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.

氨基酸与生物活性分子的偶联已成为在药物发现中优化先导候选药物的药理学特征的一种很有前途的策略。本研究描述了 N-酰基氨基酸向各种 N-杂环的光催化 Minisci 型转移反应。值得注意的是，该方案能够将氨基酸直接偶联成杂环 C-H 键，无需预功能化底物。使用了多种 N-杂环、氨基酸、寡肽和药物来证明所提出的方法的潜力。此外，这种方法在 DNA 编码的文库化学中的应用证明了该方法的重要性。还探索了各种合成变换和初步机制研究。