Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (2): 533-540.DOI: 10.6023/cjoc201608023 Previous Articles     Next Articles



吕强a,b, 唐庆红b, 付群梅b, 戴明b, 刘世梦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 上海 200032;
    c 上海应用技术大学 化学与环境工程学院 上海 201418
  • 收稿日期:2016-08-25 修回日期:2016-09-28 发布日期:2016-10-09
  • 通讯作者: 朱为宏
  • 基金资助:


Synthesis and Bioactivity of 1-Methyl-3-aryl-6-(trifluoromethyl)pyridazin-4(1H)-one Derivatives

Lü Qianga,b, Tang Qinghongb, Fu Qunmeib, Dai Mingb, Liu Shimengb, Zhu Weihonga, Du Pac, Lü Longb   

  1. a School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai 200237;
    b 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:2016-08-25 Revised:2016-09-28 Published:2016-10-09
  • Supported by:

    Project supported by National Key Technologies R&D Program (No. 2016YFD0300708).

A novel series of 3-aryl pyridazinone was proposed on the base of structure activity relationships of diverse protoporphyrinogen oxidase inhibitors. Synthetic method of 3-aryl pyridazinones was investigated and 9 compounds were synthesized for interior screening test of herbicidal activity and crop safety. Bioassay results showed that most of 3-aryl-pyridazi-nones exhibit excellent pre- or post-emergence herbicidal activity. Herein, 3-(2,4-dichloro-5-(cyclopentyloxy)phenyl)-1-methyl-6-(trifluoro methyl) pyridazin-4(1H)-one (Ie) with high activity was selected as a post-herbicide candidate into corn field trial. The results showed that Ie exhibited higher total effective rate against weeds at the dose of 60 g a.i./hm2 than mesotrione at 105 g a.i./hm2, and safety to corn after emergence as well.

Key words: 3-aryl pyridazinone, protoporphyrinogen oxidase inhibitor, synthesis, biological activity