Optimization of a 1,4,7-Triazacyclononane-1,4-diacetic acid (NODA) Derivative Radiofluorination by Al 18 F Complexation Using a Design of Experiments Approach.

Autor:	San C; Laboratoire GBCM, EA7528, Conservatoire National des Arts et Métiers, HESAM Université, 2 rue Conté, 75003, Paris, France.; Unité Claude Kellershohn, Institut de Recherche Saint-Louis, Hôpital Saint-Louis, Université Paris Cité, 1 avenue Claude Vellefaux, 75010, Paris, France., Hosten B; Unité Claude Kellershohn, Institut de Recherche Saint-Louis, Hôpital Saint-Louis, Université Paris Cité, 1 avenue Claude Vellefaux, 75010, Paris, France.; INSERM UMR-S 1144, Optimisation Thérapeutique en Neuropsychopharmacologie, Université Paris Cité, 4 avenue de l'Observatoire, 75006, Paris, France., Vignal N; Unité Claude Kellershohn, Institut de Recherche Saint-Louis, Hôpital Saint-Louis, Université Paris Cité, 1 avenue Claude Vellefaux, 75010, Paris, France., Beddek M; Unité Claude Kellershohn, Institut de Recherche Saint-Louis, Hôpital Saint-Louis, Université Paris Cité, 1 avenue Claude Vellefaux, 75010, Paris, France., Pillet M; Laboratoire SYMME, EA 4144, Université Savoie Mont-Blanc, 7 chemin de Bellevue, 74940, Annecy, France., Sarda-Mantel L; Unité Claude Kellershohn, Institut de Recherche Saint-Louis, Hôpital Saint-Louis, Université Paris Cité, 1 avenue Claude Vellefaux, 75010, Paris, France., Port M; Laboratoire GBCM, EA7528, Conservatoire National des Arts et Métiers, HESAM Université, 2 rue Conté, 75003, Paris, France., Dioury F; Laboratoire GBCM, EA7528, Conservatoire National des Arts et Métiers, HESAM Université, 2 rue Conté, 75003, Paris, France.
Jazyk:	angličtina
Zdroj:	Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2023 Dec 19; Vol. 29 (71), pp. e202302745. Date of Electronic Publication: 2023 Oct 31.
DOI:	10.1002/chem.202302745
Abstrakt:	Fluorine-18 ( 18 F) is the most favorable positron emitter for radiolabeling Positron Emission Tomography (PET) probes. However, conventional 18 F labeling through covalent C-F bond formation is challenging, involving multiple steps and stringent conditions unsuitable for sensitive biomolecular probes whose integrity may be altered. Over the past decade, an elegant new approach has been developed involving the coordination of an aluminum fluoride {Al 18 F} species in aqueous media at a late-stage of the synthetic process. The objective of this study was to implement this method and to optimize radiolabeling efficiency using a Design of Experiments (DoE). To assess the impact of various experimental parameters on {Al 18 F} incorporation, a pentadentate chelating agent NODA-MP-C4 was prepared as a model compound. This model carried a thiourea function present in the final conjugates resulting from the grafting of the chelating agent onto the probe. The formation of the radioactive complex Al 18 F-NODA-MP-C4 was studied to achieve the highest radiochemical conversion. A complementary "cold" series study using the natural isotope 19 F was also conducted to guide the radiochemical operating conditions. Ultimately, Al 18 F-NODA-MP-C4 was obtained with a reproducible and satisfactory radiochemical conversion of 79±3.5 % (n=5). (© 2023 The Authors. Chemistry - A European Journal published by Wiley-VCH GmbH.)
Databáze:	MEDLINE
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