9-benzyloxy-2-cyclopropyl-6-(1-phenyl-cyclopentylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione → 2-cyclopropyl-9-hydroxy-6-(1-phenyl-cyclopentylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione

Participants

Reaction Steps

A solution of 9-benzyloxy-2-cyclopropyl-6-(1-phenyl-cyclopentylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione (286) (180 mg, 0.38 mmol) in ethanol (20 mL) was degassed, Pd—C (10%) (15 mg) added and hydrogenated for 1 h. The catalyst was filtered off, washed with ethanol (3×20 mL) and dichloromethane (2×15 mL), The combined solvent was concentrated and the solid was washed with n-pentane to get pure 2-cyclopropyl-9-hydroxy-6-(1-phenyl-cyclopentylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione (287) (140 mg, 96.25%) as a white solid.

Provenance & Evidence