Cu/Pd-Catalyzed cis-Borylfluoroallylation of Alkynes for the Synthesis of Boryl-Substituted Monofluoroalkenes.

ABSTRACT

Monofluoroalkenes normally act as metabolically stable bioisosteres for amide groups (-NH-CO-) and have widespread applications in drug discovery. Additionally, they are widely used as building blocks in organic synthesis. In this study, the Cu/Pd-catalyzed cis-borylfluoroallylation of alkynes was achieved, providing a modular and general tactic for the preparation of monofluorinated alkene scaffolds with high regioselectivity and stereoselectivity. Moreover, an array of synthetic building blocks can be generated by downstream transformations.