Chemical Research in Chinese Universities ›› 2018, Vol. 34 ›› Issue (6): 918-922.doi: 10.1007/s40242-018-8148-4

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One-step Construction of Xanthone Scaffold Assisted by Microwave Irradiation to Optimize the Synthesis of DMXAA

JIANG Zhenlei1, LIU Jie1,2, ZHOU Fan1, ZHANG Jianrun1, LIU Zhijun1, ZHANG Chao1, CHEN Heru1,3   

  1. 1. Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, P. R. China;
    2. Department of Allergy, the Third Affiliated Hospital of Shenzhen University, Shenzhen 518020, P. R. China;
    3. Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Guangzhou 510632, P. R. China
  • Received:2018-05-07 Online:2018-12-01 Published:2018-08-23
  • Contact: CHEN Heru E-mail:thrchen@jnu.edu.cn
  • Supported by:
    Supported by the National Natural Science Foundation of China(No.81172982) and the Natural Science Foundation of Guangdong Province, China(No.2015A030311012).

Abstract: An efficient and concise synthesis of 5,6-dimethylxanthenone-4-acetic acid(DMXAA) was developed. The overall yield of this 3-step procedure was 82%. The key reaction is the one-step construction of xanthone scaffold between 2,5-dibromo-3,4-dimethylbenzoic acid and 2-hydroxyphenyl-acetic acid assisted by microwave irradiation.

Key words: 5,6-Dimethylxanthenone-4-acetic acid, Xanthone, Microwave irradiation, Anti-cancer