反应详情

(2S,4S)-1-[2-[(4-Ethoxycarbonylbicyclo[2.2.2]-oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carboxamide (1.00 g) was dissolved in 2-propanol (10 mL) with heating, and a solution of 4-toluenesulfonic acid monohydrate (541 mg) in 2-propanol (4 mL) was added thereto. After ice-cooling and subsequent 1 hour of stirring, the precipitate were collected by filtration, washed with 2-propanol (5 mL) and then blast-dried at 60° C., thereby obtaining a colorless solid of (2S,4S)-1-[2-[(4-ethoxycarbonylbicyclo[2.2.2]-oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carboxamide 4-toluenesulfonate (1.28 g, yield: 88%).

1. temperaturewith heating
2. temperatureAfter ice-cooling and subsequent 1 hour
3. filtrationthe precipitate were collected by filtration
4. washwashed with 2-propanol (5 mL)
5. customblast-dried at 60° C.