Lu, Jianwu; Shi, Yinfei; Li, Xiao; Liang, Xiaomin; Wang, Yinquan; Yuan, Shun; Wu, Taizhi published the artcile< Understanding and Controlling the Formation of an N-Alkyl Impurity in Olmesartan Medoxomil: A Derivative via Michael-Type Addition between Tetrazole and Mesityl Oxide In Situ Generated from Acetone>, COA of Formula: C19H16O, the main research area is olmesartan medoxomil API impurity quality by design definitive screening.
An unknown impurity was detected in olmesartan medoxomil active pharmaceutical ingredient (API), which was determined as 2-methyl-4-oxopentan-2-yl-protected olmesartan medoxomil by NMR and mass spectrometry (MS). The formation mechanism of this impurity was investigated. In summary, the tetrazole of the final product was condensed with the potential genotoxic compound mesityl oxide generated from acetone self-condensation in acidic conditions to form the N-Alkyl impurity. Further quality control of the reaction was investigated using statistical methods (design of experiment, DoE) via a definitive screening design. The key factors of the reaction were determined to control the process parameters. Three batches of validation experiments showed that the generation of the N-Alkyl impurity was suppressed (<0.1%) and the residual mesityl oxide was not detected (<2.5 ppm). Organic Process Research & Development published new progress about Antihypertensives. 76-84-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C19H16O, COA of Formula: C19H16O.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts