头孢唑肟钠的合成研究  

Synthesis process of ceftizoxime sodium

作　　者：朱佳[1] 蒋忠良[1] 

机构地区：[1]同济大学化学系,上海200092

出　　处：《精细与专用化学品》2010年第10期21-23,共3页Fine and Specialty Chemicals

摘　　要：以乙酰乙酸乙酯为起始原料,经亚硝化、溴化、甲基化、环合一锅反应后,水解得到氨噻肟酸,其与N-羟基邻苯二甲酰亚胺反应得到新型邻苯二甲酰亚胺氨噻肟活性酯,然后与7-氨基-3-去乙酰氧基头孢酸（7-ADCA）经酰化、成盐等反应得到所要合成的药物头孢唑肟钠。此合成工艺有效可行,总收率为58%,其结构用IR、~1HNMR和MS进行了表征。该工艺操作简便,步骤简洁,具有良好的应用前景。The synthesis of ceftizoxime sodium was introduced in this paper.Cefotaxime ammonia acid was first prepared from the ethyl acetoacetate to carry out nitrozation,bromination,methylation,cyclization-pot reaction, and hydrolysis.Then a new active ester which is called phthalimide ammonia cefotaxime was composed by the reaction with N-hydroxyphthalimide,and the ceftizoxime sodium was obtained by the new active ester and 7- ADCA.The process was feasible and effective,and the yield was 58%,the structure was characterized by IR, ~1HNMR and MS.The synthetic process can be carried out in simple manufacturing facilities and no complicated procedure compared with the known methods.So the experiment provides an economical manufacturing process for preparing the ceftizoxime sodium.

关 键 词：头孢唑肟钠 抗生素 氨噻肟酸 活性酯 N-羟基邻苯二甲酰亚胺 

分 类 号：TQ463.6[化学工程—制药化工]