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Identification and Synthesis of Impurities During a Novel Process Development of Rivaroxaban
Author(s) -
Yu Jun,
Qiu PengCheng,
Ke Bin,
Chen Hui,
Zhao ChuanMeng,
Zhang FuLi
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3355
Subject(s) - chemistry , rivaroxaban , impurity , resolution (logic) , combinatorial chemistry , stereochemistry , organic chemistry , medicine , computer science , warfarin , atrial fibrillation , artificial intelligence
During the development of rivaroxaban, seven process‐related impurities have been identified and synthesized. These structures are confirmed by nuclear magnetic resonance spectroscopy and high‐resolution mass spectrometry. The impurities ( S )‐2‐(2‐((4‐(5‐(aminomethyl)‐2‐oxooxazolidin‐3‐yl)phenyl)amino)ethoxy)acetohydrazide ( A ) and ( S )‐4‐(4‐(((2‐oxooxazolidin‐5‐yl)methyl)amino)phenyl)morpholin‐3‐one ( F ) are confirmed and distinguished from their isomers by single‐crystal diffraction. This work proves to be valuable in regard to complying with regulatory norms and assessing the quality of rivaroxaban.