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Issue 38, 2015
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Diastereoselective synthesis of P-chirogenic phosphoramidate prodrugs of nucleoside analogues (ProTides) via copper catalysed reaction

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Abstract

The first copper-catalysed diastereoselective synthesis of P-chiral phosphoramidate prodrugs (ProTides) is reported. This procedure allows the synthesis of diastereomeric-enriched mixtures of ProTides. Application of this methodology to the asymmetric phosphorylation of purine and pyrimidine nucleoside analogues is presented.

Graphical abstract: Diastereoselective synthesis of P-chirogenic phosphoramidate prodrugs of nucleoside analogues (ProTides) via copper catalysed reaction

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Publication details

The article was received on 16 Jan 2015, accepted on 02 Apr 2015 and first published on 02 Apr 2015


Article type: Communication
DOI: 10.1039/C5CC00448A
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Chem. Commun., 2015,51, 8070-8073
  • Open access: Creative Commons BY license
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    Diastereoselective synthesis of P-chirogenic phosphoramidate prodrugs of nucleoside analogues (ProTides) via copper catalysed reaction

    F. Pertusati and C. McGuigan, Chem. Commun., 2015, 51, 8070
    DOI: 10.1039/C5CC00448A

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