Process for the production of paroxetine
US6583287B1 · kind B1 · utility
2Cited by
1References
14Claims
0Family size
Assignee
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Key dates
| Filing date | Jul 30, 2001 |
| Grant date | Jun 24, 2003 |
| Priority date | — |
| Expiry date | Jul 30, 2021 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P25/24
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process for the production of paroxetine is described, wherein N-substituted derivatives of 4-(p-fluorophenyl)-3-hydroxymethyl-1,2,3,6-tetrahydropyridine are treated according to the following sequence of reactions: (a) hydrogenation catalyzed by transition metal complexes with chiral diphosphinic ligands; (b) —OH derivatisation and nucleophilic substitution, the substituent being sesamol; (c) N-dealkylation. The process is highly stereospecific and brings about the formation of intermediates enriched with the desired isomeric components, which are converted into paroxetine in quantitative yields.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.