Palladium-catalyzed 1,2-selective intermolecular arylamination of 1,3-dienes

Transition metal-catalyzed transformations of 1,3-dienes have always been an important research topic for chemists, but highly selective intermolecular 1,2-arylamination of 1,3-dienes has not been reported. In this study, we present a method for the palladium-catalyzed 1,2-difunctionalization of conjugated dienes. This approach offers an efficient pathway for the 1,2-selective arylamination of 1,3-dienes, demonstrating remarkable chemo- and regioselectivity, as well as a broad substrate scope and excellent functional group tolerance. Furthermore, this method shows compatibility with the late-stage functionalization of drug molecules and has the potential for scalable production, underscoring its synthetic utility for practical applications in organic synthesis. This method provides an effective means for the 1,2-selective arylamination of 1,3-dienes, demonstrating a wide substrate scope and excellent functional group tolerance and solving the problem of poor selectivity in dienes.