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 concentrated 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. concentrationThe DCM extracts were concentrated
7. custompurified by flash chromatography (0-10% 2 M ammonia in methanol)