CHEMICAL PROCESS FOR THE PREPARATION OF INTERMEDIATES TO OBTAIN N-FORMYL HYDROXYLAMINE COMPOUNDS

Title:

CHEMICAL PROCESS FOR THE PREPARATION OF INTERMEDIATES TO OBTAIN N-FORMYL HYDROXYLAMINE COMPOUNDS

Document Type and Number:

WIPO Patent Application WO2004076053

Kind Code:

A3

Abstract:

Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features : (1) make use of a particular beta-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products. See Formula (I).

Inventors:

PRASHAD MAHAVIR (US)
KIM HANG-YONG (US)
HU BIN (US)
SLADE JOEL (US)
KAPA PRASAD KOTESWARA (US)
GIRGIS MICHAEL JOHN (US)

Application Number:

PCT/US2004/005159

Publication Date:

December 02, 2004

Filing Date:

February 20, 2004

Export Citation:

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Assignee:

NOVARTIS AG (CH)
NOVARTIS PHARMA GMBH (AT)
PRASHAD MAHAVIR (US)
KIM HANG-YONG (US)
HU BIN (US)
SLADE JOEL (US)
KAPA PRASAD KOTESWARA (US)
GIRGIS MICHAEL JOHN (US)

International Classes:

A61P31/04; C07C51/487; C07C239/20; C07D401/12; (IPC1-7): C07C239/20; C07D401/12; C07B53/00; C07C259/06; A61K31/44; A61P31/04

Domestic Patent References:

WO2002102790A1

2002-12-27

Foreign References:

US6576772B1	2003-06-10
US6423690B1	2002-07-23

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