[NH:1]1[CH:5]=[CH:4][N:3]=[N:2]1.Br[CH2:7][CH2:8][N:9]1[C:13](=[O:14])[C:12]2=[CH:15][CH:16]=[CH:17][CH:18]=[C:11]2[C:10]1=[O:19].C(=O)([O-])[O-].[Cs+].[Cs+]>CN(C=O)C>[N:1]1([CH2:7][CH2:8][N:9]2[C:10](=[O:19])[C:11]3[C:12](=[CH:15][CH:16]=[CH:17][CH:18]=3)[C:13]2=[O:14])[CH:5]=[CH:4][N:3]=[N:2]1Add 1H-1,2,3-triazole (250 g, 3.51 mol), N-(2-bromoethyl) phthalimide (942 g, 3.52 mol) and 1500 mL of DMF to a 5-L round bottom flask fitted with a mechanical stirrer, a nitrogen inlet and temperature probe; cool the mixture to 15° C. Stir the mixture until all the solids are nearly dissolved and then cool in an ice-water bath. Add cesium carbonate (1145 g, 3.51 mol) in portions over 10 min. The reaction mixture exotherms to 21° C. Allow the mixture to stir and come to RT overnight. Pour the reaction mixture into a 12-L flask containing 8 L of ice-water. Stir the suspension for 30 min and then filter and rinse the solid with 3 L of water. Air-dry for 2 h. Recrystallize the mixture of regioisomers from 7 L of absolute ethanol. Isolate the solid by filtration and air-dry. Recrystallize again from 16 L of absolute ethanol. Again isolate the solid by filtration and rinse with fresh ethanol (1000 mL). Vacuum-dry the solid at 40° C. to give the title compound as a white solid, 292.7 g (34%). MS (EI) m/z 243 [M+1]+.
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