Efficient Synthesis and Iodine-Functionalization of Pyrazoles via KIO/PhSeSePh System under Acidic Conditions.
作者信息
Peglow Thiago J, Thomaz João Pedro S S C, Nobre Patrick C, Scimmi Cecilia, Santi Claudio, Nascimento Vanessa
机构信息
SupraSelen Laboratory, Department of Chemistry, Federal University Fluminense, Institute of Chemistry, Campus do Valonguinho, 24020-141, Niterói-RJ, Brazil.
Group of Catalysis, Synthesis and OrganicGreen Chemistry, Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123, Perugia, Italy.
出版信息
Chem Asian J. 2024 Dec 2;19(23):e202400749. doi: 10.1002/asia.202400749. Epub 2024 Oct 22.
This manuscript reports a novel method for the direct iodination of the C-4 pyrazole ring generated in situ by the reaction of 1,1,3,3-tetramethoxypropane and various hydrazines. In this approach, potassium iodate (KIO) is used as the iodinating agent and (PhSe) is used as catalysts under acidic conditions. This protocol provides a convenient method for the efficient synthesis of 4-iodo-1-aryl-1H-pyrazoles, valuable intermediates for several different coupling reactions.
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