Visible-Light-Driven Three-Component Reaction of Unactivated Alkenes Enables Access to Monofluoro ?-Amino Acids

A strategy for the synthesis of diverse protected a-monofluoro-?-amino acid derivatives has been developed. This reaction assembles a simple enamide, quinoxalin-2(1H)-one, and diethyl 2-bromo-2-fluoromalonate through a three-component reaction driven by visible light. The advantages of this protocol include the simplicity of its operation, mild conditions, high functional group tolerance, and applicability to a wide variety of substrates. The synthesis of this fluorine-containing amino acid derivative has significant value for potential applications in medicinal chemistry and chemical biology.