| 抗血吸虫药物吡喹酮的新合成路线 |
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| 引用本文： | 程训官,郑小红,夏铸,张昕宇,王宇,余瑜. 抗血吸虫药物吡喹酮的新合成路线[J]. 重庆医科大学学报, 2011, 36(10): 1208-1210 |
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| 作者姓名： | 程训官 郑小红 夏铸 张昕宇 王宇 余瑜 |
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| 作者单位： | 重庆医科大学药学院药物化学教研室、重庆市药物工程研究中心,重庆,400016 |
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| 基金项目： | 国家自然科学基金资助项目(编号:30772595、30171070、30371632); 科技重大专项资助项目(编号:2010ZX09401-306-1-1); 重庆市科委攻关资助项目(编号:20021425); 重庆市教委资助项目(编号:20021804) |
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| 摘 要： | 目的:构建一条绿色、环保且能适合工业化生产抗血吸虫药物吡喹酮的新合成路线.方法:以苯乙胺为原料,用氯乙酰氯酰化,再用邻苯二甲酰亚胺钾氨基化反应,在P2O5作用下经Bischler-Napieralski环合反应制得N-[(1-亚甲基)-3,4-二氢异喹啉]邻苯二甲酰亚胺,经肼解和还原得到1-氨甲基-1,2,3,4-四氢...
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| 关 键 词： | 吡喹酮 合成 环合 四氢异喹啉 血吸虫病 |
A new and efficient method for the synthesis of praziquantel,an antischistosomiasis drug |
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| CHENG Xun-guan , ZHENG Xiao-hong , XIA Zhu , ZHANG Xin-yu , WANG Yu , YU Yu. A new and efficient method for the synthesis of praziquantel,an antischistosomiasis drug[J]. Journal of Chongqing Medical University, 2011, 36(10): 1208-1210 |
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| Authors: | CHENG Xun-guan ZHENG Xiao-hong XIA Zhu ZHANG Xin-yu WANG Yu YU Yu |
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| Affiliation: | CHENG Xun-guan,ZHENG Xiao-hong,XIA Zhu,ZHANG Xin-yu,WANG Yu,YU Yu(Department of Pharmacochemistry,College of Pharmacy,Chongqing Medical University,Chongqing Engineering Research Center for Drug) |
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| Abstract: | Objective:To establish an industrial synthetic route for praziquantel.Methods:Praziquantel was synthesized with an overall yield of about 32.8% from phenylethylamine via acylation,amination with phthalimide potassium,Bischler-Napieralski cyclization,hydrazine solution,reduction,followed by acylation with cyclohexanecarboxylic acid chloride and chloroacetyl chloride,and then cyclization.Results:Target structures werecharacterized by IR,UV and MS.Conclusion:The method has the advantages of convenient operatio... |
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| Keywords: | praziquantel synthesis cyclization tetrahydroisoquinoline schistosomiasis |
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