Studies On Iridium-catalyzed C?n Bond Formation Via C-h Bond Activation

Quinazolinone is ubiquitous framework in drugs and natural products because of their various biological activities.As a result,the construction and modification of quinazolinones have been attractive for the organic chemists.Meanwhile,the field of transition-metal-catalyzed C-H bond activation has become one of the most attractive areas in both organometallic chemistry and organic synthetic chemistry.The direct functionalizations of non-activated C-H bond represent an efficient method to maximize atom-economy and simplify chemical synthesis steps.Recently,our group has developed a series of transition-metal-catalyzed construction and modification of quinazolinones.However,we found it was not easy to regioselectivity obtain mono-substituted products in the metal-catalyzed C-H avtivation reactions for the arylation,alkenylation,allylation or sulfamidation of quinazolinones.In this thesis,we have developed an Ir-catalyzed direct mono-amidation of 2-arylquinazolinones via C-H bond activation with quinazolinone acting as a directing group.Compared to our previous work,mono-sulfamidated products were selectively obtained with high yields by changing the ratio of substrates,the loading of catalyst,acid additive and reaction time.