Photoredox‐Catalyzed Minisci‐Type Acylation of Heterocyclic C−H Bonds with Amino Acid‐Tethered Dihydropyridines

Abstract Conjugation of amino acids to bioactive molecules has emerged as a promising strategy for optimizing pharmacological profiles of lead candidates in drug discovery. This study describes a photocatalytic Minisci‐type transfer reaction of N ‐acyl amino acids into various N ‐heterocycles. Notably, this protocol enables direct conjugation of amino acids into heterocyclic C−H bonds, eliminating the need for prefunctionalized substrates. A diverse array of N ‐heterocycles, amino acids, oligopeptides, and drugs were used to demonstrate the potential of the proposed approach. In addition, the importance of this approach is demonstrated through its application in the DNA‐encoded library chemistry. Various synthetic transformations and preliminary mechanistic investigations were also explored.