Patent ID: 11939303
Assignee: POLITECHNIKA GDANSKA
Field: Pharmaceuticals (Chemistry)
Classification: CPC C  A  G | IPC A  C  G

Claim 3:
4. Method for the preparation of compound presented by the general formula 1:, wherein R1═H or F or CF3 or OCF3; R2═H or F or CF3 or Cl or Br or I or CH3 or OCH3 or Et or iPr or NO2; R3═H or F or CF3 or OCF3; R4═H or F or CF3 or Cl or Br or I or CH3 or OCH3; R5═H or F or CF3, while the method is carried out in several steps according to scheme 1:, while in the first step, 4-((trimethylsilyl)ethynyl)phenol (3) is obtained by the Sonogashira coupling reaction of p-iodophenol and trimethylsilylacetylene and this step is carried out under reflux, while in the second step, 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol derivatives are obtained as a result of the 1,3-dipolar cycloaddition reaction of the azide derivative with 4-ethynylphenol or with 4-((trimethylsilyl)ethynyl)phenol (3) in the presence of tetrabutylammonium fluoride (TBAF), and in the third step the final product is obtained by the reaction of sulfamoyl chloride generated in situ with the 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol derivative (4) and this step is carried out under anhydrous conditions.