反应详情

Under an atmosphere of nitrogen to a solution of a 7.11 g of (R)-4-chloromethyl-[1,3,2]dioxathiolane 2,2-dioxide (MW=156.59; 1.38 eq.) in 95 mL of acetonitrile were added 6.34 g of 4-(4-aminophenyl)-morpholin-3-one (APMO) (MW=192.22; 1 eq.) and 3.29 g (MW=138.21; 0.72 eq.) of potassium carbonate. The reaction mixture was stirred for 24 h at room temperature. Then the resulting suspension was cooled to 0° C. After stirring for at least 2 h at this temperature, the product was isolated by filtration and the filter cake was washed with 50 mL of acetonitrile. After drying in vacuo at 30° C., 12.09 g of the crystalline title compound (MW=402.90) were isolated. Yield=91.0%.

1. temperatureThen the resulting suspension was cooled to 0° C
2. stirringAfter stirring for at least 2 h at this temperature
3. customthe product was isolated by filtration
4. washthe filter cake was washed with 50 mL of acetonitrile
5. customAfter drying in vacuo at 30° C.