反应详情

Into a vial was added Intermediate 10 (60.0 mg, 0.361 mmol), (R)-(1-(5,6-diaminopyridin-2-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone dihydrochloride (Intermediate 1) (131 mg, 0.361 mmol), diisopropylethyl amine (314 μL, 1.80 mmol), O-(7-Azabenzotriazol-1-yl)-N,N,N′,N′,-tetramethyluronium hexafluorophosphate (HATU) (206 mg, 0.541 mmol), and N,N-dimethylformamide (3.0 mL). The reaction mixture was stirred at room temperature for 2 h. The mixture was purified via flash chromatography (0-6% methanol in dichloromethane) to afford (R)—N-(2-amino-6-(3-(pyrrolidine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)-1-(3-methyl-1H-pyrazol-1-yl)cyclopropanecarboxamide or (R)—N-(2-amino-6-(3-(pyrrolidine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)-1-(5-methyl-1H-pyrazol-1-yl)cyclopropanecarboxamide (62 mg).

1. customThe mixture was purified via flash chromatography (0-6% methanol in dichloromethane)