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An Organotrifluoroborate for Broadly Applicable One‐Step 18F‐Labeling |
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| Authors: | Zhibo Liu Maral Pourghiasian Mark Alex Radtke Joseph Lau Dr. Jinhe Pan Gemma M. Dias Dr. Donald Yapp Dr. Kuo‐Shyan Lin Prof. Dr. Francois Bénard Prof. Dr. David M. Perrin |
| Affiliation: | 1. Chemistry Department, University of British Columbia, 2036 Main Mall, Vancouver, BC, V6T‐1Z1 (Canada);2. Experimental Therapeutics, B.C. Cancer Research Agency, 675 West 10th Avenue, Vancouver, BC, V5Z‐1L3 (Canada);3. Molecular Oncology, B.C. Cancer Research Agency, 675 West 10th Avenue, Vancouver, BC, V5Z‐1L3 (Canada) |
| 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. |
| Keywords: | 18F‐labeling bioconjugation click chemistry peptides PET imaging |