含5-氨基噻唑环核双酰胺类化合物的合成及生物活性研究

Synthesis and biological activity of diamide compounds containing

摘要:

以商品化双酰胺基本骨架为先导，设计并合成了13个含5-氨基噻唑环核的苯甲酰脲类化合物，优化了Thompson等报道的基于Ugi四组件反应2,4二取代-5-氨基噻唑中间体的合成方法，其结构均经1H NMR、13C NMR、IR和MS 分析确证。初步离体杀虫活性测试结果表明，该类化合物具有很好的杀虫活性：当浓度为10 ppm，化合物5f、5g、5h、5j和5m对蚊幼虫均显示100%的杀虫活性，且当浓度降至5 ppm和2 ppm时，化合物5j的活性仍有100%，高于阳性对照；当浓度为600 ppm，化合物5d，5g对棉铃虫和玉米螟均显示100%的杀虫活性。

Abstract:

Using the basic skeleton of commercialized benzoyl urea as leading compound, thirteen compounds were designed and synthesized by introducing 5-aminothiazole moiety into benzoylurea. The literature synthetic method of 2,4-disubstituted-5-aminothiazole derivatives based on the Ugi four-component reaction by Thompson has been optimized, their structures of all these compounds have been comfirmed by 1H NMR, 13C NMR, IR and MS. Their results of bioassay showed that most of the title compounds exhibited excellent insecticidal activities. Among them, compounds 5f, 5g, 5h, 5j and 5m showed 100% insecticidal activity against mosquito larvae at a concentration of 10 ppm, furthermore, when the concentration decreased to 5 ppm and 2 ppm, compound 5j still showed 100% activity which was higher than that of positive control; Compounds 5d and 5j showed 100% insecticidal activity against cotton bollworm and corn borer at a concentration of 600 ppm.