Synthesis And Biological Research Of Polysubstituted Pyroles And Fused-Pyrazole

There are varieties of heterocyclic compounds widely distributing in nature. They are accounting for about 1/3 of the total number of the organic matter as we known and many kinds of them have important physiological effects. One or more heteroatoms (same or different) can be contained in heterocyclic compounds with the number of rings depending. As a great important component of heterocyclic compounds, the nitrogen contained heterocyclic compounds show considerable biological activities, such as antibacterial, anti tumor, low toxicity and high absorption. Besides, nitrogen contained heterocyclic compounds are widely used in the fields of metal catalytic materials, dyes and the medical drugs as their structures are more likely to be modified.The first part of this dissertation developed a reaction of producing pyrrole derivatives effectively by [3+2] dipolar cyclization. In this reaction, the imine compounds were achieved from the combination of amino ester compounds firstly. Then, a series of pyrrole derivatives with considerable productivity were compounded by the 1,3 dipolarophile of imine compounds and nitrile substrate under the catalysis of base. The pyrrole skeleton, constituting the core structural element, can be found in a number of natural alkaloids. Many pyrrole derivatives possess various vital bioactivities including antioxidant activity, inhibition of the quinine-dependent amine oxidases, antimicrobial property, anti tumor, anti inflammatory and antibiotic activities. In addition, pyrazolone (another anticancer), a kind of antineoplastic, antibacterial and anti-inflammatory compound, is widely applied as common luminescent material dyestuff, as well as metal-chelating extraction agent.In the second part of this paper, the synthesis of pyrazole derivatives by [3+2] cyclization reaction and the bioactivity tests were introduced. As results, pyrazole derivatives can be efficiently compounded by the combination of three groups of pyrazole and diethyl aminomalonate, as well as the positive bioactivity tests consequences indicate the high bioactivity.