从异丁司特中间体中分离和鉴定一种杂质。
Separation and identification of an impurity from the istradefylline intermediate.
作者信息
Xu Haojie, Wang Yiyun, Wang Hongyi, Zheng Zhonghui, Meng Zihui, Xue Min, Xu Zhibin
机构信息
School of Chemistry and Chemical Engineering, Beijing Institute of Technology 102488 Beijing China
Shandong Xinhua Pharmaceutical Co., Ltd. No.1 Lutai Avenue 255086 Zibo Shandong China.
出版信息
RSC Adv. 2020 Apr 8;10(25):14493-14499. doi: 10.1039/c9ra09074f.
Istradefylline is a selective adenosine antagonist for the A receptor, and it is used to treat the Parkinson's disease and improve dyskinesia in the early stage of the Parkinson's disease. An impurity in the istradefylline intermediate A (6-amino-1,3-diethyl-2,4-(1,3)-pyrimidinedione) was identified by high performance liquid chromatography (HPLC); it was separated by preparative HPLC and further characterized by UV, IR, MS, NMR, 2D NMR and single-crystal XRD analyses. The impurity was identified as ()--ethyl-2-cyano-3-ethylamino-2-butenamide, which originated from the synthetic process of the intermediate A. The structure of this impurity might affect the efficiency and safety of istradefylline; therefore, the research and control of this impurity are necessary for ensuring the quality of istradefylline.
异他必利是一种选择性A受体腺苷拮抗剂，用于治疗帕金森病并改善帕金森病早期的运动障碍。通过高效液相色谱（HPLC）鉴定了异他必利中间体A（6-氨基-1,3-二乙基-2,4-(1,3)-嘧啶二酮）中的一种杂质；通过制备型HPLC将其分离，并通过紫外、红外、质谱、核磁共振、二维核磁共振和单晶X射线衍射分析进一步表征。该杂质被鉴定为( )-乙基-2-氰基-3-乙基氨基-2-丁烯酰胺，它源自中间体A的合成过程。这种杂质的结构可能会影响异他必利的有效性和安全性；因此，对该杂质进行研究和控制对于确保异他必利的质量是必要的。
Zotero 插件