Cesium carbonate → HCID 11518118, compound

Participants

Reaction Conditions

Reaction Steps

5-chloro-2-methyl-3-{4-[3-(1-piperidinyl)propoxy]phenyl}-4(3H)-quinazolinone synthesized in Example 27 (100 mg, 0.24 mmol), phenylboric acid (90 mg, 0.73 mmol) and cesium carbonate (480 mg, 1.45 mmol) were mixed in 1,4-dioxane (1 mL), and the atmosphere in the system was replaced by nitrogen. Pd2(dba)3 (15 mg, 0.012 mmol) and tri-t-butylphosphine (10 mg, 0.036 mmol) were added, and stirred at 100° C. for 12 hours. Distilled water was added to the reaction mixture, and the mixture extracted with chloroform. The organic phase was washed by saturated brine, and dried with anhydrous sodium sulfate. The product was purified by thin layer silica gel chromatography, and the title compound (20 mg, 18%) was obtained as a colorless solid.

Provenance & Evidence