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Synthesis of 3′-deoxy-3′-[18F]fluoro-1-β-D-xylofuranosyluracil ([18F]-FMXU) for PET

✍ Scribed by M. M. Alauddin; J. Balatoni; J. Gelovani

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
201 KB
Volume
48
Category
Article
ISSN
0022-2135

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✦ Synopsis

The synthesis of a pyrimidine analog, 3 0 -deoxy-3 0 -[ 18 F]-fluoro-1-b-d-xylofuranosyluracil ([ 18 F]-FMXU) is reported. 5-Methyluridine 1 was converted to its dimethoxytrityl derivatives 2 and 3 as a mixture. After separation the 2 0 , 5 0 -di-methoxytrityluridine 2 was converted to its 3 0 -triflate 4 followed by derivatization to the respective N 3 -t-Boc product 5. The triflate 5 was reacted with tetrabutylammonium[ 18 F]fluoride to produce 6, which by acid hydrolysis yielded compound 7. The crude preparation was purified by HPLC to obtain the desired product [ 18 F]-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/ mmol at the end of synthesis (EOS). The synthesis time was 67-75 min from the end of bombardment (EOB).

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