A Dynamic Kinetic Asymmetric Transformation in the α‐Hydroxylation of Racemic Malonates and Its Application to Biologically Active Molecules

Sly like a “DBFOX”: The chiral α-hydroxy malonate 2 can be prepared in high yield and with up to 98 % ee from racemic malonate 1 through α-hydroxylation using oxaziridine 3 and is catalyzed by the (R,R)-DBFOX-Ph/NiII complex (see scheme). Biologically useful molecules have been prepared by using this method and illustrate its efficiency.