Herein, we report the synthesis of unprecedented N-acetylsulfilimine and -sulfoximine analogues under mild conditions. Deprotection of the N-acetylsulfoximine allows the preparation of the corresponding NH-sulfoximine. Zolimidine is a methylsulfonyl-substituted drug with an imidazo[1,2-α]pyridine core used for the treatment of peptic ulcer. Herein, we report the synthesis of unprecedented N-acetylsulfilimine