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来那替尼的合成 被引量：4

Synthesis of Neratinib
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摘要 对羟基苯甲酸甲酯经硝化、还原、乙酰化及醚化制得3-乙酰胺基-4-乙氧基苯甲酸甲酯(7),7再经硝化、还原、缩合、环合、氯代等反应制得关键中间体3-氰基-4-氯-6-乙酰胺基-7-乙氧基喹啉(12),12与3-氯-4-(吡啶-2-甲氧基)苯胺缩合并脱去乙酰基后再和4-二甲胺基巴豆酰氯反应制得来那替尼,总收率约29%。 Neratinib was synthesized from methyl 4-hydroxybenzoate by nitration, reduction, acetylation, etherification, nitration, reduction, condensation with trans-3- （dimethylamino） acrylonitrile, cyclization and chlorination to give 6- （acetylamino） -4-chloro-3-cyano-7-ethoxyquinoline （12）, which was subjected to condensation with 3-chloro-4- （2-pyridinylmethoxy） aniline, deprotection and then acylation with 4-dimethylamino-2-butenoyl chloride with an overall yield of about 29 %.
作者 陈峰 张生平 王佩倍 李月珍 赖宜生
机构地区 中国药科大学新药研究中心 中国药科大学理学院有机化学教研室
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2014年第8期701-705,共5页 Chinese Journal of Pharmaceuticals
关键词 来那替尼 EGFR抑制剂 抗肿瘤药 合成 neratinib EGFR inhibitor anticancer agent synthesis
分类号 R978.7 [医药卫生—药品]
  • 相关文献

参考文献10

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二级参考文献30

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共引文献2

同被引文献14

  • 1杜鼎,方建新.具有生物活性的喹啉类化合物的最新进展[J].有机化学,2007,27(11):1318-1336. 被引量：35
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  • 10刘宝,尤启冬,李志裕.3-氰基-7-喹啉酰胺衍生物的合成和生物活性研究[J].药学学报,2009,44(8):879-884. 被引量：7

引证文献4

二级引证文献2

中国医药工业杂志
2014年 第8期

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