RESUMO
Arylsulfonyl group-bearing α,ß-unsaturated enol esters were readily assembled via the Cs2CO3-mediated union of 2-bromoallyl sulfones and cinnamic acids. The overall transformation is equivalent to an sp2 carbon-oxygen coupling reaction, and therefore constitutes a formal vinylic substitution. Several of the products display promising levels of antiproliferative activities higher than that of the anticancer drug carboplatin. Thiophenol reacted with 2-bromoallyl sulfones under identical conditions to afford α-thiophenyl-α'-tosyl acetone via an apparent aerial oxidation.
Assuntos
Antineoplásicos , Proliferação de Células , Ésteres , Antineoplásicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Ésteres/química , Ésteres/farmacologia , Ésteres/síntese química , Humanos , Proliferação de Células/efeitos dos fármacos , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura Molecular , Sulfonas/química , Sulfonas/farmacologia , Sulfonas/síntese química , Relação Estrutura-Atividade , Compostos de Vinila/química , Compostos de Vinila/farmacologia , Compostos de Vinila/síntese químicaRESUMO
Benzannulation reactions involve construction of a benzene ring from acyclic precursors. This class of reactions offer a versatile and often superior alternative to aromatic substitution for construction of substituted arenes. Selected pioneering and recent reports of various benzannulation reactions are categorised and discussed in this review.