August 16, 2025

Rapid Access to Spiro4.6-(di)benzodiazepine Indenes: Regioselective Rh(III)-Catalyzed Cascade C-H Activation/Spiroannulation.

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C-H activation enables regioselective synthesis of diazepine indenes, suggesting potential applications in medicinal chemistry.

The spiroannulation results in good to excellent yields of α-keto/ester-substituted indenamines with spirocyclic diazepine frameworks,
The method demonstrates broad substrate scope and functional group tolerance across various conditions,
This process uses Cp*Rh(III) catalyst for a one-pot reaction without silver additives or external oxidants,
Potential relevance in medicinal chemistry is highlighted through the construction of bioactive ester conjugates.

Naskar et al. (2025) studied this question.

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