Abstract
2′-Deoxy-2′-[18F]fluoro-5-methyl-1-β-d-arabi nofuranosyluracil ([18F]-FMAU) is an established PET probe used to monitor cellular proliferation. For clinical applications, a fully automated cGMP-compliant radiosynthesis would be preferred. However, the current synthesis of [18F]-FMAU requires a multistep procedure, making the development of an automated protocol difficult and complicated. Recently, we have developed a significantly simplified one-pot reaction condition for the synthesis of [18F]-FMAU in the presence of Friedel-Crafts catalysts. Here, we report a fully automated synthesis of [18F]-FMAU based on a one reactor radiosynthesis module using our newly developed synthetic method. The product was purified on a semi-preparative high-performance liquid chromatography integrated with the synthesis module using 6% EtOH in 10 mM phosphate buffer or 8% MeCN/water. [18F]-FMAU was obtained in 12±3% radiochemical yield (decay corrected overall yield based on [18F]-F-, n=4) with 383±33 mCi/βmol specific activity at the time of injection. The -/- anomer ratio was 4:6. The overall reaction time was about 150 min from the end of bombardment and the radiochemical purity was >99%. This automated synthesis should also be suitable for the production of other 5-substituted thymidine analogues.
Original language | English (US) |
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Pages (from-to) | 201-206 |
Number of pages | 6 |
Journal | Nuclear Medicine and Biology |
Volume | 38 |
Issue number | 2 |
DOIs | |
State | Published - Feb 2011 |
Keywords
- Automated synthesis
- F-18 labeling
- Friedel-Crafts catalysts
- PET probe
- [F]-FMAU
ASJC Scopus subject areas
- Molecular Medicine
- Radiology Nuclear Medicine and imaging
- Cancer Research