An efficient synthesis of 2H-thiopyran-3,4-dicarboxylate derivatives via one-pot reactions between acetylenic esters, arylisothiocyanates and enaminones in water is described.The advantages of this work were: (1) the reaction was performed under neutral and more important in water as the solvent. (2) No catalyst was required for this reaction. (3) The simplicity of the present procedure made it...

In this paper, the synthesis of various enaminones from the reaction of 3-aminocoumarin and ethyl-2,4-dioxo-4-arylbutanoate in the presence of p-toluene sulfonic acid is reported. The reaction was examined under different solvents and catalytic systems, which clearly proved the importance of acidic catalyst in this organic transformation. This work was also accompanied by density functional the...

A series of novel pyrazolodibenzo[1,4]diazepines has been synthesized with good overall yields. The diarylpyrazole intermediates, with structure similarity to biologically relevant compounds such as currently marketed drugs like rimonabant or celecoxib, were prepared by a tandem sequence amine-exchange/heterocyclization starting from readily available enaminones and arylhydrazines. The key step...

A series of new poly-functionalized two-carbon-tethered fused acridine/indole pairs were synthesized via Brønsted acid-promoted domino reactions between indoline-2,3-dione and C(2)-tethered indol-3-yl enaminones. The reactions were further expanded to prepare C-tethered fused acridine/pyridine pairs, N-substituted amino acids, N-cyclopropyl and N-aryl substituted fused acridine derivatives, as ...