Реакция #42303

Уравнение реакции

3-(cyanomethyl)-5-[(dipropylamino)carbonyl]benzoic acid

3-(aminocarbonyl)-5-[(dipropylamino)carbonyl]benzoic acid

(2R,3S)-3-amino-1-[(3-methoxybenzyl)amino]-4-phenyl-2-butanol

(2R,3S)-3-amino-4-(3,5-difluorophenyl)-1-[(3-methoxybenzyl)amino]-2-butanol trifluoroacetate

HATU

→

title compound

N1-{(1S,2R)-1-benzyl-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl}-5-(cyanomethyl)-N3,N3-dipropylisophthalamide

Растворители

dichloromethane

Условия реакции

Обработка

1. 1
   Другоеovernight
2. 2
   ТемператураAfter cooling
3. 3
   Промывкаthe mixture is washed with water
4. 4
   Другоеthe organic phase is separated
5. 5
   Сушкаdried over magnesium sulfate

Методика

A mixture of 3-(cyanomethyl)-5-[(dipropylamino)carbonyl]benzoic acid (IX, 0.13 g), (2R,3S)-3-amino-1-[(3-methoxybenzyl)amino]-4-phenyl-2-butanol (VIII, 0.14 g), HATU (0.17 g), and dichloromethane (10 mL) is stirred at 40 degrees C. overnight. After cooling, the mixture is washed with water and the organic phase is separated and dried over magnesium sulfate and taken to dryness under reduced pressure. Chromatography (silica gel) gives the title compound, M+H=571.2

Источник