反应详情

To a stirred solution of 1,2,3,4-tetrahydro-isoquinoline-7-carboxylic acid methylamide (96 mg, 0.5 mmol) in acetonitrile (3.0 ml) is added 2-chloro-(4-cyclobutyl-piperazine)-acetamide (109 mg, 0.5 mmol, 1.0 eq.), K2CO3 (138 mg, 1.0 mmol, 2.0 eq.), and NaI (10 mg). The resulting mixture is stirred at rt overnight. Water (10.0 ml) is added to quench the reaction, and the acetonitrile is evaporated. The residue is extracted with DCM (10 ml×3), and the combined organic phase is dried over sodium sulfate and concentrated. The residue is purified by PTLC (EtOAc/4% TEA plus 4% EtOH) to give the title compound. MS (+VE) m/z 371.1 (M++1).

1. customto quench
2. customthe reaction
3. customthe acetonitrile is evaporated
4. extractionThe residue is extracted with DCM (10 ml×3)
5. dry with materialthe combined organic phase is dried over sodium sulfate
6. concentrationconcentrated
7. customThe residue is purified by PTLC (EtOAc/4% TEA plus 4% EtOH)