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

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

Volume: 6 Issue: 1

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

Affiliation:

Keywords: Azomycin nucleoside, Hypoxia sensitizer, FAZA, One step synthesis, Synthons, Solvents' effect

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.

Cite this article as:

Kumar P., Emami S., McEwan J.B. A. and Wiebe I. L., Development of an Economical, Single Step Synthesis of FAZA, a Clinical Hypoxia Marker, and Potential Synthons to Prepare its Positional Analogs, Letters in Drug Design & Discovery 2009; 6 (1) . https://dx.doi.org/10.2174/157018009787158616