反应详情

温度

110 °C

To a 15 mL microwave reaction vial was added 6-chloro-2-methyl-4-(4-methyl-3,4,5,6-tetrahydro-2H-[1,2]bipyrazinyl-5′-ylamino)-2H-pyridazin-3-one (71 mg, 211 μmol, Eq: 1.00) in 7 mL n-butanol and 1.4 mL water. Argon was bubbled through the suspension. To the slurry was added potassium (2-(acetoxymethyl)-3-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)phenyl)trifluoroborate (149 mg, 211 μmol, Eq: 1.00), then X-PHOS (15.1 mg, 31.7 μmol, Eq: 0.15) with stirring. To this mixture was added bis(dibenzylideneacetone)palladium (9.12 mg, 15.9 μmol, Eq: 0.075). The tube was sealed and heated at 110° C. (bath temp) for 3 hrs then cooled to room temperature. A solution of NaOH (84 mg, 2.11 mmol, 10 eq) in water (1.5 mL) was added and the reaction was stirred for 3 days.

1. customTo a 15 mL microwave reaction
2. customArgon was bubbled through the suspension
3. customThe tube was sealed
4. temperaturethen cooled to room temperature