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1. EP2133350 - A method for the preparation of an enantiomerically pure benzazepine

Office
European Patent Office
Application Number 09165233
Application Date 10.04.2008
Publication Number 2133350
Publication Date 16.12.2009
Publication Kind B1
IPC
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
CPC
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
Applicants MERCK SHARP & DOHME
Inventors KEMPERMAN GERARDUS JOHANNES
SEERDEN JOHANNES PAULUS GERARDUS
Designated States
Priority Data 07105979 11.04.2007 EP
08736037 10.04.2008 EP
09165233 10.04.2008 EP
Title
(DE) Verfahren für die Herstellung eines enantiomerenreinen Benzazepins
(EN) A method for the preparation of an enantiomerically pure benzazepine
(FR) Procédé de préparation de benzazépine pure énantiomorphiquement
Abstract
(EN) The invention relates to a method for the preparation of a cyclic compound according to formula III comprising reacting a compound according to Formula I and a compound according to formula II, wherein in Formula I, R 1 , R 2 , R 3 and R 4 may be hydrogen or substituent groups comprising one or more carbon atoms and/or hetero-atoms, wherein R 1 , R 2 , R 3 and R 4 can be combined in aromatic or aliphatic ring structures, - Y is a ring element comprising 1 - 3 substituted or unsubstituted carbon atoms and/or heteroatoms in the ring and - R 5 is hydrogen or a hydrocarbon substituent group comprising one or more carbon atoms and optionally one or more hetero atoms, and wherein in Formula II, Z 1 and Z 2 are, leaving groups, X is a reactive functional hydrocarbon group for subsequent ring closure, comprising one or more carbon atoms and a reactive functional group and having a chain of between 1 to 6 atoms between the carbon atom attached to the central carbon atom of formula II and the reactive functional group and R 8 is hydrogen or a hydrocarbon substituent different from X making the central carbon atom of formula II a chiral centre in Formula III and wherein reactive functional group X can be or can be extended to be compound of formula IV which can be ring closed to produce the polycyclic component of formula V. More in particular, the invention relates to the preparation of mirtazapine precursors and mirtazapine preferably having a substantial enantiomeric excess.