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Synthesis of 18 F‐labeled cyclooxygenase‐2 (COX‐2) inhibitor as a potential PET imaging agent
Author(s) -
Tian Haibin,
Lee Zhenghong
Publication year - 2006
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.1074
Subject(s) - chemistry , nucleophilic substitution , yield (engineering) , pet imaging , specific activity , high performance liquid chromatography , radiochemistry , extraction (chemistry) , imaging agent , solid phase extraction , nuclear chemistry , nucleophile , chromatography , medicinal chemistry , enzyme , in vivo , organic chemistry , positron emission tomography , nuclear medicine , catalysis , medicine , materials science , microbiology and biotechnology , biology , metallurgy
A new PET tracer for COX‐2 imaging, the 6‐ethoxy‐3‐(4‐methanesulfonylphenyl)‐4‐(4‐[ 18 F]fluorophenyl)pyran‐2‐one ([ 18 F]EFMP), was synthesized. For F‐18 radiolabeling, a trimethylammonium precursor and a brominated precursor were synthesized from 1,1,2,3‐tetrachlorocycloprop‐2‐ene in 6 steps. The radiolabeling was achieved through nucleophilic substitution using no‐carrier‐added (n.c.a.) fluorine‐18. Solid‐phase extraction and semi‐preparative‐HPLC purification produced [ 18 F]EFMP in 14.6±3.3% ( n =4) decay corrected radiochemical yield with a specific activity of 487±85.1 ( n =4) Ci/mmol and greater than 98% radiochemical purity. Copyright © 2006 John Wiley & Sons, Ltd.