反应详情

A mixture of 3-(6-bromo-pyridin-2-yl)-8-chloro-imidazo[1,2-a]pyrazine (from Example 38 supra) (1.44 g, 4.65 mmol), 1-methylpiperazine (2.1 g, 21 mmol), and diisopropylethylamine (2.7 g, 21 mmol) in 2-propanol (300 mL) was stirred and heated at reflux overnight. The solution was then cooled to room temperature, concentrated under reduced pressure. The resulted solid was washed with water, partitioned between CH2Cl2 and brine. The organic layer was dried over Na2SO4 and filtered. The filtrate was concentrated under reduced pressure. The crude product was purified by chromatography (CH2Cl2:CH3OH, 100:1) to give 3-(6-bromo-pyridin-2-yl)-8-(4-methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazine. (Yield 1.27 g, 73%).

1. temperatureheated
2. temperatureat reflux overnight
3. concentrationconcentrated under reduced pressure
4. washThe resulted solid was washed with water
5. custompartitioned between CH2Cl2 and brine
6. dry with materialThe organic layer was dried over Na2SO4
7. filtrationfiltered
8. concentrationThe filtrate was concentrated under reduced pressure
9. customThe crude product was purified by chromatography (CH2Cl2:CH3OH, 100:1)