Studies On Synthesis And Properties Of N-Oxygen-o-Aminobenzamide Derivatives With Bioactivity

Amide derivatives which have a broad spectrum biological activities,have been widely used in medicine,agricultural and environmental protection.were reported early in the 1960s as insecticide.In recent years,the ryanodine receptor action agent Anthranilic acid amide derivativesas insecticidal activity compounds of research,has become one of the hot spot of creating new pesticide,highly active compounds are being found.This paper summarizes the research and development status of amidefungicide,pesticides,herbicides and the development trend in the future,and reviews the process of such herbicides from development to application.The detailed structure optimization characteristics and structure-activity relationships of amide derivatives are introduced in this paper.It also introduces some typical compound’s structural characteristics,synthesis method and biological activity.These is have combined with "the structure connection method" and"biological electronics row" which have different action mechanism.Totally 31 compounds N-oxygen-o-aminobenzamide derivatives,have been synthesised by the methods which have been mentioned above.were synthesized by chemical structure target compound by used of IR,HPLC,GC,1H NMR,LC/MS,GC/MS spectrum method.These compounds have been divided into three-series according to their structures as following:(1)N-alkoxy-5-chlorine-o-aminobenzamide derivatives(Ⅰ1～Ⅰ12):(2)N-alkoxy-5-cyan-o-aminobenzamide derivatives(Ⅱ1～Ⅱ5):(3)N-alkoxy-o-aminobenzamide derivatives(Ⅲ1～Ⅲ14):The bioassays of insecticidal activity were carried out according to the operation procedure of pesticide bioassay.The results showed that compounds Ⅰ,Ⅱ and Ⅲ exhibited different extent of insecticidal activity against Lepidoptera pest(e.g.Mythimna separata),Homoptera pest(e.g.Aphis fabae and Nephotettix cincticeps)and acaricidal activity against Mite(e.g.Tetranychus urticae).For example,at a concentration of 100 mg/L,Ⅰ2～Ⅰ12,Ⅲ1,Ⅲ3,Ⅲ4,Ⅲ8,Ⅲ10 and Ⅲ13 The results have showed that these compounds have different insecticidal activity by the Mythimna separata.the death rate of 100%,but to tetranchus urticae and aphis fabae activity is extremely low,didn’t even activity.at a concentration of 100 mg/L,The results have showed Ⅰ8,Ⅰ9,Ⅰ12 and Ⅲ10 by the Nephotettix cincticeps Insecticidal activities are higher than 90%.These is studies on qualitative structure-activity relationship of the synthesized compound I,II and III,and proposed the precursor structure of these three compounds,which provide important information for further creation research of promising active compounds.