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【结 构 式】 
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【药物名称】SNJ-1558 【化学名称】N1-[1(S)-[2-(Dimethylamino)acetylhydrazonomethyl]-3-methylbutyl]-N2-(4-fluorophenylsulfonyl)-L-valinamide 【CA登记号】438003-89-5 【 分 子 式 】C21H34FN5O4S 【 分 子 量 】471.59863 |
【开发单位】Senju (Originator) 【药理作用】Alzheimer's Dementia, Treatment of , Anticataract Agents, Cerebrovascular Diseases, Treatment of, Cognition Disorders, Treatment of, Ischemic Stroke, Treatment of, NEUROLOGIC DRUGS, OCULAR MEDICATIONS, Ophthalmic Drugs, Stroke, Treatment of, mu-Calpain (Calpain-1) Inhibitors |
合成路线1
Swern oxidation of the sulfonyl dipeptide alcohol (I) in the presence of sulfur trioxide-pyridine complex and DMSO affords aldehyde (II). This is then condensed with (dimethylamino)acetohydrazide (III) to produce the target N-acyl hydrazone
| 【1】 Nakamura, M.; Inoue, J.; Exploration of peptidyl hydrazones as water-soluble calpain inhibitors. Bioorg Med Chem Lett 2002, 12, 12, 1603. |
| 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) | 57913 | (2S)-2-{[(4-fluorophenyl)sulfonyl]amino}-N-[(1S)-1-(hydroxymethyl)-3-methylbutyl]-3-methylbutanamide | C17H27FN2O4S | 详情 | 详情 | |
| (II) | 60378 | (2S)-2-{[(4-fluorophenyl)sulfonyl]amino}-N-[(1S)-1-formyl-3-methylbutyl]-3-methylbutanamide | C17H25FN2O4S | 详情 | 详情 | |
| (III) | 40924 | 2-(dimethylamino)acetohydrazide | 539-64-0 | C4H11N3O | 详情 | 详情 |
Extended Information