Nickel Photocatalytic Access to β‐Arylated β‐Amino Acids

Noncanonical amino acids are prevalent handles in drug discovery to improve pharmacological properties. Here, we present a nickel‐photocatalytic method that yields β‐arylated β‐amino acids from abundant aspartic acid as natural amino acid and widely available (hetero)aryl bromides as cross‐coupling electrophiles. Utilizing dimethoxyethane as solvent and tert ‐butyl tetramethylguanidine (BTMG) as base gives highest yields, and various functional groups were tolerated in the final amino acid products. More than 21 non‐canonical amino acids were obtained in up to good yields, and diversification enabled the synthesis of bioactive derivatives, ready for follow‐up application. This concept of using naturally occurring amino acids as starting materials allows for access to non‐canonical counterparts under mild and photocatalytic control.