反应详情

Ethyl 4-aminobicyclo[2.2.2]octane-1-carboxylate hydrobromide (612 mg), potassium carbonate (608 mg) and N,N-dimethylformamide (4 mL) were mixed together. To this mixture, (2S,4S)-4-fluoro-1-[2-(benzenesulfonyloxy)acetyl]pyrrolidine-2-carbonitrile (625 mg) was added at 40° C. and the mixture was further stirred for 1 hour. Subsequently, water (10 mL) was added and the resulting crystal was collected by filtration. This product was washed with water (5 mL) and dried at 50° C. under reduced pressure to give (2S,4S)-1-[2-[(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]ac etyl]-4-fluoropyrrolidine-2-carbonitrile as a colorless powder (581 mg, 83% yield). This compound was identical to the compound obtained in Example 7.

1. filtrationthe resulting crystal was collected by filtration
2. washThis product was washed with water (5 mL)
3. customdried at 50° C. under reduced pressure