| 抗肿瘤新药琥珀酸瓦他拉尼合成工艺改进 |
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| 引用本文： | 张秋荣,朱楠,曹运华,王盟盟,杨志敏,季聪慧,杨志华,刘宏民. 抗肿瘤新药琥珀酸瓦他拉尼合成工艺改进[J]. 中南药学, 2011, 9(9): 655-657. DOI: 10.3969/j.issn.1672-2981.2011.09.005 |
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| 作者姓名： | 张秋荣 朱楠 曹运华 王盟盟 杨志敏 季聪慧 杨志华 刘宏民 |
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| 作者单位： | 郑州大学药学院,郑州,450001 |
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| 基金项目： | 郑州大学大学生创新性实验计划项目基金资助 |
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| 摘 要： | 目的优化琥珀酸瓦他拉尼的合成工艺。方法以苯并呋喃酮为原料,与4-吡啶甲醛缩合后,依次经过重排、取代、成盐反应合成了琥珀酸瓦他拉尼。结果琥珀酸瓦他拉尼的总收率32.9%,高于文献报道的收率22.2%。结论改进后的工艺,缩短了反应时间,操作简单,适合工业化生产。
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| 关 键 词： | 琥珀酸瓦他拉尼 抗肿瘤药物 合成工艺 |
Synthesis of a novel antitumor agent:vatalanib succinate |
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| ZHANG Qiu-rong,ZHU Nan,CAO Yun-hua,WANG Meng-meng,YANG Zhi-min,JI Cong-hui,YANG Zhi-hua,LIU Hong-min. Synthesis of a novel antitumor agent:vatalanib succinate[J]. Central South Pharmacy, 2011, 9(9): 655-657. DOI: 10.3969/j.issn.1672-2981.2011.09.005 |
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| Authors: | ZHANG Qiu-rong ZHU Nan CAO Yun-hua WANG Meng-meng YANG Zhi-min JI Cong-hui YANG Zhi-hua LIU Hong-min |
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| Affiliation: | ZHANG Qiu-rong,ZHU Nan,CAO Yun-hua,WANG Meng-meng,YANG Zhi-min,JI Cong-hui,YANG Zhi-hua,LIU Hong-min(College of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001) |
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| Abstract: | Objective To optimize the synthesis of vatalanib succinate.Methods Vatalanib succinate was synthesized by condensing 2H-bezofuran-3-one with 4-pyridinecarboxaldyde,and followed by rearrangement,substitution and salt formation.Results The total yield was 32.9%,far more than 22.2%,as reported in the literature.Conclusion The process is improved with high yield,and the reaction condition is mild,suitable for industrial production. |
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| Keywords: | vatalanib succinate antitumor agents synthesis |
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