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18 F‐FESB: synthesis and automated radiofluorination of a novel 18 F‐labeled pet tracer for β ‐amyloid plaques
Author(s) -
Kumar Piyush,
Zheng Weizhong,
McQuarrie Stephen A.,
Jhamandas Jack H.,
Wiebe Leonard I.
Publication year - 2005
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1011
Subject(s) - chemistry , trifluoromethanesulfonate , ionic liquid , tetrafluoroborate , benzene , yield (engineering) , nucleophilic substitution , hexafluorophosphate , nucleophile , radiochemistry , chromatography , medicinal chemistry , nuclear chemistry , organic chemistry , catalysis , materials science , metallurgy
1‐(2′‐[ 18 F]‐fluoroethoxy)‐2,5‐ bis (4′‐methoxystyryl)benzene ( 18 F‐FESB) was synthesized in ∼76% radiochemical yield (specific activity >58.6 GBq or 1.58 Ci/µmol) in an Advanced Cyclotron Systems' automated synthesis unit by nucleophilic substitution of 1‐(2′‐toluenesulfonylethoxy)‐2,5‐ bis (4′‐methoxystyryl)benzene and purified using reversed phase column chromatography. When performed in the presence of ionic fluid, either 1‐butyl‐3‐methylimidazolium tetrafluoroborate (Bmimtetrafluoroborate; BmimBF 4 ) or 1‐ethyl‐3‐methylimidazolium trifluoromethanesulfonate (Emimtriflate; EmimTFMS), radiochemical yields of 18 F‐FESB ranged from 17 to 76%. The radiochemical yields were consistently lower (∼3–7%) in the absence of these ionic fluids. Copyright © 2005 John Wiley & Sons, Ltd.