2-(Di-tert-butylphosphino)biphenyl → 2-{4-[4-(4-Ethoxy-phenyl)-piperidin-1-yl]-phenyl}-N-ethyl-propionamide

Participants

Reaction Conditions

Reaction Steps

41 mg (0.20 mmol) 4-(4-Ethoxy-phenyl)-piperidine (XV.1) are added to a mixture of 51 mg (0.20 mmol) 2-(4-bromo-phenyl)-N-ethyl-propionamide (IV.3), 77 mg (0.80 mmol) sodium tert-butyrat, 24 mg (0.08 mmol) 2-(di-tert-butylphosphino)biphenyl and 18 mg (0.02 mmol) tris-(dibenzylidenaceton)-dipalladium(0) in 1 mL 1,4-dioxane. The mixture is stirred for 12 h at 45° C. After that time, the solvent is removed in vacuo and the residue is purified by HPLC (column: Waters XBridge 50; eluent A: water+0.1% NH4OH, eluent B: MeOH) to yield the desired product.

Provenance & Evidence