在含水介质中钯高效催化咪唑并[1,2-a]吡啶类化合物与芳基氯代物的碳氢芳基化反应（英文）  

Efficient Pd-Catalyzed Direct C—H Bond Arylation of Imidazo-[1,2-a]pyridines with Aryl Chlorides in Aqueous Medium

作　　者：穆兵 李敬亚 邹大鹏[4] 吴豫生[4,3] 常俊标 吴养洁[4] 

机构地区：[1]郑州大学药学院,郑州450001 [2]郑州师范学院化学化工学院,郑州450044 [3]郑州泰基鸿诺医药股份有限公司,郑州450001 [4]郑州大学化学与分子工程学院,郑州450001

出　　处：《有机化学》2018年第1期95-102,共8页Chinese Journal of Organic Chemistry

基　　金：supported by the National Natural Science Foundation of China(No.21702191);the Scientific and Technological Project of Henan Province(No.172102210555);the Postdoctoral Science Foundation of Henan Province(No.2014003)~~

摘　　要：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.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 significant advancement in the implementation of the direct C—H bond arylation of imidazo[1,2-a]pyridines with aryl chlorides.

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 

分 类 号：O621.251[理学—有机化学]