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 Synthesis of Fluconazole
  • Synthesis of Fluconazole
  • (CAS NO.: ), with its systematic name of 1H--1-ethanol, alpha-(2,4-difluorophenyl)-alpha-(1H-1,2,4-triazol-1-ylmethyl)-, could be produced through many synthetic methods.

    Following is one of the synthesis routes: The Friedel-Crafts condensation of 1,3-di (I) with chloroacetyl chloride (II) by means of AlCl3 yields alpha-chloro-2,4-difluoroacetophenone (III), which is treated with 1,2,4- (IV) and triethylamine in refluxing ethyl acetate giving alpha-(1H-12,4-triazol-1-yl)-2,4-diftuoroacetophenone (V). The reaction of (V) with trimethylsulfoxonium iodide (VI) by means of NaOH in toluene affords 1-[2-(2,4-di fluorophenyl)-2,3-epoxypropyl]- (VII), which is finally treated again with 1,2,4-triazole (IV) and K2CO3 in hot DMF.

    Synthesis of Fluconazole


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