Study On The Synthetic Technologyand Biologocalactivity Of Novel N-containing Heterocyclic Pyrazolradmides

Studying the synthesis of heterocyclic compounds is one of most spirited itemsin organic synthesis research and development, especially N-containing heterocycliccompounds have been widely utilized in the production of medicines, pesticides,fine-chemical intermediates and other fields owing to its high biological activity andbroad spectrum.This thesis mainly focuses on the synthesis of the part of active N-containingheterocyclic compounds comp, we synthesized some kinds of compounds usingseveral simple test methods, such as pyrazole amides,1,3,4-thiodiazole andimidazolinone. Subsequently, the biological activities was studied and discoveredthat part of N-containing heterocyclic compounds have better activities. Based onexperiments, new reactions are revealed and the mechanism of reaction has also beeninvested. In the end, the better process was chosen to prepare a series of the targetcompound in order to find novel bioactive compounds.The viewpoints of pesticides were generalized in the first chapter of my paperand some developments in civil and abroad and suggestions of one’s own were alsoput forward.The second chapter mostly summarizes the chlorantraniliprole. Synthesis ofbenzamides intermediates and a variety of novel cholrantraniliprole derivatives wereintroduced, and their structures were confirmed. Subsequently, the bactericidal effectwas studied via biological activity test. The results present that part of thesecompounds have a higher antibacterial effect on diamondback moth and beetarmyworm.The synthetic methods and the activities of1,3,4-thiadiazole are reviewed in thethird chapter. Based on the synthetic method of5-alkyl-2-1,3,4-thiadiazole,5-(2,6- difluorophenyl)-1,3,4-thiadiazole-2-amine was prepared, and then five novel1,3,4-thiadiazole amide compounds were prepared through amidation reaction. Thesynthetic method possesses a variety of advantages in terms of the simplicity, easyto-operation and high yield. The structure of target compounds were performed withIR and1H NMR, meanwhile, its bactericidal effect was studied via biologicalactivity test. The results present that part of these compounds have a higherantibacterial effect on Gibberella zeae and Cercospora arachidicola.In the last chapter, a new chemical reagent2-(2,6-difluorophenyl)-1H-imidazol-5(4H)-one was synthesized fromN-(2-amino-2-oxoethyl)-2,6-difluorobenzamide by dehydration in the presence ofPOCl3as catalyst. The structure of target compound had been characterized by IR,1H NMR and GC-MS. The reaction mechanism was proposed.