Water → 7-(2-methoxy-4,6-dimethylpyridin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one

Participants

Reaction Conditions

Reaction Steps

KTB (655 mg) was added to a solution of 5-[2-fluoro-4-(2-methoxy-4,6-dimethylpyridin-3-yl)phenyl]-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxamide (1.52 g) in NMP (15 mL), and the mixture was stirred at 90° C. for 30 minutes. KTB (40 mg) was added to the reaction mixture, and the mixture was stirred at 90° C. for 30 minutes. Further, KTB (40 mg) was added to the reaction mixture, and the mixture was stirred at 90° C. for 30 minutes. The reaction mixture was cooled to room temperature. Water (3 mL) was added to the reaction mixture. The solid was precipitated. After stirring for one hour directly, the precipitated solid was collected by filtration. The residue was washed with water (1 mL). The resulting solid was suspended in 1-propanol/water (9/1) (2 mL) and dissolved by heating under reflux. The solution was cooled to room temperature over one hour. The precipitated solid was collected by filtration. The resulting solid was dried under reduced pressure at 50° C. to give the title compound (872 mg). The instrumental data were identical to those of the title compound synthesized in Example 4.

Provenance & Evidence