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Synthesis of 18F-labeled cyclooxygenase-2 (COX-2) inhibitor as a potential PET imaging agent

✍ Scribed by Haibin Tian; Zhenghong Lee

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
144 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis

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. Solidphase extraction and semi-preparative-HPLC purification produced [ 18 F]EFMP in 14.6 AE 3.3% (n ¼ 4) decay corrected radiochemical yield with a specific activity of 487 AE 85.1 (n ¼ 4) Ci/mmol and greater than 98% radiochemical purity. Copyright

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