反应详情

温度

60 °C

5.74 g (59.7 mmol) of ammonium carbonate and 1.46 g (29.8 mmol) of sodium cyanide were dissolved in 33 ml of water. 2.57 g (14.9 mmol) of a solution of the compound from Example 12A in 33 ml of ethanol were added dropwise at room temperature and the mixture was stirred at 60° C. overnight. The reaction mixture was concentrated to a quarter of its original volume and extracted repeatedly with dichloromethane and ethyl acetate, and the organic phases were dried over sodium sulphate, filtered and concentrated. This gave 675 mg (19% of theory) of the title compound as a diastereomer mixture which was reacted without further purification.

1. concentrationThe reaction mixture was concentrated to a quarter of its original volume
2. extractionextracted repeatedly with dichloromethane and ethyl acetate
3. dry with materialthe organic phases were dried over sodium sulphate
4. filtrationfiltered
5. concentrationconcentrated
6. customThis gave 675 mg (19% of theory) of the title compound as a diastereomer mixture which was reacted without further purification