Simple enzymatic process for preparing cefazolin

摘要

Preparing cefazolin (A) involves acylating 7-amino-3-[(methyl-1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid with tetrazole containing acetic acid in the presence of biocatalyst containing penicillin amidase at pH of 6-8 and at -20 - 40 [deg]C; and precipitating (A) by adding an acid to lower the pH below 3.5 at 0-20 [deg]C. Preparing cefazolin (A) involves acylating 7-amino-3-[(methyl-1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid (I) or its salt with tetrazole containing acetic acid of formula (II) in the presence of biocatalyst containing penicillin amidase (EC 3.5.1.11) (100 - 50000 units per liter) at pH of 6 - 8 and at -20 - 40 (preferably 0 - 10)[deg]C; and precipitating (A) by adding an acid to lower the pH below 3.5 at 0 - 20[deg]C. [Image] R : ester or amide of the acid. ACTIVITY : Antibiotic. No biological data is given. MECHANISM OF ACTION : None given.