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2-Fluoro-3-(methoxymethoxy)pyridine → (2-Fluoro-3-(methoxymethoxy)pyridin-4-yl)(2-fluoro-5-(2-fluoropyridin-3-yl)phenyl)methanol

HRID 335950
Notizen
Druckvorschau

Reaktionsgleichung

Reaktionsgleichung von HRID 335950
C([Li])CCC.[F:6][C:7]1[C:12]([O:13][CH2:14][O:15][CH3:16])=[CH:11][CH:10]=[CH:9][N:8]=1.[F:17][C:18]1[CH:25]=[CH:24][C:23]([C:26]2[C:27]([F:32])=[N:28][CH:29]=[CH:30][CH:31]=2)=[CH:22][C:19]=1[CH:20]=[O:21]>C1COCC1>[F:6][C:7]1[C:12]([O:13][CH2:14][O:15][CH3:16])=[C:11]([CH:20]([C:19]2[CH:22]=[C:23]([C:26]3[C:27]([F:32])=[N:28][CH:29]=[CH:30][CH:31]=3)[CH:24]=[CH:25][C:18]=2[F:17])[OH:21])[CH:10]=[CH:9][N:8]=1
KomponentenVersuchsvorschriftAufarbeitungQuellen und NachweiseNotizen zur Reaktion

Komponenten

5

Edukt 3

HCID 673829612-Fluoro-3-(methoxymethoxy)pyridineHCID 866584942-Fluoro-5-(2-fluoropyridin-3-yl)benzaldehydeHCID 178418339Butyllithium

Produkt 1

HCID 67383057(2-Fluoro-3-(methoxymethoxy)pyridin-4-yl)(2-fluoro-5-(2-fluoropyridin-3-yl)phenyl)methanolAusbeute 68,3 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 8028
Tetrahydrofuran
Lösungsmittel
3×

Versuchsvorschrift

DIPA (3.5 mL, 24.97 mmol) was dissolved in dry THF (10 mL) under nitrogen and cooled in a dry ice bath. Butyllithium solution (2.5 m in hexanes, 10.0 mL, 25.00 mmol) was added and after stirring for a few minutes 2-fluoro-3-(methoxymethoxy)pyridine (3.71 g, 23.64 mmol) in dry THF (25 mL) was added dropwise. The reaction was stirred for 1 h. A solution of 2-fluoro-5-(2-fluoropyridin-3-yl)benzaldehyde (4.71 g, 21.49 mmol) in dry THF (40 mL) was added dropwise over 10 min. The reaction was removed from the cold bath and stirred for an additional 15 min. Saturated sodium bicarbonate (20 mL) was added followed by EtOAc (300 mL) and water (400 mL). The phases were mixed and separated and the organic dried with magnesium sulfate before evaporating to dryness under reduced pressure. Purification using silica chromatography (hexane to EtOAc gradient) gave the desired (2-fluoro-3-(methoxymethoxy)pyridin-4-yl)(2-fluoro-5-(2-fluoropyridin-3-yl)phenyl)methanol (5.52 g, 14.67 mmol). MS m/z=377.1 [M+H]+. Calculated for C19H15F3N2O3: 376.10.

Aufarbeitung

  1. temperaturecooled in a dry ice bath
  2. additionwas added dropwise
  3. customThe reaction was removed from the cold bath
  4. stirringstirred for an additional 15 min
  5. additionSaturated sodium bicarbonate (20 mL) was added
  6. additionThe phases were mixed
  7. customseparated
  8. dry with materialthe organic dried with magnesium sulfate
  9. custombefore evaporating to dryness under reduced pressure
  10. customPurification

Quellen und Nachweise

ORD-Eintrag
ord-8353aa960090478498bd3d31c871439f
Quelldatensatz
uspto-grants-2014_11
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US08883782B2

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