Intramolecular oxidative CÀH amination of 2-aminobenzophenones was achieved in the presence of potassium tert-butoxide and dimethyl sulfoxide. A series of functionalized acridones were prepared in moderate to excellent yields in a mild, efficient, and transition-metal-free manner.
Light-driven
[2 + 2] cycloaddition of olefins is a kind of atom-economic
and green transformation for building cyclobutane scaffolds, which
are widely found in bioactive compounds and natural products. Although
great progress has been made in the (dia)stereoselective synthesis
of anti-cyclobutanes by photocycloadditions, the
selective synthesis of syn-cyclobutanes is still
full of challenges. Herein, we report a visible light-triggered and
catalyst- and template-free [2 + 2] cycloaddition strategy of chalcones
as a solid-state reaction in water to afford syn-cyclobutanes in high yields with excellent diastereoselectivity.
A copper-catalyzed, ligand-free intramolecular C−N coupling of (E)-2-(2-bromophenyl)-3-arylacrylamides has been developed. This protocol provides an efficient and practical synthetic route for the biologically important (E)-3-arylideneindolin-2ones from o-bromophenylacetic acids and aromatic or conjugated alkenyl aldehydes. Readily available starting materials, mild and noble metal-free conditions, high efficiency, and good tolerability for phenolic hydroxyl groups make this approach attractive and applicable.
The synthesis, structure confirmation, stability and isomerization features of suffrutines A, B and their N-fused analogues were reported. Biological tests showed that the introduction of nitrogen atom might be beneficial to the anticancer activity.
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