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1. CA2693436 - PREPARATION OF N-ALKYLATED OPIATES BY REDUCTIVE AMINATION

Office
Canada
Application Number 2693436
Application Date 16.06.2008
Publication Number 2693436
Publication Date 22.01.2009
Publication Kind A1
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
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
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
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
Applicants MALLINCKRODT INC.
Inventors GROTE, CHRISTOPHER W.
ORR, BRIAN
JIANG, TAO
CANTRELL, GARY L.
Priority Data 60/950,127 17.07.2007 US
Title
(EN) PREPARATION OF N-ALKYLATED OPIATES BY REDUCTIVE AMINATION
(FR) PREPARATION D'OPIACES N-ALKYLES PAR AMINATION REDUCTRICE
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.