Recent Advances in the Activation of Unactivated Tertiary Amide C–N Bonds

Amides are readily available and commonly occur in both natural and synthetic worlds. Their direct activation and transformation would greatly facilitate the synthesis and modification of target functional molecules and provide references to the degradation and reutilization of polyamides, thus attracting much attention from the synthetic community. However, due to the strong resonance effect, it is well known that the activation and cleavage of amide C–N bonds are very challenging, especially for the unactivated tertiary amides. To our delight, with continuous efforts being devoted, great advances still have been obtained in this research field during the past decade years. In this mini‐review, we summarize the recent progress focusing on the activation of unactivated tertiary amide C–N bonds by utilizing transition metals, acids, and bases, and look forward to providing efficient references as a good tool‐book for the scientific workers from related research fields.