Ammonia → 4-(Imidazo[1,2-a]pyridin-3-yl)piperidin-4-ol
反応式
C(OC([N:8]1[CH2:13][CH2:12][C:11]([OH:23])([C:14]2[N:18]3[CH:19]=[CH:20][CH:21]=[CH:22][C:17]3=[N:16][CH:15]=2)[CH2:10][CH2:9]1)=O)(C)(C)C.N>C(Cl)Cl>[N:16]1[CH:15]=[C:14]([C:11]2([OH:23])[CH2:10][CH2:9][NH:8][CH2:13][CH2:12]2)[N:18]2[CH:19]=[CH:20][CH:21]=[CH:22][C:17]=12参加物
4
実験手順
To a stirred solution of 4-hydroxy-4-imidazo[1,2-a]pyridin-3-yl-piperidine-1-carboxylic acid tert-butyl ester (2.0 g 6.26 mmol) in CH2Cl2 (100 ml) trifluoro acetic acid (10 ml) was added at room temperature. The reaction mixture was stirred at room temperature for 24 hrs. At the end, the reaction mixture was basified with methanolic ammonia and concentrated to dryness. The residue was directly chromatographed over silica-gel column and eluted with methanol:10% methanolic ammonia. The product, 4-imidazo[1,2-a]pyridin-3-yl-piperidin-4-ol was obtained as yellow oil; Yield; 620 mg (48%); 218 (M+H).
後処理
- concentrationconcentrated to dryness
- customThe residue was directly chromatographed over silica-gel column
- washeluted with methanol
出典と根拠
- ORDレコード
- ord-3a5b1d94642e402d8a067c1d4b7dd0fe
- 出典データセット
- uspto-grants-2007_06
- 特許番号
- US07235569B2
反応ノート
読み込み中…