反应详情

147.6 mg 2-(5-Azetidine-3-yl-[1,2,4]triazole-3-yl)-pyridine×2HCl (intermediate example 44.0) are dissolved in 4.3 ml NMP. After addition of 0.16 ml triethylamine the reaction mixture is stirred for one hour. 192 mg (0.49 mmol) 4-(3-Bromo-2-methyl-6-phenylimidazo[1,2-a]pyrimidin-7-yl)benzaldehyde and 0.05 mL acetic acid are added and the reaction mixture is stirred for 23 hours at room temperature. 114.1 mg (0.54 mmol) NaBH(OAc)3, are added in portions and the reaction mixture is stirred at room temperature for three days. The reaction mixture is treated with 30 mL saturated NaHCO3 and stirred for 45 minutes. The precipitate is filtered off, washed with water and dried. After chromatography of the precipitate on silica gel (dichloromethane/methanol) 3.5 mg (1.2%) of the desired product are obtained.

1. stirringthe reaction mixture is stirred for 23 hours at room temperature
2. stirringthe reaction mixture is stirred at room temperature for three days
3. stirringstirred for 45 minutes
4. filtrationThe precipitate is filtered off
5. washwashed with water
6. customdried