反应详情

To a suspension of (R)-2-Amino-6-tert-butoxycarbonylamino-hexanoic acid methyl ester (3.000 g, 10.108 mmol), 3,5-dimethyl-4-fluorophenylboronic acid (3.398 g, 20.216 mmol), Cu(OAc)2 (2.019 g, 11.119 mmol), and molecular sieves 4 Å (7.591 g) in 45 mL of dichloromethane, triethylamine (2.8 mL, 20.216 mmol) was added. After stirring at room temperature under O2 for 87 h, the reaction mixture was filtered through a pad of Celite and washed with dichloromethane. The filtrate was concentrated under reduced pressure. The product was isolated by Flash chromatography (silica gel) eluting with 0-30% ethyl acetate/hexanes to give the title compound as colorless oil (3.084 g, 80% yield). LC-MS: tR=9.8 min; m/z 383 (M+H)+.

1. filtrationthe reaction mixture was filtered through a pad of Celite
2. washwashed with dichloromethane
3. concentrationThe filtrate was concentrated under reduced pressure
4. customThe product was isolated by Flash chromatography (silica gel)
5. washeluting with 0-30% ethyl acetate/hexanes