Abstract
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 18F synthons 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.
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Buckingham, F., Kirjavainen, A. K., Forsback, S., Krzyczmonik, A., Keller, T., Newington, I. M., … Gouverneur, V. (2015). Organomediated Enantioselective 18F Fluorination for PET Applications. Angewandte Chemie - International Edition, 54(45), 13366–13369. https://doi.org/10.1002/anie.201506035
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