反应详情

温度

130 °C

To a 5 mL microwave tube is added 4-[(3-Bromo-2-methyl-imidazo[1,2-a]pyrazin-8-ylamino)-methyl]-benzenesulfonamide (0.15 g, 0.379 mmol), 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenol (0.084 g, 0.417 mmol), Na2CO3 (0.1 g, 0.95 mmol), Pd(OAc)2 (approx. 7 mg, 0.028 mmol), and (oxidi-2,1-phenylene)bis(diphenylphosphine) (20 mg, 0.038 mmol). The mixture is suspended in DMF (3 mL) and water (1 mL) and the vessel is sealed under a nitrogen atmosphere. The reaction vessel is heated to 130° C. in the CEM microwave for 20 min then allowed to cool and filtered through Celite and washed with EtOAc. The filtrate is evaporated and the residue is taken up in DMSO and purified by prep HPLC. The product, 4-{[3-(4-Hydroxy-phenyl)-imidazo[1,2-a]pyrazin-8-ylamino]-methyl}-benzenesulfonamide, is obtained as a white solid (15 mg, 10%) LC-MS m/z 410 [M+H]+.

1. temperatureto cool
2. filtrationfiltered through Celite
3. washwashed with EtOAc
4. customThe filtrate is evaporated
5. custompurified by prep HPLC