Modular Room Temperature Synthesis of Sulfoximidoyl Amidines Enabled by Pd-Catalyzed Cascade Aza-Claisen Rearrangement Strategy

Reported herein is a concise synthesis of sulfoximidoyl amidines enabled by a Pd-catalyzed cascade aza-Claisen rearrangement and nucleophilic reaction at room temperature. Free NH-sulfoximines and N-allylynamides were employed as the modular building blocks to produce the expected sulfoximine amidine derivatives in highly chemoselective models and in 100% atom efficiency. A broad range of functional groups were well tolerated under these gentle reaction conditions to give the desired products in generally good to excellent yields.