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1. WO2000039122 - PROCESS FOR THE PREPARATION OF AN ACETATE SALT OF PAROXETINE OR PAROXETINE ANALOGUES

Publication Number WO/2000/039122
Publication Date 06.07.2000
International Application No. PCT/GB1999/004367
International Filing Date 22.12.1999
Chapter 2 Demand Filed 10.07.2000
IPC
C07D 405/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
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 405/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
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
9828780.829.12.1998GB
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 ACETATE DE PAROXETINE ET DE SES ANALOGUES
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 crystallising the acetate salt from a solvent capable of dehydrating an aqueous solution by forming an azeotrope. 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 concerne un nouveau procédé de préparation d'un acétate d'un composé de formule (1), dans laquelle R1 représente un groupe phényle substitué, de préférence 3,4-méthylènedioxyphényle; lequel procédé consiste à cristalliser l'acétate à partir d'un solvant capable de déshydrater une solution aqueuse par formation d'un azéotrope. L'isomèrei(trans) (-)de 4-(4'-fluorophényl)-3-(3',4'-méthylènedioxyphénoxyméthyl)-pipéridine(paroxétine) est un composé important présentant les propriétés des médicaments antidépresseur et anti-Parkinson. Ce composé est utilisé en thérapie sous la forme d'un chlorhydrate, pour le traitement, entre autres, de la dépression, des troubles obsessionnels impulsifs et de la panique.
Also published as
US09869501
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