Preparation of 7-amino-.delta.3-cephem derivatives

C - Chemistry – Metallurgy – 12 – P

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C12P 19/00 (2006.01) C12P 35/02 (2006.01)

Patent

CA 1048950

PREPARATION OF 7-AMINO-.DELTA.3-CEPHEM DERIVATIVES WITH CARRIER BOUND PENICILLIN ACYLASE Abstract 7-Amino-.DELTA.3-cephem derivatives of the formula: Image wherein R is hydrogen, hydroxyl, amino, cyano, -O-CO-NH2, Image wherein n is 4 to 6, -O-CO R1, -NH-CO-R1, Image wherein R1 is straight or branched chain alkyl of 1 to 4 carbon atoms, Het or S-Het wherein Het is a 5- or 6-membered heteroaromatic ring unsubstituted or substituted by 1 to 3 alkyl moieties of 1 to 3 carbon atoms or said ring having a positive charge; and X is hydrogen, or if R has a positive charge, X is a negative charge, which comprises contacting a compound of the formula: Image or a salt thereof, wherein R and X are as above defined, R2 is phenyl, phenoxy, 2-thienyl or 2-furyl unsub- stituted or substituted by amino, hydroxyl or alkyl of 1 to 3 carbon atoms; and R3 is hydrogen, amino, hydroxyl or alkyl of 1 to 3 carbon atoms, with penicillin acylase which is bound by covalent bonds to a water-soluble carrier and isolating the product produced. The penicillin acylase may be in a form which is enclosed in a water-insoluble carrier material.

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