تفاعل #1350577

معادلة التفاعل

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

2-fluorophenylacetic acid

1-hydroxybenzotriazole hydrate

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

N, N-Diisopropylethylamine

→

title compound

المردود 32.2%

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

المردود 32.2%

المذيبات

chloroform

brine

ظروف التفاعل

المعالجة

1. 1
   غسيلthe organic layer washed with further brine
2. 2
   تجفيفdried over magnesium sulphate
3. 3
   تركيزconcentrated in vacuo
4. 4
   أخرىThe crude product was purified by column chromatography (ethyl acetate-toluene, 1:1)

الإجراء التجريبي

A mixture of 3-(3-aminophenyl)-4-bromo-1-methylpyrazole (30 mg, 0.12 mmol), 2-fluorophenylacetic acid (18 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-Diisopropylethylamine (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 (ethyl acetate-toluene, 1:1), giving the title compound (15 mg, 32%). Rf 0.52 (ethyl acetate-toluene, 1:1).

المصدر