Synthesis of N-benzyl pyridones from para-quinone methides (p-QMs) at room temperature: evaluation of in vitro blood-stage antiplasmodial activity

被引：0
作者：
Venkatesh, Rapelly [1 ]
Gurukkalot, Keerthana [2 ]
Rajendran, Vinoth [2 ]
Kandasamy, Jeyakumar [1 ]
机构：
[1] Pondicherry Univ, Dept Chem, Pondicherry 605014, India
[2] Pondicherry Univ, Dept Microbiol, Pondicherry 605014, India
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2025年 / 23卷 / 02期
关键词：
2-PYRIDONES; DESIGN; FUNCTIONALIZATION; 4-PYRIDONES; ALKYLATION; INHIBITOR; DISCOVERY; MALARIA;
D O I：
10.1039/d4ob01686f
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
We present a method for synthesizing N-benzyl pyridones from para-quinone methides (p-QMs) and 2- or 4-hydroxy pyridines in the presence of a base at room temperature. The reaction proceeds through 1,6-Michael addition reaction. Simple operation, good to excellent yields, broad substrate scope, and good functional group tolerance are the salient features of the developed methodology. The synthesized N-benzyl pyridones displayed significant in vitro blood-stage antiplasmodial activity at sub-micromolar concentration.
引用
收藏
页码：383 / 388
页数：6
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