反应详情

Into a vial were added 1-(3-oxomorpholino)cyclopropanecarboxylic acid (33 mg, 0.2 mmol), (R)-(1-(5,6-diaminopyridin-2-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone dihydrochloride (77.5 mg, 0.2 mmol), O-(7-azabenzotriazol-1-yl)-N,N,N′,N′,-tetramethyluronium hexafluorophosphate (135 mg, 0.4 mmol), diisopropylethyl amine (155 μL, 0.9 mmol) and N,N-dimethylformamide (3.0 mL). The reaction mixture was stirred at room temperature for 3 h. The mixture was directly loaded to a column and purified via flash chromatography (0-6% methanol in dichloromethane) to afford N-(2-amino-6-(3-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-3-yl)piperidin-1-yl)pyridin-3-yl)-1-(3-oxomorpholino)cyclopropanecarboxamide (77.0 mg, 94.7%). MS (ES+) (M+H) 457.3; LCMS retention time 1.56 min (Method L).

1. custompurified via flash chromatography (0-6% methanol in dichloromethane)