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Site‐Specific Deoxyfluorination of Small Peptides with [ 18 F]Fluoride
Author(s) -
Rickmeier Jens,
Ritter Tobias
Publication year - 2018
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201807983
Subject(s) - chemistry , residue (chemistry) , peptide , fluoride , phenylalanine , tyrosine , stereochemistry , combinatorial chemistry , biochemistry , amino acid , inorganic chemistry
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‐[ 18 F]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 [ 18 F]fluoride results in minimal structural perturbation of the peptide, which is desirable in the labeling of tracer candidates.