An Efficient Access to Heteroaryl/Aryl-Annulated Pyridine Derivatives and a Study of Their Mosquito Larvicidal Activity Against Dengue Vector

Dedicated to Professor K. C. Majumdar on his 78^th birthday

Abstract

We report a convergent synthesis of heteroaryl/aryl-annulated pyridine and quinoline derivatives by a metal-free Povarov reaction. para-Toluene sulfonic acid was used as the catalyst in this reaction, which produced the products in good yields from the corresponding aromatic amines and ethyl vinyl ether. A pyridocoumarin and a pyridopyrimidine product were evaluated for their mosquito larvicidal activity against the third instar larvae of the dengue vector mosquito Aedes aegypti. Examination of morphological changes in the larvae showed damage to the target body part after treatment with both the pyridocoumarin and pyridopyrimidine products at the LC₅₀ concentrations.

Key words

pyridocoumarins - pyridopyrimidines - Povarov reaction - metal-free synthesis - insecticides

Publication History

Received: 22 January 2024

Accepted: 22 January 2024

Accepted Manuscript online:
22 January 2024

Article published online:
22 February 2024

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