反应详情

温度

50 °C

A mixture of (2S,4S)-2-carbamoyl-4-fluoro-pyrrolidine-1-carboxylic acid tert-butyl ester (1.0 g), conc. Hydrochoric acid (0.6 ml) and 1-butanol (10 ml) is heated for 48 hours at 50° C. The reaction mixture is evaporated and partitioned dichloromethane and aqueous sodium bicarbonate, the dichloromethane layers are dried over sodium sulphate and evaporated. A solution of 7M ammonia in methanol (10 ml) is added to the residue and the mixture is stood for 60 hours at room temperature in a sealed vessel. Evaporation and trituration with ethanol gives the title compound as a white solid.

1. customThe reaction mixture is evaporated
2. custompartitioned dichloromethane and aqueous sodium bicarbonate
3. dry with materialthe dichloromethane layers are dried over sodium sulphate
4. customevaporated
5. additionA solution of 7M ammonia in methanol (10 ml) is added to the residue
6. customEvaporation and trituration with ethanol