The efficient copper-mediated oxidative C–H alkynylaiton of benzhydrazides was accomplished with terminal alkynes. Thus, a hetero-aromatic removable N-2-pyridylhydrazide allowed for domino C–H/N–H functionalization. The approach featured remarkable functional group compatibility and ample substrates scope. Thereby, highly functionalized aromatic and hetero-aromatic isoindolin-1-ones were accessed with high efficacy with rate-limiting C–H cleavage.
Keywords: copper; benzhydrazides; 3-methyleneisoindolin-1-one; removable directing group
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Xiong, F.; Li, B.; Yang, C.; Zou, L.; Ma, W.; Gu, L.; Mei, R.; Ackermann, L. Beilstein Arch. 2021, 202139. doi:10.3762/bxiv.2021.39.v1
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