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18F labeling strategies for unmodified peptides with [18F]fluoride require 18F-labeled prosthetics for bioconjugation more often with cysteine thiols or lysine amines. Here we explore selective radical chemistry to target aromatic residues applying C-H 18F-trifluoromethylation. We report a one-step route to [18F]CF3SO2NH4 from [18F]fluoride and its application to direct [18F]CF3 incorporation at tryptophan or tyrosine residues using unmodified peptides as complex as recombinant human insulin. The fully automated radiosynthesis of octreotide[Trp(2-CF218F)] enables in vivo positron emission tomography imaging.

Original publication




Journal article


J Am Chem Soc

Publication Date





1180 - 1185


Chlorofluorocarbons, Methane, Fluorine Radioisotopes, Methylation, Peptides, Positron-Emission Tomography, Radiopharmaceuticals, Sulfur Compounds