Crystal Form of Olmutinib

Journal of the Korean Chemical Society

article

Chang Yeob Lee¹  Young Taek Sohn¹ 

[1] College of Pharmacy, Duksung Women’s University

关键词: Olmutinib;    Crystal form;    DSC;    TG;    PXRD;   

DOI  :  10.5012/jkcs.2019.63.1.7

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Olmutinib, N-[3-({2-[4-(4-methylpiperazine-1-yl)aniline]thieno[3,2-d]Pyrimidin-4-yl}oxy)phenyl]prop-2-enamide dihydrochloride monohydrate, OlitaTM is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) that was developed by Boehringer Ingelheim and Hanmi Pharmaceutical Co. Ltd for the treatment of non-small cell lung cancer (NSCLC). The aim of this work was to investigate the existence of polymorphs and pseudopolymorphs of olmutinib. Three crystal forms of olmutinib have been isolated by recrystallization and characterized by differential scanning calorimetry (DSC), thermogravimetric (TG) analysis and powder X-ray diffractometry (PXRD). From the DSC and TG data it was confirmed that Form 1 is monohydrate, Form 2 is dihydrate, Form 3 is 1.5 hydrate. The PXRD patterns of three crystal forms were different respectively. After storage of 1 month at 2 o C, 24% RH (Relative Humidity), Form 1, Form 2, and Form 3 were not transformed.

【 授权许可】

Unknown