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Citation: Lü Qiang, Tang Qinghong, Fu Qunmei, Dai Ming, Liu Shimeng, Zhu Weihong, Du Pa, Lü Long. Synthesis and Bioactivity of 1-Methyl-3-aryl-6-(trifluoromethyl) pyridazin-4(1H)-one Derivatives[J]. Chinese Journal of Organic Chemistry, ;2017, 37(2): 533-540. doi: 10.6023/cjoc201608023 shu

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

Lü Qiang ^a,b ,
Tang Qinghong ^b ,
Fu Qunmei ^b ,
Dai Ming ^b ,
Liu Shimeng ^b ,
Zhu Weihong ^a,*,, ,
Du Pa ^c ,
Lü Long ^b

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

Corresponding author: Zhu Weihong, whzhu@ecust.edu.cn
Received Date: 25 August 2016
Revised Date: 28 September 2016

Fund Project: National Key Technologies R & D Program 2016YFD0300708

Figures(4)

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.
- 3-aryl pyridazinone,
- protoporphyrinogen oxidase inhibitor,
- synthesis,
- biological activity
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