5-fluoro-3-(2-pyridin-3-yl-vinyl)-1H-indole → 5-fluoro-3-(2-pyridin-3-yl-ethyl)-1H-indole

HRID 2382046ノート

反応式

HRID 2382046 の反応式
[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][CH:6]=[C:5]2[CH:11]=[CH:12][C:13]1[CH:14]=[N:15][CH:16]=[CH:17][CH:18]=1>CO.[Pd]>[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][CH:6]=[C:5]2[CH2:11][CH2:12][C:13]1[CH:14]=[N:15][CH:16]=[CH:17][CH:18]=1

参加物

4

反応物 1

HCID 685566735-fluoro-3-(2-pyridin-3-yl-vinyl)-1H-indole

生成物 1

HCID 685543805-fluoro-3-(2-pyridin-3-yl-ethyl)-1H-indole収率 50%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 887Methanol溶媒

実験手順

A solution of 5-fluoro-3-(2-pyridin-3-yl-vinyl)-1H-indole (3 mmol) in MeOH (10 mL) is treated with Pd/C (200 mg) and shaken in a Parr apparatus under 40 atm of H2 for 18 h. The mixture is filtered through Celite and the filtrate is concentrated in vacuo. The residue is purified by silica gel chromatography eluting with 0%-10% MeOH in DCM to afford 5-fluoro-3-(2-pyridin-3-yl-ethyl)-1H-indole (360 mg, 50%, 2 steps).

後処理

  1. filtrationThe mixture is filtered through Celite
  2. concentrationthe filtrate is concentrated in vacuo
  3. customThe residue is purified by silica gel chromatography
  4. washeluting with 0%-10% MeOH in DCM

出典と根拠

ORDレコード
ord-dff4e11dd51545a3a3b5a51217f55027
出典データセット
uspto-grants-2012_09
特許番号
US08258130B2

反応ノート

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