An Operationally Simple Approach to Indole Derivatives from 2-Alkenylanilines Utilizing an Oxidation–Intramolecular Cyclization–Elimination Sequence

Abstract

Herein we describe a novel route to indole derivatives from a variety of N-substituted 2-alkenylanilines. This route features three operationally simple steps: (1) oxidation to convert N-substituted 2-alkenylanilines into epoxide intermediates, (2) intramolecular cyclization, and (3) the acid-catalyzed elimination of water.

Keywords

• metal-free indole synthesis
• epoxidation
• intramolecular cyclization