Pd-catalyzed efficient synthesis of 3-formylindole derivatives with diaziridinone

Abstract

This work describes an efficient Pd-catalyzed annulation process of acetal alkynes, aryl iodides, and di-t-butyldiaziridinone to afford a variety of 3-formylindoles and their derivatives. The reaction likely proceeds through a regioselective Heck reaction followed by aryl C–H activation to form a pallada(II)cycle, which is bisaminated with diaziridinone via a pallada(IV)cycle. The utility of the current reaction process is demonstrated by the facile synthesis of bioactive indoles.