反应详情

温度

75 °C

To Methyl 3-(3-(1-(2-(benzyloxy)phenyl)cyclopropylamino)-5-bromo-2-oxopyrazin-1(2H)-yl)-4-methylbenzoate (Example 167b, 543 mg) in ethanol (15 mL) was added ammonium formate (855 mg) and 10% Pd/C (103 mg) and the reaction was heated at 75° C. for 1 h. The mixture was filtered through celite and the solids washed with ethanol. The filtrate was collected and the volatiles removed in vacuo to give a pale yellow solid. Dichloromethane and water were added and the organic layer separated. The aqueous layer was further extracted with dichloromethane and ethyl acetate. The combined organic extracts were dried (Na2SO4) and the solvent removed in vacuo to give the subtitle product an off white foam (331 mg).

1. filtrationThe mixture was filtered through celite
2. washthe solids washed with ethanol
3. customThe filtrate was collected
4. customthe volatiles removed in vacuo
5. customto give a pale yellow solid
6. customthe organic layer separated
7. extractionThe aqueous layer was further extracted with dichloromethane and ethyl acetate
8. dry with materialThe combined organic extracts were dried (Na2SO4)
9. customthe solvent removed in vacuo