Ammonium formate → 1-Azetidin-3-ylmethyl-6-fluoro-1H-indole

HRID 720391Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 720391
C([N:14]1[CH2:17][CH:16]([CH2:18][N:19]2[C:27]3[C:22](=[CH:23][CH:24]=[C:25]([F:28])[CH:26]=3)[CH:21]=[CH:20]2)[CH2:15]1)(C1C=CC=CC=1)C1C=CC=CC=1.C([O-])=O.[NH4+]>[Pd].C(O)C>[NH:14]1[CH2:17][CH:16]([CH2:18][N:19]2[C:27]3[C:22](=[CH:23][CH:24]=[C:25]([F:28])[CH:26]=3)[CH:21]=[CH:20]2)[CH2:15]1

Komponenten

5

Edukt 2

HCID 2723923Ammonium formateHCID 692042621-(1-benzhydryl-azetidin-3-ylmethyl)-6-fluoro-1H-indole

Produkt 1

HCID 218920951-Azetidin-3-ylmethyl-6-fluoro-1H-indole

Reagenzien, Katalysatoren, Lösungsmittel 2

HCID 23938PalladiumKatalysatorHCID 702EthanolLösungsmittel

Versuchsvorschrift

A mixture of 1-(1-benzhydryl-azetidin-3-ylmethyl)-6-fluoro-1H-indole (0.6 g, 1.6 mmol), palladium on carbon (10%, cat.amount) and ammonium formate (0.2 g, 3.2 mmol) in ethanol (20 mL) was refluxed for 30 min. The mixture was filtered through celite and the solvent removed under vacuum. Diphenylmethane was removed by triturating the residue with ether, methylene chloride and decanting. The remaining product was dried under vacuum. The crude material was directly used in next step without further purification.

Aufarbeitung

  1. temperaturewas refluxed for 30 min
  2. filtrationThe mixture was filtered through celite
  3. customthe solvent removed under vacuum
  4. customDiphenylmethane was removed
  5. customby triturating the residue with ether, methylene chloride
  6. customdecanting
  7. customThe remaining product was dried under vacuum
  8. customThe crude material was directly used in next step without further purification

Quellen und Nachweise

ORD-Eintrag
ord-82e8dae6fdae43dc84e9dd76f8e83df3
Quelldatensatz
uspto-grants-2006_11
Patentnummer
US07135479B2

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