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DOI: 10.1055/a-2726-4405
Cp*Rh-Catalyzed NH-Indole-Directed C–H Activation/Annulation Toward Indole-Fused Polycyclic Compounds
Autor*innen
Financial support from NSFC (Grant Nos. 21872028), Natural Science Foundation of Fujian Province (Grant No. Grant No.2025H0007, 2024H6034), the Fujian Province University Fund for New Century Excellent Talents are great acknowledged.
Gefördert durch: NSFC 21872028
Gefördert durch: Natural Science Foundation of Fujian Province 2024H6034,2025H0007
Abstract
Indole-fused polycyclic compounds, prevalent in bioactive natural products and pharmaceuticals with antiviral, anti-tumor, and antibacterial activities, represent privileged scaffolds in medicinal chemistry. Consequently, the development of efficient strategies remains ongoing. As a powerful complement to traditional multistep approaches, NH-indole-directed C–H activation/annulation, leveraging the inherent directing ability of the indole N–H group, has emerged as a particularly efficient and step-economical approach. This review comprehensively summarizes recent key progress in the synthesis of diverse indole-fused polycycles encompassing [1,2]-, [2,3]-, and [1,7]-fused derivatives through Cp*Rh(III)-catalyzed NH-indole-directed C–H functionalization. The transformations discussed utilize readily available arylindoles and versatile coupling partners such as alkenes, alkynes, diazo compounds, and carbon monoxide, enabling rapid access to structurally complex indole polycycles under generally mild conditions. While significant strides have been made, future challenges including mechanistic elucidation, cost-effective catalyst alternatives, and the synthesis of elusive medium-sized indole-fused rings are also highlighted.
Keywords
Rhodium-catalyzed - NH-indole-directed - C–H activation - Annulation - Indole-fused polycyclic compoundsPublikationsverlauf
Eingereicht: 10. September 2025
Angenommen nach Revision: 17. Oktober 2025
Accepted Manuscript online:
17. Oktober 2025
Artikel online veröffentlicht:
20. November 2025
© 2025. Thieme. All rights reserved.
Georg Thieme Verlag KG
Oswald-Hesse-Straße 50, 70469 Stuttgart, Germany
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