Radiosynthesis of 2'-deoxy-2'-[18F]-fluoro-5-methyl-1-β-L-arabinofuranosyluracil([18F]-L-FMAU) for PET

Radiosynthesis of 2'-deoxy-2-[F-18]-fluoro-5-methyl-1-beta-L-arabinofuranosyluracil ([F-18]-L-FMAU) is reported. Compound 1 was synthesized and converted to 2-triflate 2. Compound 3 was prepared from 2 using tetrabutylammonium[F-18]fluoride, converted to 4, and then coupled with 5. The crude product was hydrolyzed, and purified by HPLC to obtain 7a. The radiochemical yield of [F-18]-L-FMAU was 26% decay corrected (d.c.) in four runs with radiochemical purity >99% and specific activity 2200 mCi/mu mol. The synthesis time was 3.3-3.5 h from the end of bombardment (EOB). (c) 2007 Elsevier Ltd. All rights reserved.