Using microwave radiation in the intramolecular cyclization and SNAr reaction of the synthetic pathway proposed for development of norfloxacin derivatives [Empleo de la radiación de microondas en las reacciones de ciclación intramolecular y SNA de la ruta sintetica propuesta para la obtencion de derivados de norfloxacina]
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abstract
A method is proposed to speed-up the development of intermediate molecules in the synthesis of norfloxacin analogues assisted by microwave.The correct adjustmentofparameters like potencyand temperature, allowed to achieve the 6,7-difluoro4- hydroxyquinoline as product of the intramolecular cyclization reaction from 3A-difluoroacrylate in solution with Eaton%27s reagent, reaching moderate yields and having shorter reaction time. In similar way, SNAr reaction over (-7 of f1uoroquinolone ring presented good yields in a range of 20 to 60 minutes of reaction using the complex quinolone-boron or quinolone acid, using different heterocyclic amines. An alternative synthetic pathway with mild conditions of reaction could be used to prepare a wide range of norfloxacin analogues.
A method is proposed to speed-up the development of intermediate molecules in the synthesis of norfloxacin analogues assisted by microwave.The correct adjustmentofparameters like potencyand temperature, allowed to achieve the 6,7-difluoro4- hydroxyquinoline as product of the intramolecular cyclization reaction from 3A-difluoroacrylate in solution with Eaton's reagent, reaching moderate yields and having shorter reaction time. In similar way, SNAr reaction over (-7 of f1uoroquinolone ring presented good yields in a range of 20 to 60 minutes of reaction using the complex quinolone-boron or quinolone acid, using different heterocyclic amines. An alternative synthetic pathway with mild conditions of reaction could be used to prepare a wide range of norfloxacin analogues.
