| 3-氯-4-(3-氟苄氧基)苯胺的合成 |
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| 引用本文： | 李连连,张庆文. 3-氯-4-(3-氟苄氧基)苯胺的合成[J]. 中国现代应用药学, 2011, 28(3): 245-246 |
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| 作者姓名： | 李连连 张庆文 |
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| 作者单位： | 上海医药工业研究院化学制药部，上海 200437;上海医药工业研究院化学制药部，上海 200437 |
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| 基金项目： | 国家“重大新药创制”科技重大专项(2009ZX09301-007)；上海市基础研究重点项目(09JC1413200) |
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| 摘 要： | 目的开发一条适合产业化的3-氯-4-（3-氟苄氧基）苯胺的合成工艺路线。方法以间氟氯苄和2-氯-4-硝基苯酚为原料，依次经碳酸钾存在下的缩合反应、铁粉／氯化铵还原得到3-氯-4-（3-氟苄氧基）苯胺。结果总收率为82％。所得产物经TLC、熔点和核磁共振氢谱表征，具有高纯度。结论本方法原料价廉易得，操作简便，环境污染更小，预期适合工业化生产。
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| 关 键 词： | 3-氯-4-（3-氟苄氧基）苯胺 拉帕替尼 合成 间氟氯苄 2-氯-4-硝基苯酚 |
| 收稿时间： | 2010-06-23 |
Practical Synthesis of 3-Chloro-4-(3-fluorobenzyloxy) aniline |
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| LI Lianlian and ZHANG Qingwen. Practical Synthesis of 3-Chloro-4-(3-fluorobenzyloxy) aniline[J]. The Chinese Journal of Modern Applied Pharmacy, 2011, 28(3): 245-246 |
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| Authors: | LI Lianlian and ZHANG Qingwen |
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| Affiliation: | Division of Medicinal Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China;Division of Medicinal Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China |
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| Abstract: | OBJECTIVE To develop a practical process for 3-chloro-4-(3-fluorobenzyloxy)aniline. METHODS 3-Chloro- 4-(3-fluorobenzyloxy)aniline was synthesized from 1-(chloromethyl)-3-fluorobenzene and 2-chloro-4-nitrophenol via condensation in the presence of potassium carbonate, followed by reduction with Fe/NH4Cl. RESULTS The overall yield of this process was 82%. The target product was characterized by TLC, melting point and 1H-NMR. CONCLUSION This synthetic process features are cheap and readily available starting materials, robustness, less waste burden, thus should be amenable to industrial production. |
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| Keywords: | 3-chloro-4-(3-fluorobenzyloxy) aniline lapatinib synthesis 1-(chloromethyl)-3-fluorobenzene 2-chloro-4- nitrophenol |
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