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

IF 2.7 3区化学 Q1 CHEMISTRY, ORGANIC

Organic & Biomolecular Chemistry Pub Date : 2024-11-06 DOI:10.1039/d4ob01686f

Rapelly Venkatesh , Keerthana Gurukkalot , Vinoth Rajendran , Jeyakumar Kandasamy

引用次数: 0

Abstract

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.

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室温下从对醌甲酰胺（p-QMs）合成 N-苄基吡啶酮：体外血浆抗疟活性评估。

我们介绍了一种室温下在碱存在下从对醌甲酰胺（p-QMs）和 2-或 4-羟基吡啶合成 N-苄基吡啶酮的方法。反应通过 1,6-迈克尔加成反应进行。该方法操作简单、产率高甚至极高、底物范围广、官能团耐受性好，这些都是其显著特点。合成的 N-苄基吡啶酮在亚微摩尔浓度下具有显著的体外血浆抗疟活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Organic & Biomolecular Chemistry 化学-有机化学

CiteScore

5.50

自引率

9.40%

发文量

1056

审稿时长

1.3 months

期刊介绍： Organic & Biomolecular Chemistry is an international journal using integrated research in chemistry-organic chemistry. Founded in 2003 by the Royal Society of Chemistry, the journal is published in Semimonthly issues and has been indexed by SCIE, a leading international database. The journal focuses on the key research and cutting-edge progress in the field of chemistry-organic chemistry, publishes and reports the research results in this field in a timely manner, and is committed to becoming a window and platform for rapid academic exchanges among peers in this field. The journal's impact factor in 2023 is 2.9, and its CiteScore is 5.5.