反应详情

2-(1H-Benzotriazol-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate (75 mg) and ethyldiisopropylamine (74 μL) are added to a solution of 2-imidazol-1-yl-pyrimidine-5-carboxylic acid (40 mg) in N,N-dimethylformamide (5 mL) at room temperature. The solution is stirred for 10 min prior to the addition of cyclopropyl-[1-(3-phenyl-[1,2,4]oxadiazol-5-yl)-piperidin-4-yl]amine (60 mg). The resulting mixture is stirred at 60° C. for 3 h, cooled to room temperature over night, and concentrated in vacuo. The crude product is purified by HPLC(H2O/MeOH/TFA). LC (method 1): tR=1.50 min; Mass spectrum (ESI+): m/z=457 [M+H]+.

1. stirringThe resulting mixture is stirred at 60° C. for 3 h
2. concentrationconcentrated in vacuo
3. customThe crude product is purified by HPLC(H2O/MeOH/TFA)