Reaktion #60670

Reaktionsgleichung

4-(5-Bromo-pyridine-2-yl)-piperazine-1-carbaldehyde

4-Fluorobenzeneboronic acid

EtOH

Na2CO3

→

title product

Ausbeute 94.7%

4-(5-(4-Fluoro-phenyl)-pyridine-2-yl)-piperazine-1-carbaldehyde

Ausbeute 94.7%

Lösungsmittel

Toluene

toluene

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturAfter cooling the mixture
2. 2
   Sonstigeseparated
3. 3
   WaschenThe organic phase was washed with water and brine
4. 4
   Filtrationfiltered through a pad of celite
5. 5
   Trocknendried over Na2SO4
6. 6
   SonstigeThe solvent were removed in vacuo

Vorschrift

4-(5-Bromo-pyridine-2-yl)-piperazine-1-carbaldehyde (100 mg, 0.37 mmol), 4-Fluorobenzeneboronic acid (55 mg, 0.39 mmol), (1,1′-bis(diphenylphosphino)ferrocene)-dichloropalladium(II) (10 mg, 0.01 mmol), Toluene (2 ml), EtOH (0.5 ml) and 2M Na2CO3 solution (0.5 ml, 1 mmol) were heated at 80° C. under N2 overnight. After cooling the mixture was diluted with toluene and separated. The organic phase was washed with water and brine, filtered through a pad of celite and dried over Na2SO4. The solvent were removed in vacuo affording 100 mg (94%) of the title product as a beige powder.

Quelle