反应详情

A mixture of 4-[5-(2-methyl-4-methylsulfanyl-phenyl)-2,3-dihydro-benzofuran-2-yl]-piperidine-1-carboxylic acid isopropyl ester (20 mg), aqueous hydrogen peroxide solution (35%; 3.5 μL) and 1,1,1,3,3,3-hexafluoro-2-propanol (200 μL) is stirred at room temperature for 2 h. The reaction mixture is diluted with dichloromethane and extracted with sodium thiosulfate solution (10%; 2 mL). The organic phase is washed with brine, dried over MgSO4 and the solvent is evaporated. The residue is chromatographed on silica gel (dichloromethane/methanol 95:5) to give the title compound. Yield: 9 mg (43% of theory); LC (method 2): tR=1.45 min; Mass spectrum (ESI+): m/z=442 [M+H]+.

1. extractionextracted with sodium thiosulfate solution (10%; 2 mL)
2. washThe organic phase is washed with brine
3. dry with materialdried over MgSO4
4. customthe solvent is evaporated
5. customThe residue is chromatographed on silica gel (dichloromethane/methanol 95:5)