Studies On The Synthesis Of New [1,2,4] Triazole And Close The Tricyclic Type Zhuo Fused Heterocyclic

Many 6-7-5 tricyclic 1.2.4-triazolobenzoheteroazepines are of interest due to their properties as therapeutic agent, in particular, as psychiatric drugs. On the other hand, 5-7-5 tricyciic thienotriazoloazepines show important biological activities. They have also been used as drugs or candidates as antipsychotic agents, and for treatment of osteoporosis. These two kinds of heterocycles have received considerable attention.The present thesis was concentrated on the synthesis of unprecedented 2-oxo-1.2,4-triazolobenzoxazepine derivatives. 2-thio-1,2,4-triazolobenzoxazepine derivatives, and novel thieno-1.2,4- triazoloazepine derivatives.The first chapter serves as a brief treatise on 6-7-5 tricyclic 1,2,4-triazolo fused benzoheteroazepines derivatives and 5-7-5 tricyclic 1,2.4-triazole fused thienoazepines derivatives.The second chapter is about the synthesis of some kinds of chroman-4-ones. 6,7-dihydrobenzo[b]thiophen-4(5H)-one, and their corresponding hydrazones.The third chapter aims at the synthesis of 6-7-5 tricyclic 2-oxo-[ 1.2,4]tnazolo[3.2-d][1.5]benzoxazepine derivatives. A series of these novel tricyclic compounds were prepared featuring acid-induced ring closure of the geminal arylazo isocyanato compounds, which were prepared from chroman-4-ones in three steps, followed by feasible ring expansion with simultaneous insertion of the nitrogen atom into the carbon skeleton. The structure of the products was comfirmed by IR, 1H NMR, 13C NMR, MS. HRMS and X-ray analysis. The mechanism for the rearrangement was also discussed.In chapter four we prepared a series of novel tricyclic 2-thio-[l,2,4]triazolo[3,2-d][l,5]benzoxazepine derivatives using the acid-induced ring closure of the geminal arylazo isocyanato compounds. The structure of one of the products has been determined by X-ray diffraction analysis.The chapter five aims at the synthesis of neutral 1,2,4-triazolo 5-7-5 tricyclic compounds. On one hand, we used azo carbenium ions derived from ethoxy carbonyl hydrazones as building blocks, followed by cycloaddition, rearrangement and hydrolysis, to get neutral 2-substituted-5,6-dihydro-4H-thieno[2,3-f] -l,2,4-triazolo[l,5-a]azepine. On the other hand, utilizing the cycloaddition of isocyanic acid with arylhydrazone, followed by oxidation , acid-induced ring closure and rearrangement, we couldn't achieve the synthesis of the target triazolone compounds.The chapter six is mainly about the experimental section, which corresponds to the synthesis of the compounds mentioned in the former chapters. Furthermore, the spectra data have also been oresented.