The synthetic route of 4-Fluorobenzenesulfonamide has been constantly updated, and we look forward to future research findings.
These common heterocyclic compound, 402-46-0, name is 4-Fluorobenzenesulfonamide, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Quality Control of 4-Fluorobenzenesulfonamide
Example 44; 4-{2-[4-(4-Sulfamoylphcnyl)pipcrazin-l-yl]cthyl}pipcridinc-l-carboxylic acid tert-butyl ester hydrochloride; EPO A mixture of 4-fluorobenzenesulfonamide (1.00 g, 5.71 mmol) and piperazine (2.46 g, 28.54 mmol) in water (12 mL) was heated at 1000C for 2Oh. The resulting precipitate was collected filtration and washed with water and toluene to give 4-piperazin-l- ylbenzenesulfonamide: RT = 0.49 min; m/z (ES+) = 242.13 [M+H]+. A solution of 4-piperazin- 1-ylbenzenesulfonamide (0.46 g, 1.89 mmol) and 4-(2-oxoethyl)piperidine-l-carboxylic acid tert-butyl ester (0.43 g, 1.89 mmol) in DCM (50 mL) and THF (7 mL) with molecular sieves (0.90 g) was stirred under argon at rt for Ih. Sodium acetoxyborohydride (0.52 g, 2.46 mmol) was added and the reaction mixture was stirred for a further 2.5h. The reaction mixture was quenched with saturated NaHCO3 solution and extracted with EtOAc. The organic extracts were washed with brine, dried (MgSO4) and the solvent was removed under vacuum. The resulting solid was purified by recrystallisation (EtOAc) then dissolved in THF and 1 M HCl in dioxane (0.95 equivalents), the solvent was removed under vacuum and the resulting solid was washed with Et2O to afford the title compound: RT = 2.51 min; m/z (ES+) = 453.33 [M+H]+.
The synthetic route of 4-Fluorobenzenesulfonamide has been constantly updated, and we look forward to future research findings.
Reference:
Patent; PROSIDION LIMITED; WO2007/3964; (2007); A1;,
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