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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. The approach featured remarkable functional group compatibility and ample substrate scope. Thereby, highly functionalized aromatic and heteroaromatic isoindolin-1-ones were accessed with high efficacy with rate-limiting C-H cleavage.

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