Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
During the synthetic process development studies of Ezetimibe, an impurity was detected in the final product at levels ranging from 0.05% to 0.15% in reverse phase gradient high performance liquid chromatography (HPLC) method and its molecular weight is determined by LC–MS analysis. The impurity is Desfluoro-ezetimibe[1].
References:
[1]. Bellur Atici E, et al. Identification, synthesis and characterization of process related desfluoro impurity of ezetimibe and HPLC method validations. J Pharm Anal. 2015 Dec;5(6):356-370.
[2]. Lee DH, et al. Ezetimibe, an NPC1L1 inhibitor, is a potent Nrf2 activator that protects mice from diet-induced nonalcoholic steatohepatitis. Free Radic Biol Med. 2016 Sep 12;99:520-532.