| 拉帕替尼新中间体的合成 |
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| 引用本文： | 郭卿,李雁武,任学状,袁建勇.拉帕替尼新中间体的合成[J].化学通报,2017,80(4):392-395. |
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| 作者姓名： | 郭卿 李雁武 任学状 袁建勇 |
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| 作者单位： | 重庆医科大学药学院,重庆医科大学药学院,重庆医科大学药学院,重庆医科大学药学院 |
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| 摘 要： | 通过使用市售的5-溴糠醛与2-甲磺酰基乙胺进行亲和加成得到席夫碱,该席夫碱通过还原氢化、氨基保护和与硼酸酯反应,得到一种拉帕替尼的新中间体5-((苄基(2-(甲基磺酰基)乙基)氨基)甲基)呋喃-2-基硼酸,四步反应总收率为66.32%。
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| 关 键 词： | 拉帕替尼 有机镁络合物 合成 |
| 收稿时间： | 2016/3/19 0:00:00 |
| 修稿时间： | 2016/6/17 0:00:00 |
Synthesis of a novel intermediate of lapatinib |
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| Guo Qing,Li Yanwu,Ren Xuezhuang and Yuan Jianyong.Synthesis of a novel intermediate of lapatinib[J].Chemistry,2017,80(4):392-395. |
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| Authors: | Guo Qing Li Yanwu Ren Xuezhuang and Yuan Jianyong |
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| Institution: | Pharmacy college,Chongqing Medical University,Pharmacy college,Chongqing Medical University,Pharmacy college,Chongqing Medical University,Pharmacy college,Chongqing Medical University |
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| Abstract: | A schiff base was synthesized from commercially available 5-bromo- 2-furaldehyde and 2-(Methylsulfonyl)ethaneamine in the nucleophilicSadditionalSreaction.A novel intermediate of lapatinib was synthesized from the schiff base by a reaction with Sldium borohydride and the amino protection reaction in 66.32% overall yield. |
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| Keywords: | Lapatinib Organomagnesium complex synthesis |
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