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Synthesis of Novel 4-Fluoro-2H-pyrazol-3-ylamines
Authors:Giuseppe Cocconcelli  Chiara Ghiron  Simon Haydar  Iolanda Micco
Institution:1. Siena Biotech S.p.A. , Siena, Italy;2. Chemical Sciences and Neuroscience Discovery Research, Wyeth Research , Princeton, New Jersey, USA
Abstract:A new and efficient synthesis for the preparation of novel 4-fluoro-2H-pyrazol-3-ylamines is described. It involves the reaction of an acyl chloride with fluoroacetonitrile and sequential ring closure of the α-fluoro-β-ketonitrile with hydrazine. Utilizing this synthetic protocol, we have synthesized a variety of 4-fluoro-2H-pyrazol-3-ylamines with different steric and electronic demands.
Keywords:Aminopyrazole  fluoro  4-fluoro-2H-pyrazol-3-ylamines
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