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1. WO2000039123 - PROCESS FOR THE PREPARATION OF AN ACETATE SALT OF PAROXETINE OR PAROXETINE ANALOGUES

Publication Number WO/2000/039123
Publication Date 06.07.2000
International Application No. PCT/GB1999/004370
International Filing Date 22.12.1999
Chapter 2 Demand Filed 10.07.2000
IPC
C07D 211/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
18with substituted hydrocarbon radicals attached to ring carbon atoms
20with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
22by oxygen atoms
CPC
A61P 1/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 17/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
14for baldness or alopecia
C07D 211/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
18with substituted hydrocarbon radicals attached to ring carbon atoms
20with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
22by oxygen atoms
Applicants
  • SMITHKLINE BEECHAM PLC [GB/GB]; New Horizons Court Brentford Middlesex TW8 9EP, GB (AllExceptUS)
  • CRAIG, Andrew, Simon [GB/GB]; GB (UsOnly)
  • JONES, David, Alan [GB/GB]; GB (UsOnly)
  • MAN, John [GB/GB]; GB (UsOnly)
Inventors
  • CRAIG, Andrew, Simon; GB
  • JONES, David, Alan; GB
  • MAN, John; GB
Agents
  • WEST, Vivien; Corporate Intellectual Property SmithKline Beecham Two New Horizons Court Brentford Middlesex TW8 9EP, GB
Priority Data
9828781.629.12.1998GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF AN ACETATE SALT OF PAROXETINE OR PAROXETINE ANALOGUES
(FR) PROCEDE DE PREPARATION D'UN SEL D'ACETATE DE PAROXETINE OU D'ANALOGUES DE PAROXETINE
Abstract
(EN)
The present invention relates to a new process for the preparation of an acetate salt of a compound of formula (1) in which R1 is a substituted phenyl group, preferably 3,4-methylenedioxyphenyl; the process comprising contacting a solution of the compound of formula (1) with an amine acetic acid salt. The (-) $i(trans) isomer of 4-(4'-fluorophenyl)-3-(3',4'methylenedioxyphenoxymethyl)-piperidine (paroxetine) is an important compound having antidepressant and anti-Parkinson properties. This compound is used in therapy as the hydrochloride salt to treat inter alia depression, obsessive compulsive disorder (OCD) and panic.
(FR)
La présente invention a trait à un nouveau procédé de préparation d'un sel d'acétate d'un composé représenté par la formule (1), dans laquelle R1 est un groupe phényle substitué, de préférence du 3,4-méthylènedioxyphényle; le procédé comporte les étapes consistant à mettre en contact une solution du composé représenté par la formule (1) avec un sel d'acide acétique aminé. L'isomère $i(trans) (-) de 4-(4'-fluorophényle)-3-(3',4'méthylènedioxyphénoxyméthyle)-pipéridine (paroxétine) est un composé important possédant des propriétés d'antidépresseur et anti-Parkinson. Ce composé est utilisé en thérapie comme un sel de chlorhydrate pour traiter entre autres la dépression, les troubles compulsifs obsessionnels (OCD) et la panique.
Also published as
US09869471
Latest bibliographic data on file with the International Bureau