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Trifluoroacetic acid → 3-(Trifluoromethyl)-5,6-dihydro-1,6-naphthyridin-7(8H)-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Tert-butyl 7-oxo-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxylate | HCID 59017436 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 3-(Trifluoromethyl)-5,6-dihydro-1,6-naphthyridin-7(8H)-one | HCID 23533628 | 100% |
反応手順
To a solution of tert-butyl 7-oxo-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxylate (3.60 g, 11.4 mmol) in methylene chloride (14 mL) was added trifluoroacetic Acid (6.75 mL) and the resulting mixture was stirred at room temperature for 0.5 h. The solution was evaporated under reduced pressure and the residue was dissolved in CH2Cl2. The mixture was neutralized by the slow addition of a solution of saturated NaHCO3 and the organic layer was removed. The aqueous layer was extracted with CH2Cl2 four times, and the combined organic layers were dried over MgSO4, filtered, and evaporated in vacuo to afford 2.45 g (100%) of desired product as a yellow solid. LC-MS calculated for C9H7F3N2O: (M+H)+217; found 217.0.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07307086B2 |
| 出典データセット | uspto-grants-2007_12 |
| ORD ID | ord-1e8e3f645d484d7aa5ba2f8e4d7ac5ca |
| 出典メモ | uspto-grants-2007_12 |