反应详情

To a microwave tube was added N-(2-bromopyridin-4-yl)-2,6-dichlorobenzamide (0.25 g, 0.72 mmol), 2-chloro-6-isopropylpyrimidin-4-amine (0.16 g, 0.94 mmol), Pd2(dba)3 (0.020 g, 0.022 mmol), XantPhos (0.008 g, 0.014 mmol), Cs2CO3 (0.47 g, 1.4 mmol) dioxane (20 mL) and DME (5 mL). The mixture was degassed with N2 for 10 min. The resulting mixture was irradiated in a microwave reactor at 130° C. for 2 hours and then cooled to room temperature. The mixture was filtered through Celite and concentrated under reduced pressure. The residue was purified by column chromatography (EtOAc/Petrolum ether=20/80 to 30/70) to give 2,6-dichloro-N-(2-(2-chloro-6-isopropylpyrimidin-4-ylamino)pyridin-4-yl)benzamide (370 mg, yield: 90%). LCMS (ESI) m/z: 436.0 [M+H+].

1. customThe mixture was degassed with N2 for 10 min
2. customThe resulting mixture was irradiated in a microwave reactor at 130° C. for 2 hours
3. filtrationThe mixture was filtered through Celite
4. concentrationconcentrated under reduced pressure
5. customThe residue was purified by column chromatography (EtOAc/Petrolum ether=20/80 to 30/70)