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Updated: Jun 18, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Rh-Catalyzed Asymmetric Arylative Cyclization of Alkyne-Tethered Aliphatic Ketones: Access to Enantioenriched
Mingfeng Zhang1,2, Haining Xu1,2, Qi Chen1,2
1School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Abstract:
By employing a simple and readily available chiral difluorphos ligand, a highly enantioselective rhodium-catalyzed asymmetric arylation tandem cyclization of heteroatom-containing alkyne-tethered aliphatic ketones with boronic acids was achieved under mild conditions. This protocol offers efficient and practical access to a broad spectrum of chiral heterocyclic tertiary allylic alcohols bearing trisubstituted or tetrasubstituted alkene functionality in good yields (up to 86%) with excellent enantioselectivities (up to 99% ee). Moreover, the synthetic utility of this methodology has been demonstrated via the rapid and concise construction of various structurally intriguing chiral heterocyclic architectures.
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