5-吡唑酰胺类化合物的合成及其杀虫活性研究  

Synthesis and Insecticidal Activity of 5-Pyrazolecarboxamide Derivatives

作　　者：刘杰[1] 谢化鹏[1] 宋宝安[1] 胡德禹[1] 杨松[1] 金林红[1] 薛伟[1] 吴剑[1] 徐维明[1] 

机构地区：[1]贵州大学精细化工研究开发中心绿色农药与农业生物工程教育部重点实验室和国家重点实验室培育基地,贵阳550025

出　　处：《有机化学》2010年第9期1347-1353,共7页Chinese Journal of Organic Chemistry

基　　金：贵州省农药学国家重点学科人才基地(No.黔人领发[2008]3号);贵州省科技厅重点实验室能力建设资助项目

摘　　要：采用活性基团拼接法,以2,3-二氯吡啶和马来酸二乙酯为起始原料,由胺基化合物与中间体6合成了10个新的5-吡唑酰胺类化合物,通过IR,1HNMR,13CNMR和元素分析对其结构进行了表征.初步生物活性测试结果表明,在100μg/mL浓度下,化合物7a～7j具有一定杀虫活性.其中化合物7a和7d对褐飞虱的防治效果分别为57.6%和64.4%,与对照药剂噻嗪酮杀虫活性基本相当.作用机制测试结果表明7d对褐飞虱乙酰胆碱酯酶活性的抑制率为75.21%,高于噻嗪酮对褐飞虱乙酰胆碱酯酶的抑制率(52.17%).Ten 5-pyrazolecarboxamide derivatives were synthesized by the reaction of amine and intermediate 6 starting from 2,3-dichloropyridine and diethyl maleate. Their structures were identified by elemental analysis,IR,1H NMR and 13C NMR spectra. The preliminary bioassay showed that compounds 7a～7j had moderate insecticidal activities against Nilaparvata lugens （Stal）,7a and 7d possessed good insecticidal activity with the mortality rate of 57.6% and 64.4% at a concentration of 100 μg/mL,respectively,similarly to the control （buprofezin）. Insecticidal mechanism of 7d indicated that it has a good inhibitive activity against Brown planthopper acetylcholinesterase with rate of 75.2% than the commercial control buprofezin （52.2%）.

关 键 词：吡唑酰胺衍生物 乙酰胆碱酯酶 合成 杀虫活性 

分 类 号：TQ450.21[化学工程—农药化工]