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| 卡奈替尼的合成工艺改进 | |
| 引用本文： | 刘剑峰,韩建奎,侯桂华,徐文方. 卡奈替尼的合成工艺改进[J]. 齐鲁药事, 2011, 30(10): 559-561 |
| 作者姓名： | 刘剑峰 韩建奎 侯桂华 徐文方 |
| 作者单位： | 1. 山东大学齐鲁医院,山东济南,250012 2. 山东大学医学院,山东济南,250012 3. 山东大学药学院,山东济南,250012 |
| 摘 要： | 目的改进抗肿瘤药物卡奈替尼的合成工艺。方法以2-氨基-4-氟苯甲酸和乙酸甲脒为起始原料,经环合、硝化、氯化、取代、氢化、酰化等反应制得抗肿瘤药物卡奈替尼。结果目标化合物的结构经1H-NMR谱和质谱确证。总收率为23.4%,比文献收率提高了17.2%。结论改进后的方法操作简便,有利于工业化生产。 |
| 关 键 词： | 2-氨基-4-氟苯甲酸 乙酸甲脒 卡奈替尼 抗肿瘤药 |
Improved synthesis of canertinib |
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| LIU Jian-feng,HAN Jian-kui,HOU Gui-hua,XU Wen-fang. Improved synthesis of canertinib[J]. qilu pharmaceutical affairs, 2011, 30(10): 559-561 | |
| Authors: | LIU Jian-feng HAN Jian-kui HOU Gui-hua XU Wen-fang |
| Affiliation: | LIU Jian-feng1,HAN Jian-kui1,HOU Gui-hua2,XU Wen-fang3(1.Qilu Hospital of Shandong University,Jinan 250012,China,2.School of Medicine,Shandong University,3.School of Pharmaceutical Sciences,China) |
| Abstract: | Objective To improve the synthetic procedure of canertinib.Methods Canertinib was synthesized from 2-amino-4-fluorobenzoic acid and formamidine acetate via cyclization,nitration,chlorinationb,substitution,hydrogenize,acylation,etc.Results The structure of target compound was confirmed by 1H-NMR,MS and the overall yield was 23.4%.Compared with the reported method,the overall yield was improved by 17.2%.Conclusion This synthetic process was suitable for industrial preparation. |
| Keywords: | 2-amino-4-fluorobenzoic acid Formamidine acetate Canertinib Antitumor |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ | |