A simple and convenient one‐pot three‐component method to synthesize 1,2,3‐triazole‐based 2,3‐dihydrofuran derivatives from the condensation of 5,5‐dimethylcyclohexane‐1,3‐dione, substituted phenacyl bromide, triethylamine and 1,2,3‐triazole based benzaldehyde using a mixture of CH3CN/water as a reaction medium is described. The current protocol delivers numerous advantages such as good yield, short reaction time, easy work‐up and simplicity in the procedure as it uses a green method and an eco‐friendly catalyst. The target compounds are screened for their in‐vitro anticancer activity and most of the compounds are found to exhibit promising activity compared to standard drug Doxorubicin. Molecular docking studies performed on caspase‐3 and COVID‐19 main protease revealed well defined binding interactions and docking scores.
A library of new 1,2,3‐triazole based benzofuran derivatives was constructed via synthesizing them through the Rap‐Stoermer reaction in moderate to good yields. Various reaction conditions were examined to develop an optimized synthetic route for affording the desired products in good yields. All the synthesized compounds were characterized by 1H‐NMR, 13C‐NMR, FT‐IR, and mass spectral data. The title compounds were screened in vitro for their potential antimicrobial properties and most of the compounds exhibited promising antimicrobial activities.
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