4-Benzyl-4-piperidinol → 1-[2-(4-Benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2,6-dimethyl-pyridin-4-yl)-urea

Beteiligte Stoffe

Reaktionsschritte

A suspension of commercially available 4-benzyl-piperidin-4-ol (383 mg, 2.0 mmol). NaHCO3 (672 mg, 8.0 mmol) and 1-(2-chloro-ethyl)-3-(2,6-dimethyl-pyridin-4-yl)-urea (Example D1., 227.7 mg 1.0 mmol) in THF (4 mL) is stirred at 50° C. for 4 days. The mixture is quenched with Na2CO3 (10 mL) and extracted with CH2Cl2 (3×10 mL). The organic extracts are washed with sat. aq. Na2CO3 (10 mL), dried (Na2SO4), filtered and evaporated. The residue is purified by HPLC to provide the title compound.

Herkunft & Nachweise