反应详情

温度

130 °C

A mixture of [3-(6-bromo-pyridin-2-yl)-imidazo[1,2-a]pyrazin-8-yl]-(2-morpholin-4-yl-ethyl)-amine (from Example 41 supra) (0.403 g, 1.0 mmol), [2-amino-2-(3-chloro-phenyl)-ethyl]-carbamic acid tert-butyl ester (from Example 78 supra) (0.406 g, 1.5 mmol), Pd2(dba)3(60 mg), Davephos (80 mg), K2CO3 (207 mg, 1.5 mmol) in dioxane (25 mL) in a sealed tube was bubbled with N2 for several minutes and then heated under N2 at 130° C. overnight. The solution was then cooled to room temperature and filtered. The filtrate was concentrated under reduced pressure. The obtained residue was purified by chromatography (CH2Cl2:MeOH, 50:1 to 20:1) to give crude (2-(3-chloro-phenyl)-2-{6-[8-(2-morpholin-4-yl-ethylamino)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-ylamino}-ethyl)-carbamic acid tert-butyl ester. (Yield 210 mg). LC-MS: [M+H]+ 593.

1. customwas bubbled with N2 for several minutes
2. temperatureThe solution was then cooled to room temperature
3. filtrationfiltered
4. concentrationThe filtrate was concentrated under reduced pressure
5. customThe obtained residue was purified by chromatography (CH2Cl2:MeOH, 50:1 to 20:1)