3-Bromopyridine → tert-butyl (3R)-3-methyl-4-pyridin-3-ylpiperazine-1-carboxylate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (0.145 g, 0.16 mmol) and 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (0.183 g, 0.32 mmol) were added to a mixture of Sodium tert-butoxide (0.912 g, 9.49 mmol), 3-bromopyridine (0.610 mL, 6.33 mmol),(R)-tert-butyl 3-methylpiperazine-1-carboxylate (1.901 g, 9.49 mmol) and toluene (20 mL) under nitrogen. The mixture was heated at 85 °C for 16 hours before being cooled to RT and filtered through celite. The filtrate was concentrated and the reaction mixture was seperated by flash silica chromatography, elution gradient 20 to 40% EtOAc in heptane. No product was isolated. .

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