反应详情

温度

100 °C

5-bromo-3-(1,1-dioxidotetrahydro-3-thienyl)-1H-indole-7-carboxamide (0.035 g, 0.098 mmol) and 1-{[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-thienyl]methyl}hexahydro-1H-azepine (0.038 g, 0.130 mmol, 1.3 eq) was dissolved in a 6:1 solution of 1,4 dioxane/water in a 20 mL microwave reaction vessel. Potassium carbonate (0.068, 0.490 mmol, 5 eq) was added and the solution was degassed with Argon. PdCl2(dppf) (0.012 g, 0.017 mmol, 0.17 eq) was added and the reaction was heated in a microwave at 100° C. for 20 min. The solution was passed through a StratoSphere SPE PL-Thiol MP SPE column to remove palladium and purified on Gilson preparative HPLC using Acetonitrile/Water with 0.1% TFA. The desired fractions were concentrated, giving 0.0052 g (12%) of the title compound.

1. customthe solution was degassed with Argon
2. customto remove palladium
3. custompurified on Gilson preparative HPLC
4. concentrationThe desired fractions were concentrated