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Ligand‐Enabled γ‐C(sp <sup>3</sup> )−H Olefination of Free Carboxylic Acids

Kiron Kumar Ghosh, Alexander Uttry, Arup Mondal, Francesca Ghiringhelli, Philipp Wedi, Manuel van Gemmeren

2020Angewandte Chemie International Edition81 citationsDOIOpen Access PDF

Abstract

We report the ligand-enabled C-H activation/olefination of free carboxylic acids in the γ-position. Through an intramolecular Michael addition, δ-lactones are obtained as products. Two distinct ligand classes are identified that enable the challenging palladium-catalyzed activation of free carboxylic acids in the γ-position. The developed protocol features a wide range of acid substrates and olefin reaction partners and is shown to be applicable on a preparatively useful scale. Insights into the underlying reaction mechanism obtained through kinetic studies are reported.

Topics & Concepts

Ligand (biochemistry)Carboxylic acidChemistryStereochemistryCombinatorial chemistryMedicinal chemistryOrganic chemistryBiochemistryReceptorCatalytic C–H Functionalization MethodsSynthesis and Catalytic ReactionsAsymmetric Hydrogenation and Catalysis
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