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1. (WO2004031155) ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF BOTH ENANTIOMERS OF 10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ [b,f]AZEPINE-5-CARBOXAMIDE AND NEW CRYSTAL FORMS THEREOF

Pub. No.:    WO/2004/031155    International Application No.:    PCT/EP2003/011034
Publication Date: Apr 15, 2004 International Filing Date: Oct 6, 2003
IPC: C07D 223/24
C07F 15/00
Applicants: NOVARTIS AG
NOVARTIS PHARMA GMBH
MATHES, Christian
SEDELMEIER, Gottfried
BLATTER, Fritz
PFEFFER, Sabine
GRIMLER, Dominique
Inventors: MATHES, Christian
SEDELMEIER, Gottfried
BLATTER, Fritz
PFEFFER, Sabine
GRIMLER, Dominique
Title: ENANTIOSELECTIVE PROCESS FOR THE PREPARATION OF BOTH ENANTIOMERS OF 10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ [b,f]AZEPINE-5-CARBOXAMIDE AND NEW CRYSTAL FORMS THEREOF
Abstract:
The invention relates to a novel process for the manufacture of substituted enantiopure 10hydroxy-­dihydrodibenz[b,f]azepines (la), (lb) wherein each of R1 and R2, independently, are hydrogen, halogen, amino or nitro; and each of R3 and R4, independently, are hydrogen or C1-C6alkyl; by transfer hydrogenation of 10-oxo-dihydrodibenz[b,f]azepines; and to novel catalysts of formula (III'a) and (III'b) wherein M is Ru, Rh, Ir, Fe, Co or Ni; L1 is hydrogen; L2 represents an aryl or aryl-aliphatic residue; and the further radicals have the meanings as defined herein; and to new crystal forms of both enantiomers of 10,11-dihydro-10 hydroxy-5Hdibenz[b,f]azepine-5-carboxamide, obtainable by the new processes, their usage in the production of pharmaceutical preparations, new pharmaceutical preparations comprising these new crystal forms and/or the use of these new crystal forms in the treatment of disorders such as epilepsy, or in the production of pharmaceutical formulations which are suitable for this treatment.