反应详情

To a stirred solution of 6-bromo-1,2,3,4-tetrahydro-isoquinoline hydrochloride (3.09 g, 12.4 mmol) in acetonitrile (50.0 ml) is added 2-chloro-(4-cyclobutyl-piperazine)-acetamide (2.69 mg, 12.4 mmol, 1.0 eq.), K2CO3 (5.14 g, 37.3 mmol, 3.0 eq.), and NaI (400 mg). The resulting mixture is stirred at rt overnight. Water (40.0 ml) is added to quench the reaction, and then the acetonitrile is evaporated. The residue is extracted with DCM (40 ml×3). The combined organic phase is dried over sodium sulfate, and the solvent is removed under reduced pressure to give a residue that is purified by flash silica gel chromatography (EtOAc/4% TEA) to give the title compound. MS (+VE) m/z 392.2 (M++1).

1. customto quench
2. customthe reaction
3. customthe acetonitrile is evaporated
4. extractionThe residue is extracted with DCM (40 ml×3)
5. dry with materialThe combined organic phase is dried over sodium sulfate
6. customthe solvent is removed under reduced pressure
7. customto give a residue that
8. customis purified by flash silica gel chromatography (EtOAc/4% TEA)