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Title: Synthesis of n-tert-butyl-alpha-(4-[f-18]fluorophenyl)nitrone ([f-18]fpbn) for in-vivo detection of free-radicals
Authors: Bormans, Guy ×
Kilbourn, Mr #
Issue Date: Feb-1995
Publisher: John wiley & sons ltd
Series Title: Journal of labelled compounds & radiopharmaceuticals vol:36 issue:2 pages:103-110
Abstract: We have synthesized the fluorine-18 labeled derivative of N-tert-butyl-alpha-phenylnitrone (PEN), a free radical spin trapping agent widely used with electron spin resonance (ESR). N-tert-Butyl-alpha-(4-[F-18]fluorophenyl)nitrone ([F-18]FPBN) could be prepared with low radiochemical yield (3% decay corrected) by the direct aromatic nucleophilic substitution of N-tert-butyl-alpha-(4-nitrophenyl)nitrone with [F-18]fluoride. An alternate two step synthesis route consisted of the nucleophilic [F-18]fluoride substitution of 4-N,N,N-trimethylammonium benzaldehyde triflate to yield 4-[F-18]fluorobenzaldehyde, which was distilled into a vial containing N-tert-butyl-hydroxylamine in 2N NaOH. 4-[F-18]Fluorobenzaldehyde readily reacted with the hydroxylamine to form [F-18]FPBN. [F-18]FPBN was obtained in overall decay corrected yields of 24% in a total synthesis time <45 min. and was suitable for further applications in in vivo studies of free radicals.
ISSN: 0362-4803
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiopharmacy
× corresponding author
# (joint) last author

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