Facile Synthesis of 2‐(Perfluoroalkyl)indoles through a Michael Addition/Cu^I‐Catalyzed Annulation Process

Abstract

Abstract A practical and economical process for the synthesis of perfluoroalkylated indole compounds has been developed. The Michael addition of 2‐iodo‐ or 2‐bromoanilines to methyl perfluoroalk‐2‐ynoates affords N ‐( o ‐haloaryl)enamines, which subsequently undergo a copper‐catalyzed annulation reaction to give 2‐perfluoroalkyl‐substituted indoles in good to excellent yields. This method displays excellent functional group tolerance and is carried out in one pot under mild conditions.