1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) → tert-butyl N-[(3S)-1-[6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-6-oxo-3-piperidyl]carbamate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

A mixture of 6-(6-methylpyrazin-2-yl)-1H-pyrazolo[4,3-c]pyridine (75 mg, 0.36 mmol), tert-butyl N-[(3S)-1-(6-bromo-2-pyridyl)-6-oxo-3-piperidyl]carbamate (158 mg, 0.426 mmol), tris(dibenzylideneacetone)dipalladium(0) (32 mg, 0.036 mmol), xantphos (42 mg, 0.071 mmol), and sodium tert-butoxide (70 mg, 0.71 mmol) in toluene 6.0 mL was stirred at 100° C. 18 h. The reaction was filtered through celite. The crude product was purified by flash chromatography (EtOAc/Heptane eluted at 100% EtOAc) to give tert-butyl N-[(3S)-1-[6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-6-oxo-3-piperidyl]carbamate (50 mg) in 28% yield.

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