Remote Construction of N‐Heterocycles via 1,4‐Palladium Shift‐Mediated Double C–H Activation

In the past years, Pd0-catalyzed C(sp3)−H activation provided efficient and step-economical methods to synthesize carbo- heterocycles via direct C(sp2)−C(sp3) bond formation. We report herein that a 1,4-Pd shift allows access N-heterocycles which are difficult build reaction. It is shown o-bromo-N-methylanilines undergo at N-methyl group, followed by intramolecular trapping C(sp2)−H or another nitrogen substituent remote C−C formation generate biologically relevant isoindolines β-lactams. The product selectivity influenced employed ligand, with NHCs favoring of coupling against products arising from N-demethylation.