| N-（3-氯-4-（3-氟苯甲氧基）苯基）-6-碘喹唑啉-4-胺盐酸盐的合成 |
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| 引用本文： | 王武伟,江珂,李飞,张宏娟,王秀珍. N-（3-氯-4-（3-氟苯甲氧基）苯基）-6-碘喹唑啉-4-胺盐酸盐的合成[J]. 化工中间体, 2008, 4(11): 28-30 |
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| 作者姓名： | 王武伟 江珂 李飞 张宏娟 王秀珍 |
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| 作者单位： | 南京医科大学药学院,江苏,南京,210029 |
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| 摘 要： | 以2-氯-4-硝基苯酚为原料，经Williamson反应得3-氯-4-（3-氟苯甲氧基）硝基苯，硝基还原后与4-氯-6-碘喹唑啉缩合得到抗肿瘤药物拉帕替尼的重要中间体N-（3-氯-4-（3-氟苯甲氧基）苯基）-6-碘喹唑啉-4-胺盐酸盐，总收率约62％。中间体及目标产物结构经1HNMR和MS得以证实。
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| 关 键 词： | N-(3-氯-4-(3-氟苯甲氧基)苯基)-6-碘喹唑啉-4-胺 拉帕替尼 中间体 合成 |
Synthesis of N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine hydrochloride |
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| Wang Wuwei,Jiang Ke,Li Fei,Zhang Hongjuan,Wang Xiuzhen. Synthesis of N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine hydrochloride[J]. , 2008, 4(11): 28-30 |
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| Authors: | Wang Wuwei Jiang Ke Li Fei Zhang Hongjuan Wang Xiuzhen |
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| Affiliation: | Wang Wuwei Jiang Ke Li Fei Zhang Hongjuan Wang Xiuzhen (College of Pharmacy, Nanjing Medical University, Nanjing 210029) |
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| Abstract: | N-（3-chloro-4-（3-fluorobenzyloxy）phenyl）-6-iodoquinazolin-4-amine, the key inter- mediate of antitumor agent lapatinib, was synthesized from 2-chloro-4-nitrophenol via Williamson reaction to give 3-chloro-4-（3-fluorobenzyloxy）-nitroben- zene, followed by nitro reduction to produce the corresponding aromatic amino, which was subjected to reaction with 4-chloro-6-iodoquinazoline with an overall yield about 62%.The structures of the intermediates and the target compound were confirmed by 1HNMR and MS. |
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| Keywords: | N-（3-chloro-4-（3-fluorobenzyloxy）phenyl）-6-iodoquinazolin-4-amine lapatinib intermediate synthesis |
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