Modular synthesis of unsymmetrical indolyl diketones from ynediones via sequential aza-Michael addition/C–H functionalization†

Herein, we disclose an efficient approach for the synthesis of unsymmetrical indolyl diketones from easily accessible 1,2-alkynediones involving a sequential aza-Michael addition/C–H Functionalization process. The two-step, one-pot strategy involves the aza-Michael addition of an aniline generating the N-aryl enaminones followed by iodine-mediated C–H functionalization.