The Improvement of Synthetic Process for Ceftaroline Fosamil
Using GHYH as starting material,sulfonate was obtained under the reation of GHYH and benzenesulfonyl chloride.A substitution reaction occurs with PTT.Methyl toluenesulfonate as the methylation reagent,cresol and immobilized penioillin acylase were used to remove the carboxyl and amino protecting groups.Rereacted with ATDE-Cl and recrystallized in a mixture of acetic acid and water to obtain Ceftaroline fosamil.The improved synthesis route does not use methanesulfonyl chloride,simple operation,phosphorus free wastewater,less impurities,cheap raw materials,quality improvement and little environmental pollution,and is a suitable synthisis method for industrial prodution.