Base‐Mediated Synthesis of 4‐Arylpyridin‐2‐one Derivatives and Exploring Their Cytotoxic Properties Against BT474 Cancer Cell Line

ABSTRACT A novel approach was proposed to the synthesis of 4‐arylpyridin‐2‐one derivatives, including ones annulated at the N(1)‐C(6) positions with an isoquinoline moiety (2‐aryl‐6,7‐dihydro‐4 H ‐pyrido[2,1‐ a ]isoquinolin‐4‐ones). The method is based on the reaction of N ‐(4‐oxo‐2‐aryl‐3,4,6,7‐tetrahydro‐2 H ‐pyrido[2,1‐ a ]isoquinolin‐3‐yl)benzamides with bases in DMSO. At room temperature, this reaction leads to the elimination of a benzamide molecule, while heating induces cleavage of the N(5)─C(6) bond, providing a route to 4‐arylpyridin‐2‐one derivatives. Cytotoxic activity of the synthesized compounds was evaluated against the BT474 breast cancer cell line.