反应详情

Heat a mixture of 4-[4-(5-bromo-3-methyl-pyridin-2-yl)-2-(R)-methyl-piperazin-1-yl]-2-chloro-6-(4-fluoro-phenyl)-pyrimidine (7.7 g, 16.2 mmol), (R)-2-methylpyrrolidine hydrobromide [prepared essentially as described by Nijhuis et. al. (1989) J. Org. Chem. 54(1):209] (3.5 g, 21.1 mmol) and K2CO3 (5.1 g, 37.3 mmol) in DMA at 110° C. for 16 h. Partition the mixture between EtOAc and water, dry (Na2SO4) the organic layer and concentrate under reduced pressure. Purify with flash silica gel column eluting with 10% EtOAc/hexanes. Concentrate under reduced pressure to give the title compound.

1. temperatureHeat
2. customprepared essentially
3. customPartition the mixture between EtOAc and water
4. dry with materialdry (Na2SO4) the organic layer
5. concentrationconcentrate under reduced pressure
6. customPurify with flash silica gel column
7. washeluting with 10% EtOAc/hexanes
8. concentrationConcentrate under reduced pressure