盐酸头孢他美酯的合成

Synthesis of Cefetamet pivoxil hydrochloride

盐酸头孢他美酯是一口服前体药,口服后在体内迅速水解为具有抗菌活性的头孢他美。本文报道了盐酸头孢他美酯的制备方法,其生产工艺简单,成本低廉:以3-去乙酰氧基-7-氨基头孢烷酸(7-ADCA)为起始物与活性酯反应,先制备头孢他美(酸),然后和特戊酸卤甲酯反应生成头孢他美酯,最后头孢他美酯成盐得盐酸头孢他美酯。

Cefetamet pivoxil hydroehloride belong to the class of orally absorbed prodrug esters which is hydrolyzed to the active parent compound--cefetamet in vivo. This paper describes the preparation of cefetamet pivoxil hydrochloride. Its production process is simple and low cost： 7--amino--3--deacetoxyl--cophalosproanie acid （7--ADCA） used as the starting material, was reacted with the active ester to give cefetamet and then the product cefetamet was esterified with haloalkyacylate. The resulting ester could be converted to its hydrocloride as the final product.