Synthesis And Activities Of Substituted Isoxazolyl Acylureas

In the article, we dissertated comprehensively the functional mechanism, the relationship of structure, the synthetical methods and the safety of acylureas, substituted isoxazolyl acylureas and substituted pyrimidine acylureas.In order to seek insecticides with good biological activities, we have modified the main structure of acylureas by Bioisosterism Principles and Structure Link Wory, to Oxacillin active groups of 5-methyl-3-phenyl-4-isoxazole introduce to acylureas. Thirteen novel compounds of N-substituted phenyl-5-methyl-4- isoxazolyl acylureas(I,II) were synthesized with phenyl formaldehyde,Hydroxylamine HCl,ethylacetoacetate,oxalyl chloride and substituted aniline as starting materials.The other series of six novel compounds of N-substituted pyrimidine-5-methyl-3-isoxazolyl acylureas(III) were synthesized with ethyl oxalate,acetone,oxalyl chloride and substituted pyrimidine as starting materials. Structures of nineteen novel compounds were characterized by IR, 1H NMR spectra and elemental analysis. Based on the idiographic structure, we discuss synthesis condition, spectrum properties and physic-chemical constant of the target compounds at last. The title compounds are listed as follows:I N-substituted phenyl-5-methyl-3-phenyl-4-isoxazolyl acylureasII N-substituted phenyl-5-methyl-3-(4-chlorine phenyl)-4-isoxazolyl acylureasIII N-(4,6-two substituted pyrimidine)-5-methyl-3-isoxazolyl acylureastoIn the article, the antifungal activities of two series compounds (I,II) against Botrytis cinerea pers and Rhizoctonia cereailes were respectively tested by the mycelium growth rate method, and the results indicated that they had good antifungal activity against Botrytis cinerea pers, and the value of IIa,IIb,IIc,IId,IIg,IIh are better than others. The herbicidal activity of the series compounds(III)against Digitaria,Chingma Abution and Rape, and the results indicated that they had phytocidal activity, and the inhibition rape rate of compounds IIIa, IIIb, IIIe against the main root length are better than others .