Study On CuH Catalyzed Cyclization Reaction Of Alkenylaryl Isocyanides:Synthesis Of Indole Derivatives

Indoles are important sturctural unit of alkaloids and pharmaceutical agents, such as Tryptophan (for nutritional agents), Indomethacin (for inflammation). In addition, indoles are important synthetic intermediates, which were widely used as the building blocks in organic synthesis. Hence, development of the new approaches for the synthesis of indoles is highly desirable for organic chemists.Recently, various transformations based on CuH catalysis have been attracted considerable attentions. While most of substrates are limited to unsaturated hydrocarbons, this fact which highly restrict their further applications. As a consequence, copper-catalyzed cyclization reactions of alkenylaryl isocyanides are quite rare. Therefore, development of a novel approach for the cyclization of alkenylaryl isocyanides via copper catalysis manner is highly appealing and this transformation will be quite valuable and very useful for organic synthesis.In this thesis, we developed a new method for the synthesis of indole derivatives, by employing 2-vinylaryl isocyanides as substrates, CuOAc as catalyst, PPh3 as ligand and PhSiH3 as hydrogen source via in situ generating CuH species manner under mild condition. Furthermore, this strategy provides a new avenue for synthesis of the versatile indole derivatives.