摘要/Abstract

3-芳基咪唑并[1，2-a]吡啶骨架广泛存在于药物结构中，在药物学方面具有重要的地位及在材料化学、有机化学等方面也具有潜在的应用价值.在含水介质中，利用醋酸钯催化咪唑并[1，2-a]吡啶及其衍生物与芳基/杂芳基氯代物的碳氢芳基化反应，简便、高效地合成系列3-芳基咪唑并[1，2-a]吡啶类化合物，并以较好至优秀的收率获得芳基化产品.该方法采用廉价易得的芳基/杂芳基氯代物和咪唑并[1，2-a]吡啶类化合物为偶联反应的底物，且底物的范围能够拓展至缺电子、富电子的芳基氯代物和杂芳基氯代物及多种基团取代的咪唑并[1，2-a]吡啶类化合物.
关键词: 碳氢芳基化, 咪唑并[1,2-a]吡啶, 3-芳基咪唑并[1,2-a]吡啶, 芳基/杂芳基氯代物, 含水介质
An efficient and practical protocol for palladium-catalyzed direct C—H bond arylation of imidazo[1,2-a]pyridines with cheap aryl/heteroaryl chlorides has been developed. Various imidazo[1,2-a]pyridines with electron-neutral, electron-poor, electron-rich, even sterically hindered aryl chlorides and heteroaryl chlorides were successfully applied to the reaction in aqueous medium to achieve the 3-arylimidazo[1,2-a]pyridines in mostly good to excellent yields, thus representing a signi?- cant advancement in the implementation of the direct C—H bond arylation of imidazo[1,2-a]pyridines with aryl chlorides.
Key words: C-H bond arylation, imidazo[1,2-a]pyridines, 3-arylimidazo[1,2-a]pyridines, aryl/heteroaryl chlorides, aqueous medium


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