PURPOSE: To prepare cephradine useful as an antibacterial agent, by the acylation of 7-aminodesacetoxycephalosporanic acid (7-ADCA) in the presence of an acylase produced by bacteria belonging to Acetobacter genus.
CONSTITUTION: Cephradine is prepared by (1) culturing bacteria belonging to Azotobacter genus, e.g. Anzotovacter No.5686 (FERM-P No.1661), fixing the bacterial cell obtained by separating from the medium followed by washing, or an enzyme existing in the bacterial cell, to a water-insoluble carrier such as actibated alumina, etc., to obtain an immobilized enzyme, and (3) acrylating 7-ADCA in a buffer solution containing D-α-(1,4-cyclohexadienyl)-glycine lower alkyl (pref. methyl) ester, in the presence of the above immobilized enzyme at 18W22°C, pH 6.8W7.2 for 1W15hr. The concentration of the 7-ADCA in the reaction system is 0.1W50mg/ml, pref. 5W20mg/ml, and the molar ratio of the glycine ester to the 7-ADCA is 2W20, pref. 1.5W4.
MATSUMOTO IKUO
KUBOTA ISAO
