A Biocatalytic Route to Highly Enantioenriched β-Hydroxydioxinones

A novel biocatalytic system to access a wide variety of beta-hydroxydioxinones from beta-ketodioxinones employing commercial engineered ketoreductases has been developed. This practical system provides a remarkably straightforward solution to limitations in accessing certain chemical scaffolds common in beta-hydroxydioxinones that are of great interest due to their diversification capabilities. A few highlights of this system are that it is high yielding, highly enantioselective, and chromatography-free. We have demonstrated both a wide substrate scope and a high degree of scalability