Reaktion #1862208

Reaktionsgleichung

5-bromo-3-(1H-pyrazol-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-c]pyridine

3-Pyridylboronic acid

Potassium acetate

Water

Water

→

3-(1H-pyrazol-3-yl)-5-(pyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-c]pyridine

Ausbeute 48.0%

Lösungsmittel

Acetonitrile

Sodium carbonate

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeA microwave reaction vials
2. 2
   Einengenwas concentrated
3. 3
   Sonstigethe residue was purified on silica
4. 4
   Wascheneluted with 0 to 7% MeOH in DCM with 1% NH4OH

Vorschrift

A microwave reaction vials was charged with 5-bromo-3-(1H-pyrazol-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-c]pyridine as an off-white solid (153.7 mg 0.44 mmol), 3-Pyridylboronic acid (81.62 mg, 0.66 mmol), 1,1′-Bis(diphenylphosphino)ferrocenepalladium (II) chloride (36.15 mg, 0.044 mmol), 1.00 M of Potassium acetate in Water (0.66 mL, 0.66 mmol), 1.00 M of Sodium carbonate in Water (0.66 mL, 0.66 mmol), and Acetonitrile (3 mL). The reaction mixture was heated under microwave at 130° C. for 20 minutes The mixture was concentrated and the residue was purified on silica eluted with 0 to 7% MeOH in DCM with 1% NH4OH to afford 3-(1H-pyrazol-3-yl)-5-(pyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-c]pyridine (73.4 mg, 48%).

Quelle