Abstract
The synthesis of a pyrimidine analog, 3′-deoxy-3′-[18F]-fluoro-1-β-D-xylofuranosyluracil ([18F]-FMXU) is reported. 5-Methyluridine 1 was converted to its di-methoxytrityl derivatives 2 and 3 as a mixture. After separation the 2′,5′-di-methoxytrityluridine 2 was converted to its 3′-triflate 4 followed by derivatization to the respective N3-t-Boc product 5. The triflate 5 was reacted with tetrabutylammonium[18F]fluoride to produce 6, which by acid hydrolysis yielded compound 7. The crude preparation was purified by HPLC to obtain the desired product [18F]-FMXU. The radiochemical yields were 25–40% decay corrected (d. c.) with an average of 33% in four runs. Radiochemical purity was >99% and specific activity was >74 GBq/µmol at the end of synthesis (EOS). The synthesis time was 67–75 min from the end of bombardment (EOB). Copyright © 2005 John Wiley & Sons, Ltd.
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