Development of 18 F-Labeled hydrophilic trans -cyclooctene as a bioorthogonal tool for PET probe construction.

We report the development of a hydrophilic 18 F-labeled a-TCO derivative [ 18 F]3 (log  P = 0.28) through a readily available precursor and a single-step radiofluorination reaction (RCY up to 52%). We demonstrated that [ 18 F]3 can be used to construct not only multiple small molecule/peptide-based PET agents, but protein/diabody-based imaging probes in parallel.