Synthesis of 4-Alkylindoles from 2-Alkynylanilines via Dearomatization- and Aromatization-Triggered Alkyl Migration

Org Lett. 2021 Mar 19;23(6):2130-2134. doi: 10.1021/acs.orglett.1c00280. Epub 2021 Mar 10.

Abstract

A simple method for rapid synthesis of 4-alkylindoles from 2-alkynylanilines was reported. The protocol involves an oxidative dearomatization and an aromatization triggered regioselective alkyl migration. A range of alkyl groups including linear, branched, or cycloalkyl groups can be introduced into the C4 position of indole.

Publication types

  • Research Support, Non-U.S. Gov't