Chemoenzymatic Dynamic Kinetic Asymmetric Transformations of ß-Hydroxyketones.

Herein we report on the development and application of chemoenzymatic Dynamic Kinetic Asymmetric Transformation (DYKAT) of α-substituted ß-hydroxyketones (ß-HKs), using Candida antartica lipase B (CALB) as transesterification catalyst and a ruthenium complex as epimerization catalyst. An operationally simple protocol allows for an efficient preparation of highly enantiomerically enriched α-substituted ß-oxoacetates. The products were obtained in yields up to 95 % with good diastereomeric ratios.