反应详情

A suspension of 1-(5-chloro-3-methylpyridin-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid ethyl ester (600 mg), cyclopropylboronic acid (369 mg), 1,1′-bis(di-tert-butylphosphino)ferrocene (51 mg), palladium acetate (24 mg) and tripotassium phosphate (1.83 g) in 1,4-dioxane (5 ml) was stirred under reflux for 6 hours. After completion of the reaction, the mixture was allowed to cool, and chloroform was added, filtered through Celite, and then the filtrate was evaporated in vacuo. The obtained residue was purified with silica gel chromatography (n-hexane/ethyl acetate) to give 1-(5-cyclopropyl-3-methylpyridin-2-yl)-5-methyl-1H-pyrazole-4-carboxylic acid ethyl ester (462 mg) as a yellow solid. MS (ESI) m/z: 286 (M+H)+.

1. temperatureunder reflux for 6 hours
2. customAfter completion of the reaction
3. temperatureto cool
4. filtrationfiltered through Celite
5. customthe filtrate was evaporated in vacuo
6. customThe obtained residue was purified with silica gel chromatography (n-hexane/ethyl acetate)