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1. EP2167505 - PREPARATION OF N-ALKYLATED OPIATES BY REDUCTIVE AMINATION

Office
European Patent Office
Application Number 08771136
Application Date 16.06.2008
Publication Number 2167505
Publication Date 31.03.2010
Publication Kind B1
IPC
C07D 489/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
489Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro furan ring systems, e.g. derivatives of -morphinan of the formula:
02with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
C07D 489/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
489Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro furan ring systems, e.g. derivatives of -morphinan of the formula:
06with a hetero atom directly attached in position 14
08Oxygen atom
CPC
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
C07D 489/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
489Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
02with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
C07D 489/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
489Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
06with a hetero atom directly attached in position 14
08Oxygen atom
Applicants MALLINCKRODT LLC
Inventors GROTE CHRISTOPHER W
ORR BRIAN
JIANG TAO
CANTRELL GARY L
Designated States
Priority Data 95012707 17.07.2007 US
Title
(DE) HERSTELLUNG VON N-ALKYLIERTEN OPIATEN DURCH REDUKTIVE AMINIERUNG
(EN) PREPARATION OF N-ALKYLATED OPIATES BY REDUCTIVE AMINATION
(FR) PRÉPARATION D'OPIACÉS N-ALKYLÉS PAR AMINATION RÉDUCTRICE
Abstract
(EN)
The present invention is directed to the reduction of an N-imine moiety or a hemiaminal moiety of a morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.

(FR)
L'invention concerne la réduction d'un groupe N-imine ou d'un groupe hémiaminal d'un morphinane en présence d'un catalyseur asymétrique au ruthénium, au rhodium, ou à l'iridium et d'une source d'hydrogène.