QbD理念在新型抗菌药磷酸特地唑胺工艺研究中的应用

摘要

Objective Study on the synthesis of the antibacterial drug tedizolid phosphate.Methods Guided by the concept of Quality,by Design (QbD),intermediate A and tetrabenzyl pyrophosphate were employed to synthesize tedizolid phosphate.Results The target product was obtained with 58％ yield and 99.2％ HPLC purity.Conclusion The newly developmented synthetic process with mild reaction conditions avoided the generation of hydrolysis of impurities of hydrolysis and dimer impurities to ensure the quality of tedizolid phosphate.%目的 抗菌药磷酸特地唑胺的工艺研究.方法 QbD理念指导工艺研究,以中间体A和焦磷酸四苄酯为原料合成磷酸特地唑胺.结果 以58％的总收率实现了磷酸特地唑胺的制备,HPLC纯度为99.2％.结论 新开发的工艺反应条件温和,有效地避免了水解杂质、二聚体杂质的产生,保证了磷酸特地唑胺的产品质量.