Tetrahydrofuran → 6-Methoxy-4,4-dimethyl-1,2,3,4-tetrahydroisoquinoline

HRID 51643노트

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HRID 51643 반응식
C(OC(=O)CC1C=CC(C#C[C:14]2[CH:23]=[CH:22][C:21]3[CH:20]([N:24]([CH:26]4CC4)C)CC[C:17]([CH3:30])([CH3:29])[C:16]=3[CH:15]=2)=CC=1F)C.[H-].[Al+3].[Li+].[H-].[H-].[H-].[O:39]1CCC[CH2:40]1>>[CH3:40][O:39][C:14]1[CH:15]=[C:16]2[C:21](=[CH:22][CH:23]=1)[CH2:20][NH:24][CH2:26][C:17]2([CH3:29])[CH3:30]

참가 물질

4

실험 절차

A solution of 6-methoxy-4,4-dimethyl-1,2,3,4-tetrahydro-isoquinoline-1-one (Intermediate 17, 3.5 g, 17 mmol) in 100 mL of anhydrous tetrahydrofuran was treated with lithium aluminum hydride (1.3 g, 34.25 mmol) in small portions and the resulting suspension was refluxed for 3 hours under argon. The reaction mixture was then cooled in an ice bath and cautiously quenched with saturated aqueous sodium sulfate solution and the resulting slurry was filtered and the filter-cake washed well with ethyl acetate. The filtrate and washings were evaporated in vacuo to a brown oil which was dissolved in chloroform, the solution was dried over anhydrous magnesium sulfate, filtered and evaporated in vacuo to afford the title compound (3.2 g, ˜100%).

후처리

  1. temperaturethe resulting suspension was refluxed for 3 hours under argon
  2. temperatureThe reaction mixture was then cooled in an ice bath
  3. customcautiously quenched with saturated aqueous sodium sulfate solution
  4. filtrationthe resulting slurry was filtered
  5. washthe filter-cake washed well with ethyl acetate
  6. customThe filtrate and washings were evaporated in vacuo to a brown oil which
  7. dissolutionwas dissolved in chloroform
  8. dry with materialthe solution was dried over anhydrous magnesium sulfate
  9. filtrationfiltered
  10. customevaporated in vacuo

출처 및 근거

ORD 기록
ord-e093211aeae14c44a87d4fb781e86054
출처 데이터셋
uspto-grants-2004_03
특허 번호
US06713647B2

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