反应详情

A 10 mL three-necked flask equipped with reflux condenser was charged with [1S -(1α, 2α, 3α)]-methyl 1-(1,3-benzodioxol-5-yl)-2,3-dihydro-3-[2-(2-hydroxyethoxy)-4-methoxyphenyl]-5-propoxy-1H-indene-2-carboxylate (34 mg, 0.071 mmol), THF (1 mL), MeOH (0.5 mL) and LiOH—H2O (15 mg, 0.355 mmol). The solution was heated to reflux for 12 h, cooled to room temperature and acidified with citric acid monohydrate (40 mg, 0.19 mmol) to pH 3.0. Upon complete hydrolysis, EtOAc (20 mL) and H2O (20 mL) was added, the organic phase washed with brine (15 mL), dried (MgSO4) and concentrated in vacuo affording (+) (1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid as a white solid (30 mg, 81%).

1. customA 10 mL three-necked flask equipped
2. temperaturewith reflux condenser
3. temperatureThe solution was heated
4. temperatureto reflux for 12 h
5. additionwas added
6. washthe organic phase washed with brine (15 mL)
7. dry with materialdried (MgSO4)
8. concentrationconcentrated in vacuo