| 吉非替尼的合成工艺改进 |
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| 引用本文： | 杜鹏,潘春跃,彭东明. 吉非替尼的合成工艺改进[J]. 中国新药杂志, 2006, 15(21): 1849-1851 |
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| 作者姓名： | 杜鹏 潘春跃 彭东明 |
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| 作者单位： | 中南大学化学化工学院,长沙,410083 |
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| 摘 要： | 目的：合成吉非替尼。方法：以4，5-双甲氧基邻氨基苯甲酸为起始原料，经过环合、脱甲基、乙酰化、氯化、氨基化、水解、缩合等步骤后得吉非替尼。结果：以4，5-双甲氧基邻氨基苯甲酸计，总收率为11.6％。目标产物经红外光谱、核磁共振氢谱、元素分析确证其结构；该工艺在分离过程中不需过柱。结论：本方法条件温和，操作简单，适合于工业化生产。
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| 关 键 词： | 吉非替尼 表皮生长因子受体 药物合成 |
| 文章编号： | 1003-3734（2006）21-1849-03 |
| 收稿时间： | 2006-06-02 |
| 修稿时间： | 2006-06-02 |
An improved synthetic process for gefitinib |
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| DU Peng,PAN Chun-yue,PENG Dong-ming. An improved synthetic process for gefitinib[J]. Chinese Journal of New Drugs, 2006, 15(21): 1849-1851 |
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| Authors: | DU Peng PAN Chun-yue PENG Dong-ming |
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| Affiliation: | College of Chemistry and Engineering, Central South University, Changsha 410083, China |
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| Abstract: | Objective: To synthesize gefitinib. Method; Starting from 4, 5-dirnethoxy-2-amino-benzoic acid, the target compound was obtained via several steps including cyclization, demethylation, acetylation, chlorination, ammoniated, hydrolysis and condensation. Result; A total yield of gefitinib was 11.6%. The structure was confirmed by element analysis, IR and 1H-NMR. Conclusion: This easily manipulated synthetic process without column chromatography is worthy to have further pilot manufacture. |
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| Keywords: | gefitinib epidermal growth factor receptor (EGFR) drug synthesis |
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