Synthesis and purification of the anti-viral agent 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine (FIAC) labeled with iodine-125.

Abstract

The 125I labeled analog of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine (FIAC) has been prepared for studies on the imaging of herpes simplex virus (HSV) encephalitis infections in animals. Iodination of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)cytosine X HCl (FAC X HCl) with Na 125I and NaI/HIO3 in aqueous acetic acid, and subsequent removal of residual iodine by CCl4 extraction and ion exchange chromatography, yielded [125I]FIAC in aqueous solution with a specific activity of 45.5 mCi/mmol in 44% radiochemical yield, and with a radiopurity of 96-97%. Methods for further purification are described.

• Authors: M E Perlman, P S Conti, B Schmall, K A Watanabe
• Journal: International journal of nuclear medicine and biology (Int J Nucl Med Biol) Vol. 11 Issue 3-4 Pg. 215-8 ( 1984) ISSN: 0047-0740 [Print] United States
• PMID: 6530342 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antiviral Agents
• Iodine Radioisotopes
• Cytarabine
• fiacitabine

Topics

• Animals
• Antiviral Agents
• Chromatography, High Pressure Liquid
• Cytarabine (analogs & derivatives, analysis)
• Encephalitis (diagnostic imaging)
• Herpes Simplex (diagnostic imaging)
• Humans
• Iodine Radioisotopes
• Isotope Labeling (methods)
• Radionuclide Imaging