【作者】 陈林； 李江红； 任凤英； 石克金； 杨晨； 颜军； 苟小军；

【Author】 Chenlin;Lijianghong;Renfengying;Shikejin;Yangchen;Yanjun;Gouxiaojun;Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province,Sichuan Industrial Institute of Antibiotics,Chengdu university;

【机构】 抗生素研究与再评价四川省重点实验室四川抗菌素工业研究所成都大学；

【摘要】 目的合成头孢妥仑酯关键中间体7-ATCA。方祛GCLE与4-甲基-5-甲酰基噻唑发生Wittig反应得到DPTC,之后,苯酚脱除2-位羧基保护基对-甲氧基苄基,再用青霉素G酰化酶脱除7-位苯乙酰基,得到目标产物。结果收率30%,Z-式含量93%,该中间体不必进一步纯化可直接用于头孢妥仑酯的制备。结论本工艺简单易行,为生产提供了依据。更多还原

【Abstract】 Objective:To prepare 7-ATCA,the key intermediate of cefditoren pivoxil.Methods:GCLE reacted with 5-formyl-4-methylthiazole via Wittig reaction to give DPTC,followed by cleavage of p-methoxy benzyl of 2-position protective group with phenol and7-position phenyl acetyl with Penicillin G acylase Finally,the product,7-ATCA,was obtained.Result:The overall yield was 30%include of 93%Z-isomer.Conclusion:This process was prone to operate while it provided a basis for pilot scale production.更多还原