EP 1515958 A2 20050323 - PROCESS FOR THE SYNTHESIS OF MOSAPRIDE
Title (en)
PROCESS FOR THE SYNTHESIS OF MOSAPRIDE
Title (de)
VERFAHREN ZUR HERSTELLUNG VON MOSAPRIDE
Title (fr)
PROCEDE DE SYNTHESE DU MOSAPRIDE
Publication
Application
Priority
- HU 0300042 W 20030612
- HU P0201980 A 20020613
Abstract (en)
[origin: WO03106440A2] The invention relates to a process for the synthesis of mosapride citrate of formula (I), the chemical name: (R,S)-4-amino-5-chloro-2-ethoxy-N-{ [4-(4-fluoro-benzyl)-2 morpholinyl]-methyl}benzamide citrate dihydrate, (I), (II) reacting the compound of formula (II) with di-tert-butyl-dicarbonate in an alcohol in the presence of a base, the obtained product is ethylated in an inert solvent in the presence of a base, the obtained compound is hydrolyzed with an alkyl-hydroxide and the obtained salt neutralized with an acid, the obtained product is chlorinated, and the obtained compound of formula (VI) is reacted with the compound of formula (VII), (VI), (VII) where BOC is tert-butoxy-carbonyl protecting group and removing the protecting group from the obtained compound of formula (VIII) the mosapride base is prepared, (VIII) where BOC is defined as above and in desired case with an acid, preferably with citric acid a pharmaceutically acceptable salt, preferably the mosapride citrate dehydrate of formula (I) is produced.
IPC 1-7
CPC (source: EP)
C07D 265/30 (2013.01); Y02P 20/55 (2015.11)
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LI LU MC NL PT RO SE SI SK TR
DOCDB simple family (publication)
WO 03106440 A2 20031224; WO 03106440 A3 20040617; AU 2003242867 A1 20031231; AU 2003242867 A8 20031231; EP 1515958 A2 20050323; HU 0201980 D0 20020828; HU P0201980 A2 20040301; HU P0201980 A3 20080630
DOCDB simple family (application)
HU 0300042 W 20030612; AU 2003242867 A 20030612; EP 03760090 A 20030612; HU P0201980 A 20020613