State Key Laboratory of Coordination Chemistry, Chemistry and Biomedicine Innovation Center of Nanjing University, Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, China.
Methods Mol Biol. 2022;2371:31-42. doi: 10.1007/978-1-0716-1689-5_3.
Cyclic peptides are an important class of bioactive compounds for the chemical biology and pharmaceutical industry. Chemical synthesis of highly constrained cyclic peptides is often challenging. Here we describe the synthetic strategy of peptide macrocyclization through late-stage palladium-catalyzed C-H activation. These methods utilize endogenous backbone amides in the peptide sequence as directing groups and are efficient in the preparation of small-to-middle size peptide macrocycles.
环肽是化学生物学和制药行业中一类重要的生物活性化合物。高度约束的环肽的化学合成通常具有挑战性。在这里，我们描述了通过晚期钯催化 C-H 活化进行肽大环化的合成策略。这些方法利用肽序列中的内源性骨架酰胺作为导向基团，在小至中等大小的肽大环的制备中非常有效。
