反应详情

温度

75 °C

To 3-[5-bromo-2-oxo-3-[[1-[2-(phenylmethoxy)phenyl]cyclopropyl]amino]-1(2H)-pyrazinyl]-5-fluoro-4-methyl-benzoic acid, methyl ester (Example 259a, 9.2 g) in ethanol (400 mL) was added ammonium formate (14.04 g) and 10% Pd/C (1.693 g). The reaction was heated at 75° C. for 1 h, filtered through celite washing the celite with further warm ethanol (100 mL) followed by dichloromethane (2000 mL) and the combined filtrates were evaporated, diluted with dichloromethane (1000 mL) and washed with water, dried (MgSO4) and evaporated to give the subtitle compound (6.16 g).

1. filtrationfiltered through celite
2. washwashing the celite
3. temperaturewith further warm ethanol (100 mL)
4. customthe combined filtrates were evaporated
5. additiondiluted with dichloromethane (1000 mL)
6. washwashed with water
7. dry with materialdried (MgSO4)
8. customevaporated