Straightforward Access to Enantioenriched cis -3-Fluoro-dihydroquinolin-4-ols Derivatives via Ru(II)-Catalyzed-Asymmetric Transfer Hydrogenation/Dynamic Kinetic Resolution.
Ricardo Molina BetancourtPhannarath PhansavathVirginie Ratovelomanana-VidalPublished in: Molecules (Basel, Switzerland) (2022)
Herein we report a practical method for the asymmetric transfer hydrogenation/dynamic kinetic resolution of N -Boc 3-fluoro-dihydrotetrahydroquinolin-4-ones into the corresponding cis -fluoro alcohols in 70-96% yields, up to 99:1 diastereomeric ratio (dr) and up to >99% ee (enantiomeric excess) by using the ruthenium complex Ts-DENEB and a formic acid/triethylamine (1:1) mixture as the hydrogen donor under mild conditions.