反应详情

402 mg (1.27 mmol) 2-Methyl-6-(5-piperidine-4-yl-2H-[1,2,4]triazole-3-yl)-pyridine×2HCl are dissolved in 10 mL NMP. After addition of 0.43 mL triethylamine the reaction mixture is stirred for one hour. 500 mg (1.27 mmol) 6-(2,6-Difluorophenyl)-5-(4-formylphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid methyl ester and 0.13 mL acetic acid are added. The reaction mixture is stirred over night at room temperature. 296.3 mg (1.40 mmol) NaBH(OAc)3, are added in portions and the reaction mixture is stirred at room temperature for 5 hours. After treatment of the reaction mixture with saturated NaHCO3 the precipitate is filtered off, washed with water and dried. After chromatography of the precipitate on silica gel (dichloromethane/methanol) 368.6 mg (44.4%) 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 5 hours
3. filtrationAfter treatment of the reaction mixture with saturated NaHCO3 the precipitate is filtered off
4. washwashed with water
5. customdried