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Updated: Apr 1, 2026

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
Published on: September 28, 2022
Highly efficient and fast pre-activation cyclization of the long peptide: Succinimidyl ester-amine reaction revisited
Se-Hwan Choi1, Woo-jin Jeong1, Sung-ju Choi1
1Translational Research Center for Protein Function Control & Department of Materials Science & Engineering, Yonsei University, Seoul 120-749, Republic of Korea.
Abstract:
A new method for the pre-activation cyclization of a long peptide is described. The approach involves the formation of a pre-activated succinimidyl ester species in advance of amidation, which completely eliminates the potentially troublesome amine end-capping side reaction. The cyclization reactions proceed with high efficiency and fast reaction kinetics for the long peptide with 25 residues. The exploration and large-scale preparation of synthetic cyclic peptides should become more accessible and feasible with this approach. This method has a potential to be further applied for the synthesis of much longer and more complex cyclic peptides.
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