Modular synthesis of unsymmetrical indolyl diketones from ynediones 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 -aryl enaminones followed by iodine-mediated C-H functionalization.