Synthesis and Antiproliferative Activity of Polysubstituted Tetrahydropyridine and Piperidin‐4‐one‐3‐carboxylate Derivatives

A highly atom‐economic one‐pot multicomponent synthesis of polysubstituted tetrahydropyridines (THPs) is described. The reaction of anilines, aromatic aldehydes, and β‐keto esters proceeds in the presence of catalytic amount of zirconium tetrachloride, and the products can be further converted to the corresponding piperidin‐4‐one‐3‐carboxylates under acidic conditions. The two sets of products were evaluated for their anticancer activity and some of these compounds, particularly the piperidin‐4‐one‐3‐carboxylates have significant anticancer activity.