反应详情

温度

100 °C

To 4-chloro-6-[(2R)-2-ethyl-1-pyrrolidinyl]-2-pyrimidinamine (40 mg, 0.176 mmol) and (4-cyano-3-fluorophenyl)boronic acid (29.1 mg, 0.176 mmol) was added 1,4-dioxane (3 mL) followed by sat. aq. NaHCO3 (0.5 mL), and the mixture was purged with N2 for 10 minutes into a sealable tube. Pd(Ph3P)4 (20.4 mg, 0.018 mmol) was added, the tube was sealed, and the reaction mixture was stirred overnight at 100° C. The mixture was poured onto water and EtOAc. The organic layer was separated, washed with brine, dried (MgSO4), filtered and concentrated. Flash chromatography on SiO2 (gradient: 100° ACHCl3 to 95:5:0.5 CHCl3:CH3OH:NH4OH) afforded the title compound (52 mg) as a solid. LC-MS (ES) m/z=312 [M+H]+.

1. customthe mixture was purged with N2 for 10 minutes into a sealable tube
2. customthe tube was sealed
3. customThe organic layer was separated
4. washwashed with brine
5. dry with materialdried (MgSO4)
6. filtrationfiltered
7. concentrationconcentrated