反应详情

Add 1-hydroxybenzotriazole hydrate (63.8 mg; 417 μmol), 1-trityl-1H-imidazole-4-carboxylic acid (148 mg, 417 μmol) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (79.9 mg, 417 μmol) to anhydrous acetonitrile (7 mL). Stir the reaction mixture at room temperature for 1 hr. Then add 1-[4-(4-aminomethyl-benzyloxy)-2-hydroxy-3-trifluoromethyl-phenyl]-3,3-dimethyl-butan-1-one hydrochloride (150 mg, 347 μmol) and triethylamine (97 μL, 695 μmol). Stir the reaction mixture at room temperature overnight. Quench the reaction with water and the solid, filter the solid and dry to give the title compound (220 mg, 301 μmol). MS (m/z): 730 (M−1).

1. stirringStir the reaction mixture at room temperature overnight
2. customQuench
3. customthe reaction with water
4. filtrationthe solid, filter the solid
5. customdry