反应详情

3-(2-bromoethyl)-1-(2-fluorophenyl)-3,4-dihydro-1H-2,1,3-benzothiadiazine 2,2-dioxide (0.96 g, 0.25 mmol) was dissolved in an 8 M solution of methylamine in ethanol (4 ml) and was stirred in a capped vial at room temperature for two hours. The reaction mixture was evaporated and the residue purified by flash chromatography (SiO2, 0-5% 7 M NH3-methanol/dichloromethane). The purified free-base was dissolved in dichloromethane (3 mL) and treated with hydrogen chloride (1.0 mL of a 2 M solution in ethyl ether), resulting in a white precipitate that was evaporated and dried under vacuum to afford 2-[1-(2-fluorophenyl)-2,2-dioxido-1,4-dihydro-3H-2,1,3-benzothiadiazin-3-yl]-N-methylethanamine (0.071 g, 85%) as a white solid:

1. customThe reaction mixture was evaporated
2. customthe residue purified by flash chromatography (SiO2, 0-5% 7 M NH3-methanol/dichloromethane)
3. dissolutionThe purified free-base was dissolved in dichloromethane (3 mL)
4. additiontreated with hydrogen chloride (1.0 mL of a 2 M solution in ethyl ether),
5. customresulting in a white precipitate that
6. customwas evaporated
7. customdried under vacuum