Transition-metal free C3-amidation of quinoxalin-2(1H)-ones using Selectfluor as a mild oxidant

【作者】 黄广超； 李冰； 袁金伟； 杨亮茹； 肖咏梅； 毛璞； 屈凌波；

【Author】 Guangchao Huang;Bing Li;Jinwei Yuan;Liangru Yang;Yongmei Xiao;Pu Mao;Lingbo Qu;School of Chemistry and Chemical Engineering, Henan University of Technology;College of Chemistry, Zhengzhou University;

【机构】 河南工业大学,化学化工学院； 郑州大学,化学学院；

【摘要】 Quinoxalin-2（1H）-ones have attracted considerable attention since they are endowed with significant biological activities and outstanding chemical properties.They have been extensively investigated in organic synthesis,materials chemistry and pharmaceuticals.¹ Due to their importance,the functionalization of quinoxalin-2（1H）-ones has become an attractive research topic.Recently,many quinoxalin-2（1H）-one derivatives with different substituents on their C-3position have achieved via the direct C-H bond functionalization,including the arylation,phosphonation,etc.^2,3 Herein,we reported a practical and efficient transition-metal-free approach for the direct amidation of quinoxalin-2（1H）-ones with amidates using Selectfluor reagent as a mild oxidant （Scheme 1）.This protocol features mild reaction conditions,broad substrate scope,good yields,and could serve as an efficient approach for the functionalization of quinoxalin-2（1H）-ones.更多还原

【Abstract】 Quinoxalin-2（1H）-ones have attracted considerable attention since they are endowed with significant biological activities and outstanding chemical properties.They have been extensively investigated in organic synthesis,materials chemistry and pharmaceuticals.¹ Due to their importance,the functionalization of quinoxalin-2（1H）-ones has become an attractive research topic.Recently,many quinoxalin-2（1H）-one derivatives with different substituents on their C-3position have achieved via the direct C-H bond functionalization,including the arylation,phosphonation,etc.^2,3 Herein,we reported a practical and efficient transition-metal-free approach for the direct amidation of quinoxalin-2（1H）-ones with amidates using Selectfluor reagent as a mild oxidant （Scheme 1）.This protocol features mild reaction conditions,broad substrate scope,good yields,and could serve as an efficient approach for the functionalization of quinoxalin-2（1H）-ones.更多还原