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

作　　者：赵奇奇[1,2] 黄世盛 李永强[1] 熊丽霞[1] 刘玉秀[1] 张朋丽 李亚玲 刘爱玲[1,3] 汪清民 ZHAO Qi-qi;HUANG Shi-sheng;LI Yong-qiang;XIONG Li-xia;LIU Yu-xiu;ZHANG Peng-li;LI Ya-ling;LIU Ai-ling;WANG Qing-min(State Key Laboratory of Elemento-Organic Chemistry,College of Chemistry,Collaborative Innovation Center of Chemical Science and Engineering(Tianjin),Nankai University,Tianjin 300071,China;Patent Examination Cooperation(Beijing)Center of the Patent Office,CNIPA,Beijing 100160,China;Tianjin Ringpu Bio-tcchnology Co.,Ltd.,Tianjin 300000,China)

机构地区：[1]南开大学元素有机化学国家重点实验室化学学院天津化学化工协同创新中心,天津300071 [2]国家知识产权局专利局专利审查协作北京中心,北京100160 [3]天津瑞普生物技术股份有限公司,天津300000

出　　处：《农药》2020年第9期636-638,共3页Agrochemicals

基　　金：国家自然科学基金(21672117)。

摘　　要：[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.

关 键 词：苯基吡唑 酰脲 杀虫活性 

分 类 号：TQ460.3[化学工程—制药化工]