tert-Butyl piperazine-1-carboxylate → Tert-butyl 4-[4-(2,2,2-trifluoroethoxy)phenyl]piperazine-1-carboxylate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

1-bromo-4-(2,2,2-trifluoroethoxy)benzene (14.5 g, 57 mmol) was dissolved in toluene (250 ml) under an argon atmosphere. tert-Butyl piperazine-1-carboxylate (12.7 g, 68 mmol), sodium tert-butoxide (7.6 g, 79.5 mmol) rac-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (200 mg, 0.32 mmol) and tris(dibenzylideneacetone)dipalladium(0) (200 mg, 0.2 mmol) were added and the reaction heated to 80° C. for 4 hours. The mixture was then cooled and filtered through Celite to yield crude tert-butyl 4-[4-(2,2,2-trifluoroethoxy)phenyl]piperazine-1-carboxylate (32.47 g).

Herkunft & Nachweise