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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%。
Four kinds of 2-amino-4-substituted-6-trifluoromethyl pyrimidine intermediates were synthesized by cyclization, chlorination, methoxylation and amination reaction using trifluoroacetoacetic acid ethyl ester and guanidine hydrochloride as starting materials Ⅰa ~ Ⅰd), Ⅰ with o-methoxycarbonyl benzenesulfonyl isocyanate nucleophilic addition, synthesis of three containing different substituted pyrimidine ring sulfonylurea compounds (Ⅱ b ~ Ⅱ d). Amino-4-dimethylamino-6-trifluoromethylpyrimidine (Id) and N [-2 - (’4-dimethylamino-6-trifluoromethyl) pyrimidinyl] -2- Methoxycarbonylbenzenesulfonylureas (Ⅱd) is a new compound whose structure has been characterized by 1H NMR and MS. The results of the preliminary herbicidal activity test showed that N- (2-methoxy-6-trifluoromethyl) pyrimidinyl] -2-methoxycarbonylbenzenesulfonylurea (IIc) ./ha control of barnyardgrass and crabgrass were 70% and 50% respectively.