Cu(II)-catalyzed coupling of aromatic C-H bonds with malonates

Article abstract of DOI:10.1021/acs.orglett.5b00193

A new Cu(II)-catalyzed oxidative coupling of arenes with malonates has been developed using an amide-oxazoline directing group. The reaction proceeds via C(sp²)-H activation and malonate coupling, followed by intramolecular oxidative N-C bond formation. A variety of arenes bearing different substituents are shown to be compatible with this reaction.