To efficiently obtain the subject antibiotic substance without generating by products by reacting 6-aminopenicillanic acid or 7-aminocephalosporanic acid with amides in the presence of a penicillin acrylase and an enzyme inhibitor under a specific condition.
This antibiotic substance of formula V or formula VI is obtained by reacting 6-aminopenicillanic acid of formula I or 7-aminocephalosporanic acid of formula II with amides (or their salt) of formula III [wherein, R is a (substituted)hydrocarbon with 6-membered ring; R1 is H, a halogen, methyl, methoxy, a 1-4C alkenyl, methylene combined with an organic group through O, S or N; R2 and R3 are each H or a 1-3C alkyl] in the ratio of the acid to the amide of 1 mol/(1-6) mol in the presence of a free or immobilized penicillin acylase at -5°C to +35°C in an aqueous medium and in the presence of an enzyme inhibitor of formula IV [wherein, R4 is a 1-5C alkyl, a (substituted) aromatic ring, H, or the like; Y is absent, O, S, CH2, phyenylene, or the like; R5 is a carboxyl or the like; R6 is H, OH, CH3, or the like] added in a molarity of 0.0001-0.2.
AURO ROBERUTO TATSURIAANI
EMIRIAANO KANNASU
ANJIERO BECHIYUREERI
