反应详情

Dissolve 3′-(4-fluoro-phenyl)-3,4,5,6-tetrahydro-2H-[1,2′]bipyrazinyl (0.160 g, 0.619 mmol) in DCE (5 mL). Add racemic 1-(2-hydroxy-propyl)-1H-pyrazole-4-carbaldehyde (0.175 g, 1.14 mmol) followed by sodium triacetoxyborohydride (0.262 g, 1.24 mmol) and stir at room temperature for 72 hr. Purify via SCX chromatography, followed by silica gel chromatography, eluting with 100:0 to 0:100 hexanes:ethyl acetate then 10:90 methanol:ethyl acetate, to give the racemic mixture of the free bases of the title compounds (223 mg, 91%).

1. customPurify via SCX chromatography
2. washeluting with 100:0 to 0:100 hexanes
3. customethyl acetate then 10:90 methanol:ethyl acetate, to give