Study On The Synthesis And Bioactivity Of 1,5-Diaryl-3-hydroxypyrazole

Heterocyclic compounds as medicines and pesticides have been developed most quickly and have become the new trend in the development. In the new developed medical and pesticidal heterocyclic compounds are the most important domain. 3-Hydroxypyrazoles show biological activities of the CDKs (Cyclin-Dependent Kinases) inhibitors and 5-lipoxygenase inhibitors, and 3-Hydroxypyrazoles demonstrated potent activation of sol. guanylate cyclase and potent inhibition of platelet aggregation. 3-Hydroxypyrazoles are the one kind of the most important intermediates in the fields of the organic synthesize and which play essential roles in some biosynthetic and metabolic pathways. In this thesis, the method for preparation of bioactivity compounds 1,5-diaryl-3-hydroxypyrazoles has been studied and their bioactivity has also been measured.3-Arylpropenates were reacted with phenylhydrazine catalyzed by sodium methoxylate, which gained 1,5-diaryl-3-pyrzolidinones. Their yields are about 50-80%. The structures of these products have been confirmed by elemental analyst, IR, 1H-NMR, UV and MS. Furthermore, we obtained the crystal of 5-(3,4-dimethylphenyl)-1-phenyl-3-pyrazolidinone by slow evaporation of an ethanol solution and the crystal structure was characterized by XDR.1,5-Diaryal-pyrazolidinones were oxidized by oxygen of air in DMF, catalyzed by ferrous chloride, which gained 1,5-diaryl-1H-3-hydroxypyrazol. Their yields are about 61%. The structures of these products have been confirmed by elemental analyst, IR, 1H-NMR, UV and MS. Furthermore, we obtained the crystals of 5-(3,4 -dimethylphenyl)-1-phenyl-1H-3-hydroxypyrazole and 5-(4-methoxyphenyl)- 1-phenyl-1H-3-hydroxypyrazole by slow evaporation of an ethanol solution and the crystal structures were characterized by XRD. The bioactivities of 1,5-diaryl-1H-3-hydroxypyrazoles in this thesis are being tested.