Base-Promoted Tandem Synthesis of 2‑Substituted Indoles and N‑Fused Polycyclic Indoles

Herein is developed a base-promoted approach for the synthesis of C2-substituted indoles and -fused polycyclic indoles via 5-- cyclization of 2-alkynyl anilines, followed by a 1,3'-acyl migration or a dearomatizing Michael addition process. A range of N-H free indoles and 8,9-dihydropyrido[1,2-]indol-6(7)-one scaffolds were synthesized in good to excellent yields with broad scope.