Regioselective palladium-catalyzed monoarylation of azoles was achieved using iodobenzoate immobilized on an insoluble polymer support. The positional selectivity for the coupling reaction was dramatically influenced by the presence of CuI. No diarylation was observed in either case. Unsymmetrical diarylation was also obtained with the polymer support using sequential coupling reactions.
Novel antibacterial biaryl oxazolidinones bearing an aza-, an oxa-, or a thiabicyclo[3.1.0]hex-6-yl ring system were synthesized, and their in vitro antibacterial activity and structure-activity relationships (SAR) were evaluated. Most of the synthesized biaryl bicyclo[3.1.0]hex-6-yl oxazolidinones showed good antibacterial activity against the Gram-positive and -negative bacteria tested. Regarding SAR trends among the C-ring subtypes, the pyridyl ring was preferable to the phenyl ring. The results showed that the structural variety of the C-ring has a greater impact on antibacterial activity than that of the B-ring. A cyano group at the D-ring C-6 position plays an important role in the highly potent antibacterial activity.
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