Synthesis of [¹⁸F]‐(S)‐fluoxetine: A selective serotonine uptake inhibitor

Abstract

Abstract The (S)‐N‐methyl‐γ‐[4‐(trifluoromethyl)phenoxy]benzenepropanamine, an antidepressant with potential applications in the treatment of other illnesses was labelled with fluorine‐18 for Positron Emission Tomography studies. The synthesis was accomplished from the [ 18 F]‐4‐chlorobenzotrifluoride where [ 18 F]‐(S)‐Fluoxetine was obtained with a radiochemical yield of 9–10% (decay corrected) and a specific radioactivity of 100–150 mCi/μmol (3.70–5.55 GBq/μmol) in a total synthesis time of 150 min. A facile isotopic exchange reaction was desmonstrated; it is expected to reduce the specific activity of the final [ 18 F]‐product. The experimental parameters play an important role, which is discussed.