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Updated: Feb 11, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Direct Enantioselective α-Allylation of Unfunctionalized Cyclic Ketones with Alkynes through Pd-Amine Cooperative
1Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore, 117543, Singapore.
Abstract:
The first direct enantioselective α-allylation of unfunctionalized cyclic ketones using alkynes as an economical choice of reagent is reported. This transformation uses a simple procedure with commercially available palladium, chiral bisphosphine ligand and chiral amine catalysts, and affords valuable ketones with a α-tertiary stereocenter in good to high enantiopurity. In this transformation, a chiral palladium complex containing the (S)-DIFLUORPHOS ligand catalyzes the isomerization of alkynes into an electrophilic allylpalladium species, which is attacked by the enamine generated in situ from the condensation of (R)-prolinol with the ketone substrate.
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