Transition-metal-catalyzed regiodivergent sulfonylation of aziridrines for the synthesis of β-amino sulfones

beta-Amino sulfones find extensive applications in pharmaceuticals, natural products, agrochemicals, and organic synthesis. Meanwhile, aziridine units are recognized as valuable intermediates in contemporary synthetic chemistry for efficient synthesis of beta-functionalized amines through ring-opening reactions. However, the ring-opening sulfonylation of aziridines via SO2 insertion, granting access to beta-amino sulfones, remains unexplored. In this paper, we present a novel transition-metal-catalyzed system for the first regiodivergent sulfonylation of aziridines using SO2 insertion to produce beta-amino sulfones successfully. This method is distinguished by its mild reaction conditions, a broad substrate scope, ease of execution, and exceptional regioselectivity. We developed the first transition-metal-catalyzed, regiodivergent sulfonylation of aziridines, enabling the efficient synthesis of diverse beta-amino sulfones under mild conditions with broad substrate compatibility and high regioselectivity.