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YE Lianbao, WU Jieyu, YANG Jiebo, LUO Jiaoyan, HU Qiaohong. Synthesis of the related substances of gefitinib[J]. Journal of China Pharmaceutical University, 2014, 45(6): 667-670. DOI: 10.11665/j.issn.1000-5048.20140608
Citation: YE Lianbao, WU Jieyu, YANG Jiebo, LUO Jiaoyan, HU Qiaohong. Synthesis of the related substances of gefitinib[J]. Journal of China Pharmaceutical University, 2014, 45(6): 667-670. DOI: 10.11665/j.issn.1000-5048.20140608
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Synthesis of the related substances of gefitinib

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    • Abstract
  • To strengthen the quality control over gefitinib and establish its quality criterion, four related substances of gefitinib were identified based on the synthetic route and synthesized, and their structures were confirmed by 1H NMR and MS. These substances were 4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-ol( A ), N-(3-chloro-4-fluorophenyl)-6, 7-dimethoxyquinazolin-4-amine( B ), 4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propylamino)ethanol( C )and N-(3, 4-dichlorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine( D ).
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    • References (8)
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    Zhang H,Zhao JH,Wang H.Synthesis of 4-(3-chloro-4-fluoro-phenylamineo)-7-methoxy- 6-(3-morpholin-4-yl-propoxy)-quinazoline: CN,200810122242.2[P].2009-04-08.
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