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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Auteurs principaux:	Constantin Mamat, Christian Jentschel, Martin Köckerling, Jörg Steinbach
Format:	article
Langue:	EN
Publié:	MDPI AG 2021
Sujets:	M(CO)<sub>3</sub> <sup>99m</sup>Tc matched pair theranostic approach click chemistry bioorthogonal Organic chemistry QD241-441
Accès en ligne:	https://doaj.org/article/465b5f80fc874b51b4d614c57761cea9
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spelling	oai:doaj.org-article:465b5f80fc874b51b4d614c57761cea92021-11-11T18:36:00ZStrategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core10.3390/molecules262166291420-3049https://doaj.org/article/465b5f80fc874b51b4d614c57761cea92021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6629https://doaj.org/toc/1420-3049The 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.Constantin MamatChristian JentschelMartin KöckerlingJörg SteinbachMDPI AGarticleM(CO)<sub>3</sub><sup>99m</sup>Tcmatched pairtheranostic approachclick chemistrybioorthogonalOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6629, p 6629 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	M(CO)<sub>3</sub> <sup>99m</sup>Tc matched pair theranostic approach click chemistry bioorthogonal Organic chemistry QD241-441
spellingShingle	M(CO)<sub>3</sub> <sup>99m</sup>Tc matched pair theranostic approach click chemistry bioorthogonal Organic chemistry QD241-441 Constantin Mamat Christian Jentschel Martin Köckerling Jörg Steinbach Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core
description	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.
format	article
author	Constantin Mamat Christian Jentschel Martin Köckerling Jörg Steinbach
author_facet	Constantin Mamat Christian Jentschel Martin Köckerling Jörg Steinbach
author_sort	Constantin Mamat
title	Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core
title_short	Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core
title_full	Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core
title_fullStr	Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core
title_full_unstemmed	Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core
title_sort	strategic evaluation of the traceless staudinger ligation for radiolabeling with the tricarbonyl core
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/465b5f80fc874b51b4d614c57761cea9
work_keys_str_mv	AT constantinmamat strategicevaluationofthetracelessstaudingerligationforradiolabelingwiththetricarbonylcore AT christianjentschel strategicevaluationofthetracelessstaudingerligationforradiolabelingwiththetricarbonylcore AT martinkockerling strategicevaluationofthetracelessstaudingerligationforradiolabelingwiththetricarbonylcore AT jorgsteinbach strategicevaluationofthetracelessstaudingerligationforradiolabelingwiththetricarbonylcore
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Strategic Evaluation of the Traceless Staudinger Ligation for Radiolabeling with the Tricarbonyl Core

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