反应详情

4-Amino-6-methyl-1-(pyridine-2-sulfonyl)-azepan-3-ol HCl salt (0.21 g, 0.59 mmol) was dissolved in 5 ml DMF. To this solution, was added Boc-Leu-OH (0.22 g, 0.88 mmol) and HBTU (0.34 g, 0.90 mmol) and then NMM (0.24 g, 2.4 mmol). The mixture was stirred at RT overnight. DMF was removed under high vacuum. The residue was diluted in EtOAc and washed with H2O, 10% NaHCO3 and brine. Purification by column chromatography gave the title compound (0.2 g, 68% yield). MS (M+H+): 499.1; 1H-NMR (400 Hz, CDCl3): 8.75(d, 1H), 8.0-7.75(m, 2H), 7.5 5(m, 1H) 5.10(m, 1H), 4.15-2.90(m, 10H), 2.10-1.48(m, 14H), 1.00(m, 9H)

1. customDMF was removed under high vacuum
2. additionThe residue was diluted in EtOAc
3. washwashed with H2O, 10% NaHCO3 and brine
4. customPurification by column chromatography