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Aminoheterocycles as synthons for combinatorial Biginelli reactions

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Abstract

Chlorotrimethylsilane (TMSCl) has been utilized as an efficient promoter and water scavenger in the synthesis of diverse dihydropyrimidines via Biginelli type MCR-heterocyclization using aminoheterocycles. High yields and a simple workup of target compounds enable the facile generation of combinatorial libraries comprising more than 2,000 compounds of high structural and functional diversity. A representative set of 89 compounds is described.

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Authors and Affiliations

  1. Enamine Ltd, 23 A. Matrosova St., Kyiv, 01103, Ukraine

    Sergey V. Ryabukhin, Andrey S. Plaskon, Sergey Yu. Boron & Dmitriy M. Volochnyuk

  2. National Taras Shevchenko University, 62 Volodymyrska St., Kyiv, 01033, Ukraine

    Sergey V. Ryabukhin, Andrey S. Plaskon & Andrey A. Tolmachev

  3. Institute of Organic Chemistry, National Academy of Sciences of Ukraine, 5 Murmanska St., Kyiv, 02094, Ukraine

    Dmitriy M. Volochnyuk

Authors
  1. Sergey V. Ryabukhin
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  2. Andrey S. Plaskon
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  3. Sergey Yu. Boron
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  4. Dmitriy M. Volochnyuk
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  5. Andrey A. Tolmachev
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Correspondence to Sergey V. Ryabukhin.

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Ryabukhin, S.V., Plaskon, A.S., Boron, S.Y. et al. Aminoheterocycles as synthons for combinatorial Biginelli reactions. Mol Divers 15, 189–195 (2011). https://doi.org/10.1007/s11030-010-9253-6

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  • DOI: https://doi.org/10.1007/s11030-010-9253-6

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