反应详情

A solution of (R)-3-(2-chloropyrimidin-4-yl)-4-phenyloxazolidin-2-one (83 mg, 0.30 mmol) and 1-(3,4-dichlorophenyl)ethanamine (260 mg, 1.37 mmol, 4.5 equiv) in DMSO (1.5 mL) was heated at 110° C. for 1½ h. The reaction mixture was diluted with EtOAc (8 mL) and washed with water (30 mL). After separation, the aqueous phase was extracted with EtOAc (3×8 mL). Combined organics were dried over Na2SO4, filtered and concentrated. Silica gel column chromatography (EtOAc/Heptane 0 to 40%) provided (R)-3-(2-((R)-1-(3,4-dichlorophenyl)ethylamino)pyrimidin-4-yl)-4-phenyloxazolidin-2-one and (R)-3-(2-((S)-1-(3,4-dichlorophenyl)ethylamino)pyrimidin-4-yl)-4-phenyloxazolidin-2-one.

1. washwashed with water (30 mL)
2. customAfter separation
3. extractionthe aqueous phase was extracted with EtOAc (3×8 mL)
4. dry with materialCombined organics were dried over Na2SO4
5. filtrationfiltered
6. concentrationconcentrated