新型芳氧吡啶肟醚类化合物的设计、合成和杀虫活性  

Design,synthesis and insecticidal activities of aryloxypyridinyl ethanone oxime ethers

作　　者：杜士杰[1] 杨冬燕 万川[3] 赵峰海 覃兆海[3] DU Shijie;YANG Dongyan;WAN Chuan;ZHAO Fenghai;QIN Zhaohai(Guizhou Provincial Key Laboratory for Biodiversity Conservation and Utilization in the Fanjing Mountain Region,Tongren University,Tongren 554300,Guizhou Province,China;College of Chemistry and Chemical Engineering,Zhongkai University of Agriculture and Engineering,Guangzhou 510225,China;Innovation Center of Pesticide Research,College of Science,China Agricultural University,Beijing 100193,China)

机构地区：[1]铜仁学院,贵州省梵净山地区生物多样性保护与利用重点实验室,贵州铜仁554300 [2]仲恺农业工程学院化学化工学院,广州510225 [3]中国农业大学理学院农药创新研究中心,北京100193

出　　处：《农药学学报》2021年第3期476-482,共7页Chinese Journal of Pesticide Science

基　　金：“十三五”国家科技支撑计划资助项目(2017YFD0200504);中国博士后科学基金资助项目(2019M653843XB);贵州省科技厅科技创新人才团队资助项目(黔科合平台人才[2020]5009);贵州省重点实验室项目(黔科合平台人才[2020]2003号);贵州省科学技术基金(黔科合基础[2020]1Y053);贵州省教育厅普通高等学校工程研究中心建设项目(黔教合KY字[2017]024);铜仁市中药民族药现代化研究与开发利用重点实验室(铜市科研[2019]03号);铜仁市科技局科技支撑计划项目(铜市科研[2020]128号).

摘　　要：以芳氧吡啶乙酮分子插件为基础,设计合成了一系列芳氧吡啶乙酮肟醚类化合物,其结构经核磁共振氢谱、碳谱及高分辨质谱等确证。初步杀虫活性测定结果表明,该系列化合物对棉蚜Aphis gossypii(Glover)具有较好的杀虫活性,其中化合物5a和6i在50μg/mL下对棉蚜的致死率分别为76.8%和70.1%,具有作为先导化合物进一步研究的价值;但其对小菜蛾的杀虫活性较差,在100μg/mL下的致死率普遍低于30%。该系列化合物主要体现出了新烟碱类化合物的活性特征,为进一步研究其构效关系提供了新思路。Based on the structure of the plug-in molecule aryloxypyridine methanone,a novel series of aryloxypyridine methanone oxime ethers containing several active units(pyridine,thiazole,diaryl ether,and oxime ether)were synthesized and characterized by 1H NMR,13C NMR and HRMS.The insecticidal activities were also investigated.The target compounds had moderate to good activity against Aphis gossypii(Glover),while compounds 5a and 6i showed excellent insecticidal activities with the lethal rate of 76.8%and 70.1%at the concentration of 50μg/mL,respectively.However,the lethal rate of the target compounds was lower than 30%at the concentration of 100μg/mL,showing poor insecticidal activities against Plutella xylostella.This series of compounds mainly demonstrated the active characteristics of neonicotinoids,and provided a new idea for further study of their structureactivity relationship.

关 键 词：分子插件法 芳氧吡啶乙酮 肟醚 新农药创制 杀虫活性 

分 类 号：S482.3[农业科学—农药学] O626.32[农业科学—植物保护]