反应详情

Dissolve {2-[3′-(4-fluoro-phenyl)-2,3,5,6-tetrahydro-[1,2′]bipyrazinyl-4-yl]-ethyl}-methyl-amine (0.111 g, 0.352 mmol) in dichloromethane (4 mL). Add resin-bound morpholine (0.155 g, 0.387 mmol) followed by 1,2-dimethylimidazole-5-sulfonyl chloride (0.075 g, 0.387 mmol) and shake at ambient temperature for 72 hr. Filter, concentrate and purify (SCX chromatography, followed by silica gel chromatography, eluting with 100:0 to 0:100 hexanes:ethyl acetate, then 10:90 methanol:ethyl acetate, then 20:80 methanol:ethyl acetate) to give the free base of the title compound (118 mg, 71%).

1. filtrationFilter
2. concentrationconcentrate
3. custompurify (SCX chromatography
4. washeluting with 100:0 to 0:100 hexanes