反应详情

To a suspension of Boc-Leu-OH.H2O (0.997 g) and DTrp-OMe.HCl (1.021 g) in dichloromethane (10 ml) were added TEA (0.6 ml) and HOBT.H2O (0.615 g) under argon. EDCI.HCl (0.769 g) was added to the mixture at 0°-5° C. The resulting reaction mixture was stirred at room temperature for 16 h, washed successively with water, 10% aq. citric acid, sat. NaHCO3 and brine, dried over MgSO4, filtered, and concentrated under reduced pressure. The residue was triturated with hexane to give the product (1.665 g). FAB-MS(m/e,(C23H33N3O5 +H)+):432

1. customThe resulting reaction mixture
2. washwashed successively with water, 10% aq. citric acid, sat. NaHCO3 and brine
3. dry with materialdried over MgSO4
4. filtrationfiltered
5. concentrationconcentrated under reduced pressure
6. customThe residue was triturated with hexane