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1. JP2010533719 - 還元的アミノ化によるN-アルキル化オピエートの調製

Office
Japan
Application Number 2010517045
Application Date 16.06.2008
Publication Number 2010533719
Publication Date 28.10.2010
Publication Kind A5
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 489/12
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:
09containing 4aH-8, 9 c-Iminoethano- phenanthro furan ring systems condensed with carbocyclic rings or ring systems
10with a bridge between positions 6 and 14
12the bridge containing only two carbon atoms
A61K 31/485
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
485Morphinan derivatives, e.g. morphine, codeine
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
C07B 53/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
53Asymmetric syntheses
C07B 61/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
61Other general methods
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 マリンクロッド エルエルシー
Inventors グロート, クリストファー ダブリュー.
オーアー, ブライアン
チアン, タオ
カントレル, ゲイリー エル.
Agents 大塩 竹志
Priority Data 60/950,127 17.07.2007 US
Title
(JA) 還元的アミノ化によるN-アルキル化オピエートの調製
Abstract
(JA)

本発明は、ルテニウム不斉触媒、ロジウム不斉触媒、もしくはイリジウム不斉触媒および水素源の存在下における、モルフィナンのN−イミン部分もしくはヘミアミナール部分の還元を対象とする。本発明は、N−アルキル化モルフィナン、それらの塩、中間体、および類似体の調製のための改善された合成方法を対象とする。本発明の一態様において、当該合成方法は、ルテニウム不斉触媒、ロジウム不斉触媒、もしくはイリジウム不斉触媒および水素源を用いて、モルフィナンのN−イミン部分またはヘミアミナール部分を対応するアルキル基に還元する。