N-heterocyclic sulfones constitute the core of several pharmaceuticals, including the antityrpanosomal drug Nifurtimox. Their biological relevance and architectural complexity makes them valued targets and inspires the development of more selective and atom-economical strategies for their construction and post-modification. In this embodiment, we describe a flexible approach to sp3-rich N-heterocyclic sulfones, which hinges on the efficient annulation of a novel sulfone-embedded anhydride with 1,3-azadienes and aryl aldimines. Further elaboration of the lactam esters has facilitated the construction of a library of vicinally functionalized sulfone-embedded N-heterocycles.
