Synthesis of [11C]granisetron, a possible positron emission tomography ligand for 5-HT3 receptor studies

Abstract

[11C]Granisetron, a selective 5-HT3 antagonist, was synthesized by N-alkylation of the desmethyl compound using [11C]methyl iodide as the labelling agent in a total synthesis time of 40 min, including semi-preparative HPLC purification. Approximately 40 mCi (1.5 GBq) of the radioligand was obtained with a specific activity of 200–250 mCi/μmol (7.4–9 GBq/μmol). Chemical (≥96%) and radiochemical purity (≥99%) were determined using analytical HPLC. © 1998 John Wiley & Sons, Ltd.