Improved Synthesis of 2-deoxy-2-[18F]fluoro-5-Methyl-1-β-DArabinofuranosyluracil ([18F]FMAU)

Zibo      Li; Hancheng      Cai; Peter      S. Conti

Abstract

[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 HBr activation of the sugar prior to the coupling with silylated uracil. This multiple step procedure makes the development of an automated protocol difficult and complicated. In this study, we report the use of Friedel-Crafts catalysts for an improved synthesis of [18F]FMAU, which also includes a significantly simplified one-pot reaction condition.

Keywords: [18F]FMAU, PET probe, friedel-crafts catalysts, radiosynthesis, cellular proliferation, 1-deoxy-1-bromo-2-deoxy-2-[18F]fluoro-3, 5-di-O-benzoyl-D-arabinofuranose, NCA, Conjugation Time, TMSOTf