Method for synthesizing cefuroxime sodium

Abstract

The invention relates to a synthesis method for cefuroxime acid, which includes the following steps: (1) N-acylation reaction is first carried out by using 7-ACA and methoxy imino furan ammonium acetate as materials; then, the 3 bit acetyl of the reaction product is hydrolyzed; finally MDCC is crystallized out by using hydrochloride in water phase; (2) the MDCC and a strong carbamoyl agent P-isocyanate are done with nucleophilic addition in an organic solvent to obtain chlorosulfonation cefuroxime; cefuroxime acid is obtained after the hydrolyzation; then a product is crystallized. The main technical features of the method are as follows: the adoption of a strong alkaline environment is avoided during the period of the hydrolysis of the step (1); while the mild-conditioned enzymatic hydrolysis is adopted to cause the yield of the product to be improved by more than 8 percent and reach 93 percent, and the stability of the product can be improved at the same time. The cefuroxime acid of the step (2) crystallizing in the water phase environment facilitates the removing of impurities and acid media, improves the stability of products and lowers the production cost simultaneously.

Description

Technical field [0001] The invention relates to a method for synthesizing cefuroxime acid. Background technique [0002] Cefuroxime series belong to the second generation of cephalosporins, which have a broad-spectrum antibacterial effect. The distinguishing feature is the high stability of the hydrolytic enzymes that produce drug-damaging effects on bacteria, thus ensuring excellent antibacterial activity. It is rarely used in clinical applications. An adverse reaction occurred. [0003] Cefuroxime was first successfully developed and patented by Glaxo Wellcome. The product was first marketed in the UK, Ireland, Germany and Italy in 1978 under the trade name "Cilixin", and subsequently sold in many countries and regions around the world. It was approved by the U.S. FDA on December 28, 1987, and was listed in the U.S. in 1988. Because of its definite curative effect, it is widely used to fight various infections caused by sensitive fungi. In the early 1990s, the drug had become a...

AI Technical Summary

Problems solved by technology

Although the yields of these two steps are relatively high, the strong alkaline environment used in the first step is extremely destructive to β-lactam antibiotics, which not only affects the yield of the product but also damages the stability of the product. sex

A large amount of organic solvent is consumed in the second crystallization process, and there are two main disadvantages: 1) high production cost, 2) crystallization in the organic phase is not conducive to the removal of impurities and affects the stability of the product