4-Aminopyridine → HCID 58063524, compound

Participants

Reaction Steps

3-[4-(3-Chlorophenyl)-1H-1,2,3-triazol-1-yl]-6-fluoro-1-(2,2,2-trifluoroethyl)-1,3,4,5-tetrahydro-2H-1-benzazepin-2-one (20 mg, 0.046 mmol), pyridin-4-amine 6.39 mg, 0.068 mmol), palladium(II) acetate (2.047 mg, 9.12 μmol), Xantphos (7.91 mg, 0.014 mmol), and cesium carbonate (44.6 mg, 0.137 mmol) were combined and dissolved in dioxane (912 μl). The reaction was irradiated in the microwave at 180° C. for 15 minutes. The completed reaction was filtered and concentrated in vacuo. Analytically pure material was obtained by purification by preparative HPLC Reverse phase (C-18), eluting with acetonitrile/water+0.05% formic acid. Lyophilisation afforded 6-fluoro-3-{4-[3-(pyridin-4-ylamino)phenyl]-1H-1,2,3-triazol-1-yl}-1-(2,2,2-trifluoroethyl)-1,3,4,5-tetrahydro-2H-1-benzazepin-2-one.

Provenance & Evidence