新型含噁唑单元的吡唑酰胺衍生物的合成及其生物活性  

Synthesis and Bioactivities of Novel Pyrazole Amides Carrying Oxazole Moiety

作　　者：张敏 郑丹丹 倪亚丹 梁凯 荀校 胡兰萍[1] 陈庆文 杨冰 梁志鹏[2] 丁颖 石健[2] 戴红[1] Zhang Min;Zheng Dandan;Ni Yadan;Liang Kai;Xun Xiao;Hu Lanping;Chen Qingwen;Yang Bing;Liang Zhipeng;Ding Ying;Shi Jian;Dai Hong(College of Chemistry and Chemical Engineering,Nantong University,Nantong,Jiangshu 226019;Analysis and Testing Center,Nantong University,Nantong,Jiangshu 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6期1772-1778,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)资助项目。

摘　　要：为了寻找具有良好生物活性的吡唑酰胺化合物,基于氯虫苯甲酰胺的结构,在吡唑环的5-位引入取代噁唑环单元,合成出了一系列新型吡唑酰胺,利用^1H NMR, ^13C NMR和元素分析对其目标产物的结构进行了确证.生测结果表明,所有目标化合物在500μg/mL时对粘虫均显示出较好的杀虫活性(致死率≥90%). 5个化合物在100μg/mL时对粘虫的防治效果可达90%~100%,3个化合物在100μg/mL时对苜蓿蚜的杀死率为90%~100%.另外,2个化合物在500μg/mL时对朱砂叶螨的防效可达80%~100%.In order to find new pyrazole amides with wonderful bioactivities,a series of novel pyrazole amide derivatives were synthesized by introducing substituted oxazole ring into the C-5 position of pyrazole skeleton based on the lead chlorantraniliprole.The aimed compounds were structurally characterized through ^1 H NMR,^13C NMR and elemental analysis.The preliminary bioassay results exhibited that all the title compounds displayed more than 90%insecticidal activities against Mythimna separata(Walker)at 500μg/mL.At the dosage of 100μg/mL,five compounds possessed 90%~100%insecticidal activities against Mythimna separata(Walker),and three compounds exhibited insecticidal property against Aphis craccivora with 90%~100%.Additionally,at the dosage of 500μg/mL,two compounds possessed insecticidal activity against Tetranychus cinnabarinus with 80%~100%.

关 键 词：噁唑 吡唑酰胺 合成 生物活性 

分 类 号：O623.626[理学—有机化学] TQ450.1[理学—化学]