Rh(iii)-catalyzed cascade annulation reaction of N,N-dimethyl enaminones with iodonium ylides to give substituted isocoumarins

Abstract

The assembly of isocoumarins starting from easily available N,N-dimethyl enaminones and iodonium ylides via a Rh(III)-catalyzed C–H bond activation/annulation cascade reaction is herein described. This protocol proceeds under mild conditions and provides access to a wide variety of isocoumarin derivatives in good to excellent yields with good functional group compatibility. Furthermore, the gram-scale synthesis and various further chemical transformations enhance its synthetic utility.