Synthesis And Bioactivity Of Oxime Ether Acylamides And Pyrimidines Compounds

Oxime ethers and their derivatives have been extensively used in medicine as well as in pesticide because of their high bioactivities. Many of them have been developed to be insecticide, fungicide, herbicide and so on. Further more, oxime ether group is often acted as active groups in new pesticide discovery due to their high efficiency, low toxicity and short residual. Since pyrimidine derivatives also showed excellent bioactivities in medicine and agrochemicals, much attention have been given to these compounds. In recent years, many pyrimidine derivatives used as pesticide have been reported, such as pyrimidine amines, pyrimidine ureas and pyrimidine acrylates are good fungicide. In this paper, novel oxime ethers and pyrimidine derivates are designed and synthesized according to sub-structure linkage, bioisosterism theories. Furthermore, the bioactivities of these new compounds are tested, and some of them showed excellent pesticide and fungicide activitiy. The main contents are as follows:1. The recent research progress and commercial compounds of oxime ethers and pyrimidine derivatives are reviewed, Structure activity relationship of oxime ethers are introduced in detail.2. On the basis of agrochemical reasonal design theroy and the QSAR (quantitative structure-activity relationship), eighteen oxime ether acylamidesâ… , eleven pyrimidine aminesâ…¡and six pyrimidine ethersâ…¢are designed and synthesized. All of these new compounds are confirmed by ~1H NMR, LC/MS, GC/MS, HPLC and IR.3. Bioactivities of these new compounds were tested by the Standard Operation Procedure of the bioassay department of Hunan Branch of National Pesticide R&D South Center. These compounds showed different pesticide and fungicide activity.4. According to the result of bioactivity, structure activity relationship of these compounds were summarized, which could be used to guide the further modification research.