A fully automated synthesis of [18F]-FEAU and [18F]-FMAU using a novel dual reactor radiosynthesis module

✍ Scribed by Vincenzo Paolillo; Stefan Riese; Juri G. Gelovani; Mian M. Alauddin

• Publisher: John Wiley and Sons
• Year: 2009
• Tongue: French
• Weight: 340 KB
• Volume: 52
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.1674

✦ Synopsis

Abstract

2′‐Deoxy‐2′‐[^18^F]fluoro‐5‐substituted‐1‐β‐D‐arabinofuranosyluracils, including 2′‐deoxy‐2′‐[^18^F]fluoro‐5‐methyl‐1‐β‐D‐arabinofuranosyluracil [^18^F]FMAU and [^18^F]FEAU are established radiolabeled probes to monitor cellular proliferation and herpes simplex virus type 1 thymidine kinase (HSV1‐tk) reporter gene expression with positron emission tomography. For clinical applications, a fully automated CGMP‐compliant radiosynthesis is necessary for production of these probes. However, due to multiple steps in the synthesis, no such automated synthetic protocols have been developed. We report here a fully automated synthesis of [^18^F]‐FEAU and [^18^F]‐FMAU on a prototype dual reactor module TRACERlab FX FN. The synthesis was performed by using a computer‐programmed standard operating procedure, and the product was purified on a semipreparative high‐performance liquid chromatography (HPLC) integrated with the synthesis module using 12% EtOH in 50 mM Na~2~HPO~4~. Finally, the percentage of alcohol was adjusted to 7% by adding Na~2~HPO~4~ and filtered through a Millipore filter to make dose for human. The radiochemical yield on the fluorination was 40±10% (n=10), and the overall yields were 4±1% (d. c.), from the end of the bombardment; [^18^F]FEAU (n=7) and [^18^F]FMAU (n=3). The radiochemical purity was >99%, specific activity was 1200–1300 mCi/µmol. The synthesis time was 2.5 h. This automated synthesis should be suitable for production of [^18^F]FIAU, [^18^F]FFAU, [^18^F]FCAU, [^18^F]FBAU and other 5‐substitued thymidine analogues. Copyright © 2009 John Wiley & Sons, Ltd.