METHOD FOR MANUFACTURING AN INTERMEDIATE FOR THE SYNTHESIS OF CEPHALOSPORIN ANTIBIOTICS

摘要

PURPOSE: Provided is a method for manufacturing an intermediate for the synthesis of cephalosporin antibiotics to inhibit the production of lactone compounds, thereby increasing production yield and cutting off production cost. CONSTITUTION: The manufacturing method of an intermediate of the formula(1) comprises the steps of: hydrolyzing a compound of the formula(4) at -30 to -10 deg.C for 0.5-3 hours in a mixed solvent of an organic solvent and water, wherein the organic solvent is selected from tetrahydrofuran, methylenechloride, N,N-dimethylformamide, N,N-dimethylacetamide, acetonitrile, ethylacetate, aceton, methanol, ethanol, isopropanol, t-butanol or their mixture; acylating the compound of the formula(3) with an acylating agent of R1COY(wherein, Y is halogen, dialkylphsphate, diarylphosphate or 2-mercaptobenzothiazole) in a buffer of pH 7-10 without separation or purification to obtain a compound of the formula(2); and protecting a carboxyl group of the compound of the formula(2) to obtain a compound of the formula(1).