Site‐Selective Rhodium(III)‐Catalyzed C−H Amination of 7‐Azaindoles with Anthranils: Synthesis and Anticancer Evaluation

The site‐selective C−H amination reaction of 7‐azaindoles with various benzisoxazoles as amination surrogates under cationic rhodium(III) catalysis is described. This transformation efficiently provides a range of ortho ‐aminated N ‐aryl‐7‐azaindoles with excellent site‐selectivity and functional group compatibility. The formed ortho ‐aminated 7‐azaindoles were readily transformed into biologically relevant heterocycles such as azaindoloacridine, azaindoloacridone, and bis‐indole compounds. Moreover, the synthetic derivatives were tested for in vitro anticancer activity against human breast adenocarcinoma cells (MCF‐7), human renal carcinoma cells (786‐O), and human prostate adenocarcinoma cells (DU145). Notably, some synthetic compounds were found to display most potent anticancer activity, compared to that of anticancer doxorubicin as a positive control. magnified image