Photocatalytic Transition-Metal-Free Direct 3-Acetalation of Quinoxaline-2(1H)-ones  

作　　者：Chunhua Ma Hui Meng Jing Li Xianguang Yang Yuqin Jiang Bing Yu 

机构地区：[1]Collaborative Innovation Centre of Henan Provincefor Green Manufacturing of Fine Chemicals,Key Laboratory of Green Chemical Media and Reactions,Ministry of Education,Henan Engineering Research Centre of Chiral Hydroxyl Pharmaceutical,Henan Engineering Laboratoryof Chemical Pharmaceutical and Biomedical Materials,School of Chemistry and Chemical Engineering,HenanNormal University,Xinxiang,Henan453007,China [2]Green Catalysis Centre,College of Chemistry,Zhengzhou University,Zhengzhou,Henan 45001,China

出　　处：《Chinese Journal of Chemistry》2022年第22期2655-2662,共8页中国化学（英文版）

基　　金：financial support from the National Natural Science Foundation of China(Nos.82003585,21971224);the Technical innovation Team of Henan Normal University(No.2022TD03);the Postgraduate Education Reform Project of Henan Province(Nos.2019SJGLX008Y,2019SJGLX034Y);the PostgraduateEducation Reformand QualityImprovement Project of Henan Province(No.YJS2021AL079);the Scienceand Technology Research Project(No.222102310244).

摘　　要：A general transition-metal-free visible-light-promoted 3-acetalation reaction of quinoxaline-2(1H)-ones was developed under mild conditions.By employing 1,2,3,5-tetrakis(carbazol-9-yl)-4,6-dicyanobenzene(4CzIPN)as an inexpensive photocatalyst,and glyoxylic acid acetal as a radical source,various acetalated quinoxaline-2(1H)-ones were constructed in moderate to good yields.Moreover,the versatility of this protocol is highlighted by the successful application in the late-stage modification of drug molecules and the various functionality transformations.The excellent antitumor activity of the acetalated product demonstrated that this streamlined and sustainable approach could have emerged as a powerful strategy for structural modification in medicinal chemistry.

关 键 词：Photocatalysis Transition-metal-free Synthetic methods Radical reactions Antitumor activity 

分 类 号：O62[理学—有机化学]