Organomediated Enantioselective 18F-Fluorination for PET Applications
: Buckingham F, Kirjavainen AK, Forsback S, Krzyczmonik A, Keller T, Newington IM, Glaser M, Luthra SK, Solin O, Gouverneur V,
Publisher: Wiley
: 2015
: Angewandte Chemie International Edition
: Angew Chem Int Edit
: 127
: 45
: 13564
: 13567
: 4
DOI: https://doi.org/10.1002/anie.201506035(external)
The first organomediated asymmetric 18F fluorination has been accomplished using a chiral imidazolidinone and [18F]N-fluorobenzenesulfonimide. The method provides access to enantioenriched 18F-labeled -α-fluoroaldehydes (>90% ee), which are versatile chiral 18Fsynthons for the synthesis of radiotracers. The utility of this process is demonstrated with the synthesis of the PET (positron emission tomography) tracer (2S,4S)-4-[18F]fluoroglutamic acid.