Synthesis Candidates Herbicide Through Optimization Quinclorac Containing 3-Methyl-1H-pyrazol-5-yl

文献类型： 外文期刊

第一作者： Luo, Dingfeng

作者： Luo, Dingfeng;Zhou, Xiaomao;Li, Zuren;Bai, Lianyang;Luo, Dingfeng;Bai, Haodong;Zhou, Xiaomao;Wu, Lamei;Zhang, Chengjia;Wu, Zhongchi;Li, Zuren;Bai, Lianyang

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关键词： quinclorac; intermediate derivatization methods (IDMs); barnyard grass; herbicidal activity; field assay

期刊名称：FRONTIERS IN CHEMISTRY （ 影响因子：3.693； 五年影响因子：4.204 ）

ISSN： 2296-2646

年卷期： 2021 年 9 卷

页码：

收录情况： SCI

摘要： To enhance quinclorac potency, twenty-five derivatives were synthesized containing 3-methyl-1H-pyrazol-5-yl by intermediate derivatization methods (IDMs). These compounds were confirmed by melting point (mp), (HNMR)-H-1, (CNMR)-C-13, and HRMS. The compound 1,3-dimethyl-1H-pyrazol-5-yl 3,7-dichloroquinoline-8-carboxylate (10a) was determined by X-ray diffraction. The activity of these compounds substituent on the phenyl was: electron-drawing group > neutral group > donor-drawing group, the results was like that of substituted benzyl group on pyrazole. The herbicidal activity assays showed that compounds 1-(2-fluorophenyl)-3-methyl-1H-pyrazol-5-yl 3,7-dichloroquinoline-8-carboxylate (8l, EC50 = 10.53 g/ha) and 10a (EC50 = 10.37 g/ha) had an excellent inhibition effect on barnyard grass in greenhouse experiment. Greenhouse safety experiment of rice exhibited almost no difference in plant height and fresh weight treated 10a at stage 1 similar to 2-leaf of rice after 14 days but 8l had a detrimental effect. Two season field assays showed 10a herbicidal activity on barnyard grass at 150 g/ha as equal as 300 g/ha quinclorac in fields in 2019 and 2020. The study demonstrated that 10a could be further researched as a potential herbicide to control barnyard grass in fields.

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