Abstract

Rh(III)‐catalyzed spiro‐annulation of sulfoximines with maleimides leads to the diastereoselective synthesis of spirocyclic‐1,2‐benzisothiazole heterocycles is disclosed here. This strategy rapidly assembles five‐membered sulfur‐nitrogen‐containing spirocyclic molecules in one‐step. Moreover, the method is scalable and exhibits favorable diastereoselectivity, moderate functional group tolerance, and excellent site‐selectivity.

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