تفاعل #59046

معادلة التفاعل

[4′-(2-methanesulfonyloxyethoxy)-2′,6′-dimethylbiphenyl-4-yloxy]acetate

4-((1R,2S)-2-amino-1-hydroxypropyl)phenol

Water

ethyl acetate

→

ethyl (4′-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-2′,6′-dimethylbiphenyl-4-yloxy)acetate

المذيبات

N,N-dimethylformamide

ظروف التفاعل

المعالجة

1. 1
   أخرىThe organic layer was separated
2. 2
   غسيلwashed with water and brine
3. 3
   تجفيفdried over anhydrous magnesium sulfate
4. 4
   أخرىThe solvent was evaporated under reduced pressure
5. 5
   أخرىthe residue was purified by silica gel column chromatography (eluent:methylene chloride/methanol=10/1)

الإجراء التجريبي

A mixture of [4′-(2-methanesulfonyloxyethoxy)-2′,6′-dimethylbiphenyl-4-yloxy]acetate and 4-((1R,2S)-2-amino-1-hydroxypropyl)phenol (0.71 g) in N,N-dimethylformamide (10 mL) was stirred at 80° C. overnight. Water and ethyl acetate were added to the reaction mixture. The organic layer was separated, washed with water and brine, and dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel column chromatography (eluent:methylene chloride/methanol=10/1) to afford ethyl (4′-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-2′,6′-dimethylbiphenyl-4-yloxy)acetate (0.47 g).

المصدر