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Radical C4–H Arylation of 1,4‐Dihydropyridines with Cyanoarenes

4‐Aryl‐1,4‐dihydropyridines are prevalent pharmacophores and versatile building blocks in medicinal and synthetic chemistry. Herein, we demonstrated a mechanistically distinct radical‐radical cross‐coupling approach to 4‐aryl‐1,4‐dihydropyridines, via direct C4–H arylation of 1,4‐dihydropyridines… Click to show full abstract

4‐Aryl‐1,4‐dihydropyridines are prevalent pharmacophores and versatile building blocks in medicinal and synthetic chemistry. Herein, we demonstrated a mechanistically distinct radical‐radical cross‐coupling approach to 4‐aryl‐1,4‐dihydropyridines, via direct C4–H arylation of 1,4‐dihydropyridines with readily available cyanoarenes. This mild protocol is initiated by the direct photoexcitation of 1,4‐dihydropyridines, eliminating the need for expensive photocatalysts and enabling operation under ambient air conditions.

Keywords: arylation dihydropyridines; chemistry; dihydropyridines cyanoarenes; radical arylation; arylation

Journal Title: Helvetica Chimica Acta
Year Published: 2024

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