Palladium Catalyzed Regioselective C4‐Arylation and Olefination of Indoles and Azaindoles

Abstract A convergent strategy for the synthesis of biologically relevant C4‐substituted indole scaffolds was demonstrated using Pd(II)‐catalyzed remote C−H functionalization of indoles and azaindoles. The reaction displays high regioselectivity for the C4‐position of indole‐3‐carbaldehydes using glycine as an inexpensive transient directing group. Notable features of this transformation include the selective formation of six‐membered palladacyle and excellent functional group tolerance. magnified image