반응 #313395

반응 방정식

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

용매

acetonitrile

반응 조건

후처리

1. 1
   workup.STIRRINGThe reaction was stirred at ambient temperature for 14 hours
2. 2
   추출extracted with ethyl acetate
3. 3
   기타the organic phase separated
4. 4
   건조dried (MgSO4)
5. 5
   기타the solvent removed at reduced pressure
6. 6
   기타The product was obtained as an oil
7. 7
   기타used without further purification (0.041 g, 94%)

실험 절차

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%).

출처