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凡德他尼重要中间体7-羟基-4-(4-溴-2-氟苯胺基)-6-甲氧基喹唑啉的合成 被引量：2

Synthesis of 4-(4-Bromo-2-fluoranilino)-7-hydroxy-6-methoxyquinazoline
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摘要 以4-羟基-3-甲氧基苯甲酸为起始原料,经过酯化、保护羟基、硝化、还原、环合、氯化、与4-溴-2-氟苯胺缩合、钯碳脱保护合成凡德他尼(Vandetanib)的重要中间体7-羟基-4-(4-溴-2-氟苯胺基)-6-甲氧基喹唑啉,总收率42.6%。 4-（4-Bromo-2-fluoranilino）-7-hydroxy-6-methoxyquinazoline is a key intermediate for vandetanib,which is an antagonist of the vascular endothelial growth factor receptor（VEGFR）and the epidermal growth factor receptor（EGFR）.The title compound was obtained from 4-hydroxy-3-methoxybenzoic acid in several steps in an overall yield of 42.6%.
作者 李龙 王福东 李勇 李荣东
机构地区 湖南中医药大学药学院药学基础教学实验中心
出处 《精细化工中间体》 CAS 2011年第6期41-43,共3页 Fine Chemical Intermediates
基金 2008年湖南省教育厅大学生研究性学习和创新性试验计划项目
关键词 合成 凡德他尼 中间体 酪氨酸激酶抑制剂 synthesis Vandetanib intermediate kinase inhibitor
分类号 R736.1 [医药卫生—肿瘤]
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参考文献8

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二级参考文献6

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共引文献6

同被引文献13

  • 1李铭东,曹萌,吉民.盐酸埃洛替尼的合成[J].中国医药工业杂志,2007,38(4):257-259. 被引量：10
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  • 6吉民;孙敏;吴晓晴.2-(4-氨基喹唑啉基)苯并[d]噻唑类衍生物及其用途[P]中国,1017010182010.
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引证文献2

精细化工中间体
2011年 第6期

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