马来酸阿法替尼原料药降解杂质的制备与结构推测

Degradation Impurity of Afatinib Maleate:The Preparation and Structural Characterization

在马来酸阿法替尼原料药稳定性实验的基础上,对其降解杂质进行了制备,所得样品在相同高效液相色谱条件下与降解杂质的保留时间一致。结合样品的ESI-MS、NMR图谱推测,该降解杂质为阿法替尼的水解、分子内环合产物。提供了马来酸阿法替尼原料药杂质研究的对照品,且为其质量控制和贮存条件的设立提供了依据。

This article describes the preparation of the degradation impurity of afatinib maleate on the basis of the investigation on its stability.In respect of the retention time at the identical high performance liquid chromatography(HPLC)condition,the afforded product was consistent with the degradation impurity.In accordance with its ESI-MS and NMR spectra,the impurity was envisioned as a hydrolytic cyclization product.Taken together,this research not only culminated in a reference substance for the impurity study of afatinib maleate,but also directed its quality control and storage.