Palladium‐Catalyzed Aryl Amination–Heck Cyclization Cascade: A One‐Flask Approach to 3‐Substituted Indoles

Abstract

Two for the price of one: A Pd/dppf-based catalyst provides access to the title compounds from 1,2-dihalogenated aromatic compounds and allylic amines in a single reaction flask. The initial aryl amination step occurs with excellent selectivity for the aryl iodide to ensure the formation of a single indole regioisomer, which can be functionalized in situ by N-arylation (see scheme). dba=dibenzylideneacetone, dppf=1,1′-bis(diphenylphospanyl)ferrocene. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2008/z703763_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.