期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

达沙替尼合成综述

A Review of the Synthesis of Dasatinib
下载PDF
导出
摘要 达沙替尼是络氨酸激酶抑制剂,用于治疗白血病。本文以中间体2-氨基-N-(2-氯-6-甲基苯基)-5-噻唑甲酰胺(7)为中心对达沙替尼的合成路线进行阐述,并对合成路线进行初步评价。 Dasatinib,a tyrosine kinase inhibitor,is used to treat leukemia.In this article,the synthetic route of dasatinib is reviewed with the intermediate 2-amino-N-(2-chloro-6-methylphenyl)-5-thiazolecarboxamide(7)focus.And the synthetic routes are preliminarily evaluated.
作者 梁根浩 LIANG Gen-hao(Department of Pharmacy,West Anhui Health Vocational College,Liuan,Anhui 237000,China)
机构地区 皖西卫生职业学院药学系
出处 《浙江化工》 CAS 2020年第4期13-15,共3页 Zhejiang Chemical Industry
关键词 达沙替尼 合成路线 2-氨基-N-(2-氯-6-甲基苯基)-5-噻唑甲酰胺 dasatinib synthetic routes 2-amino-N-(2-chloro-6-methylphenyl)-5-thiazolecarboxamide
分类号 TQ463 [化学工程—制药化工]
  • 相关文献

参考文献10

二级参考文献49

  • 1黄胜炎（摘）.国外新批准上市的药物新制剂新剂型（108）[J].中国制药信息,2006,22(12):25-26. 被引量：1
  • 2Lombardo L J, Lee FY, Chen P, et al. Discovery of N-(2- chloro-6-methylphenyl) -2- (6- (4- (2-hydroxylethyl) - piperazin- 1-yl)-2-methylpyrimidin-4-ylamino) thiazole- 5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays [J]. J Med Chem, 2004, 47 (27) : 6658-6661.
  • 3Chen BC, Droghini R, Lajeunesse J, et al. Process for preparing 2-aminothizole-5-aromatic carboxamides as kinase inhibitors: US, 20060004067 [P]. 2006-01-05. (CA 2006, 144: 108343)
  • 4Zhao RL, Gove S, Sundeen JE, et al. A new facile synthesis of 2-aminothiazole-5-carboxylates [J]. Tetrahedron Lett, 2001, 42 (11) : 2101-2102.
  • 5Das J, Padmanabha R, Chen P, et al. Cyclic protein tyrosine kinase inhibitors: US, 20040054186 [P]. 2004-03-18. (CA, 2004, 140: 253556)
  • 6Fernandez F, Garcia-Mera X, Morales M, et al. A short, efficient synthesis of substituted uracil: an indane carbocyclic nucleoside [J]. Synthesis, 2001, (2) : 239-242.
  • 7Das J, Chen P, Norris D, et al. 2-Aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6- methylphenyl) -2- [ [6- [4- (2-hydroxyethyl) -1-piperazinyl] - 2-methyl-4-pyrimidinyl] amino] - 1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor [J]. J Med Chem, 2006, 49 (23) : 6819-6832.
  • 8Mclntyre JA, Castaner J, Bayes M. Dasatinib: Treatment of leukemia treatment of solid tumors Bcr-Abl and Src kinase inhibitor [J]. Drug Future, 2006, 31 (4): 291-303.
  • 9Das J, Moquin RV, Lin J, et al. Discovery of 2-aminoheteroaryl-benzothiazole-6-anilides as potent p56^kk inhibitors [J]. Bioorg Med Chem Lett, 2003, 13 (15) : 2587-2590.
  • 10Wityak J, Das J, Moquin RV, et al. Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56^Lck [J]. Bioorg Med Chem Lett, 2003, 13 (22) : 4007-4010.

共引文献27

浙江化工
2020年 第4期

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部