反应详情

A solution of 9-benzyloxy-2-methyl-6-(1-pyrrolo[2,3-b]pyridin-1-yl-cyclopentylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione (407) (60 mg, 0.12 mmol) in ethanol (10 mL) was degassed, Pd—C (10%) (6 mg) added and hydrogenated for 40 min (hydrogen bludder) (TLC, 5% methanol in dichloromethane, Rf=0.2). The catalyst was filtered of and washed with 10% dichloromethane in ethanol (3×20 mL). The combined solvents were concentrated and the resulting sticky solid was washed with pentane to get pure 9-hydroxy-2-methyl-6-(1-pyrrolo[2,3-b]pyridin-1-yl-cyclopentylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione (408) (38 mg, 78%) as an off-white solid.

1. filtrationThe catalyst was filtered of and
2. washwashed with 10% dichloromethane in ethanol (3×20 mL)
3. concentrationThe combined solvents were concentrated
4. washthe resulting sticky solid was washed with pentane