Direct Hydrodefluorination of CF₃-Alkenes via a Mild S_N2′ Process Using Rongalite as a Masked Proton Reagent

Abstract

A concise and efficient hydrodefluorination process was developed for the synthesis of <i>gem</i>-difluoroalkenes. This reaction employs rongalite as a masked proton source and does not require any additional catalysts or reductants. Notably, trifluoromethyl alkenes having both terminal and internal double bonds are compatible with this process, allowing for a wider range of substrates. The successful late-stage functionalizations of pharmaceuticals and gram-scale syntheses were used to demonstrate the viability of this method.