Site‐Selective C–H Amidation of 2‐Aryl Quinazolinones Using Nitrene Surrogates

The site‐selective modifications of quinazolinones constitute a pivotal topic in drug discovery and material science. Herein, we describe the rhodium(III)‐catalyzed C–H amidation of 2‐aryl quinazolin‐4(3 H )‐ones with a range of nitrene surrogates including dioxazolones, organic azides, and N ‐methoxyamides. Complete site‐selectivity and functional group tolerance are observed. Notably, the large‐scale reaction and late‐stage functionalization highlight the synthetic potential of the developed protocol. Combined mechanistic investigations elucidate a plausible reaction mechanism of this process.