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    An efficient synthesis of 2,4,7-trisubstituted pyrimido[1,2-a][1,3,5]triazin-6-ones

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    Fulltext not available
    Authors
    Sachdeva, N.
    Dolzhenko, Anton
    Lim, S.
    Ong, W.
    Chui, W.
    Date
    2015
    Type
    Journal Article
    
    Metadata
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    Citation
    Sachdeva, N. and Dolzhenko, A. and Lim, S. and Ong, W. and Chui, W. 2015. An efficient synthesis of 2,4,7-trisubstituted pyrimido[1,2-a][1,3,5]triazin-6-ones. New Journal of Chemistry. 39 (6): pp. 4796-4804.
    Source Title
    New Journal of Chemistry
    DOI
    10.1039/c5nj00405e
    ISSN
    1144-0546
    School
    School of Pharmacy
    URI
    http://hdl.handle.net/20.500.11937/25264
    Collection
    • Curtin Research Publications
    Abstract

    © 2015 The Royal Society of Chemistry and the Centre National de la Recherche Scientifique. A method for the preparation of novel pyrimido[1,2-a][1,3,5]triazin-6-one derivatives functionalized in positions 2, 4, and 7 of the ring was developed. Diversity in the derivatization of the pyrimido[1,2-a][1,3,5]triazin-6-one scaffold was successfully achieved by the introduction of substituents into positions 2 and 7 via two complementary approaches for the synthesis of key intermediates viz. pyrimidinylguanidines. Variations in position 4 of the pyrimido[1,2-a][1,3,5]triazine ring were made available by the regioselective introduction of various substituents via the triazine ring closure with corresponding aldehydes. The scope of the method was illustrated by the preparation of a library of 66 pyrimido[1,2-a][1,3,5]triazin-6-ones, which was demonstrated to be a source for new selective anticancer agents. Tautomeric preferences and anticancer properties were also explored for the prepared compounds.

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