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Potassium Carbonate → HCID 18388216, Verbindung

HRID 2296743
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Druckvorschau

Reaktionsgleichung

Reaktionsgleichung von HRID 2296743
Br[C:2]1[C:3](=[O:8])[O:4][CH2:5][CH2:6][CH:7]=1.[F:9][C:10]1[CH:11]=[C:12](B(O)O)[CH:13]=[CH:14][C:15]=1[F:16].C(=O)([O-])[O-].[K+].[K+].[F-].[K+]>O1CCCC1.C1C=CC([P]([Pd]([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)[P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)=CC=1.C(OCC)(=O)C.O>[F:9][C:10]1[CH:11]=[C:12]([C:2]2[C:3](=[O:8])[O:4][CH2:5][CH2:6][CH:7]=2)[CH:13]=[CH:14][C:15]=1[F:16]
KomponentenVersuchsvorschriftAufarbeitungQuellen und NachweiseNotizen zur Reaktion

Komponenten

9

Edukt 4

HCID 11430Potassium CarbonateHCID 522689Potassium FluorideHCID 27343373,4-Difluorobenzeneboronic acidHCID 108560293-bromo-5,6-dihydro-2H-pyran-2-one

Produkt 1

HCID 18388216HCID 18388216, VerbindungAusbeute 33,6 %

Reagenzien, Katalysatoren, Lösungsmittel 4

HCID 178418397
HCID 178418397, Verbindung
Katalysator
HCID 962WaterLösungsmittel
HCID 8028TetrahydrofuranLösungsmittel
HCID 8857Ethyl AcetateLösungsmittel

Versuchsvorschrift

A solution of 3-bromo-5,6-dihydropyran-2-one (87.4 g, 0.49mol), 3,4-difluorophenylboronic acid (91.4 g, 0.58 mol), potassium carbonate (99.9 g, 0.72 mol), potassium fluoride (85.4 g, 1.47 mol) and tetrakis(triphenylphosphine)palladium (0) (12 g, 0.01 mol) in tetrahydrofuran (600 ml) was thoroughly degassed and then heated at reflux for 48 hours under an atmosphere of nitrogen. The solution was cooled to room temperature and water (1000 ml) and ethyl acetate (1000 ml) were added. The organic phase was washed with saturated brine and dried (MgSO4) and the solvent removed in vacuo. The residue was dissolved in dichloromethane and the solution filtered through a pad of silica gel. The filtrate was evaporated to dryness and the residue recrystallized from diethyl ether to give the title compound 34.6 g. mp 82-85° C. 1H NMR (360 MHz. CDCl3) δ 2.63 (2H, td J 6.2 Hz and 4.5 Hz), 4.49 (2H, t J 6.3 Hz), 7.01 (1H, t J 4.5 Hz), 7.11-7.23 (2H, m), 7.32-7.38 (1H, m).

Aufarbeitung

  1. temperatureheated
  2. temperatureat reflux for 48 hours under an atmosphere of nitrogen
  3. washThe organic phase was washed with saturated brine
  4. dry with materialdried (MgSO4)
  5. customthe solvent removed in vacuo
  6. dissolutionThe residue was dissolved in dichloromethane
  7. filtrationthe solution filtered through a pad of silica gel
  8. customThe filtrate was evaporated to dryness
  9. customthe residue recrystallized from diethyl ether

Quellen und Nachweise

ORD-Eintrag
ord-b9dbf88f80b54005bd18c5c9a176acd9
Quelldatensatz
uspto-grants-2002_12
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US06489343B2

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