Sulfamide → 5-fluoro-3-(1-methylethyl)-3,4-dihydro-1H-2,1,3-benzothiadiazine-2,2-dioxide

Participants

Reaction Conditions

Reaction Steps

N-(1-methylethyl)-(2-amino-6-fluorophenyl)methylamine (0.3 g, 1.6 mmol) and sulphamide (5.08 g, 2.5 mmol) were suspended in 7 ml of dry pyridine and the mixture stirred at 115° C. for 24 hours in argon atmosphere. After cooling at room temperature the solvent was removed in vacuo and the residue dissolved in EtOAc (50 ml) and washed with 5N HCl (2×50 ml). Solvents removal afforded 5-fluoro-3-(1-methylethyl)-3,4-dihydro-1H-2,1,3-benzothiadiazine-2,2-dioxide as a pale yellow solid.

Provenance & Evidence