4.6 Article

A new vinyl selenone-based domino approach to spirocyclopropyl oxindoles endowed with anti-HIV RT activity

期刊

ORGANIC & BIOMOLECULAR CHEMISTRY
卷 14, 期 6, 页码 2015-2024

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ob02451j

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资金

  1. Fondazione Cassa di Risparmio Perugia Project Nuovi catalizzatori eterogenei per lo sviluppo di processi sintetici green in flusso [2014.0100.021]
  2. Fondo per il sostegno della ricerca di base Composti organici ed ibridi inorgano-organici del selenio nella sintesi ecocompatibile di molecole bioattive - University of Perugia
  3. Consorzio CINMPIS - Bari (Consorzio Interuniversitario Nazionale di Metodologie e Processi Innovativi di Sintesi)
  4. KU Leuven [GOA 15/019/TBA]

向作者/读者索取更多资源

Herein, we disclose a general and flexible access to spirocyclopropyl oxindoles by a domino Michael/intramolecular nucleophilic substitution pathway with variously substituted vinyl selenones and enolizable oxindoles in aqueous sodium hydroxide solution. The spirocyclopropyl oxindole being a privileged scaffold, some of the synthesized compounds were selected for biological evaluation. Compound 3m showed selective anti-HIV-1 activity thanks to its ability to inhibit the reverse transcriptase.

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