反应详情

温度

90 °C

2-Chloro-4-[(3S)-3-methylmorpholin-4-yl]-6-(methylsulfonylmethyl)pyrimidine (700 mg, 2.29 mmol) was dissolved in a solution of 18% DMF in a mixture of 7:3:2 DME:water:ethanol (7 mL). (4-Amino-3-methoxy-phenyl)boronic acid (574 mg, 3.43 mmol), 2M sodium carbonate solution (4 mL) and dichlorobis(triphenylphosphine) palladium (81 mg) was then added to the solution and refluxed at 90° C. for 1 hour. The reaction was allowed to cool to room temp then partitioned between ethyl acetate (50 mL) and water (50 mL), the organics dried over magnesium sulphate, filtered and concentrated in vacuo. The residue was dissolved in dichloromethane and filtered to remove insoluble material. The filtrates were purified using a companion.

1. temperatureto cool to room temp
2. customthen partitioned between ethyl acetate (50 mL) and water (50 mL)
3. dry with materialthe organics dried over magnesium sulphate
4. filtrationfiltered
5. concentrationconcentrated in vacuo
6. dissolutionThe residue was dissolved in dichloromethane
7. filtrationfiltered
8. customto remove insoluble material
9. customThe filtrates were purified