反应详情

[1-(4-biphenylyl)-2-(4-morpholinyl)ethyl]methylamine (150 mg, 0.52 mmol) was added to a solution of (6,7-dimethyl-2-oxo-1(2H)-quinolinyl)acetic acid (100 mg, 0.43 mmol), (benzotriazol-1-yloxy) tris(dimethylamino) phosphonium-hexafluorophosphate (BOP) (230 mg, 0.52 mmol) and diisopropylethylamine (280 mg, 2.15 mmol) in dimethylformamide (DMF) (5 mL). The reaction mixture was stirred at room temperature for 3 h, filtered and washed with DMF. The crude was purified by preparative HPLC (YMC CombiPrep ODS-A, 50×20 mm, 20 mL/min, A: acetonitrile B: water, A: 10 to 90% over 10 min, UV detection at 214 nm) to give the title compound (43 mg, 16%), MS (ES) m/e 510 [M+H]+.

1. filtrationfiltered
2. washwashed with DMF
3. customThe crude was purified by preparative HPLC (YMC CombiPrep ODS-A, 50×20 mm, 20 mL/min
4. waitA: acetonitrile B: water, A: 10 to 90% over 10 min