反应详情

To a mixture of 4-[4-(5-bromo-3-methyl-pyridin-2-yl)-2-(R)-methyl-piperazin-1-yl]-6-(4-fluoro-phenyl)-2-(2-methyl-pyrrolidin-1-yl)pyrimidine (700 mg, 1.33 mmol) and Zn(CN)2 (94 mg, 0.799 mmol) in DMF, add Pd(PPh3)4 (77 mg, 0.067 mmol). Purge the reaction mixture for 10 min with dry N2. Heat the stirring reaction mixture overnight at 80° C., cool to room temperature and partition between water and EtOAc. Dry the solution (Na2SO4), concentrate under reduced pressure. Purify the residue by flash column eluting with EtOAc-Hexanes (1:1) to afford the title compound as a white solid.

1. customPurge the reaction mixture for 10 min with dry N2
2. temperatureHeat
3. customthe stirring reaction mixture overnight at 80° C.
4. custompartition between water and EtOAc
5. dry with materialDry the solution (Na2SO4)
6. concentrationconcentrate under reduced pressure
7. customPurify the residue by flash column
8. washeluting with EtOAc-Hexanes (1:1)