반응 #48694

반응 방정식

(2R,3S,5R)-5-[(1S,2S)-1-benzyloxy-2-dibenzylamino-3-(3,5-difluorophenyl)-propyl]-2-(2,2-dimethylpropoxy)-3-methylmorpholine-4-carboxylic acid tert-butyl ester

→

desired compound

수율 97.3%

(2R,3S,5R)-5-[(1S,2S)-2-Amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2-(2,2-dimethylpropoxy)-3-methylmorpholine-4-carboxylic acid tert-butyl ester

수율 97.3%

용매

ethyl acetate

반응 조건

후처리

1. 1
   여과Filter the suspension through a pad
2. 2
   여과of filtering agent
3. 3
   세척wash with ethyl acetate
4. 4
   농축concentrate

실험 절차

Stir (2R,3S,5R)-5-[(1S,2S)-1-benzyloxy-2-dibenzylamino-3-(3,5-difluorophenyl)-propyl]-2-(2,2-dimethylpropoxy)-3-methylmorpholine-4-carboxylic acid tert-butyl ester (645 mg, 0.87 mmol) and 20% palladium hydroxide on carbon (60% moisture, 645 mg) in ethyl acetate (10 mL) under one-atmosphere of hydrogen gas at room temperature overnight. Filter the suspension through a pad of filtering agent, wash with ethyl acetate and concentrate to give the desired compound (400 mg, 97%).

출처