高质量头孢地尼晶体的制备方法  

The preparation of high quality cefdinir crystal

作　　者：付德才[1] 石少龙[1] 谷明明[1] 郑美玲[1] 刘倩[1] 

机构地区：[1]河北科技大学化学与制药工程学院,河北石家庄050018

出　　处：《中国药物化学杂志》2014年第4期311-313,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的探索制备高质量头孢地尼的方法,确定制备方法的较佳工艺条件。方法 7-氨基-3-乙烯基头孢烯酸(7-AVCA)与2-(2-氨基-4-噻唑)-2(Z)-三苯甲氧亚氨乙酸活性硫酯(2)缩合后,经甲磺酸中和形成三元复合物而分离,再经磷酸水解脱除保护基析出头孢地尼和磷酸复合物,最后通过精制得到目标化合物头孢地尼。结果与结论该制备方法操作简单,产品质量好,总收率达74.5%。High quality cefdinir crystal was obtained by condensation, hydrolysis and purification as well as optimum reaction conditions were determined. The three element complex was seperated from reaction mix- ture after the condensation of 2-benzothiazolyl-（Z）-2-（2-aminothiazol-4-yl ）-2-tripheny-lmethoxyiminothio- acetate with 7-amino-3-vinyl-3-cephem-4-carboxylic acid （7-AVCA） by adding methylsulfonic acid. Using 85 % phosphoric acid in the presence of acetonitrile to deblock triphenylmethyl group gave the solid salt of cefdinir and phosphoric acid. Cefdinir crystal was obtained by purification of cefdinir and phosphoric acid salt with sodium hydrate solution and then acidation in the total yield 74.5 %. The preparation route had the advertage of high quality product and easy operation.

关 键 词：头孢地尼 7-氨基-3-乙烯基头孢烯酸 三苯甲基活性硫酯 制备 

分 类 号：R914[医药卫生—药物化学]