| Title | 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 |
| Publication Type | Journal Article |
| Year of Publication | 2014 |
| Authors | Liu, Z, Hundal-Jabal, N, Wong, M, Yapp, D, Lin, K-S, Benard, F, Perrin, DM |
| Journal | Med. Chem. Commun. |
| Volume | 5 |
| Pagination | 171-179 |
| 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). |
| URL | http://dx.doi.org/10.1039/C3MD00328K |
| DOI | 10.1039/C3MD00328K |
