The Synthesis Of Vinyl Derivatives And The Study Of Ethyl Difluorobromoacetate As A Novel N-formylation Reagent

Quinoline derivatives and formamide derivatives are important compounds which widely exist in natural products and pharmaceuticals.Much attention has been paid owing to their special physiological activities and irreplaceable role in the fields of medicine and agriculture.In addition,formamide is an important structural unit in synthetic chemistry and can be used for the further transformation.Therefore,this paper mainly focus on the synthesis of vinylquinoline derivatives and the application of ethyl difluorobromoacetate as a novel N-formylation reagent.This paper is mianly divided into three parts:?1?The synthesis of vinylquinoline derivatives were introudced and various formylation reagents were discussed;?2?The Palladium-catalyzed dimerization of N-arylpropargylamines for cascade synthesis of 3-vinylquinolines had been developed.The reaction was carried out under mild conditions to afford a variety of synthetically and pharmaceutically important quinoline derivatives in moderate to good yields.?3?Ethyl bromodifluoroacetate?BrCF₂COOEt?was first used as the N-formylating reagent in the copper-catalyzed N-formylation of amines.A range of amines underwent the N-formylation smoothly to furnish the N-formamides in moderate to exellent yields.The reaction adopted commercially available materials and had the merits of simple operation and excellent functional groups compatibility.