反应详情

温度

80 °C

1-(tert-Butoxycarbonyl)indole-2-boronic acid (900 mg, 3.5 mmol), 3,5-dibromo-pyridine (810 mg, 3.5 mmol), KOAc (1.01 g, 10.4 mmol) and Pd(dppf)Cl2 (252 mg, 0.35 mmol) are mixed in 1,4-dioxane (70 mL) and heated to 80° C. for 2 hours. The mixture is filtered and the filtrate is concentrated. The residue is dissolved in DCM and washed with water. The organic layer is separated, dried over Na2SO4, filtered and concentrated to afford the crude product which is purified by column chromatography to give 320 mg of 2-(5-bromo-pyridin-3-yl)-indole-1-carboxylic acid tert-butyl ester.

1. filtrationThe mixture is filtered
2. concentrationthe filtrate is concentrated
3. dissolutionThe residue is dissolved in DCM
4. washwashed with water
5. customThe organic layer is separated
6. dry with materialdried over Na2SO4
7. filtrationfiltered
8. concentrationconcentrated
9. customto afford the crude product which
10. customis purified by column chromatography