Potassium Carbonate → 4-{4-[3-(7-Fluoro-quinolin-6-ylmethyl)-imidazo[1,2-b]pyridazin-6-yl]-pyrazol-1-yl}-piperidine-1-carboxylic acid tert-butyl ester

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

A microwave tube was charged with 6-(6-chloro-imidazo[1,2-b]pyridazin-3-ylmethyl)-7-fluoro-quinoline (Stage 180.2, 500 mg, 1.599 mmol), 4-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyrazol-1-yl]-piperidine-1-carboxylic acid tert-butyl ester (prepared as described in published patent application WO 2007/066185 p. 9 & 10; 905 mg, 2.398 mmol), Pd(PPh3)2Cl2 (56 mg), 2 M K2CO3 (2.158 mL) and DME (5 mL) and was heated at 90° C. for 2 h under stirring. The RM was extracted with EtOAc and aqueous NaHCO3. The organic layer was dried and concentrated in vacuo. The reside was dried under vacuum (12 mbar) for 3 days to afford the title compound (tR 4.5 min (conditions 3), MH+=528)

Herkunft & Nachweise