One-Pot Approach to 1,2-Disubstituted Indoles via Cu(II)-Catalyzed Coupling/Cyclization under Aerobic Conditions and Its Application for the Synthesis of Polycyclic Indoles

A straightforward assembly of 1,2-disubstituted indoles has been developed through a Cu­(II)-catalyzed domino coupling/cyclization process. Under aerobic conditions, a wide range of 1,2-disubstituted indole derivatives were efficiently and facilely synthesized from 2-alkynylanilines and boronic acids. 2-(2-Bromoaryl)-1-aryl-1H-indoles, which were selectively generated in one pot under the Cu catalysis, afforded the indolo­[1,2-f]­phenanthridines via Pd-catalyzed intramolecular direct C­(sp²)–H arylation. The one-pot tandem approaches to the polycyclic indole derivatives were also successfully achieved.