反应详情

To a solution of 2-morpholin-4-yl-5,6,7,8-tetrahydropyrido[3,4-b]pyrazine (60 mg, 0.27 mmol) in acetonitrile (5 mL) is added NaI (50 mg, 0.333 mmol), K2CO3 (200 mg, 1.45 mmol) and 2-chloro-1-(4-cyclobutyl-piperazin-1-yl)-ethanone (100 mg, 0.463 mmol). The mixture is stirred overnight at rt. The mixture is diluted with DCM (25 mL) and filtered through Celite. The filtrate is concentrated and the residue is purified by PTLC eluting with EtOAc/MeOH/NEt3 (90:10:10) to yield the title compound. 1H NMR (300 MHz, CDCl3) δ 7.90 (1H, s), 3.85 (2H, m), 3.72 (4H, m), 3.63-3.60 (4H, m), 3.50 (2H, t), 3.40 (2H, s), 2.92-2.87 (3H, m), 2.74-2.69 (2H, m), 2.51 (2H, t), 2.34-2.26 (4H, m), 2.09-1.67 (m, 6H); MS (+VE) m/z 401.26 (M++1).

1. filtrationfiltered through Celite
2. concentrationThe filtrate is concentrated
3. customthe residue is purified by PTLC
4. washeluting with EtOAc/MeOH/NEt3 (90:10:10)