Potassium Carbonate → (4-Morpholin-4-yl-phenyl)-[8-(2-phenoxy-phenyl)-[1,2,4]triazolo[1,5-a]pyrazin-2-yl]-amine

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

To a solution of (8-chloro-[1,2,4]triazolo[1,5-a]pyrazin-2-yl-(4-morpholin-4-yl-phenyl)-amine (0.15 g, 0.45 mmol, 1 eq) in a mixture of ethanol:toluene (1:4) (10 ml) is taken in a dry pressure tube, palladium acetate (0.01 g, 0.045 mmol, 0.1 eq), anhydrous potassium carbonate (0.125 g, 0.90 mmol, 2 eq), 2-dicyclo-hexylphosphino-2′,6′-dimethoxybiphenyl, S-Phos (0.027 g, 0.06 mmol, 0.13 eq) and 2-phenoxyphenylboronic acid (0.19 g, 0.90 mmol, 2 eq) are added and the reaction mixture is degasified with nitrogen. The reaction mixture is heated to 120° C. for 1 hour. The reaction mixture is concentrated and the residue is taken in 25% methanol in dichloromethane (50 ml) and filtered through celite to remove the inorganics and the filtrate is concentrated and purified by silica column using (230-400) mesh to get the product as pale yellow solid.

Herkunft & Nachweise