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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 search for and find new active substances, a series of novel 1,3,4-oxadiazole-containing oxadiazole derivatives were designed and prepared by using the active group splicing method. Pyrazole amide compounds were synthesized.The structures of the target compounds were confirmed by ~ 1H NMR, ~ (13) C NMR and elemental analysis.The preliminary bioassay results showed that some of the target compounds showed good insecticidal activity. When tested at a concentration of 500μg / m L, five compounds could kill 80% ~ 100% of the armyworm, and four of them showed similar efficacy and control efficacy against the armyworm. In addition, 1 Methyl-3-ethyl-4-chloro-N- {[5- (4-methylphenyl) -1,3,4-oxadiazol-2-yl] methyl} -5-carboxamide (9 g) kill 100% of aphids at a test concentration of 500 μg / mL.