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Pyridine → methyl 6-fluoro-2-oxo-2,3-dihydro-1H-indole-5-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Pyridine | HCID 1049 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 5-(2-Chloroacetyl)-6-fluoroindolin-2-one | HCID 10609359 | — |
| 反応物 | 1,4-Dioxane hydrochloride | HCID 20443148 | — |
| 生成物 | methyl 6-fluoro-2-oxo-2,3-dihydro-1H-indole-5-carboxylate | HCID 66636241 | — |
反応手順
A solution of the compound obtained in Step A (3.24 mmoles) in pyridine (99 mmol) is stirred at 90° C. for 2 hours. The reaction mixture is cooled to ambient temperature and then filtered. The solid obtained is washed with ethanol and dried in vacuo at 50° C. The compound is dissolved in MeOH (80 mL), and 0.434 mmol of potassium carbonate is added. The mixture is stirred at 80° C. for 5 hours. After cooling to ambient temperature, 4M HCl/dioxane solution is added (pH 3) and the mixture is evaporated to dryness. The residue obtained is triturated in water, filtered, washed with water and then dried in vacuo at 50° C. to yield the title product.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08133889B2 |
| 出典データセット | uspto-grants-2012_03 |
| ORD ID | ord-be6bc99c71784e91b8441cddd25d1798 |
| 出典メモ | uspto-grants-2012_03 |