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

Alexander V. Kachur, William R. Dolbier, Sydney M. Evans, Chyng Yann Shiue, Grace G. Shiue, Kirsten A. Skov, Ian R. Baird, Brian R. James, An Rong Li, Alex Roche, Cameron J. Koch

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

We report on the preparation of a hypoxia marker 2-(2-nitroimidazol-1[H]-yl)-N-(3-fluoropropyl)acetamide (EF1) and its 18F analog, 2-(2-nitroimidazol-1[H]-yl)-N-(3-[18F]fluoropropyl)acetamide ([18F]-EF1). Two methods for the preparation of 3-fluoropropylamine, the EF1 side chain, are described. [18F]-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 (EBr1) by carrier-added 18F in DMSO at 120°C.Our results demonstrate the preparation of clinically relevant amounts of [18F]-EF1 for use as a non-invasive hypoxia marker with detection using positron emission tomography (PET). Copyright (C) 1999 Elsevier Science Ltd.

Original languageEnglish (US)
Pages (from-to)643-650
Number of pages8
JournalApplied Radiation and Isotopes
Volume51
Issue number6
DOIs
StatePublished - Dec 1999
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Radiation

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