反应详情

温度

100 °C

To a solution of 4-[(1R,2S)-2-amino-1-hydroxypropyl]-phenol (75.4 mg) in N,N-dimethylformamide (1 ml) were added diisopropylamine (72.9 μl) and methyl 4′-(2-bromoethoxy)-3-(isopropylthio)-4-biphenylcarboxylate (142 mg) in N,N-dimethylformamide (0.4 ml) at room temperature and stirred at 100° C. for 4 hours. The reaction mixture was diluted with ethyl acetate and washed with saturated sodium bicarbonate aqueous solution, water and brine, dried over magnesium sulfate and concentrated in vacuo. The residue was purified with silica gel column chromatography to give methyl 4′-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-amino]ethoxy]-3-(isopropylthio)-4-biphenylcarboxylate (113 mg).

1. washwashed with saturated sodium bicarbonate aqueous solution, water and brine
2. dry with materialdried over magnesium sulfate
3. concentrationconcentrated in vacuo
4. customThe residue was purified with silica gel column chromatography