New Synthetic Method Development On Copper-Catalyzed Synthesis Of Heterocyclic Amides With Molecular Oxygen As The Terminal Oxidant

Amides are quite important organic compounds in organic chemistry, which are prevalent scaffolds widely existing in numerous compounds ranging from biologically active natural products, pharmaceuticals to synthetic materials. As a result, the formation of amides is of great importance in organic synthesis.Chemists have developed numerous methods for the formation of amides. The classic mode is using stoichiometric activating agents to preactive the free carboxylic acids, rendering an active intermediate which is readily reacting with amines to generate a amide. Later on, catalytic direct formation of amides from unactivated carboxylic acids and amines were developed. In recent years, with the development of new organic methodologies, chemists found that aldehydes, alcohols and alkynes can be employed to the synthesis of amides in some catalytic systems. Despite such advances in this area, we stongly believe this area still has substantial room for further development. Therefore, developing more novel organic methodology to prepare valuable amides with new structure is still of great significance in organic chemistry.On the basis of our previous related work and continuous interesting in copper/oxygen catalytic system, in this thesis, we study molecular oxygen promoted Cu-catalyzed amidation of aryl ketones or unactivated carboxylic acids with azoles. In addition, transamidation of benzimidazole amides with a variety of amines on a simple condition are also studied.