5-Chloro-1-[1-[2-(indan-2-yl)ethyl]-1,2,3,6-tetrahydropyridin-4-yl]-1H-indole → 5-Chloro-1-[1-[2-(indan-2-yl)ethyl]piperidin-4-yl]-1H-indole

HRID 1267163ノート

反応式

HRID 1267163 の反応式
[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([C:11]1[CH2:12][CH2:13][N:14]([CH2:17][CH2:18][CH:19]3[CH2:27][C:26]4[C:21](=[CH:22][CH:23]=[CH:24][CH:25]=4)[CH2:20]3)[CH2:15][CH:16]=1)[CH:6]=[CH:5]2.[H][H]>[Pt]=O.C(O)(=O)C>[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([CH:11]1[CH2:12][CH2:13][N:14]([CH2:17][CH2:18][CH:19]3[CH2:27][C:26]4[C:21](=[CH:22][CH:23]=[CH:24][CH:25]=4)[CH2:20]3)[CH2:15][CH2:16]1)[CH:6]=[CH:5]2

参加物

5

実験手順

A mixture of 5-Chloro-1-[1-[2-(indan-2-yl)ethyl]-1,2,3,6-tetrahydropyridin-4-yl]-1H-indole. 28a. (1.9 g), acetic acid (50 ml), and platinum oxide (0.1 g) was shaken for 3 h under 3 atm. hydrogen pressure. The mixture was filtered and evaporated in vacuo. The residue was dissolved in ethyl acetate and the organic phase was shaken with dilute ammonium hydroxide and then worked up in a conventional manner. Further purification was done on silica gel eluted with ethyl acetate-heptane (1:1) to give 2.0 g of crude product. The crude product was crystallized (ethyl acetate), and the title compound was collected by filtration (1.1 g, 58%).

後処理

  1. filtrationThe mixture was filtered
  2. customevaporated in vacuo
  3. dissolutionThe residue was dissolved in ethyl acetate
  4. customFurther purification
  5. washeluted with ethyl acetate-heptane (1:1)

出典と根拠

ORDレコード
ord-ee136bb019b346959e90ef7a167379a8
出典データセット
uspto-grants-2003_04
特許番号
US06552044B2

反応ノート

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