新型含1,2,4-噁二唑结构的酰胺类化合物的设计、合成及生物活性

Design,Synthesis and Biological Activity of Novel Amides Containing 1,2,4-Oxadiazole

本文以tioxazafen为先导化合物,结合虱螨脲及溴虫氟苯双酰胺的活性结构片段,通过活性亚结构拼接方法,在1,2,4-噁二唑结构中引入酰胺基,设计并合成了9个含1,2,4-噁二唑结构的酰胺类化合物,并对化合物通过^(1)H NMR、^(13)C NMR和HRMS进行了结构表征,以及杀虫、杀螨活性测试,活性测试结果表明,大部分化合物具有一定的生物活性,其中化合物7 g杀虫和杀螨活性最好,在100 mg/L浓度下对小菜蛾和朱砂叶螨的活性分别达到了84%和78%。

9 amides containing 1,2,4-oxadiazole structure had been designed and synthesized by using tioxazafen as the leading compound,combined with the active structural fragments of acaricide and bromoflufenicomide,with the active substructure splicing method.The structure of the compounds were characterized by ^(1)H NMR,^(13)C NMR and HRMS,and insecticidal and acaricidal activity were tested,The results of activity test showed that most of the compounds had certain biological activities,among which compound 7 g had the best insecticidal and acaricidal activity,and the activity against Plutella xylostella and Tetranychus cinnabarinus reached 84%and 78%respectively at the concentration of 100 mg/L.