4.6 Article

Ecofriendly aminochalcogenation of alkenes: a green alternative to obtain compounds with potential anti-SARS-CoV-2 activity

Journal

NEW JOURNAL OF CHEMISTRY
Volume 47, Issue 14, Pages 6591-6601

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d2nj06218f

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Here, a solvent- and metal-free methodology for the aminochalcogenation of alkenes using molecular iodine as a catalyst, DMSO as a stoichiometric oxidant, and different nucleophiles under microwave irradiation is reported. The eco-friendly approach provided the desired products with good to excellent yields in just 20 minutes. Additionally, the antiviral activity of twenty compounds obtained by this methodology against the coronavirus SARS-CoV-2 was evaluated, and two compounds (4d and 5b) showed potent antiviral activity with low cytotoxicity, suggesting promising potential as antiviral agents.
Here, we report a solvent- and metal-free methodology for the aminochalcogenation of alkenes, using molecular iodine as a catalyst, DMSO as a stoichiometric oxidant, and different nucleophiles under microwave irradiation. This ecofriendly approach provided the desired products with good to excellent yields in just 20 minutes. In addition, twenty compounds obtained by this methodology were referred for evaluation of potential antiviral activity against the coronavirus SARS-CoV-2. Two of the evaluated compounds (named 4d and 5b) showed potent antiviral activity, with a low cytotoxic profile resulting in a promising selectivity index.

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