Synthesis And Biological Activity Of Pyrazolyl Acrylonitrile Ethers Derivatives

Plant diseases cause the reduction of food and limit the development of agriculture all over the world.Pesticides can control them effectively.However,the novel pesticides need to discover due to the increasing resistance.Pyrazole compounds and acrylonitrile compounds,have become a hot field in pesticides.Pyrazole compounds often exhibited high biological activity,low toxicity,broad-spectrum,and structural changes.Numerous pyrazole derivatives have been developed as commercial pesticides,such as fluazolate,fenpyroximate,fipronil,and pyraclostrobin.Moreover,acrylonitrile compounds have attracted attention because of the novel structure,high activity,low toxicity on mammals and fish,and no cross-resisitance to existing insecticides.One of the best known acrylonitrile derivatives is cyenopyrafen,which integrates the advantages of pyrazole compounds and acrylonitrile compounds and possesses high safety level on beneficial insects and high acaricidal activity.Cyenopyrafen displayed excellent bioactive to controlling spider mites during all life stages.According to the above mentioned research,cyenopyrafen was considered as a lead compound,the novel title pyrazole acrylonitrile compounds were designed and synthesized,with acaricidal activity.The bioassay results showed compounds A1,A2,B1,B4,B8,B9 and B10 showing geeat acaricidal activity in 2.5mg/L.From the SAR,finding ether bond maybe the key to its high acaricidal activity and pyrazolyl has an effect on the biological activity possibly.