5-(Benzyloxy)-6-(6-methylpyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole → 6-(6-Methylpyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-5-ol

HRID 1662000노트

반응식

HRID 1662000 반응식
C([O:8][C:9]1[CH:10]=[C:11]2[C:15](=[CH:16][C:17]=1[C:18]1[CH:19]=[N:20][C:21]([CH3:24])=[CH:22][CH:23]=1)[N:14]([CH:25]1[CH2:30][CH2:29][CH2:28][CH2:27][O:26]1)[N:13]=[CH:12]2)C1C=CC=CC=1>CCO.CCOC(C)=O.[Pd]>[CH3:24][C:21]1[N:20]=[CH:19][C:18]([C:17]2[CH:16]=[C:15]3[C:11]([CH:12]=[N:13][N:14]3[CH:25]3[CH2:30][CH2:29][CH2:28][CH2:27][O:26]3)=[CH:10][C:9]=2[OH:8])=[CH:23][CH:22]=1

참가 물질

5

반응물 1

HCID 667671245-(Benzyloxy)-6-(6-methylpyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole

생성물 1

HCID 667672706-(6-Methylpyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-5-ol수율 88.2%

시약·촉매·용매 3

HCID 23938Palladium촉매HCID 702Ethanol용매HCID 8857Ethyl Acetate용매

실험 절차

To a solution of 5-(benzyloxy)-6-(6-methylpyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole (1.44 g, 3.60 mmol) in EtOH (50 mL) and EtOAc (50 mL) is added Pd/C (500 mg, 10% wt) under N2. The resulting mixture is degassed by evacuation and backfilled with nitrogen. Then the reaction mixture is stirred at RT under H2 atmosphere overnight. The reaction mixture is filtered. The filtrate is concentrated to give the product (982 mg, 88.0% yield). MS (m/z): 310.1 (M+H).

후처리

  1. customThe resulting mixture is degassed by evacuation
  2. filtrationThe reaction mixture is filtered
  3. concentrationThe filtrate is concentrated

출처 및 근거

ORD 기록
ord-2df150b927da41ff9120a366eb031085
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08030302B2

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