Work

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

Year: 2026

Type: article

Abstract: 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.

Source: Asian Journal of Organic Chemistry

DOI: 10.1002/ajoc.70580

Authors: Xia Zhang, Jin Huang, Xiao‐Kang Nie, Xin Cui, Yan Jiang, Zhuo Tang, Guang‐Xun Li

Institutions: Xihua University, Chinese Academy of Sciences, Chengdu Institute of Biology, Xichang University

Language: English

Topic: Advanced Synthetic Organic Chemistry

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: bronze

Funder: National Natural Science Foundation of China

OpenAlex ID: W7224967685

FWCI:

Cites: 41

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Related to: 10