Construction of 1,4-benzodiazepine skeleton from 2-(arylamino)benzamides through PhI(OAc)2-mediated oxidative C–N bond formation.

New compounds involving the biologically important 1,4-benzodiazepine skeleton were conveniently constructed from 2-(arylamino)benzamides through Phl(OAc)(2)-mediated oxidative C-N bond formation. The attractive features of this new synthetic strategy include mild reaction conditions, the heavy-metal-free characteristic of the oxidative coupling process, and the flexibility to tolerate a broad scope of substrates.