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抗肿瘤药物dacomitinib的合成工艺

程海博, 徐斌, 张惠斌, 周金培

程海博, 徐斌, 张惠斌, 周金培. 抗肿瘤药物dacomitinib的合成工艺[J]. 中国药科大学学报, 2014, 45(2): 165-169. DOI: 10.11665/j.issn.1000-5048.20140206
引用本文: 程海博, 徐斌, 张惠斌, 周金培. 抗肿瘤药物dacomitinib的合成工艺[J]. 中国药科大学学报, 2014, 45(2): 165-169. DOI: 10.11665/j.issn.1000-5048.20140206
CHENG Haibo, XU Bin, ZHANG Huibin, ZHOU Jinpei. Synthetic process of antitumor drug dacomitinib[J]. Journal of China Pharmaceutical University, 2014, 45(2): 165-169. DOI: 10.11665/j.issn.1000-5048.20140206
Citation: CHENG Haibo, XU Bin, ZHANG Huibin, ZHOU Jinpei. Synthetic process of antitumor drug dacomitinib[J]. Journal of China Pharmaceutical University, 2014, 45(2): 165-169. DOI: 10.11665/j.issn.1000-5048.20140206

抗肿瘤药物dacomitinib的合成工艺

Synthetic process of antitumor drug dacomitinib

  • 摘要: 对抗肿瘤药物dacomitinib合成工艺进行改进。以4-氟-2-氨基苯甲酸为原料,经环合、硝化、卤代、偶联以及还原等反应,得到dacomitinib。目标化合物经质谱、核磁共振氢谱确证化学结构。以11步反应总收率36.1%,单步收率75%~90%合成目标化合物,无需特殊试剂和复杂分离纯化过程,降低了成本,优化了反应条件,操作更加简单实用。
    Abstract: This paper describes a practical process for the preparation of antitumor drug dacomitinib. It was synthesized by eleven steps from 2-amino-4-fluorobenzoic acid by cyclization, nitration, halogenation, coupling and reduction reactions with the total yield of 36. 1% and one-step yield of 75%-90 %. The intermediates and target compound were characterized by NMR and MS. This practical synthetic process of dacomitinib highlights comparable yield, low-cost, optimized condition and easier purification.
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出版历程
  • 刊出日期:  2014-04-24

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