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Current Medicinal Chemistry

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ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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Mini-Review Article

Recent Advances in the Synthesis of the Antidepressant Paroxetine

Author(s): Joana Santos, Maria Fernanda Proença*, Ana Joao Rodrigues, Patricia Patrício and Helena Sofia Domingues

Volume 28, Issue 15, 2021

Published on: 26 October, 2020

Page: [2960 - 2973] Pages: 14

DOI: 10.2174/0929867327666201026144848

Price: $65

Abstract

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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