Patent ID: 6458558
Filing Date: 2002-10-01
Classification: C07D,C12P

Abstract:
A process for the preparation of Cefuroxime acid (I) starting from deacetyl 7-glutaryl ACA (II), which comprises the following steps, without recovery of any intermediates:a) extracting a deacetyl 7-glutaryl ACA (II) aqueous solution at pH 1-3 and at a temperature of 0-15Â° C. with an organic solvent, to obtain an organic phase containing deacetyl 7-glutaryl ACA (II) b) adjusting said organic phase to pH 6-8, then drying such phase by distillation under vacuum at a temperature below or equal to 25Â° C.; c) reacting deacetyl 7-glutaryl ACA (II) with an activated isocyanate at temperatures ranging from âˆ’30 to 0Â° C., to obtain (6R,7R)-7-[(4-carboxy-1-oxobutyl)amino]-3-carbamoyloxymethyl-ceph-3-em-4-carboxylic acid (III) d) extracting said compound (III) from the reaction mixture with water at pH of 6-8 and at a temperature of 0-15Â° C.; e) transforming compound (III) into (6R,7R)-7-amino-3-carbamoyloxymethyl-ceph-3-em-4-carboxylic acid (IV) by glutaryl acylase enzymatic hydrolysis, at pH 7-9 and at a temperature of 20-30Â° C.;f) condensing compound (IV) with a 2-furanyl(sin-methoxyimino)acetic acid halide or anhydride, to obtain the desired Cefuroxime acid (I).