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 a thiol-liable protecting group for secondary amines, a bis-NBD-substituted TACN was obtained as the first example in the preparation of partially substituted TACN without strict stoichiometric control and column chromatography. Upon facile deprotection of NBD using solid-phase synthesis, a series of TACN-peptide conjugates with different bioactive peptides and chelating units were derivatized from the TACN building block, demonstrating the potential widespread application of this work.
Original language | English |
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Article number | e202400053 |
Number of pages | 5 |
Journal | Chemistry-Methods |
Volume | 5 |
Issue number | 5 |
Early online date | 3 Feb 2025 |
DOIs | |
Publication status | Published - May 2025 |
User-Defined Keywords
- 1,4,7-Triazacyclononane (TACN)
- nitrobenzoxadiazole (NBD)
- peptide conjugates
- Positron Emission Tomography (PET)
- protecting group