反应详情

A mixture of 2-hydroxy-4'-(methylsulfonyl) isobutyrophenone (100 g), 3-fluorophenylacetic acid (83 g), 1-cyclohexyl-3-(2-morpholinoethyl)carbodiimide metho-p-toluenesulfonate (225 g) and DMAP (25 g) in CH2Cl2 (2 L) was mechanically stirred for 17 h at r.t. A solution of 1N HCl (1 L) was then added and the organic phase was separated, washed with a saturated solution of Na2 CO3 (0.4 L) and dried over MgSO4. After concentration, the residue was purified by silica gel chromatography, eluting with 30% EtOAc/hexane to give the title compound as a white solid (133 g).

1. customthe organic phase was separated
2. washwashed with a saturated solution of Na2 CO3 (0.4 L)
3. dry with materialdried over MgSO4
4. concentrationAfter concentration
5. customthe residue was purified by silica gel chromatography
6. washeluting with 30% EtOAc/hexane