Nickel Photocatalytic Access to β‐Arylated β‐Amino Acids
Year: 2026
Type: article
Abstract: 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.
Source: Advanced Synthesis & Catalysis
DOI: 10.1002/adsc.70586
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: hybrid
Estimated APC paid: $4,650
OpenAlex ID: W7165022279