反应详情

2-Chloro-4-(methylsulfonylmethyl)-6-morpholin-4-yl-pyrimidine (5 g, 17.1 mmol), was dissolved in a mixture of DMF:DME:water:ethanol (16.5 mL:41 mL:18 mL:12 mL). 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)aniline (5.62 g, 25.6 mmol), a 2M aqueous solution of sodium carbonate (25 mL), and dichlorobis(triphenylphosphine) palladium (600 mg) were added and the mixture refluxed for 5 hours under a nitrogen atmosphere. The mixture was cooled, diluted with water and extracted into DCM. The organic layer was dried over Na2SO4, filtered and evaporated. The crude material was dissolved in minimum of hot DCM then hexane added and the precipitate filtered to give the desired material (1.6 g).

1. temperaturethe mixture refluxed for 5 hours under a nitrogen atmosphere
2. temperatureThe mixture was cooled
3. extractionextracted into DCM
4. dry with materialThe organic layer was dried over Na2SO4
5. filtrationfiltered
6. customevaporated
7. dissolutionThe crude material was dissolved in minimum of hot DCM
8. additionhexane added
9. filtrationthe precipitate filtered