新型含氯代噻唑基团和嘧啶环的吡唑肟醚类衍生物的合成及其生物活性研究  

Synthesis and Biological Activity Evaluation of Novel Pyrazole Oxime Ether Derivatives Containing Chlorothiazole Group and Pyrimidine Rings

作　　者：杨亚喆 林大勇[1] 傅翠蓉[1] 邹小毛[1] 

机构地区：[1]南开大学元素有机化学研究所元素有机化学国家重点实验室天津化学化工协同创新中心,天津300071

出　　处：《有机化学》2015年第1期100-108,共9页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.20772067;21472102)资助项目~~

摘　　要：为解决抗性问题,寻找新的活性化合物,在前期工作基础上,运用生物等排原理,以吡唑肟醚为骨架,引入了第二代新烟碱类重要药效团氯代噻唑和另一重要基团嘧啶环,设计合成了系列新型吡唑肟醚类化合物.以1H NMR,IR,元素分析及MS进行结构确证,并进行了杀虫、杀螨及杀菌活性测定.部分具有氯代噻唑环的A系列化合物显示了良好的杀蚊虫活性(100%,5 mg·L-1)、杀豆蚜活性(100%,200 mg/L)和杀螨活性(100%,200 mg/L);具有嘧啶环的B系列化合物显示了一定的杀菌活性.On the basis of our previous work, in order to seeking for novel compounds with bioactivities to settle for the resistance problem, two series of novel pyrazole oxime ether derivatives have been designed and synthesized containing chlorothiazole group and pyrimidine rings applying the bioisosterism. Their structures were determined by 1^H NMR, IR, elemental analysis and MS, and their bioactivities were performed. Nearly half of the target compounds of series A with chlorothiazole group exhibited good insecticidal activity against culex pipiens pallens （100%, 5 mg.·L^-1）, several compounds of series A showed good activity against Aphis laburni Kaltenbach （100%, 200 mg/L） and Tetranychus cinnabarinus （100%, 200 mg/L）, and the compounds of series B with pyrimidine rings exhibited certain fungicidal activity.

关 键 词：吡唑肟醚 氯代噻唑 嘧啶环 合成 生物活性 

分 类 号：O626[理学—有机化学] TQ450.1[理学—化学]