of molecules.Electrochemical trifluoromethylation,as a green and efficient synthesis strategy,has become an important means of constructing trifluoromethyl containing molecules.As the most representative trifluoromethylation reagent,Langlois reagent has shown broad application prospects in electrochemically mediated trifluoromethylation reactions of small organic molecules due to its advantages of easy availability of raw materials,mild reaction conditions,and easy operation.This article systematically reviews the research progress of this reagent in electrochemical trifluoromethylation reactions in the past five years from three directions:C—H bond trifluoromethylation,O—H trifluoromethylation,and S—H trifluoromethylation,with a focus on key scientific issues such as reaction mechanism,regioselectivity,and substrate applicability.
作者
何卫保
易荣楠
杨梓
伍智林
何卫民
He Weibao;Yi Rongnan;Yang Zi;Wu Zhilin;He Weimin(Research Center for Technical and Vocational Education Studies,Hunan Chemical Vocational Technology College,Zhuzhou 412000;Key Laboratory of Food&Environment&Drug Monitoring and Testing of Universities in Hunan Province,Hunan Police Academy,Changsha 410138;Hunan Provincial University Key Laboratory of the Fundamental and Clinical Research on Functional Nucleic Acid,Changsha Medical University,Changsha 410219;School of Chemistry and Chemical Engineering,University of South China,Hengyang 421001)
出处
《有机化学》
北大核心
2025年第10期3534-3545,共12页
Chinese Journal of Organic Chemistry
基金
长沙市自然科学基金(No.104872)资助项目。
