Copper Catalyzed Intramolecular N-Arylation of Ketene Aminals at Room Temperature: Synthesis of 2-Amino-3-cyanoindoles

Various 2-amino-3-cyanoindoles are synthesized through copper catalyzed intramolecular N-arylations of ketene aminals at room temperature for the first time with 60-99% yields within 0.1-2 h. Controlled regioselective N-arylations of unsymmetrical ketene aminals are also studied. Further, a new double heteroannulation approach is demonstrated for the synthesis of 11-aminoindolo[2,3-b]quinolines from acyclic and nonheterocyclic precursors.