Lewis Acid Catalyzed Asymmetric α-Hydroxylation of Racemic Malonates

Significance

Chiral α-hydroxy malonates are an important class of building blocks for the synthesis of drug targets. However, the catalytic, asymmetric α-hydroxylation of malonates has been a challenge. The authors report the first Lewis acid catalyzed asymmetric α-hydroxylation of racemic malonates and demonstrate the potential of this methodology in the synthesis of biologically active molecules.