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

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

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 1 , 2009

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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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Article Details

Year: 2009
Page: [82 - 85]
Pages: 4
DOI: 10.2174/157018009787158616

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