One-pot Stereoselective Synthesis of trans-2,3-Diaminoindolines through Differentiated 2,3-Diamination of Electrophilic Indolines

Despite recent advances in the synthesis of 2,3-diaminoindole derivatives, construction of 2,3-diaminoindolines, which have differentiated diamine moieties, has yet to be achieved. In this work, we introduce a concise one-pot protocol for differentiated diamination between a dual electrophilic indole reagent and amines to access a variety of past inaccessible 2,3-diaminoindolines. Furthermore, the synthetic utility of this protocol could be demonstrated by a gram-scale reaction and further transformation of obtained 2,3-diaminoindolines.