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Detalle de: O-Pyrazolylpropynyl-Hydroxylamines as Versatile Intermediates in the Synthesis of Compounds of Pharmacological Interest

Title O-Pyrazolylpropynyl-Hydroxylamines as Versatile Intermediates in the Synthesis of Compounds of Pharmacological Interest
Abstract

Through an optimised Pd/Cu-catalysed cross-coupling reaction of 4-iodopyrazoles with 2-propyn-1-ol, followed by Mitsunobu transformation with N-hydroxyphthalimide and subsequent hydrazinolysis, O-[(pyrazol-4-yl)-prop-2-ynyl]-hydroxylamines were obtained in good yields. Their usefulness as intermediates in the synthesis of pharmaceuticals is exemplified by the first reported intramolecular cyclization of O-(2-propynyl)-hydroxylamines to yield 4,5-dihydro-isoxazoles.

Apa Reference Rodríguez-Franco, M. I., Dorronsoro, I., & Martínez, A. (2001). O-Pyrazolylpropynyl-Hydroxylamines as Versatile Intermediates in the Synthesis of Compounds of Pharmacological Interest. Synthesis, 2001(11), 1711–1715. 10.1055/s-2001-16768
Doi 10.1055/S-2001-16768
Publication Date 2001
Publication Type Article
Researcher Ana Martínez
Ontology
Research Groups Translational Medicinal and Biological Chemistry
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