An efficient approach to 1,2,3-trisubstituted indole via rhodium catalyzed carbene Csp3–H bond insertion

Abstract

A method for convenient synthesis of N-alkyl-2-aryl-indole-3-carbaldehyde has been described. A variety of highly valuable indolyl aldehydes have been prepared through this method. Electron donating groups on both aromatic rings (anilinyl and benzyl) facilitate the formation of the desired products. A benzylic C–H insertion by rhodium carbene is the key step for this transformation.