The Research Of α-amidation And Amination Based On Quinoline N-oxides

Quinoline and its derivatives are an important heterocyclic compound which widely found in drugs,natural products and functional materials.Quinoline deri vatives exhibit potential biological activity,particularly in the areas of biological preservatives,antimalarials and antibacterial.In addition,quinoline derivatives were widely used in molecular recognition,materials,coordination chemistry and other fields.Therefore,the synthesis of quinoline derivatives has become one of the hotspots in organic synthesis.Quinoline N-oxides have the advantages of high reactivity,good regional se lectivity and easy transformation.In view of the functionalization of quinoline N-oxides,we will give.a detailed introduction to the results obtained from our studies on the synthesis of quinoline derivatives based on quinoline N-oxides.The paper includes the following three parts:In the first part,we summarized the use of quinoline derivatives,the synthe sis of quinoline compounds and the research results and progress in functionaliz ation of quinoline N-oxides.In the second part,we described a simple and efficient method in the synth esis of a-amide quinoline.We synthesized a series of a-amide quinoline compou nds up to 95%which are carried out in the presence of FeCl3 as accelerator an d stirring at 120℃ for 12 hours by using quinoline N-oxides and nitrile as reac tion substrate.The main advantages of this method are the high yield of the targ et product,simple conditions,easy to handle and high atomic utilization.In the third part,we introduced the synthesize of N,N-dimethyl-a-quinoline u nder the reaction of quinoline N-oxides and DMF catalyzed by copper salts.Th e method achieves the amination of quinoline without the additional reduction o f quinoline N-oxides,which is simple and efficient.