Synthesis of 2'-deoxy-2'-[.sup.18F]fluoro-5-methyl-1-B-D-arabinofuranosyluracil (.sup.18F-FMAU)
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.
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- OSTI Identifier:
- University of Southern California (Los Angeles, CA) DOESC
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- Resource Relation:
- Patent File Date: 2011 Jul 15
- Research Org:
- Univ. of Southern California, Los Angeles, CA (United States)
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- Country of Publication:
- United States
- 60 APPLIED LIFE SCIENCES; 37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
Other works cited in this record:Improved synthesis of 2′-deoxy-2′-[18F]-fluoro-1-β-d-arabinofuranosyl-5-iodouracil ([18F]-FIAU)
journal, May 2010
- Anderson, Harry; Pillarsetty, NagaVaraKishore; Cantorias, Melchor
- Nuclear Medicine and Biology, Vol. 37, Issue 4, p. 439-442
The improved syntheses of 5-substituted 2′-[18F]fluoro-2′-deoxy-arabinofuranosyluracil derivatives ([18F]FAU, [18F]FEAU, [18F]FFAU, [18F]FCAU, [18F]FBAU and [18F]FIAU) using a multistep one-pot strategy
journal, July 2011
- Cai, Hancheng; Li, Zibo; Conti, Peter S.
- Nuclear Medicine and Biology, Vol. 38, Issue 5, p. 659-666
Automated synthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-β-d-arabinofuranosyluracil ([18F]-FMAU) using a one reactor radiosynthesis module
journal, February 2011
- Li, Zibo; Cai, Hancheng; Conti, Peter S.
- Nuclear Medicine and Biology, Vol. 38, Issue 2, p. 201-206
Synthesis of 2′-deoxy-2′-[18F]fluoro-β-D-arabinofuranosyl nucleosides, [18F]FAU, [18F]FMAU, [18F]FBAU and [18F]FIAU, as potential PET agents for imaging cellular proliferation: synthesis of [18F]labelled FAU, FMAU, FBAU, FIAU
journal, April 2003
- Mangner, Thomas J.; Klecker, Raymond W.; Anderson, Lawrence
- Nuclear Medicine and Biology, Vol. 30, Issue 3, p. 215-224
Design and Optimization of Coin-Shaped Microreactor Chips for PET Radiopharmaceutical Synthesis
journal, February 2010
- Elizarov, A. M.; van Dam, R. M.; Shin, Y. S.
- Journal of Nuclear Medicine, Vol. 51, Issue 2, p. 282-287
Rapid Prototyping of Microfluidic Systems in Poly(dimethylsiloxane)
journal, October 1998
- Duffy, David C.; McDonald, J. Cooper; Schueller, Olivier J. A.
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