| 厄洛替尼的合成工艺改进 |
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| 引用本文： | 贺新昌,;高上婷,;霍文龙,;郑丽敏,;宋宏锐.厄洛替尼的合成工艺改进[J].中国药物化学杂志,2014(5):384-386. |
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| 作者姓名： | 贺新昌 ;高上婷 ;霍文龙 ;郑丽敏 ;宋宏锐 |
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| 作者单位： | [1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016; [2]沈阳五核生物科技有限公司,辽宁沈阳110043 |
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| 摘 要： | 目的研究和优化厄洛替尼的合成工艺。方法以3,4-二羟基苯甲酸乙酯和2-氯乙基甲醚为起始原料,经O-烷基化、硝化、还原、环合、卤代和N-烷基化6步反应制得厄洛替尼。结果总收率为56.8%(以3,4-二羟基苯甲酸乙酯计),纯度大于99%(HPLC法)。结论该合成路线工艺稳定、环境污染小、成本低,有利于工业化生产。
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| 关 键 词： | 厄洛替尼 合成工艺 抗肿瘤药 |
Improved synthesis of erlotinib |
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| HE Xin-chang;GAO Shang-ting;HUO Wen-long;ZHENG Li-min;SONG Hong-rui.Improved synthesis of erlotinib[J].Chinese Journal of Medicinal Chemistry,2014(5):384-386. |
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| Authors: | HE Xin-chang;GAO Shang-ting;HUO Wen-long;ZHENG Li-min;SONG Hong-rui |
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| Affiliation: | HE Xin-chang, GAO Shang-ting, HUO Wen-long, ZHENG Li-min, SONG Hong-rui ( 1. Key Laboratory of Structure-Based Drug Design and Discovery ( Shenyang Pharmaceutical University), Ministry of Education, Shenyang 110016, China; 2. Shenyang Wuhe Biotechnology Co. , Ltd. , Shenyang 110043, China) |
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| Abstract: | Edotinib, a in advanced non-small cell lung cancer GER1/EGFR tyrosinase inhibitors, for each category of non-small cell lung cancer patients was effective, not only to prolong survival of patients, but also to improve patient quality of life, so to optimize erlotinib synthetic route is very meaningful. Erlotinib was synthesized from ethyl 3,4-dihydroxybenzoate and 2-chloroether via O-alkylation, nitration, reduction, cyclization, chlorination and N-alkylation. Compared with the original document, a new synthetic route mainly in reaction time, temperature, solvent, various aspects was improved. Such as the reaction temperature increased, the reaction time reduced, etc. The total yield was 56. 8 % and the purity of the target product was 99% （HPLC）. The process was less pollution and low cost, which is suitable for industrial production. |
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| Keywords: | erlotinib synthesis process antitumor drug |
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