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Trifluoroacetic acid → (5S)-3-[3-fluoro-4-[4-(hydroxymethyl)imidazol-1-yl]phenyl]-5-[(isoxazol-3-ylamino)methyl]oxazolidin-2-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | 3-(4-(4-Hydroxymethylimidazol-1-yl)-3-fluorophenyl)-5(R)-(N-(t-butoxycarbonyl)isoxazol-3-ylaminomethyl)oxazolidin-2-one | HCID 53975256 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | (5S)-3-[3-fluoro-4-[4-(hydroxymethyl)imidazol-1-yl]phenyl]-5-[(isoxazol-3-ylamino)methyl]oxazolidin-2-one | HCID 497419 | 66.9% |
反応手順
3-(4-(4-Hydroxymethylimidazol-1-yl)-3-fluorophenyl)-5(R)-(N-(t-butoxycarbonyl)isoxazol-3-ylaminomethyl)oxazolidin-2-one (360 mg, 0.76 mM) was dissolved in dichloromethane (10 ml) and treated with trifluoroacetic acid (10 ml). After stirring for 30 minutes solvent was evaporated, the residue repeatedly evaporated to dryness with dichloromethane (3×10 ml), and the resulting gum dissolved in water (10 ml). The solution was made basic with concentrated aqueous ammonia, and the resulting precipitate filtered, washed with water and dried to give title product (190 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07087629B2 |
| 出典データセット | uspto-grants-2006_08 |
| ORD ID | ord-a0a6c4dccdde4393b6c140e0b62c2cd2 |
| 出典メモ | uspto-grants-2006_08 |