Abstract
A cannabinoid receptor antagonist, SR144385, has been labeled with fluorine-18. [18F] SR144385 was synthesized in a multi-step reaction in which fluorine-18 was introduced by nucleophilic halogen displacement on a bromo precursor. The fluorine-18 labeled intermediate was deprotected and coupled with 1-aminopiperidine to give [18F]SR144385. The time for radiosynthesis, HPLC purification, and formulation was 2 hours from end-of-bombardment. [18F] SR144385 of high radiochemical purity was obtained at end-of-synthesis with an average (n=11) specific radioactivity of 1852 mCi/μmol and an average isolated, non-decay corrected radiochemical yield of 4% from potassium [18F] fluoride. Copyright © 1999 John Wiley & Sons, Ltd.
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