Greener synthesis of indolizine analogues using water as a base and solvent: study for larvicidal activity against Anopheles arabiensis

Abstract

Greener synthesis of a series of novel indolizine analogues have been achieved by the cyclization of aromatic cycloimmoniumylides with electron deficient alkynes in presence of water as the base and solvent at 80 °C. Yield of the title compounds was good and reactions performed were eco-friendly. The structures of these newly synthesized compounds have been confirmed by spectroscopic techniques such as FTIR, NMR, LC-MS and elemental analysis. Characterized title compounds were evaluated for larvicidal activity against Anopheles arabiensis by standard WHO larvicidal assay using Temephos as standard at 4 μg/mL. Title compounds 2e, 2f and 2g emerged as promising larvicidal agents.

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The title compounds 2a-j have been synthesized by two step chemical reaction, purified by recrystallization method at 69-83% yield. Larvicidal results revealed that, title compounds 2e and 2g emerged as promising larvicidal agents compared to standard compound.

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