Реакция #48671

Уравнение реакции

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

Растворители

tetrahydrofuran

ethyl acetate

Условия реакции

Обработка

1. 1
   ПромывкаWash with water and saturated aqueous sodium chloride
2. 2
   Сушкаdry (magnesium sulfate)
3. 3
   Фильтрацияfilter
4. 4
   Концентрированиеconcentrate
5. 5
   ДругоеPurify on silica gel
6. 6
   Промывкаeluting with 20

Методика

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.

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