| 引用本文: | 高雅莉,倪欣,马俊杰.新型小分子血管内皮细胞生长因子受体抑制剂呋喹替尼的合成研究[J].中国现代应用药学,2020,37(24):2962-2965. |
| GAO Yali,NI Xin,MA Junjie.Study on Synthesis of Novel Small Molecule Vascular Endothelial Growth Factor Receptor Inhibitor Fruquintinib[J].Chin J Mod Appl Pharm(中国现代应用药学),2020,37(24):2962-2965. |
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| 摘要: |
| 目的 研究新型小分子血管内皮细胞生长因子受体抑制剂呋喹替尼的制备工艺。方法 以4-甲氧基-2-羟基苯甲醛为原料，经亲核取代、水解、分子内Perkin、傅克酰基化、脱甲基化、酰胺化和亲核取代反应制备目标产物呋喹替尼。结果 中间体和目标产物呋喹替尼的结构经1H-NMR、13C-NMR和ESI-MS确证。结论 整条路线避免了使用氯化亚砜带来的废气排放问题，使实验操作更加安全，目标产物的纯化采用结晶析出的方法，后处理操作简单高效。 |
| 关键词: 抗肿瘤 呋喹替尼 合成工艺 |
| DOI：10.13748/j.cnki.issn1007-7693.2020.24.003 |
| 分类号:R914.4 |
| 基金项目:国家自然科学基金项目（81602970）；福建医科大学启航基金项目（2019QH1123）；泉州市科技计划项目（2018C074R） |
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| Study on Synthesis of Novel Small Molecule Vascular Endothelial Growth Factor Receptor Inhibitor Fruquintinib |
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GAO Yali1, NI Xin2, MA Junjie2
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1.Department of Pharmacy, The Second Affiliated Hospital of Fujian Medical University, Quanzhou 362000, China;2.School of Medicine, Huaqiao University, Quanzhou 362000, China
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| Abstract: |
| OBJECTIVE To study the preparation process of novel small molecule vascular endothelial growth factor receptor inhibitor fruquintinib. METHODS The target compound furaquininib was prepared via nucleophilic substitution, hydrolysis, intramolecular Perkin, Friedel-Crafts acylation, demethylation, amidation and nucleophilic substitution reaction by using 4-methoxy-2-hydroxybenzaldehyde as a raw material. RESULTS The structures of the intermediates and target compound fruquintinib were confirmed by 1H-NMR, 13C-NMR and ESI-MS. CONCLUSION The whole route avoids the exhaust emission problems caused by the use of thionyl chloride, and makes the experimental operation safer. In addition, the target compound is purified by crystallization, which makes workup simpler and more efficient. |
| Key words: antitumor fruquintinib synthesis process |
