Crystal Form of Olmutinib 


Vol. 63,  No. 1, pp. 7-11, Feb.  2019
10.5012/jkcs.2019.63.1.7


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  Abstract

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 oC, 24% RH (Relative Humidity), Form 1, Form 2, and Form 3 were not transformed.

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  Cite this article

[IEEE Style]

C. Y. Lee and Y. T. Sohn, "Crystal Form of Olmutinib," Journal of the Korean Chemical Society, vol. 63, no. 1, pp. 7-11, 2019. DOI: 10.5012/jkcs.2019.63.1.7.

[ACM Style]

Chang Yeob Lee and Young Taek Sohn. 2019. Crystal Form of Olmutinib. Journal of the Korean Chemical Society, 63, 1, (2019), 7-11. DOI: 10.5012/jkcs.2019.63.1.7.

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ISSN(Print) 1017-2548
ISSN(Online) 2234-8530