A Simple and Efficient Enantioselective Synthesis of (S)-Esmolol

The stereoselective synthesis of (S)-methyl-2-[4-(2-hydroxy-2-(isopropyl amino)-ethoxy]-phenylacetate has been carried out in six steps with an overall yield of 65.6%. The key intermediate is chiral epoxide (7), which was achieved by applying Sharpless asymmetric dihydroxylation method with high enantiomeric purity and in excellent yields.