反应详情

To a solution of 1-(5-bromo-pyridin-3-yl)-4,4-dimethyl-pent-1-yn-3-one (1 eq, 770 mg, 2.89 mmol) in THF (12 ml) is added pyridine-2-carboxamidine (1.5 eq, 684 mg, 4.34 mmol) and Na2CO3 (2.4 eq, 736 mg, 6.94 mmol). The resulting mixture is heated using microwave radiation for 1 h at 150° C. The solvent is removed in vacuo and the residue is partitioned between sat. aqueous NaHCO3 solution and DCM. The organic portion is dried (MgSO4) and concentrated in vacuo. The resulting residue is purified using column chromatography (DCM/MeOH) to give the title compound; [M+H]+=369/371.

1. temperatureThe resulting mixture is heated
2. customfor 1 h
3. customat 150° C
4. customThe solvent is removed in vacuo
5. customthe residue is partitioned between sat. aqueous NaHCO3 solution and DCM
6. dry with materialThe organic portion is dried (MgSO4)
7. concentrationconcentrated in vacuo
8. customThe resulting residue is purified