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US 2007/0105830 A1Published application
Processes for the preparations of cefepime
AssigneeSandoz Ltd.
InventorsJohannes Ludescher, Hubert Sturm, Siegfried Wolf
Life of this patent
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Abstract
This invention provides processes for preparing cefepime, including crystalline intermediates of Formula V.
Claims18
A process for producing a compound of formula I
- wherein a compound of formula IIA or IIB
- wherein
- R1 is a trialkylsilyl group,
- R is hydrogen or a trialkylsilyl group,
- n is 0-2 and
- X signifies chloride, bromide or iodide
- is reacted with a reactive derivative of formula III
- wherein Y signifies halogen or a leaving group, to form a compound of formula IV or V
- wherein T is trialkylsilyl, the silyl protecting groups, if present, are removed, or the compound of formula IV as the acid addition salt of formula V is isolated wherein m is 0 or 1 and the compound of formula IV
- or the compound of formula V is cyclised with thiourea, and subsequently the compound of formula I is isolated.
7 more elements
A compound of formula V, wherein Y and X are Cl.
A process for producing the compound of formula I
- characterised in that a compound of formula VIII
- is desilylated in a protic solvent, and subsequently reacted with N-methylpyrrolidine to form a compound of formula X, and this is then converted into the compound of formula I
A process for producing the compound of formula I wherein a compound of formula IIA, in unsolvated or solvated form, is reacted optionally after addition of a base, with a compound of formula XII
- in acetone or aqueous acetone, and the compound of formula I precipitated in crystalline form from the reaction mixture by adding HCl.
Dependencies are inferred from the claim text.