Premium
Synthesis of [ 18 F]‐(S)‐fluoxetine: A selective serotonine uptake inhibitor
Author(s) -
Hammadi Akli,
Crouzel Christian
Publication year - 1993
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580330805
Subject(s) - chemistry , yield (engineering) , radiochemistry , trifluoromethyl , specific activity , fluorine , fluoxetine , chemical synthesis , nuclear chemistry , positron emission tomography , medicinal chemistry , organic chemistry , nuclear medicine , in vitro , serotonin , biochemistry , enzyme , medicine , alkyl , materials science , receptor , metallurgy
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.