反应详情

1-(3-Dimethylamino-propyl)-3-ethyl-carbodiimide (EDC, 12 mg) in N,N-dimethylformamide (0.1 mL) is added to a solution of [1-(5-chloro-pyrimidin-2-yl)-piperidin-4-yl]-cyclopropyl-amine (5 mg), 4-(2-methyl-imidazol-1-yl)-benzoic acid (6 mg), 1-hydroxy-benzo-triazole (3 mg), and triethylamine (15 μL) in N,N-dimethylformamide (0.4 mL) at room temperature. The solution is stirred for 18 h and then submitted to chromatography on reversed phase (HPLC, acetonitrile/water/trifluoroacetic acid) to give the pure title compound. LC (method 19): tR=3.97 min; Mass spectrum (ESI+): m/z=437 [M+H]+.