Pd-Catalyzed Regioselective Mono-Arylation: Quinazolinone as the Inherent Directing Group for C(sp<sup>2</sup>)–H Activation

Abstract

The Pd-catalyzed quinazolinone-directed regioselective monoarylation of aromatic rings by C–H bond activation is developed. A broad substrate scope is demonstrated for both quinazolinone as well as diaryliodonium triflates. The use of a base was found to be crucial for this transformation, unlike for the known nitrogen-directed arylations. All of the novel quinazolinones of biological interest were synthesized by using the operationally simple Pd­(II)-catalyzed arylation reaction

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