Cesium carbonate → 1-[3-(Bromomethyl)benzyl]-3-(2-fluorophenyl)-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide

Participants

Reaction Steps

In an analogous manner to general procedure IV, 1-(2-fluorophenyl)-1,3-dihydro-2,1,3-benzothiadiazole2,2-dioxide (0.20 g, 0.75 mmol) was treated with cesium carbonate (0.24 g, 0.75 mmol) and 1,3-bis(bromomethyl)benzene) (0.80 g, 3.00 mmol) to provide 0.23 g (70%) of 1-[3-(bromomethyl)benzyl]-3-(2-fluorophenyl)-1,3-dihydro-2,1,3-benzothiadiazole2,2-dioxide. MS (ES) m/z 446.7; HPLC purity 98.5% at 210-370 nm, 10.8 min.; Xterra RP18, 3.5 u, 150×4.6 mm column, 1.2 mL/min, 85/15-5/95 (Ammon. Form. Buff. Ph=3.5/ACN+MeOH) for 10 min, hold 4 min

Provenance & Evidence