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1. NZ582668 - PREPARATION OF N-ALKYLATED OPIATES BY REDUCTIVE AMINATION

Office
New Zealand
Application Number 582668
Application Date 18.01.2010
Publication Number 582668
Publication Date 24.02.2012
Publication Kind A
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 SpecGx LLC
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
Abstract
(EN)
Patent 582668 Disclosed is a process for preparing N-alkylated morphinan compounds of formula (II) where the variables are as disclosed in the description. The process includes reducing an N-imine or hemiaminal morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source that is a protic compound.