Original-quality ceftriaxone sodium and pharmaceutical preparation thereof

2015 
The invention discloses original-quality ceftriaxone sodium and a pharmaceutical preparation thereof. The key technology and industrialization of the third generation of cephalosporin antibiotics active ester intermediate wins the second prize of National Scientific and Technological Progress Award, and the third generation of cephalosporin antibiotics intermediate AE active ester is a key factor for affecting the internal quality of the ceftriaxone sodium. A preparation method comprises the steps that 1, boron trifluoride-acetonitrile serves as a catalyst, and on the condition that acetonitrile serves as solvent, a triazine ring is reacted with 7-ACA to generate 7-ACT; 2, triethylamine and aminothiazoly loximate are added into the solvent, a chloroformate activator is dropwise added slowly during cooling mixing, the 7-ACT is added for a one-pot reaction after stirring is conducted, and ceftriaxone is obtained; 3, a salt-forming agent is added, and the ceftriaxone sodium is obtained. According to the preparation method, use of a condensing agent with higher price is avoided, the process route is shortened, operation is easy, the reaction condition is mild, the product yield is high, the purity is good, and industrial production is easy.
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