反应详情

A mixture of 6-chloro-N-(pyridin-3-ylmethyl)pyrazin-2-amine (49 mg, 0.22 mmol), 2-methoxy-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol (52 mg, 0.20 mmol), (PPh3)4Pd (23 mg, 0.020 mmol) and a Na2CO3 solution (0.22 mmol of a 2 M solution) in toluene (10 ml) was heated under reflux overnight. After removal of the solvents, the residue was dissolved in CH2Cl2 (150 ml), dried (Na2SO4), filtered and the CH2Cl2 removed in vacuo. The residue was purified by column chromatography, eluting with a n-hexane:ethyl acetate gradient mixture to obtain the desired product (62 mg, 75%).

1. temperatureunder reflux overnight
2. customAfter removal of the solvents
3. dissolutionthe residue was dissolved in CH2Cl2 (150 ml)
4. dry with materialdried (Na2SO4)
5. filtrationfiltered
6. customthe CH2Cl2 removed in vacuo
7. customThe residue was purified by column chromatography
8. washeluting with a n-hexane