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

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 F-18-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/mu mol) and at > 98% purity. PET imaging shows in vivo stability and tumor uptake.