反应详情

温度

80 °C

To a solution of methyl 4-(2-pyrazinyl)-3-pyridinecarboxylate (400 mg; may be prepared as described in Intermediate 19) in methanol (20 mL) and water (3 mL) LiOH was added (44.5 mg). The reaction mixture was stirred at 80° C. for 2 h. The reaction mixture was filtered to remove the inorganic salts and evaporated in vacuo. The residue was dissolved in MeOH (20 ml), Pd/C (300 mg) was added and the reaction mixture was placed under hydrogen at 3 bar for 2 days. The reaction was monitored by LCMS which showed complete conversion of starting material. Then the catalyst was filtered by means of a celite plug and the filter was washed with MeOH. Then the solvent was evaporated in vacuo and the residue dissolved in 25 ml of MeOH to give a solution of the title compound, used directly in subsequent reactions.

1. filtrationThe reaction mixture was filtered
2. customto remove the inorganic salts
3. customevaporated in vacuo
4. dissolutionThe residue was dissolved in MeOH (20 ml)
5. additionPd/C (300 mg) was added
6. waitthe reaction mixture was placed under hydrogen at 3 bar for 2 days
7. filtrationThen the catalyst was filtered by means of a celite plug
8. washthe filter was washed with MeOH
9. customThen the solvent was evaporated in vacuo
10. dissolutionthe residue dissolved in 25 ml of MeOH