| Quinoxaline and benzimidazole are both privileged structural motifs distributed in many biological and pharmaceutical compounds.Moreover,their derivatives also have extensive applications in material science and fluorescent probes.Therefore,the synthesis of quinoxalines and benzimidazoles has drawn considerable attention from the synthetic chemists,with numerous synthetic methods developed.Nevertheless,among the existing methods few synthetic pathways provided access to benzo[4,5]imidazole[1,2-α]-quinoxalines,which contain both quinoxaline and benzimidazole skeletons.Therefore,development of synthetic approaches toward to benzo[4,5]imidazole[1,2-α]-quinoxaline compounds is of great important for both medicinal and material chemistry.In this dissertation,we established an I2-promoted sp3 C-H amination reaction for the construction of benzo[4,5]imidazo[1,2-α]-quinoxaline frameworks from2-（2-methyl-1H-benzo[d]imidazol-1-yl）anilineprecursors.Twenty-four benzo[4,5]imidazo[1,2-α]-quinoxaline products were synthesized from readily accessible substrates under the optimal reaction conditions.The features of this synthetic method include direct sp3 C-H amination,no use of transition metals,simple operation,high yields,and gram-scale synthesis. |
