One-Pot Synthesis of alpha-Ketoamides from alpha-Keto Acids and Amines Using Ynamides as Coupling Reagents

A one-pot strategy for alpha-keto amide bond formation have been developed by using ynamides as coupling reagents under extremely mild reaction conditions. Diversely structural alpha-ketoamides were afforded in up to 98% yield for 36 examples. This reaction features advantages such as practical coupling procedure, wide functional group tolerance, and extremely mild conditions and has potential applications in synthetic and medicinal chemistry.