反应详情

Under an atmosphere of argon protective gas, 5-cyano-2-{(4S)-5-cyano-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydropyrimidin-4-yl}benzenesulfonyl chloride (20 mg, 42 μmol) was dissolved in absolute dichloromethane (2.5 ml), morpholine (7.3 μl, 83 μmol; 2 eq.) was added at room temperature and the mixture was stirred overnight. The reaction mixture was then concentrated under reduced pressure and the residue was purified by preparative HPLC (column: Gromsil C-18, 10 μm; mobile phase: acetonitrile/water+0.1% TFA 10:90→90:10). This gave a colorless amorphous solid (8.6 mg, 35% of theory).

1. concentrationThe reaction mixture was then concentrated under reduced pressure
2. customthe residue was purified by preparative HPLC (column: Gromsil C-18, 10 μm; mobile phase: acetonitrile/water+0.1% TFA 10:90→90:10)
3. customThis gave a colorless amorphous solid (8.6 mg, 35% of theory)