A transition metal‐free approach for the generation of radical intermediates via EDA complexes had been developed. This approach enables a cross‐dehydrogenative C−O coupling of oximes with acetonitrile, ketones and esters with high yields and regioselectivities. Perfluorobutyl iodide was used as the unique electron acceptor to trigger a new radical formation. The radical pathway was confirmed by UV‐Vis spectroscopy, radical inhibiting, trapping and kinetics experiments.magnified image

A base-mediated [3 + 3] benzannulation strategy for the conversion of 1,3-bis(sulfonyl)propenes and β,γ-unsaturated α-ketoesters to diaryl sulfones has been developed. This method provides facile, metal-free and efficient access to highly substituted diaryl sulfones in good to excellent yields. In addition, the sulfonyl group could be easily removed or converted to other functional groups via an organostannane intermediate.

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A series of meta-amido bromophenol derivatives were designed and synthesized. The compounds were found to potently inhibit the growth of Mycobacterium tuberculosis H37Ra. They also exhibited moderate inhibitory activity against Mycobacterium tuberculosis H37Rv and multidrug-resistant strains. The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. Moderate cytotoxicities and good metabolic stability were observed for the selected compounds. The results demonstrated meta-amido bromophenols as a new class of antitubercular agents with good potentials.

α-Nitro-β,β-diaryl-propionates were prepared with good yields and excellent enantioselectivities via asymmetric conjugate addition of t-butyl nitroacetate to in situ generated o-quinone methides.