Introducing a sulfone-embedded anhydride to the anhydride-imine reaction for the modular synthesis of N-heterocyclic sulfones bearing vicinal stereocenters

Abstract

A flexible approach to sp3-rich N-heterocyclic sulfones, which hinges on the efficient annulation of an easy-to-prepare sulfone-embedded anhydride with 1,3-azadienes and aryl aldimines, is described.

Regiodivergent synthesis of sulfone-tethered lactam–lactones bearing four contiguous stereocenters

“…In the last decade, we have sought to popularize the 1,3-azadiene-anhydride reaction for the stereocontrolled synthesis of lactam-bearing 5-aryl-4( E )-pentenoic acids of type 1 (ref. 10) (Fig. 2A) and subsequent post-diversification.…”