摘要/Abstract

基于新型杀虫剂氯虫苯甲酰胺的结构，设计合成出一系列新型含取代异噁唑单元的N-吡啶基吡唑酰胺衍生物，其目标化合物的结构均经核磁氢谱、碳谱及元素分析等方法确证.初步的室内杀虫活性测试数据表明，在500 μg/mL测试浓度下，所有目标化合物对粘虫的杀虫效果均达100%.4个化合物在100 μg/mL测试浓度下对粘虫的杀死率为80%~100%，2个化合物在20 μg/mL测试浓度下对粘虫仍有40%~50%的防效.5个化合物在500 μg/mL测试浓度下对蚜虫有较高的杀虫作用，其致死率为90%~100%.此外，2个化合物在500 μg/mL测试浓度下对朱砂叶螨有70%~80%的致死率.
关键词: 异噁唑, N-吡啶基吡唑, 合成, 生物活性
A series of new N-pyridylpyrazole amides bearing substituted isoxazole moiety were designed and prepared based on chlorantraniliprole. These compounds were structurally determined through ¹H NMR, ¹³C NMR and elemental analyses. Bioassay results displayed that all designed compounds showed a mortality rate of 100% towards Oriental armyworm at the dosage of 500 μg/mL. At the dosage of 100 μg/mL, the mortality rates of four compounds towards Oriental armyworm were 80%~100%. Two compounds had 40%~50% insecticidal activities towards Oriental armyworm at the concentration of 20 μg/mL. At the concentration of 500 μg/mL, five compounds demonstrated 90%~100% insecticidal activities against Aphis medicaginis. Moreover, at the dosage of 500 μg/mL, two compounds exhibited 70%~80% insecticidal activities against Tetranychus cinnabarinus.
Key words: isoxazole, N-pyridylpyrazole, synthesis, biological activity


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