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Journal Article

Site‐Specific Deoxyfluorination of Small Peptides with [18F]Fluoride

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Rickmeier,  Jens
Research Department Ritter, Max-Planck-Institut für Kohlenforschung, Max Planck Society;

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Ritter,  Tobias
Research Department Ritter, Max-Planck-Institut für Kohlenforschung, Max Planck Society;

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Citation

Rickmeier, J., & Ritter, T. (2018). Site‐Specific Deoxyfluorination of Small Peptides with [18F]Fluoride. Angewandte Chemie International Edition, 57(43), 14207-14211. doi:10.1002/anie.201807983.


Cite as: https://hdl.handle.net/21.11116/0000-0003-5755-C
Abstract
Radiolabeled receptor‐binding peptides are an important class of positron emission tomography tracers owing to achievable high binding affinities and their rapid blood clearance. Herein, a method to introduce a 4‐[18F]fluoro‐phenylalanine residue into peptide sequences is reported, by chemoselective radio‐deoxyfluorination of a tyrosine residue using a traceless activating group. The replacement of only one hydrogen atom with [18F]fluoride results in minimal structural perturbation of the peptide, which is desirable in the labeling of tracer candidates.