An efficient access to heteroaryl/aryl-annulated pyridine derivatives and study of their mosquito larvicidal activity against dengue vector

Synlett Pub Date : 2024-01-22 DOI:10.1055/a-2251-1849
Pamela Pal, Sayanti Show, Sukanya Das, S. Bhakta, Swarupa Mondal, Priya Roy, Tapas Ghosh, Raj Kumar Nandi
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Abstract

Herein we report a convergent synthesis of heteroaryl/aryl-annulated pyridine and quinoline derivatives by metal-free Povarov reaction. Para-toluene sulfonic acid has been used as catalyst in this reaction which produced the products in good yields from corresponding aromatic amines and ethyl vinyl ether. Synthesized compounds pyridocoumarin and pyridopyrimidine were evaluated for mosquito larvicidal activity against third instar larvae of Aedes aegypti. Observation on morphological changes in Ae. aegypti (L.) larvae was meant to decide damaged target body part after the treatment with both with pyridocoumarin and pyridopyrimidine at LC50 concentrations.

Abstract Image

杂芳基/芳基环化吡啶衍生物的高效获取途径及其对登革热病媒的杀蚊幼虫活性研究
在此,我们报告了一种通过无金属 Povarov 反应聚合合成杂芳基/芳基环化吡啶和喹啉衍生物的方法。对甲苯磺酸在该反应中用作催化剂,可从相应的芳香胺和乙烯基乙醚中生成产率良好的产物。评估了合成的吡啶香豆素和吡啶嘧啶对埃及伊蚊三龄幼虫的杀蚊虫活性。观察埃及伊蚊(L.)幼虫的形态变化,以确定在使用 LC50 浓度的吡啶香豆素和吡啶嘧啶处理后受损的目标身体部位。
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