Paroxetine is a potent inhibitor of serotonin reuptake and is widely prescribed
for the treatment of depression and other neurological disorders. The synthesis of paroxetine
and the possibility to prepare derivatives with a specific substitution pattern that may
allow their use as biological probes is an attractive topic especially for medicinal
chemists engaged in neurosciences research. Considering the extensive work that was developed
in the last decade on the total synthesis of paroxetine, this review summarizes
the most important contributions in this field, organized according to the reagent that was
used as a starting material. Most of the methods allowed to prepare paroxetine in 4-9
steps with an overall yield of 9-66%. Despite the progress made in this area, there is still
room for improvement, searching for new eco-friendly and sustainable synthetic alternatives.
Keywords: Paroxetine, synthetic methods, N-substituted piperidones, 4-fluorobenzaldehyde, substituted pyridines,
α, β-unsaturated carbonyl compounds, 1, 3-dicarbonyl compounds.
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