反应详情

9-benzyloxy-6-[1-(4-chlorophenyl)-cyclopentylmethyl]-2-cyclopropyl-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione (327) (30 mg, 0.06 mmol) was taken up in acetic acid (1 mL) and H2SO4 (0.2 mL) was added slowly to the reaction at 0° C. and stirring was continued at room temperature for 1 h. The reaction was quenched with aqueous saturated NaHCO3 and extracted with ethyl acetate (2×15 ml). The combined extracts were dried and concentrated under reduced pressure. The obtained crude product was purified by preparative HPLC to get 6-[1-(4-chlorophenyl)-cyclopentylmethyl]-2-cyclopropyl-9-hydroxy-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione (328) as an off-white solid (14 mg, 57%).

1. customThe reaction was quenched with aqueous saturated NaHCO3
2. extractionextracted with ethyl acetate (2×15 ml)
3. customThe combined extracts were dried
4. concentrationconcentrated under reduced pressure
5. customThe obtained crude product
6. customwas purified by preparative HPLC