Study On The Synthesis Of New Containing Pyrazole Ring Aminophosphonate And 1,4-DPHs Derivatives

The pyrazole derivatives have extensive biological activities, such as antibacterial, antiphlogistic, fall blood sugar, and anti-tuberculosis. Besides, they are also very important heterocyclic compounds of pesticide, and they have the activities such as weeding, insecticidal, sterilizing . In recent years ,the synthesis and biological activity of pyrazole compounds has increasingly become the hot issue of heterocyclic chemical research.In this paper, we put the pyrazole ring into the other active groups, and expect higher bioactive compounds. Besides, we also study the synthesis method of the pyrazole derivatives, and find out the best reaction conditions by means of green chemisty.This thesis includes three chapters.In the first chapter, the synthesis and biological activty ofα-aminophosphonate derivatives containing novel substituted pyrazole.1. A series of novelα-aminophosphonate derivatives containing substituted pyrazole were synthesized with substituted pyrazolyl aldehyde, arylamine and diethylphosphone under microwave-assisted out using any catalysts and solvent, and studied its preliminary bioassay. The advantages of this method include high efficiency, good yields, simple experimental procedures and environmentally benigncy.2. A serious of novelα-aminophosphonates derivatives containing pyrazole and benzothiazole were synthesized with substituted pyrazole aldehyde, 2-aminobenzothiazole and diethylphosphone under microwave-assisted without using any catalysts and solvent. The advantages of this method is simple experimental procedures and environmentally benigncy.In the second chapter, the study on the condesation synthesis of 4-substituent pyrazole aldehyde with active methylene compounds.We studied the synthesis methods of Knoevenagel condensation in the presence of inexpensive thiourea, pyrazole aldehyde react with active methylene compound under microwave-assisted solvent-free conditions. The advantages of this method include simple experimental procedures, inexpensive catalyst and environmentally benigncy.In the third chapter, the study on the synthesis of 1,4-dihydropyridines containing novel substituted pyrazole.A series of novel 1,4-dihydropyridines containing substituted pyrazole were synthesized with substituted pyrazolyl aldehyde,β-ketoester, and ammonium acetate in one-pot under sulfamic acid catalysis in ethanol. We find a simple and efficient, low new ways by means of study about the synthesis.In summary, a series of novel compounds contained pyrazole with potential biological activities were designed and prepared in this theis. In their preparation, several improved synthetic methodologies with simple procedure, high efficiency and envirenmental benigncy were developed. It is expected that these methods may find more applications in synthetic organic chemistry and related areas. In addition, some of the compounds prepared in this thesis showed moderated biological activities.