Synthesis, Biological Activity Of Urail And Pyrimidine Derivatives

Protoporphyrinogen oxidase inhibitors, with very many characteristic, such as high efficiency, low toxicity and so on, attract more and more attention of pesticide scientists. Moreover, α-amino phosphonate compounds displayed a wide range of biological activities, In order to find novel PPO lead compounds with high activity and low toxicity, a series of uracil derivertives containing benzothiazole unit were designed and synthesized (Ⅰ 01-Ⅰ09). Secondly, twelve α-amino phosphonate compounds contains of uracil moiety were designed and synthesized (Ⅱ 01-Ⅱ 12). In addition, α-amino phosphonate compounds containing the pyrimidine ring were designed and synthesized (Ⅲ01-Ⅲ07).Their general structures are as follows:(1)N-(6-substitutedbenzo[d]thiazol-2-yl)-3-(3-methyl-2,6-dioxo-4-(trifluoromethyl)-2,3-dihydropyrimidin-1(6H)-yl)benzamide (Ⅰ 01-Ⅰ 09):(2)Diethyl(((2-chloro-4-substituted-5-(3-methyl-2,6-dioxo-4-(trifluoromethyl)-2,3-d ihydropyrimidin-1(6H)-yl)phenyl)amino)(phenyl)methyl)phosphonate (Ⅱ01-Ⅱ12):(3)Diethyl(((2-((4,6-dimethoxypyrimidin-2-yl)oxy)phenyl)amino)(substituted phenyl)methyl)phosphonate(Ⅲ01-Ⅲ07):All target compounds were confirmed by 1HNMR, and some of them were characterized by IR,31PNMR and MS. Synthetic methods and reaction of conditions of the related and target compounds were also studied and explored.In the preliminary activity of target compounds were envaluated. The preliminary biossays results indicated that some compounds have good herbicide activity. The structure-activity relationship of target compounds was summarized.