咪唑并[1,2-a]吡啶的碳氢三氟甲基化研究进展

Research Progress of C—H Trifluoromethylation of Imidazo[1,2-a]pyridines

三氟甲基取代氮杂芳烃结构广泛存在于医药、农药等药物分子中。因此,开发有效的引入三氟甲基的方法持续受到关注。在这些方法中,通过直接碳氢官能化策略在分子中引入三氟甲基已成为有机氟化学中的研究热点。C3位取代的咪唑并[1,2-a]吡啶类氮杂环因其较好的生物活性,引起了化学工作者的广泛关注。综述了到目前为止咪唑并[1,2-a]吡啶C3位的三氟甲基化反应,并从催化策略上对反应进行总结、归纳及分析,并对该反应的发展做出展望。

CF_(3)-containing heteroarenes have been widely used in pharmaceuticals,pesticide and other drug molecules.As a consequence,the development of efficient trifluoromethylation methods has attracted continuous interest in organic synthesis.Among them,the most conventional protocol is the direct C—H trifluoromethylation methods.C3-substituted imidazo[1,2-a]pyridines have attracted extensive attention of chemists because of their good biological activity.The trifluoromethylation of imidazo[1,2-a]pyridines at C3 is reviewed.Base on the catalytic strategy,the reaction is summarized and analyzed,and the development of this reaction is prospected.