Gold(I)-catalyzed reactions of electron-poor
alkynes are still
a challenging process. A straightforward synthesis of phosphorus-based
heterocycles, namely, 2-phenyl 1H-isophosphinoline
2-oxides 1, is reported. The reaction used PPh3AuCl precatalyst in combination with triflic acid under microwave
activation and afforded isophosphinoline 2-oxides 1 in
moderate to quantitative yields through a fully regioselective 6-endo-dig
hydroarylation cyclization, paving the way toward an effective synthesis
of phosphorus heterocycles.
The present study aims to investigate the in vitro antibacterial activities of several isophosphinoline-2-oxides that can be perceived as combined bio isosteres of coumarins and flavonoids. More specifically, antibacterial activity was evaluated against four bacterial strains, including the Gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa and the Gram-positive bacteria Staphylococcus aureus and Enterococcus faecalis by using disk diffusion assay. Notably, isophosphinoline-2-oxide compounds showed promising and highly selective antimicrobial activity against S. aureus.
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