【摘要】 以三氟乙酰乙酸乙酯和盐酸胍为原料,经环合、氯化、甲氧基化、胺化反应合成了4种2-氨基-4-取代-6-三氟甲基嘧啶中间体(Ⅰa~Ⅰd),Ⅰ与邻甲氧羰基苯磺酰异氰酸酯亲核加成,合成了3种含不同取代嘧啶环的磺酰脲化合物(Ⅱb~Ⅱd)。其中2-氨基-4-二甲胺基-6-三氟甲基嘧啶(Ⅰd)和N[-2-(′4-二甲胺基-6-三氟甲基)嘧啶基]-2-甲氧羰基苯磺酰脲(Ⅱd)为新化合物,结构经1H NMR和MS表征。初步除草活性测定结果表明,N-[2-′(4-甲氧基-6-三氟甲基)嘧啶基]-2-甲氧羰基苯磺酰脲(Ⅱc)在浓度为200 ga.i./ha时对稗草和马唐的防效分别为70%和50%。更多还原

【Abstract】 Four 2-amino-4-substitued-6-trifluoromethylpyrimidines(Ⅰa~Ⅰd) were synthesized from guanidine hydrochloride and ethyl trifluoroacetoacetate by cyclization,chlorination,methoxylation and amination.N-[2′-(4-substituted-6-trifluoromethyl)pyrimidyl]-2-methoxycarbonylphenylsulfonylureas(Ⅱb~Ⅱd) were obtained from Ⅰ and 2-methyloxycarbonylbenzene sulfonylisocyanate.2-amino-4-dimethylamino-6-trifluoromethylpyrimidine(Ⅰd) and N-[2′-(4-dimethylamino-6-trifluoromethyl)pyrimidyl]-2-methoxycarbonylphenylsulfonylurea(Ⅱd) were new compounds and the structurs were confirmed by ~1H NMR and MS.Biological activity testing in the greenhouse indicated that N-[2′-(4-methoxyl6-trifluoromethyl)pyrimidyl]-2-methoxycarbonylphenylsulfonylurea(Ⅱc) showed good herbicidal activity,with 200 ga.i./ha providing 70% and 50% inhibition rate of Echinochloa Crusgalli(L.) Baeuv and Digitaria Sanguinalis(L.) Scop.更多还原