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

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.