反应详情

Methylsulfonyl bromide (0.96 mL) is added to a solution of {(S)-6-[(R)-4-hydroxymethyl-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester (2.00 g) and triethylamine (1.98 mL) in dichloromethane (20 mL) chilled in an ice bath. The cooling bath is removed, and the solution is stirred at room temperature overnight. More dichloromethane is added, and the resulting solution is washed with aqueous NaHCO3 solution and brine, dried (Na2SO4), and concentrated. The residue is chromatographed on silica gel (cyclohexane/ethyl acetate) to give the title compound. LC (method 2): tR=1.24 min.

1. temperaturechilled in an ice bath
2. customThe cooling bath is removed
3. additionMore dichloromethane is added
4. washthe resulting solution is washed with aqueous NaHCO3 solution and brine
5. dry with materialdried (Na2SO4)
6. concentrationconcentrated
7. customThe residue is chromatographed on silica gel (cyclohexane/ethyl acetate)