title: Improved synthesis of 2'-deoxy-2'-[18F]fluoro-5-methyl-1-β-D-arabinofuranosyluracil ([18F]FMAU).
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.
authors.affiliation: Molecular Imaging Center, Department of Radiology, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA.
authors.forename: Zibo
authors.initials: Z
authors.lastname: Li
authors.forename: Hancheng
authors.initials: H
authors.lastname: Cai
authors.forename: Peter S
authors.initials: PS
authors.lastname: Conti
mesh_terms: D001086:Arabinofuranosyluracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D002384:Catalysis; D005472:Fluorouracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D012821:Silanes / Q000378:metabolism; D012997:Solvents / Q000378:metabolism; D013696:Temperature; D013997:Time Factors
chemical_list: C496306:2'-deoxy-2'-18F-fluoro-5-fluoro-1-beta-D-arabinofuranosyluracil; D019275:Radiopharmaceuticals; D012821:Silanes; D012997:Solvents; C520781:hexamethyldisilane; D001086:Arabinofuranosyluracil; D005472:Fluorouracil