| 阿巴卡韦中间体2-杂氮双环[2,2,1]庚-5-烯-3-酮的合成 |
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| 引用本文： | 陈灿,郭莉娜,李宏伟,侯仲轲. 阿巴卡韦中间体2-杂氮双环[2,2,1]庚-5-烯-3-酮的合成[J]. 精细化工中间体, 2006, 36(5): 36-38 |
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| 作者姓名： | 陈灿 郭莉娜 李宏伟 侯仲轲 |
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| 作者单位： | 湖南化工研究院,药物研究所,湖南,长沙,410007;华中师范大学,湖北,武汉,430079 |
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| 摘 要： | 采用一步法由对甲基苯亚磺酸钠与氯化氰及1,3-环戊二烯合成目标物2-杂氮双环[2,2,1]庚-5-烯-3-酮。反应条件为:n(对甲基苯亚磺酸钠)∶n(氯化氰)∶n(1,3-环戊二烯)=0.48∶1.05∶1,反应温度控制在15℃,反应7h,反应中控制pH=5,可得纯度为95%的产品,收率由文献报道的64%提高到78%。
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| 关 键 词： | 一步法 合成 2-杂氮双环[2 2 1]庚-5-烯-3-酮 |
| 文章编号： | 1009-9212(2006)05-0036-03 |
| 收稿时间： | 2006-07-12 |
| 修稿时间： | 2006-07-12 |
Synthesis of 2-Azabicyclo[2,2,1]hept-5-en-3-one as an Intermediate for Abacavir |
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| CHEN Can,GUO Li-na,LI Hong-wei,HOU Zhong-ke. Synthesis of 2-Azabicyclo[2,2,1]hept-5-en-3-one as an Intermediate for Abacavir[J]. Fine Chemical Intermediates, 2006, 36(5): 36-38 |
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| Authors: | CHEN Can GUO Li-na LI Hong-wei HOU Zhong-ke |
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| Affiliation: | 1. Institute of Pharmaceuticals, Hunan Research Institute of Chemical Industry, Changsha 410007, China; 2. Central China Normal University, Wuhan 430079, China |
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| Abstract: | 2-Azabicyclohept-5-en-3-one was synthesized from sodium-p-toluene sulfinate with cyanogens chloride and cyclopentadiene by one-pot process.The optimal conditions were as follow: the mole ratio of sodium-p-toluene sulfinate:cyanogens chloride:cyclopentadiene was 0.48∶1.05∶1,the reaction temperature 15℃,reaction time 5 h and pH of the reaction 5.Under these optimal conditions,the purity of product was 95%,and The yield was increased from 64% to 78%. |
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| Keywords: | one-pot process synthesis 2-azabicyclohept-5-en-3-one |
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