头孢噻肟酸的THF合成工艺探索  

The THF Synthesis Process of Cefotaxime Acid

作　　者：陆宏龙 覃艺群 

机构地区：[1]广西卫生职业技术学院药学系,广西南宁530023

出　　处：《广州化工》2012年第9期104-106,共3页GuangZhou Chemical Industry

摘　　要：头孢噻肟酸是一种重要的药物中间体,主要是以AE-活性酯(苯并噻唑活性酯MEAM)和7-ACA(7-氨基头孢烷酸)为原料合成头孢噻肟酸。目前主要是以二氯甲烷为主要溶媒,该工艺非常成熟,但所用溶媒太多,产品含量不高,使得应用受到一定限制。本工艺使用四氢呋喃(THF)和水为主要溶媒,从降低成本及改善晶形的角度,探索不同溶媒比例对合成产率及晶型的影响.在最佳溶媒比例下,重量收率可达165%以上。Cefotaxime acid was an importantion of mid - drug. The experimental process on synthesis of cefotaxime acid was studied by using 7 - ACA am inoeephalo sporanic acid （7 - ACA） and MEAM as raw material under the catalytic act ion of DMA. At present, it really used CH2CL2 as chief liquid intermediary, and the technology was very mature, however, because using liquid intermediary was too much, the percent of output was lower and the application was restricted to some extend. THF and water were used as liquid to the synthesis of cefotaxime acid. The effects of the amount of catalyst, the ratio of the reactants, the choice of the solvent and the pH of crystalization were investigated. The yield of cefotaxime acid was over 165% under the optimum conditions.

关 键 词：头孢噻肟酸 合成工艺 四氢呋喃(THF) 

分 类 号：O62[理学—有机化学]