EP 1140832 A1 20011010 - PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES
Title (en)
PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES
Title (de)
VERFAHREN ZUR HERSTELLUNG VON ARYLPIPERIDINCARBINOL-ZWISCHENPRODUKTEN UND DERIVATEN
Title (fr)
PROCEDE DE PREPARATION D'INTERMEDIAIRES ET DE DERIVES DE ARYLPIPERIDINE CARBINOL
Publication
Application
Priority
- US 9930365 W 19991217
- US 21839398 A 19981222
Abstract (en)
[origin: WO0037443A1] A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II), where X is halogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 haloalkyl, hydroxy, or hydrogen; and R2 and R3 each is C1-C4 alkyl and R2 and R3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (+/-)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (-)-trans configuration.
IPC 1-7
IPC 8 full level
C07C 253/30 (2006.01); C07C 255/41 (2006.01); C07D 211/78 (2006.01)
CPC (source: EP)
C07C 255/41 (2013.01); C07D 211/78 (2013.01); C07B 2200/07 (2013.01)
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 0037443 A1 20000629; AU 2200400 A 20000712; EP 1140832 A1 20011010; EP 1140832 A4 20041103; HU P0104036 A2 20020228; HU P0104036 A3 20030428; JP 2002533325 A 20021008
DOCDB simple family (application)
US 9930365 W 19991217; AU 2200400 A 19991217; EP 99966475 A 19991217; HU P0104036 A 19991217; JP 2000589515 A 19991217