反应 #48656

反应方程式

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

hydrogen

→

desired compound

收率 88.3%

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

收率 88.3%

溶剂

ethanol

反应条件

后处理

1. 1
   其他flush with nitrogen
2. 2
   workup.ADDITIONdilute slurry with ethanol (175 mL)
3. 3
   过滤filter through a filtering agent
4. 4
   洗涤wash with ethanol
5. 5
   浓缩concentrate

实验过程

Dissolve (1S,2S)-5-(R)-[1-benzyloxy-2-dibenzylamino-3-(3,5-difluorophenyl)-propyl]-2-(R)-benzyloxymethylmorpholine-4-carboxylic acid tert-butyl ester (4.750 g, 6.226 mmol) in ethanol (63 mL) and add 20% palladium hydroxide on carbon (4.750 g). Stir under one atmosphere of hydrogen gas for 42 hours, flush with nitrogen, dilute slurry with ethanol (175 mL), filter through a filtering agent, wash with ethanol and concentrate to give the desired compound (2.213 g, 88.3%).

来源