One-pot synthesis of 4-(imidazol-1-yl)indole derivatives through a sequential dearomatization and Ag-catalyzed cyclization/Cs 2 CO 3 -mediated addition/aromatization reaction.

A convenient one-pot assembly of 4-(imidazol-1-yl)indole derivatives from easily accessible o -alkynylanilines and imidazoles has been developed. The sequential dearomatization and Ag(I)-catalyzed cyclization/Cs 2 CO 3 -mediated conjugate addition/aromatization cascade reactions exhibit high efficiency and excellent selectivity. The combined use of a silver(I) salt and cesium carbonate is significant for facilitating this domino transformation. The 4-(imidazol-1-yl)indole products could be easily converted to the corresponding derivatives and might be valuable in biological chemistry and medicinal science.