Studies On Synthesis And Properties Of Pyrimidinyl Ethers And Oxime Ethers With Biological Activities

Pyrimidines show high biological activities, so people in medicine and agrochemical attach great importance to develop this serial compouds. In the recent year, more and more pyrimidine compouds have been used for agrochemical. for example, pyrimidine amides, pyrimidine glands and pyrimidine acrylates are used as fungicide, Pyrimidine sulfonylureas, pyrimidine salicylic acid and triazolopyrimidine sulfonamides are used as herbicide. Herbicides containing pyrimidine heterocycle have not only unique action of their own, but also high bioactivity.Oxime ethers are very important active compoudes, and many of them are used as insecticide, fungicide, herbicide and so on. Further more, oxime ethers group is often used in new pesticide discovery because of their high biological activities and their good environmental profiles.In this paper, novel pyrimidine and oxime ethers derivatives were designed and synthesized by ways of random synthesis and analogue synthesis ,and their spectrum properties, biological activities, quantitative structure-activity relationship were studied meanwhile. What the paper studied may be summarized as follows:1. Two series of pyrimidines with herbicide activity and oxime ethers are summarized in the paper, and the relationship between the structure and activity is summarized too.2. Thirty-six unreported compounds in four series were synthesized. The structure of all these compounds were confirmed by LC, LC/MS, ¹H NMR.These compounds are summarized as follow:F₁-F₁₀: pyrimidinyloxy benzyl amine derivative (10)F₁₁-F₂₀: pyrimidinyloxy benzoic acid benzene ester derivative (10)F₂₁-F₃₀: indanone oxime ether derivative (10)F31-F36: pyrimidinyloxy oxime ether derivative (6)3. The route and condition for N- alkylation of different amine is probed.4. 1,4-dioxane is creatively used as solvent in synthesize of pyrimidinyloxy benzoic acid benzene ester derivative.5. Biological activities of the new compounds mentioned were studied and a group of new lead compounds possessed excellent herbicide activities containing pyrimidinyloxy benzoic acid benzene ester frame.