تفاعل #313395

معادلة التفاعل

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

المذيبات

acetonitrile

ظروف التفاعل

المعالجة

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

الإجراء التجريبي

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%).

المصدر