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Synthesis of new hypoxia markers EF1 and [F-18]-EF1

TitleSynthesis of new hypoxia markers EF1 and [F-18]-EF1
Publication TypeJournal Article
Year of Publication1999
AuthorsKachur, AV, Dolbier, WR, Evans, SM, Shiue, CY, Shiue, GG, Skov, KA, Baird, IR, James, BR, Li, AR, Roche, A, Koch, CJ
JournalApplied Radiation and Isotopes
Volume51
Pagination643-650
Date PublishedDec
Type of ArticleArticle
ISBN Number0969-8043
KeywordsADDUCTS, CARCINOMA, CELLS, DEPENDENCE, F-18 FLUOROMISONIDAZOLE, IMAGING TUMOR HYPOXIA, INVIVO, ischemia, NONINVASIVE ASSESSMENT, REDUCTION
Abstract

We report on the preparation of a hypoxia marker 2-(2-nitroimidazol-1[H]-yl)-N-(3-fluoropropyl)acetamide (EF1) and its F-18 analog, 2-(2-nitroimidazol-1[H]-yl)-N-(3-[F-18]fluoropropyl)acetamide ([F-18]-EF1). Two methods for the preparation of 3-fluoropropylamine, the EF1 side chain, are described. [F-18]-EF1 was prepared with a radiochemical yield of 2% by nucleophilic substitution of bromine in 2-(2-nitroimidazol-1[H]-yl)-N-(3-bromopropyl) acetamide (EBrl) by carrier-added F-18 in DMSO at 120 degrees C. Our results demonstrate the preparation of clinically relevant amounts of [F-18]-EF1 for use as a non-invasive hypoxia marker with detection using positron emission tomography (PET). (C) 1999 Elsevier Science Ltd. All rights reserved.

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