Cu-catalyzed alkynylation of thiosulfonate-based peptide: an efficient approach to S-alkynyl-containing cyclic peptides - Details

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Zhang, Z. (Zhang, Z..) ^[1] | Ying, J. (Ying, J..) ^[2] | Lu, Q. (Lu, Q..) ^[3] | Zhang, Q. (Zhang, Q..) ^[4] | Xu, C. (Xu, C..) ^[5]

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Abstract：

Cyclic　peptides　are　highly　valued　in　drug　discovery　due　to　their　enhanced　biological　properties.　Despite　their　potential,　the　construction　of　an　S-alkynyl　moiety　in　a　cyclic　peptide　remains　challenging　due　to　limited　synthetic　strategies.　Herein,　we　describe　a　copper-catalyzed　alkynylation　of　thiosulfonate-based　peptides,　enabling　efficient　and　selective　synthesis　of　S-alkynylated　cysteines　and　peptides.　The　adjustment　of　the　amount　of　base　could　significantly　increase　the　efficiency.　This　method　features　a　broad　substrate　scope,　operational　simplicity　and　compatibility　with　complex　peptide　structures.　©　2025　The　Royal　Society　of　Chemistry.

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[ 1 ] [Zhang Z.]Key Laboratory of Molecular Synthesis and Functionalization Discovery, College of Chemistry, Fuzhou University, Fuzhou, 350108, China
[ 2 ] [Ying J.]Key Laboratory of Molecular Synthesis and Functionalization Discovery, College of Chemistry, Fuzhou University, Fuzhou, 350108, China
[ 3 ] [Lu Q.]Key Laboratory of Molecular Synthesis and Functionalization Discovery, College of Chemistry, Fuzhou University, Fuzhou, 350108, China
[ 4 ] [Zhang Q.]Key Laboratory of Molecular Synthesis and Functionalization Discovery, College of Chemistry, Fuzhou University, Fuzhou, 350108, China
[ 5 ] [Xu C.]Key Laboratory of Molecular Synthesis and Functionalization Discovery, College of Chemistry, Fuzhou University, Fuzhou, 350108, China
[ 6 ] [Xu C.]Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, CAS, Shanghai, 200032, China

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Organic Chemistry Frontiers

ISSN： 2052-4110

Year： 2025

Issue： 8

Volume： 12

Page： 2752-2758

4 . 6 0 0

JCR@2023

CAS Journal Grade：2

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