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

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 [18F]-4-chlorobenzotrifluoride where [18F]-(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 [18F]-product. The experimental parameters play an important role, which is discussed.