反应详情

3-Bromo-5-trimethylsilanylethynyl-pyridine (1.0 eq, 1.22 g, 4.78 mmol), pivaloyl chloride (1.1. eq, 0.647 ml, 5.26 mmol) and copper(I) chloride (0.2 eq, 95 mg, 0.96 mmol) are dissolved in DMF (8 ml). The resulting mixture is heated using microwave radiation at 120° C. for 30 min. The mixture is filtered and washed with EtOAc. The filtrate is concentrated in vacuo and partitioned between sat. aqueous NaHCO3 solution and EtOAc. The organic portion is separated, dried (MgSO4) and concentrated in vacuo to afford the title compound; [M+H]+=266/268.

1. temperatureThe resulting mixture is heated
2. customat 120° C.
3. customfor 30 min
4. filtrationThe mixture is filtered
5. washwashed with EtOAc
6. concentrationThe filtrate is concentrated in vacuo
7. custompartitioned between sat. aqueous NaHCO3 solution and EtOAc
8. customThe organic portion is separated
9. dry with materialdried (MgSO4)
10. concentrationconcentrated in vacuo