反应详情

温度

60 °C

To a mixture of 5-hydroxy-1-methyl-6-oxo-2-(1-phenyl-cyclopentylmethyl)-1,6-dihydro-pyrimidine-4-carboxylic acid ethyl ester (175 mg, 0.491 mmol) and methyl amine (0.98 ml, 1.96 mmol, 2M in THF) was added a catalytic amount of Me3AI under argon atmosphere in a sealed tube and it was heated at 60° C. for 16 h. After completion of the reaction, it was quenched with ice slowly and then extracted with EtOAc. The combined organic layer was then washed with water and brine. It was then dried over Na2SO4 and concentrated under vacuum. Purification by preparative HPLC provided the title compound as an off-white solid (40 mg, 24%). LCMS: m/z=342.0 (MH+).

1. additionwas added a catalytic amount of Me3AI under argon atmosphere in a sealed tube
2. customAfter completion of the reaction, it
3. customwas quenched with ice slowly
4. extractionextracted with EtOAc
5. washThe combined organic layer was then washed with water and brine
6. dry with materialIt was then dried over Na2SO4
7. concentrationconcentrated under vacuum
8. customPurification by preparative HPLC