反应详情

温度

150 °C

6-(2-chloropyridin-3-yl)-N-methylpyrimidin-4-amine (897 mg, 4.1 mmol), 5-amino-6-methylisoquinolin-1(2H)-one (779 mg, 4.5 mmol), 2-dicyclohexylphosphino-2′-(N,N-dimethylamino)biphenyl (128 mg, 0.33 mmol) and tris(dibenzylideneacetone)dipalladium (0) (149 mg, 0.16 mmol) were added to a microwave tube. The tube was capped and flushed with nitrogen, and then lithium bis(trimethylsilyl)amide (16.9 mL, 1.0 M solution in THF) was added. The mixture was heated in a microwave reactor at 150° C. for 15 min. The reaction mixture was quenched with saturated aqueous sodium bicarbonate then extracted with DCM. The DCM extracts were conccentrated and purified by flash chromatography (0-10% 2 M ammonia in methanol) to give the title compound (380 mg, 26%). MS (M+H)+ 359.

1. customThe tube was capped
2. customflushed with nitrogen
3. additionlithium bis(trimethylsilyl)amide (16.9 mL, 1.0 M solution in THF) was added
4. customThe reaction mixture was quenched with saturated aqueous sodium bicarbonate
5. extractionthen extracted with DCM
6. custompurified by flash chromatography (0-10% 2 M ammonia in methanol)