Regio‐, Site‐ and Stereo‐Selective Aziridination of Conjugated Dienes Enabled by Palladium/Copper/Iodide/Oxygen Cooperation

Vinylaziridines are important building blocks in organic chemistry, especially in the synthesis of nitrogen-containing heterocycles. The direct and efficient transfer of an appropriate nitrogen source to readily accessible conjugated dienes is a notable methodology. The Pd-catalyzed oxidative 1,2-difunctionalization of conjugated dienes through a π-allyl-palladium species should be an ideal method for the selective synthesis of vinylaziridines. However, this method faces the challenge of regioselectivity, often resulting in 1,4-difunctionalization instead. In this study, we developed a Pd-catalyzed aerobic 1,2-difunctionalization of conjugated dienes via a π-allyl-palladium species to achieve regio-, site- and stereo-selective aziridination under the synergistic effects of Pd