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Microwave-assisted synthesis of 4-quinolylhydrazines followed by nickel boride reduction: a convenient approach to 4-aminoquinolines and derivatives
Authors:Sandra Gemma  Gagan Kukreja  Pierangela Tripaldi  Maria Altarelli  Matteo Bernetti  Silvia Franceschini  Luisa Savini  Giuseppe Campiani  Caterina Fattorusso
Affiliation:a European Research Centre for Drug Discovery and Development, Università di Siena, via Aldo Moro, 53100 Siena, Italy
b Dipartimento Farmaco Chimico Tecnologico, Università di Siena, via Aldo Moro, 53100 Siena, Italy
Abstract:Nickel(II) chloride/sodium borohydride combination was employed for the reduction of 4-hydrazinoquinoline derivatives to the corresponding anilines. This reductive protocol was efficiently applied for the reductive cleavage of monosubstituted hydrazines. We described herein the microwave-assisted synthesis of 4-hydrazinoquinolines, which furnished a high yielding and rapid two-step procedure for the synthesis, under mild conditions, of 4-aminoquinolines as antimalarial precursors.
Keywords:Nickel boride   Reduction   Hydrazines   Microwave   4-Aminoquinolines
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