1-Boc-3-methylpyrazole-5-boronic acid → 5-{2-[4-(1-Tert-butoxycarbonylamino-cyclobutyl)-phenyl]-3-phenyl-imidazo[1,2-a]pyridin-6-yl}-3-methyl-pyrazole-1-carboxylic acid tert-butyl ester

Participants

Reaction Conditions

Reaction Steps

A mixture of {1-[4-(6-bromo-3-phenyl-imidazo[1,2-a]pyridin-2-yl)-phenyl]-cyclobutyl}-carbamic acid tert-butyl ester (50 mg) and 1-tert-butoxycarbonyl-3-methylpyrazole-5-boronic acid (44 mg) in dioxane (1 mL) and water (0.43 mL) was placed under argon and [1,1-bis-(diphenylphosphino)-ferrocene]-dichloropalladium-dichlormethane-complex (7.9 mg) added. The mixture was heated at 110° C. under microwave irradiation for 60 minutes. On cooling the mixture was partitioned between DCM and water and extracted. The organic portion was dried and concentrated in vacuo to give the crude title compound which was used in the next step without further purification.

Provenance & Evidence