Tetrahydrofuran → {4-[1-(2,6-Dichloro-benzoyl)-piperidin-4-yloxy]-phenyl}-carbamic acid tert-butyl ester

Participants

Reaction Conditions

Reaction Steps

To an ice-cooled solution of (4-hydroxy-phenyl)-carbamic acid tert-butyl ester (422.8 mg, 2.02 mmol), (2,6-dichlorobenzoyl)-(4-hydroxy-piperidin-1-yl)-methanone (552.8 mg, 2.01 mmol), and triphenylphosphine (1.09 g, 4.16 mmol) in THF (20 mL) is added diethyl azodicarboxylate (1.0 mL, 2.20 mmol). The reaction mixture is stirred at 22° C. for 17 hours. After removal of solvent, the residue is purified on a silica gel chromatography with ethyl acetate-hexanes to provide a white solid (606.2 mg, 64.8% yield, ES+(m/z) 465.1 [M+H]).

Provenance & Evidence