反应详情

21.5 g 2,5-difluoro-nitrobenzene, 52.3 g 1-benzyl-4-amino-piperidine and 100 ml N-methyl-piperidone were stirred at 100° C. for 3 h. After cooling the mixture was treated distributed between water and ethyl acetate and the aqeous layer was extracted 2× with ethyl acteate. The combined organic layers were extracted 5× with water, and the solvent was removed by evaporation. The target compound was crystallized from methanol to yield 38.7 g orange crystals (mp. 86–87° C.).

1. temperatureAfter cooling the mixture
2. additionwas treated
3. extractionthe aqeous layer was extracted 2× with ethyl acteate
4. extractionThe combined organic layers were extracted 5× with water
5. customthe solvent was removed by evaporation
6. customThe target compound was crystallized from methanol