Abstract

A noval method for the synthesis of optically active β-hydroxy sulfones was developed. Through a substitution/dynamic kinetic resolution–asymmetric transfer hydrogenation, the presented method was based on one-pot enantioselective organic transformations of α–bromoindenones and sodium arylsulfinate. The protocol employed RuCl2[(S,S)–TsDPEN](mesitylene) as a catalyst, and sodium formate as a hydrogen source, affording various optically pure vicinal stereocenters β-hydroxy sulfones in high yields with excellent enantioselectivities (up to 99%) and diastereomeric ratios (up to 99:1) under mild reaction conditions.

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