An Efficient Solid‐Phase Synthetic Approach to Prepare TACN‐Functionalized Peptides DOI Open Access
Yik‐Hoi Yeung, Pak‐Lun Lam, Waygen Thor

et al.

Chemistry - Methods, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 3, 2025

Abstract 1,4,7‐triazacyclononane (TACN) derivatives play important roles in various metal‐based biomedical applications. However, the unmanageable functionalization of TACN remains a long‐standing challenge to yield useful partially substituted building blocks. Herein, by utilizing nitrobenzoxadiazole (NBD) as thiol‐liable protecting group for secondary amines, bis ‐NBD‐substituted was obtained first example preparation without strict stoichiometric control and column chromatography. Upon facile deprotection NBD using solid‐phase synthesis, series TACN‐peptide conjugates with different bioactive peptides chelating units were derivatized from block, demonstrating potential widespread application this work.

Language: Английский

An Efficient Solid‐Phase Synthetic Approach to Prepare TACN‐Functionalized Peptides DOI Open Access
Yik‐Hoi Yeung, Pak‐Lun Lam, Waygen Thor

et al.

Chemistry - Methods, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 3, 2025

Abstract 1,4,7‐triazacyclononane (TACN) derivatives play important roles in various metal‐based biomedical applications. However, the unmanageable functionalization of TACN remains a long‐standing challenge to yield useful partially substituted building blocks. Herein, by utilizing nitrobenzoxadiazole (NBD) as thiol‐liable protecting group for secondary amines, bis ‐NBD‐substituted was obtained first example preparation without strict stoichiometric control and column chromatography. Upon facile deprotection NBD using solid‐phase synthesis, series TACN‐peptide conjugates with different bioactive peptides chelating units were derivatized from block, demonstrating potential widespread application this work.

Language: Английский

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