Chinese Journal of Organic Chemistry >
Synthesis and Bioactivity of 1-Methyl-3-aryl-6-(trifluoromethyl)pyridazin-4(1H)-one Derivatives
Received date: 2016-08-25
Revised date: 2016-09-28
Online 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.
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
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