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　　　　　　　　　　　　　 学号：3100902050 J I A N G S U U N I V E R S I T Y 本 科 毕 业 论 文 在水中合成八元环的环状磺酰胺 Syntheses of Eight-membered Ring Sultams in Water 学院名称： 药学院 专业班级： 制药工程1002 学生姓名： 胡德美 指导教师姓名： 周爱华 指导教师职称： 教授 二O一四 年 六 月  在水中合成八元环的环状磺酰胺 专业班级： 学生姓名 指导教师： 职称：教授 Syntheses of Eight-membered Ring Sultams in Water Abstract Objective:This topic is for the synthesis of eight-membered ring Sultams in water .Sulfonamides as important intermediates in organic synthesis are playing significant roles in drug discovery. Recently, sultams have attracted more attention due to their varieties of biological activities, these include an HIV integrase inhibitor, a carbonic anhydrase inhibitor, an MMP inhibitor, an HIV-1 protease inhibitor, and an inhibitor of both falcipain-2 and Plasmodium falciparum W-2.7, so these have drawn much attention from medicinal chemists. Furthermore, this environmentally friendly water instead of organic solvents as reaction medium ，which not only conducive environment friendly but also in line with the initiative of green chemistry and atom economy .Here, the Vinyl sulfonamide protocols employ intermolecular Michael-addition by NaOH in water, followed by an intramolecular 8-endo-tet epoxide ring-opening reaction which closes the eight-membered ring. The reactions proceeded well and afforded the respective sultams in good yields under environmentally friendly conditions. Key words：Ring Sultamsorganic synthesis; environmentally friendly; Vinyl sulfonamide； ring-opening  目录 引言 1 第一章 综述 2 1.1 前言 2 1.2 磺酰胺类化合物的发展现状 2 1.3 磺酰胺类化合物生物活性 3 1.3.1 抗癌活性 3 1.3.2 杀菌活性 3 1.3.3利尿作用 3 1.3.4具有抗病毒活性的磺酰胺 4 1.4 已报道的环状磺酰胺的合成方法 4 1.4.1 Diels-Alder反应合成环状磺酰胺[16] 4 1.4.2 Heck反应合成环状磺酰胺[19] 4 1.4.