Automated synthesis of 2 '-deoxy-2 '-[F-18]fluoro-5-methyl-1-beta-D-arabinofuranosyluracil ([F-18]-FMAU) using a one reactor radiosynthesis module

作者：Li Zibo; Cai Hancheng; Conti Peter S^*

来源：Nuclear Medicine and Biology, 2011, 38(2): 201-206.

DOI：10.1016/j.nucmedbio.2010.08.010

• [F-18]-FMAU
• PET probe
• Friedel-Crafts catalysts
• F-18 labeling
• Automated synthesis

2'-Deoxy-2'-[F-18]fluoro-5-methyl-1-beta-D-arabinofuranosyluracil ([F-18]-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 [F-18]-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 [F-18]-FMAU in the presence of Friedel-Crafts catalysts. Here, we report a fully automated synthesis of [F-18]-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. [F-18]-FMAU was obtained in 12 +/- 3% radiochemical yield (decay corrected overall yield based on [F-18]-F-, n=4) with 383 +/- 33 mCi/mu mol specific activity at the time of injection. The alpha/beta 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.

• 出版日期2011-2