| 摘要 |
<p>PROBLEM TO BE SOLVED: To simply obtian the subject compound useful for antibiotics, etc., by reacting a 7-protected amino-3-halogenomethyl-cephem carboxylic acid ester with a 5-mercaptothiazole compound and subsequently reacting the reaction product with a tetrazole acetic acid. SOLUTION: This method for producing the highly pure cefazolin of formula V comprises reacting a 7-phenylacetic amino-2-halongenomethyl-3cephem-4- carboxylic acid ester of formula I (X is a halogen; R<1> is a carboxylic acid- protecting group) with 2-methyl-5-mercapto-1,3,4-thiadiazole of formula II in the presence of a base in at least one of water, organic solvents, etc., deesterifying the reaction product in the presence of a phenol compound, subjecting the reaction product to a phenyl acetic acid-removing reaction using immobilized penicillin G acylase, and further reaction the obtained compound of formula III with a 1H-tetrazole-1-acetic acid of formula IV in the presence of an acid halide in an organic solvent.</p> |
