반응 #1350579

반응 방정식

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

수율 38.0%

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

수율 38.0%

용매

chloroform

brine

반응 조건

후처리

1. 1
   세척the organic layer washed with further brine
2. 2
   건조dried over magnesium sulphate
3. 3
   농축concentrated in vacuo
4. 4
   기타The crude product was purified by column chromatography (chloroform-methanol, 99:1)

실험 절차

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).

출처