Synthesis and purification of the anti-viral agent 1-(2-deoxy-2-fluoroβ-d-arabinofuranosyl)-5-IODOCYTOSINE (cas 1122-44-7) (FIAC) labeled with iodine-125☆

Add time:10/01/2019    Source:sciencedirect.com

The 125I labeled analog of 1-(2-deoxy-2-fluoro-β-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-β-d-arabinofuranosyl)cytosine-HCI (FAC·HCI) 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.

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