反応式
[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][C:10]=1[NH:11][C:12]([C:14]([O:17]C(=O)C)([CH3:16])[CH3:15])=[O:13])[NH:7][C:6](=[O:21])[CH2:5]2.[OH-].[Na+].Cl>CO>[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][C:10]=1[NH:11][C:12](=[O:13])[C:14]([OH:17])([CH3:16])[CH3:15])[NH:7][C:6](=[O:21])[CH2:5]2参加物
5
実験手順
Acetic acid 1-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-6-ylcarbamoyl)-1-methyl-ethyl ester 11a (2.035 mg, 6.9 mmol) was dissolved in 20 mL of methanol under stirring at room temperature, and 20 mL of sodium hydroxide solution (0.7 M) was then added to the solution. The reaction solution was stirred for 4 hours. The reaction was completed until TLC showed the disappearance of starting materials, and the above solution was neutralized with hydrochloric acid (1 M) and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography and dried to give N-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-6-yl)-2-hydroxy-2-methyl-propionamide 11b (900 mg, yield 59.2%) as a white solid.
後処理
- stirringThe reaction solution was stirred for 4 hours
- customthe solvent was evaporated under reduced pressure
- customThe residue was purified by silica gel column chromatography
- customdried
出典と根拠
- ORDレコード
- ord-c4dc06b3c2b84397bc6c68ecbdcea45f
- 出典データセット
- uspto-grants-2012_10
- 特許番号
- US08299069B2
関連ノート
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