反应详情

To a solution of 3-benzyl-7-(tert-butoxycarbonyl)-3,7-diazabicyclo[3.3.0]-octane hydrochloride (91.1 g, 269 mmol; from step (d) above) in methanol (250 mL) under a N2 atmosphere there was added 10% Pd/C (w/w; 9.8 g). The N2 atmosphere was exchanged for H2 (1 atm of pressure) and the reaction was stirred for 18 h. The reaction was filtered through a pad of cellulose to remove the catalyst. The filtrate was concentrated in vacuo to afford an off-white solid. The solid was slurried in EtOAc and collected. After drying in a vacuum oven for 18 h at 60° C./66.5 Pa (0.5 mm Hg) there was obtained 58.0 g (87%) of the title compound as an off-white solid.

1. filtrationThe reaction was filtered through a pad of cellulose
2. customto remove the catalyst
3. concentrationThe filtrate was concentrated in vacuo
4. customto afford an off-white solid
5. customcollected
6. customAfter drying in a vacuum oven for 18 h at 60° C./66.5 Pa (0.5 mm Hg) there