Synthesis of [18 F]-labeled EF3 [2-(2-nitroimidazol-1-yl)-N-(3, 3, 3-trifluoropropyl)-acetamide], a marker for PET detection of hypoxia

…, B Georges, V Grégoire, J Marchand-Brynaert

Index: Josse, Olivier; Labar, Daniel; Georges, Benoit; Gregoire, Vincent; Marchand-Brynaert, Jacqueline Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 3 p. 665 - 675

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Citation Number: 52

Abstract

[18F]-2-(2-Nitroimidazol-1-yl)-N-(3, 3, 3-trifluoropropyl)-acetamide ([18F]-EF3) has been prepared, in 65% chemical yield and 5% radiochemical yield, by coupling 2, 3, 5, 6- tetrafluorophenyl 2-(2-nitroimidazol-1-yl) acetate 1 with [18F]-3, 3, 3-trifluoropropylamine 7. This original radiolabelled key-synthon was obtained in 40% overall chemical yield by oxidative [18F]-fluorodesulfurization of ethyl N-phthalimido-3-aminopropane dithioate 4, ...