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【结 构 式】

【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
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