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Triethylamine → {4-[({[1-(1,1-dimethylethyl)-3-methyl-1H-pyrazol-5-yl]carbonyl}amino)methyl]phenyl}boronic acid

HRID 562113
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HRID 562113 반응식
[NH2:1][CH2:2][C:3]1[CH:8]=[CH:7][C:6]([B:9]([OH:11])[OH:10])=[CH:5][CH:4]=1.[CH3:12][C:13]([N:16]1[C:20]([C:21](Cl)=[O:22])=[CH:19][C:18]([CH3:24])=[N:17]1)([CH3:15])[CH3:14].C(N(CC)CC)C>CN(C=O)C>[CH3:15][C:13]([N:16]1[C:20]([C:21]([NH:1][CH2:2][C:3]2[CH:4]=[CH:5][C:6]([B:9]([OH:11])[OH:10])=[CH:7][CH:8]=2)=[O:22])=[CH:19][C:18]([CH3:24])=[N:17]1)([CH3:12])[CH3:14]
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참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 2734312(4-(Aminomethyl)phenyl)boronic acidHCID 27993401-tert-Butyl-3-methyl-1H-pyrazole-5-carbonyl chloride

생성물 1

HCID 66723191{4-[({[1-(1,1-dimethylethyl)-3-methyl-1H-pyrazol-5-yl]carbonyl}amino)methyl]phenyl}boronic acid

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

To a solution of [4-(aminomethyl)phenyl]boronic acid (145 mg, 0.966 mmol) in DMF (2 mL) was added 1-(1,1-dimethylethyl)-3-methyl-1H-pyrazole-5-carbonyl chloride (290 mg, 1.45 mmol) and triethylamine (403 μL, 2.90 mmol). The reaction was stirred for 2 h. It was then quenched and partitioned between EtOAc and H2O and the organic layer was concentrated to give {4-[({[1-(1,1-dimethylethyl)-3-methyl-1H-pyrazol-5-yl]carbonyl}amino)methyl]phenyl}boronic acid.

후처리

  1. customIt was then quenched
  2. custompartitioned between EtOAc and H2O
  3. concentrationthe organic layer was concentrated

출처 및 근거

ORD 기록
ord-c852f3348bd64c5cb6263fb886c0a836
출처 데이터셋
uspto-grants-2011_11
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08063071B2

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