Studies On Synthesis And Properties Of Picolinamide Compounds With Biological Activities

The synonym of the future novel pesticide must have the characteristics of high efficiency,safety and environmentally-friend.Picolinamide compounds as the significant branch of heterocyclic compounds,it has the advantages of broad spectrum,high efficiency,low toxicity.In recent years,the design,synthesis and biological activity research of Picolinamide compounds have become one of hot topic of today’s green pesticide discovery,because of its Excellent electron transitivity and hydrophilia.The main research contents are as follows:1.The rencent research and development of Picolinamide compoundswhich have insecticidal activity,bactericidal activity and herbicidal activity were reviewed in this thesis.2.Two series of twenty novel Picolinamide compounds were designed and reportered by using the Flonicamid as lead compounds based on pesticide molecular design methods,such as "analogue synthesis","the principle of bioisosterisms","the principle of prodrugs".These compounds can be divided into two series as followings:(1)The picolinamide compounds of N-alkyl(2)The picolinamide compounds of N-alkoxy3.The synthetic conditions and reaction mechanism for intermediates,target compounds were sudied particularly,and structures of the prepared compunds were confirmed by 1H NMR、MS and IR.4.The bioassays of insecticidal activity were carried out according to the operation procedure of pesticide bioassay.The results showed that compounds I and II exhibited different extent of insecticidal activity against Armyworm(e.g.Mythimna separata)and Aphid(e.g.Aphis fabae).For example,at a concentration of 500 mg/L,compounds Ⅰa、Ⅰc、Ⅰd、Ⅱb、Ⅱd showed 100%inhibition ratio of insecticidal activity against Mythimna separata,and compounds Ⅰc、Ⅰd、Ⅱa、Ⅱd also showed more higher insecticidal activity against Aphis fabae.5.The bioassays of fungicidal and herbicidal activities were carried out according to the operation procedure of pesticide bioassay.The results showed that some compound of I and II exhibited good control efficiency against Puccinia Sorghi,but these compounds showed low herbicidal activities.