依折麦布环醚杂质的制备及其晶体结构表征

Preparation and Crystal Structures of Cyclizate Ether Impurity of Ezetimibe

药物杂质与药品的安全性和稳定性密切相关,对药物杂质进行充分研究是药品质量控制的必要过程。依折麦布、尿素在无水乙醇和无水甲醇溶剂中,室温存放可顺利获得依折麦布环醚杂质晶体,该环醚杂质结构经单晶衍射表征。结果显示,晶胞参数a=6.140 7(4),b=7.660 3(5),c=11.145 5(7),α=72.497(5)°,β=99.535(2)°,γ=85.538(5)。属于三斜晶系,P1空间群。

Drug impurities are closely related to the safety assessment and stability of drugs. A comprehensive study of impurities is critical process for the drug quality control. Cyclizate ether impurity crystal of Ezetimibe was prepared by put Ezetimibe and urea in anhydrous ethanol and anhydrous methanol solvent under room temperature. The crystal structure of cyclizate ether impurity was confirmed by X-ray single crystal diffractometer. The results present that the cell parameters a = 6. 140 7（ 4）,b = 7. 660 3（ 5）,c = 11. 145 5（ 7）,α = 72. 497（ 5） °,β = 99. 535（ 2） °,γ = 85. 538（ 5） °,and belongs to triclinic,space group P1.