Piperidin-4-ol → HCID 66750857, compound

Participants

Reaction Steps

A solution of 2,2,2-trichloroethyl 4-(2-tert-butylphenyl)piperazine-1-carboxylate (Example 60, 0.40 g, 1.02 mmol), piperidin-4-ol (0.50 g, 4.94 mmol), and N-ethyl-N-(1-methylethyl)propan-2-amine (0.158 g, 1.22 mmol) in DMSO (5 mL) was stirred for 3 days at 110° C. The reaction mixture was poured into saturated NaHCO3 solution and extracted with ethyl acetate. The organic layer was washed with brine, dried over MgSO4, and the solvent was evaporated under reduced pressure to give a crude product. The product was purified by flash column chromatography (silica gel, n-hexane/ethyl acetate=50:50 to 0:100 then ethyl acetate/methanol=100/0 to 70/30) to provide 1-{[4-(2-tert-butylphenyl)piperazin-1-yl]carbonyl}piperidin-4-ol (0.121 g, 34%) as a yellow solid.

Provenance & Evidence