含5-氨基噻唑环核苯甲酰脲类化合物的合成及生物活性

Synthesis and Biological Activity of Benzoylurea Compounds Containing 5-Aminothiazole Unit

摘要:

以课题组前期研究所发现的高杀虫活性化合物Ⅴj为先导，通过噻唑环2位苯基引入取代基，设计并合成了19个含5-氨基噻唑环核苯甲酰脲类化合物，收率81.4%~95.8%，其结构均经1H NMR和13C NMR分析确证。初步离体杀虫活性测试结果表明：在质量浓度为600 mg/L时，所有化合物均显示一定的杀虫活性；其中化合物 Ⅵ i ~ o对粘虫及化合物Ⅵ k、Ⅵ m和Ⅵ n对棉铃虫和玉米螟均显示100%的杀虫活性。

Abstract:

Employing the high insecticidal active compound Ⅴj which was found in our previous work as a leading compound, 19 benzoyl urea compounds containing 5-aminothiazole ring have been designed and synthesized (yield: 81.4~95.8%) by introducing different substituent to the 2-position phenyl of thiazole ring. The structures of all these compounds were confirmed by 1H NMR and 13C NMR. Preliminary results of in vitro insecticidal activity test showed that all the title compounds displayed certain insecticidal activity at the concentration of 600 mg/L (W/W). Among them, compounds Ⅵ i ~ o showed 100% lethal activity against armyworm, Besides, three compounds Ⅵ k,Ⅵ m and Ⅵ n also exhibited 100% fatality rate against cotton bollworm and corn borer.