Indoles from Simple Anilines and Alkynes: Palladium-Catalyzed C-H Activation Using Dioxygen as the Oxidant

摘要

Indoles are ubiquitous bioactive heterocycles in nature.Their importance in medicinal chemistry has stimulated considerable interest from organic chemists, and has encouraged the development of new synthetic strategies to prepare these compounds. In the past decades, transition-metal-catalyzed intermolecular cyclizations of ortho-halogenated anilines with internal alkynes have emerged as a powerful method for constructing indoles (Scheme la).