US 8,772,491 B2 · Process for the preparation of solifenacin succinate

Abstract

The present invention relates to a process for the preparation of Solifenacin succinate by condensing a compound of formula (IVb) with (RS)-3-quinuclidinol, wherein, R represents methyl, ethyl, isopropyl; to produce a diastereomeric mixture of (1S)-3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic acid (3RS)-1-azabicyclo[2.2.2]oct-3-yl ester, which is treated with succinic acid in a solvent or mixture of solvents to produce optically pure Solifenacin succinate, Formula (X).

Claims15

Dependent claims

A process for the preparation of Solifenacin succinate of formula (I);

which comprises:
(i) condensing a compound of formula (IVb) with (RS)-3-quinuclidinol of formula (Va),
wherein, R represents methyl, ethyl or isopropyl;
to produce a diastereomeric mixture of (1S)-3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic acid (3RS)-1-azabicyclo[2.2.2]oct-3-yl ester,
(ii) treating the diastereomeric mixture of step (i) with succinic acid in a solvent or mixture of solvents to produce optically pure Solifenacin succinate (I).

2 more elements

Dependencies are inferred from the claim text.

Facts

Application

13/261,551Filed 20 Jun 2011

Priority

IN 1815/CHE/201028 Jun 2010

Published

US 2013/0123502 A116 May 2013

Granted

8 Jul 2014

Term ends

Not estimatedThe source records don’t support an estimate.

Classification2 codes

C07D 453/02
Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids: containing not further condensed…
C07D
Heterocyclic compounds

Process for the preparation of solifenacin succinate

Life of this patent

Process for the preparation of solifenacin succinate

Life of this patent

Abstract

Claims15