تفاعل #48655

معادلة التفاعل

triethylamine

acetic anhydride

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

→

title compound

المردود 45.5%

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

المردود 45.5%

المذيبات

tetrahydrofuran

ظروف التفاعل

المعالجة

1. 1
   تركيزConcentrate
2. 2
   أخرىpurify
3. 3
   غسيل(silica gel chromatography, eluting with 50:50 to 60:40 ethyl acetate:hexanes)

الإجراء التجريبي

Add triethylamine (0.009 mL, 0.066 mmol) and acetic anhydride (0.004 mL, 0.044 mmol) to a solution of (2R,5R)-(5-[(1S,2S)-2-amino-3-(3,5-difluorophenyl)-1-hydroxypropyl]-2-phenoxymethyl-morpholine-4-carboxylic acid tert-butyl ester (0.021 g, 0.044 mmol) in tetrahydrofuran (0.44 mL) and stir at room temperature for 1 hour. Concentrate and purify (silica gel chromatography, eluting with 50:50 to 60:40 ethyl acetate:hexanes) to give the title compound as a white foam (0.010 g, 45.5%).

المصدر