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

HRID 2382046노트

반응식

HRID 2382046 반응식
[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

참가 물질

4

반응물 1

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

생성물 1

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

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 887Methanol용매

실험 절차

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).

후처리

  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

출처 및 근거

ORD 기록
ord-dff4e11dd51545a3a3b5a51217f55027
출처 데이터셋
uspto-grants-2012_09
특허 번호
US08258130B2

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