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An Organotrifluoroborate for Broadly Applicable One-Step 18F-Labeling

TitleAn Organotrifluoroborate for Broadly Applicable One-Step 18F-Labeling
Publication TypeJournal Article
Year of Publication2014
AuthorsLiu, Z, Pourghiasian, M, Radtke, MAlex, Lau, J, Pan, J, Dias, GM, Yapp, D, Lin, K-S, Bénard, F, Perrin, DM
JournalAngewandte Chemie International Edition
Keywords18F-labeling, bioconjugation, click chemistry, PEPTIDES, PET imaging

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.