| Title | An Organotrifluoroborate for Broadly Applicable One-Step 18F-Labeling |
| Publication Type | Journal Article |
| Year of Publication | 2014 |
| Authors | Liu, Z, Pourghiasian, M, Radtke, MAlex, Lau, J, Pan, J, Dias, GM, Yapp, D, Lin, K-S, Bénard, F, Perrin, DM |
| Journal | Angewandte Chemie International Edition |
| Volume | 53 |
| Pagination | 11876–11880 |
| ISSN | 1521-3773 |
| Keywords | 18F-labeling, bioconjugation, click chemistry, PEPTIDES, PET imaging |
| Abstract | A new zwitterionic organotrifluoroborate is appended to three radiosynthons that afford undergo facile bioconjugation to several clinically relevant peptides and one enzyme inhibitor. Molecularly complex bioconjugates are 18F-labeled in a single aqueous step in rapid time (<15 min) without HPLC purification to afford tracers in good yields (>200 mCi, 20–40 %) at high specific activity (≥3 Ci/μmol) and at >98 % purity. PET imaging shows in vivo stability and tumor uptake. |
| URL | http://dx.doi.org/10.1002/anie.201406258 |
| DOI | 10.1002/anie.201406258 |
