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Highly Enantioselective Iridium(I)‐Catalyzed Hydrocarbonation of Alkenes: A Versatile Approach to Heterocyclic Systems Bearing Quaternary Stereocenters

Andrés Arribas, Martín Calvelo, David F. Fernández, Catarina A. B. Rodrigues, José L. Mascareñas, Fernando López

2021Angewandte Chemie International Edition53 citationsDOIOpen Access PDF

Abstract

We report a versatile, highly enantioselective intramolecular hydrocarbonation reaction that provides a direct access to heteropolycyclic systems bearing chiral quaternary carbon stereocenters. The method, which relies on an iridium(I)/bisphosphine chiral catalyst, is particularly efficient for the synthesis of five-, six- and seven-membered fused indole and pyrrole products, bearing one and two stereocenters, with enantiomeric excesses of up to >99 %. DFT computational studies allowed to obtain a detailed mechanistic profile and identify a cluster of weak non-covalent interactions as key factors to control the enantioselectivity.

Topics & Concepts

StereocenterEnantioselective synthesisIridiumIntramolecular forceEnantiomerCombinatorial chemistryOrganocatalysisChemistryPyrroleCatalysisIndole testStereochemistryOrganic chemistryAsymmetric Hydrogenation and CatalysisCatalytic C–H Functionalization MethodsAsymmetric Synthesis and Catalysis
Highly Enantioselective Iridium(I)‐Catalyzed Hydrocarbonation of Alkenes: A Versatile Approach to Heterocyclic Systems Bearing Quaternary Stereocenters | Litcius