C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 239/20 (2006.01) A61K 31/44 (2006.01) A61P 31/04 (2006.01) C07B 53/00 (2006.01) C07C 259/06 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2516465
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).
L'invention porte sur des procédés améliorés de préparation d'intermédiaires utiles pour préparer des N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl ou -hétéroaryl)-azacyclo4-7alcanes ou thiazacyclo4-7alcanes antibactériens possédant une ou plusieurs des caractéristiques suivantes: (1) ils utilisent un intermédiaire de .beta.-lactame particulier; (2) et également des agents de résolution, des acides propioniques substitués énantiomériquement purs, notamment l'acide (R)-2-butyl-3-hydroxy-propionique; (3) ils évitent l'utilisation du peroxyde d'hydrogène; et (4) ils facilitent la production réduisant la débenzylation sélective de sous-produits résiduaires .
Girgis Michael John
Hu Bin
Kapa Prasad Koteswara
Kim Hong Yong
Prashad Mahavir
Fetherstonhaugh & Co.
Novartis Ag
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