反应 #313395

反应方程式

ammonium chloride

3-methoxybenzylamine

(1R,2S)-[2-(3,4-difluoro-phenyl)-1-oxiranyl-ethyl]-carbamic acid tert-butyl ester

lithium triflate

→

(1S,2R)-[1-(3,4-Difluoro-benzyl)-2-hydroxy-3-(3-methoxy-benzylamino)-propyl]-carbamic acid tert-butyl ester

溶剂

acetonitrile

反应条件

后处理

1. 1
   workup.STIRRINGThe reaction was stirred at ambient temperature for 14 hours
2. 2
   萃取extracted with ethyl acetate
3. 3
   其他the organic phase separated
4. 4
   干燥dried (MgSO4)
5. 5
   其他the solvent removed at reduced pressure
6. 6
   其他The product was obtained as an oil
7. 7
   其他used without further purification (0.041 g, 94%)

实验过程

A solution of (1R,2S)-[2-(3,4-difluoro-phenyl)-1-oxiranyl-ethyl]-carbamic acid tert-butyl ester (0.03 g, 0.1 mmol) in acetonitrile (1 mL) was treated with lithium triflate (0.032 g, 0.2 mmol) and stirred at ambient temperature for 20 minutes. Then 3-methoxybenzylamine (0.016 mL, 0.12 mmol) was added to the reaction neat in one portion. The reaction was stirred at ambient temperature for 14 hours. The reaction was poured into saturated ammonium chloride solution (5 mL), extracted with ethyl acetate, the organic phase separated, dried (MgSO4) and the solvent removed at reduced pressure. The product was obtained as an oil and used without further purification (0.041 g, 94%). MS: 437 (M+H, 100%).

来源