反应详情

温度

135 °C

A sealed tube was charged with the mixture of {4-[3-(6-bromo-pyridin-2-yl)-imidazo[1,2-a]pyrazin-8-ylamino]-cyclohexyl}-carbamic acid tert-butyl ester (from Example 40 supra) (487 mg, 1.0 mmol), compound (2-amino-2-phenyl-ethyl)-carbamic acid tert-butyl ester (from Example 51 supra) (354 mg, 1.5 mmol), Pd2(dba)3(46 mg, 0.05 mmol), Davephos (78 mg, 0.2 mmol), K2CO3 (207 mg, 1.5 mmol) and dioxane (20 mL). The mixture was bubbled with N2 for several minutes and then heated under N2 at 135° C. for 17 hours. The solution was then cooled to room temperature and filtered. The filtrate was concentrated under reduced pressure. The residue was purified by chromatography (CH2Cl2:MeOH, 100:1) to give crude (4-{3-[6-(2-tert-butoxycarbonylamino-1-phenyl-ethylamino)-pyridin-2-yl]-imidazo[1,2-a]pyrazin-8-ylamino}-cyclohexyl)-carbamic acid tert-butyl ester. (Yield 0.38 g).

1. customThe mixture was 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 residue was purified by chromatography (CH2Cl2:MeOH, 100:1)