Synthesis of Novel 1,4‐Diazepane‐Spirooxindole Frameworks via Catalytic (6 + 1) Annulation of Diazooxindoles with Hexahydropyrimidines

Abstract Herein, we have developed a catalytic (6 + 1) annulation of diazooxindoles with hexahydropyrimidines under rhodium or copper catalysis. This strategy offers a general and efficient method for constructing pharmacologically relevant 1,4‐diazepane‐spirooxindole frameworks in moderate to excellent yields. Diverse synthetic transformations of the obtained products have also been achieved to obtain more complex and even drug‐like spirooxindoles, demonstrating the broad synthetic utility of this approach.