Microwave-Assisted Mannich Reaction of 2-Hydroxy-chalcones

A series of Mannich base derivatives of 2-hydroxy-chalcones were obtained expediently in good to excellent yields by microwave-assisted Mannich reaction. The regioselectivity of the reaction occurred preferentially at the C-3 position of the 2-hydroxy-chalcone backbone. In comparison with conventional results, results from microwave possesses give better yields in shorter times. Further vasorelaxation assay showed that 2-hydroxy-3-((4-methylpiperazin-1-yl)methyl)-4,6-dimethoxymethoxy-3'-bromo-chalcone 8 significantly decreased maximal PE-induced contraction (Emax=1005.97%, EC50=10.20.51M).