Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (1): 95-102.DOI: 10.6023/cjoc201710029 Previous Articles     Next Articles

Special Issue: 庆祝吴养洁院士九十华诞专辑 碳氢活化合辑2018-2019

Articles

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

穆兵a,b, 李敬亚d, 邹大鹏c, 吴豫生c,d, 常俊标a,c, 吴养洁c   

  1. a 郑州大学药学院 郑州 450001;
    b 郑州师范学院化学化工学院 郑州 450044;
    c 郑州大学化学与分子工程学院 郑州 450001;
    d 郑州泰基鸿诺医药股份有限公司 郑州 450001
  • 收稿日期:2017-10-24 修回日期:2017-11-27 发布日期:2017-11-28
  • 通讯作者: 吴豫生, 常俊标, 吴养洁 E-mail:yusheng.wu@tetranovglobal.com;changjunbiao@zzu.edu.cn;wyj@zzu.edu.cn
  • 基金资助:

    国家自然科学基金(No.21702191)、河南省科技攻关项目(No.172102210555)和河南省博士后科研(No.2014003)资助项目.

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

Mu Binga,b, Li Jingyad, Zou Dapengc, Wu Yushengc,d, Chang Junbiaoa,c, Wu Yangjiec   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b College of Chemistry and Chemical Engineering, Zhengzhou Normal University, Zhengzhou 450044;
    c College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001;
    d Tetranov Biopharm, LLC, Zhengzhou 450001
  • Received:2017-10-24 Revised:2017-11-27 Published:2017-11-28
  • Contact: 10.6023/cjoc201710029 E-mail:yusheng.wu@tetranovglobal.com;changjunbiao@zzu.edu.cn;wyj@zzu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21702191), the Scientific and Technological Project of Henan Province (No. 172102210555) and the Postdoctoral Science Foundation of Henan Province (No. 2014003).

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