反应详情

The procedure in Example 18, Step 4, starting from 2-chloro-3-[(2R)-2-methylpiperazin-1-yl]pyrazine* (0.48 g, 2.28 mmol) and 2-({2-[3-(dimethylamino)propyl]pyridin-3-yl}oxy)ethanol (from Step 1; 0.46 g, 2.07 mmol) was followed. The crude product was purified on a column of silica (100 mm, i.d.=30 mm) with CHCl3/MeOH/NH4OH (80:20:0.5; 200 mL, followed by 60:40:1) as eluent to give 0.48 g (58%) of the title compound as a colorless oil. HRMS m/z calcd for C21H32N6O2 (M)+ 400.2587. found 400.2571. *Reported in WO 00/76984, Example 192, Step 2.

1. customThe crude product was purified on a column of silica (100 mm, i.d.=30 mm) with CHCl3/MeOH/NH4OH (80:20:0.5; 200 mL, followed by 60:40:1) as eluent