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

Pamela Pal, Sayanti Show,Sukanya Das,Sayantika Bhakta, Swarupa Mondal, Priya Roy,Tapas Ghosh,Raj Kumar Nandi

Synlett(2024)

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摘要
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.
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