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Diethyl Ether → tert-Butyl 4-((4-chloro-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazole-1-carboxylate

HRID 592459
Notizen
Druckvorschau

Reaktionsgleichung

Reaktionsgleichung von HRID 592459
CCOCC.Cl[C:7]1[N:12]=[C:11]([Cl:13])[C:10]([C:14]([F:17])([F:16])[F:15])=[CH:9][N:8]=1.[NH2:18][C:19]1[CH:20]=[N:21][N:22]([C:24]([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25])[CH:23]=1.C(N(CC)CC)C>[Cl-].[Zn+2].[Cl-].ClCCCl.CC(O)(C)C>[Cl:13][C:11]1[C:10]([C:14]([F:17])([F:16])[F:15])=[CH:9][N:8]=[C:7]([NH:18][C:19]2[CH:20]=[N:21][N:22]([C:24]([O:26][C:27]([CH3:30])([CH3:29])[CH3:28])=[O:25])[CH:23]=2)[N:12]=1
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Komponenten

7

Edukt 4

HCID 3283Diethyl EtherHCID 8471TriethylamineHCID 27827742,4-Dichloro-5-(trifluoromethyl)pyrimidineHCID 59587648tert-butyl 4-amino-1H-pyrazole-1-carboxylate

Produkt 1

HCID 86712334tert-Butyl 4-((4-chloro-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazole-1-carboxylate

Reagenzien, Katalysatoren, Lösungsmittel 2

HCID 3007855
Zincchloride
Katalysator
HCID 21868497Tert-butyl alcohol 1,2-dichloroethaneLösungsmittel2×

Versuchsvorschrift

A 1.0 M solution of zinc chloride in Et2O (4.0 mL, 4.0 mmol) was added to 2,4-dichloro-5-trifluoromethylpyrimidine (0.49 mL, 3.6 mmol) in a 1:1 mixture of DCE/t-BuOH (40 mL) at 0° C. under a nitrogen atmosphere. The mixture was stirred for 1 hour before tert-butyl 4-amino-1H-pyrazole-1-carboxylate (0.606 g, 3.31 mmol) and triethylamine (0.51 mL, 3.7 mmol) in a 1:1 mixture of DCE/t-BuOH (30 mL) was added. The mixture was allowed to warm to room temperature and stirred for 20 hours before concentrating in vacuo and adding gradually to 100 mL water. The resulting precipitate was removed by vacuum filtration and washed with DCM. The filtrate was purified using silica gel column chromatography (0-30% EtOAc in DCM) to give the title compound A61 (0.170 g, 14%). LCMS-D: rt 3.622 min; m/z 362.1 [M−H]−.

Aufarbeitung

  1. additionwas added
  2. concentrationbefore concentrating in vacuo
  3. additionadding gradually to 100 mL water
  4. customThe resulting precipitate was removed by vacuum filtration
  5. washwashed with DCM
  6. customThe filtrate was purified

Quellen und Nachweise

ORD-Eintrag
ord-38986704d2844390b2810cd3a8b257d9
Quelldatensatz
uspto-grants-2016_01
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US09238644B2

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