Copper-mediated oxidative C−H/N−H activations with alkynes by removable hydrazides

The efficient copper-mediated oxidative C–H alkynylation of benzhydrazides was accomplished with terminal alkynes. Thus, a heteroaromatic removable N -2-pyridylhydrazide allowed for domino C–H/N–H functionalization. approach featured remarkable functional group compatibility and ample substrate scope. Thereby, highly functionalized aromatic isoindolin-1-ones were accessed high efficacy rate-limiting cleavage.