反应详情

To a solution of (S)-3-((R)-6-(4-fluoro-3-methylbenzyloxy)-2-(4-fluoro-3-methylphenoxy)hexanoyl)-4-isopropyloxazolidin-2-one (100 mg, 0.20 mmol) dissolved in 2 mL of THF, methanol, and 50 wt % NH2OH in H2O (2:2:1) was added KCN (4.0 mg, 0.06 mmol). The resulting mixture stirred for 3 days at room temperature. The reaction was quenched by the addition of 1M aqueous HCl (10 mL) and the resulting mixture extracted with ethyl acetate (3×10 mL). The combined organic layers were washed with brine (2×5 mL). The product was isolated by flash column chromatography eluting with 0% to 10% methanol/DCM to give the title compound (54.2 mg) as colorless oil.

1. customThe reaction was quenched by the addition of 1M aqueous HCl (10 mL)
2. extractionthe resulting mixture extracted with ethyl acetate (3×10 mL)
3. washThe combined organic layers were washed with brine (2×5 mL)
4. customThe product was isolated by flash column chromatography
5. washeluting with 0% to 10% methanol/DCM