反应详情

A solution of 4-chloro-6-(3-chloro-4-trifluoromethyl-phenyl)-pyrimidine (0.200 g, 0.68 mmol), (R,R)-2-methyl-propane-2-sulfinic acid [2-amino-1-(4-fluoro-phenyl)-ethyl]-amide (0.720 g, 2.79 mmol) and DIPEA (0.18 mL, 1.02 mmol) in DMF (5 mL) was heated at 80° C. for 16 h. The reaction mixture was cooled to rt, diluted with EtOAc (20 mL) and washed with NaCl (sat. aq., 2×30 mL). The organic layer was dried (MgSO4) and concentrated under reduced pressure. The crude residue was purified (FCC) to give the title compound (0.172 g, 50%) as a yellow solid. MS (ESI+): calcd for C23H23ClF4N4OS m/z 514.12. found 515.1 (M+H)+.

1. washwashed with NaCl (sat. aq., 2×30 mL)
2. dry with materialThe organic layer was dried (MgSO4)
3. concentrationconcentrated under reduced pressure
4. customThe crude residue was purified (FCC)