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.