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【结 构 式】 
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【药物名称】 【化学名称】4-(Benzyloxy)-2-(4-fluorophenyl)-3-(4-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-6-amine 【CA登记号】215307-20-3 【 分 子 式 】C25H19FN4O 【 分 子 量 】410.45478 |
【开发单位】R.W. Johnson (Originator) 【药理作用】Antiarthritic Drugs, Antipsoriatics, DERMATOLOGIC DRUGS, GASTROINTESTINAL DRUGS, Irritable Bowel Syndrome, Agents for, TREATMENT OF MUSCULOSKELETAL & CONNECTIVE TISSUE DISEASES, p38 Protein Kinase Inhibitors, TNF-alpha Production Inhibitors |
合成路线1
Sylilated hydroxymethylpyridine (I) was condensed with ethyl 4-fluorobenzoate (II) in the presence of sodium hemamethyldisilazide to produce the silyloxy ketone (III). Subsequent reaction of (III) with diaminopyrimidine (IV) in the presence of H2SO4 in refluxing dimethoxyethane yielded the title pyrrolopyridine.
| 【1】 Henry, J.R.; Rupert, K.C.; Dodd, J.H.; Turchi, I.J.; Wadsworth, S.A.; Cavender, D.E.; Schafer, P.H.; Siekierka, J.J.; Potent inhibitors of the MAP kinase p38. Bioorg Med Chem Lett 1998, 8, 23, 3335. |
| 【2】 Dodd, J.H.; Henry, J.R.; Rupert, K. (Ortho-McNeil Pharmaceutical, Inc.); Substd. pyrrolopyridines useful in the treatment of inflammatory diseases. WO 9847899 . |
| 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) | 22829 | 4-([[tert-butyl(dimethyl)silyl]oxy]methyl)pyridine; tert-butyl(dimethyl)silyl 4-pyridinylmethyl ether | C12H21NOSi | 详情 | 详情 | |
| (II) | 22830 | ethyl 4-fluorobenzoate | 451-46-7 | C9H9FO2 | 详情 | 详情 |
| (III) | 22831 | 2-[[tert-butyl(dimethyl)silyl]oxy]-1-(4-fluorophenyl)-2-(4-pyridinyl)-1-ethanone | C19H24FNO2Si | 详情 | 详情 | |
| (IV) | 26862 | 4-(benzyloxy)-2,6-pyridinediamine | C12H13N3O | 详情 | 详情 |
Extended Information