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1、分类号学号湖南口弋学祠页习匕学毛乞七仑文安非他酮、经基安非他酮及其类似物的合成研究研究生姓名陈科培养单位湖南大学化学化工学院指导教师姓名、职称胡艾希教授学科专业应用化学研究方向精细化学品合成与应用论文提交日期年月,即摘要安非他酮、轻基安非他酮是抗抑郁新药。本文以间氯苯丙酮、苯丙酮、对节一,一、一一一一、一氧基苯丙酮和甲氧基蔡丙酮为原料经澳代氨基甲基丙醇甲基乙醇胺的胺化反应合成新型抗抑郁药安非他酮、轻基安非他酮及其类似物。以间氯苯丙酮为起始原料,经的。一卤代合成一卤一一氯苯基卜一丙酮,一一一一卤氯苯基
2、卜丙酮在溶剂中于室温下与叔丁胺反应合成抗抑郁药安非。用作反应介质合成安非他酮的反应时间从报道以、甲醇等作他酮乙睛溶剂的几十个小时、几天大大的缩短到小时。以间氯苯丙酮为起始原料,在国内首次通过引入手性辅助剂,一酒石酸二甲酷不对称合成一安非他。一,,酮合成安非他酮的路线简单可行并且符合光学纯药物给药的发展趋势因此具有重要的实际意义。、一,一以苯丙酮对节氧基苯丙酮和甲氧基蔡丙酮为原料经漠代合成中间体一一一一、一一一一一一一一一一嗅苯基丙酮澳节氧基苯基丙酮和嗅甲氧基蔡基。,、一一一,一丙酮在中分别与叔丁胺反
3、应快速高收率合成苯基〔二甲一一丙酮、一一一,一二甲基一一基乙基氨基节氧基苯基卜乙基氨基丙一一一一一,一一一一。酮和甲氧基蔡基升二甲基乙基氨基飞丙酮等叔丁胺基芳基丙酮类化合物。在国内首次由间氯苯丙酮的浪化产物一嗅一一氯苯基卜一丙酮与一氨基一一甲基丙醇在中反应合成新型抗抑郁药轻基安非他酮。本合成路线反应时间短,反应收率高、操作方便。一一一一、一一一一一一一一首次在国内以嗅苯基丙酮嗅节氧基苯基丙酮和嗅甲氧基一一蔡基一一丙酮等中间体与一氨基一一甲基一丙醇反应,高收率合成有潜在抗抑一一,一一一、一一一,,郁活
4、性的经基安非他酮类似物苯基,三甲基吗琳醇节氧基苯勤一一一一一一一,,一一一。三甲基吗琳醇和甲氧基蔡勤三甲基吗琳醇三种新化合物首次在国内以间氯苯丙酮、苯丙酮、对节氧基苯丙酮和一甲氧基蔡丙酮的一甲基,澳化产物中间体与乙醇胺反应高收率合成具有潜在抗抑郁活性的化合物一一,一一一、一一,一一一、一一氯苯基升二甲基吗琳醇苯基二甲基吗琳醇节氧基苯基卜,一二甲基一一吗琳醇和一一甲氧基一一蔡基,一二甲基一一吗琳醇四种新化合物。关键词安非他酮一安非他酮轻基安非他酮一吗琳醇合成一一一,一一一,一一,一一,一一一,一一一,
5、一一一一,一冲一一,一,,一,印叩冲即甲目录摘要···························,·············································,··········⋯⋯··············································································⋯⋯第一章绪论盐酸安非他酮研究概况··········································⋯⋯选题与
6、研究内容······················································⋯⋯第二章盐酸安非他酮及类似物的合成实验部分·······························································⋯⋯结果与讨论························································⋯⋯‘⋯小结········································
7、································⋯⋯第三章盐酸轻基安非他酮及类似物的合成实验·······························································⋯⋯部分·············································’‘‘‘”二””结果与讨论⋯⋯小结·····································································
8、···⋯⋯结论···························································,························⋯⋯致谢····················································································⋯⋯参考文献···················································