反应详情

(2-{(E)-3-[1-(4-Bromo-benzenesulfonyl)-1H-pyrrol-3-yl]-allanoylamino}-phenyl)-carbamic acid tert-butyl ester (3.0 g) and 1-methyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (1.71 g) are dissolved in DME (93 mL), (Ph3P)3PdCl2 (580 mg) and 2M Na2CO3-solution (55 mL) are added and the resulting mixture is heated under reflux temperature under an inert gas atmosphere. The solution is filtered and evaporated. The residue is treated with water and dichloromethane. The organic phase is separated, dried and evaporated. The crude product is purified by silica gel flash chromatography. The title compound is obtained in 902 mg yield.

1. temperaturethe resulting mixture is heated
2. temperatureunder reflux temperature under an inert gas atmosphere
3. filtrationThe solution is filtered
4. customevaporated
5. additionThe residue is treated with water and dichloromethane
6. customThe organic phase is separated
7. customdried
8. customevaporated
9. customThe crude product is purified by silica gel flash chromatography