Identification, characterization, synthesis of major metabolites biotransformed from vonoprazan fumarate

A first synthetic research concerning four observed metabolites and their deuterium-labeled analogues of reflux esophagitis drug vonoprazan fumarate is reported. Among which the synthetic methods of three metabolites M-I, M-III, M-IV-Sul, and four stable isotop labeled analogues M-I-d(4), M-II-d(4), M-III-d(4), M-IV-Sul-d(4) have not yet been reported before. The structures of these compounds were elucidated on the basis of MS and NMR spectroscopy. (C) 2022 Elsevier Ltd. All rights reserved.