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【结 构 式】 
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【分子编号】58666 【品名】N-[((5S)-3-{3-fluoro-4-[formyl(methyl)amino]phenyl}-2-oxo-1,3-oxazolidin-5-yl)methyl]acetamide 【CA登记号】 |
【 分 子 式 】C14H16FN3O4 【 分 子 量 】309.2972632 【元素组成】C 54.37% H 5.21% F 6.14% N 13.59% O 20.69% |
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：(XV)Amine (XII) was acylated by acetic anhydride in pyridine to afford acetamide (XIII). The N-Boc protecting group of (XIII) was then removed under acidic conditions to give amine (XIV), which was converted into formamide (XV) by treatment with p-nitrophenyl formate. Finally, thionation of both amide groups of (XV) by means of Lawesson's reagent in hot dioxane provided the target bis-thioamide.
| 【1】 Singh, U.; Gordeev, M.F.; Luehr, G.W.; Gadwood, R.C.; Jain, R.; Hackbarth, C.J.; Trias, J.; Patel, D.V.; Lopez, S.; Acyclic C-group oxazolidinones: Antimicrobial 4'-acylamino, 4'-urea and 4'-thiourea phenyloxazolidinones. 41st Intersci Conf Antimicrob Agents Chemother (Dec 16 2001, Chicago) 2001, Abst F-1045. |
| 【2】 Patel, D.V.; Gadwood, R.C.; Gordeev, M.F.; Luehr, G.W. (Pharmacia Corp.); Oxazolidinones and their use as antiinfectives. EP 1200416; US 6441005; WO 0109107 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XII) | 58663 | tert-butyl 4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-2-fluorophenyl(methyl)carbamate | C16H22FN3O4 | 详情 | 详情 | |
| (XIII) | 58664 | tert-butyl 4-{(5S)-5-[(acetylamino)methyl]-2-oxo-1,3-oxazolidin-3-yl}-2-fluorophenyl(methyl)carbamate | C18H24FN3O5 | 详情 | 详情 | |
| (XIV) | 58665 | N-({(5S)-3-[3-fluoro-4-(methylamino)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide | C13H16FN3O3 | 详情 | 详情 | |
| (XV) | 58666 | N-[((5S)-3-{3-fluoro-4-[formyl(methyl)amino]phenyl}-2-oxo-1,3-oxazolidin-5-yl)methyl]acetamide | C14H16FN3O4 | 详情 | 详情 |
Extended Information