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Rapid Access to 3‑Substituted Pyridines and Carbolines via a Domino, Copper-free, Palladium-Catalyzed Sonogashira Cross-Coupling/6π-Aza Cyclization Sequence

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posted on 2021-11-30, 19:36 authored by Dilipkumar Uredi, Amarender Goud Burra, E. Blake Watkins
Herein, we report a one-pot, three-component method for the preparation of 3-substituted pyridines and carbolines via copper-free, palladium-catalyzed Sonogashira cross-coupling with aryl iodides, followed by 6π-aza cyclization. This arylation cross-coupling/annulation cascade provides easy access to substituted, fused pyridines from readily available substrates in good yields (67–92%) with complete selectivity.

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