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【结 构 式】

【药物名称】Pazopanib Hydrochloride, GW-786034

【化学名称】5-[4-[N-(2,3-Dimethyl-2H-indazol-6-yl)-N-methylamino]pyrimidin-2-ylamino]-2-methylbenzenesulfonamide hydrochloride

【CA登记号】635702-64-6, 444731-52-6 (as free base)

【 分 子 式 】C21H24ClN7O2S

【 分 子 量 】473.9799

【开发单位】GlaxoSmithKline (US).

【药理作用】Oncolytic, Angiogenesis Inhibitor, VEGFR-2 Tyrosine Kinase Inhibitor

合成路线1

 

1 Arundathy NP, Bonnie FW, Albert BS, et al. 2009. Cancer treatment method. US 064577; US 20090005406A1.
2 Hopf C. 2008. Methods for the identification of JAK kinase interacting molecules and for the purification of JAK kinases. EP 2058307A1.
3 Richard AB, Mark L, William H.2008. Treatment method. US 064577; US 20080293691A1.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 67351 2-Ethylaniline;o-Amino ethylbenzene;2-ethylbenzenamine 578-54-1 C8H11N 详情 详情
(II) 67352 2-ethyl-5-nitroaniline 20191-74-6 C8H10N2O2 详情 详情
(III) 67353 3-methyl-6-nitro-2H-indazole 6494-19-5 C8H7N3O2 详情 详情
(IV) 67354 2,3-dimethyl-6-nitro-2H-indazole 444731-73-1 C9H9N3O2 详情 详情
(V) 67355 2,3-dimethyl-2H-indazol-6-amine 444731-72-0 C9H11N3 详情 详情
(VI) 67356 N-(2-chloropyrimidin-4-yl)-2,3-dimethyl-2H-indazol-6-amine 444731-74-2 C13H12ClN5 详情 详情
(VII) 67357 N-(2-chloropyrimidin-4-yl)-N,2,3-trimethyl-2H-indazol-6-amine 444731-75-3 C14H14ClN5 详情 详情
(VIII) 67358 2-amino-5-methylbenzenesulfonamide   C7H10N2O2S 详情 详情

合成路线2

 

1 Philip AH, Amogh B, Mui C, et al. 2008. Discovery of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl) amino [-2-pyrimidintl] amino]-2-methyl-benzenesulfonamide (Pazopanib). A novel and Potent Endothelial Growth Factor Receptor Inhibitor. J Med Chem, 51: 4632~4640.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 67351 2-Ethylaniline;o-Amino ethylbenzene;2-ethylbenzenamine 578-54-1 C8H11N 详情 详情
(II) 67352 2-ethyl-5-nitroaniline 20191-74-6 C8H10N2O2 详情 详情
(III) 59942 3-methyl-6-nitro-1H-indazole 6494-19-5 C8H7N3O2 详情 详情
(IV) 67354 2,3-dimethyl-6-nitro-2H-indazole 444731-73-1 C9H9N3O2 详情 详情
(V) 67355 2,3-dimethyl-2H-indazol-6-amine 444731-72-0 C9H11N3 详情 详情
(VI) 67356 N-(2-chloropyrimidin-4-yl)-2,3-dimethyl-2H-indazol-6-amine 444731-74-2 C13H12ClN5 详情 详情
(VII) 67357 N-(2-chloropyrimidin-4-yl)-N,2,3-trimethyl-2H-indazol-6-amine 444731-75-3 C14H14ClN5 详情 详情

合成路线3

 

1 陈燕,方正,韦萍.2010. 盐酸帕唑帕尼的合成。中国医药工业杂志,(5)41: 326~328.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 67351 2-Ethylaniline;o-Amino ethylbenzene;2-ethylbenzenamine 578-54-1 C8H11N 详情 详情
(II) 67352 2-ethyl-5-nitroaniline 20191-74-6 C8H10N2O2 详情 详情
(III) 67353 3-methyl-6-nitro-2H-indazole 6494-19-5 C8H7N3O2 详情 详情
(IV) 67354 2,3-dimethyl-6-nitro-2H-indazole 444731-73-1 C9H9N3O2 详情 详情
(V) 67359 2-ethylaniline hydrochloride   C9H11N3.HCl 详情 详情
(VI) 67356 N-(2-chloropyrimidin-4-yl)-2,3-dimethyl-2H-indazol-6-amine 444731-74-2 C13H12ClN5 详情 详情
(VII) 67357 N-(2-chloropyrimidin-4-yl)-N,2,3-trimethyl-2H-indazol-6-amine 444731-75-3 C14H14ClN5 详情 详情
Extended Information