Diastereoselective Intramolecular Friedel–Crafts Cyclizations of Substituted Methyl 2-(1<i>H</i>-indole-1-carbonyl)acrylates: Efficient Access to Functionalized 1<i>H</i>-Pyrrolo[1,2-<i>a</i>]indoles

Abstract

A general, catalytic method for the diastereoselective synthesis of functionalized 1H-pyrrolo[1,2-a]indoles via an intramolecular Friedel-Crafts alkylation of N-acyl indoles is reported. Products were obtained in excellent yields (up to 98%) with high diastereoselectivities (up to >25:1 dr).