4-Phenylpiperidine → N-(1-Benzyloxy-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-(R)-yl)-4-(4-phenyl-piperidin-1-yl)-benzenesulfonamide

Participants

Reaction Conditions

Reaction Steps

To a solution of 100 mg of N-(1-benzyloxy-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-(R)-yl)-4-fluoro-benzenesulfonamide from Step A in 2 mL of methylsulfoxide was added 100 mg of 4-phenyl piperidine. The solution was heated to 70° C. for 5 days. The reaction was cooled, and the mixture extracted with ethyl acetate. The organic layers were washed twice with NaCl(aq.) solution, followed by drying over Na2SO4(s). Filtration, solvent removal, was followed by dilution with ethyl ether. Filtration of the resulting solids, washing with ethyl ether and methanol, and drying gave 83 mg of an off-white solid. MS: 1063 (2M+H), 532 (M+H).

Provenance & Evidence