Synthesis and purification of the anti-viral agent 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine (FIAC) labeled with iodine-125.
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.
D000818:Animals; D000998:Antiviral Agents; D002851:Chromatography, High Pressure Liquid; D003561:Cytarabine / Q000031:analogs & derivatives* / Q000032:analysis; D004660:Encephalitis / Q000000981:diagnostic imaging; D006561:Herpes Simplex / Q000000981:diagnostic imaging; D006801:Humans; D007457:Iodine Radioisotopes; D007553:Isotope Labeling / Q000379:methods; D011877:Radionuclide Imaging
D000998:Antiviral Agents; D007457:Iodine Radioisotopes; D003561:Cytarabine; C026023:fiacitabine