Rhodium-catalyzed 2-arylquinazolinone C-H Activation

Quinazolinones are important fused heterocyclic scaffolds because of their broad spectrum of medicinal and pharmacological properties.They have extensive application prospects in medicine,pesticides and other fields.Therefore,the synthesis of quinazolinones compounds has been a hot topic in the field of organic synthesis workers.Recently,nitrogen-containing heterocycles as the directing groups play a crucial role in transition-metal-catalyzed C-H bond functionalization reactions,which has been widely used in the field of organic synthesis,because it can be directly,efficiently,and selectively achieve aromatic compounds C_sp2-H functionalization.The quinazolinone skeleton is a nitrogen-containing directing group that enables functionalization at the 2-position aryl group.Therefore,we use transition metal catalyzed C-H activation to achieve the derivatization of 2-aryl quinazolinone.Based on the above two directions,we have carried on the following two aspects of the research:1)we have developed a Rh^?-catalyzed C–H activation/amination of ortho2-arylquinazolin-4?3H?-ones using N-alkyl-O-benzoyl-hydroxylamines as aminating agents.The reaction proceeded under mild reaction conditions and possess high functional group tolerance.2)we have developed a Rh^?-catalyzed oxidative coupling cyclization of2-arylquinazolin-4?3H?-ones and two mole of alkynes via a tandem oxidative C-H functionalization-annulation and amide alcoholysis synthesize a series of polycyclic fused heterocyclic compounds.