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

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

Volume: 4 Issue: 1

Author(s): Zibo Li, Hancheng Cai and Peter S. Conti

Affiliation:

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

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.

Cite this article as:

Li Zibo, Cai Hancheng and S. Conti Peter, Improved Synthesis of 2-deoxy-2-[18F]fluoro-5-Methyl-1-β-DArabinofuranosyluracil ([18F]FMAU), Current Radiopharmaceuticals 2011; 4 (1) . https://dx.doi.org/10.2174/1874471011104010024