Synthetic study demonstrates palladium-catalyzed [4 + 2] annulation of 1,3-butadienes, highlighting an efficient route to bioactive benzosultam scaffolds.
Herein, we have demonstrated a palladium‐catalyzed [4 + 2] annulation reaction to acquire benzosultam frameworks from readily accessible 2‐iodo‐arylsulfonamides and feedstock material 1,3‐butadienes. The synthetic transformation involves consecutive CC and CN bond formations by following intermolecular Heck‐type coupling and intramolecular Tsuji–Trost allylic amination via a transient π‐allyl‐Pd‐intermediate to enable benzosultams. Operational simplicity, broad substrate scope, viability of functional groups, scalability, and further synthetic transformations are the significance of the protocol.
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Shanmugam et al. (2026) studied this question.
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