- Process for manufacture of cephalosporin such as ceftazidime and intermediate thereof
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This invention relates to reactive derivative of 2-(2-amino-4-thiazolyl)-(Z)-2-?(1-tert butoxycarbonyl-l-methylethoxy) imino!acetic acid of the following formula I STR1 as well as to the use thereof in the manufacture of cephalosporin antibiotic such as ceftazidime of formula II. STR2
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- Process for the production of cephalosporin derivatives
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New process for the production of the pentahydrate of ceftazidime of formula STR1 characterized in that the ester group of the compound of formula STR2 or an acid addition salt thereof, is cleaved by the sole use of aqueous hydrochloric acid, and the resulting ceftazidime is either crystallized directly from the reaction mixture as the pentahydrate by adding a base, or first of all the dihydrochloride of the ceftazidime is isolated by adding acetone and/or ethanol or another anti-solvent which is miscible with water, and this is converted into the pentahydrate by known methods.
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- Process for recovering ceftazidime
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A process for recovering ceftazidime from an aqueous solution containing it, said solution being at a pH in the range 2.0 to 5.5, which comprises contacting the said solution with a non-functional macroreticular resin suitable for adsorbing ceftazidime, eluting the ceftazidime and isolating it, if desired in the form of a salt or hydrate.
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- (6R,7R)-7-[(Z)-2-(2-Aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetamido]-3-(1-pyridiniummethyl)-ceph-3-em-4-carboxylate and salts thereof
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Cephalosporin antibiotics of the general formula STR1 (wherein Ra and Rb, which may be the same or different, each represent a C1-4 alkyl group or Ra and Rb together with the carbon atom to which they are attached form a C3-7 cycloalkylidene group; and R4 represents hydrogen or a 3- or 4-carbamoyl group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms. A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties, is (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimono) acetamido]-3-(1-pyridiniummethyl)-ceph-3-em-4 carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of such antibiotics.
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