Copper-mediated C-H(sp²)/C-H(sp³) coupling of benzoic acid derivatives with ethyl cyanoacetate: an expedient route to an isoquinolinone scaffold.

A facile, copper-mediated, direct C-H(sp(2))/C-H(sp(3)) bond coupling of benzoic acid derivatives with ethyl cyanoacetate by the deployment of an 8-aminoquinoline moiety as a bidentate directing group is disclosed. Such a unique transformation provides a new strategy for the construction of an isoquinolinone scaffold as one of the privileged cores.