反应详情

温度

90 °C

Under nitrogen atmosphere, to a mixture of ethyl (αS)-α-[[(1,1-dimethylethoxy)carbonyl]amino]-4-(trifluoromethanesulfonyloxy)benzenepropionate (66.2 g), 4-ethoxymethyl-2,6-dimethoxyphenylboric acid (54.0 g), triphenylphosphine (9.83 g) and N-methylpyrrolidone (330 ml) were added palladium acetate (1.68 g) and diisopropylamine (24.9 g), and the mixture was heated at 90° C. After stirring for 1 hour at the same temperature, the mixture was cooled and toluene and water were added. The organic layers were washed with 10% aqueous citric acid solution and saturated aqueous NaCl solution and dried over magnesium sulfate. The solvent was removed in vacuo to yield ethyl (αS)-α-[[(1,1-dimethylethoxy)carbonyl]amino]-4′-ethoxymethyl-2′,6′-dimethoxy(1,1′-biphenyl)-4-propionate (90.1 g) as oil.

1. temperaturethe mixture was cooled
2. washThe organic layers were washed with 10% aqueous citric acid solution and saturated aqueous NaCl solution
3. dry with materialdried over magnesium sulfate
4. customThe solvent was removed in vacuo