[Cl:1][C:2]1[CH:3]=[C:4]([CH:12]=[CH:13][C:14]=1[Cl:15])[CH2:5][NH:6][C:7]([CH3:11])([CH3:10])[CH2:8][OH:9].O1[CH2:18][CH:17]1[CH2:19][N:20]1C(=O)C2C(=CC=CC=2)C1=O.S(=O)(=O)(O)O>O>[Cl:1][C:2]1[CH:3]=[C:4]([CH:12]=[CH:13][C:14]=1[Cl:15])[CH2:5][N:6]1[C:7]([CH3:11])([CH3:10])[CH2:8][O:9][CH:17]([CH2:19][NH2:20])[CH2:18]1A mixture of Intermediate 2 (0.260 g) and 2-(oxiran-2-ylmethyl)-1H-isoindole-1,3(2H)-dione (0.205 g) was heated at 80° C. under nitrogen for 3 h. The mixture was treated with concentrated sulphuric acid (0.3 ml) then stirred at 150° C. for 18 h. The mixture was treated with water (25 ml) then washed with ethyl acetate (2×25 ml). The dark aqueous phase was basified to ˜pH 11 using 5M aqueous sodium hydroxide then extracted with ethyl acetate (2×25 ml). The combined organic extracts were washed with water and brine, dried (Na2SO4) and concentrated under vacuum to give the title compound as a brown oil (0.225 g).
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