Pd(II)‐Catalyzed Selective Amination of Inert γ‐C(sp3)−O Bonds of Aliphatic Amides with Hydrazines

The first palladium‐catalyzed selective amination of inert methyl and methylene γ‐C(sp3)−O bonds of aliphatic amides with hydrazines by using the strategy of 8‐aminoquinoline‐directed C(sp3)−H activation/β‐O elimination/hydrofunctionalization is reported. This method features a broad scope of hydrazines, affording an efficient and simple method for the synthesis of corresponding γ‐hydrazine substituted carboxylic acid derivatives that are commonly seen in drug molecules and other bioactive compounds.