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A new 18F-heteroaryltrifluoroborate radio-prosthetic with greatly enhanced stability that is labelled by 18F-19F-isotope exchange in good yield at high specific activity

TitleA new 18F-heteroaryltrifluoroborate radio-prosthetic with greatly enhanced stability that is labelled by 18F-19F-isotope exchange in good yield at high specific activity
Publication TypeJournal Article
Year of Publication2014
AuthorsLiu, Z, Hundal-Jabal, N, Wong, M, Yapp, D, Lin, K-S, Benard, F, Perrin, DM
JournalMed. Chem. Commun.
Volume5
Pagination171-179
Abstract

An 18F-heteroaryltrifluoroborate was designed as a novel radioprosthetic for PET imaging. The stability of the new prosthetic was confirmed using 19F-NMR spectroscopy: the solvolytic half-life was measured to be >16 000 min. Conjugation to RGD gave a stable radiotracer precursor for kit-like labeling by 18F-19F isotope exchange in 15 min. The total radiosynthetic procedure including HPLC purification requires <45 min. A plasma stability assay showed negligible defluoridation following 150 min and stability is corroborated by in vivo imaging showing minimal bone uptake. With Curie levels of 18F-fluoride{,} yields of 20% and specific activities as high as 3 Ci [small mu ]mol-1 (110 GBq [small mu ]mol-1) are achieved (n = 3).

URLhttp://dx.doi.org/10.1039/C3MD00328K
DOI10.1039/C3MD00328K