Enantioselective Synthesis of Axially Chiral Multifunctionalized Biaryls via Asymmetric Suzuki–Miyaura Coupling

Substituted 2-formylarylboronic acids were successfully employed as substrates for asymmetric Suzuki–Miyaura coupling. By virtue of the coupling with dialkoxyphosphinyl substituted naphthyl bromides and 2-nitronaphthalen-1-yl triflouromethanesulfonate, a series of novel multifunctionalized axially chiral biaryls were prepared in 53–97% yields with up to 97% ee using palladium-Cy-MOP as the catalyst. The methodology provides a highly efficient and practical strategy for the synthesis of novel multifunctionalized axially chiral biaryls.