Title of article :
Synthesis of [18F]-labeled EF3 [2-(2-nitroimidazol-1-yl)-N-(3,3,3-trifluoropropyl)-acetamide], a marker for PET detection of hypoxia Original Research Article
Author/Authors :
Olivier Josse، نويسنده , , Daniel Labar، نويسنده , , Benoît Georges، نويسنده , , Vincent Gregoire، نويسنده , , Jacqueline Marchand-Brynaert، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2001
Pages :
11
From page :
665
To page :
675
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, followed by deprotection with hydrazine of the resulting [18F]-N-phthalimido-3,3,3-trifluoropropylamine 5. All the process was performed within 90 min, from the [18F]-HF production in the cyclotron to the purification of the final target.
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2001
Journal title :
Bioorganic and Medicinal Chemistry
Record number :
1301415
Link To Document :
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