反应 #1350579

反应方程式

3-(3-aminophenyl)-4-bromo-1-methylpyrazole

2-methoxyphenylacetic acid

1-hydroxybenzotriazole hydrate

2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluoro-phosphate

N, N-Diisopropyl-ethylamine

→

title compound

收率 38.0%

N-[3-(4-bromo-1-methylpyrazol-3-yl)phenyl]-2-(2-methoxyphenyl)acetamide

收率 38.0%

溶剂

chloroform

brine

反应条件

后处理

1. 1
   洗涤the organic layer washed with further brine
2. 2
   干燥dried over magnesium sulphate
3. 3
   浓缩concentrated in vacuo
4. 4
   其他The crude product was purified by column chromatography (chloroform-methanol, 99:1)

实验过程

A mixture of 3-(3-aminophenyl)-4-bromo-1-methylpyrazole (30 mg, 0.12 mmol), 2-methoxyphenylacetic acid (20 mg, 0.12 mmol), 1-hydroxybenzotriazole hydrate (16 mg, 0.12 mmol) and 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluoro-phosphate (46 mg, 0.12 mmol) were dissolved in chloroform (1.5 ml). N, N-Diisopropyl-ethylamine (0.02 ml, 0.13 mmol) was added and the mixture stirred at room temperature for 16 h. The reaction mixture was then poured into brine and the organic layer washed with further brine, dried over magnesium sulphate and then concentrated in vacuo. The crude product was purified by column chromatography (chloroform-methanol, 99:1), giving the title compound (18 mg, 38%) as a colourless solid. Rf 0.65 (chloroform-methanol, 98:2).

来源