Crystalline cephalosporin hydrohalide salts
AssigneeThe Upjohn Company
InventorsMahendra I. Amin, Jay A. Campbell
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Abstract
Crystalline hydrohalide salts of the cephalosporin antibiotic ceftiofur, processes for their manufacture, and pharmaceutical compositions containing one of these salts are provided.
Claims13
A cephalosporin hydrohalide compound of the formula
- where X is chloride or bromide.
A process for preparing a crystalline cephalosporin hydrohalide salt of the formula ##STR2## where X is chloride or bromide, which comprises the steps of (a) treating the N-tritylamino cephalosporin compound of the formula ##STR3## with a solution of a polar organic solvent and water and hydrogen halide, where halide is chloride or bromide, in an amount which is at least stoichiometrically equivalent to the amount of the N-trityl compound (3) in the mixture,
- (b) heating the mixture from step (a) to a temperature of at least 45.degree. C. and for a time sufficient to effect detritylation,
- (c) decreasing the concentration of the polar organic solvent in the aqueous phase of mixture from step (b) to effect formation of crystalline cephalosporin hydrohalide salt (1),
- (d) separating the crystalline cephalosporin hydrohalide salt from the slurry mixture from step (c),
- (e) washing the separated crystalline cephalosporin hydrohalide salt from step (d) with water and polar organic solvent, and drying the washed crystalline cephalosporin hydrohalide salt from step (e).
Dependencies are inferred from the claim text.