Desymmetrization‐like Catalytic Enantioselective Fluorination of Malonates and Its Application to Pharmaceutically Attractive Molecules

Abstract

At the leading edge: Chiral fluoromalonates can be prepared with very high stereocontrol by enantioselective fluorination of racemic malonates and using a Zn(OAc)2/DBFOXPh catalyst (see scheme), thus providing an efficient alternative route to conventional microbial desymmetrization for the preparation of fluorinated chiral building blocks. Several pharmaceutically attractive compounds were prepared by using this method.