高纯度头孢替坦二钠合成工艺研究  

Study on the synthetic technology of high purity cefotetan disodium

作　　者：贾全 田洪年 张立斌 魏宝军 

机构地区：[1]华北制药河北华民药业有限责任公司研发中心,石家庄052165

出　　处：《中国新药杂志》2017年第22期2746-2748,共3页Chinese Journal of New Drugs

摘　　要：目的:研究高纯度头孢替坦二钠制备工艺。方法:以7β-氨基-7a-甲氧基-3-(1-甲基-1H-四唑-5-硫甲基)-8-氧代-5-硫-1-杂氮双环[4.2.0]辛-2-烯-2-甲酸二苯基甲酯(7-MAC)为起始原料,经酰化、水解、脱保护、缩合重排、氧化铝层析、结晶成酸再经溶解、成盐、脱色、无菌过滤、冻干得无菌头孢替坦二钠。结果:头孢替坦二钠纯度达到99.57%,质量水平远远高于JP16标准。结论:该工艺可行性强,摩尔收率达到61%,适用于产业化生产。Objective： To explore the synthetic technology of high purity cefotetan disodium. Methods：Taking（6 R,7 S）-benzhydryl-3-（（1-methyl-1 H-tetrazol-5-ylthio） methyl）-7-amino-7-methoxy-8-oxo-5-thia-1-azabicyclo[4. 2. 0]oct-2-ene-2-carboxylate（7-MAC） as initial raw material,aseptic cefotetan disodium was prepared through acylation,hydrolysis,deprotection,condensation and rearrangement,aluminum oxide chromatography,acid crystallization and dissolution again,salifying,decoloration,aseptic filtration,and lyophilizing. Results： The purity of cefotetan disodium reached 99. 57%,which was far higher than the quality standard regulated by JP16.Conclusion： The established technology is appropriate for the industrial production with high feasibility and molar yield of 61%.

关 键 词：头孢替坦二钠 抗生素 合成工艺 

分 类 号：R914.5[医药卫生—药物化学]