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Issue 42, 2010
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A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions

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Abstract

A very short and efficient synthesis of the important drug candidate telaprevir, featuring a biocatalytic desymmetrization and two multicomponent reactions as the key steps, is presented. The classical issue of lack of stereoselectivity in Ugi- and Passerini-type reactions is circumvented. The atom economic and convergent nature of the synthetic strategy require only very limited use of protective groups.

Graphical abstract: A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions

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Publication details

The article was received on 26 Jul 2010, accepted on 03 Sep 2010 and first published on 20 Sep 2010


Article type: Communication
DOI: 10.1039/C0CC02823A
Citation: Chem. Commun., 2010,46, 7918-7920
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    A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions

    A. Znabet, M. M. Polak, E. Janssen, F. J. J. de Kanter, N. J. Turner, R. V. A. Orru and E. Ruijter, Chem. Commun., 2010, 46, 7918
    DOI: 10.1039/C0CC02823A

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