吡啶基吡唑类杀虫剂Tyclopyrazoflor的合成与杀虫活性

Synthesis and insecticidal activity of pyridine pyrazole insecticide Tyclopyrazolor

本文以3-氯-1H-吡唑-4-胺为起始原料,经过8步反应制得Tyclopyrazoflor。采用’HNMR、3CNMR和MS对其结构进行了确证。测试了Tyclopyrazoflor对桃蚜、棉蚜、小菜蛾、朱砂叶螨、褐飞虱的杀虫活性。结果表明,该路线总收率为33.96%,适合大规模制备。Tyclopyrazoflor显示出了优异的杀虫活性。在质量浓度为10 mg·L^(-1)时,对桃蚜的致死率高达89.9%,对棉蚜具有74.8%的致死率,对小菜蛾有74.1%的致死率,质量浓度为100mg·L^(-1)时,对朱砂叶螨也有不错的防治效果。

The synthesis route of the novel pyridine pyrazole insecticide Tyclopyrazolor was optimized,which was synthesized through an 8-step reaction starting from 3-chloro-1H-pyrazole-4-amine.The structure of Tyclopyrazolor was confirmed using'H NMR,3C NMR,and MS.The insecticidal activity of Tyclopyrazolor against Myzus persicae,Aphis gossypii Glover,Plutella xylostella,Tetranychus cinnabarinus,and Nilaparvata lugens were tested.The results indicated that the total yield of this route was 33.96%,which was suitable for large-scale preparation,and Tycloprazoflor exhibited excellent insecticidal activity.When the mass concentration was 10 mg·L^(-1),the mortality rate of Tycloprazoflor against Myzus persicae,Aphis gossypi Glover and Plutella xylostella was 89.9%,74.8%and 74.1%,respectively.And Tycloprazoflor also had excellent activity against Plutlla xylostella at 100 mg·L^(-1).