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Diisopropylamine → 3-[4-(4-Fluoro-phenyl)-thiazol-2-yl]-N,N-diisopropyl-acrylamide

HRID 1873772
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HRID 1873772 반응식
[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[N:9]=[C:10]([CH:13]=[CH:14][C:15]([OH:17])=O)[S:11][CH:12]=2)=[CH:4][CH:3]=1.[CH:18]([NH:21][CH:22]([CH3:24])[CH3:23])([CH3:20])[CH3:19].C(N(CC)CC)C.CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F>CN(C=O)C>[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2[N:9]=[C:10]([CH:13]=[CH:14][C:15]([N:21]([CH:22]([CH3:24])[CH3:23])[CH:18]([CH3:20])[CH3:19])=[O:17])[S:11][CH:12]=2)=[CH:6][CH:7]=1
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참가 물질

6

반응물 4

HCID 7912DiisopropylamineHCID 8471TriethylamineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 687134823-[4-(4-Fluoro-phenyl)-thiazol-2-yl]-acrylic Acid

생성물 1

HCID 687106003-[4-(4-Fluoro-phenyl)-thiazol-2-yl]-N,N-diisopropyl-acrylamide

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

98 mg (0.39 mmol) of 3-[4-(4-fluoro-phenyl)-thiazol-2-yl]-acrylic acid, 79.6 mg (0.78 mmol) of diisopropylamine, 119.35 mg (1.17 mmol) of triethylamine and 164.5 mg (0.43 mmol) of HATU in 5 ml of DMF were stirred at room temperature for 2 h. The reaction mixture was concentrated, and water and ethyl acetate were added. The organic phase was separated, washed and evaporated. The residue was purified by chromatography (RP18). Yield: 39 mg.

후처리

  1. concentrationThe reaction mixture was concentrated
  2. additionwater and ethyl acetate were added
  3. customThe organic phase was separated
  4. washwashed
  5. customevaporated
  6. customThe residue was purified by chromatography (RP18)

출처 및 근거

ORD 기록
ord-8da3d2a4f8374f5cad5dfc9b6a610118
출처 데이터셋
uspto-grants-2012_11
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08304438B2

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