This review focuses on the progress in catalytic asymmetric difluoroalkylation to construction of difluoroalkylated stereogenic centers. Synthetic methods, active intermediates involved and asymmetric strategies applied were summarized.
A visible-light-mediated selective difluoroalkylation of α-trifluoromethyl alkenes with difluoroalkylating reagents was developed. This protocol allowed the formation of gem-difluoroalkene difluoroacetates and trifluoromethylated difluoroacetamides.
Light-promoted direct aromatic C–H difluroalkylation of aniline derivatives with bromodifluoro esters and amides has been disclosed. This reaction operates under catalyst-free conditions and features a broad substrate scope.
The selective installation of fluorine-containing groups adjacent to sterically hindered alkyl groups has been utilized for the synthesis and derivatization of biologically active molecules.
An approach to the synthesis of difluoroalkylated quinolino[2,1-b]quinazolinones has been developed using unactivated alkynes containing quinazolinones and ethyl iododifluoroacetate or iododifluoramides under visible light irradiation.