SYNTHESIS OF AMORPHOUS CEPHROXIM ACETYL

摘要

PURPOSE: A synthetic method is provided which omits a crystallization stage by addition of side reaction inhibitors. CONSTITUTION: Cefuroxime sodium is esterified using the side reaction inhibitors such as transition metal, alkali metal halide, zinc chloride, zinc bromide, zinc iodide, sodium iodide, followed by dispersion in a solvent such as water, hexane, cyclohexane or isopropyl ether to give 1-acetoxyethyl(6R, 7R)-3-carbamoyloxymethyl-7-£(z)-2-(fur-2- yl)-2-methoxy-iminoacetamido|cefu-3-em-4-carboxylate. For example, 40ml of dimethyl acetamide, 10g of Cefuroxime sodium and 5g zinc chloride are stirred at 10 degree C for 30 minutes, followed by addition of 3.6ml of ethyl bromoacetate at 10 degree C for 2 hours. A separated organic fraction is dispersed in 900ml of isopropyl ether to give the title compounds.