A mild and efficient method for the regioselective iodination of pyrazoles

…, I Dorronsoro, AI Hernández-Higueras, G Antequera

Index: Rodriguez-Franco, Maria Isabel; Dorronsoro, Isabel; Hernandez-Higueras, Ana I; Antequera, Gema Tetrahedron Letters, 2001 , vol. 42, # 5 p. 863 - 865

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Citation Number: 74

Abstract

The iodination of NH or N-benzylpyrazoles using elemental iodine in the presence of CAN as the in situ oxidant is a mild and efficient method to prepare 4-iodopyrazoles containing even electron-withdrawing substituents. The reaction is regioselective since the iodine atom preferred pyrazole instead of the benzyl group, and the 4-pyrazolic position instead of other possible positions in the heterocycle.