Identification, Synthesis, and Characterization of Novel Baricitinib Impurities.

ABSTRACT: Baricitinib is a novel active pharmaceutical ingredient used in the treatment of rheumatoid arthritis, and it acts as an inhibitor of Janus kinase. During the synthesis of baricitinib, three unknown impurities were identified in several batches between 0.10 and 0.15% using high-performance liquid chromatography. The unknown compounds were isolated and identified as N-((3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-5-oxotetrahydrofuran-3-yl)methyl)ethane sulfonamide (lactone impurity, BCL), 2-(3-(4-(7H-[4,7'-bipyrrolo[2,3-d]pyrimidin]-4'-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile (dimer impurity, BCD), and 2-(1-(ethylsulfonyl)-3-(4-(7-(hydroxymethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyra

SUBMITTER: Vaddamanu G 

PROVIDER: S-EPMC10018714 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature