EP 2137148 A1 20091230 - PROCESS FOR THE PREPARATION OF PERINDOPRIL ERBUMINE SALT AND NOVEL POLYMORPH (S) THEREOF
Title (en)
PROCESS FOR THE PREPARATION OF PERINDOPRIL ERBUMINE SALT AND NOVEL POLYMORPH (S) THEREOF
Title (de)
VERFAHREN ZUR HERSTELLUNG VON PERINDOPRILERBUMINSALZ UND NEUER POLYMORPH (S) DAVON
Title (fr)
PROCÉDÉ DE PRÉPARATION D'UN SEL DE PÉRINDOPRIL ERBUMINE ET SON OU SES NOUVEAUX POLYMORPHES
Publication
Application
Priority
IN 2007000120 W 20070322
Abstract (en)
[origin: WO2008114270A1] A single pot process for the preparation of perindopril erbumine salt according to which condensation of (2S, 3aS, 7aS)-octahydroindole-2-carboxylic acid benzyl ester para toluene sulfonate with N-((S-)-ethoxy carbonyl -1-ethyl-(S)-alanine, catalytic hydrogenation of benzyl ester of (2S, 3aS, 7aS)-1-{2-[1-(ethoxycarbonyl)-(S)-butylamino]-(S)propionyl}- octahydro-indole-2-carboxylate and conversion of (2S,3aS, 7aS)-1-{2-[1-ethoxycarbonyl)_(S)-butylamino]-(S)-propionyl}octahydroindole-2-carboxylic acid to its perindopril erbumine salt are carried out in a single pot using a single solvent such as isopropyl acetate to obtain perindopril erbumine salt of very high purity. Also a novel polymorph S of perindopril erbumine having X-ray diffraction peaks of 9.10, 14.64, 15.37, 16.58, 17.39, 19.99, 20.62, 21.50, 22.15, 22.60, 24.20, 27.55 ± 0.2 at 2T values. Also processes for preparing the novel polymorph S.
IPC 8 full level
C07D 209/42 (2006.01)
CPC (source: EP)
C07D 209/42 (2013.01)
Citation (search report)
See references of WO 2008114270A1
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 MT NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
DOCDB simple family (application)
IN 2007000120 W 20070322; EP 07827487 A 20070322