Organic Letters· 2026Q1
Palladium-Catalyzed Three-Component Dearomative Carbofluoroallylation of Polycyclic Indoles with gem -Difluorocyclopropanes and Ketones
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- Q1SCImago
- 2026year
Short summary
A new palladium-catalyzed reaction creates complex ketone-indolines with a 2-fluoroallylic motif from polycyclic indoles, gem-difluorocyclopropanes, and ketones.
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Key points
- Developed a palladium-catalyzed, three-component reaction for dearomative carbofluoroallylation.
- Synthesizes complex ketone-indolines with a linear 2-fluoroallylic motif.
- Demonstrates broad substrate scope and high functional group tolerance.
- Enables late-stage functionalization of natural product derivatives.
- Products can be readily elaborated into various fluoroallylic scaffolds.
AI-generated from the title and abstract; the full text is not read.
Abstract
Abstract We herein report a robust palladium-catalyzed, three-component dearomative carbofluoroallylation of polycyclic indoles using gem-difluorocyclopropanes and ketones. This method enables the diversity-oriented synthesis (DOS) of complex ketone-indolines featuring a linear 2-fluoroallylic motif. With its broad substrate scope and high functional group tolerance, the protocol is highly effective for the late-stage functionalization of natural product derivatives. Moreover, the cross-coupling adducts can be readily elaborated into a variety of distinct fluoroallylic scaffolds, demonstrating the significant synthetic utility of this approach.
The authors' abstract, as published at the source. Organic Letters, 2026 · DOI ↗
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Field: Pharmaceutical Science
Pharmaceutical SciencePharmacology, Toxicology and Pharmaceutics