Regioselective Syntheses of 1,2‐Benzothiazine 1‐Imines by Rhodium‐Catalyzed Annulation Reactions of Sulfondiimines

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Unprecedented 1,2‐benzothiazine 1‐imines have been prepared from sulfondiimines by regioselective rhodium‐catalyzed annulation reactions with diazo keto esters and α‐substituted (pseudo)halo acetophenones as coupling partners. A representative product was characterized by single crystal X‐ray structure analysis, and the applicability of the resulting three‐dimensional heterocycles to Buchwald‐Hartwig‐type amination reactions is shown. magnified image