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Synthesis of 2'-deoxy-2'-[.sup.18F]fluoro-5-methyl-1-B-D-arabinofuranosyluracil (.sup.18F-FMAU)

United States Patent

December 16, 2014
View the Complete Patent at the US Patent & Trademark Office
The present invention relates to methods of synthesizing .sup.18F-FMAU. In particular, .sup.18F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated into a fully automated cGMP-compliant radiosynthesis module, which results in a reduction in synthesis time and simplifies reaction conditions. The one-pot reaction conditions are also suitable for the production of 5-substituted thymidine or cytidine analogs. The products from the one-pot reaction (e.g. the labeled thymidine or cytidine analogs) can be used as probes for imaging tumor proliferative activity. More specifically, these [.sup.18F]-labeled thymidine or cytidine analogs can be used as a PET tracer for certain medical conditions, including, but not limited to, cancer disease, autoimmunity inflammation, and bone marrow transplant.
Li; Zibo (Logan, UT), Cai; Hancheng (Troy, MI), Conti; Peter S. (Pasadena, CA)
University of Southern California (Los Angeles, CA)
13/ 183,924
July 15, 2011
STATEMENT REGARDING FEDERALLY-SPONSORED RESEARCH This invention was made with government support under contract No. DE-SC0002353 awarded by the Department of Energy. The U.S. Government may have certain rights in this invention.