Chinese Journal of Organic Chemistry ›› 2022, Vol. 42 ›› Issue (5): 1551-1556.DOI: 10.6023/cjoc202110007 Previous Articles     Next Articles



楚治良a, 陈晖娟a, 单帅a, 王晓娜a, 高春芳a, 渠桂荣b, 刘忠于a,*(), 郭海明b,*()   

  1. a 中国人民解放军联勤保障部队第989医院 河南洛阳 471031
    b 河南师范大学化学化工学院 河南新乡 453007
  • 收稿日期:2021-10-08 修回日期:2022-01-26 发布日期:2022-02-10
  • 通讯作者: 刘忠于, 郭海明
  • 基金资助:
    国家自然科学基金(U1604283); 国家科技重大专项(2014ZX09J14101-01A); 洛阳市科技计划医疗卫生(1720001A-8)

One-Step Synthesis of 1,2,4-Triazolo[3,4-i]purine Derivatives

Zhiliang Chua, Huijuan Chena, Shuai Shana, Xiaona Wanga, Chunfang Gaoa, Guirong Qub, Zhongyu Liua(), Haiming Guob()   

  1. a The 989th Hospital of the Joint Logistics Support Force of Chinese People's Liberation Army, Luoyang, Henan 471031
    b School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007
  • Received:2021-10-08 Revised:2022-01-26 Published:2022-02-10
  • Contact: Zhongyu Liu, Haiming Guo
  • Supported by:
    National Natural Science Foundation of China(U1604283); National Science and Technology Major Project(2014ZX09J14101-01A); Medical and Health Project of Luoyang Science and Technology Plan(1720001A-8)

1,2,4-Triazolo[3,4-i]purine derivatives are potential xanthine oxidase (XO) inhibitors and expected to be used in the treatment of gout. A new one-step method for the preparation of 1,2,4-triazolo[3,4-i]purine derivatives has been reported. Seventeen novel 1,2,4-triazolo[3,4-i]purine derivatives were synthesized with 6-hydrazinyl-N9-substituted purine and aliphatic monocarboxylic acid as starting materials and anhydrous magnesium sulfate as dehydrating agent. The method is easy to operate without using other catalysts and oxidants, and the yield is good. Meanwhile, the factors affecting the reaction were discussed, which laid a foundation for the study of 1,2,4-triazolo[3,4-i]purine compounds

Key words: 6-hydrazinyl-N9-substituted purine, aliphatic monocarboxylic acid, 1,2,4-triazolo[3,4-i]purine derivative