Synthesis Of 3a, 5-diaryl-[1, 2, 4]-oxodiazolo-[5,4-d][1, 5]benzothiazepines Drivatives

1,5-Benzothiazepines are a kind of compounds which have important biological activities,often used as depressant and medicines for cardiovascular disease. Their syntheses, structures and pharmacological activities have attracted wide attention. The C=N imine double bond in the molecules is one of the major parts where chemical reactions occurred. Meanwhile five or six members heterocycle brought to the parent is also a series of compounds used to cure nerve illnesses. In addition we combined 1,2,4-oxodiazole which has strong biological activities with 1,5- benzothiazepines by 1,3-dipolar cycoladdition reaction respectively, and a series of derivatives with novel structures were synthesized.The thesis includes two major parts:The first part is about literature review. The important synthetic methods, structure and chemical transformation of 1, 5-benzothiazepine derivatives that have been studied in china and other countries were explicated systematically and briefly elucidated quinoxaline.The second part is about experimental content. Major work as follows:1. Synthesie of novel 1-(quinoxalino-2-yl)-3a, 5-diaryl-[1,2,4] oxodiazolo [5,4-d][1,5]benzothiazepines.Starting with o-phenylenediamine and fructose, synthesized quinoxaline- 2- carboxaldehyde, in high yield, and transformated it into quinoxalino-2-hydroximoyl chloride, then reacted with 2, 4-diaryl-2, 3-dihydro-1, 5-benzothiazepines to yield 15 novel compounds.2. Synthesis of 2,4-diaryl-3-(1,2,4-triazolo-1-yl)-2,3-dihydro-1,5- benzothia- zepine derivatives.