含取代噁唑环的新型吡唑酰胺类化合物的合成与生物活性研究  

Synthesis and Biological Activities of Novel Pyrazole Amide Compounds Containing Substituted Oxazole Unit

作　　者：戴红[1] 梁凯 周钱 倪亚丹 钱程 钱宏炜 李玲 石玉军[1] 梁志鹏[2] 石健[2] 高磊 吴新星 Dai Hong;Liang Kai;Zhou Qian;Ni Yadan;Qian Cheng;Qian Hongwei;LiLing;ShiYujun;LiangZhipeng;Shi Jian;Gao Lei;Wu Xinxing(College of Chemistry and Chemical Engineering,Nantong University,Nantong,Jiangsu 226019;Analysis and Testing Center,Nantong University,Nantong,Jiangsu 226019)

机构地区：[1]南通大学化学化工学院,江苏南通226019 [2]南通大学分析测试中心,江苏南通226019

出　　处：《有机化学》2020年第12期4350-4356,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21372135);南通市科技计划(No.MS12019060);南通大学高层次人才(No.03083031)资助项目。

摘　　要：采用活性单元拼接的方法,以新型吡唑酰胺类杀螨剂吡螨胺为先导结构,在吡唑酰胺分子结构中引入取代噁唑活性单元,设计合成出15个结构新颖的含取代噁唑环的吡唑酰胺类衍生物.目标化合物的结构通过1H NMR,13C NMR和元素分析等进行了表征.初步室内杀虫活性测试结果表明,在500μg/m L测试浓度下,多数目标化合物对粘虫(Orientalarmyworm)有着较高的杀虫活性(致死率≥90%).其中1个目标化合物在500μg/m L测试浓度下对蚜虫(Aphis medicaginis)的致死率达100%.此外,2个目标化合物在500μg/m L测试浓度下对朱砂叶螨(Tetranychus cinnabarinus)的致死率都为30%.In search of new pyrazole amide derivatives with wonderful bioactivities,fifteen novel pyrazole amide compounds were designed and synthesized by introducing substituted oxazole unit into pyrazole amide skeleton based on the lead compound tebufenpyrad.The structures of the title compounds were confirmed by 1 H NMR,13 C NMR and elemental analysis.The preliminary bioassay data exhibited that most of target compounds had more than 90%insecticidal activities against Oriental armyworm at the concentration of 500μg/mL.At the concentration of 500μg/m L,one compound displayed 100%mortality rate against Aphis medicaginis.In addition,two compounds showed 30%insecticidal activity against Tetranychus cinnabarinus at the concentration of 500μg/m L.

关 键 词：噁唑 吡唑酰胺 合成 生物活性 

分 类 号：O626[理学—有机化学] TQ454.2[理学—化学]