反应详情

150 mg (0.4 mmol) (RS)-2-oxo-1-[4-(4-trifluoromethyl-benzyloxy)-phenyl]-pyrrolidine-3-carboxylic acid is dissolved in 4 ml THF. 59 mg (0.43 mmol) of 1-hydroxybenzotriazole and 80 mg (0.42 mmol) of N-(3-dimethylaminopropyl)-N′-ethyl-carbodiimide-hydrochloride is added and the reaction mixture is stirred at RT for 30 min. After cooling to 0° C. 4 ml of concentrated ammonia is added and the resulting mixture stirred at RT for 1 hour. Dilution with water, extraction and chromatography (silica gel, ethyl acetate) yields 15 mg (10%) of a colorless solid. MS: m/e=379.2 (M+H)+.

1. temperatureAfter cooling to 0° C
2. stirringthe resulting mixture stirred at RT for 1 hour
3. extractionDilution with water, extraction and chromatography (silica gel, ethyl acetate)