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【结 构 式】 
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【分子编号】63394 【品名】N-[2-[(2-amino-2-oxo-1-{[(phenylmethyl)oxy]methyl}ethyl)amino]-1-(cyclohexylmethyl)-2-oxoethyl]-4-morpholinecarboxamide 【CA登记号】 |
【 分 子 式 】C24H36N4O5 【 分 子 量 】460.5738 【元素组成】C 62.59% H 7.88% N 12.16% O 17.37% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(VIII)N-Boc-O-Benzyl-L-serine (V) is treated with ammonium hydroxide and EDC/HOBt to afford the corresponding amide (VI). Subsequent acidic cleavage of the N-Boc group of (VI) provides O-benzyl-L-serinamide (VII). Then, coupling between cyclohexylalanine derivative (IV) and serinamide (VII) in the presence of EDC/HOBt furnishes the dipeptide derivative (VIII). Finally, dehydration of the terminal amide function of (VIII) by means of cyanuric chloride leads to the target nitrile.
| 【1】 Frye, L.L.; Cywin, C.L.; Morwick, T.; Spero, D.M.; Thomson, D.; Ward, Y. (Boehringer Ingelheim Pharmaceuticals Inc.); Cpds. useful as reversible inhibitors of cathepsin S. JP 2002538151; US 6395897; WO 0051998 . |
| 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) | 16886 | (2S)-3-(benzyloxy)-2-[(tert-butoxycarbonyl)amino]propionic acid; N-alpha-t-BOC-o-benzyl-L-serine | 23680-31-1 | C15H21NO5 | 详情 | 详情 |
| (IV) | 63391 | 3-cyclohexyl-N-(4-morpholinylcarbonyl)alanine | C14H24N2O4 | 详情 | 详情 | |
| (VI) | 63392 | 1,1-dimethylethyl 2-amino-2-oxo-1-{[(phenylmethyl)oxy]methyl}ethylcarbamate | C15H22N2O4 | 详情 | 详情 | |
| (VII) | 63393 | 2-amino-3-[(phenylmethyl)oxy]propanamide | C10H14N2O2 | 详情 | 详情 | |
| (VIII) | 63394 | N-[2-[(2-amino-2-oxo-1-{[(phenylmethyl)oxy]methyl}ethyl)amino]-1-(cyclohexylmethyl)-2-oxoethyl]-4-morpholinecarboxamide | C24H36N4O5 | 详情 | 详情 |
Extended Information