Base‐Promoted Cascade C−N and C−C Formation: An Approach to Pyrido[1,2‐a]pyrimidinones from Ynones and 2‐Methylpyrimidin‐4‐ols

Abstract An efficient base‐promoted approach for the synthesis of pyrido[1,2‐ a ]pyrimidinones from ynones and 2‐methylpyrimidin‐4‐ols have been developed via the C−N and C−C formation procedure. Diversely structural pyrido[1,2‐ a ]pyrimidinones were afforded in up to 95% yield for 29 examples. This reaction featured with advantages such as practical tandem procedure, wide functional group tolerance and metal‐free conditions, which has potential application in synthetic and medicinal chemistry.