反应详情

温度

0 °C

p-Hydroxyphenylacetamide (1 g) was dissolved in DMF (5 ml) under nitrogen atmosphere and the solution was cooled to 0° C. Cesium fluoride (3.02 g) and sodium iodide (0.1 g) were added thereto and the mixture was stirred for 1 hour. Then (R)-epichlorohydrin (0.62 g, 98.4% e.e.) was added thereto and the mixture was stirred for 30 hours at the same temperature. After the reaction, the reaction mixture was dropped over a period of one hour in isopropylamine (9 g) previously cooled to 10° C. The temperature of the solution was raised to room temperature and stirred for 12 hours. Then the product was treated in the same manner as Example 1 to give 1.53 g of (S)-atenolol (yield 87%, optical purity 98.3% e.e.) as colorless crystals.

1. stirringthe mixture was stirred for 30 hours at the same temperature
2. customAfter the reaction
3. temperaturepreviously cooled to 10° C
4. temperatureThe temperature of the solution was raised to room temperature
5. stirringstirred for 12 hours
6. additionThen the product was treated in the same manner as Example 1