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【结 构 式】 
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【药物名称】 【化学名称】N-(5-Phenyloxazol-2-yl)isoquinolin-6-amine 【CA登记号】 【 分 子 式 】C18H13N3O 【 分 子 量 】287.32381 |
【开发单位】Bristol-Myers Squibb (Originator) 【药理作用】IMMUNOMODULATING AGENTS, Treatment of Autoimmune Diseases, Treatment of Transplant Rejection, Inosine 5'-Monophosphate Dehydrogenase (IMPDH) Inhibitors |
合成路线1
Treatment of 6-aminoisoquinoline (I) with 1,1'-thiocarbonyldi-2(1H)-pyridone (II) provides the isothiocyanate (III). Subsequent condensation of (III) with 2-azidoacetophenone (IV) in the presence of triphenylphosphine affords the title oxazole derivative.
| 【1】 Chen, P.; Norris, D.; Haslow, K.D.; Dhar, T.G.M.; Pitts, W.J.; Watterson, S.H.; Cheney, D.L.; Bassolino, D.A.; Fleener, C.A.; Rouleau, K.A.; Hollenbaugh, D.L.; Townsend, R.M.; Barrish, J.C.; Iwanowicz, E.J.; Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors. Bioorg Med Chem Lett 2003, 13, 7, 1345. |
| 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) | 64245 | 6-isoquinolinamine; 6-isoquinolinylamine | C9H8N2 | 详情 | 详情 | |
| (II) | 61696 | 1-{[2-oxo-1(2H)-pyridinyl]carbothioyl}-2(1H)-pyridinone | C11H8N2O2S | 详情 | 详情 | |
| (III) | 64246 | 6-isothiocyanatoisoquinoline; 6-isoquinolinyl isothiocyanate | C10H6N2S | 详情 | 详情 | |
| (IV) | 26720 | 2-azido-1-phenyl-1-ethanone | C8H7N3O | 详情 | 详情 |
Extended Information