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).
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