抗生素替加环素合成研究  

Synthesis of tigecycline

作　　者：刘文杰[1] 宗在伟[1] 杨建楠[1] 胡振[1] 胡文波[1] 

机构地区：[1]江苏奥赛康药业股份有限公司,南京211112

出　　处：《中国抗生素杂志》2011年第10期762-764,共3页Chinese Journal of Antibiotics

摘　　要：目的优化替加环素合成工艺,制备合格替加环素产品。方法以9-氨基米诺环素硫酸盐为原料,与氯乙酸酐反应得中间体9-氯乙酰氨基米诺环素,再与叔丁胺反应生成替加环素。结果合成的目标化合物经核磁共振氢谱、质谱、红外确认结构。Objective To optimize the synthesis processof tigecycline, and prepare qualified products. Method A two-step procedure for synthesis of tigecycline was developed. In the first step, the starting material 9-amino-minocycline sulfate was converted to the intermediate 9-chloroacetylamino-minocycline by treatment with chloroacetic acid anhydride. And then, tigecycline was preparated by the reaction of the intermediate with tert- butylamine. Result The structure of the target compound was characterized by 1H-NMR, MS and IR. Conclusion The technology improce the yield oftigecycline

关 键 词：抗生素 合成 替加环素 

分 类 号：R978.1[医药卫生—药品]