Catalytic Asymmetric Mono‐Fluorination of α‐Keto Esters: Synthesis of Optically Active β‐Fluoro‐α‐Hydroxy and β‐Fluoro‐α‐Amino Acid Derivatives

Enantioselective mono-fluorination of α-keto esters was achieved using a mildly basic palladium μ-hydroxo complex as catalyst. Subsequent one-pot reduction afforded optically active β-fluoro-α-hydroxy esters. These compounds were then converted into β-fluoro-α-amino esters, which are potentially useful in medicinal chemistry research.