Water → tert-butyl N-[(3S)-1-[3-methyl-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]pyrazin-2-yl]-3-piperidyl]carbamate

Participants

Reaction Conditions

Reaction Steps

To a solution of tert-butyl N-[(3S)-1-[3-chloro-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]pyrazin-2-yl]-3-piperidyl]carbamate (50 mg, 0.096 mmol), trimethylboroxine (36 mg, 0.29 mmol) and [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II) dichloromethane adduct (8.0 mg, 0.0095 mmol) in acetonitrile 2.0 mL was added 1.00M sodium carbonate in water (0.19 mL, 0.19 mmol) and 1.00M potassium acetate in Water (0.19 mL, 0.19 mmol). The reaction mixture was heated in microwave at 140° C. for 40 min. The reaction was filtered through celite. The crude product was purified by flash chromatography (EtOAc/Heptane eluted at 80% EtOAc) to give the desired product 34 mg 70% yield. MS (ESI) m/z: 502.2.

Provenance & Evidence