反应详情

A solution of (S)-3-(2-chloropyrimidin-4-yl)-4-isopropyloxazolidin-2-one (90 mg, 0.37 mmol), iPr2NEt (0.455 mL, 2.61 mmol, 7.0 equiv) and 1-(biphenyl-4-yl)ethanamine hydrochloride (87 mg, 0.37 mmol) in DMSO (1 mL) was heated at 110° C. for 2 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 10 to 50%) provided (S)-3-(2-((R)-1-(biphenyl-4-yl)ethylamino)pyrimidin-4-yl)-4-isopropyloxazolidin-2-one and (S)-3-(2-((S)-1-(biphenyl-4-yl)ethylamino)pyrimidin-4-yl)-4-isopropyloxazolidin-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