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Title: Thymidine- and AZT-linked 5-(1,3-dioxoalkyl)tetrazoles and 4-(1,3-dioxoalkyl)-1,2,3-triazoles
Author: Bosch Hereu, Lluís
Delelis, Olivier
Subra, Frédéric
Deprez, Eric
Witvrow, Myriam
Vilarrasa i Llorens, Jaume
Keywords: VIH (Virus)
Inhibidors de la integrasa
Integrase inhibitors
HIV (Viruses)
Issue Date: 1-Mar-2012
Publisher: Elsevier Ltd
Abstract: N3 of thymidine and of 3′-azido-3′-deoxythymidine (AZT) has been linked to a tetrazole ring by condensation of nucleoside-derived 2-oxonitriles with the lithium salt of 5-acetyl-1-(4-fluorobenzyl)tetrazole (obtained by a 'click' reaction). 4-Acetyl-1,2,3-triazole, also prepared by a Cu-catalysed cycloaddition, has been similarly linked. A route for the conjugation of NRTIs with pharmacophoric elements of integrase inhibitors (INIs) has thus been disclosed.
Note: Versió postprint del document publicat a:
It is part of: Tetrahedron Letters, 2012, vol. 53, num. 3, p. 514-518
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ISSN: 0040-4039
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)

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