A general Cu-catalyzed, regioselective method for the -3-arylation of hydantoins is described. The protocol utilizes aryl(trimethoxyphenyl)iodonium tosylate as the arylating agent in the presence of triethylamine and a catalytic amount of a simple Cu-salt. The method is compatible with structurally diverse hydantoins and operates well with neutral aryl groups or aryl groups bearing weakly donating/withdrawing elements. It is also applicable for the rapid diversification of pharmaceutically relevant hydantoins.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7309330 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.0c00642 | DOI Listing |
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