Copper-catalyzed Synthesis Of N-arviamide And Benzoxazole Derivatives

Amide and benzoxazole derivatives are present in a wide variety ofbiologically active molecules, pharmaceutical and organic materials. Therefore, it isnecessary to use effective method to build sp2C-C or C-hetero atom bonds that hasbecome an important research direction in organic chemistry. Copper-catalyticcross-coupling reactions are widely applied to form these bonds in organic synthesis.Developing the simple, efficient, green synthesis method has become a currentresearch focus. The main contents of this paper are as follows:In the first chapter, a number of methods for synthesis of amide compounds areintroduced by name reactions. And some methods to building the benzoxazole unit havealso described.In the second chapter, an improved protocol for synthesis of N-arylamides by thecopper-catalyzed reaction of aryl halides with nitriles is introduced. The use of nitrilesas nitrogen nuclepohiles can make the synthesis of N-arylamides more simple than thatusing amides through in situ hydrolysis. And use of acetaldoxime as the hydrolysisreagent instead of H2O facilitates the operation of the reaction. The significantlydecreased amount of nitriles, along with use of weak base, makes this transformationatom-efficient and environmentally benign.In the third chapter, a wide variety of benzoxazole derivatives can be synthesizedby the approach utilizing o-dihalobenzene as the partners of the nitriles. Reactionmechanism involves hydrolysis of the nitriles, an intermolecular C-N cross-coupling,and an intramolecular C-O cross-coupling. One-pot of this reaction undergo so muchreaction processes and get a good yield, it make this reaction conducive to apply in thesynthesis of natural products and drug molecules.