反应详情

To a solution of (S)-pyrrolidine-2-carboxylic acid cyclopropylamide (3.4 mmol) in THF (5 mL) at 0° C. was added BH3 (6.3 mL, 1 M in THF) dropwise. It was then warmed to room temperature and heated to reflux for 20 hours. The cooled reaction was acidified with 3M HCl (2.5 mL) and stirred at 75° C. for 10 minutes. The reaction was concentrated and the residue was basified with 2M NaOH. It was then extracted with 10% of methanol in dichloromethane. The organic layer was dried and concentrated to give a yellow oil of cyclopropyl-(S)-1-pyrrolidine-2-ylmethyl-amine.

1. temperatureheated
2. temperatureto reflux for 20 hours
3. customThe cooled reaction
4. concentrationThe reaction was concentrated
5. extractionIt was then extracted with 10% of methanol in dichloromethane
6. customThe organic layer was dried
7. concentrationconcentrated