新型含1,3,4-噁二唑结构的吡唑酰胺类化合物的合成与杀虫活性研究

Synthesis and Insecticidal Activities of Novel Pyrazole Amides Containing 1,3,4-Oxadiazole Moiety

为了寻找与发现新的活性物质,以杀虫剂吡螨胺为先导化合物,采用活性基团拼接的方法,设计并制备了一系列未见文献报道的新型含1,3,4-噁二唑结构的吡唑酰胺类化合物.通过~1H NMR,^(13)C NMR和元素分析测试确认了目标化合物的结构.初步的生物活性测试结果显示,部分目标化合物表现出较好的杀虫活性.在测试浓度为500μg/m L时,有5个化合物对粘虫的杀灭活性可达80%~100%,其中4个化合物对粘虫的防治效果与对照药剂唑虫酰胺接近.此外,1-甲基-3-乙基-4-氯-N-{[5-(4-甲基苯基)-1,3,4-噁二唑-2-基]甲基}-1H-吡唑-5-甲酰胺(9g)在测试浓度为500μg/m L时对蚜虫的杀死率为100%.

In order to find new pesticide with potent bioactivities, a series of novel pyrazole amides carrying 1,3,4-oxadiazole moiety were prepared according to the structure of tebufenpyrad. The structures of the title compounds were characterized by 1H NMR, 13C NMR and elemental analysis. Preliminary bioassay data showed that some target compounds displayed good insecticidal activities. At the concentration of 500 μg/m L, five compounds had insecticidal activity against Oriental armyworm with 80%100%, and four compounds displayed comparable insecticidal activity against Oriental armyworm to that of the control tolfenpyrad. In addition, 1-methyl-3-ethyl-4-chloro-N-{[5-（4-methylphenyl）-1,3,4-oxadiazol-2-yl）methyl]-1H-pyrazole-5-carboxamide（9g） exhibited 100% insecticidal activity against Aphis medicaginis at 500 μg/m L.