Synthesis And Antibacterial Activity Of Quinoline ?-carbonyl Ester Compounds

Pesticide is important to the developing of agricultural modernization.However,the extensive use of pesticide is harmful to ecological environment.Meanwhile,with the strengthening of people's environmental protection awareness and food safety,developing the environmentally friendly,effective,low toxicity and residue compatible pesticides have become the subject in the research of pesticide.Improving traditional synthetic methods of pesticide intermediates with high efficient conform to be a hot topic in today's pesticide field.Quinoline ring and carbonyl are important skeletons in pesticide structure,and have great potential for development,especially nitrogen-containing quinoline ring,which often appears in the natural product skeleton and has high development value.Therefore,the study of green synthesis of novel compounds containing quinoline rings and carbonyl groups has attracted much attention.A new method for the synthesis of quinoline ?-carbonyl esters based on 8-methylquinoline and benzoylformic acid was explored and the biological activity of some new compounds was studied in order to obtain new compounds with good biological activity,Lay the foundation for the development of new pesticides.The main achievements of this paper are as follows: 1.A new compound of quinoline ?-carbonyl ester was synthesized by direct dehydrogenation coupling reaction with 8-methylquinoline and ?-carbonyl acid catalyzed by palladium-catalyzed C(sp3)-H.The structures of the products were characterized by high resolution mass spectrometry,1H and 13 C NMR.2.The reaction conditions were optimized,the optimum reaction conditions were obtained,and the reaction yield was improved.3.The substrate was extended under optimal conditions,indicating that the reaction had a good generalization.4.Studying on the reaction process,puting forward the possible reaction mechanism,and preliminary validation;5.The experimental results showed that quinoline ?-carbonyl ester compounds had good bioactivity.In conclusion,a new method for the synthesis of quinoline ?-carbonyl ester compounds has been developed and we synthesized 26 new compounds that have not reported in the literature,The results showed that the new compounds of quinoline ?-carbonyl ester had good biological activity and could be used as a reference for studying the bioactivity of quinoline skeleton compounds.The research results of this paper have important theoretical and practical significance for the research of heterocyclic pesticide creation and synthesis methodology.