Efficient Synthesis of Poly‐substituted Pyridine Cyclic Imides by the Tandem Aromatization and Intramolecular Ester/Amide Lactamisation Reactions

ABSTRACT

Poly‐substituted pyridines fused with cyclic imide represent a privileged class of core structural motifs widely found in pharmaceuticals and agrochemicals. In this study, we report a simple and practical strategy for the efficient synthesis of such compounds, achieving up to 97% yield. The reaction employs readily available starting materials derived from commercial amines. The key transformation involves a tandem process comprising selective dehydrogenative aromatization followed by amide formation via the intramolecular aminolysis of ester. This protocol is amenable to gram‐scale synthesis and enables the preparation of a range of useful derivatives. Furthermore, preliminary biological activity screening revealed micromolar‐range anticancer potency toward U937 cell line.