4-Methoxybenzenesulfonyl chloride → N-{2-[3'-(4-Fluoro-phenyl)-2,3,5,6-tetrahydro-[1,2']bipyrazinyl-4-yl]-ethyl}-4-methoxy-N-methyl-benzenesulfonamide hydrochloride

Participants

Reaction Steps

Dissolve 4-methoxy-benzenesulfonyl chloride (0.110 g, 0.530 mmol, 1.1 eq.) in dichloromethane (4 mL). Add {2-[3′-(4-fluoro-phenyl)-2,3,5,6-tetrahydro-[1,2′]bipyrazinyl-4-yl]-ethyl}-methyl-amine (0.150 g, 0.480 mmol, 1 eq.). Add morpholine, polymer-bound (0.220 g, 0.530 mmol, 1.1 eq.). Stir at room temperature for 2 hr. Purify by SCX chromatography (column washed with methanol and extracted with 7N NH3/MeOH) to afford the free base of the title compound (0.187 g, 80% yield). MS (loop): m/z=486.0 [M+H].

Provenance & Evidence