1-Benzyl-4-(pyridin-3-YL)piperidin-4-OL → 4-(Pyridin-3-yl)piperidin-4-ol

HRID 1643433

反応式

HRID 1643433 の反応式
C([N:8]1[CH2:13][CH2:12][C:11]([C:15]2[CH:16]=[N:17][CH:18]=[CH:19][CH:20]=2)([OH:14])[CH2:10][CH2:9]1)C1C=CC=CC=1.C([O-])=O.[NH4+]>[Pd].CO.C(Cl)(Cl)Cl>[N:17]1[CH:18]=[CH:19][CH:20]=[C:15]([C:11]2([OH:14])[CH2:10][CH2:9][NH:8][CH2:13][CH2:12]2)[CH:16]=1

参加物

6

反応条件

温度
68 °C

実験手順

(Apparatus: 1 I three-necked flask with condenser) Palladium on charcoal (10%, catalytic amount) was added to a solution of 1-benzyl-4-(pyridin-3-yl)piperidin-4-ol (32 g) in methanol (220 ml), followed by ammonium formate solution (22.7 g in 50 ml of water). The reaction mixture was refluxed at 68° C. overnight. Thin layer chromatography control: 20% methanol in chloroform. The mixture was filtered over Celite and the filtrate was concentrated in vacuo. The residue was washed with acetone (100 ml) in order to obtain the desired compound in a pure form. Yield: 17.3 g (81%)

後処理

  1. filtrationThe mixture was filtered over Celite
  2. concentrationthe filtrate was concentrated in vacuo
  3. washThe residue was washed with acetone (100 ml) in order

出典と根拠

ORDレコード
ord-e09f3ab50bd2422d8bb92ccb82c28e45
出典データセット
uspto-grants-2012_02
特許番号
US08119805B2

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