反应详情

A mixture of 3-(6-bromo-pyridin-2-yl)-8-(4-methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazine (from Example 39 supra) (0.187 g, 0.5 mmol), benzylamine (0.075 g, 0.7 mmol), Pd2(dba)3 (30 mg), Davephos (40 mg), NaOtBu (70 mg, 0.73 mmol) in dioxane (20 mL) was bubbled with N2 for several minutes and then heated under N2 at reflux overnight. The solution was then cooled to room temperature and filtered. The filtrate was concentrated under reduced pressure. The residue was purified firstly by chromatography (CH2Cl2:CH3OH, 100:1), then by preparative-HPLC to give benzyl-{6-[8-(4-methyl-piperazin-1-yl)-imidazo[1,2-a]pyrazin-3-yl]-pyridin-2-yl}-amine. (Yield 70 mg, 35%). 1HNMR (300 MHz, CDCl3): δ 8.70 (d, 1H, J=4.5 Hz), 7.88 (s, 1H), 7.51-7.24 (m, 7H), 7.02 (d, 1H, J=7.2 Hz), 6.37 (d, 1H, J=8.1 Hz), 5.03-5.02 (m, 1H), 4.62 (d, 2H, J=3.9 Hz), 4.24 (brs, 4H), 2.61-2.58 (m, 4H), 2.36 (s, 3H). LC-MS: [M+H]+ 400.

1. customwas bubbled with N2 for several minutes
2. temperatureheated under N2
3. temperatureat reflux overnight
4. filtrationfiltered
5. concentrationThe filtrate was concentrated under reduced pressure
6. customThe residue was purified firstly by chromatography (CH2Cl2:CH3OH, 100:1)