反应详情

温度

20 °C

8-(Benzyloxy)-2-(7-(2-methoxyethoxy)-imidazo[1,2-a]pyridin-3-yl)quinoline (5.0 g, 11.75 mmol) was slurried in MeOH (117.5 ml). Ammonium formate (7.410 g, 117.5 mmol) and Pd(OH)2/C (0.8252 g, 0.5876 mmol) were added. The reaction mixture was heated to reflux for 2 hours, then cooled to 20° C. Formic acid was added to the slurry until solids went into solution. The mixture was filtered and the filter paper was washed with 10% formic acid in methanol. The filtrate was concentrated to an oil. To the oil was added an excess of NH3 in methanol and resulting the solids were concentrated to dryness. Water was added to the solids and the slurry was stirred for 1 hour (pH was 6.5-7.0 by pH paper). The solids were collected by filtration and then taken up in toluene and concentrated to dryness under vacuum dry for 12 hours to obtain 3.8 g (96% yield) of the desired product.

1. temperatureThe reaction mixture was heated
2. temperatureto reflux for 2 hours
3. filtrationThe mixture was filtered
4. washthe filter paper was washed with 10% formic acid in methanol
5. concentrationThe filtrate was concentrated to an oil
6. additionTo the oil was added an excess of NH3 in methanol
7. customresulting the solids
8. concentrationwere concentrated to dryness
9. additionWater was added to the solids
10. filtrationThe solids were collected by filtration
11. concentrationconcentrated to dryness under vacuum
12. customdry for 12 hours