5-氨基噻唑脲类化合物的合成及生物活性

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

以高杀虫活性化合物1-[(2-苯基-4-对甲氧基苯基)噻唑-5-基]-3-(3,5-二氟苯甲酰基)脲(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-氨基噻唑环核的苯甲酰脲类化合物,收率81.4%～95.8%,其结构均经1HNMR和13CNMR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Ⅵi～o对黏虫及化合物Ⅵk、Ⅵm和Ⅵn对棉铃虫和玉米螟均显示100%的杀虫活性。

Employing compound with high insecticidal activity, 1-(3,5-difluoro-benzoyl)-3-[4-(4-methoxyphenyl)-2-phenyl-thiazol-5-yl]-urea(Ⅴj) as leading compound, nineteen benzoyl urea compounds containing 5-aminothiazole ring were designed and synthesized with 81.4%~95.8% yields by introducing different substituent to the 2-position phenyl of thiazole ring. The structures of all these compounds were confirmed by 1HNMR and 13 CNMR. Preliminary results of in vitro insecticidal activity test showed that all of the title compounds displayed certain insecticidal activities at 600 mg/L. Among them, compounds Ⅵi^o showed 100% lethal activity against armyworm. Besides, compounds Ⅵk,Ⅵm and Ⅵn also exhibited 100% fatality rate against cotton bollworm and corn borer.