反应详情

Dissolve {2-[3′-(4-fluoro-phenyl)-2,3,5,6-tetrahydro-[1,2′]bipyrazinyl-4-yl]-ethyl}-methyl-carbamic acid tert-butyl ester (3.8 g, 9.16 mmol, 1 eq.) in dichloromethane (20 mL). Add trifluoroacetic acid (41.2 g, 27.8 mL, 366.4 mmol, 40 eq.). Stir at room temperature for 1.5 hr. Partition the reaction mixture between aqueous 5N NaOH (pH aqueous layer=14) and dichlormethane. Separate the layers. Extract the aqueous layer with dichloromethane (2×50 mL). Combine the organic layers, dry over anhydrous Na2SO4, filter and concentrate to afford the title preparation (3.04 g, 100% yield). MS (loop): m/z=316.3 [M+H].

1. customPartition the reaction mixture between aqueous 5N NaOH (pH aqueous layer=14) and dichlormethane
2. customSeparate the layers
3. extractionExtract the aqueous layer with dichloromethane (2×50 mL)
4. dry with materialCombine the organic layers, dry over anhydrous Na2SO4
5. filtrationfilter
6. concentrationconcentrate
7. customto afford the title
8. custompreparation (3.04 g, 100% yield)