Expedient synthesis of [18F]-labeled α-trifluoromethyl ketones

Several [F-18]-labeled alpha-trifluoromethyl ketones have been synthesized. Reactions of 2,2-difluoro-1-aryl-1-trimethylsiloxyethenes (1a-d) with [F-18]-F-2 at low temperature produced [F-18]-labeled alpha-trifluoromethyl ketones (2a-d). Radiolabeled products were isolated by purification with column chromatography in 22-28% yields, decay corrected (d.c.) in three runs per compound. Radiochemical purity was >99% with specific activities 15-20 GBq/mmol at the end of synthesis (EOS). The synthesis time was 35-40 min from the end of bombardment (EOB). This one-step simple method is highly useful for the radiochemical synthesis of potential biologically active [F-18]-labeled alpha-trifluoromethyl ketones for PET imaging. Copyright (C) 2003 John Wiley Sons, Ltd.