Open AccessApplication of Palladium-Mediated 18F-Fluorination to PET Radiotracer Development: Overcoming Hurdles to Translation
Author(s) -
Adam S. Kamlet,
Constanze N. Neumann,
Eunsung Lee,
Stephen M. Carlin,
Christian K. Moseley,
Nickeisha A. Stephenson,
Jacob M. Hooker,
Tobias Ritter
Publication year - 2013
Publication title -
plos one
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.99
H-Index - 332
ISSN - 1932-6203
DOI - 10.1371/journal.pone.0059187
Subject(s) - positron emission tomography , pet imaging , palladium , radiochemistry , chemistry , electrophile , combinatorial chemistry , nanotechnology , nuclear medicine , materials science , medicine , organic chemistry , catalysis
New chemistry methods for the synthesis of radiolabeled small molecules have the potential to impact clinical positron emission tomography (PET) imaging, if they can be successfully translated. However, progression of modern reactions from the stage of synthetic chemistry development to the preparation of radiotracer doses ready for use in human PET imaging is challenging and rare. Here we describe the process of and the successful translation of a modern palladium-mediated fluorination reaction to non-human primate (NHP) baboon PET imaging–an important milestone on the path to human PET imaging. The method, which transforms [ 18 F]fluoride into an electrophilic fluorination reagent, provides access to aryl– 18 F bonds that would be challenging to synthesize via conventional radiochemistry methods.
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