头孢吡肟中间体合成条件考察  

THE INVESTIGATION OF THE SYNTHESIS OF THE KEY INTERMEDIATE OF CEFEPIME DIHYDROCHLORIDE

作　　者：包立道[1] 多丽霞 秦荣[3] 

机构地区：[1]内蒙古医学院药学系,内蒙古呼和浩特010059 [2]嘉事堂药业北京医药生物新技术分公司 [3]内蒙古医学院第一附属医院

出　　处：《内蒙古医学院学报》2004年第2期105-107,共3页Acta Academiae Medicinae Neimongol

摘　　要：目的 :在现有的实验室条件下以 7-ACA为原料合成头孢吡肟中间体 ,并在一定程度上提高收率。方法 :与国外文献报道的相关方法具有一致性 ,同时 ,采用正交实验设计方法考察了一些关键步骤 (时间、温度、剂量 )对中间体收率的影响。结果 :中间体收率为 3 2 .7%。结论 :该方法使中间体的合成更易于控制 ,避免了一些繁杂的操作 。Objective: In current laboratorial condition, using 7-ACA to synthesize 7-amino-3-[(1-methyl-1-pyrrolidine)methyl]-3-cephem-4-carboxylic acid hydrochloride which is the key intermediate of the synthesis of cefepime dihydrochloride, and increase the yield. Methods: This method is consistent with the methods which have been reported on foreign literature, and this orthogonal experimental design has investigated some key step (time, temperature, dosage). Results: The average yield was 32.7%. Conclusion: The new method has advantages such as convenient operation and high yield, avoids some miscellaneous operations, found the best way to synthesize the intermediate.

关 键 词：头孢吡肟 中间体 正交设计 三甲基碘硅烷 

分 类 号：R914[医药卫生—药物化学] R978.11[医药卫生—药学]