One-step radiosynthesis of 4-nitrophenyl 2-[(18) F]fluoropropionate ([(18) F]NFP); improved preparation of radiolabeled peptides for PET imaging

Mohammad B Haskali, Peter D Roselt, John A Karas, Wayne Noonan, Christian W Wichmann, Andrew Katsifis, Rodney J Hicks, Craig A Hutton
Journal of Labelled Compounds & Radiopharmaceuticals 2013, 56 (14): 726-30
The versatile (18) F-labeled prosthetic group, 4-nitrophenyl 2-[(18) F]fluoropropionate ([(18) F]NFP), was synthesized in a single step in 45 min from 4-nitrophenyl 2-bromopropionate, with a decay corrected radiochemical yield of 26.2% ± 2.2%. Employing this improved synthesis of [(18) F]NFP, [(18) F]GalactoRGD - the current 'gold standard' tracer for imaging the expression of αV β3 integrin - was prepared with high specific activity in 90 min and 20% decay corrected radiochemical yield from [(18) F]fluoride.

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