Direct construction of biaryl-bridged 8–11 membered N-heterocycles via gold(i)-catalyzed intramolecular [4 + 2] benzannulation of N-tethered diynyl benzaldehydes

Abstract

An efficient method for the expeditious synthesis of architecturally challenging biaryl-bridged 8–11 membered N-heterocycles that relies on gold(I)-catalyzed intramolecular [4 + 2] benzannulation of N-tethered diynyl benzaldehydes is described. A diverse array of biaryl-bridged 8–11 membered N-heterocycles that are otherwise difficult to prepare by conventional methods could be readily accessed under mild reaction conditions. This transformation features high functional group tolerance and a broad substrate scope.