张雅婷, 高占宇, 徐婧, 刘秉知, 秦培文, 纪明山. 新型吡唑丙烯腈酯类衍生物的合成及其杀螨活性[J]. 农药学学报, 2024, 26(4): 716-723. DOI: 10.16801/j.issn.1008-7303.2024.0061
    引用本文: 张雅婷, 高占宇, 徐婧, 刘秉知, 秦培文, 纪明山. 新型吡唑丙烯腈酯类衍生物的合成及其杀螨活性[J]. 农药学学报, 2024, 26(4): 716-723. DOI: 10.16801/j.issn.1008-7303.2024.0061
    ZHANG Yating, GAO Zhanyu, XU Jing, LIU Bingzhi, QIN Peiwen, JI Mingshan. Synthesis and acaricidal activity of novel pyrazole acrylonitrile derivatives[J]. Chinese Journal of Pesticide Science, 2024, 26(4): 716-723. DOI: 10.16801/j.issn.1008-7303.2024.0061
    Citation: ZHANG Yating, GAO Zhanyu, XU Jing, LIU Bingzhi, QIN Peiwen, JI Mingshan. Synthesis and acaricidal activity of novel pyrazole acrylonitrile derivatives[J]. Chinese Journal of Pesticide Science, 2024, 26(4): 716-723. DOI: 10.16801/j.issn.1008-7303.2024.0061

    新型吡唑丙烯腈酯类衍生物的合成及其杀螨活性

    Synthesis and acaricidal activity of novel pyrazole acrylonitrile derivatives

    • 摘要: 为了获得活性更好的吡唑丙烯腈类杀螨剂,采用 1,3-二甲基-1H-吡唑-5-羧酸乙酯为原料,通过布兰克氯甲基化、脱卤、缩合和酯化4步反应合成了 17 个新型吡唑丙烯腈酯类衍生物,并采用浸虫法测定目标化合物对朱砂叶螨Tetranychus cinnabarinus的杀螨活性,计算死亡率和致死中浓度 (LC50)。结果表明,目标化合物具有优良的杀螨活性,其中化合物 5q5k 相比于商品化杀螨剂腈吡螨酯 (LC50 = 0.61 mg/L) 具有更高的杀螨活性,其LC50 值分别为 0.17 和 0.22 mg/L。

       

      Abstract: In order to obtain acaricides of pyrazole acrylonitrile with better acaricidal activity for mitecontrol, seventeen novel ester derivatives were synthesized via four steps of Blanc chloromethylation reaction, dehalogenation reaction, condensation reaction and esterification reaction using ethyl 1,3-dimethyl-1H-pyrazole-5-carboxylate as the starting material. Furthermore, their acaricidal activity against Tetranychus cinnabarinus was assessed by immersion test, and the mortality rate and lethal mid-range concentration LC50 were calculated. The results show that the target compounds display excellent acaricidal activity against T. cinnabarinus, and compared with the commercial pesticide cyenopyrafen (LC50 = 0.61 mg/L), compounds 5q and 5k possess significantly higher acaricidal activity against T. cinnabarinus with LC50 values of 0.17 and 0.22 mg/L, respectively.

       

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