Synthesis of Indole Derivatives and Cascade Reactions
Summary
The indole nucleus is a privileged scaffold in natural products, pharmaceuticals and agrochemicals. Its unique electronic structure and reactivity at the C2 and C3 positions have spurred the development of numerous synthetic methodologies. Cascade reactions, in which multiple bond-forming events occur sequentially in a single operation, have emerged as a powerful platform for rapid and atom-efficient assembly of complex indole-derived architectures. Key strategies include dearomatisation-driven cyclisations, spirocyclisations and ring-expansion processes. By harnessing metal catalysis, organocatalysis and multifunctional reagents, chemists now access spirocyclic indolenines, polycyclic alkaloid cores and heteroaromatic frameworks in high yield and stereocontrol. These advances not only streamline synthetic routes but also open avenues to structurally diverse libraries for drug discovery and agrochemical development.
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Synthesis of Indole Derivatives and Cascade Reactions publication trend
The graph below shows the total number of articles in synthesis of indole derivatives and cascade reactions across all publications each year (not limited to Nature Index journals).
Technical terms
Indole: A bicyclic aromatic heterocycle composed of a benzene ring fused to a pyrrole ring, prevalent in natural products and pharmaceuticals.
Cascade reaction: A sequence of two or more bond-forming transformations that proceed in a single operation without isolation of intermediates, maximising efficiency.
Dearomatisation: The conversion of an aromatic system into a non-aromatic or partially saturated structure, often used to introduce complexity and three-dimensionality.
Spirocyclisation: A reaction that creates a spiro centre—an atom shared by two rings—yielding rigid, three-dimensional spirocyclic architectures.
References
- Modular Synthesis of Polycyclic Alkaloid Scaffolds via an Enantioselective Dearomative Cascade. Organic Letters (2020).
- A Thiol-Mediated Three-Step Ring Expansion Cascade for the Conversion of Indoles into Functionalized Quinolines. Organic Letters (2021).
- Pd-catalyzed cascade allylic alkylation and dearomatization reactions of indoles with vinyloxirane. Organic & Biomolecular Chemistry (2016).
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