中文关键词:双氢青蒿素合成青蒿砜氨基二硫代甲酸酯 英文关键词:Dihydroartemisinin, Synthesis, Artemisone, Aminodithioformate 基金项目:国家自然科学基金项目（21462032）、宁夏自然科学基金项目(NZ17001)、宁夏大学研究生创新项目(GIP201643) 和宁夏大学大学生创新创业训练计划（国家级）项目(G201610749014)资助

作者	单位	E-mail
唐磊	宁夏大学 化学化工学院	345633423@qq.com
杨茂祥	宁夏大学 化学化工学院
马富莉	宁夏大学 化学化工学院
李学强	宁夏大学 化学化工学院 宁夏天然药物工程技术研究中心
魏梦雪	宁夏大学 化学化工学院 宁夏天然药物工程技术研究中心	weimengxue@nxu.edu.cn

摘要点击次数:2573 全文下载次数:0 中文摘要: 以双氢青蒿素（DHA）为原料，与草酰氯发生酰化反应，然后经硫代吗啉取代反应、双氧水氧化反应得到青蒿砜1，青蒿砜1经过烷基化反应、脱硅保护基和碘代反应得到青蒿砜-碘代物2α。以三乙胺为催化剂，碘代物2α与哌嗪类化合物、CS2在“一锅煮”条件下得到青蒿砜—氨基二硫代甲酸酯化合物（3a~3d），所有目标化合物的结构经1H NMR，13C NMR，IR和HR-ESI-MS得到确证。 英文摘要: A practical preparation of artemisone-aminodithioformate hybrid compounds was achieved from dihydroartemisinin and thiomorpholine. The dihydroartemisinin was treated with oxalyl chloride followed by mixing the mixture with a solution of thiomorpholine in dichloromethane, efficiently affording artemisinin-thiomorpholine complex. Then oxidation of the raw mixture with hydrogen peroxide in the presence of sodium tungstate gave the artemisone 1 with 48% yield for three steps. The artemisone 1 was alkylated with a silyl protected 6-iodo-1-hexanol, then desilylation and iodination of the alkylate compound successfully delivered the corresponding iodide 2α, and the yield for these three steps was 22.1%. Finally, introduction of the piperazidines into the artemisone motif was realized with carbon disulphide as the linkage, where four artemisone-aminodithioformate hybrid compounds (3a-3d) were obtained from a triethylamine promoted one-pot reaction of iodide 2α, piperazidine and carbon disulphide from room temperature to reflux. The structures of all the synthetic compounds are identified by 1H NMR, 13C NMR, IR and HR-ESI-MS. 查看全文查看/发表评论下载PDF阅读器 相关附件：版权转让声明书修改说明 -->