Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (6): 1342-1347.DOI: 10.6023/cjoc201412034 Previous Articles     Next Articles



吕强a,b, 芦昕婷b, 张基胜b, 张志国b, 朱为宏a, 杜葩c, 吕龙b   

  1. a 华东理工大学化学与分子工程学院 上海 200237;
    b 中国科学院上海有机化学研究所 有机氟化学重点实验室 上海 200032;
    c 上海应用技术学院化学与环境工程学院 上海201418
  • 收稿日期:2014-12-19 修回日期:2015-02-05 发布日期:2015-02-10
  • 通讯作者: 杜葩
  • 基金资助:

    "十二五"国家科技支撑计划(No. 2011BAE06B02)资助项目.

Synthesis and Bioactivity of 2-(Pyridyl-2-formyl)pyrimidine Derivatives

Lü Qianga,b, Lu Xintingb, Zhang Jishengb, Zhang Zhiguob, Zhu Weihonga, Du Pac, Lü Longb   

  1. a School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai 200237;
    b Key laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Science, Shanghai 200032;
    c School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418
  • Received:2014-12-19 Revised:2015-02-05 Published:2015-02-10
  • Supported by:

    Project supported by the National Key Technologies R&D Program (No. 2011BAE06B02)

Based on the structural optimization of 2-benzoyl pyrimidine derivatives, eight 2-(pyridyl-2-formyl)pyrimidine derivatives have been specifically designed and synthesized for evaluation of their interior fungicidal activities. 2-(Pyridyl-2-formyl)pyrimidine derivatives show excellent activity against cucumber downy mildew and cucumber powdery mildew. Among them, 2-chloro-N-{[2-(4,6-dimethoxypyrimidine-2-carbonyl)pyridin-3-yl]oxy}-N-methylbenzamide (6b) exhibits comparable protective and curative activity against cucumber powdery mildew to reference Metrafenone. EC50 and EC90 of the protective activity are 0.69 and 2.89 mg/L, respectively, and those of curative activity are 0.13 and 1.6 mg/L. 6b also shows excellent upward translocation in plants and rainfast performance. Especially, its persistent efficacy period of the protective activity against cucumber powdery mildew can last 15~20 d.

Key words: 2-(pyridyl-2-formyl)pyrimidine, synthesis, fungicidal activity