Stereoselective\nSynthesis of Maralixibat via VO(acac)<sub>2</sub>/Schiff Base-Catalyzed\nAsymmetric Oxidation of Its Sulfide\nIntermediate

The stereoselective synthesis of maralixibat was achieved\nby harnessing\nthe chiral transferring effect of the stereogenic <i>R</i>-sulfoxide functionality, which was obtained via the VO(acac)<sub>2</sub>/Schiff base-catalyzed asymmetric oxidation of a phenylthiophenol\nprochiral intermediate. The <i>R</i>-sulfoxide intermediate\nunderwent a ring closure reaction to form the seven-membered ring\ncore structure with the desired stereochemistry, ultimately ensuring\nthe drug’s exceptional isomeric purity and synthetic efficiency.