Development of an Economical, Single Step Synthesis of FAZA, a Clinical Hypoxia Marker, and Potential Synthons to Prepare its Positional Analogs
A. J.B. McEwan,
L. I. Wiebe.
F-18 analog of 1-α-D-(5-deoxy-5-fluoro-(1S,2R,3S,4S) arabinofuranosyl)-2-nitroimidazole (FAZA) is a clinical PET tracer for diagnosing hypoxic tumors in cancer patients. Original synthesis of FAZA is lengthy, expensive and low yielding (∼12%). Current procedure is fast, economical, and affords FAZA (25%) in a single step, along with three useful synthons, 3, 4 and 5, to prepare other positional analogues of FAZA. Their chemical ratio depends on the solvent and reaction conditions.
Keywords: Azomycin nucleoside, Hypoxia sensitizer, FAZA, One step synthesis, Synthons, Solvents' effect
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