反应详情

温度

80 °C

To the rapidly stirred 80° C. suspension of methanesulfonyl chloride (0.88 g, 7.72 mmol) and sodium bicarbonate (3.24 g, 38.6 mmol) in acetonitrile (400 mL), 3-amino-4-(2,4,5-trifluorophenyl)butanoic acid ((±)-Ia, 1.5 g, 6.43 mmol) is added over period of 2 h. The resulting suspension was further stirred for 16 h at 80° C., after which time the fine suspension was cooled to 0° C. and filtered. The filtrate was evaporated under reduced pressure to afford 1.34 g (96% yield) of racemic 4-(2,4,5-trifluorobenzyl)azetidin-2-one ((±)-IIa) as pale yellow crystalline solid.

1. additionis added over period of 2 h
2. temperatureafter which time the fine suspension was cooled to 0° C.
3. filtrationfiltered
4. customThe filtrate was evaporated under reduced pressure