反応 #48671

反応方程式

triethylamine

acetic anhydride

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

→

title compound

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

溶媒

tetrahydrofuran

ethyl acetate

反応条件

後処理

1. 1
   洗浄Wash with water and saturated aqueous sodium chloride
2. 2
   乾燥dry (magnesium sulfate)
3. 3
   ろ過filter
4. 4
   濃縮concentrate
5. 5
   その他Purify on silica gel
6. 6
   洗浄eluting with 20

実験手順

Add triethylamine (0.030 g, 0.30 mmol) and acetic anhydride (0.024 g, 0.23 mmol) to (R)-5-[(1S,2S)-2-amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2-ethoxymorpholine-4-carboxylic acid tert-butyl ester (0.095 g, 0.228 mmol) in tetrahydrofuran (4 mL) at room temperature. Stir 4 hours and dilute with ethyl acetate. Wash with water and saturated aqueous sodium chloride, dry (magnesium sulfate), filter and concentrate. Purify on silica gel, eluting with 20:80 to 100% ethyl acetate:hexanes to give the title compound.

出典