Abstract

Herein, we describe a novel O2N˙-triggered ordered addition 7-endo cyclization reaction with excellent chemo- and regioselectivity. With such a strategy, structurally diverse nitro-benzo[b]azepines were prepared with 28 examples. Large-scale operation and handy N-Ts and N-Cbz deprotection reveal the promising utility of this methodology. Mechanistic studies suggest that the reaction proceeds through a radical pathway.

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