Synthesis of Alkyl-Substituted Pyridines by Directed Pd(II)-Catalyzed C–H Activation of Alkanoic Amides

Abstract

A general alkylation protocol for substituted iodopyridines was developed (32 examples, 44–97% yield). The reaction is based on the Pd(II)-catalyzed C–H activation of 8-aminoquinoline-derived alkanoic amides and it employs a catalyst cocktail of Pd(OAc)₂ (10 mol%), NaI (30 mol%), and (BuO)₂POOH (20 mol%), with Ag₂CO₃ as base.

Key words

alkylation - 8-aminoquinoline - C–H activation - palladium - pyridine

• References and Notes


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