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Nitrogen → (5S)-5-(Aminomethyl)-3-(3-fluoro-4-(4-morpholinyl)phenyl)-2-oxazolidinone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Nitrogen | HCID 947 | — |
| 反応物 | Ammonium formate | HCID 2723923 | — |
| 反応物 | (S)-5-((dibenzylamino)methyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one | HCID 11213668 | — |
| 触媒 | Palladium | HCID 23938 | — |
| 溶媒 | Acetone | HCID 180 | — |
| 生成物 | (5S)-5-(Aminomethyl)-3-(3-fluoro-4-(4-morpholinyl)phenyl)-2-oxazolidinone | HCID 10780199 | 88% |
反応手順
(S)-5-((dibenzylamino)methyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one (0.95 g, 2 mmol), 0.5 g 10 wt % Pd—C and ammonium formate (1.3 g, 20 mmol) were added to 20 mL acetone and the air was replaced with N2. The mixture was heated to reflux and stirred for 10 hours. The mixture was filtered and separated by water. The organic layer was washed with brine, dried over anhydrous magnesium sulfate, filtered, and the solvent evaporated to provide 0.52 g of white solid in 88% yield.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08658789B2 |
| 出典データセット | uspto-grants-2014_02 |
| ORD ID | ord-40566736bbfb4d2a8947a776376ad043 |
| 出典メモ | uspto-grants-2014_02 |