反应详情

温度

170 °C

(1-bromo-4-chloro-imidazo[1,2-a]quinoxaline (intermediate example 1.1, 1 mL, 0.2M in NMP), 2-amino-ethanol (2 eq, 0.8 mL, 0.5 M in NMP) and DIPEA (3 eq, 103 μL) were combined in a sealed vial and heated at 170° C. under microwave irradiation for 60 min. After cooling, [4-[(cyclopropylamino)carbonyl]phenyl]-boronic acid (1.5 eq, 0.3 mL, 1 M in NMP), Pd(dppf)Cl2 (0.1 eq, 533 μL, 0.0375 M in NMP) and potassium carbonate (600 μL, 1M in water) were added and the mixture was heated at 140° C. under microwave irradiation for 40 min. After cooling, the solution was filtered and subjected to preparative HPLC to give N-cyclopropyl-4-[4-(2-hydroxy-ethylamino)-imidazo[1,2-a]quinoxalin-1-yl]-benzamide (10.19 mg, 13%): UPLC-MS: RT==0.82 min; m/z (ES+) 388.4 [MH+]; required MW=387.4.

1. temperatureAfter cooling
2. temperaturethe mixture was heated at 140° C. under microwave irradiation for 40 min
3. temperatureAfter cooling
4. filtrationthe solution was filtered