反应详情

2-{5-Bromo-6-oxo-4-[(1R,2R,3R,5S)-2,6,6-trimethylbicyclo[3.1.1]hept-3-ylamino]pyridazin-1(6H)-yl}-N-(pyridin-4-ylmethyl)acetamide (62 mg, 0.131 mmol), cyclopropylboronic acid (45 mg, 0.524 mmol), [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium (II) (13 mg, 0.013 mmol) and potassium carbonate (72 mg, 0.524 mmol) in 1,4-dioxane-water (9/1, 0.7 mL) were stirred in a nitrogen stream at 100° C. for 6 hours. After cooling the reaction solution was concentrated, and the resulting residue was purified by silica gel chromatography (chloroform/methanol=8/1) to give the desired product (42 mg, 74% yield).

1. temperatureAfter cooling the reaction solution
2. concentrationwas concentrated
3. customthe resulting residue was purified by silica gel chromatography (chloroform/methanol=8/1)