PROCESS FOR PREPARATION OF INTERMEDIATE USEFUL IN SYNTHESIS OF CEFDITOREN

摘要

PURPOSE: A process for the preparation of an intermediate useful in the synthesis of cefditoren is provided, thereby preparing the high quality cefditoren intermediate without using any organic solvent at room temperature. CONSTITUTION: A process for the preparation of 7 - amino - 3 - £2 - (4 - methylthiazol - 5 - yl) vinyl| - 3 - cephem carboxylic acid of the formula (I) as an intermediate useful in the synthesis of cefditoren comprises reacting 7 - phenylacetamido - 3 - £2 - (4 - methylthiazol - 5 - yl) vinyl| - 3 - cephem carboxylic acid of the formula (II) with penicillin G amidase to remove a phenylacet group at 7-site, wherein the reaction temperature is 5 to 40 deg. C and the reaction pH is 8 to 8.5; a filtration process of the immobilized penicillin G amidase is optionally added after the completion of the reaction; and a crystallization process by adding an organic solvent into the filtered solution to control pH of the solution is optionally added.