反应详情

Combine 1-amino-N-[(4R)-5,6-dihydro-4H-imidazo[1,2-a][1]benzazepin-4-yl]cyclopropanecarboxamide (160 mg, 0.57 mmol), 4-chlorobenzoic acid (106 mg, 0.68 mmol) and O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (HATU) (259.0 mg, 0.68 mmol;) in N,N-dimethylformamide (4 mL). Add diisopropylethylamine (DIEA) (0.25 mL, 1.42 mmol) and stir the reaction at ambient temperature for approximately 5 hours under nitrogen. Dilute the reaction with ethyl acetate, wash with sodium bicarbonate, water (2×), and brine, dry over sodium sulfate, and concentrate the organic layer under reduced pressure. Purify the residue by flash chromatography (40% EtOAc/hexanes to 100% EtOAc) to give the title compound (190.0 mg, 80%): MS (m/z): 421 (M+1).

1. customthe reaction at ambient temperature for approximately 5 hours under nitrogen
2. additionDilute
3. washwash with sodium bicarbonate, water (2×), and brine
4. dry with materialdry over sodium sulfate
5. concentrationconcentrate the organic layer under reduced pressure
6. customPurify the residue by flash chromatography (40% EtOAc/hexanes to 100% EtOAc)