反应详情

154 mg (0.49 mmol) 2-Methyl-6-(5-piperidine-4-yl-2H-[1,2,4]triazole-3-yl)-pyridine×2HCl are dissolved in 4.2 mL NMP. After addition of 0.16 mL triethylamine the reaction mixture is stirred for one hour. 350 mg (50% pure) 2-Cyclopropyl-4-[6-(4-fluorophenyl)-[1,2,4]triazolo[1,5-a]pyrimidin-5-yl]-benzaldehyde and 0.05 mL acetic acid are added. The reaction mixture is stirred over night at room temperature. 113 mg (0.54 mmol) NaBH(OAc)3, are added in portions and the reaction mixture is stirred at room temperature for 18 hours. The reaction mixture is treated with saturated NaHCO3 and stirred for 20 minutes. The precipitate is filtered off, washed with water and dried. After chromatography of the precipitate on silica gel (dichloromethane/methanol) 192.2 mg (63.8%) of the desired product are obtained.

1. stirringThe reaction mixture is stirred over night at room temperature
2. stirringthe reaction mixture is stirred at room temperature for 18 hours
3. stirringstirred for 20 minutes
4. filtrationThe precipitate is filtered off
5. washwashed with water
6. customdried