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Organomediated Enantioselective 18F Fluorination for PET Applications |
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| Authors: | Faye Buckingham Dr Anna K Kirjavainen Dr Sarita Forsback Anna Krzyczmonik Thomas Keller Dr Ian M Newington Dr Matthias Glaser Dr Sajinder K Luthra Prof Olof Solin Prof Véronique Gouverneur |
| Institution: | 1. University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA (UK);2. Turku PET Centre, Radiopharmaceutical Chemistry Laboratory, Kiinamyllynkatu 4–8, 20520 Turku (Finland);3. GE Healthcare, The Grove Centre, White Lion Road, Amersham, HP7 9LL (UK) |
| 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. |
| Keywords: | asymmetric synthesis enamines fluorine‐18 organocatalysis positron emission tomography |