反应详情

To a nitrogen-purged round bottomed flask was added benzyl 3-(3-chloropyrazin-2-yloxy)azetidine-1-carboxylate (see PREPARATION P20.1; 0.400 g, 0.688 mmol) and Pd/C (0.10 g, 0.094 mmol) and EtOH (10 mL). Hydrogen gas was bubbled through the solution for 1 minute, then a balloon of hydrogen gas was placed atop the round bottomed flask. After 30 minutes, the balloon was removed and the round bottomed flask sealed with a rubber septum. After 16 hours, the reaction was filtered through CELITE® and the cake was washed liberally with EtOAc. The filtrate was concentrated in vacuo to give crude 2-(azetidin-3-yloxy)pyrazine (0.188 g, 181% yield), as a off-white solid. The product was carried forward in the next step without further purification. MS (ESI) m/z 152.1 (MH+).

1. customTo a nitrogen-purged round bottomed flask
2. customHydrogen gas was bubbled through the solution for 1 minute
3. customthe balloon was removed
4. customthe round bottomed flask sealed with a rubber septum
5. waitAfter 16 hours
6. filtrationthe reaction was filtered through CELITE®
7. washthe cake was washed liberally with EtOAc
8. concentrationThe filtrate was concentrated in vacuo