反应详情

温度

0 °C

TEA (1.05 mL, 7.5 mmol) was added to a solution of (R)-3-(aminomethyl)-1-N-Boc-pyrrolidine (1 g, 5 mmol) in DCM (25 mL) at 0° C. Methanesulfonyl chloride (0.43 mL, 5.5 mmol) was then added. After stirring at 0° C. for 2 h, the reaction mixture was diluted with water. The organic phase was separated, dried (MgSO4), filtered and concentrated. The crude material was treated with 1M HCl in MeOH (25 mL) at RT and stirred at RT for 20 h. The volatiles were removed under reduced pressure to afford 0.95 g of 72 as a white solid.

1. customThe organic phase was separated
2. dry with materialdried (MgSO4)
3. filtrationfiltered
4. concentrationconcentrated
5. additionThe crude material was treated with 1M HCl in MeOH (25 mL) at RT
6. stirringstirred at RT for 20 h
7. customThe volatiles were removed under reduced pressure