Experimental study demonstrates palladium-catalyzed amidative annulation of indene, indicating an efficient synthetic route to spirocyclic N-heterocycles.
N-Heterocycles are a class of pivotal values in diverse fields, and methods for their efficient construction are highly desired. Herein, we report a palladium-catalyzed allylic C(sp3)-H amidative annulation of indene, accessing spiro[indene-1,2′-pyrrolidine] derivatives with tetrasubstituted stereogenic centers. Optimized conditions afford good-to-excellent yields (up to 91%) with broad substrate tolerance. Gram-scale synthesis and further derivatizations demonstrate the synthetic utility of the reaction.
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Yang et al. (2026) studied this question.
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