Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core
The traceless Staudinger ligation with its two variants is a powerful biorthogonal conjugation method not only for the connection of biomolecules, but also for the introduction of fluorescence- or radiolabels under mild reaction conditions. Herein, the strategic evaluation of the traceless Staudinge...
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| Main Authors: | , , , |
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| Format: | article |
| Language: | EN |
| Published: |
MDPI AG
2021
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| Subjects: | |
| Online Access: | https://doaj.org/article/465b5f80fc874b51b4d614c57761cea9 |
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| Summary: | The traceless Staudinger ligation with its two variants is a powerful biorthogonal conjugation method not only for the connection of biomolecules, but also for the introduction of fluorescence- or radiolabels under mild reaction conditions. Herein, the strategic evaluation of the traceless Staudinger ligation for radiolabeling <sup>99m</sup>Tc using the <i>fac</i>-[Tc(CO)<sub>3</sub>]<sup>+</sup> core is presented. A convenient and high-yielding three-step synthetic procedure of dipicolylamine-based phosphanols as ligands for the mild radiolabeling was developed. The labeling was accomplished using a tricarbonyl kit and a <sup>99m</sup>Tc-pertechnetate generator eluate showing 87% radiochemical conversion. The respective rhenium-based, non-radioactive reference compounds were synthesized using (Et<sub>4</sub>N)<sub>2</sub>[Re(CO)<sub>3</sub>Br<sub>3</sub>] as precursor. All products were analyzed by NMR, MS, and elemental analysis. Additional XRD analyses were performed. |
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