Rhodium‐Catalyzed Regioselective Direct C–H Amidation of 2,4‐Diarylquinazoline with Sulfonyl Azides: An Example of Steric Hindrance Regulated Mono‐ and Diamidation Selectivity

Abstract An unprecedented steric hindrance controlled regioselective rhodium‐catalyzed direct C–H amidation of 2,4‐diarylquinazoline was described. Sulfonyl azides were used as the amine source to provide a variety of amide‐functionalized 2,4‐diarylquinazolines in high efficiency. The reaction proceeded under mild conditions, had good functional group tolerance with a broad scope of substrates, and afforded moderate to good product yields. Excellent monoamidation selectivity was achieved with the assistance of meta substituents.