EP 2043999 A2 20090408 - A PROCESS FOR THE PREPARATION OF VENLAFAXINE HYDROCHLORIDE
Title (en)
A PROCESS FOR THE PREPARATION OF VENLAFAXINE HYDROCHLORIDE
Title (de)
VERFAHREN ZUR HERSTELLUNG VON VENLAFAXINHYDROCHLORID
Title (fr)
PROCÉDÉ POUR LA PRÉPARATION DE CHLORHYDRATE DE VENLAFAXINE
Publication
Application
Priority
- IN 2006000474 W 20061127
- IN 1483MU2005 A 20051130
Abstract (en)
[origin: WO2007069277A2] A process for preparing venlafaxine hydrochloride and also a process for preparing l-[2-amino- l-(4-methoxy phenyl)ethyl]cyclohexanol hydrochloride, an intermediate of venlafaxine hydrochloride are disclosed. p-Methoxy phenyl acetonitrile is condensed with cyclohexanone in the presence of a base selected from alkali metal alkoxides and solvent selected from C4 alcohol at - 10 to - 5° C to obtain l-[cyano-l-(p-methoxy phenyl)m ethyl] cyclohexanol which is directly converted it into the l-[2-amino-l-(4-methoxy phenyl)ethyl] cyclohexanol without being isolated. The molar ratio of base to p-methoxy phenyl acetonitrile or cyclohexanone used is 0.1 to 0.4:1. The l-[2-amino-l-(4-methoxy phenyl)ethyl] cyclohexanol is converted its hydrochloride salt and subsequently formylated to venlafaxine base. The venlafaxine base is further converted into its salt namely venlafaxine hydrochloride. Both venlafaxine hydrochloride and l-[2-amino-l-(4-methoxy ?henyl)ethyl] cyclohexanol hydrochloride are obtained in high yield with high purity.
IPC 8 full level
C07C 213/02 (2006.01); C07C 217/74 (2006.01)
CPC (source: EP)
C07C 213/02 (2013.01)
C-Set (source: EP)
Citation (search report)
See references of WO 2007069277A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA HR MK RS
DOCDB simple family (publication)
WO 2007069277 A2 20070621; WO 2007069277 A3 20070726; EP 2043999 A2 20090408
DOCDB simple family (application)
IN 2006000474 W 20061127; EP 06847321 A 20061127