A general approach to N-heterocyclic scaffolds using domino Heck-aza-Michael reactions

摘要

Palladium-catalyzed domino Heck-aza-Michael reactions for the synthesis of a series of Cl-substituted tetrahydro-P-carbolines, tetrahydroisoquinolines and isoindolines are described. The domino process involves the initial intermolecular Heck reaction of an aryl bromide with an electron deficient alkene, followed by an intramolecular aza-Michael reaction to form the new 7V-heterocycle in high yield.