Pd-Catalyzed Ring-Closing/Ring-Opening Cross Coupling Reactions: Enantioselective Diarylation Of Unactivated Olefins

Pd-catalyzed chemo-, regio-, and enantioselective ring-closing/ring-opening cross coupling reaction has been developed with diverse aryl halide-tethered alkenes and benzocyclobutenols as substrates, which renders the highly enantioselective diarylation of unactivated alkenes and provides a convenient method toward chiral 2,3-dihydrobenzofurans bearing a quaternary stereocenter with excellent enantioselectivities (up to 98% ee). The application in concise synthesis of the analogue of cannabinoid receptor 2 agonists is described.