Intermediates for linezolid and related compounds

Details Intermediates for linezolid and related compounds Intermediates for linezolid and related compounds

2004-07-20

2008-09-30

McKane, Joseph (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

C548S465000

Reexamination Certificate

active

07429661

ABSTRACT:
The present invention provides a novel process for preparation of 5 aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus, the key intermediate of linezolid is prepared by a) reacting N-[3-Chloro-2-(R)-hydroxypropyl]-3-fluoro-4-morpholinyl aniline with potassium phthalimide; b) subjecting N-[3-pthalimido-2-(R)-hydroxypropyl]-3-fluoro-4-(morpholinyl) aniline produced in the above step to carbonylation; and c) reacting (S)-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidiriyl]methyl]phthalimide produced in the above step with hydrazine hydrate to produce (S)-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]amine.

REFERENCES:
patent: 5688792 (1997-11-01), Barbachyn et al.
patent: 5837870 (1998-11-01), Pearlman et al.
patent: 7034017 (2006-04-01), Straub et al.
patent: 7307163 (2007-12-01), Mohan Rao et al.
patent: 4024 (1979-09-01), None
patent: 50827 (1982-05-01), None
patent: 0275742 (1988-07-01), None
patent: 2506769 (1982-12-01), None
patent: WO 95/07271 (1995-03-01), None
patent: WO 99/24393 (1999-05-01), None
J. Med Chem, 39(3), 673-679 (1996).
Tetrahedron Lett., 40(26), 4855, 1999.
International Search Report dated Jul. 20, 2004.
Abstract of CN 1355165A.

Affiliated with

Also associated with

Rating

Intermediates for linezolid and related compounds does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Intermediates for linezolid and related compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Intermediates for linezolid and related compounds will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3974728