Development of an Economical, Single Step Synthesis of FAZA, a Clinical Hypoxia Marker, and Potential Synthons to Prepare its Positional Analogs

P.      Kumar; S.      Emami; A.   J.B.   McEwan; L.   I.   Wiebe

Letters in Drug Design & Discovery

Author(s): P. Kumar, S. Emami, A. J.B. McEwan and L. I. Wiebe

DOI: 10.2174/157018009787158616

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Development of an Economical, Single Step Synthesis of FAZA, a Clinical Hypoxia Marker, and Potential Synthons to Prepare its Positional Analogs

Page: [82 - 85] Pages: 4

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Abstract

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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