含酰脲基团的苯基吡唑类杀虫剂的合成及生物活性

Synthesis and Insecticidal Activity Studies of Phenylpyrazole Derivatives Containing an Acylurea Moiety

[目的]为了获得具有较好杀虫活性的化合物。[方法]基于活性片段拼接和中间体衍生化法,将苯基吡唑与酰脲基团结合。[结果]合成了8个结构新颖的5-酰脲基苯基吡唑类化合物,并对其进行了杀虫活性测试,其中化合物4d在5 mg/kg下对小菜蛾的活性为100%,化合物4d、4g在0.25 mg/kg下对蚊幼虫的活性为100%。[结论]目标化合物具有较好的杀虫活性,但相对于氟虫腈活性有所降低。

[Aims] The paper aims to discover compounds with good insecticidal activity.[Methods] Based on the Intermediate Derivatization Method and fragment combination,phenylpyrazole and acylurea groups were combined.[Results] Eight structure novel phenylpyrazole derivatives containing an acylurea moiety were synthesized,and the insecticidal activities were evaluated.The activity of compound 4 d against diamondback moth was 100% at 5 mg/kg,and the activity of compounds 4 d and 4 g against mosquito larvae was 100% at 0.25 mg/kg.[Conclusions] The target compounds show good insecticidal activity,however,the activity is some lower than fipronil.