反応 #48657

反応方程式

triethylamine

acetic anhydride

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

→

title compound

収率 68.4%

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

収率 68.4%

溶媒

tetrahydrofuran

反応条件

後処理

1. 1
   濃縮concentrate
2. 2
   その他purify
3. 3
   洗浄(silica gel chromatography, eluting with 6:94 to 9:91 methanol:dichloromethane)

実験手順

Add triethylamine (0.623 mL, 4.473 mmol) and acetic anhydride (0.281 mL, 2.982 mmol) to a solution of (R)-5-[2-(S)-amino-3-(3,5-difluorophenyl)-1-(S)-hydroxypropyl]-2-(R)-hydroxymethylmorpholine-4-carboxylic acid tert-butyl ester (1.20 g, 2.982 mmol) in tetrahydrofuran (30 mL). Stir at room temperature for 45 minutes, concentrate and purify (silica gel chromatography, eluting with 6:94 to 9:91 methanol:dichloromethane) to give the title compound as a white foam (0.906 g, 68.4%).

出典