Pyruvic Acid → 6-Chloro-1H-indole-2-carboxylic acid
反応式
[Cl:1][C:2]1[CH:3]=[CH:4][C:5](I)=[C:6]([CH:8]=1)[NH2:7].[C:10]([OH:15])(=[O:14])[C:11]([CH3:13])=O.C1N2CCN(CC2)C1>CN(C=O)C.C([O-])(=O)C.[Pd+2].C([O-])(=O)C>[Cl:1][C:2]1[CH:8]=[C:6]2[C:5]([CH:13]=[C:11]([C:10]([OH:15])=[O:14])[NH:7]2)=[CH:4][CH:3]=1参加物
6
反応条件
- 温度
- 110 °C
実験手順
5-Chloro-2-iodoaniline (5.8 g, 23 mmol) and pyruvic acid (8 mL, 115 mmol) were dissolved in DMF (100 mL). DABCO (12.8 g, 115 mmol) was added and N2 (g) was bubbled through solution for 20 minutes, then palladium acetate (1.03 g, 4.6 mmol) was added. The reaction was heated to 110° C. for 1 hour then submitted to aqueous workup and purified by silica gel chromatography (0-100% EtOAc in hexanes) to yield the title compound.
後処理
- customN2 (g) was bubbled through solution for 20 minutes
- custompurified by silica gel chromatography (0-100% EtOAc in hexanes)
出典と根拠
- ORDレコード
- ord-3c37bce5ab274f138cbbbc2e7c60824b
- 出典データセット
- uspto-grants-2015_04
- 特許番号
- US09000025B2
反応ノート
読み込み中…