A one-pot multicomponent tandem reaction for the rapid synthesis of 2-amino-3-benzylindoles

Abstract

The simultaneous introduction of two functional groups into molecules via a one-pot process is of great importance for the synthesis of complex molecules. However, this remains a challenging task due to the need for precise control of regio- and chemo-selectivity. In this paper, we present a novel oxidative cross-dehydrogenation coupling (CDC) reaction that selectively introduces two nucleophiles at the C2,3-positions of indoles, thereby constructing the C–N and C–C bonds simultaneously in one pot. This method offers a streamlined and efficient approach for functionalizing indoles with high selectivity, expanding the synthetic toolbox for the construction of complex organic frameworks.