A novel versatile precursor suitable for 18F-radiolabeling via 'click chemistry'.

Autor: Lugato, B., Stucchi, S., Ciceri, S., Iannone, M.N., Turolla, E.A., Giuliano, L., Chinello, C., Todde, S., Ferraboschi, P.
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Zdroj: Journal of Labelled Compounds & Radiopharmaceuticals; Aug2017, Vol. 60 Issue 10, p466-480, 15p
Abstrakt: As an effort to improve 18F-radiolabeling of biomolecules in method robustness and versatility, we report the synthesis and radiolabeling of a new azido precursor potentially useful for the so-called 'click reaction,' in particular the ligand-free version of the copper(I)-catalyzed alkyne-azide cycloaddition. The new azido precursor may help to overcome problems sometimes exhibited by most of the currently used analogues, as it is safe to handle and it displays long-term chemical stability, thus facilitating the development of new radiolabeling procedures. Moreover, the formed 18F-labeled 1,2,3-triazole is potentially metabolically stable and could enhance the in vivo circulation time. The above azido precursor was successfully radiolabeled with 18F, with 51% radiochemical yield (nondecay-corrected). As a proof of concept, the 18F-labeled azide was then tested with a suitable alkyne functionalized aminoacid ( l-propargylglycine), showing 94% of conversion, and a final radiochemical yield of 27% (>99% radiochemical purity), nondecay-corrected, with a total preparation time of 104 minutes. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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