新型吡唑丙烯腈酯类衍生物的合成及其杀螨活性  

Synthesis and acaricidal activity of novel pyrazole acrylonitrile derivatives

作　　者：张雅婷 高占宇 徐婧[3] 刘秉知 秦培文 纪明山[1,2] ZHANG Yating;GAO Zhanyu;XU Jing;LIU Bingzhi;QIN Peiwen;JI Mingshan(Plant Protection College,Shenyang Agricultural University,Shenyang 110161,China;Biological Pesticide Engineering Center of Liaoning Province,Shenyang 110161,China;Institute of Plant Protection,Liaoning Academy of Agricultural Sciences,Shenyang,110161,China)

机构地区：[1]沈阳农业大学植物保护学院,沈阳110161 [2]辽宁省生物农药工程中心,沈阳110161 [3]辽宁省农业科学院植物保护研究所,沈阳110161

出　　处：《农药学学报》2024年第4期716-723,共8页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金(31801780).

摘　　要：为了获得活性更好的吡唑丙烯腈类杀螨剂,采用1,3-二甲基-1H-吡唑-5-羧酸乙酯为原料,通过布兰克氯甲基化、脱卤、缩合和酯化4步反应合成了17个新型吡唑丙烯腈酯类衍生物,并采用浸虫法测定目标化合物对朱砂叶螨Tetranychus cinnabarinus的杀螨活性,计算死亡率和致死中浓度(LC_(50))。结果表明,目标化合物具有优良的杀螨活性,其中化合物5q和5k相比于商品化杀螨剂腈吡螨酯(LC_(50)=0.61 mg/L)具有更高的杀螨活性,其LC_(50)值分别为0.17和0.22 mg/L。In order to obtain acaricides of pyrazole acrylonitrile with better acaricidal activity for mitecontrol,seventeen novel ester derivatives were synthesized via four steps of Blanc chlorome-thylation reaction,dehalogenation reaction,condensation reaction and esterification reaction using ethyl 1,3-dimethyl-1H-pyrazole-5-carboxylate as the starting material.Furthermore,their acaricidal activity against Tetranychus cinnabarinus was assessed by immersion test,and the mortality rate and lethal mid-range concentration LC_(50) were calculated.The results show that the target compounds display excellent acaricidal activity against T.cinnabarinus,and compared with the commercial pesticide cyenopyrafen(LC_(50)=0.61 mg/L),compounds 5q and 5k possess significantly higher acaricidal activity against T.cinnabarinus with LC_(50) values of 0.17 and 0.22 mg/L,respectively.

关 键 词：吡唑丙烯腈 合成 朱砂叶螨 杀螨活性 腈吡螨酯 

分 类 号：S482.5[农业科学—农药学] TQ450.1[农业科学—植物保护]