反应详情

To a round bottomed flask add 7-chloro-3-iodo-imidazo[1,2-a]pyridine (3.0 g, 0.011 mol), add 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline (2.6 g, 1.1 equiv.), potassium carbonate (4.5 g, 3 equiv.), dioxane (40 mL), and water (20 mL). Deoxygenate this mixture thoroughly with N2 then add dichlorobis(triphenylphosphine)palladium (II) (0.23 g, 0.03 equiv.) and reflux the reaction overnight under N2. Concentrate the reaction to dryness and slurry in DCM. Filter this slurry thru Celite® and wash with DCM. Concentrate the filtrate then purify by silica plug (EtOAc to 5% MeOH: DCM to 10% MeOH: DCM) to give a pale grey solid (2.6 g, 100%). MS (ES), m/z 244 (M+1).

1. customDeoxygenate this mixture thoroughly with N2
2. customthe reaction overnight under N2
3. concentrationConcentrate
4. customthe reaction to dryness and slurry in DCM
5. filtrationFilter this slurry thru Celite®
6. washwash with DCM
7. concentrationConcentrate the filtrate
8. customthen purify by silica plug (EtOAc to 5% MeOH: DCM to 10% MeOH: DCM)