A new two-stage regioselective access to nonsymmetric 3,5-diarylisoxazoles starting from readily available 2-aryl-1,1-dibromocyclopropanes is developed. The strategy based on the nitrosation/Suzuki arylation sequence ensures good yields of the products and a wide scope of substituents in both aryl rings. Using this strategy, a panel of combretastatin A-4 (CA-4) analogues presented by 3,5-diarylisoxazole structural motif was synthesized and evaluated for their biological activity[a] G.

A new convenient and versatile halogenating system (R 4 NHal/ NOHSO 4 ), giving straightforward and general access to halogenated 3,5diaryl-and alkylarylisoxazoles, pyrazoles and electron-rich benzenes from the corresponding scaffolds, is suggested. The method provides excellent regioselectivity, scalability to the gram scale, and a broad scope for both aromatics and halogens. A three-step, one-pot reaction protocol was developed, and a series of 3,5-diaryl-4-haloisoxazoles has been efficiently synthesized from 1,2-diarylcyclopropanes under suggested nitrosating− halogenating conditions.

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A new method for the synthesis of thiocyanato and isothiocyanatoalkyl phenyl sulfides by the reaction of unsaturated compounds with ethyl benzenesulfenate and trimethylsilyl isothio cyanate has been suggested. Regio and stereoselectivity of the reaction was studied, having taken alkenes, dienes, and alkynes as examples.