反应详情

Sodium tetrahydroborate (19 mg, 0.50 mmol) was added to a mixture of 4-acetyl-6-chloro-3-ethoxy-2-(2-oxo-1,3-oxazolidin-5-yl)benzonitrile (100 mg, 0.34 mmol) (racemic mixture from step 3) in methanol (1.6 mL, 38 mmol) at 0° C. and the reaction mixture was stirred at room temperature for 10 minutes and evaporated. The residue was diluted with ethyl acetate, washed with 1 N HCl, brine, dried over sodium sulfate, filtered and concentrated to give the desired compound as a mixture of four diastereomers, 58 mg, 55%. LCMS calculated for C14H16ClN2O4 (M+H)+: m/z=311.1; found: 311.1.

1. customevaporated
2. additionThe residue was diluted with ethyl acetate
3. washwashed with 1 N HCl, brine
4. dry with materialdried over sodium sulfate
5. filtrationfiltered
6. concentrationconcentrated