反应详情

In a reaction vial, 3-[2,6-difluoro-3-(propane-1-sulfonylamino)-benzoyl]-1H-pyrrolo[2,3-b]pyridine-5-carboxylic acid (41, 13 mg, 0.031 mmol) is dissolved in 0.5 mL of N,N-dimethylformamide and O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (17 mg, 0.046 mmol) is added followed by triethylamine (21 μL, 0.15 mmol). The mixture is stirred for 15 minutes, then pyridin-3-ylamine (42, 29 mg, 0.31 mmol) is added and the reaction is stirred at room temperature overnight. The reaction is diluted with water and ethyl acetate. The aqueous phase is separated and extracted with ethyl acetate. The organic layers are combined and dried with sodium sulfate, filtered and the filtrate concentrated under vacuum. The resulting material is purified by reverse phase chromatography to provide the desired compound. MS (ESI) [M+H+]+=500.0.

1. stirringthe reaction is stirred at room temperature overnight
2. customThe aqueous phase is separated
3. extractionextracted with ethyl acetate
4. dry with materialdried with sodium sulfate
5. filtrationfiltered
6. concentrationthe filtrate concentrated under vacuum
7. customThe resulting material is purified by reverse phase chromatography