反应 #42303

反应方程式

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

溶剂

dichloromethane

反应条件

后处理

1. 1
   其他overnight
2. 2
   温度After cooling
3. 3
   洗涤the mixture is washed with water
4. 4
   其他the organic phase is separated
5. 5
   干燥dried over magnesium sulfate

实验过程

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

来源