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帕唑帕尼盐酸盐的合成 被引量：4

Synthesis of Pazopanib Hydrochloride
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摘要 目的合成帕唑帕尼盐酸盐并改进合成工艺。方法以3-甲基-6-硝基-1H-吲唑为起始原料,经N-甲基化、还原、亲核取代、成盐等反应制得帕唑帕尼盐酸盐。结果所得产物经核磁共振氢谱、质谱、红外等确证其结构。结论该工艺原料易得,方法简便,适合工业化生产。 OBJECTIVE To synthesis pazopanib hydrochloride and optimize the process.METHODS Pazopanib hydrochloride was synthesized from 3-methyl-6-nitro-1H-indazole via N-methylation,reduction,nucleophilic substitution and salification.RESULTS Chemical structure of pazopanib hydrochloride was confirmed by 1H-NMR,MS and IR.CONCLUSION The method is suitable for industry.
作者 祁浩飞 王兵 刘冰妮 刘默 刘登科
机构地区 天津工业大学 天津药物研究院天津市新药设计与发现重点实验室
出处 《中国现代应用药学》 CAS CSCD 北大核心 2011年第1期58-59,66,共3页 Chinese Journal of Modern Applied Pharmacy
基金 天津市自然科学基金重点项目(10JCZDJC21900)
关键词 帕唑帕尼盐酸盐 抗肿瘤药 合成 pazopanib hydrochloride antitumor agent synthesis
分类号 TQ460.6 [化学工程—制药化工]
  • 相关文献

参考文献6

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  • 2汤仲明.2009年美国FDA批准新药介绍[J].国际药学研究杂志,2010,37(1):8-15. 被引量：12
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共引文献11

同被引文献24

  • 1Sloan B, Scheinfeld N S. Pazopanib, a VEGF receptor tyrosine kinase inhibitor for cancer therapy [J]. Curr Opin Investig Drugs, 2008, 9 (12): 1 324-1 335.
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  • 7Babu S, Dagnino R J, Ouellette M,et ol. Methods for preparing in- dazole compounds [ P ]. WO : 2006048745, 2006-05 - 11.
  • 8Harris PA, BOLOOR A, CHEUNG M, et al. Discovery of 5-[ [4- [ 2,3-dimethyl-2H-indazol-6-yl )methylamino ] -2-pyrimidinyl ] amino]-2-methyl-benzenesuffonamide (pazopanib),a nobel and potent vascular endothelial growth factor receptor inhibitor [ J ]. J Med.Chem., 2008,51 (7):4632-4640.
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引证文献4

二级引证文献9

中国现代应用药学
2011年 第1期

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