Piperidine → HCID 59299346, compound

Participants

Reaction Conditions

Reaction Steps

Dissolve 3-(4-bromo-2-chloro-benzyl)-1-cyclohexyl-piperidin-2-one (Example 55) (0.20 g, 0.54 mmol), piperidine (0.21 mL, 2.16 mmol), palladium (II) acetate (12 mg, 0.05 mmol) and rac-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (67 mg, 0.11 mmol) in toluene (1 mL) with cesium carbonate (264 mg, 0.81 mmol) and heat at 90° C. 16 h. Pass the mixture through an SCX ion exchange column washing with methanol and eluting with 1N ammonia in methanol and evaporate. Purify the residue by preparative reversed phase HPLC chromatography to give the title compound (98 mg, 48%). MS (ES+) nz/z=376 (M+H)+.

Provenance & Evidence