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Updated: Jan 19, 2026

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
Published on: September 28, 2022
Macrocyclization of Biaryl-Bridged Peptides through Late-Stage Palladium-Catalyzed C(sp2)-H Arylation
Qingqing Bai1, Zengbing Bai1, Huan Wang1
1State 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 210093 , China.
Abstract:
Macrocyclic peptides are promising scaffolds of bioactive compounds and clinical therapeutics. Herein, we develop a strategy for the macrocyclization of biaryl-bridged peptides through late-stage Pd-catalyzed C(sp2)-H arylation. This method displays broad substrate scope and high efficiency in the synthesis of peptide conjugates with various bioactive molecules. Furthermore, we applied this method to prepare peptide macrocycles with aryl-aryl cross-links. Our results show the effectiveness of backbone amide groups as directing groups in Pd-catalyzed C-H functionalization of peptides.
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