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1. US20100197921 - Preparation of N-alkylated opiates by reductive amination

Office
United States of America
Application Number 12668900
Application Date 16.06.2008
Publication Number 20100197921
Publication Date 05.08.2010
Grant Number 08729266
Grant Date 20.05.2014
Publication Kind B2
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
CPC
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
Applicants Christopher W. Grote
Mallinckrodt LLC
Brian Orr
Tao Jiang
Gary L. Cantrell
Inventors Christopher W. Grote
Brian Orr
Tao Jiang
Gary L. Cantrell
Title
(EN) Preparation of N-alkylated opiates by reductive amination
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.