Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (11): 3009-3015.DOI: 10.6023/cjoc201806035 Previous Articles     Next Articles

Special Issue: 有机小分子-金属协同催化



袁硕a,b,c, 王四喜a, 陈锦杰a, 赵龙飞a,b,c, 余斌a,b,c,d, 刘宏民a,b,c   

  1. a 郑州大学药学院 郑州 450001;
    b 新药创制与药物安全性评价河南省协同创新中心 郑州 450001;
    c 教育部药物关键制备技术重点实验室 郑州 450001;
    d 广东省新药筛选重点实验室 广州 510033
  • 收稿日期:2018-06-21 修回日期:2018-07-16 发布日期:2018-07-24
  • 通讯作者: 余斌, 刘宏民;
  • 基金资助:


Aniline-Promoted Synthesis of Isobenzofuranone Derivatives

Yuan Shuoa,b,c, Wang Sixia, Chen Jinjiea, Zhao Longfeia,b,c, Yu Bina,b,c,d, Liu Hongmina,b,c   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b Co-Innovation Center of Henan Province for New Drug R & D and Preclinical Safety, Zhengzhou 450001;
    c Key Laboratory of Technology of Drug Preparation, Ministry of Education, Zhengzhou 450001;
    d Guangdong Provincial Key Laboratory of New Drug Screening, Guangzhou 510033
  • Received:2018-06-21 Revised:2018-07-16 Published:2018-07-24
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 81430085, 81773562, 81703326), the National Key Research Program of Proteins (No. 2016YFA0501800), the Scientific Program of Henan Province (No. 182102310123), the China Postdoctoral Science Foundation (No. 2018M630840), the Open Project of Guangdong Provincial Key Laboratory of New Drug Screening (No. GDKLNDS-2018OF006), the Key Research Program of Higher Education of Henan Province (No. 18B350009), and the Undergraduate Innovation and Entrepreneurship Training Program of Zhengzhou University (No. 201810459101).

Isobenzofuranone derivatives are widely found in nature and have shown diverse biological activities. In this work, the aniline-promoted synthesis of isobenzofuranone derivatives starting from 2-carboxybenzaldehyde and substituted acetophenones under mild reaction conditions is reported. This method has broad substrate scope, high yields, and is operationally convenient, and therefore could serve as an attractive strategy for practical synthesis of isobenzofuranone derivatives.

Key words: isobenzofuranone derivatives, aniline, cascade reactions