反应详情

温度

60 °C

(R)-3-[N′-(5-Acetyl-2H-pyrazole-3-carbonyl)-N-(5′-chloro-2′-fluorobiphenyl-4-ylmethyl)hydrazino]-2-hydroxypropionic acid (95.5 mg, 0.2 mmol) was dissolved in acetone (886 μL, 12.1 mmol). Et3N (70 μL, 503 μmol) and (S)-2-t-butoxycarbonylamino-3-methyl-butyric acid chloromethyl ester (56.1 mg, 211 μmol) were added, and the resulting mixture was stirred at 60° C. for 6 hours. The solvent was removed in vacuo and the residue was purified using flashy chromatography (normal phase; MeOH:EtOAc=0:50). The pure fractions were collected, concentrated, then dissolved in MeCN (630 μL, 12.1 mmol). A solution of 4.0 M HCl in 1,4-dioxane (503 μL, 2.0 mmol) was added, and the resulting mixture was stirred at room temperature for 2 hours. The solvent was removed in vacuo to yield the title compound (90 mg).

1. customThe solvent was removed in vacuo
2. customthe residue was purified
3. customThe pure fractions were collected
4. concentrationconcentrated
5. stirringthe resulting mixture was stirred at room temperature for 2 hours
6. customThe solvent was removed in vacuo