反应详情

温度

105 °C

A mixture of {1-[4-(7-bromo-3-phenyl-imidazo[1,2-a]pyridin-2-yl)-phenyl]-cyclobutyl}-carbamic acid tert-butyl ester (150 mg), [1-(tert-butoxycarbonyl)-1H-pyrazol-4-yl]boronic acid (123 mg), 1,1′-bis(diphenylphosphino)ferrocene-dichloropalladium(II) (24 mg) and sodium carbonate (92 mg) in dioxane (3.1 mL) and water (0.4 mL) was degassed, placed under an argon atmosphere and heated at 105° C. under microwave irradiation for 30 minutes. On cooling, a further portion of catalyst was added (24 mg) and the mixture heated for a further 30 minutes under microwave irradiation. On cooling, the reaction was partitioned between aqueous ammonium chloride solution and DCM and the organic phase washed with brine, dried and concentrated in vacuo to give the crude title compound (183 mg) which was used in the next step (deprotection of both Boc groups under the standard conditions given in Example 1.0) without further purification.

1. customwas degassed
2. temperatureOn cooling
3. additiona further portion of catalyst was added (24 mg)
4. temperaturethe mixture heated for a further 30 minutes under microwave irradiation
5. temperatureOn cooling
6. customthe reaction was partitioned between aqueous ammonium chloride solution and DCM
7. washthe organic phase washed with brine
8. customdried
9. concentrationconcentrated in vacuo